PE20161369A1 - Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona sustituidos con tetrazolona - Google Patents
Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona sustituidos con tetrazolonaInfo
- Publication number
- PE20161369A1 PE20161369A1 PE2016001576A PE2016001576A PE20161369A1 PE 20161369 A1 PE20161369 A1 PE 20161369A1 PE 2016001576 A PE2016001576 A PE 2016001576A PE 2016001576 A PE2016001576 A PE 2016001576A PE 20161369 A1 PE20161369 A1 PE 20161369A1
- Authority
- PE
- Peru
- Prior art keywords
- mgat2
- inhibitors
- alkyl
- compounds
- membered
- 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
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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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
- A61P1/16—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- 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
-
- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A61P27/06—Antiglaucoma agents or miotics
-
- 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
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- 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
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- 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
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- 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
-
- 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
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- 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
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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
- C07D401/02—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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
-
- 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
-
- 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
- C07D417/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Ophthalmology & Optometry (AREA)
- Urology & Nephrology (AREA)
- Endocrinology (AREA)
- Emergency Medicine (AREA)
- Child & Adolescent Psychology (AREA)
- Dermatology (AREA)
- Gastroenterology & Hepatology (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Vascular Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Se refiere a compuestos de formula I o un esteroisomero, tautomero, sal farmaceuticamente aceptable, polimorfo, solvato o hidrato, donde: el anillo A es independientemente fenilo o heteroarilo de 5 a 6 miembros opcionalmente sustituidos; R1 es es (CH2)m-(carbociclo C3-C6 sustituido); (CH2)m-(heteroarilo de 5 a 6 miembros sustituido), entre otros; R2 es alquilo C1-C4, cicloalquilo C3-C4 y haloalquilo C1-C4; R3 es H, F, alquilo C1-C4 y CN; R4 es H, F y alquilo C1-C4; o R3 y R4 se pueden unir para formar un carbociclo de 3 a 6 miembros; m es 0, 1, 2, 3 o 4. Son compuestos preferidos: (S)-3-(5-oxo-4,5-dihidro-1H-tetrazol-1-il)-4-(p-tolil)-6-(4-(4,4,4- trifluorobutoxi)fenil)-6-(trifluorometil)-5,6-dihidropiridin-2(1H)-ona; entre otros. Tambien se refiere a una composicion farmaceutica y a un metodo de tratamiento. Dichos compuestos son inhibidores de monoacilglicerol aciltransferasa tipo 2 (MGAT2), siendo utiles en el tratamiento de diabetes, obesidad, entre otros
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201461949490P | 2014-03-07 | 2014-03-07 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20161369A1 true PE20161369A1 (es) | 2016-12-17 |
Family
ID=52686513
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2016001576A PE20161369A1 (es) | 2014-03-07 | 2015-03-05 | Inhibidores de monoacilglicerol aciltransferasa 2 (mgat2) de dihidropiridinona sustituidos con tetrazolona |
Country Status (31)
Country | Link |
---|---|
US (6) | US9688656B2 (es) |
EP (1) | EP3114120B1 (es) |
JP (1) | JP6449919B2 (es) |
KR (1) | KR102336371B1 (es) |
CN (1) | CN106061968B (es) |
AU (1) | AU2015227140B2 (es) |
BR (1) | BR112016019487B1 (es) |
CA (1) | CA2941951C (es) |
CL (1) | CL2016002238A1 (es) |
CY (1) | CY1121746T1 (es) |
DK (1) | DK3114120T3 (es) |
EA (1) | EA030561B1 (es) |
ES (1) | ES2719713T3 (es) |
HR (1) | HRP20190668T1 (es) |
HU (1) | HUE044272T2 (es) |
IL (1) | IL247592B (es) |
LT (1) | LT3114120T (es) |
MA (1) | MA39335B1 (es) |
MX (1) | MX2016011223A (es) |
MY (1) | MY176921A (es) |
NZ (1) | NZ724890A (es) |
PE (1) | PE20161369A1 (es) |
PH (1) | PH12016501517B1 (es) |
PL (1) | PL3114120T3 (es) |
PT (1) | PT3114120T (es) |
RS (1) | RS58740B1 (es) |
SG (1) | SG11201607393XA (es) |
SI (1) | SI3114120T1 (es) |
