CO5271661A1 - Pirimidonas de bifenilo con actividad contra aterosclerosis - Google Patents
Pirimidonas de bifenilo con actividad contra aterosclerosisInfo
- Publication number
- CO5271661A1 CO5271661A1 CO01011957A CO01011957A CO5271661A1 CO 5271661 A1 CO5271661 A1 CO 5271661A1 CO 01011957 A CO01011957 A CO 01011957A CO 01011957 A CO01011957 A CO 01011957A CO 5271661 A1 CO5271661 A1 CO 5271661A1
- Authority
- CO
- Colombia
- Prior art keywords
- alkyl
- alkoxy
- mono
- aryl
- halogen
- Prior art date
Links
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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/56—One oxygen atom and one sulfur atom
-
- 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
-
- 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
-
- 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
- A61P3/06—Antihyperlipidemics
-
- 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
- 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
- A61P9/08—Vasodilators for multiple indications
-
- 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
- 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/60—Three or more oxygen or sulfur atoms
-
- 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
- C07D239/95—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
-
- 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
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Life Sciences & Earth Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Diabetes (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Neurosurgery (AREA)
- Obesity (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Immunology (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Emergency Medicine (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Un compuesto de formula (I): <EMI FILE="01011957_1" ID="1" IMF=JPEG >en la que:Ra es hidrógeno, halógeno, alquilo C(1-3), alcoxilo-C(1-3), hidroxialquilo C(1-3), alquilC(1-3)tio, alquil C(1-3)-sulfinilo, aminoalquiloC(1-3), mono- o di-alquilC(1-3), aminoalquilo C(1-3), alquilC(1-3) carbonilaminoalquiloC(1-3), alcoxiC(1-3) alquil C(1-3) carbonilaminoalquilo C(1-3), alquil C(1-3)sulfonilaminoalquilo C(1-3), alquil C(1-3)carboxilo, o alquilC(1-3)-carboxialquiloC(1-3),Rb es hidrógeno, halógeno, alquilo C(1-3) o hidroxialquiloC(1-3), con la condición de que Ra y Rb no sean simultáneamente hidrógeno; oRa y Rb son conjuntamente (CH2)n, en el que n es 3 ó 4, para formar con los átomos de carbono de anillo de pirimidina a los que están unidos, un anillo carbocíclico fusionado de 5 o 6 miembros; o Ra y Rb junto con los átomos de carbono de anillo de pirimidina a los que están unidos, forman un anillo benzo o heteroarílico fusionado que esta opcionalmente sustituido con 1, 2 , 3 o 4 sustituyentes, que pueden ser iguales o diferentes seleccionados entre halógeno, alquilo C(1-4), ciano, alcoxiloC(1-4), alquilC(1-4), tio o de mono- a perfluoro- alquilo C(1-4);Rc es hidrógeno o alquilo C(1-3);R2 es un grupo arilo o heteroarilo opcionalmente sustituido con 1, 2, 3, ó 4 sustituyentes que pueden ser iguales o