公开(公告)号：US20040266844A1

公开(公告)日：2004-12-30

申请号：US10481667

申请日：2004-08-26

发明人： Peter Prokofievich Denisenko ,  Nikolay Sergeevich Sapronov ,  Alexander Alexandrovich Tarasenko

IPC分类号： A61K031/428 ,  A61K031/423 ,  A61K031/4184

CPC分类号： A61K31/357 ,  A61K31/36 ,  A61K31/4184 ,  C07D235/06 ,  C07D235/08 ,  C07D263/56 ,  C07D317/46 ,  C07D317/52 ,  Y02A50/401 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/47 ,  Y02A50/471 ,  Y02A50/473 ,  Y02A50/475 ,  Y02A50/479 ,  Y02A50/481

摘要： The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising administering an effective amount of a compound of formula I as defined herein, or pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula I. Some of the compounds of formula I are novel and are also described in the present invention, together with pharmaceutical or veterinary compositions containing them.

摘要翻译： 本发明涉及治疗和/或预防微生物感染的方法，包括施用有效量的本文定义的式I化合物或其药学上可接受的盐或衍生物，前药，互变异构体和/或异构体 。 本发明还涉及一种用于保护受试者免受辐射损伤的方法，癌症放射治疗的方法和用作式I化合物的抗微生物剂或放射防护剂。一些式I化合物是新颖的，也描述于 本发明以及含有它们的药物或兽用组合物。

公开(公告)号：US20040224955A1

公开(公告)日：2004-11-11

申请号：US10851710

申请日：2004-05-21

申请人： Boehringer Ingelheim (Canada) Ltd.

发明人： Pierre Louis Beaulieu ,  Gulrez Fazal ,  James Gillard ,  George Kukolj ,  Volkhard Austel

IPC分类号： C07D471/02 ,  A61K031/498 ,  A61K031/4745 ,  A61K031/4184

CPC分类号： C07D401/04 ,  C07D235/18 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D417/14 ,  C07D471/04 ,  Y10S514/894

摘要： A compound of the formula I: 1 wherein: X is CH or N; Y is O or S; Z is OH, NH2, NMeR3, NHR3; OR3 or 5- or 6-membered heterocycle, having 1 to 4 heteroatoms selected from O, N and S, said heterocycle being optionally substituted with from 1 to 4 substituents; A is N, COR7 or CR5, wherein R5 is H, halogen, or (C1-6) alkyl and R7 is H or (C1-6 alkyl), with the proviso that X and A are not both N; R6 is H, halogen, (C1-6 alkyl) or OR7, wherein R7 is H or (C1-6 alkyl); R1 is selected from the group consisting of 5- or 6-membered heterocycle having 1 to 4 heteroatoms selected from O, N, and S, phenyl, phenyl(C1-3)alkyl, (C2-6)alkenyl, phenyl(C2-6)alkenyl, (C3-6)cycloalkyl, (C1-6)alkyl, CF3, 9- or 10-membered heterobicycle having 1 to 4 heteroatoms selected from O, N and S, wherein said heterocycle, phenyl, phenyl(C2-6)alkenyl and phenyl(C1-3)alkyl), alkenyl, cycloalkyl, (C1-6)alkyl, and heterobicycle are all optionally substituted with from 1 to 4 substituents; R2 is selected from (C1-6)alkyl, (C3-7)cycloalkyl, (C3-7)cycloalkyl(C1-3)alkyl, (C6-10)bicycloalkyl, adamantyl, phenyl, and pyridyl, all of which is optionally substituted with from 1 to 4 substituents; R3 is selected from H, (C1-6)alkyl, (C3-6)cycloalkyl, (C3-6)cycloalkyl(C1-6)alkyl, (C6-10)aryl, (C6-10)aryl(C1-6)alkyl, (C2-6)alkenyl, (C3-6)cycloalkyl(C2-6)alkenyl, (C6-10)aryl(C2-6)alkenyl, Nnull(C1-6) alkylnull2, NHCOO(C1-6)alkyl(C6-10)aryl, NHCO(C6-10)aryl, (C1-6)alkyl-5- or 10-atom heterocycle, having 1 to 4 heteroatoms selected from O, N and S, and 5- or 10-atom heterocycle having 1 to 4 heteroatoms selected from O, N and S; wherein said alkyl, cycloalkyl, aryl, alkenyl and heterocycle are all optionally substituted with from 1 to 4 substituents; n is zero or 1; or a detectable derivative or salt thereof. The compounds of the invention may be used as inhibitors of hepatitis C virus replication. The invention further provides a method for treating or preventing hepatitis C virus infection.

