公开(公告)号：US06667376B2

公开(公告)日：2003-12-23

申请号：US10104740

申请日：2002-03-22

Applicant: Dominique Charmot ,  Han-Ting Chang ,  Manikandan Jayaraman ,  Victor Nava-Salgado

Inventor： Dominique Charmot ,  Han-Ting Chang ,  Manikandan Jayaraman ,  Victor Nava-Salgado

IPC: C08F200

CPC classification number: C07D295/24 ,  C07C329/16 ,  C07C2601/14 ,  C07D207/46 ,  C07D209/30 ,  C07D291/06 ,  C08F2/38 ,  C08F293/005

Abstract: Control agents that have an oxygen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers, particularly vinyl monomers.

Abstract translation: 具有共价键合到硫代羰基部分上的氧 - 氮键的对照试剂被提供用于多种单体，特别是乙烯基单体的活性型自由基聚合。

公开(公告)号：US20030204034A1

公开(公告)日：2003-10-30

申请号：US10104740

申请日：2002-03-22

Applicant: Symyx Technologies, Inc.

Inventor： Dominique Charmot ,  Han-Ting Chang ,  Manikandan Jayaraman ,  Victor Nava-Salgado

IPC: C08F004/04

CPC classification number: C07D295/24 ,  C07C329/16 ,  C07C2601/14 ,  C07D207/46 ,  C07D209/30 ,  C07D291/06 ,  C08F2/38 ,  C08F293/005

Abstract: Control agents that have an oxygen-nitrogen bond covalently bonded to a thiocarbonyl moiety are provided for living-type free radical polymerization of a wide variety of monomers, particularly vinyl monomers.

Abstract translation: 具有共价键合到硫代羰基部分上的氧 - 氮键的对照试剂被提供用于多种单体，特别是乙烯基单体的活性型自由基聚合。

公开(公告)号：US20030153510A1

公开(公告)日：2003-08-14

申请号：US10362149

申请日：2003-02-19

Inventor： Michael W Cappi ,  Thilo Fuchs ,  Robert Eckl ,  Silke Schabbert

IPC: A61K038/04 ,  C07K005/04

CPC classification number: C07D295/185 ,  C07D211/32 ,  C07D211/52 ,  C07D213/38 ,  C07D213/74 ,  C07D217/06 ,  C07D295/24 ,  C07D309/12 ,  C07D401/12 ,  C07D405/12

Abstract: The present invention relates to compounds of formula (I): 1 or a pharmaceutically acceptable salt, solvate, hydrate or a pharmaceutically acceptable formulation thereof. Those compounds can be used for inhibiting factor Xa and for the prevention and/or treatment of thromboembolic conditions.

Abstract translation: 本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物，水合物或其药学上可接受的制剂。 那些化合物可用于抑制因子Xa和用于预防和/或治疗血栓栓塞症状。

公开(公告)号：US06538141B1

公开(公告)日：2003-03-25

申请号：US09869798

申请日：2001-09-24

Applicant: Jean-Philippe Gillet ,  Olivier Guerret ,  Jean-Pierre Lascombe

Inventor： Jean-Philippe Gillet ,  Olivier Guerret ,  Jean-Pierre Lascombe

IPC: A61K21372

CPC classification number: C07D295/24 ,  C07C291/04

Abstract: The invention concerns a method for preparing nitroxides, which consists in oxidising, in a two-phase medium, using an aliphatic peroxide, secondary amines with steric hindrance or having a —CH in the nitrogen atom &agr;.

Abstract translation: 本发明涉及一种制备氮氧化物的方法，该方法包括在二相介质中使用脂肪族过氧化物，具有空间位阻的仲胺或在氮原子中具有-CH的α氧化。

公开(公告)号：US06498275B1

公开(公告)日：2002-12-24

申请号：US09700370

申请日：2000-11-15

Applicant: Roger J Butlin ,  Thorsten Nowak ,  Jeremy N Burrows ,  Michael H Block

Inventor： Roger J Butlin ,  Thorsten Nowak ,  Jeremy N Burrows ,  Michael H Block

IPC: C07C23305

CPC classification number: C07D295/192 ,  A61K31/167 ,  C07C235/16 ,  C07C317/40 ,  C07C317/42 ,  C07C317/44 ,  C07C323/65 ,  C07D295/096 ,  C07D295/13 ,  C07D295/15 ,  C07D295/205 ,  C07D295/24 ,  C07D295/26

Abstract: The use of compounds of the formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs: wherein: Ring C is phenyl or a carbon linked heteroaryl ring substituted as defmed within; R1 is an ortho substituent as defined within; n is 1 or 2; A—B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.

