公开(公告)号：EP3112347A4

公开(公告)日：2017-07-05

申请号：EP15755976

申请日：2015-02-27

申请人： KISSEI PHARMACEUTICAL

发明人： INOUE HITOSHI ,  OHNO KOHSUKE ,  NAKAMURA TETSUYA ,  OHSAWA YUSUKE

IPC分类号： C07D205/04 ,  A61K31/397 ,  A61P1/04 ,  A61P27/02 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00

CPC分类号： C07D205/04

摘要： [Problem] The present invention provides a novel compound having an S1P 1 receptor antagonistic activity. [Solution] The present invention provides a compound represented by the general formula (I): (in the formula, R 1 , R 2 and R 3 are each a hydrogen atom, a halogen atom, a C 1-6 alkyl group, a halo C 1-6 alkyl group or the like, R 4 is a C 1-6 alkyl group or the like, R 5 is a C 1-6 alkyl group or the like, R 6 is a C 1-6 alkyl group or the like, R 7 is a hydrogen atom, a halogen atom, a C 1-6 alkyl group or the like, R 8 is a halogen atom, a C 1-6 alkyl group, a halo C 1-6 alkyl group, a C 1-6 alkoxy group or the like, and R 9 is a hydrogen atom or a C 1-6 alkyl group.) or a pharmaceutically acceptable salt thereof, a pharmaceutical compositions containing same, and use thereof. The compounds of the present invention have an excellent SIP 1 receptor antagonistic activitiy and therefore are useful as an agent for the treatment or prevention of antoimmune diseases and the like.

摘要翻译： [课题]本发明提供具有S1P 1受体拮抗作用的新型化合物。 本发明提供了由通式（I）表示的化合物：（式中，R 1，R 2和R 3各自为氢原子，卤素原子，C 1-6烷基， 卤代C 1-6烷基等，R 4为C 1-6烷基等，R 5为C 1-6烷基等，R 6为C 1-6烷基或 例如，R 7是氢原子，卤原子，C 1-6烷基等，R 8是卤原子，C 1-6烷基，卤代C 1-6烷基， C 1-6烷氧基等，R 9为氢原子或C 1-6烷基）或其药学上可接受的盐，含有其的药物组合物及其用途。 本发明化合物具有优异的SIP1受体拮抗活性，因此可用作治疗或预防抗免疫疾病等的药剂。

公开(公告)号：EP1679304A4

公开(公告)日：2006-11-15

申请号：EP04792252

申请日：2004-10-05

申请人： KISSEI PHARMACEUTICAL

发明人： KOBAYASHI JUNICHI ,  NAKAMURA TETSUYA ,  MURANAKA HIDEYUKI ,  ISHIKAWA TAKEHIRO ,  TAMAI TETSURO ,  AKAHANE SATOSHI

IPC分类号： C07C233/43 ,  A61K31/18 ,  A61K31/192 ,  A61K31/216 ,  A61K31/235 ,  A61K31/36 ,  A61K31/4184 ,  A61P1/14 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P13/02 ,  A61P25/24 ,  A61P43/00 ,  C07C311/08 ,  C07C311/21 ,  C07D235/24

CPC分类号： C07D235/24 ,  C07C233/43 ,  C07C311/21

摘要： A compound having potent irritative activity against a human β3-adrenergic receptor and high selectivity therefor and represented by the general formula (I) (wherein R1 is hydrogen or lower alkyl; R2 and R3 each independently is hydrogen or lower alkyl; R4, R5, and R6 each independently is hydrogen, halogeno, lower alkyl, or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogeno, lower alkyl, lower alkoxy, etc.; R9 is -COR10, -A1-COR10, -O-A2-COR10, etc.; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, -OCH2, etc.), a prodrug of the compound, or a pharmacologically acceptable salt of either.

公开(公告)号：EP1593666A4

公开(公告)日：2006-10-18

申请号：EP04706789

申请日：2004-01-30

申请人： KISSEI PHARMACEUTICAL

发明人： KOBAYASHI JUNICHI ,  NAKAMURA TETSUYA ,  SUZUKI RITSU ,  MURANAKA HIDEYUKI ,  OZAWA TOMONAGA ,  KAI YUICHIRO ,  ISHIKAWA TAKEHIRO ,  KONDO TATSUHIRO ,  TAMAI TETSURO ,  AKAHANE SATOSHI

IPC分类号： A61K31/195 ,  A61P1/00 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P13/00 ,  C07C217/14 ,  C07C217/20 ,  C07D307/79

CPC分类号： C07D307/79 ,  A61K31/195 ,  C07C217/18 ,  C07C217/20 ,  C07C323/62 ,  C07C2601/04

摘要： Compounds represented by the general formula (I) which exhibit potent stimulating activity on beta3-adrenaline receptor and high selectivity therefor, or pharmacologically acceptable salts thereof; pharmaceutical compositions containing the same; and use thereof: (I) wherein R and R are each hydrogen or lower alkyl; R , R , R , and R are each hydrogen, halogeno, lower alkyl, or lower alkoxy; R and R are each hydrogen, halogeno, lower alkyl, halo lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, hydroxyl, lower acyl, carboxyl, or the like; and R is -C(O)-R , -A -C(O)-R , -O-A -C(O)-R , or tetrazol-5-yl.

