公开(公告)号：US08252810B2

公开(公告)日：2012-08-28

申请号：US12368069

申请日：2009-02-09

申请人： Fumihiro Ozaki ,  Motohiro Soejima ,  Tasuku Ishida ,  Yoshihiko Norimine ,  Nobuyuki Kurusu ,  Eriko Doi ,  Toshihiko Kaneko ,  Daiju Hasegawa ,  Kiyoaki Kobayashi ,  Noboru Yamamoto

发明人： Fumihiro Ozaki ,  Motohiro Soejima ,  Tasuku Ishida ,  Yoshihiko Norimine ,  Nobuyuki Kurusu ,  Eriko Doi ,  Toshihiko Kaneko ,  Daiju Hasegawa ,  Kiyoaki Kobayashi ,  Noboru Yamamoto

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D221/02

CPC分类号： C07D451/06 ,  C07D451/02 ,  C07D451/04 ,  C07D519/00

摘要： Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.

摘要翻译： 由式（I）表示的化合物及其药学上可接受的盐具有优异的钠通道抑制作用，可用作各种神经痛，神经病，癫痫，失眠，早泄等的治疗剂和止痛剂。 其中Q表示亚乙基等，R 1，R 2和R 3表示氢等，X 1表示C 1-6亚烷基等，X 2表示C 1-6亚烷基等，A 1表示5〜6元杂环基 等，A2代表C6-14芳基等。

公开(公告)号：US20100331310A1

公开(公告)日：2010-12-30

申请号：US12867024

申请日：2009-02-09

申请人： Fumihiro Ozaki ,  Motohiro Soejima ,  Tasuku Ishida ,  Yoshihiko Norimine ,  Nobuyuki Kurusu ,  Eriko Doi ,  Toshihiko Kaneko ,  Daiju Hasegawa ,  Kiyoaki Kobayashi ,  Noboru Yamamoto

发明人： Fumihiro Ozaki ,  Motohiro Soejima ,  Tasuku Ishida ,  Yoshihiko Norimine ,  Nobuyuki Kurusu ,  Eriko Doi ,  Toshihiko Kaneko ,  Daiju Hasegawa ,  Kiyoaki Kobayashi ,  Noboru Yamamoto

IPC分类号： C07D451/02 ,  A61K31/517 ,  A61K31/535 ,  C07D498/02 ,  C07D513/02 ,  A61K31/4985 ,  A61P25/08 ,  A61K31/501 ,  A61P25/00 ,  A61K31/46 ,  A61K31/506 ,  A61K31/55 ,  A61K31/53 ,  A61K31/498 ,  A61K31/5365 ,  A61P15/00 ,  A61P3/10 ,  A61K31/495 ,  A61K31/5377

CPC分类号： C07D451/06 ,  C07D451/02 ,  C07D451/04 ,  C07D519/00

摘要： Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.

摘要翻译： 由式（I）表示的化合物及其药学上可接受的盐具有优异的钠通道抑制作用，可用作各种神经痛，神经病，癫痫，失眠，早泄等的治疗剂和止痛剂。 其中Q表示亚乙基等，R 1，R 2和R 3表示氢等，X 1表示C 1-6亚烷基等，X 2表示C 1-6亚烷基等，A 1表示5〜6元杂环基 等，A2代表C6-14芳基等。

公开(公告)号：US20090270369A1

公开(公告)日：2009-10-29

申请号：US12368069

申请日：2009-02-09

申请人： Fumihiro Ozaki ,  Motohiro Soejima ,  Tasuku Ishida ,  Yoshihiko Norimine ,  Nobuyuki Kurusu ,  Eriko Doi ,  Toshihiko Kaneko ,  Daiju Hasegawa ,  Kiyoaki Kobayashi ,  Noburu Yamamoto

发明人： Fumihiro Ozaki ,  Motohiro Soejima ,  Tasuku Ishida ,  Yoshihiko Norimine ,  Nobuyuki Kurusu ,  Eriko Doi ,  Toshihiko Kaneko ,  Daiju Hasegawa ,  Kiyoaki Kobayashi ,  Noburu Yamamoto

IPC分类号： A61K31/55 ,  C07D453/02 ,  A61K31/46 ,  A61K31/53 ,  C07D471/04 ,  C07D487/04 ,  A61P25/00

CPC分类号： C07D451/06 ,  C07D451/02 ,  C07D451/04 ,  C07D519/00

摘要： Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.

