WO1998024780A3 - Substituted pyrimidinone and pyridinone compounds and their use - Google Patents

Substituted pyrimidinone and pyridinone compounds and their use Download PDF

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Publication number
WO1998024780A3
WO1998024780A3 PCT/US1997/022949 US9722949W WO9824780A3 WO 1998024780 A3 WO1998024780 A3 WO 1998024780A3 US 9722949 W US9722949 W US 9722949W WO 9824780 A3 WO9824780 A3 WO 9824780A3
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WO
WIPO (PCT)
Prior art keywords
compounds
diseases
substituted pyrimidinone
maladies
prophylaxis
Prior art date
Application number
PCT/US1997/022949
Other languages
French (fr)
Other versions
WO1998024780A2 (en
Inventor
Ulrike D Spohr
Michael J Malone
Nathan B Mantlo
Jeff A Zablocki
Original Assignee
Amgen Inc
Ulrike D Spohr
Michael J Malone
Nathan B Mantlo
Jeff A Zablocki
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 Amgen Inc, Ulrike D Spohr, Michael J Malone, Nathan B Mantlo, Jeff A Zablocki filed Critical Amgen Inc
Priority to NZ335992A priority Critical patent/NZ335992A/en
Priority to IL13018197A priority patent/IL130181A0/en
Priority to BR9713863-0A priority patent/BR9713863A/en
Priority to HU0001140A priority patent/HUP0001140A3/en
Priority to AU55254/98A priority patent/AU735901C/en
Priority to KR10-1999-7005022A priority patent/KR100476586B1/en
Priority to JP52590298A priority patent/JP2002514196A/en
Priority to CA002274093A priority patent/CA2274093C/en
Priority to EP97951678A priority patent/EP0948496A2/en
Publication of WO1998024780A2 publication Critical patent/WO1998024780A2/en
Publication of WO1998024780A3 publication Critical patent/WO1998024780A3/en

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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    • A61P19/00—Drugs for skeletal disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • 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
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/64—One oxygen atom attached in position 2 or 6
    • C07D213/643—2-Phenoxypyridines; Derivatives thereof
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
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    • 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

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  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Endocrinology (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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Abstract

Selected novel substituted pyrimidinone and pyridone compounds are effective for prophylaxis and treatment of diseases, such as TNF-α, IL-1β, IL-6 and/or IL-8 mediated diseases, and other maladies, such as pain and diabetes. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving inflammation, pain, diabetes and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
PCT/US1997/022949 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridinone compounds and their use WO1998024780A2 (en)

Priority Applications (9)

Application Number Priority Date Filing Date Title
NZ335992A NZ335992A (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use
IL13018197A IL130181A0 (en) 1996-12-05 1997-12-04 Substituted pyrimidone and pyridone compounds and methods of use
BR9713863-0A BR9713863A (en) 1996-12-05 1997-12-04 Compound or a pharmaceutically acceptable salt thereof, pharmaceutical composition, prophylaxis or treatment processes, to lower plasma concentrations, to decrease prostaglandin production, and to decrease cyclooxygenase enzyme activity
HU0001140A HUP0001140A3 (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use
AU55254/98A AU735901C (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use
KR10-1999-7005022A KR100476586B1 (en) 1996-12-05 1997-12-04 Substituted pyrimidinone compound, pharmaceutical composition comprising such compound and method for treatment
JP52590298A JP2002514196A (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use
CA002274093A CA2274093C (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridinone compounds and their use
EP97951678A EP0948496A2 (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US3212896P 1996-12-05 1996-12-05
US60/032,128 1996-12-05
US5095097P 1997-06-13 1997-06-13
US60/050,950 1997-06-13
US97605397A 1997-11-21 1997-11-21
US08/976,053 1997-11-21

Publications (2)

Publication Number Publication Date
WO1998024780A2 WO1998024780A2 (en) 1998-06-11
WO1998024780A3 true WO1998024780A3 (en) 1998-07-30

Family

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Application Number Title Priority Date Filing Date
PCT/US1997/022949 WO1998024780A2 (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridinone compounds and their use

Country Status (13)

Country Link
EP (1) EP0948496A2 (en)
JP (1) JP2002514196A (en)
KR (1) KR100476586B1 (en)
CN (1) CN1328277C (en)
AU (1) AU735901C (en)
BG (1) BG65129B1 (en)
BR (1) BR9713863A (en)
CA (1) CA2274093C (en)
CZ (1) CZ9902016A3 (en)
HU (1) HUP0001140A3 (en)
IL (1) IL130181A0 (en)
NZ (1) NZ335992A (en)
WO (1) WO1998024780A2 (en)

Cited By (13)

