CN105008329B - 作为fasn抑制剂的哌嗪衍生物 - Google Patents

作为fasn抑制剂的哌嗪衍生物 Download PDF

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Publication number
CN105008329B
CN105008329B CN201480016107.3A CN201480016107A CN105008329B CN 105008329 B CN105008329 B CN 105008329B CN 201480016107 A CN201480016107 A CN 201480016107A CN 105008329 B CN105008329 B CN 105008329B
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China
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bases
pharmaceutically acceptable
atom
compound
acceptable salt
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Expired - Fee Related
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CN201480016107.3A
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English (en)
Chinese (zh)
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CN105008329A (zh
Inventor
W.施特勒
C.察克拉基迪斯
M.弗里泽-哈米姆
B.罗伊特纳
D.维恩克
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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
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic 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
    • 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
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0014—Skin, i.e. galenical aspects of topical compositions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/02—Suppositories; Bougies; Bases therefor; Ovules
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs 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
    • 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
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/02—Heterocyclic 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
    • C07D217/08—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic 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
    • C07D217/24—Oxygen atoms
    • Y—GENERAL 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
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against 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)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Hematology (AREA)
  • Rheumatology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (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)
CN201480016107.3A 2013-03-21 2014-02-24 作为fasn抑制剂的哌嗪衍生物 Expired - Fee Related CN105008329B (zh)

Applications Claiming Priority (3)

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

Publications (2)

Publication Number Publication Date
CN105008329A CN105008329A (zh) 2015-10-28
CN105008329B true CN105008329B (zh) 2018-01-05

Family

ID=47912880

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201480016107.3A Expired - Fee Related CN105008329B (zh) 2013-03-21 2014-02-24 作为fasn抑制剂的哌嗪衍生物

Country Status (10)

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

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MY191366A (en) 2013-03-13 2022-06-20 Forma Therapeutics Inc Novel compounds and compositions for inhibition of fasn
MX379846B (es) 2015-06-18 2025-03-11 89Bio Ltd Derivados de 4-bencil y 4-benzoil piperidina sustituidos.
AU2016280255A1 (en) 2015-06-18 2018-02-08 Cephalon, Inc. 1, 4-substituted piperidine derivatives
PL3458448T3 (pl) 2016-04-25 2021-12-06 Forma Therapeutics, Inc. Inhibitory fasn do zastosowania w leczeniu niealkoholowego stłuszczeniowego zapalenia wątroby
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

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011048018A1 (en) * 2009-10-19 2011-04-28 Boehringer Ingelheim International Gmbh Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use

Family Cites Families (6)

* 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
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
MY191366A (en) * 2013-03-13 2022-06-20 Forma Therapeutics Inc Novel compounds and compositions for inhibition of fasn

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2011048018A1 (en) * 2009-10-19 2011-04-28 Boehringer Ingelheim International Gmbh Cyclopentanecarboxamide derivatives, medicaments containing such compounds and their use

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
DATABASE REGISTRY;CAS;《CAS》;20120808 *
Synthesis and cytotoxicity of 2-phenylquinazolin-4(3H)-one derivatives;Hee-Kyung Rhee等;《European Journal of Medicinal Chemistry》;20110531;第46卷(第9期);3900-3908 *

Also Published As

Publication number Publication date
EP2976328A1 (en) 2016-01-27
IL241513A0 (en) 2015-11-30
ES2634875T3 (es) 2017-09-29
US20160280655A1 (en) 2016-09-29
EP2976328B1 (en) 2017-05-03
JP2016515550A (ja) 2016-05-30
AR095707A1 (es) 2015-11-04
JP2018188452A (ja) 2018-11-29
AU2014234721A1 (en) 2015-11-05
WO2014146747A1 (en) 2014-09-25
EP2976328B2 (en) 2019-07-03
US9809552B2 (en) 2017-11-07
CA2907657A1 (en) 2014-09-25
JP6412553B2 (ja) 2018-10-24
CN105008329A (zh) 2015-10-28

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