MX2015010377A - Moduladores de las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos. - Google Patents

Moduladores de las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos.

Info

Publication number
MX2015010377A
MX2015010377A MX2015010377A MX2015010377A MX2015010377A MX 2015010377 A MX2015010377 A MX 2015010377A MX 2015010377 A MX2015010377 A MX 2015010377A MX 2015010377 A MX2015010377 A MX 2015010377A MX 2015010377 A MX2015010377 A MX 2015010377A
Authority
MX
Mexico
Prior art keywords
compositions
modulators
modifying enzymes
methyl modifying
methyl
Prior art date
Application number
MX2015010377A
Other languages
English (en)
Other versions
MX363392B (es
Inventor
Brian K Albrecht
James Edmund Audia
Victor S Gehling
Jean-Christophe Harmange
Rishi G Vaswani
Andrew S Cook
Les A Dakin
Martin Duplessis
Christopher G Nasveschuk
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
Priority claimed from PCT/US2014/015706 external-priority patent/WO2014124418A1/en
Publication of MX2015010377A publication Critical patent/MX2015010377A/es
Publication of MX363392B publication Critical patent/MX363392B/es

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

Abstract

Se proveen en la presente, agentes que tienen la Fórmula estructural (II) (ver Fórmula) para modular las enzimas histonas modificadoras de los metilos, composiciones y sus usos, por ejemplo, como agentes anti-cáncer.
MX2015010377A 2012-02-10 2014-02-11 Moduladores de las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos. MX363392B (es)

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 (2)

Publication Number Publication Date
MX2015010377A true MX2015010377A (es) 2015-10-29
MX363392B MX363392B (es) 2019-03-20

Family

ID=48948171

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2015010377A MX363392B (es) 2012-02-10 2014-02-11 Moduladores de las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos.

Country Status (19)

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

Families Citing this family (59)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2841142C (en) 2010-06-23 2020-12-15 Ryan D. Morin Biomarkers for non-hodgkin lymphomas and uses thereof
WO2013075084A1 (en) 2011-11-18 2013-05-23 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
WO2014124418A1 (en) * 2013-02-11 2014-08-14 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CA2862289C (en) * 2012-02-10 2019-11-26 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2014151142A1 (en) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CN105308038B (zh) 2013-04-30 2018-05-29 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的抑制剂
EP3019494B1 (en) 2013-07-10 2017-06-21 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
AU2015340614B2 (en) * 2014-10-28 2018-07-19 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
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
US20180037568A1 (en) * 2015-02-13 2018-02-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TW201708210A (zh) * 2015-06-30 2017-03-01 葛蘭素史克智慧財產（第二）有限公司 Ｚｅｓｔｅ同源物２增強子之抑制劑
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
US10493076B2 (en) 2015-08-24 2019-12-03 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
CA3000983A1 (en) 2015-10-06 2017-04-13 The Regents Of The University Of Colorado, A Body Corporate 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
CA3011186A1 (en) 2016-01-29 2017-08-03 Epizyme, Inc. Combination therapy for treating cancer
KR20230042756A (ko) 2016-03-15 2023-03-29 오리존 지노믹스 에스.에이. 고형 종양의 치료에 사용하기 위한 lsd1 억제제의 조합물
KR102424709B1 (ko) 2016-05-31 2022-07-22 칼비스타 파마슈티컬즈 리미티드 혈장 칼리크레인 저해제로서 피라졸 유도체
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
US11147819B2 (en) 2016-06-17 2021-10-19 Epizyme, Inc. EZH2 inhibitors for treating cancer
CA3039059A1 (en) 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
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
AU2018210141A1 (en) 2017-01-20 2019-08-29 Constellation Pharmaceuticals, Inc. Solid dispersions of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
US11642346B2 (en) 2017-03-31 2023-05-09 Epizyme, Inc. Combination therapy for treating cancer
US20230201212A1 (en) 2017-06-13 2023-06-29 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
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
US11529344B2 (en) 2017-11-14 2022-12-20 Pfizer Inc. EZH2 inhibitor combination therapies
GB201719881D0 (en) 2017-11-29 2018-01-10 Kalvista Pharmaceuticals Ltd Solid forms of plasma kallikrein inhibitor and salts thereof
HUE057912T2 (hu) 2017-11-29 2022-06-28 Kalvista Pharmaceuticals Ltd Plazma kallikrein inhibitort tartalmazó dózisformák
WO2019133674A1 (en) 2017-12-28 2019-07-04 Constellation Pharmaceuticals, Inc. Pharmacokinetic enhancement of ezh2 inhibitors through combination therapies
CA3089639A1 (en) 2018-01-31 2019-08-08 Mirati Therapeutics, Inc. Imidazo[1,2-c]pyrimidinyl compounds as prc2 inhibitors
EP3765458B1 (en) 2018-03-14 2023-01-11 Biogen MA Inc. O-glycoprotein-2-acetamido-2-deoxy-3-d-glycopyranosidase inhibitors
BR112020021194A2 (pt) * 2018-04-18 2021-03-23 Constallation Pharmaceuticals, Inc. moduladores de enzimas modificadoras de metila, composições e usos dos mesmos
WO2020011607A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
SG11202102379XA (en) 2018-09-19 2021-04-29 Biogen Ma Inc O-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
US20200131156A1 (en) * 2018-10-30 2020-04-30 H. Lundbeck A/S ARYLSULFONYLPYROLECARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS
TW202039482A (zh) 2018-12-05 2020-11-01 美商百健Ｍａ公司 嗎啉基、哌嗪基、氧氮雜環庚烷基及二氮雜環庚烷基o-醣蛋白-2-乙醯胺基-2-去氧-3-d-葡萄哌喃醣苷酶抑制劑
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
US20220259197A1 (en) 2019-03-08 2022-08-18 Biogen Ma Inc. Azetidinyl o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
EP4010333A1 (en) 2019-08-09 2022-06-15 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
KR20220066892A (ko) 2019-08-22 2022-05-24 주노 쎄러퓨티크스 인코퍼레이티드 Ｔ 세포 요법 및 제스트 동족체 2의 인핸서 (ｅｚｈ2) 억제제의 병용 요법 및 관련 방법
UY38934A (es) 2019-10-29 2021-05-31 Biogen Ma Inc Inhibidores de o-glucoproteína-2-acetamido-2-deoxi-3-d-glucopiranosidasa espirocíclica
IL300365A (en) 2020-08-03 2023-04-01 Biogen Ma Inc Crystal forms of O-glycoprotein-2-acetamido-2-deoxy-3-D-glucopyranosidase inhibitor
WO2022150962A1 (en) 2021-01-12 2022-07-21 Westlake Pharmaceutical (Hangzhou) Co., Ltd. Protease inhibitors, preparation, and uses thereof

