WO2005082348A3 - Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism - Google Patents

Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism Download PDF

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Publication number
WO2005082348A3
WO2005082348A3 PCT/US2005/006128 US2005006128W WO2005082348A3 WO 2005082348 A3 WO2005082348 A3 WO 2005082348A3 US 2005006128 W US2005006128 W US 2005006128W WO 2005082348 A3 WO2005082348 A3 WO 2005082348A3
Authority
WO
WIPO (PCT)
Prior art keywords
inhibitors
present
dipeptidylpeptidase
glucose metabolism
regulating glucose
Prior art date
Application number
PCT/US2005/006128
Other languages
French (fr)
Other versions
WO2005082348A2 (en
Inventor
William W Bachovchin
Hung-Sen Lai
Wengen Wu
Original Assignee
Tufts College
William W Bachovchin
Hung-Sen Lai
Wengen Wu
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
Priority to RU2006133899/04A priority Critical patent/RU2379315C2/en
Priority to JP2007501012A priority patent/JP4781347B2/en
Priority to AU2005216970A priority patent/AU2005216970B2/en
Priority to BRPI0507972-1A priority patent/BRPI0507972A/en
Application filed by Tufts College, William W Bachovchin, Hung-Sen Lai, Wengen Wu filed Critical Tufts College
Priority to EP05723831A priority patent/EP1729757A2/en
Priority to KR1020137002340A priority patent/KR20130016435A/en
Priority to CA002558106A priority patent/CA2558106A1/en
Priority to KR1020067019660A priority patent/KR101292707B1/en
Priority to CN200580011588XA priority patent/CN1942182B/en
Priority to MXPA06009589A priority patent/MXPA06009589A/en
Publication of WO2005082348A2 publication Critical patent/WO2005082348A2/en
Publication of WO2005082348A3 publication Critical patent/WO2005082348A3/en
Priority to IL177644A priority patent/IL177644A0/en
Priority to NO20064307A priority patent/NO20064307L/en
Priority to IL217853A priority patent/IL217853A0/en

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • A61K31/19Carboxylic acids, e.g. valproic acid
    • A61K31/195Carboxylic acids, e.g. valproic acid having an amino group
    • A61K31/197Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid, pantothenic acid
    • A61K31/198Alpha-aminoacids, e.g. alanine, edetic acids [EDTA]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/69Boron compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F5/00Compounds containing elements of Groups 3 or 13 of the Periodic System
    • C07F5/02Boron compounds
    • C07F5/025Boronic and borinic acid compounds

Abstract

The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods of using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.
PCT/US2005/006128 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism WO2005082348A2 (en)

Priority Applications (13)

Application Number Priority Date Filing Date Title
KR1020137002340A KR20130016435A (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv
AU2005216970A AU2005216970B2 (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism
BRPI0507972-1A BRPI0507972A (en) 2004-02-23 2005-02-23 compound, pharmaceutical composition, use of a compound, method for inhibiting the proteolytic activity of a postproline cleavage enzyme and packaged pharmaceutical composition
KR1020067019660A KR101292707B1 (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv
EP05723831A EP1729757A2 (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism
JP2007501012A JP4781347B2 (en) 2004-02-23 2005-02-23 Peptidyl peptidase IV inhibitors for controlling glucose metabolism
CA002558106A CA2558106A1 (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism
RU2006133899/04A RU2379315C2 (en) 2004-02-23 2005-02-23 Dipeptidyl peptidase iv inhibitors
CN200580011588XA CN1942182B (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase IV for regulating glucose metabolism
MXPA06009589A MXPA06009589A (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism.
IL177644A IL177644A0 (en) 2004-02-23 2006-08-22 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism
NO20064307A NO20064307L (en) 2004-02-23 2006-09-22 Inhibitors of dipeptidyl peptidase IV for the regulation of glucose metabolism
IL217853A IL217853A0 (en) 2004-02-23 2012-01-31 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US54722704P 2004-02-23 2004-02-23
US60/547,227 2004-02-23
US59933604P 2004-08-06 2004-08-06
US60/599,336 2004-08-06

Publications (2)

Publication Number Publication Date
WO2005082348A2 WO2005082348A2 (en) 2005-09-09
WO2005082348A3 true WO2005082348A3 (en) 2005-12-29

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2005/006128 WO2005082348A2 (en) 2004-02-23 2005-02-23 Inhibitors of dipeptidylpeptidase iv for regulating glucose metabolism

Country Status (13)

Country Link
US (4) US20050203027A1 (en)
EP (1) EP1729757A2 (en)
JP (1) JP4781347B2 (en)
KR (2) KR20130016435A (en)
AU (1) AU2005216970B2 (en)
BR (1) BRPI0507972A (en)
CA (1) CA2558106A1 (en)
IL (2) IL177644A0 (en)
MX (1) MXPA06009589A (en)
NO (1) NO20064307L (en)
RU (1) RU2379315C2 (en)
TW (1) TWI382836B (en)
WO (1) WO2005082348A2 (en)

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Also Published As

Publication number Publication date
EP1729757A2 (en) 2006-12-13
WO2005082348A2 (en) 2005-09-09
US20090062235A1 (en) 2009-03-05
TWI382836B (en) 2013-01-21
US20050203027A1 (en) 2005-09-15
IL217853A0 (en) 2012-03-29
NO20064307L (en) 2006-11-15
IL177644A0 (en) 2008-04-13
AU2005216970B2 (en) 2011-07-07
JP4781347B2 (en) 2011-09-28
MXPA06009589A (en) 2007-03-26
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US20140018545A1 (en) 2014-01-16
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