AR035349A1 - 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
- AR035349A1 AR035349A1 ARP010104760A ARP010104760A AR035349A1 AR 035349 A1 AR035349 A1 AR 035349A1 AR P010104760 A ARP010104760 A AR P010104760A AR P010104760 A ARP010104760 A AR P010104760A AR 035349 A1 AR035349 A1 AR 035349A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- mono
- halogen
- compounds
- alkoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 8
- 238000004519 manufacturing process Methods 0.000 title abstract 3
- 239000003814 drug Substances 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 2
- 238000002360 preparation method Methods 0.000 title abstract 2
- 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
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 7
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 5
- 101100440695 Dictyostelium discoideum corB gene Proteins 0.000 abstract 5
- 125000003118 aryl group Chemical group 0.000 abstract 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 3
- -1 C1- alkylthio 6 Chemical group 0.000 abstract 3
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 abstract 3
- 125000005010 perfluoroalkyl group Chemical group 0.000 abstract 3
- 125000004400 (C1-C12) 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
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 2
- 125000002102 aryl alkyloxo group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 abstract 2
- 229910052760 oxygen Inorganic materials 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical group OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 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
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl 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
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 108010024976 Asparaginase Proteins 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 238000010640 amide synthesis reaction Methods 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [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
- 125000004181 carboxyalkyl 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
- 125000002496 methyl group Chemical group [H]C([H])([H])* 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
- 125000004482 piperidin-4-yl group Chemical group N1CCC(CC1)* 0.000 abstract 1
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 abstract 1
- 239000011593 sulfur Substances 0.000 abstract 1
- 238000002560 therapeutic procedure Methods 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
- C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
- C07D221/04—Ortho- or peri-condensed ring systems
-
- 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
- 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
- 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
-
- 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
- A61P9/12—Antihypertensives
-
- C—CHEMISTRY; METALLURGY
- C04—CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
- C04B—LIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
- C04B35/00—Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/622—Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
- C04B35/626—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
- C04B35/63—Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
- C04B35/632—Organic additives
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D211/74—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
- C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
- C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D215/36—Sulfur atoms
-
- 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
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Ceramic Engineering (AREA)
- Manufacturing & Machinery (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Cardiology (AREA)
- Rheumatology (AREA)
- Structural Engineering (AREA)
- Materials Engineering (AREA)
- Inorganic Chemistry (AREA)
- Hematology (AREA)
