CA2862289C - Modulators of methyl modifying enzymes, compositions and uses thereof - Google Patents

Modulators of methyl modifying enzymes, compositions and uses thereof Download PDF

Info

Publication number
CA2862289C
CA2862289C CA2862289A CA2862289A CA2862289C CA 2862289 C CA2862289 C CA 2862289C CA 2862289 A CA2862289 A CA 2862289A CA 2862289 A CA2862289 A CA 2862289A CA 2862289 C CA2862289 C CA 2862289C
Authority
CA
Canada
Prior art keywords
methyl
piperidin
alkylene
compound
cancer
Prior art date
Legal status (The legal status 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 status listed.)
Active
Application number
CA2862289A
Other languages
English (en)
French (fr)
Other versions
CA2862289A1 (en
Inventor
Brian K. Albrecht
James Edmund Audia
Andrew S. Cook
Les A. Dakin
Martin Duplessis
Victor S. Gehling
Jean-Christophe Harmange
Christopher G. Nasveschuk
Rishi G. Vaswani
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Constellation Pharmaceuticals Inc
Original Assignee
Constellation Pharmaceuticals 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 Constellation Pharmaceuticals Inc filed Critical Constellation Pharmaceuticals Inc
Publication of CA2862289A1 publication Critical patent/CA2862289A1/en
Application granted granted Critical
Publication of CA2862289C publication Critical patent/CA2862289C/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/08—Drugs for disorders of the urinary system of the prostate
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • 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
    • A61P35/00—Antineoplastic 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
    • 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
    • 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
    • C07D405/00—Heterocyclic 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
    • C07D405/14—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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
    • C07D417/04—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/14—Heterocyclic 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic 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
    • C07D487/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Dermatology (AREA)
  • Neurosurgery (AREA)
  • Pulmonology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (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)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Hydrogenated Pyridines (AREA)
CA2862289A 2012-02-10 2013-02-11 Modulators of methyl modifying enzymes, compositions and uses thereof Active CA2862289C (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261597695P 2012-02-10 2012-02-10
US61/597,695 2012-02-10
US201261667821P 2012-07-03 2012-07-03
US61/667,821 2012-07-03
PCT/US2013/025639 WO2013120104A2 (en) 2012-02-10 2013-02-11 Modulators of methyl modifying enzymes, compositions and uses thereof

Publications (2)

Publication Number Publication Date
CA2862289A1 CA2862289A1 (en) 2013-08-15
CA2862289C true CA2862289C (en) 2019-11-26

Family

ID=48948171

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2862289A Active CA2862289C (en) 2012-02-10 2013-02-11 Modulators of methyl modifying enzymes, compositions and uses thereof

Country Status (20)

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

Families Citing this family (64)

