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1. 发明专利

HRP980125A2 DOLASTATIN-15 DERIVATIVES IN COMBINATION WITH TAXANES 未知
公开(公告)号：HRP980125A2
公开(公告)日：1999-02-28
申请号：HRP980125
申请日：1998-03-10
申请人： ANDREAS HAUPT
发明人： HAUPT ANDREAS
IPC分类号： A61K38/00 , A61K31/337 , A61K38/07 , A61K38/08 , A61K38/15 , A61P35/00 , C07K5/08 , C07K5/10 , C07K7/00 , A61K38/04 , A61K31/335
摘要： The present invention provides compositions and methods for the treatment of cancer in a subject wherein compounds of Formula I as defined herein in combination with paclitaxel, taxotere or modified taxane or taxoid analogs provide enhanced anticancer effects over the effects achieved with the individual compounds.

2. 发明授权

US08921406B2 5-ring heteroaromatic compounds and their use as binding partners for 5-HT5 receptors 有权
标题翻译： 5环杂芳族化合物及其作为5-HT5受体的结合伴侣的用途
公开(公告)号：US08921406B2
公开(公告)日：2014-12-30
申请号：US11990731
申请日：2006-08-21
申请人： Wilhelm Amberg , Astrid Netz , Andreas Kling , Michael Ochse , Udo Lange , Andreas Haupt , Francisco Javier Garcia-Ladona , Alfred Hahn
发明人： Wilhelm Amberg , Astrid Netz , Andreas Kling , Michael Ochse , Udo Lange , Andreas Haupt , Francisco Javier Garcia-Ladona , Wolfgang Wernet
IPC分类号： A61K31/415 , A61K31/4168 , A61K31/4192 , A61K31/4196 , C07D233/88 , C07D231/38 , C07D249/04 , C07D249/14 , C07D405/04 , C07D409/04 , C07D233/70
CPC分类号： C07D417/04 , C07D231/38 , C07D233/70 , C07D233/88 , C07D249/14 , C07D405/04 , C07D409/04 , C07D413/04
摘要： The invention relates to 5-ring heteroaromatic compounds of general formula (I), their use for the treatment and/or prevention of diseases, and medicaments containing same.
摘要翻译：本发明涉及通式（I）的5-环杂芳族化合物，其用于治疗和/或预防疾病的用途，以及含有它们的药物。

3. 发明授权

US08492540B2 1,2,4,-triazin-3,5-dione compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译： 1,2,4-三嗪-3,5-二酮化合物，适用于治疗对多巴胺D3受体调节作用的疾病
公开(公告)号：US08492540B2
公开(公告)日：2013-07-23
申请号：US12740714
申请日：2008-10-31
申请人： Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Hervé Geneste , Karla Drescher , Liliane Unger , Ana Lucia Relo , Anton Bespalov
发明人： Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Hervé Geneste , Karla Drescher , Liliane Unger , Ana Lucia Relo , Anton Bespalov
IPC分类号： C07D253/075 , C07D403/14 , A61K31/53 , A61P25/18 , A61P25/30 , A61P25/00
CPC分类号： C07D403/12
摘要： The invention relates to compounds of the formula I: wherein A is a saturated or unsaturated hydrocarbon chain having a chain length of 4 to 6 carbon atoms, the hydrocarbon chain being unsubstituted or substituted by 1, 2 or 3 methyl groups; R1 is selected from the group consisting of hydrogen, C1-C3 alkyl and fluorinated C1-C3 alkyl; R2 is hydrogen, halogen, cyano, C1-C3 alkyl, C1-C3 alkoxy, fluorinated C1-C3 alkyl or fluorinated C1-C3 alkoxy; R3 is selected from the group consisting of branched C4-C6 alkyl and C3-C6 cycloalkyl, and R4 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C3-alkyl and fluorinated C3-C6 cycloalkyl. and the physiologically tolerated salts of these compounds and the N-oxides thereof. The invention also relates to a pharmaceutical composition that comprises at least one compound of the formula I and/or at least one physiologically tolerated acid addition salt thereof, and further to a method for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists, said method comprising administering an effective amount of at least one compound or physiologically tolerated acid addition salt of the formula I to a subject in need thereof.
摘要翻译：本发明涉及式I化合物：其中A是链长为4-6个碳原子的饱和或不饱和烃链，烃链未被取代或被1,2或3个甲基取代; R1选自氢，C1-C3烷基和氟化C1-C3烷基; R2是氢，卤素，氰基，C1-C3烷基，C1-C3烷氧基，氟化C1-C3烷基或氟化C1-C3烷氧基; R3选自支链C4-C6烷基和C3-C6环烷基，R4为C1-C6烷基，C3-C6环烷基，氟化C1-C3-烷基和氟化C3-C6环烷基。以及这些化合物的生理上耐受的盐及其N-氧化物。本发明还涉及包含至少一种式I化合物和/或其至少一种生理上耐受的酸加成盐的药物组合物，还涉及治疗有益于多巴胺D3受体拮抗剂或多巴胺D3的病症的方法所述方法包括向有需要的受试者施用有效量的至少一种式I化合物或生理学上耐受的酸加成盐。

