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公开(公告)号:US20100256123A1
公开(公告)日:2010-10-07
申请号:US12438627
申请日:2007-08-24
申请人: Shogo Sakuma , Tsuyoshi Endo , Toshiyasu Imai , Noriko Kanakubo , Masahiko Arai , Toshihiro Takahashi , Tomio Yamakawa , Makoto Tsuda , Kazuhide Inoue , Kenji Hirate , Takako Hirate
发明人: Shogo Sakuma , Tsuyoshi Endo , Toshiyasu Imai , Noriko Kanakubo , Masahiko Arai , Toshihiro Takahashi , Tomio Yamakawa , Makoto Tsuda , Kazuhide Inoue , Kenji Hirate , Takako Hirate
IPC分类号: A61K31/551 , C07D243/10 , A61P29/00
CPC分类号: C07D243/20 , C07D243/22 , C07D243/24
摘要: A compound having the following formula (II) or its pharmacologically acceptable salt is used as a P2X4 receptor antagonist: in which R11 represents hydrogen or an alkyl group having 1-8 carbon atoms; R21 represents an alkyl group having 1-8 carbon atoms, an alkoxy group having 1-8 carbon atoms, an alkyl group having 1-8 carbon atoms and having 1-3 halogen substituents, or hydroxyl; and R31 is hydrogen or a halogen atom.
摘要翻译: 使用具有下式(II)或其药理学上可接受的盐的化合物作为P2X4受体拮抗剂:其中R11表示氢或具有1-8个碳原子的烷基; R21表示碳原子数1〜8的烷基,碳原子数为1〜8的烷氧基,碳原子数1〜8的烷基,卤素取代基1-3个,羟基, R 31为氢或卤素原子。
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公开(公告)号:US20110092703A1
公开(公告)日:2011-04-21
申请号:US12672818
申请日:2008-08-08
申请人: Shogo Sakuma , Tsuyoshi Endo , Noriko Kanakubo , Masahiko Arai , Toshihiro Takahashi , Toshiyasu Imai , Kumiko Taguchi , Eriko Nakata , Nobutaka Mochiduki , Masatoshi Ushioda , Makoto Tsuda , Kazuhide Inoue
发明人: Shogo Sakuma , Tsuyoshi Endo , Noriko Kanakubo , Masahiko Arai , Toshihiro Takahashi , Toshiyasu Imai , Kumiko Taguchi , Eriko Nakata , Nobutaka Mochiduki , Masatoshi Ushioda , Makoto Tsuda , Kazuhide Inoue
IPC分类号: C07D241/04
CPC分类号: A61K31/495 , A61K31/496 , C07D241/04 , C07D405/12
摘要: A P2X4 receptor antagonist is a compound represented by the formula (I) or a pharmacologically acceptable salt thereof, which is used as a preventive or therapeutic agent for neuropathic pains: Wherein B is aryl or the like that can have a substituent; Y is C1-5 alkylene that can have a double bond; Z is O, S or the like; each of R1, R2 and R3 independently is hydrogen, C1-8 alkyl or the like; R4 is hydrogen, C1-8 alkyl or the like; each of P and Q independently is hydrogen, halogen, C1-8 alkyl or the like; W is C1-8 alkyl or the like; and each of n and m independently is 1 or 2.
摘要翻译: P2X4受体拮抗剂是由式(I)表示的化合物或其药理学上可接受的盐,其用作神经性疼痛的预防或治疗剂:其中B是可以具有取代基的芳基等; Y是可具有双键的C 1-5亚烷基; Z是O,S等; R 1,R 2和R 3各自独立地为氢,C 1-8烷基等; R4是氢,C1-8烷基等; P和Q各自独立地是氢,卤素,C 1-8烷基等; W是C 1-8烷基等; n和m各自独立地为1或2。
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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。
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公开(公告)号:US20130172550A1
公开(公告)日:2013-07-04
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: C07D243/10 , C07D491/056 , C07D409/04 , C07D413/10 , C07D417/10 , C07D471/04 , C07D401/10
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。
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公开(公告)号:US08470814B2
公开(公告)日:2013-06-25
申请号:US13148728
申请日:2010-02-15
IPC分类号: C07D403/10 , A61K31/5513 , A61P25/04
CPC分类号: C07D243/10 , C07D403/10 , C07D413/10
摘要: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
摘要翻译: 作为P2X4受体拮抗剂,使用式(I)表示的二氮平二酮衍生物或其药理学上可接受的盐,其中,R1表示氢原子,碳原子数为1〜8的烷基等,R2,R3表示 氢原子,碳原子数1〜8的烷基,卤素原子等,R4和R5表示氢原子,碳原子数1〜8的烷基等,W表示四唑等 。
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公开(公告)号:US20110319610A1
公开(公告)日:2011-12-29
申请号:US13148728
申请日:2010-02-15
IPC分类号: C07D403/10 , C07D413/10
CPC分类号: C07D243/10 , C07D403/10 , C07D413/10
摘要: A diazepinedione derivative represented by the formula (I) or a pharmacologically acceptable salt thereof is used as a P2X4 receptor antagonist: wherein R1 represents a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, R2 and R3 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a halogen atom, or the like, R4 and R5 represent a hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or the like, and W represents tetrazole or the like.
