公开(公告)号：EP1951654B1

公开(公告)日：2011-05-25

申请号：EP05823580.5

申请日：2005-11-25

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  SUBASH CHANDER REDDY, kesireddy

IPC分类号： C07C209/42 ,  C07C231/02

CPC分类号： C07C247/14 ,  C07C231/12 ,  C07C2601/16 ,  C07C233/52

摘要： The present invention provides an improved and commercially viable process for the preparation of oseltamivir phosphate. Thus, for example, ethyl (3R,4R,5S)-4-amino-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate is acetylated with acetic anhydride in methylene chloride in the presence of triethyl amine in the absence of water to give ethyl (3R,4R,5S)-4-(acetylamino)-5-azido-3-(1-ethylpropoxy)-1-cyclohexene-1-carboxylate.

公开(公告)号：EP2295430A2

公开(公告)日：2011-03-16

申请号：EP09174213.0

申请日：2007-07-25

申请人： Hetero Drugs Limited

发明人： Parthasaradhi Reddy, Bandi ,  Rathnakar Reddy, Kura ,  Raji Reddy, Rapolu ,  Muralidhara Reddy, Dasari ,  Peter Paul Raj, Medabalimi

IPC分类号： C07D409/06 ,  A61K31/4178

CPC分类号： C07D409/06

摘要： Crystalline solid of eprosartan acetate and a process for the preparation thereof which comprises dissolving crude eprosartan free base in acetic acid, adding methylene chloride at a temperature below about 40 °C and collecting the precipitated eprosartan acetate crystalline solid.

摘要翻译： 乙酸依普罗沙坦的结晶固体及其制备方法，其包括将粗制的依普罗沙坦游离碱溶解在乙酸中，在低于约40℃的温度下加入二氯甲烷并收集沉淀的依普罗沙坦乙酸酯结晶固体。

公开(公告)号：EP2215083A2

公开(公告)日：2010-08-11

申请号：EP07870533.2

申请日：2007-12-07

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, bandi ,  RATHNAKAR REDDY, kura ,  RAJI REDDY, rapolu ,  MURALIDHARA REDDY, dasari ,  RAMAKRISHNA REDDY, matta

IPC分类号： C07D403/10

CPC分类号： C07D403/10 ,  C07D235/02

摘要： The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2'-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield.

公开(公告)号：EP2213665A1

公开(公告)日：2010-08-04

申请号：EP10160342.1

申请日：2007-08-17

申请人： Hetero Drugs Limited

发明人： Parthasaradhi Reddy, Bandi ,  Rathnakar Reddy, Kura ,  Raji Reddy, Rapolu ,  Muralidhara Reddy, Dasari ,  Srinvasa Rao, Thungathurthy

IPC分类号： C07D239/94 ,  A61K31/517

CPC分类号： C07D239/94

摘要： Crystalline particles of erlotinib hydrochloride having mean particle size (D 50 ) ranging from about 4 µm to 15 µm and 90 volume-% of the particles (D 90 ) ranging from about 14 µm to 30 µm, process of preparation and pharmaceutical composition thereof.

摘要翻译： 平均粒度（D 50）为约4μm〜15μm，90体积％的颗粒（D 90）为约14μm〜30μm的结晶粒子，其制备方法及其药物组成。

公开(公告)号：EP2176241A2

公开(公告)日：2010-04-21

申请号：EP07827536.9

申请日：2007-08-17

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari ,  SRINIVASA RAO, Thungathurthy

IPC分类号： C07D239/94 ,  A61K31/517

CPC分类号： C07D239/94

摘要： The present invention provides a novel and stable hydrated form of erlotinib free base, and a process for its preparation thereof. The present invention also provides a process for preparation of erlotinib hydrochloride crystalline polymorph A substantially free of polymorph B. The present invention further relates to erlotinib hydrochloride crystalline particles having mean particle size (D
50 ) ranging from about 4 μm to 15 μm and 90 volume-% of the particles (D
90 ) ranging from about 14 μm to 30 μm, to the methods for the manufacture of said crystalline particles, and to pharmaceutical compositions comprising said crystalline particles.

公开(公告)号：EP1748998B1

公开(公告)日：2010-01-27

申请号：EP04735319.8

申请日：2004-05-28

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, B. Hetero House ,  RATHNAKAR REDDY, kura Hetero Drugs Limited (R & D) ,  RAJI REDDY, rapolu Hetero Drugs Limited (R & D) ,  MURALIDHARA REDDY, D. Hetero Drugs Limited (R & D)

IPC分类号： C07D401/12

CPC分类号： C07D401/12

摘要： The present invention relates to a process for stereoselective synthesis of substituted sulfoxides either as a single enantiomer or in an enantiomerically enriched form. Thus, 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)methyl]thio]-1H-benzimidazole is reacted with (R)-camphorsulfonyl chloride to form a mixture of 1-(R)-camphorsulfonyl-5-(and 6-)methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methylthio]-1H-benzimidazole, oxidized to obtain a diastereomeric excess of 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole over 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(R)-sulfinyl]-1H-benzimidazole, the diastereomers are separated by fractional crystallization and the separated 1-(R)-camphorsulfonyl-(5- and 6-)-methoxy-2-[(3,5-dimethyl-4-methoxy-2-pyridyl)methyl-(S)-sulfinyl]-1H-benzimidazole is deprotected to give esomeprazole.

