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公开(公告)号:US06734203B2
公开(公告)日:2004-05-11
申请号:US10169409
申请日:2002-07-01
申请人: Akira Matsuhisa , Isao Kinoyama , Akira Toyoshima , Takahito Nakahara , Masahiro Takeuchi , Minoru Okada
发明人: Akira Matsuhisa , Isao Kinoyama , Akira Toyoshima , Takahito Nakahara , Masahiro Takeuchi , Minoru Okada
IPC分类号: A61K314184
CPC分类号: C07D213/64 , A61K31/36 , A61K31/416 , A61K31/4188 , A61K31/424 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/437 , A61K31/4453 , A61K31/4468 , A61K31/454 , A61K31/47 , A61K31/4709 , A61K31/497 , A61K31/4985 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/519 , A61K31/5375 , A61K31/551 , C07C233/41 , C07C235/14 , C07C237/04 , C07C255/24 , C07C255/25 , C07C255/58 , C07C259/06 , C07C271/28 , C07C311/37 , C07C317/28 , C07C323/25 , C07C2601/02 , C07C2601/14 , C07C2602/10 , C07C2603/74 , C07D209/16 , C07D211/58 , C07D213/38 , C07D213/74 , C07D213/89 , C07D215/12 , C07D233/64 , C07D235/02 , C07D235/14 , C07D239/26 , C07D241/12 , C07D241/20 , C07D295/13 , C07D307/14 , C07D317/58 , C07D333/68 , C07D335/06 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/06 , C07D471/04 , C07D495/04
摘要: This invention relates to medicaments, particularly novel fused imidazolium derivatives useful for the treatment of cancers and novel synthetic intermediate compounds thereof. The novel imidazolium derivatives fused with an aryl or heteroaryl ring, characterized in that the 1- and/or 3-position is substituted by an alkyl group etc. having a substituent selected from the group consisting of —ORa, —SRa and the like, have excellent anti-tumor activity and low toxicity and are useful as anticancer agents having wide margins of safety.
摘要翻译: 本发明涉及药物,特别是可用于治疗癌症的新型稠合咪唑衍生物及其新型合成中间体化合物。与芳基或杂芳基环稠合的新型咪唑衍生物,其特征在于1-和/或3-位被取代 通过具有选自-OR,-SRa等的取代基的烷基等具有优异的抗肿瘤活性和低毒性,并且可用作具有宽的安全边缘的抗癌剂。
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公开(公告)号:US06673799B1
公开(公告)日:2004-01-06
申请号:US09787672
申请日:2001-03-21
申请人: Nobuaki Taniguchi , Isao Kinoyama , Takashi Kamikubo , Akira Toyoshima , Kiyohiro Samizu , Eiji Kawaminami , Masakazu Imamura , Hiroyuki Moritomo , Akira Matsuhisa , Masaaki Hirano , Yoji Miyazaki , Eisuke Nozawa , Minoru Okada , Hiroshi Koutoku , Mitsuaki Ohta
发明人: Nobuaki Taniguchi , Isao Kinoyama , Takashi Kamikubo , Akira Toyoshima , Kiyohiro Samizu , Eiji Kawaminami , Masakazu Imamura , Hiroyuki Moritomo , Akira Matsuhisa , Masaaki Hirano , Yoji Miyazaki , Eisuke Nozawa , Minoru Okada , Hiroshi Koutoku , Mitsuaki Ohta
IPC分类号: C07D23174
CPC分类号: C07D295/192 , C07D213/85 , C07D241/08 , C07D295/205 , C07D295/215 , C07D295/26
摘要: This application relates to a piperazino-substituted novel cyanophenyl derivative in which a substituted carbamoyl or substituted sulfamoyl group having an aryl, heterocyclic or the like group that may have a substituent group is bonded to one nitrogen atom on the piperazine ring. The compound of this application has an anti-androgen action and is useful in preventing or treating prostatic cancer, benign prostatic hyperplasia and the like diseases.
