EA029089B9 - Модуляторы метил-модифицирующих ферментов, композиции и их применение - Google Patents

Модуляторы метил-модифицирующих ферментов, композиции и их применение

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Publication number
EA029089B9
EA029089B9 EA201591474A EA201591474A EA029089B9 EA 029089 B9 EA029089 B9 EA 029089B9 EA 201591474 A EA201591474 A EA 201591474A EA 201591474 A EA201591474 A EA 201591474A EA 029089 B9 EA029089 B9 EA 029089B9
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EA
Eurasian Patent Office
Prior art keywords
modulators
compositions
modifying enzymes
methyl modifying
methyl
Prior art date
Application number
EA201591474A
Other languages
English (en)
Other versions
EA029089B1 (ru
EA201591474A1 (ru
Inventor
Брайан К. Албрехт
Джеймс Эдмунд Аудиа
Эндрю С. Кук
Лес А. Дакин
Мартин Даплессис
Виктор С. Гелинг
Жан-Кристоф Арманж
Кристофер Дж. Насвещук
Риши Г. Васуани
Original Assignee
Констеллейшен Фармасьютикалс, Инк.
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Publication date
Application filed by Констеллейшен Фармасьютикалс, Инк. filed Critical Констеллейшен Фармасьютикалс, Инк.
Priority claimed from PCT/US2014/015706 external-priority patent/WO2014124418A1/en
Publication of EA201591474A1 publication Critical patent/EA201591474A1/ru
Publication of EA029089B1 publication Critical patent/EA029089B1/ru
Publication of EA029089B9 publication Critical patent/EA029089B9/ru

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    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/10Drugs for disorders of the urinary system of the bladder
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Hydrogenated Pyridines (AREA)

Abstract

Изобретение относится к агентам для модулирования метил-модифицирующего фермента, имеющим структурную формулу (II)и их фармацевтическим приемлемым солям. Кроме того, изобретение обеспечивает фармацевтическую композицию, предусматривающую их использование, а также их применение для лечения рака.
EA201591474A 2012-02-10 2014-02-11 Модуляторы метил-модифицирующих ферментов, композиции и их применение EA029089B9 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US201261597695P 2012-02-10 2012-02-10
US201261667821P 2012-07-03 2012-07-03
PCT/US2013/025639 WO2013120104A2 (en) 2012-02-10 2013-02-11 Modulators of methyl modifying enzymes, compositions and uses thereof
PCT/US2014/015706 WO2014124418A1 (en) 2013-02-11 2014-02-11 Modulators of methyl modifying enzymes, compositions and uses thereof

Publications (3)

Publication Number Publication Date
EA201591474A1 EA201591474A1 (ru) 2016-01-29
EA029089B1 EA029089B1 (ru) 2018-02-28
EA029089B9 true EA029089B9 (ru) 2019-01-31

Family

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EA201591474A EA029089B9 (ru) 2012-02-10 2014-02-11 Модуляторы метил-модифицирующих ферментов, композиции и их применение

Country Status (19)

Country Link
US (8) US9085583B2 (ru)
EP (1) EP2812001B1 (ru)
JP (2) JP5989805B2 (ru)
AR (1) AR094755A1 (ru)
AU (1) AU2013216721B2 (ru)
BR (1) BR112015018508B1 (ru)
CA (1) CA2862289C (ru)
CY (1) CY1119060T1 (ru)
DK (1) DK2953941T3 (ru)
EA (1) EA029089B9 (ru)
ES (1) ES2632241T3 (ru)
HR (1) HRP20171030T1 (ru)
LT (1) LT2953941T (ru)
MX (1) MX363392B (ru)
MY (1) MY172156A (ru)
NZ (1) NZ628762A (ru)
PT (1) PT2953941T (ru)
UA (1) UA117362C2 (ru)
WO (1) WO2013120104A2 (ru)