TR (1) | TR201906325T4 (es) |
WO (1) | WO2015134699A1 (es) |
ZA (1) | ZA201606174B (es) |
Families Citing this family (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
ES2719713T3 (es) | 2014-03-07 | 2019-07-12 | Bristol Myers Squibb Co | Inhibidores de MGAT2 de dihidropiridinona sustituidos con tetrazolona |
ES2666569T3 (es) | 2014-06-11 | 2018-05-07 | Bristol-Myers Squibb Company | Piridinonas sustituidas como inhibidores de MGAT2 |
CN105218518B (zh) * | 2015-09-15 | 2018-01-12 | 青岛科标检测研究院有限公司 | 一种可用于制备供热采暖系统清洗剂的化合物及其制备方法 |
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 |
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 |
BR112021012428A2 (pt) | 2019-01-11 | 2021-09-08 | Shionogi & Co., Ltd. | Derivado de dihidropirazolopirazinona tendo atividade inibitória de mgat2 |
KR20240056719A (ko) * | 2021-09-08 | 2024-04-30 | 시오노기 앤드 컴파니, 리미티드 | 항비만 작용이 관여하는 질환의 예방 및 치료용 의약 |
EP4201923A1 (en) | 2021-12-23 | 2023-06-28 | Karl-Franzens-Universität Graz | 5-substituted 2,3-dihydropyridin-4-ones and process for preparing the same |
Family Cites Families (6)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5614492A (en) | 1986-05-05 | 1997-03-25 | The General Hospital Corporation | Insulinotropic hormone GLP-1 (7-36) and uses thereof |
US20100016365A1 (en) | 2008-07-17 | 2010-01-21 | Auspex Pharmaceuticals, Inc. | Substituted 4-amino-piperidines |
US8791091B2 (en) | 2011-12-02 | 2014-07-29 | Bristol-Myers Squibb Company | Aryl dihydropyridinone and piperidinone MGAT2 inhibitors |
BR112015029598A2 (pt) | 2013-05-29 | 2017-07-25 | Bristol Myers Squibb Co | inibidores de di-hidropiridinona mgat2 |
ES2719713T3 (es) * | 2014-03-07 | 2019-07-12 | Bristol Myers Squibb Co | Inhibidores de MGAT2 de dihidropiridinona sustituidos con tetrazolona |
CN106068265B (zh) | 2014-03-07 | 2020-05-22 | 百时美施贵宝公司 | 用于治疗代谢病症的二氢吡啶酮mgat2抑制剂 |
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2015
- 2015-03-05 ES ES15710686T patent/ES2719713T3/es active Active
- 2015-03-05 LT LTEP15710686.5T patent/LT3114120T/lt unknown
- 2015-03-05 RS RS20190436A patent/RS58740B1/sr unknown
- 2015-03-05 EP EP15710686.5A patent/EP3114120B1/en active Active
- 2015-03-05 AU AU2015227140A patent/AU2015227140B2/en active Active
- 2015-03-05 MY MYPI2016703163A patent/MY176921A/en unknown
- 2015-03-05 CA CA2941951A patent/CA2941951C/en active Active
- 2015-03-05 WO PCT/US2015/018870 patent/WO2015134699A1/en active Application Filing
- 2015-03-05 KR KR1020167027385A patent/KR102336371B1/ko active IP Right Grant
- 2015-03-05 TR TR2019/06325T patent/TR201906325T4/tr unknown
- 2015-03-05 MA MA39335A patent/MA39335B1/fr unknown
- 2015-03-05 MX MX2016011223A patent/MX2016011223A/es active IP Right Grant
- 2015-03-05 PE PE2016001576A patent/PE20161369A1/es active IP Right Grant
- 2015-03-05 BR BR112016019487-0A patent/BR112016019487B1/pt active IP Right Grant
- 2015-03-05 PL PL15710686T patent/PL3114120T3/pl unknown
- 2015-03-05 US US15/123,773 patent/US9688656B2/en active Active
- 2015-03-05 CN CN201580012204.XA patent/CN106061968B/zh active Active
- 2015-03-05 PT PT15710686T patent/PT3114120T/pt unknown
- 2015-03-05 HU HUE15710686 patent/HUE044272T2/hu unknown
- 2015-03-05 NZ NZ72489015A patent/NZ724890A/en unknown
- 2015-03-05 SG SG11201607393XA patent/SG11201607393XA/en unknown
- 2015-03-05 JP JP2016573680A patent/JP6449919B2/ja active Active
- 2015-03-05 DK DK15710686.5T patent/DK3114120T3/da active
- 2015-03-05 EA EA201691670A patent/EA030561B1/ru not_active IP Right Cessation
- 2015-03-05 SI SI201530657T patent/SI3114120T1/sl unknown
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2016
- 2016-08-01 PH PH12016501517A patent/PH12016501517B1/en unknown
- 2016-09-01 IL IL247592A patent/IL247592B/en active IP Right Grant
- 2016-09-06 CL CL2016002238A patent/CL2016002238A1/es unknown
- 2016-09-06 ZA ZA2016/06174A patent/ZA201606174B/en unknown
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2017
- 2017-05-23 US US15/602,515 patent/US9896431B2/en active Active
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2018
- 2018-01-10 US US15/866,871 patent/US10093650B2/en active Active
- 2018-08-30 US US16/117,107 patent/US10329273B2/en active Active
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2019
- 2019-04-09 HR HRP20190668TT patent/HRP20190668T1/hr unknown
- 2019-05-08 CY CY20191100492T patent/CY1121746T1/el unknown
- 2019-05-09 US US16/407,441 patent/US10538505B2/en active Active
- 2019-11-26 US US16/695,239 patent/US11479538B2/en active Active
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