PE20090157A1 - Derivados de pirimidinona como moduladores del receptor acoplado a proteina g 119 (gpr119) - Google Patents
Derivados de pirimidinona como moduladores del receptor acoplado a proteina g 119 (gpr119)Info
- Publication number
- PE20090157A1 PE20090157A1 PE2008000679A PE2008000679A PE20090157A1 PE 20090157 A1 PE20090157 A1 PE 20090157A1 PE 2008000679 A PE2008000679 A PE 2008000679A PE 2008000679 A PE2008000679 A PE 2008000679A PE 20090157 A1 PE20090157 A1 PE 20090157A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- gpr119
- modulators
- protein
- aryl
- Prior art date
Links
- 102100033839 Glucose-dependent insulinotropic receptor Human genes 0.000 title abstract 2
- 101000996752 Homo sapiens Glucose-dependent insulinotropic receptor Proteins 0.000 title abstract 2
- 102000004169 proteins and genes Human genes 0.000 title abstract 2
- 108090000623 proteins and genes Proteins 0.000 title abstract 2
- VTGOHKSTWXHQJK-UHFFFAOYSA-N pyrimidin-2-ol Chemical class OC1=NC=CC=N1 VTGOHKSTWXHQJK-UHFFFAOYSA-N 0.000 title abstract 2
- 102000005962 receptors Human genes 0.000 title abstract 2
- 108020003175 receptors Proteins 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 4
- YCIPQJTZJGUXND-UHFFFAOYSA-N Aglaia odorata Alkaloid Natural products C1=CC(OC)=CC=C1C1(C(C=2C(=O)N3CCCC3=NC=22)C=3C=CC=CC=3)C2(O)C2=C(OC)C=C(OC)C=C2O1 YCIPQJTZJGUXND-UHFFFAOYSA-N 0.000 abstract 1
- 208000001145 Metabolic Syndrome Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 201000000690 abdominal obesity-metabolic syndrome Diseases 0.000 abstract 1
- 206010012601 diabetes mellitus Diseases 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- 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
- A61P3/04—Anorexiants; Antiobesity agents
-
- 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
- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Obesity (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Child & Adolescent Psychology (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Ophthalmology & Optometry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
SE REFIERE A COMPUESTOS DERIVADOS DE PIRIMIDINONA DE FORMULA (I) DONDE R ESTA AUSENTE O ES O; R1 ES H, ALQUILO(C1-C12), HALOALQUILO(C1-C12), C(O)-ARILO(C6-C14), ENTRE OTROS; R2 ES ALQUILO(C1-C12), HALOALQUILO(C1-C12), C(O)-ALQUILO(C1-C12), ALQUILEN(C1-C12)-O-ARILO(C6-C14), ENTRE OTROS; R3 ES ALQUILO(C1-C12), C(O)-ARILO(C6-C14), C(O)-ALQUILO(C1-C12), ENTRE OTROS; R4 ES H, ALQUILO(C1-C12), ALQUILEN(C1-C12)-O-ALQUILO(C1-C12), ALQUILEN(C1-C12)-O-ARILO(C6-C14), ENTRE OTROS; R10 ES H, ALQUILO(C1-C12), HETEROARILO DE 5 A 14 MIEMBROS, CICLOALQUILO(C3-C10), ENTRE OTROS; R11 ES H, ALQUILO(C1-C12), CICLOALQUILO(C3-C10), ENTRE OTROS; R12 ES H, ALQUILO(C1-C12), HETEROCICLOALQUILO DE 3 A 10 MIEMBROS, ALCOXI(C1-C12), ENTRE OTROS. SON COMPUESTOS PREFERIDOS LOS COMPUESTOS DE FORMULA (i), (ii), (iii), ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR ACOPLADO A PROTEINA G 119 (GPR119) SIENDO UTILES EN EL TRATAMIENTO DE DIABETES TIPO 1 Y 2, OBESIDAD, SINDROME METABOLICO
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US92546507P | 2007-04-20 | 2007-04-20 | |
| US95332307P | 2007-08-01 | 2007-08-01 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090157A1 true PE20090157A1 (es) | 2009-03-27 |
Family
ID=39651245
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008000679A PE20090157A1 (es) | 2007-04-20 | 2008-04-18 | Derivados de pirimidinona como moduladores del receptor acoplado a proteina g 119 (gpr119) |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US8318751B2 (es) |
| EP (1) | EP2148870A1 (es) |
| JP (1) | JP2010524941A (es) |
| CN (1) | CN101754961A (es) |
