PE20090774A1 - Compuestos heterociclicos como moduladores de la enzima dgat1 - Google Patents
Compuestos heterociclicos como moduladores de la enzima dgat1Info
- Publication number
- PE20090774A1 PE20090774A1 PE2008001688A PE2008001688A PE20090774A1 PE 20090774 A1 PE20090774 A1 PE 20090774A1 PE 2008001688 A PE2008001688 A PE 2008001688A PE 2008001688 A PE2008001688 A PE 2008001688A PE 20090774 A1 PE20090774 A1 PE 20090774A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- benzo
- dichloro
- imidazole
- formula
- Prior art date
Links
- 102100036869 Diacylglycerol O-acyltransferase 1 Human genes 0.000 title abstract 2
- 101000927974 Homo sapiens Diacylglycerol O-acyltransferase 1 Proteins 0.000 title abstract 2
- 150000002391 heterocyclic compounds Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- GEAXLHPORCRESC-UHFFFAOYSA-N chlorocyclohexatriene Chemical class ClC1=CC=C=C[CH]1 GEAXLHPORCRESC-UHFFFAOYSA-N 0.000 abstract 1
- 239000008103 glucose Substances 0.000 abstract 1
- PEDCQBHIVMGVHV-UHFFFAOYSA-N glycerol Substances OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 229910052760 oxygen Inorganic materials 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 229910052717 sulfur Inorganic materials 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms 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
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
-
- 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
- A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric 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
-
- 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
-
- 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
- A61P35/00—Antineoplastic agents
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Dermatology (AREA)
- Child & Adolescent Psychology (AREA)
- Hospice & Palliative Care (AREA)
- Vascular Medicine (AREA)
- Urology & Nephrology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Physical Education & Sports Medicine (AREA)
- Gastroenterology & Hepatology (AREA)
- Nutrition Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Abstract
SE REFIERE A COMPUESTOS HETEROCICLICOS DE FORMULA A-Q-B-C-D DONDE A ES ALQUILO, ALCOXILO, CICLOALQUILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS; Q ES HETEROCICLO O HETEROARILO DE 5 MIEMBROS DIVALENTE O TRIVALENTE; B ES HETEROARILO DIVALENTE OPCIONALMENTE SUSTITUIDO DE FORMULA (I), (II), ENTRE OTROS, DONDE X1 Y X2' SON CADA UNO O, NH, S, ENTRE OTROS; X1', X2, X3 Y X4 SON CADA UNO N O CH; C ES UN COMPUESTO DE FORMULA (III), ARILO O HETEROARILO BICICLICO, EN DONDE R1 ES H, CN, HALOGENO, ENTRE OTROS; R'1, R2 Y R'2 SON CADA UNO H, HALOGENO, CF3, ENTRE OTROS; D ES H, OH, CN, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 6-[5-(4-CLORO-FENIL)-[1,3,4]-OXADIAZOL-2-IL]-2-(2,6-DICLORO-FENIL)-1H-BENZO-IMIDAZOL, 6-(5-TERBUTIL-[1,3,4]-OXADIAZOL-2-IL)-2-(2,6-DICLORO-FENIL)-1H-BENZO-IMIDAZOL, 6-(5-CICLOHEXIL-[1,3,4]-OXADIAZOL-2-IL)-2-(2,6-DICLORO-FENIL)-1H-BENZO-IMIDAZOL, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES DE LA ENZIMA ACIL-TRANSFERASA DE ACIL-CoA-DIACIL-GLICEROL 1 (DGAT1) SIENDO UTILES EN EL TRATAMIENTO DE LA OBESIDAD, DIABETES TIPO 2, TOLERANCIA DETERIORADA DE LA GLUCOSA
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US97606407P | 2007-09-28 | 2007-09-28 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20090774A1 true PE20090774A1 (es) | 2009-07-17 |
Family
ID=39971086
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2008001688A PE20090774A1 (es) | 2007-09-28 | 2008-09-26 | Compuestos heterociclicos como moduladores de la enzima dgat1 |
Country Status (27)
| Country | Link |
|---|---|
| US (2) | US7879850B2 (es) |
| EP (1) | EP2205595B1 (es) |
| JP (1) | JP5675359B2 (es) |
| KR (1) | KR101616133B1 (es) |
| CN (1) | CN101932576B (es) |
| AR (1) | AR066169A1 (es) |
| AU (1) | AU2008303541B2 (es) |
| BR (1) | BRPI0817272A2 (es) |
| CA (1) | CA2701053C (es) |
| CL (1) | CL2008002871A1 (es) |
| CO (1) | CO6251263A2 (es) |