- Pain & Pain Management (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Pyridine Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos de pirimidinona de fórmula (1) en la que: R1 es un grupo arilo, opcionalmente sustituido con 1, 2, 3 o 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, mono a perfluoro-alcoxi C1-4 arilo, y arilalquilo 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 di-alquil C1-3 aminoalquilo C1-3, alquil C1-3 carbonilaminoalquilo C1-3, alcoxi C1-3 alquil C1-3 carbonilaminoalquilo C1-3, alquil C1-3 sulfonilaminoalquilo C1-3, alquil C1-3 carboxi, alquil C1-3 carboxialquilo C1-3; R3 es hidrógeno, halógeno, alquilo C1-3, o hidroxialquilo C1-3; o R2 y R3 junto con los átomos de carbono del anillo de piridona a los que están unidos forman un anillo carbocíclico condensado de 5- o 6-miembros; o R2 y R3 junto con los átomos de carbono del anillo de piridona a los que están unidos forman un anillo benzo o heteroarílico condensado, opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes, que pueden ser iguales o diferentes, seleccionados de halógeno, alquilo C1-4, ciano, alcoxi C1-3-alquilo C1-3, alcoxi C1-4, o alquil C1-4 tio, o mono a perfluoroalquilo C1-4; R4 es hidrógeno, alquilo C1-6 que puede estar sustituido o no sustituido con 1, 2 o 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 C1-6 amino; o R4 es Het-alquilo C0-4 en el que Het es un anillo heterociclilo de 5 a 7 miembros que comprende N y opcionalmente O o S, y en el que N puede estar sustituido con COR7, COOR7, CONR9R10, o alquilo C1-6 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de hidroxi, halógeno, OR7, COR7, carboxi, COOR7, CONR9R10 o NR9R10, por ejemplo, piperidin-4-ilo, pirrolidin-3-ilo; R5 es un arilo o un anillo heteroarílico opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquil C1-6 tio, 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 un arilo o un anillo heteroarílico que está además opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquil C1-6 tio, alquil C1-6 sulfonilo, arilalcoxi C1-6, hidroxi, halógeno, CN, COR7, carboxi, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono a perfluoroalquilo C1-4 y mono a perfluoro-alcoxi C1-4, o alquilo C5-10; R7 y R8 son independientemente hidrógeno 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 uno o dos sustituyentes seleccionados de hidroxi, oxo, alquilo C1-4, alquil C1-4 carboxi, arilo, v-g- fenilo, o aralquilo, v-g- bencilo, por ejemplo, morfolina o piperazina; y X es un grupo alquileno C2-4 (opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de metilo y etilo), CH=CH, (CH2)nS o (CH2)nO en las que n es 1, 2 o 3. Estos compuestos son inhibidores de la enzima Lp-PLA2 y son de utilidad en terapia, en particular para tratar arteriosclerosis. También se dan a conocer: composiciones farmacéuticas que los comprenden, el uso de tales compuestos en la fabricación de medicamentos, y un proceso para la preparación de dichos compuestos. El proceso para preparar un compuesto de fórmula (1) comprende hacer reaccionar un compuesto ácido de fórmula (2) en la que X, R1, R2 y R3 son como se definen aquí anteriormente, con un compuesto de amino de fórmula (3): R6-R5-CH2NHR4 en la que R4, R5 y R6 son como se definen aquí anteriormente; en condiciones de formación de amidas.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
GBGB0024808.8A GB0024808D0 (en) | 2000-10-10 | 2000-10-10 | Novel compounds |
Publications (1)
Publication Number | Publication Date |
---|---|
AR035349A1 true AR035349A1 (es) | 2004-05-12 |
Family
ID=9901006
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP010104760A AR035349A1 (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 (29)
Country | Link |
---|---|
US (2) | US20040063753A1 (es) |
EP (2) | EP1326841B1 (es) |
JP (1) | JP4212354B2 (es) |
KR (1) | KR100824134B1 (es) |
CN (2) | CN1951917B (es) |
AR (1) | AR035349A1 (es) |
AT (1) | ATE538096T1 (es) |
AU (2) | AU2002210524B2 (es) |
BR (1) | BRPI0114576B1 (es) |
CA (1) | CA2425268C (es) |
CY (2) | CY1112442T1 (es) |
CZ (1) | CZ304558B6 (es) |
DK (2) | DK1326841T3 (es) |
