AR035068A1 - Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestos - Google Patents
Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestosInfo
- Publication number
- AR035068A1 AR035068A1 ARP010104761A ARP010104761A AR035068A1 AR 035068 A1 AR035068 A1 AR 035068A1 AR P010104761 A ARP010104761 A AR P010104761A AR P010104761 A ARP010104761 A AR P010104761A AR 035068 A1 AR035068 A1 AR 035068A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- mono
- halogen
- optionally substituted
- compounds
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- 239000003814 drug Substances 0.000 title abstract 2
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 11
- 229910052736 halogen Inorganic materials 0.000 abstract 8
- 150000002367 halogens Chemical class 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 5
- 229910052739 hydrogen Inorganic materials 0.000 abstract 5
- 239000001257 hydrogen Substances 0.000 abstract 5
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 5
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 4
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 4
- 125000003118 aryl group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 125000005010 perfluoroalkyl group Chemical group 0.000 abstract 4
- 125000004400 (C1-C12) alkyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 abstract 3
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 abstract 2
- YNAVUWVOSKDBBP-UHFFFAOYSA-N Morpholine Chemical compound C1COCCN1 YNAVUWVOSKDBBP-UHFFFAOYSA-N 0.000 abstract 2
- 229920001774 Perfluoroether Polymers 0.000 abstract 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 abstract 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 2
- 229910052757 nitrogen Inorganic materials 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 229910052717 sulfur Inorganic materials 0.000 abstract 2
- 125000006595 (C1-C3) alkylsulfinyl group Chemical group 0.000 abstract 1
- 125000004455 (C1-C3) alkylthio group Chemical group 0.000 abstract 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 1
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 1
- 102000016752 1-Alkyl-2-acetylglycerophosphocholine Esterase Human genes 0.000 abstract 1
- 125000004575 3-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 108010024976 Asparaginase Proteins 0.000 abstract 1
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000005157 alkyl carboxy group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 abstract 1
- 125000005605 benzo group Chemical group 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 125000002837 carbocyclic group Chemical group 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 125000005842 heteroatom Chemical group 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 abstract 1
- 125000004043 oxo group Chemical group O=* 0.000 abstract 1
- 239000001301 oxygen Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 239000011593 sulfur Chemical group 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/34—One oxygen atom
- C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
-
- 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
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/04—Antibacterial agents
-
- 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
-
- 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
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
- C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 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
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Rheumatology (AREA)
- Neurosurgery (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Emergency Medicine (AREA)
- Pain & Pain Management (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Hospice & Palliative Care (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Obesity (AREA)
- Urology & Nephrology (AREA)
- Immunology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Compuestos de pirimidinona de fórmula (1) en donde: R1 es un grupo arilo, opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquiltio C1-6, hidroxi, halógeno, CN, y mono a perfluoroalquilo C1-4; R2 es halógeno, alquilo C1-3, alcoxi C1-3, hidroxialquilo C1-3, alquiltio C1-3, alquilsulfinilo C1-3, aminoalquilo C1-3, mono- o dialquil C1-3aminoalquilo C1-3, alquil C1-3carbonilaminoalquilo C1-3, alcoxi C1-3alquil C1-3carbonilaminoalquilo C1-3, alquil C1-3sulfonilaminoalquilo C1-3, alquil C1-3carboxi, alquil C1-3carboxialquilo C1-3, y R3 es hidrógeno, halógeno, alquilo C1-3, o hidroxialquilo C1-3; o R2 y R3 junto con los átomos de C del anillo de pirimidona