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41. 发明授权

US08119676B2 Substituted benzimidazolone derivatives, medicaments comprising them and their use 有权
标题翻译：取代的苯并咪唑酮衍生物，包含它们的药物及其用途
公开(公告)号：US08119676B2
公开(公告)日：2012-02-21
申请号：US12438712
申请日：2007-08-24
申请人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Alfred Hahn, legal representative , Wilfried Hornberger , Liliane Unger , Juliana Ruiz Caro
发明人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Juliana Ruiz Caro
IPC分类号： A61K31/4184 , C07D235/24
CPC分类号： A61K31/4184 , C07D235/26
摘要： The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型苯并咪唑酮衍生物，其中取代基R 1，R 2，R 3，A 1，A 2和B如权利要求1中所定义，其组合物及其用于预防和 /或加压素依赖性疾病的治疗。

42. 发明申请

US20100152168A1 SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE 有权
标题翻译：取代的苄嘧磺隆衍生物，包括它们的药物及其用途
公开(公告)号：US20100152168A1
公开(公告)日：2010-06-17
申请号：US12438712
申请日：2007-08-24
申请人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Juliana Ruiz Caro
发明人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wolfgang Wernet , Wilfried Hornberger , Liliane Unger , Juliana Ruiz Caro
IPC分类号： A61K31/551 , C07D409/14 , C07D251/02 , C07D211/06 , C07D243/00 , A61K31/497 , A61K31/53 , A61K31/454 , A61P25/22 , A61P25/24
CPC分类号： A61K31/4184 , C07D235/26
摘要： The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型苯并咪唑酮衍生物，其中取代基R 1，R 2，R 3，A 1，A 2和B如权利要求1中所定义，其组合物及其用于预防和 /或加压素依赖性疾病的治疗。

43. 发明申请

US20120115842A1 Substituted Oxindole Derivatives, Medicaments Containing Said Derivatives and Use Thereof 审中-公开
标题翻译：取代的羟吲哚衍生物，含有所述衍生物的药物及其用途
公开(公告)号：US20120115842A1
公开(公告)日：2012-05-10
申请号：US11794582
申请日：2005-12-30
申请人： Wilfried Lubisch , Thorsten Oost , Liliane Unger , Wilfried Hornberger , Herve Geneste
发明人： Wilfried Lubisch , Thorsten Oost , Liliane Unger , Wilfried Hornberger , Herve Geneste
IPC分类号： A61K31/404 , C07D401/04 , A61K31/454 , C07D209/42 , C07D413/04 , A61K31/5377 , A61P3/10 , A61P13/00 , A61P7/00 , A61P9/12 , A61P9/04 , A61P9/10 , A61P13/12 , A61P1/00 , A61P1/06 , A61P1/16 , A61P1/04 , A61P1/08 , A61P25/22 , A61P25/28 , A61P25/18 , A61P25/00 , A61P9/00 , C07D403/04
CPC分类号： C07D209/40 , C07D401/04 , C07D403/04 , C07D403/14 , C07D413/14
摘要： The invention relates to novel oxindole derivatives of general formula (I), wherein substituents A, B, X and Y are defined as in claim 1, medicaments containing said derivatives, and the use thereof in the prophylaxis and/or treatment of vasopressin-dependent and/or oxytocin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型羟基吲哚衍生物，其中取代基A，B，X和Y如权利要求1中所定义，含有所述衍生物的药物及其在预防和/或治疗加压素依赖性中的用途和/或催产素依赖性疾病。

44. 发明授权

US07902379B2 Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them 有权
标题翻译：杂芳基取代的1,3-二氢吲哚-2-酮衍生物和含有它们的药物
公开(公告)号：US07902379B2
公开(公告)日：2011-03-08
申请号：US10574211
申请日：2004-09-30
申请人： Wilfried Lubisch , Wilfried Hornberger , Thorsten K. Oost , Daryl Richard Sauer , Liliane Unger , Wolfgang Wernet , Hervé Geneste
发明人： Wilfried Lubisch , Wilfried Hornberger , Thorsten K. Oost , Daryl Richard Sauer , Liliane Unger , Wolfgang Wernet , Hervé Geneste
IPC分类号： C07D209/02
CPC分类号： C07D401/14 , C07D401/12 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： The present invention relates to novel 1,3-dihydroindol-2-one (oxindole) derivatives of the formula (I) in which A, R3, R4, R5 R6 and R7 are defined according to claim 1, and to medicaments containing them for the treatment of diseases. In particular, the novel oxindole derivatives can be used for the control and/or prophylaxis of various vasopressin-dependent or oxytocin-dependent diseases.
摘要翻译：本发明涉及式（I）的新的1,3-二氢吲哚-2-酮（羟吲哚）衍生物，其中A，R3，R4，R5 R6和R7如权利要求1所定义，以及含有它们的药物用于治疗疾病。特别地，新型羟基吲哚衍生物可用于控制和/或预防各种加压素依赖性或催产素依赖性疾病。

45. 发明申请

US20120172335A1 SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE 有权
标题翻译：取代的苄嘧磺隆衍生物，包括它们的药物及其用途
公开(公告)号：US20120172335A1
公开(公告)日：2012-07-05
申请号：US13302194
申请日：2011-11-22
申请人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wilfried Homberger , Liliane Unger , Juliana Ruiz Caro , Wolfgang Wernet , ALfred Hahn
发明人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wilfried Homberger , Liliane Unger , Juliana Ruiz Caro , Wolfgang Wernet , ALfred Hahn
IPC分类号： A61K31/69 , A61P13/00 , A61P7/02 , A61P9/12 , A61P9/00 , A61P13/12 , A61P1/00 , A61P1/04 , A61P25/22 , A61P25/00 , A61P25/28 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/30 , A61P3/10
CPC分类号： A61K31/4184 , C07D235/26
摘要： The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型苯并咪唑酮衍生物，其中取代基R 1，R 2，R 3，A 1，A 2和B如权利要求1中所定义，其组合物及其用于预防和 /或加压素依赖性疾病的治疗。

