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
3.
PROCESS AND INTERMEDIATES USEFUL FOR PREPARING NIRMATRELVIR
C07C 69/14 - Acetic acid esters of monohydroxylic compounds
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
C07K 5/083 - Tripeptides the side chain of the first amino acid being acyclic, e.g. Gly, Ala
4.
IL-12 VARIANTS, ANTI-PD1 ANTIBODIES, FUSION PROTEINS, AND USES THEREOF
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 16/28 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against receptors, cell surface antigens or cell surface determinants
7.
COMBINATION OF A BRAF INHIBITOR, AN EGFR INHIBITOR, AND A PD-1 ANTAGONIST FOR THE TREATMENT OF BRAF V600E-MUTANT, MSI-H/DMMR COLORECTAL CANCER
A61M 5/20 - Automatic syringes, e.g. with automatically actuated piston rod, with automatic needle injection, filling automatically
A61M 5/24 - Ampoule syringes, i.e. syringes with needle for use in combination with replaceable ampoules or cartridges, e.g. automatic
A61M 5/32 - NeedlesDetails of needles pertaining to their connection with syringe or hubAccessories for bringing the needle into, or holding the needle on, the bodyDevices for protection of needles
A61M 5/34 - Constructions for connecting the needle
9.
PROCESS FOR PRODUCING OF VACCINE FORMULATIONS WITH PRESERVATIVES
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
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
The present invention relates to methods of administering a composition comprising the OspA fusion proteins of SEQ ID NO: 1 (LipSI D1 -S2D1 ), SEQ ID NO: 2 (Lip-S4D1 -S3hybD1 ), and SEQ ID NO: 3 (Lip-S5D 1 -S6D1 ) for eliciting an immune response protective against Lyme disease in a subject, such as vaccinating a subject against Lyme disease, and for treating, preventing, and/or reducing the risk of Lyme disease.
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
C07K 16/24 - Immunoglobulins, e.g. monoclonal or polyclonal antibodies against material from animals or humans against cytokines, lymphokines or interferons
18.
IMMUNOGENIC COMPOSITIONS COMPRISING CONJUGATED CAPSULAR SACCHARIDE ANTIGENS AND USES THEREOF
A61K 47/64 - Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
The invention relates to RNA molecules encoding an E. coli fimbrial H antigen (FimH). The present disclosure further relates to compositions comprising the RNA molecules formulated in a lipid nanoparticle (RNA-LNP). The present disclosure further relates to the use of the RNA 5molecules, RNA-LNPs and compositions for the prevention of E.coli infection, including urinary tract infection.
The present disclosure provides solid forms of 6-((3S,4S)-4-methyl-1-(pyrimidin-2-ylmethyl)pyrrolidin-3-yl)-1-(tetrahydro-2H-pyran-4-yl)-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one, and methods of preparing and using the same.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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 403/14 - 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
22.
MELANOCORTIN 4 RECEPTOR ANTAGONISTS AND USES THEREOF
Described herein are compounds of Formula I: I and their pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R7, RF, t1, Y1, and Y2 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.
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 31/4439 - 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 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61P 1/08 - Drugs for disorders of the alimentary tract or the digestive system for nausea, cinetosis or vertigoAntiemetics
A61P 21/00 - Drugs for disorders of the muscular or neuromuscular system
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
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 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
The disclosure provides a method of treating cancer comprising administering to a subject in need thereof with a therapeutically effective amount of PF-07220060. The disclosure also provides a method of treating cancer comprising administering to a subject in need thereof with a therapeutically effective amount of PF-07220060 and an endocrine therapy agent.
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
3-PHENYL-1-BENZOTHIOPHENE-2-CARBOXYLIC ACID DERIVATIVES AS BRANCHED-CHAIN ALPHA KETO ACID DEHYDROGENASE KINASE INHIBITORS FOR THE TREATMENT OF DIABETES, KIDNEY DISEASES, NASH AND HEART FAILURE
The present invention refers to compounds of Formula (I) as branched-chain alpha keto acid dehydrogenase kinase inhibitors and/or degraders for the treatment of e.g. diabetes, kidney diseases, NASH and heart failure. Preferred compounds are e.g. 3-phenyl-1-benzothiophene-2- carboxylic acid derivatives. An exemplary compound is e.g. 3-(5,7-difluoro-3,4-dihydro-2H-1- benzopyran-6-yl)-6-fluoro-1-benzothiophene-2-carboxylic acid (example 1) The present application discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof.
A61K 31/343 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
A61K 31/352 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. cannabinols, methantheline
A61K 31/381 - Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
A61P 1/16 - Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/04 - Inotropic agents, i.e. stimulants of cardiac contractionDrugs for heart failure
A61P 13/12 - Drugs for disorders of the urinary system of the kidneys
C07D 307/85 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 409/04 - 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 directly linked by a ring-member-to-ring- member bond
25.
METHODS AND DOSING REGIMENS COMPRISING A CDK2 INHIBITOR AND A CDK4 INHIBITOR FOR TREATING CANCER
This disclosure relates to combination therapies for use in treating cancer, comprising a CDK2 inhibitor of Formula (I) and a selective CDK4 inhibitor of Formula (II), each as further described herein, optionally in further combination with an additional anti-cancer agent.