a los que están unidos forman un anillo carbocíclico condensado de 5- o 6-miembros; o R2 y R3 junto con los átomos de C del anillo de pirimidona a los que están unidos forman un anillo benzo o heteroarílico condensado, opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes, que pueden ser iguales o diferentes, seleccionados de halógeno, alquilo C1-4, ciano, alcoxi C1-6, alquil C1-6tio, o mono a perfluoroalquilo C1-4; R4 es hidrógeno, alquilo C1-6 que puede estar sustituido o no sustituido con 1, 2 ó 3 sustituyentes seleccionados de hidroxi, halógeno, OR7, COR7, carboxi, COOR7, CONR9R10, NR9R10, NR7COR8, mono. o di-(hidroxialquil C1-6)amino y N-hidroxialquil C1-6-N-alquil C1-6amino; o R4 es Het-alquilo C0-4 en el que Het es un anillo heterociclilo de 5- a 7-miembros que contiene N y opcionalmente O ó S, y en el que N puede estar sustituido con COR7, COOR7, CONR9R10, o alquilo C1-6 opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados de hidroxi, halógeno, OR7, COR7, carboxi, COOR7, CONR9R10 o NR9R10, por ejemplo, piperidin-4-ilo, pirrolidin-3-ilo; R5 es arilo o un anillo heteroarílico opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquil C1-6tio, arilalcoxi C1-6, hidroxi, halógeno, CN, COR7, carboxi, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono a perfluoroalquilo C1-4 y mono a perfluoroalcoxi C1-4; R6 es arilo o un anillo heteroarílico que está además opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-18, alcoxi C1-18, alquil C1-6tio, alquil C1-6sulfonilo, arilalcoxi C1-6, hidroxi, halógeno, CN, COR7, carboxi, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono a perfluoroalquilo C1-4 y mono a perfluoroalcoxi C1-4, o alquilo C5-10; R7 es hidrógeno o alquilo C1-12, por ejemplo alquilo C1-4 (v.g. metilo o etilo); R8 es hidrógeno, O-alquilo C1-6, o alquilo C1-12, por ejemplo alquilo C1-4 (v.g. metilo o etilo); R9 y R10 que pueden ser iguales o diferentes se seleccionan cada uno de hidrógeno, o alquilo C1-12, o R9 y R10 junto con el nitrógeno al que están unidos forman un anillo de 5- a 7-miembros que contiene opcionalmente uno o más heteroátomos adicionales seleccionados de oxígeno, nitrógeno y azufre, y está opcionalmente sustituido con 1 ó 2 sustituyentes seleccionados de hidroxi, oxo, alquilo C1-4, alquil C1-4carboxi, arilo, v.g. fenilo, o aralquilo, v.g. bencilo, ppor ejemplo, morfolina o piperazina; y X es alquileno C2-4, opcionalmente sustituido con 1, 2 ó 3 sustituyentes seleccionados de metilo, etilo, o CH=CH. Dichos compuestos tienen buena actividad como inhibidores de la enzima Lp-PLA2 y por lo tanto son útiles en terapia, en particular para el tratamiento de la ateroesclerosis. También se dan a conocer un proceso para su preparación, composiciones farmacéuticas que los comprenden, y el uso de tales compuestos en la fabricación de medicamentos.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0024807.0A GB0024807D0 (en) | 2000-10-10 | 2000-10-10 | Novel compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR035068A1 true AR035068A1 (es) | 2004-04-14 |
Family
ID=9901005
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP010104761A AR035068A1 (es) | 2000-10-10 | 2001-10-10 | Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestos |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US7169924B2 (es) |
| EP (1) | EP1337517B1 (es) |
| JP (1) | JP2004511473A (es) |
| AR (1) | AR035068A1 (es) |
| AT (1) | ATE415392T1 (es) |
| AU (1) | AU2002223599A1 (es) |
| CA (1) | CA2459746A1 (es) |
| DE (1) | DE60136736D1 (es) |
| ES (1) | ES2317949T3 (es) |
| GB (1) | GB0024807D0 (es) |
| WO (1) | WO2002030911A1 (es) |
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE437862T1 (de) * | 2000-02-16 | 2009-08-15 | Smithkline Beecham Plc | Pyrimidin-5-onderivate als ldl-pla2 inhibitoren |
| GB0024807D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| GB0119793D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel compounds |
| GB0127139D0 (en) * | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
| GB0127140D0 (en) * | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
| GB0208279D0 (en) * | 2002-04-10 | 2002-05-22 | Glaxo Group Ltd | Novel compounds |
| GB0208280D0 (en) * | 2002-04-10 | 2002-05-22 | Glaxo Group Ltd | Novel compounds |
| EP1735457A4 (en) | 2004-04-16 | 2007-08-29 | Glaxo Group Ltd | METHODS FOR DETECTING Lp-PLA2 ACTIVITY AND INHIBITION OF Lp-PLA2 ACTIVITY |
| US20150017671A1 (en) | 2004-04-16 | 2015-01-15 | Yaping Shou | Methods for detecting lp-pla2 activity and inhibition of lp-pla2 activity |
