AR006833A1 - MONOCYCLE BETA LACTAM COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM, USE OF SUCH COMPOUNDS TO PREPARE MEDICINES, PROCEDURE TO PREPARE SUCH COMPOUNDS, INTERMEDIATE COMPOUNDS AND PROCEDURES TO PREPARE SUCH INTERMEDIATE COMPOUNDS. - Google Patents
MONOCYCLE BETA LACTAM COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM, USE OF SUCH COMPOUNDS TO PREPARE MEDICINES, PROCEDURE TO PREPARE SUCH COMPOUNDS, INTERMEDIATE COMPOUNDS AND PROCEDURES TO PREPARE SUCH INTERMEDIATE COMPOUNDS.Info
- Publication number
- AR006833A1 AR006833A1 ARP970101682A ARP970101682A AR006833A1 AR 006833 A1 AR006833 A1 AR 006833A1 AR P970101682 A ARP970101682 A AR P970101682A AR P970101682 A ARP970101682 A AR P970101682A AR 006833 A1 AR006833 A1 AR 006833A1
- Authority
- AR
- Argentina
- Prior art keywords
- compounds
- prepare
- procedures
- pharmaceutical composition
- composition containing
- Prior art date
Links
Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/04—Centrally acting analgesics, e.g. opioids
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P39/00—General protective or antinoxious agents
- A61P39/06—Free radical scavengers or antioxidants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Toxicology (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Cardiology (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Compuestos de beta-lactama monocíclicos de la fórmula (I), en la cual: R1 es hidrógeno o un éster correspondiente farmacéuticamente aceptable o unade sus sales farmacéuticamente aceptables; R2 y R3, que pueden ser iguales o diferentes, se seleccionan ambos de hidrógeno o alquilo C(1-6) sustituidoopcionalmente; X es un grupo X(CH2)m en el cual X es CO, CONR4, COO, CONR4CO, CONHO O CH2 en los cuales R4 es hidrógeno o alquilo C(1-6) y m es 0 oun número entero de 1 a 12; o una cadena de alquileno C(1-12) interrumpida opcionalmente por X; e Y es un grupo arilo sustituido opcionalmente; quetienen la configuración absoluta (4R, SS); son inhibidores de la enzima Lp-PLA2 y son útiles en el tratamiento de la aterosclerosis; composiciónfarmacéutica que los contiene, uso de dichos compuestos para preparar medicamentos, procedimiento para preparar dichos compuestos intermediarios yprocedimientos para preparar dichos compuestos intermediarios.Monocyclic beta-lactam compounds of formula (I), in which: R1 is hydrogen or a corresponding pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof; R2 and R3, which may be the same or different, are both selected from hydrogen or optionally substituted C (1-6) alkyl; X is a group X (CH2) m in which X is CO, CONR4, COO, CONR4CO, CONHO or CH2 in which R4 is hydrogen or C (1-6) alkyl and m is 0 or an integer from 1 to 12; or a C (1-12) alkylene chain optionally interrupted by X; and Y is an optionally substituted aryl group; which have the absolute configuration (4R, SS); they are inhibitors of the Lp-PLA2 enzyme and are useful in the treatment of atherosclerosis; pharmaceutical composition containing them, use of said compounds to prepare drugs, process to prepare said intermediate compounds and procedures to prepare said intermediate compounds.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9608646.7A GB9608646D0 (en) | 1996-04-26 | 1996-04-26 | Novel compounds |
| GBGB9623756.5A GB9623756D0 (en) | 1996-11-15 | 1996-11-15 | Novel compounds |
| GBGB9625121.0A GB9625121D0 (en) | 1996-12-03 | 1996-12-03 | Novel compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR006833A1 true AR006833A1 (en) | 1999-09-29 |
Family
ID=27268259
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP970101682A AR006833A1 (en) | 1996-04-26 | 1997-04-24 | MONOCYCLE BETA LACTAM COMPOUNDS, PHARMACEUTICAL COMPOSITION CONTAINING THEM, USE OF SUCH COMPOUNDS TO PREPARE MEDICINES, PROCEDURE TO PREPARE SUCH COMPOUNDS, INTERMEDIATE COMPOUNDS AND PROCEDURES TO PREPARE SUCH INTERMEDIATE COMPOUNDS. |
