公开(公告)号：US20070021330A1

公开(公告)日：2007-01-25

申请号：US10561718

申请日：2004-05-19

Applicant: Frank Wu ,  Suanne Nakajima ,  Yat Or ,  Zhi-Hui Lu ,  Ying Sun ,  Zhenwei Miao ,  Zhe Wang

Inventor： Frank Wu ,  Suanne Nakajima ,  Yat Or ,  Zhi-Hui Lu ,  Ying Sun ,  Zhenwei Miao ,  Zhe Wang

IPC: A61K38/12 ,  C07K5/12 ,  A61K31/4709

CPC classification number: C07K5/06139 ,  A61K38/00 ,  C07K5/06165

Abstract: The present invention relates to compounds of Formula (I), or a pharmaceutically acceptable salt, ester, or prodrug, thereof, which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.

Abstract translation: 本发明涉及抑制丝氨酸蛋白酶活性，特别是丙型肝炎病毒（HCV）NS3-NS4A蛋白酶活性的式（I）化合物或其药学上可接受的盐，酯或前药。 因此，本发明的化合物干扰丙型肝炎病毒的生命周期，也可用作抗病毒剂。 本发明还涉及药物组合物，其包含用于给患有HCV感染的受试者施用的上述化合物。 本发明还涉及通过施用包含本发明化合物的药物组合物来治疗受试者的HCV感染的方法。

公开(公告)号：US20050222119A1

公开(公告)日：2005-10-06

申请号：US11128732

申请日：2005-05-13

Applicant: Eugene Thorsett ,  Christopher Semko ,  Dimitrios Sarantakis ,  Michael Pleiss ,  Anthony Kreft ,  Andrei Konradi ,  Francine Grant ,  Darren Dressen ,  Susan Ashwell ,  Reinhardt Baudy ,  Louis Lombardo

Inventor： Eugene Thorsett ,  Christopher Semko ,  Dimitrios Sarantakis ,  Michael Pleiss ,  Anthony Kreft ,  Andrei Konradi ,  Francine Grant ,  Darren Dressen ,  Susan Ashwell ,  Reinhardt Baudy ,  Louis Lombardo

IPC: A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/02 ,  C07K5/06 ,  C07K5/078

CPC classification number: A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/0215 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

公开(公告)号：US20050143391A1

公开(公告)日：2005-06-30

申请号：US10510626

申请日：2003-04-08

Applicant: Elena Carceller Gonzalez ,  Jorge Salas Solana ,  Cristina Alvarez Farrerons ,  Juan Andreu Azanza

Inventor： Elena Carceller Gonzalez ,  Jorge Salas Solana ,  Cristina Alvarez Farrerons ,  Juan Andreu Azanza

IPC: A61K38/00 ,  A61P25/28 ,  A61P29/00 ,  A61P35/04 ,  C07K5/078 ,  A61K31/496 ,  A61K31/454 ,  A61K31/506 ,  C07D413/04 ,  C07D43/02

CPC classification number: C07K5/06165 ,  A61K38/00

Abstract: The present invention relates to new compounds of Formula (I) and the salts, solvates and prodrugs thereof, wherein the meanings for the various substituents are as disclosed in the description. These compounds are useful as integrin α4 antagonists.

Abstract translation: 本发明涉及式（I）的新化合物及其盐，溶剂合物和前药，其中各种取代基的含义如说明书中所公开的。 这些化合物可用作整联蛋白α4拮抗剂。

公开(公告)号：US06806279B2

公开(公告)日：2004-10-19

申请号：US10024665

申请日：2001-12-17

Applicant: Michelle R. Arkin ,  Robert S. McDowell ,  Johan D. Oslob ,  Brian C. Raimundo ,  Nathan D. Waal ,  Chul Hyun Yu

Inventor： Michelle R. Arkin ,  Robert S. McDowell ,  Johan D. Oslob ,  Brian C. Raimundo ,  Nathan D. Waal ,  Chul Hyun Yu

IPC: C07D40104

CPC classification number: C07K5/06026 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06165

Abstract: Compounds of formulae I and I′, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.

Abstract translation: 式I和I'的化合物，其制备方法，含有它们的药物组合物及其使用方法。 该化合物是IL-2 / IL-2R结合的拮抗剂; 并且可用于治疗白细胞介素-2介导的疾病，例如自身免疫性疾病（例如类风湿性关节炎，多发性硬化，葡萄膜炎和银屑病），同种异体移植排斥和移植物抗宿主病。

公开(公告)号：US20040198989A1

公开(公告)日：2004-10-07

申请号：US10715852

申请日：2003-11-19

Applicant: G.D. Searle & Co.