摘要翻译: 本申请涉及哌嗪取代的新型氰基苯基衍生物,其中具有可具有取代基的芳基,杂环等基团的取代氨基甲酰基或取代氨磺酰基与哌嗪环上的一个氮原子键合。 本申请的化合物具有抗雄激素作用,可用于预防或治疗前列腺癌,良性前列腺增生等疾病。
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公开(公告)号:US07569688B2
公开(公告)日:2009-08-04
申请号:US11155595
申请日:2005-06-20
申请人: Masaaki Hirano , Eiji Kawaminami , Akira Toyoshima , Hiroyuki Moritomo , Norio Seki , Ryutaro Wakayama , Minoru Okada , Toshiyuki Kusayama
发明人: Masaaki Hirano , Eiji Kawaminami , Akira Toyoshima , Hiroyuki Moritomo , Norio Seki , Ryutaro Wakayama , Minoru Okada , Toshiyuki Kusayama
IPC分类号: C07D235/06 , C07D401/06
CPC分类号: C07D401/06 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , C07D235/06 , C07D235/12 , C07D277/64 , C07D277/84 , C07D339/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.
摘要翻译: 本发明提供含有丙-1,3-二酮衍生物作为活性成分,特别是GnRH受体拮抗剂的药物组合物。 此外,提供具有GnRH拮抗作用的丙烷-1,3-二酮衍生物。
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公开(公告)号:US20050267110A1
公开(公告)日:2005-12-01
申请号:US11155595
申请日:2005-06-20
申请人: Masaaki Hirano , Eiji Kawaminami , Akira Toyoshima , Hiroyuki Moritomo , Norio Seki , Ryutaro Wakayama , Minoru Okada , Toshiyuki Kusayama
发明人: Masaaki Hirano , Eiji Kawaminami , Akira Toyoshima , Hiroyuki Moritomo , Norio Seki , Ryutaro Wakayama , Minoru Okada , Toshiyuki Kusayama
IPC分类号: A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61P5/24 , A61P35/00 , C07D235/06 , C07D235/12 , C07D277/64 , C07D277/84 , C07D339/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , A61K31/53 , A61K31/385 , A61K31/423
CPC分类号: C07D401/06 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , C07D235/06 , C07D235/12 , C07D277/64 , C07D277/84 , C07D339/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.
摘要翻译: 本发明提供含有丙-1,3-二酮衍生物作为活性成分,特别是GnRH受体拮抗剂的药物组合物。 此外,提供具有GnRH拮抗作用的丙烷-1,3-二酮衍生物。
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公开(公告)号:US06960591B2
公开(公告)日:2005-11-01
申请号:US10311688
申请日:2001-07-04
申请人: Masaaki Hirano , Eiji Kawaminami , Akira Toyoshima , Hiroyuki Moritomo , Norio Seki , Ryutaro Wakayama , Minoru Okada , Toshiyuki Kusayama
发明人: Masaaki Hirano , Eiji Kawaminami , Akira Toyoshima , Hiroyuki Moritomo , Norio Seki , Ryutaro Wakayama , Minoru Okada , Toshiyuki Kusayama
IPC分类号: A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , A61P5/24 , A61P35/00 , C07D235/06 , C07D235/12 , C07D277/64 , C07D277/84 , C07D339/06 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
CPC分类号: C07D401/06 , A61K31/4184 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/4725 , A61K31/506 , A61K31/5377 , C07D235/06 , C07D235/12 , C07D277/64 , C07D277/84 , C07D339/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04
摘要: Provided is a pharmaceutical composition containing a propane-1,3-dione derivative as the active ingredient, particularly a GnRH receptor antagonist. Also, provided is a propane-1,3-dione derivative having a GnRH antagonistic effect.
