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31. 发明授权

US5296479A Treatment of psychosis using 1-cycloalkylpiperidines 失效
标题翻译：使用1-环烷基哌啶治疗精神病
公开(公告)号：US5296479A
公开(公告)日：1994-03-22
申请号：US831887
申请日：1992-02-06
申请人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
发明人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/451 , A61K31/47 , A61P25/00 , A61P25/18 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/32 , C07D211/46 , C07D401/06 , C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , C07D211/22 , C07D211/24 , C07D211/32
摘要： There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
摘要翻译：提供了可用于治疗哺乳动物的生理或药物诱发的精神病或运动障碍的环烷基哌啶化合物。这些新型化合物是选择性的σ受体拮抗剂，并且具有与典型的抗精神病药相关的运动障碍副作用的低潜力。

32. 发明授权

US5169855A Piperidine ether derivatives as psychotropic drugs or plant fungicides 失效
标题翻译：哌啶衍生物作为精神药物或植物杀真菌剂
公开(公告)号：US5169855A
公开(公告)日：1992-12-08
申请号：US506961
申请日：1990-03-28
申请人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
发明人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
IPC分类号： A01N43/40 , A61K31/4427 , A61K31/445 , A61K31/4458 , A61K31/4462 , A61K31/4465 , A61K31/451 , A61P25/00 , C07D211/22 , C07D211/46 , C07D401/06 , C07D401/12 , C07D413/12 , C07D417/12
CPC分类号： C07D401/06 , A01N43/40 , C07D211/22 , C07D211/46 , C07D401/12 , C07D413/10 , C07D417/12
摘要： There are provided piperidine ether derivatives, pharmaceutical and agricultural compositions containing them useful for treating physiological or drug induced psychosis or dyskinesia in a mammal or fungal disease in plants. Also provided are methods for preparing these compounds.

33. 发明授权

US5116846A N-aralkyl piperidine derivatives as psychotropic drugs 失效
标题翻译： N-ARALKYL PIPERIDINE衍生物作为PSYCHOTROPIC DRUGS
公开(公告)号：US5116846A
公开(公告)日：1992-05-26
申请号：US500573
申请日：1990-03-28
申请人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
发明人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
IPC分类号： A61K31/435 , A61K31/4427 , A61K31/4433 , A61K31/445 , A61K31/4465 , A61K31/451 , A61P25/00 , A61P25/18 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/32 , C07D211/34 , C07D401/06 , C07D405/06 , C07D409/06
CPC分类号： C07D401/06 , C07D211/22 , C07D211/32 , C07D211/34 , C07D405/06 , C07D409/06
摘要： There are provided N-aralkyl piperidine derivatives which are selective sigma receptor antagonists. These compounds and pharmaceutical compositions containing them are useful for treating physiological or drug induced psychosis or dyskinesia in a mammal.

34. 发明授权

US07157578B2 4-(2-butylamino)-2, 7-dimethyl-8-(2-methyl-6-methoxypyrid-3-YL) pyrazolo-[1,5-A]-1,3,5-triazine, its enantiomers and pharmaceutically acceptable salts as corticotropin releasing factor receptor ligands 有权
标题翻译： 4-（2-丁基氨基）-2,7-二甲基-8-（2-甲基-6-甲氧基吡啶-3-基）吡唑并[1,5-A] -1,3,5-三嗪，其对映体和药学上可接受的盐作为促肾上腺皮质激素释放因子受体配体
公开(公告)号：US07157578B2
公开(公告)日：2007-01-02
申请号：US10358652
申请日：2003-02-05
申请人： Paul J. Gilligan
发明人： Paul J. Gilligan
IPC分类号： C07D403/12 , A61K31/53 , A61P25/22 , A61P25/24 , A61P9/12 , A61P3/04
CPC分类号： A61K31/53 , C07D487/04
摘要： Corticotropin releasing factor (CRF) antagonists of Formula (I): and its use in treating anxiety, depression, and other psychiatric, neurological disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress.
摘要翻译：式（I）的促肾上腺皮质激素释放因子（CRF）拮抗剂及其用于治疗焦虑，抑郁和其他精神病学，神经障碍以及治疗与精神病理学障碍和应激相关的免疫学，心血管或心脏相关疾病和结肠超敏反应的用途。