The present disclosure relates to RNA molecules encoding a varicella zoster virus (VZV). The present disclosure further relates to compositions comprising the RNA molecules formulated in a lipid nanoparticle (RNA-LNP). The present disclosure further relates to the use of the RNA molecules, RNA-LNPs and compositions for the treatment or prevention of herpes zoster or shingles.
The invention relates to compositions and methods for the preparation, manufacture and therapeutic use of ribonucleic acid immunogenic compositions and/or vaccines comprising polynucleotide molecules preferably encoding one or more influenza antigens, such as hemagglutinin antigens, wherein the composition is frozen or lyophilized.
A61K 39/145 - Orthomyxoviridae, e.g. influenza virus
A61P 31/16 - Antivirals for RNA viruses for influenza or rhinoviruses
28.
SOLID FORMS OF 2-[(4-{6-[(4-CYANO-2-FLUOROBENZYL)OXY]PYRIDIN-2-YL}PIPERIDIN-1-YL)METHYL]-1-[(2S)-OXETAN-2-YLMETHYL]-1H-BENZIMIDAZOLE-6-CARBOXYLIC ACID, 1,3-DIHYDROXY-2-(HYDROXYMETHYL)PROPAN-2-AMINE SALT
The invention provides solid forms of 2-[(4-{6-[(4-Cyano-2- fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-[(2S) -oxetan-2-ylmethyl]-1lH-benzimidazole-6-carboxylic acid, 1,3- dihydroxy-2-(hydroxymethyl)propan-2-amine salt for example, Form 1 or Form 2; as well as pharmaceutical compositions, and the uses thereof in treating diseases, conditions or disorders modulated by GLP-1 R in a mammal, such as a human. Formula (I)
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
Vectors and nucleic acid constructs for improved antibody production are provided. Also provided are methods of making and using the vectors and constructs.
The present disclosure relates to compositions and methods for the optimal large-scale production of rAAV vectors using the baculovirus expression vector system in insect cells.
The present invention relates to new conjugated capsular saccharide antigens (glycoconjugates), immunogenic compositions comprising said glycoconjugates and uses thereof.
The present invention relates to new conjugated capsular saccharide antigens (glycoconjugates), immunogenic compositions comprising said glycoconjugates and uses thereof.
The invention relates to compositions and methods for the preparation, manufacture and therapeutic use ribonucleic acid vaccines comprising polynucleotide molecules encoding one or more influenza antigens, such as hemagglutinin antigens.
The invention relates to vaccination of human subjects, in particular elderly, against bacterial infections, wherein the bacterial infection is not pneumococcal, and COVID-19 infections.
Materials and methods useful for therapy, including cancer therapy, that combine an agent that blocks the CD47/SIRPa interaction with a DHFR inhibitor are provided.
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 38/17 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from animalsPeptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from humans
A61P 35/02 - Antineoplastic agents specific for leukemia
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
The present disclosure provides methods for producing a compound having a chemical formula of Formula I, wherein R1 and R2 are independently a i) linear or branched or cyclic, ii) saturated or unsaturated, and iii) substituted or unsubstituted hydrocarbon group comprising 1 to 30 carbon atoms; R3 is a i') linear or branched or cyclic, ii') saturated or unsaturated, and iii') substituted or unsubstituted hydrocarbon group; and L1, L2 and L3 independently are linkers.
C07C 69/24 - Esters of acyclic saturated monocarboxylic acids having the carboxyl group bound to an acyclic carbon atom or to hydrogen having three or more carbon atoms in the acid moiety esterified with monohydroxylic compounds
C07C 209/24 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds
C07C 209/26 - Preparation of compounds containing amino groups bound to a carbon skeleton by reductive alkylation of ammonia, amines or compounds having groups reducible to amino groups, with carbonyl compounds by reduction with hydrogen
C07C 219/06 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having the hydroxy groups esterified by carboxylic acids having the esterifying carboxyl groups bound to hydrogen atoms or to acyclic carbon atoms of an acyclic saturated carbon skeleton
C07C 219/24 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups or amino groups bound to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
37.
3,4-DIHYDRO-2,7-NAPHTHYRIDINE-1,6(2H,7H)-DIONES AS MEK INHIBITORS
The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and R4 are as defined herein. The invention further relates to pharmaceutical compositions comprising such compounds and salts, and to methods and uses of such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject in need thereof. The invention further relates to solid forms of 8-((2-fluoro-4-(methylthio)phenyl)amino)-2-(2-hydroxyethoxy)-7-methyl-3,4- dihydro-2,7-naphthyridine-1,6(2H,7H)-dione.
A61K 31/4375 - 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 six-membered ring having nitrogen as a ring hetero atom, e.g. quinolizines, naphthyridines, berberine, vincamine
Method for treating vitiligo, including active and stable non-segmental vitiligo, using compounds and analogues which inhibit certain kinases including Janus Kinase (JAK), said method comprising the step of administering to the subject in need thereof 1-[(2S,5R)-2-methyl-5-(7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-1-piperidinyl]-2-propen-1-one, or a pharmaceutically acceptable salt thereof.
