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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。
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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.
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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.
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公开(公告)号:US5412096A
公开(公告)日:1995-05-02
申请号:US230625
申请日:1994-05-24
IPC分类号: C07D211/48 , C07D471/10 , C07D491/10 , C07D491/107 , C07D491/20 , C07D491/22 , C07D495/10 , C07D495/20 , C07D495/22 , C07D497/20 , C07D497/22 , C07D405/02
CPC分类号: C07D471/10 , C07D211/48 , C07D491/10 , C07D495/10
摘要: Hydrochloride salts of heterocyclic spiro compounds are provided and can be represented by the following general formula: ##STR1## wherein A represents piperidine or N alkyl piperidine or N alkylene attached to a non adjacent piperidine ring carbon, X is S or O, Y is carbonyl, thiocarbonyl, methylene, R.sup.5 methylene, ##STR2## alk in which R.sup.1 to R.sub.3,R.sub.6,R.sub.7 are H or alkyl, R.sub.4 is H, alkyl, COOH, or ester, or --C alkyl, R.sub.5 is halo, OH,SH, O alkyl, S alkyl, O acyl or S acyl, and Z, and Z.sub.2 are O or S. The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.
摘要翻译: 提供了杂环螺环化合物的盐酸盐,并且可以由以下通式表示:其中A表示哌啶或N烷基哌啶或连接于非相邻哌啶环碳的N亚烷基,X为S或O,Y为羰基 ,其中R 1至R 3,R 6,R 7为H或烷基,R 4为H,烷基,COOH或酯或-C烷基,R 5为卤素,OH,SH, O烷基,S烷基,O酰基或S酰基,Z和Z2是O或S.上述化合物作用于毒蕈碱性乙酰胆碱受体,从而激活中枢神经系统中的乙酰胆碱神经功能。
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公开(公告)号:US5041549A
公开(公告)日:1991-08-20
申请号:US470093
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## wherein A represents piperidine or N alkyl piperidine or N alkylene attached to a non adjacent piperidine ring carbon, X is S or O, Y is carbonyl, thiocarbonyl, methylene, R.sup.5 methylene, ##STR2## in which R.sup.1 to R.sub.3, R.sub.6, R.sub.7 are H or alkyl, R.sub.4 is H, alkyl, --COOH, or ester, or ##STR3## R.sub.5 is halo, OH, SH, O alkyl, S alkyl, O acyl or S acyl, and Z.sub.1 and Z.sub.2 are O or S.The above compounds act upon muscarinic acetylcholine receptors, thereby activating the acetylcholine nervous functions in the central nervous system.
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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: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。
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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。)
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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)
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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。
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