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1h pyrrolo [2,3-c] pyridin-3 (6H) - 7 - onas and pyrazolo [3,4-c] pyridin-3 (6H) - 7 - onas as inhibitors of Protein Bet
专利权人:
INCYTE CORPORATION
发明人:
ANDREW P. COMBS,THOMAS P. MADUSKUIE,NIKKO FALAHATPISHEH
申请号:
ARP150101214
公开号:
AR100160A1
申请日:
2015.04.22
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
At present, they are related to substituted pyridine and substituted pyridine. They constitute B protein inhibitors such as BRD2, Bd3, bd4 and brd-t, which are helpful for the treatment of cancer and other diseases. 1. Claim 1: a formula compound (1),O select a medically acceptable salt from this product with the following characteristics: x = C = or cr831222; r8313;This is O, s, or nr.83044;Z is CH or N; each of R¹ and R² are independently selected from H, halo, C₁₋₆ alkyl,C₂₋₆ alkenyl,1. C 83228331 asphalt;C₁₋₆ haloalkyl,Cy1,CN ORSRᵃ¹,C (O) RC (O) NR RC (O) OROC (O) ROC (O) NR RNR RNo. 7580;; 1 C (o) r7495;; 1No. 7580; 1 C (o) or7491; 1,NR C (O) NR RC (3DNR) RC (3DNR) NR RNR C (3DNR) NR RNR S (O) RNR S (O) RNR S (O) NR RS (O) RS (O) NR RS (O) Ry S (O) NR Rwhere each of said C₁₋₆ alkyl,C₂₋₆ alkenyl,and C₂₋₆ alkynyl are optionally substituted with 1, 2, 3, 4, or 5 substituents independently selected from RA; or R¹ and R² together with the carbon atom to which they are attached form a C₃₋₁₀ cycloalkyl group or a 4-10 membered heterocycloalkyl group, each optionally substituted with 1, 2 or 3 substituents independently selected from RA; R³ is H or C₁₋₆ alkyl optionally substituted with 1, 2 or 3 substituents independently selected from halo, Cy, CN, NO₂,Or7491.,7491;C (O) RC (o) No. 758080; R 7496;]C (O) OROC (O) ROC (O) NR RC (3DNR) NR RNR C (3DNR) NR R7580; 749696;No. 7580; - No. 7495;No. 7580; C (o) 7491; 22. No. 7580; 2 C (o) No. 7580; 2No. 7580; No. 7495;Nr7580802 km2 (o) 83222; r74955 km2,NR S (O) NR RS (O) RS (o) No. 7580; R 7496;]S (o) 8322; r74952 and S (o) 8322; nr7580; r74962;R es H halo alquilo CC₂₋₄ alkenyl,1. C 83228331 asphalt;C₁₋₄ haloalkyl,CN ORSRᵃ³,C (O) RC (O) NRᶜ³Rᵈ³,C (O) OROC (O) ROC (O) NR RNR RNR C (O) RNo. 7580; 3 C (o) or7491; 3,No. 7580; + C (o) 7580; + r749696; + 3C (= No. 749773; 3) r74955; 3C (= No. 749773; 3) No. 7580; 3 r749696; 3NR C (3DNR) NR RNR S (O) RNR S (O) RNR S (O) NR RS (O) RS (o) No. 7580; 3 r749696; 3S (O) Ro S (O) NR RR es
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