-
1.
公开(公告)号:US6133258A
公开(公告)日:2000-10-17
申请号:US68534
申请日:1998-05-13
申请人: Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
发明人: Jun-ichi Shishikura , Hiroshi Inami , Tomoyuki Yasunaga , Masaaki Hirano , Shuichi Sakamoto , Kazushige Ohno , Masamichi Okada , Shin-ichi Tsukamoto
IPC分类号: A61K31/5415 , A61K31/542 , C07D513/04
CPC分类号: A61K31/5415
摘要: Neuroprotective agents based on inhibition of kainic acid neurotoxicity and compounds useful as neuroprotective agents based on inhibition of kainic acid neurotoxicity. An inhibitors of kainic acid neurotoxicity, comprising as an active ingredient a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof, and a pyridothiazine derivative represented by the following general formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein symbols in the formula have the following respective meanings: the ring A: a pyridine ring; ##STR2## R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 may be the same or different and each represent a hydrogen atom or a lower alkyl, cycloalkyl, alkenyl, aryl, carboxyl or lower alkoxycarbonyl group which may have substituent(s), or are not present, with the proviso that R.sup.2 and R.sup.3 may together form a nitrogen-containing heterocyclic group which may have nitrogen atoms as another hetero atom, may be fused with a benzene ring and may have a lower alkyl group as a substituent.
摘要翻译: PCT No.PCT / JP96 / 03339 Sec。 371日期1998年5月13日 102(e)日期1998年5月13日PCT 1996年11月14日PCT PCT。 出版物WO97 / 17970 日期1997年5月22日基于抑制红藻氨酸神经毒性的神经保护剂和基于抑制红藻氨酸神经毒性作用的神经保护剂的化合物。 作为活性成分的红藻氨酸神经毒性抑制剂,含有下述通式(I)所示的吡哆噻嗪衍生物或其药学上可接受的盐,以及下述通式(I)表示的吡哒嗪衍生物或其药学上可接受的盐 其中式中的符号具有以下各自的含义:环A:吡啶环; R 1,R 2,R 3,R 4和R 5可以相同或不同,各自表示氢原子或可以具有取代基或不存在的低级烷基,环烷基,烯基,芳基,羧基或低级烷氧基羰基, 条件是R2和R3可以一起形成可以具有氮原子作为另一个杂原子的含氮杂环基,可以与苯环稠合并且可以具有低级烷基作为取代基。
-
公开(公告)号:US6096743A
公开(公告)日:2000-08-01
申请号:US809087
申请日:1997-03-05
申请人: Jun-ichi Shishikura , Hiroshi Inami , Shuichi Sakamoto , Shin-ichi Tsukamoto , Masao Sasamata , Masamichi Okada , Mitsuo Fujii
发明人: Jun-ichi Shishikura , Hiroshi Inami , Shuichi Sakamoto , Shin-ichi Tsukamoto , Masao Sasamata , Masamichi Okada , Mitsuo Fujii
IPC分类号: C07D403/04 , A61K31/498 , A61K31/4985 , A61P25/14 , A61P25/28 , C07D241/44 , C07D471/04 , C07D521/00 , C07D403/10
CPC分类号: C07D231/12 , C07D233/56 , C07D241/44 , C07D249/08
摘要: A 1,2,3,4-tetrahydroquinoxalinedione derivative represented by the following formula (I) or salt thereof, an NMDA-glycine receptor and/or AMPA receptor antagonist or kainic acid neurotoxicity inhibitor containing the derivative or salt. In addition, a pharmaceutical composition comprising said compound and a pharmaceutically acceptable carrier: ##STR1## wherein the substituents are as described in the specification.
