公开(公告)号：US20080020010A1

公开(公告)日：2008-01-24

申请号：US11827959

申请日：2007-07-13

申请人： Vasu Nair ,  Byung I. Seo ,  Vinod R. Uchil

发明人： Vasu Nair ,  Byung I. Seo ,  Vinod R. Uchil

IPC分类号： A61K31/4412 ,  A61K9/02 ,  A61K9/72 ,  A61P31/18 ,  C07D211/86

CPC分类号： C07D213/64 ,  C07D213/68

摘要： A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other integrase-based anti-HIV agents). Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.

摘要翻译： 描述了在吡啶酮支架上构建的一类新的二酮酸，其通过抑制HIV整合酶设计为HIV复制的抑制剂。 这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用， 疫苗和其他治疗剂，特别是其它抗HIV化合物（包括其它基于整合酶的抗HIV药物）。 还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

公开(公告)号：US07888375B2

公开(公告)日：2011-02-15

申请号：US11827959

申请日：2007-07-13

申请人： Vasu Nair ,  Byung I. Seo ,  Vinod R. Uchil

发明人： Vasu Nair ,  Byung I. Seo ,  Vinod R. Uchil

IPC分类号： A61K31/44 ,  C07D211/86

CPC分类号： C07D213/64 ,  C07D213/68

摘要： A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HIV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other integrase-based anti-HIV agents). Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.

摘要翻译： 描述了在吡啶酮支架上构建的一类新的二酮酸，其通过抑制HIV整合酶被设计为HIV复制的抑制剂。 这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用， 疫苗和其他治疗剂，特别是其它抗HIV化合物（包括其它基于整合酶的抗HIV药物）。 还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。

公开(公告)号：US20100092427A1

公开(公告)日：2010-04-15

申请号：US12309017

申请日：2007-07-13

申请人： Vasu Nair ,  Byung I. Seo ,  Vinod R. Uchil ,  Guochen Chi

发明人： Vasu Nair ,  Byung I. Seo ,  Vinod R. Uchil ,  Guochen Chi

IPC分类号： A61K31/4412 ,  C07D213/64 ,  A61K38/21 ,  A61K39/395 ,  A61P31/18

CPC分类号： C07D213/64 ,  C07D213/68

摘要： A new class of diketo acids constructed on pyridinone scaffolds, designed as inhibitors of HTV replication through inhibition of HIV integrase, is described. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described. Compounds of the present application include those of formula I and include tautomers, regioisomers, geometric isomers, and pharmaceutically acceptable salts thereof, wherein the pyridinone scaffold and R groups are as otherwise defined in the specification. These are combined, with any number of typical other anti-HIV agents (including other integrase-based anti-HIV agents) and other combination therapeutic agents described herein, to provide an effective treatment modality for HIV infections, including AIDS and ARC.

摘要翻译： 描述了在吡啶酮支架上构建的一类新的二酮酸，其通过抑制HIV整合酶设计为HTV复制的抑制剂。 这些化合物可用于预防或治疗艾滋病毒感染和治疗AIDS和ARC，作为化合物或作为药学上可接受的盐与药学上可接受的载体，单独使用或与抗病毒剂，免疫调节剂，抗生素联合使用， 疫苗和其他治疗剂，特别是可用于产生组合抗HIV鸡尾酒的其它抗HIV化合物（包括其它抗HIV整合酶试剂）。 还描述了治疗AIDS和ARC的方法以及治疗或预防HIV感染的方法。 本申请的化合物包括式I的化合物，并且包括互变异构体，区域异构体，几何异构体及其药学上可接受的盐，其中吡啶酮支架和R基团如本说明书另有定义。 将这些与任何数量的典型的其它抗HIV剂（包括其它基于整合酶的抗HIV剂）和本文所述的其它组合治疗剂组合起来，为HIV感染（包括AIDS和ARC）提供有效的治疗方式。