Inventor： Daniel P. Getman ,  Gary A. DeCrescenzo ,  John N. Freskos ,  Michael L. Vazquez ,  James A. Sikorski ,  Balekudru Devadas ,  Srinivasan Nagarajan ,  David L. Brown ,  Joseph J. McDonald

IPC: C07D211/32

CPC classification number: C07K5/021 ,  A61K38/00 ,  C07K5/06139 ,  C07K5/06165

Abstract: Selected heterocyclecarbonyl amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease. The present invention relates to such retroviral protease inhibitors and, more particularly, relates to selected novel compounds, composition and method for inhibiting retroviral proteases, such as human immunodeficiency virus (HIV) protease, prophylactically preventing retroviral infection or the spread of a retrovirus, and treatment of a retroviral infection.

Abstract translation: 选择的杂环羰基氨基酸羟乙基氨基磺酰胺化合物作为逆转录病毒蛋白酶抑制剂是有效的，特别是作为HIV蛋白酶的抑制剂。 本发明涉及这种逆转录病毒蛋白酶抑制剂，更具体地涉及所选择的新化合物，用于抑制逆转录病毒蛋白酶如人类免疫缺陷病毒（HIV）蛋白酶的组合物和方法，预防性地预防逆转录病毒感染或逆转录病毒的扩散，以及 治疗逆转录病毒感染。

公开(公告)号：US20030149049A1

公开(公告)日：2003-08-07

申请号：US10024665

申请日：2001-12-17

Inventor： Michelle R. Arkin ,  Robert S. McDowell ,  Johan D. Oslob ,  Brian C. Raimundo ,  Nathan D. Waal ,  Chul Hyun Yu

IPC: A61K031/506 ,  A61K031/496 ,  A61K031/454 ,  A61K031/4439 ,  A61K031/427 ,  A61K031/422 ,  A61K031/4178 ,  A61K031/4184 ,  C07D43/02 ,  C07D43/14

CPC classification number: C07K5/06026 ,  A61K38/00 ,  C07K5/06034 ,  C07K5/06043 ,  C07K5/0606 ,  C07K5/06078 ,  C07K5/06165

Abstract: Compounds of formulae I and Inull, methods of making them, pharmaceutical compositions containing them, and methods for their use. The compounds are antagonists of IL-2/IL-2R binding; and are useful for the treatment of interleukin-2 mediated diseases, such as autoimmune diseases (such as rheumatoid arthritis, multiple sclerosis, uveitis, and psoriasis), allograft rejection, and graft-versus-host disease.

Abstract translation: 式I和I'的化合物，其制备方法，含有它们的药物组合物及其使用方法。 该化合物是IL-2 / IL-2R结合的拮抗剂; 并且可用于治疗白细胞介素-2介导的疾病，例如自身免疫性疾病（例如类风湿性关节炎，多发性硬化，葡萄膜炎和银屑病），同种异体移植排斥和移植物抗宿主病。

公开(公告)号：US20030104571A1

公开(公告)日：2003-06-05

申请号：US10309756

申请日：2002-12-04

Inventor： Mark L. Smith ,  Kenneth E. Palmer ,  Gregory P. Pogue ,  John A. Lindbo ,  Kathleen M. Hanley ,  David P. Mannion ,  Gershon M. Wolfe

IPC: C12P021/06 ,  C07K014/00

CPC classification number: C07K5/06165 ,  A61K38/00 ,  B01D15/1885 ,  B01D15/3804 ,  C07K5/06139

Abstract: A plurality of proteins of interest, or peptides of interest, or other genetically expressed materials, are screened and subsequently produced using any of a variety of expression systems. The plurality of proteins are extracted from a plurality of separate, processed green juices, each green juice containing one of the proteins of interest. A multi-channel apparatus processes the various green juices, one green juice per channel. The apparatus is computer controlled such that the various valves in each channel and pump are controlled in an automated manner to extract each protein of interest and deliver each protein of interest into its own storage vessel.