摘要翻译: 作为P2X4受体拮抗剂,使用式(I)表示的二氮平二酮衍生物或其药理学上可接受的盐,其中,R1表示氢原子,碳原子数为1〜8的烷基等,R2,R3表示 氢原子,碳原子数1〜8的烷基,卤素原子等,R4和R5表示氢原子,碳原子数1〜8的烷基等,W表示四唑等 。
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公开(公告)号:US06787552B2
公开(公告)日:2004-09-07
申请号:US10344496
申请日:2003-02-11
申请人: Shogo Sakuma , Tsuyoshi Endo , Atsushi Tendo , Toshihiro Takahashi , Shinichi Yoshida , Kunio Kobayashi , Nobutaka Mochizuki , Tomio Yamakawa , Takashi Kanda , Seiichiro Masui
发明人: Shogo Sakuma , Tsuyoshi Endo , Atsushi Tendo , Toshihiro Takahashi , Shinichi Yoshida , Kunio Kobayashi , Nobutaka Mochizuki , Tomio Yamakawa , Takashi Kanda , Seiichiro Masui
IPC分类号: A61K31421
CPC分类号: C07D413/04 , C07D263/32 , C07D277/24
摘要: Compounds of the general formula (I) or salts thereof and activators of PPAR&dgr; (peroxisome proliferator activated receptor &dgr;) containing the compounds or the salts as the active ingredient: wherein R1 and R2 each are hydrogen, C1-8 alkyl, an aryl or heterocyclic group which may be substituted, or the like; A is oxygen, sulfur, or the like; X1 and X2 are each a free valency, oxygen, S(O)p (wherein p is an integer of 0 to 2), C(═O), C(═O)NH, NHC(═O), CH═CH, or the like; Y is optionally substituted C1-8 alkylene; Z is oxygen or sulfur; R3 and R4 are each optionally substituted C1-8 alkyl; and R8 is hydrogen or C1-8 alkyl, with the proviso that when X1 is a free valency, X2 is not O or S(O)p, while when X1 is C(═O)NH, X2 is not a free valency.
摘要翻译: 通式(I)的化合物或其盐和含有化合物或其盐作为活性成分的PPARdta(过氧化物酶体增殖物活化受体δ)的活化剂:其中R 1和R 2各自为氢,C 1-8 烷基,可被取代的芳基或杂环基等; A是氧,硫等; X 1和X 2各自为自由价,氧,S(O)p(其中p为0至2的整数),C(= O),C(= O)NH,NHC(= O),CH = CH等; Y是任选取代的C 1-8亚烷基; Z是氧或硫; R 3和R 4各自为任选取代的C 1-8烷基; 并且R 8是氢或C 1-8烷基,条件是当X 1是自由价时,X 2不是O或S(O)p,而当X 1是C(O) = O)NH,X 2不是自由价。
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公开(公告)号:US20130178625A1
公开(公告)日:2013-07-11
申请号:US13811714
申请日:2011-07-27
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。
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公开(公告)号:US20130184459A1
公开(公告)日:2013-07-18
申请号:US13811909
申请日:2011-07-27
IPC分类号: C07D239/70 , C07D403/10
CPC分类号: C07D239/70 , C07D401/04 , C07D403/04 , C07D403/10 , C07D413/04 , C07D471/04
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 C1-8 alkoxy, hydroxyl, cyano, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene ring or the like.
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; R 14是C 1-8烷氧基,羟基,氰基,任选具有取代基的杂环基等; 并且由W1和相邻的苯环组成的稠环是萘环等。
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公开(公告)号:US08680110B2
公开(公告)日:2014-03-25
申请号:US13811909
申请日:2011-07-27
IPC分类号: A61K31/517 , A61K31/519 , C07D239/70
CPC分类号: C07D239/70 , C07D401/04 , C07D403/04 , C07D403/10 , C07D413/04 , C07D471/04
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 C1-8 alkoxy, hydroxyl, cyano, a heterocyclic group optionally having a substituent or the like; and the condensed ring consisting of W1 and the neighboring benzene ring is naphthalene ring or the like.
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; R 14是C 1-8烷氧基,羟基,氰基,任选具有取代基的杂环基等; 并且由W1和相邻的苯环组成的稠环是萘环等。
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