HUP0001140A2 - Szubsztituált pirimidinon és piridonszármazékok, továbbá ezeket tartalmazó gyógyászati készítmények - Google Patents

Szubsztituált pirimidinon és piridonszármazékok, továbbá ezeket tartalmazó gyógyászati készítmények

Info

Publication number
HUP0001140A2
HUP0001140A2 HU0001140A HUP0001140A HUP0001140A2 HU P0001140 A2 HUP0001140 A2 HU P0001140A2 HU 0001140 A HU0001140 A HU 0001140A HU P0001140 A HUP0001140 A HU P0001140A HU P0001140 A2 HUP0001140 A2 HU P0001140A2
Authority
HU
Hungary
Prior art keywords
group
nr5r21
formula
aryl
compounds
Prior art date
Application number
HU0001140A
Other languages
English (en)
Inventor
Michael J. Malone
Nathan B. Mantlo
Ulrike D. Spohr
Jeff A. Zablocki
Original Assignee
Amgen Inc.
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. filed Critical Amgen Inc.
Publication of HUP0001140A2 publication Critical patent/HUP0001140A2/hu
Publication of HUP0001140A3 publication Critical patent/HUP0001140A3/hu

Links

Classifications

    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological 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
    • 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
    • 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
    • A61P19/06—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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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]
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • 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
    • C07D409/02—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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

Abstract

A találmány tárgyát az (I) általános képletű vegyületek, valamintezeket tartalmazó gyógyászati készítmények képezik. Az (I) általánosképletű vegyületek különböző betegségek kezelésére, mint például aTNF-a, IL-1b, IL-6 és/vagy IL-8 által közvetített betegségek vagyegyéb rendellenes állapotok, mint fájdalom és diabétesz kezeléséreadható. Még közelebbről a találmány szerinti vegyületek eredményesenalkalmazhatók gyulladással kapcsolatos betegségek és állapotokmegelőzésére és kezelésére. A találmány tárgyához tartoznak evegyületek előállítására alkalmazható közbenső termékek és eljárásokis. Az (I) általános képletben a szubsztituensek jelentése igensokféle, így például X jelentése oxigénatom, kénatom vagy -NR5, ahol a képletben az (y)-naljelzett -VC(R)W- képletű molekularész jelentése (a), (b), (c), (d),(e), (f) vagy (g) általános képletű csoport, azzal a feltétellel, hogya -VC(R)W- képletű csoportban az aril-, heteroaril-, cikloalkil- ésheterociklusos csoportok össz-száma 0-tól 3-ig terjedő egész szám; U jelentése -NR21 vagy -CHR21; és n értéke 1-től 3-ig terjedő egész szám; R3 és R4 jelentése egymástól függetlenül -Z-Y, azzal a feltétellel,hogy R4 jelentése hidrogénatomtól, szubsztituált arilcsoporttól,(szubsztituált aril)-metil-csoporttól vagy (szubsztituált aril)-etil-csoporttól eltérő, és az aril-, heteroaril-, cikloalkil- ésheterociklusos csoportok össz-száma minden egyes -Y és -Z-Y csoportban0-tól 3-ig terjedő egész szám; ahol mindegyik Z jelentése egymástólfüggetlenül (1) alkil-, alkenil- vagy alkinilcsoport, amelyek adott esetbenkülönféle csoportokkal lehetnek szubsztituálva; (2) heterociklusos csoport, amely adott esetben különféle csoportokkallehet szubsztituálva; vagy (3) aril- vagy heteroarilcsoport, amelyek adott különféle csoportokkallehetnek szubsztituálva; mindegyik Y jelentése egymástól függetlenül (1) hidrogénatom; (2) halogénatom, ciano- vagy nitrocsoport; (3) -C(O)-R20, -C(O)-OR21, -C(O)-NR5R21 vagy -C(NR5)-NR5R21 általánosképletű csoport, (4) -OR21, -O-C(O)-R21, -O-C(O)-NR5R21 vagy -O-C(O)-NR22-S(O)2-R20általános képletű csoport; (5) -SR21, -S(O)-R20, -S(O)2-R20, -S(O)2-NR5R21, -S(O)2-NR22-C(O)-R21,-S(O)2-NR22-C(O)-OR20 vagy -S(O)2-NR22-C(O)-NR5R21 általános képletűcsoport; R11 és R12 jelentése adott esetben szubsztituált aril- vagyheteroarilcsoport. Ó
HU0001140A 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use HUP0001140A3 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US3212896P 1996-12-05 1996-12-05
US5095097P 1997-06-13 1997-06-13
US97605397A 1997-11-21 1997-11-21
PCT/US1997/022949 WO1998024780A2 (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridinone compounds and their use

