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公开(公告)号:US20050096322A1
公开(公告)日:2005-05-05
申请号:US10505939
申请日:2003-02-27
申请人: Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人: Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号: A61P19/00 , A61P19/08 , A61P19/10 , A61P43/00 , C07D487/04 , A61K31/503
CPC分类号: C07D487/04
摘要: As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.
摘要翻译: 本发明人为了通过促进成骨细胞的功能开发具有促进骨形成刺激作用的治疗剂而作出努力的结果,发现某些含氮杂环化合物表现出强有力的骨形成刺激 对成骨细胞的作用,因此可以作为抗代谢性骨病的优异的预防或治疗剂,由此建立本发明。 因此,本发明提供了3,6-二取代的1,2,4-三唑并[4,3-b]哒嗪化合物或其药学上可接受的盐,以及包含这种化合物和药学上可接受的载体的药物组合物, 特别是骨形成剂。
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公开(公告)号:US07173033B2
公开(公告)日:2007-02-06
申请号:US11190859
申请日:2005-07-28
申请人: Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人: Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号: C07D487/04 , A61K31/5025 , A61P19/08
CPC分类号: C07D487/04
摘要: As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention.Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.
摘要翻译: 本发明人为了通过促进成骨细胞的功能开发具有促进骨形成刺激作用的治疗剂而作出努力的结果,发现某些含氮杂环化合物表现出强有力的骨形成刺激 对成骨细胞的作用,因此可以作为抗代谢性骨病的优异的预防或治疗剂,由此建立本发明。 因此,本发明提供了3,6-二取代的1,2,4-三唑并[4,3-b]哒嗪化合物或其药学上可接受的盐,以及包含这种化合物和药学上可接受的载体的药物组合物, 特别是骨形成剂。
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公开(公告)号:US20050261297A1
公开(公告)日:2005-11-24
申请号:US11190859
申请日:2005-07-28
申请人: Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
发明人: Susumu Igarashi , Ryo Naito , Yoshinori Okamoto , Noriyuki Kawano , Issei Tsukamoto , Ippei Sato , Makoto Takeuchi , Hiroyuki Kanoh , Masato Kobori
IPC分类号: A61P19/00 , A61P19/08 , A61P19/10 , A61P43/00 , C07D487/04 , A61K31/503 , A61K31/55
CPC分类号: C07D487/04
摘要: As a result of an effort made by us for the purpose of developing a therapeutic agent having a bone formation-stimulating effect by promoting the functions of osteoblasts, the present inventors discovered that a certain nitrogen-containing heterocyclic compound exhibits a potent bone formation-stimulating effect on the osteoblast and thus can serve as an excellent prophylactic or therapeutic agent against a metabolic bone disease, whereby establishing the present invention. Thus, the present invention provides a 3,6-disubstituted 1,2,4-triazolo[4,3-b]pyridazine compound or a pharmaceutically acceptable salt thereof as well as a pharmaceutical composition comprising such a compound and a pharmaceutically acceptable carrier, especially a bone-forming agent.
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公开(公告)号:US07196080B2
公开(公告)日:2007-03-27
申请号:US10480543
申请日:2002-06-13
申请人: Masahiro Iwata , Noriyuki Kawano , Hiroyuki Kaizawa , Tomofumi Takuwa , Issei Tsukamoto , Ryushi Seo , Kiyoshi Yahiro , Miki Kobayashi , Makoto Takeuchi
发明人: Masahiro Iwata , Noriyuki Kawano , Hiroyuki Kaizawa , Tomofumi Takuwa , Issei Tsukamoto , Ryushi Seo , Kiyoshi Yahiro , Miki Kobayashi , Makoto Takeuchi
IPC分类号: A61K31/496 , C07D401/06 , C07D401/14 , C07D413/14 , C07D213/79
CPC分类号: C07D213/79 , A61K31/439 , A61K31/4418 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/4436 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/506 , A61K31/5355 , A61K31/5377 , A61K31/55 , C07D213/81 , C07D213/89 , C07D401/12 , C07D405/12 , C07D409/14 , C07D413/12 , C07D417/12 , C07D487/08
摘要: The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (wherein R1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like, R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like, R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, and n: 0 or 1).
