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1. 发明授权

US08853281B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US08853281B2
公开(公告)日：2014-10-07
申请号：US13139962
申请日：2009-12-18
申请人： Susana Ayesa , Anna Karin Belfrage , Bjorn Classon , Urszula Grabowska , Ellen Hewitt , Vladimir Ivanov , Daniel Jönsson , Pia Kahnberg , Peter Lind , Magnus Nilsson , Lourdes Odén , Mikael Pelcman , Horst Wähling
发明人： Susana Ayesa , Anna Karin Belfrage , Bjorn Classon , Urszula Grabowska , Ellen Hewitt , Vladimir Ivanov , Daniel Jönsson , Pia Kahnberg , Peter Lind , Magnus Nilsson , Lourdes Odén , Mikael Pelcman , Horst Wähling
IPC分类号： A01N33/02 , A61K31/13 , A01N37/00 , A61K31/21 , A01N33/00 , A61K31/16 , A01N37/18 , A61K31/165 , A01N35/00 , A61K31/12 , A01N33/18 , A01N33/24 , A61K31/04 , A01N29/00 , A61K31/02 , A01N29/02 , C07D231/00 , C07D413/00 , C07D295/22 , C07D307/02 , C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00 , C07C261/00 , C07C269/00 , C07C271/00 , C07D405/12 , C07D403/12 , C07C271/24 , C07D417/12 , C07C311/21 , C07D241/24 , C07D401/12 , C07D277/36 , C07D307/85 , C07D307/68 , C07D277/56 , C07D295/215 , C07C237/24 , C07D231/40 , C07D207/34 , C07D213/71 , C07D231/14 , C07D239/80 , C07D213/40
CPC分类号： C07C311/21 , C07C237/24 , C07C271/24 , C07C2601/02 , C07C2601/04 , C07C2601/06 , C07C2601/08 , C07D207/34 , C07D213/40 , C07D213/71 , C07D231/14 , C07D231/40 , C07D239/80 , C07D241/24 , C07D277/36 , C07D277/56 , C07D295/215 , C07D307/68 , C07D307/85 , C07D401/12 , C07D403/12 , C07D405/12 , C07D417/12
摘要： Compounds of the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain.
摘要翻译：式Ⅰ化合物，其中R1a是H; 并且R 1b是C 1 -C 6烷基，碳环或Het; 或R 1a和R 1b一起限定具有3-6个环原子的饱和环胺; R2a和R2b是H，卤素，C1-C4烷基，C1-C4卤代烷基，C1-C4烷氧基; 或R 2a和R 2b与它们所连接的碳原子一起形成C 3 -C 6环烷基; R3是支链C 5 -C 10烷基链，C 2 -C 4卤代烷基或C 3 -C 7环烷基甲基，R 4是Het，碳环基，如说明书中所定义的任选取代，以及其药学上可接受的盐，水合物和N-氧化物; 是组织蛋白酶S的抑制剂，并且可用于治疗牛皮癣，自身免疫性疾病和其它疾病如哮喘，动脉硬化，COPD和慢性疼痛。

