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1. (WO2005068425) NEW CRYSTALLINE FORM OF PERINDOPRIL
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2005/068425    International Application No.:    PCT/EP2005/000283
Publication Date: 28.07.2005 International Filing Date: 13.01.2005
Chapter 2 Demand Filed:    08.11.2005    
IPC:
C07D 209/42 (2006.01)
Applicants: LEK PHARMACEUTICALS D.D. [SI/SI]; Verovskova 57, 1526 Ljubljana (SI) (For All Designated States Except US).
RUCMAN, Rudolf [SI/SI]; (SI) (For US Only)
Inventors: RUCMAN, Rudolf; (SI)
Agent: GRUBB, Philip; Novartis AG, Corporate Intellectual Property, CH-4002 Basel (CH).
THOMSEN, Peter, R.; Novartis AG, Corporate Intellectual Property, CH-4002 Basel (CH)
Priority Data:
P-200400012 14.01.2004 SI
Title (EN) NEW CRYSTALLINE FORM OF PERINDOPRIL
(FR) NOUVELLE FORME CRISTALLINE DE PERINDOPRIL
Abstract: front page image
(EN)The present invention relates to the process for a preparation of ACE inhibitor perindopril starting from the stereospecific amino acid N-[(S)-carbethoxy-1-butyl]­(S)-alanine, which is protected by trimethylsilyl group and converted to reactive acid chloride using thionylchloride or its complex with 1-H-benzotriazole (1:1), which reacts with (2S, 3aS, 7aS)-octahydroindole-2-carboxylic acid with a protected carboxyl group. This invention relates also to a new crystalline form of perindopril and to a new amorphous form of perindopril.
(FR)La présente invention se rapporte à un procédé de préparation de l'inhibiteur d'ACE perindopril, à partir de l'acide aminé stéréospécifique N-[(S)-carbéthoxy-1-butyl]-(S)-alanine, lequel est protégé par un groupe triméthylsilyle est transformé en chlorure acide réactif à l'aide de thionylchlorure ou de son complexe avec le 1-H-benzotriazole (1:1), qui réagit avec l'acide (2S, 3aS, 7aS)-octahydroindole-2-carboxylique présentant un groupe carboxyle protégé. La présente invention se rapporte également à une nouvelle forme cristalline du perindopril et à une nouvelle forme amorphe du perindopril.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, 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, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SM, 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, 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, HU, IE, IS, IT, LT, LU, MC, NL, 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)