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1.发明授权Substituted tetrahydropyridine and piperidine carboxylic acids as muscarinic antagonists 失效取代的四氢吡啶和哌啶羧酸作为毒蕈碱拮抗剂
公开(公告)号：US5446057A
公开(公告)日：1995-08-29
申请号：US126942
申请日：1993-09-24
IPC分类号： C07D211/78 , C07D405/12 , C07D211/42 , A61K31/44
CPC分类号： C07D405/12 , C07D211/78
摘要： Substituted tetrahydropyridines and piperidinecarboxylic acids and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which muscarinic antagonists are useful as agents for inhibiting gastric acid release, for treating bradycardia, bronchoconstriction, urinary incontinence, atonic conditions of the gut and bladder, Parkinson's disease, dystonias, and Alzheimer's disease.
摘要翻译： 本发明描述了取代的四氢吡啶和哌啶羧酸及其衍生物，以及其制备方法及其药物组合物，其中毒蕈碱拮抗剂可用作抑制胃酸释放的药物，用于治疗心动过缓，支气管收缩，尿失禁， 肠和膀胱，帕金森病，肌张力障碍和阿尔茨海默病。
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2.发明授权Azabicyclo and azacyclo oxime and amine cholinergic agents and methods of treatment 失效氮杂双环和吖嗪肟和胺类胆碱能药剂及治疗方法
公开(公告)号：US5346911A
公开(公告)日：1994-09-13
申请号：US110904
申请日：1993-08-24
申请人： Corinne E. Augelli-Szafran , Stephen D. Barrett , Bradley W. Caprathe , Adam A. Galan , Juan C. Jaen , David J. Lauffer , Walter H. Moos , Michael R. Pavia , Kathryn B. Sanders , Haile Tecle , Anthony J. Thomas
发明人： Corinne E. Augelli-Szafran , Stephen D. Barrett , Bradley W. Caprathe , Adam A. Galan , Juan C. Jaen , David J. Lauffer , Walter H. Moos , Michael R. Pavia , Kathryn B. Sanders , Haile Tecle , Anthony J. Thomas
IPC分类号： C07D211/72 , C07D451/04 , C07D453/02 , C07D487/08 , A61K31/44 , C07D211/70
CPC分类号： C07D211/72 , C07D451/04 , C07D453/02 , C07D487/08
摘要： Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds which are azabicyclo[2.2.1]oximes, azabicyclo[2.2.2]oximes, azabicyclo[2.2.1]amines, azabicyclo[2.2.2]amines, azabicyclo[3.2.1]oximes, and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms are disclosed.
摘要翻译： 含有偶氮二环[2.2.1]肟，氮杂双环[2.2.2]肟，氮杂双环[2.2.1]胺，氮杂双环[2.2.2]胺，氮杂双环[3.2.1] 肟和含有杂环肟的胺，其中杂环含有3至7个碳原子。
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公开(公告)号：US5514812A
公开(公告)日：1996-05-07
申请号：US257858
申请日：1994-06-10
申请人： Ruth Bucsh , Juan C. Jaen , Edgardo Laborde , Anthony J. Thomas
发明人： Ruth Bucsh , Juan C. Jaen , Edgardo Laborde , Anthony J. Thomas
IPC分类号： C07D453/02 , C07D487/08
CPC分类号： C07D487/08 , C07D453/02
摘要： The instant invention is a selective formation of the Z-oxime and O-alkylation of 1-azabicyclo 2.2.1!heptan-3-one and 1-azabicyclo 2.2.2!heptan-3-one oximes to produce compounds with muscarinic activity. The process is capable of scale-up for industrial purposes as it provides better yields and ease of preparation. Intermediates are also described.
摘要翻译： 本发明是选择性形成1-氮杂双环[2.2.1]庚-3-酮和1-氮杂二环[2.2.2]庚-3-酮肟的Z-肟和O-烷基化，以产生具有毒蕈碱的化合物 活动。 该过程能够在工业目的上进行放大，因为它提供更好的产量和易于准备。 还描述了中间体。
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4.发明授权Azabicyclo and azacyclo oxime and amine cholinergic agents and methods of treatment 失效氮杂双环和吖嗪肟和胺类胆碱能药剂及治疗方法
公开(公告)号：US5482938A
公开(公告)日：1996-01-09
申请号：US189620
申请日：1994-02-01
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/46 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/28 , A61P43/00 , C07D205/06 , C07D207/22 , C07D211/72 , C07D223/06 , C07D225/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D451/10 , C07D453/02 , C07D471/08 , C07D487/08 , A61K31/535 , C07D413/00
CPC分类号： C07D487/08 , C07D211/72 , C07D451/04 , C07D453/02
摘要： Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds are disclosed which are azabicyclo[2.2.2]oximes, azabicyclo[2.2.2]-amines, azabicyclo[3.2.1]oximes and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 3 to 7 carbon atoms.
