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

Модуляторы метил-модифицирующих ферментов, композиции и их применение

Info

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
Authority
EA
Eurasian Patent Office
Prior art keywords
modulators
compositions
modifying enzymes
methyl modifying
methyl
Prior art date
Application number
EA201591474A
Other languages
English (en)
Russian (ru)
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.
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 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

Links

Classifications

    • 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
    • CCHEMISTRY; METALLURGY
    • 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
    • CCHEMISTRY; METALLURGY
    • 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

Landscapes

  • 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)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Dermatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (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)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
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

ID=48948171

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201591474A EA029089B9 (ru) 2012-02-10 2014-02-11 Модуляторы метил-модифицирующих ферментов, композиции и их применение

Country Status (20)

Country Link
US (8) US9085583B2 (https=)
EP (1) EP2812001B1 (https=)
JP (2) JP5989805B2 (https=)
AR (1) AR094755A1 (https=)
AU (1) AU2013216721B2 (https=)
BR (1) BR112015018508B1 (https=)
CA (1) CA2862289C (https=)
CY (1) CY1119060T1 (https=)
DK (1) DK2953941T3 (https=)
EA (1) EA029089B9 (https=)
ES (1) ES2632241T3 (https=)
HR (1) HRP20171030T1 (https=)
LT (1) LT2953941T (https=)
MX (1) MX363392B (https=)
MY (1) MY172156A (https=)
NZ (1) NZ628762A (https=)
PT (1) PT2953941T (https=)
SM (1) SMT201700340T1 (https=)
UA (1) UA117362C2 (https=)
WO (1) WO2013120104A2 (https=)

Families Citing this family (67)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130102477A1 (en) 2010-06-23 2013-04-25 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
NZ628762A (en) 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
KR20230156450A (ko) 2012-10-15 2023-11-14 에피자임, 인코포레이티드 암을 치료하는 방법
SI2953941T1 (sl) * 2013-02-11 2017-08-31 Constellation Pharmaceuticals, Inc. Modulatorji metil-modificirajočih encimov, sestavki in uporabe le-teh
WO2014151142A1 (en) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2991980B1 (en) 2013-04-30 2019-01-02 Glaxosmithkline Intellectual Property (No. 2) Limited Enhancer of zeste homolog 2 inhibitors
KR20160030221A (ko) 2013-07-10 2016-03-16 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 제스트 인핸서 상동체 2 억제제
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
WO2015200650A1 (en) * 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
CN107148419A (zh) * 2014-10-28 2017-09-08 葛兰素史密斯克莱知识产权(第2 号)有限公司 Zeste增强子同源物2抑制剂
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
AR102767A1 (es) 2014-12-05 2017-03-22 Lilly Co Eli Inhibidores de ezh2
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
US20180221362A1 (en) 2015-08-03 2018-08-09 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
WO2017035234A1 (en) 2015-08-24 2017-03-02 Epizyme, Inc. Method for treating cancer
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ezh2抑制劑
US10577350B2 (en) * 2015-08-28 2020-03-03 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
AU2016333982A1 (en) 2015-10-06 2018-04-26 Epizyme, Inc. Method of treating medulloblastoma with an EZH2 inhibitor
US20180321256A1 (en) 2015-11-05 2018-11-08 Epizyme, Inc. Flow cytometry for monitoring histone h3 methylation status
EP3407978A4 (en) 2016-01-29 2020-01-15 Epizyme Inc POLYTHERAPY FOR THE TREATMENT OF CANCER
