EA199800109A1 - Azetidinone derivatives for the treatment of atherosclerosis - Google Patents
Azetidinone derivatives for the treatment of atherosclerosisInfo
- 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
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.
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 |
---|---|
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)
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 |
CZ341098A3 (en) * | 1996-04-26 | 1999-03-17 | Smithkline Beecham Plc | Azetidinone derivatives for treating atherosclerosis |
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 |
MX2009012188A (en) | 2007-05-11 | 2010-02-24 | Univ Jefferson | Methods of treatment and prevention of neurodegenerative diseases and disorders. |
US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
CN105748480A (en) | 2007-05-11 | 2016-07-13 | 宾夕法尼亚大学理事会 | Methods of treatment of skin ulcers |
US8637536B2 (en) | 2010-12-06 | 2014-01-28 | Glaxo Group Limited | Pyrimidinone compounds for use in the treatment of diseases or conditions mediated by Lp-PLA2 |
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 |
CA2843102A1 (en) | 2011-07-27 | 2013-01-31 | Glaxo Group Limited | Bicyclic pyrimidone compounds |
CA2842965A1 (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 |
BR112015017759B1 (en) | 2013-01-25 | 2022-05-24 | Glaxosmithkline Intellectual Property Development Limited | LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 INHIBITOR COMPOUNDS (LP-PLA2) BASED ON 2,3-DIHYDROIMIDAZOLE[1,2-C]PYRIMIDIN5(1H)-ONA, AND A PHARMACEUTICAL COMPOSITION COMPRISING SUCH COMPOUNDS |
JP2016508995A (en) | 2013-01-25 | 2016-03-24 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドGlaxosmithkline Intellectual Property Development Limited | Compound |
CA2899143A1 (en) | 2013-01-25 | 2014-07-31 | 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 |
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)
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 |
MA23834A1 (en) * | 1994-12-22 | 1996-10-01 | Smithkline Beecham Plc | PROCESS FOR THE PREPARATION OF INHIBITOR COMPOUNDS OF THE LP-PLA2 ENZYME AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM |
-
1996
- 1996-06-20 HU HU9901153A patent/HUP9901153A3/en unknown
- 1996-06-20 TR TR97/01762T patent/TR199701762T1/en unknown
- 1996-06-20 EA EA199800109A patent/EA199800109A1/en unknown
- 1996-06-20 JP JP50477297A patent/JP2002515852A/en active Pending
- 1996-06-20 NZ NZ311684A patent/NZ311684A/en unknown
- 1996-06-20 BR BR9609445A patent/BR9609445A/en unknown
- 1996-06-20 CA CA002225627A patent/CA2225627A1/en not_active Abandoned
- 1996-06-20 IL IL12265096A patent/IL122650A0/en unknown
- 1996-06-20 CN CN96196661A patent/CN1197452A/en active Pending
- 1996-06-20 PL PL96324240A patent/PL324240A1/en unknown
- 1996-06-20 AU AU63050/96A patent/AU708032B2/en not_active Ceased
- 1996-06-20 SK SK1784-97A patent/SK178497A3/en unknown
- 1996-06-20 WO PCT/EP1996/002765 patent/WO1997002242A1/en not_active Application Discontinuation
- 1996-06-20 KR KR1019970709952A patent/KR19990028630A/en not_active Application Discontinuation
- 1996-06-20 EP EP96922030A patent/EP0840725A1/en not_active Withdrawn
- 1996-06-20 AP APAP/P/1997/001161A patent/AP728A/en active
- 1996-06-20 CZ CZ974221A patent/CZ422197A3/en unknown
- 1996-06-28 PE PE1996000496A patent/PE8998A1/en not_active Application Discontinuation
- 1996-06-28 MA MA24298A patent/MA23922A1/en unknown
-
1997
- 1997-12-30 NO NO976158A patent/NO976158L/en unknown
- 1997-12-31 OA OA70172A patent/OA10648A/en unknown
-
1998
- 1998-01-07 MX MX9800186A patent/MX9800186A/en unknown
- 1998-01-28 BG BG102214A patent/BG102214A/en unknown
Also Published As
Publication number | Publication date |
---|---|
AU6305096A (en) | 1997-02-05 |
PE8998A1 (en) | 1998-03-20 |
HUP9901153A3 (en) | 1999-11-29 |
CZ422197A3 (en) | 1998-06-17 |
BR9609445A (en) | 1999-04-06 |
MX9800186A (en) | 1998-07-31 |
JP2002515852A (en) | 2002-05-28 |
SK178497A3 (en) | 1998-07-08 |
PL324240A1 (en) | 1998-05-11 |
EP0840725A1 (en) | 1998-05-13 |
OA10648A (en) | 2002-09-25 |
NZ311684A (en) | 2000-04-28 |
AP9701161A0 (en) | 1998-01-31 |
BG102214A (en) | 1998-08-31 |
IL122650A0 (en) | 1998-08-16 |
HUP9901153A2 (en) | 1999-08-30 |
KR19990028630A (en) | 1999-04-15 |
NO976158L (en) | 1998-02-25 |
NO976158D0 (en) | 1997-12-30 |
TR199701762T1 (en) | 1998-05-21 |
AP728A (en) | 1999-01-29 |
CN1197452A (en) | 1998-10-28 |
WO1997002242A1 (en) | 1997-01-23 |
AU708032B2 (en) | 1999-07-29 |
MA23922A1 (en) | 1996-12-31 |
CA2225627A1 (en) | 1997-01-23 |
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