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WO2004080958A3 - Procede pour preparer des tetrahydrotriazolopyrazines et leurs produits intermediaires - Google Patents

Procede pour preparer des tetrahydrotriazolopyrazines et leurs produits intermediaires Download PDF

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Publication number
WO2004080958A3
WO2004080958A3 PCT/US2004/006429 US2004006429W WO2004080958A3 WO 2004080958 A3 WO2004080958 A3 WO 2004080958A3 US 2004006429 W US2004006429 W US 2004006429W WO 2004080958 A3 WO2004080958 A3 WO 2004080958A3
Authority
WO
WIPO (PCT)
Prior art keywords
tetrahydrotriazolopyrazines
intermediates
useful
pyrazines
triazolo
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/US2004/006429
Other languages
English (en)
Other versions
WO2004080958A2 (fr
Inventor
Jaume Balsells
Jinchu Liu
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.)
Merck and Co Inc
Original Assignee
Merck and Co 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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of WO2004080958A2 publication Critical patent/WO2004080958A2/fr
Publication of WO2004080958A3 publication Critical patent/WO2004080958A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/04—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

L'invention concerne un nouveau procédé pour préparer des 5,6,7,8-tétrahydro[1,2,4]-triazolo[4,3-?]pyrazines substituées qui sont utilisées dans la synthèse des inhibiteurs de dipeptidyl-peptidase-IV dans le traitement du diabète de type 2. L'invention concerne également des produits intermédiaires également utilisés, obtenus lors du procédé.
PCT/US2004/006429 2003-03-07 2004-03-03 Procede pour preparer des tetrahydrotriazolopyrazines et leurs produits intermediaires Ceased WO2004080958A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US45274803P 2003-03-07 2003-03-07
US60/452,748 2003-03-07

Publications (2)

Publication Number Publication Date
WO2004080958A2 WO2004080958A2 (fr) 2004-09-23
WO2004080958A3 true WO2004080958A3 (fr) 2004-12-23

Family

ID=32990678

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2004/006429 Ceased WO2004080958A2 (fr) 2003-03-07 2004-03-03 Procede pour preparer des tetrahydrotriazolopyrazines et leurs produits intermediaires

Country Status (3)

Country Link
AR (1) AR043443A1 (fr)
TW (1) TW200500368A (fr)
WO (1) WO2004080958A2 (fr)

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7132443B2 (en) 2001-06-27 2006-11-07 Smithklinebeecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US7470700B2 (en) 2003-08-13 2008-12-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
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
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7638638B2 (en) 2003-05-14 2009-12-29 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
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
WO2007112347A1 (fr) 2006-03-28 2007-10-04 Takeda Pharmaceutical Company Limited Inhibiteurs de la dipeptidyl peptidase
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
HRP20170712T1 (hr) 2010-04-02 2017-07-28 Ogeda Sa Novi spojevi selektivnih antagonista nk-3 receptora, farmaceutski pripravak i postupci za uporabu kod poremećaja uzrokovanih nk-3 receptorima
US10065960B2 (en) 2010-04-02 2018-09-04 Ogeda Sa NK-3 receptor selective antagonist compounds, pharmaceutical composition and methods for use in NK-3 receptors mediated disorders
CN102372716A (zh) 2010-08-09 2012-03-14 江苏恒瑞医药股份有限公司 酞嗪酮类衍生物、其制备方法及其在医药上的应用
CN101973997B (zh) * 2010-09-30 2012-06-06 浙江大学 一种磷酸西他列汀侧链的制备方法
WO2013001514A1 (fr) 2011-06-29 2013-01-03 Ranbaxy Laboratories Limited Dispersions solides de sitagliptine et leurs procédés de préparation
EP2726483A1 (fr) 2011-06-30 2014-05-07 Ranbaxy Laboratories Limited Nouveaux sels de sitagliptine
DK2763992T3 (en) 2011-10-03 2016-04-25 Euroscreen Sa NOVEL CHIRAL N-acyl-5,6,7, (8-substituted) -tetrahydro [1,2,4] triazolo [4,3-a] pyrazines as selective NK-3 receptor antagonists, PHARMACEUTICAL COMPOSITION AND METHODS FOR THE use in the NK-3 receptor mediated diseases
WO2013084210A1 (fr) 2011-12-08 2013-06-13 Ranbaxy Laboratories Limited Forme amorphe de sels de sitagliptine
SG11201702368PA (en) 2014-09-25 2017-04-27 Ogeda Sa Novel chiral synthesis of n-acyl-(3-substituted)-(8-substituted)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazines
ES2638266T3 (es) 2015-10-22 2017-10-19 F.I.S.- Fabbrica Italiana Sintetici S.P.A. Procedimiento mejorado para la preparación de triazol y una de sus sales
US10047094B1 (en) 2017-02-10 2018-08-14 F.I.S.—Fabbrica Italiana Sintetici S.p.A. Process for the preparation of triazole and salt thereof
EP3424927B1 (fr) 2017-07-04 2019-04-17 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Procédé efficace de préparation de la sitagliptine au moyen d'une très efficace préparation d'acide 2,4,5-trifluorophenylacétique intermédiaire
BR112020013449A2 (pt) * 2018-01-09 2020-12-01 Jiangsu Hengrui Medicine Co., Ltd. métodos de preparação de um inibidor de parp e de um intermediário do mesmo e método de purificação de um intermediário
EP3524605B1 (fr) 2018-02-13 2019-11-27 F.I.S.- Fabbrica Italiana Sintetici S.p.A. Nouveau procédé efficace pour la préparation de sitagliptine