4. 发明授权

US08476275B2 N-[piperazinyl hetaryl]arylsufonamide compounds with affinity for the dopamine D3 receptor 失效
标题翻译：对多巴胺D3受体具有亲和力的N- [哌嗪基杂芳基]芳基磺酰胺化合物
公开(公告)号：US08476275B2
公开(公告)日：2013-07-02
申请号：US13117269
申请日：2011-05-27
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean Colm Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean Colm Turner
IPC分类号： A61K31/496 , A61K31/506 , C07D213/72 , C07D213/74 , C07D239/48
CPC分类号： C07D213/74 , C07D213/76 , C07D239/48 , C07D239/50 , C07D403/04 , C07D403/14 , C07D487/08
摘要： The invention related to N-[(piperazinyl)hetaryl]arylsulfonamide compounds of the general formula (I) in which Q is a bivalent, 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Ra which is/are selected, independently of each other, from halogen, CN, NO2, CO2R4, COR5, C1-C4-alkyl and C1-C4-haloalkyl; Ar is phenyl or a 6-membered heteroaromatic radical which possesses 1 or 2 N atoms as ring members and which optionally carries one or two substituents Rb, which is/are selected from halogen, NO2, CN, CO2R4, COR5, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl and C1-C4-haloalkyl, with it also being possible for two radicals Rb which are bonded to adjacent C atoms of Ar to be together C3-C4-alkylene; R1 is hydrogen, C1-C4-alkyl, C1-C4-haloalkyl, C3-C6-cycloalkyl, C3-C6-cycloalkyl-C1-C4-alkyl, C1-C4-hydroxyalkyl, C1-C4-alkoxy-C1-C4-alkyl, C3-C4-alkenyl or C3-C4-alkynyl; with the radicals n, R1, R2, R3, R4 and R5 having the meanings given in the patent claims, to the N-oxides and to the physiologically tolerated acid addition salts of these compounds and to pharmaceutical compositions which comprise at least one N-[(piperazinyl)hetaryl]arylsulfonamide compound as claimed in one of claims 1 to 10 and/or at least one physiologically tolerated acid addition salt of I and/or an N-oxide of I, where appropriate together with physiologically acceptable carriers and/or auxiliary substances for treating diseases which respond to influencing by dopamine D3 receptor antagonists or agonists, in particular for treating diseases of the central nervous system and disturbances of kidney function.
摘要翻译：本发明涉及通式（I）的N - [（哌嗪基）杂芳基]芳基磺酰胺化合物，其中Q是具有1或2个N原子作为环成员的二价，6元杂芳族基团，并且任选地带有一个或两个被卤素，CN，NO 2，CO 2 R 4，COR 5，C 1 -C 4 - 烷基和C 1 -C 4卤代烷基独立地选择的取代基R a; Ar是苯基或6元杂芳族基，其具有1或2个N原子作为环成员，并且任选地带有一个或两个选自卤素，NO 2，CN，CO 2 R 4，COR 5，C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 炔基，C 3 -C 6 - 环烷基，C 3 -C 6 - 环烷基-C 1 -C 4 - 烷基和C 1 -C 4卤代烷基，与Ar的相邻C原子一起C3-C4-亚烷基; R 1是氢，C 1 -C 4烷基，C 1 -C 4卤代烷基，C 3 -C 6环烷基，C 3 -C 6环烷基-C 1 -C 4烷基，C 1 -C 4羟烷基，C 1 -C 4烷氧基-C 1 -C 4 - 烷基，C 3 -C 4 - 烯基或C 3 -C 4 - 炔基; 具有如专利权利要求中给出的含义的基团n，R 1，R 2，R 3，R 4和R 5与这些化合物的N-氧化物和生理上耐受的酸加成盐以及包含至少一种N- 和/或至少一种I的生理学耐受的酸加成盐和/或I的N-氧化物，其中适宜地与生理上可接受的载体和/或用于治疗对多巴胺D3受体拮抗剂或激动剂影响的疾病的辅助物质，特别是用于治疗中枢神经系统疾病和肾功能障碍。

