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公开(公告)号：US5744458A
公开(公告)日：1998-04-28
申请号：US899086
申请日：1997-07-23
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/4439 , A61K31/496 , A61P25/04 , C07D207/09 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D295/073 , C07D403/06 , C07D403/12 , C07D207/04
CPC分类号： C07D295/073 , A61K31/404 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compound of formula II has the structure: ##STR1## wherein X.sub.4, X.sub.5 ; R.sub.1, R.sub.2 ; and Ar and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂的方法。 式II化合物具有以下结构：其中X 4，X 5; R1，R2; Ar和n如说明书中所述。
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2.发明授权公开(公告)号：US06180623B2
公开(公告)日：2001-01-30
申请号：US09436057
申请日：1999-11-08
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： A61K31337
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04 , Y02A50/422
摘要： Compounds having kappa opioid agonist activity, compositions containing them and methods of using them as analgesics and anti-pruritic agents are provided. The compounds of formula IV have the structure: wherein X9; R1, R2, R3, R4; and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。式IV化合物具有以下结构：其中X 9; R 1，R 2，R 3，R 4; andn如说明书中所述。
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公开(公告)号：US07294647B2
公开(公告)日：2007-11-13
申请号：US10455545
申请日：2003-06-05
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04 , Y02A50/422
摘要： Compounds having kappa opioid agonist activity, compositions containing them and 5 method of using them as analgesics and pruritic agents are provided.The compounds of formulae I, II, III and IV have the structure: wherein X, X4, X5, X7, X9; R1, R2, R3, R4; and Y, Z and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和5种使用它们作为止痛剂和瘙痒剂的方法。 式I，II，III和IV的化合物具有以下结构：其中X，X 4，X 5，X 7，X， SUB> 9
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公开(公告)号：USRE38133E1
公开(公告)日：2003-06-03
申请号：US10066909
申请日：2002-02-04
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D40110
CPC分类号： A61K31/4439 , A61K31/404 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, III and IV have the structure: wherein: X, X4, X5, X7, X9; R1, R2, R3, R4; and Y, Z and n are as described in the specification.
摘要翻译： 具有κ阿片激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂的方法。式I，II，III和IV化合物具有以下结构：其中：X，X4，X5，X7，X9; R1，R2 ，R3，R4; 和Y，Z和n如说明书中所述。
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5.发明授权
公开(公告)号：US6028063A
公开(公告)日：2000-02-22
申请号：US307517
申请日：1999-05-07
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/496 , A61P17/04 , A61P25/04 , C07D207/09 , C07D207/12 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D273/08 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/675
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compounds of formula III having the structure: ##STR1## wherein Ar and X.sup.7 ;R.sub.1 and R.sub.2 ; andn are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。 具有以下结构的式III化合物：其中Ar和X 7; R1和R2; 和n如说明书中所述。
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公开(公告)号：US5945443A
公开(公告)日：1999-08-31
申请号：US34661
申请日：1998-03-03
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/4439 , A61K31/496 , A61P25/04 , C07D207/09 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D295/073 , C07D403/06 , C07D403/12 , C07D207/06
CPC分类号： C07D295/073 , A61K31/404 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compound of formulae IV having the structure: ##STR1## wherein X.sub.9 ;R.sub.1, R.sub.2, R.sub.3, R.sub.4 ;and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂的方法。 具有以下结构的式IV化合物：其中X 9; R1，R2，R3，R4; 和n如说明书中所述。
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7.发明授权
公开(公告)号：US5981513A
公开(公告)日：1999-11-09
申请号：US45522
申请日：1998-03-21
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/496 , A61P17/04 , A61P25/04 , C07D207/09 , C07D207/12 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D273/08 , C07D401/12 , C07D403/06 , C07D403/12 , C07D207/04
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compounds of formula II having the structure: ##STR1## wherein X.sub.4, X.sub.5 ;R.sub.1, R.sub.2 ; andAr and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。 具有以下结构的式II化合物：其中X 4，X 5; R1，R2; Ar和n如说明书中所述。
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8.发明授权Kappa agonist compounds pharmaceutical formulations and method of prevention and treatment of pruritus therewith 失效卡帕激动剂化合物药物制剂及其预防和治疗瘙痒的方法
公开(公告)号：US5763445A
公开(公告)日：1998-06-09
申请号：US891833
申请日：1997-07-14
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/496 , A61P17/04 , A61P25/04 , C07D207/09 , C07D207/12 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D273/08 , C07D401/12 , C07D403/06 , C07D403/12
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compounds of formular I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ; R.sub.1, R.sub.2, R.sub.3, R.sub.4 ; and Y, Z and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂和抗瘙痒剂的方法。 式I，II，III和IV的化合物具有以下结构：X（X），X（X），X R1，R2，R3，R4; Y，Z和n如说明书所述。
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9.发明授权公开(公告)号：US06960612B2
公开(公告)日：2005-11-01
申请号：US10455687
申请日：2003-06-05
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/405 , A61K31/4427 , A61K31/4439 , A61K31/495 , A61K31/496 , A61P17/04 , A61P25/04 , C07D207/09 , C07D207/12 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D273/08 , C07D401/12 , C07D403/06 , C07D403/12 , A61K31/44 , A61K31/675
CPC分类号： A61K31/404 , A61K31/40 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04 , Y02A50/422
摘要： Methods for prevention or treatment of pruritus are provided. The methods comprise administering to a patient an effective amount of a kappa opioid receptor agonist compound. The involved kappa opioid receptor agonist compounds are of the type represented by the following formula III wherein R1, R2, Ar, X7, and n are as defied in the specification.
摘要翻译： 提供预防或治疗瘙痒症的方法。 所述方法包括向患者施用有效量的κ阿片受体激动剂化合物。 所涉及的κ阿片样物质受体激动剂化合物是由下式III表示的类型，其中R 1，R 2，Ar，X 7， 和n在说明书中是不合适的。
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公开(公告)号：US5688955A
公开(公告)日：1997-11-18
申请号：US796078
申请日：1997-02-05
申请人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
发明人： Lawrence I. Kruse , An-Chih Chang , Diane L. DeHaven-Hudkins , John J. Farrar , Forrest Gaul , Virendra Kumar , Michael Anthony Marella , Alan L. Maycock , Wei Yuan Zhang
IPC分类号： C07D295/12 , A61K31/40 , A61K31/404 , A61K31/4439 , A61K31/496 , A61P25/04 , C07D207/09 , C07D209/08 , C07D209/18 , C07D209/42 , C07D213/56 , C07D241/04 , C07D403/06 , C07D403/12 , C07D401/10
CPC分类号： A61K31/404 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, III and IV have the structure: ##STR1## wherein X, X.sub.4, X.sub.5, X.sub.7, X.sub.9 ; R.sub.1, R.sub.2, R.sub.3, R.sub.4 ; and Y, Z and n are as described in the specification.
摘要翻译： 提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂的方法。 （I）其中X，X 4，X 5，X 7，X 9，X 9，X 9， R1，R2，R3，R4; Y，Z和n如说明书所述。
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