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1. 发明授权

US06018020A Amino acid derivatives 失效
标题翻译：氨基酸衍生物
公开(公告)号：US06018020A
公开(公告)日：2000-01-25
申请号：US96570
申请日：1998-06-12
申请人： Michael Richard Attwood , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
发明人： Michael Richard Attwood , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
IPC分类号： C12N15/09 , A01N43/34 , A01N43/36 , A61K38/00 , A61P31/12 , A61P31/14 , C07C205/04 , C07C205/45 , C07C271/18 , C07D207/12 , C07D207/20 , C07D211/70 , C07D223/04 , C07D227/04 , C07D405/10 , C07D407/10 , C07D409/10 , C07K7/06 , A61K38/08
CPC分类号： C07K7/06 , A61K38/00
摘要： The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.7 represent lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl;R.sup.8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; andR.sup.9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower alkoxycarbonyl,and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.
摘要翻译：本发明提供下式的氨基酸衍生物，其中E代表CHO或B（OH）2; R 1表示低级烷基（任选被卤素，氰基，低级烷硫基，芳基 - 低级烷硫基，芳基或杂芳基取代），低级烯基或低级炔基; R 2表示任选被羟基，羧基，芳基，氨基羰基或低级环烷基取代的低级烷基; 并且R 3表示氢或低级烷基; 或R 2和R 3一起表示任选被羟基取代的二 - 或三亚甲基; R4代表低级烷基（任选被羟基，低级环烷基，羧基，芳基，低级烷硫基，氰基 - 低级烷硫基或芳基 - 低级烷硫基取代），低级烯基，芳基或低级环烷基; R5代表低级烷基（任选被羟基，低级烷硫基，芳基，芳基 - 低级烷硫基或氰基 - 低级烷硫基取代）或低级环烷基; R6代表氢或低级烷基; R7代表低级烷基（任选被羟基，羧基，芳基或低级环烷基取代）或低级环烷基; R8代表任选被羟基，羧基或芳基取代的低级烷基; 并且R 9表示低级烷基羰基，羧基 - 低级烷基羰基，芳基羰基，低级烷基磺酰基，芳基磺酰基，低级烷氧基羰基或芳基 - 低级烷氧基羰基，以及式I酸性化合物与碱的碱，其为用作抗病毒剂的病毒蛋白酶抑制剂，治疗或预防丙型肝炎，丙型肝炎和人类GB病毒引起的感染。

2. 发明授权

US06372883B1 Antiviral medicaments 失效
标题翻译：抗病毒药物
公开(公告)号：US06372883B1
公开(公告)日：2002-04-16
申请号：US09265617
申请日：1999-03-10
申请人： Michael Richard Attwood , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
发明人： Michael Richard Attwood , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
IPC分类号： A61K3808
CPC分类号： C07K7/06 , A61K38/00 , Y02P20/55
摘要： The invention is concerned with amino acid derivatives of the formula and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.
摘要翻译：本发明涉及式I的氨基酸衍生物和式I酸性化合物与碱的盐，其为用作抗病毒剂的病毒蛋白酶抑制剂，特别是用于治疗或预防由丙型肝炎，丙型肝炎和人类GB病毒引起的感染。

