公开(公告)号：US20220081385A1

公开(公告)日：2022-03-17

申请号：US17419939

申请日：2019-12-27

Applicant: Lupin Limited

Inventor： Navnath Ambadas Kadam ,  Rohidas Shivaji Sulake ,  Rajinder Singh Siyan ,  Nandu Baban Bhise ,  Girij Pal Singh ,  Rajesh Harishankar Vyas

IPC: C07C67/313

Abstract: The present invention relates to novel pharmaceutically acceptable salts of Bempedoic acid, novel intermediates of Bempedoic acid, novel crystalline form of Bempedoic acid and novel processes for the preparation of Bempedoic acid or its intermediates thereof.

公开(公告)号：US10479776B2

公开(公告)日：2019-11-19

申请号：US15573082

申请日：2016-05-10

Applicant: LUPIN LIMITED

Inventor： Sachin Arun Sasane ,  Devendrakumar Paramsukh Varma ,  Rajesh Harishankar Vyas ,  Nandu Baban Bhise ,  Girij Pal Singh ,  Krishnat Hanmant Kumbhar

IPC: C07D401/06

Abstract: The present invention provides an improved process for the preparation of Efinaconazole in higher yield by the ring-opening addition reaction of epoxytriazole with 4-methylenepiperidine or its acid addition salt under mild conditions without using a large excess of 4-methylenepiperidine in the presence of an alkali or an alkaline earth metal halide.

公开(公告)号：US10377712B2

公开(公告)日：2019-08-13

申请号：US15577102

申请日：2016-05-26

Applicant: LUPIN LIMITED

Inventor： Palash Sanphui ,  Ananda Pundlik Sapdhare ,  Arunkumar Digambar Patil ,  Hemraj Mahadeorao Lande ,  Gurvinder Pal Singh ,  Puma Chandra Ray ,  Nandu Baban Bhise ,  Girij Pal Singh ,  Mithun Dasharath Surwase ,  Shantanu Gokuldas Varade ,  Govind Dnyanoba Ausekar ,  Radhakrishna Bhikaji Shivdavkar

IPC: C07D209/48 ,  C07C315/04

Abstract: The present invention provides an improved process for preparation of an intermediate of apremilast. The present invention also provides an improved process for preparation of apremilast. This invention also provides novel polymorphs of apremilast. The present invention also provides pharmaceutical compositions of novel polymorphs of apremilast. This invention also provides a process for preparation of novel polymorphs of apremilast, which are cost-effective, robust, and viable at plant scale.

公开(公告)号：US20180099991A1

公开(公告)日：2018-04-12

申请号：US15727856

申请日：2017-10-09

Applicant: Lupin Limited

Inventor： Palash Sanphui ,  Radhakrishna Bhikaji Shivdavkar ,  Rajesh Vyas ,  Nandu Baban Bhise ,  Girij Pal Singh

IPC: C07J9/00 ,  C07C279/14 ,  C07C229/26 ,  C07C215/10 ,  C07C277/00 ,  C07C227/16 ,  C07C213/08

CPC classification number: C07J9/005 ,  C07B2200/13 ,  C07C213/08 ,  C07C215/10 ,  C07C227/16 ,  C07C229/26 ,  C07C277/00 ,  C07C279/14

Abstract: The invention relates to salts of Obeticholic Acid, their amorphous and crystalline polymorphic form and processes for preparation thereof.

公开(公告)号：US20140357871A1

公开(公告)日：2014-12-04

申请号：US14369811

申请日：2013-01-09

Applicant: LUPIN LIMITED

Inventor： Rajinder Singh Siyan ,  Yogesh Subhas Aher ,  Nandu Baban Bhise ,  Girij Pal Singh ,  Sunilkumar Vinubhai Gohel

IPC: C07D249/04

CPC classification number: C07D249/04

Abstract: The present invention relates to a novel process for preparation of rufinamide (I) comprising: reacting 2,6-difluorobenzyl azide (II) and propiolic acid (III) in a mixture of alcohol and water to produce 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid (IV), esterifying the acid (IV) to ester (V) and treating ester (V) with ammonia. The invention further relates to process for purification of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid (IV), by crystallization from a mixture of alcohol and water. The present invention also provides process for purification of rufinamide (I) by crystallization from mixture of polar aprotic solvent with water or alcohol.

