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61. 发明授权

US5532266A Acrylacetamides 失效
标题翻译：丙烯酰胺
公开(公告)号：US5532266A
公开(公告)日：1996-07-02
申请号：US453811
申请日：1995-05-30
申请人： Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk , Frank Mauler , Manfred Stohrer , Andrew Barber
发明人： Rudolf Gottschlich , Karl-August Ackermann , Helmut Prucher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk , Frank Mauler , Manfred Stohrer , Andrew Barber
IPC分类号： A61K31/435 , A61K31/165 , A61K31/17 , A61K31/35 , A61K31/40 , A61K31/4025 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/535 , A61P7/10 , A61P11/08 , A61P11/14 , A61P25/04 , A61P25/08 , A61P25/28 , A61P29/00 , A61P43/00 , C07C233/00 , C07C233/05 , C07C233/08 , C07D207/08 , C07D207/09 , C07D207/12 , C07D215/00 , C07D217/06 , C07D217/14 , C07D295/12 , C07D295/135 , C07D311/84 , C07D401/06 , C07D403/06 , C07D405/06 , C07D405/12 , C07D409/06 , C07D413/06 , C07D207/36 , C07D207/325
CPC分类号： C07D405/06 , C07D207/09 , C07D207/12 , C07D217/14 , C07D311/84 , C07D405/12
摘要： Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.
摘要翻译：其中Q为R4-CH（CH2Z）-NA-，R1为Ar，具有3-7个C原子的环烷基或C 4 -C 8 - 环烷基-C 1 -C 4烷基的新的芳基乙酰胺， C7-烷基，R2是Ar，R3是H，OH，OA或A，R4是A或可以被F，Cl，Br，I，OH，OA，CF3，NO2，NH2等任意取代一次或两次的苯基， NHA，NHCOA，NHSO2A或NA2，R5和R6各自独立地为H，F，Cl，Br，I，OH，OA，CF3，NH2，NHA，NA2，NHCOA，NHCONH2，亚甲二氧基，A是具有1-7个C原子的烷基，以及其生理上可接受的盐。

62. 发明授权

US5418237A Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US5418237A
公开(公告)日：1995-05-23
申请号：US262256
申请日：1994-06-13
申请人： Henning Bottcher , Hartmut Greiner , Christoph Seyfried , Gerd Bartoszyk
发明人： Henning Bottcher , Hartmut Greiner , Christoph Seyfried , Gerd Bartoszyk
IPC分类号： A61K31/495 , A61K31/40 , A61K31/496 , A61K31/5377 , A61P9/12 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D209/14 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12 , C07D413/06 , C07D498/10 , C07D403/00
CPC分类号： C07D401/06 , C07D209/14 , C07D401/12 , C07D403/04 , C07D403/06 , C07D405/12
摘要： Indole derivatives of formula I ##STR1## wherein Ind, Q and Ar are as defined herein, and their salts, are active on the central nervous system.
摘要翻译：其中Ind，Q和Ar如本文所定义的式I的吲哚衍生物及其盐在中枢神经系统上是有活性的。

63. 发明授权

US07371756B2 Use of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and its physiologically acceptable salts 有权
标题翻译： 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪及其生理上可接受的盐
公开(公告)号：US07371756B2
公开(公告)日：2008-05-13
申请号：US10994226
申请日：2004-11-23
申请人： Gerd Bartoszyk , Christoph Seyfried , Christoph Von Amsterdam , Henning Boettcher , Ewen Sedman
发明人： Gerd Bartoszyk , Christoph Seyfried , Christoph Von Amsterdam , Henning Boettcher , Ewen Sedman
IPC分类号： A61K31/497
CPC分类号： A61K31/496 , A61K31/00 , A61K31/495 , A61K31/497
摘要： 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof, for the treatment of sub-type anxiety disorders chosen from the sub-types: panic disorder with or without agoraphobia, agoraphobia, obsessive-compulsive spectrum disorders, social phobia, posttraumatic stress disorder, acute stress indication or generalized anxiety disorder, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, anorexia, and fibromyalgia. A preferred salt is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride.
摘要翻译： 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪或其生理上可接受的盐，用于治疗选自以下的亚型焦虑症子类型：伴有或不伴有恐惧症的恐慌症，广场恐惧症，强迫症频谱障碍，社交恐惧症，创伤后应激障碍，急性应激指征或广泛性焦虑症，双相情感障碍，躁狂症，痴呆，物质相关疾病，性功能障碍，饮食失调，肥胖，厌食和纤维肌痛。优选的盐是1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪盐酸盐。

