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41. 发明授权

US07834048B2 Azabicycloheptyl compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的氮杂双环庚基化合物
公开(公告)号：US07834048B2
公开(公告)日：2010-11-16
申请号：US11665421
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/403 , C07D209/52
CPC分类号： C07D401/12 , C07D209/52 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; 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-C4-alkylcarbonyl 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R 1是H，可以被C 3 -C 6环烷基取代的C 1 -C 6烷基，氟化的C 1 -C 6 - 烷基，C 3 -C 6环烷基， C 3 - C 6 - 烯基，氟化C 3 -C 6 - 烯基，甲酰基，乙酰基或丙酰基; 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R a; 其中变量Ra具有权利要求书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。

42. 发明申请

US20100152179A9 TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS 审中-公开
标题翻译：中枢神经系统疾病的治疗
公开(公告)号：US20100152179A9
公开(公告)日：2010-06-17
申请号：US12195937
申请日：2008-08-21
申请人： R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Yixian Chen , Jurgen Dinges , Karla Drescher , Peer Jacobson , Hwan-soo Jae , Ravi Kurukulasuriya , James T. Link , David J. Madar , Jyoti R. Patel , Marina A. Pliushchev , Jeffrey J. Rohde , Lynne E. Rueter , Qi Shuai , Bryan K. Sorensen , Jiahong Wang , Karsten M. Wicke , Martin Winn , Dariusz Wodka , Vince Yeh , Hong Yong
发明人： R. Scott Bitner , Kaitlin E. Browman , Michael E. Brune , Yixian Chen , Jurgen Dinges , Karla Drescher , Peer Jacobson , Hwan-soo Jae , Ravi Kurukulasuriya , James T. Link , David J. Madar , Jyoti R. Patel , Marina A. Pliushchev , Jeffrey J. Rohde , Lynne E. Rueter , Qi Shuai , Bryan K. Sorensen , Jiahong Wang , Karsten M. Wicke , Martin Winn , Dariusz Wodka , Vince Yeh , Hong Yong
IPC分类号： A61K31/496 , A61P25/00 , A61K31/5375 , A61K31/445 , A61K31/16
CPC分类号： C07D403/12 , A61K31/44 , A61K31/495 , C07D207/267 , C07D401/12 , C07D401/14
摘要： A method for treating a patient suffering from disorders and deficits of the central nervous system associated with diabetes, associated with aging and neurodegeneration, comprising attention deficit disorder in general, attention deficit hyperactivity disorder (ADHD), Alzheimer's disease (AD), mild cognitive impairment, senile dementia, AIDS dementia, neurodegeneration, depression, and schizophrenia, comprising administering to a patient in need of such treatment an effective amount of a selective inhibitor of the 11-β-hydroxysteroid dehydrogenase Type 1 enzyme activity.
摘要翻译：一种治疗患有与老化和神经变性相关的糖尿病中枢神经系统紊乱和缺陷的患者的方法，包括注意力缺陷障碍，注意力缺陷多动障碍（ADHD），阿尔茨海默病（AD），轻度认知障碍老年性痴呆，艾滋病痴呆，神经退行性疾病，抑郁症和精神分裂症，包括向需要这种治疗的患者施用有效量的11-羟基类固醇脱氢酶1型酶活性的选择性抑制剂。