Abstract translation: 本发明涉及一种制备呋喃酰胺（I）的新方法，其包括：将2,6-二氟苄基叠氮化物（II）和丙炔酸（III）在醇和水的混合物中反应，得到1-（2,6-二氟苄基 ）-1H-1,2,3-三唑-4-甲酸（IV），将酸（IV）酯化为酯（V）并用氨处理酯（V）。 本发明还涉及通过从醇和水的混合物中结晶来纯化1-（2,6-二氟苄基）-1H-1,2,3-三唑-4-羧酸（Ⅳ）的方法。 本发明还提供了通过极性非质子传递溶剂与水或醇的混合物的结晶来纯化rufinamide（I）的方法。

公开(公告)号：US20210300917A1

公开(公告)日：2021-09-30

申请号：US16621036

申请日：2018-06-09

Applicant: Lupin Limited

Inventor： Lalitkumar Dilipsing Rajput ,  Vasant Chhabu Vyavhare ,  Radhakrishna Bhikaji Shivdavkar ,  Yuvraj Dadasaheb Sudrik ,  Rangan Mitra ,  Sangram Gokhale ,  Sunilkumar Vinubhai Gohel ,  Rajinder Singh Siyan ,  Nandu Baban Bhise ,  Girij Pal Singh

IPC: C07D471/04

Abstract: Various crystalline and amorphous solid state forms of an apoptosis-inducing agent and preparations thereof are disclosed. Also discloses the use of crystalline forms for the preparation of amorphous form of apoptosis-inducing agent. Further discloses a process for preparation of the apoptosis-inducing agent. (Formula I)

公开(公告)号：US10251850B2

公开(公告)日：2019-04-09

申请号：US15868284

申请日：2018-01-11

Applicant: LUPIN LIMITED

Inventor： Pankaj Ramchandra Chaudhari ,  Sukhdeo Sampat Gunjal ,  Raju Muktaji Walunj ,  Anurag Trivedi ,  Rajinder Singh Siyan ,  Nandu Baban Bhise ,  Girij Pal Singh

IPC: C07C59/245 ,  A61K31/145 ,  A61K31/095 ,  C07C323/25 ,  C07C319/12 ,  G01N30/88 ,  G01N30/02 ,  G01N23/20

Abstract: The present invention provides process for preparation of cysteamine bitartrate comprising reacting cysteamine or its salt with tartaric acid. The present invention further provides crystalline form L1 of cysteamine bitartrate having characteristic diffraction peaks at 10.36, 14.54, 17.23, 18.03, 19.24, 20.76, 21.20, 22.02, 23.37, 23.64, 27.71, 28.28, 29.26, 31.33, 32.84, 33.83, 35.51, 36.74±0.2 degree two theta in an X-ray diffraction pattern and process for preparation thereof. The present invention provides crystalline form L2 of cysteamine bitartrate having characteristic diffraction peaks at 7.4, 10.3, 11.0, 11.4, 14.4, 14.9, 18.6, 19.4, 20.1, 20.8, 21.9, 22.3, 22.5, 23.5±0.2 degree two theta in an X-ray diffraction pattern and process for preparation thereof.

公开(公告)号：US20180222836A1

公开(公告)日：2018-08-09

申请号：US15749905

申请日：2016-08-04

Applicant: Lupin Limited

Inventor： Anurag Anil Smart ,  Yogesh Subhash Aher ,  Sunilkumar Vinubhai Gohel ,  Rajinder Singh Siyan ,  Nandu Baban Bhise ,  Girij Pal Singh

IPC: C07C51/41 ,  C07C59/265 ,  A61P3/12 ,  A61P7/08 ,  A61P13/12

CPC classification number: C07C51/418 ,  A61K9/143 ,  A61K33/26 ,  A61P3/12 ,  A61P7/08 ,  A61P13/12 ,  C07C51/412 ,  C07C51/42 ,  C07C51/43 ,  C07C59/265

Abstract: A one-pot process is disclosed for the preparation of pharmaceutical grade ferric citrate that includes preparing a ferric hydroxide slurry followed by treatment with a citrate ion source to yield pharmaceutical grade ferric citrate.

公开(公告)号：US20180155270A1

公开(公告)日：2018-06-07

申请号：US15577365

申请日：2016-05-27

Applicant: Lupin Limited

Inventor： Vishal Gautam Gaikwad ,  Sadanand Nilkanth Patil ,  Rajinder Singh Siyan ,  Nandu Baban Bhise ,  Girij Pal Singh

IPC: C07C209/08 ,  C07C211/27 ,  C07C211/30 ,  C07C29/147 ,  C07C31/38 ,  C07C17/16 ,  C07C22/08 ,  C07C5/03

CPC classification number: C07C209/08 ,  C07C5/03 ,  C07C17/16 ,  C07C22/08 ,  C07C29/147 ,  C07C31/38 ,  C07C209/70 ,  C07C211/27 ,  C07C211/30 ,  C07C2523/42 ,  C07C2523/44 ,  C07C2525/02

Abstract: The present invention provides one pot process for preparation of highly pure unsaturated cinacalcet hydrochloride (II) comprising: i) converting 3-(trifluromethyl) cinnamic acid (III) into 3-(3-(trifluoromethyl)phenyl)prop-2-en-1-ol (IV), ii) converting 3-(3-(trifluoromethyl)phenyl)prop-2-en-1-ol (IV) to compound (V), wherein R is Cl, Br, I, tosylate and mesylate, Formula (V) iii) reacting compound (V) with (R)-1-(1-Naphthyl) ethylamine (VI) in presence of base followed by treatment with hydrochloric acid. The present invention further provides conversion of unsaturated cinacalcet hydrochloride (II) to cinacalcet hydrochloride (I).