发明名称 COMPOUNDS AS MODULATORS OF RORC
摘要 The present invention encompasses compounds of the formula (I): wherein the variables are defined herein which are suitable for the modulation of RORC and the treatment of diseases related to the modulation of RORC. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them.;
申请公布号 US2016251310(A1) 申请公布日期 2016.09.01
申请号 US201414916576 申请日期 2014.09.04
申请人 COOK Brian;HUBER John d.;HUGHES Robert Owen;KIRRANE, JR. Thomas Martin;LASOTA Celina;LI Xiang;LIANG Shuang;MUGGE Andreas;ZHANG Qiang 发明人 COOK Brian Nicholas;HUBER John D.;HUGHES Robert Owen;KIRRANE, Jr. Thomas Martin;LASOTA Celina;LI Xiang;LIANG Shuang;MUGGE Ingo Andreas;ZHANG Qiang
分类号 C07D209/96;C07D403/10;C07D401/14;C07D413/10;C07D209/08;C07D401/04;C07D403/04 主分类号 C07D209/96
代理机构 代理人
主权项 1. A compound of formula (I) R1 is: —CN, —S(O)mC1-6alkyl, —S(O)mC1-6cyanoalkyl, —S(O)mC1-6haloalkyl, —S(O)mC3-6cycloalkyl, —S(O)mC1-6 hydroxyalkyl, —S(O)mC1-6alkyloxy, —SO2NRaRb, —NRaS(O)mC1-6alkyl, —NRaS(O)mC3-6cycloalkyl, —S(O)(NRc)C1-6alkyl, —S(O)(NRc)C3-6cycloalkyl or —S(O)(NRc)NRaRb wherein Ra and Rb are each independently H, C1-6alkyl, C3-6cycloalkyl, C1-6haloalkyl, C1-6cyanoalkyl, or C1-6alkyloxy or; Ra and Rb taken together with the nitrogen to which they are attached form a C2-6 heterocyclic ring optionally containing 1-4 additional groups selected from NH, O and S; and m is 0, 1 or 2; and Rc is each independently H, C1-6alkyl, C3-6cycloalkyl, or C1-6alkyloxy; W is: C6-14 aryl, a C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, saturated and partially saturated C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, or saturated and partially saturated C3-12 cycloalkyl ring, wherein each W is optionally substituted with 0-4 substituents selected from the group consisting of cyano, halo, hydroxy, C1-6alkyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 alkenyl, C1-6 haloalkenyl, C1-6 alkynyl, C1-6 haloalkynyl, C3-6 cycloalkyl, C3-6 heterocycle containing 1-4 groups selected from NH, O and S, C1-6 alkoxy, C3-6 cycloalkyl-oxy, —S(O)mC1-6 alkyl, —S(O)mC3-6 cycloalkyl, CN, —C(O)—NRcRd, —C(O)—ORc, —NRcRd, NRcRd—C1-6alkyl-, and RcO—C1-6alkoxy NRcRd—C1-6alkoxy-, wherein Rc and Rd is each independently H, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, C3-12 cycloalkyl, C6-14 aryl, C2-6 heterocycle containing 1-4 groups selected from NH, O and S, or a C2-10heteroaryl containing 1-4 groups selected from N, NH, O and S, or Rc and Rd taken together with the nitrogen to which they are attached form a C2-6 heterocyclic ring optionally containing 1-4 additional groups selected from NH, O and S; R2 is: —C1-6alkyl, —C3-6cycloalkyl, —C1-6alkyloxy, —C1-6 hydroxyalkyl, —C1-6haloalkyl, —H, —C(O)ORe, or —C(O)NReRf, wherein Re and Rf is each independently H or C1-6 alkyl; R3 is: —C1-6alkyl, —C3-6cycloalkyl, —C1-6alkyloxy; —H, —C(O)ORe, or C(O)NReRf, wherein Re and Rf is each independently H or C1-6 alkyl; or R2 and R3 taken together with the carbon to which they are attached form a C3-12 carbocyclic ring or a C2-10 heterocyclic containing 1-4 groups selected from NH, O and S; R4 is: —H, —C1-6alkyl, —C1-6alkyloxy, or —C3-6cycloalkyl; X, Y and Z are chosen independently from