5. 发明授权

US08440694B2 Quinoline compounds suitable for treating disorders that respond to modulation of the serotonin-5-HT6 receptor 有权
标题翻译：喹啉化合物适用于治疗对血清素-5-HT6受体调节作用的疾病
公开(公告)号：US08440694B2
公开(公告)日：2013-05-14
申请号：US13613344
申请日：2012-09-13
申请人： Sean Colm Turner , Wilfried Braje , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Matthias Mayrer , Andrea Hager-Wernet
发明人： Sean Colm Turner , Wilfried Braje , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Matthias Mayrer , Wolfgang Wernet
IPC分类号： A61K31/47 , A61P3/04 , A61P25/00 , A61P25/18 , A61P25/28 , A61P25/30 , C07D215/36
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The present invention relates to novel quinoline compounds of the formula (I) and to the salts thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. In formula (I) R is a moiety of the formula (R) wherein * indicates the binding site to the quinolinyl radical and wherein A, B, X′, Y, Q, R1, R2, R3, R4, R5, m, n, p, q, Ra, Rb, X and Ar are as defined in claim 1.
摘要翻译：本发明涉及式（I）的新颖喹啉化合物及其盐。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。在式（I）中，R是式（R）的部分，其中*表示与喹啉基的结合位点，其中A，B，X'，Y，Q，R 1，R 2，R 3，R 4，R 5， n，p，q，Ra，Rb，X和Ar如权利要求1所定义。

6. 发明申请

US20130018047A1 N-PHENYL-(PIPERAZINYL OR HOMOPIPERAZINYL)-BENZENESULFONAMIDE OR BENZENESULFONYL-PHENYL-(PIPERAZINE OR HOMOPIPERAZINE) COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 审中-公开
标题翻译： N-苯基 - （哌嗪酰基或对羟基苯甲酰基） - 苯磺酰胺或苯并呋喃基 - 苯基 - （哌嗪或或邻苯二酚）化合物，适用于治疗调节SEROTONIN 5-HT6受体的病症
公开(公告)号：US20130018047A1
公开(公告)日：2013-01-17
申请号：US13618865
申请日：2012-09-14
申请人： Andreas Haupt , Frauke Pohlki , Karla Drescher , Karsten Wicke , Liliane Unger , Ana-Lucia Relo , Anton Bespalov , Barbara Vogg , Gisela Backfisch , Juergen Delzer , Min Zhang , Yanbin Lao
发明人： Andreas Haupt , Frauke Pohlki , Karla Drescher , Karsten Wicke , Liliane Unger , Ana-Lucia Relo , Anton Bespalov , Barbara Vogg , Gisela Backfisch , Juergen Delzer , Min Zhang , Yanbin Lao
IPC分类号： A61K31/495 , A61K31/496 , A61P25/30 , A61K31/551
CPC分类号： C07D241/04 , C07D243/08 , C07D295/096 , C07D317/46
摘要： The present invention relates to N-phenyl-(piperazinyl or homopiperazinyl)-benzenesulfonamide or benzenesulfonyl-phenyl-(piperazine or homopiperazine) compounds, pharmaceutical compositions containing them, and their use in therapy. The compounds possess valuable therapeutic properties and are particularly suitable for treating diseases that respond to modulation of the serotonin 5-HT6 receptor.
摘要翻译：本发明涉及N-苯基 - （哌嗪基或高哌嗪基） - 苯磺酰胺或苯磺酰基 - 苯基 - （哌嗪或高哌嗪）化合物，含有它们的药物组合物及其在治疗中的用途。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT6受体的调节作出反应的疾病。