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2841142C (en) 2010-06-23 2020-12-15 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
AU2013216721B2 (en) 2012-02-10 2017-09-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
RS56207B1 (sr) * 2013-02-11 2017-11-30 Constellation Pharmaceuticals Inc Modulatori enzima koji modifikuju metil, njihove kompozicije i upotreba
EP2970305B1 (en) * 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
JP6373973B2 (ja) 2013-04-30 2018-08-15 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited Zesteホモログ2エンハンサー阻害剤
CA2917463A1 (en) 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
EP3033334A1 (en) * 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
WO2015078417A1 (zh) * 2013-11-29 2015-06-04 四川好医生药业集团有限公司 吡咯并嘧啶化合物及其在制备降血糖药物中的用途
EP3160940A4 (en) * 2014-06-25 2018-05-02 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
RU2017118165A (ru) * 2014-10-28 2018-11-29 Глэксосмитклайн Интеллекчуал Проперти (Но.2) Лимитед Ингибиторы энхансера гомолога 2 zestes
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ezh2抑制劑
WO2016130396A1 (en) * 2015-02-13 2016-08-18 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
UY36758A (es) * 2015-06-30 2016-12-30 Glaxosmithkline Ip No 2 Ltd Inhibidores del potenciador del homólogo zeste 2
WO2017018975A1 (en) 2015-07-24 2017-02-02 Constellation Pharmaceuticals, Inc. Combination therapies for modulation of histone methyl modifying enzymes
AU2016302747A1 (en) 2015-08-03 2018-02-22 Constellation Pharmaceuticals, Inc. EZH2 inhibitors and modulation of regulatory T-cell function
WO2017025493A1 (en) * 2015-08-12 2017-02-16 Bayer Pharma Aktiengesellschaft Quinoline ezh2 inhibitors
CN108025191A (zh) 2015-08-24 2018-05-11 Epizyme股份有限公司 治疗癌症的方法
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
EP3371175A4 (en) 2015-10-06 2019-09-25 Epizyme Inc METHOD FOR TREATING A MEDULLOBLASTOMA WITH AN EZH2 INHIBITOR
US20180321256A1 (en) 2015-11-05 2018-11-08 Epizyme, Inc. Flow cytometry for monitoring histone h3 methylation status
WO2017132518A1 (en) 2016-01-29 2017-08-03 Epizyme, Inc. Combination therapy for treating cancer
SG10201913331VA (en) 2016-03-15 2020-03-30 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of solid tumors
HUE049918T2 (hu) 2016-05-31 2020-11-30 Kalvista Pharmaceuticals Ltd Pirazol-származékok mint plazma kallikrein inhibitorok
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
US11147819B2 (en) 2016-06-17 2021-10-19 Epizyme, Inc. EZH2 inhibitors for treating cancer
CA3039059A1 (en) * 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
WO2018102687A2 (en) 2016-12-02 2018-06-07 Epizyme, Inc. Combination therapy for treating cancer
AU2018210141A1 (en) 2017-01-20 2019-08-29 Constellation Pharmaceuticals, Inc. Solid dispersions 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
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
US20230201212A1 (en) 2017-06-13 2023-06-29 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
WO2019014191A1 (en) 2017-07-10 2019-01-17 Constellation Pharmaceuticals, Inc. GENE EXPRESSION INDUCED BY EZH2 INHIBITOR
US11459315B2 (en) 2017-11-09 2022-10-04 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2019097369A1 (en) 2017-11-14 2019-05-23 Pfizer Inc. Ezh2 inhibitor combination therapies
LT3716952T (lt) 2017-11-29 2022-04-11 Kalvista Pharmaceuticals Limited Vaisto formos, apimančios plazmos kalikreino inhibitorių
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
CN111757734A (zh) 2017-12-28 2020-10-09 星座制药公司 通过组合疗法的ezh2抑制剂的药代动力学增强
CN112004816B (zh) 2018-01-31 2024-01-05 米拉蒂医疗股份有限公司 Prc2抑制剂
ES2942211T3 (es) 2018-03-14 2023-05-30 Biogen Ma Inc Inhibidores de la O-glucoproteína-2-acetamido-2-desoxi-3-D-glucopiranosidasa
FI3781561T3 (fi) * 2018-04-18 2024-06-13 Constellation Pharmaceuticals Inc Metyyliä muuntavien entsyymien modulaattoreita, niiden koostumuksia ja käyttöjä
EP3823671B1 (en) 2018-07-09 2024-02-07 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
JOP20210036A1 (ar) 2018-09-19 2021-02-25 Biogen Ma Inc مثبطات او- جليكوبروتين-2-أسيتاميدو-2-ديوكسي-3-دي-جلوكوبيرانوسيداز
US20200131156A1 (en) * 2018-10-30 2020-04-30 H. Lundbeck A/S ARYLSULFONYLPYROLECARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS
EP3891146B1 (en) 2018-12-05 2023-09-27 Biogen MA Inc. Morpholinyl, piperazinyl, oxazepanyl and diazepanyl derivatives useful as o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
WO2020139339A1 (en) 2018-12-27 2020-07-02 Constellation Pharmaceuticals, Inc. Ezh2 and androgen receptor signaling inhibitors as tools for targeting prostate cancer
CN110357840B (zh) * 2019-01-22 2022-04-12 石家庄和中科技有限公司 4-糠硫基戊酮-2的制备方法
TW202045501A (zh) 2019-02-04 2020-12-16 美商百健Ma公司 雙環醚o-糖蛋白-2-乙醯胺基-2-去氧-3-d-哌喃葡萄糖苷酶抑制劑
EP3935055A1 (en) 2019-03-08 2022-01-12 Biogen MA Inc. Azetidinyl 0-glyc0pr0tein-2-acetamid0-2-deoxy-3-d-gluc0pyran0sidase inhibitors
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
EP4017527A1 (en) 2019-08-22 2022-06-29 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
CN114929709A (zh) 2019-10-29 2022-08-19 比奥根Ma公司 螺环o-糖蛋白-2-乙酰胺基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂
IL300365A (en) 2020-08-03 2023-04-01 Biogen Ma Inc Crystal forms of O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitor
WO2022150962A1 (en) 2021-01-12 2022-07-21 Westlake Pharmaceutical (Hangzhou) Co., Ltd. Protease inhibitors, preparation, and uses thereof