| AR (1) | AR066120A1 (es) |
| CA (1) | CA2684634A1 (es) |
| CL (1) | CL2008001125A1 (es) |
| MX (1) | MX2009011359A (es) |
| PE (1) | PE20090157A1 (es) |
| TW (1) | TW200845996A (es) |
| WO (1) | WO2008130584A1 (es) |
Families Citing this family (48)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2078719A4 (en) * | 2006-09-28 | 2009-11-11 | Dainippon Sumitomo Pharma Co | COMPOUND WITH BICYCLIC PYRIMIDINE STRUCTURE AND THE COMPOUND CONTAINING PHARMACEUTICAL COMPOSITION |
| CN101686980A (zh) * | 2007-04-20 | 2010-03-31 | 先灵公司 | 四氢吡啶并[4,3-d]嘧啶酮衍生物及其使用方法 |
| US20110065671A1 (en) * | 2008-05-19 | 2011-03-17 | Harris Joel M | Bicyclic heterocycle derivatives and use thereof as gpr119 modulators |
| CA2730593A1 (en) | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and use thereof as gpr119 modulators |
| CA2730606A1 (en) | 2008-07-16 | 2010-01-21 | Schering Corporation | Bicyclic heterocycle derivatives and methods of use thereof |
| AR076928A1 (es) * | 2009-05-28 | 2011-07-20 | Otsuka Pharma Co Ltd | Derivados de 3h-pirido[4, 3-d]pirimidin-4-ona, un metodo para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la manufactura de un medicamento para el tratamiento o prevencion de enfermedades relacionadas con el estres. |
| WO2011107494A1 (de) | 2010-03-03 | 2011-09-09 | Sanofi | Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung |
| JP2013522279A (ja) | 2010-03-18 | 2013-06-13 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 糖尿病及び関連状態の治療で用いるgpr119作動薬とddp−iv阻害薬リナグリプチンの組合せ |
| US8530413B2 (en) | 2010-06-21 | 2013-09-10 | Sanofi | Heterocyclically substituted methoxyphenyl derivatives with an oxo group, processes for preparation thereof and use thereof as medicaments |
| TW201215388A (en) | 2010-07-05 | 2012-04-16 | Sanofi Sa | (2-aryloxyacetylamino)phenylpropionic acid derivatives, processes for preparation thereof and use thereof as medicaments |
| TW201215387A (en) | 2010-07-05 | 2012-04-16 | Sanofi Aventis | Spirocyclically substituted 1,3-propane dioxide derivatives, processes for preparation thereof and use thereof as a medicament |
| TW201221505A (en) | 2010-07-05 | 2012-06-01 | Sanofi Sa | Aryloxyalkylene-substituted hydroxyphenylhexynoic acids, process for preparation thereof and use thereof as a medicament |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2014011926A1 (en) | 2012-07-11 | 2014-01-16 | Elcelyx Therapeutics, Inc. | Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk |
| EP2718279B1 (en) | 2011-06-09 | 2016-08-10 | Rhizen Pharmaceuticals SA | Novel compounds as modulators of gpr-119 |
| WO2013037390A1 (en) | 2011-09-12 | 2013-03-21 | Sanofi | 6-(4-hydroxy-phenyl)-3-styryl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| WO2013045413A1 (en) | 2011-09-27 | 2013-04-04 | Sanofi | 6-(4-hydroxy-phenyl)-3-alkyl-1h-pyrazolo[3,4-b]pyridine-4-carboxylic acid amide derivatives as kinase inhibitors |
| UA125503C2 (uk) | 2012-06-13 | 2022-04-13 | Інсайт Холдинґс Корпорейшн | Заміщені трициклічні сполуки як інгібітори fgfr |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| WO2014172644A2 (en) | 2013-04-19 | 2014-10-23 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| UA121669C2 (uk) | 2015-02-20 | 2020-07-10 | Інсайт Корпорейшн | Біциклічні гетероцикли як інгібітори fgfr |
| US11091477B2 (en) * | 2016-08-12 | 2021-08-17 | Madera Therapeutics, LLC | Protein kinase regulators |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| SI3788047T1 (sl) | 2018-05-04 | 2024-11-29 | Incyte Corporation | Trdne oblike inhibitorja fgfr in postopki priprave le-teh |
| CN112566912A (zh) | 2018-05-04 | 2021-03-26 | 因赛特公司 | Fgfr抑制剂的盐 |
