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1. 发明授权

US08013018B2 Aminoindane derivative or salt thereof 有权
标题翻译：氨基茚满衍生物或其盐
公开(公告)号：US08013018B2
公开(公告)日：2011-09-06
申请号：US12305254
申请日：2007-07-17
申请人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
发明人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
IPC分类号： A01N37/12 , A01N37/44 , A01N33/18 , A01N33/24 , A61K31/24 , A61K31/04
CPC分类号： C07C211/42 , C07C215/42 , C07C215/44 , C07C217/52 , C07C235/40 , C07C255/58 , C07C2602/08 , C07D209/40 , C07D221/16 , C07D295/12 , C07D307/82 , C07D333/78
摘要： Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain.A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3 -dihydro-1-benzofuran, 2,3-dihydro-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
摘要翻译：提供了具有更宽安全裕度的NMDA受体拮抗剂的化合物，可用作治疗或预防阿尔茨海默病，脑血管性痴呆，帕金森病，缺血性中风或疼痛的药剂。一种新型化合物或其盐，其特征在于其具有在茚满的环戊二烯基的碳原子上具有氨基和可以被取代的R 1（低级烷基，环烷基， - 低级亚烷基 - 芳基，芳基等） b]噻吩，环戊二烯并[b]呋喃，环戊二烯并[b]吡啶或环戊并[c]吡啶环，或2,3-二氢-1-苯并呋喃，2,3-二氢-1-苯并噻吩，二氢吲哚环，或并且在它们旁边的碳原子上具有R2和R3（相同或不同，各个低级烷基或芳基），以及包含与活性组分相同的NMDA受体拮抗剂。

2. 发明申请

US20090186916A1 AMINOINDANE DERIVATIVE OR SALT THEREOF 有权
标题翻译：氨基衍生物或其盐
公开(公告)号：US20090186916A1
公开(公告)日：2009-07-23
申请号：US12305254
申请日：2007-07-17
申请人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
发明人： Satoshi Hayashibe , Shingo Yamasaki , Kazushi Watanabe , Nobuyuki Shiraishi , Daisuke Suzuki , Hiroaki Hoshii , Junya Ohmori , Takatoshi Kanayama
IPC分类号： A61K31/135 , C07C211/38 , C07D333/78 , C07D307/93 , C07D221/04 , A61K31/381 , A61K31/343 , A61K31/44 , A61P25/00
CPC分类号： C07C211/42 , C07C215/42 , C07C215/44 , C07C217/52 , C07C235/40 , C07C255/58 , C07C2602/08 , C07D209/40 , C07D221/16 , C07D295/12 , C07D307/82 , C07D333/78
摘要： Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain.A novel compound or a salt thereof, which is characterized in that it has an amino group and R1 (lower alkyl, cycloalkyl, -lower alkylene-aryl, aryl which may be substituted, and the like) on carbon atoms of indane, cyclopenta[b]thiophene, cyclopenta[b]furan, cyclopenta[b]pyridine, or cyclopenta[c]pyridine ring, or 2,3-dihydrdo-1-benzofuran, 2,3-dihydrdo-1-benzothiophene, indoline ring, or the like, and has R2 and R3 (the same or different, each lower alkyl or aryl) on carbon atoms beside them, and an NMDA receptor antagonist comprising the same as an active component.
摘要翻译：提供了具有更宽安全裕度的NMDA受体拮抗剂的化合物，可用作治疗或预防阿尔茨海默病，脑血管性痴呆，帕金森病，缺血性中风或疼痛的药剂。一种新型化合物或其盐，其特征在于其具有在茚满的环戊二烯基的碳原子上具有氨基和可以被取代的R 1（低级烷基，环烷基， - 低级亚烷基 - 芳基，芳基等） b]噻吩，环戊二烯并[b]呋喃，环戊二烯并[b]吡啶或环戊二烯并[c]吡啶环，或2,3-二氢-1-苯并呋喃，2,3-二氢-1-苯并噻吩，二氢吲哚环或并且在它们旁边的碳原子上具有R2和R3（相同或不同，各个低级烷基或芳基），以及包含与活性组分相同的NMDA受体拮抗剂。

