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1. 发明授权

US4939136A New anellated indole derivatives 失效
标题翻译：新型吲哚衍生物
公开(公告)号：US4939136A
公开(公告)日：1990-07-03
申请号：US210976
申请日：1988-06-24
申请人： Hans H. Haeck , Derk Hamminga , Ineke Van Wijngaarden , Wouter Wouters
发明人： Hans H. Haeck , Derk Hamminga , Ineke Van Wijngaarden , Wouter Wouters
IPC分类号： A61K31/395 , A61K31/41 , A61K31/435 , A61K31/535 , A61K31/54 , A61K31/55 , A61P1/00 , A61P1/04 , A61P1/08 , A61P9/06 , A61P9/08 , A61P9/10 , A61P11/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P37/08 , A61P43/00 , C07D403/06 , C07D471/06 , C07D487/06 , C07D491/04 , C07D498/06 , C07D513/06 , C07D519/00
CPC分类号： C07D471/06 , C07D487/06 , C07D513/06
摘要： The invention relates to new anellated indole derivatives of general formula 2, ##STR1## wherein p1 R.sub.0 is alkyl or alkoxy having 1-4 C-atoms, phenylalkoxy having 1-3 C-atoms in the alkoxy group, hydroxy, halogen, trifluoromethyl, trifluoromethoxy, trifluoromethylthio, or a group R.sub.7 S(O).sub.p, wherein R.sub.7 is alkyl having 1-4 C-atoms and p has the value 0, 1 or 2, or R.sub.0 is a group R.sub.8 R.sub.9 N, R.sub.8 R.sub.9 N--CO--CH.sub.2 -- or R.sub.8 R.sub.9 --N--CO wherein R.sub.8 and R.sub.9 are hydrogen or alkyl having 1-4 C-atoms or R.sub.8 R.sub.9 N forms a saturated 5- or 6-membered ring and n has the value 0, 1 or 2, Z together with the carbon atom and nitrogen atom to which Z is bound and the intermediate carbon atom, forms a heterocyclic group consisting of 5-8 ring atoms, in which, in addition to the nitrogen atom already present, a --CO--group or a second hetero atom from the group N, O, S, S-O or SO.sub.2 may be present, which ring may be substituted with 1-3 alkyl groups having 1-4 C-atoms, a phenyl group or a spiroalkyl group (C.sub.2 -C.sub.5), or which ring may be anellated with a saturated or non-saturated carbocyclic or heterocyclic ring which consists of 5- or 6-ring atoms and which may be substituted with halogen, alkyl or alkoxy having 1-4 C-atoms, andm has the values 1-5,one of the groups R.sub.2, R.sub.3 and R.sub.4 is hydrogen, alkyl having 1-6 C-atoms, cycloalkyl having 3-7 C-atoms, alkenyl having 2-6 C-atoms or phenylalkyl having 1-3 C-atoms in the alkyl group, and the two other groups independently of each other are hydrogen or alkyl having 1-6 C-atoms,and the pharmaceutically acceptable acid addition salts thereof. These compounds are strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and have a considerably longer-lasting effect and lower toxicity in comparison with related known compounds.