diferentes seleccionados entre alquiloC(1-18), alcoxilo-C(1-18), alquilC(1-18)tio, aril-alcoxilo C(1-18), hidroxilo, halógeno, CN, COR6, carboxilo, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, de mono-a perfluoro alquilo C(1-4), de mono a perfluoro-alcoxiC(1-4) arilo, y aril-alquilo C(1-4); R3 es hidrógeno, alquiloC(1-6), que puede estar no sustituido o sustituido con 1, 2 o 3 sustituyentes seleccionados entre hidroxilo, halógeno, OR6, COR6, - 2 - carboxilo, COOR6, CONR8R9, NR8R9, NR8COR9, mono- o di-(hidroxialquil C(1-6)) amino y N -hidroxialquil C(1-6) -N-alquil C(1-6) amino; o R3 es Het-alquiloC(0-4), en el que Het es un anillo heterocíclico de 5 a 7 miembros que comprende N y, opcionalmente O o S, unido a través de un átomo de carbono anular y en el que N puede estar sustituido con COR6, COOR6, CONR8R9, o alquiloC(1-6), opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados entre hidroxilo, halógeno, OR6, COR6, carboxilo, COOR6, CONR8R9 o NR8R9;R4 es un anillo arílico o heteroarílico opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes que pueden ser iguales o diferentes seleccionados entre alquilo C(1-18), alcoxilo C(1-18) alquilC(1-18), tio, aril-alcoxiloC(1-18), hidroxilo, halógeno, CN, COR6, carboxilo, COOR6, NR6COR7, CONR8R9, SO2NR8R9, NR6SO2R7, NR8R9, de mono a prefluoro-alquilo C(1-4), y de mono- a perfluoro-alcoxilo C(1-4);R5 es un anillo arílico o heteroarílico que además está opcionalmente sustituido con 1, 2, 3 ó 4 sustituyentes que pueden ser iguales o diferentes, seleccionados entre alquilo C(1-18), (preferiblemente alquilo C(1-6)), alcoxiloC(1-18) (preferiblemente alcoxiC(1-6)), alquilC(1-18)tio(preferiblemente alquilC(1-6)tio), aril alcoxilo C(1-18), (preferiblemente aril-alcoxi C(1-6)), hidroxilo, halógeno, CN, COR6, carboxilo, COOR6, CONR8R9, NR6COR7, SO2NR8R9, NR6SO2R7, NR8R9, de mono- a perfluoro-alquilo C(1-4), y de mono- a perfluoro-alcoxilo C(1-4);R6 y R7 son independientemente hidrógeno o alquilo C(1-20), tal como, por ejemplo, alquilo C(1-4);R8 y R9, que pueden ser iguales o diferentes son seleccionados cada uno entre hidrógeno y alquilo C(1-12), o R8 y R9 junto con el nitrógeno al estan unidos forman un anillo de 5 a 7 miembros que contiene opcionalmente uno o mas heteroátomos adicionales seleccionados entre oxígeno, nitrógeno y azufre, y está opcionalmente sustituido con uno o dos sustituyentes seleccionados entre hidroxilo, oxo, alquilo C(1-4), alquil C(1-4)CO, arilo, y aralquilo; o R8 y R9, que pueden ser iguales o diferentes, son seleccionados cada uno, entre CH2R10, CHR11CO2H o una sal del mismo en los que:R10 es COOH o una sal del mismo, COOR12, CONR6R7, CN, CH2OH o CH2OR6;R11 es una cadena lateral aminoácido tal como CH2OH de serina;R12 es alquilo C(1-4) o un grupo éster farmacéuticamente aceptable e hidrolizable in vivo;N es un número entero de 1 a 4;X es O o S;Y es (CH2)p(O)q en el que p es 1, 2 o 3 y q es 0, o p es 2 ó 3 y q es 1; yZ es O o un enlace.1 Un compuesto de la fórmula (IA):<EMI FILE="01011957_2" ID="2" IMF=JPEG >en la que: Ra, Rb, Rc,n, R2, R3, R4 ,R5 y X son como se definieron en la reivindicación 1.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0003636A GB0003636D0 (en) | 2000-02-16 | 2000-02-16 | Novel compounds |
