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1. 发明申请

WO2006084688A1 HIV protease inhibitors 审中-公开
标题翻译： HIV蛋白酶抑制剂
公开(公告)号：WO2006084688A1
公开(公告)日：2006-08-17
申请号：PCT/EP2006/001135
申请日：2006-02-09
申请人： MEDIVIR AB , EKEGREN Jenny , HALLBERG, Anders , WALLBERG, Hans , SAMUELSSON, Bertil , KANNAN, Mahalingan
发明人： EKEGREN Jenny , HALLBERG, Anders , WALLBERG, Hans , SAMUELSSON, Bertil , KANNAN, Mahalingan
IPC分类号： C07C271/22 , C07C311/06 , C07C275/24 , C07D213/42 , C07D241/12 , C07D333/58 , C07D317/58 , C07D261/08 , A61K31/18 , A61K31/17 , A61K31/325 , A61K31/38 , A61K31/42 , A61K31/44 , A61K31/495
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; A1 and A" are terminal groups as defined in the specification. The compounds have utility as HIV-I 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; A1和A“是本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。

2. 发明申请

WO2007048557A1 PROTEASE INHIBITORS 审中-公开
标题翻译： PROTEASE抑制剂
公开(公告)号：WO2007048557A1
公开(公告)日：2007-05-03
申请号：PCT/EP2006/010194
申请日：2006-10-23
申请人： MEDIVIR AB , SUND, Christian , LINDBORG, Björn , KALAYANOV, Genadiy , SAMUELSSON, Bertil , WALLBERG, Hans , HALLBERG, Anders
发明人： SUND, Christian , LINDBORG, Björn , KALAYANOV, Genadiy , SAMUELSSON, Bertil , WALLBERG, Hans , HALLBERG, Anders
IPC分类号： C07C271/22 , C07C311/06 , C07C275/24 , C07D213/42 , C07D241/12 , C07D333/58 , C07D317/58 , C07D261/08 , A61K31/18 , A61K31/17 , A61K31/325 , A61K31/38 , A61K31/42 , A61K31/44 , A61K31/495
CPC分类号： C07D213/42 , C07C271/22 , C07C275/24 , C07C2602/08 , C07D241/12 , C07D277/24 , C07D333/50
摘要： Compounds of the formula (I), wherein R 1 , R 2 , X and N are as defined in the specification; L is F, NH 2 , NHAlk or N(Alk) 2 n is 1 or 2; 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）的化合物，其中R 1，R 2，X和N如说明书中所定义; L是F，NH 2，NHAlk或N（Alk）2 n是1或2; 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。

3. 发明申请

WO2005073195A2 HCV NS-3 SERINE PROTEASE INHIBITORS 审中-公开
标题翻译： HCV NS-3丝氨酸蛋白酶抑制剂
公开(公告)号：WO2005073195A2
公开(公告)日：2005-08-11
申请号：PCT/SE2005/000097
申请日：2005-01-28
申请人： MEDIVIR AB , ROSENQUIST, Åsa , THORSTENSSON, Fredrik , JOHANSSON, Per-Ola , KVARNSTRÖM, Ingemar , SAMUELSSON, Bertil , WALLBERG, Hans
发明人： ROSENQUIST, Åsa , THORSTENSSON, Fredrik , JOHANSSON, Per-Ola , KVARNSTRÖM, Ingemar , SAMUELSSON, Bertil , WALLBERG, Hans
IPC分类号： C07D215/00
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：描述了拟肽化合物，其抑制丙型肝炎病毒（HCV）的NS3蛋白酶。该化合物具有下式，其中变量定义如说明书中所提供。所述化合物包含碳环P2单元以及与更远离天然底物的标称切割位点的抑制剂的那些部分的新型连接，该连接反转远侧的肽键相对于切割近侧的取向站点。

