JP6005753B2 - 治療の方法 - Google Patents

治療の方法 Download PDF

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Publication number
JP6005753B2
JP6005753B2 JP2014540115A JP2014540115A JP6005753B2 JP 6005753 B2 JP6005753 B2 JP 6005753B2 JP 2014540115 A JP2014540115 A JP 2014540115A JP 2014540115 A JP2014540115 A JP 2014540115A JP 6005753 B2 JP6005753 B2 JP 6005753B2
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Japan
Prior art keywords
methyl
indole
oxo
pyridinyl
carboxamide
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Expired - Fee Related
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JP2014540115A
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Japanese (ja)
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JP2015501784A5 (enExample
JP2015501784A (ja
Inventor
アンナ、ケイ.バシル
ソーレン、ベインケ
ラビンダー、クマール、プリンジャ
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GlaxoSmithKline Intellectual Property No 2 Ltd
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GlaxoSmithKline Intellectual Property No 2 Ltd
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    • 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
    • C07D401/02—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 two hetero rings
    • C07D401/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • 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
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C12N9/00—Enzymes; Proenzymes; Compositions thereof; Processes for preparing, activating, inhibiting, separating or purifying enzymes
    • C12N9/10—Transferases (2.)
    • C12N9/1003—Transferases (2.) transferring one-carbon groups (2.1)
    • C12N9/1007—Methyltransferases (general) (2.1.1.)
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    • 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
    • A61K31/405—Indole-alkanecarboxylic acids; Derivatives thereof, e.g. tryptophan, indomethacin
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    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Zoology (AREA)
  • Wood Science & Technology (AREA)
  • Genetics & Genomics (AREA)
  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Biochemistry (AREA)
  • Molecular Biology (AREA)
  • General Engineering & Computer Science (AREA)
  • Microbiology (AREA)
  • Biotechnology (AREA)
  • Urology & Nephrology (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Neurosurgery (AREA)
  • Reproductive Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Cardiology (AREA)
JP2014540115A 2011-11-04 2012-11-02 治療の方法 Expired - Fee Related JP6005753B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161555650P 2011-11-04 2011-11-04
US61/555,650 2011-11-04
PCT/US2012/063235 WO2013067296A1 (en) 2011-11-04 2012-11-02 Method of treatment

Publications (3)

Publication Number Publication Date
JP2015501784A JP2015501784A (ja) 2015-01-19
JP2015501784A5 JP2015501784A5 (enExample) 2015-12-24
JP6005753B2 true JP6005753B2 (ja) 2016-10-12

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Application Number Title Priority Date Filing Date
JP2014540115A Expired - Fee Related JP6005753B2 (ja) 2011-11-04 2012-11-02 治療の方法

Country Status (11)

Country Link
US (2) US9242962B2 (enExample)
EP (1) EP2773754B1 (enExample)
JP (1) JP6005753B2 (enExample)
KR (1) KR20140095073A (enExample)
CN (1) CN104039956A (enExample)
AU (1) AU2012332297B2 (enExample)
BR (1) BR112014010803A2 (enExample)
CA (1) CA2854447A1 (enExample)
ES (1) ES2600161T3 (enExample)
RU (1) RU2621148C2 (enExample)
WO (1) WO2013067296A1 (enExample)

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WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CA2894222A1 (en) 2012-12-21 2014-06-26 Epizyme, Inc. 1,4-pyridone bicyclic heteroaryl compounds
US9045477B2 (en) 2013-03-15 2015-06-02 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
US9969716B2 (en) 2013-08-15 2018-05-15 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
WO2015077194A1 (en) * 2013-11-22 2015-05-28 Bristol-Myers Squibb Company Inhibitors of lysine methyl transferase
WO2015120372A2 (en) * 2014-02-10 2015-08-13 University Of Rochester Compositions and methods to inhibit ezh2 for the treatment of cardiovascular diseases
AU2015225775B2 (en) * 2014-03-07 2017-06-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of Zeste Homolog 2 inhibitors
PL3121175T3 (pl) * 2014-03-17 2020-06-01 Daiichi Sankyo Company, Limited Pochodne 1,3-benzodioksolu jako inhibitory ezh1 i/lub ezh2
MA40848A (fr) * 2014-10-28 2021-05-05 Glaxosmithkline Ip No 2 Ltd Inhibiteurs d'ezh2 (enhancer of zeste homolog 2)
CA2964629A1 (en) * 2014-11-06 2016-05-12 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
BR112017009440A2 (pt) * 2014-11-06 2017-12-19 Dana Farber Cancer Inst Inc uso de composições que modulam a estrutura de cromatina quanto à doença do enxerto versus hospedeiro (gvhd)
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
CA2994394A1 (en) * 2015-08-03 2017-02-09 Constellation Pharmaceuticals, Inc. Ezh2 inhibitors and modulation of regulatory t-cell function
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
WO2017040190A1 (en) 2015-08-28 2017-03-09 Constellation Pharmaceuticals, Inc. Crystalline forms of (r)-n-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1h-indole-3-carboxamide
CN105541801B (zh) * 2016-01-18 2018-07-17 常州大学 Ezh2甲基转移酶抑制剂gsk126的合成方法
WO2017184999A1 (en) 2016-04-22 2017-10-26 Dana-Farber Cancer Institute, Inc. Ezh2 inhibitors and uses thereof
JP2019524872A (ja) * 2016-06-20 2019-09-05 ノバルティス アーゲー 癌の治療に有用なイミダゾピリミジン化合物
US10968215B2 (en) * 2016-09-07 2021-04-06 Shanghai Haihe Pharmaceutical Co., Ltd. Pyrido five-element aromatic ring compound, preparation method therefor and use thereof
WO2018075598A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
CN110191879A (zh) * 2017-01-25 2019-08-30 恩瑞生物医药科技(上海)有限公司 一种组蛋白甲基转移酶ezh2抑制剂、其制备方法及其医药用途
WO2020011607A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
TWI837231B (zh) 2018-11-29 2024-04-01 日商第一三共股份有限公司 含有ezh1/2雙重抑制劑之醫藥組合及其用途
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US20160074394A1 (en) 2016-03-17
KR20140095073A (ko) 2014-07-31
US9242962B2 (en) 2016-01-26
AU2012332297A1 (en) 2014-05-22
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CA2854447A1 (en) 2013-05-10
WO2013067296A1 (en) 2013-05-10
JP2015501784A (ja) 2015-01-19
BR112014010803A2 (pt) 2017-04-25
AU2012332297B2 (en) 2016-01-07
CN104039956A (zh) 2014-09-10
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