MX2021008050A - Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2). - Google Patents
Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2).Info
- Publication number
- MX2021008050A MX2021008050A MX2021008050A MX2021008050A MX2021008050A MX 2021008050 A MX2021008050 A MX 2021008050A MX 2021008050 A MX2021008050 A MX 2021008050A MX 2021008050 A MX2021008050 A MX 2021008050A MX 2021008050 A MX2021008050 A MX 2021008050A
- Authority
- MX
- Mexico
- Prior art keywords
- hydroxy
- halogen
- hydrogen
- dihydropyrazolopyrazinone
- acyltranferase
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000002759 monoacylglycerols Chemical class 0.000 title 1
- 229910052736 halogen Inorganic materials 0.000 abstract 4
- 150000002367 halogens Chemical class 0.000 abstract 4
- 150000002431 hydrogen Chemical group 0.000 abstract 4
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 4
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- -1 cyano, carboxy Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- 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
- C07D487/10—Spiro-condensed 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
- A61K31/4985—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
- A61K31/499—Spiro-condensed pyrazines or piperazines
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
-
- 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
-
- 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
- C07D487/12—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 three hetero rings
- C07D487/20—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
- C07D491/20—Spiro-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Diabetes (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Child & Adolescent Psychology (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Endocrinology (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a un compuesto representado por la siguiente fórmula. (ver Fórmula) Un compuesto representado por, en donde R1 es hidrógeno, hidroxi, o similares; R2a y R2b pueden ser tomados en conjunto con un átomo de carbono adyacente para formar el anillo B, el anillo B es un carbociclo no aromático sustituido o no sustituido o un heterociclo no aromático sustituido o no sustituido; R3a es hidrógeno, halógeno, hidroxi, o similares; R3b es hidrógeno, halógeno, hidroxi, o similares; R4a es un grupo representado por la fórmula: (ver Fórmulas) L3 es un enlace sencillo o alquileno sustituido o no sustituido, R7 es hidrógeno, halógeno, hidroxi, o similares, y R4b es halógeno, ciano, carboxi, o similares, o su sal farmacéuticamente aceptable.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2019003073 | 2019-01-11 | ||
| PCT/JP2020/000553 WO2020145369A1 (ja) | 2019-01-11 | 2020-01-10 | Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MX2021008050A true MX2021008050A (es) | 2021-08-05 |
Family
ID=71520981
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2021008050A MX2021008050A (es) | 2019-01-11 | 2020-01-10 | Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2). |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US12227509B2 (es) |
| EP (1) | EP3909583A4 (es) |
| JP (1) | JP7608166B2 (es) |
| KR (1) | KR20210114001A (es) |
| CN (2) | CN119409703A (es) |
| AU (1) | AU2020207716A1 (es) |
| BR (1) | BR112021012428A2 (es) |
| CA (1) | CA3126334A1 (es) |
| MX (1) | MX2021008050A (es) |
| TW (1) | TWI840489B (es) |
| WO (1) | WO2020145369A1 (es) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022016394A (ja) * | 2020-07-10 | 2022-01-21 | 塩野義製薬株式会社 | Mgat2阻害活性を有するジヒドロピラゾロピラジノン誘導体を含有する医薬組成物 |