公开(公告)号：US20040192748A1

公开(公告)日：2004-09-30

申请号：US10654452

申请日：2003-09-03

申请人： Boehringer Ingelheim Parmaceuticals, Inc.

发明人： Antonio Jose del Moral Barbosa JR. ,  Daniel R. Goldberg ,  Abdelhakim Hammach ,  Pingrong Liu ,  Neil Moss ,  Mark Stephen Ralph ,  Gregory Paul Roth ,  Christoper Ronald Sarko ,  Fariba Soleymanzadeh ,  Andre White

IPC分类号： A61K031/4184 ,  C07D43/02 ,  C07D235/24

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D235/26 ,  C07D249/08 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/06 ,  C07D417/04 ,  C07D471/10 ,  C07D491/10

摘要： Disclosed are benzimidazolone compounds of formulas (I) & (II): 1 wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.

摘要翻译： 公开了式（I）和（II）的苯并咪唑酮化合物：其中R1，R2，R3，R4，R5，X，L，m，n和t如本文所定义。 该化合物抑制涉及炎症过程的细胞因子的产生，因此可用于治疗涉及诸如慢性炎性疾病的炎症的疾病和病理状况。 还公开了制备这些化合物的方法和包含这些化合物的药物组合物。

公开(公告)号：US20040162327A1

公开(公告)日：2004-08-19

申请号：US10777304

申请日：2004-02-12

申请人： Boehringer Ingelheim Pharma KG

发明人： Kai Donsbach ,  Irmgard Hof

IPC分类号： A61K031/4184 ,  C07D43/02

CPC分类号： C07D235/20

摘要： The invention relates to a crystalline sodium salt of 4null-null2-n-propyl-4-methyl-6-(1-methyl-benzimidazol-2-yl)benzimidazol-1-ylmethylnullbiphenyl-2-carboxylic acid (INN: telmisartan), processes for preparing it and the use thereof for preparing a pharmaceutical composition.

摘要翻译： 本发明涉及4' - [2-正丙基-4-甲基-6-（1-甲基 - 苯并咪唑-2-基）苯并咪唑-1-基甲基]联苯-2-羧酸（INN）的结晶钠盐 ：替米沙坦），其制备方法及其用于制备药物组合物的用途。

公开(公告)号：US20040122002A1

公开(公告)日：2004-06-24

申请号：US10169988

申请日：2002-09-27

发明人： Hans Guenter Striegel ,  Stefan Laufer ,  Karola Tollmann ,  Susanne Tries

IPC分类号： A61K031/542 ,  A61K031/5383 ,  A61K031/519 ,  A61K031/4745 ,  A61K031/428 ,  A61K031/423 ,  A61K031/4184 ,  A61K031/407

CPC分类号： C07D487/04

摘要： The present invention relates to fused pyrrole compounds of the formula 1. 1 in which at least one of the radicals R1, R2, R3 is 4-sulphur-substituted phenyl. These compounds are in particular pyrrolizines, indolizines and heteroanalogues having selective inhibitory action on isoenzyme-2 of prostaglandin H synthase (COX-2). The invention also relates to pharmaceutical compositions which contain these compounds; and the use of these compounds for the treatment of disorders of the rheumatic type.

摘要翻译： 本发明涉及式1的稠合吡咯化合物，其中基团R 1，R 2，R 3中的至少一个是4-硫取代的苯基。 这些化合物特别是对前列腺素H合成酶（COX-2）的同工酶-2具有选择性抑制作用的吡咯烷，中氮茚和杂芳族化合物。 本发明还涉及含有这些化合物的药物组合物; 以及这些化合物用于治疗风湿性疾病的用途。

公开(公告)号：US20040110757A1

公开(公告)日：2004-06-10

申请号：US10472631

申请日：2003-09-22

发明人： Thomas Arrhenius ,  Yujin Huang ,  Lin Zhang ,  Rossy Serafimov ,  Alex Nadzan ,  Dominic G Spinella

IPC分类号： A61K031/53 ,  A61K031/506 ,  A61K031/4439 ,  A61K031/4245 ,  A61K031/4184

CPC分类号： C07D239/26 ,  A61K31/4184 ,  A61K31/4245 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/53 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

摘要： This invention is a method of treatment and prophylaxis of diseases regulatable by angiogenesis, including novel FLT-1 ligands and pharmaceutical compositions containing them, useful in the methods for the treatment and prophylaxis of these diseases, as well as intermediates and processes useful for the preparation of the compounds of the invention as claimed.