Country Status (17)
| Country | Link |
|---|---|
| EP (1) | EP0915843A1 (en) |
| JP (1) | JP2000509049A (en) |
| AR (1) | AR006833A1 (en) |
| AU (1) | AU2698697A (en) |
| BR (1) | BR9709196A (en) |
| CA (1) | CA2252696A1 (en) |
| CZ (1) | CZ341098A3 (en) |
| HU (1) | HUP9901359A3 (en) |
| ID (1) | ID16660A (en) |
| IL (1) | IL126696A0 (en) |
| MA (1) | MA26426A1 (en) |
| NO (1) | NO984939L (en) |
| NZ (1) | NZ332476A (en) |
| PE (1) | PE64398A1 (en) |
| PL (1) | PL329530A1 (en) |
| TR (1) | TR199802160T2 (en) |
| WO (1) | WO1997041098A1 (en) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE437862T1 (en) | 2000-02-16 | 2009-08-15 | Smithkline Beecham Plc | PYRIMIDINE-5-ONE DERIVATIVES AS LDL-PLA2 INHIBITORS |
| US6982251B2 (en) | 2000-12-20 | 2006-01-03 | Schering Corporation | Substituted 2-azetidinones useful as hypocholesterolemic agents |
| US7071181B2 (en) | 2001-01-26 | 2006-07-04 | Schering Corporation | Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors |
| MEP27808A (en) | 2001-01-26 | 2010-10-10 | Schering Corp | Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications |
| ATE331512T1 (en) | 2001-01-26 | 2006-07-15 | Schering Corp | USE OF AZETIDINONE SUBSTITUTED COMPOUNDS FOR THE TREATMENT OF SITOSTEROLHEMIA |
| CN1275949C (en) | 2001-03-28 | 2006-09-20 | 先灵公司 | Enantioselective Synthesis of 2-Azetidinone Intermediates |
| AR038956A1 (en) * | 2001-05-25 | 2005-02-02 | Schering Corp | USE OF A COMPOUND REGULATING THE PRODUCTION OR LEVELS OF BETA AMILOID PEPTIDES FOR THE MANUFACTURE OF A MEDICINAL PRODUCT TO TREAT ALZHEIMER'S DISEASE AND / OR TO REGULATE SUCH LEVELS OF BETA AMILOID PEPTIDES IN A SUBJECT |
| US7053080B2 (en) | 2001-09-21 | 2006-05-30 | Schering Corporation | Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors |
| JP2005504091A (en) | 2001-09-21 | 2005-02-10 | シェーリング コーポレイション | Treatment of xanthomas with azetidinone as a sterol absorption inhibitor |
| US7056906B2 (en) | 2001-09-21 | 2006-06-06 | Schering Corporation | Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women |
| WO2004043457A1 (en) | 2002-11-06 | 2004-05-27 | Schering Corporation | Cholesterol absorptions inhibitors for the treatment of autoimmune disorders |
| US7459442B2 (en) | 2003-03-07 | 2008-12-02 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| MXPA05009501A (en) | 2003-03-07 | 2005-10-18 | Schering Corp | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholeterolemia. |
| CA2517571C (en) | 2003-03-07 | 2011-07-05 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| EP1606287B1 (en) | 2003-03-07 | 2013-10-02 | Merck Sharp & Dohme Corp. | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| WO2008140449A1 (en) | 2007-05-11 | 2008-11-20 | Thomas Jefferson University | Methods of treatment and prevention of neurodegenerative diseases and disorders |
| EP2155225B1 (en) | 2007-05-11 | 2015-07-08 | The Trustees of the University of Pennsylvania | Methods of treatment of skin ulcers |
| UY33766A (en) | 2010-12-06 | 2012-06-29 | Glaxo Group Ltd | COMPOUNDS WITH PYRIMIDINONE STRUCTURE FOR USE IN THE TREATMENT OF DISEASES MEDIATED BY Lp-PLA2 |
| WO2012080497A2 (en) | 2010-12-17 | 2012-06-21 | Glaxo Group Limited | Methods of 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 |
| TW201321382A (en) | 2011-07-27 | 2013-06-01 | Glaxo Group Ltd | Compounds |
| 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 |
| PE20151251A1 (en) | 2013-01-25 | 2015-09-10 | Glaxosmithkline Ip Dev Ltd | DERIVATIVES [5,6] IMIDAZO PYRIMIDONE BICYCLIC WITH ACTIVITY ON LP-PLA2 ENZYMES |
| AU2014210259B2 (en) | 2013-01-25 | 2016-11-03 | Glaxosmithkline Intellectual Property Development Limited | Compounds |