7. 发明授权

US08008488B2 Pyrimidin-2-one compounds and their use as dopamine D3 receptor ligands 有权
标题翻译：嘧啶-2-酮化合物及其作为多巴胺D3受体配体的用途
公开(公告)号：US08008488B2
公开(公告)日：2011-08-30
申请号：US10548931
申请日：2004-03-12
申请人： Hervé Geneste , Andreas Kling , Wilfried Braje , Andreas Haupt , Liliane Unger
发明人： Hervé Geneste , Andreas Kling , Wilfried Braje , Andreas Haupt , Liliane Unger
IPC分类号： C07D403/06 , C07D403/14 , C07D401/06 , C07D401/14 , A61K31/505 , A61K31/506 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/22 , A61P25/30
CPC分类号： C07D239/36 , C07D239/52 , C07D239/54 , C07D239/553 , C07D239/56 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/14
摘要： The invention relates to pyrimidin 2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula, A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of the formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X—Y can also jointly represent C═CH, C═CH—CH2 or CH—CH═CH; R1 and R2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases which respond to the influence of dopamine D3 receptor ligands.
摘要翻译：除了（I）的衍生物和互变异构体以及所述化合物的生理学上可接受的盐之外，本发明涉及通式（I）的嘧啶-2-酮化合物。在所述式中，A表示可以具有双键或三键的直链或支链C 3 -C 6烯基和/或不与嘧啶酮环的氮原子相邻并且选自O，S， C（O），NR 3，C（O）NR 3，NR 3 C（O），OC（O）和C（O）O; B表示式（II）的基团，其中X表示CH2或N，Y表示CH2或CH2CH2，或X-Y也可共同表示C = CH，C = CH-CH 2或CH-CH = CH ; R1和R2定义为在说明书和权利要求书中引用的; 并且Ar表示任选取代的芳族基团。本发明还涉及含有至少一种化合物（I）和所述化合物的互变异构体，衍生物和/或酸加成盐，任选地与生理上可接受的载体和/或辅助剂一起的药剂。本发明还涉及式（I）化合物及其互变异构体，衍生物和药理学上可接受的酸加成盐的用途，用于制备用于治疗对多巴胺D3受体配体的影响作出反应的疾病的药剂。

