公开(公告)号：EP2295431A3

公开(公告)日：2011-08-03

申请号：EP09174231.2

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： Substantially pure eprosartan free base and a process for the preparation thereof, which comprises suspending eprosartan acetate in water, adjusting the pH of the suspension to about 6.7 to 7.5 with a base, and collecting the precipitated substantially pure eprosartan base.

公开(公告)号：EP2213647A1

公开(公告)日：2010-08-04

申请号：EP10154348.6

申请日：2007-06-26

申请人： Hetero Drugs Limited

发明人： Parthasaradhi Reddy, Bandi ,  Rathnakar Reddy, Kura ,  Raji Reddy, Rapolu ,  Muralidhara Reddy, Dasari ,  Vsv Prasad, Valivarthi

IPC分类号： C07C46/10 ,  C07C50/32

CPC分类号： C07C50/32 ,  C07B2200/07 ,  C07B2200/13 ,  C07C46/10 ,  Y10T428/2982

摘要： The present invention relates to a novel and stable crystalline form of atovaquone (atovaquone Form B), to processes for its preparation and to pharmaceutical compositions comprising it.

摘要翻译： 本发明涉及新型且稳定的阿托瓦醌结晶形式（阿托瓦醌形式B），其制备方法以及包含其的药物组合物。

公开(公告)号：EP2204359A1

公开(公告)日：2010-07-07

申请号：EP10156919.2

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： A process for preparation of the acetyl compound of formula III:

which comprises acetylating the amino compound of formula II:

with acetic anhydride in an organic solvent in the presence of an organic or inorganic base in the absence of water to give the acetyl compound of formula III.

摘要翻译： 制备式III的乙酰基化合物的方法：其包括在有机或无机碱的存在下，在不存在水的情况下，将乙酸酐在有机溶剂中乙酸酐乙酰化，得到式 III。

公开(公告)号：EP2160376A2

公开(公告)日：2010-03-10

申请号：EP07805631.4

申请日：2007-06-26

申请人： Hetero Drugs Limited

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

IPC分类号： C07C50/14

CPC分类号： C07C50/32 ,  C07B2200/07 ,  C07B2200/13 ,  C07C46/10 ,  Y10T428/2982

摘要： The present invention relates to two novel and stable crystalline forms of atovaquone, to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also provides crystalline particles of atovaquone having a specific surface area of from about 0.7 m2/g to about 4 m2/g, methods for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles. The present invention further provides an improved and commercially viable process for preparation of atovaquone substantially free of undesired isomeric impurity, namely cis-2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone.

摘要翻译： 本发明涉及两种新型且稳定的阿托伐醌结晶形式，其制备方法和包含它们的药物组合物。 本发明还提供比表面积为约0.7m 2 / g-约4m 2 / g的阿托瓦醌晶体颗粒，用于制造所述晶体颗粒的方法和包含所述晶体颗粒的药物组合物。 本发明进一步提供了制备基本上不含不希望的异构体杂质即顺式-2- [4-（4-氯苯基）环己基] -3-羟基-1,4-萘醌的阿托瓦醌的改进的和商业上可行的方法。

公开(公告)号：EP2159225A1

公开(公告)日：2010-03-03

申请号：EP09173144.8

申请日：2005-06-15

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： C07D471/04 ,  A61K31/4375 ,  A61P31/00

CPC分类号： C07D471/04

摘要： Gemifloxacin lactate and gemiflxacin formate, processes for the preparation thereof and pharmaceutical compositions containing gemifloxacin lactate or gemiflxacin formate.

摘要翻译： 乳酸氨米沙星和甲酸吉非那星，其制备方法和含有吉非沙星乳酸盐或甲酸吉西他滨的药物组合物。

公开(公告)号：EP1863822B1

公开(公告)日：2009-10-14

申请号：EP05732994.8

申请日：2005-03-29

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RAJI, Reddy, Rapolu, Hetero Drugs Ltd. (R & D) ,  RATHNAKAR, Reddy Kura, Hetero Drugs Ltd. (R & D) ,  MURALI, Nagabelli, Hetero Drugs Ltd. (R & D) ,  MURALIDHARA, Reddy, Dasari