| WO2014114249A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | 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 |
| EP4056571A4 (en) | 2019-11-09 | 2024-01-24 | 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 (14)
| 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 |
| IL89835A0 (en) * | 1988-04-11 | 1989-12-15 | Merck & Co Inc | Substituted azetidinones,their preparation and pharmaceutical compositions containing them |
| IL99658A0 (en) * | 1990-10-15 | 1992-08-18 | Merck & Co Inc | Substituted azetidinones and pharmaceutical compositions containing them |
| WO1993000332A1 (en) * | 1991-06-25 | 1993-01-07 | Merck & Co., Inc. | Substituted azetidinones as anti-inflammatory and antidegenerative agents |
| IL102582A0 (en) * | 1991-07-23 | 1993-01-14 | Schering Corp | Substituted beta-lactam compounds useful as hypocholesterolemic agents and processes for the preparation thereof |
| CA2108584C (en) * | 1992-10-27 | 1998-11-24 | James B. Doherty | Substituted azetidinones as anti-inflammatory and antidegenerative agents |
| WO1994013636A1 (en) * | 1992-12-17 | 1994-06-23 | Merck & Co., Inc. | New substituted azetidinones as anti-inflammatory and antidegenerative agents |
| EP0658205B1 (en) * | 1993-06-25 | 2000-03-15 | Smithkline Beecham Plc | Lipoprotein associated phospholipase a2, inhibitors thereof and use of the same in diagnosis and therapy |
| DE69434609T2 (en) * | 1993-10-06 | 2006-09-21 | Icos Corp., Bothell | Acethylhydrolase of the platelet activating factor |
| 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 |
| WO1996029307A1 (en) * | 1995-03-23 | 1996-09-26 | Japan Tobacco Inc. | Diphenylmethyl-azetidinone compounds and elastase inhibitor |
| TR199701762T1 (en) * | 1995-07-01 | 1998-05-21 | Smithkline Beecham P.L.C. | Azetidinone derivatives for the treatment of atherosclerosis. |
| WO1997021676A1 (en) * | 1995-12-08 | 1997-06-19 | Smithkline Beecham Plc | Azetidinone compounds for the treatment of atherosclerosis |
-
1997
- 1997-04-15 IL IL12669697A patent/IL126696A0/en unknown
- 1997-04-15 CA CA002252696A patent/CA2252696A1/en not_active Abandoned
- 1997-04-15 HU HU9901359A patent/HUP9901359A3/en unknown
- 1997-04-15 CZ CZ983410A patent/CZ341098A3/en unknown
- 1997-04-15 WO PCT/EP1997/001898 patent/WO1997041098A1/en not_active Ceased
- 1997-04-15 JP JP9538507A patent/JP2000509049A/en active Pending
- 1997-04-15 TR TR1998/02160T patent/TR199802160T2/en unknown
- 1997-04-15 AU AU26986/97A patent/AU2698697A/en not_active Abandoned
- 1997-04-15 PL PL97329530A patent/PL329530A1/en unknown
- 1997-04-15 BR BR9709196A patent/BR9709196A/en not_active Application Discontinuation
- 1997-04-15 EP EP97920699A patent/EP0915843A1/en not_active Withdrawn
- 1997-04-15 NZ NZ332476A patent/NZ332476A/en unknown
- 1997-04-24 PE PE1997000311A patent/PE64398A1/en not_active Application Discontinuation
- 1997-04-24 AR ARP970101682A patent/AR006833A1/en unknown
- 1997-04-24 MA MA24565A patent/MA26426A1/en unknown
- 1997-04-25 ID IDP971394A patent/ID16660A/en unknown
-
1998
- 1998-10-23 NO NO984939A patent/NO984939L/en not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| NO984939L (en) | 1998-12-23 |
| HUP9901359A2 (en) | 1999-08-30 |
| MA26426A1 (en) | 2004-12-20 |
| BR9709196A (en) | 1999-05-25 |
| HUP9901359A3 (en) | 2000-03-28 |
| PE64398A1 (en) | 1999-01-06 |
| NZ332476A (en) | 2000-06-23 |
| CZ341098A3 (en) | 1999-03-17 |
| JP2000509049A (en) | 2000-07-18 |
| NO984939D0 (en) | 1998-10-23 |
| CA2252696A1 (en) | 1997-11-06 |
| WO1997041098A1 (en) | 1997-11-06 |
| EP0915843A1 (en) | 1999-05-19 |
| IL126696A0 (en) | 1999-08-17 |
| PL329530A1 (en) | 1999-03-29 |
| TR199802160T2 (en) | 1999-04-21 |
| ID16660A (en) | 1997-10-30 |
| AU2698697A (en) | 1997-11-19 |
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