43. 发明申请

US20100137280A1 AZETIDIN COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR 有权
标题翻译：适用于治疗响应调节SEROTONIN 5-HT6受体的疾病的AZETIDIN化合物
公开(公告)号：US20100137280A1
公开(公告)日：2010-06-03
申请号：US12532406
申请日：2008-03-20
申请人： Thomas Schultz, SR. , Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Matthias Mayrer
发明人： Thomas Schultz, SR. , Wilfried Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Matthias Mayrer
IPC分类号： A61K31/404 , A61K31/437 , A61K31/4184 , A61K31/416 , C07D403/10 , C07D413/02 , C07D401/14 , C07D471/04 , C07D487/04 , A61K31/506 , A61P25/00 , A61P3/04 , A61P25/30 , A61P25/18
CPC分类号： C07D471/04 , C07D403/04
摘要： The present invention relates to compounds of formula (I) wherein A is C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-hydroxyalkyl, C2-C6-alkenyl, C2-C6-halo-alkenyl, C3-C6-cycloalkyl, aryl-C1-C4-alkyl, aryl-C2-C4-alkenyl, aryl or hetaryl, is a single or double bond; X1 and X2 are N, CRx1, NRx2, or CRx3Rx4; Rx1, Rx3 and Rx4 are H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, etc. or two geminal radicals Rx3 and Rx4 together with the carbon atom to which they are bound may form a carbonyl group or a 3- to 6-membered carbocyclic or heterocyclic spiro-annulated ring; Rx2 is hydrogen, C1-C6-alkyl, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; or two vicinal radicals Rx1, Rx2, Rx3 or Rx4 together with X1 and X2 form a five- or six-membered carbocyclic or heterocyclic fused ring; Y1, Y2 and Y3 are N or CRy; Ry is H, halogen, CN, NO2, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylcarbonyl, C1-C6-haloalkyl, etc.; wherein a maximum of 3 of the radicals X1, X2, Y1, Y2 and Y3 are selected from NRx1 and N; R1 is hydrogen, C1-C6-alkyl, C1-C6-hydroxyalkyl, C1-C6-haloalkyl, etc.; R2 is C1-C4-alkyl or C1-C4-haloalkyl; n is 0, 1 or 2; physiologically tolerated acid addition salts and the N-oxides thereof, pharmaceutical composition comprising them, a method for treating medical disorders selected from diseases of the central nervous system, addiction diseases or obesity, said method comprising administering an effective amount of such compounds to a subject in need and the use of such a compound for preparing a pharmaceutical compositions.
摘要翻译：本发明涉及式（I）化合物，其中A为C 1 -C 6 - 烷基，C 1 -C 6 - 卤代烷基，C 1 -C 6羟基烷基，C 2 -C 6 - 烯基，C 2 -C 6 - 卤代烯基，C 3 -C 6 - 环烷基，芳基-C 1 -C 4烷基，芳基-C 2 -C 4 - 烯基，芳基或杂芳基，是单键或双键; X1和X2是N，CRx1，NRx2或CRx3Rx4; Rx1，Rx3和Rx4是H，卤素，CN，NO2，C1-C6-烷基，C1-C6-烷氧基，C1-C6-烷基羰基等，或两个偕根基Rx3和Rx4与它们所在的碳原子一起结合可形成羰基或3-至6-元碳环或杂环螺环状环; Rx2是氢，C1-C6-烷基，C1-C6-烷基羰基，C1-C6-卤代烷基等; 或两个连位基Rx1，Rx2，Rx3或Rx4与X1和X2一起形成五元或六元碳环或杂环稠环; Y1，Y2和Y3为N或CRy; Ry是H，卤素，CN，NO 2，C 1 -C 6 - 烷基，C 1 -C 6 - 烷氧基，C 1 -C 6 - 烷基羰基，C 1 -C 6 - 卤代烷基等; 其中基团X1，X2，Y1，Y2和Y3中的最多3个选自NRx1和N; R1是氢，C1-C6-烷基，C1-C6-羟基烷基，C1-C6-卤代烷基等; R2是C1-C4-烷基或C1-C4卤代烷基; n为0,1或2; 生理耐受的酸加成盐及其N-氧化物，包含它们的药物组合物，治疗选自中枢神经系统疾病，成瘾疾病或肥胖症的医学病症的方法，所述方法包括向受试者施用有效量的这些化合物并且使用这种化合物来制备药物组合物。