| GB0101437A GB0101437D0 (en) | 2001-01-19 | 2001-01-19 | Novel Compounds |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CO5271661A1 true CO5271661A1 (es) | 2003-04-30 |
Family
ID=26243663
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CO01011957A CO5271661A1 (es) | 2000-02-16 | 2001-02-15 | Pirimidonas de bifenilo con actividad contra aterosclerosis |
Country Status (32)
| Country | Link |
|---|---|
| US (10) | US20020103213A1 (es) |
| EP (2) | EP1686119B1 (es) |
| JP (1) | JP4095804B2 (es) |
| KR (1) | KR100781425B1 (es) |
| CN (1) | CN1179952C (es) |
| AR (1) | AR030190A1 (es) |
| AT (2) | ATE333446T1 (es) |
| AU (2) | AU2001235466B2 (es) |
| BG (1) | BG66014B1 (es) |
| BR (1) | BRPI0108396B1 (es) |
| CA (1) | CA2400554C (es) |
| CO (1) | CO5271661A1 (es) |
| CY (2) | CY1105649T1 (es) |
| CZ (1) | CZ304450B6 (es) |
| DE (2) | DE60139429D1 (es) |
| DK (2) | DK1686119T3 (es) |
| ES (2) | ES2330552T3 (es) |
| GC (1) | GC0000221A (es) |
| HK (1) | HK1053466A1 (es) |
| HU (1) | HU229479B1 (es) |
| IL (2) | IL151236A (es) |
| MX (1) | MXPA02008062A (es) |
| MY (1) | MY135732A (es) |
| NO (1) | NO324691B1 (es) |
| NZ (1) | NZ520752A (es) |
| PL (1) | PL209824B1 (es) |
| PT (2) | PT1686119E (es) |
| SI (2) | SI1686119T1 (es) |
| SK (1) | SK287296B6 (es) |
| TW (1) | TW550259B (es) |
| UA (1) | UA73762C2 (es) |
| WO (1) | WO2001060805A1 (es) |
Families Citing this family (61)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HU229479B1 (en) * | 2000-02-16 | 2014-01-28 | Glaxo Group Ltd | Pyrimidine-4-one derivatives |
| GB0024807D0 (en) | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| WO2002032863A1 (en) * | 2000-10-20 | 2002-04-25 | Biovitrum Ab | 2-, 3-, 4-, or 5-substituted-n1-(benzensulfonyl)indoles and their use in therapy |
| GB0119793D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel compounds |
| GB0119795D0 (en) * | 2001-08-14 | 2001-10-03 | Smithkline Beecham Plc | Novel process |
| GB0127143D0 (en) * | 2001-11-10 | 2002-01-02 | Smithkline Beecham | Novel compounds |
| GB0127141D0 (en) * | 2001-11-10 | 2002-01-02 | 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 |
| WO2003057671A1 (fr) * | 2001-12-28 | 2003-07-17 | Takeda Chemical Industries, Ltd. | Compose biaryle et son utilisation |
| US6939863B2 (en) | 2002-01-04 | 2005-09-06 | Wei-Jan Chen | Prevention of atherosclerosis and restenosis |
| GB0208280D0 (en) * | 2002-04-10 | 2002-05-22 | Glaxo Group Ltd | Novel compounds |
| GB0208279D0 (en) * | 2002-04-10 | 2002-05-22 | Glaxo Group Ltd | Novel compounds |
| US20050227974A9 (en) * | 2002-08-01 | 2005-10-13 | Euro-Celtique S.A. | Aminoalkyl-substituted aryl compounds and their use as sodium channel blockers |
| JP4366122B2 (ja) * | 2003-06-24 | 2009-11-18 | 日立オムロンターミナルソリューションズ株式会社 | 紙葉類搬送装置 |
| GB0320522D0 (en) | 2003-09-02 | 2003-10-01 | Glaxo Group Ltd | Formulation |
| CN1875002B (zh) | 2003-11-05 | 2011-08-03 | 霍夫曼-拉罗奇有限公司 | 作为ppar激动剂的苯基衍生物 |