2. 发明申请

US20110112089A1 Cysteine Protease Inhibitors 审中-公开
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US20110112089A1
公开(公告)日：2011-05-12
申请号：US13009773
申请日：2011-01-19
申请人： Magnus NILSSON , Xiao-Xiong ZHOU , Lourdes ODEN , Bjorn CLASSON , Rolf NOREN , Urszula GRABOWSKA , Philip JACKSON , Philip FALLON , Andrew CARR , Mark LILEY , Matt TOZER , Tony JOHNSON , Victor DIAZ , Laia CRESPO , Jussi KANGASMETSA , Thierry BONNAUD
发明人： Magnus NILSSON , Xiao-Xiong ZHOU , Lourdes ODEN , Bjorn CLASSON , Rolf NOREN , Urszula GRABOWSKA , Philip JACKSON , Philip FALLON , Andrew CARR , Mark LILEY , Matt TOZER , Tony JOHNSON , Victor DIAZ , Laia CRESPO , Jussi KANGASMETSA , Thierry BONNAUD
IPC分类号： A61K31/5365 , A61K31/407 , A61K31/427 , A61K31/454 , A61K31/497 , A61K31/4439 , A61K31/4178 , A61P19/10 , A61P35/00 , A61P37/00 , A61P19/08
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(═O)2; where Ra is H, C1-C4 alkyl or CH3C(═O); R5 is independently selected from H or methyl; E is —C(═O)—, —S(═O)m—, —NR5S(═O)m—, —NR5C(═O)—, —OC(═O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or hetorocycle; m is independently 0, 1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：式II的化合物，其中R 1和R 2中的一个是卤素，另一个是H或卤素; R3是C1-C4直链或支链，任选氟化的烷基; R4是H; 或R 3与R 4一起，相邻的主链碳定义：任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O，NR a，S，S（= O）2的杂原子的C 4 -C 6饱和杂环; 其中R a是H，C 1 -C 4烷基或CH 3 C（= O）; R5独立地选自H或甲基; E是-C（= O） - ， - S（= O）m - ， - NR 5 S（= O）m - ， - NR 5 C（= O） - ， - OC（= O）取代的，单环或双环的，碳环或环状的; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

3. 发明授权

US06489364B2 Antiviral protease inhibitors 失效
标题翻译：抗病毒蛋白酶抑制剂
公开(公告)号：US06489364B2
公开(公告)日：2002-12-03
申请号：US09887758
申请日：2001-06-21
申请人： Bjorn Classon , Ingemar Sven-Anders Kvarnstrom , Bengt Bertil Samuelsson
发明人： Bjorn Classon , Ingemar Sven-Anders Kvarnstrom , Bengt Bertil Samuelsson
IPC分类号： A01N3718
CPC分类号： C07D213/30 , C07C235/14 , C07C237/22 , C07C2601/02 , C07C2601/16 , C07C2602/08 , C07D213/40 , C07D277/24 , C07D309/10 , C07D333/16 , C07D405/12 , C07D407/12 , C07D493/04
摘要： Compounds of formula (I), wherein A′ and A″ are independently the same or different group of formula (II) wherein: R′ is H, CH3, C(CH3)2, —ORa, —N(Ra)2, —N(Ra)ORa or —DP; R′″ is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, —C(═O)—, —S(O)— or S(O)2—; P is an optionally substituted, mono or bicyclic carbo- or hetereocycle; R″ is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or —C(═O)N(R′″)—; Q is absent, a bond, —CH(OH)— or CH2—; or R″ together with Q, M and R′ define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R′ is —ORa, —, N(Ra)2, —N(Ra)ORa or -DP, if M is a bond and Q is absent; X is H, OH, OCH3, Y is H, OH, OCH3, but X and Y are not both H; Z′ and Z″ are independently —(CH2)mP where P is as defined above; n and m are independently 0, 1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-mannaro-1,4:6,3-dilactone intermediates.
摘要翻译：式（I）化合物，其中A'和A“独立地是相同或不同的式（II）基团，其中：R'是H，CH 3，C（CH 3）2，-OR a，-N（R a）2 ，-N（Ra）OR a或-DP; R“'是H或CH 3; R a是H，C 1 -C 3烷基; D是键，亚烷基，-C（= O） - ， - S（O） - 或S（O）2 - P是任选取代的单或双环碳 - 或杂环; R“是H，在天然氨基酸，羧基乙酰胺或（CH 2）nDP基团中发现的任何侧链; M是键或-C（= O）N（R“'） - ; Q不存在，键，-CH（OH） - 或CH2-; 或R“与Q，M和R'一起定义任选取代的5或6元碳环或杂环，其任选地与另外的5或6元碳环或杂环稠合; 条件是R'为-OR a， - ，N（R a）2，-N（R a）OR a或-DP，若M为键且Q不存在; X是H，OH，OCH 3，Y是H，OH，OCH 3，但X和Y不同时为H; Z'和Z“独立地为 - （CH 2）m P，其中P如上所定义; n和m独立地为0,1或2; 其药学上可接受的盐和前药具有用作HIV的天冬氨酰蛋白酶抑制剂。它们可以从新的2,5-di-O-苄基-L-肉豆蔻酰-1,4：6,3-二酮中间体的容易的两步合成中制备。