44. 发明申请

US20090143383A1 ARYLOXYETHYLAMINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO MODULATION OF THE DOPAMINE D3 RECEPTOR 有权
标题翻译：适用于治疗多巴胺D3受体调节症状的ARYLOXYYHYLAMINE化合物
公开(公告)号：US20090143383A1
公开(公告)日：2009-06-04
申请号：US12296739
申请日：2007-04-13
申请人： Roland Grandel , Wilfried Martin Braje , Andreas Haupt , Sean Colm Turner , Udo Lange , Karla Drescher , Liliane Unger
发明人： Roland Grandel , Wilfried Martin Braje , Andreas Haupt , Sean Colm Turner , Udo Lange , Karla Drescher , Liliane Unger
IPC分类号： A61K31/5377 , C07D413/02 , C07D403/02 , A61K31/44 , A61K31/506 , C07D401/02
CPC分类号： C07D213/76 , C07D239/69
摘要： The present invention relates to aryloxyethylamine compounds of the formula I and the physiologically tolerated acid addition salts thereof. The variables have the meanings given in the claims and the description. 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的芳氧基乙胺化合物及其生理上耐受的酸加成盐。变量具有权利要求书和说明书中给出的含义。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。

45. 发明申请

US20090131452A1 BENZENESULFONANILIDE 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受体调节的病症的苯并呋喃半导体化合物
公开(公告)号：US20090131452A1
公开(公告)日：2009-05-21
申请号：US12262455
申请日：2008-10-31
申请人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
发明人： Wilfried Martin Braje , Sean Colm Turner , Andreas Haupt , Udo Lange , Karla Drescher , Karsten Wicke , Liliane Unger , Mario Mezler , Wolfgang Wernet , Matthias Mayrer , Ana Jongen-Relo , Anton Bespalov , Min Zhang
IPC分类号： A61K31/496 , C07D295/182 , C07D405/12 , A61P25/00 , A61K31/495
CPC分类号： C07D295/12 , C07D405/12
摘要： The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I′ and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are particularly suitable, for treating diseases that respond to modulation of the serotonin 5-HT6 receptor. wherein R1 is hydrogen or methyl R2 is hydrogen or methyl R3 hydrogen, fluorine C1-C2 alkoxy or fluorinated C1-C2 alkoxy; R4 is hydrogen, C1-C4 alkyl or fluorinated C1-C4 alkyl; R5 is hydrogen, fluorine, C1-C2 alkyl fluorinated C1-C2 alkyl C1-C2 alkoxy or fluorinated C1-C2 alkoxy; and R6 is hydrogen, fluorine or chlorine.
摘要翻译：本发明涉及式I和I'的新型苯磺酰苯胺化合物和生理上耐受的酸加成盐及其N-氧化物。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R1是氢或甲基R2是氢或甲基R3氢，氟C1-C2烷氧基或氟化C1-C2烷氧基; R4是氢，C1-C4烷基或氟化C1-C4烷基; R5是氢，氟，C1-C2烷基氟化C1-C2烷基C1-C2烷氧基或氟化C1-C2烷氧基; R6是氢，氟或氯。

46. 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。

47. 发明申请

US20090048326A1 Azabicycloheptyl compounds suitable for treating disorders that respond to modulation of the dopamine D3 receptor 有权
标题翻译：适用于治疗对多巴胺D3受体调节作出反应的疾病的氮杂双环庚基化合物
公开(公告)号：US20090048326A1
公开(公告)日：2009-02-19
申请号：US11665421
申请日：2005-10-14
申请人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
发明人： Karla Drescher , Andreas Haupt , Liliane Unger , Sean C. Turner , Wilfried Braje , Roland Grandel
IPC分类号： A61K31/403 , A61P25/00 , C07D209/52
CPC分类号： C07D401/12 , C07D209/52 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to a compound of the formula (I) wherein R1 is H, C1-C6-alkyl which may be substituted by C3-C6-cycloalkyl, fluorinated C1-C6-alkyl, C3-C6-cycloalkyl, fluorinated C3-C6-cycloalkyl, C3-C6-alkenyl, fluorinated C3-C6-alkenyl, formyl, acetyl or propionyl; 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-C4-alkylcarbonyl 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R 1是H，可以被C 3 -C 6环烷基取代的C 1 -C 6烷基，氟化的C 1 -C 6 - 烷基，C 3 -C 6环烷基， C 3 - C 6 - 烯基，氟化C 3 -C 6 - 烯基，甲酰基，乙酰基或丙酰基; 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R a; 其中变量Ra具有权利要求书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。