Abstract translation: 使用式（I）化合物及其盐; 和所述式（I）化合物的药学上可接受的体内可切割前药; 和所述化合物或所述前药的药学上可接受的盐：其中：环C是苯基或被定义在其中的碳连接的杂芳基环; R 1是如在其中所定义的邻位取代基; n是1或2; AB是如所定义的连接基团 其中R 2和R 3如本文所定义; R 4是羟基，氢，卤素，氨基或甲基; 在制备用于升高温血动物（例如人）中PDH活性的药物中的用途。 还描述了制备式（I）化合物的药物组合物，方法和方法。

公开(公告)号：US20020193383A1

公开(公告)日：2002-12-19

申请号：US10132677

申请日：2002-04-22

Applicant: Recordati S.A., Chemical and Pharmaceutical Comoany

Inventor： Amedeo Leonardi ,  Gianni Motta ,  Carlo Riva ,  Rodolfo Testa

IPC: A61K031/496 ,  A61K031/495 ,  C07D43/02 ,  C07D241/04

CPC classification number: C07D213/81 ,  C07D209/08 ,  C07D213/82 ,  C07D241/24 ,  C07D295/13 ,  C07D295/24 ,  C07D307/68 ,  C07D333/38

Abstract: The present invention is directed to novel 1-(N-phenylaminoalkyl)piperazine derivatives substituted at the position 2 of the phenyl ring. Pharmaceutical compositions comprising the compounds of the invention also are contemplated. The compounds of the present invention also are contemplated for use in treating neuromuscular dysfunction of the lower urinary tract in a mammal.

Abstract translation: 本发明涉及在苯环的2位被取代的新的1-（N-苯基氨基烷基）哌嗪衍生物。 还考虑了包含本发明化合物的药物组合物。 本发明的化合物也可用于治疗哺乳动物中下泌尿道的神经肌肉功能障碍。

公开(公告)号：US06344560B1

公开(公告)日：2002-02-05

申请号：US09564221

申请日：2000-05-03

Applicant: Brendan J. Geelan ,  Brigitte Benage ,  Gerald J. Abruscato ,  Kirk A. Schlup ,  Ruben S. Grewal ,  Andrew J. Eisenstein

Inventor： Brendan J. Geelan ,  Brigitte Benage ,  Gerald J. Abruscato ,  Kirk A. Schlup ,  Ruben S. Grewal ,  Andrew J. Eisenstein

IPC: C07F906

CPC classification number: C07D295/24 ,  C07B63/04 ,  C07C291/02 ,  C07D211/94

Abstract: A nitroaromatic compound is used to enhance the solubility of a nitroxyl compound in an aromatic hydrocarbon solvent.

Abstract translation: 硝基芳族化合物用于增强硝酰基化合物在芳族烃溶剂中的溶解度。

公开(公告)号：US5972977A

公开(公告)日：1999-10-26

申请号：US847386

申请日：1997-04-23

Applicant: Kenneth W. Narducy ,  Efraim Duzman ,  John Michael Carney ,  Allan Lee Wilcox

Inventor： Kenneth W. Narducy ,  Efraim Duzman ,  John Michael Carney ,  Allan Lee Wilcox

IPC: C07D207/46 ,  A61K31/00 ,  A61K31/135 ,  A61K31/15 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/44 ,  A61K31/4412 ,  A61P27/00 ,  A61P27/14 ,  C07C291/02 ,  C07D213/89 ,  C07D295/24 ,  C07D213/30 ,  C07D213/74

CPC classification number: C07D213/89 ,  A61K31/135 ,  A61K31/40 ,  A61K31/4015 ,  A61K31/44 ,  A61K31/4412 ,  C07C291/02 ,  C07D295/24

Abstract: Ophthalmic pharmaceutical compositions containing a pharmaceutically acceptable ophthalmic carrier and an inflammation-treating amount of a nitrone compound are disclosed. Also disclosed are methods for treating ocular inflammation conditions, such as uveitis, using pharmaceutical compositions.