ES (2) | ES2378059T3 (es) |
GB (1) | GB0024808D0 (es) |
GC (1) | GC0000307A (es) |
HK (2) | HK1144941A1 (es) |
HU (1) | HU230767B1 (es) |
IL (2) | IL155278A0 (es) |
MX (1) | MXPA03003176A (es) |
MY (1) | MY135766A (es) |
NO (1) | NO325107B1 (es) |
NZ (1) | NZ525225A (es) |
PL (1) | PL207560B1 (es) |
PT (2) | PT2258688E (es) |
SI (2) | SI2258688T1 (es) |
TW (1) | TWI293293B (es) |
WO (1) | WO2002030904A1 (es) |
ZA (1) | ZA200302785B (es) |
Families Citing this family (38)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU3546601A (en) * | 2000-02-16 | 2001-08-27 | Smithkline Beecham Plc | Pyrimidine-4-one derivatives as LDL-PLA<sub>2</sub> inhibitors |
GB0119793D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel compounds |
GB0127140D0 (en) * | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
GB0127139D0 (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 |
US20150017671A1 (en) | 2004-04-16 | 2015-01-15 | Yaping Shou | Methods for detecting lp-pla2 activity and inhibition of lp-pla2 activity |
JP4812751B2 (ja) | 2004-04-16 | 2011-11-09 | グラクソ グループ リミテッド | Lp−PLA2活性およびLp−PLA2活性阻害を検出する方法 |
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 |
US20080090851A1 (en) * | 2006-10-13 | 2008-04-17 | Colin Andrew Leach | Bicyclic Heteroaromatic Compounds |
MX2009012197A (es) | 2007-05-11 | 2010-01-15 | Univ Pennsylvania | Metodos para tratamiento de ulceras en la piel. |
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 |
US8575348B2 (en) | 2009-07-28 | 2013-11-05 | Auspex Pharmaceuticals, Inc | Quinolone inhibitors of lipoprotein-associated phospholipase A2 |
US9512104B2 (en) * | 2009-07-28 | 2016-12-06 | Auspex Pharmaceuticals, Inc. | Quinolone inhibitors of lipoprotein-associated phospholipase A2 |
US20120220624A1 (en) * | 2009-10-19 | 2012-08-30 | Tony Siu | Pyrazolo [3,4-b] pyridin-4-one kinase inhibitors |
US9011821B2 (en) | 2010-06-18 | 2015-04-21 | Whitehead Institute For Biomedical Research | PLA2G16 as a target for antiviral compounds |
JP2013544854A (ja) * | 2010-12-06 | 2013-12-19 | グラクソ グループ リミテッド | 化合物 |
MX2013006342A (es) * | 2010-12-06 | 2013-08-26 | Glaxo Group Ltd | Compuestos de pirimidinona para usarse en el tratamiento de enfermedades o afecciones mediadas por fosfolipasa asociada con lipoproteinas a2 (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 |
WO2013000108A1 (zh) * | 2011-06-27 | 2013-01-03 | 中国科学院上海药物研究所 | 唑类杂环化合物、其制备方法、药物组合物和用途 |
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 |
EP2751094B1 (en) | 2011-09-01 | 2018-06-20 | Glaxo Group Limited | Novel crystal form |
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 LP-PLA2 INHIBITORS |
CN105008365B (zh) | 2013-01-25 | 2017-03-15 | 葛兰素史密斯克莱知识产权发展有限公司 | 化合物 |
EP2764866A1 (en) | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
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 |
CN104840963B (zh) * | 2015-05-26 | 2018-02-16 | 河北东康生物科技有限公司 | 含脂蛋白相关性磷脂酶a2抑制剂的药物组合物及应用 |
WO2016198691A1 (en) | 2015-06-11 | 2016-12-15 | Basilea Pharmaceutica Ag | Efflux-pump inhibitors and therapeutic uses thereof |
CN112574221B (zh) * | 2019-09-30 | 2022-03-04 | 上海纽思克生物科技有限公司 | 四环嘧啶酮类化合物、其制备方法、其组合物和用途 |
AU2020379796C1 (en) | 2019-11-09 | 2024-05-02 | Shanghai SIMR Biotechnology Co., Ltd | Tricyclic dihydroimidazopyrimidone derivative, preparation method therefor, pharmaceutical composition and use thereof |
CN112510260B (zh) * | 2020-11-27 | 2022-11-04 | 珠海市赛纬电子材料股份有限公司 | 电解液添加剂、非水电解液和锂离子电池 |
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 |
Family Cites Families (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5769527A (en) | 1986-07-17 | 1998-06-23 | Vari-Lite, Inc. | Computer controlled lighting system with distributed control resources |
US5585246A (en) | 1993-02-17 | 1996-12-17 | Biometric Imaging, Inc. | Method for preparing a sample in a scan capillary for immunofluorescent interrogation |
DE69423436T2 (de) | 1993-06-25 | 2000-09-07 | Smithkline Beecham P.L.C., Brentford | An lipoprotein gebundene phospholipase a2, inhibitoren davon und deren verwendung für diagnose und therapie |
