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1. WO2007084697 - PROCESS FOR PREPARING A CRYSTALLINE FORM OF TEGASEROD MALEATE

Publication Number WO/2007/084697
Publication Date 26.07.2007
International Application No. PCT/US2007/001492
International Filing Date 18.01.2007
IPC
C07D 209/14 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
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
CPC
A61P 1/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
C07D 209/14
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
04Indoles; Hydrogenated indoles
10with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
14Radicals substituted by nitrogen atoms, not forming part of a nitro radical
Applicants
  • TEVA PHARMACEUTICAL INDUSTRIES LTD. [IL]/[IL] (AE, AG, AL, AM, AT, AU, AZ, BA, BE, BF, BG, BJ, BR, BW, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, GR, GT, GW, HN, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LV, LY, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MY, MZ, NA, NE, NG, NI, NL, NO, NZ, OM, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SI, SK, SL, SM, SN, SV, SY, SZ, TD, TG, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VC, VN, ZA, ZM, ZW)
  • TEVA PHARMACEUTICALS USA, INC. [US]/[US] (BB)
  • FRENKEL, Gustavo [IL]/[IL] (UsOnly)
  • INI, Santiago [IL]/[IL] (UsOnly)
Inventors
  • FRENKEL, Gustavo
  • INI, Santiago
Agents
  • BRIDE, Patrick, J.
Priority Data
60/760,30618.01.2006US
60/872,95004.12.2006US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARING A CRYSTALLINE FORM OF TEGASEROD MALEATE
(FR) PROCEDE DE PREPARATION D'UNE FORME CRISTALLINE DE MALEATE DE TEGASEROD
Abstract
(EN)
Provided is a process for preparing tegaserod maleate Form B comprising reacting N- amino-N'-pentylguanidine hydroiodide ('AGP-HI') and 5-Methoxy-1 H-indole-3- carbaldehyde ('MICHO') in an aqueous reaction mixture to obtain tegaserod base; extracting the tegaserod base with a water immiscible organic solvent to obtain a mixture; combining the mixture with n-propanol to obtain a slurry; and combining the slurry with maleic acid to obtain tegaserod maleate Form B.
(FR)
La présente invention concerne un procédé de préparation de maléate de tégasérod.
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