35. 发明授权

US07153961B2 Salt and crystalline form thereof of a corticotropin releasing factor receptor antagonist 有权
标题翻译：促肾上腺皮质激素释放因子受体拮抗剂的盐及其结晶形式
公开(公告)号：US07153961B2
公开(公告)日：2006-12-26
申请号：US10985115
申请日：2004-11-10
申请人： Paul J. Gilligan , Shelly Renee Rabel Riley , Paul A. Meenan
发明人： Paul J. Gilligan , Shelly Renee Rabel Riley , Paul A. Meenan
IPC分类号： C07D487/04 , A61K31/53 , A61P3/04 , A61P25/22 , A61P25/24
CPC分类号： C07D487/04
摘要： The present invention provides 4-(bis(2-methoxyethyl)amino)-2,7-dimethyl-8-(2-methyl-4-methoxyphenyl)-[1,5-a]-pyrazolo-1,3,5-triazine benzenesulfonate salt and a crystalline polymorph thereof. Further provided are pharmaceutical compositions containing the salt and methods of treating CRF-related disorders using said salt.
摘要翻译：本发明提供4-（双（2-甲氧基乙基）氨基）-2,7-二甲基-8-（2-甲基-4-甲氧基苯基） - [1,5-a] - 吡唑并[ 三嗪苯磺酸盐及其结晶多晶型物。还提供含有盐的药物组合物和使用所述盐治疗CRF相关病症的方法。

36. 发明授权

US07026317B2 Pyrazolotriazines as CRF antagonists 有权
标题翻译：吡咯三嗪作为CRF拮抗剂
公开(公告)号：US07026317B2
公开(公告)日：2006-04-11
申请号：US09990138
申请日：2001-11-21
申请人： Paul J. Gilligan , Richard G. Wilde
发明人： Paul J. Gilligan , Richard G. Wilde
IPC分类号： C07D487/04 , A61K31/53 , A61K31/5377
CPC分类号： C07D487/04
摘要： The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.
摘要翻译：本发明涉及式（I）的吡唑并三嗪及其立体异构体，异构体和盐，其中R 1至Z 5选自某些烷基，芳基和杂芳基，作为在本说明书中定义，其中所有化合物可用作CRF拮抗剂，因此可用于治疗神经系统疾病以及多种其它CRF相关疾病或病症。

37. 发明授权

US06589952B2 Imidazo[1,2-a]pyrazines for the treatment of neurological disorders 有权
标题翻译：咪唑并[1,2-a]吡嗪治疗神经系统疾病
公开(公告)号：US06589952B2
公开(公告)日：2003-07-08
申请号：US09905097
申请日：2001-07-13
申请人： Rajagopal Bakthavatchalam , Richard G. Wilde , Paul J. Gilligan
发明人： Rajagopal Bakthavatchalam , Richard G. Wilde , Paul J. Gilligan
IPC分类号： C07D48704
CPC分类号： C07D487/04
摘要： Provided herein are novel imidazo[1,2-a]pyrazines of Formula I: wherein: X is CHR5, NR5, O, S, S(O)n or a single bond, wherein n is equal to 0, 1 or 2; D is aryl or heteroaryl attached through an unsaturated carbon atom and wherein said aryl or heteroaryl is optionally substituted at any available position with from 1-5 of A1, A2, A3, A4 and A5; R2 is C1-4 alkyl or C3-8 cycloalkyl, each of which is optionally substituted with from 1-3 hydroxy, halogen or C1-4 alkoxy, or wherein when X is a bond, R2 is optionally also CN, CF3, C2F5, C1-4 alkyl or C3-8 cycloalkyl, each of which C1-4 alkyl or C3-8 cycloalkyl is optionally substituted with from 1-3 hydroxy, halogen and C1-4 alkoxy; as well as compositions containing the same, useful in the treatment of, for example, neurological and psychological disorders characterized by corticotropin releasing factor (CRF) overexpression.
摘要翻译：本文提供了式I的新的咪唑并[1,2-a]吡嗪：其中：X是CHR 5，NR 5，O，S，S（O）n或单键，其中n等于0,1或2; D是通过不饱和碳原子连接的芳基或杂芳基，其中所述芳基或杂芳基在任何可用的位置任选被1至5个A 1，A 2，A 3，A 4和A 5取代; R 2是C 1-4烷基或C 3-8 环烷基，其各自任选被1-3个羟基，卤素或C 1-4烷氧基取代，或其中当X是键时，R 2任选地也是CN，CF 3，C 2 F 5，C 1-4烷基或C 3-8环烷基，每个C 1-4烷基或C 3-8环烷基任选被1-3个羟基，卤素和C 1-4烷氧基取代;以及含有该羟基，卤素和C 1-4烷氧基的组合物，其可用于治疗例如神经和心理障碍其特征在于促肾上腺皮质激素释放因子（CRF）过表达。

