专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

51. 发明授权

US5910586A Tricyclic aminoalkylcarboxamides; dopamine D.sub.3 receptor subtype specific ligands 失效
标题翻译：三环氨基烷基酰胺; 多巴胺D3受体亚型特异性配体
公开(公告)号：US5910586A
公开(公告)日：1999-06-08
申请号：US965275
申请日：1997-11-06
申请人： Xi Chen , Jun Yuan , Andrew Thurkauf
发明人： Xi Chen , Jun Yuan , Andrew Thurkauf
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61K31/473 , A61K31/495 , A61K31/535 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07D221/10 , C07D401/12 , C07D409/12 , C07D471/04 , C07D498/04 , C07D241/38 , C07D273/04 , C07D285/15
CPC分类号： C07D401/12 , C07D221/10 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R.sub.1 -R.sub.4 represent organic or inorganic groups;A represents an alkylene group of 2 to 6 carbon atoms optionally substituted with one or more, alkyl groups having from 1 to 4 carbon atoms;Y represents methylene, oxygen, sulfur, or NH; andX is either N, C or CH,which compounds are, useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
摘要翻译：公开了下式的化合物或其药学上可接受的酸加成盐，其中：R 1 -R 4表示有机或无机基团; A表示任选被一个或多个具有1至4个碳原子的烷基取代的2至6个碳原子的亚烷基; Y表示亚甲基，氧，硫或NH; X是N，C或CH，这些化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的药物滥用和强迫症。此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

52. 发明授权

US5688950A Tricyclic aminoalkylcarboxamides; novel dopamine D.sub.3 receptor subtype specific ligands 失效
标题翻译：三环氨基烷基酰胺; 新型多巴胺D3受体亚型特异性配体
公开(公告)号：US5688950A
公开(公告)日：1997-11-18
申请号：US636662
申请日：1996-04-23
申请人： Xi Chen , Jun Yuan , Andrew Thurkauf
发明人： Xi Chen , Jun Yuan , Andrew Thurkauf
IPC分类号： A61K31/44 , A61K31/4427 , A61K31/4433 , A61K31/47 , A61K31/473 , A61K31/495 , A61K31/535 , A61P25/00 , A61P25/16 , A61P25/18 , A61P25/24 , A61P25/28 , A61P43/00 , C07D221/10 , C07D401/12 , C07D409/12 , C07D471/04 , C07D498/04 , C07D221/06 , C07D241/36 , C07D241/40
CPC分类号： C07D401/12 , C07D221/10 , C07D409/12 , C07D471/04
摘要： Disclosed are compounds of the formula: ##STR1## or the pharmaceutically acceptable acid addition salts thereof wherein: R1-R.sub.4 represent organic or inorganic groups; A represents an alkylene group of 2 to 6 carbon atoms optionally substituted with one or more alkyl groups having from 1 to 4 carbon atoms;Y represents methylene, oxygen, sulfur, or NH; and X is either N, C or CH, which compounds are useful in the treatment of affective disorders such as schizophrenia, depression, Alzheimer's disease, movement disorders such as Parkinsonism and dystonia, and other disorders which respond to dopaminergic blockade such as substance abuse and obsessive compulsive disorders. Further, compounds of this invention may be useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents.
摘要翻译：公开了下式的化合物或其药学上可接受的酸加成盐，其中：R 1 -R 4表示有机或无机基团; A表示任选被一个或多个具有1至4个碳原子的烷基取代的2至6个碳原子的亚烷基; Y表示亚甲基，氧，硫或NH; X是N，C或CH，这些化合物可用于治疗情感障碍如精神分裂症，抑郁症，阿尔茨海默氏病，运动障碍如帕金森综合征和肌张力障碍，以及其他对多巴胺能阻滞作用的药物滥用等疾病，强迫症强迫症此外，本发明的化合物可用于治疗与使用常规精神抑制剂相关的锥体束外副作用。