| MX2024002863A (es) | 2021-09-08 | 2024-03-21 | Shionogi & Co | Medicina para la prevencion y tratamiento de enfermedades vinculadas a la actividad antiobesidad. |
Family Cites Families (47)
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| ZA200504898B (en) | 2002-12-20 | 2006-11-29 | Pharmacia Corp | Acyclic pyrazole compounds |
| RU2318818C1 (ru) | 2006-04-12 | 2008-03-10 | Общество С Ограниченной Ответственностью "Исследовательский Институт Химического Разнообразия" | Азагетероциклы, комбинаторная библиотека, фокусированная библиотека, фармацевтическая композиция и способ получения (варианты) |
| US8232282B2 (en) | 2006-09-28 | 2012-07-31 | Dainippon Sumitomo Pharma Co., Ltd. | Compound having bicyclic pyrimidine structure and pharmaceutical composition comprising the same |
| CA2673888A1 (en) | 2007-01-04 | 2008-07-17 | Merck And Co., Inc. | Bicyclic spiropiperidine beta-secretase inhibitors for the treatment of alzheimer's disease |
| CA2719538C (en) | 2008-04-07 | 2014-03-18 | Amgen Inc. | Gem-disubstituted and spirocyclic amino pyridines/pyrimidines as cell cycle inhibitors |
| CA2751244A1 (en) | 2009-02-23 | 2010-08-26 | Msd K.K. | Pyrimidin-4(3h)-one derivatives |
| KR20100097077A (ko) | 2009-02-25 | 2010-09-02 | 주식회사 중외제약 | Hsp90에 대한 억제 효능을 갖는 피리디논 유도체 |
| PL2516434T3 (pl) | 2009-12-23 | 2015-11-30 | Takeda Pharmaceuticals Co | Skondensowane heteroaromatyczne pirolidynony jako inhibitory SYK |
| JP2014051434A (ja) | 2010-12-28 | 2014-03-20 | Dainippon Sumitomo Pharma Co Ltd | 二環性ピリミジン誘導体 |
| MY161407A (en) | 2011-03-01 | 2017-04-14 | Janssen Pharmaceutica Nv | 6,7-DIHYDRO-PYRAZOLO[1,5-a]PYRAZIN-4-YLAMINE DERIVATIVES USEFUL AS INHIBITORS OF BETA-SECRETASE (BACE) |
| WO2012124744A1 (ja) | 2011-03-14 | 2012-09-20 | 大正製薬株式会社 | 含窒素縮合複素環化合物 |
| JP6042060B2 (ja) | 2011-09-26 | 2016-12-14 | サノフイ | ピラゾロキノリノン誘導体、その調製および治療上の使用 |
| PT2573073E (pt) | 2011-09-26 | 2015-02-05 | Sanofi Sa | Derivados de pirazoloquinolinona, sua preparação e sua utilização terapêutica |
| CN103012397B (zh) | 2011-09-26 | 2017-03-01 | 赛诺菲 | 吡唑并喹啉酮衍生物、其制备方法及其治疗用途 |
| US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
| EP2807147A1 (en) | 2012-01-23 | 2014-12-03 | Eli Lilly and Company | Phenyl methanesulfonamide derivatives useful as mgat - 2 inhibitors |
| SG11201404508XA (en) | 2012-01-31 | 2014-10-30 | Lilly Co Eli | Novel morpholinyl derivatives useful as mogat-2 inhibitors |
| AR089771A1 (es) | 2012-01-31 | 2014-09-17 | Lilly Co Eli | Derivados de bencil sulfonamida utiles como inhibidores de mogat-2 |
| TW201348226A (zh) | 2012-02-28 | 2013-12-01 | Amgen Inc | 作為pim抑制劑之醯胺 |
| CN104321325B (zh) | 2012-05-24 | 2016-11-16 | 诺华股份有限公司 | 吡咯并吡咯烷酮化合物 |
| JP2014005245A (ja) | 2012-06-26 | 2014-01-16 | Dainippon Sumitomo Pharma Co Ltd | 二環性ピリミジン誘導体を含有する医薬組成物 |
| JP2014009165A (ja) | 2012-06-27 | 2014-01-20 | Dainippon Sumitomo Pharma Co Ltd | 二環性ピリミジン化合物 |
| JP6099753B2 (ja) | 2012-10-03 | 2017-03-22 | アドビナス セラピューティクス リミテッド | スピロ環化合物、その組成物及びその医薬応用 |
| EP2917194B1 (en) | 2012-11-06 | 2017-09-27 | Eli Lilly and Company | Novel benzyl sulfonamide compounds useful as mogat-2 inhibitors |
| JPWO2014133134A1 (ja) | 2013-02-28 | 2017-02-02 | 味の素株式会社 | 新規テトラヒドロピリドピリミジノン誘導体 |
| ES2633440T3 (es) | 2013-03-25 | 2017-09-21 | Sanofi | Derivados de pirazolonaftiridinona como inhibidores de metAP2 (metionina aminopeptidasa 2). |
| CN104109160B (zh) | 2013-04-17 | 2017-12-15 | 上海翰森生物医药科技有限公司 | 吡咯并n杂环类化合物及其制备方法和医药用途 |
| KR102291444B1 (ko) | 2013-05-29 | 2021-08-18 | 브리스톨-마이어스 스큅 컴퍼니 | 디히드로피리디논 mgat2 억제제 |
| TW201605859A (zh) | 2013-11-14 | 2016-02-16 | 必治妥美雅史谷比公司 | 作為酪蛋白激酶1δ/ε抑制劑之新穎經取代之吡唑并-哌 |