2. 发明授权

US5198437A 1,7-annelated indolecarboxylic acid esters and amides 失效
标题翻译： 1,7-芳族吲哚羧酸酯和酰胺
公开(公告)号：US5198437A
公开(公告)日：1993-03-30
申请号：US628109
申请日：1990-12-17
申请人： Derk Hamminga , Hans H. Haeck , Ineke Van Wijngaarden , Wouter Wouters
发明人： Derk Hamminga , Hans H. Haeck , Ineke Van Wijngaarden , Wouter Wouters
IPC分类号： C07D519/00
CPC分类号： C07D519/00
摘要： 1,7-Annelated esters and amides of indolecarboxylic acids having formula 2, ##STR1## wherein R.sub.1 is halogen;n has a value of 0-2;Z together with the carbon atom, the nitrogen atom and the intermediate carbon atom, forms a heterocyclic group consisting of 6 ring atoms in which, besides the nitrogen atom already present, a second hetero atom of S is present, which ring may be annelated with a benzene ring;R.sub.3 is hydrogen, halogen, alkyl, alkoxy or alkylthio having 1-4 carbon atoms; andR.sub.2 is a group --CO--Y--R.sub.7 wherein Y is an oxygen atom, or a group --NR.sub.6, wherein R.sub.6 is hydrogen or alkyl having 1-3 C-atoms, and R.sub.7 represents a group of the formula ##STR2## wherein p has the value 1 or 2, q has the value 2 or 3, R.sub.8 is hydrogen or alkyl or hydroxyalkyl having 1 or 2 C-atoms, r is 0 or 1, and R.sub.10 is absent. The compounds and their salts are very strong selective antagonists of neuronal 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of those receptors.
摘要翻译：具有式2的吲哚羧酸的1,7-苯基化酯和酰胺，其中R1是卤素; n的值为0-2; Z与碳原子，氮原子和中间碳原子一起形成由6个环原子组成的杂环基，其中除了存在的氮原子之外，还存在S的第二杂原子，该环可以与苯环; R3是氢，卤素，烷基，烷氧基或具有1-4个碳原子的烷硫基; R2为-CO-Y-R7基团，其中Y为氧原子，或-NR6基团，其中R6为氢或具有1-3个C原子的烷基，R7为下式基团其中 p的值为1或2，q为2或3，R8为氢或具有1或2个C原子的烷基或羟烷基，r为0或1，R10不存在。化合物及其盐是神经元5-羟色胺（5-HT）受体非常强的选择性拮抗剂，可用于治疗由这些受体的过度刺激引起的症状。

3. 发明授权

US5326768A 3,4-annelated benzimidazol-2-(1H)-one 1-carboxylic acid derivatives 失效
标题翻译： 3,4-苯并咪唑-2-（1H） - 酮1-羧酸衍生物
公开(公告)号：US5326768A
公开(公告)日：1994-07-05
申请号：US951835
申请日：1992-09-28
申请人： Ineke Van Wijngaarden , Derk Hamminga , Wouter Wouters
发明人： Ineke Van Wijngaarden , Derk Hamminga , Wouter Wouters
IPC分类号： C07D487/06 , A61K31/415 , A61K31/47 , A61K31/55 , A61P43/00 , C07D451/04 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/06 , C07D498/06 , C07D513/06 , C07D519/00 , C07D471/04
CPC分类号： C07D519/00
摘要： The present invention concerns 3,4-annelated benzimidazol-2(1H)-one 1-carboxylic acid derivatives of the formula ##STR1## wherein R.sub.0, Z, A, B and C are as defined herein. Such derivatives are useful in the treatment of symptoms which are caused by over-excitation of 5-hydroxytryptamine receptors.
摘要翻译：本发明涉及式（Ia）的3,4-环氧苯并咪唑-2（1H） - 酮1-羧酸衍生物，其中R 0，Z，A，B和C如本文所定义。这些衍生物可用于治疗由5-羟色胺受体的过度激发引起的症状。

