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1. (WO2016005874) PROCESS FOR THE PREPARATION OF REGORAFENIB AND ITS CRYSTALLINE FORMS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/2016/005874 International Application No.: PCT/IB2015/055083
Publication Date: 14.01.2016 International Filing Date: 06.07.2015
IPC:
C07D 213/81 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
78
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81
Amides; Imides
Applicants:
SHILPA MEDICARE LIMITED [IN/IN]; #12-6-214/A1,Hyderabad Road Raichur-584 135, Karnataka, IN
Inventors:
RAMPALLI, Sriram; IN
UPALLA, Lav Kumar; IN
RAMACHANDRULA, Krishna Kumar; IN
PUROHIT, Prashant; IN
AKSHAY KANT, Chaturvedi; IN
Priority Data:
3391/CHE/201409.07.2014IN
3396/CHE/201409.07.2014IN
Title (EN) PROCESS FOR THE PREPARATION OF REGORAFENIB AND ITS CRYSTALLINE FORMS
(FR) PROCÉDÉ POUR LA PRÉPARATION DU RÉGORAFÉNIB ET SES FORMES CRISTALLINES
Abstract:
(EN) The present invention relates to a process for the preparation of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]-N-methylpyridine-2-carboxamide or Regorafenib (I): Formula (I). The present invention further relates to a process for the purification of 4-[4-({[4-chloro-3-(trifluoromethyl) phenyl] carbamoyl} amino)-3-fluorophenoxy]-N-methylpyridine-2- carboxamide or Regorafenib (I) to provide highly pure material. The present invention further relates to a process for the preparation stable crystalline material of 4-[4-({[4-chloro-3-(trifluoromethyl)phenyl]carbamoyl}amino)-3-fluorophenoxy]- N-methyl pyridine-2-carboxamide or Regorafenib (I) useful in the preparation of pharmaceutical compositions for the treatment of cancer.
(FR) La présente invention concerne un procédé pour la préparation de 4-[4-({[4-chloro-3- (trifluorométhyle)phényl]carbamoyl}amino)-3-fluorophénoxy]-N-méthylpyridine -2-carboxamide ou du régorafénib (I) : Formule (I). La présente invention concerne en outre un procédé pour la purification de 4-[4-({ [4-chloro-3-(trifluorométhyle)phényl]carbamoyl}amino)-3-fluorophénoxy]-N-méthylpyridine-2-carboxamide ou du régorafénib (I) pour fournir un matériau hautement pur. La présente invention concerne en outre un procédé pour la préparation d'un matériau cristallin stable de 4-[4-({[4-chloro-3-(trifluorométhyl)phényl]carbamoyl}amino) -3-fluorophénoxy]-N-méthylpyridine-2-carboxamide ou de régorafénib (I) utiles dans la préparation de compositions pharmaceutiques pour le traitement du cancer.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, 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, IR, IS, JP, KE, KG, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, 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, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (AL, 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, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
US20170204062