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1. 发明申请

WO2010117738A3 SOLID STATE FORMS OF SITAGLIPTIN SALTS 审中-公开
公开(公告)号：WO2010117738A3
公开(公告)日：2010-10-14
申请号：PCT/US2010/029098
申请日：2010-03-29
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , PILARSKI, Gideon , PERLMAN, Nurit , MITTELMAN, Ariel , KOSUTIC HULITA, Nada , KALUJNY, Marina , RAMATY, Revital
发明人： PILARSKI, Gideon , PERLMAN, Nurit , MITTELMAN, Ariel , KOSUTIC HULITA, Nada , KALUJNY, Marina , RAMATY, Revital
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/10
摘要： Solid state forms of Sitagliptin salts, processes for preparing the solid state forms, and pharmaceutical compositions thereof, are provided.

2. 发明申请

WO2009011844A1 PROCESSES FOR SOLIFENACIN PREPARATION 审中-公开
标题翻译：辛伐他汀制剂的方法
公开(公告)号：WO2009011844A1
公开(公告)日：2009-01-22
申请号：PCT/US2008/008634
申请日：2008-07-14
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , PERLMAN, Nurit , PILARSKI, Gideon
发明人： PERLMAN, Nurit , PILARSKI, Gideon
IPC分类号： C07D453/02
CPC分类号： C07D453/02
摘要： Processes for preparing solifenacin comprising distilling ethanol and organic solvent from a reaction mixture and recycling the organic solvent are described. The ethanol is removed using a Dean-Stark apparatus. Also described are processes for reducing solifenacin diastereomeric and enantiomeric impurities.
摘要翻译：描述了制备索非那新的方法，其包括从反应混合物中蒸馏出乙醇和有机溶剂并回收有机溶剂。使用Dean-Stark装置除去乙醇。还描述了降低索非那新非对映体和对映异构体杂质的方法。

3. 发明申请

WO2004069825A1 SYNTHESIS OF GATIFLOXACIN 审中-公开
标题翻译： GATIFLOXACIN的合成
公开(公告)号：WO2004069825A1
公开(公告)日：2004-08-19
申请号：PCT/US2003/025594
申请日：2003-08-14
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , NIDDAM-HILDESHEIM, Valerie , DOLITZKY, Ben-Zion , PILARSKI, Gideon , STERIMBAUM, Greta
发明人： NIDDAM-HILDESHEIM, Valerie , DOLITZKY, Ben-Zion , PILARSKI, Gideon , STERIMBAUM, Greta
IPC分类号： C07D401/04
CPC分类号： C07D215/56 , C07D401/04
摘要： Provided is a method for making (±)-1-Cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-(3-methyl-1-piperazinyl)-4-oxo-3-quinolenecarboxylic acid, commonly known as gatifloxacin, in very high purity, in a suspension in a dipolar aprotic solvent.
摘要翻译：提供了制备（±）-1-环丙基-6-氟-1,4-二氢-8-甲氧基-7-（3-甲基-1-哌嗪基）-4-氧代-3-喹啉羧酸的方法，通常称为加替沙星，非常高的纯度，在偶极非质子溶剂中的悬浮液中。

4. 发明申请

WO2006121557A1 PREGABALIN FREE OF LACTAM AND A PROCESS FOR PREPARATION THEREOF 审中-公开
标题翻译：普瑞格林不含赖氨酸及其制备方法
公开(公告)号：WO2006121557A1
公开(公告)日：2006-11-16
申请号：PCT/US2006/013360
申请日：2006-04-11
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , HEDVATI, Lilach , PILARSKI, Gideon , RAIZI, Yuriy , TOMER, Sharon , DEE NOOR, Ziv , SINGER, Claude
发明人： HEDVATI, Lilach , PILARSKI, Gideon , RAIZI, Yuriy , TOMER, Sharon , DEE NOOR, Ziv , SINGER, Claude
IPC分类号： C07C229/08 , A61K31/197 , A61P25/00 , G01N30/00
CPC分类号： C07C229/08 , G01N30/8675 , G01N2030/027 , G01N2030/8813 , G01N2030/8818
摘要： The present invention encompasses Pregabalin substantially free of Lactam and a process for obtaining Pregabalin substantially free of Lactam comprising extracting an acidic mixture containing a complex of Pregabalin with a strong mineral acid, with a C 3-8 alcohol; and combining the organic phase with an organic base.
摘要翻译：本发明包括基本上不含内酰胺的普瑞巴林，以及获得基本上不含内酰胺的普瑞巴林的方法，其包括用C 3〜3-8醇提取含有普瑞巴林与强无机酸的复合物的酸性混合物; 并将有机相与有机碱结合。

