WO2004087650A3 - Procede et intermediaires pour la preparation d'inhibiteurs d'amide d'acide beta-amino de dipeptidyle peptidase-iv - Google Patents

Procede et intermediaires pour la preparation d'inhibiteurs d'amide d'acide beta-amino de dipeptidyle peptidase-iv Download PDF

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Publication number
WO2004087650A3
WO2004087650A3 PCT/US2004/008826 US2004008826W WO2004087650A3 WO 2004087650 A3 WO2004087650 A3 WO 2004087650A3 US 2004008826 W US2004008826 W US 2004008826W WO 2004087650 A3 WO2004087650 A3 WO 2004087650A3
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WO
WIPO (PCT)
Prior art keywords
inhibitors
dipeptidyl peptidase
preparation
amino acid
acid amide
Prior art date
Application number
PCT/US2004/008826
Other languages
English (en)
Other versions
WO2004087650A2 (fr
Inventor
Remy Angelaud
Joseph D Armstrong Iii
David Askin
Jaume Balsells
Karl Hansen
Jaemoon Lee
Peter E Maligres
Nelo R Rivera
Yi Xiao
Yong-Li Zhong
Original Assignee
Merck & Co Inc
Remy Angelaud
Joseph D Armstrong Iii
David Askin
Jaume Balsells
Karl Hansen
Jaemoon Lee
Peter E Maligres
Nelo R Rivera
Yi Xiao
Yong-Li Zhong
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 Merck & Co Inc, Remy Angelaud, Joseph D Armstrong Iii, David Askin, Jaume Balsells, Karl Hansen, Jaemoon Lee, Peter E Maligres, Nelo R Rivera, Yi Xiao, Yong-Li Zhong filed Critical Merck & Co Inc
Publication of WO2004087650A2 publication Critical patent/WO2004087650A2/fr
Publication of WO2004087650A3 publication Critical patent/WO2004087650A3/fr

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C239/00Compounds containing nitrogen-to-halogen bonds; Hydroxylamino compounds or ethers or esters thereof
    • C07C239/08Hydroxylamino compounds or their ethers or esters
    • C07C239/20Hydroxylamino compounds or their ethers or esters having oxygen atoms of hydroxylamino groups etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un nouveau procédé pour la préparation d'inhibiteurs d'amide d'acide béta-amino chiral de dipeptidyle peptidase-IV, et les intermédiaires utiles obtenus par ce procédé. Les produits obtenus à partir de ce procédé instantané sont des inhibiteurs de dipeptidyle peptidase-IV et par conséquent, ils sont utiles pour le traitement de diabètes de type 2.
PCT/US2004/008826 2003-03-27 2004-03-23 Procede et intermediaires pour la preparation d'inhibiteurs d'amide d'acide beta-amino de dipeptidyle peptidase-iv WO2004087650A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45797603P 2003-03-27 2003-03-27
US60/457,976 2003-03-27

Publications (2)

Publication Number Publication Date
WO2004087650A2 WO2004087650A2 (fr) 2004-10-14
WO2004087650A3 true WO2004087650A3 (fr) 2005-01-13

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/008826 WO2004087650A2 (fr) 2003-03-27 2004-03-23 Procede et intermediaires pour la preparation d'inhibiteurs d'amide d'acide beta-amino de dipeptidyle peptidase-iv

Country Status (1)

Country Link
WO (1) WO2004087650A2 (fr)

Cited By (5)

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Publication number Priority date Publication date Assignee Title
US7842707B2 (en) 2004-07-23 2010-11-30 Nuada, Llc Peptidase inhibitors
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors

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BRPI0614732A2 (pt) * 2005-08-11 2011-04-12 Hoffmann La Roche composição farmacêutica que compreende um inibidor de dpp-iv, uso de um inibidor de dpp-iv e método para o tratamento de enfermidades associadas com nìveis de glicose sanguìnea elevados
CN102675221A (zh) 2005-09-16 2012-09-19 武田药品工业株式会社 用于制备嘧啶二酮衍生物的方法中的中间体
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TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
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CN101570538B (zh) * 2008-04-29 2011-04-20 上海博康精细化工有限公司 一种西他列汀中间体的制备方法
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EP2223923A1 (fr) 2009-02-25 2010-09-01 Esteve Química, S.A. Procédé pour la préparation d'un dérivé d'acide aminé chiral bêta et intermédiaires correspondants
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KR101253106B1 (ko) * 2009-10-01 2013-04-10 한미사이언스 주식회사 키랄 옥실레인을 이용한 시타글립틴 중간체의 제조방법
KR101222679B1 (ko) * 2009-10-21 2013-01-16 한미사이언스 주식회사 시타글립틴의 제조 방법 및 이에 사용되는 중간체
CN102093245B (zh) * 2009-12-14 2015-04-15 浙江海翔药业股份有限公司 一种西他列汀中间体、西他列汀或其盐的制备方法
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EP2392575A1 (fr) 2010-06-04 2011-12-07 LEK Pharmaceuticals d.d. Nouvelle approche synthétique pour composés à substitution ß-aminobutyryle
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CN105017260B (zh) * 2015-07-30 2017-04-19 新发药业有限公司 一种西他列汀中间体三唑并吡嗪衍生物的制备方法
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Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7842707B2 (en) 2004-07-23 2010-11-30 Nuada, Llc Peptidase inhibitors
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
US8324383B2 (en) 2006-09-13 2012-12-04 Takeda Pharmaceutical Company Limited Methods of making polymorphs of benzoate salt of 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1(2H)-pyrimidinyl]methyl]-benzonitrile
US8093236B2 (en) 2007-03-13 2012-01-10 Takeda Pharmaceuticals Company Limited Weekly administration of dipeptidyl peptidase inhibitors
US8883714B2 (en) 2008-04-07 2014-11-11 Arena Pharmaceuticals, Inc. Pharmaceutical compositions comprising GPR119 agonists which act as peptide YY (PYY) secretagogues

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