JP6412553B2 - Fasn阻害剤としてのピペラジン誘導体 - Google Patents

Fasn阻害剤としてのピペラジン誘導体 Download PDF

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Publication number
JP6412553B2
JP6412553B2 JP2016504506A JP2016504506A JP6412553B2 JP 6412553 B2 JP6412553 B2 JP 6412553B2 JP 2016504506 A JP2016504506 A JP 2016504506A JP 2016504506 A JP2016504506 A JP 2016504506A JP 6412553 B2 JP6412553 B2 JP 6412553B2
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atoms
formula
pharmaceutically acceptable
tautomer
stereoisomer
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Japanese (ja)
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JP2016515550A (ja
JP2016515550A5 (OSRAM
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
フリーゼ−ハミム,マンヤ
ロイトナー,ブリギッタ
ヴィエンケ,ディルク
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Merck Patent GmbH
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Merck Patent GmbH
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • 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
    • A61K31/496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0014Skin, i.e. galenical aspects of topical compositions
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0019Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/02Suppositories; Bougies; Bases therefor; Ovules
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines
    • C07D217/08Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with only hydrogen atoms or radicals containing only carbon and hydrogen atoms, directly attached to carbon atoms of the nitrogen-containing ring; Alkylene-bis-isoquinolines with a hetero atom directly attached to the ring nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D217/00Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
    • C07D217/24Oxygen atoms
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02ATECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Dermatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Psychiatry (AREA)
  • Oncology (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
JP2016504506A 2013-03-21 2014-02-24 Fasn阻害剤としてのピペラジン誘導体 Expired - Fee Related JP6412553B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP13001462 2013-03-21
EP13001462.4 2013-03-21
PCT/EP2014/000478 WO2014146747A1 (en) 2013-03-21 2014-02-24 Piperazine derivatives as fasn inhibitors

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2018129665A Division JP2018188452A (ja) 2013-03-21 2018-07-09 Fasn阻害剤としてのピペラジン誘導体

Publications (3)

Publication Number Publication Date
JP2016515550A JP2016515550A (ja) 2016-05-30
JP2016515550A5 JP2016515550A5 (OSRAM) 2017-03-30
JP6412553B2 true JP6412553B2 (ja) 2018-10-24

Family

ID=47912880

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2016504506A Expired - Fee Related JP6412553B2 (ja) 2013-03-21 2014-02-24 Fasn阻害剤としてのピペラジン誘導体
JP2018129665A Pending JP2018188452A (ja) 2013-03-21 2018-07-09 Fasn阻害剤としてのピペラジン誘導体

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2018129665A Pending JP2018188452A (ja) 2013-03-21 2018-07-09 Fasn阻害剤としてのピペラジン誘導体

Country Status (10)

Country Link
US (1) US9809552B2 (OSRAM)
EP (1) EP2976328B2 (OSRAM)
JP (2) JP6412553B2 (OSRAM)
CN (1) CN105008329B (OSRAM)
AR (1) AR095707A1 (OSRAM)
AU (1) AU2014234721A1 (OSRAM)
CA (1) CA2907657A1 (OSRAM)
ES (1) ES2634875T3 (OSRAM)
IL (1) IL241513A0 (OSRAM)
WO (1) WO2014146747A1 (OSRAM)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SG11201507486SA (en) 2013-03-13 2015-10-29 Forma Therapeutics Inc Novel compounds and compositions for inhibition of fasn
US10919875B2 (en) 2015-06-18 2021-02-16 89Bio Ltd Substituted 4-benzyl and 4-benzoyl piperidine derivatives
ES2821049T3 (es) 2015-06-18 2021-04-23 89Bio Ltd Derivados de piperidina 1,4 sustituidos
ES2886935T3 (es) 2016-04-25 2021-12-21 Forma Therapeutics Inc Inhibidores de FASN para su uso en el tratamiento de esteatohepatitis no alcohólica
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)
CN113382633A (zh) 2018-10-29 2021-09-10 福马治疗股份有限公司 (4-(2-氟-4-(1-甲基-1H-苯并[d]咪唑-5-基)苯甲酰基)哌嗪-1-基)(1-羟基环丙基)甲酮的固体形式

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19743435A1 (de) 1997-10-01 1999-04-08 Merck Patent Gmbh Benzamidinderivate
DE102007007751A1 (de) 2007-02-16 2008-08-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue substituierte Arylsulfonylglycine, deren Herstellung und deren Verwendung als Arzneimittel
CN101998959B (zh) * 2008-02-06 2013-08-28 生物马林药物股份有限公司 聚(adp-核糖)聚合酶(parp)的苯并噁唑甲酰胺抑制剂
JP5744886B2 (ja) * 2009-10-19 2015-07-08 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング シクロペンタンカルボキサミド誘導体、このような化合物を含む薬物及びそれらの使用
KR101261702B1 (ko) * 2011-01-07 2013-05-06 이화여자대학교 산학협력단 신규한 2-페닐퀴나졸린-4(3h)-온 유도체, 그 제조방법 및 그 약학적 조성물
CN102627610B (zh) * 2012-04-11 2014-06-25 江苏先声药物研究有限公司 一类苯并咪唑类衍生物及其应用
SG11201507486SA (en) * 2013-03-13 2015-10-29 Forma Therapeutics Inc Novel compounds and compositions for inhibition of fasn

Also Published As

Publication number Publication date
CA2907657A1 (en) 2014-09-25
JP2016515550A (ja) 2016-05-30
WO2014146747A1 (en) 2014-09-25
EP2976328B2 (en) 2019-07-03
CN105008329A (zh) 2015-10-28
EP2976328B1 (en) 2017-05-03
CN105008329B (zh) 2018-01-05
IL241513A0 (en) 2015-11-30
AR095707A1 (es) 2015-11-04
JP2018188452A (ja) 2018-11-29
AU2014234721A1 (en) 2015-11-05
ES2634875T3 (es) 2017-09-29
US20160280655A1 (en) 2016-09-29
EP2976328A1 (en) 2016-01-27
US9809552B2 (en) 2017-11-07

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