BG102214A - Производни на азетидинона за лечение на атеросклерозата - Google Patents

Производни на азетидинона за лечение на атеросклерозата

Info

Publication number
BG102214A
BG102214A BG102214A BG10221498A BG102214A BG 102214 A BG102214 A BG 102214A BG 102214 A BG102214 A BG 102214A BG 10221498 A BG10221498 A BG 10221498A BG 102214 A BG102214 A BG 102214A
Authority
BG
Bulgaria
Prior art keywords
alkyl
optionally
aryl
value
whichcan
Prior art date
Application number
BG102214A
Other languages
English (en)
Inventor
Dashyant Dhanak
Deirdre HICKEY
Robert IFE
Colin LEACH
David TEW
Original Assignee
Smithkline Beecham P.L.C.
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 GBGB9513442.5A external-priority patent/GB9513442D0/en
Priority claimed from GBGB9515056.1A external-priority patent/GB9515056D0/en
Priority claimed from GBGB9515206.2A external-priority patent/GB9515206D0/en
Priority claimed from GBGB9516985.0A external-priority patent/GB9516985D0/en
Priority claimed from GBGB9525132.8A external-priority patent/GB9525132D0/en
Priority claimed from GBGB9608651.7A external-priority patent/GB9608651D0/en
Priority claimed from GBGB9608650.9A external-priority patent/GB9608650D0/en
Application filed by Smithkline Beecham P.L.C. filed Critical Smithkline Beecham P.L.C.
Publication of BG102214A publication Critical patent/BG102214A/bg

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic 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
    • C07D205/08—Heterocyclic 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
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic 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
    • C07D205/08—Heterocyclic 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
    • C07D205/085—Heterocyclic 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 nitrogen atom directly attached in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic 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
    • C07D205/08—Heterocyclic 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
    • C07D205/09—Heterocyclic 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
    • C07D205/095—Heterocyclic 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 and with a nitrogen atom directly attached in position 3
    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D417/02—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 two hetero rings
    • C07D417/12—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 two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Азетидиноновите съединения са инхибитори на ензима LpPLA2 и могат да намерят приложение за лечение на атеросклероза. Те имат формула, в която R1 и R2, които могат да бъдат еднакви или различни, са избрани поотделно от водород, халоген или С(1-8) алкил; R4 и R5, които могат да бъдат еднакви или различни, са избрани поотделно от водород, С(1-6) алкил, С(2-6) алкенил, арил, арилС(1-4)алкил и хетероарилС(1-4)алкил, всеки от които може евентуално да бъде заместен, или R4 и R5 могат да бъдат свързанипомежду си, образувайки останалата част от С(3-7)циклоалкилов пръстен; Х е директна връзка; групата Х1(СН2)m, в която Х1 е СО, СОNR6, COO, CONR6CO или CONR60, където R6 е водород или С(1-6) алкил и m има стойност 0 или е множител със стойност от 1 до 12; групата (Х1)аХ2, в която а имастойност 0 или 1, а Х2 e C(1-12) алкиленова верига, разкъсана и/или прекъсната в края в съседство с Y от една илиповече групи Х3, избрани от 0, S(0)x, NR6, алкенова или алкинова група, където х има стойност 0, 1 или 2 или С(1-12) алкиленовата верига, евентуално прекъсната от Х1; Y e евентуално заместена ариловагрупа; Z е кислород, а R3 е С(1-8) алкил, С(3-8) циклоалкил, С(3-8)цикло-алкилС(1-6)алкил, хетероарил, хетероарил-С(1-4)алкил, арил или арилС(1-4)алкил, всеки от които може евентуално да бъде заместен, или Z e S(0)n, където n има стойност 0, 1 или 2, а R3 е хетероарил или хетероарилС(1-4)алкил, всеки от които може евентуално да бъде заместен.
BG102214A 1995-07-01 1998-01-28 Производни на азетидинона за лечение на атеросклерозата BG102214A (bg)

Applications Claiming Priority (8)

Application Number Priority Date Filing Date Title
GBGB9513442.5A GB9513442D0 (en) 1995-07-01 1995-07-01 Novel compounds
GBGB9515056.1A GB9515056D0 (en) 1995-07-22 1995-07-22 Novel compounds
GBGB9515206.2A GB9515206D0 (en) 1995-07-25 1995-07-25 Novel compounds
GBGB9516985.0A GB9516985D0 (en) 1995-08-18 1995-08-18 Novel compounds
GBGB9525132.8A GB9525132D0 (en) 1995-12-08 1995-12-08 Novel compounds
GBGB9608651.7A GB9608651D0 (en) 1996-04-26 1996-04-26 Novel compounds
GBGB9608650.9A GB9608650D0 (en) 1996-04-26 1996-04-26 Novel compounds
PCT/EP1996/002765 WO1997002242A1 (en) 1995-07-01 1996-06-20 Azetidinone derivatives for the treatment of atherosclerosis

Publications (1)

Publication Number Publication Date
BG102214A true BG102214A (bg) 1998-08-31

Family

ID=27562921

Family Applications (1)

Application Number Title Priority Date Filing Date
BG102214A BG102214A (bg) 1995-07-01 1998-01-28 Производни на азетидинона за лечение на атеросклерозата

Country Status (23)

