SG11201806116SA - An improved process for the preparation of regorafenib - Google Patents

An improved process for the preparation of regorafenib

Info

Publication number
SG11201806116SA
SG11201806116SA SG11201806116SA SG11201806116SA SG11201806116SA SG 11201806116S A SG11201806116S A SG 11201806116SA SG 11201806116S A SG11201806116S A SG 11201806116SA SG 11201806116S A SG11201806116S A SG 11201806116SA SG 11201806116S A SG11201806116S A SG 11201806116SA
Authority
SG
Singapore
Prior art keywords
natco
hyderabad
house
road
international
Prior art date
Application number
SG11201806116SA
Inventor
Pulla Reddy Muddasani
Shankar Reddy Budideti
Srinivasachary Chintalapati
Tirupathi Kotte
Sambasiva Rao Talasila
Venkaiah Chowdary Nannapaneni
Original Assignee
Natco Pharma Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Natco Pharma Ltd filed Critical Natco Pharma Ltd
Publication of SG11201806116SA publication Critical patent/SG11201806116SA/en

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—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
    • C07D213/02—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 having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—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 having three double bonds between ring members or between ring members and non-ring members 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
    • C07D213/60—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 having three double bonds between ring members or between ring members and non-ring members 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 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

INTERNATIONAL APPLICATION PUBLISHED UNDER THE PATENT COOPERATION TREATY (PCT) (19) World Intellectual Property , Organization MD 1111101110101011111 HO 111110111011101111101111011111 1111110 IIE III International Bureau 0.. .... .. (10) International Publication Number (43) International Publication Date ..... .....!;,' WO 2017/125941 Al 27 July 2017 (27.07.2017) WIPO I PCT (51) International Patent Classification: (81) Designated States (unless otherwise indicated, for every A61K 9/28 (2006.01) A61K 31/44 (2006.01) kind of national protection available): AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, (21) International Application Number: BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, PCT/IN2016/050099 DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, (22) International Filing Date: 31 March 2016 (31.03.2016) 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, (25) Filing Language: English PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, (26) Publication Language: English 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. (30) Priority Data: 201641001756 18 January 2016 (18.01.2016) IN (84) Designated States (unless otherwise indicated, for every kind of regional protection available): ARIPO (BW, GH, (71) Applicant: NATCO PHARMA LTD [IN/IN]; Natco House, Road No.2, Banjara Hills, Hyderabad 500034 (IN). GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW), Eurasian (AM, AZ, BY, KG, KZ, RU, — (72) Inventors: MUDDASANI, Pulla Reddy; Natco House, Road No.2, Banjara Hills, Hyderabad 500034 (IN). BU- DIDETI, Shankar Reddy; Natco House, Road No.2, Ban- jara Hills, Hyderabad 500034 (IN). CHINTALAPATI, Srinivasachary; Natco House, Road No.2, Banjara Hills, Hyderabad 500034 (IN). KOTTE, Tirupathi; Natco TJ, TM), European (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), OAPI (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG). Declarations under Rule 4.17: — House, Road No.2, Banjara Hills, Hyderabad 500034 (IN). TALASILA, Sambasiva Rao; Natco House, Road No.2, — of inventorship (Rule 4.17(iv)) — — Banjara Hills, Hyderabad 500034 (IN). NANNAPANENI, Published: Venkaiah Chowdary; Natco House, Road No.2, Banjara Hills, Hyderabad 500034 (IN). with international search report (Art. 21(3)) = = = = = = = = = Il 11 7r tz. kin N Il IN Il © (54) Title: AN IMPROVED PROCESS FOR THE PREPARATION OF REGORAFENIB el en. ) (57) : The present invention relates to an improved process for the preparation of Regorafenib with genotoxic impurities at 't well below threshold limit and high yield. The present invention also relates to an improved process for the preparation of regorafen- ib form-I with high purity.
SG11201806116SA 2016-01-18 2016-03-31 An improved process for the preparation of regorafenib SG11201806116SA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN201641001756 2016-01-18
PCT/IN2016/050099 WO2017125941A1 (en) 2016-01-18 2016-03-31 An improved process for the preparation of regorafenib

Publications (1)

Publication Number Publication Date
SG11201806116SA true SG11201806116SA (en) 2018-08-30

Family

ID=59361728

Family Applications (1)

Application Number Title Priority Date Filing Date
SG11201806116SA SG11201806116SA (en) 2016-01-18 2016-03-31 An improved process for the preparation of regorafenib

Country Status (5)

Country Link
US (1) US20190300484A1 (en)
AU (1) AU2016387566A1 (en)
CA (1) CA3011662A1 (en)
SG (1) SG11201806116SA (en)
WO (1) WO2017125941A1 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111053751A (en) * 2018-10-16 2020-04-24 正大天晴药业集团股份有限公司 Regorafenib sustained-release tablet and preparation method thereof
CN112851577A (en) * 2019-11-26 2021-05-28 齐鲁制药有限公司 Preparation method of regorafenib
CN113801035A (en) * 2020-06-11 2021-12-17 齐鲁制药有限公司 Regorafenib intermediate impurity, preparation method and application thereof

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2525515A (en) * 1948-05-15 1950-10-10 Eastman Kodak Co Process for preparing aminophenols
AU595417B2 (en) * 1987-02-04 1990-03-29 Sumitomo Chemical Company, Limited A benzoylurea derivative and its production and use
CN1105983A (en) * 1994-01-25 1995-08-02 兰州大学 Method for preparation of p-aminophenol
CL2004001834A1 (en) * 2003-07-23 2005-06-03 Bayer Pharmaceuticals Corp COMPOUND 4- {4- [3- (4-CHLORO-3-TRIFLUOROMETILFENIL) -UREIDO] -3-FLUOROFENOXI} -PIRIDIN-2-METHYLAMIDE, RAF INHIBITOR, VEGFR, P38 AND PDGFR KINASES, ITS SALTS; PHARMACEUTICAL COMPOSIICON; PHARMACEUTICAL COMBINATION; AND ITS USE TO TREAT HYPERPROL DISORDERS
CN1634867A (en) * 2003-12-30 2005-07-06 中国科学院大连化学物理研究所 Method for hydrogenation preparation of 4-amino-3-fluorophenol from o-fluoro-nitrobenzene and device therefor
AR081060A1 (en) * 2010-04-15 2012-06-06 Bayer Schering Pharma Ag PROCEDURE TO PREPARE 4- {4 - [({[4-CHLORINE-3- (TRIFLUOROMETIL) PHENYL] AMINO} CARBONYL) AMINO] -3-FLUOROPHENOXY} -N-METHYLPIRIDIN-2-CARBOXAMIDE
US9518020B2 (en) * 2013-10-04 2016-12-13 Hetero Research Foundation Process for Regorafenib
WO2016005874A1 (en) * 2014-07-09 2016-01-14 Shilpa Medicare Limited Process for the preparation of regorafenib and its crystalline forms

Also Published As

Publication number Publication date
CA3011662A1 (en) 2017-07-27
WO2017125941A1 (en) 2017-07-27
US20190300484A1 (en) 2019-10-03
AU2016387566A1 (en) 2018-08-09

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SG11201806116SA (en) An improved process for the preparation of regorafenib