公开(公告)号：US09580440B2

公开(公告)日：2017-02-28

申请号：US14047243

申请日：2013-10-07

Applicant: Hetero Research Foundation

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Rapolu Raji Reddy ,  Kesireddy Subash Chander Reddy ,  Bandi Vamsi Krishna

IPC: A01N43/08 ,  A61K31/34 ,  C07D493/00 ,  C07D493/04 ,  A61K9/20

CPC classification number: C07D493/04 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/34

Abstract: The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.

Abstract translation: 本发明提供了地瑞那韦的新型溶剂化形式及其制备方法。 本发明还提供了制备地瑞那韦非晶形式的新方法和包含它的药物组合物。 因此，例如，将地瑞那韦2-甲基-2-丁醇溶剂合物溶解在二氯甲烷中，在45℃下真空蒸馏，得到残留物，将环己烷加入残留物中，在20〜25℃下搅拌30小时 将分离出的固体过滤，用环己烷洗涤，在50℃下真空干燥12小时，得到地瑞那韦非晶形式。

公开(公告)号：US08669265B2

公开(公告)日：2014-03-11

申请号：US13900647

申请日：2013-05-23

Applicant: Hetero Research Foundation

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Thungathurthy Srinivas Rao

IPC: A61K31/517

CPC classification number: C07D239/94

Abstract: 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 (D50) ranging from about 4 μm to 15 μm and 90 volume-% of the particles (D90) 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.

Abstract translation: 本发明提供了一种新颖稳定的埃洛替尼游离碱的水合形式及其制备方法。 本发明还提供了一种制备基本上不含多晶型物B的盐酸埃罗替尼结晶多晶型物的方法。本发明还涉及平均粒径（D50）为约4μm至15μm和90体积％的盐酸埃罗替尼结晶颗粒， 约14μm至30μm的颗粒（D90）的百分比，制造所述结晶颗粒的方法，以及包含所述结晶颗粒的药物组合物。

公开(公告)号：US09115118B2

公开(公告)日：2015-08-25

申请号：US14264450

申请日：2014-04-29

Applicant: HETERO RESEARCH FOUNDATION

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Bandi Vamsi Krishna ,  Voggu Ramesh Reddy

IPC: C07D401/14 ,  C07D401/12

CPC classification number: C07D401/12 ,  C07D401/14

Abstract: The present invention relates to process for the resolution of omeprazole. The present invention further provides a novel compound of enantiomers of omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a solid of (R)- or (S)-omeprazole cyclic amine salt and a process for preparing it. The present invention also provides a process for the preparation of esomeprazole magnesium dehydrate substantially free of its trihydrate form. The present invention also provides a process for the preparation of recovery of chiral BINOL.

Abstract translation: 本发明涉及奥美拉唑的分辨方法。 本发明还提供了奥美拉唑环胺盐的新型对映体化合物及其制备方法。 本发明还提供（R） - 或（S） - 奥美拉唑环胺盐的固体及其制备方法。 本发明还提供一种制备基本上不含其三水合物形式的艾司替唑无水脱水制剂的方法。 本发明还提供了制备手性BINOL回收的方法。

公开(公告)号：US20140200356A1

公开(公告)日：2014-07-17

申请号：US14047243

申请日：2013-10-07

Applicant: Hetero Research Foundation

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Rapolu Raji Reddy ,  Kesireddy Subash Chander Reddy ,  Bandi Vamsi Krishna

IPC: C07D493/04

CPC classification number: C07D493/04 ,  A61K9/2027 ,  A61K9/2054 ,  A61K31/34

Abstract: The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.

Abstract translation: 本发明提供了地瑞那韦的新型溶剂化形式及其制备方法。 本发明还提供了制备地瑞那韦非晶形式的新方法和包含它的药物组合物。 因此，例如，将地瑞那韦2-甲基-2-丁醇溶剂合物溶解在二氯甲烷中，在45℃下真空蒸馏，得到残留物，将环己烷加入残留物中，在20〜25℃下搅拌30小时 将分离出的固体过滤，用环己烷洗涤，在50℃下真空干燥12小时，得到地瑞那韦非晶形式。

公开(公告)号：US09175005B2

公开(公告)日：2015-11-03

申请号：US14325869

申请日：2014-07-08

Applicant: HETERO RESEARCH FOUNDATION

Inventor： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Rapolu Raji Reddy ,  Bandi Vamsi Krishna ,  Kesireddy Subash Chander Reddy

IPC: C07D493/04 ,  C07D307/93

CPC classification number: C07D493/04 ,  C07D307/93

Abstract: The present invention provides novel crystalline hydrochloride salt of darunavir, process for its preparation and to pharmaceutical composition comprising it. The present invention also provides novel process for preparation of darunavir amorphous form and pharmaceutical composition comprising it.

Abstract translation: 本发明提供了地瑞那韦的新型结晶盐酸盐，其制备方法和包含其的药物组合物。 本发明还提供了地瑞那韦无定形形式的新方法和包含它的药物组合物。