Country Link
EP (1) EP0840725A1 (bg)
JP (1) JP2002515852A (bg)
KR (1) KR19990028630A (bg)
CN (1) CN1197452A (bg)
AP (1) AP728A (bg)
AU (1) AU708032B2 (bg)
BG (1) BG102214A (bg)
BR (1) BR9609445A (bg)
CA (1) CA2225627A1 (bg)
CZ (1) CZ422197A3 (bg)
EA (1) EA199800109A1 (bg)
HU (1) HUP9901153A3 (bg)
IL (1) IL122650A0 (bg)
MA (1) MA23922A1 (bg)
MX (1) MX9800186A (bg)
NO (1) NO976158L (bg)
NZ (1) NZ311684A (bg)
OA (1) OA10648A (bg)
PE (1) PE8998A1 (bg)
PL (1) PL324240A1 (bg)
SK (1) SK178497A3 (bg)
TR (1) TR199701762T1 (bg)
WO (1) WO1997002242A1 (bg)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997021675A1 (en) * 1995-12-08 1997-06-19 Smithkline Beecham Plc Monocyclic beta-lactame derivatives for treatment of atherosclerosis
EP0915843A1 (en) * 1996-04-26 1999-05-19 Smithkline Beecham Plc Azetidinone derivatives for the treatment of atheroscleroses
GB9608649D0 (en) * 1996-04-26 1996-07-03 Smithkline Beecham Plc Novel compounds
HU229479B1 (en) 2000-02-16 2014-01-28 Glaxo Group Ltd Pyrimidine-4-one derivatives
GB0024808D0 (en) 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
WO2008141176A1 (en) 2007-05-11 2008-11-20 The Trustees Of The University Of Pennsylvania Methods of treatment of skin ulcers
EA200971050A1 (ru) 2007-05-11 2010-06-30 Томас Джефферсон Юниверсити Способы лечения и предупреждения нейродегенеративных заболеваний и нарушений
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
WO2012076435A1 (en) 2010-12-06 2012-06-14 Glaxo Group Limited Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by lp - pla2
ES2847883T3 (es) 2010-12-17 2021-08-04 Glaxo Group Ltd Uso de inhibidores de LP-PLA2 en el tratamiento y prevención de enfermedades oculares
WO2013000267A1 (zh) 2011-06-27 2013-01-03 中国科学院上海药物研究所 唑类杂环化合物、其制备方法、药物组合物和用途
WO2013013503A1 (en) 2011-07-27 2013-01-31 Glaxo Group Limited 2,3-dihydroimidazo[1,2-c] pyrimidin-5(1h)-one compounds use as lp-pla2 inhibitors
AR087309A1 (es) 2011-07-27 2014-03-12 Glaxo Group Ltd Compuesto heterociclico de anillos condensados sustituido, composicion farmaceutica que lo comprende y su uso para la fabricacion de un medicamento para el tratamiento de enfermedades neurogenerativas y aterosclerosis
EP2948456A4 (en) 2013-01-25 2016-09-14 Glaxosmithkline Ip Dev Ltd BICYCLIC PYRIMIDONE COMPOUNDS AS LP-PLA2 INHIBITORS
WO2014114694A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors
US9296755B2 (en) 2013-01-25 2016-03-29 Glaxosmithkline Intellectual Property Development Limited 3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one compounds and their therapeutic applications
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
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
WO2021089032A1 (zh) 2019-11-09 2021-05-14 上海赛默罗生物科技有限公司 三环二氢咪唑并嘧啶酮衍生物、其制备方法、药物组合物和用途
CN115304620A (zh) 2021-05-07 2022-11-08 上海赛默罗生物科技有限公司 嘧啶酮衍生物、其制备方法、药物组合物和用途

Family Cites Families (5)

* 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
NZ228600A (en) * 1988-04-11 1992-02-25 Merck & Co Inc 1-(benzylaminocarbonyl)-4-phenoxy-azetidin-2-one derivatives
IL99658A0 (en) * 1990-10-15 1992-08-18 Merck & Co Inc Substituted azetidinones and pharmaceutical compositions containing them
GB9421816D0 (en) * 1994-10-29 1994-12-14 Smithkline Beecham Plc Novel compounds
CZ192297A3 (en) * 1994-12-22 1997-11-12 Smithkline Beecham Plc Substituted azetidin-2-ones for treating atherosclerosis, process of their preparation and use

Also Published As

Publication number Publication date
PL324240A1 (en) 1998-05-11
AP728A (en) 1999-01-29
AU708032B2 (en) 1999-07-29
AU6305096A (en) 1997-02-05
KR19990028630A (ko) 1999-04-15
CA2225627A1 (en) 1997-01-23
PE8998A1 (es) 1998-03-20
SK178497A3 (en) 1998-07-08
MX9800186A (es) 1998-07-31
NO976158D0 (no) 1997-12-30
BR9609445A (pt) 1999-04-06
AP9701161A0 (en) 1998-01-31
OA10648A (en) 2002-09-25
JP2002515852A (ja) 2002-05-28
TR199701762T1 (xx) 1998-05-21
IL122650A0 (en) 1998-08-16
EA199800109A1 (ru) 1998-10-29
CZ422197A3 (cs) 1998-06-17
HUP9901153A3 (en) 1999-11-29
MA23922A1 (fr) 1996-12-31
HUP9901153A2 (hu) 1999-08-30
NZ311684A (en) 2000-04-28
CN1197452A (zh) 1998-10-28
WO1997002242A1 (en) 1997-01-23
NO976158L (no) 1998-02-25
EP0840725A1 (en) 1998-05-13

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