Publications (2)

Publication Number Publication Date
HUP0001140A2 true HUP0001140A2 (hu) 2001-04-28
HUP0001140A3 HUP0001140A3 (en) 2002-05-28

Family

ID=27364029

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0001140A HUP0001140A3 (en) 1996-12-05 1997-12-04 Substituted pyrimidinone and pyridone compounds and methods of use

Country Status (13)

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

Families Citing this family (94)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO1999032121A1 (en) 1997-12-19 1999-07-01 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositions 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
AU1909200A (en) 1998-11-04 2000-05-22 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
DE60020595T2 (de) 1999-11-23 2006-03-16 Smithkline Beecham Corp. 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
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
ATE305787T1 (de) 1999-11-23 2005-10-15 Smithkline Beecham Corp 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
EP1136482A1 (en) 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-Amino-3-(alkyl)-pyrimidone derivatives as GSK3beta inhibitors
JP2005289808A (ja) * 2000-03-23 2005-10-20 Sanofi-Aventis ３−置換−４−ピリミドン誘導体
EP1136099A1 (en) * 2000-03-23 2001-09-26 Sanofi-Synthelabo 2-(Indolylalkylamino)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
US7189717B2 (en) 2000-04-26 2007-03-13 Eisai Co., Ltd. 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
US7115608B2 (en) * 2000-09-19 2006-10-03 Centre National De La Recherche Schentifique Pyridinone and pyridinethione derivatives having HIV inhibiting properties
GB0024808D0 (en) * 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
AU2002223500A1 (en) 2000-11-17 2002-05-27 Novo-Nordisk A/S Glucagon antagonists/inverse agonists
US6706744B2 (en) 2000-11-17 2004-03-16 Novo Nordisk A/S Glucagon antagonists/inverse agonists
US6821960B2 (en) 2000-11-17 2004-11-23 Noyo Nordisk Pharmaceuticals, Inc. Glucagon antagonists/inverse agonists
PT1674456E (pt) 2001-09-21 2008-09-11 Sanofi Aventis Utilização de 2-fluoro-3-cetoésteres para preparar 3-fluoro- 6,7,8,9-tetra-hidro-4-h-pirimido[1,2-a]pirimidin-4-onas
EP1295885A1 (en) * 2001-09-21 2003-03-26 Sanofi-Synthelabo Substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido(1,2-a)pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo(1,2-a)pyrimidin-5(1H)one derivatives
EP1295884A1 (en) * 2001-09-21 2003-03-26 Sanofi-Synthelabo 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]Pyrimidin-4-one and 7-Pyrimidinyl-2,3-Dihydroimidazo[1,2-a]Pyrimidin-5(1H)one derivatives
AU2002337498B2 (en) 2001-09-21 2006-08-10 Mitsubishi Pharma Corporation 3-substituted-4-pyrimidone derivatives