4. 发明申请

WO2007068474A1 (2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：（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：WO2007068474A1
公开(公告)日：2007-06-21
申请号：PCT/EP2006/012019
申请日：2006-12-13
申请人： MEDIVIR AB , JIANGSU HENGRUI MEDICINE COMPANY LIMITED , WALLBERG, Hans , XU, Ming, Hua , LIN, Guo, Qiang , LEI, Xin, Sheng , SUN, Piaoyang , PARKES, Kevin , JOHNSON, Tony , SAMUELSSON, Bertil
发明人： WALLBERG, Hans , XU, Ming, Hua , LIN, Guo, Qiang , LEI, Xin, Sheng , SUN, Piaoyang , PARKES, Kevin , JOHNSON, Tony , SAMUELSSON, Bertil
IPC分类号： C07D233/74 , C07D233/78 , C07D233/76
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，其它可用于治疗阻塞性气道疾病如慢性阻塞性肺疾病（COPD）。

5. 发明申请

WO2011023812A1 MICROSOMAL PROSTAGLANDIN E SYNTHASE-1 (MPGES1) INHIBITORS 审中-公开
标题翻译： MICROSOMAL PROSTAGLANDIN E SYNTHASE-1（MPGES1）抑制剂
公开(公告)号：WO2011023812A1
公开(公告)日：2011-03-03
申请号：PCT/EP2010/062596
申请日：2010-08-27
申请人： NOVASAID AB , WANNBERG, Johan , ALTERMAN, Mathias , MALM, Johan , STENBERG, Patric , WESTMAN, Jacob , WALLBERG, Hans
发明人： WANNBERG, Johan , ALTERMAN, Mathias , MALM, Johan , STENBERG, Patric , WESTMAN, Jacob , WALLBERG, Hans
IPC分类号： C07D401/04 , C07D401/14 , C07D407/14 , C07D417/14 , A61K31/454 , A61K31/4545 , A61P9/00 , A61P11/00 , A61P25/28 , A61P29/00 , A61P35/00 , A61P37/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： A compound of formula (I): as well as pharmaceutically acceptable salts thereof, and a pharmaceutical composition comprising the compound. The compound is useful for the treatment of disorder selected from inflammatory diseases, nociceptive pain, auto-immune disease, breathing disorders, fever, cancer, inflammation related anorexia, Alzheimer's disease and cardiovascular diseases.
摘要翻译：式（I）的化合物及其药学上可接受的盐以及包含该化合物的药物组合物。该化合物可用于治疗选自炎性疾病，伤害性疼痛，自身免疫疾病，呼吸障碍，发烧，癌症，炎症相关厌食症，阿尔茨海默氏病和心血管疾病的病症。

6. 发明申请

WO2003020705A1 UREA AND THIOUREA DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：尿素和硫脲衍生物作为非核苷酸逆转录酶抑制剂
公开(公告)号：WO2003020705A1
公开(公告)日：2003-03-13
申请号：PCT/EP2002/002346
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： SAHLBERG, Christer , ANTONOV, Dmitry , WALLBERG, Hans , NOREEN, Rolf
IPC分类号： C07D213/75
CPC分类号： C07D213/75 , C07D213/85
摘要： Compounds of the formula (I): where R 1 is O, S; R 2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R 3 is H, C 1 -C 3 alkyl, R 4 -R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, haloC 1 -C 6 alkyl, C 1 -C 6 alkanoyl, haloC 1 -C 6 alkanoyl, C 1 -C 6 alkoxy, haloC 1 -C 6 alkoxy, C 1 -C 6 alkyloxy-C 1 -C 6 alkyl, haloC 1 -C 6 alkyloxy-C 1 -C 6 alkyl hydroxy-C 1 -C 6 alkyl, amino-C 1 -C 6 alkyl, carboxy-C 1 -C 6 alkyl, cyano-C 1 -C 6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CR 8 R 9 ) n -, R 8 and R 9 are independently H, C 1 -C 3 alkyl, OH or R 8 and R 9 together are =0, n is 1, 2 or 3, 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）的化合物：其中R 1是O，S; R2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R3是H，C1-C3烷基，R4-R7独立地选自H，C1-C6烷基，C2-C6烯基，C2-C6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， C6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， 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 - （CR 8 R 9）n - ， - R 8和R 9独立地为H，C 1 -C 3烷基，OH或R 8和R 9一起为= 0，n为1,2或3，并且其前药和药学上可接受的盐可用作 HIV-1逆转录酶的抑制剂，特别是药物逃逸突变体。