4. 发明授权

US5183822A Substituted 3,4-annelated benzimidazol-2(1H)-ones 失效
标题翻译：取代的3,4-苯并苯并咪唑-2（1H） - 酮
公开(公告)号：US5183822A
公开(公告)日：1993-02-02
申请号：US631957
申请日：1990-12-21
申请人： Ineke Van Wijngaarden , Derk Hamminga , Wouter Wouters
发明人： Ineke Van Wijngaarden , Derk Hamminga , Wouter Wouters
IPC分类号： C07D487/06 , A61K31/415 , A61K31/47 , A61K31/55 , A61P43/00 , C07D451/04 , C07D451/12 , C07D451/14 , C07D453/02 , C07D453/06 , C07D471/06 , C07D498/06 , C07D513/06 , C07D519/00
CPC分类号： C07D519/00
摘要： The present invention is concerned with compounds of formula 1 ##STR1## wherein R.sub.0 is alkyl, alkoxy or alkylthio having 1-4 carbon atoms, hydroxy, halogen,Z, together with the carbon atom and the nitrogen atom and the intermediate carbon atom, constitutes a heterocyclic group which consists of 5-8 ring atoms, in which, besides the already present nitrogen atom, a second hetero atom from the group N, O, or S may be present, which ring may be substituted with 1-4 methyl group, or which ring may be annelated with a phenyl group optionally substituted with fluorine, or a methyl or methoxy group;A is a group of formula 2 or 3 ##STR2## wherein one of the groups R.sub.3, R.sub.4 and R.sub.5 is hydrogen, alkyl having 1-6 carbon atoms, cycloalkyl having 3-7 carbon atoms, alkenyl having 2-6 carbon atoms or phenyl alkyl having 1-3 carbon atoms in the alkyl group, and the two other groups independently of each other are hydrogen or alkyl having 1-4 carbon atoms, or wherein A is a polycyclic ring system in which one carbon atom is replaced by a tertiary nitrogen atom, for example, a ring system of formula 4, 5 or 6, ##STR3## wherein p is an integer having the value 1 or 2, q is an integer having the value 2, 3 or 4, r is an integer having the value 1, 2 or 3, and R.sub.6 is alkyl having 1-4 carbon atoms, cycloalkyl having 3-6 carbon atoms, cyclopropylmethyl, allyl, propargyl or benzyl, andB is an oxygen atom or a group .dbd.N--R, wherein R is hydrogen, alkyl having 1-6 carbon atoms or benzyl, or whereinB-A represents a group of formula 7 ##STR4## wherein R.sub.3 and R.sub.5 having the meanings defined above, and the pharmaceutically acceptable acid addition salts thereof, which are pharmaceutically active as 5-HT receptor antagonists, and pharmaceutical products containing these compounds.

5. 发明授权

US5223625A Annelated indolo [3,2,-C]lactams 失效
标题翻译：苯并吲哚并[3,2，-C]内酰胺
公开(公告)号：US5223625A
公开(公告)日：1993-06-29
申请号：US913901
申请日：1992-07-16
申请人： Ineke Van Wijngaarden , Hans H. Haeck , Derk Hamminga , Wouter Wouters
发明人： Ineke Van Wijngaarden , Hans H. Haeck , Derk Hamminga , Wouter Wouters
IPC分类号： C07D471/16 , C07D487/16 , C07D513/16 , C07D519/00
CPC分类号： C07D471/16 , C07D487/16 , C07D513/16 , C07D519/00
摘要： The invention relates to a group of new annelated indolo [3,2-c] lactam derivatives of the formula ##STR1## having an antagonistic activity on 5-HT receptors. The compounds can be used for the treatment of symptoms which are caused by excessive stimulation of said receptors in the gastrointestinal system, the central nervous system, the cardiovascular system, the respiratory system, and for alleviating or preventing withdrawal symptoms which are induced by abuse of drugs.
摘要翻译：本发明涉及对5-HT受体具有拮抗活性的一组新的具有式“IMAGE”的吲哚并[3,2-c]内酰胺衍生物。这些化合物可用于治疗由胃肠系统，中枢神经系统，心血管系统，呼吸系统中的所述受体的过度刺激引起的症状，以及用于减轻或预防由于滥用引起的戒断症状药物

6. 发明授权

US4985420A 1,7-annelated indolecarboxylic acid esters and -amides 失效
标题翻译： 1,7-芳基吲哚羧酸酯和酰胺
公开(公告)号：US4985420A
公开(公告)日：1991-01-15
申请号：US280886
申请日：1988-12-07
申请人： Derk Hamminga , Hans H. Haeck , Ineke Van Wijngaarden , Wouter Wouters
发明人： Derk Hamminga , Hans H. Haeck , Ineke Van Wijngaarden , Wouter Wouters
IPC分类号： C07D453/02 , A61K31/435 , A61P1/00 , A61P1/04 , A61P9/06 , A61P9/08 , A61P11/00 , A61P25/00 , A61P25/04 , A61P25/18 , A61P25/20 , A61P43/00 , C07D453/06 , C07D519/00
CPC分类号： C07D519/00
摘要： The invention relates to new 1,7-annelated esters and amides of indolecarboxylic acids having general formula 2, ##STR1## wherein the symbols have the meanings given in the specification. The compounds and their salts are very strong and selective antagonists of "neuronal" 5-hydroxytryptamine (5-HT) receptors, and can be used for the treatment of symptoms which are caused by over-stimulation of these receptors.

