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WO2005058845A3 - Novel glucagon antagonists/inverse agonists - Google Patents

Novel glucagon antagonists/inverse agonists Download PDF

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Publication number
WO2005058845A3
WO2005058845A3 PCT/EP2004/053580 EP2004053580W WO2005058845A3 WO 2005058845 A3 WO2005058845 A3 WO 2005058845A3 EP 2004053580 W EP2004053580 W EP 2004053580W WO 2005058845 A3 WO2005058845 A3 WO 2005058845A3
Authority
WO
WIPO (PCT)
Prior art keywords
alkyl
aryl
cycloalkenyl
heteroaryl
cycloalkyl
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/EP2004/053580
Other languages
French (fr)
Other versions
WO2005058845A2 (en
Inventor
Peter Madsen
Jesper Lau
Janos Tibor Kodra
Inge Thoeger Christensen
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.)
Novo Nordisk AS
Original Assignee
Novo Nordisk AS
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 Novo Nordisk AS filed Critical Novo Nordisk AS
Publication of WO2005058845A2 publication Critical patent/WO2005058845A2/en
Publication of WO2005058845A3 publication Critical patent/WO2005058845A3/en
Priority to US11/424,871 priority Critical patent/US20070015757A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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
    • C07D207/30—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 two double bonds between ring members or between ring members and non-ring members
    • C07D207/32—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D207/323—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 two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with only hydrogen atoms or radicals containing only hydrogen and carbon atoms directly attached to the 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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • 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
    • C07D233/96—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Obesity (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists. (I) wherein A is (II), (III) or (IV), Y is a valence bond, >C=O, =CR1-, -(CR1R2)m-, -NR1-,=N-, E is: C1-10-alkyl or C2-10-alkenyl; C3-10-cycloalkyl, C3-10-cycloalkenyl, C7-10-bicycloalkyl, C3-10-cycloakyl-C1-6-alkyl, C3-10-cycloalkenyl-C1-6-alkyl or C7-10-bicycloalkyl-C1-6-alkyl, wherein the rings may optionally be substituted with one or more substituents selected from halogen, C1-6-alkyl, C2-6-alkenyl, C1-6-alkoxy, C1-6-thioalkyl, -CF3, -OCF3, -SCF3, -OCHF2 and -SCHF2; aryl, aryloxy, arylthio, heteroaryl, aryl-C1-6-alkyl, aryloxy-C1-6-alkyl, arylthio-C1-6-alkyl, heteroaryl-C1-6-alkyl, diaryl-C1-6-alkyl or (C1-6 -alkyl)(aryl)-C1-7-alkyl, wherein the non-aromatic and aromatic rings may optinally be substituted with one or more substituents selected from halogen, C1-6-alkyl, C2-6-alkenyl, C1-6 -alkoxy, C1-6-thioalkyl, -CF3, -OCF3, -SCF3, -OCHF2, SCHF2, C3-10-cycloalkyl and C3-10-cycloalkenyl, or with two substituents on adjacent positions which are combined to form a bridge C1-6-alkylene, C2-6-alkenylene or -O-C1-6-alkylene-O-; (V) represents a phenyl, C3-8-cycloalkyl, or a 4-, 5-, 6- or 7-membered heterocycle, D is aryl or heteroaryl.
PCT/EP2004/053580 2003-12-19 2004-12-17 Novel glucagon antagonists/inverse agonists Ceased WO2005058845A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
US11/424,871 US20070015757A1 (en) 2003-12-19 2006-06-18 Novel Glucagon Antagonists/Inverse Agonists

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DKPA200301894 2003-12-19
DKPA200301894 2003-12-19

Related Child Applications (1)

Application Number Title Priority Date Filing Date
US11/424,871 Continuation US20070015757A1 (en) 2003-12-19 2006-06-18 Novel Glucagon Antagonists/Inverse Agonists

Publications (2)

Publication Number Publication Date
WO2005058845A2 WO2005058845A2 (en) 2005-06-30
WO2005058845A3 true WO2005058845A3 (en) 2005-10-20

Family

ID=34684453

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2004/053580 Ceased WO2005058845A2 (en) 2003-12-19 2004-12-17 Novel glucagon antagonists/inverse agonists

Country Status (1)