摘要翻译： 本发明提供了由通式（I）表示的化合物：或其药物上可接受的盐，worin - [R <1>和R <2>各自为氢或低级烷基; [R <3> [R <4>，R <5>和R <6>各自是氢，卤素，低级烷基或低级烷氧基; ř氢<7>和R <8>各自为卤素，低级烷基，卤代低级烷基，低级烷氧基，环烷基，芳基，杂芳基，氰基，羟基，低级酰基，羧基或类似物; [R <9>是-C（O）-R <10>，-A <1> -C（O）-R <10>，-OA <2> -C（O）-R <10>或四唑 -5-基，其显示出有效的和选择性的β3肾上腺素受体刺激活性。 本发明因此提供了包含所述化合物的药物组合物，及其用途。

公开(公告)号：EP1471049A4

公开(公告)日：2006-08-16

申请号：EP03703059

申请日：2003-01-28

申请人： KISSEI PHARMACEUTICAL

发明人： SHIOHARA HIROAKI ,  NAKAMURA TETSUYA ,  KIKUCHI NORIHIKO ,  OZAWA TOMONAGA ,  KITAZAWA MAKIO

IPC分类号： A61K31/19 ,  A61K31/22 ,  A61K31/223 ,  A61K31/225 ,  A61K31/27 ,  A61K31/341 ,  A61K31/351 ,  A61K31/40 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/50 ,  A61K31/5375 ,  A61K31/54 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10 ,  A61P5/14 ,  A61P5/16 ,  A61P9/04 ,  A61P9/06 ,  A61P9/10 ,  A61P9/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/10 ,  A61P25/24 ,  A61P27/06 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07C59/72 ,  C07C233/25 ,  C07C233/56 ,  C07C235/66 ,  C07C309/65 ,  C07C311/29 ,  C07C317/22 ,  C07C323/41 ,  C07C323/67 ,  C07D209/08 ,  C07D213/75 ,  C07D213/76 ,  C07D237/14 ,  C07D249/12 ,  C07D253/075 ,  C07D257/04 ,  C07D257/06 ,  C07D271/06 ,  C07D271/07 ,  C07D277/24 ,  C07D277/34 ,  C07D295/13 ,  C07D295/192 ,  C07D295/26 ,  C07D307/12 ,  C07D309/06 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

CPC分类号： C07D213/75 ,  A61K31/19 ,  A61K31/22 ,  A61K31/223 ,  A61K31/225 ,  A61K31/27 ,  A61K31/341 ,  A61K31/351 ,  A61K31/40 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/50 ,  A61K31/5375 ,  A61K31/54 ,  C07C59/72 ,  C07C233/25 ,  C07C233/56 ,  C07C235/66 ,  C07C309/65 ,  C07C311/29 ,  C07C317/22 ,  C07C323/41 ,  C07C323/67 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2602/08 ,  C07C2602/10 ,  C07D209/08 ,  C07D213/76 ,  C07D237/14 ,  C07D249/12 ,  C07D253/075 ,  C07D257/04 ,  C07D257/06 ,  C07D271/07 ,  C07D277/34 ,  C07D295/13 ,  C07D295/192 ,  C07D295/26 ,  C07D307/12 ,  C07D309/06 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

摘要： It is intended to provide compounds represented by the following general formula (I) which have a high affinity for human thyroid hormone receptors, in particular, human thyroid hormone receptor β, medicinal compositions containing the same, and use thereof: (I) wherein W represents O, S(O)m, CH2, etc.; R1 represents halogeno, lower alkyl, halo(lower alkyl), CN, etc.; R2 represents hydrogen, halogeno, lower alkyl, etc.; R3 represents hydroxy, etc.; R4 represents hydrogen, halogeno, alkyl, halo(lower alkyl), substituted alkyl, aryl, aralkyl, alkoxy, substituted alkoxy, alkanoyl, aroyl, -CONR7(R8), -S(O)mR9, -SO2NR7(R8), etc.; R5 represents hydrogen, halogeno, alkyl, substituted alkyl, etc.; and A represents -N(R6)CO-A1-COR10, etc.