公开(公告)号：US08680110B2

公开(公告)日：2014-03-25

申请号：US13811909

申请日：2011-07-27

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

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

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。

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。

公开(公告)号：US07652045B2

公开(公告)日：2010-01-26

申请号：US11888493

申请日：2007-07-31

申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

IPC分类号： A61K31/421 ,  A61K31/426 ,  C07D263/30 ,  C07D277/20

CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示可以具有选自C 1-8烷基，具有卤素的C 1-8烷基，卤素，羟基等的取代基的苯基等; R 2 表示C1-8烷基等; A表示氧，硫等; X表示C1-8亚烷基链等; Y表示C（-O），CH-CH等; R3，R4和R5 各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示氧或硫; R6和R7各自表示氢，C1-8烷基等; R8表示氢或C1-8烷基; R3，R4和R5中的至少一个不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。

公开(公告)号：US07648999B2

公开(公告)日：2010-01-19

申请号：US11888492

申请日：2007-07-31

申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

IPC分类号： A61K31/426 ,  A61K31/4436 ,  A61K31/4709 ,  C07D277/22 ,  C07D417/04

CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示可以具有选自C 1-8烷基，具有卤素的C 1-8烷基，卤素，羟基等的取代基的苯基等; R 2 表示C1-8烷基等; A表示氧，硫等; X表示C1-8亚烷基链等; Y表示C（-O），CH-CH等; R3，R4和R5 各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示氧或硫; R6和R7各自表示氢，C1-8烷基等; R8表示氢或C1-8烷基; R3，R4和R5中的至少一个不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。

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：US07265137B2

公开(公告)日：2007-09-04

申请号：US10486783

申请日：2002-08-02

申请人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Tomio Yamakawa ,  Takashi Kanda ,  Seiichiro Masui

IPC分类号： A61K31/421 ,  A61K31/426 ,  C07D213/30 ,  C07D277/20

CPC分类号： C07D263/62 ,  C07D263/32 ,  C07D277/24

摘要： A compound represented by the following general formula (I): (wherein R1 represents phenyl, etc. which can have substituents selected from the group consisting of C1-8 alkyl, C1-8 alkyl having halogen, halogen, hydroxyl, etc.; R2 represents C1-8 alkyl, etc.; A represents oxygen, sulfur, etc.; X represents C1-8 alkylene chain, etc.; Y represents C(═O), CH═CH, etc.; R3, R4, and R5 each represents hydrogen, C1-8 alkyl, etc.; B represents CH or nitrogen; Z represents oxygen or sulfur; R6 and R7 each represents hydrogen, C1-8 alkyl, etc.; and R8 represents hydrogen or C1-8 alkyl; provided that at least one of R3, R4, and R5 is not hydrogen) or a salt of the compound; and a PPAR-δ activator which contains the compound or salt as the active ingredient.

摘要翻译： 由以下通式（I）表示的化合物：（其中R 1表示苯基等，其可以具有选自C 1-8烷基的取代基 具有卤素，卤素，羟基等的C 1-8烷基; R 2表示C 1-8烷基等; A 表示氧，硫等; X表示C 1-8亚烷基链等; Y表示C（-O），CH-CH等; R 3 O R 4，R 5和R 5各自表示氢，C 1-8烷基等; B表示CH或氮; Z表示 氧或硫; R 6和R 7各自表示氢，C 1-8烷基等;和R 8， / SUP>表示氢或C 1-8烷基，条件是R 3，R 4和R 4中的至少一个， 5不是氢）或化合物的盐; 和含有该化合物或盐作为活性成分的PPAR-δ活化剂。

公开(公告)号：US07078422B2

公开(公告)日：2006-07-18

申请号：US10472699

申请日：2002-02-19

申请人： Shogo Sakuma ,  Tsuyoshi Endo ,  Takashi Kanda ,  Seiichiro Masui

发明人： Shogo Sakuma ,  Tsuyoshi Endo ,  Takashi Kanda ,  Seiichiro Masui

IPC分类号： A61K31/421 ,  A61K31/426 ,  C07D263/30 ,  C07D277/20

CPC分类号： C07D233/64 ,  C07D233/88 ,  C07D233/90 ,  C07D263/32 ,  C07D263/34 ,  C07D263/48 ,  C07D277/24 ,  C07D277/28 ,  C07D277/30 ,  C07D277/42 ,  C07D403/04 ,  C07D409/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/14

摘要： A phenylacetic acid derivative represented by the general formula (II) (wherein R11 and R12 each represents hydrogen, C1-8 alkyl, C1-8 alkoxy, C1-8 alkyl substituted by one to three halogen atoms, an optionally substituted phenyl, naphthyl, pyridyl, thienyl, or furyl group, etc.; X1 and Z1 each represents —C(═O)—, —C(═O)NH, —NHC(═O)—, —CH═CH—, a bond, etc.; and Y1 represents a C1-8 alkylene chain) or a salt of the derivative; and a PPARδ activator which contains the derivative or salt as the active ingredient

摘要翻译： 由通式（II）表示的苯乙酸衍生物（其中R 11和R 12各自表示氢，C 1-8烷基， C 1-8烷氧基，被1至3个卤素原子取代的C 1-8烷基，任选取代的苯基，萘基，吡啶基，噻吩基或呋喃基等。 （O） - ， - C（-O）NH，-NHC（-O） - ， - CH-CH - ，键等; Y 1表示C 1-8亚烷基链）或衍生物的盐; 和含有衍生物或盐作为活性成分的PPARδ活化剂

公开(公告)号：US08673915B2

公开(公告)日：2014-03-18

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： A61K31/498 ,  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。

公开(公告)号：US20120116073A1

公开(公告)日：2012-05-10

申请号：US13354361

申请日：2012-01-20

申请人： Shogo SAKUMA ,  Tsuyoshi Endo ,  Toshiyasu Imai ,  Noriko Kanakubo ,  Masahiko Arai ,  Toshihiro Takahashi ,  Kenji Hirate ,  Takako Hirate ,  Tomio Yamakawa ,  Makoto Tsuda ,  Kazuhide Inoue

发明人： Shogo SAKUMA ,  Tsuyoshi Endo ,  Toshiyasu Imai ,  Noriko Kanakubo ,  Masahiko Arai ,  Toshihiro Takahashi ,  Kenji Hirate ,  Takako Hirate ,  Tomio Yamakawa ,  Makoto Tsuda ,  Kazuhide Inoue

IPC分类号： C07D243/10

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。