BR112012030193B1 - Com postos m acrocíclico s inibidores de histona desacetilases, com posições farmacêuticas e seus usos - Google Patents

Com postos m acrocíclico s inibidores de histona desacetilases, com posições farmacêuticas e seus usos Download PDF

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Publication number
BR112012030193B1
BR112012030193B1 BR112012030193-4A BR112012030193A BR112012030193B1 BR 112012030193 B1 BR112012030193 B1 BR 112012030193B1 BR 112012030193 A BR112012030193 A BR 112012030193A BR 112012030193 B1 BR112012030193 B1 BR 112012030193B1
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BR
Brazil
Prior art keywords
alkyl
compound
compound according
largazole
pharmaceutically acceptable
Prior art date
Application number
BR112012030193-4A
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English (en)
Portuguese (pt)
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BR112012030193A2 (pt
Inventor
Xuedong Liu
Andrew J. Phillips
Dana Ungermannova
Christopher G. Nasveschuk
Gan Zhang
Original Assignee
The Regents Of The University Of Colorado, A Body Corporate
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Application filed by The Regents Of The University Of Colorado, A Body Corporate filed Critical The Regents Of The University Of Colorado, A Body Corporate
Publication of BR112012030193A2 publication Critical patent/BR112012030193A2/pt
Publication of BR112012030193B1 publication Critical patent/BR112012030193B1/pt

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    • 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
    • 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
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Mycology (AREA)
  • Microbiology (AREA)
  • Endocrinology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pulmonology (AREA)
  • Rheumatology (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
BR112012030193-4A 2010-05-27 2011-05-26 Com postos m acrocíclico s inibidores de histona desacetilases, com posições farmacêuticas e seus usos BR112012030193B1 (pt)

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
BR112012030193A2 BR112012030193A2 (pt) 2015-09-29
BR112012030193B1 true BR112012030193B1 (pt) 2020-11-17

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BR112012030193-4A BR112012030193B1 (pt) 2010-05-27 2011-05-26 Com postos m acrocíclico s inibidores de histona desacetilases, com posições farmacêuticas e seus usos

Country Status (17)

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

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
CN106800589B (zh) * 2013-09-02 2021-01-12 李铁旦 一类环肽类化合物、其制备方法、药物组合物及用途
PL3578179T3 (pl) * 2014-05-27 2021-06-28 Onkure, Inc. Sposób wytwarzania cyklicznych depsipeptydów
US10676504B2 (en) 2015-03-06 2020-06-09 Colorado State University Research Foundation Method for preparing largazole analogs and uses thereof
US10538534B2 (en) 2015-03-06 2020-01-21 Colorado State University Research Foundation Synthesis and utility of new capgroup largazole analogs
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
JP6691958B2 (ja) * 2016-05-20 2020-05-13 オンキュアー，インコーポレイテッド ヒストンデアセチラーゼの阻害剤としての大環状分子のチオエステルプロドラッグ
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
KR20210105375A (ko) * 2018-12-19 2021-08-26 키테라 (쑤저우) 파마슈티컬스 컴퍼니 리미티드 Cdk 저해제로서의 대환식 화합물, 이의 제조 방법, 및 의약에서의 이의 용도
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
US12227522B2 (en) 2020-12-21 2025-02-18 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
US7098186B2 (en) * 2002-08-30 2006-08-29 Astellas Pharma Inc Depsipeptide compound
CN1711086A (zh) * 2002-11-12 2005-12-21 爱尔康公司 用于治疗眼的退化性疾病的组蛋白脱乙酰酶抑制剂
US20060128660A1 (en) * 2004-12-10 2006-06-15 Wisconsin Alumni Research Foundation FK228 analogs and methods of making and using the same
CA2670223A1 (en) * 2006-11-22 2008-05-29 Karus Therapeutics Limited Depsipeptides and their therapeutic use
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
JP5719764B2 (ja) * 2008-04-11 2015-05-20 ユニバーシティ オブ フロリダ リサーチ ファウンデーション，インコーポレイテッド 大環状化合物および治療方法
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
HK1181613A1 (en) 2013-11-15
EP2575467A1 (en) 2013-04-10
ES2594500T3 (es) 2016-12-20
HUE030812T2 (en) 2017-05-29
LT2575467T (lt) 2017-01-10
CN102946732A (zh) 2013-02-27
US20130203681A1 (en) 2013-08-08
RU2012157293A (ru) 2014-07-10
US20150010541A1 (en) 2015-01-08
WO2011150283A1 (en) 2011-12-01
AU2011258110A1 (en) 2013-01-10
PL2575467T3 (pl) 2017-10-31
MX2012013507A (es) 2013-03-12
BR112012030193A2 (pt) 2015-09-29
EP2575467B1 (en) 2016-07-06
KR20130123301A (ko) 2013-11-12
RU2565076C2 (ru) 2015-10-20
US9422340B2 (en) 2016-08-23
JP2013528182A (ja) 2013-07-08
CN102946732B (zh) 2014-11-26
JP5931850B2 (ja) 2016-06-08
PT2575467T (pt) 2016-10-14
US8754050B2 (en) 2014-06-17
DK2575467T3 (en) 2016-09-26
KR20180081153A (ko) 2018-07-13
AU2011258110B2 (en) 2015-07-16
KR102028850B1 (ko) 2019-10-04
EP2575467A4 (en) 2014-10-15
CA2800958C (en) 2018-09-04
CA2800958A1 (en) 2011-12-01

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US20090264345A1 (en) Macrocyclic peptides and methods for making and using them
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
HK1181613B (en) Macrocyclic compounds useful as inhibitors of histone deacetylases
EP4433495A1 (en) Peptides and uses thereof

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]

Free format text: NOTIFICACAO DE ANUENCIA RELACIONADA COM O ART 229 DA LPI

B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B07A Application suspended after technical examination (opinion) [chapter 7.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 26/05/2011, OBSERVADAS AS CONDICOES LEGAIS.