Family Cites Families (74)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE52670B1 (en) 1981-03-03 1988-01-20 Leo Ab Heterocyclic carboxamides,compositions containing such compounds,and processes for their preparation
US5308854A (en) 1990-06-18 1994-05-03 Merck & Co., Inc. Inhibitors of HIV reverse transcriptase
ES2225979T3 (es) 1996-07-22 2005-03-16 Daiichi Suntory Pharma Co., Ltd. Derivados de arilpiperidinol y de arilpiperidina y farmacos que los contienen.
WO2003020722A1 (de) 2001-09-04 2003-03-13 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neue dihydropteridinone, verfahren zu deren herstellung und deren verwendung als arzneimittel
US6897220B2 (en) 2001-09-14 2005-05-24 Methylgene, Inc. Inhibitors of histone deacetylase
MXPA03000145A (es) 2002-01-07 2003-07-15 Pfizer Compuestos de oxo u oxi-piridina como moduladores de receptores 5-ht4.
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
CA2554120A1 (en) 2004-01-30 2005-08-18 Merck & Co., Inc. N-benzyl-3,4-dihydroxypyridine-2-carboxamide and n-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as hiv integras inhibitors
MXPA06012333A (es) 2004-04-30 2007-01-17 Takeda Pharmaceutical Compuesto de amida heterociclico y uso del mismo como un inhibidor mmp-13.
WO2005118796A2 (en) 2004-06-01 2005-12-15 The University Of North Carolina At Chapel Hill Reconstituted histone methyltransferase complex and methods of identifying modulators thereof
ZA200800901B (en) * 2005-07-14 2010-05-26 Takeda San Diego Inc Histone deacetylase inhibitors
EP1915155A1 (en) 2005-08-03 2008-04-30 Boehringer Ingelheim International GmbH Dihydropteridinones in the treatment of respiratory diseases
EP1960547A2 (en) 2005-12-08 2008-08-27 Novartis AG Effects of inhibitors of fgfr3 on gene transcription
US8053435B2 (en) 2006-11-03 2011-11-08 Korea Research Institute Of Chemical Technology Naphthalenyloxypropenyl derivatives having inhibitory activity against histone deacetylase and pharmaceutical composition comprising the same
AU2008206168B2 (en) 2007-01-19 2012-01-19 The Regents Of The University Of Michigan ADRB2 cancer markers
EP2114898A2 (en) 2007-02-16 2009-11-11 Amgen Inc. Nitrogen-containing heterocyclyl ketones and their use as c-met inhibitors
US8030344B2 (en) 2007-03-13 2011-10-04 Methylgene Inc. Inhibitors of histone deacetylase
WO2009006577A2 (en) 2007-07-03 2009-01-08 The Regents Of The University Of Michigan Compositions and methods for inhibiting ezh2
US20100298270A1 (en) 2007-07-23 2010-11-25 Syndax Pharmaceuticals, Inc. Novel Compounds and Methods of Using Them
FR2922209B1 (fr) 2007-10-12 2010-06-11 Sanofi Aventis 5,6-DIARYLES PYRIDINES SUBSTITUES EN POSITION 2 et 3, LEUR PREPARATION ET LEUR APPLICATION EN THERAPEUTIQUE.
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
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
AU2011237669B2 (en) 2010-04-06 2016-09-08 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers for disease