Abstract translation: 筛选多种感兴趣的蛋白质或感兴趣的肽，或其它遗传表达的材料，随后使用多种表达系统中的任何一种产生。 从多个单独的加工的绿汁中提取多种蛋白质，每种绿汁含有感兴趣的蛋白质之一。 多通道设备处理各种绿汁，每个通道一个绿汁。 该装置是计算机控制的，使得每个通道和泵中的各种阀以自动方式进行控制，以提取每个目的蛋白质并将感兴趣的每种蛋白质输送到其自己的储存容器中。

公开(公告)号：US06489300B1

公开(公告)日：2002-12-03

申请号：US09126958

申请日：1998-07-31

Applicant: Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Susan Ashwell ,  Reinhardt Bernhard Baudy ,  Louis John Lombardo

Inventor： Eugene D. Thorsett ,  Christopher M. Semko ,  Dimitrios Sarantakis ,  Michael A. Pleiss ,  Anthony Kreft ,  Andrei W. Konradi ,  Francine S. Grant ,  Darren B. Dressen ,  Susan Ashwell ,  Reinhardt Bernhard Baudy ,  Louis John Lombardo

IPC: C07K5078

CPC classification number: A61K31/397 ,  A61K31/4015 ,  A61K31/404 ,  A61K31/495 ,  A61K31/54 ,  A61K38/00 ,  C07K5/0215 ,  C07K5/06026 ,  C07K5/06139 ,  C07K5/06165 ,  C07K5/06191

Abstract: Disclosed are compounds which bind VLA-4. Certain of these compounds also inhibit leukocyte adhesion and, in particular, leukocyte adhesion mediated by VLA-4. Such compounds are useful in the treatment of inflammatory diseases in a mammalian patient, e.g., human, such as asthma, Alzheimer's disease, atherosclerosis, AIDS dementia, diabetes, inflammatory bowel disease, rheumatoid arthritis, tissue transplantation, tumor metastasis and myocardial ischemia. The compounds can also be administered for the treatment of inflammatory brain diseases such as multiple sclerosis.

Abstract translation: 公开了结合VLA-4的化合物。 这些化合物中的某些也抑制白细胞粘附，特别是由VLA-4介导的白细胞粘附。 这样的化合物可用于治疗哺乳动物患者，例如人类例如哮喘，阿尔茨海默氏病，动脉粥样硬化，艾滋病痴呆，糖尿病，炎性肠病，类风湿性关节炎，组织移植，肿瘤转移和心肌缺血等炎性疾病。 化合物也可以用于治疗炎性脑疾病如多发性硬化症。

公开(公告)号：US20020169133A1

公开(公告)日：2002-11-14

申请号：US10072730

申请日：2002-02-07

Inventor： Sharon Marie Dankwardt ,  Harold Edgar Van Wart ,  Keith Adrian Murray Walker

IPC: A61K038/06 ,  C07K005/08

CPC classification number: C07K14/78 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06078 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06147 ,  C07K5/06156 ,  C07K5/06165 ,  C07K5/0808

Abstract: This invention relates to compounds of Formula (I) 1 wherein R1-R7, A, Z and n are as described in the Summary of the Invention that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for their preparation.

Abstract translation: 本发明涉及式（I）化合物，其中R 1 -R 7，A，Z和n如发明概述中所述，其为前胶原C-蛋白酶的抑制剂，含有它们的药物组合物，其用途及其用途 他们的准备。

公开(公告)号：US06426402B1

公开(公告)日：2002-07-30

申请号：US09459201

申请日：1999-12-10

Applicant: Sharon Marie Dankwardt ,  Harold Edgar Van Wart ,  Keith Adrian Murray Walker

Inventor： Sharon Marie Dankwardt ,  Harold Edgar Van Wart ,  Keith Adrian Murray Walker

IPC: C07K508

CPC classification number: C07K14/78 ,  A61K38/00 ,  C07K5/06026 ,  C07K5/06034 ,  C07K5/06078 ,  C07K5/06104 ,  C07K5/06139 ,  C07K5/06147 ,  C07K5/06156 ,  C07K5/06165 ,  C07K5/0808

Abstract: This invention relates to compounds of Formula (I) wherein R1-R7, A, Z and n are as described in the Summary of the Invention that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for their preparation.

Abstract translation: 本发明涉及式（I）化合物，其中R 1 -R 7，A，Z和n如发明概述中所述，其为前胶原C-蛋白酶的抑制剂，含有它们的药物组合物，其用途及其用途 他们的准备。