64. 发明授权

US06960599B2 Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals 失效
标题翻译：杂环氨基烷基吡啶衍生物作为心理药物
公开(公告)号：US06960599B2
公开(公告)日：2005-11-01
申请号：US10311286
申请日：2001-06-19
申请人： Dieter Dorsch , Henning Boettcher , Michael Arlt , Christoph Seyfried , Gerd Bartoszyk , Juergen Harting , Rudolf Gottschlich
发明人： Dieter Dorsch , Henning Boettcher , Michael Arlt , Christoph Seyfried , Gerd Bartoszyk , Juergen Harting , Rudolf Gottschlich
IPC分类号： A61K31/443 , A61K31/4433 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61P5/00 , A61P5/06 , A61P9/00 , A61P9/10 , A61P9/12 , A61P15/08 , A61P15/10 , A61P15/12 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/28 , A61P43/00 , C07D213/38 , C07D213/64 , C07D401/12 , C07D405/12 , C07D417/12 , C07D401/02 , A61K31/44 , A61K31/47
CPC分类号： C07D213/64 , C07D213/38 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I: where R1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is saturated, unsaturated or aromatic and optionally fused to other ring structures to give a fused ring system and the heterocycle has a total of 1 to 4 N, O and/or S atoms in the ring structures and is optionally monosubstituted, disubstituted or trisubstituted by one or more of the groups -A, —OR4, —N(R4)2, —NO2, —CN, Hal, —COOR4, —CON(R4)2, —COR4, ═O; R2 is a phenyl group which is optionally monosubstituted, disubstituted, trisubstituted, tetrasubstituted or pentasubstituted by one or more of the groups Hal, -A, —O-A, —NO2 or —CN, or is a thienyl group which is optionally monosubstituted or disubstituted by one or more of the groups Hal, -A, —O-A, -NO2, —CN or thienyl; R3 is H, -A, —CO-A, —C(R4)2R2, —C(R4)2-pyridinediyl-R2; R4 is H or -A; A is C1-C6-alkyl, where 1 to 7 hydrogen atoms are optionally replaced by fluorine; —X— is —O—, —S—, sulfinyl, sulfonyl, —C(R4)2—; —Y— is —[C(R4)2]n—; —Z— is —C(R4)2—; Hal is F, Cl, Br or I; n is 1, 2, 3 or 4; and their tolerable salts and solvates and their use as medicaments.
摘要翻译：本发明涉及式I的杂环氨基烷基吡啶衍生物：其中R 1是具有1至3个环结构的杂环的基团，其中每个环结构是饱和的，不饱和的或芳族的并且任选地与其它环结构以得到稠环体系，并且杂环在环结构中总共具有1至4个N，O和/或S原子，并且任选被一个或多个基团-A，-OR单取代，二取代或三取代 -N（R 4）2，-NO 2，-CN，Hal，-COOR 2， -CON（R 4）2，-SOR 4，-O; R 2是一个苯基，其任选被一个或多个Hal，-A，-OA，-NO 2基团单取代，二取代，三取代，四取代或五取代。或-CN，或者是任选被一个或多个Hal，-A，-OA，-NO 2，-CN或噻吩基团单取代或二取代的噻吩基; R 3是H，-A，-CO-A，-C（R 4）2 R 2，，-C（R 4）2 - 吡啶二基-R 2; R 4是H或-A; A为C 1 -C 6 - 烷基，其中1至7个氢原子任选被氟取代; -X-是-O - ， - S-，亚磺酰基，磺酰基，-C（R 4）2 - 。 -Y-是 - [C（R 4）2）n - -Z-是-C（R 4）2 - ; - Hal是F，Cl，Br或I; n为1,2,3或4; 及其可耐受的盐和溶剂合物及其作为药物的用途。

65. 发明授权

US5776972A Kappa-opiate agonists for inflammatory bowel disorders 失效
标题翻译：卡帕酸激动剂用于炎症性肠病
公开(公告)号：US5776972A
公开(公告)日：1998-07-07
申请号：US671502
申请日：1996-06-27
申请人： Andrew Barber , Christoph Seyfried , Gerd Bartoszyk , Rudolf Gottschlich
发明人： Andrew Barber , Christoph Seyfried , Gerd Bartoszyk , Rudolf Gottschlich
IPC分类号： C07D207/08 , A61K31/135 , A61K31/165 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61P1/00 , A61P1/04 , A61P29/00 , A61P43/00 , C07D207/12
CPC分类号： A61K31/4025
摘要： Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms, R.sup.2 is Ar, or R.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2, R.sup.5 is OH, CH.sub.2 OH, R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring, A is alkyl having 1-7 C atoms, Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --,--CH.dbd.CH--,--CH.sub.2 --NH--,--CH.sub.2 --NA-- or a bond and Hal is F, Cl, Br or I; and/or physiologically acceptable salts and/or one of its glycosylated derivatives , and at least one physiologically acceptable excipient or auxiliary.
摘要翻译：适用于治疗炎症性肠病并含有至少一种式I g 3-7 C原子的化合物或具有4-8个C原子的环烷基烷基的药物制剂，R 2为Ar或R 1和R 2一起为“ R3是H，OH，OA或A，R4是A或可以被Hal，OH，OA，CF3，NO2，NH2，NHA，NHCOA，NHSO2A和/或NA2单取代或二取代的苯基，R5是OH， CH 2 OH，R 6和R 7各自独立地为H，Hal，OH，OA，CF 3，NH 2，NHA，NA 2，NHCOA，NHCONH 2，NO 2或亚甲二氧基，氧基与环上的相邻碳键合，A 是具有1-7个C原子的烷基，Ar是单环或双环芳族基团，其可以任选地在环中含有N，O或S原子，并且可以被A，Hal，OH，OA单取代，二取代或三取代，CF 3，NH 2，NHA，NA 2，NHCOA和/或NHCONH 2，D是CH 2，O，S，NH，NA，-CH 2 -CH 2 - ， - CH = CH - ， - CH 2 -NH-， - CH 2 - 或键，Hal为F，Cl，Br或I; 和/或生理上可接受的盐和/或其糖基化衍生物之一，和至少一种生理上可接受的赋形剂或辅助剂。