* 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
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CN110898067A (zh) 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法
KR102219441B1 (ko) * 2013-02-11 2021-02-23 콘스텔레이션 파마슈티칼스, 인크. 메틸 변형 효소 조절제, 이의 조성물 및 용도
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
ES2717680T3 (es) 2013-04-30 2019-06-24 Glaxosmithkline Ip No 2 Ltd Potenciador de inhibidores del homólogo de Zeste 2
US9556157B2 (en) 2013-07-10 2017-01-31 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
WO2015200650A1 (en) * 2014-06-25 2015-12-30 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
US20180037568A1 (en) * 2015-02-13 2018-02-08 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
CA2996412A1 (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
SG10201909413SA (en) 2015-10-06 2019-11-28 Epizyme Inc Method of treating medulloblastoma with an ezh2 inhibitor
WO2017079738A1 (en) 2015-11-05 2017-05-11 Epizyme, Inc. Flow cytometry for monitoring histone h3 methylation status
CA3011186A1 (en) 2016-01-29 2017-08-03 Epizyme, Inc. Combination therapy for treating cancer
EA201892075A1 (ru) 2016-03-15 2019-04-30 Оризон Дженомикс, С.А. Комбинации ингибиторов lsd1 для применения для лечения солидных опухолей
JP6884801B2 (ja) 2016-05-31 2021-06-09 カルビスタ・ファーマシューティカルズ・リミテッド 血漿カリクレインインヒビターとしてのピラゾール誘導体
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
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
WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
WO2018075598A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
EP3548032A2 (en) 2016-12-02 2019-10-09 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
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
US20210161883A1 (en) 2017-07-10 2021-06-03 Constellation Pharmaceuticals, Inc. Ezh2 inhibitor-induced gene expression
WO2019094552A1 (en) 2017-11-09 2019-05-16 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
MX2020005168A (es) 2017-11-29 2020-08-20 Kalvista Pharmaceuticals Ltd Formas de dosificacion que contienen un inhibidor calicreina de plasma.
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
EP3731842A1 (en) 2017-12-28 2020-11-04 Constellation Pharmaceuticals, Inc. Pharmacokinetic enhancement of ezh2 inhibitors through combination therapies
WO2019152419A1 (en) 2018-01-31 2019-08-08 Mirati Therapeutics, Inc Prc2 inhibitors
ES2942211T3 (es) 2018-03-14 2023-05-30 Biogen Ma Inc Inhibidores de la O-glucoproteína-2-acetamido-2-desoxi-3-D-glucopiranosidasa
KR102798145B1 (ko) * 2018-04-18 2025-04-22 콘스텔레이션 파마슈티칼스, 인크. 메틸 변형 효소 조절제, 이의 조성물 및 용도
JP2021531340A (ja) 2018-07-09 2021-11-18 フォンダシヨン、アジール、デ、アブグルスFondation Asile Des Aveugles 眼障害を治療するためのｐｒｃ２サブユニットの阻害
KR20210060513A (ko) 2018-09-19 2021-05-26 바이오젠 엠에이 인코포레이티드 O-당단백질-2-아세트아미도-2-데옥시-3-d-글루코피라노시다제 억제제
TW202031645A (zh) * 2018-10-30 2020-09-01 丹麥商Ｈ 朗德貝克公司 作為Kv3鉀通道激活劑之芳基磺醯基吡咯甲醯胺衍生物
EP4327814A3 (en) 2018-12-05 2024-04-24 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
WO2020163193A1 (en) 2019-02-04 2020-08-13 Biogen Ma Inc. Bicyclic ether o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
WO2020185593A1 (en) 2019-03-08 2020-09-17 Biogen Ma Inc. Azetidinyl 0-glyc0pr0tein-2-acetamid0-2-deoxy-3-d-gluc0pyran0sidase inhibitors
JP7624404B2 (ja) 2019-04-22 2025-01-30 ミラティ セラピューティクス，インク． Ｐｒｃ２阻害剤としてのナフチリジン誘導体
WO2020247475A1 (en) 2019-06-05 2020-12-10 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
CN118236503A (zh) * 2019-07-24 2024-06-25 星座制药公司 用于治疗癌症的ezh2抑制联合疗法
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
US20220298222A1 (en) 2019-08-22 2022-09-22 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
EP4051682A1 (en) 2019-10-29 2022-09-07 Biogen MA Inc. Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
CR20230118A (es) 2020-08-03 2023-06-02 Biogen Ma Inc Formas cristalinas de un inhibidor de la o-glucoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa
WO2022150962A1 (en) 2021-01-12 2022-07-21 Westlake Pharmaceutical (Hangzhou) Co., Ltd. Protease inhibitors, preparation, and uses thereof
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
DE69731070T2 (de) 1996-07-22 2005-03-17 Daiichi Suntory Pharma Co., Ltd. Arylpiperidinol und arylpiperidin-derivate und sie enthaltende arzneimittel
JP3876254B2 (ja) 2001-09-04 2007-01-31 ベーリンガー インゲルハイム ファルマ ゲゼルシャフト ミット ベシュレンクテル ハフツング ウント コンパニー コマンディトゲゼルシャフト 新規なジヒドロプテリジノン、その製造方法及びその医薬組成物としての使用
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.
