US 10,377,712 B2 · Process for preparation of apremilast and novel polymorphs thereof

Process for preparation of apremilast and novel polymorphs thereof

AssigneeLupin Limited

InventorsPalash 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

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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.

Claims12

Dependent claims

A crystalline Form M of apremilast having:

i) a Powder X-Ray diffraction (PXRD) pattern substantially in accordance with FIG. 12;
ii) a Powder X-Ray diffraction (PXRD) pattern having peaks at 5.3, 8.4, 9.8, 13.98, 14.85, 16.64, 19.59, 21.46, 27.23±0.2° 2theta value;
iii) a Thermogravimetric analysis (TGA) substantially in accordance with FIG. 13, or
iv) a differential scanning calorimetric (DSC) thermogram substantially in accordance with FIG. 14.

1 more element

Dependencies are inferred from the claim text.

Facts

Application

15/577,102Filed 26 May 2016

Priority

IN 2046/MUM/201526 May 2015

Published

US 2018/0230097 A116 Aug 2018

Granted

13 Aug 2019

Term ends

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Classification10 codes

C07D 209/48
Iso-indoles; Hydrogenated iso-indoles: with oxygen atoms in positions 1 and 3, e.g. phthalimide
A61P 17/06
Drugs for dermatological disorders: antipsoriatics
A61P 19/02
Drugs for skeletal disorders: for joint disorders, e.g. arthritis, arthrosis
A61P 43/00
Drugs for specific purposes, not provided for in groups a61p1/00-a61p41/00