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51. 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。

52. 发明授权

US07618988B2 Use of substituted aminomethyl chromans 失效
标题翻译：使用取代的氨基甲基苯并二氢吡喃酮
公开(公告)号：US07618988B2
公开(公告)日：2009-11-17
申请号：US10489960
申请日：2002-08-12
申请人： Henning Böttcher , Ralf Devant , Maria Devant, legal representative , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
发明人： Henning Böttcher , Ralf Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
IPC分类号： A61K31/135 , A61K31/33 , A61K31/395 , A61K31/535 , A61K31/54 , A61K31/58
CPC分类号： C07D405/12
摘要： Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译：其中R具有权利要求1所述含义的式I化合物或其用于治疗锥体束外运动障碍和/或锥体外系运动障碍和/或治疗中的副作用的其旋光异构体或药学上可接受的盐之一的精神分裂症引起的锥体外系症状（EPS）。

53. 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。

54. 发明授权

US07329749B2 Piperazinylcarbonylquinolines and -isoquinolines 有权
标题翻译：哌嗪基羰基喹啉和异喹啉
公开(公告)号：US07329749B2
公开(公告)日：2008-02-12
申请号：US10466487
申请日：2001-12-24
申请人： Henning Boettcher , Gerd Bartoszyk , Juergen Harting , Christoph van Amsterdam , Christoph Seyfried
发明人： Henning Boettcher , Gerd Bartoszyk , Juergen Harting , Christoph van Amsterdam , Christoph Seyfried
IPC分类号： A61K31/496 , C07D403/06
CPC分类号： C07D215/48 , A61K31/495 , C07D217/26
摘要： Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).
摘要翻译：其中R 1，R 2和R 2如权利要求1所定义的式（I）化合物是有效的5-HT 2A 2A 拮抗剂，适用于治疗精神病，精神分裂症，抑郁症，神经障碍，记忆障碍，帕金森病，肌萎缩性侧索硬化，阿尔茨海默氏病，Hutington氏病，进食障碍，贪食症，神经性厌食症，经前期综合征和/或正面影响强迫症（OCD）。

55. 发明申请

US20060229339A1 Novel use of substituted aminomethyl chromans 失效
标题翻译：新型使用取代氨基甲基苯并二氢吡喃酮
公开(公告)号：US20060229339A1
公开(公告)日：2006-10-12
申请号：US10489960
申请日：2002-08-12
申请人： Henning Böttcher , Ralf Devant , Maria Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
发明人： Henning Böttcher , Ralf Devant , Maria Devant , Gerd Bartoszyk , Hermann Russ , Frank Weber , Christoph Seyfried
IPC分类号： A61K31/4433
CPC分类号： C07D405/12
摘要： Compounds of formula I in which R has a meaning as indicated in claim 1, or one of their optical isomers or pharmaceutically acceptable salts, used for the treatment of extrapyramidal movement disorders and/or adverse effects in extrapyramidal movement disorders and/or for the treatment of extrapyramidal symptoms (EPS) induced by neuroleptics.
摘要翻译：其中R具有权利要求1所述含义的式I化合物或其用于治疗锥体束外运动障碍和/或锥体外系运动障碍和/或治疗中的副作用的其旋光异构体或药学上可接受的盐之一的精神分裂症引起的锥体外系症状（EPS）。

56. 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。

57. 发明授权

US06723725B1 Indole derivatives 失效
标题翻译：吲哚衍生物
公开(公告)号：US06723725B1
公开(公告)日：2004-04-20
申请号：US10031566
申请日：2002-01-22
申请人： Henning Böttcher , Joachim März , Hartmut Greiner , Jürgen Harting , Gerd Bartoszyk , Christoph Seyfried , Christoph van Amsterdam
发明人： Henning Böttcher , Joachim März , Hartmut Greiner , Jürgen Harting , Gerd Bartoszyk , Christoph Seyfried , Christoph van Amsterdam
IPC分类号： A61K31404
CPC分类号： C07D209/12
摘要： Indole derivatives of formula I, their salts and solvates, have valuable pharmacological properties together with good tolerability, as they have actions on the central nervous system: wherein R1 and R3 are as defined herein. The compounds have a strong affinity for 5-HT2A receptors, and furthermore exhibit 5HT2A receptor-antagonistic properties. These are therefore suitable both in veterinary and in human medicine for the treatment of functional disorders of the central nervous system and also of inflammation.
摘要翻译：式I的吲哚衍生物及其盐和溶剂合物具有有价值的药理学性质以及良好的耐受性，因为它们对中枢神经系统具有作用：其中R 1和R 3如本文所定义。这些化合物对5-HT2A受体具有强亲和力，并且还表现出5HT2A受体拮抗特性。因此，这些在兽医和人类医学中都适用于治疗中枢神经系统的功能障碍以及炎症。

58. 发明授权

US06462056B1 Oxazolidines as 5-HT2A-antagonists 失效
标题翻译：恶唑烷
公开(公告)号：US06462056B1
公开(公告)日：2002-10-08
申请号：US09380202
申请日：1999-08-25
申请人： Henning Böttcher , Helmut Prücher , Hartmut Greiner , Gerd Bartoszyk , Christoph Seyfried
发明人： Henning Böttcher , Helmut Prücher , Hartmut Greiner , Gerd Bartoszyk , Christoph Seyfried
IPC分类号： A61K31454
CPC分类号： C07D413/14
摘要： The invention relates to novel oxazolidine derivatives of the formula in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention. The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
摘要翻译：本发明涉及式（1）的新的恶唑烷衍生物，其中R1，R2和R3具有权利要求1所述的含义，其盐和制备本发明化合物的方法。式I化合物作为5-HT2A拮抗剂， 5-HT再摄取抑制，抗抑郁或抗焦虑作用，可用于生产药物。

59. 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。

60. 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。

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