公开(公告)号：US20110098480A1

公开(公告)日：2011-04-28

申请号：US12937986

申请日：2009-04-15

申请人： Shogo Sakuma ,  Rie Takahashi ,  Hideki Nakamura

发明人： Shogo Sakuma ,  Rie Takahashi ,  Hideki Nakamura

IPC分类号： C07D413/02 ,  C07D333/56

CPC分类号： C07D333/56 ,  C07D333/58 ,  C07D413/06

摘要： A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR. wherein each of R1 and R2 is hydrogen, C1-8 alkyl, C1-8 alkyl substituted with halogen, or the like; each of R3, R4, R5, and R6 is hydrogen, C1-8 alkyl, or the like; X is sulfur or the like; Y is oxygen, a bond, or the like; p is 0 or 1; A is oxygen, CH2, N—NH2, or the like; when p is 1, B is phenyl, which can have a substituent; when p is 0, B is a condensed ring such as benzisoxazole, which can have a substituent; m is an integer of 1 to 4; and n is an integer of 0 to 5.

摘要翻译： 使用由式（I）表示的化合物或其药理学上可接受的盐作为PPAR的活化剂。 其中R 1和R 2各自为氢，C 1-8烷基，被卤素取代的C 1-8烷基等; R 3，R 4，R 5和R 6各自为氢，C 1-8烷基等; X是硫等; Y是氧，键或类似物; p为0或1; A是氧，CH 2，N-NH 2等; 当p为1时，B为可具有取代基的苯基; 当p为0时，B为可以具有取代基的苯并异恶唑等稠环; m为1〜4的整数。 n为0〜5的整数。

公开(公告)号：US08648208B2

公开(公告)日：2014-02-11

申请号：US12937986

申请日：2009-04-15

申请人： Shogo Sakuma ,  Rie Takahashi ,  Hideki Nakamura

发明人： Shogo Sakuma ,  Rie Takahashi ,  Hideki Nakamura

IPC分类号： C07D209/12 ,  C07D209/18 ,  A61K31/405

CPC分类号： C07D333/56 ,  C07D333/58 ,  C07D413/06

摘要： A compound represented by the formula (I) or a pharmacologically acceptable salt thereof is used as an activator of PPAR wherein each of R1 and R2 is hydrogen, C1-8 alkyl, C1-8 alkyl substituted with halogen, or the like; each of R3, R4, R5, and R6 is hydrogen, C1-8 alkyl, or the like; X is sulfur or the like; Y is oxygen, a bond, or the like; p is 0 or 1; A is oxygen, CH2, N—NH2, or the like; when p is 1, B is phenyl, which can have a substituent; when p is 0, B is a condensed ring such as benzisoxazole, which can have a substituent; m is an integer of 1 to 4; and n is an integer of 0 to 5.

摘要翻译： 使用由式（I）表示的化合物或其药学上可接受的盐作为PPAR的活化剂，其中R 1和R 2各自为氢，C 1-8烷基，被卤素取代的C 1-8烷基等; R 3，R 4，R 5和R 6各自为氢，C 1-8烷基等; X是硫等; Y是氧，键或类似物; p为0或1; A是氧，CH 2，N-NH 2等; 当p为1时，B为可具有取代基的苯基; 当p为0时，B为可以具有取代基的苯并异恶唑等稠环; m为1〜4的整数。 n为0〜5的整数。

公开(公告)号：US20090203908A1

公开(公告)日：2009-08-13

申请号：US11920940

申请日：2006-05-24

申请人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Toshitake Hirai ,  Tomio Yamakawa ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Toshitake Hirai ,  Tomio Yamakawa ,  Seiichiro Masui

IPC分类号： C07D417/06

CPC分类号： C07D277/28

摘要： A compound having the following formula or its salt is used as an activator for PPAR: in which W2 represents a bond, C(═O) or CH2; Z2 represents an oxygen or sulfur atom; R21, R22 and R23 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, a halogen atom, an alkyl group having 1 to 8 carbon atoms which is substituted with a halogen atom or the like; and R24 and R25 independently represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms or an alkyl group having 1 to 8 carbon atoms which is substituted with a halogen atom.

摘要翻译： 具有下式的化合物或其盐用作PPAR的活化剂：其中W 2表示键，C（-O）或CH 2; Z2表示氧或硫原子; R 21，R 22和R 23独立地表示氢原子，碳原子数1〜8的烷基，碳原子数1〜8的烷氧基，卤原子，碳原子数1〜8的被卤素取代的烷基 原子等; R 24和R 25独立地表示氢原子，碳原子数1〜8的烷基或碳原子数1〜8的被卤素原子取代的烷基。

公开(公告)号：US20130217734A1

公开(公告)日：2013-08-22

申请号：US13765540

申请日：2013-02-12

申请人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Masatoshi Ushioda ,  Tomio Yamakawa ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Masatoshi Ushioda ,  Tomio Yamakawa ,  Seiichiro Masui

IPC分类号： C07D277/22

CPC分类号： C07D277/22 ,  C07D263/32 ,  C07D277/20 ,  C07D277/30 ,  C07D333/22

摘要： A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.