摘要翻译: PCT No.PCT / JP95 / 01922 Sec。 371日期1997年3月5日 102(e)1997年3月5日PCT PCT 1995年9月25日PCT公布。 公开号WO96 / 10023 日本1996年4月4日由下式(I)表示的1,2,3,4-四氢喹喔啉二酮衍生物或其盐,含有该衍生物或盐的NMDA-甘氨酸受体和/或AMPA受体拮抗剂或红藻氨酸神经毒性抑制剂。 此外,包含所述化合物和药学上可接受的载体的药物组合物:其中取代基如说明书中所述。
-
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)
-
公开(公告)号:US4996210A
公开(公告)日:1991-02-26
申请号:US470091
申请日:1990-01-25
IPC分类号: C07D491/107 , A61K31/435 , A61K31/55 , A61P25/02 , A61P25/28 , C07D211/48 , C07D405/06 , C07D453/00 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/20 , C07D491/22 , C07D495/10 , C07D495/20 , C07D495/22 , C07D497/20 , C07D497/22
CPC分类号: C07D471/10 , C07D211/48 , C07D491/10 , C07D495/10
摘要: Heterocyclic spiro compounds represented by the following general formula and salts thereof ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.
-
公开(公告)号:US4940795A
公开(公告)日:1990-07-10
申请号:US254375
申请日:1988-10-05
IPC分类号: C07D491/107 , A61K31/435 , A61K31/55 , A61P25/02 , A61P25/28 , C07D211/48 , C07D405/06 , C07D453/00 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/20 , C07D491/22 , C07D495/10 , C07D495/20 , C07D495/22 , C07D497/20 , C07D497/22
CPC分类号: C07D471/10 , C07D211/48 , C07D491/10 , C07D495/10
摘要: Heterocyclic spiro compounds represented by the following general formula and salts thereof: ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.
-
公开(公告)号:US4719207A
公开(公告)日:1988-01-12
申请号:US747018
申请日:1985-06-20
申请人: Toshinari Tamura , Makoto Yoshida , Shin-ichi Tsukamoto , Hidenori Iwamoto , Minoru Yamamoto , Soichi Kagami
发明人: Toshinari Tamura , Makoto Yoshida , Shin-ichi Tsukamoto , Hidenori Iwamoto , Minoru Yamamoto , Soichi Kagami
IPC分类号: C07D205/08 , C07D205/085 , C07F7/10 , C07K5/097 , A61K31/415 , C07D403/12 , C07D403/14
CPC分类号: C07K5/0821 , C07D205/08 , C07D205/085 , C07F7/10
摘要: Substituted azetidinone compounds are provided which have the formula: ##STR1## wherein one of R.sup.1 and R.sup.2 represents a substituted lower alkyl group, an azido group, an amino group, a lower acylamino group, a mercapto group or a lower alkylthio group and the other represents a hydrogen group, or, both represent hydrogen atoms or lower alkyl groups; R.sup.3 represents a hydrogen atom or a group shown by formula: ##STR2## (wherein X represents ##STR3## (wherein R.sup.5 represents a hydrogen atom or a lower alkyl group) and Y represents a hydroxy group, a lower alkoxy group, an amino group, a mono- or di-lower alkylamino group); R.sup.4 represents a hydrogen atom, a substituted or unsubstituted lower alkyl group or a group shown by formula: --CH.sub.2 CO--A (wherein A represents an amino group or a group shown by formula: ##STR4## (wherein X and Y are as defined above), provided that when R.sup.1 and R.sup.2 are both hydrogen atoms, at least R.sup.4 represents a group other than a hydrogen atom and provided that either R.sup.3 or R.sup.4 represents a group other than a hydrogen atom. The compounds have strong CNS action.