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH06128261A (ja) * 1992-10-20 1994-05-10 Toray Ind Inc ３環性トリアゾロ誘導体の製造方法
WO2003004498A1 (fr) * 2001-07-06 2003-01-16 Merck & Co., Inc. Pyrazines beta-amino tetrahydroimidazo (1, 2-a) et pyrazines tetrahydrotrioazolo (4, 3-a) utilisees en tant qu'inhibiteurs de la dipeptidyl peptidase dans le traitement ou la prevention du diabete
WO2004021984A2 (fr) * 2002-09-04 2004-03-18 Bristol-Myers Squibb Company Composes aromatiques heterocycliques utiles en tant que secretagogues d'hormone de croissance

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPH06128261A (ja) * 1992-10-20 1994-05-10 Toray Ind Inc ３環性トリアゾロ誘導体の製造方法
WO2003004498A1 (fr) * 2001-07-06 2003-01-16 Merck & Co., Inc. Pyrazines beta-amino tetrahydroimidazo (1, 2-a) et pyrazines tetrahydrotrioazolo (4, 3-a) utilisees en tant qu'inhibiteurs de la dipeptidyl peptidase dans le traitement ou la prevention du diabete
WO2004021984A2 (fr) * 2002-09-04 2004-03-18 Bristol-Myers Squibb Company Composes aromatiques heterocycliques utiles en tant que secretagogues d'hormone de croissance

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
GARY A. MCCORT, JEAN CLAUDE PASCAL: "A rapid and Efficient Synthesis of Imidazo[1,2-a] and 1,2,4-Triazolo[4,3-a]-piperazine Carboxylic Acids", TETRAHEDRON LETTERS, vol. 33, no. 31, 1992, GB, pages 4443 - 4446, XP002295787 *
P.J. NELSON, K.T. POTTS: "1,2,4-Triazoles VI. The Synthesis of Some s-Triazolo[4,3-a]pyrazines", JOURNAL OF ORGANIC CHEMISTRY, AMERICAN CHEMICAL SOCIETY. EASTON, US, vol. 27, 1962, pages 3243 - 3248, XP002295788, ISSN: 0022-3263 *
PATENT ABSTRACTS OF JAPAN vol. 0184, no. 27 (C - 1235) 10 August 1994 (1994-08-10) *

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7132443B2 (en) 2001-06-27 2006-11-07 Smithklinebeecham Corporation Fluoropyrrolidines as dipeptidyl peptidase inhibitors
US7550590B2 (en) 2003-03-25 2009-06-23 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7470700B2 (en) 2003-08-13 2008-12-30 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
US7579357B2 (en) 2003-08-13 2009-08-25 Takeda Pharmaceutical Company Limited Dipeptidyl peptidase inhibitors
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

Also Published As

Publication number Publication date
TW200500368A (en) 2005-01-01
AR043443A1 (es) 2005-07-27
WO2004080958A2 (fr) 2004-09-23

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