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Protease peptidomimetic inhibitors
专利权人:
VERTEX PHARMACEUTICALS INCORPORATED
发明人:
BABINE, ROBERT EDWARD,CHEN, SHU-HUI,LAMAR, JASON ERIC,SNYDER, NANCY JUNE,SUN, XICHENG,TEBBE, MARK JOSEPH,VICTOR, FRANTZ,WANG, MAY Q.,YIP, MAI YEE YVONNE,COLLADO, IVAN,GARCIA-PAREDES, CRISTINA,PARKER,
申请号:
ES07012483
公开号:
ES2450815T3
申请日:
2001.08.31
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound of formula 1 ** Formula ** or a pharmaceutically acceptable salt thereof, or a solvate of such a compound, or its salt, wherein: R0 is a bond or difluoromethylene; R1 is hydrogen, optionally substituted aliphatic group, optionally substituted cyclic group or optionally substituted aromatic group; R2 and R9 are each independently an optionally substituted aliphatic group, optionally substituted cyclic group or optionally substituted aromatic group; R3 and R5 are each independently an optionally substituted lower aliphatic group methylene and R7 is optionally substituted lower aliphatic group methylene, optionally substituted lower cyclic group methylene or optionally substituted monocyclic (aryl or heteroaryl) methylene; each of R4, R6, R8 and R10 is independently hydrogen or optionally substituted aliphatic group; it is a substituted monocyclic azaheterocyclyl, in which the monocyclic azaheterocyclyl group is substituted through a linking group by at least one substituent selected from aryl, heteroaryl, aryloxy, heteroaryloxy, aroyl or its thioxo analog, heteroaroyl or its thioxo analog, aroyloxy, heteroaroyloxy, aryloxycarbonyl, heteroaryloxycarbonyl, arylsulfonyl, heteroarylsulfonyl, arylsulfinyl, heteroarylsulfinyl, arylthio, heteroarylthio, aryldiazo, heteroaryldiazo, Y1Y2N-, Y1Y2NC (O) -, Y1Y2NC (O) Y2 O2 Y1 O2 O2 Y1 O2 Y2 O2 Y1 O2 O2 Y1, Y2 and Y3 are independently hydrogen, alkyl, aryl or heteroaryl, and Y3 is alkyl, cycloalkyl aryl or heteroaryl, or when the substituent is Y1Y2N-, then one of Y1 and Y2 can be acyl, cyclocarbonyl, aroyl, heteroaroyl, alkoxycarbonyl, cycloyloxycarbonyl , aryloxycarbonyl or heteroaryloxycarbonyl, as herein and the other of Y1 and Y2 is as previously defined, or when the substituent is Y1Y2NC (O) -, Y1Y2NC (O) O-, Y1Y2NC (O) NY3- or Y1Y2NSO2-, Y1 and Y2 can also be taken together with the N atom through which Y1e Y2 is joined to form a 4- to 7-membered azaheterocyclyl or azaheterocyclyl; and at least one of Y1 and Y2
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