BR112017009671A2 - inibidores de ezh2 e usos destes - Google Patents

inibidores de ezh2 e usos destes

Info

Publication number
BR112017009671A2
BR112017009671A2 BR112017009671A BR112017009671A BR112017009671A2 BR 112017009671 A2 BR112017009671 A2 BR 112017009671A2 BR 112017009671 A BR112017009671 A BR 112017009671A BR 112017009671 A BR112017009671 A BR 112017009671A BR 112017009671 A2 BR112017009671 A2 BR 112017009671A2
Authority
BR
Brazil
Prior art keywords
ezh2
inhibitors
ezh1
homologous
methods
Prior art date
Application number
BR112017009671A
Other languages
English (en)
Inventor
E Bradner James
Qi Jun
Kin Wong Kwok
Original Assignee
Dana Farber Cancer Inst Inc
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
Application filed by Dana Farber Cancer Inst Inc filed Critical Dana Farber Cancer Inst Inc
Publication of BR112017009671A2 publication Critical patent/BR112017009671A2/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • G—PHYSICS
    • G01—MEASURING; TESTING
    • G01N—INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00—Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48—Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/5005—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells
    • G01N33/5008—Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving human or animal cells for testing or evaluating the effect of chemical or biological compounds, e.g. drugs, cosmetics

Abstract

a presente descrição proporciona compostos de qualquer uma das fórmulas (i) e (ii). os compostos aqui descritos são inibidores de histonas metiltransferases (e.g., potenciador de zeste homólogo 1 (ezh1) e intensificador de zeste homólogo 2 (ezh2)) são úteis no tratamento e / ou prevenção de uma ampla gama de doenças (por exemplo, doenças proliferativas). a presente invenção também fornece composições farmacêuticas, kits, métodos, e usos incluindo ou usando um composto descrito aqui. ademais, também é fornecido são métodos de identificação de inibidores de ezh1 e/ou ezh2. (i) (ii)
BR112017009671A 2014-11-06 2015-11-06 inibidores de ezh2 e usos destes BR112017009671A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462076410P 2014-11-06 2014-11-06
PCT/US2015/059622 WO2016073956A1 (en) 2014-11-06 2015-11-06 Ezh2 inhibitors and uses thereof

Publications (1)

Publication Number Publication Date
BR112017009671A2 true BR112017009671A2 (pt) 2017-12-26

Family

ID=55909933

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017009671A BR112017009671A2 (pt) 2014-11-06 2015-11-06 inibidores de ezh2 e usos destes

Country Status (8)

Country Link
US (1) US11236082B2 (pt)
EP (2) EP3214935A4 (pt)
KR (1) KR20170081213A (pt)
CN (1) CN107105651A (pt)
AU (1) AU2015342774C1 (pt)
BR (1) BR112017009671A2 (pt)
CA (1) CA2964629A1 (pt)
WO (1) WO2016073956A1 (pt)

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US11541051B2 (en) 2016-12-08 2023-01-03 Icahn School Of Medicine At Mount Sinai Compositions and methods for treating CDK4/6-mediated cancer
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CN110229151B (zh) * 2018-03-06 2021-09-10 上海海和药物研究开发股份有限公司 吲嗪类化合物、其制备方法及用途
CN112154146A (zh) 2018-03-06 2020-12-29 西奈山伊坎医学院 丝氨酸苏氨酸激酶(akt)降解/破坏化合物和使用方法
CA3104209A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
CN109966479A (zh) * 2019-02-26 2019-07-05 上海长征医院 Ezh2在制备预防或治疗多囊肾病药物中的应用
EP3976044A1 (en) * 2019-06-03 2022-04-06 Icahn School of Medicine at Mount Sinai Compounds and methods for inhibiting cancers via rest inhibition
CN112341390B (zh) * 2019-08-07 2022-08-23 四川大学 用于制备靶向组蛋白甲基转移酶ezh2共价抑制剂的化合物及其制备方法和用途
EP3797777A1 (en) 2019-09-30 2021-03-31 Eberhard Karls Universität Tübingen Medizinische Fakultät Agent for the treatment of psoriasis
CN111303133A (zh) * 2020-03-25 2020-06-19 清华大学 降解ezh2蛋白的小分子化合物
WO2022042527A1 (zh) * 2020-08-24 2022-03-03 北京大学 治疗内耳及肠道上皮组织损伤相关疾病的小分子药物
CN112715484B (zh) * 2020-12-29 2022-04-22 四川省人民医院 构建视网膜色素变性疾病模型的方法、应用以及繁育方法
CN114028397A (zh) * 2021-02-01 2022-02-11 徐州医科大学 Gsk126作为ezh2抑制剂在制备预防和/或治疗缺血性脑卒中药物中的应用
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TW202400140A (zh) 2022-04-27 2024-01-01 日商第一三共股份有限公司 抗體-藥物結合物與ezh1及/或ezh2抑制劑之組合

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Also Published As

Publication number Publication date
EP3214935A4 (en) 2018-08-29
WO2016073956A1 (en) 2016-05-12
EP3214935A1 (en) 2017-09-13
KR20170081213A (ko) 2017-07-11
CN107105651A (zh) 2017-08-29
AU2015342774C1 (en) 2021-08-05
AU2015342774A1 (en) 2017-04-27
EP3885343A1 (en) 2021-09-29
CN113444086A (zh) 2021-09-28
US11236082B2 (en) 2022-02-01
AU2015342774B2 (en) 2020-01-30
US20180297993A1 (en) 2018-10-18
CA2964629A1 (en) 2016-05-12

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B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]