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公开(公告)号:US5874436A
公开(公告)日:1999-02-23
申请号:US842236
申请日:1997-04-23
申请人: James P. Demers , Sigmond Johnson , Michele Ann Weidner-Wells , Ramesh M. Kanojia , Stephanie A. Fraga , Dieter Klaubert
发明人: James P. Demers , Sigmond Johnson , Michele Ann Weidner-Wells , Ramesh M. Kanojia , Stephanie A. Fraga , Dieter Klaubert
IPC分类号: A61K31/137 , A61K31/14 , A61K31/155 , A61K31/165 , A61K31/167 , A61K31/192 , A61K31/194 , A61K31/216 , A61K31/41 , A61K31/4174 , A61K31/421 , A61K31/426 , A61K31/4418 , A61K31/4425 , A61K31/495 , A61K31/535 , C07C215/50 , C07C215/52 , C07C215/66 , C07C233/44 , C07C279/08 , C07C279/12 , C07C323/62 , C07D241/04 , C07D211/20 , C07D211/82 , C07D31/495
CPC分类号: C07C323/62 , A61K31/137 , A61K31/14 , A61K31/155 , A61K31/165 , A61K31/167 , A61K31/192 , A61K31/194 , A61K31/216 , A61K31/41 , A61K31/4174 , A61K31/421 , A61K31/426 , A61K31/4418 , A61K31/4425 , A61K31/495 , A61K31/535 , C07C215/50 , C07C215/52 , C07C215/66 , C07C233/44 , C07C279/08 , C07C279/12
摘要: The invention relates to triphenylalkyl antibacterial compounds of the general formula: ##STR1## pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of a bacterial histidine protein kinase and are thus useful as anti-infective agents against a variety of bacterial organisms, including organisms which are resistant to other known antibiotics.
摘要翻译: 本发明涉及以下通式的三苯基烷基抗菌化合物:含有化合物的药物组合物及其生产和使用方法。 这些化合物有效地抑制细菌组氨酸蛋白激酶的作用,因此可用作抗多种细菌生物体的抗感染剂,包括对其它已知抗生素具有抗性的生物体。
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公开(公告)号:US5679679A
公开(公告)日:1997-10-21
申请号:US348654
申请日:1994-12-02
申请人: Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人: Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号: A61K31/495 , C07D471/04 , C07D487/04 , C07D31/495 , C07D31/55
CPC分类号: C07D471/04 , A61K31/495 , C07D487/04
摘要: Certain aralkyl diazabicyloalkyl compounds are described for treatment of CNS disorders such as cerebral ischemia, psychoses and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein: each of R.sup.1, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 is independently selected from the group consisting of hydrido, loweralkyl, benzyl and haloloweralkyl; each of R.sup.2, R.sup.3, and R.sup.8 through R.sup.11 is independently selected from the group consisting of hydrido, hydroxy, loweralkyl, benzyl, phenoxy, benzyloxy and haloloweralkyl; n is an integer of from three to four; m is an integer of two; A is selected from the group consisting of phenyl, naphthyl, benzothienyl, benzofuranyl and thienyl and wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, loweralkyl, loweralkoxy, halo, haloloweralkyl, amino, monoloweralkylamino and diloweralkylamino; or a pharmaceutically acceptable salt thereof.