3. 发明申请

US20070197594A1 Cyclic amine derivative or salt thereof 审中-公开
标题翻译：环胺衍生物或其盐
公开(公告)号：US20070197594A1
公开(公告)日：2007-08-23
申请号：US11663628
申请日：2005-09-20
申请人： Satoshi Hayashibe , Takatoshi Kanayama , Junya Ohmori , Takahiko Tobe , Kyoichi Maeno , Yoshitsugu Shitaka , Jotarou Suzuki , Shigeki Kawabata , Nobuyuki Shiraishi , Shingo Yamasaki , Daisuke Suzuki , Hiroaki Hoshii
发明人： Satoshi Hayashibe , Takatoshi Kanayama , Junya Ohmori , Takahiko Tobe , Kyoichi Maeno , Yoshitsugu Shitaka , Jotarou Suzuki , Shigeki Kawabata , Nobuyuki Shiraishi , Shingo Yamasaki , Daisuke Suzuki , Hiroaki Hoshii
IPC分类号： A61K31/452 , C07D211/06 , C07D211/22 , C07D407/02 , A61K31/445
CPC分类号： C07C217/74 , C07C215/42 , C07C2601/08 , C07D211/22 , C07D295/088 , C07D307/94 , C07D319/14 , C07D401/06 , C07D405/04 , C07D409/04 , C07D409/10 , C07D413/04 , C07D453/02
摘要： Provided are compounds which are an NMDA antagonist having a broad safety margin and are useful as a treating agent or a preventing agent for Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, pain, etc. Concretely provided are an amine derivative or its salt characterized in that the amine-containing structure A therein bonds to a 2- or 3-cyclic condensed ring (e.g., indane, tetralone, 4,5,6,7-tetrahydrobenzothiophene, 4,5,6,7-tetrahydrobenzofuran, 7,8-dihydro-6H-indeno[4,5-b]furan, 2,3-dihydro-1H-cyclopenta[1]naphthalene) via X1 (bond or lower alkylene); and an NMDA antagonist containing it as an active ingredient thereof.
摘要翻译：提供作为具有广泛安全余地的NMDA拮抗剂的化合物，可用作阿尔茨海默病，脑血管性痴呆，帕金森病，缺血性中风，疼痛等的治疗剂或预防剂。具体地提供胺衍生物或其盐其特征在于其中含胺结构A与2-或3-环稠合环结合（例如，茚满，四氢萘酮，4,5,6,7-四氢苯并噻吩，4,5,6,7-四氢苯并呋喃， 8-二氢-6H-茚并[4,5-b]呋喃，2,3-二氢-1H-环戊二烯并[1]萘）通过X 1（键或低级亚烷基）; 和含有它作为其活性成分的NMDA拮抗剂。

4. 发明授权

US5496942A 5-substituted tetrahydrobenzimidazole compounds 失效
标题翻译： 5-取代的四氢苯并咪唑化合物
公开(公告)号：US5496942A
公开(公告)日：1996-03-05
申请号：US195566
申请日：1994-02-14
申请人： Mitsuaki Ohta , Tokuo Koide , Takeshi Suzuki , Akira Matsuhisa , Keiji Miyata , Junya Ohmori , Isao Yanagisawa
发明人： Mitsuaki Ohta , Tokuo Koide , Takeshi Suzuki , Akira Matsuhisa , Keiji Miyata , Junya Ohmori , Isao Yanagisawa
IPC分类号： C07D235/26 , C07D235/30 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , C07D471/04 , C07D279/36 , C07D235/04 , C07D235/12 , C07D235/28
CPC分类号： C07D401/06 , C07D235/26 , C07D235/30 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , C07D471/04
摘要： A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):Het--X.sup.2 --H (IIIa)wherein Het and X.sup.2 are as defined above, with a carboxylic acid represented by Formula (II): ##STR2## or a reactive derivative thereof.
摘要翻译：提供了制备由式（Ib）表示的四氢苯并咪唑衍生物的方法：其中Het表示可以被1至3个选自下列的取代基取代的杂环基：（低级烷基），低级烯基，低级炔基，环烷基 - 低级烷基，芳烷基，低级烷氧基羰基和卤素原子; 并且X 2表示与Het表示的与杂环的碳原子连接的单键。该方法包括使由式（IIIa）表示的杂环化合物：其中Het和X 2如上定义的Het-X2-H（IIIa）与式（II）表示的羧酸：（II）或其反应性衍生物。

