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21.发明授权Antibiotic derivatives of 7-phenyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids 失效7-苯基-1,4-二氢-4-氧代-3-喹啉羧酸的抗生素衍生物
公开(公告)号：US4623650A
公开(公告)日：1986-11-18
申请号：US679150
申请日：1984-12-06
IPC分类号： C07D215/56 , C07D405/04 , C07D498/06 , C07F7/18 , A61K31/47 , C07D215/18
CPC分类号： C07D405/04 , C07D215/56 , C07F7/1856
摘要： 1-Substituted-6-fluoro-7-aryl-(8-fluoro)-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by reacting the corresponding alkyl 1-substituted-6-fluoro-7-bromo-(8-fluoro)-1,4-dihydroquinol-4-one-3-carboxylate with an arylmetallic compound and hydrolyzing the ester formed.
摘要翻译： 具有抗菌活性的1-取代的6-氟-7-芳基 - （8-氟）-1,4-二氢喹啉-4-酮3-羧酸通过使相应的1-取代-6-氟-7 （8-氟）-1,4-二氢喹啉-4-酮-3-羧酸叔丁酯与芳基金属化合物反应，并水解所形成的酯。
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22.发明申请ARYLPROPIONAMIDE, ARYLACRYLAMIDE, ARYLPROPYNAMIDE, OR ARYLMETHYLUREA ANALOGS AS FACTOR XIA INHIBITORS 有权芳基酰胺，芳基丙烯酰胺，芳基丙烯酰胺或芳基甲酰胺类似物作为因子XIA抑制剂公开(公告)号：US20120270853A1
公开(公告)日：2012-10-25
申请号：US13540871
申请日：2012-07-03
申请人： Donald J.P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith
发明人： Donald J.P. Pinto , Joanne M. Smallheer , James R. Corte , Zilun Hu , Cullen L. Cavallaro , Paul J. Gilligan , Mimi L. Quan , Leon M. Smith
IPC分类号： A61K31/4178 , C07D401/14 , A61K31/4439 , C07D403/12 , A61K31/4196 , C07D401/10 , A61K31/4709 , C07D413/14 , A61K31/5377 , C07D417/14 , A61K31/541 , C07D403/14 , A61K31/551 , C07D471/08 , A61P7/02 , A61P9/10 , A61P9/00 , C07D403/10
CPC分类号： C07D403/04 , C07D233/68 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/08 , C07D487/04 , C07D487/08
摘要： The present invention provides compounds of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, L1, M and R11 are as defined herein. The compounds of Formula (I) are selective inhibitors of serine protease enzymes of the coagulation cascade and/or contact activation system; for example thrombin, factor Xa, factor XIa, factor IXa, factor VIIa and/or plasma kallikrein. In particular, it relates to compounds that are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.
摘要翻译： 本发明提供了式（I）化合物或其立体异构体，互变异构体，药学上可接受的盐或溶剂合物形式，其中变量A，L1，M和R11如本文所定义。 式（I）的化合物是凝血级联和/或接触激活系统的丝氨酸蛋白酶的选择性抑制剂; 例如凝血酶，因子Xa，因子XIa，因子IXa，因子VIIa和/或血浆激肽释放酶。 特别地，它涉及作为选择性因子XIa抑制剂或fXIa和血浆激肽释放酶的双重抑制剂的化合物。 本发明还涉及包含这些化合物的药物组合物和使用其制备血栓栓塞和/或炎症性疾病的方法。
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公开(公告)号：US20110059940A1
公开(公告)日：2011-03-10
申请号：US12990922
申请日：2009-05-07
申请人： Paul J. Gilligan , Michael G. Yang , Jianliang Shi
发明人： Paul J. Gilligan , Michael G. Yang , Jianliang Shi
IPC分类号： A61K31/18 , C07C311/00 , C07D205/04 , C07D233/61 , C07D249/08 , C07D231/12 , C07D213/42 , C07D217/24 , A61K31/24 , A61K31/195 , A61K31/397 , A61K31/4164 , A61K31/4196 , A61K31/415 , A61P25/00 , A61P25/28
CPC分类号： C07D205/04 , C07C311/19 , C07C2601/04 , C07D213/42 , C07D217/24 , C07D231/12 , C07D233/61 , C07D249/08 , C07D263/32 , C07D273/02
摘要： The disclosure provides compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their uses in inhibiting β-amyloid peptide (β-AP) production.