8. 发明申请

US20110160176A1 HETEROCYCLIC COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 失效
标题翻译：适用于治疗多巴胺D3受体调节障碍的异种化合物
公开(公告)号：US20110160176A1
公开(公告)日：2011-06-30
申请号：US12868480
申请日：2010-08-25
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry , Gisela Backfisch , Armin Beyerbach , Wilfried Lubisch
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel , Christophe Henry , Gisela Backfisch , Armin Beyerbach , Wilfried Lubisch
IPC分类号： A61K31/397 , C07D207/08 , A61K31/40 , C07D401/02 , C07D205/02 , C07D403/02 , A61K31/506 , C07D417/02 , A61K31/433 , C07D413/14 , A61K31/422 , C07D211/08 , A61K31/445 , A61P25/28
CPC分类号： C07D413/14 , C07D205/04 , C07D207/09 , C07D211/28 , C07D401/04 , C07D401/12 , C07D403/04 , C07D405/12 , C07D409/12 , C07D413/10 , C07D413/12
摘要： The invention relates to compounds of the formula (I) wherein n is 0, 1 or 2; G is CH2 or CHR3; R1 is H, C,-C6-alkyl, C,-C6-alkyl substituted by C3-C6-cycloalkyl, C1-C6-hydroxyalkyl, fluorinated C,-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6 alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; R2, R3 and R4 are, independently of each other, H, methyl, fluoromethyl, difluoromethyl, or trifluoromethyl; A is phenylene, pyridylene, pyrimidylene, pyrazinylene, pyridazinylene or thiophenylene, which can be substituted by one or more substituents selected from halogen, methyl, methoxy and CF3; E is NR5 or CH2, wherein R5 is H or C1-C3-alkyl; Ar is a cyclic radical selected from the group consisting of phenyl, a 5- or 6-membered heteroaromatic radical comprising as ring members 1, 2 or 3 heteroatoms selected from N, O and S and a phenyl ring fused to a saturated or unsaturated 5- or 6-membered carbocyclic or heterocyclic ring, where the heterocyclic ring comprises as ring members 1, 2 or 3 heteroatoms selected from N, O and S and/or 1, 2 or 3 heteroatom-containing groups each independently selected from NR8, where R8 is H, C1-C4-alkyl, fluorinated C1-C4-alkyl, C1-C4alkylcarbonyl or fluorinated C1-C4-alkylcarbonyl, and where the cyclic radical Ar may carry 1, 2 or 3 substituents Ra, wherein the variable Ra has the meanings given in the claims and in the description; and physiologically tolerated acid addition salts thereof. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.
摘要翻译：本发明涉及式（I）化合物，其中n为0,1或2; G是CH 2或CHR 3; R 1是被C 3 -C 6 - 环烷基取代的C 1 -C 6 - 烷基，C 1 -C 6 - 烷基，C 1 -C 6羟基烷基，氟化C 1 -C 6 - 烷基，C 3 -C 6环烷基，氟化C 3 -C 6 - 环烷基，C3-C6烯基，氟化C3-C6-烯基，甲酰基，乙酰基或丙酰基; R2，R3和R4彼此独立地为H，甲基，氟甲基，二氟甲基或三氟甲基; A是可以被一个或多个选自卤素，甲基，甲氧基和CF 3的取代基取代的亚苯基，亚吡啶基，亚嘧啶基，吡嗪基，哒嗪基或噻吩基; E是NR5或CH2，其中R5是H或C1-C3-烷基; Ar是选自苯基，5或6元杂芳族基团的环状基团，其包含选自N，O和S的环成员1,2或3个杂原子和与饱和或不饱和5 - 或6-元碳环或杂环，其中杂环包含作为环成员1,2或3个选自N，O和S的杂原子和/或1,2或3个各自独立地选自NR8的含杂原子的基团，其中 R8是H，C1-C4-烷基，氟化C1-C4-烷基，C1-C4烷基羰基或氟化C1-C4-烷基羰基，其中环状基团Ar可以带有1,2或3个取代基Ra，其中变量Ra具有在权利要求和说明书中给出的含义; 和其生理学耐受的酸加成盐。本发明还涉及式I化合物或其药学上可接受的盐在制备用于治疗易受多巴胺D3受体配体治疗的医学疾病的药物组合物中的用途。

