公开(公告)号：US06472529B2

公开(公告)日：2002-10-29

申请号：US09837280

申请日：2001-04-18

申请人： Hing Leung Sham ,  Daniel W. Norbeck ,  Xiaoqi Chen ,  David A. Betebenner ,  Dale J. Kempf ,  Thomas R. Herrin ,  Gondi N. Kumar ,  Stephen L. Condon ,  Arthur J. Cooper ,  Daniel A. Dickman ,  Steven M. Hannick ,  Lawrence Kolaczkowski ,  Patricia A. Oliver ,  Daniel J. Plata ,  Peter J. Stengel ,  Eric J. Stoner ,  Jieh-Heh J. Tien ,  Jih-Hua Liu ,  Ketan M. Patel

发明人： Hing Leung Sham ,  Daniel W. Norbeck ,  Xiaoqi Chen ,  David A. Betebenner ,  Dale J. Kempf ,  Thomas R. Herrin ,  Gondi N. Kumar ,  Stephen L. Condon ,  Arthur J. Cooper ,  Daniel A. Dickman ,  Steven M. Hannick ,  Lawrence Kolaczkowski ,  Patricia A. Oliver ,  Daniel J. Plata ,  Peter J. Stengel ,  Eric J. Stoner ,  Jieh-Heh J. Tien ,  Jih-Hua Liu ,  Ketan M. Patel

IPC分类号： C07D23332

CPC分类号： C07D207/27 ,  C07D207/404 ,  C07D207/408 ,  C07D223/10 ,  C07D233/32 ,  C07D233/42 ,  C07D239/10 ,  C07D239/22 ,  C07D241/08 ,  C07D241/18 ,  C07D253/06 ,  C07D263/22 ,  C07D307/20 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

摘要： A compound of the formula: is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

摘要翻译： 公开了下式的化合物作为HIV蛋白酶抑制剂。 还公开了用于抑制HIV感染的方法和组合物。

公开(公告)号：US06403805B1

公开(公告)日：2002-06-11

申请号：US09362007

申请日：1999-07-27

申请人： Eddy Jean Edgard Freyne ,  Gaston Stanislas Marcella Diels ,  José Ignacio Andrés-Gil ,  Francisco Javier Fernández-Gadea

发明人： Eddy Jean Edgard Freyne ,  Gaston Stanislas Marcella Diels ,  José Ignacio Andrés-Gil ,  Francisco Javier Fernández-Gadea

IPC分类号： C07D23332

CPC分类号： C07D401/06 ,  C07D233/36 ,  C07D233/38 ,  C07D233/70

摘要： The present invention describes compounds useful for treating warm-blooded animals suffering from disease states related to an abnormal enzymatic or catalytic activity of phosphodiesterase IV (PDE IV), and/or disease states related to a physiologically detrimental excess of cytokines, in particular allergic, atopic and inflammatory diseases, said compounds having the formula the N-oxide forms, the pharmaceutically acceptable acid or base addition salts and the stereochemically isomeric forms thereof.

摘要翻译： 本发明描述了可用于治疗患有与磷酸二酯酶IV（PDE IV）的异常酶促或催化活性相关的疾病状态的温血动物的化合物和/或与生理上有害的细胞因子过量相关的疾病状态，特别是过敏性疾病， 特应性和炎症性疾病，所述具有N-氧化物形式的化合物，其药学上可接受的酸或碱加成盐及其立体化学异构形式。

公开(公告)号：US06835741B2

公开(公告)日：2004-12-28

申请号：US10673100

申请日：2003-09-26

申请人： Natesan Murugesan ,  John E. Tellew ,  John E. Macor ,  Zhengxiang Gu

发明人： Natesan Murugesan ,  John E. Tellew ,  John E. Macor ,  Zhengxiang Gu

IPC分类号： C07D23332

CPC分类号： C07D401/12 ,  C07D261/16 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

公开(公告)号：US06307057B1

公开(公告)日：2001-10-23

申请号：US09547958

申请日：2000-04-12

申请人： David W. C. MacMillan ,  Kateri A. Ahrendt

发明人： David W. C. MacMillan ,  Kateri A. Ahrendt

IPC分类号： C07D23332

CPC分类号： C07D493/08 ,  B01J31/0237 ,  B01J31/0254 ,  B01J2231/325 ,  B01J2231/326 ,  B01J2231/348 ,  B01J2231/72 ,  C07B37/12 ,  C07B53/00 ,  C07C45/69 ,  C07C67/293 ,  C07D233/32 ,  C07D307/46 ,  C07C47/445 ,  C07C47/453 ,  C07C49/453 ,  C07C47/42 ,  C07C69/013 ,  C07C69/145

摘要： Acid addition salts of imidazolidinones are provided as catalysts for transforming a functional group within a first reactant by reaction with a second reactant. Exemplary first reactants are &agr;,&bgr;-unsaturated carbonyl compounds such as &agr;,&bgr;-unsaturated ketones and &agr;,&bgr;-unsaturated aldehydes. Chiral imidazolidinone salts can be used to catalyze enantioselective reactions, such that a chiral product is obtained from a chiral or achiral starting material in enantiomerically pure form.