摘要翻译： 本公开提供了式I化合物，包括其药学上可接受的盐，其药物组合物及其在抑制β-淀粉状蛋白肽（β-bGRAP）生产中的用途。
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![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](/abs-image/US/2010/02/16/US07662817B2/abs.jpg.150x150.jpg)
24.发明授权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：US07662817B2
公开(公告)日：2010-02-16
申请号：US12030439
申请日：2008-02-13
申请人： Paul J. Gilligan
发明人： Paul J. Gilligan
IPC分类号： C07D487/04 , C07D401/04 , A61K31/53 , A61P25/22 , A61P25/24
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 。
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25.发明授权Heterocyclyl-substituted ring-fused pyridines and pyrimidines as corticotropin releasing hormone(CRH) antagonists, useful for treating CNS and stress-related disorders 有权杂环取代的环稠合吡啶和嘧啶作为促肾上腺皮质激素释放激素（CRH）拮抗剂，用于治疗CNS和应激相关疾病公开(公告)号：US06245769B1
公开(公告)日：2001-06-12
申请号：US09145231
申请日：1998-09-01
IPC分类号： A61K314192
CPC分类号： C07D471/04 , C07D487/04
摘要： Corticotropin releasing factor (CRF) antagonists of Formula (I): and their use in treating psychiatric disorders and neurological diseases, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding disorders as well as treatment of immunological, cardiovascular or heart-related diseases and colonic hypersensitivity associated with psychopathological disturbance and stress in mammals.
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精神疾病和神经系统疾病，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍以及免疫学，心血管或心脏的治疗 与哺乳动物精神病理障碍和压力相关的疾病和结肠超敏反应。
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![Nitrogen substituted imidazo[4,5-C]pyrazoles as corticotropin releasing hormone antagonists](/abs-image/US/2001/01/16/US06174912B1/abs.jpg.150x150.jpg)
26.发明授权Nitrogen substituted imidazo[4,5-C]pyrazoles as corticotropin releasing hormone antagonists 有权氮取代的咪唑并[4,5-C]吡唑作为促肾上腺皮质激素释放激素拮抗剂公开(公告)号：US06174912B1
公开(公告)日：2001-01-16
申请号：US09138460
申请日：1998-08-21
申请人： James P. Beck , Paul J. Gilligan
发明人： James P. Beck , Paul J. Gilligan
IPC分类号： A61K314162
CPC分类号： C07D487/04
摘要： Corticotropin releasing factor (CRF) antagonists of Formulae (I) or (II): and their use in treating psychiatric disorders and neurological diseases including major depression, anxiety-related disorders, post-traumatic stress disorder, supranuclear palsy and feeding 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）或（II）的促肾上腺皮质激素释放因子（CRF）拮抗剂及其用于治疗精神疾病和神经疾病，包括主要抑郁症，焦虑相关疾病，创伤后应激障碍，核上性麻痹和进食障碍以及 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。
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公开(公告)号：US5532243A
公开(公告)日：1996-07-02
申请号：US836230
申请日：1992-02-14
申请人： Paul J. Gilligan
发明人： Paul J. Gilligan
IPC分类号： A61K31/40 , A61K31/403 , A61K31/4035 , A61P25/18 , C07D209/44 , C07D217/04 , C07D217/06 , C07D401/06 , C07D401/12 , C07D405/04 , C07D407/04 , C07D409/04 , C07D471/04 , C07D513/04 , C07F7/18 , A61K31/495 , C07D217/18 , C07D239/00
CPC分类号： C07D401/06 , C07D217/04 , C07D217/06 , C07D405/04 , C07D409/04 , C07D471/04 , C07D513/04
摘要： There are provided nitrogen-containing bicyclic compounds, pharmaceutical compositions containing these compounds and methods of using these compounds to treat physiological or drug-induced psychosis or diskinesia in a mammal.
摘要翻译： 提供含氮双环化合物，含有这些化合物的药物组合物和使用这些化合物治疗哺乳动物的生理或药物诱导的精神病或药物滥用的方法。
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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。
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29.发明授权
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.
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30.发明授权N-aralkyl piperidine derivatives as psychotropic drugs 失效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.
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