7. 发明授权

US4889849A Spasmolytically active tertiary amine derivatives 失效
标题翻译：分解活性的叔胺衍生物
公开(公告)号：US4889849A
公开(公告)日：1989-12-26
申请号：US294997
申请日：1989-01-09
申请人： Ineke Van Wijngaarden , Johannes M. A. Zwagemakers , Jan Van Dijk
发明人： Ineke Van Wijngaarden , Johannes M. A. Zwagemakers , Jan Van Dijk
IPC分类号： C07D211/46 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/455 , C07D211/32 , C07D211/58 , C07D211/62 , C07D295/18 , C07D295/194
CPC分类号： C07D295/194 , C07D211/32 , C07D211/58
摘要： The invention relates to new spasmolytically active tertiary amine derivatives and the salts thereof, of the formula (1) ##STR1## wherein the symbols have the following meanings: .circle.A is phenyl, or a 5- or 6-membered aromatic group containing 1 or 2 of the following hetero atoms: oxygen and/or sulphur and/or nitrogen;R.sub.1 and R.sub.2 may be equal or different and are hydrogen or substituents;R.sub.3 is a hydrogen atom or, together with R.sub.4, may form a ring consisting of 6 or 7 carbon atoms;R.sub.4 is a hydrogen atom or alkyl group having 1-3 carbon atoms;R.sub.5 is a straight, branched or cyclic alkyl group having 1-4 carbon atoms;R.sub.6 is a straight or branched, saturated or unsaturated alkylene group having a chain length of 2-6 carbon atoms;Z is the group NR.sub.12, wherein R.sub.12 is a hydrogen atom or an alkyl group having 1-3 carbon atoms, or Z is an oxygen atom;n has the value 0 or 1;X is a carbonyl group, thiocarbonyl group or SO.sub.2 group;R.sub.7 and R.sub.8, together with the nitrogen atom to which they are bound, constitute a fully or partly saturated heterocyclic ring consisting of 5-8 ring atoms and which may comprise in addition an O, N or S-atom as the second hetero atom, and may be substituted.
摘要翻译：本发明涉及式（1）的新的解压活性叔胺衍生物及其盐，其中符号具有以下含义：＆amp; A是苯基或5-或6-元芳基含有1或2个以下杂原子：氧和/或硫和/或氮; R 1和R 2可以相同或不同，为氢或取代基; R3是氢原子，或者与R4一起可以形成由6或7个碳原子组成的环; R4是氢原子或具有1-3个碳原子的烷基; R5是具有1-4个碳原子的直链，支链或环状烷基; R6是链长2-6个碳原子的直链或支链饱和或不饱和亚烷基; Z是NR12基团，其中R12是氢原子或具有1-3个碳原子的烷基，或Z是氧原子; n的值为0或1; X是羰基，硫代羰基或SO2基团; R7和R8与它们所结合的氮原子一起构成由5-8个环原子组成的完全或部分饱和的杂环，并且另外可以包含作为第二杂原子的O，N或S-原子，并且可以被替代。

8. 发明授权

US4874770A Aryl-substituted (N-piperidinyl)methyl- and (N-piperidinyl) methylazoles having antipsychotic properties 失效
标题翻译：具有抗精神病性质的芳基取代的（N-哌啶基）甲基和（N-哌啶基）甲基唑
公开(公告)号：US4874770A
公开(公告)日：1989-10-17
申请号：US214310
申请日：1988-07-01
申请人： Ineke Van Wijngaarden , Cornelis Kruse , Johannes A. M. Van Der Heyden , Martinus T. M. Tulp
发明人： Ineke Van Wijngaarden , Cornelis Kruse , Johannes A. M. Van Der Heyden , Martinus T. M. Tulp
IPC分类号： C07D319/00 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/495 , A61P25/18 , A61P25/20 , C07D207/32 , C07D207/335 , C07D231/12 , C07D321/00 , C07D401/06 , C07D403/06 , C07D405/12
CPC分类号： C07D207/335 , C07D231/12 , C07D401/06 , C07D403/06
摘要： The invention relates to new aryl-substituted (N-piperidinyl)methyl- and (N-piperazinyl)methylazoles having interesting pharmacological, notably antipsychotic, properties.The compounds may be prepared in a manner known for the synthesis of analogous compounds and be processed to compositions according to known methods.