EP1430056B1 (en) 2001-09-21 2005-10-26 Sanofi-Aventis Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1h)one derivatives for neurodegenerative disorders
TWI301834B (en) * 2001-10-22 2008-10-11 Eisai R&D Man Co Ltd Pyrimidone compound and pharmaceutical composition including the same
TWI330183B (hu) * 2001-10-22 2010-09-11 Eisai R&D Man Co Ltd
US6921762B2 (en) 2001-11-16 2005-07-26 Amgen Inc. Substituted indolizine-like compounds and methods of use
US6881746B2 (en) 2001-12-03 2005-04-19 Novo Nordick A/S Glucagon antagonists/inverse agonists
US6762318B2 (en) 2001-12-03 2004-07-13 Novo Nordisk A/S Glucagon antagonists
EP1458717B1 (en) * 2001-12-21 2005-09-07 Bayer HealthCare AG Aroyl pyridinones
AU2003216591A1 (en) * 2002-04-10 2003-10-20 Orichid Chemicals And Pharmaceuticals Limited Amino substituted pyrimidinone derivatives useful in the treatment of inflammation and immunological
CA2485166A1 (en) 2002-05-21 2003-12-04 Amgen Inc. Substituted pyrimidinone and pyridinone compounds
WO2004004725A2 (en) 2002-07-09 2004-01-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions of anticholinergics and p38 kinase inhibitors in the treatment of respiratory diseases
US7683069B2 (en) 2002-12-16 2010-03-23 Mitsubishi Tanabe Pharma Corporation 3-substituted-4-pyrimidone derivatives
TWI357408B (en) 2003-03-26 2012-02-01 Mitsubishi Tanabe Pharma Corp 3-substituted-4-pyrimidone derivatives
US20070167621A1 (en) 2003-04-03 2007-07-19 Pharmacia Corporation Substituted pyrimidinones
US7183287B2 (en) * 2003-04-03 2007-02-27 Pharmacia Corporation Substituted pyrimidinones
CA2533684A1 (en) * 2003-07-25 2005-02-10 Amgen Inc. Substituted pyridones and pyrimidinones with antiinflammatory properties
RU2006107553A (ru) * 2003-08-13 2007-09-20 Такеда Фармасьютикал Компани Лимитед (Jp) Производные 4-пиримидона и их применение в качестве ингибиторов пептидилпептидаз
US7429594B2 (en) 2003-08-20 2008-09-30 Amgen Inc. Substituted heterocyclic compounds and methods of use
SE0302486D0 (sv) 2003-09-18 2003-09-18 Astrazeneca Ab Novel compounds
EP1557417B1 (en) * 2003-12-19 2007-03-07 Sanofi-Aventis Substituted 8'-pyri(mi)dinyl-dihydrospiro-[cycloalkylamine]-pyrimido[1,2-a] pyrimidin-6-one derivatives
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
GB0420722D0 (en) 2004-09-17 2004-10-20 Addex Pharmaceuticals Sa Novel allosteric modulators
EP2708531A1 (en) 2004-10-13 2014-03-19 Pharmacia & Upjohn Company LLC Crystalline Forms Of 3-[5-Chloro-4-[(2,4-difluorobenzyl) oxy]-6-oxopyrimidin-1(6H)-yl]-N-(2-hydroxyethyl)-4-methylbenzamide
MX2007007330A (es) 2004-12-16 2007-10-04 Vertex Pharma Piridonas de utilidad como inhibidores de quinasas .
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
NZ566799A (en) 2005-09-14 2011-04-29 Takeda Pharmaceutical Dipeptidyl peptidase inhibitors for treating diabetes
