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Inhibitors of F1F0-ATPases of pyrazolylguanidine type and their therapeutic uses
专利权人:
LYCERA CORP;Lycera Corporation
发明人:
GLICK, Gary D.,HURD, Alexander R.,TAYLOR, Clarke B.,VANHUIS, Chad A.,GLICK GARY D,GLICK, GARY D.,HURD ALEXANDER R,HURD, ALEXANDER R.,TAYLOR CLARKE B,TAYLOR, CLARKE B.,VANHUIS CHAD A,VANHUIS, CHAD A.
申请号:
ES11846595
公开号:
ES2639439T3
申请日:
2011.12.08
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound represented by Formula I: ** Formula ** including all stereoisomers, geometric isomers and tautomers; or a pharmaceutically acceptable salt or solvate of any of the foregoing; where: A1 is phenylene or a six-membered heteroarylene; ** Formula ** R1 independently represents each time halogen, haloalkyl, alkyl, cycloalkyl, heterocycloalkyl, hydroxyl, C1-C6 alkoxy, cyano, -CO2R8, -C (O ) R9, -S (O) R9, -SO2R9, -SO2N (R10) (R11), -C (O) N (R10) (R11), -N (R10) (R11) or -N (R8) C (O) (R9); R2 is hydrogen or alkyl; R3 is aryl, aralkyl, cycloalkyl, - (C (R8) 2) m-cycloalkyl, heteroaryl, heteroaralkyl, heterocycloalkyl, - (C (R8) 2) mheterocycloalkyl, alkyl, haloalkyl, hydroxyalkyl, - (C (R8) 2) m-alkoxy, - (C (R8) 2) mO- (C (R8) 2) m-alkoxy or - (C (R8) 2) m-CN, wherein said aryl, aralkyl, cycloalkyl, heteroaryl, heteroaralkyl and heterocycloalkyl are each optionally substituted with 1, 2, or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl, hydroxyalkyl, C1-C6 alkoxy, cyano and C1-C6-CO2R8 alkylene ; R4 is hydrogen, alkyl or -C (O) R9; or R3 and R4 are considered together with the nitrogen atom to which they are attached to form a 3- to 7-membered heterocyclic ring optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of halogen, haloalkyl, hydroxyl, alkyl, cycloalkyl and C1-C6 alkoxy; R5 is hydrogen or alkyl; R6 is haloalkyl; R7 is hydrogen, halogen, alkyl or haloalkyl; R8 independently represents each time hydrogen, alkyl or cycloalkyl appears; or, when R8 appears twice bound to the same carbon atom, both occurrences are considered together with said carbon atom to form a saturated carbocyclic ring; R9 represents independently each time alkyl or cycloalkyl appears; R10 and R11 each independently represent each time hydrogen, alkyl or cycloalkyl appear; or R10 and R11 are considered in conjunction with the nitrogen atom to which they are attached to
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