BR112015018508B1 - Composto de fórmula estrutural ii, seu uso e composição farmacêutica - Google Patents

Composto de fórmula estrutural ii, seu uso e composição farmacêutica Download PDF

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Publication number
BR112015018508B1
BR112015018508B1 BR112015018508-8A BR112015018508A BR112015018508B1 BR 112015018508 B1 BR112015018508 B1 BR 112015018508B1 BR 112015018508 A BR112015018508 A BR 112015018508A BR 112015018508 B1 BR112015018508 B1 BR 112015018508B1
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BR
Brazil
Prior art keywords
methyl
compound
mmol
compounds
piperidin
Prior art date
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BR112015018508-8A
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English (en)
Portuguese (pt)
Other versions
BR112015018508A2 (pt
Inventor
Brian K. Albrecht
James Edmund Audia
Andrew S. Cook
Les A. Dakin
Martin Duplessis
Victor S. Gehling
Jean-Christophe Harmange
Christopher G. Nasveschuk
Rischi G. Vaswani
Original Assignee
Constellation Pharmaceuticals, Inc
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Publication date
Application filed by Constellation Pharmaceuticals, Inc filed Critical Constellation Pharmaceuticals, Inc
Priority claimed from PCT/US2014/015706 external-priority patent/WO2014124418A1/en
Publication of BR112015018508A2 publication Critical patent/BR112015018508A2/pt
Publication of BR112015018508B1 publication Critical patent/BR112015018508B1/pt

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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Dermatology (AREA)
  • Pulmonology (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Biomedical Technology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Hydrogenated Pyridines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
BR112015018508-8A 2012-02-10 2014-02-11 Composto de fórmula estrutural ii, seu uso e composição farmacêutica BR112015018508B1 (pt)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201261597695P 2012-02-10 2012-02-10
US201261667821P 2012-07-03 2012-07-03
USPCT/US2013/025639 2013-02-11
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 (2)

Publication Number Publication Date
BR112015018508A2 BR112015018508A2 (pt) 2017-07-18
BR112015018508B1 true BR112015018508B1 (pt) 2021-08-24

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ID=48948171

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Application Number Title Priority Date Filing Date
BR112015018508-8A BR112015018508B1 (pt) 2012-02-10 2014-02-11 Composto de fórmula estrutural ii, seu uso e composição farmacêutica