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE52670B1 (en) * 1981-03-03 1988-01-20 Leo Ab Heterocyclic carboxamides,compositions containing such compounds,and processes for their preparation
US5308854A (en) 1990-06-18 1994-05-03 Merck & Co., Inc. Inhibitors of HIV reverse transcriptase
ATE278402T1 (de) 1996-07-22 2004-10-15 Daiichi Suntory Pharma Co Ltd Arylpiperidinol und arylpiperidin-derivate und sie enthaltende arzneimittel
WO2003020722A1 (de) 2001-09-04 2003-03-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
MXPA03000145A (es) 2002-01-07 2003-07-15 Pfizer Compuestos de oxo u oxi-piridina como moduladores de receptores 5-ht4.
AU2003220401A1 (en) 2002-03-18 2003-10-08 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
TW200500341A (en) * 2002-11-12 2005-01-01 Astrazeneca Ab Novel compounds
CA2554120A1 (en) 2004-01-30 2005-08-18 Merck & Co., Inc. N-benzyl-3,4-dihydroxypyridine-2-carboxamide and n-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as hiv integras inhibitors
RU2006142305A (ru) 2004-04-30 2008-06-10 Такеда Фармасьютикал Компани Лимитед (Jp) Гетероциклическое амидное соединение и его применение в качестве ингибитора ммр-3
JP5160885B2 (ja) 2004-06-01 2013-03-13 ザ・ユニヴァーシティ・オヴ・ノース・キャロライナ・アト・チャペル・ヒル 再構成ヒストンメチルトランスフェラーゼ複合体及びそのモジュレーターの識別方法
WO2007011626A2 (en) * 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase inhibitors
EP1915155A1 (en) 2005-08-03 2008-04-30 Boehringer Ingelheim International GmbH Dihydropteridinones in the treatment of respiratory diseases
CN101326292A (zh) 2005-12-08 2008-12-17 诺瓦提斯公司 Fgfr3抑制物对基因转录的影响
WO2008054154A1 (en) 2006-11-03 2008-05-08 Korea Research Institute Of Chemical Technology Naphthalenyloxypropenyl derivatives having inhibitory activity against histone deacetylase and pharmaceutical composition comprising the same
US8058003B2 (en) 2007-01-19 2011-11-15 The Regents Of The University Of Michigan ADRB2 cancer markers
EP2114898A2 (en) 2007-02-16 2009-11-11 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
US8030344B2 (en) 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
WO2009006577A2 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US20100298270A1 (en) 2007-07-23 2010-11-25 Syndax Pharmaceuticals, Inc. Novel Compounds and Methods of Using Them
FR2922209B1 (fr) 2007-10-12 2010-06-11 Sanofi Aventis 5,6-DIARYLES PYRIDINES SUBSTITUES EN POSITION 2 et 3, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE.
EP2224928A4 (en) 2007-12-06 2012-02-15 Glaxosmithkline Llc NOVEL INHIBITORS OF SEH AND THEIR USE
TW200944506A (en) 2008-03-26 2009-11-01 Takeda Pharmaceutical Substituted pyrazole derivatives and use thereof
JP2011524894A (ja) 2008-06-18 2011-09-08 ファイザー・リミテッド ニコチンアミド誘導体
EP2365749A4 (en) 2008-11-13 2012-05-30 Merck Sharp & Dohme QUINOLONE ANTAGONISTS OF THE NEUROPEPTIDE S RECEPTOR
WO2011055270A1 (en) * 2009-11-04 2011-05-12 Wyeth Llc Indole based receptor crth2 antagonists
US8468343B2 (en) 2010-01-13 2013-06-18 Futurewei Technologies, Inc. System and method for securing wireless transmissions
US9469876B2 (en) 2010-04-06 2016-10-18 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers for metastatic prostate cancer
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
US8536179B2 (en) 2010-05-07 2013-09-17 Glaxosmithkline Llc Indoles
JP5889875B2 (ja) * 2010-05-07 2016-03-22 グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーGlaxoSmithKline LLC アザインダゾール
US8846935B2 (en) 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
JP2013540995A (ja) 2010-08-18 2013-11-07 カリス ライフ サイエンシズ ルクセンブルク ホールディングス エス.アー.エール.エル. 疾患に対する循環バイオマーカー
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
CA2810998C (en) * 2010-09-10 2024-04-09 Robert Allen Copeland Inhibitors of human ezh2, and methods of use thereof