ATE201905T1 (de) | 1993-10-06 | 2001-06-15 | Icos Corp | Acethylhydrolase des plättchen aktivierenden faktors |
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 |
CH690264A5 (fr) | 1995-06-30 | 2000-06-30 | Symphar Sa | Dérivés aminophosphonates substitués, leur procédé de préparation et leur utilisation pour la préparation de compositions pharmaceutiques. |
KR19990028630A (ko) | 1995-07-01 | 1999-04-15 | 데이비드 로버츠 | 아테롬성 동맥경화증을 치료하기 위한 아제티디논 유도체 |
FR2743912B1 (fr) | 1996-01-24 | 1998-04-10 | Matra Communication | Circuit de resolution d'equation-cle et decodeur reed-solomon incorporant un tel circuit |
US5684794A (en) | 1996-01-25 | 1997-11-04 | Hazeltine Corporation | Validation of subscriber signals in a cellular radio network |
GB9608649D0 (en) | 1996-04-26 | 1996-07-03 | Smithkline Beecham Plc | Novel compounds |
AU735901C (en) * | 1996-12-05 | 2004-02-12 | Amgen, Inc. | Substituted pyrimidinone and pyridone compounds and methods of use |
GB9626615D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | Novel compounds |
GB9626536D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | Novel compounds |
GB9626616D0 (en) | 1996-12-20 | 1997-02-05 | Symphar Sa | Novel compounds |
AU1157599A (en) | 1997-11-06 | 1999-05-31 | Smithkline Beecham Plc | Pyrimidinone compounds and pharmaceutical compositions containing them |
EP1105377B1 (en) | 1998-08-21 | 2003-10-08 | SmithKline Beecham plc | Pyrimidinone derivatives for the treatment of atherosclerosis |
GB9910079D0 (en) | 1999-05-01 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
AU766003B2 (en) | 1999-05-01 | 2003-10-09 | Smithkline Beecham Plc | Pyrimidinone compounds |
GB9910378D0 (en) | 1999-05-05 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
-
2000
- 2000-10-10 GB GBGB0024808.8A patent/GB0024808D0/en not_active Ceased
-
2001
- 2001-10-05 PT PT101777738T patent/PT2258688E/pt unknown
- 2001-10-05 DK DK01978400.8T patent/DK1326841T3/da active
- 2001-10-05 WO PCT/EP2001/011610 patent/WO2002030904A1/en active IP Right Grant
- 2001-10-05 AT AT01978400T patent/ATE538096T1/de active
- 2001-10-05 SI SI200131019T patent/SI2258688T1/sl unknown
- 2001-10-05 JP JP2002534290A patent/JP4212354B2/ja not_active Expired - Fee Related
- 2001-10-05 ES ES01978400T patent/ES2378059T3/es not_active Expired - Lifetime
- 2001-10-05 CA CA2425268A patent/CA2425268C/en not_active Expired - Fee Related
- 2001-10-05 US US10/399,022 patent/US20040063753A1/en not_active Abandoned
- 2001-10-05 AU AU2002210524A patent/AU2002210524B2/en not_active Ceased
- 2001-10-05 PT PT01978400T patent/PT1326841E/pt unknown
- 2001-10-05 DK DK10177773.8T patent/DK2258688T3/da active
- 2001-10-05 EP EP01978400A patent/EP1326841B1/en not_active Expired - Lifetime
- 2001-10-05 EP EP10177773A patent/EP2258688B1/en not_active Expired - Lifetime
- 2001-10-05 KR KR1020037005084A patent/KR100824134B1/ko active IP Right Grant
- 2001-10-05 CN CN200610128890XA patent/CN1951917B/zh not_active Expired - Fee Related
- 2001-10-05 BR BRPI0114576A patent/BRPI0114576B1/pt not_active IP Right Cessation
- 2001-10-05 AU AU1052402A patent/AU1052402A/xx active Pending
- 2001-10-05 CZ CZ2003-1009A patent/CZ304558B6/cs not_active IP Right Cessation
- 2001-10-05 IL IL15527801A patent/IL155278A0/xx unknown
- 2001-10-05 HU HU0302480A patent/HU230767B1/hu not_active IP Right Cessation
- 2001-10-05 NZ NZ525225A patent/NZ525225A/en not_active IP Right Cessation
- 2001-10-05 PL PL366334A patent/PL207560B1/pl unknown
- 2001-10-05 SI SI200131008T patent/SI1326841T1/sl unknown
- 2001-10-05 CN CNB018201253A patent/CN1280275C/zh not_active Expired - Fee Related
- 2001-10-05 MX MXPA03003176A patent/MXPA03003176A/es active IP Right Grant
- 2001-10-05 ES ES10177773T patent/ES2399325T3/es not_active Expired - Lifetime
- 2001-10-08 TW TW090124779A patent/TWI293293B/zh not_active IP Right Cessation
- 2001-10-08 MY MYPI20014669A patent/MY135766A/en unknown
- 2001-10-08 GC GCP20011661 patent/GC0000307A/en active
- 2001-10-10 AR ARP010104760A patent/AR035349A1/es active IP Right Grant