公开(公告)号：US20100029949A1

公开(公告)日：2010-02-04

申请号：US11988354

申请日：2006-07-04

申请人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Toshitake Hirai ,  Tomio Yamakawa ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Toshitake Hirai ,  Tomio Yamakawa ,  Seiichiro Masui

IPC分类号： C07D413/14 ,  C07D261/20

CPC分类号： C07D413/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/14 ,  C07D417/06

摘要： A compound having the following formula (II) or its salt is used as an activator for PPAR δ: [in which W3 is a nitrogen atom or CH; Z1 is an oxygen atom or a sulfur atom; each of R11 and R12 is a hydrogen atom, a halogen atom, a C1-C8 alkyl group, a C1-C8 alkoxy group, a C1-C8 alkyl group having a halogen substituent, or the like; each of R13 and R14 is a hydrogen atom or a C1-C8 alkyl group; A1 is pyrazole or thiophene which may have a substituent; and m is an integer of 2 to 4].

摘要翻译： 使用具有下式（II）或其盐的化合物作为PPARδ的活化剂：[其中W3是氮原子或CH; Z1是氧原子或硫原子; R 11和R 12各自为氢原子，卤素原子，C1-C8烷基，C1-C8烷氧基，具有卤素取代基的C1-C8烷基等; R 13和R 14各自为氢原子或C 1 -C 8烷基; A1是可以具有取代基的吡唑或噻吩; m为2〜4的整数]。

公开(公告)号：US08404726B2

公开(公告)日：2013-03-26

申请号：US12297436

申请日：2007-04-18

申请人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Masatoshi Ushioda ,  Tomio Yamakawa ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Masatoshi Ushioda ,  Tomio Yamakawa ,  Seiichiro Masui

IPC分类号： A61K31/426 ,  C07D277/30 ,  A61P3/00 ,  A61P9/10

CPC分类号： C07D277/22 ,  C07D263/32 ,  C07D277/20 ,  C07D277/30 ,  C07D333/22

摘要： A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.

摘要翻译： 使用由以下通式（II）表示的化合物或其盐作为PPARδ的活化剂。 其中Ga是O，CH 2等; Aa是噻唑，恶唑或噻吩，其可以具有取代基，例如C 1-8烷基，C 1-8烷氧基，卤素，被卤素取代的C 1-8烷基等; Ba是C 1-8亚烷基或C 2-8亚烯基链; R 1a和R 2a各自独立地为氢，C 1-8烷基，C 1-8烷氧基，卤素，被卤素等取代的C 1-8烷基。

公开(公告)号：US20090298896A1

公开(公告)日：2009-12-03

申请号：US12297436

申请日：2007-04-18

申请人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Masatoshi Ushioda ,  Tomio Yamakawa ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Nobutaka Mochiduki ,  Rie Takahashi ,  Masatoshi Ushioda ,  Tomio Yamakawa ,  Seiichiro Masui

IPC分类号： A61K31/426 ,  C07D277/30 ,  A61P3/00 ,  A61P9/10

CPC分类号： C07D277/22 ,  C07D263/32 ,  C07D277/20 ,  C07D277/30 ,  C07D333/22

摘要： A compound represented by the following general formula (II) or a salt thereof is used as an activator of PPARδ. wherein Ga is O, CH2 or the like; Aa is thiazole, oxazole, or thiophene, which can have a substituent such as C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like; Ba is a C1-8 alkylene or C2-8 alkenylene chain; and each of R1a and R2a independently is hydrogen, C1-8 alkyl, C1-8 alkoxy, halogen, C1-8 alkyl substituted with halogen or the like.

摘要翻译： 使用由以下通式（II）表示的化合物或其盐作为PPARδ的活化剂。 其中Ga是O，CH 2等; Aa是噻唑，恶唑或噻吩，其可以具有取代基，例如C 1-8烷基，C 1-8烷氧基，卤素，被卤素取代的C 1-8烷基等; Ba是C 1-8亚烷基或C 2-8亚烯基链; R 1a和R 2a各自独立地为氢，C 1-8烷基，C 1-8烷氧基，卤素，被卤素等取代的C 1-8烷基。

公开(公告)号：US20090240058A1

公开(公告)日：2009-09-24

申请号：US11885265

申请日：2006-02-28

申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Nobutaka Mochiduki ,  Seiichiro Masui ,  Rie Takahashi ,  Toshitake Hirai

发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Nobutaka Mochiduki ,  Seiichiro Masui ,  Rie Takahashi ,  Toshitake Hirai

IPC分类号： C07D401/02 ,  C07D231/12 ,  C07D333/24

CPC分类号： C07D231/12 ,  C07D207/325 ,  C07D207/333 ,  C07D231/22 ,  C07D307/42 ,  C07D307/46 ,  C07D333/16 ,  C07D333/22 ,  C07D401/04 ,  C07D405/04 ,  C07D409/04

摘要： A compound or its salt having the following formula (II) is used as an activator for PPAR δ: in which each of R11 and R13 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent, etc.; R12 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, an alkoxy group having 1 to 8 carbon atoms, an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent, etc.; each of R14 and R15 is a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or an alkyl group having 1 to 8 carbon atoms and a halogen atom substituent; X1 is CH or N; Z1 is an oxygen atom or a sulfur atom; W1 is an oxygen atom or CH2; and q is an integer of 2 to 4.