摘要翻译: 本发明涉及由以下通式表示的具有4型磷酸二酯酶抑制作用的化合物及其用途及其中间体化合物。
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公开(公告)号:US6017927A
公开(公告)日:2000-01-25
申请号:US860377
申请日:1997-08-28
申请人: Makoto Takeuchi , Ryo Naito , Masahiko Hayakawa , Yoshinori Okamoto , Yasuhiro Yonetoku , Ken Ikeda , Yasuo Isomura
发明人: Makoto Takeuchi , Ryo Naito , Masahiko Hayakawa , Yoshinori Okamoto , Yasuhiro Yonetoku , Ken Ikeda , Yasuo Isomura
IPC分类号: A61K31/439 , A61P1/00 , A61P11/00 , A61P11/06 , A61P13/00 , A61P13/10 , A61P29/00 , A61P31/00 , A61P43/00 , C07D221/12 , C07D453/02 , C07D471/04 , C09K19/34 , C09K19/40 , A61K31/435
CPC分类号: C07D221/12 , C07D453/02 , C09K19/3444
摘要: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. ##STR1## The compound has an antagonistic effect on muscarinic M.sub.3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.
摘要翻译: PCT No.PCT / JP95 / 02713 Sec。 371日期1997年8月28日 102(e)日期1997年8月28日PCT 1995年12月27日PCT PCT。 公开号WO96 / 20194 日本时间1997年7月4日由以下通式(I)表示的奎宁环衍生物,其盐,N-氧化物或季铵盐,以及含有它们的药物组合物。 该化合物对毒蕈碱M3受体具有拮抗作用,可用作泌尿系统疾病,呼吸系统疾病或消化系统疾病的预防或治疗。
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公开(公告)号:US06174896B1
公开(公告)日:2001-01-16
申请号:US09312392
申请日:1999-05-14
申请人: Makoto Takeuchi , Ryo Naito , Masahiko Hayakawa , Yoshinori Okamoto , Yasuhiro Yonetoku , Ken Ikeda , Yasuo Isomura
发明人: Makoto Takeuchi , Ryo Naito , Masahiko Hayakawa , Yoshinori Okamoto , Yasuhiro Yonetoku , Ken Ikeda , Yasuo Isomura
IPC分类号: A61K31439
CPC分类号: C07D221/12 , C07D453/02 , C09K19/3444
摘要: Quinuclidine derivatives represented by general following general formula (I), salts, N-oxides or quaternary ammonium salts thereof, and medicinal compositions containing the same. The compound has an antagonistic effect on muscarinic M3 receptors and is useful as a preventive or remedy for urologic diseases, respiratory diseases or digestive diseases.
摘要翻译: 由通式(I)表示的喹喔啉衍生物,其盐,N-氧化物或季铵盐,以及含有它们的药物组合物。该化合物对毒蕈碱M3受体具有拮抗作用,可用作泌尿系统的预防或治疗 疾病,呼吸系统疾病或消化系统疾病。
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公开(公告)号:US06740662B1
公开(公告)日:2004-05-25
申请号:US10111077
申请日:2002-04-19
申请人: Masahiro Iwata , Noriyuki Kawano , Tomofumi Takuwa , Ryota Shiraki , Miki Kobayashi , Makoto Takeuchi
发明人: Masahiro Iwata , Noriyuki Kawano , Tomofumi Takuwa , Ryota Shiraki , Miki Kobayashi , Makoto Takeuchi
IPC分类号: A61K31435
CPC分类号: C07D471/04 , A61K31/4375 , A61K31/439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377
摘要: 2-Oxo-1,2-dihydro-1,8-naphthyridine derivatives characterized by bearing a specific substituent, —X—R6, at the 3-position and a cyclic substituent, R5, at the 4-position; or salts thereof. The derivatives and the salts are useful as drugs, particularly preventive or therapeutic agents for respiratory diseases related to PDE IV.
