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1. WO2016135755 - AMORPHOUS APREMILAST, PREMIXES THEREOF, AND NOVEL CRYSTALLINE FORMS OF APREMILAST

Publication Number WO/2016/135755
Publication Date 01.09.2016
International Application No. PCT/IN2016/050070
International Filing Date 26.02.2016
IPC
C07D 209/48 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
44Iso-indoles; Hydrogenated iso-indoles
48with oxygen atoms in positions 1 and 3, e.g. phthalimide
A61K 31/573 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
56Compounds containing cyclopentahydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
57substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane, progesterone
573substituted in position 21, e.g. cortisone, dexamethasone, prednisone
CPC
A61K 31/4035
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
40having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
403condensed with carbocyclic rings, e.g. carbazole
4035Isoindoles, e.g. phthalimide
C07D 209/48
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02condensed with one carbocyclic ring
44Iso-indoles; Hydrogenated iso-indoles
48with oxygen atoms in positions 1 and 3, e.g. phthalimide
Applicants
  • MYLAN LABORATORIES LIMITED [IN]/[IN]
Inventors
  • JETTI, Ramakoteswara Rao
  • BHAGAVATULA, Neelima
  • DORASALA, Sivaprasad
  • BOMMAREDDY, Aggi Ramireddy
  • ACHANTA, Surya Nageswara Rao
Agents
  • HASAN, Afzal
  • HASAN, Vatsala Singh
Priority Data
1953/CHE/201515.04.2015IN
2789/CHE/201503.06.2015IN
950/CHE/201527.02.2015IN
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) AMORPHOUS APREMILAST, PREMIXES THEREOF, AND NOVEL CRYSTALLINE FORMS OF APREMILAST
(FR) APRÉMILAST AMORPHE, PRÉ-MÉLANGES CORRESPONDANT ET NOUVELLES FORMES CRISTALLINES D'APRÉMILAST
Abstract
(EN)
A process for the preparation of amorphous apremilast. A premix of amorphous apremilast with pharmaceutically acceptable excipients and process for the preparation thereof are also disclosed. Processes for the preparation of anisole and methyl ethyl ketone solvates of apremilast are disclosed, as are powder X-ray diffraction patterns characterizing those forms of apremilast.
(FR)
L'invention concerne un procédé de préparation d'aprémilast amorphe. L'invention concerne également un pré-mélange d'aprémilast amorphe des avec excipients pharmaceutiquement acceptables ainsi qu'un procédé pour sa préparation. L'invention se rapporte en outre à des procédés de préparation de solvates d'anisole et de méthyléthylcétone, ainsi qu'à des diagrammes de diffraction de rayons X sur poudres caractérisant ces formes d'aprémilast.
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