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
WO2011160206A1 (en) 2010-06-23 2011-12-29 Morin Ryan D Biomarkers for non-hodgkin lymphomas and uses thereof
US9051269B2 (en) 2011-11-18 2015-06-09 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
JP5989805B2 (ja) 2012-02-10 2016-09-07 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． メチル基変更酵素の調節物質、組成物及びその使用
CA2887243C (en) 2012-10-15 2024-04-09 Epizyme, Inc. Methods of treating cancer
MA38341B1 (fr) * 2013-02-11 2018-11-30 Constellation Pharmaceuticals Inc Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2014177982A1 (en) 2013-04-30 2014-11-06 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
AU2014288839B2 (en) 2013-07-10 2017-02-02 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
US9969716B2 (en) * 2013-08-15 2018-05-15 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
US20170217941A1 (en) * 2014-06-25 2017-08-03 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds
BR112017008840A2 (pt) * 2014-10-28 2017-12-19 Glaxosmithkline Ip No 2 Ltd intensificador de inibidores do homólogo 2 de zeste
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
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
US20180214519A1 (en) 2015-07-24 2018-08-02 Constellation Pharmaceuticals, Inc. Combination therapies for modulation of histone methyl modifying enzymes
WO2017023671A1 (en) 2015-08-03 2017-02-09 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
KR20180042356A (ko) 2015-08-24 2018-04-25 에피자임, 인코포레이티드 암 치료 방법
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
MX394355B (es) 2015-10-06 2025-03-24 Epizyme Inc Método de tratamiento de meduloblastoma con un inhibidor de ezh2.
EP3371601A1 (en) 2015-11-05 2018-09-12 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
ES3057783T3 (en) 2016-03-15 2026-03-04 Oryzon Genomics Sa Combinations of lsd1 inhibitors for use in the treatment of neoplastic diseases
DK3464271T3 (da) 2016-05-31 2020-06-15 Kalvista Pharmaceuticals Ltd Pyrazolderivater som plasma-kallikreininhibitorer
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
EP3471830A4 (en) 2016-06-17 2020-02-26 Epizyme Inc EZH2 INHIBITORS TO TREAT CANCER
CN109843870A (zh) * 2016-10-19 2019-06-04 星座制药公司 Ezh2抑制剂的合成
EP3548032A2 (en) 2016-12-02 2019-10-09 Epizyme, Inc. Combination therapy for treating cancer
US20190381025A1 (en) * 2017-01-20 2019-12-19 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
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
BR112020008325A2 (pt) 2017-11-14 2020-10-20 Pfizer Inc. terapias de combinação com o inibidor de ezh2
PT3716952T (pt) 2017-11-29 2022-04-14 Kalvista Pharmaceuticals Ltd Formas de administração que incluem um inibidor de calicreína plasmática
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
MX2020007974A (es) 2018-01-31 2020-09-07 Mirati Therapeutics Inc Inhibidores de complejo represivo polycomb 2 (prc2).
JP7453916B2 (ja) 2018-03-14 2024-03-21 バイオジェン・エムエイ・インコーポレイテッド Ｏ－糖タンパク質－２－アセトアミド－２－デオキシ－３－ｄ－グリコピラノシダーゼ阻害剤
HRP20240793T1 (hr) 2018-04-18 2024-09-13 Constellation Pharmaceuticals, Inc. Modulatori enzima koji modificiraju metil, njihovi pripravci i upotreba
EP3823671B1 (en) 2018-07-09 2024-02-07 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
US12180205B2 (en) 2018-09-19 2024-12-31 Biogen Ma Inc. O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
AR116898A1 (es) * 2018-10-30 2021-06-23 H Lundbeck As DERIVADOS DE ARILSULFONILPIRROLCARBOXAMIDA COMO ACTIVADORES DE CANALES DE POTASIO Kv3
ES2968733T3 (es) 2018-12-05 2024-05-13 Biogen Ma Inc Derivados morfolinilo, piperazinilo, oxazepanilo y diazepanilo útiles como inhibidores de o-glicoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidasa
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
JP7504898B2 (ja) 2019-02-04 2024-06-24 バイオジェン・エムエイ・インコーポレイテッド 二環式エーテル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
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
EP3980422A1 (en) 2019-06-05 2022-04-13 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer
LT4003532T (lt) 2019-07-24 2024-11-11 Constellation Pharmaceuticals, Inc. 7-chlor-2- (4-(3-metoksiazetidin-1-il)cikloheksil)-2,4-dimetil-n-((6-metil-4-(metiltio)-2-okso-1,2-dihidropiridin-3-il)metil)benzo[d][1,3]dioksol-5-karboksamido kristalinės formos
MX2022000933A (es) * 2019-07-24 2022-05-06 Constellation Pharmaceuticals Inc Inhibición de ezh2 en tratamientos combinados para el tratamiento del cáncer.
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
CN114555112A (zh) 2019-08-22 2022-05-27 朱诺治疗学股份有限公司 T细胞疗法和zeste增强子同源物2(ezh2)抑制剂的组合疗法及相关方法
AR120324A1 (es) 2019-10-29 2022-02-09 Biogen Ma Inc Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica
WO2022031701A1 (en) 2020-08-03 2022-02-10 Biogen Ma Inc. Crystaline forms of an 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
IL308348A (en) 2021-05-20 2024-01-01 Sironax Ltd RIP1 modulators including cyclic ureas aztidine, their preparation and uses
WO2023115203A1 (en) * 2021-12-20 2023-06-29 Fairhaven Pharmaceuticals Inc. Oxer1 antagonists 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
AU710594B2 (en) 1996-07-22 1999-09-23 Asubio Pharma Co., Ltd. Arylpiperidinol and arylpiperidine derivatives and pharmaceuticals containing the same