3. 发明授权

US5866684A Peptidyl inhibitors of viral proteases 失效
标题翻译：肽基蛋白酶抑制剂
公开(公告)号：US5866684A
公开(公告)日：1999-02-02
申请号：US971036
申请日：1997-11-14
申请人： Michael Richard Attwood , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
发明人： Michael Richard Attwood , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
IPC分类号： C12N15/09 , A01N43/34 , A01N43/36 , A61K38/00 , A61P31/12 , A61P31/14 , C07C205/04 , C07C205/45 , C07C271/18 , C07D207/12 , C07D207/20 , C07D211/70 , C07D223/04 , C07D227/04 , C07D405/10 , C07D407/10 , C07D409/10 , C07K7/06 , A61K38/08
CPC分类号： C07K7/06 , A61K38/00
摘要： The invention provides amino acid derivatives of the formula ##STR1## wherein E represents CHO or B(OH).sub.2 ;R.sup.1 represents lower alkyl (optionally substituted by halo, cyano, lower alkylthio, aryl-lower alkylthio, aryl or heteroaryl), lower alkenyl or lower alkynyl;R.sup.2 represents lower alkyl optionally substituted by hydroxy, carboxy, aryl, aminocarbonyl or lower cycloalkyl; andR.sup.3 represents hydrogen or lower alkyl; orR.sup.2 and R.sup.3 together represent di- or trimethylene optionally substituted by hydroxy;R.sup.4 represents lower alkyl (optionally substituted by hydroxy, lower cycloalkyl, carboxy, aryl, lower alkylthio, cyano-lower alkylthio or aryl-lower alkylthio), lower alkenyl, aryl or lower cycloalkyl;R.sup.5 represents lower alkyl (optionally substituted by hydroxy, lower alkylthio, aryl, aryl-lower alkylthio or cyano-lower alkylthio) or lower cycloalkyl;R.sup.6 represents hydrogen or lower alkyl;R.sup.7 represent lower alkyl (optionally substituted by hydroxy, carboxy, aryl or lower cycloalkyl) or lower cycloalkyl;R.sup.8 represents lower alkyl optionally substituted by hydroxy, carboxy or aryl; andR.sup.9 represents lower alkylcarbonyl, carboxy-lower alkylcarbonyl, arylcarbonyl, lower alkylsulphonyl, arylsulphonyl, lower alkoxycarbonyl or aryl-lower al koxycarbonyl,and salts of acidic compounds of formula I with bases, which are viral proteinase inhibitors useful as antiviral agents, especially for the treatment or prophylaxis of infections caused by Hepatitis C, Hepatitis G and human GB viruses.
摘要翻译：本发明提供式（I）的氨基酸衍生物，其中E表示CHO或B（OH）2; R 1表示低级烷基（任选被卤素，氰基，低级烷硫基，芳基 - 低级烷硫基，芳基或杂芳基取代），低级烯基或低级炔基; R 2表示任选被羟基，羧基，芳基，氨基羰基或低级环烷基取代的低级烷基; 并且R 3表示氢或低级烷基; 或R 2和R 3一起表示任选被羟基取代的二 - 或三亚甲基; R4代表低级烷基（任选被羟基，低级环烷基，羧基，芳基，低级烷硫基，氰基 - 低级烷硫基或芳基 - 低级烷硫基取代），低级烯基，芳基或低级环烷基; R5代表低级烷基（任选被羟基，低级烷硫基，芳基，芳基 - 低级烷硫基或氰基 - 低级烷硫基取代）或低级环烷基; R6代表氢或低级烷基; R7代表低级烷基（任选被羟基，羧基，芳基或低级环烷基取代）或低级环烷基; R8代表任选被羟基，羧基或芳基取代的低级烷基; 并且R 9表示低级烷基羰基，羧基 - 低级烷基羰基，芳基羰基，低级烷基磺酰基，芳基磺酰基，低级烷氧基羰基或芳基 - 低级烷氧基羰基，以及式I酸性化合物与碱的碱，其为用作抗病毒剂的病毒蛋白酶抑制剂，治疗或预防丙型肝炎，丙型肝炎和人类GB病毒引起的感染。

4. 发明授权

US06187905B1 Alpha-ketoamide derivatives 失效
标题翻译： α-酮酰胺衍生物
公开(公告)号：US06187905B1
公开(公告)日：2001-02-13
申请号：US09305030
申请日：1999-05-04
申请人： David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
发明人： David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Tony Michael Raynham , Francis Xavier Wilson
IPC分类号： C07K706
CPC分类号： C07K7/06 , A61K38/00 , Y02P20/55
摘要： The invention relates to &agr;-ketoamides of the general formula wherein R1 to R12 have the significances given in the description, and their salts. The &agr;-ketoamide derivatives provided by the present invention inhibit proteinases of viral origin, such as HCV protease, and can be used in the treatment of viral infections, especially viral infections caused by hepatitis C, hepatitis G and human GB viruses.
摘要翻译：本发明涉及R1至R12一般形式的α-酮酰胺具有说明书中给出的意义及其盐。由本发明提供的α-酮酰胺衍生物抑制病毒来源的蛋白酶，如HCV蛋白酶，可用于治疗病毒感染，特别是由丙型肝炎，丙型肝炎和人类GB病毒引起的病毒感染。

