CY1119060T1 - Ρυθμιστες ενζυμων μεθυλικης τροποποιησης, συνθεσεις και χρησεις αυτων - Google Patents

Ρυθμιστες ενζυμων μεθυλικης τροποποιησης, συνθεσεις και χρησεις αυτων

Info

Publication number
CY1119060T1
CY1119060T1 CY20171100718T CY171100718T CY1119060T1 CY 1119060 T1 CY1119060 T1 CY 1119060T1 CY 20171100718 T CY20171100718 T CY 20171100718T CY 171100718 T CY171100718 T CY 171100718T CY 1119060 T1 CY1119060 T1 CY 1119060T1
Authority
CY
Cyprus
Prior art keywords
compositions
methodological
modification
methods
agents
Prior art date
Application number
CY20171100718T
Other languages
English (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
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
Priority claimed from PCT/US2014/015706 external-priority patent/WO2014124418A1/en
Application filed by Constellation Pharmaceuticals, Inc. filed Critical Constellation Pharmaceuticals, Inc.
Publication of CY1119060T1 publication Critical patent/CY1119060T1/el

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

Στο παρόν παρέχονται, παράγοντες που έχουν το δομικό χημικό τύπο (II) για τη ρύθμιση ενζύμων τροποποίησης του μεθυλίου της ιστόνης, συνθέσεις και χρήσεις αυτών, για παράδειγμα ως αντικαρκινικοί παράγοντες.
CY20171100718T 2012-02-10 2017-07-05 Ρυθμιστες ενζυμων μεθυλικης τροποποιησης, συνθεσεις και χρησεις αυτων CY1119060T1 (el)

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 (1)

Publication Number Publication Date
CY1119060T1 true CY1119060T1 (el) 2018-01-10

Family

ID=48948171

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20171100718T CY1119060T1 (el) 2012-02-10 2017-07-05 Ρυθμιστες ενζυμων μεθυλικης τροποποιησης, συνθεσεις και χρησεις αυτων

Country Status (19)

