Provided herein are compounds of Formula (I), (I), or pharmaceutically acceptable salt thereof, wherein m, n, p, A1, A2, A3, A4, L, R1, R2, R3, R4, Formula (II), (II), V, X, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
Provided herein are compounds of Formula (I), (I), or pharmaceutically acceptable salt thereof, wherein m, n, p, A1, A2, A3, A4, L, R1, R2, R3, R4, Formula (II), (II), V, X, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
A61K 31/439 - 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 forming part of a bridged ring system, e.g. quinuclidine
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 31/5386 - 1,4-Oxazines, e.g. morpholine spiro-condensed or forming part of bridged ring systems
A61K 31/547 - 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 spiro-condensed or forming part of bridged ring systems
C07D 498/22 - Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
The present disclosure provides compounds and their methods of use. In particular, the compounds of the present disclosure may be useful for inhibiting RAS proteins, such as KRAS proteins. The disclosed compound may be used in the treatment of cancer and be highly selective for KRAS proteins having the G12D mutation. Alternatively or additionally, said compounds may have broad spectrum activity across a range of KRAS proteins.
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 31/4162 - 1,2-Diazoles condensed with heterocyclic ring systems
09 - Scientific and electric apparatus and instruments
16 - Paper, cardboard and goods made from these materials
41 - Education, entertainment, sporting and cultural services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Downloadable electronic publications in the nature of brochures, newspapers, and articles in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals Printed brochures about sleep disorders, sleep health, healthcare, and pharmaceuticals; Printed newsletters in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Printed articles in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals Educational services, namely, conducting seminars, conferences, lectures, and workshops in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals and distribution of educational materials in connection therewith; Arranging and conducting of seminars in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Arranging and conducting of conferences in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Arranging and conducting of lectures in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Arranging and conducting of workshops in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Providing a website featuring non-downloadable articles in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals Providing medical information; Providing a web site featuring medical information; Providing a website featuring information about health and wellness, namely, sleep disorders, sleep health, healthcare, and pharmaceuticals; Providing information in the field of sleep health via a website; Providing information in the field of the diagnosis and treatment of sleep disorders via a website; Providing a website featuring information in the field of the diagnosis and treatment of sleep disorders
09 - Scientific and electric apparatus and instruments
16 - Paper, cardboard and goods made from these materials
41 - Education, entertainment, sporting and cultural services
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Downloadable electronic publications in the nature of brochures, newspapers, and articles in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals Printed brochures about sleep disorders, sleep health, healthcare, and pharmaceuticals; Printed newsletters in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Printed articles in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals Educational services, namely, conducting seminars, conferences, lectures, and workshops in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals and distribution of educational materials in connection therewith; Arranging and conducting of seminars in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Arranging and conducting of conferences in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Arranging and conducting of lectures in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Arranging and conducting of workshops in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals; Providing a website featuring non-downloadable articles in the field of sleep disorders, sleep health, healthcare, and pharmaceuticals Providing medical information; Providing a web site featuring medical information; Providing a website featuring information about health and wellness, namely, sleep disorders, sleep health, healthcare, and pharmaceuticals; Providing information in the field of sleep health via a website; Providing information in the field of the diagnosis and treatment of sleep disorders via a website; Providing a website featuring information in the field of the diagnosis and treatment of sleep disorders
5.
NOVEL AMINE-SUBSTITUTED PHTHALAZINES AND DERIVATIVES AS SOS1 INHIBITORS
The present disclosure provides compounds of formula (Ia) that are inhibitors of SOS1, pharmaceutical compositions thereof, and methods of treating oncological diseases using the compounds and compositions disclosed herein.
The present disclosure provides compounds of formula (Ia) that are inhibitors of SOS1, pharmaceutical compositions thereof, and methods of treating oncological diseases using the compounds and compositions disclosed herein.
The present disclosure relates to methods of treating idiopathic hypersomnia with oxybate, preferably a mixture of salts of oxybate (a mixed salt oxybate).
