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公开(公告)号：US07807677B2
公开(公告)日：2010-10-05
申请号：US11884224
申请日：2006-02-09
IPC分类号： C07C271/22 , C07C275/24 , C07C311/06 , C07D213/42 , C07D241/12 , A61K31/18 , A61K31/17 , A61K31/325 , A61K31/38
CPC分类号： C07D213/42 , C07C271/22 , C07C275/24 , C07C311/06 , C07C2602/08 , C07D241/12 , C07D261/08 , C07D263/52 , C07D303/48 , C07D307/33 , C07D317/58 , C07D333/58
摘要： Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A′ and A″ are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.
摘要翻译： 式I化合物：其中R1，R2，X和N如说明书中所定义; E为N，CH; A'和A“是说明书中定义的末端基团。 该化合物可用作HIV-1蛋白酶抑制剂。
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2.发明申请(2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS 失效（2,5-DIOXOIMIDAZOLIDIN-I-YL）-N-羟基 - 乙酰胺作为金属蛋白酶抑制剂公开(公告)号：US20120015994A1
公开(公告)日：2012-01-19
申请号：US13222883
申请日：2011-08-31
申请人： Hans WALLBERG , Ming-Hua Xu , Guo-Qiang Lin , Xin-Sheng Lei , Piaoyang Sun , Kevin Parkes , Tony Johnson , Bertil Samuelsson
发明人： Hans WALLBERG , Ming-Hua Xu , Guo-Qiang Lin , Xin-Sheng Lei , Piaoyang Sun , Kevin Parkes , Tony Johnson , Bertil Samuelsson
IPC分类号： A61K31/4166 , A61P11/06 , A61P11/00 , C07D233/72
CPC分类号： C07D233/78 , C07D233/76
摘要： The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).
摘要翻译： 本发明提供式（I）化合物，其中变量如说明书中所定义。 本发明的化合物是金属蛋白酶MMP-12的抑制剂，也可用于治疗阻塞性气道疾病，如慢性阻塞性肺疾病（COPD）。
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3.发明授权公开(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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4.发明授权(2,5-dioxoimidazolidin-1-yl)-N-hydroxy-acetamides as metalloproteinase inhibitors 失效（2,5-二氧代咪唑烷-1-基）-N-羟基 - 乙酰胺作为金属蛋白酶抑制剂公开(公告)号：US08022092B2
公开(公告)日：2011-09-20
申请号：US12097192
申请日：2006-12-13
申请人： Hans Wallberg , Ming-Hua Xu , Guo-Qiang Lin , Xin-Sheng Lei , Piaoyang Sun , Kevin Parkes , Tony Johnson , Bertil Samuelsson
发明人： Hans Wallberg , Ming-Hua Xu , Guo-Qiang Lin , Xin-Sheng Lei , Piaoyang Sun , Kevin Parkes , Tony Johnson , Bertil Samuelsson
IPC分类号： C07D233/64 , A61K31/4164 , A61K31/4166
CPC分类号： C07D233/78 , C07D233/76
摘要： The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).
摘要翻译： 本发明提供式（I）化合物，其中变量如说明书中所定义。 本发明的化合物是金属蛋白酶MMP-12的抑制剂，也可用于治疗阻塞性气道疾病，如慢性阻塞性肺疾病（COPD）。
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公开(公告)号：US07671032B2
公开(公告)日：2010-03-02
申请号：US10572349
申请日：2005-01-28
申请人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Bertil Samuelsson , Hans Wallberg
发明人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Bertil Samuelsson , Hans Wallberg
CPC分类号： A61K31/47 , C07C235/40 , C07C237/04 , C07C237/10 , C07C247/04 , C07C271/22 , C07C281/02 , C07C309/73 , C07C311/51 , C07C2601/02 , C07C2601/08 , C07C2601/10 , C07D207/16 , C07D215/20 , C07D215/233 , C07D245/04 , C07D401/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/04 , C07D417/14 , C07D487/04 , C07K5/0205 , C07K5/06034 , C07K5/06052
摘要： Peptidomimetic compounds are described which inhibit the NS3 protease of the hepatitis C virus (HCV). The compounds have the formula where the variable definitions are as provided in the specification. The compounds comprise a carbocyclic P2 unit in conjunction with a novel linkage to those portions of the inhibitor more distal to the nominal cleavage site of the native substrate, which linkage reverses the orientation of peptidic bonds on the distal side relative to those proximal to the cleavage site.