5. 发明申请

WO2003072552A1 METHOD FOR PREPARING BENZISOXAZOLE METHANE SULFONYL CHLORIDE AND ITS AMIDATION TO FORM ZONISAMIDE 审中-公开
标题翻译：苯并噻唑甲磺酰氯的制备方法及其制备方法
公开(公告)号：WO2003072552A1
公开(公告)日：2003-09-04
申请号：PCT/US2003/005690
申请日：2003-02-24
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , MENDELOVICI, Marioara , GERSHON, Neomi , NIDAM, Tamar , PILARSKI, Gideon , STERINBAUM, Greta
发明人： MENDELOVICI, Marioara , GERSHON, Neomi , NIDAM, Tamar , PILARSKI, Gideon , STERINBAUM, Greta
IPC分类号： C07D261/20
CPC分类号： C07D261/20 , C07D405/12
摘要： The present invention relates to a process of preparing benzisoxazole methane sulfonic acid-chloride (BOS-CI) as an zonisamide intermediate via chlorination of benzisoxazole methane sulfonate. The present invention also disloses a process of preparing zonisamide via amidation of BOS-CI. More particularly, the present invention provides a process of preparing zonisamide, comprising the steps of : a) chlorinating BOS; salts or esters thereof, with SOCl 2 in an organic solvent and/or in the presence of a catalyst to form BOS-Cl; and b) amidating BOS-Cl in the presence of ammonia selected from the group consisting of aqueous ammonia in a biphasic system, masked ammonia and dry ammonia to form zonisamide.
摘要翻译：本发明涉及通过氯化苯并异恶唑甲烷磺酸盐制备苯并异恶唑甲磺酸氯化物（BOS-CI）作为唑烷酰胺中间体的方法。本发明还消除了通过BOS-CI的酰胺化制备唑尼沙胺的方法。更具体地，本发明提供了制备唑尼沙胺的方法，包括以下步骤：a）氯化BOS; 盐或酯，与SOCl 2在有机溶剂中和/或在催化剂存在下形成BOS-Cl; 和b）在选自二元体系中的氨水，掩蔽的氨和干氨中的氨存在下使BOS-Cl酰胺化以形成唑尼沙胺。

6. 发明申请

WO2008057559A1 PROCESSES FOR PREPARING SUBSTANTIALLY PURE PANTOPRAZOLE MAGNESIUM 审中-公开
标题翻译：制备大量纯PANTOPRAZOZO MAGNESIUM的方法
公开(公告)号：WO2008057559A1
公开(公告)日：2008-05-15
申请号：PCT/US2007/023438
申请日：2007-11-05
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , HEDVATI, Lilach , PILARSKI, Gideon
发明人： HEDVATI, Lilach , PILARSKI, Gideon
IPC分类号： C07D401/12
CPC分类号： C07D401/12
摘要： Provided are processes for preparing substantially pure pantoprazole magnesium. A mixture of pantoprazole acid, a magnesium base (in particular alkoxides) in an alcohol is prepared and an organic solvent is added to precipitate the pantoprazole magnesium.
摘要翻译：提供了制备基本上纯的泮托拉唑镁的方法。制备泮托拉唑酸，镁基（特别是醇盐）在醇中的混合物，并加入有机溶剂以沉淀泮托拉唑镁。

7. 发明申请

WO2004062571A2 SUBSTANTIALLY PURE CILOSTAZOL AND PROCESSES FOR MAKING SAME 审中-公开
标题翻译：非常纯的西洛他唑及其制备方法
公开(公告)号：WO2004062571A2
公开(公告)日：2004-07-29
申请号：PCT/US2003/000324
申请日：2003-01-06
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , MENDELOVICI, Marioara , FINKELSTEIN, Nina , PILARSKI, Gideon
发明人： MENDELOVICI, Marioara , FINKELSTEIN, Nina , PILARSKI, Gideon
IPC分类号： A61K
CPC分类号： C07C231/02 , C07D215/227 , C07D401/12 , C07C233/25
摘要： The present invention provides substantially pure cilostazol. The present invention also provides cilostazol particles that have reduced particle size.
摘要翻译：本发明提供基本上纯的西洛他唑。本发明还提供粒度减小的西洛他唑颗粒。

