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WO2008109681A3 - Procédés et intermédiaires pour la synthèse d'inhibiteurs sélectifs de dpp-iv - Google Patents

Procédés et intermédiaires pour la synthèse d'inhibiteurs sélectifs de dpp-iv Download PDF

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Publication number
WO2008109681A3
WO2008109681A3 PCT/US2008/055927 US2008055927W WO2008109681A3 WO 2008109681 A3 WO2008109681 A3 WO 2008109681A3 US 2008055927 W US2008055927 W US 2008055927W WO 2008109681 A3 WO2008109681 A3 WO 2008109681A3
Authority
WO
WIPO (PCT)
Prior art keywords
intermediates
synthesis
methods
inhibitors
dpp
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/US2008/055927
Other languages
English (en)
Other versions
WO2008109681A2 (fr
Inventor
David Alan Campbell
Emilia P T Leitao
Zhen-Ping Wu
Peng Wang
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.)
Phenomix Corp
Original Assignee
Phenomix Corp
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 Phenomix Corp filed Critical Phenomix Corp
Priority to CA002680133A priority Critical patent/CA2680133A1/fr
Priority to US12/529,016 priority patent/US20100087658A1/en
Priority to EP08743692A priority patent/EP2173709A2/fr
Priority to CN200880015066A priority patent/CN101679238A/zh
Priority to MX2009009575A priority patent/MX2009009575A/es
Publication of WO2008109681A2 publication Critical patent/WO2008109681A2/fr
Publication of WO2008109681A3 publication Critical patent/WO2008109681A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds
    • 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
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no 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
    • C07D207/14—Nitrogen atoms not forming part of a nitro radical

Landscapes

  • 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)
  • Pyrrole Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

L'invention concerne des procédés et des intermédiaires pour la synthèse d'inhibiteurs sélectifs de la dipeptidyle peptidase IV (DPP-IV). Le couplage d'un sel de carboxylate avec un dérivé de boro-proline fournit une forme protégée d'un inhibiteur de DPP-IV, qui peut être débloquée pour obtenir le composé médicinal. Le sel de carboxylate peut être une forme cristalline d'un sel de sodium ou d'un sel de dicyclohexylammonium. L'inhibiteur peut être utilisé pour le traitement du diabète.
PCT/US2008/055927 1996-08-06 2008-03-05 Procédés et intermédiaires pour la synthèse d'inhibiteurs sélectifs de dpp-iv Ceased WO2008109681A2 (fr)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CA002680133A CA2680133A1 (fr) 2007-03-08 2008-03-05 Procedes et intermediaires pour la synthese d'inhibiteurs selectifs de dpp-iv
US12/529,016 US20100087658A1 (en) 1996-08-06 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors
EP08743692A EP2173709A2 (fr) 2007-03-08 2008-03-05 Procédés et intermédiaires pour la synthèse d'inhibiteurs sélectifs de dpp-iv
CN200880015066A CN101679238A (zh) 2007-03-08 2008-03-05 用于合成选择性dpp-iv抑制剂的方法和中间体
MX2009009575A MX2009009575A (es) 2007-03-08 2008-03-05 Metodos e intemediarios para la sintesis de inhibidores selectivos de dpp-iv.

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
US89384207P 2007-03-08 2007-03-08
US60/893,842 2007-03-08
US95922607P 2007-07-12 2007-07-12
US60/959,226 2007-07-12
US2348708P 2008-01-25 2008-01-25
US61/023,487 2008-01-25
US2950608P 2008-02-18 2008-02-18
US61/029,506 2008-02-18

Publications (2)

Publication Number Publication Date
WO2008109681A2 WO2008109681A2 (fr) 2008-09-12
WO2008109681A3 true WO2008109681A3 (fr) 2008-11-13

Family

ID=39711954

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/055927 Ceased WO2008109681A2 (fr) 1996-08-06 2008-03-05 Procédés et intermédiaires pour la synthèse d'inhibiteurs sélectifs de dpp-iv

Country Status (7)

