公开(公告)号：US09156837B2

公开(公告)日：2015-10-13

申请号：US14235992

申请日：2012-07-27

申请人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

发明人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

IPC分类号： C07D277/30 ,  C07D277/56 ,  C07D211/90 ,  C07D417/12 ,  C07D471/04 ,  C07D401/12 ,  C07D277/24 ,  C07D401/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

CPC分类号： C07D471/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

摘要： A heterocyclic compound having an RORγt inhibitory activity, which is a compound of formula (I) or a salt thereof is provided. The compound has ring A, which is an optionally substituted cyclic group and is bound to a pyrazole ring though Q. Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene. R1 is a substituent. Ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2. R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group.

摘要翻译： 提供具有RORγt抑制活性的杂环化合物，其为式（I）化合物或其盐。 该化合物具有环A，其为任选取代的环状基团，并且通过Q键合至吡唑环。Q为键，任选取代的C 1-10亚烷基，任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基。 R1是取代基。 环B是噻唑环，异噻唑环或二氢噻唑环，除了R2之外，它们各自任选进一步被取代基取代。 R 2是任选取代的环羰基-C 1-6烷基，任选取代的氨基羰基-C 1-6烷基，任选取代的环C 1-6烷基，任选取代的环C 1-6烷基氨基羰基， 任选取代的氨基羰基-C 2-6烯基，任选取代的C 1-6烷基羰基氨基-C 1-6烷基，任选取代的环 - 氨基羰基，任选取代的环羰基或任选取代的非芳族杂环基。

公开(公告)号：US20140163001A1

公开(公告)日：2014-06-12

申请号：US14235992

申请日：2012-07-27

申请人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

发明人： Satoshi Yamamoto ,  Junya Shirai ,  Atsuko Ochida ,  Yoshiyuki Fukase ,  Yoshihide Tomata ,  Ayumu Sato ,  Shotaro Miura ,  Kazuko Yonemori ,  Ryokichi Koyama

IPC分类号： C07D491/107 ,  C07D417/04 ,  C07D471/04 ,  C07D417/14

CPC分类号： C07D471/04 ,  C07D417/04 ,  C07D417/14 ,  C07D491/107

摘要： Provided is a heterocyclic compound having an RORγt inhibitory activity. A compound represented by the formula (I): wherein ring A is an optionally substituted cyclic group, Q is a bond, optionally substituted C1-10 alkylene, optionally substituted C2-10 alkenylene, or optionally substituted C2-10 alkynylene, R1 is a substituent, ring B is a thiazole ring, an isothiazole ring or a dihydrothiazole ring, each of which is optionally further substituted by a substituent in addition to R2, and R2 is an optionally substituted cyclyl-carbonyl-C1-6 alkyl group, an optionally substituted aminocarbonyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkyl group, an optionally substituted cyclyl-C1-6 alkylamino-carbonyl group, an optionally substituted aminocarbonyl-C2-6 alkenyl group, an optionally substituted C1-6 alkylcarbonylamino-C1-6 alkyl group, an optionally substituted cyclyl-aminocarbonyl group, an optionally substituted cyclyl-carbonyl group or an optionally substituted non-aromatic heterocyclic group, or a salt thereof.

摘要翻译： 提供具有RORγt抑制活性的杂环化合物。 由式（I）表示的化合物：其中环A是任选取代的环状基团，Q是键，任选取代的C 1-10亚烷基，任选取代的C 2-10亚烯基或任选取代的C 2-10亚炔基，R 1是 取代基，环B是噻唑环，异噻唑环或二氢噻唑环，其中R 2独立地任选被取代基任意地进一步被R 2取代，R 2是任选取代的环羰基-C 1-6烷基，任选地 取代的氨基羰基-C 1-6烷基，任选取代的环烷基-C 1-6烷基，任选取代的环基-C 1-6烷基氨基 - 羰基，任选取代的氨基羰基-C 2-6链烯基，任选取代的C 1-6 烷基羰基氨基-C 1-6烷基，任选取代的环 - 氨基羰基，任选取代的环羰基或任选取代的非芳族杂环基，或其盐。