CA2800958C - Macrocyclic compounds useful as inhibitors of histone deacetylases - Google Patents

Macrocyclic compounds useful as inhibitors of histone deacetylases Download PDF

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Publication number
CA2800958C
CA2800958C CA2800958A CA2800958A CA2800958C CA 2800958 C CA2800958 C CA 2800958C CA 2800958 A CA2800958 A CA 2800958A CA 2800958 A CA2800958 A CA 2800958A CA 2800958 C CA2800958 C CA 2800958C
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Prior art keywords
cycloalkyl
alkyl
heterocycloalkyl
independently
heteroaryl
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CA2800958A
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English (en)
French (fr)
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CA2800958A1 (en
Inventor
Xuedong Liu
Andrew J. Phillips
Dana Ungermannova
Christopher G. Nasveschuk
Gan Zhang
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University of Colorado Colorado Springs
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University of Colorado Colorado Springs
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/08—Tripeptides
    • C07K5/0821—Tripeptides with the first amino acid being heterocyclic, e.g. His, Pro, Trp
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K11/02—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof cyclic, e.g. valinomycins ; Derivatives thereof
    • 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
    • A61K31/425—Thiazoles
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/005—Enzyme inhibitors
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/15—Depsipeptides; Derivatives thereof
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K39/00—Medicinal preparations containing antigens or antibodies
    • A61K39/395—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum
    • A61K39/39533—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals
    • A61K39/3955—Antibodies; Immunoglobulins; Immune serum, e.g. antilymphocytic serum against materials from animals against proteinaceous materials, e.g. enzymes, hormones, lymphokines
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic agents
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K11/00—Depsipeptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Pulmonology (AREA)
  • Transplantation (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CA2800958A 2010-05-27 2011-05-26 Macrocyclic compounds useful as inhibitors of histone deacetylases Active CA2800958C (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34897810P 2010-05-27 2010-05-27
US61/348,978 2010-05-27
PCT/US2011/038246 WO2011150283A1 (en) 2010-05-27 2011-05-26 Macrocyclic compounds useful as inhibitors of histone deacetylases

Publications (2)

Publication Number Publication Date
CA2800958A1 CA2800958A1 (en) 2011-12-01
CA2800958C true CA2800958C (en) 2018-09-04

Family

ID=45004403

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2800958A Active CA2800958C (en) 2010-05-27 2011-05-26 Macrocyclic compounds useful as inhibitors of histone deacetylases

Country Status (17)

Country Link
US (2) US8754050B2 (enExample)
EP (1) EP2575467B1 (enExample)
JP (1) JP5931850B2 (enExample)
KR (2) KR102028850B1 (enExample)
CN (1) CN102946732B (enExample)
AU (1) AU2011258110B2 (enExample)
BR (1) BR112012030193B1 (enExample)
CA (1) CA2800958C (enExample)
DK (1) DK2575467T3 (enExample)
ES (1) ES2594500T3 (enExample)
HU (1) HUE030812T2 (enExample)
LT (1) LT2575467T (enExample)
MX (1) MX2012013507A (enExample)
PL (1) PL2575467T3 (enExample)
PT (1) PT2575467T (enExample)
RU (1) RU2565076C2 (enExample)
WO (1) WO2011150283A1 (enExample)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102391359B (zh) * 2011-11-17 2014-07-16 南京优科生物医药研究有限公司 组蛋白去乙酰化酶抑制剂及其合成方法和制药用途
CN103232474A (zh) * 2013-04-16 2013-08-07 中国药科大学 组蛋白去乙酰化酶抑制剂
CN103524598A (zh) * 2013-09-02 2014-01-22 上海冠宇生物医药科技有限公司 一类环肽类化合物、其制备方法、药物组合物及用途
CN110156874B (zh) * 2014-05-27 2023-04-18 恩库勒公司 环缩肽化合物
WO2016144814A1 (en) * 2015-03-06 2016-09-15 Colorado State University Research Foundation Synthesis and utility of new capgroup largazole analogs
US10676504B2 (en) 2015-03-06 2020-06-09 Colorado State University Research Foundation Method for preparing largazole analogs and uses thereof
CN105131082A (zh) * 2015-09-17 2015-12-09 广州康缔安生物科技有限公司 环肽类化合物及其应用
CN106674252B (zh) * 2015-11-11 2019-10-29 复旦大学 海洋天然产物环酯肽的氟代烯烃类似物、其制备方法和用途
CA3025045A1 (en) * 2016-05-20 2017-11-23 Onkure, Inc. Thioester prodrugs of macrocycles as inhibitors of histone deacetylases
CN107286223B (zh) * 2017-07-17 2019-12-20 湖北大学 一种用于检测组蛋白位点乙酰化的重组蛋白及其应用
CN111269245B (zh) * 2018-12-04 2021-08-27 杭州百新生物医药科技有限公司 一种环状氨基嘧啶衍生物及其抑制激酶的活性和用途
WO2020125513A1 (zh) * 2018-12-19 2020-06-25 凯复制药有限公司 作为cdk抑制剂的大环化合物、其制备方法及其在医药上的应用
WO2020190827A1 (en) * 2019-03-21 2020-09-24 Merck Sharp & Dohme Corp. Inhibitors of histone deacetylase useful for the treatment or prevention of hiv infection
KR102436309B1 (ko) * 2020-05-26 2022-08-25 연세대학교 산학협력단 암의 예방 또는 치료용 약학적 조성물
WO2022140144A1 (en) 2020-12-21 2022-06-30 Colorado State University Research Foundation Synthesis of structural analogs of largazole and associated compounds

