PE20190518A1 - Inhibidores de diacilglicerol aciltransferasa 2 - Google Patents
Inhibidores de diacilglicerol aciltransferasa 2Info
- Publication number
- PE20190518A1 PE20190518A1 PE2019000392A PE2019000392A PE20190518A1 PE 20190518 A1 PE20190518 A1 PE 20190518A1 PE 2019000392 A PE2019000392 A PE 2019000392A PE 2019000392 A PE2019000392 A PE 2019000392A PE 20190518 A1 PE20190518 A1 PE 20190518A1
- Authority
- PE
- Peru
- Prior art keywords
- diacilglicerol
- aciltransferasa
- inhibitors
- fluorine
- compounds
- Prior art date
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- 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
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
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- 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
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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- A—HUMAN NECESSITIES
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- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
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- A—HUMAN NECESSITIES
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- 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
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- A—HUMAN NECESSITIES
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- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
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- 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
- C07D401/14—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 three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Ophthalmology & Optometry (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Neurology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Gastroenterology & Hepatology (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Vascular Medicine (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Child & Adolescent Psychology (AREA)
- Immunology (AREA)
- Gynecology & Obstetrics (AREA)
- Reproductive Health (AREA)
Abstract
Se refiere a compuestos de Formula (I), donde D1 y D2 son N o CH; R1 es H o (C1-C2)alquilo opcionalmente sustituido con fluor y (C3-C6)cicloalquilo; R2 es H o fluor; R3 es de formula (a), (b) o (c); R4 es H, ciano o (C1-C4)alquilo opcionalmente sustituido con -OH o -S(O)2R6; R5 es H u -OH; R6 es (C1-C4)alquilo. Tambien esta referida a composiciones farmaceuticas y metodos de preparacion. Dichos compuestos son utiles para el tratamiento de enfermedades en animales mediante inhibicion de la actividad de la diacilglicerol aciltransferasa 2 (DGAT2)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662377137P | 2016-08-19 | 2016-08-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20190518A1 true PE20190518A1 (es) | 2019-04-10 |
Family
ID=59762015
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2019000392A PE20190518A1 (es) | 2016-08-19 | 2017-08-09 | Inhibidores de diacilglicerol aciltransferasa 2 |
Country Status (44)
Families Citing this family (42)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR109179A1 (es) * | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| KR20200132852A (ko) | 2018-01-23 | 2020-11-25 | 길라 테라퓨틱스, 인코포레이티드 | 펩티드 yy 약학적 제형, 조성물, 및 방법 |
| WO2019175869A1 (en) | 2018-03-12 | 2019-09-19 | Yeda Research And Development Co. Ltd | Treatment of a heart disease |
| CA3045644C (en) | 2018-06-13 | 2024-01-16 | Pfizer Inc. | Glp-1 receptor agonists and uses thereof |
| IL281093B2 (en) | 2018-08-31 | 2025-11-01 | Pfizer | Combinations for treatment of nash/nafld and related diseases |
| RU2706026C1 (ru) * | 2018-12-28 | 2019-11-13 | Государственное бюджетное учреждение здравоохранения города Москвы Московский клинический научно-практический центр им. А.С. Логинова Департамента здравоохранения города Москвы | Способ лечения неалкогольной жировой болезни печени и сахарного диабета второго типа |
