发明名称 COMPOUNDS AS MODULATORS OF ROR GAMMA
摘要 The present invention encompasses compounds of the formula (I);;wherein the variables are defined herein which are suitable for the modulation of RORγ and the treatment of diseases related to the modulation of RORγ. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.
申请公布号 US2015291607(A1) 申请公布日期 2015.10.15
申请号 US201514683682 申请日期 2015.04.10
申请人 Boehringer Ingelheim International GmbH 发明人 BAKONYI Johanna;BRUNETTE Steven Richard;COLLIN Delphine;HUGHES Robert Owen;LI Xiang;LIANG Shuang;SIBLEY Robert;TURNER Michael Robert;WU Lifen;ZHANG Qiang
分类号 C07D487/04 主分类号 C07D487/04
代理机构 代理人
主权项 1. A compound of formula (I) wherein: R1 is: —CN;—S(O)nR6;—S(O)nNR7R8;—S(O)(NR9)R6;—N(R9)C(O)R6;—N(R9)C(O)OR6;—N(R9)S(O)nR6;—C(O)OR9;—C(O)NR7R8; or—C(O)R9; or R6, R7, R8 or R9 of R1 may be cyclized onto W to form a ring; and R2 and R3 are each independently: (A) —H;(B) C1-3 alkyl optionally substituted with one, two or three groups selected from: a) C3-6 cycloalkyl;b) —OR9;c) —CN;d) —CF3;e) -halo;f) —C(O)OR9;g) —C(O)N(R9)2;h) —S(O)nR9; andi) —S(O)nNR7R8; or(C) C3-6 cycloalkyl;(D) C3-6 heterocyclyl; orR2 and R3 are taken together with the carbon to which they are attached to form a C3-6 carbocyclic ring; orR2 and R3 are taken together with the carbon to which they are attached to form a C3-6 heterocyclic ring; orR2 or R3 may be cyclized onto W to form a ring;R4 is:(A) C1-6 alkyl optionally substituted with one, two or three groups selected from: a) C3-6 cycloalkyl;b) C3-6 heterocyclyl;c) —OR9;d) —CN;e) —S(O)nR9;f) -halo; andg) —CF3; or(B) C3-12 cycloalkyl optionally substituted with one, two or three groups selected from: a) C1-6 alkyl;b) —OR9;c) —CN;d) —S(O)nR9;e) -halo; andf) —CF3; or(C) aryl, heteroaryl or heterocyclyl each optionally substituted with one, two or three groups selected from: a) C1-6 alkyl;b) C3-6cycloalkyl;c) —OR9;d) —CN;e) —S(O)nR9;f) -halo; andg) —CF3;R5 is aryl, heteroaryl, heterocyclyl or C3-12 cycloalkyl each optionally substituted with one, two or three groups selected from:(A) C1-6 alkyl, C3-6 cycloalkyl or C3-6 heterocyclyl each optionally substituted with one, two or three groups selected from: a) C3-6 cycloalkyl;b) C3-6 heterocyclyl;c) —OR9;d) —CN;e) —S(O)nNR7R8 f) —S(O)nR9;g) -halo; andh) —CF3; or(B) —OR9;(C) —CN;(D) —CF3;(E) -halo;(F) —S(O)nNR7R8;(G) —S(O)nR9; and(H) —NR7R8;W is aryl, heteroaryl, heterocyclyl, C3-12 cycloalkyl, or alkynyl each optionally substituted with one or two groups selected from: a) C1-6 alkyl;b) C3-6 cycloalkyl;c) —OR9;d) —CN;e) —CF3;f) -halo;g) —NR7R8;h) —C(O)OR9; andi) —C(O)N(R9)2;R6 is selected from:(A) —OH;(B) C1-6 alkyl optionally substituted with one or two groups selected from: a) C3-6cycloalkyl;b) —OR9;c) —CN;d) —CF3; ande) -halo;(C) C3-6 cycloalkyl; and(D) —CF3;R7 and R8 are independently selected from:(A) —H;(B) C1-3 alkyl optionally substituted with one or two groups selected from: a) C3-6cycloalkyl;b) —OR9;c) —CN; andd) -halo; and(C) C3-6cycloalkyl; orR7 and R8, together with the nitrogen to which they are bonded, form a saturated ring with 3-6 carbon atoms wherein one carbon atom in said saturated ring may be optionally replaced by —O—, —NR9—or —S(O)n—;R9 is selected from;(A) —H;(B) C1-3 alkyl optionally substituted with one or two groups selected from: a) C3-6cycloalkyl;b) —OR9;c) —CN;d) —CF3 e) -halo; or(C) C3-6cycloalkyl; andn is 0, 1 or 2;or a pharmaceutically acceptable salt thereof.
地址 Ingelheim am Rhein DE