CN101360723A (zh) 2005-09-16 2009-02-04 武田药品工业株式会社 制备嘧啶二酮衍生物的方法
AR059898A1 (es) 2006-03-15 2008-05-07 Janssen Pharmaceutica Nv Derivados de 3-ciano-piridona 1,4-disustituida y su uso como moduladores alostericos de los receptores mglur2
TW200808763A (en) 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds I
TW200808771A (en) 2006-05-08 2008-02-16 Astrazeneca Ab Novel compounds II
TW200838536A (en) 2006-11-29 2008-10-01 Takeda Pharmaceutical Polymorphs of succinate salt of 2-[6-(3-amino-piperidin-1-yl)-3-methyl-2,4-dioxo-3,4-dihydro-2H-pyrimidin-1-ylmethy]-4-fluor-benzonitrile and methods of use therefor
WO2008104752A1 (en) * 2007-02-26 2008-09-04 Astrazeneca Ab Dihydropyridones as elastase inhibitors
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
EP1992344A1 (en) 2007-05-18 2008-11-19 Institut Curie P38 alpha as a therapeutic target in pathologies linked to FGFR3 mutation
KR20100065191A (ko) 2007-09-14 2010-06-15 오르토-맥닐-얀센 파마슈티칼스 인코포레이티드 １,３-이치환된 ４-(아릴-ｘ-페닐)-１ｈ-피리딘-２-온
CN101801951B (zh) 2007-09-14 2013-11-13 杨森制药有限公司 1’,3’-二取代的-4-苯基-3,4,5,6-四氢-2h,1’h-[1,4’]二吡啶-2’-酮
CL2008003301A1 (es) 2007-11-06 2009-10-16 Astrazeneca Ab Compuestos derivados de 3,4-dihidropirazina-2-carboxamida, inhibidores de la elastasa de neutrofilos humanos; composiciones farmacéuticas; procesos de preparación de compuestos y composición farmacéutica; y uso en el tratamiento de síndrome de dificultad respiratoria de los adultos, fibrosis quística, cáncer, entre otras.
RU2510396C2 (ru) 2008-09-02 2014-03-27 Янссен Фармасьютикалз, Инк. 3-азабицикло[3.1.0]гексильные производные в качестве модуляторов метаботропных глутаматных рецепторов
CA2741666C (en) * 2008-10-31 2017-04-11 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
AU2009319387B2 (en) 2008-11-28 2012-05-10 Addex Pharma S.A. Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
TW201036957A (en) 2009-02-20 2010-10-16 Astrazeneca Ab Novel salt 628
JP5707390B2 (ja) 2009-05-12 2015-04-30 ジャンセン ファーマシューティカルズ， インコーポレイテッド １，２，４−トリアゾロ［４，３−ａ］ピリジン誘導体およびｍＧｌｕＲ２受容体の正のアロステリック調節因子としてのその使用
RS53075B (en) 2009-05-12 2014-04-30 Janssen Pharmaceuticals Inc. 1,2,4-TRIAZOLO [4,3-A] PYRIDINE DERIVATIVES AND THEIR USE IN THE TREATMENT OR PREVENTION OF NEUROLOGICAL AND PSYCHIATRIC DISORDERS
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
WO2011039528A1 (en) 2009-10-02 2011-04-07 Astrazeneca Ab 2-pyridone compounds used as inhibitors of neutrophil elastase
EP2643320B1 (en) 2010-11-08 2015-03-04 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2649069B1 (en) 2010-11-08 2015-08-26 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
EP2661435B1 (en) 2010-11-08 2015-08-19 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