摘要翻译： 由式（I）表示的化合物及其药学上可接受的盐具有优异的钠通道抑制作用，可用作各种神经痛，神经病，癫痫，失眠，早泄等的治疗剂和止痛剂。 其中Q表示乙烯等，R 1，R 2和R 3表示氢等，X 1表示C 1-6亚烷基等，X 2表示C 1-6亚烷基等，A 1表示5〜6元杂环基 等，A2代表C6-14芳基等。

公开(公告)号：US09453000B2

公开(公告)日：2016-09-27

申请号：US12671873

申请日：2008-08-28

申请人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D471/04 ,  A61K31/437 ,  C07D487/04 ,  C07D498/04 ,  C07D403/10 ,  A61P25/28 ,  C07D403/04

CPC分类号： C07D403/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by Aβ, wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.

公开(公告)号：US20090062529A1

公开(公告)日：2009-03-05

申请号：US12200731

申请日：2008-08-28

申请人： Teiji KIMURA ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji KIMURA ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D487/04 ,  C07D498/04

CPC分类号： C07D403/10 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

摘要： A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.

摘要翻译： 由式（I）表示的化合物或其药理学上可接受的盐，其中Ar 1表示可被C 1-6烷基取代的咪唑基等，Ar 2表示可被取代的苯基等 具有C 1-6烷氧基，X 1表示双键等，Het表示可以被C 1-6烷基等取代的三唑基等，作为治疗或预防药物是有效的 由Abeta引起的疾病

公开(公告)号：US07935815B2

公开(公告)日：2011-05-03

申请号：US12200731

申请日：2008-08-28

申请人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D491/00 ,  C07D513/00 ,  C07D515/00 ,  C07D265/36 ,  C07D498/02 ,  C07D487/00 ,  C07D513/02 ,  C07D515/02 ,  C07D401/00

CPC分类号： C07D403/10 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

摘要： A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.

摘要翻译： 由式（I）表示的化合物或其药理学上可接受的盐，其中Ar 1表示可被C 1-6烷基取代的咪唑基等，Ar 2表示可被取代的苯基等 具有C 1-6烷氧基，X 1表示双键等，Het表示可以被C 1-6烷基等取代的三唑基等，作为治疗或预防药物是有效的 A＆BGR引起的疾病

公开(公告)号：US20110065696A1

公开(公告)日：2011-03-17

申请号：US12950670

申请日：2010-11-19

申请人： Teiji KIMURA ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji KIMURA ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： A61K31/437 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  A61K31/519 ,  A61K31/4439 ,  A61K31/5383 ,  A61P25/00 ,  A61P25/28

CPC分类号： C07D403/10 ,  C07D401/14 ,  C07D403/14 ,  C07D409/14

摘要： A compound represented by the formula (I): or a pharmacologically acceptable salt thereof, wherein Ar1 represents an imidazolyl group or the like which may be substituted with a C1-6 alkyl group, Ar2 represents a phenyl group or the like which may be substituted with a C1-6 alkoxy group, X1 represents a double bond or the like and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, is effective as a therapeutic or prophylactic agent for a disease caused by Aβ.

摘要翻译： 由式（I）表示的化合物或其药理学上可接受的盐，其中Ar 1表示可被C 1-6烷基取代的咪唑基等，Ar 2表示可被取代的苯基等 具有C 1-6烷氧基，X 1表示双键等，Het表示可以被C 1-6烷基等取代的三唑基等，作为治疗或预防药物是有效的 A＆BGR引起的疾病

公开(公告)号：US20110009619A1

公开(公告)日：2011-01-13

申请号：US12671873

申请日：2008-08-28

申请人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

发明人： Teiji Kimura ,  Noritaka Kitazawa ,  Toshihiko Kaneko ,  Nobuaki Sato ,  Koki Kawano ,  Koichi Ito ,  Mamoru Takaishi ,  Takeo Sasaki ,  Yu Yoshida ,  Toshiyuki Uemura ,  Takashi Doko ,  Daisuke Shinmyo ,  Daiju Hasegawa ,  Takehiko Miyagawa ,  Hiroaki Hagiwara