53. 发明授权

US5646279A Substituted 4-piperazinylmethyl 2-phenylimidazoles; dopamine receptor subtype specific ligands 失效
标题翻译：取代的4-哌嗪基甲基2-苯基咪唑; 多巴胺受体亚型特异性配体
公开(公告)号：US5646279A
公开(公告)日：1997-07-08
申请号：US457036
申请日：1995-06-01
申请人： Andrew Thurkauf , Alan Hutchison
发明人： Andrew Thurkauf , Alan Hutchison
IPC分类号： C07D233/54 , C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/04 , A61K31/415 , C07D403/06
CPC分类号： C07D233/64 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12
摘要： Disclosed are compounds and the pharmaceutically acceptable salts thereof useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism and useful in treating the extrapyramidal side effects associated with the use of conventional neuroleptic agents, which compounds have the formula: ##STR1## where R.sub.1 and R.sub.2 are independently represent hydrogen or inorganic groups.
摘要翻译：公开了可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征的化合物及其药学上可接受的盐，并且可用于治疗与使用常规精神抑制剂相关的锥体束外副作用，其中化合物具有下式：其中R 1和R 2独立地表示氢或无机基团。

54. 发明授权

US5597920A Gabaa receptor subtypes and methods for screening drug compounds using imidazoquinoxalines and pyrrolopyrimidines to bind to gabaa receptor subtypes 失效
标题翻译： Gabaa受体亚型和使用咪唑并喹啉和吡咯并嘧啶结合gabaa受体亚型筛选药物化合物的方法
公开(公告)号：US5597920A
公开(公告)日：1997-01-28
申请号：US876050
申请日：1992-04-30
申请人： Kenneth Shaw , Alan Hutchison , Andrew Thurkauf , John Tallman
发明人： Kenneth Shaw , Alan Hutchison , Andrew Thurkauf , John Tallman
IPC分类号： G01N33/53 , A61K31/495 , A61K31/505 , A61P25/08 , A61P25/20 , A61P25/28 , C07B59/00 , C07D487/04 , G01N33/534 , G01N33/566 , G01N33/94 , C07D487/06 , C07D487/02
CPC分类号： G01N33/9426 , C07B59/002 , G01N33/566 , G01N33/948 , G01N2500/20
摘要： The present invention provides methods for screening drug compounds utilizing compounds of formulas I and II, where formulas I and II are ##STR1## and the pharmaceutically acceptable salts thereof where: R.sub.1, R.sub.2, R.sub.3, and R.sub.4 represent hydrogen, halogen, alkyl or alkoxy substituents;R5 is hydrogen or lower alkyl;X and Y represent hydrogen, halogen, alkyl or alkoxy substituents; andZ is hydrogen or fluorine.The invention also provides tritium or iodine isotope radiolabeled compounds of the formulas I and II radiolabeled with tritium or isotopes of iodine.The invention further provides novel GABAa receptor subtypes which specifically bind to compounds of formulas I or II.The invention also provides GABAa receptor subtypes which are bound in situ to a compound of formula I or II.The compounds provided herein bind selectively to a novel subtype of the GABAa binding site. Selective interaction of ligands at this unique receptor population results in pharmacological specificity which may lead to superior anxiolytics, cognition enhancers, anticonvulsants and sedative hypnotics.
摘要翻译：本发明提供了利用式I和II化合物筛选药物化合物的方法，其中式I和II是其中R 1，R 2，R 3和R 4表示氢，卤素，烷基或烷氧基取代基; R5是氢或低级烷基; X和Y表示氢，卤素，烷基或烷氧基取代基; Z是氢或氟。本发明还提供用氚或碘的同位素放射性标记的式I和II的氚或碘同位素放射性标记的化合物。本发明还提供了与式I或II化合物特异性结合的新型GABAa受体亚型。本发明还提供了与式I或II化合物原位结合的GABAa受体亚型。本文提供的化合物选择性结合GABAa结合位点的新亚型。配体在这种独特的受体群体上的选择性相互作用导致药理学特异性，这可能导致优异的抗焦虑药，认知增强剂，抗惊厥药和镇静催眠药。

