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公开(公告)号:US07598264B2
公开(公告)日:2009-10-06
申请号:US10587682
申请日:2005-03-09
申请人: Wei Han , Melissa Egbertson , John S. Wai , Linghang Zhuang , Rowena D. Ruzek , Debra S. Perlow , Mark Cameron , Bruce S. Foster , Ulf H. Dolling , R. Scott Hoerrner , Philip J. Pye , Remy Angelaud , Danny E. Mancheno , David Askin
发明人: Wei Han , Melissa Egbertson , John S. Wai , Linghang Zhuang , Rowena D. Ruzek , Debra S. Perlow , Mark Cameron , Bruce S. Foster , Ulf H. Dolling , R. Scott Hoerrner , Philip J. Pye , Remy Angelaud , Danny E. Mancheno , David Askin
IPC分类号: A01N43/42 , A61K31/44 , C07D471/02 , C07D491/02 , C07D498/02 , C07D513/02
CPC分类号: C07D471/04
摘要: Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: (I) wherein a, R1?, R2?, R3?, R4? and R5? are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译: 式I的羟基(四或六) - 氢化萘啶二酮化合物是HIV整合酶和HIV复制抑制剂的抑制剂:(I)其中a,R 1?,R 2? ,R 3 ?, R 4? 并且R 5? 在本文中定义。 这些化合物可用于预防和治疗艾滋病毒感染以及预防,延迟艾滋病的发病和治疗。 这些化合物用作抗感染和艾滋病作为化合物本身或以药学上可接受的盐的形式。 化合物及其盐可以用作药物组合物中的成分,任选与其它抗病毒剂,免疫调节剂,抗生素或疫苗组合使用。
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公开(公告)号:US20100056516A1
公开(公告)日:2010-03-04
申请号:US12373907
申请日:2007-07-13
申请人: Peter D. Williams , Shankar Venkatraman , H. Marie Langford , Boyoung Kim , Theresa M. Booth , Jay A. Grobler , Donnette Staas , Rowena D. Ruzek , Mark W. Embrey , Catherine M. Wiscount , Terry A. Lyle
发明人: Peter D. Williams , Shankar Venkatraman , H. Marie Langford , Boyoung Kim , Theresa M. Booth , Jay A. Grobler , Donnette Staas , Rowena D. Ruzek , Mark W. Embrey , Catherine M. Wiscount , Terry A. Lyle
IPC分类号: A61K31/4375 , C07D471/04 , C07D413/14 , A61K31/5377 , A61P31/18
CPC分类号: C07D471/04
摘要: 1-Hydroxy naphthyridine compounds (e.g., 1-hydroxy naphthyridin-2(1H)-one compounds of Formula I are inhibitors of HIV integrase and/or HIV RNase H and inhibitors of HIV replication: (I) wherein X and R1-R6 are as defined herein. The compounds are useful in the prophylaxis and treatment of infection by HIV and in the prophylaxis, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other anti-HIV agents such as HIV antivirals, immunomodulators, antibiotics and vaccines.
摘要翻译: 式I的1-羟基萘啶化合物(例如,1-羟基萘啶-2(1H) - 酮化合物是HIV整合酶和/或HIV核糖核酸酶H和HIV复制抑制剂的抑制剂:(I)其中X和R 1 -R 6是 这些化合物可用于预防和治疗艾滋病毒感染以及艾滋病的预防,延迟发作和治疗。该化合物用于抗艾滋病毒感染和艾滋病作为化合物本身或以其形式 化合物及其盐可用作药物组合物中的成分,任选地与其它抗HIV剂如HIV抗病毒剂,免疫调节剂,抗生素和疫苗组合使用。
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