4. 发明申请

US20100003216A1 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：US20100003216A1
公开(公告)日：2010-01-07
申请号：US12557638
申请日：2009-09-11
申请人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Susana Ayesa , Bjorn Classon , Laszlo Rakos , Bertil Samuelsson
发明人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Susana Ayesa , Bjorn Classon , Laszlo Rakos , Bertil Samuelsson
IPC分类号： A61K38/21 , A61K31/47 , A61K38/06 , A61P31/12
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： Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus sych as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and 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：变量如本说明书中定义的式的化合物抑制黄病毒sych的NS3蛋白酶作为丙型肝炎病毒（HCV）。化合物包括杂环P2单元和更远离天然底物标称切割位点的那些抑制剂部分之间的新连接，该连接反转相对于靠近切割位点的末端侧的肽键的取向。

5. 发明申请

US20080234260A1 Cysteine Protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US20080234260A1
公开(公告)日：2008-09-25
申请号：US10584930
申请日：2005-01-06
申请人： Magnus Nilsson , Xiao-Xiong Zhou , Lourdes Oden , Bjorn Classon , Rolf Noren , Urszula Grabowska , Philip Jackson , Philip Fallon , Andrew Carr , Mark Liley , Matt Tozer , Tony Johnson , Victor Diaz , Laia Crespo , Jussi Kangasmetsa , Thierry Bonnaud
发明人： Magnus Nilsson , Xiao-Xiong Zhou , Lourdes Oden , Bjorn Classon , Rolf Noren , Urszula Grabowska , Philip Jackson , Philip Fallon , Andrew Carr , Mark Liley , Matt Tozer , Tony Johnson , Victor Diaz , Laia Crespo , Jussi Kangasmetsa , Thierry Bonnaud
IPC分类号： A61K31/5377 , C07D491/048 , A61K31/407 , A61P19/00 , A61K31/496
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(═O)2; where Ra is H, C1-C4 alkyl or CH3C(═O); R5 is independently selected from H or methyl; E is —C(═O)—, —S(═O)m—, —NR5S(═O)m—, —NR5C(═O)—, —OC(═O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：式II的化合物，其中R 1和R 2中的一个为卤素，另一个为H或卤素; R 3是C 1 -C 4直链或支链，任选氟化的烷基; R 4是H; 或R 3连同R 4和邻位的主链碳定义：螺-C 5 -C 7 - 环烷基，任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4烷基的取代基取代。 4卤代烷基; 或任选地与亚甲基桥连; 或具有选自O，NRa，S，S（-O）2）的杂原子的C 4 -C 6 -C 6饱和杂环。其中R a是H，C 1 -C 4烷基或CH 3 C（-O）; R 5独立地选自H或甲基; E是-C（-O） - ， - S（-O）m - ， - NR 5 S（-O）m - ，-NR 5 C（-O） - ， - OC（-O） - ，R 6是稳定的，任选取代的单环或双环碳环或杂环; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