This invention relates to combination therapies comprising talazoparib, or a pharmaceutically acceptable salt thereof, and an anti-androgen, or a pharmaceutically acceptable salt thereof, and associated pharmaceutical compositions, methods of treatment, and pharmaceutical uses for the treatment of metastatic castration-sensitive prostate cancer in subjects identified as having at least one DNA damage repair gene mutation.
A61K 31/4155 - 1,2-Diazoles not condensed and containing further heterocyclic rings
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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 31/5025 - PyridazinesHydrogenated pyridazines ortho- or peri-condensed with heterocyclic ring systems
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/04 - Antineoplastic agents specific for metastasis
40.
MODULATORS OF STING (STIMULATOR OF INTERFERON GENES)
Provided herein are compounds of the general formula (I): and pharmaceutically acceptable salts thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses thereof as modulators of STING (Stimulator of Interferon Genes).
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
The subject matter described herein is directed to methods of treating growth hormone related disorders by administering a long-acting recombinant human growth hormone. In another embodiment, a long-acting recombinant human growth hormone is administered in a composition or the combination is administered separately to treat growth deficiency in a subject previously treated with a once daily rhGH therapy.
The present invention relates to a method for identifying a candidate therapeutic for a disease caused by infection with a human cytomegalovirus (HCMV) having a glycoprotein B (gB) polypeptide, comprising contacting the HCMV gB polypeptide comprising a druggable region with a compound, wherein binding of said compound indicates a candidate therapeutic. The present invention also relates to candidate therapeutics comprising modulators and inhibitors of HCMV activity and pharmaceutical compositions comprising said modulators and inhibitors and methods of use thereof.
Method for treating moderate to severe chronic hand eczema in a subject in need thereof, which method comprises the step of administering to said subject a therapeutically effective amount of the compound of N-((1S,3S)-3-(methyl(7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)cyclobutyl)propane-1-sulfonamide, or a pharmaceutically acceptable salt thereof.
Methods for producing a compound of Formula I, Formula I, wherein R1 and R2 are independently a i) linear or branched or cyclic, ii) saturated or unsaturated, and iii) substituted or unsubstituted hydrocarbon group comprising 8 to 20 carbon atoms; R3 is a hydrocarbon group; n is an integer from 2 to 5, m is an integer from 30 to 70, and L is a linker. The method includes: a) contacting a fatty acid having a chemical formula of R1-COOH and a primary amine having a chemical formula of R2-NH2 to form an amide having a chemical formula of R1-C(O)-NH-R2; b) contacting the amide with a reducing agent to form a secondary amine having a chemical formula of R1-CH2-NH-R2; and c) contacting the secondary amine with a polyolefin-glycol compound to form the compound of Formula I. Intermediates produced in the method, salts of compound of Formula I and of intermediates.
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
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
C07C 219/02 - Compounds containing amino and esterified hydroxy groups bound to the same carbon skeleton having esterified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
C07C 229/16 - Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
The present invention relates to solid forms of 7-(5-chloro-2-(3-(5-cyano-6-((1-(3,3-difluorocyclobutyl)piperidin-4-yl)(methyl)amino)-2-methyl-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl)prop-1-yn-1-yl)phenyl)-N-(methylsulfonyl)thieno[3,2-b]pyridine-3-carboxamide, to pharmaceutical compositions comprising such solid forms, and to methods of using such solid forms and pharmaceutical compositions for the treatment of cancer.
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
46.
METHODS AND COMPOSITIONS FOR INHIBITING EXCESS NUCLEIC ACID PRECIPITATION
The present disclosure describes improved methods for use in purifying biological products made by host cells. In some embodiments, the improved methods comprise one or more steps of lysing host cells, such as with a detergent, to release the biological product, precipitating host cell DNA,such as with domiphen bromide, and then inhibiting precipitation of residual host cell DNA in a supernatant containing the biological product by adding a salt to a sufficient final concentration. In some embodiments, the biological product is a vaccine, or a viral vector for gene therapy, such as an AAV vector or a lentiviral vector.
The present disclosure provides improved methods and systems for transfecting host cells with nucleic acids, such as plasmid DNA, for purposes of efficiently producing biological products, such as AAV vectors, at large scale.
The present disclosure provides methods for purifying a recombinant AAV (rAAV) vector from a solution by affinity chromatography to produce an eluate enriched for AAV vectors (rAAV vectors).
B01D 15/38 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving specific interaction not covered by one or more of groups , e.g. affinity, ligand exchange or chiral chromatography
C12N 7/00 - Viruses, e.g. bacteriophagesCompositions thereofPreparation or purification thereof
The invention relates to solid forms of (1R,3S)-3-[3-({[3-(methoxymethyl)-1-methyl-1H-pyrazol-5-yl]carbonyl}amino)-1H-pyrazol-5-yl]cyclopentyl propan-2-ylcarbamate, to pharmaceutical compositions comprising such solid forms, and to use of such solid forms and pharmaceutical compositions for the treatment of cancer.