5. 发明授权

US06867299B2 Oxamide IMPDH inhibitors 失效
标题翻译： Oxamide IMPDH抑制剂
公开(公告)号：US06867299B2
公开(公告)日：2005-03-15
申请号：US09779116
申请日：2001-02-08
申请人： Michael John Broadhurst , Christopher Huw Hill , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Ian Reginald Kilford , Robert Murray McKinnell
发明人： Michael John Broadhurst , Christopher Huw Hill , David Nigel Hurst , Philip Stephen Jones , Paul Brittain Kay , Ian Reginald Kilford , Robert Murray McKinnell
IPC分类号： C07D263/34 , A61K31/00 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/443 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K38/21 , A61K45/06 , A61P1/18 , A61P11/00 , A61P11/06 , A61P19/02 , A61P29/00 , A61P31/00 , A61P31/04 , A61P31/12 , A61P31/14 , A61P31/16 , A61P31/18 , A61P31/20 , A61P31/22 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/02 , A61P43/00 , C07D249/08 , C07D263/32 , C07D263/48 , C07D413/12 , C07D417/12 , C07D413/14
CPC分类号： C07D413/12 , A61K31/00 , A61K38/21 , A61K45/06 , C07D263/32 , C07D263/48 , C07D417/12 , A61K2300/00
摘要： Disclosed are compounds of the general formula which are oxamide derivatives and inhibitors of the enzyme inosine monophosphate dehydrogenase (IMPDH).
摘要翻译：公开了一般形式的化合物，其是草酰胺衍生物和肌苷单磷酸脱氢酶（IMPDH）的抑制剂。

6. 发明授权

US06703387B2 Inhibitors of HPV E1 helicase enzyme 失效
标题翻译： HPV E1解酶酶抑制剂
公开(公告)号：US06703387B2
公开(公告)日：2004-03-09
申请号：US09892148
申请日：2001-06-26
申请人： David N. Hurst , Philip Stephen Jones , Kevin Edward Burdon Parkes , Martin John Parratt , Francis Xavier Wilson
发明人： David N. Hurst , Philip Stephen Jones , Kevin Edward Burdon Parkes , Martin John Parratt , Francis Xavier Wilson
IPC分类号： A61K315513
CPC分类号： C07D401/06 , C07D243/14 , C07D403/06 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12 , C07D487/04 , C07D491/04
摘要： The invention is concerned with novel benzodiazepine derivatives, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds are inhibitors of the human papillomavirus E1 helicase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HPV mediated diseases.
摘要翻译：本发明涉及新型苯二氮卓衍生物，其制备方法，药物组合物和这些化合物在医药中的用途。特别地，这些化合物是涉及病毒复制的人乳头瘤病毒E1解旋酶的抑制剂。因此，本发明的化合物可有利地用作HPV介导的疾病的治疗剂。

7. 发明授权

US07687515B2 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives 失效
标题翻译： 6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物
公开(公告)号：US07687515B2
公开(公告)日：2010-03-30
申请号：US11653600
申请日：2007-01-16
申请人： Jiaqiang Cai , Zoran Rankovic , Philip Stephen Jones , David Jonathan Bennett , Iain Cumming , Jonathan Gillespie
发明人： Jiaqiang Cai , Zoran Rankovic , Philip Stephen Jones , David Jonathan Bennett , Iain Cumming , Jonathan Gillespie
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/4745 , C07D471/02
CPC分类号： C07D471/04
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I wherein each of the substituents is given the definition as set forth in the specification and claims, pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S and/or cathepsin K related diseases such as osteoporosis, atherosclerosis, inflammation and immune disorders, such as rheumatoid arthritis, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-腈衍生物，其中每个取代基被给出如说明书和权利要求书中所阐述的定义，药物组合物包括这些以及这些衍生物用于制备用于治疗组织蛋白酶S和/或组织蛋白酶K相关疾病如骨质疏松症，动脉粥样硬化，炎症和免疫疾病如类风湿性关节炎和慢性疼痛的药物的用途，如神经性疼痛。