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
IL263235B (en) 2016-05-31 2022-07-01 Kalvista Pharmaceuticals Ltd History of pyrazoles as plasma kallikrein inhibitors
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
WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
US10457640B2 (en) 2016-10-19 2019-10-29 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of EZH2
JP7208898B2 (ja) 2016-12-02 2023-01-19 エピザイム,インコーポレイティド 癌を処置するための併用療法
JP2020506905A (ja) * 2017-01-20 2020-03-05 コンステレーション・ファーマシューティカルズ・インコーポレイテッドConstellation Pharmaceuticals,Inc. (r)−n−((4−メトキシ−6−メチル−2−オキソ−1,2−ジヒドロピリジン−3−イル)メチル)−2−メチル−1−(1−(1−(2,2,2−トリフルオロエチル)ピペリジン−4−イル)エチル)−1h−インドール−3−カルボキサミド固体分散液
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
WO2018231973A1 (en) 2017-06-13 2018-12-20 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
KR20200088386A (ko) 2017-11-14 2020-07-22 화이자 인코포레이티드 Ezh2 억제제 병용 요법
HUE057912T2 (hu) 2017-11-29 2022-06-28 Kalvista Pharmaceuticals Ltd Plazma kallikrein inhibitort tartalmazó dózisformák
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
US20210000815A1 (en) 2017-12-28 2021-01-07 Constellation Pharmaceuticals, Inc. Pharmacokinetic enhancement of ezh2 inhibitors through combination therapies
DK3746446T3 (da) 2018-01-31 2022-06-27 Mirati Therapeutics Inc PRC2-inhibitorer
AU2019234759C1 (en) 2018-03-14 2025-02-06 Biogen Ma Inc. O-glycoprotein-2-acetamido-2-deoxy-3-D-glycopyranosidase inhibitors
CR20200553A (es) * 2018-04-18 2021-04-08 Constellation Pharmaceuticals Inc Moduladores de enzimas modificadoras de metilo, composiciones y usos de estos
CA3104209A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
PE20211591A1 (es) 2018-09-19 2021-08-18 Biogen Ma Inc Inhibidores de o-glicoproteina-2-acetamido-2-desoxi-3-d-glucopiranosidasa
AR116898A1 (es) * 2018-10-30 2021-06-23 H Lundbeck As DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3
US12319679B2 (en) 2018-12-05 2025-06-03 Biogen Ma Inc. Morpholinyl, piperazinyl, oxazepanyl and diazepanyl 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
EP3921316A1 (en) 2019-02-04 2021-12-15 Biogen MA Inc. Bicyclic ether o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
JP7663503B2 (ja) 2019-03-08 2025-04-16 バイオジェン・エムエイ・インコーポレイテッド アゼチジニルo-糖タンパク質-2-アセトアミド-2-デオキシ-3-d-グルコピラノシダーゼ阻害剤
US12421228B2 (en) 2019-04-22 2025-09-23 Mirati Therapeutics, Inc. Naphthyridine derivatives as PRC2 inhibitors
US12252493B2 (en) 2019-06-05 2025-03-18 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as PRC2 inhibitors for treating cancer
WO2021016409A1 (en) * 2019-07-24 2021-01-28 Constellation Pharmaceuticals, Inc. Ezh2 inhibition in combination therapies for the treatment of cancers
WO2021016414A1 (en) 2019-07-24 2021-01-28 Constellation Pharmaceuticals, Inc. Crystalline forms of 7-chloro-2-(4-(3-methoxyazetidin-1-yl)cyclohexyl)-2,4-dimethyl-n-((6-methyl-4-(methylthio)-2-oxo-1,2-dihydropyridin-3-yl)methyl)benzo[d][1,3]dioxole-5-carboxamide
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
JP2022545467A (ja) 2019-08-22 2022-10-27 ジュノー セラピューティクス インコーポレイテッド T細胞療法とzesteホモログ2エンハンサー(EZH2)阻害剤との併用療法および関連方法
US12565504B2 (en) 2019-10-29 2026-03-03 Biogen Ma Inc. Spirocyclic O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
CN116917284A (zh) 2020-08-03 2023-10-20 渤健马萨诸塞州股份有限公司 O-糖蛋白-2-乙酰胺基-2-脱氧-3-d-吡喃葡萄糖苷酶抑制剂的结晶形式
WO2022150962A1 (en) 2021-01-12 2022-07-21 Westlake Pharmaceutical (Hangzhou) Co., Ltd. Protease inhibitors, preparation, and uses thereof
CA3218159A1 (en) 2021-05-20 2022-11-24 Zhaolan ZHANG Rip1 modulators including azetidine cyclic ureas, preparations, and uses thereof
TW202340187A (zh) * 2021-12-20 2023-10-16 加拿大商費爾哈芬製藥公司 Oxer1拮抗劑及其用途
CN118026860A (zh) * 2024-02-05 2024-05-14 福建福瑞明德药业有限公司 一种3-[1-(二甲基氨基)乙基]苯酚的制备方法

