JP6259460B2 - 脂肪酸シンターゼ阻害剤として使用するためのヒドロピロロピロール誘導体 - Google Patents

脂肪酸シンターゼ阻害剤として使用するためのヒドロピロロピロール誘導体 Download PDF

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Publication number
JP6259460B2
JP6259460B2 JP2015532318A JP2015532318A JP6259460B2 JP 6259460 B2 JP6259460 B2 JP 6259460B2 JP 2015532318 A JP2015532318 A JP 2015532318A JP 2015532318 A JP2015532318 A JP 2015532318A JP 6259460 B2 JP6259460 B2 JP 6259460B2
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formula
atoms
pharmaceutically acceptable
compound
tautomer
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JP2015532318A
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Japanese (ja)
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JP2015529229A5 (https=
JP2015529229A (ja
Inventor
シュテーレ，ヴォルフガング
ツァクラキディス，クリストス
ルースナー，ブリジッタ
ヴイエンケ，ディルク
ツァウデルナ，フランク
ヴェゲナー，アンスガー
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Merck Patent GmbH
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Merck Patent GmbH
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    • 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
    • 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
    • A61K31/407—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 other heterocyclic ring systems, e.g. ketorolac, physostigmine
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015532318A 2012-09-24 2013-08-30 脂肪酸シンターゼ阻害剤として使用するためのヒドロピロロピロール誘導体 Expired - Fee Related JP6259460B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP12006668 2012-09-24
EP12006668.3 2012-09-24
PCT/EP2013/002606 WO2014044356A1 (en) 2012-09-24 2013-08-30 Hydropyrrolopyrrole derivatives for use as fatty acid synthase inhibitors

Publications (3)

Publication Number Publication Date
JP2015529229A JP2015529229A (ja) 2015-10-05
JP2015529229A5 JP2015529229A5 (https=) 2016-10-20
JP6259460B2 true JP6259460B2 (ja) 2018-01-10

Family

ID=47088611

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2015532318A Expired - Fee Related JP6259460B2 (ja) 2012-09-24 2013-08-30 脂肪酸シンターゼ阻害剤として使用するためのヒドロピロロピロール誘導体

Country Status (16)

Country Link
US (1) US9416133B2 (https=)
EP (1) EP2897958B1 (https=)
JP (1) JP6259460B2 (https=)
KR (1) KR20150061644A (https=)
CN (1) CN104640866B (https=)
AR (1) AR092211A1 (https=)
AU (1) AU2013320636A1 (https=)
BR (1) BR112015005862A2 (https=)
CA (1) CA2885673A1 (https=)
ES (1) ES2608040T3 (https=)
HK (1) HK1210470A1 (https=)
IL (1) IL237839A0 (https=)
MX (1) MX2015003542A (https=)
RU (1) RU2015115278A (https=)
SG (1) SG11201502014XA (https=)
WO (1) WO2014044356A1 (https=)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2013132253A1 (en) 2012-03-07 2013-09-12 Institute Of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
AR095079A1 (es) 2013-03-12 2015-09-16 Hoffmann La Roche Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo
ES2753386T3 (es) 2013-03-13 2020-04-08 Forma Therapeutics Inc Derivados de 2-hidroxi-1-{4-[(4-fenil)fenil]carbonil}piperazin-1-il}etano-1-ona y compuestos relacionados como inhibidores de sintasa de ácido graso (FASN) para el tratamiento del cáncer
EP3044221B1 (en) 2013-09-11 2018-02-21 Institute of Cancer Research: Royal Cancer Hospital (The) 3-aryl-5-substituted-isoquinolin-1-one compounds and their therapeutic use
DK3074400T3 (en) 2013-11-26 2018-01-15 Hoffmann La Roche Octahydro-cyclobuta [1,2-c; 3,4-c '] dipyrrole derivatives as autotaxin inhibitors
CA2937616A1 (en) 2014-03-26 2015-10-01 F. Hoffmann-La Roche Ag Bicyclic compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors
KR20180026459A (ko) 2015-06-18 2018-03-12 세파론, 인코포레이티드 1,4-치환된 피페리딘 유도체
WO2016205590A1 (en) 2015-06-18 2016-12-22 Cephalon, Inc. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
CA2992889A1 (en) 2015-09-04 2017-03-09 F. Hoffmann-La Roche Ag Phenoxymethyl derivatives
WO2017050732A1 (en) 2015-09-24 2017-03-30 F. Hoffmann-La Roche Ag Bicyclic compounds as atx inhibitors
JP6876685B2 (ja) 2015-09-24 2021-05-26 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ａｔｘ阻害剤としての二環式化合物
BR112017026682A2 (pt) * 2015-09-24 2018-08-14 Hoffmann La Roche novos compostos bicíclicos como inibidores de dupla ação de atx/ca
WO2017156350A1 (en) 2016-03-09 2017-09-14 K-Gen, Inc. Methods of cancer treatment
RU2019132254A (ru) 2017-03-16 2021-04-16 Ф. Хоффманн-Ля Рош Аг Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca
JP7090099B2 (ja) 2017-03-16 2022-06-23 エフ．ホフマン－ラ ロシュ アーゲー Ａｔｘインヒビターとしての新規二環式化合物
LT3483164T (lt) 2017-03-20 2020-05-11 Forma Therapeutics, Inc. Pirolpirolo kompozicijos kaip piruvato kinazės (pkr) aktyvatoriai
EP3852791B1 (en) 2018-09-19 2024-07-03 Novo Nordisk Health Care AG Activating pyruvate kinase r
EP3853206B1 (en) 2018-09-19 2024-04-10 Novo Nordisk Health Care AG Treating sickle cell disease with a pyruvate kinase r activating compound
TWI767148B (zh) 2018-10-10 2022-06-11 美商弗瑪治療公司 抑制脂肪酸合成酶(fasn)
US10793554B2 (en) 2018-10-29 2020-10-06 Forma Therapeutics, Inc. Solid forms of 4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone
HRP20251148T1 (hr) 2019-09-19 2025-11-21 Novo Nordisk Health Care Ag Pripravci koji aktiviraju piruvat-kinazu r (pkr)
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
RU2008136756A (ru) * 2006-02-15 2010-03-20 Ф.Хоффманн-Ля Рош Аг (Ch) Гетеробициклические противовирусные соединения
EP2010172B1 (en) * 2006-04-07 2012-08-29 Janssen Pharmaceutica N.V. Indoles and benzoimidazoles as modulators of the histamine h4 receptor
WO2008059214A1 (en) * 2006-11-13 2008-05-22 Astrazeneca Ab Bisamlde derivatives and use thereof as fatty acid synthase inhibitors
CA2679735A1 (en) * 2007-03-01 2008-09-12 Janssen Pharmaceutica N.V. Tetrahydroisoquinoline compounds as modulators of the histamine h3 receptor
EP2170064A4 (en) * 2007-06-22 2010-08-04 Merck Sharp & Dohme 6,5-pyrrolopiperidine tachykinin receptor antagonists
WO2011048018A1 (en) 2009-10-19 2011-04-28 Boehringer Ingelheim International Gmbh Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use
WO2011056635A1 (en) 2009-10-27 2011-05-12 Glaxosmithkline Llc Benzimidazoles as fatty acid synthase inhibitors
US8633183B2 (en) * 2010-01-26 2014-01-21 Boehringer Ingelheim International Gmbh 5-alkynyl-pyrimidines
WO2012064642A1 (en) 2010-11-08 2012-05-18 Glaxosmithkline Llc Fatty acid synthase inhibitors
EP3190108B1 (en) * 2011-03-08 2021-05-19 Sagimet Biosciences Inc. Heterocyclic modulators of lipid synthesis
WO2013028445A1 (en) 2011-08-19 2013-02-28 Glaxosmithkline Llc Fatty acid synthase inhibitors

Also Published As

Publication number Publication date
US9416133B2 (en) 2016-08-16
CN104640866B (zh) 2017-06-06
HK1210470A1 (en) 2016-04-22
KR20150061644A (ko) 2015-06-04
WO2014044356A1 (en) 2014-03-27
CN104640866A (zh) 2015-05-20
MX2015003542A (es) 2015-07-17
BR112015005862A2 (pt) 2017-07-04
AR092211A1 (es) 2015-04-08
SG11201502014XA (en) 2015-04-29
ES2608040T3 (es) 2017-04-05
RU2015115278A (ru) 2016-11-20
EP2897958A1 (en) 2015-07-29
EP2897958B1 (en) 2016-09-21
CA2885673A1 (en) 2014-03-27
US20150252046A1 (en) 2015-09-10
AU2013320636A1 (en) 2015-05-07
IL237839A0 (en) 2015-05-31
JP2015529229A (ja) 2015-10-05

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