7. 发明申请

WO2002070516A2 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO2002070516A2
公开(公告)日：2002-09-12
申请号：PCT/EP2002/002328
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： LINDSTRÖM, Stefan , SAHLBERG, Christer , WALLBERG, Hans , KALYANOV, Genaidy , ODÉN, Lourdes , NAESLUND, Lotta
IPC分类号： C07D407/12
CPC分类号： C07D417/12 , A61K31/4433 , A61K31/4436 , C07C43/23 , C07C245/18 , C07D307/93 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Compounds of Formula (I), where; R 1 is O, S; R 2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R 3 is H, C 1 -C 3 alkyl, R 4 -R 7 are independently selected from H, C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl, haloC 1 -C 6 alkyl, C 1 -C 6 alkanoyl, haloC 1 -C 6 alkanoyl, C 1 -C 6 alkoxy, haloC 1 -C 6 alkoxy, C 1 -C 6 alkyloxy-C 1 -C 6 alkyl, haloC 1 -C 6 alkyloxy-C 1 -C 6 alkyl hydroxy-C 1 -C 6 alkyl, amino-C 1 -C 6 alkyl, carboxy-C 1 -C 6 alkyl, cyano-C 1 -C 6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is -(CHR 8 ) n- -D-(CHR 8 ) m -; D is -NR 9 -, -O-, -S-, -S(=O)- or -S(=O)2-; R 8 is independently H, C 1 -C 3 alkyl, halo substitutedC 1 -C 3 alkyl;R 9 is H, C 1 -C 3 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）的化合物，其中; R1为O，S; R2是任选取代的含氮杂环，其中氮位于相对于（硫）脲键的2位; R3是H，C1-C3烷基，R4-R7独立地选自H，C1-C6烷基，C2-C6烯基，C2-C6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， C6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， 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） R8独立地是H，C1-C3烷基，卤素取代的C1-C3烷基; R9是H，C1-C3烷基; n和m独立地为0,1或2; 和其前药和药学上可接受的盐，可用作HIV-1逆转录酶的抑制剂，特别是药物逃逸突变体。

8. 发明公开

EP1423368A1 UREA AND THIOUREA DERIVATIVES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：脲和硫脲衍生物作为非核苷类逆转录酶抑制剂
公开(公告)号：EP1423368A1
公开(公告)日：2004-06-02
申请号：EP02735116.2
申请日：2002-03-04
申请人： MEDIVIR AB
发明人： SAHLBERG, Christer , ANTONOV, Dmitry , WALLBERG, Hans , NOREEN, Rolf
IPC分类号： C07D213/75 , C07D213/85 , A61K31/44 , A61P31/18
CPC分类号： C07D213/75 , C07D213/85
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 -(CR8R9)n-, R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are =0, n is 1, 2 or 3, and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.

9. 发明授权

EP1373261B1 CYCLOPROPAHETEROCYCLES AS NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 有权
标题翻译： CYCLOPROPAHETEROCYCLEN比非核苷逆转录酶抑制剂
公开(公告)号：EP1373261B1
公开(公告)日：2011-05-04
申请号：EP02748329.6
申请日：2002-03-04
申请人： Medivir AB
发明人： LINDSTRÖM, Stefan , SAHLBERG, Christer , WALLBERG, Hans , KALYANOV, Genaidy , ODEN, Lourdes , NAESLUND, Lotta
IPC分类号： C07D407/12 , C07D409/12 , C07D413/12 , C07D417/12 , A61K31/44 , A61K31/35 , A61P31/18 , 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： Compounds of 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.

10. 发明公开

EP1966153A1 (2,5-DIOXOIMIDAZOLIDIN-I-YL)-N-HYDROXY-ACETAMIDES AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：（2,5-二氧代咪唑烷-1-基）-N- hydroxyacetamides ALS金属蛋白酶
公开(公告)号：EP1966153A1
公开(公告)日：2008-09-10
申请号：EP06840975.4
申请日：2006-12-13
申请人： Medivir AB
发明人： WALLBERG, Hans , XU, Ming, Hua , LIN, Guo, Qiang , LEI, Xin, Sheng , SUN, Piaoyang , PARKES, Kevin , JOHNSON, Tony , SAMUELSSON, Bertil
IPC分类号： C07D233/74 , C07D233/78 , C07D233/76
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).

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