42 - Scientific, technological and industrial services, research and design
Goods & Services
Software as a service (SAAS) services featuring software for healthcare management and patient management; Providing on-line non-downloadable software for healthcare management and patient management
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising administering to a human subject a recombinant L-asparaginase.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceuticals for the treatment and prevention of cancer,
psychiatric diseases and disorders, central nervous system
conditions, pain, sleep disorders, narcolepsy,
schizophrenia, and for use in oncology and hematology;
pharmaceutical products for the prevention and treatment of
cancer; pharmaceutical preparations and substances for the
treatment of psychiatric diseases and disorders;
pharmaceutical preparations acting on the central nervous
system; pain relief medication; pharmaceutical preparations
for use in the treatment and/or management of sleep
disorders; pharmaceutical preparations for the treatment of
narcolepsy; pharmaceutical preparations for the treatment of
schizophrenia; pharmaceutical preparations for use in
oncology and hematology.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
(1) Pharmaceuticals for the treatment and prevention of cancer, psychiatric diseases and disorders, central nervous system conditions, pain, sleep disorders, narcolepsy, schizophrenia, and for use in oncology and hematology; pharmaceutical products for the prevention and treatment of cancer; pharmaceutical preparations and substances for the treatment of psychiatric diseases and disorders; pharmaceutical preparations acting on the central nervous system; pain relief medication; pharmaceutical preparations for use in the treatment and/or management of sleep disorders; pharmaceutical preparations for the treatment of narcolepsy; pharmaceutical preparations for the treatment of schizophrenia; pharmaceutical preparations for use in oncology and hematology.
This invention relates to compounds that may be useful for inhibiting RAS proteins. More specifically, this invention relates to compounds for inhibiting a broad spectrum of KRAS mutant proteins, including KRAS G12D. The compounds of the invention may therefore be used in treating conditions mediated by KRAS proteins. For example, the compounds may be used in treating 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
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, A, L1, L2, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, A, L1, L2, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
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 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61K 31/443 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with oxygen as a ring hetero atom
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
C07D 215/227 - Oxygen atoms attached in position 2 or 4 only one oxygen atom which is attached in position 2
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 239/36 - One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
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 401/12 - 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
Various formulations for combination therapy with a liposome and an inhibitor of SR-BI, leading to enhanced uptake of the liposome by a target cell are provided and exemplified by combination therapy with CPX-351 and BLT-1. Also provided are various formulations for combination therapy with a liposome and an ENT inhibitor leading to enhanced uptake of liposome-encapsulated cytarabine by a target cell. Also provided are methods of using the formulations in combination therapy. Also provided is a method of reducing cardiotoxicity in an age-stratified patient population undergoing therapy with cytarabine and daunorubicin, CPX-351.
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 31/7076 - 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 containing purines, e.g. adenosine, adenylic acid
A61K 9/127 - Synthetic bilayered vehicles, e.g. liposomes or liposomes with cholesterol as the only non-phosphatidyl surfactant
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
This disclosure relates to methods and compositions for treating cancer using an inducible IFNalpha prodrug. When the inducible IFNalpha prodrug is in a site of interest (such as a tumor microenvironment), the protease cleavable linker is cleaved by a protease active in the site of interest, releasing an unattenuated form of IFNalpha. This conditional activity preserves the immune stimulatory effects of while limiting the systemic toxicity associated with non-inducible IFNalpha therapy.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceuticals for the treatment and prevention of cancer, psychiatric diseases and disorders, central nervous system conditions, pain, sleep disorders, narcolepsy, schizophrenia, and for use in oncology and hematology; pharmaceutical products for the prevention and treatment of cancer; pharmaceutical preparations and substances for the treatment of psychiatric diseases and disorders; pharmaceutical preparations acting on the central nervous system; pain relief medication; pharmaceutical preparations for use in the treatment and/or management of sleep disorders; pharmaceutical preparations for the treatment of narcolepsy; pharmaceutical preparations for the treatment of schizophrenia; pharmaceutical preparations for use in oncology and hematology
The present disclosure relates to methods of treating a solid tumor by administering a therapeutically effective amount of a mitogen activated protein kinase (MAPK) inhibitor having a structure, Compound: (I), or a pharmaceutically acceptable salt thereof.