IPC分类号： C07D487/04 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D403/10 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04

摘要： Disclosed is a compound represented by the formula (I): or a pharmacologically acceptable salt thereof, which is effective as a therapeutic or prophylactic agent for a disease induced by Aβ, wherein Ar1 represents an imidazolyl group which may be substituted with a C1-6 alkyl group, or the like; Ar2 represents a phenyl group which may be substituted with a C1-6 alkoxy group, or the like; X1 represents a double bond, or the like; and Het represents a triazolyl group or the like which may be substituted with a C1-6 alkyl group or the like, or the like.

摘要翻译： 公开了由式（I）表示的化合物或其药理学上可接受的盐，其作为由A＆bgr诱导的疾病的治疗或预防剂是有效的，其中Ar1表示可被C1- 6烷基等; Ar 2表示可被C 1-6烷氧基取代的苯基等; X1表示双键等; Het表示可以被C 1-6烷基等取代的三唑基等。

公开(公告)号：US20120053171A1

公开(公告)日：2012-03-01

申请号：US13138504

申请日：2010-02-24

申请人： Noritaka Kitazawa ,  Daisuke Shinmyo ,  Koichio Ito ,  Nobuaki Sato ,  Daiju Hasegawa ,  Toshiyuki Uemura ,  Toru Watanabe

发明人： Noritaka Kitazawa ,  Daisuke Shinmyo ,  Koichio Ito ,  Nobuaki Sato ,  Daiju Hasegawa ,  Toshiyuki Uemura ,  Toru Watanabe

IPC分类号： A61K31/55 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4375 ,  C07D487/04 ,  A61K31/4439 ,  C07D498/04 ,  A61P25/28 ,  C07D471/04 ,  A61P25/00 ,  A61K31/5365 ,  A61K31/437

CPC分类号： C07D417/14 ,  C07D471/04 ,  C07D471/18 ,  C07D487/04 ,  C07D498/04

摘要： A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

摘要翻译： 由式[I]表示的化合物或其药理学上可接受的盐或酯，其中环A表示与可被取代的非芳族环基稠合的五元芳族杂环基等，环B表示 可以被取代的苯基等，X1表示单键等，R1和R2各自表示C1-6烷基等，m表示0〜3的整数，n表示 0〜2，作为A＆Bgr引起的疾病的治疗剂是有效的。

公开(公告)号：US08754100B2

公开(公告)日：2014-06-17

申请号：US13138504

申请日：2010-02-24

申请人： Noritaka Kitazawa ,  Daisuke Shinmyo ,  Koichi Ito ,  Nobuaki Sato ,  Daiju Hasegawa ,  Toshiyuki Uemura ,  Toru Watanabe

发明人： Noritaka Kitazawa ,  Daisuke Shinmyo ,  Koichi Ito ,  Nobuaki Sato ,  Daiju Hasegawa ,  Toshiyuki Uemura ,  Toru Watanabe

IPC分类号： A01N43/42 ,  A61K31/44 ,  A01N43/40 ,  C07D471/02 ,  C07D491/02 ,  C07D498/02 ,  C07D401/00

CPC分类号： C07D417/14 ,  C07D471/04 ,  C07D471/18 ,  C07D487/04 ,  C07D498/04

摘要： A compound represented by the formula [I]: or a pharmacologically acceptable salt or ester thereof, wherein Ring A represents a five-membered aromatic heterocyclic group or the like fused with a non-aromatic ring group, which may be substituted, Ring B represents a phenyl group or the like which may be substituted, X1 represents a single bond or the like, R1 and R2 each represent a C1-6 alkyl group or the like, m represents an integer of 0 to 3, and n represents an integer of 0 to 2, is effective as a therapeutic agent for a disease caused by Aβ.

摘要翻译： 由式[I]表示的化合物或其药理学上可接受的盐或酯，其中环A表示与可被取代的非芳族环基稠合的五元芳族杂环基等，环B表示 可以被取代的苯基等，X1表示单键等，R1和R2各自表示C1-6烷基等，m表示0〜3的整数，n表示 0〜2，作为A＆Bgr引起的疾病的治疗剂是有效的。