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Indolamine 2,3-dioxygenase modulators, and methods of use thereof
专利权人:
INCYTE HOLDINGS CORP;Incyte Holdings Corporation
发明人:
Combs, Andrew P.,Yue, Eddy W.,COMBS ANDREW P,COMBS, ANDREW P.,YUE EDDY W,YUE, EDDY W.
申请号:
ES12178315
公开号:
ES2578404T3
申请日:
2006.05.09
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of Formula: ** Formula ** or a pharmaceutically acceptable salt thereof, for use in the treatment of cancer in combination with an anti-PD-1 antibody, in which: W, X1 and X2 are independently selected from (CRaRb) t, (CRaRb) uO (CRaRb) v, (CRaRb) uC (O) (CRaRb) v, (CRaRb) uC (O) NRc (CRaRb) v, (CRaRb) uC (O) O (CRaRb) v, (CRaRb) uC (S) (CRaRb) u, (CRaRb) uC (S) NRc (CRaRb) v, (CRaRb) uS (O) (CRaRb) v, (CRaRb) uS (O) NRc (CRaRb) v, (CRaRb) uS (O) 2 (CRaRb) v, (CRaRb) uS (O) 2NRc (CRaRb) v, (CRaRb) uNRc (CRaRb) v, and (CRaRb) uC (>; = NRd) NRc (CRaRb ) v; R2 is H, C1-6 alkyl, or C3-7 cycloalkyl; R3a and R5a are independently selected from C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, cycloalkyl, heteroaryl and heterocycloalkyl, each optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 haloalkyl, Cy1, CN, NO2, ORe1, SRe1, C (O) Rf1, C (O) NRg1Rh1, C (O) ORe1, OC ( O) Rf1, OC (O) NRg1Rh1, NRg1C (O) NRg1Rh1, NRg1Rh1, NRg1C (O) Rf1, NRg1C (O) ORe1, C (>; = NRi) NRg1Rb1, NRg1C (>; = NR ') NRg1Rb1, P (Rfl ) 2, P (ORe1) 2, P (O) Re1Rf1, P (O) ORe1ORf1, S (O) Rf1, S (O) NRg1Rb1, S (O) 2Rf1, and S (O) 2NRg1Rh1; R3b is aryl or heteroaryl each optionally substituted with 1, 2, 3, 4 or 5 substituents independently selected from halo, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, Cy2, CN, NO2, ORe1, SRe1, C (O) Rf1, C (O) NRg1Rh1, C (O) ORe1, OC (O) Rf1, OC (O) NRg1Rh1, NRg1C (O) NRg1Rh1, NRg1Rh1, NRg1C ( O) Rf1, NRg1C (O) ORe1, C (>; = NRi) NRg1Rh1, NRg1C (>; = NRi) NRg1Rh1, P (Rf1) 2, P (ORe1) 2, P (O) Re1Rf1, P (O) ORe1ORf1, S (O) Rf1, S (O) NRg1Rh1, S (O) 2Rf1, and S (O) 2NRg1Rh1; R5b is H, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl wherein said C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, aryl, cycloalkyl, heteroaryl, or heterocycloalkyl is each optionally substituted by 1, 2, 3, 4 or 5 substituents inde
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