5. 发明授权

US6121264A Imidazole-substituted quinoxalinedione derivatives 失效
标题翻译：咪唑取代的喹喔啉二酮衍生物
公开(公告)号：US6121264A
公开(公告)日：2000-09-19
申请号：US194750
申请日：1998-12-02
申请人： Shuichi Sakamoto , Junya Ohmori , Jun-ichi Shishikura , Masamichi Okada , Masao Sasamata
发明人： Shuichi Sakamoto , Junya Ohmori , Jun-ichi Shishikura , Masamichi Okada , Masao Sasamata
IPC分类号： C07D403/04 , A61K31/495 , C07D521/00 , A61K31/498 , C07D403/10 , C07D403/14
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： Imidazole-substituted quinoxalinedione derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof and pharmaceutical compositions useful as glutamate receptor antagonists and the like, which comprise said compounds or salts thereof and pharmaceutically acceptable carriers. ##STR1## (Each symbol in the formula has the following meaning: A: a group represented by a formula (CH.sub.2).sub.m or a group represented by a formula Ph--(CH.sub.2).sub.p (Ph: a phenyl group),X: an oxygen atom or a group represented by a formula NR.sup.4,R.sup.1 : a hydrogen atom, a hydroxyl group or a triazolyl group, with the proviso that X may be a bond when R.sup.1 is a triazolyl group,R.sup.2 : a hydrogen atom, a nitro group, a halogeno-lower alkyl group, a cyano group, an amino group, a mono- or di-lower alkylamino group or a halogen atom,R.sup.3 and R.sup.4 : may be the same or different from each other and each represents a hydrogen atom or a lower alkyl group,n: 0, 1 or 2,m: an integer of 2 to 6, andp: an integer of 1 to 6.
摘要翻译： PCT No.PCT / JP97 / 01905 Sec。 371日期1998年12月2日第 102（e）日期1998年12月2日PCT提交1997年6月5日PCT公布。公开号WO97 / 46555 日期：1997年12月11日由以下通式（I）表示的咪唑取代的喹喔啉二酮衍生物或其药学上可接受的盐以及用作谷氨酸受体拮抗剂等的药物组合物，其包含所述化合物或其盐和药学上可接受的载体。（式中的每个符号具有以下含义：A：由式（CH 2）m表示的基团或由式Ph-（CH 2）p（Ph：苯基）表示的基团，X：氧原子或由式NR4表示的基团，R1：氢原子，羟基或三唑基，条件是当R 1为三唑基时，X可以为键，R 2为氢原子，硝基，卤代低级烷基，氰基，氨基，一或二低级烷基氨基或卤素原子，R 3和R 4可以相同或不同，表示氢原子或低级烷基基团，n：0,1或2，m为2〜6的整数，p为1〜6的整数。

6. 发明授权

US6090804A Thiophene derivative and pharmaceutical composition thereof 失效
标题翻译：噻吩衍生物及其药物组合物
公开(公告)号：US6090804A
公开(公告)日：2000-07-18
申请号：US214228
申请日：1998-12-30
申请人： Takenori Kimura , Takeshi Murakami , Junya Ohmori , Takuma Morita , Shin-ichi Tsukamoto
发明人： Takenori Kimura , Takeshi Murakami , Junya Ohmori , Takuma Morita , Shin-ichi Tsukamoto
IPC分类号： A61K31/4245 , C07D333/24 , C07D409/04 , C07D409/06 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04 , C07D521/00 , A61K31/55 , C07D403/00 , C07D405/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D333/24 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Thiophene derivatives represented by the following general formula (I) or pharmaceutically acceptable salts thereof. Said compounds act as an anti-PCP agonist and therefore are useful as psychotropic or antischizophrenic agents and so on. ##STR1## (In the above formula, R.sub.1 is a formula --A.sub.1 --X.sub.1 --R.sub.3 ; R.sub.2 is a formula --A.sub.2 --X.sub.2 --R.sub.4 or does not exist; B ring is a 7- to 10-membered nitrogen-containing cycloalkyl ring; Ar ring is an aryl or heteroaryl ring; A.sub.1, A.sub.2 and A.sub.3 may be the same or different from one another and each represents a bond or a lower alkylene group; X.sub.1 and X.sub.2 may be the same or different from each other and each represents a bond or a formula --O--, --S--or the like; R.sub.3 and R.sub.4 may be the same or different from each other and each represents a hydrogen atom, a cyclic imido group or a lower alkyl group, a cycloalkyl group, an aryl group or an aralkyl group; with the proviso that, when Ar ring is thiazole ring, either one of A.sub.1 and A.sub.2 is a lower alkylene group. Also, when Ar ring is a benzene ring, a case in which one of R.sub.1 and R.sub.2 is methyl group or a halogen group and the other is a hydrogen atom is excluded.)
摘要翻译： PCT No.PCT / JP97 / 02255 Sec。 371日期1998年12月30日第 102（e）1998年12月30日日期PCT 1997年6月30日PCT公布。公开号WO98 / 00420 日期1998年1月8日由以下通式（I）表示的噻吩衍生物或其药学上可接受的盐。所述化合物作为抗PCP激动剂，因此可用作精神药物或抗精神分裂药物等。（在上式中，R 1为式-A 1 -X 1 -R 3; R 2为式-A 2 -X 2 -R 4或不存在; B环为7至10元含氮环烷基环; Ar环是芳基或杂芳基环; A 1，A 2和A 3可以彼此相同或不同，并且各自表示键或低级亚烷基; X 1和X 2可以彼此相同或不同，并且各自表示键或式-O-，-S-等; R 3和R 4可以相同或不同，表示氢原子，环状亚氨基或低级烷基，环烷基，芳基或芳烷基;条件是当Ar环是噻唑环时，A1和A2中的任一个是低级亚烷基，当Ar环是苯环时，其中R1和R2之一是甲基或卤素基团，另一个为氢原子。）