46. 发明申请

US20110294817A1 N-[PIPERAZINYL HETARYL]ARYLSUFONAMIDE COMPOUNDS WITH AFFINITY FOR THE DOPAMINE D3 RECEPTOR 失效
标题翻译：具有多巴胺D3受体亲和性的N- [哌嗪基]维生素A亚磺酰胺化合物
公开(公告)号：US20110294817A1
公开(公告)日：2011-12-01
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 C. Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer , Sean C. Turner
IPC分类号： A61K31/496 , A61P13/12 , A61P25/00 , C07D401/04 , A61K31/4995
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。

47. 发明申请

US20090105224A1 Tetrahydrobenzazepines and their use in the modulation of the dopamine d3 receptor 失效
标题翻译：四氢苯并吖嗪及其在调节多巴胺d3受体中的用途
公开(公告)号：US20090105224A1
公开(公告)日：2009-04-23
申请号：US10583590
申请日：2004-12-17
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
IPC分类号： C07D223/16 , A61K31/55 , A61P25/00
CPC分类号： C07D223/16 , C07D409/12
摘要： The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides.The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.
摘要翻译：本发明涉及通式Ⅰ的四氢苯并吖庚因，其中变量Ar，A，B，Y，R 1和R 2具有权利要求1所示的含义，以及这些化合物的N-氧化物，生理上耐受的酸加成盐的这些化合物和N-氧化物的生理上耐受的酸加成盐。本发明还涉及药物组合物，其包含至少一种式I的四氢苯并氮杂化合物，I的物理耐受的酸加成盐，式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物，并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。

48. 发明申请

US20060160809A1 N-[(piperazinyl)hetaryl]arylsulfonamide compounds 失效
公开(公告)号：US20060160809A1
公开(公告)日：2006-07-20
申请号：US10823317
申请日：2004-04-13
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl Sauer , Sean Turner
IPC分类号： A61K31/53 , A61K31/506 , A61K31/501
CPC分类号： C07D213/76 , C07D213/74 , C07D239/69 , C07D401/04 , C07D487/08
摘要： The invention relates 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.

49. 发明授权

US08791148B2 Substituted benzimidazolone derivatives, medicaments comprising them and their use 有权
标题翻译：取代的苯并咪唑酮衍生物，包含它们的药物及其用途
公开(公告)号：US08791148B2
公开(公告)日：2014-07-29
申请号：US13302194
申请日：2011-11-22
申请人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wilfried Homberger , Liliane Unger , Juliana Ruiz Caro , Alfred Hahn
发明人： Torsten Arndt , Thorsten Oost , Wilfried Lubisch , Wilfried Homberger , Liliane Unger , Juliana Ruiz Caro , Wolfgang Wernet
IPC分类号： A61K31/4184 , C07D235/26
CPC分类号： A61K31/4184 , C07D235/26
摘要： The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
摘要翻译：本发明涉及通式（I）的新型苯并咪唑酮衍生物，其中取代基R 1，R 2，R 3，A 1，A 2和B如权利要求1中所定义，其组合物及其用于预防和 /或加压素依赖性疾病的治疗。

50. 发明授权

US08207160B2 Tetrahydrobenzazepines and their use in he modulation of the dopamine D3 receptor 失效
标题翻译：四氢苯并吖嗪及其在多巴胺D3受体调节中的应用
公开(公告)号：US08207160B2
公开(公告)日：2012-06-26
申请号：US10583590
申请日：2004-12-17
申请人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
发明人： Wilfried Braje , Andreas Haupt , Wilfried Lubisch , Roland Grandel , Karla Drescher , Herve Geneste , Liliane Unger , Daryl R. Sauer
IPC分类号： A61P25/00 , A61K31/55 , C07D223/16 , C07D409/12
CPC分类号： C07D223/16 , C07D409/12
摘要： The invention relates to tetrahydrobenzazepines of the general formula I in which the variables Ar, A, B, Y, R1 and R2 have the meanings indicated in claim 1, as well as the N-oxides of these compounds, the physiologically tolerated acid addition salts of these compounds and the physiologically tolerated acid addition salts of the N-oxides. The invention also relates to a pharmaceutical composition that comprises at least one tetrahydrobenzazepine compound of the formula I, the physically tolerated acid addition salt of I, the N-oxide of compound of the formula I and/or the physically tolerated acid addition salts of the N-oxides of I, and further to the use of a compound according to the present invention for treating disorders that respond beneficially to dopamine D3 receptor antagonists or dopamine D3 agonists. The compounds according to the invention are preferably useful for the treatment of disorders of the central nervous system such as schizophrenia and depression and for the treatment of renal function disorders.
摘要翻译：本发明涉及通式Ⅰ的四氢苯并吖庚因，其中变量Ar，A，B，Y，R 1和R 2具有权利要求1所示的含义，以及这些化合物的N-氧化物，生理上耐受的酸加成盐的这些化合物和N-氧化物的生理上耐受的酸加成盐。本发明还涉及药物组合物，其包含至少一种式I的四氢苯并氮杂化合物，I的物理耐受的酸加成盐，式I化合物的N-氧化物和/或其物理上耐受的酸加成盐 I的N-氧化物，并且进一步使用根据本发明的化合物用于治疗有益于多巴胺D3受体拮抗剂或多巴胺D3激动剂的病症。根据本发明的化合物优选可用于治疗中枢神经系统疾病如精神分裂症和抑郁症以及治疗肾功能障碍。

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