-
2003
- 2003-04-08 IL IL155278A patent/IL155278A/en not_active IP Right Cessation
- 2003-04-09 ZA ZA200302785A patent/ZA200302785B/en unknown
- 2003-04-09 NO NO20031626A patent/NO325107B1/no not_active IP Right Cessation
- 2003-12-08 HK HK10111562.3A patent/HK1144941A1/xx not_active IP Right Cessation
- 2003-12-08 HK HK03108904.5A patent/HK1058036A1/xx not_active IP Right Cessation
-
2004
- 2004-07-28 US US10/900,489 patent/US7235566B2/en not_active Expired - Lifetime
-
2012
- 2012-03-07 CY CY20121100228T patent/CY1112442T1/el unknown
-
2013
- 2013-02-08 CY CY20131100118T patent/CY1113648T1/el unknown
Also Published As
Similar Documents
Publication | Publication Date | Title |
---|---|---|
AR035349A1 (es) | 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 | |
AR035068A1 (es) | 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 | |
AR036107A1 (es) | Derivados de 6-fenilpirrolpirimidindiona, antagonista de los receptores a2 de la adenosina, particularmente del subtipo a2, de aplicacion en la prevencion de la degranulacion de los mastocitos; composiciones farmaceuticas formuladas con dichos compuestos y uso de los mismos en la preparacion de medi | |
AR035497A1 (es) | Compuestos no-imidazol, composicion farmaceutica que los comprenden y el uso de los mismos para la preparacion de medicamentos | |
PT1289955E (pt) | Piperidinas para utilizacao como antagonistas dos receptores da orexina | |
AR035111A1 (es) | Procedimiento para preparar un compuesto de pirimidinona | |
AR023152A1 (es) | Compuesto tienopirimidina, procedimiento para producirlo, composicion farmaceutica que lo comprende y uso de dicho compuesto para preparar dichacomposicion | |
HUP0201935A2 (hu) | A SYK tirozin-protein-kináz inhibitoraiként alkalmazható purinszármazékok | |
AR050267A1 (es) | Derivados de urea ciclicos sustituidos con heterociclo, su preparacion y su uso farmaceutico como inhibidores de quinasa | |
AR002011A1 (es) | Compuestos derivados de piperidina, sus sales y n-oxidos, procedimiento de preparacion y composiciones farmaceuticas. | |
AR016666A1 (es) | Derivados de pirimidinona, un procedimiento para su preparacion y una composicion farmaceutica que los contiene | |
AR010396A1 (es) | Compuestos de quinolina y de quinazolina utiles en terapia, formulacion farmaceutica que los contiene, su uso en la fabricacion de un medicamento,procedimiento para su produccion y compuestos utiles en dicho procedimiento | |
AR025975A1 (es) | Compuestos quimicos. | |
KR950321212A (ko) | 4-아미노-1-피페리딜벤조일구아니딘 | |
AR010795A1 (es) | Compuestos derivados de sulfonamidas, procedimiento para su preparacion y una composicion farmaceutica | |
AR011101A1 (es) | Compuesto derivado de acidos arilsulfonilaminohidroxiamicos y composicion farmaceutica que lo contiene | |
AR051202A1 (es) | Derivados heterociclicos y su uso como inhibidores de la estearoil-coa desaturasa | |
BG103258A (en) | Azinyloxy- and phenoxydiaryl derivatives of carboxylic acids, their preparation and application as mixed eta/etb endothelin-receptor antagonists | |
AR031526A1 (es) | Nuevas fenilpiperazinas, composiciones farmaceuticas que las contienen, metodos para preparar los compuestos y las composiciones y uso de los compuestos en la preparacion de un medicamento. | |
AR050084A1 (es) | Derivados de bencimidazolona como inhibidores de hsp90 | |
MXPA05008584A (es) | Compuestos heterociclicos utiles como activadores de nurr-1. | |
AR056613A1 (es) | Compuestos derivados de lapachona, su preparacion y metodos de uso de los mismos para el tratamiento o prevencion de trastornos proliferativos celulares y composiciones farmaceuticas que los contienen | |
SE9703377D0 (sv) | New compounds | |
NZ511584A (en) | Benzoxazole substituted piperazine and piperidine derivatives useful for treating central nervous disorders, depression and anxiety | |
AR034585A1 (es) | Nuevos compuestos de dihidropirimidina ciano substituidos y su uso para tratar padecimientos |
Legal Events
Date | Code | Title | Description |
---|---|---|---|
FG | Grant, registration |