9. 发明申请

US20110098235A1 ANTINEOPLASTIC PEPTIDES 有权
标题翻译：抗生素PEPTIDES
公开(公告)号：US20110098235A1
公开(公告)日：2011-04-28
申请号：US12869314
申请日：2010-08-26
申请人： Wilhelm AMBERG , Teresa BARLOZZARI , Harald BERNARD , Ernst BUSCHMANN , Andreas HAUPT , Hans-Guenther HEGE , Bernd JANSSEN , Andreas KLING , Helmut LIETZ , Kurt RITTER , Martina ULLRICH , Jürgen WEYMANN , Thomas ZIERKE
发明人： Wilhelm AMBERG , Teresa BARLOZZARI , Harald BERNARD , Ernst BUSCHMANN , Andreas HAUPT , Hans-Guenther HEGE , Bernd JANSSEN , Andreas KLING , Helmut LIETZ , Kurt RITTER , Martina ULLRICH , Jürgen WEYMANN , Thomas ZIERKE
IPC分类号： A61K38/08 , A61P35/00
CPC分类号： C07K7/06 , A61K38/00 , C07K5/101 , C07K7/02
摘要： The present invention provides antineoplastic peptides of formula I, R1R2N-CHX-CO-A-B-D-E-(G)S-K I wherein R1, R2, X, A, B, D, G, K and s have the meanings stated in the description. The compounds have antineoplastic activity.
摘要翻译：本发明提供式I的抗肿瘤肽，R1R2N-CHX-CO-A-B-D-E-（G）S-K I，其中R1，R2，X，A，B，D，G，K和s具有说明书中所述的含义。该化合物具有抗肿瘤活性。

10. 发明申请

US20110009380A1 QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译：适用于治疗依托莫司汀5-HT6受体调节的病症的喹啉化合物
公开(公告)号：US20110009380A1
公开(公告)日：2011-01-13
申请号：US12532407
申请日：2008-03-23
申请人： Sean Colm Turner , Andreas Haupt , Wilfried Braje , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Alfred Hahn , Matthias Mayrer
发明人： Sean Colm Turner , Andreas Haupt , Wilfried Braje , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Alfred Hahn , Matthias Mayrer
IPC分类号： A61K31/4709 , C07D401/02 , A61K31/4725 , C07D401/14 , A61P25/00 , A61P25/28 , A61P25/18
CPC分类号： C07D401/04 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to novel quinoline compounds. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R is a moiety of the formula wherein A, R1 to R4 are as defined in the claims and the specification, n is 0, 1 or 2; m is 0, 1, 2 or 3; Ra, Rb are independently selected from the group consisting of halogen, CN, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C(O)Raa, C(O)NRccRbb and NRccRbb; X is CH2, C(O), S, S(O) or S(O)2; which is located in the 3- or 4-position of the quinoline ring; Ar is a radical Ar1, Ar2—Ar3 or Ar2—O—Ar3, wherein Ar1, Ar2 and Ar3 are each independently selected from the group consisting of aryl or hetaryl wherein aryl or hetaryl moieties may be unsubstituted or may carry 1, 2, 3 substituents Rx, wherein and physiologically tolerated acid addition salts and the N-oxides thereof.
摘要翻译：本发明涉及新颖的喹啉化合物。该化合物具有有价值的治疗特性，特别适用于治疗对血清素5-HT 6受体调节作出反应的疾病。其中R是下式的部分，其中A，R 1至R 4如权利要求和说明书中所定义，n为0,1或2; m为0,1,2或3; R a，R b独立地选自卤素，CN，C 1 -C 4 - 烷基，C 1 -C 4卤代烷基，C 1 -C 4 - 烷氧基，C 1 -C 4卤代烷氧基，C（O）R aa，C（O）NR c R b b 和NRccRbb; X是CH 2，C（O），S，S（O）或S（O）2; 其位于喹啉环的3-或4-位; Ar是Ar1，Ar2-Ar3或Ar2-O-Ar3基团，其中Ar1，Ar2和Ar3各自独立地选自芳基或杂芳基，其中芳基或杂芳基部分可以是未取代的或可以携带1,2,3 取代基Rx，其中和生理上耐受的酸加成盐及其N-氧化物。

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