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
EP0867183B1 (en) 1996-07-22 2004-10-06 Daiichi Suntory Pharma Co., Ltd. Arylpiperidinol and arylpiperidine derivatives and drugs containing the same
PT1427730E (pt) 2001-09-04 2006-11-30 Boehringer Ingelheim Pharma Novas di-hidropteridinonas, processo para sua preparação e sua utilização como medicamento
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
JP2007519735A (ja) 2004-01-30 2007-07-19 メルク エンド カムパニー インコーポレーテッド Hivインテグラーゼ阻害剤として有用であるn−ベンジル−3,4−ジヒドロキシピリジン−2−カルボキサミド及びn−ベンジル−2,3−ジヒドロキシピリジン−4−カルボキサミド化合物
BRPI0510305A (pt) 2004-04-30 2007-10-02 Takeda Pharmaceutical composto ou um sal do mesmo, pródroga ou um sal da mesma, agente farmacêutico, método de produção do composto ou um sal do mesmo, inibidor de metaloproteinase de matriz ou um sal do mesmo ou uma pródroga do mesmo, método de inibir uma metaloproteinase de matriz, e, uso de um composto ou de um sal do mesmo ou de uma pródroga do mesmo
DE602005017781D1 (de) 2004-06-01 2009-12-31 Univ North Carolina Rekonstituierter histon-methyltransferase-komplex und verfahren zur identifizierung von modulatoren dafür
EA200800321A1 (ru) * 2005-07-14 2008-06-30 Такеда Сан Диего, Инк. Ингибиторы гистондеацетилазы
WO2007014838A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Dihydropteridinones in the treatment of respiratory diseases
JP2009523410A (ja) 2005-12-08 2009-06-25 ノバルティス アクチエンゲゼルシャフト 遺伝子転写に対するfgfr3の阻害剤の効果
JP5277171B2 (ja) 2006-11-03 2013-08-28 コリア リサーチ インスティテュート オブ ケミカル テクノロジーズ ヒストン脱アセチル化酵素阻害活性を有するナフタレニルオキシプロペニル誘導体およびこれを含む薬学組成物
JP5513128B2 (ja) 2007-01-19 2014-06-04 ザ リージェンツ オブ ザ ユニバーシティ オブ ミシガン Adrb2癌マーカー
AU2008219166B2 (en) 2007-02-16 2013-05-16 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
US20090012031A1 (en) * 2007-07-03 2009-01-08 The Regents Of The University Of Michigan EZH2 Cancer Markers
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
WO2009119880A1 (en) 2008-03-26 2009-10-01 Takeda Pharmaceutical Company Limited Substituted pyrazole derivatives and use thereof
CA2725481A1 (en) 2008-06-18 2009-12-23 Pfizer Limited Nicotinamide derivatives
WO2010056564A1 (en) 2008-11-13 2010-05-20 Merck Sharp & Dohme Corp. Quinolone neuropeptide s receptor antagonists
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
WO2011127219A1 (en) 2010-04-06 2011-10-13 Caris Life Sciences Luxembourg Holdings Circulating biomarkers for disease
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
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
UA110112C2 (uk) 2010-05-07 2015-11-25 Глаксосмітклайн Ллс Індоли
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
BR112013005806B1 (pt) 2010-09-10 2022-05-10 Epizyme, Inc Métodos para detectar se um indivíduo é um candidato para o tratamento com ou responsivo a um inibidor de ezh2 e usos terapêuticos do dito inibidor de ezh2
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. 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
US20130310379A1 (en) 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
ES2607064T3 (es) 2010-12-01 2017-03-29 Glaxosmithkline Llc Indoles
WO2012115885A1 (en) 2011-02-22 2012-08-30 Caris Life Sciences Luxembourg Holdings, S.A.R.L. Circulating biomarkers
ES2951688T3 (es) 2011-02-28 2023-10-24 Epizyme Inc Compuestos de heteroarilo biciclico fusionados en 6,5 sustituidos
JO3363B1 (ar) * 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TWI598336B (zh) * 2011-04-13 2017-09-11 雅酶股份有限公司 經取代之苯化合物
EP2755962B1 (en) 2011-09-13 2017-03-01 Glaxosmithkline LLC Azaindazoles
CA2850570A1 (en) 2011-09-30 2013-04-04 Glaxosmithkline Llc Methods of treating cancer
WO2013067302A1 (en) 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
WO2013067300A1 (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
EP2780013A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
EP2780014A4 (en) * 2011-11-18 2015-07-01 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
NZ628762A (en) 2012-02-10 2016-07-29 Constellation Pharmaceuticals Inc Modulators of methyl modifying enzymes, compositions and uses thereof
EP3536314A1 (en) 2012-03-12 2019-09-11 Epizyme, Inc. Inhibitors of human ezh2, and methods of use thereof
PT3184523T (pt) 2012-04-13 2019-09-26 Eisai R&D Man Co Ltd Bromidrato de n-((4,6-dimetil-2-oxo-l,2-di-hidropiridin- 3-il)metil)-5-(etil(tetra-hidro-2h-piran-4-il)amino)-4- metil-4¿-(morfolinometil)-[l,1¿-bofenil]-3-carboxamida para utilização no tratamento de uma doença proliferativa celular do sistema hematológico
SG10201912111TA (en) 2012-04-13 2020-02-27 Epizyme Inc Combination therapy for treating cancer
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
JP6254169B2 (ja) 2012-09-28 2017-12-27 ファイザー・インク ベンズアミドおよびヘテロベンズアミド化合物
MX2015004721A (es) * 2012-10-15 2016-01-25 Epizyme Inc Compuestos de benceno sustituidos.
KR20230156450A (ko) 2012-10-15 2023-11-14 에피자임, 인코포레이티드 암을 치료하는 방법
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
EP2914296B2 (en) 2012-11-01 2021-09-29 Infinity Pharmaceuticals, Inc. Treatment of cancers using pi3 kinase isoform modulators
EP2908843B1 (en) 2012-11-19 2019-09-04 Agency For Science, Technology And Research 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
US9895390B2 (en) 2012-12-10 2018-02-20 Children's Medical Center Corporation Methods and assays for combination treatment of cancer
EP2934531A4 (en) 2012-12-19 2016-06-15 Glaxosmithkline Llc COMBINATION
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
SI2953941T1 (sl) 2013-02-11 2017-08-31 Constellation Pharmaceuticals, Inc. Modulatorji metil-modificirajočih encimov, sestavki in uporabe le-teh
WO2014151142A1 (en) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2991980B1 (en) * 2013-04-30 2019-01-02 Glaxosmithkline Intellectual Property (No. 2) Limited Enhancer of zeste homolog 2 inhibitors
WO2015010078A2 (en) * 2013-07-19 2015-01-22 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
WO2015200650A1 (en) * 2014-06-25 2015-12-30 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds

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