6. 发明申请

US20070161574A1 Hcv ns-3 serine protease inhibitors 有权
标题翻译： Hcv ns-3丝氨酸蛋白酶抑制剂
公开(公告)号：US20070161574A1
公开(公告)日：2007-07-12
申请号：US10572418
申请日：2005-01-28
申请人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Susana Ayesa , Bjorn Classon , Laszlo Rakos , Bertil Samuelsson
发明人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Susana Ayesa , Bjorn Classon , Laszlo Rakos , Bertil Samuelsson
IPC分类号： A61K38/05 , A61K38/04 , C07K5/10 , C07K5/08
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： Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus such as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and 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：变量如本说明书中所定义的式的化合物抑制黄病毒如NSC蛋白酶如丙型肝炎病毒（HCV）。化合物包括杂环P2单元和更远离天然底物标称切割位点的那些抑制剂部分之间的新连接，该连接反转相对于靠近切割位点的末端侧的肽键的取向。

7. 发明授权

US06291687B1 Antiviral protease inhibitors 失效
标题翻译：抗病毒蛋白酶抑制剂
公开(公告)号：US06291687B1
公开(公告)日：2001-09-18
申请号：US09402499
申请日：1999-12-14
申请人： Bjorn Classon , Ingemar Sven-Anders Kvarnstrom , Bengt Bertil Samuelsson
发明人： Bjorn Classon , Ingemar Sven-Anders Kvarnstrom , Bengt Bertil Samuelsson
IPC分类号： C07D49304
CPC分类号： C07D213/30 , C07C235/14 , C07C237/22 , C07C2601/02 , C07C2601/16 , C07C2602/08 , C07D213/40 , C07D277/24 , C07D309/10 , C07D333/16 , C07D405/12 , C07D407/12 , C07D493/04
摘要： Compounds of the formula I: wherein: A′ and A″ are independently the same or different group of the formula II: wherein: R′ is H. CH3, C(CH3)2, —ORa, —N(Ra)2, —N(Ra)ORa or —DP R′″ is H or CH3; Ra is H, C1-C3 alkyl; D is a bond, alkylene, —C(═O)—, —S(O)— or —S(O)2—; P is an optionally substituted, mono or bicyclic carbo- or heterocycle; R″ is H, any of the sidechains found in the natural amino acids, carboxacetamide, or a group (CH2)nDP; M is a bond or —C(═O)N(R′″)—; Q is absent, a bond, —CH(OH)— or —CH2—; or R″ together with Q , M and R′ define an optionally substituted 5 or 6 membered carbo- or heterocyclic ring which is optionally fused with a further 5 or 6 membered carbo- or heterocyclic ring; with the proviso that R′ is —ORa, —N(Ra)2, —N(Ra)ORa or —DP, if M is a bond and Q is absent; X is H, OH, OCH3; Y is H, OH, OCH3, but X and Y are not both H; Z′ and Z″ are independently —(CH2)mP where P is as defined above; n and m are independently 0,1 or 2; and pharmaceutically acceptable salts and prodrugs thereof have utility as aspartyl protease inhibitors of HIV. They can be prepared in a facile two step synthesis from novel 2,5-di-O-benzyl-L-maannaro-1,4:6,3 dilactone intermediates.
摘要翻译：式I化合物：其中：A'和A“独立地是相同或不同的式II的基团：其中：R'是H.CH 3，C（CH 3）2，-OR a，-N（R a）2 ，-N（R a）OR a或-DPR“'是H或CH 3; R a是H，C 1 -C 3烷基; D是键，亚烷基，-C（= O） - ， - S（O） - 或-S（O）2 - ; P是任选取代的单或双环碳 - 或杂环; R“是H，在天然氨基酸，羧基乙酰胺或（CH 2）nDP基团中发现的任何侧链; M是键或-C（= O）N（R”'） - ; Q不存在，-CH（OH） - 或-CH 2 - ;或R'与Q，M和R'一起定义任选取代的5或6元碳环或杂环，其任选地与另外的 5或6元碳环或杂环;条件是R'为-OR a，-N（R a）2，-N（R a）OR a或-DP，若M为键且Q不存在; X为H ，OH，OCH 3; Y是H，OH，OCH 3，但X和Y不同时为H; Z'和Z“独立地为 - （CH 2）m P，其中P如上所定义; n和m独立地为0,1 或2;及其药学上可接受的盐和前药可用作HIV的天冬氨酰蛋白酶抑制剂。它们可以从新的2,5-di-O-苄基-L-马那罗-1,4：6,3二酮中间体的容易的两步合成中制备。