| 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 |
| TW200608976A (en) | 2004-05-08 | 2006-03-16 | Neurogen Corp | 4,5-disubstituted-2-aryl pyrimidines |
| DE102004061005A1 (de) * | 2004-12-18 | 2006-06-22 | Bayer Healthcare Ag | 3-Cycloalkyl-1,2,4-triazin-5(2H)-one |
| US20080090851A1 (en) * | 2006-10-13 | 2008-04-17 | Colin Andrew Leach | Bicyclic Heteroaromatic Compounds |
| US20080090852A1 (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 |
| US8962633B2 (en) | 2007-05-11 | 2015-02-24 | Thomas Jefferson University | Methods of treatment and prevention of metabolic bone diseases and disorders |
| ES2540933T3 (es) * | 2007-05-11 | 2015-07-14 | Thomas Jefferson University | Métodos de tratamiento y prevención de enfermedades y trastornos neurodegenerativos |
| EA018101B1 (ru) * | 2007-05-11 | 2013-05-30 | Дзе Трастиз Оф Дзе Юниверсити Оф Пенсильвания | Способы лечения кожных язв |
| US8637524B2 (en) | 2009-07-28 | 2014-01-28 | Auspex Pharmaceuticals, Inc | Pyrimidinone inhibitors of lipoprotein-associated phospholipase A2 |
| TW201209043A (en) * | 2010-05-17 | 2012-03-01 | Glaxo Group Ltd | Novel processes |
| JP6053675B2 (ja) | 2010-06-18 | 2016-12-27 | ホワイトヘッド・インスティチュート・フォア・バイオメディカル・リサーチ | 抗ウイルス化合物のためのターゲットとしてのｐｌａ２ｇ１６ |
| CN104478812A (zh) * | 2010-12-06 | 2015-04-01 | 葛兰素集团有限公司 | 用于治疗由Lp-PLA2介导的疾病或病症的嘧啶酮化合物 |
| WO2012075917A1 (en) * | 2010-12-06 | 2012-06-14 | Glaxo Group Limited | Compounds |
| TW201307324A (zh) * | 2010-12-06 | 2013-02-16 | Glaxo Group Ltd | 化合物 |
| WO2012080497A2 (en) | 2010-12-17 | 2012-06-21 | Glaxo Group Limited | Methods of treatment and prevention of eye diseases |
| CN102643269B (zh) * | 2011-02-21 | 2014-07-23 | 天津药物研究院 | 一类含吡唑结构的磷脂酶a2抑制剂及用途 |
| CN103476414B (zh) * | 2011-03-16 | 2015-07-08 | 中国科学院上海药物研究所 | 季铵盐类化合物、其制备方法、药物组合物及用途 |
| 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 |
| WO2013000267A1 (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 |
| AU2012289492B2 (en) | 2011-07-27 | 2016-02-04 | Glaxo Group Limited | 2,3-dihydroimidazo[1,2-c] pyrimidin-5(1H)-one compounds use as Lp-PLA2 inhibitors |
| CN103827116B (zh) * | 2011-07-27 | 2016-08-31 | 葛兰素集团有限公司 | 用作LP-PLA2抑制剂的2,3-二氢咪唑并[1,2-c]嘧啶-5(1H)-酮化合物 |
| BR112014001634A2 (pt) | 2011-07-27 | 2017-02-14 | Glaxo Group Ltd | compostos bicíclicos de pirimidona |
| WO2014114694A1 (en) | 2013-01-25 | 2014-07-31 | Glaxosmithkline Intellectual Property Development Limited | 2,3-dihydroimidazol[1,2-c]pyrimidin-5(1h)-one based lipoprotein-associated phospholipase a2 (lp-pla2) inhibitors |
| JP2016508995A (ja) | 2013-01-25 | 2016-03-24 | グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ | 化合物 |
| 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 |
| WO2015087239A1 (en) | 2013-12-11 | 2015-06-18 | Ranbaxy Laboratories Limited | Processes for the preparation of darapladib and its intermediates |
| WO2015092687A2 (en) | 2013-12-17 | 2015-06-25 | Ranbaxy Laboratories Limited | Process for the purification of darapladib |
| WO2015114479A1 (en) | 2014-01-28 | 2015-08-06 | Ranbaxy Laboratories Limited | Crystalline forms of darapladib oxalate, adipate, succinate, phosphate, sulphate, fumaratetartrate, nitrate and borate |
