-
公开(公告)号:US06258813B1
公开(公告)日:2001-07-10
申请号:US09254489
申请日:1999-03-09
IPC分类号: A61K31496
CPC分类号: C07D213/74 , C07D213/38 , C07D239/42 , C07D295/073 , C07D295/096 , C07D295/155 , C07D401/12 , C07D405/12 , C07D409/12
摘要: Piperazine derivatives of the formula I in which R1 and R2 have the meanings given in claim 1 are dopamine ligands with a selectivity for the D4 receptor and are suitable for the treatment and prophylaxis of states of anxiety, depression, schizophrenia, obsessions, Parkinson's disease, tardive dyskinesia, nausea and disorders of the gastro-intestinal tract.
摘要翻译: R1和R2具有权利要求1中给出的含义的式Iin的哌嗪衍生物是对D4受体具有选择性的多巴胺配体,并且适用于治疗和预防焦虑,抑郁,精神分裂症,痴呆,帕金森病,迟发性 运动障碍,恶心和胃肠道疾病。
-
公开(公告)号:US20060264419A1
公开(公告)日:2006-11-23
申请号:US10552065
申请日:2004-03-08
申请人: Kai Schiemann , Karl-August Ackermann , Michael Arlt , Dirk Finsinger , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried , Oliver Schadt
发明人: Kai Schiemann , Karl-August Ackermann , Michael Arlt , Dirk Finsinger , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried , Oliver Schadt
IPC分类号: A61K31/551 , A61K31/5377 , A61K31/496 , A61K31/4439 , A61K31/416
CPC分类号: C07D231/12 , A61K31/415 , C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/06 , C07D409/10 , C07D413/12 , C07D451/06 , C07D453/06 , C07D471/04 , C07D471/10 , C07D487/08 , C07D491/08
摘要: The compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, R4 and R5 have the meanings indicated in Claim (1), are suitable as ligands of 5 HT receptors.
摘要翻译: 式(I)化合物及其盐和溶剂合物,其中X,R 1,R 2,R 3,R 3, SUP> 4和R 5具有权利要求(1)所示的含义,适合作为5HT受体的配体。
-
3.
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。
-
公开(公告)号:US06395780B1
公开(公告)日:2002-05-28
申请号:US09559831
申请日:2000-04-28
申请人: Michael Arlt , Gerd Bartoszyk
发明人: Michael Arlt , Gerd Bartoszyk
IPC分类号: A61K3119
CPC分类号: A61K31/19 , A61K31/00 , A61K31/145
摘要: The invention relates to inhibitors of the glycine cleavage system and their use as potential antipsychotic agents. The invention relates furthermore to a process for treating humans having psychosis, psychosis associated with an illness, schizophrenia, Alzheimers disease or other related psychotic disorders.
摘要翻译: 本发明涉及甘氨酸裂解体系的抑制剂及其作为潜在抗精神病药的用途。 本发明还涉及治疗患有精神病,与疾病相关的精神病,精神分裂症,阿尔茨海默病或其它相关精神病的人的方法。
-
公开(公告)号:US07842695B2
公开(公告)日:2010-11-30
申请号:US10552064
申请日:2004-03-10
申请人: Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人: Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号: A61K31/497 , A61K31/435 , A01N43/40 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号: C07D231/12 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要: Compounds of formula (I) and salts thereof, in which the following definitions apply: X is N or CH; R1 is H, A, Hal, (CH2)nHet, (CH2)nAr, C3-7-cycloalkyl, CF3, NO2, CN, C(NH)(OH), or OCF3; R2 is (CH2)nHet, (CH2)nAr, or C3-7-cycloalkyl, or CF3; R3 and R4 denote H or an organic radical. Compounds of formula (I) are useful as ligands of 5-HT receptors and useful in the treatment of disorders such as anxiety, depression, obsessive-compulsive disorder and pain.
摘要翻译: 式(I)化合物及其盐,其中适用以下定义:X为N或CH; R1是H,A,Hal,(CH2)nHet,(CH2)nAr,C3-7-环烷基,CF3,NO2,CN,C(NH)(OH)或OCF3; R2是(CH2)nHet,(CH2)nAr或C3-7-环烷基或CF3; R3和R4表示H或有机基团。 式(I)化合物可用作5-HT受体的配体,可用于治疗焦虑,抑郁,强迫症和疼痛等疾病。
-
公开(公告)号:US20070010531A1
公开(公告)日:2007-01-11
申请号:US10552064
申请日:2004-03-10
申请人: Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
发明人: Oliver Schadt , Michael Arlt , Dirk Finsinger , Kai Schiemann , Christoph Van Amsterdam , Gerd Bartoszyk , Christoph Seyfried
IPC分类号: A61K31/497 , A61K31/4439 , A61K31/416 , C07D403/02
CPC分类号: C07D231/12 , C07D231/40 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/04 , C07D413/14
摘要: Compounds of the formula (I) and salts and solvates thereof, in which X, R1, R2, R3, and R5 have the meanings indicated in claim 1, are suitable as ligands of 5 HT receptors.
