[go: up one dir, main page]

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
Application number
MX2021008050A
Other languages
English (en)
Inventor
Manabu Katou
Toshihiro Wada
yusuke Tateno
Original Assignee
Shionogi & Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shionogi & Co filed Critical Shionogi & Co
Publication of MX2021008050A publication Critical patent/MX2021008050A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/10Spiro-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/499Spiro-condensed pyrazines or piperazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/04Anorexiants; Antiobesity agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/12Heterocyclic 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
    • C07D487/20Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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
    • C07D491/20Spiro-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.
MX2021008050A 2019-01-11 2020-01-10 Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2). MX2021008050A (es)

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)

* Cited by examiner, † Cited by third party
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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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

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

Similar Documents

Publication Publication Date Title
CL2018001618A1 (es) Un medicamento que comprende a) compuestos heterociclicos nitrogenados fusionados, moduladores de cen y cpe, y b) un compuestyo o anticuerpo con actividad antiinfluenza; y su uso para la influenza.
TW200735877A (en) Aminodihydrothiazine derivatives
SA520411017B1 (ar) Mgat-2 مشتق ذو حلقة ملتحمة له نشاط مثبط لـ
MX2017013809A (es) Derivados de piridona policiclica sustituida y profarmaco de los mismos.
CL2017001967A1 (es) Composición agroquímica
CO2021008681A2 (es) Inhibidor de 15-pgdh
MX2023000630A (es) Inhibidor de rock, y método de preparacion para el mismo y uso del mismo.
GT200900283A (es) "terapia de combinación con un compuesto actuando como un inhibidor del receptor adp plaquetario".
CY1113813T1 (el) Νεες ενωσεις που εχουν ανασταλτικη δραστικοτητα εναντια στον εξαρτωμενο απο το νατριο μεταφορεα
MX2019001640A (es) Composiciones farmaceuticas que contienen derivados de piridona policiclicos sustituidos y profarmacos de los mismos.
AR058433A1 (es) Derivado de 1,1-dioxido de 1,4-benzotiazepina ,procedimiento para su preparacion ,medicamentos que comprenden este compuesto y su uso
CL2012002526A1 (es) Uso de compuestos inhibidores de dpp iv de formula (i) o (ii) o una de sus sales, para el tratamiento de falla cardiaca.
EA200401304A1 (ru) Набор для ингаляции с ингаляционным порошком, содержащим тиотропий
UY31674A1 (es) Derivado heterocíclico fusionado y su uso
ECSP22005485A (es) Compuestos macrocíclicos como agonistas de sting y métodos y usos de los mismos
AR083060A1 (es) Compuesto de ciclopropano y composiciones farmaceuticas que lo contienen
MX2021008050A (es) Derivado de dihidropirazolopirazinona que tiene actividad inhibidora de monoacilglicerol aciltransferasa 2 (mgat2).
CL2022001353A1 (es) Inhibidores de egfr
DOP2021000272A (es) Uso terapéutico de agonista trigonal de los receptores de glucagon, glp-1 y gip o conjugado de los mismos para enfermedades hepáticas
AR091888A1 (es) Compuestos de urea y su uso como inhibidores de enzimas
AR114270A1 (es) Compuestos de 4-metildihidropirimidinona y su uso farmacéutico
MX2023003245A (es) Derivados de amina novedosos.
AR042037A1 (es) Profarmaco de celecoxib
DOP2006000133A (es) Derivados de 4,5 diarilpiroxol, su preparación y su aplicación en terapeútica
UY26568A1 (es) Nuevos derivados de amidas heterocíclicas