公开(公告)号：EP1853592A1

公开(公告)日：2007-11-14

申请号：EP06718299.8

申请日：2006-01-12

申请人： Schering Corporation

发明人： THIRUVENGADAM, Tiruvettipuram, K. ,  WANG, Tao ,  LIAO, Jing ,  CHIU, John, S. ,  TSAI, David, J. S. ,  LEE, Hong-chang ,  WU, Wenxue ,  FU, Xiaoyong

IPC分类号： C07D405/08 ,  C07D493/10 ,  C07D307/88

CPC分类号： C07D307/77 ,  C07D307/885 ,  C07D307/92 ,  C07D405/06

摘要： The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: Formula (I)

摘要翻译： 本发明涉及制备伊巴辛类似物的改进方法。 该化合物可用作凝血酶受体拮抗剂。 改进的方法可允许通过结晶进行更容易的纯化，更容易的可缩放性和对所需对映体的改进的加工产率中的至少一个。 合成这种喜巴辛类似物的步骤的实例如下：式（I）

公开(公告)号：EP2035364A2

公开(公告)日：2009-03-18

申请号：EP07796585.3

申请日：2007-06-29

申请人： Schering Corporation

发明人： THIRUVENGADAM, Tiruvettipuram, K. ,  WANG, Tao ,  CHIU, John, S. ,  LIAO, Jing

IPC分类号： C07C201/06 ,  C07C205/55 ,  C07C251/44

CPC分类号： C07C251/44 ,  C07C201/06 ,  C07C249/08 ,  C07C2601/16 ,  C07C205/56 ,  C07C251/42

摘要： This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; Chemical formula should be inserted here as it appears on the abstract in paper form. wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Chemical formula should be inserted here as it appears on the abstract in paper form. Where R1 and R2 are as defined above.

摘要翻译： 该申请公开提供了一种通过由钼VI / VII过氧配合物介导的肟官能团的直接（一步）氧化将硝基官能团引入到还含有不饱和位和/或氧官能团位点的化合物的方法 该方法包括：（a）提供含有肟官能团的式I的底物; 其中R 1和R 2独立地选自直链，支链或环状的烷基和直链，支链或环状的烯基，任选被取代，条件是R 1或R 2中的至少一个含有碳/碳双键; 和（b）使式I的底物与钼氧化络合物接触，从而将所述肟官能团氧化为硝基官能团，得到式III的结构。 其中R1和R2如上所定义。

公开(公告)号：EP1853592B1

公开(公告)日：2011-03-02

申请号：EP06718299.8

申请日：2006-01-12

申请人： Schering Corporation

发明人： THIRUVENGADAM, Tiruvettipuram, K. ,  WANG, Tao ,  LIAO, Jing ,  CHIU, John, S. ,  TSAI, David, J. S. ,  LEE, Hong-chang ,  WU, Wenxue ,  FU, Xiaoyong

IPC分类号： C07D405/08 ,  C07D493/10 ,  C07D307/88

CPC分类号： C07D307/77 ,  C07D307/885 ,  C07D307/92 ,  C07D405/06

摘要： The present invention relates to an improved process for preparing imbacine analogs. The compounds are useful as thrombin receptor antagonists. The improved process may allow for at least one of easier purification by crystallization, easier scalability, and improved process yield on the desired enantiomer. An example of a step in the synthesis of such a himbacine analog is as follows: Formula (I)

公开(公告)号：EP1831162A1

公开(公告)日：2007-09-12

申请号：EP05854581.5

申请日：2005-12-19

申请人： Schering Corporation

发明人： THIRUVETTIPURAM, Thiruvengadam, K. ,  CHIU, John, S. ,  FU, Xiaoyong ,  MCALLISTER, Timothy, L.

IPC分类号： C07D205/08

CPC分类号： C07D205/08 ,  C07H17/02

摘要： A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a ß-(substituted-amino)amide, a ß-(substituted-amino)acid ester, or a ß-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

公开(公告)号：EP1701953A1

公开(公告)日：2006-09-20

申请号：EP05705212.8

申请日：2005-01-07

申请人： SCHERING CORPORATION

发明人： THIRUVENGADAM, Tiruvettipuram, K. ,  WU, Wenxue ,  WANG, Tao ,  CHIU, John, S. ,  BOGDANOWICH-KNIPP, Susan ,  PAVLOVSKY, Anastasia ,  GREENLEE, William, J. ,  GRAZIANO, Michael, P. ,  KOSOGLOU, Teddy ,  CHINTALA, Madhu ,  CHACKALAMANNIL, Samuel

IPC分类号： C07D405/06 ,  C07D307/00 ,  C07D213/00

CPC分类号： C07D417/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D405/06 ,  C07D405/14 ,  C07D413/14

摘要： A crystalline polymorph of a bislulfate salt of a thrombin receptor antagonist compound, which exhibits a powder x-ray diffraction profile substantially the same as that shown in FIG. 1, or which exhibits a differential scanning calorimtery profile substantially the same as that shown in FIG. 3, and is represented by the formula for Compound 2: Chemical formula should be inserted here as it appears on the abstract in paper form. and processes for preparing Compound 2 are disclosed. Pharmaceutical compositions comprising the polymorph of the bisulfate salt and at least one excipient or carrier, and methods of using the polymorph of Compound 2 to treat a variety of physiological disorders, such as thrombosis, are also disclosed.