Abstract

Disclosed herein are methods and systems for characterization, diagnosis, and treatment of cancer. Aspects of the present disclosure are directed to methods for prediction and identification of various molecular features of cancer using analysis of germline genetic information (e.g., polymorphisms). Certain aspects pertain to identification of one or more genetic abnormalities (e.g., mutations, translocations, etc.) of a cancer in a subject following genotyping the subject as having one or more polymorphisms associated with the one or more genetic abnormalities. Also disclosed are methods for diagnosis and characterization of cancer, as well as methods for treatment of cancer having particular genetic abnormalities associated with one or more polymorphisms.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer

Abstract

The present application relates to isoquinoline compounds of Formula (I), to processes for their preparation and to compositions comprising them. More particularly, the present application relates to compound of Formula (I) that have activity as inhibitors of Bcl2-associated X protein (BAX) and/or Bcl-2 antagonist killer (BAK), and to their use in the treatment of diseases, disorders or conditions treatable by inhibiting BAX and/or BAK such as neurodegenerative diseases, disorders or conditions. The present application relates to isoquinoline compounds of Formula (I), to processes for their preparation and to compositions comprising them. More particularly, the present application relates to compound of Formula (I) that have activity as inhibitors of Bcl2-associated X protein (BAX) and/or Bcl-2 antagonist killer (BAK), and to their use in the treatment of diseases, disorders or conditions treatable by inhibiting BAX and/or BAK such as neurodegenerative diseases, disorders or conditions.

IPC Classes  ?

• C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present application relates to pyrimidopyridone and pteridone compounds of Formula I, to processes for their preparation and to compositions comprising them More particularly, the present application relates to compound of Formula I that have activity as inhibitors of the general control nonderepressible 2 (GCN2) kinase and to their use in the treatment of diseases, disorders or conditions treatable by inhibiting GCN2 kinase such as cancers and neuronal diseases.

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 35/00 - Antineoplastic agents
• C07D 475/00 - Heterocyclic compounds containing pteridine ring systems

Abstract

The present application relates to triazolopyridopyrimidine and dihydroimidazopyridopyrimidine compounds that have activity as inhibitors of the general control nonderepressible 2 (GCN2) kinase, to processes for their preparation, to compositions comprising them, and to their use, for example, in therapy More particularly, the present application relates to compounds useful in the treatment of diseases, disorders or conditions treatable by inhibiting GCN2 kinase such as cancers and neuronal diseases. Formula (I)

IPC Classes  ?

• C07D 471/14 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61P 25/00 - Drugs for disorders of the nervous system
• A61P 35/00 - Antineoplastic agents

Abstract

There is described herein a pan-cancer transcriptional signature. In one aspect, there is described a method of diagnosing cancerous cells in a patient, the method comprising: a) providing a sample containing genetic material from patient cells suspected of being cancerous; b) determining or measuring expression levels in the patient cells of at least 3 of the 1919 genes listed in Table B; c) computing a score using a classifier that takes said expression level values as input, the classifier having been previously trained on known cancerous and non-cancerous samples; wherein the score provides a likelihood of a cancerous cell.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G16B 25/10 - Gene or protein expression profilingExpression-ratio estimation or normalisation
• G16B 40/20 - Supervised data analysis
• G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems

Abstract

The present application relates to halo-substituted aza-heteroaryl compounds of Formula (I): (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer. The present application relates to halo-substituted aza-heteroaryl compounds of Formula (I): (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 471/10 - Spiro-condensed systems
• C07D 498/10 - Spiro-condensed systems

Abstract

The present application relates to halo-substituted heterocyclic compounds of Formula (I): or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer. The present application relates to halo-substituted heterocyclic compounds of Formula (I): or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61K 31/541 - Non-condensed thiazines containing further heterocyclic rings
• A61K 31/5415 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one sulfur as the ring hetero atoms, e.g. sulthiame ortho- or peri-condensed with carbocyclic ring systems, e.g. phenothiazine, chlorpromazine, piroxicam
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61K 31/695 - Silicon compounds
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 417/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 471/04 - Ortho-condensed systems
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 487/10 - Spiro-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07D 491/107 - Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
• C07D 491/113 - Spiro-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
• C07D 495/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems
• C07D 498/10 - Spiro-condensed systems
• C07F 7/08 - Compounds having one or more C—Si linkages

Abstract

The present application relates to substituted amino aza-heteroaryl compounds of Formula (I) and substituted aza-heteroaryl compounds of Formula II or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer. The present application relates to substituted amino aza-heteroaryl compounds of Formula (I) and substituted aza-heteroaryl compounds of Formula II or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis. The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

IPC Classes  ?

• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• A61P 35/00 - Antineoplastic agents
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 487/08 - Bridged systems

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis. The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

IPC Classes  ?

• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 487/08 - Bridged systems
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 498/04 - Ortho-condensed systems
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 239/48 - Two nitrogen atoms

Abstract

There is described herein a method of prognosing and/or predicting disease progression and/or in subject with prostate cancer, the method comprising: a) providing a sample containing mitochondrial genetic material from prostate cancer cells; b) sequencing the mitochondrial genetic material with respect to at least 1 patient biomarker selected from CSB1, OHR, ATP8 and HV1 (hypervariable region 1); c) comparing the sequence of said patient biomarkers to control or reference biomarkers to determine mitochondrial single nucleotide variations (mtSNVs); and d) determining the a prostate cancer prognosis; wherein a relatively worse outcome is associated with the presence of mtSNVs in CSB1, OHR, ATP8 and a relatively better outcome is associated with the presence of mtSNVs in HV1.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
• G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
• C12Q 1/6881 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for tissue or cell typing, e.g. human leukocyte antigen [HLA] probes

Abstract

Disclosed herein are methods and systems for characterization, diagnosis, and treatment of cancer. Aspects of the present disclosure are directed to methods for prediction and identification of various molecular features of cancer using analysis of germline genetic information (e.g., polymorphisms). Certain aspects pertain to identification of one or more genetic abnormalities (e.g., mutations, translocations, etc.) of a cancer in a subject following genotyping the subject as having one or more polymorphisms associated with the one or more genetic abnormalities. Also disclosed are methods for diagnosis and characterization of cancer, as well as methods for treatment of cancer having particular genetic abnormalities associated with one or more polymorphisms.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• C07K 14/82 - Translation products from oncogenes
• A61P 13/08 - Drugs for disorders of the urinary system of the prostate

Abstract

The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer. (I) The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer. (I)

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 213/55 - AcidsEsters

Abstract

The present application relates to quinazoline compounds of Formula (I), to processes for their preparation and to compositions comprising them. More particularly, the present application relates to compound of Formula (I) that have activity as inhibitors of the general control nonderepressible 2 (GCN2) kinase and to their use in the treatment of diseases, disorders or conditions treatable by inhibiting GCN2 kinase such as cancers and neuronal diseases.

IPC Classes  ?

• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 25/02 - Drugs for disorders of the nervous system for peripheral neuropathies
• A61P 35/00 - Antineoplastic agents
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings

Abstract

The present application relates to isoquinoline compounds of Formula (I), to processes for their preparation and to compositions comprising them. More particularly, the present application relates to compound of Formula (I) that have activity as inhibitors of Bcl2- associated X protein (BAX) and/or Bcl-2 antagonist killer (BAK), and to their use in the treatment of diseases, disorders or conditions treatable by inhibiting BAX and/or BAK such as neurodegenerative diseases, disorders or conditions.

IPC Classes  ?

• C07D 217/22 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol

Abstract

There is described herein a method of predicting disease progression risk in a subject with prostate cancer, the method comprising: a) providing a sample containing RNA and DNA material from tumour cells; b) determining or measuring values for substantially all of patient features listed for PRONTO-e or PRONTO-m in Table 6, and some or all reference or control features set forth in Table 6; c) comparing said patient features to the reference or control features; and d) computing a prediction score using a classifier that takes said patient feature values as input, the classifier having been previously trained on samples from a population of early prostate cancer patients.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment

Abstract

The present application relates to halo-substituted aza-heteroaryl compounds of Formula (I): (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/502 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
• A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61P 35/00 - Antineoplastic agents
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 471/10 - Spiro-condensed systems
• C07D 498/10 - Spiro-condensed systems

Abstract

The present application relates to substituted amino aza-heteroaryl compounds of Formula (I) and substituted aza-heteroaryl compounds of Formula II or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 403/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings

Abstract

The present application relates to substituted heterocyclic compounds of Formula (I) and substituted compound of Formula (II): (I) (II) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/53 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/4995 - Pyrazines or piperazines forming part of bridged ring systems
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61P 35/00 - Antineoplastic agents
• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems

Abstract

The present application relates to halo-substituted heterocyclic compounds of Formula (I): or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting HPK1, such as cancer.

IPC Classes  ?

• C07D 401/04 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring- member bond
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/395 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
• A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/4965 - Non-condensed pyrazines
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 471/04 - Ortho-condensed systems
• C07D 491/048 - Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered
• C07D 498/14 - Ortho-condensed systems

Abstract

The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer. The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07K 16/32 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products from oncogenes
• A61P 35/00 - Antineoplastic agents
• C07B 59/00 - Introduction of isotopes of elements into organic compounds
• C07D 213/55 - AcidsEsters
• C07D 213/56 - Amides
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Abstract

The present application is directed to compounds of Formula (I), (II), (III) or (IV) compositions comprising these compounds, methods for their preparation and their uses, for example, as acyl hydrazone linkers, which can link two chemical entities together for further use as medicaments and/or diagnostics. The present application is directed to compounds of Formula (I), (II), (III) or (IV) compositions comprising these compounds, methods for their preparation and their uses, for example, as acyl hydrazone linkers, which can link two chemical entities together for further use as medicaments and/or diagnostics.

IPC Classes  ?

• C07D 239/34 - One oxygen atom
• C07D 213/64 - One oxygen atom attached in position 2 or 6
• C07D 215/40 - Nitrogen atoms attached in position 8
• C07D 237/14 - Oxygen atoms
• C07D 241/18 - Oxygen or sulfur atoms
• C07D 241/44 - Benzopyrazines with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
• C07D 249/12 - Oxygen or sulfur atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 498/18 - Bridged systems

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

IPC Classes  ?

• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61P 35/00 - Antineoplastic agents
• C07D 239/48 - Two nitrogen atoms
• C07D 241/36 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/551 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogens as ring hetero atoms, e.g. clozapine, dilazep
• A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue
• A61P 35/00 - Antineoplastic agents
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 487/08 - Bridged systems

Abstract

The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer. (I)

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings

Abstract

There is described herein a method of predicting disease progression risk in a subject with prostate cancer, the method comprising: a) providing a sample containing RNA and DNA material from tumour cells; b) determining or measuring values for substantially all of patient features listed for PRONTO-e or PRONTO-m in Table 6, and some or all reference or control features set forth in Table 6; c) comparing said patient features to the reference or control features; and d) computing a prediction score using a classifier that takes said patient feature values as input, the classifier having been previously trained on samples from a population of early prostate cancer patients.