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 31/353 - 3,4-Dihydrobenzopyrans, e.g. chroman, catechin
A61K 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
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
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
Provided herein are compounds of Formula (I), (I), or pharmaceutically acceptable salt thereof, wherein m, n, p, L, R1, R2, R3, R4, R5, R6, Formula (AA), (AA), V, X, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein n, m, A1, A2, A3, A4, A5, A6, L1, L2, R1, R2, R3, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound N of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
Provided herein are compounds of Formula (I), or pharmaceutically acceptable salt thereof, wherein n, m, A1, A2, A3, A4, A5, A6, L1, L2, R1, R2, R3, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound N of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
Provided herein are stable, aqueous, non-lyophilized formulations of L-asparaginase. Also provided herein are methods of using such formulations in the treatment of one or more diseases, disorders, or conditions (for example, cancers such as Acute Lymphoblastic Leukemia (ALL) or Lymphoblastic Lymphoma (LBL)) that are treatable by asparagine depletion.
The present disclosure relates to crystalline forms of (S)-5-((3-(4-(4-fluorophenyl)-1H-imidazol-2-yl)chroman-6-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one, Compound (I) or a salt, solvate, or solvate salt thereof.
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
Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
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
09 - Scientific and electric apparatus and instruments
16 - Paper, cardboard and goods made from these materials
41 - Education, entertainment, sporting and cultural services
Goods & Services
Instructional and educational materials in the nature of electronic publications, namely, downloadable brochures concerning healthcare and medicine; Downloadable electronic publications in the nature of downloadable brochures concerning healthcare and medicine Instructional and educational materials in the nature of printed brochures concerning healthcare and medicine; Printed instructional and educational brochures concerning healthcare and medicine Educational services, namely, providing educational speakers, classes, workshops, conferences, and seminars in the fields of healthcare and medicine, and distribution of training materials in connection therewith; Educational webinars in the fields of healthcare and medicine; Providing non-downloadable electronic publications in the nature of non-downloadable electronic brochures concerning healthcare and medicine
44 - Medical, veterinary, hygienic and cosmetic services; agriculture, horticulture and forestry services
Goods & Services
Promoting public awareness of medical conditions, medical research, and options for diagnosis, treatment, and management; Promoting public awareness by means of public advocacy of medical conditions, medical research, and options for diagnosis, treatment, and management Providing medical information; Providing online medical information; Providing a website featuring information in the fields of healthcare, medicine, and cancer and oncological disorders
33.
DEFIBROTIDE FOR USE IN PREVENTING AND TREATING SEPSIS
The present disclosure provides methods of preventing, lessening the effects, or treating sepsis comprising administering a prophylactically effective amount of defibrotide to a subject in need thereof.
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal 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
A61K 31/4433 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with oxygen as a ring hetero atom
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as cancer.
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 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 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 417/14 - 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 three or more hetero rings
The disclosure provides a modified protein that is a combination of (i) an L-asparaginase and (ii) one or more (poly)peptide(s), wherein the (poly)peptide consists solely of proline and alanine amino acid residues, and methods of preparation and use thereof.
The disclosure is directed to compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. The disclosure is also directed to pharmaceutical compositions containing compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof, and uses of the pharmaceutical compositions in treating diseases, conditions, and disorders associated with fatty acid amide hydrolase (FAAH) activity.
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
A61K 31/497 - Non-condensed pyrazines containing further heterocyclic rings
A61K 31/4465 - Non-condensed piperidines, e.g. piperocaine only substituted in position 4
The present disclosure provides compositions and methods for treating cancer in a human subject comprising dosing a human subject with a monotherapy or combination therapy involving L-asparaginase. Combination therapies disclosed herein include combination therapies with functionalized or unfunctionalized L-asparaginase in combination with a BCL-XL inhibitor, a BCL-2 inhibitor, a CD20 inhibitor, an mTOR inhibitor, or another anticancer agent.
A61K 38/50 - Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
A61K 31/635 - Compounds containing para-N-benzene- sulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonohydrazide having a heterocyclic ring, e.g. sulfadiazine
Provided herein are methods of treating fibromyalgia, post-traumatic stress disorder, irritable bowel syndrome, and irritable bowel disease in a patient with a slow wave sleep deficit by administering oxybate or a pharmaceutically acceptable salt thereof.
123412344, Formula (II), (II), V, X, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
A61P 25/00 - Drugs for disorders of the nervous system
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
Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as 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
C07D 239/47 - One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
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 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 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 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
43.
TRICYCLIC PHTHALAZINES AND DERIVATIVES AS SOS1 INHIBITORS
The present disclosure provides compounds that are inhibitors of SOS1, pharmaceutical compositions thereof, and methods of treating oncological diseases using the compounds and compositions disclosed herein.
The present disclosure provides compounds of formula (la) that are inhibitors of SOS1, pharmaceutical compositions thereof, and methods of treating oncological diseases using the compounds and compositions disclosed herein.
Low-viscosity nucleic acid compositions that can be administered by oral or multiple parenteral routes may allow for less frequent dosing than nucleic acid products currently on the market. In particular, low-viscosity defibrotide formulations for subcutaneous, intramuscular, intradermal, and intraperitoneal administration are more convenient to the patient and/or are administered outside of the hospital setting. Formulations of the invention may be used for the treatment of numerous conditions including for example, treatment of peripheral arteriopathies, treatment of acute renal insufficiency, treatment of acute myocardial ischemia, and treatment and prevention of sinusoidal obstruction syndrome or VOD.
A61K 31/7105 - Natural ribonucleic acids, i.e. containing only riboses attached to adenine, guanine, cytosine or uracil and having 3'-5' phosphodiester links
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61K 9/00 - Medicinal preparations characterised by special physical form
A61M 5/145 - Pressure infusion, e.g. using pumps using pressurised reservoirs, e.g. by means of pistons
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
A61K 38/50 - Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
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 47/60 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
The present disclosure provides methods of preventing, lessening the effects, or treating organ injury and/or organ rejection optionally associated with organ transplant comprising administering defibrotide. The defibrotide can be administered to the donor organ via the donor organ's artery, to the donor organ via a preservation bath, or to the patient.
A61K 31/711 - Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
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
A61K 9/00 - Medicinal preparations characterised by special physical form
This disclosure provides methods for treating a disease or disorder by administering pharmaceutical compounds. In particular, the disclosure relates to treating posttraumatic stress disorder in an individual in need thereof by administering a fatty acid amid hydrolase inhibitor or a pharmaceutically acceptable salt thereof.
This invention relates to novel compounds. The compounds of the invention are kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Raf kinases, e.g., B-Raf and C-Raf. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Raf kinases, for example, cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia.
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
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 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
53.
SULFONAMIDE OREXIN RECEPTOR AGONISTS AND USES THEREOF
1234122, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
C07D 213/42 - Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
C07D 231/12 - Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 239/26 - Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
C07D 307/94 - Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom spiro-condensed with carbocyclic rings or ring systems, e.g. griseofulvins
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
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceuticals, medical and veterinary preparations;
sanitary preparations for medical purposes; dietetic food
and substances adapted for medical or veterinary use, food
for babies; dietary supplements for human beings and
animals; plasters, materials for dressings; material for
stopping teeth, dental wax; disinfectants; preparations for
destroying vermin; fungicides, herbicides.
55.