摘要翻译： 描述了抑制丙型肝炎病毒（HCV）的NS3蛋白酶的拟肽化合物。 化合物具有式，其中变量定义如说明书中所提供。 这些化合物包括碳环P2单元，其与与天然底物的标称切割位点更远侧的抑制剂的那些部分的新连接结合，该连接反转了远端侧的肽键相对于接近切割的位置的取向 现场。
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6.发明申请(2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS 失效（2,5-DIOXOIMIDAZOLIDIN-I-YL）-N-羟基 - 乙酰胺作为金属蛋白酶抑制剂公开(公告)号：US20090215846A1
公开(公告)日：2009-08-27
申请号：US12097192
申请日：2006-12-13
申请人： Hans Wallberg , Ming-Hua Xu , Guo-Qiang Lin , Xin-Sheng Lei , Piaoyang Sun , Kevin Parkes , Tony Johnson , Bertil Samuelsson
发明人： Hans Wallberg , Ming-Hua Xu , Guo-Qiang Lin , Xin-Sheng Lei , Piaoyang Sun , Kevin Parkes , Tony Johnson , Bertil Samuelsson
IPC分类号： A61K31/4174 , C07D233/74 , A61P11/00
CPC分类号： C07D233/78 , C07D233/76
摘要： The invention provides compounds of the formula (I) wherein the variables are as defined in the specification. The compounds of the invention are inhibitors of metalloproteinase MMP-12 and are among other things useful for the treatment of obstructive airway diseases, such as chronic obstructive pulmonary disease (COPD).
摘要翻译： 本发明提供式（I）化合物，其中变量如说明书中所定义。 本发明的化合物是金属蛋白酶MMP-12的抑制剂，也可用于治疗阻塞性气道疾病，如慢性阻塞性肺疾病（COPD）。
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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。
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公开(公告)号：US06458772B1
公开(公告)日：2002-10-01
申请号：US09249317
申请日：1999-02-12
申请人： Xiao-Xiong Zhou , Nils Gunnar Johansson , Horst Wahling , Christian Sund , Hans Wallberg , Lourdes Salvador , Stefan Lindstrom , Christer Sahlberg
发明人： Xiao-Xiong Zhou , Nils Gunnar Johansson , Horst Wahling , Christian Sund , Hans Wallberg , Lourdes Salvador , Stefan Lindstrom , Christer Sahlberg
IPC分类号： A61K3170
CPC分类号： C07D213/80 , C07C271/22 , C07D213/85 , C07D307/68 , C07D473/32 , C07D513/04 , C07F9/4006 , C07F9/404 , C07F9/4075 , C07F9/572 , C07H17/08 , C07H19/00 , C07H19/16 , C40B40/00
摘要： Compounds of the formula I or corresponding monohydroxynucleoside derivatives wherein: R1 is hydroxy, amino or carboxy: optionally having esterified/amide bonded thereon; a C4-C22 saturated or unsaturated, optionally substituted fatty acid or alcohol, or an aliphatic L-amino acid; R2 is the residue of an aliphatic L-amino acid; L1 is a trifunctional linker group; L2 is absent or a difunctional linker group; and pharmaceutically acceptable salts thereof have favorable pharmacological properties and are antivirally active.
摘要翻译： 式I或相应的单羟基核苷衍生物的化合物，其中：R 1是羟基，氨基或羧基：任选地在其上键合有酯化/酰胺; C 4 -C 22饱和或不饱和，任选取代的脂肪酸或醇或脂族L-氨基酸; R 2 是脂族L-氨基酸的残基; L1是三官能连接基团; L2不存在或双官能连接基团;其药学上可接受的盐具有有利的药理学性质并具有抗病毒活性。
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公开(公告)号：US20080249102A1
公开(公告)日：2008-10-09
申请号：US11884224
申请日：2006-02-09
IPC分类号： A61K31/4965 , C07C233/00 , A61K31/164 , C07D303/00 , A61K31/336 , A61K31/27 , C07C271/06 , C07C303/36 , A61K31/42 , A61P31/18 , C07D261/02 , A61K31/18 , C07C275/00 , A61K31/17 , C07D213/02 , A61K31/44 , C07D241/10
CPC分类号： C07D213/42 , C07C271/22 , C07C275/24 , C07C311/06 , C07C2602/08 , C07D241/12 , C07D261/08 , C07D263/52 , C07D303/48 , C07D307/33 , C07D317/58 , C07D333/58
摘要： Compounds of the formula I: wherein R1, R2, X and N are as defined in the specification; E is N, CH; A′ and A″ are terminal groups as defined in the specification. The compounds have utility as HIV-1 protease inhibitors.
摘要翻译： 式I化合物：其中R 1，R 2，X和N如说明书中所定义; E为N，CH; A'和A“是说明书中定义的末端基团。 该化合物可用作HIV-1蛋白酶抑制剂。
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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。
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