摘要翻译： 提供咪唑啉酮的酸加成盐作为用于通过与第二反应物反应转化第一反应物中的官能团的催化剂。 示例性的第一反应物是α，β-不饱和羰基化合物，例如α，β-不饱和酮和α，β-不饱和醛。 手性咪唑烷酮盐可用于催化对映选择性反应，使得手性产物以手性或非手性起始原料以对映体纯的形式获得。

公开(公告)号：US06638937B2

公开(公告)日：2003-10-28

申请号：US09737201

申请日：2000-12-14

申请人： Natesan Murugesan ,  John E. Tellew ,  John E. Macor ,  Zhengxiang Gu

发明人： Natesan Murugesan ,  John E. Tellew ,  John E. Macor ,  Zhengxiang Gu

IPC分类号： C07D23332

CPC分类号： C07D401/12 ,  C07D261/16 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04

摘要： Novel biphenyl sulfonamide compounds which are combined angiotensin and endothelin receptor antagonists are claimed along with methods of using such compounds in the treatment of conditions such as hypertension and other diseases, as well as pharmaceutical compositions containing such compounds.

公开(公告)号：US06515138B2

公开(公告)日：2003-02-04

申请号：US10091770

申请日：2002-03-06

申请人： William David Weir ,  Donald Robert Weyler ,  William Joseph Grieco

发明人： William David Weir ,  Donald Robert Weyler ,  William Joseph Grieco

IPC分类号： C07D23332

CPC分类号： C07D233/36 ,  C07C29/1285 ,  C12C11/02 ,  C07C31/04

摘要： An improved transesterification process is disclosed for forming certain (meth)acrylates by the transesterification of an alkyl (meth)acrylate with a hydroxyl alkyl imidazolidin-2-one using a transesterification catalyst in the presence of a polymerization inhibitor.

公开(公告)号：US06291681B1

公开(公告)日：2001-09-18

申请号：US09780253

申请日：2001-02-09

申请人： Juergen Fleckenstein ,  Bernd Kraemer ,  Joachim Veits

发明人： Juergen Fleckenstein ,  Bernd Kraemer ,  Joachim Veits

IPC分类号： C07D23332

CPC分类号： C07D491/04 ,  C07D233/32

摘要： The present invention is directed to a process for the production of 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid and of 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid anhydride, starting from meso-2,3-bis(benzylamino)succinic acid dialkali metal salt. The process involves reacting meso-2,3-bis(benzylamino)succinic acid dialkali metal salt with phenyl chloroformate in a monophasic solvent system consisting of an about 2:1 to 1:1 mixture of a water-miscible ether and an aqueous alkali metal hydroxide solution, at a temperature not exceeding about 40° C. The resulting 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid dialkali metal salt is converted, by acidification, into the desired 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid, which is then either isolated, or converted, by heating with acetic anhydride, in an aromatic hydrocarbon as the organic solvent, into the desired 2-oxo-1,3-dibenzyl-cis-4,5-imidazolidinedicarboxylic acid anhydride, which is in turn, isolated. Each product is an important intermediate in the multi-stage process for the manufacture of biotin (vitamin H).

摘要翻译： 本发明涉及2-氧代-1,3-二苄基 - 顺-4,5-咪唑烷二羧酸和2-氧代-1,3-二苄基 - 顺-4,5-咪唑烷二羧酸的制备方法 酸酐，从内消旋-2,3-双（苄基氨基）琥珀酸二碱金属盐开始。 该方法包括使内消旋-2,3-双（苄基氨基）琥珀酸二碱金属盐与氯甲酸苯酯在单相溶剂体系中反应，所述单相溶剂系统由水混溶性乙醚和碱金属水溶液的约2:1至1:1混合物组成 氢氧化物溶液，温度不超过约40℃。所得2-氧代-1,3-二苄基 - 顺-4,5-咪唑烷二羧酸二碱金属盐通过酸化转化成所需的2-氧代-1 ，3-二苄基 - 顺-4,5-咪唑烷二羧酸，然后通过用作为有机溶剂的芳族烃中的乙酸酐加热分离或转化成所需的2-氧代-1,3-二苄基 - 顺式-4,5-二咪唑烷二羧酸酐，依次分离。 每个产品是生物素（维生素H）生产的多阶段过程中的重要中间体。