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WO2012035549A3 - Procédé amélioré pour la synthèse de dérivés d'acides bêta-aminés - Google Patents

Procédé amélioré pour la synthèse de dérivés d'acides bêta-aminés Download PDF

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Publication number
WO2012035549A3
WO2012035549A3 PCT/IN2011/000621 IN2011000621W WO2012035549A3 WO 2012035549 A3 WO2012035549 A3 WO 2012035549A3 IN 2011000621 W IN2011000621 W IN 2011000621W WO 2012035549 A3 WO2012035549 A3 WO 2012035549A3
Authority
WO
WIPO (PCT)
Prior art keywords
synthesis
amino acid
acid derivatives
improved process
beta amino
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/IN2011/000621
Other languages
English (en)
Other versions
WO2012035549A2 (fr
Inventor
Rajesh Jain
Jagadeeshwar R Rao
Siripragada Mahender Rao
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Panacea Biotec Ltd
Original Assignee
Panacea Biotec 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 Panacea Biotec Ltd filed Critical Panacea Biotec Ltd
Publication of WO2012035549A2 publication Critical patent/WO2012035549A2/fr
Publication of WO2012035549A3 publication Critical patent/WO2012035549A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • C07D233/58—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/10—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 condensed with carbocyclic rings or ring systems
    • C07D243/14—1,4-Benzodiazepines; Hydrogenated 1,4-benzodiazepines
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La présente invention concerne un procédé amélioré ainsi qu'un/des intermédiaire(s) pour la synthèse de dérivés d'acides bêta-aminés représentés par la formule (I). Les composés représentés par la formule (I) servent d'inhibiteurs DPP-IV et sont utiles dans le traitement du diabète de type 2.
PCT/IN2011/000621 2010-09-13 2011-09-12 Procédé amélioré pour la synthèse de dérivés d'acides bêta-aminés Ceased WO2012035549A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN2164/DEL/2010 2010-09-13
IN2164DE2010 IN2010DE02164A (fr) 2010-09-13 2011-09-12

Publications (2)

Publication Number Publication Date
WO2012035549A2 WO2012035549A2 (fr) 2012-03-22
WO2012035549A3 true WO2012035549A3 (fr) 2012-10-11

Family

ID=44898127

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2011/000621 Ceased WO2012035549A2 (fr) 2010-09-13 2011-09-12 Procédé amélioré pour la synthèse de dérivés d'acides bêta-aminés

Country Status (3)

Country Link
AR (1) AR082971A1 (fr)
IN (1) IN2010DE02164A (fr)
WO (1) WO2012035549A2 (fr)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2015145333A1 (fr) 2014-03-26 2015-10-01 Sun Pharmaceutical Industries Limited Procédé de préparation de sitagliptine et son intermédiaire

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004058266A1 (fr) * 2002-12-20 2004-07-15 Merck & Co., Inc. Derives de 3-amino-4-phenylbutanoique acide utilises en tant qu'inhibiteurs de dipeptidyl peptidase pour le traitement ou la prevention du diabete
WO2006104997A2 (fr) * 2005-03-29 2006-10-05 Merck & Co., Inc. Sels d'acide tartarique d'un inhibiteur de la dipeptidyl peptidase iv
WO2009093269A1 (fr) * 2008-01-24 2009-07-30 Panacea Biotec Limited Nouveaux composés hétérocycliques
WO2010097420A1 (fr) * 2009-02-25 2010-09-02 Esteve Química, S.A. Procédé de préparation d'un dérivé béta aminoacide chiral et intermédiaires utilisés dans ledit procédé

Family Cites Families (21)

