NO984939L - Azetidinone derivatives for the treatment of atherosclerosis - Google Patents

Azetidinone derivatives for the treatment of atherosclerosis

Info

Publication number
NO984939L
NO984939L NO984939A NO984939A NO984939L NO 984939 L NO984939 L NO 984939L NO 984939 A NO984939 A NO 984939A NO 984939 A NO984939 A NO 984939A NO 984939 L NO984939 L NO 984939L
Authority
NO
Norway
Prior art keywords
hydrogen
atherosclerosis
treatment
alkyl
pharmaceutically acceptable
Prior art date
Application number
NO984939A
Other languages
Norwegian (no)
Other versions
NO984939D0 (en
Inventor
Colin Andrew Leach
Deidre Mary Bernadette Hickey
Robert John Ife
Colin Theobald
Dashyant Dhanak
Original Assignee
Smithkline Beecham Plc
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 claimed from GBGB9608646.7A external-priority patent/GB9608646D0/en
Priority claimed from GBGB9623756.5A external-priority patent/GB9623756D0/en
Priority claimed from GBGB9625121.0A external-priority patent/GB9625121D0/en
Application filed by Smithkline Beecham Plc filed Critical Smithkline Beecham Plc
Publication of NO984939D0 publication Critical patent/NO984939D0/en
Publication of NO984939L publication Critical patent/NO984939L/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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 linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • 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
    • 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
    • A61P3/08Drugs 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
    • A61P39/00General protective or antinoxious agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P39/00General protective or antinoxious agents
    • A61P39/06Free radical scavengers or antioxidants
    • 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C07D205/09Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams with a sulfur atom directly attached in position 4

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Diabetes (AREA)
  • Rheumatology (AREA)
  • Toxicology (AREA)
  • Dermatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Biochemistry (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Utvalgte forbindelser med formel (I): SOCH CR2RJ-----XY hvori R"1 er hydrogen eller en tilsvarende farmasøytisk godtagbar ester eller et av dets farmasøytisk akseptable salter; R2 og R3 som kan være de samme eller forskjellige, er hver valgt fra hydrogen eller eventuelt substituert C(i_6)alkyl; X er en gruppe X'(CH2)m hvor x< er co- CONR4. COO, CONR4CO, CONHO eller CH2O hvor R4 er hydrogen eller C(-|_6)alkyl og m er O eller et helt tall fra 1 til 12; eller en C(i_i2)alkylenkjede eventuelt avbrutt av X1; og Y er en eventuelt substituert arylgruppe; som har absolutt konfigurasjon (4R.SS); er inhibitorer for enzymet Lp-PLA2 °9 kan derfor anvendes ved behandling aterosklerose.Selected compounds of formula (I): SOCH CR2RJ ----- XY wherein R "1 is hydrogen or a corresponding pharmaceutically acceptable ester or one of its pharmaceutically acceptable salts; R 2 and R 3 which may be the same or different, are each selected from hydrogen or optionally substituted C (1-6) alkyl; X is a group X '(CH2) m where x <is co-CONR4. COO, CONR4CO, CONHO or CH2O where R4 is hydrogen or C (- | 6) alkyl and m is O or an integer from 1 to 12; or a C (I2) alkylene chain optionally interrupted by X1; and Y is an optionally substituted aryl group, having absolute configuration (4R.SS); are inhibitors of the enzyme Lp-PLA2 ° 9 can therefore be used in treating atherosclerosis.

NO984939A 1996-04-26 1998-10-23 Azetidinone derivatives for the treatment of atherosclerosis NO984939L (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
GBGB9608646.7A GB9608646D0 (en) 1996-04-26 1996-04-26 Novel compounds
GBGB9623756.5A GB9623756D0 (en) 1996-11-15 1996-11-15 Novel compounds
GBGB9625121.0A GB9625121D0 (en) 1996-12-03 1996-12-03 Novel compounds
PCT/EP1997/001898 WO1997041098A1 (en) 1996-04-26 1997-04-15 Azetidinone derivatives for the treatment of atherosclerosis

Publications (2)

Publication Number Publication Date
NO984939D0 NO984939D0 (en) 1998-10-23
NO984939L true NO984939L (en) 1998-12-23

Family

ID=27268259

Family Applications (1)

Application Number Title Priority Date Filing Date
NO984939A NO984939L (en) 1996-04-26 1998-10-23 Azetidinone derivatives for the treatment of atherosclerosis

