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Tricyclic FUSED thiophene derivatives as inhibitors of Jak
专利权人:
INCYTE CORPORATION
发明人:
申请号:
ARP130103980
公开号:
AR093308A1
申请日:
2013.10.31
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
These compounds modulate the activity of Janus Kinase (JAK) and are useful for the treatment of diseases associated with the activity of jak including, for example, inflammatory disorders, autoimmune disorders, cancer and other diseases.Claim 1: a compound of the formula (1) or a pharmaceutically acceptable Salt of this, where the Ring System of the formula (2) is Aromatic; each u207b u207b u207b is selected regardless of a Single Bond and a double Bond; and is n o cr u2074; x u00b9 is selected cr u00b9, cr u00b9r u00b9 u1d43, C (= o), N, o and S nr u00b9,; X is selected from cr u00b2, C (= o), N,Nr u00b2 and C (= nr u00b2 u1d43); X is selected from cr u00b3 and nr u00b3 x u2074 is selected; c and N; and x u2075 is c or C; x u2074 is selected; and x u2075 C and N; provided that: (i) the selections for each of x u00b9, X, X, x u2074, x u2075 and u207b u207b Valencia u207b maintain adequate; (ii) when x u00b9 is o or s, X is not Nr u00b2 and x u00b2 u207b u207b u207bx u00b3 is not - C (= o) - cr u00b3 -; (iii) when x u00b9 is nr u00b9, x u00b2 u207b u207b u207bx u00b3 is not - - - nr u00b2 nr u00b3; (iv) when x u2074 is n,X u00b9 u207b u207b u207bx u00b2 u207b u207b u207bx u00b3 is not nr u00b2 nr u00b3 = N - - -; and (V) when x u2075 is n, x u00b9 u207b u207b u207bx u00b2 is not - - - and nr u00b9 nr u00b2 x u00b9 u207b u207b u207bx u00b2 u207b u207b u207bx u00b3 is not - - - cr u00b9r u00b9 u1d43 nr u00b2 cr u00b3 =; r u00b9 is selected from h, Halo, CN, nh u2082, alkyl c u2081 u208b u2083 c u2081 u208b u2083, alkoxy and haloalquilo c u2081 u208b u2083 r u00b9 u1d43 is selected; One of nh u2082 h, alkyl, Halo, CN, and c u2081 u208b u2083 haloalquilo c u2081 u208b u2083; r u00b2 u1d43 Selects CN, Oh, och u2083 and no u2082; R u00b2 is selected from h, alkyl, Halo, c u2081 u208b u2086, alquenilo c u2082 u208b u2086, alquinilo c u2082 u208b u2086,Haloalquilo c u2081 u208b u2086 c u2081 u208b u2086 alkyl, alkoxy, CN, c u2081 u208b u2086 - S - C (= o
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