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
This disclosure relates to the design of E. coli mutated FimH polypeptides that result in improved biochemical properties and immunogenicity, compositions comprising such polypeptides, and uses thereof.
A reversibly gated effector polypeptide e.g. a chimeric antigen receptor (protease-activating CD45-gate CAR) comprising an extracellular CD45 recruiting domain, a protease-cleavable linker, and a polypeptide comprising an extracellular ligand binding domain, a transmembrane domain, and an intracellular domain. Nucleic acids including vectors and expression vectors that encode the protease-activating CD45-gate CAR and cells including immune cells such as T cells that comprise and express the nucleic acids. Methods of treatment of various conditions including various forms of cancer comprising administering the cells including CAR T cell therapy. In some embodiments, the CD45 gate at least partially inhibits activation of the protease-activating CD45-gate CAR when the protease-activating CD45-gate CAR binds antigen. The inhibition is at least partially diminished, relieved and/or eliminated when the protease-activating CD45-gate CAR is exposed to a protease that can cleave the linker.
The invention relates to imidazopyridines of Formula (I) and pharmaceutically acceptable salts thereof, wherein R0 to R5 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.
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
The present invention provides compositions comprising a recombinant AAV and one or more pharmaceutically acceptable excipients. The compositions have improved stability and shelf life as compared to other AAV compositions.
The invention relates to benzimidazoles of Formula (I) and pharmaceutically acceptable salts thereof, wherein R1 to R6 are as defined in the description; to their use in medicine; to compositions containing them; to processes for their preparation; and to intermediates used in such processes. The benzimidazoles of Formula (I) are ITK inhibitors and are therefore potentially useful in the treatment of a wide range of disorders including, atopic dermatitis.
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
55.
METHODS OF IDENTIFYING A TUMOR THAT IS SENSITIVE TO TREATMENT WITH TALAZOPARIB AND METHODS OF TREATMENT THEREOF
The present invention relates to a method of identifying a metastatic tumor determined to have a mutation in homologous recombination pathway genes, that is sensitive to treatment with talazoparib, or a pharmaceutically acceptable salt thereof, and methods of treatment thereof, comprising a) determining a homologous recombination deficiency score from a biopsy of the metastatic tumor; and b) administering talazoparib, or a pharmaceutically acceptable salt thereof, if the homologous recombination deficiency score is at least 33%, wherein the mutation is not germline BRCA1 or germline BRCA2. The present invention also relates to a method of selecting a subject determined to have a metastatic tumor with a mutation in homologous recombination pathway genes, for treatment with talazoparib, or a pharmaceutically acceptable salt thereof.
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
A pharmaceutical soft gelatin capsule dosage form comprising a soft gelatin shell and a fill, wherein: (a) the soft gelatin shell comprises gelatin and at least one plasticizer; and (b) the fill comprises an anti-oxidant, at least one solvent, and talazoparib or a pharmaceutically acceptable salt thereof. Said pharmaceutical composition for use in treating cancer.
The present invention relates to new immunogenic compositions comprising conjugated Streptococcus pneumoniae capsular saccharide antigens (glycoconjugates), kits comprising said immunogenic compositions and uses thereof. Immunogenic compositions of the present invention will typically comprise at least one glycoconjugate from a S. pneumoniae serotype not found in PREVNAR®, SYNFLORIX® and/or PREVNAR 13®. The invention also relates to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said novel immunogenic compositions.
An injector, comprising a housing arranged along a longitudinal axis and configured to receive a medicament cartridge; an injection drive mechanism for driving a piston, the piston forming part of the medicament cartridge, the injection drive mechanism injecting a medicament when the piston is forwardly displaced; and a needle hiding element, which is slidably attached to the housing and positionable in at least one of an extended orientation and a retracted orientation, wherein in the extended orientation the needle hiding element protrudes forwardly from the housing and in the retracted orientation, the needle hiding element is locked relative to the housing.
A61M 5/20 - Automatic syringes, e.g. with automatically actuated piston rod, with automatic needle injection, filling automatically
A61M 5/24 - Ampoule syringes, i.e. syringes with needle for use in combination with replaceable ampoules or cartridges, e.g. automatic
A61M 5/315 - PistonsPiston-rodsGuiding, blocking or restricting the movement of the rodAppliances on the rod for facilitating dosing
A61M 5/32 - NeedlesDetails of needles pertaining to their connection with syringe or hubAccessories for bringing the needle into, or holding the needle on, the bodyDevices for protection of needles
59.
IMMUNOGENIC COMPOSITIONS FOR USE IN PNEUMOCOCCAL VACCINES
An object of the present invention is to provide immunogenic compositions for protection against S. pneumoniae, in particular against S. pneumoniae serogroup 15, while limiting the number of conjugates. The present invention therefore relates to new immunogenic compositions for use in pneumococcal vaccines and to vaccination of human subjects, in particular infants and elderly, against pneumococcal infections using said immunogenic compositions.
The present disclosure provides methods for purifying a recombinant AAV (rAAV) vector from a solution by anion-exchange chromatography (AEX) to produce an eluate enriched for full capsids and depleted of empty capsids.