摘要翻译: 提供具有下式的取代的氮杂环丁酮化合物:其中R 1和R 2之一表示取代的低级烷基,叠氮基,氨基,低级酰氨基,巯基或低级烷硫基 另一个表示氢基团,或者都表示氢原子或低级烷基; R3表示氢原子或由下式表示的基团:其中X表示
(其中R5表示氢原子或低级烷基),Y表示羟基,低级烷氧基,氨基 ,一或二低级烷基氨基); R 4表示氢原子,取代或未取代的低级烷基或由式-CH 2 CO-A(其中A表示氨基或由下式表示的基团:其中X和Y如上所定义) ),条件是当R 1和R 2均为氢原子时,至少R 4表示氢原子以外的基团,只要R 3或R 4表示除氢原子以外的基团,则该化合物具有强CNS作用。 -
公开(公告)号:US6090804A
公开(公告)日:2000-07-18
申请号:US214228
申请日:1998-12-30
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。)
-
公开(公告)号:USRE34653E
公开(公告)日:1994-07-05
申请号:US909639
申请日:1992-07-07
IPC分类号: C07D491/107 , A61K31/435 , A61K31/55 , A61P25/02 , A61P25/28 , C07D211/48 , C07D405/06 , C07D453/00 , C07D471/10 , C07D487/10 , C07D491/10 , C07D491/20 , C07D491/22 , C07D495/10 , C07D495/20 , C07D495/22 , C07D497/20 , C07D497/22 , C07D705/02
CPC分类号: C07D471/10 , C07D211/48 , C07D491/10 , C07D495/10
摘要: Heterocyclic spiro compounds represented by the following general formula and salts thereof: ##STR1## The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.
摘要翻译: 由以下通式表示的杂环螺环化合物及其盐:上述化合物作用于毒蕈碱性乙酰胆碱受体,由此激活中枢神经系统中的乙酰胆碱神经功能。
-
公开(公告)号:US4629736A
公开(公告)日:1986-12-16
申请号:US656165
申请日:1984-09-28
IPC分类号: C07C59/125 , C07C227/08 , C07K5/02 , C07K5/06 , C07C103/52 , A61K37/02
CPC分类号: C07K5/06026 , C07C227/08 , C07C59/125 , C07K5/02
摘要: Fatty acid derivatives represented by the general formula ##STR1## and salts thereof. The compounds of this invention have excellent fibrinolytic action and a highly improved solubility.
摘要翻译: 由通式“IMAGE”表示的脂肪酸衍生物及其盐。 本发明的化合物具有优异的纤维蛋白溶解作用和高度改善的溶解性。
-
公开(公告)号:US5521180A
公开(公告)日:1996-05-28
申请号:US495619
申请日:1995-08-03
申请人: Mitsuo Fujii , Takayuki Suzuki , Satoshi Hayashibe , Shin-ichi Tsukamoto , Shin-ichi Yatsugi , Tokio Yamaguchi
发明人: Mitsuo Fujii , Takayuki Suzuki , Satoshi Hayashibe , Shin-ichi Tsukamoto , Shin-ichi Yatsugi , Tokio Yamaguchi
IPC分类号: C07D265/30 , A61K31/535
CPC分类号: C07D265/30
摘要: A morpholine derivative represented by formula (I) or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sup.1 and R.sup.3, which may be the same or different, each represent a hydrogen atom or a lower alkyl group; R.sup.2 represents a halogen atom; and the dotted line indicates an optional double bond. These compounds exhibit a selective 5-HT reuptake inhibitory activity and a selective 5-HT.sub.2 receptor antagonistic activity and useful as a therapeutic agent for depression, anxiety, etc. with reduced side effects.
摘要翻译: PCT No.PCT / JP94 / 00186 Sec。 371日期:1995年8月3日 102(e)日期1995年8月3日PCT 1994年2月8日PCT PCT。 公开号WO94 / 18182 日本美国专利申请公开说明书(公告)日本公开一般公开说明书(公开号)(Ⅰ)所示的吗啉衍生物或其药学上可接受的盐:其中R 1和R 3可以相同或不同,各自表示氢原子或低级 烷基; R2表示卤原子; 虚线表示可选的双键。 这些化合物表现出选择性的5-HT再摄取抑制活性和选择性的5-HT2受体拮抗活性,并且可用作抑制,焦虑等的治疗剂,副作用降低。
-
-
-
-
-
-
-
-
-