66. 发明授权

US5693655A 3-indolylpiperidines 失效
标题翻译： 3-吲哚基哌啶
公开(公告)号：US5693655A
公开(公告)日：1997-12-02
申请号：US426405
申请日：1995-04-21
申请人： Henning Bottcher , Joachim Marz , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk
发明人： Henning Bottcher , Joachim Marz , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk
IPC分类号： A61K31/4427 , A61K31/445 , A61K31/454 , A61P9/10 , A61P9/12 , A61P25/04 , A61P25/20 , A61P25/24 , A61P43/00 , C07D209/14 , C07D211/14 , C07D401/14 , C07D491/04 , C07D491/056
CPC分类号： C07D401/14 , C07D491/04
摘要： 3-Indolylpiperidines of the formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are in each case independently of one another H, A, OH, OA, F, Cl, Br, Z, CN, CF.sub.3, COOH, CONH.sub.2, CONHA, CONA.sub.2, or COOA, or R.sup.1 and R.sup.2 and also R.sup.3 and R.sup.4 in each case together are also methylenedioxy, R.sup.5 is H or OH, R.sup.6 is H or R.sup.5 and R.sup.6 together are also a bond, A is alkyl having 1 to 6 C atoms and n is 2, 3, 4, 5 or 6, and to their physiologically acceptable salts, exhibit action on the central nervous system, in particular dopamine-agonistic or dopamine-antagonistic action.
摘要翻译：式I的3-吲哚基哌啶其中R 1，R 2，R 3和R 4各自独立地为H，A，OH，OA，F，Cl，Br，Z，CN，CF 3，COOH，CONH 2 ，CONHA，CONA2或COOA，或者R 1和R 2以及R 3和R 4在一起也是亚甲二氧基，R 5是H或OH，R 6是H或R 5，R 6一起也是键，A是具有1至 6个C原子，n为2,3,4,5或6及其生理上可接受的盐，对中枢神经系统，特别是多巴胺激动剂或多巴胺拮抗作用表现出作用。

67. 发明授权

US5242925A Piperazinylbenzodioxane derivatives 失效
标题翻译：哌嗪衍生物衍生物
公开(公告)号：US5242925A
公开(公告)日：1993-09-07
申请号：US933556
申请日：1992-08-24
申请人： Henning Boettcher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk
发明人： Henning Boettcher , Christoph Seyfried , Hartmut Greiner , Gerd Bartoszyk
IPC分类号： A61K31/495 , A61K31/357 , A61K31/496 , A61P9/02 , A61P9/08 , A61P9/10 , A61P9/12 , A61P25/00 , A61P25/04 , A61P25/20 , A61P25/24 , A61P25/26 , A61P25/28 , A61P35/00 , C07D405/04 , C07D405/12 , C07D405/14 , C07D453/02
CPC分类号： C07D405/12 , C07D405/14 , C07D453/02
摘要： Piperazinylbenzodioxane derivatives of formula I ##STR1## wherein B is an indol-3-yl or benzimidazol-1-yl radical which is unsubstituted or monosubstituted by CN, CO--R.sup.1, C.sub.n H.sub.2n --R.sup.1, Hal, OH, OA, O--C.sub.n H.sub.2n --CO--R.sup.1, or NHR.sup.2, and Q is C.sub.n H.sub.2n, or a physiologically acceptable salt thereof. The derivatives are active in the central nervous system, especially as serotonin agonists and antagonists.
摘要翻译：式I的哌嗪基苯并二恶烷衍生物其中B是未被取代或被CN，CO-R 1，C n H 2n-R 1，Hal，OH，OA，O-C n H 2n的单取代的吲哚-3-基或苯并咪唑-1-基 -CO-R 1或NHR 2，Q为C n H 2n，或其生理上可接受的盐。衍生物在中枢神经系统中是有活性的，特别是作为血清素激动剂和拮抗剂。