WO2003079986A2 (en) 2002-03-18 2003-10-02 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
EP1713773A4 (en) 2004-01-30 2009-09-23 Merck & Co Inc N-BENZYL-3,4-DIHYDROXYPYRIDINE-2-CARBOXYLIC AMID AND N-BENZYL-2,3-DIHYDROXYPYRIDINE-4-CARBOXYLIC AMIDE COMPOUNDS SUITABLE AS INHIBITORS OF THE HIV INTEGRASE
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
EP1765994B1 (en) 2004-06-01 2009-11-18 The University of North Carolina at Chapel Hill Reconstituted histone methyltransferase complex and methods of identifying modulators thereof
AU2006270322A1 (en) * 2005-07-14 2007-01-25 Takeda San Diego, Inc. Histone deacetylase inhibitors
JP2009503014A (ja) 2005-08-03 2009-01-29 ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング 呼吸器系疾患の治療におけるジヒドロプテリジノン
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
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
AU2008206168B2 (en) 2007-01-19 2012-01-19 The Regents Of The University Of Michigan ADRB2 cancer markers
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
WO2009015203A1 (en) 2007-07-23 2009-01-29 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.
US20100261743A1 (en) 2007-12-06 2010-10-14 Glaxosmithkline Llc Novel seh inhibitors and their use
US20090270361A1 (en) 2008-03-26 2009-10-29 Takeda Pharmaceutical Company Limited 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 NEURO PEPTIDE-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
CA2795776A1 (en) 2010-04-06 2011-10-13 Caris Life Sciences Luxembourg Holdings, S.A.R.L. Circulating biomarkers for disease
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
ES2528269T3 (es) * 2010-05-07 2015-02-06 Glaxosmithkline Llc Azaindazoles
ES2534804T3 (es) 2010-05-07 2015-04-28 Glaxosmithkline Llc Indazoles
PH12012502194A1 (en) * 2010-05-07 2014-09-05 Glaxosmithkline Llc Indoles
AU2011291599B2 (en) 2010-08-18 2015-09-10 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers for disease
AU2011298987B2 (en) 2010-09-10 2017-09-28 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
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
AU2012220872A1 (en) 2011-02-22 2013-09-12 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers
EP2681216B1 (en) * 2011-02-28 2017-09-27 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
JO3438B1 (ar) * 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
TW201733984A (zh) * 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
ES2624986T3 (es) * 2011-09-13 2017-07-18 Glaxosmithkline Llc Azaindazoles
EP2760452A4 (en) 2011-09-30 2015-04-01 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
AU2012332297B2 (en) * 2011-11-04 2016-01-07 Glaxosmithkline Intellectual Property (No.2) Limited Method of treatment
WO2013075083A1 (en) * 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals 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
US9085583B2 (en) 2012-02-10 2015-07-21 Constellation—Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TR201904660T4 (tr) 2012-03-12 2019-05-21 Epizyme Inc İnsan EZH2 inhibitörleri ve bunun kullanım yöntemleri.
IL308807B2 (en) 2012-04-13 2025-08-01 Epizyme Inc Combination therapy for treating cancer
DK3184523T3 (da) 2012-04-13 2019-08-19 Epizyme Inc N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl(tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4' -(morphofinomethyl)-[1,1'-biphenyl]-3-carboxamidhydrobromid til anvendelse i behandlingen af en sygdom med celleproliferation i det hæmatologiske system.
WO2013173441A2 (en) 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
US20150239842A1 (en) * 2012-09-28 2015-08-27 Pfizer Inc. Benzamide and heterobenzamide compounds
CN110898067A (zh) 2012-10-15 2020-03-24 Epizyme股份有限公司 癌症治疗方法
PE20150886A1 (es) * 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
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
KR102229478B1 (ko) 2012-11-01 2021-03-18 인피니티 파마슈티칼스, 인코포레이티드 Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료
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
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
KR102219441B1 (ko) 2013-02-11 2021-02-23 콘스텔레이션 파마슈티칼스, 인크. 메틸 변형 효소 조절제, 이의 조성물 및 용도
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
ES2717680T3 (es) * 2013-04-30 2019-06-24 Glaxosmithkline Ip No 2 Ltd Potenciador de inhibidores del homólogo de Zeste 2
US9624205B2 (en) * 2013-07-19 2017-04-18 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