CRe wherein Re is: —H, -halo, —C1-6alkyl, —C1-6 haloalkyl, —C1-6 haloalkenyl, —C1-6 haloalkynyl, —C3-6 cycloalkyl, —C1-6 alkoxy, —C3-6 cycloalkyloxy, —O C1-6alkyl, —O C3-6 cycloalkyl, —S(O)mC1-6 alkyl, —S(O)mC3-6 cycloalkyl, CN, —C(O)—NRfRg, —C(O)—ORf, or —NRfRg, wherein Rf and Rg is each independently H or —C1-6 alkyl; C1-6 alkenyl, C1-6 alkynyl, C3-12 cycloalkyl, C6-14 aryl, C3-6 heterocycle containing 1-4 groups selected from N, NH, O and S, or a C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S; R5 is: —H -halo, —C1-6 alkyl, C1-6 alkenyl, —C1-6 alkoxy, —S(O)mC1-6alkyl, —C6-14 aryl, —C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, —C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, —CN, —C3-C6cycloalkyl, or —C1-6haloalkyl, wherein R5 may be optionally substituted with 0-5 halo, C1-6 alkyl, C1-6 alkoxy, —S(O)mC1-6alkyl, C6-14 aryl, C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, or a C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, CN, C3-C6cycloalkyl, OH or —C(O)—NRaRb, R6 is: -halo, —C1-6 alkyl —C1-6 alkenyl, —C1-6 alkoxy, —S(O)mC1-6alkyl, —C6-14 aryl, —C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, —C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, —H, —CN, —C3-C6cycloalkyl, or —C1-6haloalkyl, wherein R6 may be optionally substituted with 0-5 halo, C1-6 alkyl, C1-6 alkoxy, —S(O)mC1-6alkyl, C6-14 aryl, C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, or a C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, CN, C3-C6cycloalkyl, OH or —C(O)—NRaRb, or R5 and R6 taken together with the carbon to which they attached form a C3-12 carbocyclic ring or a C2-10 heterocyclic containing 1-4 groups selected from N, NH, O and S; L is: a direct bond, —C═C— —S(O)m—, —NRaS(O)m, —S(O)mNRa— —O—, —C(O)—, —(CH2)n—, —O—(CH2)n—, —N(Ra)—, —N(Ra)—(CH2)n—, —(CH2)n—N(Ra)—, —C(O)—N(Ra)—, —C(O)—N(Ra)—(CH2)n— or —N(Ra)—C(O)—N(Rb)—; wherein Ra and Rb is each independently H or C1-3 alkyl; R7 is: halo, cycloalkyl, cycloalkenyl, —C6-14 aryl, —C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, wherein R7 may be optionally substituted with 0-5 substituents selected from the group consisting of halogen, hydroxy, C1-6alkyl, C1-6 haloalkyl, C1-6 hydroxyalkyl, C1-6 haloalkenyl, C1-6 haloalkynyl, C3-6 cycloalkyl, C3-7 heterocycle containing 1-4 groups selected from N, NH, O and S, C6-14 aryl, C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, C1-6 alkoxy, C1-6 haloalkoxy, C3-6 cycloalkyloxy, —S(O)mC1-6 alkyl, —S(O)mC3-6 cycloalkyl, CN, —C(O)—NRcRd, —C(O)—ORc, NRcRd and NRcRdC1-6alkyl-, wherein Rc and Rd is each independently H, C1-6 alkyl, C1-6 alkenyl, C1-6 alkynyl, cycloalkyl, —C6-14 aryl, C2-10 heterocyclyl containing 1-4 groups selected from N, NH, O and S, or a C2-10 heteroaryl containing 1-4 groups selected from N, NH, O and S, wherein each heterocyclyl, aryl or heteroaryl is optionally substituted by C1-6 alkyl, C1-6 alkoxy; or Rc and Rd—together with the nitrogen to which they are attached form a C2-6 heterocyclic ring optionally containing 1-4 additional groups selected from N, NH, O and S; each n is independently 1-4; each m is independently 0-2; or a pharmaceutically acceptable salt thereof.
地址 Ridgefield CT US