Country Link
EP (1) EP2173709A2 (fr)
CN (1) CN101679238A (fr)
AR (1) AR065666A1 (fr)
CA (1) CA2680133A1 (fr)
MX (1) MX2009009575A (fr)
TW (1) TW200843784A (fr)
WO (1) WO2008109681A2 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7786312B2 (en) 2005-08-01 2010-08-31 Phenomix Corporation Methods of preparing heterocyclic boronic acids and derivatives thereof

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CL2007002499A1 (es) 2006-08-30 2008-03-14 Phenomix Corp Sales citrato y tartrato de compuestos derivados de acido pirrolidinilaminoacetilpirrolidinboronico, inhibidores de dpp-iv; metodo de preparacion; forma solida; combinacion farmaceutica, util para el tratamiento de diabetes.
UY32030A (es) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "tratamiento para diabetes en pacientes inapropiados para terapia con metformina"
MX370599B (es) 2008-08-15 2019-12-18 Boehringer Ingelheim Int Derivados de purina para su uso en el tratamiento de enfermedades relacionadas con fab.
AR074990A1 (es) 2009-01-07 2011-03-02 Boehringer Ingelheim Int Tratamiento de diabetes en pacientes con un control glucemico inadecuado a pesar de la terapia con metformina
AR075204A1 (es) 2009-01-29 2011-03-16 Boehringer Ingelheim Int Inhibidores de dpp-4 y composiciones farmaceuticas que los comprenden, utiles para tratar enfermedades metabolicas en pacientes pediatricos, particularmente diabetes mellitus tipo 2
JP2012517977A (ja) 2009-02-13 2012-08-09 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング Ｄｐｐ−４阻害剤（リナグリプチン）を任意で他の抗糖尿病薬と組み合わせて含む抗糖尿病薬
EP2504002B1 (fr) 2009-11-27 2019-10-09 Boehringer Ingelheim International GmbH Traitement de patients diabétiques génotypés par des inhibiteurs de dpp-iv tels que la linagliptine
JP2013522279A (ja) 2010-03-18 2013-06-13 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 糖尿病及び関連状態の治療で用いるｇｐｒ１１９作動薬とｄｄｐ−ｉｖ阻害薬リナグリプチンの組合せ
AU2011249722B2 (en) 2010-05-05 2015-09-17 Boehringer Ingelheim International Gmbh Combination therapy
ES2802243T3 (es) 2010-06-24 2021-01-18 Boehringer Ingelheim Int Terapia para la diabetes
WO2013174767A1 (fr) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh Dérivé de xanthine en tant qu'inhibiteur de la dpp-4 à utiliser dans la modification de l'apport alimentaire et dans la régulation des préférences alimentaires
CN111533675B (zh) * 2019-11-29 2021-09-28 杭州华东医药集团新药研究院有限公司 杂环硼酸化合物的杂质及其控制方法

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060264400A1 (en) * 2003-11-12 2006-11-23 Campbell David A Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-iv
WO2007016356A1 (fr) * 2005-08-01 2007-02-08 Phenomix Corporation Procedes de preparation d'acides boroniques heterocycliques et de derives de ceux-ci

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20060264400A1 (en) * 2003-11-12 2006-11-23 Campbell David A Pyrrolidine compounds and methods for selective inhibition of dipeptidyl peptidase-iv
WO2007016356A1 (fr) * 2005-08-01 2007-02-08 Phenomix Corporation Procedes de preparation d'acides boroniques heterocycliques et de derives de ceux-ci

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7786312B2 (en) 2005-08-01 2010-08-31 Phenomix Corporation Methods of preparing heterocyclic boronic acids and derivatives thereof

Also Published As

Publication number Publication date
EP2173709A2 (fr) 2010-04-14
TW200843784A (en) 2008-11-16
AR065666A1 (es) 2009-06-24
WO2008109681A2 (fr) 2008-09-12
MX2009009575A (es) 2009-11-12
CN101679238A (zh) 2010-03-24
CA2680133A1 (fr) 2008-09-12

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