公开(公告)号：EP1087958A1

公开(公告)日：2001-04-04

申请号：EP99924627.5

申请日：1999-06-10

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, Fat ,  TAO, Yong ,  LI, Yiwei ,  DOUCETTE, Gary

IPC分类号： C07D309/30 ,  C07D309/10

CPC分类号： C07D309/10 ,  C07D309/30

摘要： A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2'-position group of lovastatin without requiring protection/deprotection of 13-OH of lovastatin and lactone ring opening/closure.

公开(公告)号：EP0883622A1

公开(公告)日：1998-12-16

申请号：EP97903172.0

申请日：1997-02-26

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, F. ,  DESILETS, Denis ,  LEE, Sue ,  CAPPELLETTO, Tullio ,  LI, Wanren

IPC分类号： A61K31 ,  A61P1 ,  A61P43 ,  C07D513

CPC分类号： C07D513/04

摘要： Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+/K+-ATPase. The compounds are 3-substituted 1,2,4-thiadiazole [4,5-a]benzimidazole and 3-substituted imidazo[1,2-d]-1,2,4-thiadiazoles corresponding to general formula (I) where X and Z either represented an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is selected from a wide range, e.g. heterocyclics and carbonyl groups.

公开(公告)号：EP1615941A1

公开(公告)日：2006-01-18

申请号：EP04721787.2

申请日：2004-03-19

申请人： APOTEX INC.

发明人： TAM, Tim Fat ,  KARIMIAN, Khashayar ,  HU, Shui, Sheng ,  CHOW, Anna ,  STOREY, Richard William

IPC分类号： C07H17/00 ,  C07H17/08 ,  A61K31/7048 ,  A61P31/04

CPC分类号： C07H17/08 ,  C07H17/00

摘要： Azithromycin isopropanolate of the empirical formula azithromycin: [H20]x: [isopropanol]y is obtained from the crystallization of azithromycin in isopropanol and water. The x and y values is confirmed by single X-ray diffraction determination. In one embodiment x=1.5 and y=0.25. In another embodiment x=0.75 and y=0.5.

公开(公告)号：EP1087958B1

公开(公告)日：2002-09-04

申请号：EP99924627.5

申请日：1999-06-10

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, Fat ,  TAO, Yong ,  LI, Yiwei ,  DOUCETTE, Gary

IPC分类号： C07D309/30 ,  C07D309/10

CPC分类号： C07D309/10 ,  C07D309/30

摘要： A process is disclosed for the preparation of simvastatin which enables highly regio selective C-methylation of the 2'-position group of lovastatin without requiring protection/deprotection of 13-OH of lovastatin and lactone ring opening/closure.

公开(公告)号：EP1058690A1

公开(公告)日：2000-12-13

申请号：EP99906005.6

申请日：1999-02-23

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim F. ,  LEUNG-TOUNG, Regis C. S. H. ,  LI, Wanren

IPC分类号： C07K5/062 ,  C07K5/065 ,  A61K38/05 ,  C07D285/08 ,  A61K31/425

CPC分类号： C07D285/08 ,  C07K5/06034 ,  C07K5/06043

摘要： Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of general formula (I), where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.

公开(公告)号：EP0883622B1

公开(公告)日：2002-05-15

申请号：EP97903172.1

申请日：1997-02-26

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, F. ,  DESILETS, Denis ,  LEE, Sue ,  CAPPELLETTO, Tullio ,  LI, Wanren

IPC分类号： C07D513/04 ,  A61K31/415

CPC分类号： C07D513/04

摘要： Novel thiadiazole compounds are provided, which are effective as proton pumps inhibitors, useful in treating peptic ulcers by inhibition of the proton pump enzyme H+/K+-ATPase. The compounds are 3-substituted 1,2,4-thiadiazole [4,5-a]benzimidazole and 3-substituted imidazo[1,2-d]-1,2,4-thiadiazoles corresponding to general formula (I) where X and Z either represented an optionally substituted benzene ring fused to the diazole nucleus, or represent a variety of independent chemical groupings (hydrogen, lower alkyl, halo, etc.) and Y is selected from a wide range, e.g. heterocyclics and carbonyl groups.

公开(公告)号：EP0883606A1

公开(公告)日：1998-12-16

申请号：EP97903184.0

申请日：1997-02-26

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, F. ,  DESILETS, Denis ,  LEE, Sue ,  CAPPELLETTO, Tullio ,  LI, Wanren

IPC分类号： A61K31 ,  A61P1 ,  A61P43 ,  C07C319 ,  C07C321 ,  C07D285 ,  C07D513

CPC分类号： C07D285/08 ,  C07C319/24 ,  C07C321/20 ,  C07C321/22

摘要： Thiols are trapped, and converted to disulfide compounds, by a process of reacting them with compounds containing a 1,2,4-thiadiazole ring structure carrying a substituent at position 3 of the thiadiazole ring, and being unsubstituted at position N-2. The process is useful pharmacologically, in inhibiting certain thiol-containing enzymes such as H+/K+-ATPase (the proton pump), and industrially, in selective removal of thiol compounds from gas or liquid mixtures.

公开(公告)号：EP0840730A1

公开(公告)日：1998-05-13

申请号：EP96922717.0

申请日：1996-07-17

申请人： APOTEX INC.

发明人： KARIMIAN, Khashayar ,  TAM, Tim, Fat ,  BRAGANZA, John, Frederick ,  GOLDBERG, Yuri ,  ZINGHINI, Salvatore

IPC分类号： C07D249 ,  C07D521

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56

摘要： A process to prepare a compound of formula (I) wherein Y and Z can be identical or different and represent a halogene. The bis-triazole compounds of formula (I) and intermediates have antifungal activity.