IPC Classes  ?

• C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G16B 20/00 - ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations

Abstract

The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics. Specifically claimed are: (1) compounds containing reactive functional groups (compound of formula I), compounds containing compounds to be linked together (compound of formula II) and compounds having a reactive functional group/a compound to be linked (compound of formula IV), (2) an antibody-drug conjugate (compound of formula III), wherein the antibody is covalently attached by a linker to one or more drugs, (3) pharmaceutical compositions comprising compounds of Formula (II) or Formula (III), (4) treatment/diagnosis of disease comprising compounds of Formula (II) or Formula (III), and (5) methods of preparing an ADC of Formula III.

IPC Classes  ?

• C07D 498/18 - Bridged systems
• C07D 215/42 - Nitrogen atoms attached in position 4
• C07D 223/16 - BenzazepinesHydrogenated benzazepines
• C07D 311/68 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
• C07D 335/06 - BenzothiopyransHydrogenated benzothiopyrans
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• A61K 38/07 - Tetrapeptides
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 487/14 - Ortho-condensed systems
• A61P 35/04 - Antineoplastic agents specific for metastasis
• C07D 471/14 - Ortho-condensed systems
• C07D 498/14 - Ortho-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

The present application is directed to compounds of Formula (I)-(VIII): compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• A61P 35/00 - Antineoplastic agents
• C07C 323/60 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
• C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom

Abstract

The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07D 213/56 - Amides
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/46 - Hybrid immunoglobulins

Abstract

The present application is directed to compounds of Formula (I), (II), (III) or (IV) compositions comprising these compounds, methods for their preparation and their uses, for example, as acyl hydrazone linkers, which can link two chemical entities together for further use as medicaments and/or diagnostics.

IPC Classes  ?

• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• A61K 31/4196 - 1,2,4-Triazoles
• A61K 31/44 - Non-condensed pyridinesHydrogenated derivatives thereof
• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 31/47 - QuinolinesIsoquinolines
• A61K 31/4709 - Non-condensed quinolines containing further heterocyclic rings
• A61K 31/4965 - Non-condensed pyrazines
• A61K 31/498 - Pyrazines or piperazines ortho- or peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
• A61K 31/50 - PyridazinesHydrogenated pyridazines
• A61K 31/501 - PyridazinesHydrogenated pyridazines not condensed and containing further heterocyclic rings
• A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61K 31/537 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61K 49/00 - Preparations for testing in vivo
• A61P 35/00 - Antineoplastic agents
• C07D 213/64 - One oxygen atom attached in position 2 or 6
• C07D 213/65 - One oxygen atom attached in position 3 or 5
• C07D 215/40 - Nitrogen atoms attached in position 8
• C07D 237/14 - Oxygen atoms
• C07D 239/34 - One oxygen atom
• C07D 241/18 - Oxygen or sulfur atoms
• C07D 249/12 - Oxygen or sulfur atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 498/18 - Bridged systems
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/46 - Hybrid immunoglobulins

Abstract

There is described herein a pan-cancer transcriptional signature. In one aspect, there is described a method of diagnosing cancerous cells in a patient, the method comprising: a) providing a sample containing genetic material from patient cells suspected of being cancerous; b) determining or measuring expression levels in the patient cells of at least 3 of the 1919 genes listed in Table B; c) computing a score using a classifier that takes said expression level values as input, the classifier having been previously trained on known cancerous and non-cancerous samples; wherein the score provides a likelihood of a cancerous cell.

IPC Classes  ?

• C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G16B 20/00 - ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
• G16B 25/10 - Gene or protein expression profilingExpression-ratio estimation or normalisation

Abstract

The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

IPC Classes  ?

• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 471/08 - Bridged systems

Abstract

The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/02 - Antineoplastic agents specific for leukemia
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

The present application relates to novel compounds of Formula (I) containing a E3 ubiquitin ligase binding moiety linked to a Raf protein kinase binding moiety. The present application also includes methods and uses of the compounds, for example, for inhibiting and/or degrading V600E mutant B-Raf. I

IPC Classes  ?

• C07D 471/04 - Ortho-condensed systems
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The present application relates to the treatment of nematode infections. For example, the application relates to the use of compounds of Formula I and/or II as defined herein for treatment of a nematode infection or a disease, disorder or condition arising from a nematode infection:

IPC Classes  ?

• A61K 31/495 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
• A01N 43/60 - 1,4-DiazinesHydrogenated 1,4-diazines
• A61P 33/10 - Anthelmintics
• A61K 31/445 - Non-condensed piperidines, e.g. piperocaine

Abstract

In an aspect, there is provided a method for diagnosing or prognosing a subject with cancer, the method comprising: providing cancer DNA sequencing data from a cancer sample comprising cancer DNA from the subject; comparing the cancer DNA sequencing data with control DNA sequencing data to determine genetic aberrations; determining, from the genetic aberrations, the clonal and subclonal populations present in the sample; constructing a phylogenetic map of the clonal and subclonal populations; assigning to the subject a risk level associated with a better or worse patient outcome or response to therapy; wherein a relatively higher risk level is associated with a higher level of evolution and number of subclonal populations and a relatively lower risk level is associated with a lower level of evolution and number of subclonal populations.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G16B 10/00 - ICT specially adapted for evolutionary bioinformatics, e.g. phylogenetic tree construction or analysis
• G16B 20/20 - Allele or variant detection, e.g. single nucleotide polymorphism [SNP] detection
• G16B 30/10 - Sequence alignmentHomology search
• G16B 40/10 - Signal processing, e.g. from mass spectrometry [MS] or from PCR
• G16B 45/00 - ICT specially adapted for bioinformatics-related data visualisation, e.g. displaying of maps or networks
• G16H 50/20 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for computer-aided diagnosis, e.g. based on medical expert systems
• G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment
• G16H 50/50 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for simulation or modelling of medical disorders

Abstract

The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

IPC Classes  ?