摘要翻译: 2-氧代-1,2-二氢-1,8-二氮杂萘衍生物,其特征在于在3-位具有特定取代基-X-R 6,在4-位具有环取代基R 5; 或其盐。 衍生物和盐可用作药物,特别是与PDE IV相关的呼吸道疾病的预防或治疗剂。
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公开(公告)号:US06432963B1
公开(公告)日:2002-08-13
申请号:US09581595
申请日:2000-06-15
申请人: Hiroyuki Hisamichi , Ryo Naito , Souichirou Kawazoe , Akira Toyoshima , Kazuhito Tanabe , Eiichi Nakai , Atsushi Ichikawa , Akiko Orita , Makoto Takeuchi
发明人: Hiroyuki Hisamichi , Ryo Naito , Souichirou Kawazoe , Akira Toyoshima , Kazuhito Tanabe , Eiichi Nakai , Atsushi Ichikawa , Akiko Orita , Makoto Takeuchi
IPC分类号: C07D23948
CPC分类号: C07D239/42 , C07D231/12 , C07D233/56 , C07D239/38 , C07D239/47 , C07D239/48 , C07D239/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12
摘要: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].
摘要翻译: 由通式(I)表示的嘧啶-5-甲酰胺衍生物或其盐[其中每个符号具有以下含义; X:O,S,NR1,CO,NR1CO,CONR1,C = N-OR1或键,Y 可以被OR 1或-NHR 1取代的低级亚烷基或键,Z:O,NR 2或键,A:H或可以具有取代基的低级烷基,可以是-CO-低级烷基 具有取代基,可以具有取代基的芳基,可以具有取代基的杂芳基,可以具有取代基的环烷基或可以具有取代基的含氮饱和杂环基,B:可以具有取代基的芳基, 或可以具有取代基的杂芳基,R 1,R 2:H,低级烷基或-CO-低级烷基]。
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公开(公告)号:US20050234055A1
公开(公告)日:2005-10-20
申请号:US11154591
申请日:2005-06-17
申请人: Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
发明人: Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
IPC分类号: A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/538 , C07D231/12 , C07D231/14 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/02 , C07D417/02 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00 , C07D43/02 , C07D49/02
CPC分类号: C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译: 药物,特别是具有钙释放依赖性钙通道抑制作用的药物组合物,特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式(I)表示的吡唑衍生物, (在该式中,每个符号具有以下含义:B:亚苯基,含氮,二价饱和环基或可被Alk,X:-NR 1取代的单环,二价杂芳族环基团 其中R 1,R 2,R 3,R 3,R 3,R 3, -NR 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基,其可以具有一个或多个 取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。
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公开(公告)号:US07247635B2
公开(公告)日:2007-07-24
申请号:US11154591
申请日:2005-06-17
申请人: Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
发明人: Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Yoshinori Okamoto , Jun Ishikawa , Makoto Takeuchi
IPC分类号: C07D231/12 , A61K31/415
CPC分类号: C07D231/12 , C07D231/14 , C07D233/56 , C07D249/08 , C07D401/12 , C07D403/12 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14
摘要: Drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-dependent calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-dependent calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: B: phenylene, a nitrogen-containing, divalent, saturated ring group, or a monocyclic, divalent heteroaromatic ring group which may be substituted with Alk, X: —NR1—CR2R3—, —CR2R3—NR1—, —NR1—SO2—, —SO2—NR1— or —CR4═CR5—, and A: benzene ring which may have one or more substituents; mono-, di- or tricyclic fused heteroaryl which may have one or more substituents; cycloalkyl which may have one or more substituents; a nitrogen-containing, saturated ring group which may have one or more substituents; lower alkenyl which may have one or more substituents; lower alkynyl which may have one or more substituents; or Alk which may have one or more substituents).
摘要翻译: 药物,特别是具有钙释放依赖性钙通道抑制作用的药物组合物,特别是含有上述化合物作为活性成分的钙释放依赖性钙通道抑制剂的下述通式(I)表示的吡唑衍生物, (在该式中,每个符号具有以下含义:B:亚苯基,含氮,二价饱和环基或可被Alk,X:-NR 1取代的单环,二价杂芳族环基团 其中R 1,R 2,R 3,R 3,R 3,R 3, -NR 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - , - SO 2 - 可以具有一个或多个取代基的一个 - 二环或三环稠合杂芳基,其可以具有一个或多个 取代基;可具有一个或多个取代基的环烷基;可具有一个或多个取代基的含氮饱和环基团 ents 可以具有一个或多个取代基的低级烯基; 可以具有一个或多个取代基的低级炔基; 或Alk,其可以具有一个或多个取代基)。
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