7. 发明授权

US5686482A N-(3-pyrrolidinyl) benzamide derivative 失效
标题翻译： N-（3-吡咯烷基）苯甲酰胺衍生物
公开(公告)号：US5686482A
公开(公告)日：1997-11-11
申请号：US718576
申请日：1996-10-02
申请人： Junya Ohmori , Kyoichi Maeno , Kazuyuki Hidaka , Kazuhiro Nakato , Shuichi Sakamoto , Shin-ichi Tsukamoto
发明人： Junya Ohmori , Kyoichi Maeno , Kazuyuki Hidaka , Kazuhiro Nakato , Shuichi Sakamoto , Shin-ichi Tsukamoto
IPC分类号： C07D207/14 , C07D207/06 , A61K31/40
CPC分类号： C07D207/14
摘要： N-(3-Pyrrodinyl)benzamide derivatives represented by the following general formula (I) which have potent and selective antagonism against dopamine D.sub.3 and/or D.sub.4 receptor and are useful as a psychotropic, a schizophrenia-treating agent and the like, or a pharmaceutically acceptable salt thereof or a pharmaceutical preparation thereof. ##STR1##
摘要翻译： PCT No.PCT / JP95 / 00818 Sec。 371日期1996年10月2日第 102（e）日期1996年10月2日PCT提交1995年4月26日PCT公布。公开号WO95 / 29891 日期：1995年11月9日由以下通式（I）表示的N-（3-吡咯烷基）苯甲酰胺衍生物，其具有对多巴胺D3和/或D4受体的有效和选择性拮抗作用，并且可用作精神药物，精神分裂症治疗剂和或其药学上可接受的盐或其药物制剂。（一）

8. 发明授权

US5283244A Fused pyrazine derivatives 失效
标题翻译：稠合吡嗪衍生物
公开(公告)号：US5283244A
公开(公告)日：1994-02-01
申请号：US50225
申请日：1993-05-03
申请人： Shuichi Sakamoto , Junya Ohmori , Hirokazu Kubota , Masao Sasamata , Masamichi Okada , Kazuyuki Hidaka
发明人： Shuichi Sakamoto , Junya Ohmori , Hirokazu Kubota , Masao Sasamata , Masamichi Okada , Kazuyuki Hidaka
IPC分类号： C07D241/44 , A61K31/495 , C07D241/52 , C07D401/04 , C07D401/14 , C07D403/04 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04 , C07D521/00 , A61K31/535 , C07D403/02
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D403/04
摘要： The present invention is a pyrazine derivative which has glutamate receptor antagonizing activity, represented by formula: ##STR1## wherein Z represents C or N, provided that two Zs are not N atoms at the same time; R.sup.1 represents: ##STR2## wherein ##STR3## represents ##STR4## R.sup.6 represents H or alkyl, and R.sup.7 and R.sup.8 represent each H, alkyl, nitro or phenyl, or alternatively R.sup.7 and R.sup.8 are combined together to represent butadienylene or 1,4-butylene; R.sup.2 and R.sup.3 represent each H, F, cyano, acyl, nitro, alkyl, morpholino or one of said species of R.sup.1 ; R.sup.4 and R.sup.5 represent each H, hydroxyl, alkyl, cycloalkyl, heterocycle, phenyl, or Y-substituted alkyl; Y represents hydroxyl, acyloxy, F-substituted methyl, cycloalkyl, tetrahydrofuryl, carboxyl, alkoxycarbonyl or ##STR5## R.sup.9 and R.sup.10 represent each H or alkyl, or alternatively R.sup.9 and R.sup.10 are combined together to represent a 5- or 6-membered cyclic group which may contain oxygen atom(s).
摘要翻译： PCT No.PCT / JP91 / 01498 Sec。 371日期：1993年5月5日 102（e）日期1993年5月5日PCT 1991年11月1日PCT PCT。出版物WO92 / 07847 本发明是具有谷氨酸受体拮抗活性的吡嗪衍生物，其由下式表示：（*化学结构*）其中Z表示C或N，条件是两个Z不同时为N原子; R1表示：（*化学结构*）其中（*化学结构*）表示（*化学结构*）R6表示H或烷基，R7和R8表示H，烷基，硝基或苯基，或者R7和R8组合一起代表丁二烯或1,4-丁烯; R 2和R 3表示每个H，F，氰基，酰基，硝基，烷基，吗啉代或所述R1的一种; R4和R5代表H，羟基，烷基，环烷基，杂环，苯基或Y-取代的烷基; Y表示羟基，酰氧基，F取代的甲基，环烷基，四氢呋喃基，羧基，烷氧基羰基或（*化学结构*）R9和R10表示每个H或烷基，或者R9和R10组合在一起代表5-或6- 可以含有氧原子的多元环状基团。