摘要翻译： 公开了含有有机氮的环状肟和胺取代的化合物，其是氮杂双环[2.2.2]肟，氮杂双环[2.2.2] - 胺，氮杂双环[3.2.1]肟和含胺杂环肟，其中杂环包含3 至7个碳原子。
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5.发明授权4-(N-substituted amino)-2-butynyl-1-carbamates and thiocarbamates and derivatives thereof as centrally acting muscarinic agents 失效4-（N-取代氨基）-2-丁炔基-1-氨基甲酸酯和硫代氨基甲酸酯及其衍生物作为中枢作用毒蕈碱药
公开(公告)号：US4996201A
公开(公告)日：1991-02-26
申请号：US388777
申请日：1989-08-02
IPC分类号： A61K31/27 , A61K31/40 , A61K31/495 , A61K31/535 , A61K31/5375 , A61P25/02 , A61P25/28 , C07C271/20 , C07C271/24 , C07C271/28 , C07C333/04 , C07D205/04 , C07D211/14 , C07D211/22 , C07D295/12 , C07D295/125
CPC分类号： C07D295/125 , C07C271/20 , C07D205/04
摘要： 4-(N-Substituted amino)-2-butynyl-1-carbamates and thiocarbamates and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.
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公开(公告)号：US4782071A
公开(公告)日：1988-11-01
申请号：US926163
申请日：1986-11-03
IPC分类号： C07D211/16 , C07D211/52 , C07D213/74 , C07D213/75 , C07D295/215 , A01N43/40 , C07D239/02
CPC分类号： C07D213/74 , C07D211/16 , C07D211/52 , C07D213/75 , C07D295/215
摘要： Certain tetrasubstituted alkyl, aryl, pyridinyl, piperidinyl, and piperazinyl urea compounds stimulate the release of acetylcholine and are thus useful analgesic agents for alleviating pain or as cholinergic agents which are useful for the amelioration of the symptoms of cognitive decline in the elderly.These compounds have the general formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.4 are phenyl or substituted phenyl, and R.sub.3 is pyridinyl.Pharmaceutical compositions including these compounds as well as methods for the preparation of the compounds are also disclosed.
摘要翻译： 某些四取代的烷基，芳基，吡啶基，哌啶基和哌嗪基脲化合物刺激乙酰胆碱的释放，因此可用于缓解疼痛或用作改善老年人认知衰退症状的胆碱能药物的镇痛药。 这些化合物具有通式“IMAGE”，其中R 1，R 2和R 4是苯基或取代的苯基，R 3是吡啶基。 还公开了包括这些化合物的药物组合物以及制备化合物的方法。
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7.发明授权(Substituted-phenyl)-5-oxo-2-pyrrolidinepropanoic acids and esters thereof, and use for reversing electroconvulsive shock-induced amnesia 失效（取代的苯基）-5-氧代-2-吡咯烷丙酸及其酯，用于逆转电惊厥性休克诱发的遗忘症
公开(公告)号：US4584313A
公开(公告)日：1986-04-22
申请号：US607376
申请日：1984-05-07
IPC分类号： A61K31/40 , A61K31/4015 , A61P25/28 , C07D207/26 , C07D207/36
CPC分类号： C07D207/26
摘要： Certain 5-oxo-3-(unsubstituted-phenyl)- or 5-oxo-3-(substituted phenyl)-2-pyrrolidinepropanoic acids and 5-oxo-.beta.-(unsubstituted-phenyl)- or 5-oxo-.beta.-(substituted-phenyl)-2-pyrrolidinepropanoic acids, their pharmaceutically acceptable esters and metal and amine cation salts, pharmaceutical compositions employing these compounds, and a method of treating senility or of reversing amnesia are disclosed.