Embodiments described herein provide a solution to the measurement of various dystrophins expressed in a cell or tissue. The solution to this problem is a specific and sensitive quantitative method to measure endogenous and/or exogenous dystrophin (e.g., engineereddystrophin) expression in skeletal muscle tissue, which provides a substantial benefit to drug development and monitoring of treatment.
This invention relates to compositions that include a polypeptide derived from E. coli or a fragment thereof; and modified O-polysaccharide molecules derived from E. coli lipopolysaccharides and conjugates thereof, and methods of use thereof.
The present invention relates to methods for purifying bacterial polysaccharides, in particular for removing impurities from cellular lysates of bacteria producing polysaccharides.
A parenteral aqueous suspension formulation for corticosteroids without polyethylene glycol (PEG) or Polysorbate (PS) that has better resuspendability, longer stability compared to commercially available formulations, and additionally allows for stable formulations of higher concentrations of corticosteroids that were not previously feasible. Preferably, the corticosteroid is methylprednisolone acetate or medroxyprogesterone acetate.
A61K 31/57 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
A61K 31/573 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
Antibodies, and antigen-binding fragments thereof, that specifically bind to Cluster of Differentiation 1a (CD1a) are provided. Embodiments include uses, and associated methods of using the antibodies, and antigen-binding fragments thereof.
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
A61P 37/00 - Drugs for immunological or allergic disorders
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
This invention relates to crystalline and amorphous forms of 1,5-anhydro-3-({5-chloro-4-[4-fluoro-2-(2-hydroxypropan-2-yl)-1-(propan-2-yl)-1H-benzimidazol-6-yl]pyrimidin-2-yl}amino)-2,3-dideoxy-D-threo-pentitol, to pharmaceutical compositions comprising such solid forms, and to use of such solid forms and pharmaceutical compositions for the treatment of cancer.
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
The present disclosure describes single agent and combination therapies and uses for the treatment of cancer and/or cancer-associated diseases. The single agent and combinations therapies include a BCMA antibody.
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
The present disclosure provides assay and method for using assay for streamlined assay preparation and testing. These assay are useful for pathogen (e.g., viral or bacterial) detection. The present disclosure also provides assay assemblies and means to prevent or minimize the formation of bubbles when using puncturing elements in fluidic devices or chambers.
The invention relates to compounds of Formula l"wherein R, R1, R2, R3, p, q and q' are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating coronavirus infection such as COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of coronaviruses such as SARS-CoV-2 with the compounds.
A61K 31/4015 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide
A61K 31/407 - Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with heterocyclic ring systems, e.g. ketorolac, physostigmine
A61K 31/454 - Non-condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
C07D 207/16 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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
71.
COMPUTERIZED DECISION SUPPORT TOOL AND MEDICAL DEVICE FOR RESPIRATORY CONDITION MONITORING AND CARE
Technology is disclosed for monitoring a user's respiratory condition and provide decision support by analyzing a user's audio data. Spoken phonemes may be detected within audio data, and acoustic features may be extracted for the phonemes. A distance metric may be computed to compare phoneme feature sets of a user. Based on the comparison, a determination about the user's respiratory condition, such as whether the user has a respiratory condition (e.g., an infection) and/or whether the condition is changing, may be made. Some aspects include predicting the user's respiratory condition in the future utilizing the phoneme feature sets. Decision support tools in the form of computer applications or services may utilize the detected or predicted respiratory condition information to initiate an action for treating a current condition or mitigating a future risk.
The present invention relates to the discovery of chemically and physically stable topical formulations comprising (R)-4-(5-(4-methoxy-3-propoxyphenyl)pyridin-3-yl)-1,2-oxaborolan-2-ol (PF-07038124) for treating inflammatory disorders and to methods of preparing the topical formulations.
This invention relates to combination therapies comprising a cyclin dependent kinase 4 (CDK4) inhibitor of Formula (I) or a pharmaceutically acceptable salt thereof, and an antiandrogen, optionally in further combination with an additional anti-cancer agent, and associated methods of treatment, pharmaceutical compositions, and uses thereof.
A61K 31/4166 - 1,3-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. phenytoin
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
The present invention provides for the treatment of patients with pediatric cancer and/or a HER2-expressing pediatric cancer with an anti-HER2 antibody-drug conjugate (ADC). In one embodiment, the anti-HER2 ADC is T(kK183C+K290C)-vc0101 (PF-06804103), in which the antibody T(kK183C+K290C) is linked to the auristatin drug 2-methylalanyl-N-[(3R,4S,5S)-3-methoxy-1-{(2S)-2-[(1R,2R) -1-methoxy-2-methyl-3-oxo-3-{[(1S)-2-phenyl-1-(1,3-thiazol-2-yl) ethyl]amino}propyl]pyrrolidin-1-yl}-5-methyl-1-oxoheptan-4-yl]-N- methyl-L-valinamide (also known as "0101") via the cleavable linker maleimidocaproyl-valine-citrulline-p-aminobenzyloxycarbonyl (also known as "vc").
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
The invention relates to a purification method of a recombinantly-produced RSV Fprotein in trimeric form.According to the invention, the method sequentially comprises an anion exchangechromatography step, a cHA chromatography step and a HIC step.The invention is also directed to a pharmaceutical product including an RSV F protein purified by such a method.
