CO2023004366A2 - Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 - Google Patents
Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2Info
- Publication number
- CO2023004366A2 CO2023004366A2 CONC2023/0004366A CO2023004366A CO2023004366A2 CO 2023004366 A2 CO2023004366 A2 CO 2023004366A2 CO 2023004366 A CO2023004366 A CO 2023004366A CO 2023004366 A2 CO2023004366 A2 CO 2023004366A2
- Authority
- CO
- Colombia
- Prior art keywords
- formula
- compounds
- acyltransferase
- diacylglycerol
- preparation
- Prior art date
Links
- 102100035762 Diacylglycerol O-acyltransferase 2 Human genes 0.000 title 1
- 101710167503 Diacylglycerol O-acyltransferase 2 Proteins 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004095 oxindolyl group Chemical class N1(C(CC2=CC=CC=C12)=O)* 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 5
- 201000010099 disease Diseases 0.000 abstract 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000008338 non-alcoholic fatty liver disease Diseases 0.000 abstract 2
- 206010053219 non-alcoholic steatohepatitis Diseases 0.000 abstract 2
- 201000001320 Atherosclerosis Diseases 0.000 abstract 1
- 206010007558 Cardiac failure chronic Diseases 0.000 abstract 1
- 229940127194 DGAT2 inhibitor Drugs 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 206010016654 Fibrosis Diseases 0.000 abstract 1
- 206010019708 Hepatic steatosis Diseases 0.000 abstract 1
- 208000035150 Hypercholesterolemia Diseases 0.000 abstract 1
- 208000031226 Hyperlipidaemia Diseases 0.000 abstract 1
- 208000008589 Obesity Diseases 0.000 abstract 1
- 208000020832 chronic kidney disease Diseases 0.000 abstract 1
- 230000006999 cognitive decline Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 230000004761 fibrosis Effects 0.000 abstract 1
- 235000020824 obesity Nutrition 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 239000000651 prodrug Substances 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1
Classifications
-
- 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
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
-
- 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
- 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
- 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
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/32—Oxygen atoms
- C07D209/34—Oxygen atoms in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- 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
- 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
- C07D405/02—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 two hetero rings
- C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Obesity (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Cardiology (AREA)
- Gastroenterology & Hepatology (AREA)
- Heart & Thoracic Surgery (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Indole Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Se inventan compuestos de fórmula I y sales farmacéuticamente aceptables, ésteres y profármacos de los mismos, que son inhibidores de DGAT2. También se proporcionan métodos de preparación de compuestos de Fórmula I, composiciones farmacéuticas que comprenden compuestos de Fórmula I y métodos de uso de estos compuestos para tratar la esteatosis hepática, esteatohepatitis no alcohólica (EHNA), fibrosis, diabetes mellitus de tipo 2, obesidad, hiperlipidemia, hipercolesterolemia, ateroesclerosis, declive cognitivo, demencia, enfermedades cardiorrenales tales como enfermedades renales crónicas e insuficiencia cardíaca y enfermedades y afecciones relacionadas, que comprenden administrar un compuesto de Fórmula I a un paciente que lo necesita.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US202063089063P | 2020-10-08 | 2020-10-08 | |
PCT/US2021/053681 WO2022076496A1 (en) | 2020-10-08 | 2021-10-06 | Preparation of oxindole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
CO2023004366A2 true CO2023004366A2 (es) | 2023-04-27 |
Family
ID=78709520
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
CONC2023/0004366A CO2023004366A2 (es) | 2020-10-08 | 2023-04-05 | Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 |
Country Status (18)
Country | Link |
---|---|
US (2) | US20220112181A1 (es) |
EP (1) | EP4225735A1 (es) |
JP (1) | JP7482324B2 (es) |
KR (1) | KR20230079427A (es) |
CN (1) | CN116457346A (es) |
AR (1) | AR123701A1 (es) |
AU (1) | AU2021358946A1 (es) |
CA (1) | CA3195032A1 (es) |
CL (1) | CL2023000978A1 (es) |
CO (1) | CO2023004366A2 (es) |
CR (1) | CR20230160A (es) |
DO (1) | DOP2023000068A (es) |
EC (1) | ECSP23034049A (es) |
IL (1) | IL301799A (es) |
MX (1) | MX2023003844A (es) |
PE (1) | PE20240217A1 (es) |
TW (1) | TW202229232A (es) |
WO (1) | WO2022076496A1 (es) |
Families Citing this family (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2023233033A1 (en) * | 2022-06-03 | 2023-12-07 | Domain Therapeutics | Novel par-2 inhibitors |
US20240254114A1 (en) | 2022-12-02 | 2024-08-01 | Merck Sharp & Dohme Llc | Preparation of fused azole derivatives as novel diacylglyceride 0-acyltransferase 2 inhibitors |