Country Status (17)

Country Link
EP (1) EP0915843A1 (en)
JP (1) JP2000509049A (en)
AR (1) AR006833A1 (en)
AU (1) AU2698697A (en)
BR (1) BR9709196A (en)
CA (1) CA2252696A1 (en)
CZ (1) CZ341098A3 (en)
HU (1) HUP9901359A3 (en)
ID (1) ID16660A (en)
IL (1) IL126696A0 (en)
MA (1) MA26426A1 (en)
NO (1) NO984939L (en)
NZ (1) NZ332476A (en)
PE (1) PE64398A1 (en)
PL (1) PL329530A1 (en)
TR (1) TR199802160T2 (en)
WO (1) WO1997041098A1 (en)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1686119B1 (en) 2000-02-16 2009-07-29 Smithkline Beecham Plc Pyrimidine-5-one derivatives as LDL-PLA2 inhibitors
US6982251B2 (en) 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
IL156445A0 (en) 2001-01-26 2004-01-04 Schering Corp Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
AR035533A1 (en) 2001-01-26 2004-06-02 Schering Corp USE OF AT LEAST AN INHIBITOR OF THE ABSORPTION OF THE STEROLS OR THEIR SALTS, SOLVATOS, PHARMACEUTICALLY ACCEPTABLE DRUGS OR MIXTURES OF THE SAME FOR THE PREPARATION OF A MEDICINAL PRODUCT FOR THE TREATMENT OF SITOSTEROLEMIA, COMPOSITIONS OF THE PHARMACEUTICAL USE
EE05453B1 (en) 2001-03-28 2011-08-15 Schering Corporation Process for the preparation of azetidinone intermediates
ES2275007T3 (en) * 2001-05-25 2007-06-01 Schering Corporation USE OF SUBSTITUTED AZETIDINONE DERIVATIVES IN THE TREATMENT OF ALZEIMER'S DISEASE.
US7056906B2 (en) 2001-09-21 2006-06-06 Schering Corporation Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
MXPA04002573A (en) 2001-09-21 2004-06-18 Schering Corp Treatment of xanthoma with azetidinone derivatives as sterol absorption inhibitors.
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
WO2004043457A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorptions inhibitors for the treatment of autoimmune disorders
EP1601668B1 (en) 2003-03-07 2008-08-27 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
CA2517572C (en) 2003-03-07 2011-12-13 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia
JP2006519869A (en) 2003-03-07 2006-08-31 シェーリング コーポレイション Substituted azetidinone compounds, processes for preparing substituted azetidinone compounds, their formulations and uses
US7459442B2 (en) 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
AU2008251467B2 (en) 2007-05-11 2014-07-31 The Trustees Of The University Of Pennsylvania Methods of treatment of skin ulcers
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
CN101986785A (en) 2007-05-11 2011-03-16 托马斯杰弗逊大学 Methods of treatment and prevention of neurodegenerative diseases and disorders
PE20140421A1 (en) 2010-12-06 2014-04-26 Glaxo Group Ltd PYRIMIDINONE-DERIVED COMPOUNDS AS Lp-PLA2 INHIBITORS
EP2651403B1 (en) 2010-12-17 2020-12-02 Glaxo Group Limited Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases
WO2013000267A1 (en) 2011-06-27 2013-01-03 中国科学院上海药物研究所 Azole heterocyclic compound, preparation method, pharmaceutical composition and use
EP2739627A4 (en) 2011-07-27 2015-01-21 Glaxo Group Ltd 2,3-dihydroimidazo[1,2-c]pyrimidin-5(1h)-one compounds use as lp-pla² inhibitors
AR087309A1 (en) 2011-07-27 2014-03-12 Glaxo Group Ltd HETEROCICLIC COMPOUND OF SUBSTITUTED CONDENSED RINGS, PHARMACEUTICAL COMPOSITION THAT INCLUDES IT AND ITS USE FOR THE MANUFACTURE OF A MEDICINAL PRODUCT FOR THE TREATMENT OF NEUROGENERATIVE DISEASES AND ATEROSCLEROSIS
BR112015017768A2 (en) 2013-01-25 2017-07-11 Glaxosmithkline Ip Dev Ltd compounds
AU2014210260B2 (en) 2013-01-25 2016-08-04 Glaxosmithkline Intellectual Property Development Limited Bicyclic pyrimidone compounds as inhibitors of Lp-PLA2
EP2948452B1 (en) 2013-01-25 2017-08-09 GlaxoSmithKline Intellectual Property Development Limited 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors
WO2016012917A1 (en) 2014-07-22 2016-01-28 Glaxosmithkline Intellectual Property Development Limited 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2
WO2016012916A1 (en) 2014-07-22 2016-01-28 Glaxosmithkline Intellectual Property Development Limited 1,2,3,5-tetrahydroimidazo[1,2-c]pyrimidine derivatives useful in the treatment of diseases and disorders mediated by lp-pla2
CN112778331B (en) 2019-11-09 2022-07-05 上海赛默罗生物科技有限公司 Tricyclic dihydroimidazopyrimidinone derivatives, preparation method, pharmaceutical composition and application thereof
CN115304620A (en) 2021-05-07 2022-11-08 上海赛默罗生物科技有限公司 Pyrimidone derivatives, preparation method, pharmaceutical composition and application thereof
TWI896037B (en) 2023-07-17 2025-09-01 大陸商上海樞境生物科技有限公司 Bicyclic [5,6] imidazole pyrimidone derivatives, preparation methods and applications thereof