US8575203B2 (en) 2010-04-21 2013-11-05 Boehringer Ingelheim International Gmbh Chemical compounds
EP2566327B1 (en) * 2010-05-07 2017-03-29 Glaxosmithkline LLC Indoles
EP2566479B1 (en) 2010-05-07 2014-12-24 GlaxoSmithKline LLC Azaindazoles
WO2011140325A1 (en) 2010-05-07 2011-11-10 Glaxosmithkline Llc Indazoles
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
KR102061353B1 (ko) * 2010-09-10 2020-01-02 에피자임, 인코포레이티드 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
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
WO2012075080A1 (en) 2010-12-01 2012-06-07 Glaxosmithkline Llc Indoles
WO2012115885A1 (en) 2011-02-22 2012-08-30 Caris Life Sciences Luxembourg Holdings, S.A.R.L. Circulating biomarkers
EP2681216B1 (en) * 2011-02-28 2017-09-27 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
JO3438B1 (ar) 2011-04-13 2019-10-20 Epizyme Inc مركبات بنزين مستبدلة بأريل أو أريل غير متجانس
EP2755962B1 (en) * 2011-09-13 2017-03-01 Glaxosmithkline LLC Azaindazoles
CN103987842A (zh) 2011-09-30 2014-08-13 葛兰素史密斯克莱有限责任公司 治疗癌症的方法
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
WO2013067302A1 (en) * 2011-11-04 2013-05-10 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
CA2862289C (en) * 2012-02-10 2019-11-26 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2014124418A1 (en) 2013-02-11 2014-08-14 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EP2825161B1 (en) 2012-03-12 2019-01-02 Epizyme, Inc. Inhibitors of human ezh2, and methods of use thereof
CN104768555B (zh) 2012-04-13 2018-10-30 Epizyme股份有限公司 用于治疗癌症的联合治疗
LT3184523T (lt) 2012-04-13 2020-02-10 Epizyme Inc N-((4,6-dimetil-2-okso-1,2-dihidropiridin-3-il)metil)-5-(etil (tetrahidro-2h-piran-4-il)amino)-4-metil-4'-(morfolinometil)-[1,1'-bifenil]-3-karboksamido hidrobromidas, skirtas naudoti hematologinės sistemos proliferacinio sutrikimo gydymui
WO2013173441A2 (en) * 2012-05-16 2013-11-21 Glaxosmithkline Llc Enhancer of zeste homolog 2 inhibitors
EP2900653A1 (en) * 2012-09-28 2015-08-05 Pfizer Inc. Benzamide and heterobenzamide compounds
TWI588131B (zh) * 2012-10-15 2017-06-21 雅酶股份有限公司 經取代苯化合物
RU2018145311A (ru) 2012-10-15 2019-02-18 Эпизайм, Инк. Способы лечения рака
CN103794728A (zh) 2012-10-30 2014-05-14 中国科学院长春光学精密机械与物理研究所 高导电性有机透明导电薄膜的制备方法
ES2691742T5 (es) 2012-11-01 2022-03-18 Infinity Pharmaceuticals Inc Tratamiento de cánceres utilizando moduladores de isoformas de PI3 cinasa
WO2014077784A1 (en) 2012-11-19 2014-05-22 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
WO2014100080A1 (en) 2012-12-19 2014-06-26 Glaxosmithkline Llc Combination
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
WO2014151142A1 (en) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
CN105308038B (zh) * 2013-04-30 2018-05-29 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的抑制剂
WO2015010078A2 (en) * 2013-07-19 2015-01-22 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