| JP2009521427A (ja) * | 2005-12-23 | 2009-06-04 | アストラゼネカ・アクチエボラーグ | 胃食道逆流症及び過敏性腸症候群の治療のためのピラゾール |
| US20080090851A1 (en) * | 2006-10-13 | 2008-04-17 | Colin Andrew Leach | Bicyclic Heteroaromatic Compounds |
| US7705005B2 (en) * | 2006-10-13 | 2010-04-27 | Glaxo Group Limited | Bicyclic heteroaromatic compounds |
| US20080090852A1 (en) * | 2006-10-13 | 2008-04-17 | Colin Andrew Leach | Bicyclic Heteroaromatic Compounds |
| JP2010506852A (ja) * | 2006-10-13 | 2010-03-04 | グラクソ グループ リミテッド | 二環式ヘテロ芳香族化合物 |
| 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 |
| EP2583099B1 (en) | 2010-06-18 | 2016-11-02 | Whitehead Institute for Biomedical Research | Pla2g16 as a target for antiviral compounds |
| UY33766A (es) | 2010-12-06 | 2012-06-29 | Glaxo Group Ltd | COMPUESTOS CON ESTRUCTURA DE PIRIMIDINONA PARA USO EN EL TRATAMIENTO DE ENFERMEDADES MEDIADAS POR Lp-PLA2 |
| WO2012080497A2 (en) | 2010-12-17 | 2012-06-21 | Glaxo Group Limited | Methods of treatment and prevention of eye diseases |
| WO2012129792A1 (zh) * | 2011-03-30 | 2012-10-04 | 中国科学院上海药物研究所 | 嘧啶酮类化合物、其制备方法及药物组合物和用途 |
| US20140171431A1 (en) | 2011-06-27 | 2014-06-19 | Jianhua Shen | Azole heterocyclic compound, preparation method, pharmaceutical composition and use |
| TW201321382A (zh) | 2011-07-27 | 2013-06-01 | Glaxo Group Ltd | 化合物 |
| 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 |
| FR2994184B1 (fr) * | 2012-08-02 | 2017-12-08 | Biomerieux Sa | Procedes de fonctionalisation et reactifs utilises dans de tels procedes utilisant un anhydride aza-isatoique ou un de ses derives, molecules biologiques ainsi traitees et kits |
| PE20151251A1 (es) | 2013-01-25 | 2015-09-10 | Glaxosmithkline Ip Dev Ltd | Derivados [5,6] biciclicos de imidazo pirimidona con actividad sobre enzimas lp-pla2 |
| 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 |
| US20140283157A1 (en) | 2013-03-15 | 2014-09-18 | Diadexus, Inc. | Lipoprotein-associated phospholipase a2 antibody compositions and methods of use |
| 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 |
| CN107709314A (zh) | 2015-06-11 | 2018-02-16 | 巴斯利尔药物国际股份公司 | 外排泵抑制剂及其治疗性用途 |
| CN111825695B (zh) * | 2019-04-15 | 2022-04-12 | 中国科学院上海药物研究所 | 噁唑烷酮类化合物、其制备方法、用途及其药物组合物 |
| US11591840B1 (en) * | 2019-10-31 | 2023-02-28 | Andersen Corporation | Power window operators, windows and methods |
| EP4056571A4 (en) | 2019-11-09 | 2024-01-24 | Shanghai Simr Biotechnology Co., Ltd. | TRICYCLIC DIHYDROIMIDAZOPYRIMIDONE DERIVATIVE, METHOD FOR THE PRODUCTION THEREOF, PHARMACEUTICAL COMPOSITION AND USE THEREOF |
| 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 |
| WO2025024605A1 (en) * | 2023-07-25 | 2025-01-30 | University Of Florida Research Foundation, Incorporated | Rev-erb antagonists |
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|---|---|---|---|---|
| EP1028955B1 (en) * | 1997-11-06 | 2003-07-16 | SmithKline Beecham plc | Pyrimidinone compounds and pharmaceutical compositions containing them |
| ATE437862T1 (de) * | 2000-02-16 | 2009-08-15 | Smithkline Beecham Plc | Pyrimidin-5-onderivate als ldl-pla2 inhibitoren |
| GB0024807D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| US6649610B1 (en) * | 2001-05-23 | 2003-11-18 | University Of Central Florida | 2-oxo-1, 4-benzoxazine compounds for treatment of tuberculosis |
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2000
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- 2001-10-05 ES ES01986682T patent/ES2317949T3/es not_active Expired - Lifetime
- 2001-10-05 JP JP2002534297A patent/JP2004511473A/ja active Pending
- 2001-10-05 DE DE60136736T patent/DE60136736D1/de not_active Expired - Lifetime
- 2001-10-05 AU AU2002223599A patent/AU2002223599A1/en not_active Abandoned
- 2001-10-05 CA CA002459746A patent/CA2459746A1/en not_active Abandoned
- 2001-10-05 AT AT01986682T patent/ATE415392T1/de not_active IP Right Cessation
- 2001-10-05 US US10/398,977 patent/US7169924B2/en not_active Expired - Fee Related
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2006
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| US7462620B2 (en) | 2008-12-09 |
| US20040058941A1 (en) | 2004-03-25 |
| ES2317949T3 (es) | 2009-05-01 |
| JP2004511473A (ja) | 2004-04-15 |
| DE60136736D1 (de) | 2009-01-08 |
| EP1337517B1 (en) | 2008-11-26 |
| CA2459746A1 (en) | 2002-04-18 |
| EP1337517A1 (en) | 2003-08-27 |
| GB0024807D0 (en) | 2000-11-22 |
| US20060241126A1 (en) | 2006-10-26 |
| US7169924B2 (en) | 2007-01-30 |
| AU2002223599A1 (en) | 2002-04-22 |
| WO2002030911A1 (en) | 2002-04-18 |
| ATE415392T1 (de) | 2008-12-15 |
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