EA199800109A1 - Производные азетидинона для лечения атеросклероза - Google Patents

Производные азетидинона для лечения атеросклероза

Info

Publication number
EA199800109A1
EA199800109A1 EA199800109A EA199800109A EA199800109A1 EA 199800109 A1 EA199800109 A1 EA 199800109A1 EA 199800109 A EA199800109 A EA 199800109A EA 199800109 A EA199800109 A EA 199800109A EA 199800109 A1 EA199800109 A1 EA 199800109A1
Authority
EA
Eurasian Patent Office
Prior art keywords
alkyl
aryl
atherosclerosis
6alkyl
heteroaryl
Prior art date
Application number
EA199800109A
Other languages
English (en)
Inventor
Дашиант Дханак
Деирдре Мэри Бернадетт Хикки
Роберт Джон Айфе
Колин Эндрю Лич
Дэвид Грэхэм Тью
Original Assignee
Смитклайн Бичам Плс
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 GBGB9608650.9A external-priority patent/GB9608650D0/en
Priority claimed from GBGB9608651.7A external-priority patent/GB9608651D0/en
Application filed by Смитклайн Бичам Плс filed Critical Смитклайн Бичам Плс
Publication of EA199800109A1 publication Critical patent/EA199800109A1/ru

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

Abstract

Производные азетидинона формулы (I), где каждый из Rи R, которые могут быть одинаковыми или различными, выбран из водорода, галогена или Cалкила; каждый из Rи R, которые могут быть одинаковыми или различными, выбран из Cалкила, Cалкенила, арила, арил(C)алкила и гетероарила(C)алкила, каждый из которых может быть необязательно замещенным, или Rи Rмогут быть связаны вместе с образованием остатка (C)циклоалкильного кольца; X обозначает связывающую группу; Y обозначает необязательно замещенную арильную группу; Z обозначает кислород и Rобозначает Cалкил, Cциклоалкил, Cциклоалкил Cалкил, гетероарил, гетероарил(C)алкил, арил или арил(C)алкил, каждый из которых может быть необязательно замещен, или Z обозначает S(O), где n равно 0, 1 или 2, и Rобозначает Cалкил, Cциклоалкил, Cциклоалкил Cалкил, арил, арил(C)алкил, гетероарил или гетероарил(C)алкил, каждый из которых может быть необязательно замещен, являются ингибиторами фермента LpPLAи пригодны для использования в терапии, в частности для лечения атеросклероза.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA199800109A 1995-07-01 1996-06-20 Производные азетидинона для лечения атеросклероза EA199800109A1 (ru)

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
GBGB9608650.9A GB9608650D0 (en) 1996-04-26 1996-04-26 Novel compounds
GBGB9608651.7A GB9608651D0 (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
EA199800109A1 true EA199800109A1 (ru) 1998-10-29

Family

ID=27562921

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800109A EA199800109A1 (ru) 1995-07-01 1996-06-20 Производные азетидинона для лечения атеросклероза

Country Status (23)

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

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
GB9608649D0 (en) * 1996-04-26 1996-07-03 Smithkline Beecham Plc Novel compounds
PL329530A1 (en) * 1996-04-26 1999-03-29 Smithkline Beecham Plc Derivatives of azetidinone for use in treatment of arterial atheromatosis
AU2001235466B2 (en) * 2000-02-16 2004-04-22 Glaxo Group Limited Pyrimidine-4-one derivatives as LDL-PLA2 inhibitors
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
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
KR101461659B1 (ko) 2007-05-11 2014-11-17 토마스 제퍼슨 유니버시티 신경변성 질환 및 장애의 치료 및 예방 방법
EP2649053B1 (en) 2010-12-06 2015-11-04 Glaxo Group Limited Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by lp-pla2
US20130267544A1 (en) 2010-12-17 2013-10-10 Peter Adamson Use of LP-PLA2 Inhibitors in the Treatment and Prevention of Eye Diseases
US20140171431A1 (en) 2011-06-27 2014-06-19 Jianhua Shen 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 AND USE AS INHIBITORS OF LP-PLA2
BR112014001634A2 (pt) 2011-07-27 2017-02-14 Glaxo Group Ltd compostos bicíclicos de pirimidona
CN105008365B (zh) 2013-01-25 2017-03-15 葛兰素史密斯克莱知识产权发展有限公司 化合物
MX2015009633A (es) 2013-01-25 2015-11-30 Glaxosmithkline Ip Dev Ltd Inhibidores de fosfolipasa a2 asociada con lipoproteinas basados en 2,3-dihidroimidazol[1,2-c] pirimidin-5(1h)-ona.
AU2014210260B2 (en) 2013-01-25 2016-08-04 Glaxosmithkline Intellectual Property Development Limited Bicyclic pyrimidone compounds as inhibitors of 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
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
PE20230092A1 (es) 2019-11-09 2023-01-16 Shanghai Simr Biotechnology Co Ltd Derivado triciclico de dihidroimidazopirimidona, metodo de preparacion del mismo, composicion farmaceuticas y uso del mismo
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
DZ1958A1 (fr) * 1994-12-22 2002-02-17 Smithkline Beecham Plc Composés inhibiteurs de l'enzyme l-lpa compositionpharmaceutiques les composant et procédés pour leur préparation.

Also Published As

Publication number Publication date
WO1997002242A1 (en) 1997-01-23
OA10648A (en) 2002-09-25
NO976158D0 (no) 1997-12-30
TR199701762T1 (xx) 1998-05-21
CZ422197A3 (cs) 1998-06-17
AU6305096A (en) 1997-02-05
CN1197452A (zh) 1998-10-28
BR9609445A (pt) 1999-04-06
KR19990028630A (ko) 1999-04-15
HUP9901153A3 (en) 1999-11-29
AP728A (en) 1999-01-29
MA23922A1 (fr) 1996-12-31
MX9800186A (es) 1998-07-31
AP9701161A0 (en) 1998-01-31
BG102214A (en) 1998-08-31
IL122650A0 (en) 1998-08-16
PL324240A1 (en) 1998-05-11
CA2225627A1 (en) 1997-01-23
NZ311684A (en) 2000-04-28
NO976158L (no) 1998-02-25
AU708032B2 (en) 1999-07-29
SK178497A3 (en) 1998-07-08
HUP9901153A2 (hu) 1999-08-30
EP0840725A1 (en) 1998-05-13
PE8998A1 (es) 1998-03-20
JP2002515852A (ja) 2002-05-28

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