BR112013016033A2 (pt) 2010-12-23 2018-06-05 Pfizer moduladores do receptor de glucagon
IL227559A (en) 2011-02-08 2016-04-21 Pfizer Glucagon receptor modulator
ES2543050T3 (es) 2011-02-28 2015-08-14 Array Biopharma, Inc. Inhibidores de serina/treonina quinasa
WO2013014569A1 (en) 2011-07-22 2013-01-31 Pfizer Inc. Quinolinyl glucagon receptor modulators
US9187462B2 (en) 2011-08-04 2015-11-17 Array Biopharma Inc. Substituted quinazolines as serine/threonine kinase inhibitors
CA2853024C (en) 2011-11-11 2017-08-22 Pfizer Inc. 2-thiopyrimidinones
CN103130787B (zh) * 2011-11-24 2015-06-10 南开大学 嘧啶酮酰胺类化合物及其制备方法、抗hiv活性和抗tmv活性
SI2820009T1 (en) 2012-03-01 2018-05-31 Array Biopharma, Inc. Serine / Threonine kinase inhibitors
BR112015004548A2 (pt) 2012-08-27 2017-08-08 Array Biopharma Inc inibidores de serina/treonina para tratamento de doenças hiperproliferativas
JO3368B1 (ar) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv مركبات 6، 7- ثاني هيدرو بيرازولو [5،1-a] بيرازين- 4 (5 يد)- اون واستخدامها بصفة منظمات تفارغية سلبية لمستقبلات ميجلور 2
JO3367B1 (ar) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv مركبات 2،1، 4- ثلاثي زولو [3،4-a] بيريدين واستخدامها بصفة منظمات تفارغية موجبة لمستقبلات ميجلور 2
ES2860298T3 (es) 2014-01-21 2021-10-04 Janssen Pharmaceutica Nv Combinaciones que comprenden moduladores alostéricos positivos del receptor glutamatérgico metabotrópico de subtipo 2 y su uso
DK3431106T3 (da) 2014-01-21 2021-03-15 Janssen Pharmaceutica Nv Kombinationer omfattende positive allosteriske modulatorer eller orthosteriske agonister af metabotrop glutamaterg subtype 2-receptor og anvendelse af disse
KR101693781B1 (ko) * 2014-10-06 2017-01-09 한양대학교 에리카산학협력단 다이플루오로알킬기가 도입된 방향족 화합물의 제조 방법
EP3292109A1 (en) 2015-05-05 2018-03-14 Pfizer Inc 2-thiopyrimidinones
CN107200731B (zh) * 2017-06-11 2020-10-23 湖南科技大学 一种含噻唑环吡啶酮衍生物及其制备方法和应用
CN110078674B (zh) * 2019-04-10 2022-11-01 昆明理工大学 一种2-烃基胺基嘧啶酮的制备方法
JOP20220125A1 (ar) 2019-11-25 2023-01-30 Amgen Inc مركبات حلقية غير متجانسة على هيئة مثبطات دلتا-5 ديساتوراز وطرق لاستخدامها
CN115650906A (zh) * 2022-11-04 2023-01-31 苏州艾缇克药物化学有限公司 一种2-氨基异烟酸的制备方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE1271116B (de) * 1965-05-04 1968-06-27 Bayer Ag Verfahren zur Herstellung von 4-Hydroxypyrimidinen
JPS6163680A (ja) * 1984-09-05 1986-04-01 Kanto Ishi Pharma Co Ltd ピリミド〔１，２−ａ〕ベンズイミダゾ−ル誘導体及びその製造方法
US5620999A (en) * 1994-07-28 1997-04-15 Weier; Richard M. Benzenesulfonamide subtituted imidazolyl compounds for the treatment of inflammation
IL123950A (en) * 1995-10-06 2001-04-30 Merck & Co Inc Transformed imidazoles with anti-cancer and cytokine-inhibiting activity and pharmaceutical preparations containing them
WO1997016442A1 (en) * 1995-10-31 1997-05-09 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use

