ECSP22026478A - Inhibidor de diacilglicerol aciltransferasa 2 - Google Patents
Inhibidor de diacilglicerol aciltransferasa 2Info
- Publication number
- ECSP22026478A ECSP22026478A ECSENADI202226478A ECDI202226478A ECSP22026478A EC SP22026478 A ECSP22026478 A EC SP22026478A EC SENADI202226478 A ECSENADI202226478 A EC SENADI202226478A EC DI202226478 A ECDI202226478 A EC DI202226478A EC SP22026478 A ECSP22026478 A EC SP22026478A
- Authority
- EC
- Ecuador
- Prior art keywords
- diacylglycerol
- acytransferase
- inhibitor
- inhibitors
- dgat2
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 4
- 150000001982 diacylglycerols Chemical class 0.000 title 1
- 102100027840 Acyl-CoA wax alcohol acyltransferase 1 Human genes 0.000 abstract 2
- 101000698136 Homo sapiens Acyl-CoA wax alcohol acyltransferase 1 Proteins 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 abstract 1
- 239000000825 pharmaceutical preparation 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
- C07D401/14—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
-
- 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
- A61K31/13—Amines
- A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
-
- 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
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
-
- 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
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7048—Compounds having saccharide radicals and heterocyclic rings having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin, digitoxin or digoxin
-
- 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
-
- 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
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
-
- 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)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Molecular Biology (AREA)
- Gastroenterology & Hepatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Enzymes And Modification Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
En la presente se describen compuestos de la Fórmula (I) en donde R1, R2, R3, R4, R5, R6, R7, R8 y R9 se definen en la presente, su uso como inhibidores de diacilglicerol aciltransferasa 2 (DGAT2), composiciones farmacéuticas que contienen dichos inhibidores y el uso de dichos inhibidores para tratar, por ejemplo, NASH.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962911094P | 2019-10-04 | 2019-10-04 | |
| US202063074123P | 2020-09-03 | 2020-09-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP22026478A true ECSP22026478A (es) | 2022-05-31 |
Family
ID=72826929
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSENADI202226478A ECSP22026478A (es) | 2019-10-04 | 2022-04-04 | Inhibidor de diacilglicerol aciltransferasa 2 |
Country Status (20)
| Country | Link |
|---|---|
| US (2) | US11471458B2 (es) |
| EP (1) | EP4038060B1 (es) |
| JP (1) | JP7161081B2 (es) |
| KR (1) | KR20220079906A (es) |
| CN (1) | CN114787146A (es) |
| AU (1) | AU2020358955B2 (es) |
| CA (1) | CA3095028A1 (es) |
| CL (1) | CL2022000835A1 (es) |
| CO (1) | CO2022004286A2 (es) |
| CR (1) | CR20220139A (es) |
| DO (1) | DOP2022000070A (es) |
| EC (1) | ECSP22026478A (es) |
| ES (1) | ES2966340T3 (es) |
| IL (1) | IL291763A (es) |
| MX (1) | MX2022004035A (es) |
| PE (1) | PE20221444A1 (es) |
| PH (1) | PH12022550812A1 (es) |
| PY (1) | PY2060348A (es) |
| TW (1) | TWI771766B (es) |
| WO (1) | WO2021064590A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11202111244XA (en) | 2019-04-12 | 2021-11-29 | Blueprint Medicines Corp | Pyrrolotriazine derivatives for treating kit- and pdgfra-mediated diseases |
| UA129065C2 (uk) | 2019-12-23 | 2025-01-01 | Елджі Кем, Лтд. | Аміноарильна похідна сполука, корисна як інгібітор діацилгліцеролацилтрансферази-2, та її використання |
| 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 |