The invention relates to a purification method of an RSV protein, wherein a load solution comprising the RSV protein is contacted with an anion exchange chromatography medium, whereby the RSV protein binds to the anion exchange chromatography medium, the anion exchange chromatography medium is washed with at least one wash solution and the RSV protein is eluted from the anion exchange chromatography medium.According to the invention, the wash solution has a pH between 3.0 and 6.5, whereby the removal of host cell proteins is enhanced.The invention is also directed to a pharmaceutical product including an RSV protein purified by such a method.
This invention relates to combination therapies for use in treating cancer, comprising a cyclin dependent kinase 2 (CDK2) inhibitor of Formula (I), as further described herein, and a cyclin dependent kinase 4/6 (CDK4/6) inhibitor, optionally in further combination with an additional anti-cancer agent=.
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 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The invention relates to compounds of Formula (I) wherein R1, R2, p, m, A, Z1, Z2, Z3 and Z4 are as defined herein, pharmaceutical compositions comprising the compounds, methods of treating COVID-19 in a patient by administering therapeutically effective amounts of the compounds, and methods of inhibiting or preventing replication of SARS-CoV-2 with the compounds.
The present disclosure provides human IL-2 variants, recombinant oncolytic viruses comprising the IL-2 variant, compositions comprising the IL-2 variant or recombinant oncolytic virus, and use of the IL-2 variants, recombinant oncolytic virus, or compositions for treating cancer in an individual.
The invention relates to a computer-controlled injector, comprising: a housing configured to receive a medicament cartridge; an injection drive mechanism comprising a computer-controlled motor for driving a piston within said medicament cartridge, for injecting the medicament; a data tag attachable to said medicament cartridge; and an electromagnetic detector disposed within said housing and being connectable to the data tag upon mounting of said medicament cartridge into said housing, said electromagnetic detector permitting data to be read from or written to said data tag. The electromagnetic detector is configured to read or write data irrespectively of a rotational orientation of said medicament cartridge within said computer-controlled injector.
A61K 31/423 - Oxazoles condensed with carbocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/519 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
A61K 31/565 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
A topical formulation for use in the treatment of a dermatological condition comprising: a JAK inhibitor in an oil-in-water emulsion; white petrolatum in an amount of 10% by wt; less than 0.7 ppm butyl hydroxytoluene (BHT) by wt.; oleyl alcohol in an amount of 2% by wt.; and an antimicrobial agent. A topical formulation for use in the treatment of a dermatological condition comprising: a JAK inhibitor as an oil in purified water emulsion; white petrolatum in an amount of 10% by wt.; tocopherol in an amount of less than 6.5 ppm; oleyl alcohol in an amount of 2% by wt.; polyethylene glycol 400 in an amount of 10% by wt.; diethylene glycol monoethyl ether in an amount of 15% by wt.; mineral oil in an amount of 5% by wt.; an emulsifying wax in an amount of 10% by wt.; and an antimicrobial agent comprises 2-phenoxyethanol in an amount of 1 % by wt.; wherein the topical formulation is free of BHT and thereby maintains a yellowness index of less than 6 when stored at 40 degrees C for 16 weeks and not more than 10 when stored for 24 weeks at 40 degrees C. Said composition for use in treating or preventing a disease or condition selected from psoriasis, atopic dermatitis, atopic eczema, chronic hand eczema, uticaria, vitiligo, cutaneous lupus and alopecia areata.
Benzodiazepine derivatives of formula (Ie) wherein one of R1 and R2 is a benzodiazepinyl-containing group of formula (II) in which R8 is H or halo; the other of R1 and R2 is a group Z selected from H, C3-C6 cycloalkyl, halo, -NHR9, benzyl, phenyl, 4- to 10-membered heterocyclyl and 4- to 10-membered heteroaryl, wherein phenyl, heterocyclyl and heteroaryl are unsubstituted or substituted by one or two substituents selected from 4- to 10-membered heterocyclyl which is unsubstituted or substituted by OR, and from C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, halo, -OR, -(CH2)mOR, -NR2, -(CH2)mNR2, -NHR", -SOmNR2, -SOmR, -SR, nitro, -CO2R, -CN, -CONR2, -NHCOR, -CH2NR10R11 and -NR10R11, in which each R is independently H or C1-C6 alkyl, R" is C3-C6 cycloalkyl and m is 1 or 2; R9 is selected from phenyl and 4- to 10-membered heteroaryl wherein phenyl and heteroaryl are unsubstituted or substituted by halo; R10 and R11 are each independently H or C1-C6 alkyl; or R10 and R11 form, together with the N atom to which they are attached, either (a) a morpholine ring which is optionally bridged by a -CH2- group linking two ring carbon atoms that are positioned para to each other, or (b) a spiro group of the following formula (b): and ring A is a ring of one of the following structural formulae (I-1), (I-2) and (I-3): and ring A is a ring of one of the following structural formulae (I-1), (1-2) and (1-3): in which Y is selected from O, S, SO2 and NR, wherein R is as defined above, and each of R2 to R7 is independently H, C1-C6 alkyl, C1-C6 hydroxyalkyl, C3-C6 cycloalkyl, halo, -OR, -CH2OR, -NR2, -CH2NR12R13, -NRCOOR, -CH2OR, -SOmNR2, -SOmR, - CH2SOmR, nitro, -CO2R, -CN, -CONR2 or -NHCOR, in which R and m are as defined above and R12 and R13 are each independently H, C1-C6 alkyl, benzyl, 4- to 10-membered heterocyclyl or R12 and R13 form, together with the N atom to which they are attached, a 4- to 10-membered heteroaryl which is unsubstituted or a 4- to 10-membered heterocyclyl which is unsubstituted or substituted with C1-C6 alkyl or halo, or any two of R2 to R7 that bond to the same carbon atom form a spiro ring selected from a C3-C6 cycloalkyl spiro ring and a spiro oxetane ring of the following structure: (Formula A) and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
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
84.