Also Published As

Publication number Publication date
US9085583B2 (en) 2015-07-21
MX363392B (es) 2019-03-20
US20170056388A1 (en) 2017-03-02
US20190125737A1 (en) 2019-05-02
CA2862289A1 (en) 2013-08-15
JP5989805B2 (ja) 2016-09-07
UA117362C2 (uk) 2018-07-25
JP5989923B2 (ja) 2016-09-07
CA2862289C (en) 2019-11-26
NZ628762A (en) 2016-07-29
US9980952B2 (en) 2018-05-29
MY172156A (en) 2019-11-15
US20160333016A1 (en) 2016-11-17
ES2632241T3 (es) 2017-09-12
BR112015018508A2 (pt) 2017-07-18
US9371331B2 (en) 2016-06-21
PT2953941T (pt) 2017-07-13
EA201591474A1 (ru) 2016-01-29
EP2812001A2 (en) 2014-12-17
HRP20171030T1 (hr) 2017-10-06
US20170312262A9 (en) 2017-11-02
DK2953941T3 (en) 2017-07-24
BR112015018508B1 (pt) 2021-08-24
AU2013216721A1 (en) 2014-09-04
LT2953941T (lt) 2017-09-11
US20150368229A1 (en) 2015-12-24
AU2013216721B2 (en) 2017-09-28
JP2016507573A (ja) 2016-03-10
WO2013120104A2 (en) 2013-08-15
CY1119060T1 (el) 2018-01-10
US20150376190A1 (en) 2015-12-31
JP2015506985A (ja) 2015-03-05
US20150011546A1 (en) 2015-01-08
EP2812001B1 (en) 2017-06-14
AR094755A1 (es) 2015-08-26
EP2812001A4 (en) 2015-09-02
EA029089B1 (ru) 2018-02-28
WO2013120104A3 (en) 2014-03-06
EA029089B9 (ru) 2019-01-31
US20150259351A1 (en) 2015-09-17
USRE47428E1 (en) 2019-06-11
US9469646B2 (en) 2016-10-18
US10016405B2 (en) 2018-07-10

Similar Documents

Publication Publication Date Title
MY172156A (en) Modulators of methyl modifying enzymes, compositions and uses thereof
PH12015501720A1 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013075083A8 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
WO2013075084A8 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
WO2015023915A8 (en) Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof
WO2012068589A3 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
MX2015003874A (es) Modulacion de ire1.
PH12014502697B1 (en) New diazaspirocycloalkane and azaspirocycloalkane
TW201611725A (en) Pest control agent
PH12015501393A1 (en) Pesticidal compositions and processes related thereto
MX2013002417A (es) Composiciones pesticidas.
EA201590292A1 (ru) Соединения, которые являются sip-модулирующими агентами и/или atx-модулирующими агентами
TR201900038T4 (tr) GPR6'nın tetrahidropiridopirazin modülatörleri.
MX340831B (es) Composiciones pesticidas.
AU2013225533A8 (en) Amido spirocyclic amide and sulfonamide derivatives
IN2015DN03029A (es)
MX2014014832A (es) Pirrolopirimidona y pirrolopiridona, inhibidores de tanquirasa.
MX364069B (es) Moduladores de la proteína activadora de 5-lipoxigenasa.
MX2016014179A (es) Derivados quinazolindiona farcologicamente activos.
CA2875305C (en) Fbxo3 inhibitors
WO2014097318A3 (en) Agents for eliminating tumour-initiating cells
MX2015006419A (es) Tratamiento de la intolerancia al gluten y padecimientos relacionados.
UA70698U (ru) Применение 2-метил-3-фениламинометилхинолин-4-она как противогипоксического, актопротекторного и антиалкогольного средства
UA72478U (ru) Применение полентара как средства фригопротекторного действия
UA80618U (en) Use of n-steroylethanolamine as radiomodifier