Abstract translation: 公开了含有药学上可接受的眼用载体和炎症治疗量的硝酮化合物的眼用药物组合物。 还公开了使用药物组合物治疗眼部炎症病症如葡萄膜炎的方法。

公开(公告)号：US5972939A

公开(公告)日：1999-10-26

申请号：US179135

申请日：1998-10-26

Applicant: Robert H. Chen ,  Min Xiang ,  John B. Moore, Jr. ,  Mary Pat Beavers

Inventor： Robert H. Chen ,  Min Xiang ,  John B. Moore, Jr. ,  Mary Pat Beavers

IPC: C07D295/08 ,  A61K31/16 ,  A61K31/167 ,  A61K31/216 ,  A61K31/40 ,  A61K31/4409 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/5375 ,  A61K31/5377 ,  A61P1/00 ,  A61P1/06 ,  A61P1/12 ,  A61P43/00 ,  C07C233/41 ,  C07C233/78 ,  C07C323/36 ,  C07C323/42 ,  C07D211/26 ,  C07D211/58 ,  C07D213/81 ,  C07D295/092 ,  C07D295/13 ,  C07D295/22 ,  C07D295/24 ,  C07D317/68 ,  C07D333/38 ,  A61K31/535 ,  C07C233/34 ,  C07D295/14

CPC classification number: C07D213/81 ,  C07C233/41 ,  C07C233/78 ,  C07C323/36 ,  C07C323/42 ,  C07D211/26 ,  C07D211/58 ,  C07D295/088 ,  C07D295/13 ,  C07D295/24 ,  C07D333/38 ,  C07C2101/10 ,  C07C2101/14

Abstract: The compounds of formula I are useful in treating gastrointestinal disorders associated with antagonizing the motilin receptor disorders. The compounds compete with erythromycin and motilin for the motilin receptor. In addition the compounds are antagonists of the contractile smooth muscle response to those ligands.

Abstract translation: 式I化合物可用于治疗与拮抗胃动素受体紊乱相关的胃肠道疾病。 这些化合物与红霉素和胃动素与胃动素受体竞争。 此外，化合物是对这些配体的收缩平滑肌反应的拮抗剂。

公开(公告)号：US5844025A

公开(公告)日：1998-12-01

申请号：US755882

申请日：1996-12-02

Applicant: Glen Thomas Cunkle ,  Thomas F. Thompson ,  Volker H. von Ahn ,  Roland A. E. Winter

Inventor： Glen Thomas Cunkle ,  Thomas F. Thompson ,  Volker H. von Ahn ,  Roland A. E. Winter

IPC: C07D209/46 ,  C07C7/20 ,  C07C17/42 ,  C07C239/20 ,  C07D209/08 ,  C07D211/94 ,  C07D295/24 ,  C08F2/40 ,  C08K5/3435 ,  C08K5/34

CPC classification number: C07D295/24 ,  C07C17/42 ,  C07C239/20 ,  C07D211/94 ,  C08K5/3435

Abstract: 1,2-Bis-adducts of stable hindered nitroxide compounds with substituted ethylenes are prepared by reacting two equivalents of nitroxyl compound with an ethylenically unsaturated compound such as styrene or an acrylate ester. These adducts are very effective inhibitors to prevent the premature polymerization of ethylenically unsaturated monomers when such monomers are distilled, processed or stored.

Abstract translation: 通过使两当量的硝酰基化合物与烯属不饱和化合物如苯乙烯或丙烯酸酯反应来制备稳定的受阻氮氧化物与取代的乙烯的1,2-双加合物。 当这些单体蒸馏，加工或储存时，这些加合物是防止烯属不饱和单体过早聚合的非常有效的抑制剂。