| US10065945B2 (en) | 2014-01-24 | 2018-09-04 | Merck Sharp & Dohme Corp. | Isoquinoline derivatives as MGAT2 inhibitors |
| US9777020B2 (en) | 2014-01-24 | 2017-10-03 | Abbvie Inc. | Furo-3-carboxamide derivatives and methods of use |
| EP3112369A4 (en) | 2014-02-27 | 2017-09-20 | The University of Tokyo | Fused pyrazole derivative having autotaxin inhibitory activity |
| JP2017078024A (ja) | 2014-02-28 | 2017-04-27 | 味の素株式会社 | 新規テトラヒドロピリドピリミジノン誘導体 |
| BR112016019487B1 (pt) | 2014-03-07 | 2023-01-17 | Bristol-Myers Squibb Company | Inibidores de di-hidropiridinona mgat2 tetrazolonasubstituídos, composição farmacêutica e seus usos |
| MX2016011105A (es) | 2014-03-07 | 2016-12-12 | Bristol Myers Squibb Co | Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona para usarse en el tratamiento de trastornos metabolicos. |
| EA032255B1 (ru) | 2014-03-27 | 2019-04-30 | Янссен Фармацевтика Нв | ЗАМЕЩЕННЫЕ ПРОИЗВОДНЫЕ 4,5,6,7-ТЕТРАГИДРОПИРАЗОЛО[1,5-a]ПИРАЗИНА И ПРОИЗВОДНЫЕ 5,6,7,8-ТЕТРАГИДРО-4H-ПИРАЗОЛО[1,5-a][1,4]ДИАЗЕПИНА В КАЧЕСТВЕ ИНГИБИТОРОВ Ros1 |
| EP3154944B1 (en) | 2014-06-11 | 2018-03-14 | Bristol-Myers Squibb Company | Substituted pyridinones as mgat2 inhibitors |
| JP2017171579A (ja) | 2014-08-11 | 2017-09-28 | 味の素株式会社 | 新規テトラヒドロピリドピリミジノン誘導体 |
| AU2015357498B2 (en) | 2014-12-06 | 2019-09-12 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP3237420B1 (en) | 2014-12-22 | 2018-09-26 | Eli Lilly and Company | Erk inhibitors |
| JP2018052818A (ja) | 2015-01-28 | 2018-04-05 | 武田薬品工業株式会社 | スルホンアミド化合物 |
| JP2016164154A (ja) | 2015-02-26 | 2016-09-08 | 塩野義製薬株式会社 | オートタキシン阻害活性を有する7位無置換縮合ピラゾール誘導体 |
| WO2017069224A1 (ja) * | 2015-10-22 | 2017-04-27 | 塩野義製薬株式会社 | Mgat2阻害活性を有するスピロ環誘導体 |
| US10335401B2 (en) * | 2015-12-21 | 2019-07-02 | Shionogi & Co., Ltd. | Non-aromatic heterocyclic derivative having MGAT2 inhibitory activity |
| JP6665575B2 (ja) | 2016-02-23 | 2020-03-13 | ブラザー工業株式会社 | プログラム |
| JP2020158390A (ja) * | 2017-06-20 | 2020-10-01 | 塩野義製薬株式会社 | Mgat2阻害活性を有する非芳香族複素環誘導体およびそれらを含有する医薬組成物 |
| TWI782056B (zh) * | 2017-07-14 | 2022-11-01 | 日商鹽野義製藥股份有限公司 | 具有mgat2抑制活性的縮合環衍生物 |
-
2020
- 2020-01-10 KR KR1020217023263A patent/KR20210114001A/ko not_active Withdrawn
- 2020-01-10 TW TW109100924A patent/TWI840489B/zh active
- 2020-01-10 EP EP20739159.0A patent/EP3909583A4/en active Pending
- 2020-01-10 WO PCT/JP2020/000553 patent/WO2020145369A1/ja not_active Ceased
- 2020-01-10 JP JP2020565216A patent/JP7608166B2/ja active Active
- 2020-01-10 CN CN202411241356.4A patent/CN119409703A/zh active Pending
- 2020-01-10 BR BR112021012428-4A patent/BR112021012428A2/pt not_active Application Discontinuation
- 2020-01-10 MX MX2021008050A patent/MX2021008050A/es unknown
- 2020-01-10 US US17/422,108 patent/US12227509B2/en active Active
- 2020-01-10 CA CA3126334A patent/CA3126334A1/en active Pending
- 2020-01-10 AU AU2020207716A patent/AU2020207716A1/en not_active Abandoned
- 2020-01-10 CN CN202080018835.3A patent/CN113557021A/zh active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20220135577A1 (en) | 2022-05-05 |
| CN113557021A (zh) | 2021-10-26 |
| EP3909583A1 (en) | 2021-11-17 |
| CA3126334A1 (en) | 2020-07-16 |
| BR112021012428A2 (pt) | 2021-09-08 |
| EP3909583A4 (en) | 2022-08-17 |
| KR20210114001A (ko) | 2021-09-17 |
| US12227509B2 (en) | 2025-02-18 |
| TW202043235A (zh) | 2020-12-01 |
| CN119409703A (zh) | 2025-02-11 |
| TWI840489B (zh) | 2024-05-01 |
| JPWO2020145369A1 (ja) | 2021-11-25 |
| JP7608166B2 (ja) | 2025-01-06 |
| AU2020207716A1 (en) | 2021-07-15 |
| WO2020145369A1 (ja) | 2020-07-16 |
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