Family Cites Families (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4680391A (en) * 1983-12-01 1987-07-14 Merck & Co., Inc. Substituted azetidinones as anti-inflammatory and antidegenerative agents
IL89835A0 (en) * 1988-04-11 1989-12-15 Merck & Co Inc Substituted azetidinones,their preparation and pharmaceutical compositions containing them
IL99658A0 (en) * 1990-10-15 1992-08-18 Merck & Co Inc Substituted azetidinones and pharmaceutical compositions containing them
WO1993000332A1 (en) * 1991-06-25 1993-01-07 Merck & Co., Inc. Substituted azetidinones as anti-inflammatory and antidegenerative agents
ES2107548T3 (en) * 1991-07-23 1997-12-01 Schering Corp SUBSTITUTED BETA-LACTAMA COMPOUNDS USEFUL AS HYPOCHOLESTEROLEMIC AGENTS AND PROCEDURES FOR THEIR PREPARATION.
TW275621B (en) * 1992-10-27 1996-05-11 Merck & Co Inc
WO1994013636A1 (en) * 1992-12-17 1994-06-23 Merck & Co., Inc. New substituted azetidinones as anti-inflammatory and antidegenerative agents
EP0658205B1 (en) * 1993-06-25 2000-03-15 Smithkline Beecham Plc Lipoprotein associated phospholipase a2, inhibitors thereof and use of the same in diagnosis and therapy
EP1096016B1 (en) * 1993-10-06 2006-01-11 Icos Corporation Platelet-activating factor acetylhydrolase
GB9421816D0 (en) * 1994-10-29 1994-12-14 Smithkline Beecham Plc Novel compounds
CN1175246A (en) * 1994-12-22 1998-03-04 史密丝克莱恩比彻姆有限公司 Substituted azetidin-2-ones for treatment of atherosclerosis
AU5014496A (en) * 1995-03-23 1996-10-08 Japan Tobacco Inc. Diphenylmethyl-azetidinone compounds and elastase inhibitor
JP2002515852A (en) * 1995-07-01 2002-05-28 スミスクライン・ビーチャム・パブリック・リミテッド・カンパニー Azetidinone derivatives for the treatment of atherosclerosis
WO1997021676A1 (en) * 1995-12-08 1997-06-19 Smithkline Beecham Plc Azetidinone compounds for the treatment of atherosclerosis

Also Published As

Publication number Publication date
CA2252696A1 (en) 1997-11-06
JP2000509049A (en) 2000-07-18
CZ341098A3 (en) 1999-03-17
AR006833A1 (en) 1999-09-29
BR9709196A (en) 1999-05-25
HUP9901359A3 (en) 2000-03-28
HUP9901359A2 (en) 1999-08-30
MA26426A1 (en) 2004-12-20
WO1997041098A1 (en) 1997-11-06
IL126696A0 (en) 1999-08-17
NZ332476A (en) 2000-06-23
ID16660A (en) 1997-10-30
EP0915843A1 (en) 1999-05-19
TR199802160T2 (en) 1999-04-21
PE64398A1 (en) 1999-01-06
AU2698697A (en) 1997-11-19
NO984939D0 (en) 1998-10-23
PL329530A1 (en) 1999-03-29

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