WO2015114657A3 - Amorphous form of sitagliptin free base - Google Patents

Amorphous form of sitagliptin free base Download PDF

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Publication number
WO2015114657A3
WO2015114657A3 PCT/IN2015/000035 IN2015000035W WO2015114657A3 WO 2015114657 A3 WO2015114657 A3 WO 2015114657A3 IN 2015000035 W IN2015000035 W IN 2015000035W WO 2015114657 A3 WO2015114657 A3 WO 2015114657A3
Authority
WO
WIPO (PCT)
Prior art keywords
free base
amorphous form
sitagliptin free
sitagliptin
provides
Prior art date
Application number
PCT/IN2015/000035
Other languages
French (fr)
Other versions
WO2015114657A2 (en
Inventor
Shri Prakash Dhar Dwivedi
Brij Khera
Kumar Kamlesh SINGH
Kirtipalsinh Sajjansinh Solanki
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 WO2015114657A2 publication Critical patent/WO2015114657A2/en
Publication of WO2015114657A3 publication Critical patent/WO2015114657A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

Abstract

The present invention provides an amorphous form of sitagliptin free base of Formula (I). The invention further provides a process for preparation of an amorphous form of sitagliptin free base. The process comprises a) providing a solution or suspension of sitagliptin free base in one or more solvents; and b) obtaining the amorphous form of sitagliptin free base by the removal of the solvent.(I)
PCT/IN2015/000035 2014-01-21 2015-01-21 Amorphous form of sitagliptin free base WO2015114657A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN212/MUM/2014 2014-01-21
IN212MU2014 IN2014MU00212A (en) 2014-01-21 2015-01-21

Publications (2)

Publication Number Publication Date
WO2015114657A2 WO2015114657A2 (en) 2015-08-06
WO2015114657A3 true WO2015114657A3 (en) 2015-10-08

Family

ID=53059374

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2015/000035 WO2015114657A2 (en) 2014-01-21 2015-01-21 Amorphous form of sitagliptin free base

Country Status (2)

Country Link
IN (1) IN2014MU00212A (en)
WO (1) WO2015114657A2 (en)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2016016260A (en) 2016-12-08 2018-06-07 Alparis Sa De Cv New solid forms of sitagliptin.
CN109580833B (en) * 2018-12-31 2021-12-03 辰欣药业股份有限公司 Method for determining enantiomer impurities in sitagliptin raw material and preparation
KR20210057603A (en) 2019-11-12 2021-05-21 제이투에이치바이오텍 (주) Process for preparing sitagliptin

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004085661A2 (en) * 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
WO2009070314A2 (en) * 2007-11-26 2009-06-04 Teva Pharmaceutical Industries Ltd. Crystalline form of sitagliptin
WO2010131025A1 (en) * 2009-05-11 2010-11-18 Generics [Uk] Limited Sitagliptin synthesis
WO2011049344A2 (en) * 2009-10-21 2011-04-28 Hanmi Holdings Co., Ltd. Method of preparing sitagliptin and intermediates used therein
WO2012131005A1 (en) * 2011-03-29 2012-10-04 Krka, Tovarna Zdravil, D.D., Novo Mesto Pharmaceutical composition of sitagliptin

Family Cites Families (13)

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Publication number Priority date Publication date Assignee Title
UA74912C2 (en) 2001-07-06 2006-02-15 Merck & Co Inc Beta-aminotetrahydroimidazo-(1,2-a)-pyrazines and tetratriazolo-(4,3-a)-pyrazines as inhibitors of dipeptylpeptidase for the treatment or prevention of diabetes
JO2625B1 (en) 2003-06-24 2011-11-01 ميرك شارب اند دوم كوربوريشن Phosphoric acid salt of a dipeptidyl peptidase-IV inhibitor
US20060287528A1 (en) 2003-09-02 2006-12-21 Wenslow Robert M Novel crystalline forms of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
EP1667524A4 (en) 2003-09-23 2009-01-14 Merck & Co Inc Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor
EP1909776A2 (en) 2005-07-25 2008-04-16 Merck & Co., Inc. Dodecylsulfate salt of a dipeptidyl peptidase-iv inhibitor
US8334385B2 (en) 2007-11-02 2012-12-18 Glenmark Generics Limited Process for the preparation of R-sitagliptin and its pharmaceutically acceptable salts thereof
US20100041885A1 (en) 2008-03-25 2010-02-18 Nurit Perlman Crystalline forms of sitagliptin phosphate
EP2650297A1 (en) 2008-07-03 2013-10-16 Ratiopharm GmbH Crystalline salts of sitagliptin
WO2010122578A2 (en) 2009-04-20 2010-10-28 Msn Laboratories Limited Process for the preparation of sitagliptin and its intermediates
MX2012001842A (en) 2009-08-13 2012-03-07 Sandoz Ag Crystalline compound of 7-[(3r)-3-amino-1-oxo-4-(2, 4, 5-trifluorphenyl)butyl]-5, 6, 7, 8-tetrahydro-3-(tri fluormethyl)-1, 2, 4 -triazolo[4,3-a]pyrazine.
EP2407469A1 (en) 2010-07-13 2012-01-18 Chemo Ibérica, S.A. Salt of sitagliptin
WO2012076973A2 (en) 2010-12-09 2012-06-14 Aurobindo Pharma Limited Novel salts of dipeptidyl peptidase iv inhibitor
US20150025080A1 (en) 2011-06-29 2015-01-22 Ranbaxy Laboratories Limited Solid dispersions of sitagliptin and processes for their preparation

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004085661A2 (en) * 2003-03-24 2004-10-07 Merck & Co., Inc Process to chiral beta-amino acid derivatives
WO2009070314A2 (en) * 2007-11-26 2009-06-04 Teva Pharmaceutical Industries Ltd. Crystalline form of sitagliptin
WO2010131025A1 (en) * 2009-05-11 2010-11-18 Generics [Uk] Limited Sitagliptin synthesis
WO2011049344A2 (en) * 2009-10-21 2011-04-28 Hanmi Holdings Co., Ltd. Method of preparing sitagliptin and intermediates used therein
WO2012131005A1 (en) * 2011-03-29 2012-10-04 Krka, Tovarna Zdravil, D.D., Novo Mesto Pharmaceutical composition of sitagliptin

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
KIM DOOSEOP ET AL: "(2R)-4-Oxo-4-[3-(Trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3- a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine: A Potent, Orally Active Dipeptidyl Peptidase IV Inhibitor for the Treatment of Type 2 Diabetes", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY, US, vol. 48, 1 January 2005 (2005-01-01), pages 141 - 151, XP002529729, ISSN: 0022-2623, [retrieved on 20041213], DOI: 10.1021/JM0493156 *

Also Published As

Publication number Publication date
IN2014MU00212A (en) 2015-08-28
WO2015114657A2 (en) 2015-08-06

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