WO2011100325A3 - Polymorphs of sunitinib salts - Google Patents

Polymorphs of sunitinib salts Download PDF

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Publication number
WO2011100325A3
WO2011100325A3 PCT/US2011/024194 US2011024194W WO2011100325A3 WO 2011100325 A3 WO2011100325 A3 WO 2011100325A3 US 2011024194 W US2011024194 W US 2011024194W WO 2011100325 A3 WO2011100325 A3 WO 2011100325A3
Authority
WO
WIPO (PCT)
Prior art keywords
polymorphs
sunitinib
salts
compositions
sunitinib salts
Prior art date
Application number
PCT/US2011/024194
Other languages
French (fr)
Other versions
WO2011100325A2 (en
Inventor
Pavel Vraspir
Maurizio Paiocchi
Alexandr Jegorov
Francesca Scarpitta
Original Assignee
Sicor Inc.
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 Sicor Inc. filed Critical Sicor Inc.
Publication of WO2011100325A2 publication Critical patent/WO2011100325A2/en
Publication of WO2011100325A3 publication Critical patent/WO2011100325A3/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents

Abstract

Polymorphs of Sunitinib malate and other salts have been prepared. Compositions comprising Sunitinib base, L-malic acid and another carboxylic acid are also described. Such polymorphs and compositions are useful, for example, in preparing pharmaceutical compositions.
PCT/US2011/024194 2010-02-09 2011-02-09 Polymorphs of sunitinib salts WO2011100325A2 (en)

Applications Claiming Priority (12)

Application Number Priority Date Filing Date Title
US30261910P 2010-02-09 2010-02-09
US61/302,619 2010-02-09
US30564710P 2010-02-18 2010-02-18
US61/305,647 2010-02-18
US30660110P 2010-02-22 2010-02-22
US61/306,601 2010-02-22
US34801510P 2010-05-25 2010-05-25
US61/348,015 2010-05-25
US35209010P 2010-06-07 2010-06-07
US61/352,090 2010-06-07
US36071110P 2010-07-01 2010-07-01
US61/360,711 2010-07-01

Publications (2)

Publication Number Publication Date
WO2011100325A2 WO2011100325A2 (en) 2011-08-18
WO2011100325A3 true WO2011100325A3 (en) 2011-12-15

Family

ID=43899612

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2011/024194 WO2011100325A2 (en) 2010-02-09 2011-02-09 Polymorphs of sunitinib salts

Country Status (1)

Country Link
WO (1) WO2011100325A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2709110T3 (en) 2012-03-23 2019-04-15 Laurus Labs Ltd An improved process for the preparation of sunitinib and its acid addition salts
WO2015031604A1 (en) 2013-08-28 2015-03-05 Crown Bioscience, Inc. Gene expression signatures predictive of subject response to a multi-kinase inhibitor and methods of using the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020156292A1 (en) * 2000-02-15 2002-10-24 Tang Peng Cho Pyrrole substituted 2-indolinone protein kinase inhibitors
WO2009067674A2 (en) * 2007-11-21 2009-05-28 Teva Pharmaceutical Industries Ltd. Polymorphs of sunitinib base and processes for preparation thereof
WO2010023474A1 (en) * 2008-08-25 2010-03-04 Generics [Uk] Limited Novel polymorphs of sunitinib and processes for their preparation

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PT3168218T (en) 2001-08-15 2019-01-11 Pharmacia & Upjohn Co Llc A crystal comprising an l-malic acid salt of n-[2-(diethylamino)ethyl]-5-[(5-fluoro-1,2-dihydro-2-oxo-3h-indol-3-ylidene)methyl]-2,4-dimethyl-1h-pyrrole-3-carboxamide for use as a medicament
CN101939314B (en) 2007-12-12 2014-04-02 麦迪凯姆股份公司 Polymorphic forms of a 3-pyrrole substituted 2-indolinone
JP2011512396A (en) 2008-02-21 2011-04-21 ジェネリクス・(ユーケー)・リミテッド Novel polymorphs and methods for their preparation
EP2098521A1 (en) 2008-03-06 2009-09-09 Ratiopharm GmbH Crystal forms of N-[2-(diethylamino) ethyl]-5-[fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrolle-3-carboxamide and methods for their prepparation
KR20100135910A (en) 2008-04-16 2010-12-27 낫코 파마 리미티드 Novel polymorphic forms of sunitinib base
WO2009156837A2 (en) 2008-06-26 2009-12-30 Medichem, S.A. Amorphous form of a 3-pyrrole substituted 2-indolinone malate salt
EP2342195B1 (en) 2008-07-24 2014-09-10 Medichem, S.A. Crystalline forms of a 3-pyrrole substituted 2-indolinone malate salt
KR20110036588A (en) 2008-07-24 2011-04-07 테바 파마슈티컬 인더스트리즈 리미티드 Sunitinib and salts thereof and their polymorphs
EP2181991A1 (en) 2008-10-28 2010-05-05 LEK Pharmaceuticals D.D. Novel salts of sunitinib

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20020156292A1 (en) * 2000-02-15 2002-10-24 Tang Peng Cho Pyrrole substituted 2-indolinone protein kinase inhibitors
WO2009067674A2 (en) * 2007-11-21 2009-05-28 Teva Pharmaceutical Industries Ltd. Polymorphs of sunitinib base and processes for preparation thereof
WO2010023474A1 (en) * 2008-08-25 2010-03-04 Generics [Uk] Limited Novel polymorphs of sunitinib and processes for their preparation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
CAIRA M R: "CRYSTALLINE POLYMORPHISM OF ORGANIC COMPOUNDS", TOPICS IN CURRENT CHEMISTRY, SPRINGER, BERLIN, DE, vol. 198, 1 January 1998 (1998-01-01), pages 163 - 208, XP001156954, ISSN: 0340-1022, ISBN: 978-3-540-36760-4, DOI: DOI:10.1007/3-540-69178-2_5 *

Also Published As

Publication number Publication date
WO2011100325A2 (en) 2011-08-18

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