• C07D 487/04 - Ortho-condensed systems
• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 471/04 - Ortho-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• C07F 5/02 - Boron compounds
• C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen

Abstract

The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula (IV): compositions comprising these compounds and their uses, for example as medicaments and /or diagnostics. Specifically claimed are: (1) compounds containing reactive functional groups (compound of formula I), compounds containing compounds to be linked together (compound of formula II) and compounds having a reactive functional group/a compound to be linked (compound of formula IV), (2) an antibody-drug conjugate (compound of formula III), wherein the antibody is covalently attached by a linker to one or more drugs, (3) pharmaceutical compositions comprising compounds of Formula (II) or Formula (III), (4) treatment/diagnosis of disease comprising compounds of Formula (II) or Formula (III), and (5) methods of preparing an ADC of Formula III.

IPC Classes  ?

• C07D 498/18 - Bridged systems
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 215/42 - Nitrogen atoms attached in position 4
• C07D 223/16 - BenzazepinesHydrogenated benzazepines
• C07D 311/68 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
• C07D 335/06 - BenzothiopyransHydrogenated benzothiopyrans
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/46 - Hybrid immunoglobulins
• C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine

Abstract

The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents

Abstract

The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

IPC Classes  ?

• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

IPC Classes  ?

• C07D 487/14 - Ortho-condensed systems
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

The present application is directed to compounds of Formula (I)-(VI): (I), (II), (III), (IV), (V) (VI), (VII) and (VIII), compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics.

IPC Classes  ?

• C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07C 323/52 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
• C07D 498/18 - Bridged systems
• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C07K 5/062 - Dipeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala

Abstract

There is described herein a method of prognosing endocrine-only treatment in a subject with breast cancer, the method comprising: a) providing a tumor sample of the breast cancer; b) determining the expression level of at least 40 of the genes listed in Table 4 in the tumor sample; c) comparing said expression levels to a reference expression level of the group of genes from control samples from a cohort of subjects; and d) determining the residual risk associated with the breast cancer; wherein a statistically significant difference or similarity in the expression of the group of genes compared to the reference expression level corresponds to a residual risk associated with breast cancer.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G16H 50/30 - ICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for calculating health indicesICT specially adapted for medical diagnosis, medical simulation or medical data miningICT specially adapted for detecting, monitoring or modelling epidemics or pandemics for individual health risk assessment

Abstract

There is provided herein a method for determining a likelihood of resistance to anthracyclin, or poor survival, in a patient with cancer by identifying upregulation of at least one histone gene in the patient.

IPC Classes  ?

• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G16B 25/00 - ICT specially adapted for hybridisationICT specially adapted for gene or protein expression
• A61K 31/136 - Amines, e.g. amantadine having aromatic rings, e.g. methadone having the amino group directly attached to the aromatic ring, e.g. benzeneamine
• A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Abstract

In an aspect, there is provided a method for diagnosing or prognosing a subject with cancer, the method comprising: providing cancer DNA sequencing data from a cancer sample comprising cancer DNA from the subject; comparing the cancer DNA sequencing data with control DNA sequencing data to determine genetic aberrations; determining, from the genetic aberrations, the clonal and subclonal populations present in the sample; constructing a phylogenetic map of the clonal and subclonal populations; assigning to the subject a risk level associated with a better or worse patient outcome or response to therapy; wherein a relatively higher risk level is associated with a higher level of evolution and number of subclonal populations and a relatively lower risk level is associated with a lower level of evolution and number of subclonal populations.

IPC Classes  ?

• C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
• G06F 19/22 - for sequence comparison involving nucleotides or amino acids, e.g. homology search, motif or Single-Nucleotide Polymorphism [SNP] discovery or sequence alignment
• G06F 19/14 - for phylogeny or evolution, e.g. evolutionarily conserved regions determination or phylogenetic tree construction
• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer

Abstract

There is described herein a method of determining the likelihood of disease or disease progression in a patient with respect to prostate cancer, the method comprising: a) providing a biological fluid sample, preferably urine, from the patient containing miRNA; b) determining or measuring the abundance of at least one miRNA biomarker selected from the group consisting of: hsa-miR-3195, hsa-let-7b-5p, hsa-miR-144-3p, hsa-miR-451 a, hsa-miR-148a-3p, hsa-miR- 512-5p, and hsa-miR-431 -5p; c) comparing the abundance of said at least one miRNA biomarker in the sample with a reference or control abundance of at least one miRNA biomarker; and d) determining the likelihood of disease or disease progression; wherein a likelihood of disease or disease progression is higher when there is statistically significant higher abundance in the sample in comparison with the reference or control abundance.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C07H 21/02 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids with ribosyl as saccharide radical
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation

Abstract

There is described herein a method of prognosing and/or predicting disease progression and/or in subject with prostate cancer, the method comprising: a) providing a sample containing mitochondrial genetic material from prostate cancer cells; b) sequencing the mitochondrial genetic material with respect to at least 1 patient biomarker selected from CSB1, OHR, ATP8 and HV1 (hypervariable region 1); c) comparing the sequence of said patient biomarkers to control or reference biomarkers to determine mitochondrial single nucleotide variations (mtSNVs); and d) determining the a prostate cancer prognosis; wherein a relatively worse outcome is associated with the presence of mtSNVs in CSB1, OHR, ATP8 and a relatively better outcome is associated with the presence of mtSNVs in HV1.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/22 - for sequence comparison involving nucleotides or amino acids, e.g. homology search, motif or Single-Nucleotide Polymorphism [SNP] discovery or sequence alignment

Abstract

There is described herein, a method of diagnosing a subject with prostate cancer comprising: (a) determining an expression level of at least 1 gene in a test sample from the subject selected from the group consisting of the genes identified in Fig. 4b; and (b) comparing the expression level of the at least 1 gene in the test sample with a reference expression level of the at least 1 gene from control samples of healthy subjects; wherein a statistically significant difference in the expression of the at least 1 gene in the test sample compared to the reference expression level is an indication that the subject has prostate cancer.

IPC Classes  ?

• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G01N 33/483 - Physical analysis of biological material
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation

Abstract

There is described herein a method for determining a risk of recurrence of cancer following a cancer therapy of a patient, comprising determining genomic instability of a tumour of the patient from a biopsy by identifying genome regions of the biopsy wherein the regions are at least loci rankings 1-15 of specific 31-loci and using copy number calls and calculating a plurality of statistical distances between the CNA tumour profile and a reference profile of recurring cancer patients to determine the risk of cancer recurrence following the cancer therapy of the patient.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 17/18 - Complex mathematical operations for evaluating statistical data
• G06F 19/18 - for functional genomics or proteomics, e.g. genotype-phenotype associations, linkage disequilibrium, population genetics, binding site identification, mutagenesis, genotyping or genome annotation, protein-protein interactions or protein-nucleic acid interactions

Abstract

There is described herein a method of prognosing and/or predicting disease progression in subject with prostate cancer, the method comprising: a) providing a sample containing genetic material from cancer cells; b)determining or measuring at least 2 patient biomarkers regarding the prostate cancer tumor selected from the group consisting of: T category, ACTL6B methylation, TCERGL1 methylation, chr7:61 Mbp inter-chromosomal translocation, ATM single nucleotide variants and MYC copy number aberrations; c) comparing said patient biomarkers to corresponding reference or control biomarkers; and d) determining the likelihood of disease progression; wherein a likelihood of disease progression is higher with each of ACTL6B hyper-methylation, TCERGL1 hypo-methylation, higher T category, and higher incidences of chr7:61 Mbp inter-chromosomal translocation, ATM single nucleotide variants and MYC copy number aberrations, when the difference is statistically significant on comparison with the reference or control biomarkers.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation

Abstract

There is described herein a method of prognosing endocrine-only treatment in a subject with breast cancer, the method comprising: a) providing a tumor sample of the breast cancer; b) determining the expression level of at least 40 of the genes listed in Table 4 in the tumor sample; c) comparing said expression levels to a reference expression level of the group of genes from control samples from a cohort of subjects; and d) determining the residual risk associated with the breast cancer; wherein a statistically significant difference or similarity in the expression of the group of genes compared to the reference expression level corresponds to a residual risk associated with breast cancer.

IPC Classes  ?

• C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation

Abstract

There is described herein a method of predicting a benefit of anthracycline therapy for a subject with breast cancer, the method comprising: a) providing a sample of a breast cancer tumour of the subject; b) determining the level of expression in the sample for a group of genes comprising at least 3 of: GZMB, PRF1, SELL, CCL22, CXCL10, CXCL13, IL8, IRF1 and STAT3; c) comparing said expression levels to a reference expression level of the group of genes from control samples from a population; and d) determining the benefit of anthracycline therapy for the subject; wherein a statistically significant difference or similarity in the expression of the group of genes compared to the reference expression level correlates to an immune score; a relatively low immune score being associated with a greater benefit of anthracycline therapy, and a relatively high immune score being associated with a lesser benefit of anthracycline therapy

IPC Classes  ?

• C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation

Abstract

There is provided herein a method for determining a likelihood of resistance to anthracyclin, or poor survival, in a patient with cancer by identifying upregulation of at least one histone gene in the patient.

IPC Classes  ?

• C04B 40/06 - Inhibiting the setting, e.g. mortars of the deferred action type containing water in breakable containers
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin

Abstract

Described herein are approaches for the improved detection, identification, and/or quantification of target nucleic acids. These approaches provide a means of detecting, identifying, and/or quantifying rare target nucleic acid molecules, including DNA and RNA molecules, from the same sample, and in the same reaction, by using "hairpin barcode primers," as the term is defined herein, to incorporate unique barcodes into target nucleic acids in a PCR pre-amplification step.

IPC Classes  ?

• G01N 33/53 - ImmunoassayBiospecific binding assayMaterials therefor

Abstract

In one aspect, there is provided a compound comprising an acetylated carboxymethylcellulose (CMC-Ac) covalently linked to: at least one poly(ethylene glycol) (PEG), and podophyllotoxin or derivatives thereof. In another aspect, a self- assembling nanoparticle composition comprising such compounds is provided.

IPC Classes  ?

• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• A61K 31/365 - Lactones
• A61K 9/14 - Particulate form, e.g. powders
• A61P 35/00 - Antineoplastic agents
• C08B 11/12 - Alkyl or cycloalkyl ethers with substituted hydrocarbon radicals substituted with acid radicals substituted with carboxylic radicals
• C08G 65/332 - Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides or esters thereof

Abstract

Methods, systems, devices and computer impemented methods of prognosing or classifying patients using a biomarker comprising a plurality of subnetwork modules are disclosed. In some embodiments, the method comprises determining an activity of a plurality of genes in a test sample of a patient, wherein the plurality of genes are associated with the plurality of subnetwork modules. An expression profile is constructed using the activity of the plurality of genes. The dysregulation of each of the plurality of subnetwork modules is determined by calculating a score proportional to a degree of dysregulation in each of the plurality of subnetwork modules from the expression profile. The patient is prognosed or classified by inputting each dysregulation score into a model for predicting patient outcomes for patients having a disease, and inputting a clinical indicator of the patient into the model, to obtain a risk associated with the disease.

IPC Classes  ?

• C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
• C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• C40B 60/00 - Apparatus specially adapted for use in combinatorial chemistry or with libraries
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G06F 19/12 - for modelling or simulation in systems biology, e.g. probabilistic or dynamic models, gene-regulatory networks, protein interaction networks or metabolic networks
• G06F 19/20 - for hybridisation or gene expression, e.g. microarrays, sequencing by hybridisation, normalisation, profiling, noise correction models, expression ratio estimation, probe design or probe optimisation

Abstract

Systems, methods and computer-readable media are provided for determining the amount of sequencing required to achieve a target sequencing quality of a genetic sample to be sequenced. The method comprises receiving a genetic sample and sequencing a portion of the genetic sample. A sequencing quality metric belonging to a category of sequencing quality metrics is generated from the sequencing. The amount of sequencing of the genetic sample required to achieve the target sequencing quality is determined by inputting the sequencing quality metric into a trained model. A system is also disclosed for genetic sequencing. Corresponding methods and computer-readable media are also provided.

IPC Classes  ?

• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)
• C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G06F 19/22 - for sequence comparison involving nucleotides or amino acids, e.g. homology search, motif or Single-Nucleotide Polymorphism [SNP] discovery or sequence alignment

Abstract

The invention features methods, devices, and kits for predicting the responsiveness of a cancer patient (e.g., a breast cancer patient, such as a grade 1, 2, or 3 breast cancer patient) to anthracycline treatment by determining the expression levels of four chromosomal instability (CIN) genes including HDGF, KIAA0286, RFC4, and MSH6, collectively referred to as CIN4. Patients that have a low CIN4 score benefit from anthracycline treatment compared patients with a high CIN4 score.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61P 35/00 - Antineoplastic agents
• C07H 21/00 - Compounds containing two or more mononucleotide units having separate phosphate or polyphosphate groups linked by saccharide radicals of nucleoside groups, e.g. nucleic acids
• C12M 1/34 - Measuring or testing with condition measuring or sensing means, e.g. colony counters
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

There is provided herein, systems, devices and methods for determining a risk of recurrence of cancer following a cancer therapy of a patient by determining genomic instability of a tumour. There is further provided systems, devices and methods for categorizing a patient into a prognostic cancer sub-group by using copy number alterations.

IPC Classes  ?

• G06F 19/18 - for functional genomics or proteomics, e.g. genotype-phenotype associations, linkage disequilibrium, population genetics, binding site identification, mutagenesis, genotyping or genome annotation, protein-protein interactions or protein-nucleic acid interactions
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)

Abstract

A method for identifying a target molecular profile associated with a target cell population. A set of reference molecular profiles and a set of sample molecular profiles are received. Each sample molecular profile is associated with a sample cell from a sample cell population, which includes a mixture of target cells and reference cells. Each of the sample molecular profiles is indicative of a respective target molecular profile. An average target molecular profile is calculated. A proportion value is calculated for each sample molecular profile. A respective target molecular profile is calculated for each sample molecular profile based on the respective calculated proportion value and a closest similarity to the average target molecular profile.

IPC Classes  ?

• C04B 40/06 - Inhibiting the setting, e.g. mortars of the deferred action type containing water in breakable containers
• C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C40B 30/00 - Methods of screening libraries
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G01N 33/483 - Physical analysis of biological material
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G06F 19/00 - Digital computing or data processing equipment or methods, specially adapted for specific applications (specially adapted for specific functions G06F 17/00;data processing systems or methods specially adapted for administrative, commercial, financial, managerial, supervisory or forecasting purposes G06Q;healthcare informatics G16H)
• G06F 19/10 - Bioinformatics, i.e. methods or systems for genetic or protein-related data processing in computational molecular biology (in silico methods of screening virtual chemical libraries C40B 30/02;in silico or mathematical methods of creating virtual chemical libraries C40B 50/02)

Abstract

Compounds comprising acetylated carboxymethylcellulose covalently linked to at least one poly( ethylene glycol) and at least one hydrophobic drug comprising taxane have shown to have utility in the preparation of self-assembling nanoparticles. Said nanoparticles exhibit activity in the treatment of cancers including breast, lung, pancreatic and metastatic cancers. Said taxane may be any taxane including cabazitaxel and larotaxel.

IPC Classes  ?

• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 47/38 - CelluloseDerivatives thereof
• A61K 49/00 - Preparations for testing in vivo
• A61K 49/10 - Organic compounds
• A61K 9/14 - Particulate form, e.g. powders
• A61P 35/00 - Antineoplastic agents

Abstract

This invention relates to newly characterized COLCA1 and COLCA2 and their use in the treatment and risk assessment of colon cancer.