55. 发明授权

US07365068B2 Substituted aryl acylthioureas and related compounds; inhibitors of viral replication 失效
标题翻译：取代的芳基酰基硫脲和相关化合物; 病毒复制抑制剂
公开(公告)号：US07365068B2
公开(公告)日：2008-04-29
申请号：US11131013
申请日：2005-05-17
申请人： Avinash Phadke , Dawei Chen , Milind Deshpande , Andrew Thurkauf , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
发明人： Avinash Phadke , Dawei Chen , Milind Deshpande , Andrew Thurkauf , Xiangzhu Wang , Yiping Shen , Cuixian Liu , Jesse Quinn , Junko Ohkanda , Shouming Li
IPC分类号： A61K31/496 , A61K31/444 , A61K31/5377 , C07D211/78 , C07D401/02 , C07D401/06 , C07D413/02 , C07D413/06
CPC分类号： C07D295/15 , C07C335/26 , C07D211/22 , C07D211/46 , C07D211/60 , C07D211/64 , C07D211/78 , C07D213/56 , C07D213/82 , C07D215/54 , C07D231/14 , C07D233/54 , C07D233/64 , C07D233/90 , C07D237/24 , C07D239/28 , C07D241/24 , C07D241/44 , C07D249/06 , C07D253/07 , C07D261/18 , C07D263/34 , C07D263/58 , C07D265/30 , C07D271/12 , C07D277/56 , C07D277/68 , C07D285/06 , C07D307/68 , C07D307/84 , C07D307/85 , C07D309/38 , C07D311/58 , C07D333/38 , C07D401/04 , C07D401/12 , C07D405/04 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D419/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： The invention provides compounds and pharmaceutically acceptable salts of Formula I wherein the variables A1, A2, R1, R2, V, W, X, Y, and Z are defined herein. Certain compounds of Formula I described herein which possess potent antiviral activity. The invention particularly provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. The invention also provides pharmaceutical compositions containing one or more compound of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease or disorder. These infectious diseases include viral infections, particularly HCV infections. The invention is particularly includes methods of treating human patients suffering from an infectious disease, but also encompasses methods of treating other animals, including livestock and domesticated companion animals, suffering from an infectious disease.Methods of treatment include administering a compound of Formula I as a single active agent or administering a compound of Formula I in combination with on or more other therapeutic agent.
摘要翻译：本发明提供式I的化合物和药学上可接受的盐，其中变量A 1，A 2，R 1，R 2， / SUB>，V，W，X，Y和Z在本文中定义。某些本文所述的具有强抗病毒活性的式I化合物。本发明特别提供了作为丙型肝炎病毒复制的有效和/或选择性抑制剂的式I化合物。本发明还提供含有一种或多种式I化合物或这些化合物的盐，溶剂化物或酰化前药以及一种或多种药学上可接受的载体，赋形剂或稀释剂的药物组合物。本发明还包括通过向这些患者施用一定量的有效减少疾病或病症的体征或症状的式I化合物来治疗患有某些感染性疾病的患者的方法。这些传染病包括病毒感染，特别是HCV感染。本发明特别包括治疗患有感染性疾病的人类患者的方法，还包括治疗其它动物（包括患有传染病的家畜和驯养的伴侣动物）的方法。治疗方法包括给予式I化合物作为单一活性剂或将一种式I化合物与一种或多种其它治疗剂组合施用。