9. 发明授权

US4791132A Phenyl, Pyrrolidin-2-yl substituted pyrroles having antipsychotic properties 失效
标题翻译：具有抗精神病性质的苯基，吡咯烷-2-基取代的吡咯
公开(公告)号：US4791132A
公开(公告)日：1988-12-13
申请号：US94746
申请日：1987-09-09
申请人： Ineke Van Wijngaarden , Cornelis G. Kruse , Roelof Van Hes , Johannes A. M. Van Der Heyden
发明人： Ineke Van Wijngaarden , Cornelis G. Kruse , Roelof Van Hes , Johannes A. M. Van Der Heyden
IPC分类号： A61K31/40 , A61P25/00 , C07D207/32 , C07D207/333 , C07D207/335 , C07D403/04 , C07D405/04 , C07D207/30
CPC分类号： C07D207/333 , C07D207/335 , C07D403/04 , C07D405/04
摘要： The invention relates to a group of new phenyl, pyrrolidin-2-yl substituted 5-ring heterocyclic compounds of the formula ##STR1## wherein A is an unsaturated heterocyclic 5-ring having at least one nitrogen or oxygen atom in the ring, with the proviso that the phenyl substituent is in a meta-position with respect to the 2-pyrrolidinyl substituent.The compounds have interesting pharmacological, notably antipsychotic properties.

10. 发明授权

US5424313A Bibyclic heteroacrylpiperazine derivatives having psychotropic activity, and pharmaceutical compositions containing these derivatives 失效
标题翻译：具有精神活性的双环异丙基哌嗪衍生物和含有这些衍生物的药物组合物
公开(公告)号：US5424313A
公开(公告)日：1995-06-13
申请号：US135189
申请日：1993-10-12
申请人： Jan Hartog , Berend Olivier , Ineke Van Wijngaarden , Cornelis G. Kruse , Johannes A. M. Van Der Heyden , Dirkje A. Van Dalen-Van Der AA
发明人： Jan Hartog , Berend Olivier , Ineke Van Wijngaarden , Cornelis G. Kruse , Johannes A. M. Van Der Heyden , Dirkje A. Van Dalen-Van Der AA
IPC分类号： A61K31/40 , A61K31/403 , A61K31/404 , A61K31/42 , A61K31/423 , A61K31/4245 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/536 , A61K31/5377 , A61K31/538 , A61P7/02 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , C07D209/08 , C07D215/38 , C07D215/40 , C07D215/42 , C07D217/02 , C07D217/22 , C07D231/56 , C07D241/42 , C07D241/44 , C07D261/20 , C07D263/54 , C07D263/56 , C07D263/57 , C07D263/58 , C07D265/36 , C07D271/12 , C07D277/62 , C07D307/79 , C07D307/82 , C07D311/18 , C07D311/22 , C07D311/58 , C07D317/46 , C07D317/58 , C07D317/66 , C07D319/00 , C07D319/08 , C07D319/18 , C07D319/20 , C07D321/10 , C07D327/06 , C07D333/54 , C07D333/58 , C07D405/04 , C07D241/04 , A61K31/50
CPC分类号： C07D333/54 , C07D209/08 , C07D215/40 , C07D215/42 , C07D217/02 , C07D231/56 , C07D241/42 , C07D261/20 , C07D263/56 , C07D263/57 , C07D263/58 , C07D265/36 , C07D271/12 , C07D277/62 , C07D307/79 , C07D307/82 , C07D311/18 , C07D311/22 , C07D311/58 , C07D317/46 , C07D317/66 , C07D319/08 , C07D319/18 , C07D319/20 , C07D321/10 , C07D327/06
摘要： The invention relates to new compositions with pyschotropic activity which comprise a compound of formula 1 of the formula sheet as the active substance. The compounds of formula 1 are for the greater part new compounds. The invention therefore also relates to these new compounds and to the preparation thereof in a manner known for the synthesis of analogous compounds.
摘要翻译：本发明涉及具有次氯酸活性的新组合物，其包含式1化合物作为活性物质。式1的化合物主要是新的化合物。因此，本发明也涉及这些新化合物及其以合成类似化合物已知的方式制备本发明。

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