BENZODIAZEPINE DERIVATIVES USEFUL IN TREATING A RESPIRATORY SYNCYTIAL VIRUS INFECTION
Benzodiazepine derivatives of formula (lb) wherein: R1 is H or halo; Y is selected from O, S, SO, SO2 and NR; one or two of V, W and X is or are N or CH and the other one or two is or are CH; R2 is a group selected from C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkyl, halo, -OR, -NHR", -SOmNR2, -SOmR, nitro, -CO2R, -CN, -CONR2, -NHCOR and -NR11R12; each R is independently H or C1-C6 alkyl; R11 and R12 are each independently H or C1-C6 alkyl; or R11 and R12 form, together with the N atom to which they are attached, either (a) a morpholine ring which is optionally bridged by a -CH2- group linking two ring carbon atoms that are positioned para to each other, or (b) a spiro group of the following formula (b): R" is C3-C6 cycloalkyl; m is 1 or 2; n is 0, 1 or 2; and each of R3 to R10 is independently selected from H, C1-C6 alkyl, halo, -OR, -NR2,-NHR", -SOmNR2, -SOmR, nitro, -CO2R, -CN, -CONR2, -NHCOR, -NR13R14 wherein R13 and R14 form, together with the N atom to which they are attached, a morpholine ring, and the following options (i) to (iii): (i) any two of R3 to R10 that bond to the same carbon atom form a C3-C6 spiro ring; (ii) any two of R3 to R10 that bond to non-adjacent carbon atoms form a C1-C3 bridgehead group linking the carbon atoms to which they are bonded; and (iii) any two of R3 to R10 that bond to adjacent carbon atoms form, together with the carbon atoms to which they are bonded, a C3-C6 cycloalkyl group; and wherein each alkyl group or moiety recited above is linear or branched; and the pharmaceutically acceptable salts thereof are inhibitors of RSV and can therefore be used to treat or prevent an RSV infection.
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 31/554 - 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 sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
Methods for preparing ((S)-2,2-difluorocyclopropyl)-((1R,5S)-3-(2-((1-methyl-1H-pyrazol-4-yl)amino)pyrimidin-4-yl)-3,8-diazabicyclo[3.2.1]-octan-8-yl)methanone and intermediates used in the processes of preparation thereof.
A compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are each independently hydrogen or hydroxy; wherein R1 and R2 are not both hydroxy. Also provided are methods of treatment as Janus Kinase inhibitors and pharmaceutical compositions containing the compounds of the invention and combinations thereof with other therapeutic agents.
The present invention relates to polypeptides and cytomegalovirus (CMV) antigens that include at least two introduced amino acid mutations relative to the amino acid sequence of the wild-type HCMV glycoprotein B (gB). In some embodiments, the polypeptide is stabilized in a conformation alternative to the gB postfusion conformation. Also disclosed are compositions including the polypeptides and uses thereof.
Technology is disclosed for detecting scratch events and predicting flares of pruritus, utilizing motion data sensed from a wearable sensor. Detecting scratch may be done with a two-tier approach by first detecting a hand motion from motion sensed data and then classifying that hand motion as a scratch event using one or more computerized classification models. Embodiments may focus on detecting nighttime scratch by utilizing motion sensed data captured during a user's detected sleep opportunity. Additionally, historical scratch event data may be used to predict a user's itch and flare risk for a future time interval. Decision support tools in the form of computer applications or services may utilize the detected scratch events or predicted itch or flare risk to initiate an action for reducing current itch and/or mitigating future risk, including initiating a treatment protocol that includes therapeutic agent.
Described herein are compounds of Formula I and their pharmaceutically acceptable salts, wherein R1, R2, R3, X1, Y1, Y2, Y3, Y4 and Y5 are defined herein; their use as MC4R antagonists; pharmaceutical compositions containing such compounds and salts; the use of such compounds and salts to treat, for example, cachexia, anorexia, or anorexia nervosa; and intermediates and processes for preparing such compounds and salts.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 31/5377 - 1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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
Described herein are pyrrolo{2,3-d}pyrimidine derivatives, their use as Janus Kinase (JAK) inhibitors, and pharmaceutical compositions containing them.