IPC Classes  ?

• C07K 14/47 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans from vertebrates from mammals
• A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
• A61P 35/00 - Antineoplastic agents
• C12N 15/12 - Genes encoding animal proteins
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G01N 33/53 - ImmunoassayBiospecific binding assayMaterials therefor
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer
• G01N 33/68 - Chemical analysis of biological material, e.g. blood, urineTesting involving biospecific ligand binding methodsImmunological testing involving proteins, peptides or amino acids

Abstract

In one aspect, there is provided a compound comprising an acetylated carboxymethylcellulose (CMC- Ac) covalently linked to: at least one poly(ethylene glycol) (PEG), and at least one hydrophobic drug. In another aspect, a self-assembling nanoparticle composition comprising such compounds is provided.

IPC Classes  ?

• C08B 11/12 - Alkyl or cycloalkyl ethers with substituted hydrocarbon radicals substituted with acid radicals substituted with carboxylic radicals
• A61K 47/48 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers, inert additives the non-active ingredient being chemically bound to the active ingredient, e.g. polymer drug conjugates
• A61K 9/14 - Particulate form, e.g. powders
• A61P 35/00 - Antineoplastic agents
• C08G 65/332 - Polymers modified by chemical after-treatment with organic compounds containing oxygen containing carboxyl groups, or halides or esters thereof
• A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
• A61K 31/4745 - QuinolinesIsoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenanthrolines

Abstract

In one aspect, the present invention provides a thermosensitive liposome comprising a lipid bilayer comprising 1,2-dipalmitoyl-sn-glycero-3-phosphatidylcholine (DPPC) and a compound of formula (I): C17H35(CH2)p(CO)q(OCH2CH2)nOH wherein p is an integer selected from 0 or 1; q is an integer selected from 0 or 1; p + q = 1; and n is an integer selected from about 10 to about 100.

IPC Classes  ?

• A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
• A61K 47/24 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing atoms other than carbon, hydrogen, oxygen, halogen, nitrogen or sulfur, e.g. cyclomethicone or phospholipids
• A61K 47/34 - Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers
• A61P 35/00 - Antineoplastic agents
• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• A61K 31/7068 - Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
• A61K 49/00 - Preparations for testing in vivo

Abstract

There is provided herein a method for determining a likelihood of resistance to anthracyclin, or poor survival, in a patient with cancer by identifying upregulation of at least one histone gene in the patient.

IPC Classes  ?

• A61K 31/704 - Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin, digitoxin
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
• C12Q 1/6837 - Enzymatic or biochemical coupling of nucleic acids to a solid phase using probe arrays or probe chips
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers
• G16B 25/10 - Gene or protein expression profilingExpression-ratio estimation or normalisation

Abstract

The present application is directed to compounds of Formula (l)-(VIII): compositions comprising these compounds and their uses, for example as medicaments and/or diagnostics.

IPC Classes  ?

• A61K 47/54 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• A61P 35/00 - Antineoplastic agents
• C07C 323/60 - Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
• C07D 207/46 - Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with hetero atoms directly attached to the ring nitrogen atom
• C07D 498/18 - Bridged systems
• C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/30 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants from tumour cells
• C07K 16/46 - Hybrid immunoglobulins

Abstract

The present application relates to compounds of Formula I or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB and/or by degrading BCL6, such as cancer.

IPC Classes  ?

• A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

The present application relates to compounds of Formula I (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

IPC Classes  ?

• A61K 31/437 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/538 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• A61K 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
• A61K 31/553 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and at least one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 471/04 - Ortho-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or
• C07F 5/02 - Boron compounds
• C07F 7/10 - Compounds having one or more C—Si linkages containing nitrogen

Abstract

There is described herein a method of predicting disease progression risk in a subject with prostate cancer, the method comprising: a) providing a sample containing RNA and DNA material from tumour cells; b) determining or measuring values for substantially all of patient features listed for PRONTO-e or PRONTO-m in Table 6, and some or all reference or control features set forth in Table 6; c) comparing said patient features to the reference or control features; and d) computing a prediction score using a classifier that takes said patient feature values as input, the classifier having been previously trained on samples from a population of early prostate cancer patients.

IPC Classes  ?

• C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G16B 20/00 - ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
• G16B 40/00 - ICT specially adapted for biostatisticsICT specially adapted for bioinformatics-related machine learning or data mining, e.g. knowledge discovery or pattern finding

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

IPC Classes  ?

• A61P 19/04 - Drugs for skeletal disorders for non-specific disorders of the connective tissue
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing three or more hetero rings
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 487/08 - Bridged systems

Abstract

There is described herein a method of predicting disease progression risk in a
subject with
prostate cancer, the method comprising: a) providing a sample containing RNA
and DNA
material from tumour cells; b) determining or measuring values for
substantially all of
patient features listed for PRONTO-e or PRONTO-m in Table 6, and some or all
reference
or control features set forth in Table 6; c) comparing said patient features
to the reference
or control features; and d) computing a prediction score using a classifier
that takes said
patient feature values as input, the classifier having been previously trained
on samples
from a population of early prostate cancer patients.

IPC Classes  ?

• C12Q 1/6809 - Methods for determination or identification of nucleic acids involving differential detection
• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G16B 20/00 - ICT specially adapted for functional genomics or proteomics, e.g. genotype-phenotype associations
• G16B 40/00 - ICT specially adapted for biostatisticsICT specially adapted for bioinformatics-related machine learning or data mining, e.g. knowledge discovery or pattern finding

IPC Classes  ?