38. 发明授权

US5109002A Antipsychotic 1-cycloalkylpiperidines 失效
标题翻译：抗生素1-环丙基哌啶
公开(公告)号：US5109002A
公开(公告)日：1992-04-28
申请号：US570199
申请日：1990-08-20
申请人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
发明人： Gary A. Cain , Paul J. Gilligan , Sang W. Tam
IPC分类号： A61K31/445 , A61K31/4427 , A61K31/451 , A61K31/47 , A61P25/00 , A61P25/18 , C07D211/22 , C07D211/24 , C07D211/26 , C07D211/32 , C07D211/46 , C07D401/06 , C07D401/12 , C07D401/14
CPC分类号： C07D401/12 , C07D211/22 , C07D211/24 , C07D211/32
摘要： There are provided cycloalkyl piperidine compounds which are useful in the treatment of physiological or drug-induced psychosis or dyskinesia in a mammal. These novel compounds are selective sigma receptor antagonists and have a low potential for movement disorder side effects associated with typical antipsychotic agents.
摘要翻译：提供了可用于治疗哺乳动物的生理或药物诱发的精神病或运动障碍的环烷基哌啶化合物。这些新型化合物是选择性的σ受体拮抗剂，并且具有与典型的抗精神病药相关的运动障碍副作用的低潜力。

39. 发明授权

US4797490A Process for the preparation of 3-(2'-fluorophenyl)pyridine 失效
标题翻译：制备3-（2'-氟苯基）吡啶的方法
公开(公告)号：US4797490A
公开(公告)日：1989-01-10
申请号：US907176
申请日：1986-09-15
申请人： Paul J. Gilligan , Paul R. McGuirk , Michael J. Witty
发明人： Paul J. Gilligan , Paul R. McGuirk , Michael J. Witty
IPC分类号： C07D213/26
CPC分类号： C07D213/26
摘要： 6-Fluoro-7-pyridylquinolone carboxylic esters and acids having antibacterial activity are prepared by coupling of a 2-fluorophenyl-metallic compound with a pyridyl bromide or iodide in the presence of a transition metal catalyst, nitrating and hydrogenating the pyridyl-2-fluorophenyl compound formed, introducing a substituent on the nitrogen of the amine formed, and cyclizing after reacting with a dialkyl or dibenzyl ethoxymethylene malonate to form a 6-fluoro-7-pyridyl-1,4-dihydroquinol-4-one 3-carboxylate, and hydrolyzing to the corresponding acid.
摘要翻译：通过在过渡金属催化剂的存在下将2-氟苯基 - 金属化合物与吡啶基溴化物或碘化物偶联制备6-硝基-7-吡啶基喹诺酮羧酸酯和具有抗菌活性的酸，硝化并氢化吡啶-2-氟苯基形成的化合物，在形成的胺的氮气上引入取代基，并在与二烷基或二苄基乙氧基亚甲基丙二酸酯反应后环化形成6-氟-7-吡啶基-1,4-二氢喹啉-4-酮3-羧酸酯，和水解成相应的酸。

40. 发明授权

US4636506A 7-heterocyclic-1,4-dihydroquinolones 失效
标题翻译： 7-杂环-1,4-二氢喹诺酮类
公开(公告)号：US4636506A
公开(公告)日：1987-01-13
申请号：US719663
申请日：1985-04-04
申请人： Paul J. Gilligan , Paul R. McGuirk , Michael J. Witty
发明人： Paul J. Gilligan , Paul R. McGuirk , Michael J. Witty
IPC分类号： C07D215/56 , C07D401/04 , C07D471/06 , C07D513/06 , A61K31/47 , C07D215/18
CPC分类号： C07D401/04 , C07D215/56 , C07D471/06 , C07D513/06
摘要： 1-Alkyl-6,8-difluoro-7-heterocyclic-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by conventional cyclization methods.
摘要翻译：通过常规环化法制备具有抗菌活性的1-烷基-6,8-二氟-7-杂环-1,4-二氢喹啉-4-酮3-羧酸。

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