GAMMA-HYDROXYBUTYRATE COMPOSITIONS AND THEIR USE FOR THE TREATMENT OF DISORDERS
Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
123456121233, Y and Z are defined herein. Also provided herein are pharmaceutical compositions comprising a compound of Formula (I) or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I) or pharmaceutically acceptable salt thereof, e.g., in the treatment of a disease or disorder that is treatable by administration of an Orexin agonist.
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
A61P 43/00 - Drugs for specific purposes, not provided for in groups
57.
DEFIBROTIDE FOR THE TREATMENT AND PREVENTION OF ACUTE RESPIRATORY DISTRESS SYNDROME
The present disclosure provides methods of preventing, lessening the effects, or treating acute respiratory distress syndrome (ARDS) comprising administering defibrotide.
A61K 31/711 - Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61K 9/00 - Medicinal preparations characterised by special physical form
A61P 11/00 - Drugs for disorders of the respiratory system
C12Q 1/00 - Measuring or testing processes involving enzymes, nucleic acids or microorganismsCompositions thereforProcesses of preparing such compositions
58.
DOSING AND ADMINISTRATION OF RECOMBINANT L-ASPARAGINASE
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising dosing a human subject with L-asparaginase.
Provided herein are stable, aqueous, non-lyophilized formulations of L-asparaginase. Also provided herein are methods of using such formulations in the treatment of one or more diseases, disorders, or conditions (for example, cancers such as Acute Lymphoblastic Leukemia (ALL) or Lymphoblastic Lymphoma (LBL)) that are treatable by asparagine depletion.
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising dosing a human subject with L-asparaginase.
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising dosing a human subject with L-asparaginase.
A61K 38/50 - Hydrolases (3) acting on carbon-nitrogen bonds, other than peptide bonds (3.5), e.g. asparaginase
A61K 9/00 - Medicinal preparations characterised by special physical form
A61K 47/60 - 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 macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
A61P 35/02 - Antineoplastic agents specific for leukemia
62.
DOSING AND ADMINISTRATION OF RECOMBINANT L-ASPARAGINASE
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising dosing a human subject with L-asparaginase.
05 - Pharmaceutical, veterinary and sanitary products
Goods & Services
Pharmaceuticals, medical and veterinary preparations; sanitary preparations for medical purposes; dietetic food and substances adapted for medical or veterinary use, food for babies; dietary supplements for human beings and animals; plasters, materials for dressings; material for stopping teeth, dental wax; disinfectants; preparations for destroying vermin; fungicides, herbicides.
64.
METHODS OF PURIFYING CHARGE-SHIELDED FUSION PROTEINS
The present invention relates to method of purifying charge-shielded proteins from a cell lysate or periplasmic releasate using hydrophobic interaction chromatography as a first chromatography steps. Also provided herein are compositions comprising charge-shielded proteins and methods of treatment using purified charge-shielded proteins.
B01D 15/32 - Bonded phase chromatography, e.g. with normal bonded phase, reversed phase or hydrophobic interaction
B01D 15/36 - Selective adsorption, e.g. chromatography characterised by the separation mechanism involving ionic interaction, e.g. ion-exchange, ion-pair, ion-suppression or ion-exclusion
B01D 15/42 - Selective adsorption, e.g. chromatography characterised by the development mode, e.g. by displacement or by elution
65.
METHODS OF PURIFYING CHARGE-SHIELDED FUSION PROTEINS
The present invention relates to method of purifying charge- shielded proteins from a cell lysate or periplasmic releasate using hydrophobic interaction chromatography as a first chromatography steps. Also provided herein are compositions comprising charge- shielded proteins and methods of treatment using purified charge-shielded proteins.
C07K 1/20 - Partition-, reverse-phase or hydrophobic interaction chromatography
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
One embodiment of the present invention is to improve the safety and efficacy of the administration of GHB or a salt thereof to a patient. It has been discovered that the concomitant administration of an MCT inhibitor, such as diclofenac, valproate, or ibuprofen, will affect GHB administration. For example, it has been discovered that diclofenac lowers the effect of GHB in the body, thereby potentially causing an unsafe condition. Furthermore, it has been discovered that valproate increases the effect of GHB on the body, thereby potentially causing an unsafe condition.
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
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 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
G16H 20/10 - ICT specially adapted for therapies or health-improving plans, e.g. for handling prescriptions, for steering therapy or for monitoring patient compliance relating to drugs or medications, e.g. for ensuring correct administration to patients
The invention relates to modified release oral formulations of therapeutic agents, including gamma hydroxybutyrate (GHB), paracetamol, codeine or oxycodone, which are resistant to alcohol induced dose dumping. Provided are formulations that have improved resistance to rapid release of the active ingredient in the presence of increasing amounts of alcohol. Also provided are formulations that can reduce or prevent the release of the active ingredient following exposure to alcohol-containing media. The invention also relates to methods of making the formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
Provided herein are methods of treating fibromyalgia, post-traumatic stress disorder, irritable bowel syndrome, and irritable bowel disease in a patient with a slow wave sleep deficit by administering oxybate or a pharmaceutically acceptable salt thereof.
The disclosure provides a modified protein that is a combination of (i) an L-asparaginase and (ii) one or more (poly)peptide(s), wherein the (poly)peptide consists solely of proline and alanine amino acid residues, and methods of preparation and use thereof.
C07K 1/00 - General processes for the preparation of peptides
C07H 21/04 - 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 deoxyribosyl as saccharide radical
A61K 38/02 - Peptides of undefined number of amino acidsDerivatives thereof
A61K 38/48 - Hydrolases (3) acting on peptide bonds (3.4)
C07K 14/00 - Peptides having more than 20 amino acidsGastrinsSomatostatinsMelanotropinsDerivatives thereof
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitor enantiomers of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, with high enantiomeric excess (% ee). The disclosure also relates to method of using the compound of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal 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
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitors of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (I-A), (I-B), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
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
A61K 45/06 - Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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
75.
FUSED BICYCLIC RAF INHIBITORS AND METHODS FOR USE THEREOF
The present disclosure relates to fused bicyclic Raf inhibitors of formula (I), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof. The disclosure also relates to method of using the compound of formula (I), (II), or (III), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal 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
C07D 417/14 - 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 three or more hetero rings
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 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
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 31/4178 - 1,3-Diazoles not condensed and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
The present disclosure generally relates to improved synthesis of fused bicyclic Raf inhibitor enantiomers of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, with high enantiomeric excess (%ee). The disclosure also relates to method of using the compound of formula (I), (Ia), (Ib), (II), (IIa), or (IIb), or a pharmaceutically acceptable salt, tautomer, or stereoisomer thereof, for treating diseases such as cancer, including colorectal cancer.
C07D 405/04 - 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 directly linked by a ring-member-to-ring- member bond
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
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
77.
SUBCUTANEOUS DELIVERY OF HIGH CONCENTRATION FORMULATIONS
The present disclosure provides high concentration low viscosity defibrotide formulations administered via an automated injection device. The device is calibrated for optimum flow rate and administration of the high concentration low viscosity formulation.
A61M 5/152 - Pressure infusion, e.g. using pumps using pressurised reservoirs, e.g. by means of pistons flexible pressurised by contraction of elastic reservoirs
A61K 31/711 - Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
The present disclosure relates to methods of treating idiopathic hypersomnia with oxybate, preferably a mixture of salts of oxybate (a mixed salt oxybate).
Low-viscosity, high concentration nucleic acid compositions that can be administered by multiple parenteral routes may allow for less frequent dosing than nucleic acid products currently on the market. In particular, low-viscosity defibrotide formulations for subcutaneous, intramuscular, and intraperitoneal administration are more convenient to the patient and/or are administered outside of the hospital setting. Formulations of the invention may be used for the treatment of numerous conditions including for example, treatment of peripheral arteriopathies, treatment of acute renal insufficiency, treatment of acute myocardial ischemia, and treatment and prevention of sinusoidal obstruction syndrome or VOD.