48. 发明申请

US20080171751A1 Triazole 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受体调节反应的三唑化合物
公开(公告)号：US20080171751A1
公开(公告)日：2008-07-17
申请号：US11792596
申请日：2005-12-01
申请人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
发明人： Liliane Unger , Andreas Haupt , Armin Beyerbach , Karla Drescher , Wilfried Braje , John Darbyshire , Sean C. Turner , Gisela Backfisch
IPC分类号： A61K31/496 , C07D403/14 , A61P25/00
CPC分类号： C07D403/12
摘要： The invention relates to compounds of the formula I: wherein n is 1 or 2, Ar is a C-bound 1,2,4-triazol radical which carries a radical R1 on the remaining carbon atom and a radical R1a on one of the nitrogen atoms; R1 is hydrogen, C1-C6 alkyl, C3-C6 cycloalkyl, C1-C4 alkoxymethyl, fluorinated C1-C6 alkyl, fluorinated C3-C6 cycloalkyl, fluorinated C1-C4 alkoxymethyl, or optionally substituted phenyl or 5- or 6-membered heteroaryl; R1a is hydrogen or C1-C4 alkyl; and R2 is C1-C6 alkyl, C3-C6 cycloalkyl, fluorinated C1-C6 alkyl or fluorinated C3-C6 cycloalkyl; and to the physiologically tolerated acid addition salts of these compounds. The invention also relates to a pharmaceutical composition that comprises at least one triazole 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 triazole 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n是1或2，Ar是在剩余的碳原子上带有自由基R 1的C结合的1,2,4-三唑基，和其中一个氮原子上的基团R 1a， R 1是氢，C 1 -C 6烷基，C 3 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，氟化C 1 -C 6烷基，氟化C 1 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基，氟化C 1 -C 4烷氧基甲基或任选取代的苯基或5-或6位的C 1 -C 6烷基，杂芳基; R 1a是氢或C 1 -C 4烷基; R 2是C 1 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，C 3 -C 6烷基，氟化C 1 -C 6烷基或氟化C 3 -C 6环烷基; 以及这些化合物的生理上耐受的酸加成盐。本发明还涉及一种药物组合物，其包含至少一种式I的三唑化合物和/或其至少一种生理上耐受的酸加成盐，还涉及治疗有益于多巴胺D 3的病症的方法受体拮抗剂或多巴胺D 3激动剂，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III的三唑化合物或生理耐受的酸加成盐。

49. 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.

50. 发明授权

US6124294A Triazole compounds and the use thereof 失效
标题翻译：三唑化合物及其用途
公开(公告)号：US6124294A
公开(公告)日：2000-09-26
申请号：US765916
申请日：1997-01-14
申请人： Beate Hellendahl , Annegret Lansky , Rainer Munschauer , Siegfried Bialojan , Liliane Unger , Hans-Jurgen Teschendorf , Karsten Wicke , Karla Drescher
发明人： Beate Hellendahl , Annegret Lansky , Rainer Munschauer , Siegfried Bialojan , Liliane Unger , Hans-Jurgen Teschendorf , Karsten Wicke , Karla Drescher
IPC分类号： C07D249/08 , A61K31/41 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/505 , A61K31/53 , A61P1/08 , A61P25/18 , A61P25/20 , A61P25/24 , A61P25/26 , C07D249/12 , C07D249/14 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14
CPC分类号： C07D403/12 , C07D249/12
摘要： The present invention relates to triazole compounds of the following formula: where R.sup.1, R.sup.2, A, B and Ar have the meanings stated in the description. The compounds according to the invention have a high affinity for the dopamine D3 receptor and can therefore be used to treat disorders which respond to dopamine D.sub.3 ligands.
摘要翻译： PCT No.PCT / EP95 / 02781 Sec。 371日期1997年1月14日 102（e）日期1997年1月14日PCT提交1995年7月14日PCT公布。公开号WO96 / 02520 日期1996年2月1日本发明涉及下式的三唑化合物：其中R1，R2，A，B和Ar具有说明书中所述的含义。根据本发明的化合物对多巴胺D3受体具有高亲和力，因此可用于治疗对多巴胺D3配体作出反应的病症。

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