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Pub. No.:    WO/2005/066117    International Application No.:    PCT/IB2003/006200
Publication Date: 21.07.2005 International Filing Date: 29.12.2003
C07C 255/41 (2006.01)
Applicants: WOCKHARDT LIMITED [IN/IN]; Wockhardt Towers, Bandra-Kurla Complex, Bandra (East), Mumbai 400 051, Marashtra (IN) (For All Designated States Except US).
JAWEED MUKARRAM, Siddiqui, Mohammed [IN/IN]; (IN).
KHAN, Rashid, Abdul, Rehman [IN/IN]; (IN).
YADAV, Ram, Prasad [IN/IN]; (IN).
SHAIKH, Zakir, Gafoor [IN/IN]; (IN)
Inventors: JAWEED MUKARRAM, Siddiqui, Mohammed; (IN).
KHAN, Rashid, Abdul, Rehman; (IN).
YADAV, Ram, Prasad; (IN).
SHAIKH, Zakir, Gafoor; (IN)
WOCKHARDT LIMITED; c/o SESHA, Ramesh, Wockhardt Towers, Bandra-Kurla Complex, Bandra (East), Mumbai 400 051, Marashtra (IN)
Priority Data:
Abstract: front page image
(EN)The present invention relates to stable crystalline polymorphic forms C and D of (E)-N,N-diethyl-2-cyan-3-(3,4-dihydroxy-5-nitrophenyl)acrylamide (Entacapone) and their preparation processes. (E)-Entacapone Form C is obtained by condensing 3,4-Dihydroxy-5-nitrobenzaldehyde and N,N-Diethylcyanoacetamide in presence of a base followed by addition of acetic acid after the reaction is over and crystallization step. (E)-Entacapone Form D is prepared from Entacapone Form C, Crystallographically pure (E)-Entacapone Form A or Crystallographically essentially pure From A. Polymorphic forms C and D of (E)-Entacapone are characterized by specific Infra Red (IR) and X-ray powder diffraction peak values.
(FR)L'invention concerne les polymorphes cristallins stables C et D de (E)-N,N-diéthyl-2-cyan-3-(3,4-dihydroxy-5-nitrophényl)acrylamide (Entacapone) et leur préparation. (E)-Entacapone de forme C est obtenue par condensation de 3,4-dihydroxy-5-nitrobenzaldehyde et N,N-diéthylcyanoacetamide en présence d'une base suivi par l'addition de l'acide acétique après la réaction et une cristallisation subséquente. (E)-Entacapone de forme D est obtenue à partir de l'entacapone de forme C, (E)-entacapone de forme A pur ou sensiblement pur d'un point de vue cristallographique. Les polymorphes C et D de (E)-entacapone sont caractérisées par valeurs crêtes d'infra rouge (IR) et diffraction des rayons X sur poudre.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, 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, HU, IE, IT, LU, MC, NL, 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)