公开(公告)号：US06680319B2

公开(公告)日：2004-01-20

申请号：US10052325

申请日：2002-01-17

申请人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Elena Poggesi

发明人： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Elena Poggesi

IPC分类号： A61K31422

CPC分类号： C07D261/18

摘要： The invention relates to novel N-(substituted phenyl)-N′-[&ohgr;-(3-substituted phenyl-4-isoxazolecarbonylamino)alkyl]piperazines, their N-oxides, and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD), and other conditions. The compounds may be administered alone or in combination with an anticholinergic compound.

摘要翻译： 本发明涉及新的N-（取代的苯基）-N' - （ - （ω-（3-取代的苯基-4-异恶唑氨基）烷基]哌嗪，它们的N-氧化物及其药学上可接受的盐。 该化合物具有增强的α1-肾上腺素能受体的选择性和降低血压的低活性。 该化合物可用于治疗下尿路阻塞性综合征，包括良性前列腺增生（BPH），以及治疗下尿路症状（LUTS）和神经源性下尿路功能障碍（NLUTD）等情况。 化合物可以单独施用或与抗胆碱能化合物组合施用。

公开(公告)号：US06369089B1

公开(公告)日：2002-04-09

申请号：US09840675

申请日：2001-04-23

申请人： Robert M. Burk ,  Yariv Donde

发明人： Robert M. Burk ,  Yariv Donde

IPC分类号： A61K31422

CPC分类号： C07D493/08

摘要： The present invention provides novel compounds represented by the general formula I. wherein m is an integer of from 1 to 3; n is 0 or an integer of from 1 to 4; R is selected from the group consisting of CO2H, CO2 R6, CH2OH, CH2O R6 P(O)(OH)2,  and CONR3R4; R1 and R2 are independently selected from the group consisting of H, R6, C1-C6 alkenyl, C1-C6 alkynyl, C3-C7 cycloalkyl, C4-C12 alkylcycloalkyl, C6-C10 aryl, C7-C12 alkyl aryl radicals and heteroatom-substituted derivatives thereof, wherein one or more of the hydrogen or carbon atoms in said radicals is replaced with a halogen, nitrogen or sulfur-containing radical; R3 and R4 are selected from the group consisting of H and R6; and X is selected from the group consisting of H, R6, hydroxy, N(R6)2, CON(R6)2, SR6, sulfoxy, sulfone, halogen, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl; Y is O or S; Z is N or CH and pharmaceutically acceptable salts thereof. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.

摘要翻译： 本发明提供由通式Ⅰ表示的新型化合物，其中m为1〜3的整数，n为0或1〜4的整数，R选自CO 2 H，CO 2 R 6，CH 2 OH， CH 2 O 6 P（O）（OH）2和CONR 3 R 4; R 1和R 2独立地选自H，R 6，C 1 -C 6烯基，C 1 -C 6炔基，C 3 -C 7环烷基，C 4 -C 12烷基环烷基，C 6 -C 10芳基，C 7 -C 12烷基芳基和其杂原子取代的衍生物，其中所述基团中的一个或多个氢或碳原子被卤素，氮或含硫基团取代; R 3和R 4选自 由H和R6组成的组; 和X选自H，R6，羟基，N（R6）2，CON（R6）2，SR6，磺氧基，砜，卤素，COOR6，NO2，CN和OR6，其中R6是C1-C6烷基; Y为O或S; Z是N或CH及其药学上可接受的盐。 新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病 ，血小板聚集和血栓形成。

公开(公告)号：US06831088B2

公开(公告)日：2004-12-14

申请号：US10643476

申请日：2003-08-19

申请人： Paul Vincent Fish ,  Jackie Diane Kendall ,  Gavin Alistair Whitlock

发明人： Paul Vincent Fish ,  Jackie Diane Kendall ,  Gavin Alistair Whitlock

IPC分类号： A61K31422

CPC分类号： C07D263/34 ,  C07D271/06 ,  C07D271/07 ,  C07D413/12

摘要： Compounds of formula (1): and their salts, solvates, prodrugs, etc., wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

摘要翻译： 式（1）的化合物及其盐，溶剂化物，前药等，其中取代基具有本文提及的值，为前胶原C-蛋白酶（PCP）抑制剂，并且可用于由PCP介导的病症。

公开(公告)号：US06441005B1

公开(公告)日：2002-08-27

申请号：US09625756

申请日：2000-07-26

申请人： Mikhail F. Gordeev ,  Gary W. Luehr ,  Dinesh V. Patel ,  Robert C. Gadwood

发明人： Mikhail F. Gordeev ,  Gary W. Luehr ,  Dinesh V. Patel ,  Robert C. Gadwood

IPC分类号： A61K31422

CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.

摘要翻译： 提供了恶唑烷酮及其合成方法。 还提供制备生物活性恶唑烷酮的方法以及包含恶唑烷酮的药学上可接受的组合物。 本文公开的恶唑烷酮可以容易地合成并用于各种应用中，包括用作抗微生物剂。 在一个实施方案中，提供了各种硫代酰胺甲基恶唑烷酮及其合成和使用的方法。

公开(公告)号：US06414003B1

公开(公告)日：2002-07-02

申请号：US09708542

申请日：2000-11-09

申请人： Tsuneo Kanamaru ,  Masafumi Nakao ,  Hiroyuki Tawada ,  Keiji Kamiyama

发明人： Tsuneo Kanamaru ,  Masafumi Nakao ,  Hiroyuki Tawada ,  Keiji Kamiyama

IPC分类号： A61K31422

CPC分类号： C07D413/06 ,  C07D263/48 ,  C07D413/14 ,  C07D471/04 ,  C12P17/16

摘要： An anti-Helicobacter pylori agent comprising a compound represented by the formula: wherein A represents an aromatic ring group which may be substituted; R1 and R2, whether identical or not, each represent a hydrogen atom or a hydrocarbon group which may be substituted; R3 and R4, whether identical or not, each represent a hydrogen atom, a hydrocarbon group which may be substituted, an acyl group, a carbamoyl group which may be substituted, or a carboxyl group which may be esterified; or a salt thereof.