* Cited by examiner, † Cited by third party
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
JP4530852B2 (ja) 2002-07-15 2010-08-25 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病治療のためのピペリジノピリミジンジペプチジルペプチダーゼ阻害剤
BR0315381A (pt) 2002-10-18 2005-08-23 Merck & Co Inc Composto ou um sal farmaceuticamente aceitável deste, composição farmacêutica, e, métodos para inibir a atividade da enzima dipeptidil peptidase-iv em um mamìfero em necessidade disto, para tratar diabetes em um mamìfero em necessidade disto, para tratar diabete não dependente de insulina (tipo 2) em um mamìfero em necessidade disto, para tratar hiperglicemia em um mamìfero em necessidade disto, para tratar a obesidade em um mamìfero em necessidade disto, para tratar um ou mais distúrbios de lipìdios selecionados do grupo de dislipidemia, hiperlipidemia, hipertrigliceridemia, hipercolesterolemia, hdl baixo e ldl alto em um mamìfero em necessidade disto, e para tratar em um mamìfero em necessidade disto uma ou mais condições
CA2504735C (fr) 2002-11-07 2009-06-23 Merck & Co., Inc. Derives de phenylalanine utilises comme inhibiteurs de la dipeptidyl peptidase dans le traitement ou la prevention du diabete
AR043515A1 (es) 2003-03-19 2005-08-03 Merck & Co Inc Procedimiento para preparar derivados quirales beta aminoacidos mediante hidrogenacion asimetrica
CA2533893A1 (fr) 2003-07-31 2005-02-10 Merck & Co., Inc. Hexahydrodiazepinones utilises en tant qu'inhibiteurs de la dipeptidyl peptidase iv pour le traitement ou la prevention du diabete
GB0324236D0 (en) 2003-10-16 2003-11-19 Astrazeneca Ab Chemical compounds
EP1682120A4 (fr) 2003-11-04 2009-05-27 Merck & Co Inc Derives de phenylalanine fusionnes utilises comme inhibiteurs de la dipeptidyl peptidase-iv dans le traitement ou la prevention du diabete
EP1756106A4 (fr) 2004-05-18 2008-12-17 Merck & Co Inc Derives de la cyclohexylalanine utilises comme inhibiteurs de la dipeptidyl peptidase-iv pour le traitement ou la prevention des diabetes
EP1598341A1 (fr) 2004-05-21 2005-11-23 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Inhibiteurs de DPP-IV
EP1604989A1 (fr) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Inhibiteurs de DPP-IV
EP1604662A1 (fr) 2004-06-08 2005-12-14 Santhera Pharmaceuticals (Deutschland) Aktiengesellschaft Derivés de la benzyl amine du acide carboxylique (2R) de la 1-[(3R)-Amino-4-(2-fluoro-phenyl)-butyl]-pyrrolidine et composés similaires pour l'utilisation comme inhibiteurs de la peptidase dipeptidyl IV (DPP-IV) pour le traitement de la diabetes mellitus de type 2
GB0413389D0 (en) 2004-06-16 2004-07-21 Astrazeneca Ab Chemical compounds
JP4963671B2 (ja) 2004-06-21 2012-06-27 メルク・シャープ・エンド・ドーム・コーポレイション 糖尿病の治療または予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としてのアミノシクロヘキサン
JP2008510810A (ja) 2004-08-23 2008-04-10 メルク エンド カムパニー インコーポレーテッド 糖尿病の治療または予防のためのジペプチジルペプチダーゼ−ｉｖ阻害剤としての縮合トリアゾール誘導体
ATE481969T1 (de) 2004-10-01 2010-10-15 Merck Sharp & Dohme Aminopiperidine als dipeptidylpeptidase-iv- inhibitoren zur behandlung oder prävention von diabetes
AR052879A1 (es) 2005-01-24 2007-04-11 Merck & Co Inc Procedimiento para preparar derivados de beta aminoacidos quirales por hidrogenacion asimetrica
EP1702916A1 (fr) 2005-03-18 2006-09-20 Santhera Pharmaceuticals (Schweiz) GmbH Inhibiteurs de DPP-IV
EP1943215A2 (fr) 2005-10-31 2008-07-16 Brystol-Myers Squibb Company Inhibiteurs à base d amide et de bêta-amino de pyrrolidinyle de la dipeptidyl peptidase iv et procédés
EP1971614A1 (fr) 2005-11-14 2008-09-24 Probiodrug AG Derives de pyrrolidine a fusion de cyclopropyle, en tant qu'inhibiteurs de dipeptidyle peptidase iv (dp iv)
WO2007063928A1 (fr) 2005-11-30 2007-06-07 Toray Industries, Inc. Nouveau derive non cyclique d’amine carboxamide et sel de celui-ci

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004058266A1 (fr) * 2002-12-20 2004-07-15 Merck & Co., Inc. Derives de 3-amino-4-phenylbutanoique acide utilises en tant qu'inhibiteurs de dipeptidyl peptidase pour le traitement ou la prevention du diabete
WO2006104997A2 (fr) * 2005-03-29 2006-10-05 Merck & Co., Inc. Sels d'acide tartarique d'un inhibiteur de la dipeptidyl peptidase iv
WO2009093269A1 (fr) * 2008-01-24 2009-07-30 Panacea Biotec Limited Nouveaux composés hétérocycliques
WO2010097420A1 (fr) * 2009-02-25 2010-09-02 Esteve Química, S.A. Procédé de préparation d'un dérivé béta aminoacide chiral et intermédiaires utilisés dans ledit procédé

Non-Patent Citations (3)

* 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]py razin-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, no. 1, 13 January 2005 (2005-01-13), pages 141 - 151, XP002557878, ISSN: 0022-2623, [retrieved on 20041213], DOI: 10.1021/JM0493156 *
KIM ET AL: "Triazolopiperazine-amides as dipeptidyl peptidase IV inhibitors: Close analogs of JANUVIA(TM) (sitagliptin phosphate)", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, PERGAMON, ELSEVIER SCIENCE, GB, vol. 17, no. 12, 15 June 2007 (2007-06-15), pages 3373 - 3377, XP022097786, ISSN: 0960-894X, DOI: 10.1016/J.BMCL.2007.03.098 *
ROLF PAUL ET AL: "N,N'-Carbonyldiimidazole, a new peptide forming reagent", JOURNAL OF THE AMERICAN CHEMICAL SOCIETY, AMERICAN CHEMICAL SOCIETY, WASHINGTON, DC; US, vol. 82, no. 5, 1 January 1960 (1960-01-01), pages 4596 - 4600, XP002202500, ISSN: 0002-7863, DOI: 10.1021/JA01502A038 *

Also Published As

Publication number Publication date
WO2012035549A2 (fr) 2012-03-22
AR082971A1 (es) 2013-01-23
IN2010DE02164A (fr) 2015-07-24

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