• A61P 13/08 - Drugs for disorders of the urinary system of the prostate
• C07K 14/82 - Translation products from oncogenes
• C12N 15/113 - Non-coding nucleic acids modulating the expression of genes, e.g. antisense oligonucleotides
• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C12Q 1/6886 - Nucleic acid products used in the analysis of nucleic acids, e.g. primers or probes for diseases caused by alterations of genetic material for cancer
• G01N 33/574 - ImmunoassayBiospecific binding assayMaterials therefor for cancer

Abstract

There is described herein a method of prognosing endocrine-only treatment in a subject with breast cancer, the method comprising: a) providing a tumor sample of the breast cancer; b) determining the expression level of at least 40 of the genes listed in Table 4 in the tumor sample; c) comparing said expression levels to a reference expression level of the group of genes from control samples from a cohort of subjects; and d) determining the residual risk associated with the breast cancer; wherein a statistically significant difference or similarity in the expression of the group of genes compared to the reference expression level corresponds to a residual risk associated with breast cancer.

IPC Classes  ?

• C12Q 1/68 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions involving nucleic acids
• C40B 30/04 - Methods of screening libraries by measuring the ability to specifically bind a target molecule, e.g. antibody-antigen binding, receptor-ligand binding
• C40B 40/06 - Libraries containing nucleotides or polynucleotides, or derivatives thereof
• G01N 33/48 - Biological material, e.g. blood, urineHaemocytometers

Abstract

The present application is directed to compounds of Formula (I): compounds of Formula (II): compounds of Formula (III): and compounds of Formula IV: compositions comprising these compounds and their uses, for example in the treatment or diagnosis of diseases and conditions, including, for example, cancer.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 215/42 - Nitrogen atoms attached in position 4
• C07D 223/16 - BenzazepinesHydrogenated benzazepines
• C07D 311/68 - Benzo [b] pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulfur atoms in position 2 or 4 with nitrogen atoms directly attached in position 4
• C07D 335/06 - BenzothiopyransHydrogenated benzothiopyrans
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 498/18 - Bridged systems
• C07K 5/027 - Peptides having up to four amino acids in a fully defined sequenceDerivatives thereof containing at least one abnormal peptide link in which at least a gamma-amino acid is involved, e.g. statine
• C07K 16/00 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
• C07K 16/46 - Hybrid immunoglobulins

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting interactions with BCL6 BTB, such as cancer.

IPC Classes  ?

• A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• A61K 31/55 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
• A61P 35/00 - Antineoplastic agents
• A61P 35/02 - Antineoplastic agents specific for leukemia
• C07D 487/14 - Ortho-condensed systems
• C07D 519/00 - Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups or

Abstract

The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer.

IPC Classes  ?

• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 213/56 - Amides
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
• C07D 405/12 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 405/14 - Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

The present application is directed to compounds of Formula (I), (II), (III) or (IV): compositions comprising these compounds, methods for their preparation and their uses, for example as medicaments and/or diagnostics.

IPC Classes  ?

• A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
• A61K 47/68 - Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additivesTargeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
• C07D 213/64 - One oxygen atom attached in position 2 or 6
• C07D 213/65 - One oxygen atom attached in position 3 or 5
• C07D 215/40 - Nitrogen atoms attached in position 8
• C07D 237/14 - Oxygen atoms
• C07D 239/34 - One oxygen atom
• C07D 241/18 - Oxygen or sulfur atoms
• C07D 249/12 - Oxygen or sulfur atoms
• C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 403/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 498/18 - Bridged systems
• C07K 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants

Abstract

The present application relates to nicotinamide phosphoribosyltransferase (NAMPT) inhibitor-linker conjugates of Formula (I) comprising NAMPT inhibitors linked to linker groups, to processes and intermediates for their preparation, and to compositions comprising these compounds, as well as their use, for example, in the treatment or diagnosis of diseases and conditions, including, but not limited to, cancer. (I)

IPC Classes  ?

• A61K 31/4545 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
• C07D 401/14 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings

Abstract

The present application relates to compounds of Formula (I) or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, to compositions comprising these compounds or pharmaceutically acceptable salts, solvates and/or prodrugs thereof, and various uses in the treatment of diseases, disorders or conditions that are treatable by inhibiting or blocking NUAK kinase, such as cancers and fibrosis.

IPC Classes  ?

• A61K 31/5383 - 1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
• C07D 239/48 - Two nitrogen atoms
• C07D 241/36 - Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
• C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
• C07D 409/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
• C07D 451/02 - Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamineCyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.02,4] nonane ring systems, e.g. tropaneCyclic acetals thereof
• C07D 471/10 - Spiro-condensed systems
• C07D 487/04 - Ortho-condensed systems
• C07D 498/04 - Ortho-condensed systems

Abstract

The present application relates to isoquinoline compounds of Formula (I), to processes for their preparation and to compositions comprising them. More particularly, the present application relates to compound of Formula (I) that have activity as inhibitors of Bcl2- associated X protein (BAX) and/or Bcl-2 antagonist killer (BAK), and to their use in the treatment of diseases, disorders or conditions treatable by inhibiting BAX and/or BAK such as neurodegenerative diseases, disorders or conditions.

IPC Classes  ?

• A61K 31/472 - Non-condensed isoquinolines, e.g. papaverine
• A61K 31/4725 - Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
• A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
• C07D 217/22 - Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring