JP2020502058A - ジアシルグリセリドｏ−アシルトランスフェラーゼ２の阻害薬として有用なインダゾール誘導体 - Google Patents

ジアシルグリセリドｏ−アシルトランスフェラーゼ２の阻害薬として有用なインダゾール誘導体 Download PDF

Info

Publication number
JP2020502058A
JP2020502058A JP2019526217A JP2019526217A JP2020502058A JP 2020502058 A JP2020502058 A JP 2020502058A JP 2019526217 A JP2019526217 A JP 2019526217A JP 2019526217 A JP2019526217 A JP 2019526217A JP 2020502058 A JP2020502058 A JP 2020502058A
Authority
JP
Japan
Prior art keywords
indazole
carboxamide
fluorophenyl
alkyl
chlorophenyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
JP2019526217A
Other languages
English (en)
Japanese (ja)
Other versions
JP2020502058A5 (enExample
Inventor
シェン，ドン−ミン
グラハム，トーマス・エイチ
リウ，ウェンシャン
タッジ，クレア
ヴェラ，アンドレアス
ジエン，ジンロン
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp & Dohme LLC
Original Assignee
Merck Sharp & Dohme LLC
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 Merck Sharp & Dohme LLC filed Critical Merck Sharp & Dohme LLC
Publication of JP2020502058A publication Critical patent/JP2020502058A/ja
Publication of JP2020502058A5 publication Critical patent/JP2020502058A5/ja
Ceased legal-status Critical Current

Links

Classifications

    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D515/08—Bridged 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
    • A61K31/41—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
    • A61K31/415—1,2-Diazoles
    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
    • 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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles 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
    • A61K31/33—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
    • A61K31/433—Thidiazoles
    • 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
    • A61K31/4406—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 3, e.g. zimeldine
    • 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
    • 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
    • A61P3/04—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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • 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
    • 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
    • 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
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen 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
    • 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
    • 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
    • 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
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (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)
  • Obesity (AREA)
  • Hematology (AREA)
  • Cardiology (AREA)
  • Vascular Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2019526217A 2016-11-18 2017-11-13 ジアシルグリセリドｏ−アシルトランスフェラーゼ２の阻害薬として有用なインダゾール誘導体 Ceased JP2020502058A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662424066P 2016-11-18 2016-11-18
US62/424,066 2016-11-18
PCT/US2017/061223 WO2018093696A1 (en) 2016-11-18 2017-11-13 Indazole derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2

Publications (2)

Publication Number Publication Date
JP2020502058A true JP2020502058A (ja) 2020-01-23
JP2020502058A5 JP2020502058A5 (enExample) 2020-10-22

Family

ID=62145755

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2019526217A Ceased JP2020502058A (ja) 2016-11-18 2017-11-13 ジアシルグリセリドｏ−アシルトランスフェラーゼ２の阻害薬として有用なインダゾール誘導体

Country Status (12)

Country Link
US (1) US11104690B2 (enExample)
EP (1) EP3541374B1 (enExample)
JP (1) JP2020502058A (enExample)
KR (1) KR20190078646A (enExample)
CN (1) CN110121341A (enExample)
AU (1) AU2017360939B2 (enExample)
BR (1) BR112019010164A2 (enExample)
CA (1) CA3043203A1 (enExample)
MA (1) MA46856A (enExample)
MX (1) MX2019005786A (enExample)
RU (1) RU2019117556A (enExample)
WO (1) WO2018093696A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023545741A (ja) * 2020-10-08 2023-10-31 メルク・シャープ・アンド・ドーム・エルエルシー 新規なジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害剤としてのベンゾイミダゾロン誘導体の製造
JP2024501520A (ja) * 2020-12-22 2024-01-12 メルク・シャープ・アンド・ドーム・エルエルシー 新規ジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害薬としてのテトラヒドロインダゾール誘導体の調製
JP2025537517A (ja) * 2022-11-01 2025-11-18 メルク・シャープ・アンド・ドーム・エルエルシー 新規ジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害薬としてのピラゾロピリジン誘導体及びトリアゾロピリジン誘導体の調製

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MA41179A (fr) 2014-12-19 2017-10-24 Cancer Research Tech Ltd Composés inhibiteurs de parg
US20230174521A1 (en) 2020-05-18 2023-06-08 Merck Sharp & Dohme Llc 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
US20240066027A1 (en) * 2020-12-03 2024-02-29 Domain Therapeutics Novel par-2 inhibitors
PL4496795T3 (pl) 2022-03-23 2026-07-20 Ideaya Biosciences, Inc. Związki indazolowe podstawione piperazyną jako inhibitory parg
AU2023400409A1 (en) 2022-12-02 2025-06-26 Merck Sharp & Dohme Llc Preparation of fused azole derivatives as novel diacylglyceride o-acyltransferase 2 inhibitors
WO2025247370A1 (zh) * 2024-06-01 2025-12-04 中国药科大学 双环类化合物及其医药用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000502724A (ja) * 1996-09-04 2000-03-07 ファイザー・インク インダゾール誘導体、およびホスホジエステラーゼ（ｐｄｅ）タイプ▲ｉｖ▼と腫瘍壊死因子（ｔｎｆ）産生の阻害剤としてのインダゾール誘導体の使用
JP2005526007A (ja) * 2001-11-27 2005-09-02 エフ．ホフマン−ラ　ロシュ　アーゲー ベンゾチアゾール誘導体
JP2010532768A (ja) * 2007-07-12 2010-10-14 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング ピリダジノン誘導体
JP2012521429A (ja) * 2009-03-23 2012-09-13 メルク・シャープ・エンド・ドーム・コーポレイション 疼痛治療用のｐ２ｘ３受容体アンタゴニスト

Family Cites Families (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE69819311T2 (de) 1997-03-07 2004-07-29 Metabasis Therapeutics Inc., San Diego Neue benzimidazol inhibitoren der fructose-1,6-bisphosphatase
AU6691798A (en) 1997-03-07 1998-09-22 Metabasis Therapeutics, Inc. Novel indole and azaindole inhibitors of fructose-1,6-bisphosphatase
WO1998039344A1 (en) 1997-03-07 1998-09-11 Metabasis Therapeutics, Inc. Novel purine inhibitors of fructose-1,6-bisphosphatase
CZ297264B6 (cs) 1998-09-09 2006-10-11 Metabasis Therapeutics, Inc. Nové heteroaromatické inhibitory fruktóza-1,6-bisfosfatázy
CA2415742A1 (en) 2000-07-25 2002-01-31 Merck & Co., Inc. N-substituted indoles useful in the treatment of diabetes
US6852738B2 (en) 2001-01-30 2005-02-08 Merck & Co., Inc. Acyl sulfamides for treatment of obesity, diabetes and lipid disorders
WO2008011131A2 (en) 2006-07-21 2008-01-24 Takeda Pharmaceutical Company Limited Amide compounds
AR040241A1 (es) 2002-06-10 2005-03-23 Merck & Co Inc Inhibidores de la 11-beta-hidroxiesteroide deshidrogrenasa 1 para el tratamiento de la diabetes obesidad y dislipidemia
CA2495943C (en) 2002-08-29 2009-07-21 Merck & Co., Inc. Indoles having anti-diabetic activity
WO2004019869A2 (en) 2002-08-29 2004-03-11 Merck & Co., Inc. Indoles having anti-diabetic activity
CA2512879A1 (en) 2003-01-17 2004-08-12 Soumya P. Sahoo N-cyclohexylaminocarbonyl benzenesulfonamide derivatives
WO2007084413A2 (en) 2004-07-14 2007-07-26 Ptc Therapeutics, Inc. Methods for treating hepatitis c
US7868037B2 (en) 2004-07-14 2011-01-11 Ptc Therapeutics, Inc. Methods for treating hepatitis C
EA200700243A1 (ru) 2004-07-14 2007-08-31 ПиТиСи ТЕРАПЬЮТИКС, ИНК. Способы лечения гепатита с
WO2006117314A2 (en) 2005-04-30 2006-11-09 Boehringer Ingelheim International Gmbh Novel piperidin- substituted indoles and their use as ccr-3 modulators
JP2009523732A (ja) 2006-01-13 2009-06-25 ピーティーシー セラピューティクス，インコーポレーテッド Ｃ型肝炎の治療方法
US7514433B2 (en) 2006-08-03 2009-04-07 Hoffmann-La Roche Inc. 1H-indole-6-yl-piperazin-1-yl-methanone derivatives
WO2008088692A2 (en) 2007-01-12 2008-07-24 Merck & Co., Inc. Spirochromanon derivatives
EP2174343A1 (en) 2007-06-28 2010-04-14 Semiconductor Energy Laboratory Co, Ltd. Manufacturing method of semiconductor device
US20100179173A1 (en) 2007-06-28 2010-07-15 Daniel Guay Substituted fused pyrimidines as antagonists of gpr105 activity
US20110301079A1 (en) 2007-09-21 2011-12-08 Instituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Neuromedin u receptor agonists and uses thereof
WO2009058298A1 (en) 2007-10-31 2009-05-07 Merck & Co., Inc. P2x3, receptor antagonists for treatment of pain
EP2215048B1 (en) 2007-10-31 2015-10-28 Merck Sharp & Dohme Corp. P2x3 receptor antagonists for treatment of pain
CA2741666C (en) 2008-10-31 2017-04-11 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
EP2210891A1 (en) * 2009-01-26 2010-07-28 Domain Therapeutics New adenosine receptor ligands and uses thereof
JP2012520887A (ja) 2009-03-18 2012-09-10 シェーリング コーポレイション ジアシルグリセロールアシルトランスフェラーゼの阻害剤としての二環式化合物
US8946231B2 (en) 2009-03-23 2015-02-03 Merck Sharp & Dohme Corp. P2X3, receptor antagonists for treatment of pain
WO2010111058A1 (en) 2009-03-23 2010-09-30 Merck Sharp & Dohme Corp. P2x3, receptor antagonists for treatment of pain
US8927576B2 (en) 2009-04-06 2015-01-06 PTC Therpeutics, Inc. HCV inhibitor and therapeutic agent combinations
WO2014026329A1 (en) 2012-08-15 2014-02-20 Merck Sharp & Dohme Corp. N-alkylated indole and indazole compounds as rorgammat inhibitors and uses thereof
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
CA2982267C (en) 2015-05-20 2019-11-12 Eli Lilly And Company Novel dgat2 inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2000502724A (ja) * 1996-09-04 2000-03-07 ファイザー・インク インダゾール誘導体、およびホスホジエステラーゼ（ｐｄｅ）タイプ▲ｉｖ▼と腫瘍壊死因子（ｔｎｆ）産生の阻害剤としてのインダゾール誘導体の使用
JP2005526007A (ja) * 2001-11-27 2005-09-02 エフ．ホフマン−ラ　ロシュ　アーゲー ベンゾチアゾール誘導体
JP2010532768A (ja) * 2007-07-12 2010-10-14 メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング ピリダジノン誘導体
JP2012521429A (ja) * 2009-03-23 2012-09-13 メルク・シャープ・エンド・ドーム・コーポレイション 疼痛治療用のｐ２ｘ３受容体アンタゴニスト

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023545741A (ja) * 2020-10-08 2023-10-31 メルク・シャープ・アンド・ドーム・エルエルシー 新規なジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害剤としてのベンゾイミダゾロン誘導体の製造
JP7604636B2 (ja) 2020-10-08 2024-12-23 メルク・シャープ・アンド・ドーム・エルエルシー 新規なジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害剤としてのベンゾイミダゾロン誘導体の製造
JP2024501520A (ja) * 2020-12-22 2024-01-12 メルク・シャープ・アンド・ドーム・エルエルシー 新規ジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害薬としてのテトラヒドロインダゾール誘導体の調製
JP2025537517A (ja) * 2022-11-01 2025-11-18 メルク・シャープ・アンド・ドーム・エルエルシー 新規ジアシルグリセリドｏ－アシルトランスフェラーゼ２阻害薬としてのピラゾロピリジン誘導体及びトリアゾロピリジン誘導体の調製

Also Published As

Publication number Publication date
EP3541374A1 (en) 2019-09-25
AU2017360939B2 (en) 2022-03-03
AU2017360939A1 (en) 2019-05-16
KR20190078646A (ko) 2019-07-04
CN110121341A (zh) 2019-08-13
MA46856A (fr) 2019-09-25
CA3043203A1 (en) 2018-05-24
BR112019010164A2 (pt) 2019-09-17
US11104690B2 (en) 2021-08-31
RU2019117556A (ru) 2020-12-18
EP3541374A4 (en) 2020-06-10
US20190330239A1 (en) 2019-10-31
WO2018093696A1 (en) 2018-05-24
MX2019005786A (es) 2019-08-26
RU2019117556A3 (enExample) 2020-12-18
EP3541374B1 (en) 2026-08-05

Similar Documents

Publication Publication Date Title
EP3188732B1 (en) Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
US11104690B2 (en) Indazole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
US9828369B2 (en) Isoquinoline derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
EP3188730B1 (en) Tetrahydroisoquinoline derivatives useful as inhibitors of diacylglyceride o-acyltransferase 2
US11572374B2 (en) N-cyano-7-azanorbornane derivatives and uses thereof
US9056843B2 (en) Trifluoromethyl-oxadiazole derivatives and their use in the treatment of disease
US10947222B2 (en) Indole derivatives useful as inhibitors of diacylglyceride O-acyltransferase 2
US9750740B2 (en) Spirocyclic compounds as tryptophan hydroxylase inhibitors
JP6047144B2 (ja) 置換シクロプロピル化合物、このような化合物を含有する組成物および処置方法
US20150299198A1 (en) Inhibitors of the Renal Outer Medullary Potassium Channel
JP2022188014A (ja) バニン阻害剤としてのヘテロ芳香族化合物
US9745282B2 (en) Indoline compounds as aldosterone synthase inhibitors
US20130184284A1 (en) Diaminocyclohexane compounds and uses thereof
WO2025231011A1 (en) Heteroarylindole inhibitors of apol-1

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20200914

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20200914

A977 Report on retrieval

Free format text: JAPANESE INTERMEDIATE CODE: A971007

Effective date: 20210721

A131 Notification of reasons for refusal

Free format text: JAPANESE INTERMEDIATE CODE: A131

Effective date: 20210810

A601 Written request for extension of time

Free format text: JAPANESE INTERMEDIATE CODE: A601

Effective date: 20211104

A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20220208

A01 Written decision to grant a patent or to grant a registration (utility model)

Free format text: JAPANESE INTERMEDIATE CODE: A01

Effective date: 20220621

A045 Written measure of dismissal of application [lapsed due to lack of payment]

Free format text: JAPANESE INTERMEDIATE CODE: A045

Effective date: 20221025