摘要翻译: 式(I)化合物及其盐和溶剂合物,其中X,R 1,R 2,R 3和R 3, SUP> 5具有权利要求1所示的含义,适合作为5个HT受体的配体。
-
公开(公告)号:US20120028959A1
公开(公告)日:2012-02-02
申请号:US13262640
申请日:2010-03-26
申请人: Siva Sanjeeva Rao Thunuguntla , Hosahalli Subramanya , Satish Reddy Kunnam , Sekhar Reddy Sanivaru Vijay , Chakrapani Bingi , Raviraj Kusanur , Matthias Schwarz , Michael Arlt
发明人: Siva Sanjeeva Rao Thunuguntla , Hosahalli Subramanya , Satish Reddy Kunnam , Sekhar Reddy Sanivaru Vijay , Chakrapani Bingi , Raviraj Kusanur , Matthias Schwarz , Michael Arlt
IPC分类号: A61K31/55 , A61K31/4184 , C07D263/57 , A61K31/423 , C07D409/10 , C07D403/10 , C07D417/10 , A61K31/428 , C07D401/04 , A61K31/4439 , C07D413/10 , A61K31/5377 , A61P25/00 , A61P29/00 , A61P35/00 , A61P1/00 , C07D235/18
CPC分类号: C07D209/08 , C07D235/18 , C07D401/04 , C07D401/10 , C07D403/04 , C07D409/10 , C07D413/10 , C07D417/10 , C07D471/04
摘要: The invention relates to compounds of formula (I) wherein R1, R2, X1, X2, Y, Ra, Rb, Q have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis and also in the treatment of cancer disorders.
摘要翻译: 本发明涉及式(I)化合物,其中R 1,R 2,X 1,X 2,Y,R a,R b,Q具有权利要求1中给出的含义。 在治疗自身免疫性疾病如多发性硬化以及治疗癌症中。
-
公开(公告)号:US07084164B2
公开(公告)日:2006-08-01
申请号:US11232011
申请日:2005-09-22
申请人: Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
发明人: Takahiko Tobe , Takashi Sugane , Wataru Hamaguchi , Itsuro Shimada , Kyoichi Maeno , Junji Miyata , Tetsuya Kimizuka , Takeshi Suzuki , Atsuyuki Kohara , Takuma Morita , Michael Arlt , Hartmut Greiner
IPC分类号: A61K31/41 , C07D249/08
CPC分类号: C07D249/08 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/4725 , A61K31/517 , A61K31/5377 , C07D249/10 , C07D249/12 , C07D249/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/10 , C07D405/04 , C07D405/06 , C07D405/10 , C07D405/12 , C07D405/14 , C07D409/10 , C07D413/04 , C07D413/14 , C07D417/04 , C07D417/10 , C07D495/04
摘要: The invention relates to a triazole derivative with an activity inhibiting glycine transporter and for use as a pharmaceutical drug, and a novel triazole derivative. The inventive triazole derivative has an excellent activity inhibiting glycine transporter and is useful as a therapeutic agent of dementia, schizophrenia, cognitive disorders, or cognitive disorders involved in various diseases such as Alzheimer disease, Parkinson's disease, or Huntington disease or the like, or spasm involved in diseases such as nerve degenerative diseases and cerebrovascular disorders, or the like. Particularly, the pharmaceutical drug is useful for the amelioration of learning disability of dementia and the like.
-
公开(公告)号:US5869516A
公开(公告)日:1999-02-09
申请号:US648951
申请日:1996-05-16
IPC分类号: C12N9/99 , A61K31/415 , A61K31/4152 , A61K31/4155 , A61K31/44 , A61K31/4427 , A61K31/4439 , A61K31/496 , A61K31/535 , A61K31/5377 , A61K31/63 , A61P7/02 , A61P9/00 , A61P9/10 , A61P9/12 , A61P43/00 , C07D231/20 , C07D231/22 , C07D231/24 , C07D231/26 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/10 , C07D403/12 , C07D413/12 , C07F9/6503
CPC分类号: C07D401/04 , C07D231/20 , C07D403/04
摘要: 5-Pyrazolinone derivatives of the general formula I: ##STR1## in which the R.sup.1 -R.sup.3 variables are as defined herein and the physiologically acceptable salts thereof; processes for the preparation of these compounds, and in particular their use as selective inhibitors of cGMP-specific phosphodiesterase (cGMP PDE), thus as pharmaceutically active compounds.
摘要翻译: 通式I的5-吡唑啉酮衍生物:其中R1-R3变量如本文所定义,及其生理上可接受的盐; 这些化合物的制备方法,特别是其作为cGMP特异性磷酸二酯酶(cGMP PDE)的选择性抑制剂的用途,因此作为药物活性化合物。
-
公开(公告)号:US10222139B2
公开(公告)日:2019-03-05
申请号:US13635047
申请日:2011-03-15
摘要: A retention element for a spacer plane of a pipe bundle is illustrated and described. In order to be able to provide large coherent free faces of the spacer plane with simplified assembly of the spacer plane, it is proposed that two guide elements each for receiving a pipe of the pipe bundle and a spacing element which is arranged between the guide elements be provided and that an opening for the passage of a rod-like support be provided between the guide elements.
-
-
-
-
-
-
-
-
-