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1. 发明授权

US07405310B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US07405310B2
公开(公告)日：2008-07-29
申请号：US11071675
申请日：2005-03-02
申请人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Oden , Lotta Naeslund
发明人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Oden , Lotta Naeslund
IPC分类号： C07D405/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
摘要翻译：本发明涉及对HIV-1有活性且具有改善的抗药性和药代动力学特征的非核苷逆转录酶抑制剂。本发明还涉及合成这些化合物的新型中间体以及该化合物在抗病毒方法和组合物中的用途。

2. 发明授权

US06716850B2 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US06716850B2
公开(公告)日：2004-04-06
申请号：US10092752
申请日：2002-03-05
申请人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
发明人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
IPC分类号： C07D40512
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CHR8)n-—D—(CHR8)m—; D is —NR9—, —O—, —S—, —S(═O)— or —S(═O)2—; R8 is independently H, C1-C3 alkyl, halo substitutedC1-C3alkyl; R9 is H, C1-C3 alkyl; n and m are independently 0, 1 or 2; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式I化合物：其中R 1为O，S; R 2为任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3为H，C 1 -C 3烷基，R 4 -R 7独立地选自H，C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，卤代C 1 -C 6烷基，C 1 -C 6烷酰基，卤代C 1 -C 6烷酰基，C 1 -C 6烷氧基，卤代C 1 -C 6烷氧基， C 1 -C 6烷氧基-C 1 -C 6烷基，卤代C 1 -C 6烷氧基-C 1 -C 6烷基羟基-C 1 -C 6烷基，氨基-C 1 -C 6烷基，羧基-C 1 -C 6烷基，氰基-C 1 -C 6烷基，氨基，羧基，氨基甲酰基，氰基，卤素，羟基，酮基; X是 - （CHR 8）n -D-（CHR 8）m - ; D是-NR 9 - ， - O - ， - S - ， - S（= O） - 或 -S（= O）2 - ; R 8独立地是H，C 1 -C 3烷基，卤素取代的C 1 -C 3烷基; R 9是H，C 1 -C 3烷基; n和m独立地是0,1或2;以及前药和药学上可接受的盐具有用作HIV-1逆转录酶的抑制剂，特别是药物逃逸突变体。

3. 发明申请

US20050240035A1 Non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂
公开(公告)号：US20050240035A1
公开(公告)日：2005-10-27
申请号：US11071675
申请日：2005-03-02
申请人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Oden , Lotta Naeslund
发明人： Stefan Lindstrom , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Oden , Lotta Naeslund
IPC分类号： C07D335/06 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P31/18 , A61P37/04 , A61P43/00 , C07C43/23 , C07C245/18 , C07D307/93 , C07D311/78 , C07D311/94 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.
摘要翻译：本发明涉及对HIV-1有活性且具有改善的抗药性和药代动力学特征的非核苷逆转录酶抑制剂。本发明还涉及合成这些化合物的新型中间体以及该化合物在抗病毒方法和组合物中的用途。

4. 发明授权

US06894177B2 Intermediate compounds of non-nucleoside reverse transcriptase inhibitors 失效
标题翻译：非核苷逆转录酶抑制剂的中间体化合物
公开(公告)号：US06894177B2
公开(公告)日：2005-05-17
申请号：US10377057
申请日：2003-02-28
申请人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
发明人： Stefan Lindström , Christer Sahlberg , Hans Wallberg , Genaidy Kalyanov , Lourdes Salvador Odén , Lotta Naeslund
IPC分类号： C07D335/06 , A61K31/4155 , A61K31/422 , A61K31/427 , A61K31/428 , A61K31/44 , A61K31/4433 , A61K31/4436 , A61K31/4709 , A61K31/497 , A61K31/506 , A61P31/18 , A61P37/04 , A61P43/00 , C07C43/23 , C07C245/18 , C07D307/93 , C07D311/78 , C07D311/94 , C07D401/12 , C07D405/12 , C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07D311/02
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CH2)n−—D—(CH2)m—; D is —O—, —S—; n and m are independently 0 or 1; and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.
摘要翻译：式I化合物：其中; R 1是O，S; R 2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R 3是H，C 1 -C 3烷基，R 4 -R 7，独立地选自H，C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，卤代C 1 -C 6烷基，C 1 -C 12烷基，C 1 -C 6烷基，C 1〜 C 6 -C 6烷酰基，C 1 -C 6烷酰基，C 1 -C 6烷酰基，烷氧基，卤代C 1 -C 6烷氧基，C 1 -C 6烷氧基-C

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