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1. (WO2010075631) POLYMORPHIC FORM OF 5-CHLORO-N-{[(5S)-2-OXO-3-[4-(3-OXOMORPHOLIN-4-YL)PHENYL]OXA-ZOLIDIN-5-YL]-METHYL}THIOPHENE-2-CARBOXAMIDE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2010/075631 International Application No.: PCT/CA2009/001895
Publication Date: 08.07.2010 International Filing Date: 31.12.2009
IPC:
C07D 413/14 (2006.01) ,A61K 31/5377 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
14
containing three or more hetero rings
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
33
Heterocyclic compounds
395
having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
535
having six-membered rings with at least one nitrogen and at least one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
5375
1,4-Oxazines, e.g. morpholine
5377
not condensed and containing further heterocyclic rings, e.g. timolol
Applicants:
APOTEX PHARMACHEM INC [CA/CA]; 34 Spalding Drive Brantford ON N3T 6B8, CA (AllExceptUS)
BODHURI, Prabhudas [CA/CA]; CA (UsOnly)
WEERATUNGA, Gamini [CA/CA]; CA (UsOnly)
Inventors:
BODHURI, Prabhudas; CA
WEERATUNGA, Gamini; CA
Agent:
MCKINNON, Graham, J. K.; Apotex Inc. 150 Signet Drive Toronto ON M9L 1T9, CA
Priority Data:
12/347,17631.12.2008US
Title (EN) POLYMORPHIC FORM OF 5-CHLORO-N-{[(5S)-2-OXO-3-[4-(3-OXOMORPHOLIN-4-YL)PHENYL]OXA-ZOLIDIN-5-YL]-METHYL}THIOPHENE-2-CARBOXAMIDE
(FR) FORME POLYMORPHE DE LA 5-CHLORO-N-{[(5S)-2-OXO-3-[4-(3-OXOMORPHOLIN-4-YL)PHÉNYL]OXA-ZOLIDIN-S-YL]MÉTHYL}THIOPHÈNE-2-CARBOXAMIDE
Abstract:
(EN) A polymorphic form of rivaroxaban, 5-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phenyl]oxa-zolidin-5-yl]- methyl}thiophene-2-carboxamide (termed form APO-A), processes for the preparation thereof, and compositions and formulations comprising form APO-A are provided. Also provided are compositions comprising a crystalline form of rivaroxaban and solvents selected from C3 to C6 ketones, C3 to C4 amides and mixtures thereof.
(FR) L'invention concerne une forme polymorphe du rivaroxaban, la 5-chloro-N-{[(5S)-2-oxo-3-[4-(3-oxomorpholin-4-yl)phényl]oxa-zolidin-S-yl]méthyl}thiophène-2-carboxamide (appelée forme APO-A), ses procédés de préparation et des compositions et formulations comportant la forme APO-A. L'invention concerne également des compositions comportant une forme cristalline du rivaroxaban et des solvants choisis parmi les cétones en C3 à C6, les amides en C3 à C4 et les mélanges de ces composés.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, 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, PE, PG, PH, PL, PT, RO, RS, RU, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, 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, MK, MT, NL, NO, PL, PT, RO, SE, SI, SK, SM, 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:
IL213881EP2382209JP2012514010CN102292332CA2748853KR1020110130395
NZ593818AU2009335611IN1587/MUMNP/2011