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Machine translation
1. (WO2007089193) A PROCESS FOR PREPARING 2-HYDROXY-3- [5- (MORPHOLIN-4-YLMETHYL)PYRIDIN-2-YL] LH-INDOLE-5-CARBONITRILE AS A FREE BASE OR SALTS THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2007/089193    International Application No.:    PCT/SE2007/000088
Publication Date: 09.08.2007 International Filing Date: 31.01.2007
IPC:
C07D 401/04 (2006.01), A61K 31/4439 (2006.01), A61P 25/28 (2006.01)
Applicants: ASTRAZENECA AB [SE/SE]; S-151 85 Södertälje (SE) (For All Designated States Except US).
ERBECK, Silke [DE/CH]; (CH) (For US Only).
HEDBERG, Martin [SE/SE]; (SE) (For US Only).
NUSSBAUMER, Thomas [DE/CH]; (CH) (For US Only).
RYBERG, Per [SE/SE]; (SE) (For US Only).
ZISTLER, Andrea [DE/CH]; (CH) (For US Only)
Inventors: ERBECK, Silke; (CH).
HEDBERG, Martin; (SE).
NUSSBAUMER, Thomas; (CH).
RYBERG, Per; (SE).
ZISTLER, Andrea; (CH)
Agent: ASTRAZENECA AB; Global Intellectual Property, S-151 85 Södertälje (SE)
Priority Data:
60/764,542 02.02.2006 US
Title (EN) A PROCESS FOR PREPARING 2-HYDROXY-3- [5- (MORPHOLIN-4-YLMETHYL)PYRIDIN-2-YL] LH-INDOLE-5-CARBONITRILE AS A FREE BASE OR SALTS THEREOF
(FR) PROCÉDÉ DE SYNTHÈSE DU 2-HYDROXY-3-[5-(MORPHOLIN-4-YLMÉTHYL)PYRIDIN-2-YL]1H-INDOLE-5-CARBONITRILE SOUS FORME DE BASE LIBRE OU DE SES SELS
Abstract: front page image
(EN)The present invention relates to a new process for the manufacture of the compound 2-hydroxy-3-[5-(mo&phgr;holin-4-ylmethyl)pyridin-2-yl]lH'-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the 2-hydroxy-3-[5- (morpholm-4-ylmethyl)pyridin-2-yl]lH-indole-5-carbonitrile citrate, to the use of said compounds for the manufacturing of a medicament for the treatment of cognitive disorders, Alzheimer disease, dementias, chronic and acute neurodegenerative diseases, bipolar disorders, schizophrenia, diabetes, hair loss etc. and to new intermediates as well as a robust condition for catalytic cyanation for the preparation of 2-hydroxy-3-[5- (mo&phgr;holin-4-yhnethyl)pyridin-2-yl]lH-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, and to a new intermediate prepared in said process suitable for large scale manufacturing of said compounds.The invention also relates to a new use in cyanation reaction of palladium catalysts.
(FR)La présente invention concerne un nouveau procédé de fabrication du 2-hydroxy-3-[5-(morpholin-4-ylméthyl)pyridin-2-yl]1H-indole-5-carbonitrile sous forme de base libre ou de ses sels de qualité pharmaceutique, en particulier le citrate de 2-hydroxy-3-[5-(morpholin-4-ylméthyl)pyridin-2-yl]1H-indole-5-carbonitrile, l'emploi desdits composés dans la fabrication d'un médicament pour le traitement des troubles cognitifs, de la maladie d'Alzheimer, des démences, des maladies neurodégénératives chroniques et aiguës, des troubles bipolaires, de la schizophrénie, du diabète, de l'alopécie, entre autres. La présente invention concerne également de nouveaux intermédiaires ainsi qu'un mode opératoire robuste de cyanation catalytique pour la synthèse du 2-hydroxy-3-[5-(morpholin-4-ylméthyl)pyridin-2-yl]1H-indole-5-carbonitrile sous forme de base libre et de ses sels de qualité pharmaceutique, de même qu'un nouvel intermédiaire synthétisé lors dudit procédé et adapté à la fabrication à grande échelle desdits composés. La présente invention concerne également une nouvelle application à la réaction de cyanation des catalyseurs au palladium.
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, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MD, 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, SV, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, 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, LV, 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)