The present disclosure relates to recombinant nucleic acids and gene therapy vectors comprising a modified nucleic acid encoding aspartoacylase (ASPA), and variants thereof, for use in the treatment of diseases and disorders associated with a deficiency or dysfunction of ASPA, and in particular, Canavan disease.
This invention relates to compounds of general Formula (I) and pharmaceutically acceptable salts thereof, in which R1, R2, R3a, R3b, and R4 are as defined herein, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer.
A61K 31/444 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. amrinone
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
The present disclosure relates to the fields of packaging, transportation, and storage of temperature-sensitive materials, such as biological and/or pharmaceutical products. Various aspects of such packaging, transportation, and storage are provided herein for ultra-low temperature materials useful for the treatment and/or prevention of disease. The present disclosure also provides packaging materials, methods of transportation, and methods of storage for maintaining biological and/or pharmaceutical materials at ultra-low temperatures in order to maintain the integrity of the materials. The present disclosure further relates to the field of RNA to prevent or treat coronavirus infection.
The present invention discloses novel crystalline forms of (1R,3R)-3-(cyanomethyl)-3-(4-(6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyrazin-4-yl)-1H-pyrazol-1-yl)cyclobutane-1-carbonitrile, Form 1 anhydrous free base and Form 2 monohydrate, pharmaceutical composition containing them, preparations thereof and uses thereof.
THE REGENTS OF UNIVERSITY OF COLORADO, A BODY CORPORATE (USA)
Inventor
Arora, Mansi
Dann, Stephen George
Goodman Miller, Nicole Lee
Spencer, Sabrina
Vanarsdale, Todd Lee
Abstract
The invention provides a method for treating a disease or disorder, and preferably cancer, comprising administering to a subject in need thereof a therapeutically effective amount of a CDK2 inhibitor, and a therapeutically effective amount of a CDK4/6 inhibitor, wherein the CDK4/6 inhibitor prevents rebound phosphorylation mediated by CDK4 and/or CDK6 in response to the inhibition of CDK2.
The present invention relates to a composition comprising the OspA fusion protein of SEQ ID NO: 1 (LipSlDl-S2Dl), the OspA fusion protein of SEQ ID NO: 2 (Lip-S4D1- SShybD1) and the OspA fusion protein of SEQ ID NO: 3 (Lip-S5D1-S6D1) for use in a vaccine or for use in a method for eliciting an immune response in a human against Lyme disease.
C07K 14/20 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof from bacteria from Spirochaetales (O), e.g. Treponema, Leptospira
97.
TREATMENT OF TYPE 2 DIABETES OR OBESITY OR OVERWEIGHT WITH 2-[(4-{6-[(4-CYANO-2-FLUOROBENZYL)OXY]PYRIDIN-2-YL} PIPERIDIN-1-YL)METHYL]-1-[(2S)-OXETAN-2-YLMETHYL]-1H-BENZIMIDAZOLE-6-CARBOXYLIC ACID OR A PHARMACEUTICALLY SALT THEREOF
The invention provides a method for treating T2DM, obesity or overweight or for weight management control by administering to an mammal (e.g. a human) in need thereof a pharmaceutical composition twice daily in an oral dosage form, wherein the pharmaceutical composition contains 2-[(4-{6-[(4-cyano-2-fluorobenzyl)oxy]pyridin-2-yl}piperidin-1-yl)methyl]-1-5 [(2S)-oxetan-2-ylmethyl]-1H-benzimidazole-6-carboxylic acid, or a pharmaceutically salt thereof [such as its tris salt]. Moreover, the invention provides oral compositions/formulations for the methods of treatment described herein.
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
A method for treating fatty liver disease and related diseases or disorders with a therapeutically effective amount of a composition comprising from about 25 mg to about 1200 mg of (S)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-N-(tetrahydrofuran-3-yl)pyrimidine-5- carboxamide or a pharmaceutically acceptable salt thereof, and from about 5 mg to about 40 mg of 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6- methoxypyridin-2-yl)benzoic acid or a pharmaceutically acceptable salt thereof.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
99.
COMBINATIONS OF DIACYLGLYCEROL ACYLTRANSFERASE 2 INHIBITORS AND ACETYL-COA CARBOXYLASE INHIBITOR
Described herein are pharmaceutical compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-carboxamide, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto. Also described are compositions comprising 2-{5-[(3-ethoxypyridin-2-yl)oxy]pyridin-3-yl}-N-[(3S,5S)-5-fluoropiperidin-3-yl]pyrimidine-5-5 carboxamide, or pharmaceutically acceptable salt thereof and 4-(4-(1-Isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid, or pharmaceutically acceptable salt thereof, for treatment of liver disease and diseases related thereto.
A61K 31/438 - 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 the ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 3/10 - Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
A61P 9/10 - Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
The present invention relates to methods for purifying bacterial polysaccharides, in particular for removing impurities from cellular lysates of bacteria producing polysaccharides, comprising: a) acid hydrolysis; b) a first ultrafiltration/diafiltration-(UFDF-1); b) carbon filtration; c) chromatography; and d) a second ultrafiltration/diafiltration-(UFDF-2).
patents
