Provided are compounds that are modulators of urotensin-II receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of urotensin-II receptor activity wherein the disease is a cardiovascular disorder, atherosclerosis, renal failure, nephrotoxicity and diarrhea caused by antineoplastic agents, post-myocardial infarction, pulmonary hypertension, diabetes or a CNS related disease.
Provided are compounds that are modulators of urotensin-II receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of urotensin-II receptor activity.
Provided are compounds of Formula (I) or of Formula (II) that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or amelioratin diseases associated with modulation of CCR9 receptor activity.
C07D 333/38 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Provided are compounds that are modulators of CCR9 receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, provided are methods for treating or ameliorating diseases associated with modulation of CCR9 receptor activity.
C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Provided herein are intravenous and oral formulations of N-(2-acetyl-4,6-dimethylphenyl)-3 -{ [(3,4 dimethyl-5 -isoxazolyl)amino] sulfonyl }-2-thiophenecarboxamide. Also provided are methods of making and using the formulations.
Provided herein are methods of treatment of an interstitial lung disease (ILD) by administering an endothelin antagonist, such as sitaxsentan or a pharmaceutically acceptable salt thereof.
Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.
C07D 279/14 - 1,4-ThiazinesHydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
C07D 279/22 - [b, e]-condensed with two six-membered rings with carbon atoms directly attached to the ring nitrogen atom
C07D 307/68 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C07D 333/70 - Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
C07D 401/06 - 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 carbon chain containing only aliphatic carbon atoms
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
C07D 409/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4412 - Non-condensed pyridinesHydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
A61P 29/00 - Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agentsNon-steroidal antiinflammatory drugs [NSAID]
8.
PROCESSES FOR THE PREPARATION OF 4-CHLORO-3-METHYL-5-(2-(2-(6-METHYLBENZO[D][1,3]DIOXOL-5-YL)ACETYL)-3-THIENYLSULFONAMIDO) ISOXAZOLE
Provided are processes for the preparation of 4-chloro-3-methyl-5-(2-(2-(6- methylbenzo[d][1,3Jdioxol-5-yl)acetyl)-3-thienylsulfonamido)isoxazole of formula (I), a compound useful for the treatment of endothelin-mediated disorders.
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
N-(2-acetyl-4,6-dimethylphenyl)-3-([(3,4 dimethyl-5-isoxazolyl)aminosulfonyl}- 2-thiophenecarboxamide, is provided here in the form of three polymorphs (Forms A, C and E). Forms A, C and E are specified by their peaks in their X-ray powder diffraction patterns, their absorption peaks in their infrared absorption spectra in potassium bromide, their peaks in their Raman absorption spectra and their melting points.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
10.
PROCESSES FOR THE PREPARATION OF N-(2-ACETYL-4,6-DIMETHYLPHENYL)-3-{[(3,4 DIMETHYL-5-ISOXAZOLYL)AMINO}SULFONYL}-2-THIOPHENECARBOXAMIDE
Provided are processes for the preparation of N-(2-acetyl-4,6-dimethylphenyl)-3- {[(3,4 dimethyl-5-isoxazolyl)amino]sulfonyl}-2-thiophenecarboxamide, a compound useful for the treatment of endothelin-mediated disorders.
C07D 413/12 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Provided herein are polymorphs of N-(4-chloro-3-methyl-5-isoxazolyl)-2-[2-methyl- 4, 5-(methylenedioxy)phenylacetyl]thiophene-3-sulfonamide and pharmaceutical compositions thereof. Also provided are methods of treatment of endothelin-mediated disorders by administering a polymorph N-(4-chloro-3-methyl-5-isoxazolyI)-2-[2-methyl-4, 5-(methylenedioxy)phenylacetyl]thiophene-3-sulfonamide or pharmaceutical compositions thereof.
C07D 413/14 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61P 9/00 - Drugs for disorders of the cardiovascular system
A61P 11/00 - Drugs for disorders of the respiratory system
A61P 15/00 - Drugs for genital or sexual disordersContraceptives
12.
METHODS AND COMPOSITIONS FOR TREATMENT OF SLEEP APNEA COMPRISING ADMINISTRATION OF AN ENDOTHELIN ANTAGONIST
Provided herein are methods of treatment of sleep apnea by administering an endothelin antagonist, such as sitaxsentan or a pharmaceutically acceptable salt thereof to a patient in need of the treatment.
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/422 - Oxazoles not condensed and containing further heterocyclic rings
A61K 31/506 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
A61K 45/00 - Medicinal preparations containing active ingredients not provided for in groups
A61P 11/00 - Drugs for disorders of the respiratory system
Provided herein are stable lyophilized and oral formulations of sitaxsentan sodium. In certain embodiments the lyophilized formulations provided herein have improved stability upon reconstitution. Also provided are methods of making and using the formulations.
A61K 47/14 - Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
A61K 47/20 - Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing sulfur, e.g. dimethyl sulfoxide [DMSO], docusate, sodium lauryl sulfate or aminosulfonic acids
14.
METHODS AND COMPOSITIONS FOR TREATMENT OF DIASTOLIC HEART FAILURE
Provided herein are methods of treatment of diastolic heart failure (DHF) by administering an endothelin antagonist, such as sitaxsentan or a pharmaceutically acceptable salt thereof.
A61K 31/194 - Carboxylic acids, e.g. valproic acid having two or more carboxyl groups, e.g. succinic, maleic or phthalic acid
A61K 31/357 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having two or more oxygen atoms in the same ring, e.g. crown ethers, guanadrel
A61K 31/401 - ProlineDerivatives thereof, e.g. captopril
N-(4-chloro-3-methyl-5-isoxazolyl)-2-⏧2-methyl-4,5-(methylenedioxy)phenyl- acetyl]thiophene-3-sulfonamide,, sodium salt, is provided herein in the form of three polymorphs (Forms A, B and C). Forms A, B and C are specified by the peaks in their X-ray powder diffraction patterns, their absorption peaks in their infrared absorption spectra, their peaks in their Raman spectra and their melting points.
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
patents