Family Cites Families (4)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20080287479A1 (en) * | 2006-12-20 | 2008-11-20 | Pfizer Inc | Inhibitors of serine palmitoyltransferase |
WO2010077839A1 (en) * | 2008-12-15 | 2010-07-08 | Wyeth Llc (Formerly Known As Wyeth) | Substituted oxindol cb2 agonists for pain treatment |
MX2019005679A (es) * | 2016-11-18 | 2019-08-14 | Merck Sharp & Dohme | Derivados de indol de utilidad como inhibidores de diacilglicerido o-aciltransferasa 2. |
MA46856A (fr) * | 2016-11-18 | 2019-09-25 | Merck Sharp & Dohme | Dérivés d'indazole utiles en tant qu'inhibiteurs de la diacylglycéride o-acyltransférase 2 |
-
2021
- 2021-10-06 CN CN202180076390.9A patent/CN116457346A/zh active Pending
- 2021-10-06 EP EP21811162.3A patent/EP4225735A1/en active Pending
- 2021-10-06 PE PE2023001362A patent/PE20240217A1/es unknown
- 2021-10-06 JP JP2023521377A patent/JP7482324B2/ja active Active
- 2021-10-06 MX MX2023003844A patent/MX2023003844A/es unknown
- 2021-10-06 TW TW110137151A patent/TW202229232A/zh unknown
- 2021-10-06 KR KR1020237014915A patent/KR20230079427A/ko active Search and Examination
- 2021-10-06 CA CA3195032A patent/CA3195032A1/en active Pending
- 2021-10-06 CR CR20230160A patent/CR20230160A/es unknown
- 2021-10-06 US US17/494,896 patent/US20220112181A1/en active Pending
- 2021-10-06 IL IL301799A patent/IL301799A/en unknown
- 2021-10-06 WO PCT/US2021/053681 patent/WO2022076496A1/en active Application Filing
- 2021-10-06 AR ARP210102767A patent/AR123701A1/es unknown
- 2021-10-06 AU AU2021358946A patent/AU2021358946A1/en active Pending
-
2023
- 2023-04-04 CL CL2023000978A patent/CL2023000978A1/es unknown
- 2023-04-05 CO CONC2023/0004366A patent/CO2023004366A2/es unknown
- 2023-04-05 DO DO2023000068A patent/DOP2023000068A/es unknown
- 2023-05-08 EC ECSENADI202334049A patent/ECSP23034049A/es unknown
-
2024
- 2024-05-23 US US18/672,808 patent/US20240327391A1/en active Pending
Also Published As
Publication number | Publication date |
---|---|
AU2021358946A1 (en) | 2023-06-08 |
MX2023003844A (es) | 2023-04-14 |
CL2023000978A1 (es) | 2023-09-29 |
CR20230160A (es) | 2023-06-02 |
US20240327391A1 (en) | 2024-10-03 |
DOP2023000068A (es) | 2023-05-31 |
KR20230079427A (ko) | 2023-06-07 |
CN116457346A (zh) | 2023-07-18 |
JP7482324B2 (ja) | 2024-05-13 |
CA3195032A1 (en) | 2022-04-14 |
JP2023541714A (ja) | 2023-10-03 |
EP4225735A1 (en) | 2023-08-16 |
US20220112181A1 (en) | 2022-04-14 |
PE20240217A1 (es) | 2024-02-16 |
WO2022076496A1 (en) | 2022-04-14 |
AU2021358946A9 (en) | 2024-02-08 |
AR123701A1 (es) | 2023-01-04 |
ECSP23034049A (es) | 2023-06-30 |
IL301799A (en) | 2023-05-01 |
TW202229232A (zh) | 2022-08-01 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
CO2023004366A2 (es) | Preparación de derivados de oxindol como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 | |
ES2611657T3 (es) | Inhibidores de pirazol-carboxamida del factor Xa | |
MX2021013472A (es) | Moduladores de thr-? y metodos de uso de estos. | |
WO2006090817A1 (ja) | インドール化合物およびその用途 | |
CO6470847A2 (es) | Derivados amino-propiónicos sustituidos como inhibidores de neprilisina | |
AR070299A1 (es) | Derivados de pirazolopirimidinas como inhibidores de quinasas dependientes de ciclinas, usos y composiciones farmaceuticas | |
CU20110216A7 (es) | Derivados aminobutíricos sustituidos como inhibidores de neprilisina | |
DOP2023000069A (es) | Preparación de derivados de benzoimidazolona como nuevos inhibidores de la diacilglicerol o-aciltransferasa 2 | |
EA022311B1 (ru) | Оксабициклогептаны и оксабициклогептены, их получение и применение | |
DOP2013000191A (es) | Derivados de heteroarilo como modulares de nachr alfa 7 | |
KR20190020170A (ko) | 통풍 또는 고뇨산혈증과 관련된 증상의 치료 또는 예방을 위한 화합물, 조성물 및 방법 | |
US11034663B2 (en) | Tetrahydronaphtho[1,2-b]furan-2(3H)-one derivatives and preparation and uses thereof | |
AR064253A1 (es) | Compuestos de biciclocarboxiamida sustituidos composiciones farmaceuticas y una combinacion que los incluye y su uso en fabaricacion de un medicamento para el tratamiento de enfermedades mediadas por la actividad del receptor vr1 | |
JPWO2020123827A5 (es) | ||
RU2019143106A (ru) | Двойные модуляторы фарнезоидного x-рецептора и растворимой эпоксидгидролазы | |
JP2020073466A (ja) | プロドラッグ化合物およびそれらの使用 | |
ES2829286T3 (es) | Derivado de amina cíclica y utilización farmacéutica del mismo | |
AU2007341218B2 (en) | Isosorbide mononitrate derivatives for the treatment of intestinal disorders | |
JP2017512183A5 (es) | ||
EP2150550A4 (en) | NOVEL CARBAMOYLOXY ARYL ALKANE ARYLPIPERAZINE COMPOUND, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME, AND METHOD FOR TREATING PAIN, ANXIETY AND DEPRESSION BY ADMINISTERING SAID COMPOUND | |
MX2023007626A (es) | Preparacion de derivados de tetrahidroindazol como innovadores inhibidores de la diacilglicerido o-aciltransferasa 2. | |
CO2021006087A2 (es) | Compuestos aromáticos y usos farmacéuticos de los mismos | |
CN102225896B (zh) | 大黄酸的醚衍生物以及它们的治疗用途 | |
US20160244423A1 (en) | Chromene derivatives substituted by alkoxide as inhibitors of the tcr-nck interaction | |
ES2376054T3 (es) | Simmondsin para uso como un inhibidor angiogenesis. |