| AU2021356589A1 (en) | 2020-10-08 | 2023-05-25 | Merck Sharp & Dohme Llc | Preparation of benzimidazolone derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
| KR102993831B1 (ko) | 2020-10-08 | 2026-07-23 | 머크 샤프 앤드 돔 엘엘씨 | 신규 디아실글리세리드 o-아실트랜스퍼라제 2 억제제로서의 옥스인돌 유도체의 제조 |
| AU2021409234A1 (en) | 2020-12-22 | 2023-06-29 | Merck Sharp & Dohme Llc | Preparation of tetrahydroindazole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
| CN115429810B (zh) * | 2021-06-03 | 2024-03-08 | 苏州禾研生物技术有限公司 | 异黄酮类化合物在制备预防或治疗酒精性肝损伤或解酒保肝的药物中的用途 |
| CN117143008A (zh) * | 2022-08-29 | 2023-12-01 | 江阴勒森生物科技有限公司 | 一种3-溴哌啶-1-甲酸叔丁酯的制备方法 |
| AU2023400409A1 (en) | 2022-12-02 | 2025-06-26 | Merck Sharp & Dohme Llc | Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
Family Cites Families (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3773919A (en) | 1969-10-23 | 1973-11-20 | Du Pont | Polylactide-drug mixtures |
| CA1146866A (en) | 1979-07-05 | 1983-05-24 | Yamanouchi Pharmaceutical Co. Ltd. | Process for the production of sustained release pharmaceutical composition of solid medical material |
| US4485045A (en) | 1981-07-06 | 1984-11-27 | Research Corporation | Synthetic phosphatidyl cholines useful in forming liposomes |
| US4544545A (en) | 1983-06-20 | 1985-10-01 | Trustees University Of Massachusetts | Liposomes containing modified cholesterol for organ targeting |
| DE3438830A1 (de) | 1984-10-23 | 1986-04-30 | Rentschler Arzneimittel | Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung |
| US5013556A (en) | 1989-10-20 | 1991-05-07 | Liposome Technology, Inc. | Liposomes with enhanced circulation time |
| ES2111065T5 (es) | 1991-04-16 | 2005-06-16 | Nippon Shinyaku Company, Limited | Procedimiento para producir una dispersion solida. |
| US5340591A (en) | 1992-01-24 | 1994-08-23 | Fujisawa Pharmaceutical Co., Ltd. | Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine |
| JP3265680B2 (ja) | 1992-03-12 | 2002-03-11 | 大正製薬株式会社 | 経口製剤用組成物 |
| US5612359A (en) | 1994-08-26 | 1997-03-18 | Bristol-Myers Squibb Company | Substituted biphenyl isoxazole sulfonamides |
| DE19504832A1 (de) | 1995-02-14 | 1996-08-22 | Basf Ag | Feste Wirkstoff-Zubereitungen |
| TW536540B (en) | 1997-01-30 | 2003-06-11 | Bristol Myers Squibb Co | Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe |
| PT901786E (pt) | 1997-08-11 | 2007-08-07 | Pfizer Prod Inc | Disperções farmacêuticas sólidas com biodisponibilidade melhorada |
| YU66900A (sh) | 1998-05-04 | 2003-12-31 | Pfizer Products Inc. | Derivati higromicina a |
| ID26984A (id) | 1998-07-06 | 2001-02-22 | Bristol Myers Squibb Co | Senyawa-senyawa sulfonamida sebagai antagonis reseptor angiotensin endotelin ganda |
| EA011086B9 (ru) | 2004-05-12 | 2012-08-30 | Пфайзер Продактс Инк. | Производные пролина и их применение в качестве ингибиторов дипептидилпептидазы iv |
| EP2010520B1 (en) | 2006-04-20 | 2012-09-12 | Pfizer Products Inc. | Heterobicyclic amides for the prevention and treatment of glucokinase-mediated diseases |
| US20090036425A1 (en) | 2007-08-02 | 2009-02-05 | Pfizer Inc | Substituted bicyclolactam compounds |
| CA2729581A1 (en) | 2008-07-29 | 2010-02-04 | Pfizer Inc. | Fluorinated heteroaryls |
| ES2380408T3 (es) | 2008-08-28 | 2012-05-11 | Pfizer Inc. | Derivados de dioxa-biciclo[3.2.1]octano-2,3,4-triol |
| EP2406230A1 (en) | 2009-03-11 | 2012-01-18 | Pfizer Inc. | Substituted indazole amides and their use as glucokinase activators |
| WO2010103437A1 (en) | 2009-03-11 | 2010-09-16 | Pfizer Inc. | Benzofuranyl derivatives used as glucokinase inhibitors |
| CA2754523A1 (en) | 2009-03-20 | 2010-09-23 | Pfizer Inc. | 3-oxa-7-azabicyclo[3.3.1]nonanes |
| CN102438988B (zh) | 2009-04-21 | 2015-06-24 | 内尔维阿诺医学科学有限公司 | 作为hsp90抑制剂的间苯二酚衍生物 |
| CA2759843A1 (en) | 2009-05-08 | 2010-11-10 | Pfizer Inc. | Gpr 119 modulators |