8. 发明授权

US07915300B2 Cysteine protease inhibitors 有权
标题翻译：半胱氨酸蛋白酶抑制剂
公开(公告)号：US07915300B2
公开(公告)日：2011-03-29
申请号：US10584930
申请日：2005-01-06
申请人： Magnus Nilsson , Xiao-Xiong Zhou , Lourdes Oden , Bjorn Classon , Rolf Noren , Urszula Grabowska , Philip Jackson , Philip Fallon , Andrew Carr , Mark Liley , Matt Tozer , Tony Johnson , Victor Diaz , Laia Crespo , Jussi Kangasmetsa , Thierry Bonnaud
发明人： Magnus Nilsson , Xiao-Xiong Zhou , Lourdes Oden , Bjorn Classon , Rolf Noren , Urszula Grabowska , Philip Jackson , Philip Fallon , Andrew Carr , Mark Liley , Matt Tozer , Tony Johnson , Victor Diaz , Laia Crespo , Jussi Kangasmetsa , Thierry Bonnaud
IPC分类号： A61K31/407 , A61K31/34 , C07D487/04 , C07D307/00
CPC分类号： C07D491/04 , A61K31/407
摘要： A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(═O)2; where Ra is H, C1-C4 alkyl or CH3C(═O); R5 is independently selected from H or methyl; E is —C(═O)—, —S(═O)m—, —NR5S(═O)m—, —NR5C(═O)—, —OC(═O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.
摘要翻译：式II的化合物，其中R 1和R 2中的一个是卤素，另一个是H或卤素; R3是C1-C4直链或支链，任选氟化的烷基; R4是H; 或R 3与R 4一起，相邻的主链碳定义：任选被1至3个选自卤素，羟基，C 1 -C 4烷基或C 1 -C 4卤代烷基的取代基取代的螺C5-C7环烷基; 或任选地与亚甲基桥连; 或具有选自O，NR a，S，S（= O）2的杂原子的C 4 -C 6饱和杂环; 其中R a是H，C 1 -C 4烷基或CH 3 C（= O）; R5独立地选自H或甲基; E是-C（= O） - ， - S（= O）m - ， - NR 5 S（= O）m - ， - NR 5 C（= O） - ， - OC（= O）取代的，单环或双环的碳环或杂环; m独立地为0,1或2; 是组织蛋白酶K的抑制剂，可用于治疗或预防骨质疏松症。

9. 发明授权

US07608590B2 HCV NS-3 serine protease inhibitors 有权
标题翻译： HCV NS-3丝氨酸蛋白酶抑制剂
公开(公告)号：US07608590B2
公开(公告)日：2009-10-27
申请号：US10572418
申请日：2005-01-28
申请人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Susana Ayesa , Bjorn Classon , Laszlo Rakos , Bertil Samuelsson
发明人： Asa Rosenquist , Fredrik Thorstensson , Per-Ola Johansson , Ingemar Kvarnstrom , Susana Ayesa , Bjorn Classon , Laszlo Rakos , Bertil Samuelsson
IPC分类号： A61K38/00 , A61K38/04 , A61K38/05 , C07K5/08 , C07K5/10
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： Compounds of the formula where the variables are as defined in the specification inhibit the NS3 protease of flavivirus such as hepatitis C virus (HCV). The compounds comprise a novel linkage between a heterocyclic P2 unit and 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：变量如本说明书中所定义的式的化合物抑制黄病毒如NSC蛋白酶如丙型肝炎病毒（HCV）。化合物包括杂环P2单元和更远离天然底物标称切割位点的那些抑制剂部分之间的新连接，该连接反转相对于靠近切割位点的末端侧的肽键的取向。

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