Country Link
WO (1) WO2005058845A2 (en)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007530598A (en) * 2004-03-26 2007-11-01 サイトカイン・ファーマサイエンシズ・インコーポレーテッド COMPOUND, COMPOSITION, MAKING PROCESS AND METHOD OF USE FOR INHIBITION OF MACROPHAGE MIGRATION INHIBITOR
WO2007111864A2 (en) 2006-03-23 2007-10-04 Merck & Co., Inc. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
WO2007136577A2 (en) 2006-05-16 2007-11-29 Merck & Co., Inc. Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
HUE035130T2 (en) 2007-09-10 2018-05-02 Janssen Pharmaceutica Nv Process for the preparation of compounds useful as inhibitors of sglt
EP2913326B1 (en) * 2008-05-14 2020-07-15 The Scripps Research Institute Novel modulators of sphingosine phosphate receptors
AR073412A1 (en) 2008-10-03 2010-11-03 Schering Corp DERIVATIVES OF ESPIRO IMIDAZOLONA AS ANTAGONISTS OF THE GLUCAGON RECEIVER AND COMPOSITIONS THAT UNDERSTAND THEM.
US9056850B2 (en) 2008-10-17 2015-06-16 Janssen Pharmaceutica N.V. Process for the preparation of compounds useful as inhibitors of SGLT
US20110009347A1 (en) 2009-07-08 2011-01-13 Yin Liang Combination therapy for the treatment of diabetes
WO2011003976A1 (en) 2009-07-10 2011-01-13 Janssen Pharmaceutica Nv CRYSTALLISATION PROCESS FOR 1-(ß-D-GLUCOPYRANOSYL)-4-METHYL-3-[5-(4-FLUOROPHENYL)-2-THIENYLMETHYL] BENZENE
HRP20170446T1 (en) 2009-10-14 2017-05-19 Janssen Pharmaceutica Nv Process for the preparation of compounds useful as inhibitors of sglt2
AR081036A1 (en) 2010-05-11 2012-05-30 Janssen Pharmaceutica Nv PHARMACEUTICAL FORMULATIONS TO TREAT DISEASES RELATED TO THE TRANSPORTER OF GLUCOSE DEPENDENT SODIUM
KR101778617B1 (en) * 2010-11-30 2017-09-15 에스케이유화 주식회사 Method for Producing Methyl-4-hydroxyiminomethylbenzoate
RU2013127611A (en) 2010-12-23 2015-01-27 Пфайзер Инк. Glucagon receptor modulators
MX2013009140A (en) 2011-02-08 2013-10-01 Pfizer Glucagon receptor modulator.
KR101913587B1 (en) 2011-04-13 2018-10-31 얀센 파마슈티카 엔.브이. Process for the preparation of compounds useful as inhibitors of sglt2
TWI542596B (en) 2011-05-09 2016-07-21 健生藥品公司 (2S,3R,4R,5S,6R)-2-(3-((5-(4-fluorophenyl)thiophen-2-yl)methyl)-4-methylphenyl)-6-(hydroxyl L-proline and citric acid cocrystals of methyl)tetrahydro-2H-piperan-3,4,5-triol
RU2013157388A (en) 2011-07-22 2015-08-27 Пфайзер Инк. QUINOLINYL MODULATORS OF THE GLUCAGON RECEPTOR
US20170071970A1 (en) 2015-09-15 2017-03-16 Janssen Pharmaceutica Nv Co-therapy comprising canagliflozin and phentermine for the treatment of obesity and obesity related disorders

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002000612A1 (en) * 2000-06-23 2002-01-03 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO2002040444A1 (en) * 2000-11-17 2002-05-23 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO2002040446A1 (en) * 2000-11-17 2002-05-23 Novo Nordisk A/S Glucagon antagonist/inverse agonist
WO2004056763A2 (en) * 2002-12-20 2004-07-08 Novo Nordisk A/S Novel glucagon antagonists
US20040209928A1 (en) * 2002-12-30 2004-10-21 Ravi Kurukulasuriya Glucagon receptor antagonists/inverse agonists

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002000612A1 (en) * 2000-06-23 2002-01-03 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO2002040444A1 (en) * 2000-11-17 2002-05-23 Novo Nordisk A/S Glucagon antagonists/inverse agonists
WO2002040446A1 (en) * 2000-11-17 2002-05-23 Novo Nordisk A/S Glucagon antagonist/inverse agonist
WO2004056763A2 (en) * 2002-12-20 2004-07-08 Novo Nordisk A/S Novel glucagon antagonists
US20040209928A1 (en) * 2002-12-30 2004-10-21 Ravi Kurukulasuriya Glucagon receptor antagonists/inverse agonists

Also Published As

Publication number Publication date
WO2005058845A2 (en) 2005-06-30

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