摘要翻译： 某些5-氧代-3-（未取代的 - 苯基） - 或5-氧代-3-（取代的苯基）-2-吡咯烷丙酸和5-氧代-β-（未取代的 - 苯基） - 或5-氧代-β-（ 苯基）-2-吡咯烷丙酸，其药学上可接受的酯和金属和胺阳离子盐，使用这些化合物的药物组合物，以及治疗衰老或逆转遗忘症的方法。
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8.发明授权Oxime and amine substituted azabicyclo and azocyclo muscarinic agonists and methods of treatment 失效肟和胺取代的氮杂双环和偶氮环毒蕈碱激动剂和治疗方法
公开(公告)号：US5306718A
公开(公告)日：1994-04-26
申请号：US778412
申请日：1991-10-16
IPC分类号： A61K31/395 , A61K31/397 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/439 , A61K31/4439 , A61K31/46 , A61P25/00 , A61P25/02 , A61P25/04 , A61P25/28 , A61P43/00 , C07D205/06 , C07D207/22 , C07D211/72 , C07D223/06 , C07D225/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D451/02 , C07D451/04 , C07D451/06 , C07D451/10 , C07D453/02 , C07D471/08 , C07D487/08 , A61K31/00
CPC分类号： C07D487/08 , C07D211/72 , C07D451/04 , C07D453/02
摘要： Pharmaceutically useful nitrogen containing cyclic oxime and amine substituted compounds of the following general Formulas I, II and III are disclosed: ##STR1## Specifically the compounds are azabicyclo [2.2.1] omimes, azabicyclo [2.2.2] oximes, azabicyclo [2.2.1] amines, azabicyclo [2.2.2] amines, azabicyclo [3.2.1] oximes and amine containing heterocyclic oximes wherein the heterocyclic ring contains from 4 to 5 [3 to 7] carbon atoms.
摘要翻译： 公开了以下通式I，II和III的药用有用的含氮环状肟和胺取代的化合物：（*化学结构*）Ia（*化学结构*）IIb（*化学结构*）IIIc（*化学结构*） IVd具体地，化合物是氮杂双环（2.2.1），次氮杂双环（2.2.2）肟，氮杂双环（2.2.1）胺，氮杂双环（2.2.2）胺，氮杂双环（3.2.1）肟和含胺杂环肟，其中 该杂环含有4至5个（3至7个）碳原子。
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9.发明授权4-(N-substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof as centrally acting muscarinic agents 失效4-（N-取代氨基）-2-丁炔基-1-脲和硫脲及其衍生物作为中枢作用毒蕈碱药
公开(公告)号：US4988688A
公开(公告)日：1991-01-29
申请号：US388785
申请日：1989-08-02
IPC分类号： A61K31/17 , A61K31/40 , A61K31/445 , A61K31/535 , A61K31/5375 , A61P25/02 , A61P25/28 , B01J27/055 , B01J27/122 , C07B61/00 , C07C273/18 , C07C275/20 , C07C275/22 , C07C335/10 , C07C335/14 , C07D227/04 , C07D229/00 , C07D233/36 , C07D239/10 , C07D295/12 , C07D295/125 , C07D295/13 , C07D295/20
CPC分类号： C07D295/13 , C07C275/20
摘要： 4-(N-Substituted amino)-2-butynyl-1-ureas and thioureas and derivatives thereof are described, as well as methods for the preparation and pharmaceutical compositions of same, which are useful as centrally acting muscarinic agents and are useful as analgesic agents for the treatment of pain, as sleep aids and as agents for treating the symptoms of senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesia, hyperkinesia, mania, or similar conditions of cerebral insufficiency characterized by decreased cerebral acetylcholine production or release.
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10.发明授权Method of treating senile cognitive decline with N'-substituted aminopyridine adrenergic agents 失效用N-取代氨基吡啶肾上腺素能药物治疗老年认知衰退的方法
公开(公告)号：US4855308A
公开(公告)日：1989-08-08
申请号：US128831
申请日：1987-12-04
IPC分类号： C07D213/74 , C07D213/75
CPC分类号： C07D213/74 , C07D213/75
摘要： A method is disclosed for the treatment or amelioration of the symptoms of cerebral insufficiency characterized by decreased central adrenergic and/or cholinergic function employing certain N-substituted aminopyridines.
摘要翻译： 公开了一种用于治疗或改善脑功能不全的症状的方法，其特征在于使用某些N-取代的氨基吡啶使中枢肾上腺素能和/或胆碱能功能降低。
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