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ES2186821T3 - Derivados de 6- bencil- 2h-piridazin-3-ona, su preparacion y s u uso como inhibidores de la prostaglandin-g/h sintasa i y ii (cox i y cox ii). - Google Patents

Derivados de 6- bencil- 2h-piridazin-3-ona, su preparacion y s u uso como inhibidores de la prostaglandin-g/h sintasa i y ii (cox i y cox ii).

Info

Publication number
ES2186821T3
ES2186821T3 ES97108260T ES97108260T ES2186821T3 ES 2186821 T3 ES2186821 T3 ES 2186821T3 ES 97108260 T ES97108260 T ES 97108260T ES 97108260 T ES97108260 T ES 97108260T ES 2186821 T3 ES2186821 T3 ES 2186821T3
Authority
ES
Spain
Prior art keywords
sub
rent
cox
halo
prostaglandin
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.)
Expired - Lifetime
Application number
ES97108260T
Other languages
English (en)
Inventor
Darin Arthur Allen
James Patrick Dunn
Eric Brian Sjogren
David Bernard Smith
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.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Application granted granted Critical
Publication of ES2186821T3 publication Critical patent/ES2186821T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic 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
    • C07D237/10Heterocyclic 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 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
    • C07D237/14Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic agents

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

COMPUESTOS DE FORMULA I: EN DONDE LA LINEA PUNTEADA INDICA UN ENLACE OPCIONAL; R{SUB,1} ES H, HALO, ALQUILO, ALQUILOXI, AMINO, ALQUILAMINO, DIALQUILAMINO O ACILAMINO; R{SUB,3} Y R{SUB,4} SON INDEPENDIENTEMENTE H, HALO, ALQUILO, ALQUILOXI O HIDROXI; R{SUB,5} ES H, HALO, ALQUILO, ALQUILTIO, ALQUILOXI, ALQUENILOXI, ALQUINILO O ALQUENILO; CON LA CONDICION DE QUE AL MENOS UNO DE R{SUB,1}, R{SUB,3}, R{SUB,4} Y R{SUB,5} ES H; R{SUB,7} ES H, ALQUILO, CIANO O AMIDO; R{SUB,10} ES UN GRUPO REPRESENTADO POR LA FORMULA (A), (B) O (C): DONDE: X ES O O S; R{SUB,12}, R{SUB,13}, R{SUB,15} Y R{SUB,16} SON INDEPENDIENTEMENTE H, HALO, ALQUILO, ALQUILOXI O ALQUILTIO; Y R{SUB,14} ES H, HALO, ALQUILO, ALQUILTIO, ALQUILOXI, ALQUENILOXI, ALQUINILO, ALQUENILO O ,2}NR{SUB,18}R{SUB,19}, DONDE R{SUB,18} Y R{SUB,19} SON INDEPENDIENTEMENTE H O ALQUILO; SIEMPRE Y CUANDO AL MENOS DOS DE R{SUB,12}, R{SUB,13}, R{SUB,14}, R{SUB,15} Y R{SUB,16} SON H, Y QUE SI SOLO DOS DE R{SUB,12}, R{SUB,13}, R{SUB,15} Y R{SUB,16} SON H, LOSSUSTITUYENTES QUE NO SON HIDROGENO NO ESTAN TODOS ADYACENTES; Y AL MENOS UNO DE R{SUB,12} Y R{SUB,16} ES H CUANDO NI R{SUB,1} NI R{SUB,3} SON H; Y R{SUB,20} ES H, ALQUILO, HALOALQUILO, HIDROXIALQUILO O ALQUENILO. LA INVENCION SE REFIERE ASIMISMO A SUS SALES FARMACEUTICAMENTE ACEPTABLES QUE TAMBIEN SON INHIBIDORES DE LA PROSTAGLANDIN IINFLAMATORIOS Y ANALGESICOS.
ES97108260T 1996-05-30 1997-05-22 Derivados de 6- bencil- 2h-piridazin-3-ona, su preparacion y s u uso como inhibidores de la prostaglandin-g/h sintasa i y ii (cox i y cox ii). Expired - Lifetime ES2186821T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US1867296P 1996-05-30 1996-05-30

Publications (1)

Publication Number Publication Date
ES2186821T3 true ES2186821T3 (es) 2003-05-16

Family

ID=21789188

Family Applications (1)

Application Number Title Priority Date Filing Date
ES97108260T Expired - Lifetime ES2186821T3 (es) 1996-05-30 1997-05-22 Derivados de 6- bencil- 2h-piridazin-3-ona, su preparacion y s u uso como inhibidores de la prostaglandin-g/h sintasa i y ii (cox i y cox ii).