摘要翻译: 描述了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病如脑缺血,精神病和抽搐。 特别感兴趣的化合物具有下式:其中:R 1,R 4,R 5,R 6和R 7各自独立地选自氢,低级烷基,苄基和卤代低级烷基; R 2,R 3和R 8至R 11各自独立地选自氢,羟基,低级烷基,苄基,苯氧基,苄氧基和卤代低级烷基; n是3至4的整数; m是2的整数; A选自苯基,萘基,苯并噻吩基,苯并呋喃基和噻吩基,其中任何前述A基团可以进一步被一个或多个独立地选自羟基,羟基,低级烷基,低级烷氧基,卤代 ,卤代低级烷基,氨基,单低级烷基氨基和二低级烷基氨基; 或其药学上可接受的盐。
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公开(公告)号:US5958920A
公开(公告)日:1999-09-28
申请号:US954284
申请日:1997-10-20
申请人: Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
发明人: Wayne Bowen , Brian R. de Costa , Celia Dominguez , Xiao-Shu He , Kenner C. Rice
IPC分类号: A61K31/495 , C07D471/04 , C07D487/04 , C07D31/495 , C07D31/55
CPC分类号: C07D471/04 , A61K31/495 , C07D487/04
摘要: Certain aralkyl diazabicycloalkyl compounds are disclosed for treatment of CNS disorders, such as cerebral ischemia, psychosis and convulsions. Compounds of particular interest are of the formula: ##STR1## wherein m is three or four; wherein z is selected from the group consisting of ##STR2## wherein when Z is ##STR3## n and p are integers of from one to four, with a sum of four or five, and when Z is ##STR4## n and p are integers of from one to three, with a sum of three or four; wherein A is selected from the group consisting of aryl, heteroaryl, aryloxy, heteroaryloxy, aralkoxy, heteroaralkoxy, arylamino, heteroarylamino, aralkylamino, heteroaralkylamino, arylthio, heteroarylthio, aralkylthio, and heteroaralkylthio; wherein any of the foregoing A groups can be further substituted with one or more substituents independently selected from the group consisting of hydrido, hydroxy, alkyl, cycloalkyl, cycloalkylalkyl, aralkyl, aryl, alkoxy, aryloxy, aralkoxy, alkoxyalkyl, halo, haloalkyl, hydroxyalkyl, cyano, amino, monoalkylamino, dialkylamino, carboxy, carboxyalkyl, alkanoyl, alkenyl and alkynyl; or a pharmaceutically acceptable salt thereof.
摘要翻译: 公开了某些芳烷基二氮杂双环烷基化合物用于治疗中枢神经系统疾病,如脑缺血,精神病和抽搐。 特别感兴趣的化合物具有下式:其中m为三或四; 其中z选自其中当Z为n且p为1至4的整数时,其总数为4或5,当Z为n且p为1至3的整数时,其总和为 三或四; 其中A选自芳基,杂芳基,芳氧基,杂芳氧基,芳烷氧基,杂芳烷氧基,芳基氨基,杂芳基氨基,芳烷基氨基,杂芳烷基氨基,芳硫基,杂芳硫基,芳烷硫基和杂芳烷硫基。 其中前述A基团中的任一个可以进一步被一个或多个独立地选自羟基,羟基,烷基,环烷基,环烷基烷基,芳烷基,芳基,烷氧基,芳氧基,芳烷氧基,烷氧基烷基,卤素,卤代烷基, ,氰基,氨基,单烷基氨基,二烷基氨基,羧基,羧基烷基,烷酰基,烯基和炔基; 或其药学上可接受的盐。
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公开(公告)号:US5919784A
公开(公告)日:1999-07-06
申请号:US966040
申请日:1997-11-07
申请人: Daniel Lesieur , Pascal Carato , Jean-Paul Bonte , Patrick Depreux , Daniel-Henri Caignard , Mark Millan , Adrian Newman-Tancredi , Pierre Renard , Marie-Claire Rettori
发明人: Daniel Lesieur , Pascal Carato , Jean-Paul Bonte , Patrick Depreux , Daniel-Henri Caignard , Mark Millan , Adrian Newman-Tancredi , Pierre Renard , Marie-Claire Rettori
IPC分类号: A61K31/42 , A61K31/423 , A61K31/425 , A61K31/428 , A61K31/445 , A61K31/495 , A61K31/496 , A61K31/535 , A61K31/536 , A61K31/5377 , A61K31/538 , A61P25/00 , A61P25/18 , C07D263/58 , C07D265/36 , C07D277/68 , C07D279/16 , C07D413/06 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , A61K413/10 , A61K417/10 , C07D31/495 , C07D31/535
CPC分类号: C07D263/58 , C07D265/36 , C07D277/68 , C07D279/16
摘要: A compound of general formula (I): ##STR1## where A, X, R.sub.1, Y, n and Ar are defined in the description. Medicinal products containing the same are useful as D.sub.4 receptor Ligands.
摘要翻译: 通式(I)的化合物:其中A,X,R 1,Y,n和Ar在说明书中定义。 含有它们的药物可用作D4受体配体。
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