IPC分类号： C07D501/06

CPC分类号： C07D501/00

摘要： There is provided an improved process for preparing cefixime. Thus, for example, 7-amino-3-vinyl-3-cephem-4-carboxylic acid is reacted with 2-mercapto-1,3-benzothiazolyl-(Z)-2-(2-aminothiazol-4-yl)-2-(methoxycarbonyl)-methoxyimino acetate in tetrahydrofuran and water at 4°C in the presence of triethylamine. The reaction mass is extracted with ethyl acetate. 7-[2-(2-Amino-4-thiazolyl)-2-(methoxycarbonylmethoxyimino)acetamido]-3-vinyl-3-cephem-4-carboxylic acid triethylamine salt present in the aqueous layer is hydrolyzed with sodium hydroxide in less than 30 minutes and aqueous hydrochloric acid is added immediately to adjust the pH to 4.8 to 5.2. Then, aqueous hydrochloric acid is added at 35°C to adjust the pH 2.5 and cooled to crystallize cefixime trihydrate in high purity.

公开(公告)号：EP2057151A2

公开(公告)日：2009-05-13

申请号：EP06796191.2

申请日：2006-08-28

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： C07D413/06

CPC分类号： C07D413/06

摘要： The present invention relates to a process for obtaining pure aprepitant substantially free of undesired diastereomeric isomer, namely 5-[2(S)-[I (RS)- [3,5-bis(trifluoromethyl)-phenyl)ethoxy]-3-(S)-(4-fluorophenyl)-morpholin-4-yl- methyl]-3,4-dihydro-2H-1,2,4-triazol-3-one. The present invention further provides an improved process for preparation aprepitant crystalline form II. The present invention also relates to novel amorphous form of aprepitant, process for its preparation and to a pharmaceutical composition comprising it. The present invention further relates to aprepitant having mean particle size of less than about 11.5 microns, process for its preparation and to a pharmaceutical composition comprising it. Thus, for example, aprepitant having the content of diastereomeric impurity of 1.1 % is dissolved in ethyl acetate at 700C, the solution is concentrated to half the initial volume by distilling off ethyl acetate, and the resulting solid is collected at 0 - 50C to give pure aprepitant substantially free of diastereomeric impurity.

公开(公告)号：EP1973895A1

公开(公告)日：2008-10-01

申请号：EP06711356.3

申请日：2006-01-18

申请人： Hetero Drugs Limited

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

IPC分类号： C07D311/58

CPC分类号： C07D311/58

摘要： The present invention relates to a simple and commercially viable process for separation of desired isomers of nebivolol intermediates from a mixture containing undesired isomers of nebivolol intermediates. Thus, (+)-[2R*[1S*,5S*(S*)]]+[2R*[1S*,5R*(R*)]]-α,α'- [phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H-1-benzopyran-2-methanol] is dissolved in diisopropyl ether at reflux temperature and cooled to below 30°C to obtain the desired(+)-[2R*[1S*,5S*(S*)]]-alfa,alfa'-[phenylmethyliminobis(methylene)]bis[6-fluoro-3,4-dihydro-2H- 1-benzopyran-2-methanol].

公开(公告)号：EP1951654A1

公开(公告)日：2008-08-06

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.

摘要翻译： 制备式III的乙酰基化合物的方法：其包括在有机或无机碱的存在下，在不存在水的情况下，将乙酸酐在有机溶剂中乙酸酐乙酰化，得到式 III。

公开(公告)号：EP1891009A1

公开(公告)日：2008-02-27

申请号：EP05760546.1

申请日：2005-06-15

申请人： Hetero Drugs Limited

发明人： PARTHASARADHI REDDY, Bandi ,  RATHNAKAR REDDY, Kura Hetero Drugs Ltd.(R & D) ,  RAJI REDDY, Rapolu Hetero Drugs Ltd.(R & D) ,  MURALIDHARA REDDY, Dasari Hetero Drugs Ltd.(R & D) ,  SATISH KUMAR, Dandamudi, Hetero Drugs Limited (R & D)

IPC分类号： C07D211/02 ,  C07D211/90

CPC分类号： C07D211/90 ,  C07D211/82

摘要： The invention provides a novel process for the preparation of lercanidipine or a pharmaceutical acceptable salt using novel intermediates. Thus, 2,N-dimethyl-N-(3,3-diphenylpropyl)-1-amino-2-propanol is reacted with trimethylsilyl chloride in presence of triethyl amine in methylene chloride to give 2,N-dimethyl-2-(trimethylsilyloxy)-N-(3,3-diphenylpropyl)-1-propanamine, which is then reacted with 2,6-dimethyl-5-methoxycarbonyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3-carbonyl chloride for 2 hours and crystallized to obtain lercanidipine hydrochloride.