9. 发明授权

US08399663B2 Salt of 1,3,5-triazine-2,4,6-triamine derivative 失效
标题翻译： 1,3,5-三嗪-2,4,6-三胺衍生物的盐
公开(公告)号：US08399663B2
公开(公告)日：2013-03-19
申请号：US12753415
申请日：2010-04-02
申请人： Junya Ohmori , Makoto Kasai , Takenori Kimura , Noritaka Hamada , Ryo Mizoguchi , Satoshi Miyamoto , Noriyuki Kawano
发明人： Junya Ohmori , Makoto Kasai , Takenori Kimura , Noritaka Hamada , Ryo Mizoguchi , Satoshi Miyamoto , Noriyuki Kawano
IPC分类号： C07D403/12 , A61K31/53 , A61P25/28
CPC分类号： A61K31/53 , C07D403/12
摘要： Anytime obtained is uniform crystal of N-(4-fluorophenyl)-N′-phenyl-N″-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound A) and/or N,N′-bis (4-fluorophenyl)-N″-(pyrimidin-2-ylmethyl)-1,3,5-triazine-2,4,6-triamine (compound B) as a medicament or a starting material for the preparation of the medicament, and provided are a fumarate of the compound A and/or the compound B having excellent stability and a novel crystal thereof. A salt of the compound A and/or the compound B with fumaric acid enables uniform crystal to be anytime obtained, and thus, it is a compound that is very useful as a medicament or a starting material for the preparation of the medicament having excellent stability.
摘要翻译：得到的N-（4-氟苯基）-N'-苯基-N“ - （嘧啶-2-基甲基）-1,3,5-三嗪-2,4,6-三胺（化合物A）和 /或N，N'-二（4-氟苯基）-N“ - （嘧啶-2-基甲基）-1,3,5-三嗪-2,4,6-三胺（化合物B）作为药物或起始物用于制备药物的材料，并且提供具有优异的稳定性和新颖结晶的化合物A和/或化合物B的富马酸盐。化合物A和/或化合物B与富马酸的盐能够随时获得均匀的结晶，因此，作为制备具有优异稳定性的药物的药物或原料非常有用的化合物。

10. 发明授权

US5344927A Tetrahydrobenzimidazole derivatives and pharmaceutical compositions containing same 失效
标题翻译：四氢苯并咪唑衍生物和含有它们的药物组合物
公开(公告)号：US5344927A
公开(公告)日：1994-09-06
申请号：US39633
申请日：1993-03-30
申请人： Mitsuaki Ohta , Tokuo Koide , Takeshi Suzuki , Akira Matsuhisa , Keiji Miyata , Junya Ohmori , Isao Yanagisawa
发明人： Mitsuaki Ohta , Tokuo Koide , Takeshi Suzuki , Akira Matsuhisa , Keiji Miyata , Junya Ohmori , Isao Yanagisawa
IPC分类号： C07D235/26 , C07D235/30 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , C07D471/04 , A61K31/505 , A61K31/47 , C07D235/04 , C07D239/42 , C07D401/00
CPC分类号： C07D401/06 , C07D235/26 , C07D235/30 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , C07D471/04
摘要： A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof.The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.
摘要翻译：由式（I）表示的四氢苯并咪唑衍生物：其中Het表示可以被1至3个选自低级烷基，低级烯基，低级炔基基团，环烷基 - 低级烷基，芳烷基，低级烷氧基，硝基，羟基，低级烷氧基羰基和卤素原子; X表示与杂环的碳原子或氮原子键合的单键或-NH-或其药学上可接受的盐。式（I）化合物及其盐表现出对5-HT 3受体的拮抗作用。

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