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1. (WO2010073254) PROCESS FOR PREPARING EFAVIRENZ POLYMORPH
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/073254 International Application No.: PCT/IN2008/000855
Publication Date: 01.07.2010 International Filing Date: 22.12.2008
IPC:
C07D 265/18 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
265
Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
04
1,3-Oxazines; Hydrogenated 1,3-oxazines
12
condensed with carbocyclic rings or ring systems
14
condensed with one six-membered ring
18
with hetero atoms directly attached in position 2
Applicants:
HETERO RESEARCH FOUNDATION [IN/IN]; Plot N° B-80 & 81 A.P.I.E, Balanagar Hyderabad, Andhrapradesh Hyderabad 500 018, IN (AllExceptUS)
PARTHASARADHI REDDY, bandi [IN/IN]; IN (UsOnly)
RATHNAKAR REDDY, Kura [IN/IN]; IN (UsOnly)
RAJI REDDY, Rapolu [IN/IN]; IN (UsOnly)
MURALIDHARA REDDY, Dasari [IN/IN]; IN (UsOnly)
SUBASH CHANDER REDDY, Kesireddy [IN/IN]; IN (UsOnly)
Inventors:
PARTHASARADHI REDDY, bandi; IN
RATHNAKAR REDDY, Kura; IN
RAJI REDDY, Rapolu; IN
MURALIDHARA REDDY, Dasari; IN
SUBASH CHANDER REDDY, Kesireddy; IN
Priority Data:
Title (EN) PROCESS FOR PREPARING EFAVIRENZ POLYMORPH
(FR) PROCÉDÉ POUR LA PRÉPARATION D'UN POLYMORPHE DE L'ÉFAVIRENZ
Abstract:
(EN) The present invention relates to a process for the preparation of crystalline non-hygroscopic form H1 of efavirenz, and pharmaceutical compositions containing it. In accordance with the present invention efavirenz was dissolved in acetone at 25 °C - 30°C, the solution was slowly added to water at O °C - 5 °C, the separated solid was filtered, washed with mixture of acetone and water and dried at 25 °C - 35 °C under below 65 % relative humidity for 18 hours to give crystalline non-hygroscopic efavirenz form H1.
(FR) La présente invention concerne un procédé de préparation de la forme cristalline non hygroscopique H1 de l'éfavirenz, et des compositions pharmaceutiques la contenant. Le procédé consiste à dissoudre de l'éfavirenz dans de l'acétone à 25-30 °C, ajouter lentement cette solution à de l'eau à 0-5 °C, filtrer les matières solides séparées, les laver avec un mélange d'acétone et d'eau et les sécher à 25-35 °C dans une humidité relative inférieure à 65 % pendant 18 heures pour obtenir la forme cristalline non hygroscopique H1 de l'éfavirenz.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MT, NL, NO, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP2367804US20120232069ES2445090