NZ311684A - Azetidinone derivatives, preparation, and use for treating atherosclerosis - Google Patents
Azetidinone derivatives, preparation, and use for treating atherosclerosisInfo
- Publication number
- NZ311684A NZ311684A NZ311684A NZ31168496A NZ311684A NZ 311684 A NZ311684 A NZ 311684A NZ 311684 A NZ311684 A NZ 311684A NZ 31168496 A NZ31168496 A NZ 31168496A NZ 311684 A NZ311684 A NZ 311684A
- Authority
- NZ
- New Zealand
- Prior art keywords
- alkyl
- aryl
- heteroaryl
- optionally substituted
- hydrogen
- 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
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
Azetidinone compounds of formula as above in which: R1 and R2, which may be the same or different, is each selected from hydrogen, halogen or C(1-8)alkyl; R4 and R5 which may be the same or different is each selected from hydrogen, C(1-6)alkyl, C(2-6)alkenyl, aryl, aryl(C1-4)alkyl and heteroaryl(C1-4)alkyl each of which may be optionally substituted or R4 and R5 may be linked together to form the remainder of a (C3-7)cycloalkyl ring; X is a direct bond; a group X1(CH2)m in which X1 is CO, CONR6 , COO, CONR6CO, or CONR6O in which R6 is hydrogen of C(1-6)alkyl and m is 0 or an integer from 1 to 12; a group (X1)aX2 in which a is 0 or 1 and X2 is a C(1-12) alkylene chain interrupted and /or terminated at the end adjacent to Y by one or more groups X3 selected from O, S(O)X, NR6, alkene or alkyne, in which x is 0, 1, 2, or a C(1-12) alkylene chain optionally interrupted by X1; Y is an optionally substituted aryl group; Z is oxygen and R3 is C(1-8)alkyl, C(3-8)cycloalkyl, C(3-8)cycloalkylC(1-6)alkyl, heteroaryl, heteroaryl(C1-4)alkyl, aryl, or aryl(C1-4)alkyl, each of which may be optionally substituted or Z is S(O)n in which n is 0, 1 or 2 and R3 is C(1-8)alkyl, C(3-8)cycloalkyl, C(3-8)cycloalkylC(1-6)alkyl, aryl, aryl(C1-4)alkyl, heteroaryl, or heteroaryl(C1-4)alkyl, each of which may be optionally substituted are inhibitors of the enzyme Lp PLA2 and are of use in therapy, in particular treating atherosclerosis.
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 |
|---|---|
| NZ311684A true NZ311684A (en) | 2000-04-28 |
Family
ID=27562921
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| NZ311684A NZ311684A (en) | 1995-07-01 | 1996-06-20 | Azetidinone derivatives, preparation, and use for treating 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 |
|---|---|---|---|---|
| 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 |
| HUP9901359A3 (en) * | 1996-04-26 | 2000-03-28 | Smithkline Beecham Plc | Azetidinone derivatives for the treatment of atherosclerosis, process for their producing and pharmaceutical compositions containing them |
| AU3546601A (en) | 2000-02-16 | 2001-08-27 | Smithkline Beecham Plc | Pyrimidine-4-one derivatives as LDL-PLA<sub>2</sub> inhibitors |
| GB0024808D0 (en) | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| MX2009012197A (en) | 2007-05-11 | 2010-01-15 | Univ 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 |
| EP2977452A3 (en) | 2007-05-11 | 2016-05-25 | Thomas Jefferson University | Methods of treatment and prevention of neurodegenerative diseases and disorders |
| MX2013006342A (en) | 2010-12-06 | 2013-08-26 | Glaxo Group Ltd | 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 |