8. 发明授权

US06699887B2 Anti-HIV pyrazole derivatives 失效
标题翻译：抗HIV吡唑衍生物
公开(公告)号：US06699887B2
公开(公告)日：2004-03-02
申请号：US09956656
申请日：2001-09-20
申请人： Brian William Dymock , Philip Stephen Jones , John Herbert Merrett , Martin John Parratt
发明人： Brian William Dymock , Philip Stephen Jones , John Herbert Merrett , Martin John Parratt
IPC分类号： C07D23118
CPC分类号： C07D401/06 , A61K31/415 , A61K31/4439 , A61K31/506 , C07D231/18 , C07D231/20 , C07D231/22 , C07D401/12 , C07D403/06 , C07D403/12 , C07D409/06 , C07D413/06
摘要： The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.
摘要翻译：本发明包括具有抗HIV活性的新颖且已知的吡唑衍生物，其制备方法，药物组合物以及这些化合物在医药中的用途。特别地，式I化合物是参与病毒复制的人免疫缺陷病毒逆转录酶的抑制剂。因此，本发明的化合物可有利地用作HIV感染的治疗剂。

9. 发明申请

US20120283239A1 1H-[1,2,3]TRIAZOLO[4,5-c]PYRIDINE-4-CARBONITRILE DERIVATIVES 有权
标题翻译： 1H- [1,2,3]三唑[4,5-c]吡啶-4-羰基衍生物
公开(公告)号：US20120283239A1
公开(公告)日：2012-11-08
申请号：US13519924
申请日：2011-01-13
申请人： Jiaqiang Cai , David Jonathan Bennett , Philip Stephen Jones
发明人： Jiaqiang Cai , David Jonathan Bennett , Philip Stephen Jones
IPC分类号： C07D471/04 , A61K31/5377 , A61K31/496 , A61K31/54 , A61P25/00 , A61P19/10 , A61P9/10 , A61P29/00 , A61P37/00 , A61P17/06 , A61K31/437 , A61K31/551
CPC分类号： C07D471/04
摘要： The invention relates to 1H-[1,2,3]triazolo[4,5-c]pyridine-4-carbonitrile derived Cathepsin S inhibitors of Formula (I), wherein R1 is H or (C1-3)alkyl; R2 is halogen or (C1-4)alkyl, optionally substituted with one or more halogens; n is 1-3; X is O or CH2; U, V and W are CH; or one of U, V and W is N; Y is a group capable of interacting with the Sn . . . S2 substites of the active site of Cathepsin S; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及式（I）的1H- [1,2,3]三唑并[4,5-c]吡啶-4-腈衍生的组织蛋白酶S抑制剂，其中R 1是H或（C 1-3）烷基; R 2是卤素或任选被一个或多个卤素取代的（C 1-4）烷基; n为1-3; X是O或CH2; U，V和W是CH; 或U，V和W之一为N; Y是能够与Sn相互作用的组。。。组织蛋白酶S活性位点的S2位点; 或其药学上可接受的盐用于包含其的药物组合物以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿病的药物中的用途关节炎，牛皮癣，癌症和慢性疼痛，如神经性疼痛。

10. 发明授权

US07932251B2 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives 失效
标题翻译： 6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物
公开(公告)号：US07932251B2
公开(公告)日：2011-04-26
申请号：US12173623
申请日：2008-07-15
申请人： Jiaqiang Cai , Zoran Rankovic , Philip Stephen Jones , David Jonathan Bennett , Xavier Fradera
发明人： Jiaqiang Cai , Zoran Rankovic , Philip Stephen Jones , David Jonathan Bennett , Xavier Fradera
IPC分类号： A61K31/437 , A61K31/438 , A61K31/5377 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04 , C07D519/00
摘要： The present invention relates to 6-phenyl-1H-imidazo[4,5-c]pyridine-4-carbonitrile derivatives having the general Formula I to pharmaceutical compositions comprising the same as well as to the use of these derivatives for the preparation of a medicament for the treatment of cathepsin S related diseases such as atherosclerosis, obesity, inflammation and immune disorders, such as rheumatoid arthritis, psoriasis, cancer, and chronic pain, such as neuropathic pain.
摘要翻译：本发明涉及具有通式I的6-苯基-1H-咪唑并[4,5-c]吡啶-4-甲腈衍生物，其药物组合物包含它们，以及这些衍生物用于制备用于治疗组织蛋白酶S相关疾病如动脉粥样硬化，肥胖症，炎症和免疫疾病如类风湿性关节炎，牛皮癣，癌症和慢性疼痛如神经性疼痛的药物。

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