摘要翻译: 本发明提供含有丙-1,3-二酮衍生物作为活性成分,特别是GnRH受体拮抗剂的药物组合物。 此外,提供具有GnRH拮抗作用的丙烷-1,3-二酮衍生物。
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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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公开(公告)号:US20060264430A1
公开(公告)日:2006-11-23
申请号:US11399379
申请日:2006-04-07
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: A61K31/538 , A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/416 , C07D413/02 , C07D403/02
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-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, 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,特别是具有钙释放激活的钙通道抑制作用的以下通式(I)表示的吡唑衍生物和药物组合物,特别是含有上述化合物作为活性成分的钙释放激活的钙通道抑制剂, (式中,每个符号具有以下含义:D:吡唑基,其可以具有1〜3个选自-Alk, - 低级烯基, - 低级炔基, - 卤代 - 低级烷基,-Al-环烷基, -Alk-O-Alk, - 环烷基,-O-Alk,-COOH,-COO-Alk和-Hal,n:0或1,B:亚苯基,含氮二价饱和环基或单环 可以被Alk取代的二价杂芳族环基团,X:-NR 1 -CR 2,R 3,..., 2,-NR 3 -NR 1 - , - NR 1 -SO 2 - , - SO 2 - , - SO 2 或者-CR 4 -CR 5 - ,以及可以具有的A:苯环 一个o 更多取代基; 可以具有一个或多个取代基的单 - ,二 - 或三环稠合杂芳基; 可以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; 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:US07285554B2
公开(公告)日:2007-10-23
申请号:US11399379
申请日:2006-04-07
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-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, (in the formula, each symbol has the following meaning: D: pyrazolyl which may have 1 to 3 substituents selected from the group consisting of -Alk, -lower alkenyl, -lower alkynyl, -halogeno-lower alkyl, -Alk-cycloalkyl, -Alk-O-Alk, -cycloalkyl, —O-Alk, —COOH, —COO-Alk and -Hal, n: 0 or 1, 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,特别是具有钙释放激活的钙通道抑制作用的以下通式(I)表示的吡唑衍生物和药物组合物,特别是含有上述化合物作为活性成分的钙释放激活的钙通道抑制剂, (式中,每个符号具有以下含义:D:吡唑基,其可以具有1〜3个选自-Alk, - 低级烯基, - 低级炔基, - 卤代 - 低级烷基,-Al-环烷基, -Alk-O-Alk, - 环烷基,-O-Alk,-COOH,-COO-Alk和-Hal,n:0或1,B:亚苯基,含氮二价饱和环基或单环 可以被Alk取代的二价杂芳族环基团,X:-NR 1 -CR 2,R 3,..., 2,-NR 3 -NR 1 - , - NR 1 -SO 2 - , - SO 2 - , - SO 2 或者-CR 4 -CR 5 - ,以及可以具有的A:苯环 一个o 更多取代基; 可以具有一个或多个取代基的单 - ,二 - 或三环稠合杂芳基; 可以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; 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: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:US06958339B2
公开(公告)日:2005-10-25
申请号:US09773736
申请日:2001-02-02
申请人: Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , Jun Ishikawa , Makoto Takeuchi
发明人: Hirokazu Kubota , Yasuhiro Yonetoku , Keizo Sugasawa , Masashi Funatsu , Souichirou Kawazoe , Akira Toyoshima , 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 , 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: The present invention is directed to drugs, in particular, pyrazole derivatives represented by the following general formula (I) which have a calcium release-activated calcium channel inhibitory effect and medicinal compositions, in particular, calcium release-activated calcium channel inhibitors containing the above compounds as the active ingredient, wherein each substituent is defined in the specification. The present invention also relates to a pharmaceutical composition containing an effective amount of the compound of formula (I) and a pharmaceutically effective carrier.The present invention further relates to methods of treatment of diseases associated with calcium release-activated calcium channels, diseases associated with IL-2 production, and methods of treatment of allergic, inflammatory or auto-immune diseases.
摘要翻译: 本发明涉及具有钙释放激活的钙通道抑制作用的药物,特别是由以下通式(I)表示的吡唑衍生物,特别是含有上述的钙释放激活的钙通道抑制剂的药物组合物 化合物作为活性成分,其中每个取代基在说明书中定义。 本发明还涉及含有有效量的式(I)化合物和药学有效载体的药物组合物。 本发明还涉及治疗与钙释放激活的钙通道有关的疾病,与IL-2产生有关的疾病,以及治疗过敏性,炎性或自身免疫性疾病的方法。
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