CA2907657A1 - Piperazine derivatives as fasn inhibitors - Google Patents

Piperazine derivatives as fasn inhibitors Download PDF

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Publication number
CA2907657A1
CA2907657A1 CA2907657A CA2907657A CA2907657A1 CA 2907657 A1 CA2907657 A1 CA 2907657A1 CA 2907657 A CA2907657 A CA 2907657A CA 2907657 A CA2907657 A CA 2907657A CA 2907657 A1 CA2907657 A1 CA 2907657A1
Authority
CA
Canada
Prior art keywords
denotes
atoms
formula
pharmaceutically acceptable
stereoisomers
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.)
Abandoned
Application number
CA2907657A
Other languages
English (en)
French (fr)
Inventor
Wolfgang Staehle
Christos Tsaklakidis
Manja FRIESE-HAMIM
Birgitta Leuthner
Dirk Wienke
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 Patent GmbH
Original Assignee
Merck Patent GmbH
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=47912880&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CA2907657(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of CA2907657A1 publication Critical patent/CA2907657A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Dermatology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Oncology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Hematology (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)
CA2907657A 2013-03-21 2014-02-24 Piperazine derivatives as fasn inhibitors Abandoned CA2907657A1 (en)

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

Publications (1)

Publication Number Publication Date
CA2907657A1 true CA2907657A1 (en) 2014-09-25

Family

ID=47912880

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2907657A Abandoned CA2907657A1 (en) 2013-03-21 2014-02-24 Piperazine derivatives as fasn inhibitors

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 (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN112521369A (zh) 2013-03-13 2021-03-19 福马治疗股份有限公司 用于抑制fasn的化合物及组合物
CN107847765B (zh) 2015-06-18 2021-05-04 89生物有限公司 1,4-取代的哌啶衍生物
EP3310773B1 (en) 2015-06-18 2020-12-02 89Bio Ltd. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
DK3458448T3 (da) 2016-04-25 2021-08-23 Forma Therapeutics Inc Fasn-inhibitorer til anvendelse til behandling af non-alkoholisk steatohepatitis
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)
WO2020092395A1 (en) 2018-10-29 2020-05-07 Forma Therapeutics, Inc. SOLID FORMS OF (4-(2-FLUORO-4-(1-METHYL-1 H-BENZO[d]IMIDAZOL-5-YL)BENZOYL) PIPERAZIN-1-YL)(1-HYDROXYCYCLOPROPYL)METHANONE
CN117658948A (zh) * 2023-12-14 2024-03-08 辽宁省人民医院 Fasn小分子抑制剂的筛选及其应用

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
EP2247600A4 (en) 2008-02-06 2011-09-14 Biomarin Pharm Inc INHIBITORS BASED ON BENZOXAZOLE-CARBOXAMIDE COMPOUNDS OF POLY (ADP-RIBOSE) POLYMERASE (PARP) ACTIVITY
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
CN112521369A (zh) 2013-03-13 2021-03-19 福马治疗股份有限公司 用于抑制fasn的化合物及组合物

Also Published As

Publication number Publication date
JP6412553B2 (ja) 2018-10-24
ES2634875T3 (es) 2017-09-29
US20160280655A1 (en) 2016-09-29
EP2976328A1 (en) 2016-01-27
AU2014234721A1 (en) 2015-11-05
EP2976328B1 (en) 2017-05-03
CN105008329A (zh) 2015-10-28
US9809552B2 (en) 2017-11-07
AR095707A1 (es) 2015-11-04
CN105008329B (zh) 2018-01-05
WO2014146747A1 (en) 2014-09-25
JP2018188452A (ja) 2018-11-29
IL241513A0 (en) 2015-11-30
EP2976328B2 (en) 2019-07-03
JP2016515550A (ja) 2016-05-30

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Legal Events

Date Code Title Description
FZDE Discontinued

Effective date: 20180226