公开(公告)号：EP2089379A2

公开(公告)日：2009-08-19

申请号：EP06832312.0

申请日：2006-12-07

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura ,  RAJI REDDY, Rapolu ,  MURALIDHARA REDDY, Dasari

IPC分类号： C07D401/12 ,  A61K31/4439

CPC分类号： C07D401/12

摘要： The present invention relates to a novel and stable crystalline polymorph of lansoprazole, process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, lansoprazole crude is dissolved in methanol at 20 - 30 °C followed by stirring and the solution is cooled to 0 - 10 °C. The resulting solution is stirred for 1 hour to 1 hour 30 minutes at 0 - 10 °C, filtered the solid and then dried to give lansoprazole crystalline form III.

公开(公告)号：EP2033947A1

公开(公告)日：2009-03-11

申请号：EP08169272.5

申请日：2007-03-19

申请人： Hetero Drugs Limited

发明人： Reddy, Bandi Parthasaradhi ,  Reddy, Kura Rathnakar ,  Reddy, Rapolu Raji ,  Reddy, Dasari Muralidhara ,  Reddy, Kesireddy Subash Chander

IPC分类号： C07C209/84 ,  C07C211/42

CPC分类号： C07C209/84 ,  C07C2602/10 ,  C07C211/42

摘要： Process for preparing sertraline hydrochloride crystalline form I comprising (a) adding sertraline free base or sertraline mandelate to n-amyl alcohol, (b) adding hydrochloric acid at 25 °C or below, and (c) isolating sertraline hydrochloride crystalline form I.

摘要翻译： （a）将舍曲林游离碱或舍曲林扁桃酸盐加入到正戊醇中，（b）在25℃或更低温度下加入盐酸，和（c）分离舍曲林盐酸盐结晶形式I.

公开(公告)号：EP1789412B1

公开(公告)日：2008-05-07

申请号：EP04770711.2

申请日：2004-09-16

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi, Hetero House ,  RATHNAKAR REDDY, Kura, Hetero Drugs Limited R & D ,  RAJI REDDY, Rapolu, Hetero Drugs Limited R & D ,  MURALIDHARA REDDY, Dasari, Hetero Drugs Ltd R & D ,  RAMAKRISHNA REDDY, Matta, Hetero Drugs Ltd R &D

IPC分类号： C07D405/12

CPC分类号： C07D405/12

摘要： The present invention relates to crystalline alfuzosin base and processes for preparation of the said crystalline solid. Thus, for example, alfuzosin base (HPLC purity: 97%) is added to methanol and heated to reflux to form a clear solution, the solution is cooled to 25° - 30°C and stirred for 12 hours at the same temperature, the resulting solution is cooled to 10°- 15°C and stirred for 2 hours, and the resulting solid is filtered, washed with methanol and dried at 50°- 60°C for 4 hours to give 99.95% pure alfuzosin base.

公开(公告)号：EP1910393A2

公开(公告)日：2008-04-16

申请号：EP05783970.6

申请日：2005-07-05

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, bandi ,  RATHNAKAR REDDY, kura Hetero Drugs Limited (R & D) ,  RAJI REDDY, rapolu Hetero Drugs Limited (R & D) ,  MURALIDHARA REDDY, dasari Hetero Drugs Ltd. (R&D) ,  SUBASH CHANDER REDDY, kesireddy Hetero Drugs Ltd.

IPC分类号： C07H19/173

CPC分类号： C07H19/173

摘要： The present invention relates to novel crystalline alkali metal and alkaline earth metal salts of 2',3'-dideoxy-2',3'-didehydroinosine. The present invention also provides a novel process for preparation of didanosine in high yield and purity using novel intermediates. Thus, for example, 5'-O-acetyl-2',3'-dideoxy-2',3'-didehydroinosine is reacted with monomethyl amine to give 2',3'-dideoxy-2',3'-didehydro inosine, which is then reacted with sodium hydroxide and crystallized to give crystalline 2',3'-dideoxy-2',3'-didehydroinosine sodium salt. 2',3'-Dideoxy-2',3'-didehydroinosine sodium salt is hydrogenated using raney nickel catalyst in aqueous medium and then neutralized with hydrochloric acid to yield didanosine.