| 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 |
| MX2017002610A (es) | 2014-08-29 | 2017-10-11 | Tes Pharma S R L | INHIBIDORES DE ACIDO A-AMINO-ß-CARBOXIMUCONICO SEMIALDEHIDO DESCARBOXILASA. |
| CN105777653A (zh) * | 2014-12-26 | 2016-07-20 | 中国科学院上海药物研究所 | 用作Lp-PLA2抑制剂的嘧啶酮类化合物及其药物组合物 |
| 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 |
| 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 |
| WO2017106396A1 (en) * | 2015-12-16 | 2017-06-22 | Bristol-Myers Squibb Company | Heteroarylhydroxypyrimidinones as agonists of the apj receptor |
| US10878307B2 (en) * | 2016-12-23 | 2020-12-29 | Microsoft Technology Licensing, Llc | EQ-digital conversation assistant |
| ES2907130T3 (es) | 2017-09-26 | 2022-04-22 | Inst Nat Sante Rech Med | Darapladib radiomarcado, análogos del mismo y su uso como compuestos para la obtención de imágenes |
| CN110746445B (zh) * | 2019-10-16 | 2021-03-16 | 深圳海关食品检验检疫技术中心 | 一种头孢哌酮氘代内标物的制备方法 |
| 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 |
| EP4257133A1 (en) | 2022-04-05 | 2023-10-11 | Institut Pasteur | Oxo-azaheterocyclic derivatives for use in the treatment of malaria |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| PT673426E (pt) * | 1993-10-06 | 2001-11-30 | Icos Corp | Acetil-hidrolase do factor activador das plaquetas |
| GB9421816D0 (en) | 1994-10-29 | 1994-12-14 | Smithkline Beecham Plc | Novel compounds |
| AU704407B2 (en) | 1994-12-22 | 1999-04-22 | Smithkline Beecham Plc | 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. |
| TR199701762T1 (xx) | 1995-07-01 | 1998-05-21 | Smithkline Beecham P.L.C. | Damar t�kanmas� tedavisi i�in azetidinon t�revleri. |
| EP0859834A2 (en) | 1995-09-29 | 1998-08-26 | Smithkline Beecham Plc | A paf-acetylhydrolase and use in therapy |
| EP0869943A1 (en) | 1995-12-08 | 1998-10-14 | Smithkline Beecham Plc | Monocyclic beta-lactame derivatives for treatment of atherosclerosis |
| JP2000505063A (ja) | 1995-12-08 | 2000-04-25 | 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 | アテローム性動脈硬化症の治療のためのアゼチジノン化合物 |
| GB9608649D0 (en) | 1996-04-26 | 1996-07-03 | Smithkline Beecham Plc | Novel compounds |
| AU2698697A (en) | 1996-04-26 | 1997-11-19 | Smithkline Beecham Plc | Azetidinone derivatives for the treatment of atherosclerosis |
| 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 |
| JP2001522844A (ja) * | 1997-11-06 | 2001-11-20 | 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 | ピリミジノン化合物およびそれを含有する医薬組成物 |
| DE69911980T2 (de) | 1998-08-21 | 2004-09-09 | Smithkline Beecham P.L.C., Brentford | Pyrimidinonderivate zur behandlung von atheroscleros |
| SI1175408T1 (en) | 1999-05-01 | 2005-04-30 | Smithkline Beecham Plc | Pyrimidinone compounds |
| GB9910079D0 (en) | 1999-05-01 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
| GB9910378D0 (en) | 1999-05-05 | 1999-06-30 | Smithkline Beecham Plc | Novel compounds |
| HU229479B1 (en) * | 2000-02-16 | 2014-01-28 | Glaxo Group Ltd | Pyrimidine-4-one derivatives |
