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Piperidin-4-yl azetidine derivatives as JAK1 inhibitors
专利权人:
INCYTE HOLDINGS CORP;Incyte Holdings Corporation
发明人:
HUANG, Taisheng,XUE, Chu-Biao,WANG, Anlai,KONG, Ling,YE, Hai Fen,YAO, Wenqing,RODGERS, James D.,SHEPARD, Stacey,WANG, Haisheng,SHAO, Lixin,LI, Hui-Yin,LI, Qun,HUANG TAISHENG,XUE CHU-BIAO,WANG ANLAI,KONG LING,YE HAI FEN,YAO WENQING,RODGERS JAMES D,SHEPARD STACEY,WANG HAISHENG,SHAO LIXIN,LI HUI-YIN,LI QUN
申请号:
ES11711709
公开号:
ES2569539T3
申请日:
2011.03.09
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
a compound of Formula (I): ** Formula ** or a pharmaceutically acceptable salt thereof; where: X is N or CR2; Y is N or CR3; Z is H, cyano, halo, C1-3 alkyl or C1-3 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 OC (>; = O) N (R4a) C (R4b) 2); A is C1-6 alkyl, C3-14 cycloalkyl, C2-13 heterocycloalkyl, C6-14 aryl or C1-14 heteroaryl; wherein said C1-6 alkyl, C3-14 cycloalkyl, C2-13 heterocycloalkyl, C6-14 aryl and C1-14 heteroaryl are substituted individually and optionally by 1, 2, 3, 4, 5 or 6 independently selected R5 groups; or each R1 is independently C1-4 alkyl, hydroxyl, C1-4 alkoxy, fluorine, hydroxy-C1-4 alkyl or C1-4 alkoxy-C1-4 alkyl; two R1 groups together form a 2-3-carbon bridge or a bridge of formula -CH2-O-CH2; R2 is H, halo, hydroxyl, cyano, C1-4 alkyl, C1-4 haloalkoxy or C1-4 alkoxy; R3 is H, cyano, amino, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C1-6 haloalkyl, C1-6 alkoxy, C1-6 haloalkoxy, amino, C1-6 alkylamino, di-C1-6-alkylamino, C1-6 alkylsulfonyl, carbamyl, C1-6 alkylcarbamyl, di-C1-6 alkylcarbamyl, caboxi, C1-6 alkylcarbonyl or C1-6 alkoxycarbonyl; each R4 is independently H or C1-4 alkyl; or two R4 groups together with the carbon atom to which they are attached form a cycloaqluyl ring with 3, 4, 5 or 6 members; R4a is H or C1-4 alkyl; each R4b is independently H or C1-4 alkyl; or two R4b groups, together with the carbon atom to which they are attached, forms a cycloakyl ring with 3, 4, 5 or 6 members; Each R5 is independently halo, cyano, nitro, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-6 haloalkyl, halosulfanyl, C3-10 cycloalkyl, C3-10 cycloalkyl-C1-3 alkyl, C2 -10 heterocycloalkyl, C2-10 heteroaryl-C1-3 alkyl, C6-10 aryl, C6-10 aryl-C3-10 alkyl, C1-10 heteroaryl, C1-10 heteroaryl-C1-3 alkyl, ORa, SRa, C ( O) Rb, C (O) NRcRd, C (O) ORa, OC (O) Rb, OC (O) NRcRd, NRcRd, NRcC (O) Rb, NRcC (O) ORa, NRcC (O) NRcRd, C ( >; = NRe) R
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