| 摘要 |
The invention provides certain benzoxazine compounds of the Formula (I) or pharmaceutically acceptable salts thereof wherein R1, R2, Ra1, Ra2, Rb1, Rb2, Rc, Rd, and Cy are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds of the Formula (I) or pharmaceutically acceptable salts thereof, and methods of using the compounds of the Formula (I) or pharmaceutically acceptable salts thereof or pharmaceutical compositions comprising the same for treating diseases or conditions mediated by RORgammaT.; |
| 主权项 |
1. A compound of the Formula (I) or a pharmaceutically acceptable salt thereof, wherein: R1 is H or C1-C3 alkyl, R2 is H, C1-C3 alkyl, or halo; Ra1 and Ra2 are independently H, C1-C3 alkyl, trifluoromethyl, or cyclopropyl; Rb1 and Rb2 are independently H, C1-C3 alkyl, trifluoromethyl, hydroxyl, hydroxymethyl, or cyclopropyl; alternatively:
(a.) Ra1 and Rb1 together with the carbon atoms to which they are attached form a C3-C6 cycloalkyl ring;(b.) Ra1 and Rb1 together form a second bond; or(c.) Rb1 and Rb2 together with the carbon atoms to which they are attached form a C3-C6 cycloalkyl ring; Rc is
(a.) H or(b.) C1-C6 alkyl; Rd is
(a.) C1-C8 alkyl, wherein said C1-C8 alkyl of Rd is unsubstituted or independently substituted by 1 to 6 halo, C1-C3 alkoxy, hydroxy, cyano, trimethylsilyl, or methylsulfonyl;(b.) C2-C8 alkenyl, wherein said C2-C8 alkenyl of Rd is unsubstituted or independently substituted by 1 to 6 fluoro or cyano;(c.) a group of the formula -M-RCH; M is
(i.) a bond; or(ii.) C1-C6 alkylene, wherein said C1-C6 alkylene of M is unsubstituted or substituted by 1 to 6 fluoro; RCH is a ring selected from the group consisting of
(i.) C3-C9 mono- or bicycloalkyl;(ii.) phenyl; and(iii.) a 3- to 6-membered heterocyclyl, wherein said heterocyclyl of RCH contains 1 to 2 heteroatoms independently selected from the group consisting of N, O, and S;wherein RCH is unsubstituted or independently substituted by 1 to 4 halo, C1-C3 alkyl, C1-C3 trifluoroalkyl, cyano, C1-C4 alkylcarbonylamino, or oxo; Cy is
(a.) phenyl;(b.) a 5- to 7-membered, monocyclic heterocyclyl containing 1 to 3 heteroatoms independently selected from the group consisting of N, O, and S; or(c.) C3-C6 cycloalkyl;wherein Cy is unsubstituted or independently substituted by 1 to 4 Rk moieties selected from the group consisting of:
(i.) C1-C6 alkyl, wherein said C1-C6 alkyl is unsubstituted or independently substituted by 1 to 3 hydroxy or fluoro;(ii.) C1-C6 alkoxy, wherein said C1-C6 alkoxy is unsubstituted or independently substituted by 1 to 3 fluoro, hydroxy, methoxy, or phenyl;(iii.) —N(Re)2;(iv.) —O(CH2)n1C(O)N(Re)2;(v.) —O(CH2)n2CO2Rf;(vi.) hydroxyl;(vii.) oxo;(viii.) halo;(ix.) C1-C3 alkylsulfonyl;(x.) cyano;(xi.) oxetanyl;(xii.) cyclopropyl; and(xiii.) —SF5;or alternatively, two Rk moieties, when substituted on adjacent ring atoms of Cy, form a second ring, wherein said second ring is 5- to 7-membered saturated, partially saturated, or aromatic ring system that contains 0, 1, or 2 heteroatoms independently selected from the group consisting of N, O, and S; wherein said second ring is unsubstituted or substituted by 1 to 3 Rk moieties independently selected from (i)-(xii); each Re is independently H or C1-C3 alkyl, Rf is H or C1-C3 alkyl; the subscript n1 is 1, 2, or 3; and the subscript n2 is 1, 2, or 3. |