Country Status (13)

Country Link
US (1) US5886178A (es)
EP (1) EP0810218B1 (es)
JP (1) JP2790450B2 (es)
CN (1) CN1136197C (es)
AR (1) AR008377A1 (es)
AT (1) ATE229007T1 (es)
BR (1) BR9703332A (es)
CA (1) CA2205757C (es)
DE (1) DE69717537T2 (es)
DK (1) DK0810218T3 (es)
ES (1) ES2186821T3 (es)
PT (1) PT810218E (es)
TR (1) TR199700419A2 (es)

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ES2590912T3 (es) 1997-12-08 2016-11-24 Merck Patent Gmbh Proteínas de fusión heterodiméricas útiles para inmunoterapia dirigida y estimulación general del sistema inmunitario
US20030105294A1 (en) * 1998-02-25 2003-06-05 Stephen Gillies Enhancing the circulating half life of antibody-based fusion proteins
EP1071468B1 (en) * 1998-04-15 2006-06-14 Lexigen Pharmaceuticals Corp. Enhancement of antibody-cytokine fusion protein mediated immune responses by co-administration with angiogenesis inhibitor
US6680344B1 (en) 1999-06-01 2004-01-20 The University Of Texas Southwestern Medical Center Method of treating hair loss using diphenylmethane derivatives
AU3712100A (en) 1999-06-01 2000-12-18 University Of Texas Southwestern Medical Center, The Method of treating hair loss using sulfonyl thyromimetic compounds
US7067110B1 (en) 1999-07-21 2006-06-27 Emd Lexigen Research Center Corp. Fc fusion proteins for enhancing the immunogenicity of protein and peptide antigens
SK782002A3 (en) 1999-07-21 2003-08-05 Lexigen Pharm Corp FC fusion proteins for enhancing the immunogenicity of protein and peptide antigens
DE60025832T2 (de) * 1999-08-09 2006-08-31 Emd Lexigen Research Center Corp., Billerica Mehrere zytokin-antikörper komplexen
CA2391080A1 (en) 1999-11-12 2001-05-25 Merck Patent Gesellschaft Mit Beschraenkter Haftung Erythropoietin forms with improved properties
CN1406249B (zh) 2000-02-11 2010-06-16 默克专利股份有限公司 增加基于抗体的融合蛋白的循环半衰期
PT1294401E (pt) * 2000-06-29 2007-11-09 Merck Patent Gmbh Aumento das respostas imunológicas mediadas por proteínas de fusão anticorpo-citoquina por tratamento combinado com agentes que aumentam a captação de imunocitoquinas
US7151102B2 (en) * 2000-10-30 2006-12-19 Kudos Pharmaceuticals Limited Phthalazinone derivatives
RU2003129528A (ru) * 2001-03-07 2005-04-10 Мерк Патент ГмбХ (DE) Способ экспрессии белков, содержащих в качестве компонента гибридный изотип антитела
US6992174B2 (en) * 2001-03-30 2006-01-31 Emd Lexigen Research Center Corp. Reducing the immunogenicity of fusion proteins
CN100503639C (zh) 2001-05-03 2009-06-24 默克专利有限公司 重组肿瘤特异性抗体及其应用
EP2354791A1 (en) * 2001-12-04 2011-08-10 Merck Patent GmbH Immunocytokines with modulated selectivity
ES2357057T3 (es) * 2002-04-30 2011-04-15 Kudos Pharmaceuticals Limited Derivados de ftalazinona.
PT1572748E (pt) * 2002-12-17 2010-09-28 Merck Patent Gmbh Anticorpo humanizado (h14.18) do anticorpo 14.18 de rato que se liga ao gd2 e a sua fusão com a il-2
GB0305681D0 (en) 2003-03-12 2003-04-16 Kudos Pharm Ltd Phthalazinone derivatives
US7449464B2 (en) * 2003-03-12 2008-11-11 Kudos Pharmaceuticals Limited Phthalazinone derivatives
MXPA05010081A (es) 2003-03-24 2005-11-23 Hoffmann La Roche Bencil-piridazinonas como inhibidores de transcriptasa inversa.
JP4627315B2 (ja) * 2004-03-23 2011-02-09 エフ.ホフマン−ラ ロシュ アーゲー 非ヌクレオシド逆転写酵素阻害剤としてのベンジルピリダジノン誘導体
