210421-64-0

Usage

InChI:InChI=1/C18H17ClN2O6S2/c1-10-5-13-14(27-9-26-13)7-11(10)6-12(22)16-15(3-4-28-16)29(23,24)20-18-17(19)21(2)8-25-18/h3-5,7,20H,6,8-9H2,1-2H3

Upstream product

• 1008726-80-4 C₉H₉ClMgO₂ 
• 210421-71-9 N-(4-chloro-3-methyl-5-isoxazolyl)-2-(N-methyl-N'-methoxy)aminocarbonyl-3-thiophenesulfonamide 
• 117661-72-0 (3,4-methylenedioxy)-6-methylbenzyl chloride 
• 7145-99-5 5-methyl-1,3-benzodioxole 
• 20850-43-5 5-(chloromethyl)-1,3-benzodioxole 
• 1006588-99-3 C₉H₅ClN₂O₄S₂ 
• 184040-74-2 3{[(4-chloro-3-methyl-5-isoxazolyl)amino]sulfonyl}-2-thiophenecarboxylic acid 

Relevant academic research and scientific papers

Methods and compositions for treatment of sleep apnea

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.

METHODS AN COMPOSITIONS FOR TREATMENT OF AN INTERSTITIAL LUNG DISEASE

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.

SUBSTITUTED THIOPHENES

Disclosed herein are substituted pyrimidine-based endothelin modulators of Formula I, processes of preparation thereof, pharmaceutical compositions thereof, and methods of use thereof.

Formulations of sitaxsentan sodium

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.

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.

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.

POLYMORPHS OF N-(4-CHLORO-3-METHYL-5-ISOXAZOLYL)2-[2-METHYL-4,5-(METHYLENEDIOXY) PHENYLACETYL]THIOPHENE-3-SULFONAMIDE, SODIUM SALT

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.

CRYSTALLINE N-(4-CHLORO-3-METHYL-5-ISOXAZOLYL)-2-[2-METHYL-4,5-(METHYLENEDIOXY)PHENYLACETYL]-THIOPHENE-3-SULFONAMIDE

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-isoxazolyl)-2-[2-methyl-4,5-(methylenedioxy)phenylacetyl]thiophene-3-sulfonamide or pharmaceutical compositions thereof.

N-aryl thienyl-, furyl-, and pyrrolyl-sulfonamides and derivatives thereof that modulate the activity of endothelin

Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.

Sulfonamides for treatment of endothelin-mediated disorders

Thienylsulfonamides and their pharmaceutically acceptable derivatives, pharmaceutical compositions, articles of manufacture, combinations, lyophilized powders and methods for the treatment of endothelin diseases using these formulations and sulfonamides a