摘要翻译： 使用具有下式（II）的化合物或其盐作为PPARδ的活化剂：其中R11和R13各自为氢原子，具有1至8个碳原子的烷基，具有1至8个碳原子的烷氧基 碳原子数为1〜8的烷基，卤原子取代基等。 R12为氢原子，碳原子数1〜8的烷基，碳原子数1〜8的烷氧基，碳原子数1〜8的烷基和卤素原子取代基等。 R 14和R 15各自为氢原子，碳原子数1〜8的烷基或碳原子数1〜8的烷基和卤原子取代基。 X1是CH或N; Z1是氧原子或硫原子; W1是氧原子或CH2; q为2〜4的整数。

公开(公告)号：US08962613B2

公开(公告)日：2015-02-24

申请号：US13807387

申请日：2011-07-13

申请人： Shogo Sakuma ,  Masahiko Arai ,  Kunio Kobayashi ,  Yoshikazu Watanabe ,  Toshiyasu Imai ,  Kazuhide Inoue

发明人： Shogo Sakuma ,  Masahiko Arai ,  Kunio Kobayashi ,  Yoshikazu Watanabe ,  Toshiyasu Imai ,  Kazuhide Inoue

IPC分类号： C07D243/12 ,  C07D403/10 ,  A61K31/551 ,  A61P25/04 ,  C07D243/10 ,  C07D401/10 ,  C07D409/04 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D491/056 ,  C07D401/04 ,  C07D403/04 ,  C07D243/24 ,  C07D487/04

CPC分类号： C07D243/10 ,  C07D243/12 ,  C07D243/24 ,  C07D401/04 ,  C07D401/10 ,  C07D403/04 ,  C07D403/10 ,  C07D409/04 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/056

摘要： A diazepine derivative having the following formula (III) or a pharmacologically acceptable salt thereof is used as A P2X4 receptor antagonist: wherein each of R21 and R22 is hydrogen, a C1-8 alkyl group or the like; R23 is hydrogen, a C1-8 alkyl group or the like; each of R24 and R25 is hydrogen, a C1-8 alkyl group or the like; R26 is hydrogen, a C1-8 alkyl group, a halogen atom, hydroxyl, nitro, cyano, phenyl optionally having one or more substituents, or a heterocyclic group optionally having one or more substituents or the like; and p is 0 or 1.

摘要翻译： 使用具有下式（III）的二氮杂衍生物或其药理学上可接受的盐作为P2X4受体拮抗剂：其中R21和R22各自为氢，C1-8烷基等; R 23为氢，C 1-8烷基等; R 24和R 25各自为氢，C 1-8烷基等; R 26是氢，C 1-8烷基，卤素原子，羟基，硝基，氰基，任选具有一个或多个取代基的苯基，或任选具有一个或多个取代基的杂环基等; p为0或1。

公开(公告)号：US20130178625A1

公开(公告)日：2013-07-11

申请号：US13811714

申请日：2011-07-27

申请人： Masatoshi Ushioda ,  Shogo Sakuma ,  Atsushi Tendo ,  Toshiyasu Imai ,  Kazuhide Inoue

发明人： Masatoshi Ushioda ,  Shogo Sakuma ,  Atsushi Tendo ,  Toshiyasu Imai ,  Kazuhide Inoue

IPC分类号： C07D413/10 ,  C07D403/10 ,  C07D401/10 ,  C07D241/38

CPC分类号： C07D413/10 ,  C07D241/38 ,  C07D241/44 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D403/10 ,  C07D409/12

摘要： A compound having the following formula (II) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein each of R11 and R12 is hydrogen, C1-8 alkyl or the like; R13 is hydrogen, C1-8 alkyl or the like; R14 is hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl having 1-3 halogens, C1-8 hydroxyalkyl, halogen, hydroxyl, nitro, cyano, amino, C1-8 alkylamino, benzenesulfonylamino optionally having a substituent, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene, tetrahydronaphthalene, or indan ring.

摘要翻译： 使用具有下式（II）的化合物或其药理学上可接受的盐作为P2X4受体拮抗剂：其中R11和R12各自为氢，C1-8烷基等; R 13是氢，C 1-8烷基等; R14是氢，C1-8烷基，C1-8烷氧基，具有1-3个卤素的C1-8烷基，C1-8羟基烷基，卤素，羟基，硝基，氰基，氨基，C1-8烷基氨基，任选具有取代基的苯磺酰基氨基， 任选具有取代基的杂环基等; 由W1和相邻的苯环组成的稠环是萘，四氢萘或茚满环。