Also Published As

Publication number Publication date
AU2013216721B2 (en) 2017-09-28
EP2812001A4 (en) 2015-09-02
US20150376190A1 (en) 2015-12-31
MX363392B (es) 2019-03-20
US10016405B2 (en) 2018-07-10
EA201591474A1 (ru) 2016-01-29
JP2016507573A (ja) 2016-03-10
JP2015506985A (ja) 2015-03-05
LT2953941T (lt) 2017-09-11
WO2013120104A2 (en) 2013-08-15
SMT201700340T1 (it) 2017-09-07
US20160333016A1 (en) 2016-11-17
US20150259351A1 (en) 2015-09-17
EA029089B1 (ru) 2018-02-28
US9371331B2 (en) 2016-06-21
MX2015010377A (es) 2015-10-29
WO2013120104A3 (en) 2014-03-06
DK2953941T3 (en) 2017-07-24
USRE47428E1 (en) 2019-06-11
JP5989923B2 (ja) 2016-09-07
ES2632241T3 (es) 2017-09-12
BR112015018508B1 (pt) 2021-08-24
AU2013216721A1 (en) 2014-09-04
BR112015018508A2 (pt) 2017-07-18
CA2862289A1 (en) 2013-08-15
UA117362C2 (uk) 2018-07-25
US20170056388A1 (en) 2017-03-02
US9469646B2 (en) 2016-10-18
EA029089B9 (ru) 2019-01-31
EP2812001B1 (en) 2017-06-14
AR094755A1 (es) 2015-08-26
US20190125737A1 (en) 2019-05-02
HRP20171030T1 (hr) 2017-10-06
EP2812001A2 (en) 2014-12-17
US9085583B2 (en) 2015-07-21
CY1119060T1 (el) 2018-01-10
MY172156A (en) 2019-11-15
NZ628762A (en) 2016-07-29
US9980952B2 (en) 2018-05-29
US20150368229A1 (en) 2015-12-24
PT2953941T (pt) 2017-07-13
US20170312262A9 (en) 2017-11-02
US20150011546A1 (en) 2015-01-08
JP5989805B2 (ja) 2016-09-07

Similar Documents

Publication Publication Date Title
CA2862289C (en) Modulators of methyl modifying enzymes, compositions and uses thereof
EP2953941B1 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
EP2970305B1 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
JP2024012558A (ja) Ｓｕｍｏ活性化酵素の阻害薬として有用なヘテロアリール化合物
JP6445574B2 (ja) ブロモドメイン阻害剤
CA3089639C (en) Imidazo[1,2-c]pyrimidinyl compounds as prc2 inhibitors
EP3033334A1 (en) Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
JP2022537285A (ja) ベンゾイソオキサゾールスルホンアミド誘導体
TWI864112B (zh) 一類具有brd4抑制活性的化合物、其製備方法及用途
CA2864672C (en) Pyrazolopyrimidinyl inhibitors of ubiquitin-activating enzyme
JP7406008B2 (ja) Ｃｄｋ９阻害剤としての多環式アミド系誘導体、その調製方法及び用途
HK1218648B (en) Modulators of methyl modifying enzymes, compositions and uses thereof

Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20180110