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8920304D0 (en) 1989-09-08 1989-10-25 Fujisawa Pharmaceutical Co Fr901375 substance and preparation thereof
EP1548026A4 (en) * 2002-08-30 2006-03-22 Yamanouchi Pharma Co Ltd NEW DEPSIPEPTID CONNECTION
AU2003286686B2 (en) * 2002-11-12 2009-07-16 Alcon, Inc. Histone deacetylase inhibitors for treating degenerative diseases of the eye
US20060128660A1 (en) * 2004-12-10 2006-06-15 Wisconsin Alumni Research Foundation FK228 analogs and methods of making and using the same
JP5178731B2 (ja) * 2006-11-22 2013-04-10 カルス セラピューティクス リミテッド デプシペプチドおよびその治療的使用
GB0623388D0 (en) * 2006-11-23 2007-01-03 Univ Southampton Chemical compounds
GB0715750D0 (en) * 2007-08-13 2007-09-19 Karus Therapeutics Ltd Chemical compounds
AU2009234398B2 (en) * 2008-04-11 2015-01-22 University Of Florida Research Foundation, Inc. Macrocyclic compounds and methods of treatment
WO2010009334A1 (en) * 2008-07-17 2010-01-21 Colorado State University Research Foundation Method for preparing largazole analogs and uses thereof
CN102391359B (zh) * 2011-11-17 2014-07-16 南京优科生物医药研究有限公司 组蛋白去乙酰化酶抑制剂及其合成方法和制药用途

Also Published As

Publication number Publication date
WO2011150283A1 (en) 2011-12-01
CA2800958A1 (en) 2011-12-01
RU2012157293A (ru) 2014-07-10
EP2575467A1 (en) 2013-04-10
HK1181613A1 (en) 2013-11-15
MX2012013507A (es) 2013-03-12
ES2594500T3 (es) 2016-12-20
US20150010541A1 (en) 2015-01-08
EP2575467A4 (en) 2014-10-15
AU2011258110B2 (en) 2015-07-16
KR20180081153A (ko) 2018-07-13
CN102946732A (zh) 2013-02-27
US9422340B2 (en) 2016-08-23
JP5931850B2 (ja) 2016-06-08
JP2013528182A (ja) 2013-07-08
LT2575467T (lt) 2017-01-10
CN102946732B (zh) 2014-11-26
US20130203681A1 (en) 2013-08-08
US8754050B2 (en) 2014-06-17
RU2565076C2 (ru) 2015-10-20
PT2575467T (pt) 2016-10-14
HUE030812T2 (en) 2017-05-29
BR112012030193B1 (pt) 2020-11-17
PL2575467T3 (pl) 2017-10-31
AU2011258110A1 (en) 2013-01-10
KR20130123301A (ko) 2013-11-12
EP2575467B1 (en) 2016-07-06
BR112012030193A2 (pt) 2015-09-29
KR102028850B1 (ko) 2019-10-04
DK2575467T3 (en) 2016-09-26

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Publication Publication Date Title
CA2800958C (en) Macrocyclic compounds useful as inhibitors of histone deacetylases
US20220017538A1 (en) Thioester prodrugs of macrocycles as inhibitors of histone deacetylases
Class et al. Patent application title: Macrocyclic Compounds Useful as Inhibitors of Histone Deacetylases Inventors: Xuedong Liu (Niwot, CO, US) Andrew J. Phillips (Guilford, CT, US) Dana Ungermannova (Houston, TX, US) Christopher G. Nasveschuk (Stoneham, MA, US) Christopher G. Nasveschuk (Stoneham, MA, US) Gan Zhang (Niwot, CO, US) Assignees: THE REGENTS OF THE UNIVERSITY OF COLORADO
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