| EP2427448A1 (en) | 2009-05-08 | 2012-03-14 | Pfizer Inc. | Gpr 119 modulators |
| GEP20135907B (en) | 2009-06-05 | 2013-08-12 | Pfizer | L-(piperidin-4-yl)-pyrazole derivatives as gpr 119 modulators |
| WO2011005611A1 (en) | 2009-07-09 | 2011-01-13 | Merck Sharp & Dohme Corp. | Neuromedin u receptor agonists and uses thereof |
| WO2013137628A1 (ko) | 2012-03-16 | 2013-09-19 | 한국생명공학연구원 | 신규한 디아실글리세롤 아실트랜스퍼레이즈 2 억제 물질 및 이의 이용 |
| AU2013245353A1 (en) * | 2012-04-06 | 2014-09-25 | Pfizer Inc. | Diacylglycerol acyltransferase 2 inhibitors |
| AR098394A1 (es) | 2013-11-25 | 2016-05-26 | Lilly Co Eli | Inhibidores de dgat2 (diacilglicerol o-aciltransferasa 2) |
| CU24395B1 (es) | 2014-03-17 | 2019-04-04 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| US10568876B2 (en) | 2014-09-05 | 2020-02-25 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2 |
| EP3188730B1 (en) | 2014-09-05 | 2019-05-01 | Merck Sharp & Dohme Corp. | Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| WO2016036638A1 (en) | 2014-09-05 | 2016-03-10 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2 |
| AR109179A1 (es) * | 2016-08-19 | 2018-11-07 | Pfizer | Inhibidores de diacilglicerol aciltransferasa 2 |
| WO2018109607A1 (en) | 2016-12-16 | 2018-06-21 | Pfizer Inc. | Glp-1 receptor agonists and uses thereof |
| 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 |
-
2020
- 2020-09-28 TW TW109133632A patent/TWI771766B/zh not_active IP Right Cessation
- 2020-09-30 PH PH1/2022/550812A patent/PH12022550812A1/en unknown
- 2020-09-30 IL IL291763A patent/IL291763A/en unknown
- 2020-09-30 JP JP2022520162A patent/JP7161081B2/ja not_active Expired - Fee Related
- 2020-09-30 ES ES20789680T patent/ES2966340T3/es active Active
- 2020-09-30 MX MX2022004035A patent/MX2022004035A/es unknown
- 2020-09-30 PE PE2022000547A patent/PE20221444A1/es unknown
- 2020-09-30 WO PCT/IB2020/059145 patent/WO2021064590A1/en not_active Ceased
- 2020-09-30 CN CN202080083467.0A patent/CN114787146A/zh active Pending
- 2020-09-30 EP EP20789680.4A patent/EP4038060B1/en active Active
- 2020-09-30 CR CR20220139A patent/CR20220139A/es unknown
- 2020-09-30 KR KR1020227014967A patent/KR20220079906A/ko not_active Withdrawn
- 2020-09-30 AU AU2020358955A patent/AU2020358955B2/en not_active Expired - Fee Related
- 2020-10-01 CA CA3095028A patent/CA3095028A1/en active Pending
- 2020-10-02 PY PY202002060348A patent/PY2060348A/es unknown
- 2020-10-05 US US17/062,982 patent/US11471458B2/en active Active
- 2020-11-05 US US17/090,619 patent/US11065249B2/en active Active
-
2022
- 2022-04-01 DO DO2022000070A patent/DOP2022000070A/es unknown
- 2022-04-04 CO CONC2022/0004286A patent/CO2022004286A2/es unknown
- 2022-04-04 CL CL2022000835A patent/CL2022000835A1/es unknown
- 2022-04-04 EC ECSENADI202226478A patent/ECSP22026478A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| ES2966340T3 (es) | 2024-04-22 |
| TW202126635A (zh) | 2021-07-16 |
| PH12022550812A1 (en) | 2023-07-17 |
| US11065249B2 (en) | 2021-07-20 |
| JP2022543499A (ja) | 2022-10-12 |
| PE20221444A1 (es) | 2022-09-21 |
| CA3095028A1 (en) | 2021-04-04 |
| MX2022004035A (es) | 2022-05-02 |
| JP7161081B2 (ja) | 2022-10-25 |
| EP4038060C0 (en) | 2023-11-15 |
| US11471458B2 (en) | 2022-10-18 |
| PY2060348A (es) | 2022-05-20 |
| US20210100796A1 (en) | 2021-04-08 |
| AU2020358955B2 (en) | 2023-08-17 |
| TWI771766B (zh) | 2022-07-21 |
| WO2021064590A1 (en) | 2021-04-08 |
| CN114787146A (zh) | 2022-07-22 |
| US20210100798A1 (en) | 2021-04-08 |
| AU2020358955A1 (en) | 2022-04-21 |
| CO2022004286A2 (es) | 2022-04-29 |
| EP4038060B1 (en) | 2023-11-15 |
| CR20220139A (es) | 2022-05-06 |
| DOP2022000070A (es) | 2022-05-15 |
| IL291763A (en) | 2022-06-01 |
| EP4038060A1 (en) | 2022-08-10 |
| KR20220079906A (ko) | 2022-06-14 |
| CL2022000835A1 (es) | 2023-01-27 |
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