| CA3140972C (en) * | 2019-05-20 | 2024-06-18 | Pfizer Inc. | Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases |
| TWI771766B (zh) | 2019-10-04 | 2022-07-21 | 美商輝瑞股份有限公司 | 二醯基甘油醯基轉移酶2 抑制劑 |
| WO2021076817A2 (en) * | 2019-10-16 | 2021-04-22 | Ohio State Innovation Foundation | Methods and compositions related to treatment and prevention of cancer by inhibition of dgat1 and dgat2 |
| US20230045419A1 (en) | 2019-12-10 | 2023-02-09 | Pfizer Inc. | Solid Forms of 2-((4-((S)-2-(5-Chloropyridin-2-yl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((S)-oxetan-2-yl)methyl)-1H-benzo[d]imidazole-6-carboxylic acid, 1,3-Dihydroxy-2-(hydroxymethyl)propan-2-amine Salt |
| PH12022551271A1 (en) * | 2019-12-23 | 2023-11-29 | Lg Chemical Ltd | Novel amino aryl derivative useful as diacylglycerol acyltransferase 2 inhibitor and use thereof |
| CA3161640A1 (en) * | 2019-12-23 | 2021-07-01 | Seung Hyun Yoon | Novel amide derivative useful as diacylglycerol acyltransferase 2 inhibitor, and use thereof |
| SMT202400344T1 (it) | 2020-02-07 | 2024-11-15 | Gasherbrum Bio Inc | Agonisti di glp-1 eterociclici |
| WO2021161222A1 (en) * | 2020-02-11 | 2021-08-19 | Inorbit Therapeutics Ab | Compounds useful in inhibiting diacylglycerol o-acyltransferase and methods of making and using the same |
| JP2021134211A (ja) | 2020-02-24 | 2021-09-13 | ファイザー・インク | Nafld/nashおよび関連疾患の処置のための組合せ |
| JP2022058085A (ja) * | 2020-02-24 | 2022-04-11 | ファイザー・インク | ジアシルグリセロールアシルトランスフェラーゼ2阻害剤とアセチル-CoAカルボキシラーゼ阻害剤との組合せ |
| BR112022017578A2 (pt) | 2020-03-27 | 2022-10-18 | Pfizer | Tratamento do diabetes tipo 2 ou obesidade ou sobrepeso com ácido 2-[(4-{6-[(4-ciano-2-fluorobenzil)óxi]piridin-2-il}piperidin-1-il)metil]-1-[(2s)-oxetan-2-ilmetil]-1h-benzimidazol-6-carboxílico ou um sal farmacêutico do mesmo |
| US11478533B2 (en) | 2020-04-27 | 2022-10-25 | Novo Nordisk A/S | Semaglutide for use in medicine |
| TW202208359A (zh) | 2020-05-18 | 2022-03-01 | 美商默沙東藥廠 | 新穎二醯基甘油酯o-醯基轉移酶2抑制劑 |
| HUE068344T2 (hu) | 2020-06-09 | 2024-12-28 | Pfizer | Spirovegyületek mint melanokortin 4 receptor antagonisták és alkalmazásuk |
| TWI817191B (zh) * | 2020-09-04 | 2023-10-01 | 南韓商Lg化學股份有限公司 | 新穎聯芳基衍生物及其作為針對二醯基甘油醯基轉移酶2之抑制劑之用途 |
| JP7482324B2 (ja) | 2020-10-08 | 2024-05-13 | メルク・シャープ・アンド・ドーム・エルエルシー | 新規なジアシルグリセリドo-アシルトランスフェラーゼ2阻害剤としてのオキシインドール誘導体の製造 |
| MX2023003842A (es) | 2020-10-08 | 2023-04-14 | Merck Sharp & Dohme Llc | Preparacion de derivados de benzoimidazolona como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2. |
| US12029718B2 (en) | 2021-11-09 | 2024-07-09 | Cct Sciences, Llc | Process for production of essentially pure delta-9-tetrahydrocannabinol |
| CN112972654B (zh) * | 2021-03-05 | 2022-07-01 | 温州医科大学慈溪生物医药研究院 | Fgf21在制备治疗脑神经损伤的药物中的应用 |
| WO2023026180A1 (en) | 2021-08-26 | 2023-03-02 | Pfizer Inc. | Amorphous form of (s)-2-(5-((3-ethoxypyridin-2-yl)oxy)pyridin-3-yl)-n-(tetrahydrofuran-3- yl)pyrimidine-5-carboxamide |
| KR20240054335A (ko) | 2021-08-31 | 2024-04-25 | 화이자 인코포레이티드 | 2-[(4-{6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일}피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산,1,3-디히드록시-2-(히드록시메틸)프로판-2-아민 염의 고체 형태 |
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| JP2024544021A (ja) | 2021-12-06 | 2024-11-26 | ファイザー・インク | メラノコルチン4受容体アンタゴニストおよびそれらの使用 |
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| WO2025224648A1 (en) | 2024-04-26 | 2025-10-30 | Pfizer Inc. | Oral compositions/formulations of 2-({4-[(2s)-2-(4-chloro-2-fluorophenyl)-2-methyl-1,3-benzodioxol-4-yl]piperidin-1-yl}methyl)-1-[(2s)-oxetan-2-ylmethyl]-1h-benzimidazole-6-carboxylic acid or a pharmaceutically salt thereof |
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