56. 发明授权

US07323478B2 Melanin concentrating hormone receptor ligands 失效
标题翻译：黑色素浓缩激素受体配体
公开(公告)号：US07323478B2
公开(公告)日：2008-01-29
申请号：US10820344
申请日：2004-04-08
申请人： Rajagopal Bakthavatchalam , Andrew Thurkauf , Alan Hutchison
发明人： Rajagopal Bakthavatchalam , Andrew Thurkauf , Alan Hutchison
IPC分类号： A61K31/445
CPC分类号： C07D295/096
摘要： Disclosed are compounds of the formula: and the pharmaceutically acceptable salts thereof wherein Q, X, Y, Z, and R1 R9, and R12-R19 are defined herein. These compounds are selective modulators of MCH 1 receptors that are, therefore, useful in the treatment of a variety of metabolic, feeding, and sexual disorders. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also disclosed.
摘要翻译：公开了下式的化合物及其药学上可接受的盐，其中Q，X，Y，Z和R 1 R 9和R 12，本文定义了本文所述的方法。这些化合物是MCH 1受体的选择性调节剂，因此可用于治疗各种代谢，喂养和性功能障碍。还公开了治疗这种病症以及包装的药物组合物的方法。

57. 发明申请

US20050239799A1 1-phenyl-4-benzylpiperazines dopamine receptor subtype 失效
标题翻译： 1-苯基-4-苄基哌嗪多巴胺受体亚型
公开(公告)号：US20050239799A1
公开(公告)日：2005-10-27
申请号：US11167735
申请日：2005-06-27
申请人： Andrew Thurkauf , Xi Chen
发明人： Andrew Thurkauf , Xi Chen
IPC分类号： C07D295/06 , A61K31/495 , A61P25/18 , A61P43/00 , C07D241/04 , C07D295/073 , C07D295/08 , C07D295/096 , C07D295/112 , C07D295/135 , C07D317/58 , C07D319/18
CPC分类号： C07D295/073 , A61K31/495 , C07C2603/08 , C07D295/096 , C07D295/112 , C07D295/135
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1-C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, hydroxy, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.
摘要翻译：公开了下式的化合物或其药学上可接受的加成盐，其中：R 1是卤素或C 1 -C 4烷基; R 2和R 3相同或不同，表示氢，卤素，C 1 -C 4烷基，烷基，C 1 -C 4烷氧基，烷硫基，羟基，氨基，单（C 1 -C 4 - ）烷基氨基，二（C 1 -C 4 - ）烷基氨基或R 2和R 3一起代表一个与它们所连接的苯环一起形成萘基部分的4碳亚烯基部分，该化合物可用于治疗神经疾病疾病如精神分裂症，精神病抑郁症和躁狂症。

58. 发明授权

US06444819B1 Benzylpiperazinyl and piperidinyl ethanone derivatives: dopamine receptor subtype specific ligands 失效
标题翻译：苄基哌嗪基和哌啶基乙酮衍生物：多巴胺受体亚型特异性配体
公开(公告)号：US06444819B1
公开(公告)日：2002-09-03
申请号：US09975535
申请日：2001-10-11
申请人： Renata Xavier Kover , Salva Terdjanian , Jennifer Tran , Andrew Thurkauf
发明人： Renata Xavier Kover , Salva Terdjanian , Jennifer Tran , Andrew Thurkauf
IPC分类号： C07D22120
CPC分类号： C07D295/15 , C07D209/08 , C07D401/06
摘要： Disclosed are compounds of the formula: or pharmaceutically acceptable addition salts thereof wherein: Y represents oxygen or sulfur; Z is nitrogen or CH; R1, R2 and R3 independently represent organic or inorganic substituents; R4 and R4′ independently represent hydrogen, alkyl or form a ring with the atom to which they are attached; R5 represents hydrogen, alkyl, alkoxy, or alkylthio, and R6 represents hydrogen or alkyl; or R5 and R6 form a ring together with the atoms to which they are attached; and R7, R8, R9, R10, and R11 independently represent hydrogen or alkyl, which compounds are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents.
摘要翻译：公开了下式的化合物或其药学上可接受的加成盐，其中：Y表示氧或硫; Z是氮或CH; R 1，R 2和R 3独立地表示有机或无机取代基; R 4和R 4'独立地表示氢，烷基或与它们连接的原子形成环; R 5表示氢，烷基，烷氧基或烷硫基，R6代表氢或烷基; 或R 5和R 6与它们所连接的原子一起形成环; 和R 7，R 8，R 9，R 10和R 11独立地表示氢或烷基，该化合物可用于治疗和/或预防神经心理障碍，包括但不限于精神分裂症，躁狂症，痴呆，抑郁症，焦虑症，强迫行为，药物滥用，帕金森样运动障碍和与使用精神安定药有关的运动障碍。