摘要翻译： 本发明是一种治疗和预防血管生成可调节疾病的方法，包括新型FLT-1配体和含有它们的药物组合物，可用于治疗和预防这些疾病的方法，以及可用于制备的中间体和方法 的本发明化合物。

公开(公告)号：US20040087637A1

公开(公告)日：2004-05-06

申请号：US10696433

申请日：2003-10-29

申请人： Wyeth

发明人： Ping Zhou ,  Michael Gerard Kelly

IPC分类号： A61K031/4184 ,  A61K031/416

CPC分类号： C07D405/12 ,  C07D209/08 ,  C07D231/56 ,  C07D409/12

摘要： The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor. 1

公开(公告)号：US20040072862A1

公开(公告)日：2004-04-15

申请号：US10354793

申请日：2003-01-29

发明人： Catherine M. Bitler ,  Paul Wood ,  D. Timothy Anstine ,  Anke Meyer-Franke ,  Qi Zhao ,  Mohamed A. Khan

IPC分类号： A61K031/4745 ,  A61K031/4184

CPC分类号： C07D233/64 ,  A61K31/4184 ,  A61K31/437 ,  C07D235/08 ,  C07D235/10 ,  C07D235/16 ,  C07D235/20 ,  C07D401/06 ,  C07D403/06 ,  G01N2510/00

摘要： Compounds, pharmaceutical compositions, and methods of use are described which are effective in inhibiting cell death, particularly apoptotic cell death. The compositions may be used for prevention and treatment of injuries associated with cell death, including ischemia, such as results from stroke or myocardial infarction, trauma, neurodegeneration, and inflammation.

摘要翻译： 描述了有效抑制细胞死亡，特别是凋亡性细胞死亡的化合物，药物组合物和使用方法。 组合物可用于预防和治疗与细胞死亡相关的损伤，包括缺血，例如中风或心肌梗死，创伤，神经变性和炎症的结果。

公开(公告)号：US20040063768A1

公开(公告)日：2004-04-01

申请号：US10662493

申请日：2003-09-15

发明人： Derek John Denhart ,  Jonathan L. Ditta ,  Dalton King ,  John E. Macor ,  Lawrence R. Marcin ,  Ronald J. Mattson ,  Zhaoxing Meng

IPC分类号： A61K031/4184 ,  C07D403/02 ,  A61K031/416

CPC分类号： C07D209/14

摘要： The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds 1 useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.

摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐或溶剂合物和药学上可接受的制剂，其包含用于治疗早泄，抑郁，注意力缺陷多动障碍，强迫症，创伤后应激障碍 和物质滥用障碍。

公开(公告)号：US20040058972A1

公开(公告)日：2004-03-25

申请号：US10612163

申请日：2003-07-03

发明人： Peter David Davis

IPC分类号： A61K031/675 ,  A61K031/4184

CPC分类号： C07F9/65068 ,  A61K31/4184 ,  A61K31/675 ,  C07D235/32

摘要： Vascular damaging agents composed of substituted 5(6)-substituted benzimidazole-2-carbamates are provided. These agents are useful in the preparation of medicaments for the treatment of diseases involving neovascularisation, particularly for the treatment of solid tumors, macular degeneration, diabetic retinopathy, rheumatoid arthritis, psoriasis, and atherosclerosis. Embodiments include a 5(6)-substituted benzimidazole-2-carbamate of formula I 1 wherein A represents a multi-substituted alkyl group or aromatic ring.

摘要翻译： 提供由取代的5（6） - 取代的苯并咪唑-2-氨基甲酸酯组成的血管损伤剂。 这些试剂可用于制备用于治疗涉及新血管形成的疾病的药物，特别是用于治疗实体瘤，黄斑变性，糖尿病性视网膜病，类风湿性关节炎，牛皮癣和动脉粥样硬化。 实施方案包括式I的5（6） - 取代的苯并咪唑-2-氨基甲酸酯，其中A表示多取代的烷基或芳环。