| LT3827829T (lt) | 2018-09-12 | 2025-07-10 | Dong-A St Co., Ltd. | Farmacinė kompozicija, skirta panaudoti nealkoholinio kepenų suriebėjimo ligos profilaktikai arba gydymui, kurios sudėtyje yra gpr119 ligandas kaip veiklioji sudedamoji dalis |
| JP2022508953A (ja) | 2018-10-22 | 2022-01-19 | アッセンブリー バイオサイエンシズ,インコーポレイテッド | Hbvの処置のための5員のヘテロアリールカルボキサミド化合物 |
| GB2596010B (en) * | 2019-02-11 | 2023-03-01 | Madera Therapeutics Llc | Use of caseinolytic protease P function as a biomarker of drug response to imipridone-like agents |
| EP3930714A4 (en) * | 2019-02-27 | 2022-10-26 | Madera Therapeutics, LLC | USE OF CASEINOLYTIC PROTEASE P FUNCTION AS A BIOMARKER OF DRUG RESPONSE TO IMIPRIDONE-LIKE AGENTS |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| CN110156629A (zh) * | 2019-05-30 | 2019-08-23 | 广州药本君安医药科技股份有限公司 | 丙卡巴肼的合成方法 |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4045151A1 (en) | 2019-10-14 | 2022-08-24 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CA3163875A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4069695A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Derivatives of an fgfr inhibitor |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| MX2022011129A (es) * | 2020-03-11 | 2022-10-13 | Dong A St Co Ltd | Composicion farmaceutica para la prevencion o el tratamiento de la diabetes y de enfermedades metabolicas asociadas a la misma. |
| US12065494B2 (en) | 2021-04-12 | 2024-08-20 | Incyte Corporation | Combination therapy comprising an FGFR inhibitor and a Nectin-4 targeting agent |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261160A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4615441A1 (en) * | 2022-11-10 | 2025-09-17 | Ribometrix, Inc. | Compounds and compositions as eif4e inhibitors and uses thereof |
| CN119039287A (zh) * | 2023-05-29 | 2024-11-29 | 中国药科大学 | 一类四氢吡啶并嘧啶酮衍生物及其制备方法与应用 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE348152T1 (de) * | 2000-12-01 | 2007-01-15 | Astellas Pharma Inc | Verfahren zum screening von diabetes- heilverfahren |
| DE602004017703D1 (de) * | 2003-02-24 | 2008-12-24 | Arena Pharm Inc | Phenyl- und pyridylpiperidinderivate als modulatoren des glucose-metabolismus |
| CN102417508A (zh) * | 2003-07-14 | 2012-04-18 | 艾尼纳制药公司 | 作为新陈代谢调节剂的稠合芳基和杂芳基衍生物以及预防和治疗与其相关的病症 |
| EP2078719A4 (en) | 2006-09-28 | 2009-11-11 | Dainippon Sumitomo Pharma Co | COMPOUND WITH BICYCLIC PYRIMIDINE STRUCTURE AND THE COMPOUND CONTAINING PHARMACEUTICAL COMPOSITION |
-
2008
- 2008-04-17 JP JP2010504082A patent/JP2010524941A/ja active Pending
- 2008-04-17 CA CA002684634A patent/CA2684634A1/en not_active Abandoned
- 2008-04-17 EP EP08742985A patent/EP2148870A1/en not_active Withdrawn
- 2008-04-17 CN CN200880017651A patent/CN101754961A/zh active Pending
- 2008-04-17 US US12/595,906 patent/US8318751B2/en not_active Expired - Fee Related
- 2008-04-17 MX MX2009011359A patent/MX2009011359A/es unknown
- 2008-04-17 WO PCT/US2008/004938 patent/WO2008130584A1/en not_active Ceased
- 2008-04-18 PE PE2008000679A patent/PE20090157A1/es not_active Application Discontinuation
- 2008-04-18 CL CL200801125A patent/CL2008001125A1/es unknown
- 2008-04-18 TW TW097114365A patent/TW200845996A/zh unknown
- 2008-04-18 AR ARP080101617A patent/AR066120A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| EP2148870A1 (en) | 2010-02-03 |
| AR066120A1 (es) | 2009-07-22 |
| US20100113487A1 (en) | 2010-05-06 |
| CN101754961A (zh) | 2010-06-23 |
| MX2009011359A (es) | 2009-11-05 |
| CL2008001125A1 (es) | 2008-10-24 |
| CA2684634A1 (en) | 2008-10-30 |
| US8318751B2 (en) | 2012-11-27 |
| TW200845996A (en) | 2008-12-01 |
| JP2010524941A (ja) | 2010-07-22 |
| WO2008130584A1 (en) | 2008-10-30 |
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