CA2563225A1 (en) * 2004-04-15 2005-10-27 F. Hoffmann-La Roche Ag Process for preparing pyridazinone compounds
GB0419072D0 (en) 2004-08-26 2004-09-29 Kudos Pharm Ltd Phthalazinone derivatives
NZ553979A (en) * 2004-08-26 2009-05-31 Kudos Pharm Ltd 4-heteroarylmethyl substituted phthalazinone derivatives
GB0428111D0 (en) * 2004-12-22 2005-01-26 Kudos Pharm Ltd Pthalazinone derivatives
CA2623728A1 (en) * 2005-09-30 2007-04-12 F. Hoffmann-La Roche Ag Nnrt inhibitors
GB0521373D0 (en) * 2005-10-20 2005-11-30 Kudos Pharm Ltd Pthalazinone derivatives
GB0610680D0 (en) * 2006-05-31 2006-07-12 Istituto Di Ricerche D Biolog Therapeutic compounds
WO2007144652A2 (en) * 2006-06-15 2007-12-21 Kudos Pharmaceuticals Limited Parp inhibitors
US20090281086A1 (en) * 2006-06-15 2009-11-12 Kudos Pharmaceuticals Limited 2 -oxyheteroarylamide derivatives as parp inhibitors
WO2007144639A1 (en) * 2006-06-15 2007-12-21 Kudos Pharmaceuticals Limited 2 -oxybenzamide derivatives as parp inhibitors
US20080280910A1 (en) * 2007-03-22 2008-11-13 Keith Allan Menear Phthalazinone derivatives
TW200900396A (en) * 2007-04-10 2009-01-01 Kudos Pharm Ltd Phthalazinone derivatives
US20090023727A1 (en) * 2007-07-05 2009-01-22 Muhammad Hashim Javaid Phthalazinone derivatives
US7981890B2 (en) 2007-09-14 2011-07-19 Astrazeneca Ab Phthalazinone derivatives
EP2212296B1 (en) * 2007-10-17 2014-12-03 Kudos Pharmaceuticals Limited 4- [3- (4-cyclopropanecarbonyl-piperazine-i-carbonyl) -4 -fluoro-benzyl]-2h-phthalaz in-1-one
ES2524787T3 (es) 2007-11-15 2014-12-12 Msd Italia S.R.L. Derivados de piridazinona como inhibidores de PARP
UY31603A1 (es) 2008-01-23 2009-08-31 Derivados de ftalazinona
MY160340A (en) 2008-10-07 2017-02-28 Astrazeneca Uk Ltd Pharmaceutical formulation 514
TW201114756A (en) * 2009-07-15 2011-05-01 Astrazeneca Ab Phthalazinone compound
GB201219820D0 (en) 2012-11-05 2012-12-19 Isis Innovation Compounds
ES2544869B2 (es) * 2014-03-04 2016-01-18 Universidade De Vigo Derivados de piridazin-3(2H)-ona inhibidores selectivos de la isoforma B de la monoaminooxidasa
CN111153859B (zh) * 2015-04-15 2021-09-03 江苏恩华药业股份有限公司 哒嗪酮类衍生物及其应用
JP6596595B2 (ja) * 2016-03-04 2019-10-23 大塚製薬株式会社 5−メチル−6−フェニル−4,5−ジヒドロ−2h−ピリダジン−3−オン誘導体

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US4599332A (en) * 1983-12-07 1986-07-08 Warner-Lambert Company 4,5-dihydro-6-[2-[4-(1H-imidazol-1-yl)phenyl]-ethenyl]-3(2H)-pyridazinones and related compounds
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US5622948A (en) * 1994-12-01 1997-04-22 Syntex (U.S.A.) Inc. Pyrrole pyridazine and pyridazinone anti-inflammatory agents

Also Published As

Publication number Publication date
CN1136197C (zh) 2004-01-28
AR008377A1 (es) 2000-01-19
DE69717537T2 (de) 2003-11-06
CN1169426A (zh) 1998-01-07
ATE229007T1 (de) 2002-12-15
CA2205757A1 (en) 1997-11-30
BR9703332A (pt) 1998-09-22
CA2205757C (en) 2006-01-24
JP2790450B2 (ja) 1998-08-27
EP0810218B1 (en) 2002-12-04
DE69717537D1 (de) 2003-01-16
TR199700419A2 (xx) 1997-12-21
PT810218E (pt) 2003-03-31
JPH1045723A (ja) 1998-02-17
US5886178A (en) 1999-03-23
EP0810218A1 (en) 1997-12-03
DK0810218T3 (da) 2003-03-24

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