68. 发明授权

US5472961A Acetamides 失效
标题翻译：乙酰胺
公开(公告)号：US5472961A
公开(公告)日：1995-12-05
申请号：US397758
申请日：1995-03-02
申请人： Rudolf Gottschlich , Karl-August Ackermann , Christoph Seyfried , Andrew Barber , Gerd Bartoszyk , Hartmut Greiner
发明人： Rudolf Gottschlich , Karl-August Ackermann , Christoph Seyfried , Andrew Barber , Gerd Bartoszyk , Hartmut Greiner
IPC分类号： C07D413/06 , A61K31/42 , A61K31/47 , A61P9/10 , A61P25/00 , A61P25/04 , A61P43/00 , C07D235/26 , C07D263/58 , C07D265/36 , C07D265/38 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14
CPC分类号： C07D263/58 , C07D235/26 , C07D265/36 , C07D401/12 , C07D401/14 , C07D403/12 , C07D413/12 , C07D413/14
摘要： Novel acetamides of the formula I ##STR1## in which Q, R, X and Y have the meanings defined herein, have analgesic and neuroprotective properties and bind with high affinity to kappa receptors.
摘要翻译：其中Q，R，X和Y具有本文定义的含义的式I“I”的新型乙酰胺具有止痛和神经保护性质，并以高亲和力结合κ受体。

69. 发明授权

US07479492B2 Use combined 5-HT1A agonists and selective serotonin reuptake inhibitors 有权
标题翻译：使用组合的5-HT1A激动剂和选择性5-羟色胺再摄取抑制剂
公开(公告)号：US07479492B2
公开(公告)日：2009-01-20
申请号：US10432047
申请日：2001-11-02
申请人： Gerd Bartoszyk , Ewen Sedman
发明人： Gerd Bartoszyk , Ewen Sedman
IPC分类号： A61K31/50 , A61K31/4965
CPC分类号： A61K31/496 , A61K31/00
摘要： The present invention relates to the use of compounds being combined selective serotonin (5-HT) reuptake inhibitors (SSRIs) and 5-HT1A receptor agonists, in particular of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof or 3-{4-[4-(4-cyano-phenyl)-piperazin-1-yl]-butyl}-1H-indole-5-carbonitrile or a physiologically acceptable salt thereof, for the manufacture of a medicament for the treatment of chronic pain disorders or in treating other conditions where there is hyper-sensitization to painful signals, hyperalgesia, allodynia, enhanced pain perception, and enhanced memory of pain, as well as for the treatment of irritable bowel syndrome (IBS).
摘要翻译：本发明涉及化合物是组合的选择性5-羟色胺（5-HT）再摄取抑制剂（SSRI）和5-HT 1A受体激动剂，特别是1- [4-（5-氰基吲哚-3-基）丁基] - 4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪或其生理学上可接受的盐或3- {4- [4-（4-氰基 - 苯基） - 哌嗪-1-基] - 丁基} 吲哚-5-腈或其生理上可接受的盐，用于制备用于治疗慢性疼痛障碍或治疗其它对疼痛信号过敏的其他病症，痛觉过敏，异常性疼痛，增强的疼痛感知和增强的药物记忆疼痛，以及治疗肠易激综合征（IBS）。

70. 发明授权

US4563471A 4-Oxothiazolidin-2-ylidene-acetamide derivatives as CNS agents 失效
标题翻译： 4-氧代噻唑烷-2-亚基 - 乙酰胺衍生物作为CNS剂
公开(公告)号：US4563471A
公开(公告)日：1986-01-07
申请号：US608298
申请日：1984-05-08
申请人： Gerhard Satzinger , Manfred Herrmann , Edgar Fritschi , Johannes Hartenstein , Gerd Bartoszyk
发明人： Gerhard Satzinger , Manfred Herrmann , Edgar Fritschi , Johannes Hartenstein , Gerd Bartoszyk
IPC分类号： C07D317/50 , A61K31/425 , A61K31/426 , A61P21/02 , A61P25/00 , A61P25/08 , C07D277/20 , C07D277/34 , C07D417/12
CPC分类号： C07D277/34
摘要： 4-Oxothiazolidin-2-ylidene-acetamide derivatives, processes for their preparation, pharmaceutical compositions and a method for treating diseases of the central nervous system such as epilepsy are described.
摘要翻译：描述了4-氧代噻唑烷-2-亚基 - 乙酰胺衍生物，其制备方法，药物组合物和治疗中枢神经系统疾病如癫痫的方法。

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