摘要翻译： 一种抗幽门螺杆菌药物，其包含由下式表示的化合物：其中A表示可被取代的芳族环基团; R1和R2各自表示氢原子或可被取代的烃基; R 3和R 4各自表示氢原子，可被取代的烃基，酰基，可被取代的氨基甲酰基或可被酯化的羧基; 或其盐。

公开(公告)号：US06743811B2

公开(公告)日：2004-06-01

申请号：US10183198

申请日：2002-06-27

申请人： Mikhail F. Gordeev ,  Gary W. Luehr ,  Dinesh V. Patel ,  Robert C. Gadwood

发明人： Mikhail F. Gordeev ,  Gary W. Luehr ,  Dinesh V. Patel ,  Robert C. Gadwood

IPC分类号： A61K31422

CPC分类号： C07D263/20 ,  C07D413/10 ,  C07D413/12 ,  C07D417/10 ,  C07D417/12

摘要： Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.

摘要翻译： 提供了恶唑烷酮及其合成方法。 还提供制备生物活性恶唑烷酮的方法以及包含恶唑烷酮的药学上可接受的组合物。 本文公开的恶唑烷酮可以容易地合成并用于各种应用中，包括用作抗微生物剂。 在一个实施方案中，提供了各种硫代酰胺甲基恶唑烷酮及其合成和使用的方法。

公开(公告)号：US06649640B2

公开(公告)日：2003-11-18

申请号：US10272622

申请日：2002-10-15

申请人： Michael Hale ,  James Janetka ,  Francois Maltais ,  Jingrong Cao

发明人： Michael Hale ,  James Janetka ,  Francois Maltais ,  Jingrong Cao

IPC分类号： A61K31422

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/14

摘要： Described herein are compounds that are useful as protein kinase inhibitors, especially inhibitors of ERK, having the formula: where A, B, R1, R2, T and Ht are described in the specification. The compounds are useful for treating diseases in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.

摘要翻译： 本文描述了可用作蛋白激酶抑制剂，特别是ERK抑制剂的化合物，其具有下式：其中A，B，R 1，R 2，T和Ht在说明书中描述。 该化合物可用于治疗由蛋白激酶抑制剂缓解的哺乳动物疾病，特别是疾病如癌症，炎症性疾病，再狭窄和心血管疾病。

公开(公告)号：US06645993B2

公开(公告)日：2003-11-11

申请号：US10109756

申请日：2002-03-29

申请人： Paul Vincent Fish ,  Jackie Diane Kendall ,  Gavin Alistair Whitlock

发明人： Paul Vincent Fish ,  Jackie Diane Kendall ,  Gavin Alistair Whitlock

IPC分类号： A61K31422

CPC分类号： C07D263/34 ,  C07D271/06 ,  C07D271/07 ,  C07D413/12

摘要： Compounds of formula (I) and their salts, solvates and prodrugs, wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

摘要翻译： 式（I）化合物及其盐，溶剂合物和前体药物，其中取代基具有本文提及的值，是前胶原蛋白C-蛋白酶（PCP）抑制剂，并且可用于由PCP介导的病症。

公开(公告)号：US06511999B2

公开(公告)日：2003-01-28

申请号：US10071449

申请日：2002-02-08

申请人： Robert M. Burk ,  Yariv Donde

发明人： Robert M. Burk ,  Yariv Donde

IPC分类号： A61K31422

CPC分类号： C07D493/08

摘要： The present invention provides novel compounds represented by the general formula I. wherein m, n, X, Y, Z, R, R1 and R2 are as defined in the specification or a pharmaceutically acceptable salt thereof. The novel compounds are PGF2&agr; antagonists, useful in pharmaceutical compositions for treating PGF2&agr;-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.

摘要翻译： 本发明提供由通式I表示的新化合物，其中m，n，X，Y，Z，R，R 1和R 2如说明书中所定义或其药学上可接受的盐。 新型化合物是PGF2α拮抗剂，可用于治疗PGF2α介导的疾病反应的药物组合物，例如与类风湿性关节炎和牛皮癣相关的炎性反应，生殖障碍，支气管收缩性疾病（哮喘），过度骨分解（骨质疏松症），消化性溃疡，心脏病 ，血小板聚集和血栓形成。

公开(公告)号：US06486187B1

公开(公告)日：2002-11-26

申请号：US09624966

申请日：2000-07-25

申请人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

发明人： Marc Gaston Venet ,  Dominique Jean-Pierre Mabire ,  Jean Fernand Armand Lacrampe ,  Gerard Charles Sanz

IPC分类号： A61K31422

CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04 ,  C07D513/04

摘要： The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

摘要翻译： 本发明涉及配制N-氧化物的化合物，其药学上可接受的加成盐和立体化学异构形式，其中R 1是氢，羟基，C 1-6烷基或芳基; R2是氢; 任选取代的C 1-12烷基; C 3-7环烷基; C 2-8烯基，任选取代的吡咯烷基或芳基; R3是氢，任选取代的C 1-6烷基或芳基; Het是选自咪唑基，三唑基，四唑基和吡啶基的任选取代的不饱和杂环;是任选取代的不饱和单环或双环杂环; 并且芳基是任选取代的苯基。 本发明还涉及其制备方法和包含所述新化合物的组合物，以及它们作为药物的用途。