Also Published As

Publication number Publication date
AU5525498A (en) 1998-06-29
CN1328277C (zh) 2007-07-25
IL130181A0 (en) 2000-06-01
KR20000069329A (ko) 2000-11-25
EP0948496A2 (en) 1999-10-13
WO1998024780A3 (en) 1998-07-30
HUP0001140A3 (en) 2002-05-28
CZ9902016A3 (cs) 1999-11-17
CN1246857A (zh) 2000-03-08
KR100476586B1 (ko) 2005-03-18
WO1998024780A2 (en) 1998-06-11
AU735901B2 (en) 2001-07-19
CA2274093A1 (en) 1998-06-11
BG103521A (en) 2000-07-31
NZ335992A (en) 2001-09-28
BG65129B1 (bg) 2007-03-30
JP2002514196A (ja) 2002-05-14
BR9713863A (pt) 2000-03-14
CA2274093C (en) 2006-11-07
AU735901C (en) 2004-02-12

Similar Documents

Publication Publication Date Title
HUP0001140A2 (hu) Szubsztituált pirimidinon és piridonszármazékok, továbbá ezeket tartalmazó gyógyászati készítmények
HUP0400837A2 (hu) 2-feniltiazol-származékok, alkalmazásuk és az ezeket tartalmazó gyógyszerkészítmények
HUP0202810A2 (hu) Szubsztituált 2-tio-3.5-diciano-4-aril-6-aminopiridinek és eljárás az előállításukra, valamint ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0401009A2 (hu) 5-Hidroxitriptamin-6-ligandumokként alkalmazható 1-aril- vagy 1- alkil-szulfonilbenzazol-származékok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények
FI965126A0 (fi) Tri-substituoidut PDE IV -inhibiittoreina hyödylliset fenyylijohdannaiset
HUP0402507A2 (hu) N(fenilszulfonil)glicin-származékok, alkalmazásuk és az ezeket tartalmazó gyógyászati készítmények
HUP0401478A2 (hu) Fungicid hatású pirazolil-karboxanilid-származékok
YU46497B (sh) Postupak za dobijanje novih derivata pirazola
HUP0402310A2 (hu) 1,6-Naftiridin-származékok mint antidiabetikumok és ezeket tartalmazó gyógyszerkészítmények
HUP0102851A2 (hu) Parazitaellenes artemizinin-származékok (endoperoxidok), eljárás előállításukra és a vegyületeket tartalmazó gyógyászati készítmények
NZ528851A (en) N-aroyl cyclic amines
ATE250590T1 (de) Neuartiger p2x 7 rezeptor-antagonisten zur verwendung in der behandlung von entzündlichen, immuninduzierten erkrankungen oder erkrankungen des herz-kreislauf-systems
HUP0003467A2 (hu) Benzamidoximszármazékok, intermedierjeik, eljárás előállításukra és alkalmazásuk fungicidként
DE68906552D1 (de) Camptothecin-derivate und verfahren zu ihrer herstellung.
HUP0401293A2 (hu) Új dihidropteridinonok, eljárás előállításukra és alkalmazásuk gyógyszerként
DE60229267D1 (de) Oxopyrrolidin verbindungen, verfahren zur herstellung dieser verbindungen und deren verwendung zur herstellung von levetiracetam und analogen
HUP0002853A2 (hu) 6,7-Helyzetben aszimmetrikusan diszubsztituált kinoxalinkarbonsav-származékok, és ezeket a vegyületeket tartalmazó gyógyszerkészítmények
HUP0400926A2 (hu) Lipidszintcsökkentő új bifenilkarboxamidok, eljárás előállításukra és ezeket tartalmazó gyógyszerkészítmények
HUP0500136A2 (hu) Oxitocin antagonista hatású szubsztituált diketo-piperazinok, eljárás előállításukra, az ezeket tartalmazó gyógyszerkészítmények és alkalmazásuk
HUP0001957A2 (hu) Gombaellenes hatású, piridingyűrűben karbonsavszármazékokkal helyettesített 2-(metoxi-imino)-2-(piridinil-oxi-metil)-fenil-acetamid-származékok, intermedierjeik, előállításuk és alkalmazásuk
HUP0301587A2 (hu) Foszfodiészteráz V gátló hatású 5-amino-alkil-pirazolo[4,3-d]pirimidinek, ezeket tartalmazó gyógyszerkészítmények és eljárások az elżállításaikra
WO2005011697A3 (en) Sulfonamide derivatives with activity on protein kinase a and b
FR2363554A1 (fr) Nouvelles aminoalkylidenamino-1,4-dihydropyridines, leur procede de preparation et medicament les contenant
NO305602B1 (no) Optisk aktivt <beta>-aminoalkoksyboran-kompleks og fremgangsmÕte for fremstilling derav
NO941516L (no) 3-kinolylsubstituerte dihydropyridiner, fremgangsmåter for deres fremstilling og deres anvendelse

Legal Events

Date Code Title Description
FD9A Lapse of provisional protection due to non-payment of fees