WO2015111085A3 - Processes for the preparation of eltrombopag and pharmaceutically acceptable salts, solvates and intermediates thereof - Google Patents

Processes for the preparation of eltrombopag and pharmaceutically acceptable salts, solvates and intermediates thereof Download PDF

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Publication number
WO2015111085A3
WO2015111085A3 PCT/IN2015/000052 IN2015000052W WO2015111085A3 WO 2015111085 A3 WO2015111085 A3 WO 2015111085A3 IN 2015000052 W IN2015000052 W IN 2015000052W WO 2015111085 A3 WO2015111085 A3 WO 2015111085A3
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WO
WIPO (PCT)
Prior art keywords
eltrombopag
processes
preparation
pharmaceutically acceptable
acceptable salts
Prior art date
Application number
PCT/IN2015/000052
Other languages
French (fr)
Other versions
WO2015111085A2 (en
WO2015111085A8 (en
Inventor
Sanjay Jagdish Desai
Shri Prakash Dhar Dwivedi
Jayprakash Ajitsingh PARIHAR
Mahesh Laljibhai Rupapara
Dharmendra Mohanbhai KESHAVALA
Original Assignee
Cadila Healthcare Limited
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 Cadila Healthcare Limited filed Critical Cadila Healthcare Limited
Publication of WO2015111085A2 publication Critical patent/WO2015111085A2/en
Publication of WO2015111085A8 publication Critical patent/WO2015111085A8/en
Publication of WO2015111085A3 publication Critical patent/WO2015111085A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/44Oxygen and nitrogen or sulfur and nitrogen atoms
    • C07D231/46Oxygen atom in position 3 or 5 and nitrogen atom in position 4
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
    • C07C201/08Preparation of nitro compounds by substitution of hydrogen atoms by nitro groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C201/00Preparation of esters of nitric or nitrous acid or of compounds containing nitro or nitroso groups bound to a carbon skeleton
    • C07C201/06Preparation of nitro compounds
    • C07C201/12Preparation of nitro compounds by reactions not involving the formation of nitro groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/04Formation of amino groups in compounds containing carboxyl groups

Abstract

The present invention provides the processes for the preparation of eltrombopag of Formula (I) or its pharmaceutically acceptable salts. The invention also provides crystalline forms of eltrombopag.
PCT/IN2015/000052 2014-01-27 2015-01-27 Processes for the preparation of eltrombopag and pharmaceutically acceptable salts, solvates and intermediates thereof WO2015111085A2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
IN293MU2014 2014-01-27
IN293/MUM/2014 2014-01-27
IN1946/MUM/2014 2014-06-17
IN1946MU2014 2014-06-17
IN3073MU2014 2014-09-25
IN3073/MUM/2014 2014-09-25

Publications (3)

Publication Number Publication Date
WO2015111085A2 WO2015111085A2 (en) 2015-07-30
WO2015111085A8 WO2015111085A8 (en) 2015-09-03
WO2015111085A3 true WO2015111085A3 (en) 2015-11-12

Family

ID=53059376

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2015/000052 WO2015111085A2 (en) 2014-01-27 2015-01-27 Processes for the preparation of eltrombopag and pharmaceutically acceptable salts, solvates and intermediates thereof

Country Status (1)

Country Link
WO (1) WO2015111085A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10336706B2 (en) * 2014-09-05 2019-07-02 Hetero Research Foundation Crystalline form of Eltrombopag free acid
CN106146330B (en) * 2015-04-21 2018-04-06 江苏威凯尔医药科技有限公司 A kind of method for preparing eltrombopag olamine intermediate
US11161821B2 (en) * 2018-06-01 2021-11-02 Aurobindo Pharma Ltd. Process for the preparation of Eltrombopag olamine and its intermediates
CN114072386A (en) * 2019-07-04 2022-02-18 F.I.S.-菲博利佳意大利合成面料股份公司 Improved process for the preparation of key intermediates for the synthesis of eltrombopag or salts thereof

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001089457A2 (en) * 2000-05-25 2001-11-29 Smithkline Beecham Corporation Thrombopoietin mimetics
EP2236500A1 (en) * 2008-01-10 2010-10-06 Jiangsu Hengrui Medicine Co., Ltd. Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
WO2010114943A1 (en) * 2009-04-01 2010-10-07 Pliva Hrvatska D.O.O. Polymorphs of eltrombopag and eltrombopag salts and processes for preparation thereof
WO2014177517A1 (en) * 2013-04-29 2014-11-06 Esteve Química, S.A. Preparation process of an agonist of the thrombopoietin receptor

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI280128B (en) 2002-05-22 2007-05-01 Smithkline Beecham Corp 3'-[(2Z)-[1-(3,4- dimethylphenyl)-1,5-dihydro-3-methyl-5-oxo-4H-pyrazol-4-ylidene]hydrazino]-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid bis-(monoethanolamine)
JP4562523B2 (en) 2002-06-06 2010-10-13 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー Thrombopoietin mimetic

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001089457A2 (en) * 2000-05-25 2001-11-29 Smithkline Beecham Corporation Thrombopoietin mimetics
EP2236500A1 (en) * 2008-01-10 2010-10-06 Jiangsu Hengrui Medicine Co., Ltd. Bicyclo-substituted pyrazolon azo derivatives, preparation process and pharmaceutical use thereof
WO2010114943A1 (en) * 2009-04-01 2010-10-07 Pliva Hrvatska D.O.O. Polymorphs of eltrombopag and eltrombopag salts and processes for preparation thereof
WO2014177517A1 (en) * 2013-04-29 2014-11-06 Esteve Química, S.A. Preparation process of an agonist of the thrombopoietin receptor

Also Published As

Publication number Publication date
WO2015111085A2 (en) 2015-07-30
WO2015111085A8 (en) 2015-09-03

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