The present disclosure provides methods of preventing, lessening the effects, or treating organ injury and/or organ rejection optionally associated with organ transplant comprising administering defibrotide. The defibrotide can be administered to the donor organ via the donor organ's artery, to the donor organ via a preservation bath, or to the patient.
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
A61P 37/06 - Immunosuppressants, e.g. drugs for graft rejection
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising administering to a human subject a recombinant L-asparaginase.
Low-viscosity nucleic acid compositions that can be administered by oral or multiple parenteral routes may allow for less frequent dosing than nucleic acid products currently on the market. In particular, low-viscosity defibrotide formulations for subcutaneous, intramuscular, intradermal, and intraperitoneal administration are more convenient to the patient and/or are administered outside of the hospital setting. Formulations of the invention may be used for the treatment of numerous conditions including for example, treatment of peripheral arteriopathies, treatment of acute renal insufficiency, treatment of acute myocardial ischemia, and treatment and prevention of sinusoidal obstruction syndrome or VOD.
A61K 31/711 - Natural deoxyribonucleic acids, i.e. containing only 2'-deoxyriboses attached to adenine, guanine, cytosine or thymine and having 3'-5' phosphodiester links
A61K 47/12 - Carboxylic acidsSalts or anhydrides thereof
A61K 47/18 - AminesAmidesUreasQuaternary ammonium compoundsAmino acidsOligopeptides having up to five amino acids
A61M 5/00 - Devices for bringing media into the body in a subcutaneous, intra-vascular or intramuscular wayAccessories therefor, e.g. filling or cleaning devices, arm rests
Provided herein are compounds identified as inhibitors of KRAS protein activity that can be used to treat various diseases and disorders, such as cancer.
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 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
A61P 31/00 - Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
A61K 31/496 - Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
One embodiment of the present invention is to improve the safety and efficacy of the administration of GHB or a salt thereof to a patient. It has been discovered that the concomitant administration of an MCT inhibitor, such as diclofenac, valproate, or ibuprofen, will affect GHB administration. For example, it has been discovered that diclofenac lowers the effect of GHB in the body, thereby potentially causing an unsafe condition. Furthermore, it has been discovered that valproate increases the effect of GHB on the body, thereby potentially causing an unsafe condition.
A61K 31/20 - Carboxylic acids, e.g. valproic acid having a carboxyl group bound to an acyclic chain of seven or more carbon atoms, e.g. stearic, palmitic or arachidic acid
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 43/00 - Drugs for specific purposes, not provided for in groups
A61K 31/616 - Salicylic acidDerivatives thereof having the hydroxy group in position 2 esterified, e.g. salicylsulfuric acid by carboxylic acids, e.g. acetylsalicylic acid
A61K 31/505 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim
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
Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
The present invention provides compositions and methods for treating a disease treatable by asparagine depletion in a human subject comprising administering to a human subject a recombinant L-asparaginase.
Provided herein are pharmaceutical compositions and formulations comprising mixed salts of gamma-hydroxybutyrate (GHB). Also provided herein are methods of making the pharmaceutical compositions and formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
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
A61K 9/00 - Medicinal preparations characterised by special physical form
The invention relates to modified release oral formulations of therapeutic agents, including gamma hydroxybutyrate (GHB), paracetamol, codeine or oxycodone, which are resistant to alcohol induced dose dumping. Provided are formulations that have improved resistance to rapid release of the active ingredient in the presence of increasing amounts of alcohol. Also provided are formulations that can reduce or prevent the release of the active ingredient following exposure to alcohol-containing media. The invention also relates to methods of making the formulations, and methods of their use for the treatment of sleep disorders such as apnea, sleep time disturbances, narcolepsy, cataplexy, sleep paralysis, hypnagogic hallucination, sleep arousal, insomnia, and nocturnal myoclonus.
