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111. 发明授权

US06294554B1 Muscarinic antagonists 有权
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US06294554B1
公开(公告)日：2001-09-25
申请号：US09651652
申请日：2000-08-30
申请人： John W. Clader , Joseph A. Kozlowski , Stuart W. McCombie , Michael W. Miller , Susan F. Vice
发明人： John W. Clader , Joseph A. Kozlowski , Stuart W. McCombie , Michael W. Miller , Susan F. Vice
IPC分类号： A61K31445
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14
摘要： Amide derivatives of 1,4 di-substituted piperidine compounds of the formula or a pharmaceutically acceptable salt, ester or solvate thereof, wherein Q and Q1 are each —CH═, or one of Q and Q1 is —CH═ and the other is —N═; X is —CH2— or Y and Z are —C(R5)═, or one of Y and Z is —C(R5)═ and the other is —N═; R1 is 1 to 3 substituents selected from H, halogen and alkoxy; R2 and R5 are 1 to 3 substituents selected from H, halogen, alkyl and alkoxy; and R3 and R4 are H or (C1-C6)alkyl are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.
摘要翻译：式II的1,4-二取代哌啶化合物的酰胺衍生物或其药学上可接受的盐，酯或溶剂化物，其中Q和Q1各自为-CH =，或Q和Q1中的一个为-CH =，另一个为-N = ; X是-CH 2 - 或Y，Z是-C（R 5）=，或Y和Z之一是-C（R 5）=，另一个是-N =; R 1是1至3个选自H，卤素和烷氧基; R2和R5是1至3个选自H，卤素，烷基和烷氧基的取代基; 和R 3和R 4是H或（C 1 -C 6）烷基是用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和制备方法。

112. 发明授权

US6066636A Muscarinic antagonists 失效
标题翻译：毒蕈碱拮抗剂
公开(公告)号：US6066636A
公开(公告)日：2000-05-23
申请号：US340466
申请日：1999-06-28
申请人： Joseph A. Kozlowski , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice
发明人： Joseph A. Kozlowski , Stuart W. McCombie , Jayaram R. Tagat , Susan F. Vice
IPC分类号： C07D211/58 , C07D401/12 , C07D405/14 , C07D409/12 , A61K31/496 , C07D401/14 , C07D403/14 , C07D409/14
CPC分类号： C07D401/12 , C07D211/58 , C07D405/14 , C07D409/12
摘要： Heterocyclic derivatives of di-N-substituted piperazine or 1,4 di-substituted piperidine compounds in accordance with formula I (including all isomers, salts and solvates) ##STR1## wherein wherein one of Y and Z is --N-- and the other is --N-- or --CH--;X is --O--, --S--, --SO--, --SO.sub.2 -- or --CH.sub.2 --;Q is ##STR2## R is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R.sup.1, R.sup.2 and R.sup.3 are H or alkyl;R.sup.4 is alkyl, cycloalkyl or ##STR3## R.sup.5 is H, alkyl, --C(O)alkyl, arylcarbonyl, --SO.sub.2 alkyl, aryl-sulfonyl --C(O)Oalkyl, aryloxycarbonyl, --C(O)NH-alkyl or aryl-aminocarbonyl, wherein the aryl portion is optionally substituted;R.sup.6 is H or alkyl; andR.sup.7 is H, alkyl, hydroxyalkyl or alkoxyalkyl; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of treatment are also disclosed
摘要翻译：根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物的杂环衍生物（包括所有异构体，盐和溶剂化物），其中Y和Z之一是-N-并且另一个是-N- 或-CH-; X是-O - ， - S - ， - SO - ， - SO 2 - 或-CH 2 - ; Q是R是烷基，环烷基，任选取代的芳基或杂芳基; R1，R2和R3是H或烷基; R4是烷基，环烷基或R5是H，烷基，-C（O）烷基，芳基羰基，-SO2烷基，芳基 - 磺酰基-C（O）O烷基，芳氧基羰基，-C（O）NH-烷基或芳基 - 氨基羰基，芳基部分任选被取代; R6是H或烷基; 且R 7为H，烷基，羟基烷基或烷氧基烷基; 是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。还公开了药物组合物和治疗方法

113. 发明授权

US5241065A 2,3,4,5-tetrahydro-1H-3-benzazepines having anti-psychotic activity 失效
标题翻译：具有抗肌动蛋白活性的2,3,4,5-四氢-1H-苯并嗪
公开(公告)号：US5241065A
公开(公告)日：1993-08-31
申请号：US841603
申请日：1992-02-25
申请人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
发明人： Joel G. Berger , Wei K. Chang , Joseph A. Kozlowski , Guowei Zhou
IPC分类号： C07D217/24 , A61K31/55 , A61P25/00 , A61P25/18 , B01J31/24 , C07B61/00 , C07C231/12 , C07D209/34 , C07D213/56 , C07D223/16 , C07D225/06 , C07D233/64 , C07D277/30 , C07D307/54 , C07D333/24 , C07D491/056
CPC分类号： C07D223/16
摘要： A novel process for the preparation of .alpha.-substituted arylacetamides wherein the substituent is an aromatic group or a 1-alkenyl or 1-cycloalkenyl group and wherein the nitrogen atom carries no hydrogen atoms comprises the reaction of an arylacetamide having one or two hydrogen atoms on the .alpha.-carbon atom, wherein the nitrogen atom carries no hydrogen atoms, with a strong base in an inert aprotic organic solvent, followed by reaction with a zerovalent transition metal catalyst and then with a compound of the formula R.sup.4 --X, wherein R.sup.4 is selected from aromatic groups, 1-alkenyl groups and 1-cycloalkenyl groups and X is a particular leaving group, especially a triflate group. The .alpha.-substituted arylacetamides are useful as intermediates in the preparation (by reduction) of .alpha.-substituted arylethylamines, e.g., 1-substituted-2,3,4,5-tetrahydro-1H-3-benzazepines, having pharmacological activity. Certain benzazepines wherein the 1-substituent R.sup.4 is 1-(1-cycloalkenyl) are novel.
摘要翻译：用于制备α-取代的芳基乙酰胺的新方法，其中取代基是芳基或1-烯基或1-环烯基，其中氮原子不携带氢原子包括具有一个或两个氢原子的芳基乙酰胺与其中氮原子不携带氢原子，在惰性非质子有机溶剂中具有强碱，然后与零价过渡金属催化剂反应，然后与式R 4 -X的化合物反应，其中R 4为选自芳族基团，1-烯基和1-环烯基，X是特定的离去基团，特别是三氟甲磺酸酯基团。 α-取代的芳基乙酰胺可用作制备（通过还原）具有药理活性的α-取代的芳基乙胺，例如1-取代-2,3,4,5-四氢-1H-3-苯并氮杂的中间体。其中1-取代基R4是1-（1-环烯基）的某些苯并氮杂是新的。

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