1400699-63-9

Upstream product

• 50824-05-0 4-trifluoromethoxybenzyl bromide 
• 66729-00-8 3-amino-4-chloroisoquinoline 
• 1400702-33-1 ethyl 4-{[(4-iodoisoquinolin-3-yl)amino]sulfonyl}benzoate 
• 1400702-32-0 ethyl 4-[(isoquinolin-3-ylamino)sulfonyl]benzoate 
• 1400702-34-2 ethyl 4-({(4-iodoisoquinolin-3-yl)[4-(trifluoromethoxy)benzyl]amino}sulfonyl)benzoate 
• 411235-57-9 cyclopropylboronic acid 
• 25475-67-6 isoquinolin-3-amine 
• 10486-51-8 4-ethoxycarbonylbenzenesulfonyl chloride 
• 1400700-13-1 ethyl 4-({(4-bromoisoquinolin-3-yl)[4-(trifluoromethoxy)benzyl]amino}-sulfonyl)benzoate 

Downstream Products

• 1400699-64-0 4-({(4-cyclopropylisoquinolin-3-yl)[4-(trifluoromethoxy)benzyl]amino}sulfonyl)benzoic acid 

Relevant academic research and scientific papers

METHOD FOR PRODUCING SULFONAMIDE COMPOUND

PROBLEM TO BE SOLVED: To provide a method for producing a compound (I) which is excellent in reactivity, stirring performance and production workability, achieves high quality of a production intermediate and is suitable for production on an industrial scale in comparison with a conventional production method. SOLUTION: There is provided a method for producing a compound (4) which comprises: (i) chlorinating a compound (1) by reacting with a chlorination agent to obtain a compound (2); and (ii) subjecting the compound (2) to a coupling reaction with a compound (3) in the presence of a palladium catalyst to obtain a compound (4). SELECTED DRAWING: None COPYRIGHT: (C)2018,JPOandINPIT

SULFONAMIDE COMPOUND

The present invention provides novel sulfonamide compounds having TRPM8 antagonistic activity which are useful as medicaments. Specifically, the present invention provides a sulfonamide compound of the formula (I): wherein Ring A is the following formula (i), (ii), or (ix): R4 is optionally substituted alkyl, X1 and X2 are each independently tetrazolyl, tetrazolinonyl, optionally substituted triazolyl, triazolinonyl, oxadiazolonyl, optionally substituted alkanoylaminomethyl, or optionally substituted alkylsulfonylaminomethyl, or R4 and X2 combine with each other at their terminals together with the adjacent benzene to form indazolinonyl or benzoisoxazolonyl, and the other symbols are the same as described in the specification, or a pharmaceutically acceptable salt thereof.

Sulfonamide Compound

The present invention provides novel sulfonamide compounds having TRPM8 antagonistic activity which are useful as medicaments. Specifically, the present invention provides a sulfonamide compound of the formula (I): wherein Ring A is the following formula (i), (ii), or (ix): R4 is optionally substituted alkyl, X1 and X2 are each independently tetrazolyl, tetrazolinonyl, optionally substituted triazolyl, triazolinonyl, oxadiazolonyl, optionally substituted alkanoylaminomethyl, or optionally substituted alkylsulfonylaminomethyl, or R4 and X2 combine with each other at their terminals together with the adjacent benzene to form indazolinonyl or benzoisoxazolonyl, and the other symbols are the same as described in the specification, or a pharmaceutically acceptable salt thereof.

SULFONAMIDE COMPOUNDS HAVING TRPM8 ANTAGONISTIC ACTIVITY

Sulfonamide compounds having TRPM8 antagonistic activity are provided. A sulfonamide compound of formula (I) or a pharmaceutically acceptable salt thereof, or a prodrug thereof: (I) wherein Ring A is bicyclic aromatic heterocycle comprised of (a) pyridine is condensed with benzene; or (b) pyridine is condensed with monocyclic aromatic heterocycle, and Ring A binds to a sulfonylamino moiety on a carbon atom adjacent to a nitrogen atom of the pyridine ring constituting Ring A, Ring B is (a) monocyclic or bicyclic aromatic hydrocarbon; (b) monocyclic or bicyclic alicyclic hydrocarbon; (c) monocyclic or bicyclic aromatic heterocycle; or (d) monocyclic or bicyclic non-aromatic heterocycle, Ring C is (a) benzene; or (b) monocyclic aromatic heterocycle, and other symbols are the same as defined in the specification.