EA199800109A1 - Azetidinone derivatives for the treatment of atherosclerosis - Google Patents

Azetidinone derivatives for the treatment of atherosclerosis

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
Russian (ru)
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/en

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.Derivatives of azetidinone of the formula (I), wherein each of R and R, which may be the same or different, is selected from hydrogen, halogen or C1-6 alkyl; each of R and R, which may be the same or different, is selected from C1-6alkyl, Calkenyl, aryl, aryl (C) alkyl and heteroaryl (C) alkyl, each of which may be optionally substituted, or R and R may be bonded together to form a residue ( C) a cycloalkyl ring; X is a linking group; Y is an optionally substituted aryl group; Z is oxygen and R is C1-6alkyl, Cycloalkyl, Cycloalkyl C1-6alkyl, heteroaryl, heteroaryl (C) alkyl, aryl or aryl (C) alkyl, each of which may be optionally substituted, or Z is S (O), where n is 0, 1 or 2 and R. atherosclerosis. An international application was published with the report about international search.

EA199800109A 1995-07-01 1996-06-20 Azetidinone derivatives for the treatment of atherosclerosis EA199800109A1 (en)

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 (en) 1998-10-29

Family

ID=27562921

Family Applications (1)

Application Number Title Priority Date Filing Date
EA199800109A EA199800109A1 (en) 1995-07-01 1996-06-20 Azetidinone derivatives for the treatment of atherosclerosis

Country Status (23)

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

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000502079A (en) * 1995-12-08 2000-02-22 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 Monocyclic .BETA.-lactam derivatives for the treatment of atherosclerosis
GB9608649D0 (en) * 1996-04-26 1996-07-03 Smithkline Beecham Plc Novel compounds
EP0915843A1 (en) * 1996-04-26 1999-05-19 Smithkline Beecham Plc Azetidinone derivatives for the treatment of atheroscleroses
DE60139429D1 (en) * 2000-02-16 2009-09-10 Smithkline Beecham Plc Pyrimidine-5-onderivatives as LDL-PLA2 inhibitors
GB0024808D0 (en) 2000-10-10 2000-11-22 Smithkline Beecham Plc Novel compounds
US8962633B2 (en) 2007-05-11 2015-02-24 Thomas Jefferson University Methods of treatment and prevention of metabolic bone diseases and disorders
CN101687009A (en) 2007-05-11 2010-03-31 宾夕法尼亚大学理事会 Methods of treatment of skin ulcers
EA200971050A1 (en) 2007-05-11 2010-06-30 Томас Джефферсон Юниверсити METHODS OF TREATMENT AND PREVENTION OF NEURODEGENERATIVE DISEASES AND DISORDERS
TW201307324A (en) 2010-12-06 2013-02-16 Glaxo Group Ltd Compounds
EP2651403B1 (en) 2010-12-17 2020-12-02 Glaxo Group Limited Use of lp-pla2 inhibitors in the treatment and prevention of eye diseases
EP2725024A4 (en) 2011-06-27 2014-12-03 Shanghai Inst Materia Medica Azole heterocyclic compound, preparation method, pharmaceutical composition and use
BR112014001665A2 (en) 2011-07-27 2017-02-14 Glaxo Group Ltd 2,3-dihydroimidazo [1,2-c] pyrimidin-5 (1h) -one compounds used as lp-plaz inhibitors
TW201321382A (en) 2011-07-27 2013-06-01 Glaxo Group Ltd Compounds
CA2899143A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited Bicyclic pyrimidone compounds as inhibitors of lp-pla2
WO2014114248A1 (en) 2013-01-25 2014-07-31 Glaxosmithkline Intellectual Property Development Limited Compounds
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

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
SK80397A3 (en) * 1994-12-22 1998-01-14 Smithkline Beecham Plc Substituted azetidin-2-ones, preparation method thereof, farmaceutical compositions and their use

Also Published As

Publication number Publication date
AP9701161A0 (en) 1998-01-31
MX9800186A (en) 1998-07-31
BG102214A (en) 1998-08-31
HUP9901153A3 (en) 1999-11-29
IL122650A0 (en) 1998-08-16
CN1197452A (en) 1998-10-28
SK178497A3 (en) 1998-07-08
NZ311684A (en) 2000-04-28
EP0840725A1 (en) 1998-05-13
WO1997002242A1 (en) 1997-01-23
TR199701762T1 (en) 1998-05-21
PE8998A1 (en) 1998-03-20
CZ422197A3 (en) 1998-06-17
AU708032B2 (en) 1999-07-29
NO976158L (en) 1998-02-25
OA10648A (en) 2002-09-25
JP2002515852A (en) 2002-05-28
KR19990028630A (en) 1999-04-15
BR9609445A (en) 1999-04-06
NO976158D0 (en) 1997-12-30
PL324240A1 (en) 1998-05-11
AP728A (en) 1999-01-29
HUP9901153A2 (en) 1999-08-30
AU6305096A (en) 1997-02-05
CA2225627A1 (en) 1997-01-23
MA23922A1 (en) 1996-12-31

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