| 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 |
| EP2736908A1 (en) | 2011-07-27 | 2014-06-04 | Glaxo Group Limited | Bicyclic pyrimidone compounds |
| CN105008365B (en) | 2013-01-25 | 2017-03-15 | 葛兰素史密斯克莱知识产权发展有限公司 | Compound |
| SG11201505520WA (en) | 2013-01-25 | 2015-08-28 | Glaxosmithkline Ip Dev Ltd | 2,3-DIHYDROIMIDAZOL[1,2-C]PYRIMIDIN-5(1H)-ONE BASED LIPOPROTEIN-ASSOCIATED PHOSPHOLIPASE A2 (LP-PLA<sb>2</sb>) INHIBITORS |
| EP2948456A4 (en) | 2013-01-25 | 2016-09-14 | Glaxosmithkline Ip Dev Ltd | Bicyclic pyrimidone compounds as inhibitors of 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 |
| 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 |
| AU2020379796C1 (en) | 2019-11-09 | 2024-05-02 | Shanghai SIMR Biotechnology Co., Ltd | Tricyclic dihydroimidazopyrimidone derivative, preparation method therefor, pharmaceutical composition and use 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 |
| CA2208530A1 (en) * | 1994-12-22 | 1996-06-27 | Smithkline Beecham P.L.C. | Substituted azetidin-2-ones for treatment of atherosclerosis |
-
1996
- 1996-06-20 KR KR1019970709952A patent/KR19990028630A/en not_active Application Discontinuation
- 1996-06-20 JP JP50477297A patent/JP2002515852A/en active Pending
- 1996-06-20 NZ NZ311684A patent/NZ311684A/en unknown
- 1996-06-20 EP EP96922030A patent/EP0840725A1/en not_active Withdrawn
- 1996-06-20 BR BR9609445A patent/BR9609445A/en unknown
- 1996-06-20 IL IL12265096A patent/IL122650A0/en unknown
- 1996-06-20 TR TR97/01762T patent/TR199701762T1/en unknown
- 1996-06-20 AU AU63050/96A patent/AU708032B2/en not_active Ceased
- 1996-06-20 CN CN96196661A patent/CN1197452A/en active Pending
- 1996-06-20 AP APAP/P/1997/001161A patent/AP728A/en active
- 1996-06-20 SK SK1784-97A patent/SK178497A3/en unknown
- 1996-06-20 HU HU9901153A patent/HUP9901153A3/en unknown
- 1996-06-20 WO PCT/EP1996/002765 patent/WO1997002242A1/en not_active Application Discontinuation
- 1996-06-20 CZ CZ974221A patent/CZ422197A3/en unknown
- 1996-06-20 CA CA002225627A patent/CA2225627A1/en not_active Abandoned
- 1996-06-20 EA EA199800109A patent/EA199800109A1/en unknown
- 1996-06-20 PL PL96324240A patent/PL324240A1/en unknown
- 1996-06-28 MA MA24298A patent/MA23922A1/en unknown
- 1996-06-28 PE PE1996000496A patent/PE8998A1/en not_active Application Discontinuation
-
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 |
|---|---|
| NO976158D0 (en) | 1997-12-30 |
| MX9800186A (en) | 1998-07-31 |
| EP0840725A1 (en) | 1998-05-13 |
| AU708032B2 (en) | 1999-07-29 |
| IL122650A0 (en) | 1998-08-16 |
| JP2002515852A (en) | 2002-05-28 |
| TR199701762T1 (en) | 1998-05-21 |
| NO976158L (en) | 1998-02-25 |
| HUP9901153A3 (en) | 1999-11-29 |
| AP728A (en) | 1999-01-29 |
| BR9609445A (en) | 1999-04-06 |
| AU6305096A (en) | 1997-02-05 |
| KR19990028630A (en) | 1999-04-15 |
| SK178497A3 (en) | 1998-07-08 |
| BG102214A (en) | 1998-08-31 |
| WO1997002242A1 (en) | 1997-01-23 |
| MA23922A1 (en) | 1996-12-31 |
| PL324240A1 (en) | 1998-05-11 |
| OA10648A (en) | 2002-09-25 |
| CZ422197A3 (en) | 1998-06-17 |
| CN1197452A (en) | 1998-10-28 |
| CA2225627A1 (en) | 1997-01-23 |
| PE8998A1 (en) | 1998-03-20 |
| HUP9901153A2 (en) | 1999-08-30 |
| AP9701161A0 (en) | 1998-01-31 |
| EA199800109A1 (en) | 1998-10-29 |
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