8. 发明申请

WO2002102382A1 A PROCESS FOR PREPARING PAROXETINE HCl WHICH LIMITS FORMATION OF PINK COLORED COMPOUNDS 审中-公开
标题翻译：用于制备限制形成粉红色染料的化合物的异柠檬酸盐的方法
公开(公告)号：WO2002102382A1
公开(公告)日：2002-12-27
申请号：PCT/US2002/019016
申请日：2002-06-14
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , AVRUTOV, Ilya , PILARSKI, Gideon
发明人： AVRUTOV, Ilya , PILARSKI, Gideon
IPC分类号： A61K31/445
CPC分类号： C07D405/12
摘要： The present invention provides a process for preparing paroxetine HCl from paroxetine base which provides paroxetine HCl substantially free of pink-colored compounds or an impurity identified by an HPLC RRT of about 1.5. The processes of the present invention utilize a buffer, a molar ratio of HCl to paroxetine base of less than one, and crystallize/recrystallize in the presence of an effective amount of an anti-oxidant. A preferred way to create a buffer is by using ammonium chloride. A preferred anti-oxidant is ascorbic acid. The present invention also provides for re-crystallizing paroxetine HCl prepared by the above methods or any other methods in the presence of an effective amount of an anti-oxidant such as ascorbic acid. A preferred solvent system for recrystallization is a mixture of acetone and methanol. Processes of the present invention can combine these various features.
摘要翻译：本发明提供了一种从帕罗西汀碱制备帕罗西汀HCl的方法，其提供基本上不含粉红色化合物的帕罗西汀HCl或通过约1.5的HPLC RRT鉴定的杂质。本发明的方法利用缓冲液，HCl与帕罗西汀碱的摩尔比小于1，并在有效量的抗氧化剂存在下结晶/重结晶。创建缓冲液的优选方法是使用氯化铵。优选的抗氧化剂是抗坏血酸。本发明还提供了通过上述方法或任何其它方法在有效量的抗氧化剂如抗坏血酸存在下制备的帕罗西汀HCl的再结晶。用于重结晶的优选溶剂体系是丙酮和甲醇的混合物。本发明的方法可以组合这些各种特征。

9. 发明申请

WO2010009402A9 NILOTINIB INTERMEDIATES AND PREPARATION THEREOF 审中-公开
公开(公告)号：WO2010009402A9
公开(公告)日：2010-01-21
申请号：PCT/US2009/051001
申请日：2009-07-17
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , WANG, Yanling , LI, Jie , KANSAL, Vinod, Kumar , ZHU, Jirang , LIFSHITZ-LIRON, Revital , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , ARIYAMUTHU, Sundaraselvan , PILARSKI, Gideon , HE, Xungui
发明人： WANG, Yanling , LI, Jie , KANSAL, Vinod, Kumar , ZHU, Jirang , LIFSHITZ-LIRON, Revital , MISTRY, Dhirenkumar, N. , VASOYA, Sanjay, L. , ARIYAMUTHU, Sundaraselvan , PILARSKI, Gideon , HE, Xungui
IPC分类号： C07D233/61 , C07D401/04 , C07D401/14
摘要： Intermediates of Nilotinib were prepared, including, for example, 3-(trifluoromethyl- 5 -(4-methyl- 1 H-imidazole- 1 -yl)-benzeneamine; 3 -(4-(pyridin-3 -yl)pyrimidin-2-ylamino)-4- methylbenzoyl halogen dihydrochloride; and N-(3-Bromo-5-trifluoromethylphenyl)-4- methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]benzamide. Nilotinib»3HCl and its crystalline forms are also described.

10. 发明申请

WO2006122259A1 OPTICAL RESOLUTION OF 3-CARBAMOYLMETHYL-5-METHYL HEXANOIC ACID 审中-公开
标题翻译： 3-羧甲基甲基-5-甲基十六烷酸的光学分解
公开(公告)号：WO2006122259A1
公开(公告)日：2006-11-16
申请号：PCT/US2006/018273
申请日：2006-05-10
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD. , TEVA PHARMACEUTICALS USA, INC. , HEDVATI, Lilach , DEE NOOR, Ziv , SINGER, Claude , PILARSKI, Gideon
发明人： HEDVATI, Lilach , DEE NOOR, Ziv , SINGER, Claude , PILARSKI, Gideon
IPC分类号： C07C233/05 , C07C231/20 , C07C215/30 , C07C227/16 , C07C229/08 , A61K31/197 , A61P25/08
CPC分类号： C07C215/30 , C07C227/16 , C07C229/08 , C07C231/20 , C07C233/05
摘要： The invention relates to pure (R)-CMH and to the optical resolution of CMH- racemate, a key intermediate in the synthesis of (S)-Pregabalin. The invention also relates to the process for optically purifying (R)-CMH and to the process for isolatin (S)-CMH from the mother liquor.
摘要翻译：本发明涉及纯（R）-CMH和涉及（S）-Pregabalin合成中关键中间体的CMH-外消旋物的光学拆分。本发明还涉及用于从母液中旋光纯化（R）-CMH的方法和用于分离（S）-CMH的方法。

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