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US8691813B2 (en) 2008-11-28 2014-04-08 Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
US8691849B2 (en) 2008-09-02 2014-04-08 Janssen Pharmaceuticals, Inc. 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
US8841323B2 (en) 2006-03-15 2014-09-23 Janssen Pharmaceuticals, Inc. 1, 4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of MGLUR2-receptors
US8906901B2 (en) 2005-09-14 2014-12-09 Takeda Pharmaceutical Company Limited Administration of dipeptidyl peptidase inhibitors
US8906939B2 (en) 2007-03-07 2014-12-09 Janssen Pharmaceuticals, Inc. 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
US8937060B2 (en) 2009-05-12 2015-01-20 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo [4,3-A] pyridine derivatives and their use for the treatment of prevention of neurological and psychiatric disorders
US8946205B2 (en) 2009-05-12 2015-02-03 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
US8993591B2 (en) 2010-11-08 2015-03-31 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a] pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
US9012448B2 (en) 2010-11-08 2015-04-21 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of MGLUR2 receptors
US9085577B2 (en) 2009-05-12 2015-07-21 Janssen Pharmaceuticals, Inc. 7-aryl-1,2,4-triazolo[4,3-A]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
US9114138B2 (en) 2007-09-14 2015-08-25 Janssen Pharmaceuticals, Inc. 1′,3′-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2H,1′H-[1,4′] bipyridinyl-2′-ones
US9271967B2 (en) 2010-11-08 2016-03-01 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
US11993580B1 (en) 2023-12-01 2024-05-28 Neumora Therapeutics, Inc. Methods of treating neurological disorders

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US6410729B1 (en) * 1996-12-05 2002-06-25 Amgen Inc. Substituted pyrimidine compounds and methods of use
US6613942B1 (en) 1997-07-01 2003-09-02 Novo Nordisk A/S Glucagon antagonists/inverse agonists
US6335340B1 (en) 1997-12-19 2002-01-01 Smithkline Beecham Corporation compounds of heteroaryl substituted imidazole, their pharmaceutical compositons and uses
US6858617B2 (en) 1998-05-26 2005-02-22 Smithkline Beecham Corporation Substituted imidazole compounds
TWI241298B (en) * 1998-09-25 2005-10-11 Mitsubishi Chem Corp Pyrimidone derivatives
EP1126852B1 (en) 1998-11-04 2004-01-21 SmithKline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
GB9910378D0 (en) * 1999-05-05 1999-06-30 Smithkline Beecham Plc Novel compounds
US6503949B1 (en) 1999-05-17 2003-01-07 Noro Nordisk A/S Glucagon antagonists/inverse agonists
US6403596B1 (en) 1999-06-28 2002-06-11 Merck & Co., Inc. Substituted pyridones having cytokine inhibitory activity
ES2249309T3 (en) 1999-11-23 2006-04-01 Smithkline Beecham Corp COMPOUNDS OF 3,4-DIHIDRO- (1H) QUINAZOLIN-2-ONA AS INHIBITORS OF CSBP / P39 KINASA.
WO2001038314A1 (en) 1999-11-23 2001-05-31 Smithkline Beecham Corporation 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p38 kinase inhibitors
US6759410B1 (en) 1999-11-23 2004-07-06 Smithline Beecham Corporation 3,4-dihydro-(1H)-quinazolin-2-ones and their use as CSBP/p38 kinase inhibitors
EP1136099A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-(Indolylalkylamino)pyrimidone derivatives as GSK3beta inhibitors
EP1136482A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
EP1136493A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-(Thienopyridinyl)pyrimidone, 2-(furopyridinyl)pyrimidone 2-(isoquinolinyl)pyrimidone, 2-(pyridoindolyl)pyrimidone and 2-(benzofuropyridinyl)pyrimidone derivatives
JP2005289808A (en) * 2000-03-23 2005-10-20 Sanofi-Aventis 3-substituted-4-pyrimidone derivative
KR100782091B1 (en) 2000-04-26 2007-12-04 에자이 알앤드디 매니지먼트 가부시키가이샤 Medicinal compositions promoting bowel movement
NZ522773A (en) 2000-06-12 2005-06-24 Eisai Co Ltd 1,2-dihydropyridine compounds, manufacturing method thereof and use thereof
DE60117839T2 (en) * 2000-09-19 2006-11-23 Institut Curie PYRIDINONE AND PYRIDINETHION DERIVATIVES WITH HIV-INHIBITORY PROPERTIES
GB0024808D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
JP2004513935A (en) 2000-11-17 2004-05-13 ノボ　ノルディスク　アクティーゼルスカブ Glucagon antagonist / inverse agonist
US6706744B2 (en) 2000-11-17 2004-03-16 Novo Nordisk A/S Glucagon antagonists/inverse agonists
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