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WO2008109681A3 - Methods and intermediates for synthesis of selective dpp-iv inhibitors - Google Patents

Methods and intermediates for synthesis of selective dpp-iv inhibitors Download PDF

Info

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
French (fr)
Other versions
WO2008109681A2 (en
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/en
Priority to US12/529,016 priority patent/US20100087658A1/en
Priority to EP08743692A priority patent/EP2173709A2/en
Priority to CN200880015066A priority patent/CN101679238A/en
Priority to MX2009009575A priority patent/MX2009009575A/en
Publication of WO2008109681A2 publication Critical patent/WO2008109681A2/en
Publication of WO2008109681A3 publication Critical patent/WO2008109681A3/en
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

Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.
PCT/US2008/055927 1996-08-06 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors Ceased WO2008109681A2 (en)

Priority Applications (5)

Application Number Priority Date Filing Date Title
CA002680133A CA2680133A1 (en) 2007-03-08 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors
US12/529,016 US20100087658A1 (en) 1996-08-06 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors
EP08743692A EP2173709A2 (en) 2007-03-08 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors
CN200880015066A CN101679238A (en) 2007-03-08 2008-03-05 methods and intermediates for synthesis of selective dpp-iv inhibitors
MX2009009575A MX2009009575A (en) 2007-03-08 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors.

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 (en) 2008-09-12
WO2008109681A3 true WO2008109681A3 (en) 2008-11-13

Family

ID=39711954

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2008/055927 Ceased WO2008109681A2 (en) 1996-08-06 2008-03-05 Methods and intermediates for synthesis of selective dpp-iv inhibitors

Country Status (7)

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

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 (en) 2006-08-30 2008-03-14 Phenomix Corp SALES CITRATE AND TARTRATE OF COMPOUNDS DERIVED FROM PIRROLIDINILAMINOACETILPIRROLIDINBORONICO ACID, DPP-IV INHIBITORS; PREPARATION METHOD; SOLID FORM; PHARMACEUTICAL COMBINATION, USEFUL FOR THE TREATMENT OF DIABETES.
UY32030A (en) 2008-08-06 2010-03-26 Boehringer Ingelheim Int "TREATMENT FOR DIABETES IN INAPPROPRIATE PATIENTS FOR THERAPY WITH METFORMIN"
MX370599B (en) 2008-08-15 2019-12-18 Boehringer Ingelheim Int Purin derivatives for use in the treatment of fab-related diseases.
AR074990A1 (en) 2009-01-07 2011-03-02 Boehringer Ingelheim Int TREATMENT OF DIABETES IN PATIENTS WITH AN INAPPROPRIATE GLUCEMIC CONTROL THROUGH METFORMIN THERAPY
AR075204A1 (en) 2009-01-29 2011-03-16 Boehringer Ingelheim Int DPP-4 INHIBITORS AND PHARMACEUTICAL COMPOSITIONS THAT INCLUDE THEM, USEFUL TO TREAT METABOLIC DISEASES IN PEDIATRIC PATIENTS, PARTICULARLY MELLITUS DIABETES TYPE 2
JP2012517977A (en) 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 An anti-diabetic drug comprising a DPP-4 inhibitor (linagliptin) optionally in combination with other anti-diabetic drugs
EP2504002B1 (en) 2009-11-27 2019-10-09 Boehringer Ingelheim International GmbH Treatment of genotyped diabetic patients with dpp-iv inhibitors such as linagliptin
JP2013522279A (en) 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 Combination of GPR119 agonist and DDP-IV inhibitor linagliptin for use in the treatment of diabetes and related conditions
AU2011249722B2 (en) 2010-05-05 2015-09-17 Boehringer Ingelheim International Gmbh Combination therapy
ES2802243T3 (en) 2010-06-24 2021-01-18 Boehringer Ingelheim Int Diabetes therapy
WO2013174767A1 (en) 2012-05-24 2013-11-28 Boehringer Ingelheim International Gmbh A xanthine derivative as dpp -4 inhibitor for use in modifying food intake and regulating food preference
CN111533675B (en) * 2019-11-29 2021-09-28 杭州华东医药集团新药研究院有限公司 Impurities of heterocyclic boronic acid compounds and methods of controlling the same

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 (en) * 2005-08-01 2007-02-08 Phenomix Corporation Methods of preparing hetercyclic boronic acids and derivatives thereof

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 (en) * 2005-08-01 2007-02-08 Phenomix Corporation Methods of preparing hetercyclic boronic acids and derivatives thereof

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 (en) 2010-04-14
TW200843784A (en) 2008-11-16
AR065666A1 (en) 2009-06-24
WO2008109681A2 (en) 2008-09-12
MX2009009575A (en) 2009-11-12
CN101679238A (en) 2010-03-24
CA2680133A1 (en) 2008-09-12

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