59. 发明授权

US06281359B1 Aminomethyl phenyl pyridine derivatives 失效
标题翻译：氨基甲基苯基吡啶衍生物
公开(公告)号：US06281359B1
公开(公告)日：2001-08-28
申请号：US08457409
申请日：1995-06-01
申请人： Jun Yuan , Andrew Thurkauf
发明人： Jun Yuan , Andrew Thurkauf
IPC分类号： C07D40106
CPC分类号： C07D239/42 , C07C211/27 , C07D211/14 , C07D211/70 , C07D295/096 , C07D401/06
摘要： Disclosed are compounds of the formula: where S and V are various organic or inorganic substituents; G and K are the same or different and represent N or CR′ where R′ is an organic or inorganic substituent; R is hydrogen or an alkyl group; R1, X, Y, Z and T are organic or inorganic substituents; and R2 and R3 represent hydrogen or organic substituents; or NR2R3 together represents a heterocyclic ring system; and the pharmaceutically acceptable salts thereof; which are highly selective partial agonists or antagonists at brain dopamine receptor subtypes and, thus, are useful in the diagnosis and treatment of affective disorders such as schizophrenia and depression as well as certain movement disorders such as Parkinsonism.
摘要翻译：公开了下式的化合物：其中S和V是各种有机或无机取代基; G和K相同或不同，表示N或CR'，其中R'是有机或无机取代基; R是氢或烷基; R 1 X，Y，Z和T是有机或无机取代基; 且R 2和R 3表示氢或有机取代基; 或NRR2R3一起表示杂环系统;及其药学上可接受的盐; 其是脑多巴胺受体亚型的高度选择性部分激动剂或拮抗剂，因此可用于诊断和治疗情感障碍如精神分裂症和抑郁症以及某些运动障碍如帕金森综合征。

60. 发明授权

US06172229B2 1-phenyl-4-benzylpiperazines; dopamine receptor subtype specific ligands 失效
标题翻译： 1-苯基-4-苄基哌嗪; 多巴胺受体亚型特异性配体
公开(公告)号：US06172229B2
公开(公告)日：2001-01-09
申请号：US09228106
申请日：1999-01-11
申请人： Andrew Thurkauf , Xi Chen
发明人： Andrew Thurkauf , Xi Chen
IPC分类号： C07D295073
CPC分类号： C07D295/073 , A61K31/495 , C07C2603/08 , C07D295/096 , C07D295/112 , C07D295/135
摘要： Disclosed are compounds of the formula: or the pharmaceutically acceptable addition salts thereof wherein: R1 is halogen or C1-C4 alkyl; and R2 and R3 are the same or different and represent hydrogen, halogen, C1-C4 alkyl, C1-C4 alkoxy, alkylthio, hydroxy, amino, mono(C1-C4)alkylamino, di(C1-C4)alkylamino, or R2 and R3 together represent a 4 carbon alkenylene moiety that together with the phenyl ring to which they are attached form a naphthyl moiety, which compounds are useful in the treatment of neuropsycological diseases such as schizophrenia, psychotic depression and mania.
摘要翻译：公开了下式的化合物或其药学上可接受的加成盐，其中：R 1是卤素或C 1 -C 4烷基; 并且R 2和R 3相同或不同，表示氢，卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，烷硫基，羟基，氨基，单（C 1 -C 4）烷基氨基，二（C 1 -C 4）烷基氨基或R 2和R 3一起代表与其所连接的苯环一起形成萘基部分的4碳亚烯基部分，该化合物可用于治疗神经疾病疾病如精神分裂症，精神抑郁症和躁狂症。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式