WO2012051492A2 (en) 2010-10-14 2012-04-19 University Of Georgia Research Foundation, Inc. Compounds and methods for inhibiting hiv latency
WO2012068589A2 (en) 2010-11-19 2012-05-24 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
WO2012075080A1 (en) * 2010-12-01 2012-06-07 Glaxosmithkline Llc Indoles
WO2012115885A1 (en) 2011-02-22 2012-08-30 Caris Life Sciences Luxembourg Holdings, S.A.R.L. Circulating biomarkers
JP2014511389A (ja) 2011-02-28 2014-05-15 エピザイム インコーポレイテッド 置換6,5−縮合二環式ヘテロアリール化合物
TW201733984A (zh) * 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3438B1 (ar) * 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
WO2013039988A1 (en) 2011-09-13 2013-03-21 Glax0Smithkline Llc Azaindazoles
US9730925B2 (en) 2011-09-30 2017-08-15 Glaxomithkline Llc Methods of treating cancer
WO2013067302A1 (en) 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
BR112014010803A2 (pt) 2011-11-04 2017-04-25 Glaxosmithkline Intellectual Property (No 2) Ltd método de tratamento
WO2013067300A1 (en) 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013078320A1 (en) 2011-11-21 2013-05-30 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
US20130230511A1 (en) 2012-02-03 2013-09-05 Board Of Regents, The University Of Texas System Biomarkers for response to tyrosine kinase pathway inhibitors in cancer
AU2013216721B2 (en) * 2012-02-10 2017-09-28 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
ES2718900T3 (es) 2012-03-12 2019-07-05 Epizyme Inc Inhibidores de EZH2 humana y métodos de uso de los mismos
ES2745016T3 (es) 2012-04-13 2020-02-27 Epizyme Inc Bromhidrato de N-((4,6-dimetil-2-oxo-L,2-dihidropiridin-3-il)metil)-5-(etil(tetrahidro-2H-piran-4-il)amino)-4-metil-4'-(morfolinometil)-[L,1'-bifenil]-3-carboxamida para su uso en el tratamiento de un trastorno proliferativo celular del sistema hematológico
JP6340361B2 (ja) 2012-04-13 2018-06-06 エピザイム,インコーポレイティド がんを処置するための組合せ治療
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
CA2884848C (en) * 2012-09-28 2017-08-22 Pfizer Inc. Benzamide and heterobenzamide compounds
PE20150886A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
RU2018145311A (ru) 2012-10-15 2019-02-18 Эпизайм, Инк. Способы лечения рака
CN103794728A (zh) 2012-10-30 2014-05-14 中国科学院长春光学精密机械与物理研究所 高导电性有机透明导电薄膜的制备方法
JP6584952B2 (ja) 2012-11-01 2019-10-02 インフィニティー ファーマシューティカルズ, インコーポレイテッド Pi3キナーゼアイソフォームモジュレーターを用いる癌の治療
SG11201503893RA (en) 2012-11-19 2015-06-29 Agency Science Tech & Res Method of treating cancer
WO2014085666A1 (en) 2012-11-27 2014-06-05 Board Of Regents, The University Of Texas System Methods of characterizing and treating molecular subset of muscle-invasive bladder cancer
WO2014092905A1 (en) 2012-12-10 2014-06-19 Children's Medical Center Corporation Methods and assays for combination treatment of cancer
US20150313906A1 (en) 2012-12-19 2015-11-05 Glaxosmithkline Llc Combination
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
RS56207B1 (sr) 2013-02-11 2017-11-30 Constellation Pharmaceuticals Inc Modulatori enzima koji modifikuju metil, njihove kompozicije i upotreba
EP2970305B1 (en) * 2013-03-15 2017-02-22 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
JP6373973B2 (ja) * 2013-04-30 2018-08-15 グラクソスミスクライン、インテレクチュアル、プロパティー、(ナンバー2)、リミテッドGlaxosmithkline Intellectual Property (No.2) Limited Zesteホモログ2エンハンサー阻害剤
EP3022195A2 (en) * 2013-07-19 2016-05-25 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
EP3033334A1 (en) * 2013-08-15 2016-06-22 Constellation Pharmaceuticals, Inc. Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
US9374093B2 (en) 2014-01-10 2016-06-21 Freescale Semiconductor, Inc. Capacitively coupled input buffer
EP3160940A4 (en) * 2014-06-25 2018-05-02 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds

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