| GB0024808D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
| GB0024807D0 (en) * | 2000-10-10 | 2000-11-22 | Smithkline Beecham Plc | Novel compounds |
-
2001
- 2001-02-13 HU HU0204410A patent/HU229479B1/hu not_active IP Right Cessation
- 2001-02-13 UA UA2002097389A patent/UA73762C2/uk unknown
- 2001-02-13 SK SK1177-2002A patent/SK287296B6/sk not_active IP Right Cessation
- 2001-02-13 SI SI200130941T patent/SI1686119T1/sl unknown
- 2001-02-13 MX MXPA02008062A patent/MXPA02008062A/es active IP Right Grant
- 2001-02-13 CA CA002400554A patent/CA2400554C/en not_active Expired - Fee Related
- 2001-02-13 PT PT06075890T patent/PT1686119E/pt unknown
- 2001-02-13 AT AT01907522T patent/ATE333446T1/de active
- 2001-02-13 NZ NZ520752A patent/NZ520752A/en not_active IP Right Cessation
- 2001-02-13 DK DK06075890T patent/DK1686119T3/da active
- 2001-02-13 PL PL357382A patent/PL209824B1/pl unknown
- 2001-02-13 ES ES06075890T patent/ES2330552T3/es not_active Expired - Lifetime
- 2001-02-13 ES ES01907522T patent/ES2267714T3/es not_active Expired - Lifetime
- 2001-02-13 BR BRPI0108396-1A patent/BRPI0108396B1/pt not_active IP Right Cessation
- 2001-02-13 WO PCT/EP2001/001515 patent/WO2001060805A1/en active Application Filing
- 2001-02-13 EP EP06075890A patent/EP1686119B1/en not_active Expired - Lifetime
- 2001-02-13 CN CNB01806521XA patent/CN1179952C/zh not_active Expired - Fee Related
- 2001-02-13 SI SI200130614T patent/SI1263740T1/sl unknown
- 2001-02-13 DK DK01907522T patent/DK1263740T3/da active
- 2001-02-13 DE DE60139429T patent/DE60139429D1/de not_active Expired - Lifetime
- 2001-02-13 AU AU2001235466A patent/AU2001235466B2/en not_active Ceased
- 2001-02-13 AU AU3546601A patent/AU3546601A/xx active Pending
- 2001-02-13 EP EP01907522A patent/EP1263740B1/en not_active Expired - Lifetime
- 2001-02-13 JP JP2001560190A patent/JP4095804B2/ja not_active Expired - Fee Related
- 2001-02-13 CZ CZ2002-2768A patent/CZ304450B6/cs not_active IP Right Cessation
- 2001-02-13 KR KR1020027010662A patent/KR100781425B1/ko not_active IP Right Cessation
- 2001-02-13 AT AT06075890T patent/ATE437862T1/de active
- 2001-02-13 PT PT01907522T patent/PT1263740E/pt unknown
- 2001-02-13 DE DE60121550T patent/DE60121550T2/de not_active Expired - Lifetime
- 2001-02-14 MY MYPI20010671A patent/MY135732A/en unknown
- 2001-02-14 US US09/782,930 patent/US20020103213A1/en not_active Abandoned
- 2001-02-14 AR ARP010100659A patent/AR030190A1/es not_active Application Discontinuation
- 2001-02-14 GC GCP20011178 patent/GC0000221A/en active
- 2001-02-15 TW TW090103332A patent/TW550259B/zh not_active IP Right Cessation
- 2001-02-15 CO CO01011957A patent/CO5271661A1/es active IP Right Grant
-
2002
- 2002-08-13 IL IL151236A patent/IL151236A/en not_active IP Right Cessation
- 2002-08-13 NO NO20023828A patent/NO324691B1/no not_active IP Right Cessation
- 2002-08-26 BG BG107034A patent/BG66014B1/bg unknown
-
2003
- 2003-02-03 US US10/357,238 patent/US6649619B1/en not_active Expired - Lifetime
- 2003-06-09 HK HK03104052A patent/HK1053466A1/xx not_active IP Right Cessation