| CR (1) | CR11261A (es) |
| CU (1) | CU20100049A7 (es) |
| EA (1) | EA019347B1 (es) |
| EC (1) | ECSP10010051A (es) |
| ES (1) | ES2525703T3 (es) |
| IL (1) | IL203797A (es) |
| MA (1) | MA31707B1 (es) |
| MX (1) | MX2010003264A (es) |
| MY (1) | MY151551A (es) |
| NZ (1) | NZ583285A (es) |
| PE (1) | PE20090774A1 (es) |
| TN (1) | TN2010000096A1 (es) |
| TW (1) | TWI429642B (es) |
| UA (1) | UA99305C2 (es) |
| WO (1) | WO2009040410A1 (es) |
| ZA (1) | ZA201000829B (es) |
Families Citing this family (26)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20070087096A (ko) | 2004-12-14 | 2007-08-27 | 아스트라제네카 아베 | Ｄｇａｔ 억제제로서의 옥사디아졸 유도체 |
| US7749997B2 (en) | 2005-12-22 | 2010-07-06 | Astrazeneca Ab | Pyrimido [4,5-B] -Oxazines for use as DGAT inhibitors |
| NZ572586A (en) | 2006-05-30 | 2011-03-31 | Astrazeneca Ab | Substituted 5-phenylamino-1,3,4-oxadiazol-2-ylcarbonylamino-4-phenoxy-cyclohexane carboxylic acid as inhibitors of acetyl coenzyme a diacylglycerol acyltransferase |
| AR066169A1 (es) * | 2007-09-28 | 2009-07-29 | Novartis Ag | Derivados de benzo-imidazoles, utiles para trastornos asociados con la actividad de dgat |
| WO2009112445A1 (en) * | 2008-03-10 | 2009-09-17 | Novartis Ag | Method of increasing cellular phosphatidyl choline by dgat1 inhibition |
| EP2408766A1 (en) * | 2009-03-18 | 2012-01-25 | Schering Corporation | Bicyclic compounds as inhibitors of diacylglycerol acyltransferase |
| EP2519500A1 (en) | 2009-12-31 | 2012-11-07 | Piramal Healthcare Ltd. | Inhibitors of diacylglycerol acyl transferase |
| MA34097B1 (fr) | 2010-03-30 | 2013-03-05 | Novartis Ag | Utilisations d'inhibiteurs de dgat1 |
| WO2012044567A2 (en) * | 2010-09-30 | 2012-04-05 | Merck Sharp & Dohme Corp. | Imidazole derivatives |
| WO2012064569A1 (en) * | 2010-11-08 | 2012-05-18 | Merck Sharp & Dohme Corp. | Imidazole derivatives |
| PT2729142T (pt) | 2011-07-08 | 2018-10-01 | Novartis Ag | Método de tratamento de aterosclerose em sujeitos com nível elevado de triglicéridos |
| WO2013074387A1 (en) * | 2011-11-14 | 2013-05-23 | Merck Sharp & Dohme Corp. | Imidazole derivatives |
| WO2013169648A1 (en) | 2012-05-07 | 2013-11-14 | Novartis Ag | Pharmaceutical combinations comprising a dgat1 inhibtor and a triglyceride lowering drug |
| EP2903985A1 (en) | 2012-10-03 | 2015-08-12 | Advinus Therapeutics Limited | Spirocyclic compounds, compositions and medicinal applications thereof |
| US9796729B2 (en) | 2012-11-23 | 2017-10-24 | Glaxosmithkline Llc | Compounds as diacylglycerol acyltransferase inhibitors |
| ME03315B (me) * | 2012-11-23 | 2019-10-20 | Glaxosmithkline Llc | Nova jedinjenja као inhibiтori diacilglicerin acil transferaze |
| WO2014081996A1 (en) * | 2012-11-23 | 2014-05-30 | Glaxosmithkline Llc | Novel compounds as diacylglycerol acyltransferase inhibitors |
| CN103087045B (zh) * | 2013-01-11 | 2015-08-12 | 上海交通大学 | 一种苯并咪唑类杂环化合物、药物组合物及其用途 |
| CN104610152A (zh) * | 2015-02-13 | 2015-05-13 | 佛山市赛维斯医药科技有限公司 | 一类环丙基酰肼类gpr119激动剂、制备方法及其用途 |
| CN104672144A (zh) * | 2015-02-13 | 2015-06-03 | 佛山市赛维斯医药科技有限公司 | 一种环丙基酰肼和硝基苯类gpr119激动剂、制备方法及其用途 |
| KR102747096B1 (ko) | 2018-03-16 | 2024-12-26 | 앤지 파마수티컬스 잉크. | 심한 변비를 치료하기 위한 조성물 및 방법 |
| JP7657151B2 (ja) | 2018-11-27 | 2025-04-04 | ノバルティス アーゲー | 代謝性障害の処置のためのプロタンパク質コンバターゼスブチリシン／ケキシン９型（ｐｃｓｋ９）阻害剤としての環状ペプチド |
| UY38485A (es) | 2018-11-27 | 2020-06-30 | Novartis Ag | Compuestos tetrámeros cíclicos como inhibidores de proproteína convertasa subtilisina/kexina tipo 9 (pcsk9), método de tratamiento, uso y su preparación |
| WO2020110008A1 (en) | 2018-11-27 | 2020-06-04 | Novartis Ag | Cyclic pentamer compounds as proprotein convertase subtilisin/kexin type 9 (pcsk9) inhibitors for the treatment of metabolic disorder |
| WO2023084449A1 (en) | 2021-11-12 | 2023-05-19 | Novartis Ag | Diaminocyclopentylpyridine derivatives for the treatment of a disease or disorder |
| CN117466863A (zh) * | 2022-07-20 | 2024-01-30 | 盛睿泽华医药科技（苏州）有限公司 | 含芳香族取代基的苯并咪唑化合物及其制备方法和用途 |
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