UA76512C2 (en) 2001-09-04 2006-08-15 Boehringer Ingelheim Pharma Dihydropteridinones, a method for producing thereof and use thereof as medicament
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.
US7101883B2 (en) 2002-03-18 2006-09-05 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of TNF-α 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
WO2005074513A2 (en) 2004-01-30 2005-08-18 Merck & Co., Inc. N-benzyl-3,4-dihyroxypyridine-2-carboxamide and n-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as hiv integrase inhibitors
ZA200609259B (en) 2004-04-30 2008-07-30 Takeda Pharmaceutical Heterocyclic amide compound and use thereof as an mmp-13 inhibitor
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
EA200800321A1 (ru) * 2005-07-14 2008-06-30 Такеда Сан Диего, Инк. Ингибиторы гистондеацетилазы
CA2617589A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Dihydropteridinones in the treatment of respiratory diseases
KR20080080525A (ko) 2005-12-08 2008-09-04 노파르티스 아게 유전자 전사에 대한 ｆｇｆｒ３의 억제제의 효과
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
MX2009008531A (es) 2007-02-16 2009-08-26 Amgen Inc Cetonas de heterociclilo que contienen nitrogeno y su uso como inhibidores de c-met.
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
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.
EP2224928A4 (en) 2007-12-06 2012-02-15 Glaxosmithkline Llc NOVEL INHIBITORS OF SEH AND THEIR USE
PE20091653A1 (es) * 2008-03-26 2009-11-14 Takeda Pharmaceutical Derivados sustituidos de pirazol y su uso
CA2725481A1 (en) 2008-06-18 2009-12-23 Pfizer Limited Nicotinamide derivatives
US8389720B2 (en) 2008-11-13 2013-03-05 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
JP2013526852A (ja) 2010-04-06 2013-06-27 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 疾患に対する循環バイオマーカー
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
EA023788B1 (ru) * 2010-05-07 2016-07-29 ГЛЭКСОСМИТКЛАЙН ЭлЭлСи Производные индола и фармацевтические композиции на их основе
JP5864546B2 (ja) 2010-05-07 2016-02-17 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 インダゾール
WO2012005805A1 (en) 2010-05-07 2012-01-12 Glaxosmithkline Llc Azaindazoles
CA2808417A1 (en) 2010-08-18 2012-02-23 Caris Life Sciences Luxembourg Holdings, S.A.R.L. Circulating biomarkers for disease
US9175331B2 (en) 2010-09-10 2015-11-03 Epizyme, Inc. Inhibitors of human EZH2, and methods of use thereof
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
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
EP2646020B1 (en) * 2010-12-01 2016-09-21 Glaxosmithkline LLC Indoles
EP2678448A4 (en) 2011-02-22 2014-10-01 Caris Life Sciences Luxembourg Holdings S A R L CIRCULATING BIOMARKERS
WO2012118812A2 (en) 2011-02-28 2012-09-07 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
TW201733984A (zh) * 2011-04-13 2017-10-01 雅酶股份有限公司 經取代之苯化合物
JO3363B1 (ar) * 2011-04-13 2019-03-13 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
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
CN104039956A (zh) 2011-11-04 2014-09-10 葛兰素史密斯克莱知识产权（第2号）有限公司 治疗方法
WO2013067300A1 (en) * 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
WO2013067302A1 (en) * 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
EP2780014A4 (en) 2011-11-18 2015-07-01 Constellation Pharmaceuticals Inc MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
US9051269B2 (en) 2011-11-18 2015-06-09 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
JP5989805B2 (ja) * 2012-02-10 2016-09-07 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． メチル基変更酵素の調節物質、組成物及びその使用
RU2704445C2 (ru) 2012-03-12 2019-10-28 Эпизайм, Инк. Ингибиторы ezh2 человека и способы их применения
US9394283B2 (en) 2012-04-13 2016-07-19 Epizyme, Inc. Salt form of a human histone methyltransferase EZH2 inhibitor
SG10201608579UA (en) 2012-04-13 2016-12-29 Epizyme Inc Combination therapy for treating cancer
US9562041B2 (en) 2012-05-16 2017-02-07 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
CA2884848C (en) * 2012-09-28 2017-08-22 Pfizer Inc. Benzamide and heterobenzamide compounds
PE20150887A1 (es) 2012-10-15 2015-06-04 Epizyme Inc Compuestos de benceno sustituidos
CA2887243C (en) 2012-10-15 2024-04-09 Epizyme, Inc. Methods of treating cancer
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
AU2013337717B2 (en) 2012-11-01 2018-10-25 Infinity Pharmaceuticals, Inc. Treatment of cancers using PI3 kinase isoform modulators
US9889180B2 (en) 2012-11-19 2018-02-13 Agency For Science, Technology And Research Method of treating cancer
US20150292030A1 (en) 2012-11-27 2015-10-15 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
MA38341B1 (fr) 2013-02-11 2018-11-30 Constellation Pharmaceuticals Inc Modulateurs d'enzymes de modification par méthylation, compositions et utilisations associées
US9745305B2 (en) 2013-03-15 2017-08-29 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2014177982A1 (en) * 2013-04-30 2014-11-06 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
EP3022195A2 (en) * 2013-07-19 2016-05-25 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
US9969716B2 (en) 2013-08-15 2018-05-15 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
US20170217941A1 (en) * 2014-06-25 2017-08-03 Epizyme, Inc. Substituted benzene and 6,5-fused bicyclic heteroaryl compounds

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