- 2003-10-27 US US10/694,561 patent/US7153861B2/en not_active Expired - Fee Related
-
2006
- 2006-10-06 CY CY20061101441T patent/CY1105649T1/el unknown
- 2006-11-17 US US11/561,035 patent/US7470694B2/en not_active Expired - Fee Related
- 2006-11-21 US US11/561,926 patent/US7638520B2/en not_active Expired - Fee Related
-
2007
- 2007-03-15 IL IL181957A patent/IL181957A0/en unknown
-
2009
- 2009-01-06 US US12/349,086 patent/US7652019B2/en not_active Expired - Fee Related
- 2009-02-18 US US12/372,837 patent/US20090170877A1/en not_active Abandoned
- 2009-10-12 CY CY20091101045T patent/CY1109484T1/el unknown
-
2010
- 2010-02-18 US US12/707,838 patent/US20100144765A1/en not_active Abandoned
-
2011
- 2011-12-02 US US13/309,941 patent/US8871775B2/en not_active Expired - Fee Related
-
2014
- 2014-10-24 US US14/522,870 patent/US9266841B2/en not_active Expired - Fee Related
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CO5271661A1 (es) | Pirimidonas de bifenilo con actividad contra aterosclerosis | |
| CO5170521A1 (es) | Compuestos farmaceuticos de pirimidinona | |
| CO5251467A1 (es) | Derivados de piperazina | |
| CO5200783A1 (es) | Compuestos terapeuticos | |
| HRP20110957T1 (hr) | Derivati kinolina kao inhibitori fosfodiesteraza | |
| PE20091621A1 (es) | Derivados de amina como moduladores de la actividad de tlr y composiciones que los contienen | |
| CO5280059A1 (es) | Derivados de 2-ox-1-pirrolidina, procewo para prepararlos y sus aplicaciones | |
| CO5080780A1 (es) | Derivado de amida y antagonista de nociceptina | |
| PE20091335A1 (es) | Derivados de ftalazinona | |
| ECSP066967A (es) | Derivados de tetrahidroquinolina y un procedimiento para preparar los mismos | |
| RS50932B (sr) | N-oksidi kao prolekovi 4-fenil-piridinskih derivata koji su antagonisti nk1 receptora | |
| CO5180626A1 (es) | Derivados de purina inhibidores de proteina quinasa syk | |
| EA199800664A1 (ru) | Замещенные производные 4-гидрокси-фенилалкановой кислоты с агонистической активностью по отношению к ppar-гамма | |
| PE20030703A1 (es) | Inhibidores de la 17b-hidroxiesteroide deshidrogenasa tipo 3 | |
| RU2010131833A (ru) | Способы получения производных хиназолинона | |
| UY32314A (es) | Derivados de 4-fenil-piridina | |
| CO5060482A1 (es) | Derivados terapeuticos de biarilo | |
| CO5150228A1 (es) | Acidos oxamicos y derivados como ligandos de receptores tiroideos | |
| RU2015105561A (ru) | Замещенные гетероазепиноны | |
| CO5251410A1 (es) | Derivados de nitrilo como inhibidores de la captesina k | |
| RS52562B (en) | (3-ARIL-PIPERAZINE-1-IL) DERIVATI 6,7-DIALCOKSIQUINZOLINE, 6,7-DIALCOKSIFTALAZINE I | |
| PE20050145A1 (es) | Dihidroquinazolinas sustituidas como agentes antivirales | |
| CO5170529A1 (es) | Derivados de 5-(fenil sustituido)-2-piperazinil-pirimidin-(3,5- bistrifluoro-metil-bencil)-metil-amida | |
| CO5271675A1 (es) | Derivados de decahidro-isoquinolinas, proceso para su preparacion, composicion y compuestos farmaceuticos que los contienen | |
| DE69820159D1 (de) | Therapeutisch nützliche Chinoline und Quinazoline |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Application granted |