YAO WENQING,LI HUI-YIN,SHEPARD STACEY,RODGERS JAMES D.,YE HAI FEN,HUANG TAISHENG,WANG HAISHEN,WANG ANLAI,SHAO LIXIN,LI QUN,KONG LING,XUE CHU-BIAO
申请号：
NZ60231311
公开号：
NZ602313A
申请日:
2011.03.09
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
Disclosed are 3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidine and 3-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]azetidine derivatives of formula (I), wherein X is N or CR2； Y is N or CR3； Z is H, cyano, halo, alkyl, or haloalkyl； L is C(R4)2, C(=O), C(=O)N(R4a), C(=O)C(R4b)2, S(=O)2, C(=O)O, C(=O)OC(R4b)2 or C(=O)N(R4a)C(R4b)2； A is optionally substituted alkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl； each R1 is, independently alkyl, hydroxyl, alkoxy, fluoro, hydroxyalkyl, or alkoxyalkyl； or two R1 groups together form a 2- or 3-carbon bridge or a bridge of formula -CH2-O-CH2-； and wherein the remaining substituents are as defined herein. Particularly preferred compounds include: { 1-{ 1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl} -3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl} acetonitrile, propyl 4-{ 3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-1-yl} piperidine-1-carboxylate, benzyl 4-{ 3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-1-yl} piperidine-1-carboxylate, { 1-(1-{ [6-[(isopropylamino)methyl]-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl} piperidin-4-yl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl} acetonitrile, { 1-(1-{ [6-(hydroxymethyl)-2-(trifluoromethyl)pyrimidin-4-yl]carbonyl} piperidin-4-yl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl} acetonitrile, 2,4-difluorobenzyl 4-{ 3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-1-yl} piperidine-1-carboxylate, cyclopentylmethyl 4-{ 3-(cyanomethyl)-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]azetidin-1-yl} piperidine-1-carboxylate and { 1-{ 1-[3-fluoro-2-(trifluoromethyl)isonicotinoyl]piperidin-4-yl} -3-[4-(1H-pyrrolo[2,3-b]pyridin-4-yl)-1H-pyrazol-1-yl]azetidin-3-yl} acetonitrile. Further disclosed is a composition comprising a compound or salt as defined above and a pharmaceuticall