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

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
US9085583B2 (en) 2012-02-10 2015-07-21 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
EA030196B1 (ru) 2013-04-30 2018-07-31 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Ингибиторы энхансера zeste гомолога 2
WO2015004618A1 (en) 2013-07-10 2015-01-15 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
TWI636047B (zh) 2013-08-14 2018-09-21 英商卡爾維斯塔製藥有限公司 雜環衍生物
WO2015023915A1 (en) * 2013-08-15 2015-02-19 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
AU2015340614B2 (en) * 2014-10-28 2018-07-19 Glaxosmithkline Intellectual Property (No.2) Limited Enhancer of zeste homolog 2 inhibitors
GB201421085D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd New enzyme inhibitors
GB201421083D0 (en) 2014-11-27 2015-01-14 Kalvista Pharmaceuticals Ltd Enzyme inhibitors
TW201636344A (zh) 2014-12-05 2016-10-16 美國禮來大藥廠 Ｅｚｈ２抑制劑
WO2016130396A1 (en) * 2015-02-13 2016-08-18 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
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
EP3331561A1 (en) 2015-08-03 2018-06-13 Constellation Pharmaceuticals, Inc. Ezh2 inhibitors and modulation of regulatory t-cell function
WO2017025493A1 (en) * 2015-08-12 2017-02-16 Bayer Pharma Aktiengesellschaft Quinoline ezh2 inhibitors
CN108025191A (zh) 2015-08-24 2018-05-11 Epizyme股份有限公司 治疗癌症的方法
TW201718598A (zh) 2015-08-27 2017-06-01 美國禮來大藥廠 Ｅｚｈ２抑制劑
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
KR20180058829A (ko) 2015-10-06 2018-06-01 에피자임, 인코포레이티드 Ezh2 억제제로 수모세포종을 치료하는 방법
WO2017079738A1 (en) 2015-11-05 2017-05-11 Epizyme, Inc. Flow cytometry for monitoring histone h3 methylation status
EP3407978A4 (en) 2016-01-29 2020-01-15 Epizyme Inc COMBINATION THERAPY FOR TREATING CANCER
CA3017411A1 (en) 2016-03-15 2017-09-21 Oryzon Genomics, S.A. Combinations of lsd1 inhibitors for use in the treatment of solid tumors
ME03794B (me) 2016-05-31 2021-04-20 Kalvista Pharmaceuticals Ltd Derivati pirazola kao inhibitori kalikreina plazme
GB201609603D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-[(6-cyano-2-fluoro-3-methoxyphenyl)Methyl]-3-(methoxymethyl)-1-({4-[(2-ox opyridin-1-YL)Methyl]phenyl}methyl)pyrazole-4-carboxamide
GB201609607D0 (en) 2016-06-01 2016-07-13 Kalvista Pharmaceuticals Ltd Polymorphs of N-(3-Fluoro-4-methoxypyridin-2-yl)methyl)-3-(methoxymethyl)-1-({4-((2-oxopy ridin-1-yl)methyl)phenyl}methyl)pyrazole-4-carboxamide and salts
US11147819B2 (en) 2016-06-17 2021-10-19 Epizyme, Inc. EZH2 inhibitors for treating cancer
CA3039059A1 (en) * 2016-10-19 2018-04-26 Constellation Pharmaceuticals, Inc. Synthesis of inhibitors of ezh2
AU2017367768A1 (en) 2016-12-02 2019-07-18 Epizyme, Inc. Combination therapy for treating cancer
JP2020506905A (ja) * 2017-01-20 2020-03-05 コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． （ｒ）−ｎ−（（４−メトキシ−６−メチル−２−オキソ−１，２−ジヒドロピリジン−３−イル）メチル）−２−メチル−１−（１−（１−（２，２，２−トリフルオロエチル）ピペリジン−４−イル）エチル）−１ｈ−インドール−３−カルボキサミド固体分散液
US10266542B2 (en) 2017-03-15 2019-04-23 Mirati Therapeutics, Inc. EZH2 inhibitors
WO2018183885A1 (en) 2017-03-31 2018-10-04 Epizyme, Inc. Combination therapy for treating cancer
WO2018231973A1 (en) 2017-06-13 2018-12-20 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
US20210161883A1 (en) 2017-07-10 2021-06-03 Constellation Pharmaceuticals, Inc. Ezh2 inhibitor-induced gene expression
US11459315B2 (en) 2017-11-09 2022-10-04 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
AU2018369841A1 (en) 2017-11-14 2020-05-07 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
LT3716952T (lt) 2017-11-29 2022-04-11 Kalvista Pharmaceuticals Limited Vaisto formos, apimančios plazmos kalikreino inhibitorių
US20210000815A1 (en) 2017-12-28 2021-01-07 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
AU2019234759A1 (en) 2018-03-14 2020-09-17 Biogen Ma Inc. O-glycoprotein-2-acetamido-2-deoxy-3-D-glycopyranosidase inhibitors
EP3781561B1 (en) * 2018-04-18 2024-03-13 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
WO2020011607A1 (en) 2018-07-09 2020-01-16 Fondation Asile Des Aveugles Inhibition of prc2 subunits to treat eye disorders
BR112021004739A2 (pt) 2018-09-19 2021-06-01 Biogen Ma Inc. inibidores de o-glicoproteína-2-acetamido-2-desoxi-3-d-glucopiranosidase
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
MA54384A (fr) 2018-12-05 2021-10-13 Biogen Ma Inc Inhibiteurs de morpholinyle, de pipérazinyle, d'oxazépanyle et de diazépanyle o-glycoprotéine-2-acétamido-2-désoxy-3-d-glucopyranosidase
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
JP2022519639A (ja) 2019-02-04 2022-03-24 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
WO2020185593A1 (en) 2019-03-08 2020-09-17 Biogen Ma Inc. Azetidinyl 0-glyc0pr0tein-2-acetamid0-2-deoxy-3-d-gluc0pyran0sidase inhibitors
WO2021028645A1 (en) 2019-08-09 2021-02-18 Kalvista Pharmaceuticals Limited Plasma kallikrein inhibitors
WO2021035194A1 (en) 2019-08-22 2021-02-25 Juno Therapeutics, Inc. Combination therapy of a t cell therapy and an enhancer of zeste homolog 2 (ezh2) inhibitor and related methods
WO2021086966A1 (en) 2019-10-29 2021-05-06 Biogen Ma Inc. Spirocyclic o-glycoprotein-2-acetamido-2-deoxy-3-d-glucopyranosidase inhibitors
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

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
KR100537843B1 (ko) 1996-07-22 2006-04-28 다이이치 아스비오파마 가부시키가이샤 아릴피페리디놀및아릴피페리딘유도체및이들을함유하는약제
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.
AU2003220401A1 (en) 2002-03-18 2003-10-08 Bristol-Myers Squibb Company Uracil derivatives as inhibitors of tnf-alpha converting enzyme (tace) and matrix metalloproteinases
TWI319387B (en) 2002-04-05 2010-01-11 Astrazeneca Ab Benzamide derivatives
TW200500341A (en) 2002-11-12 2005-01-01 Astrazeneca Ab Novel compounds
AU2005211349A1 (en) 2004-01-30 2005-08-18 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-benzyl-3,4-dihyroxypyridine-2-carboxamide and N-benzyl-2,3-dihydroxypyridine-4-carboxamide compounds useful as HIV integrase inhibitors
US9212149B2 (en) 2004-04-30 2015-12-15 Takeda Pharmaceutical Company Limited Substituted 2-amidoquinazol-4-ones as matrix metalloproteinase-13 inhibitors
US7563589B2 (en) 2004-06-01 2009-07-21 The University Of North Carolina At Chapel Hill Reconstituted histone methyltransferase complex and methods of identifying modulators thereof
EP1904452A2 (en) * 2005-07-14 2008-04-02 Takeda San Diego, Inc. Histone deacetylase inhibitors
WO2007014838A1 (en) 2005-08-03 2007-02-08 Boehringer Ingelheim International Gmbh Dihydropteridinones in the treatment of respiratory diseases
BRPI0619548A2 (pt) 2005-12-08 2011-10-04 Novartis Ag efeitos inibidores de fgfr3 em transcrição de gene
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
US8058003B2 (en) 2007-01-19 2011-11-15 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
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.
WO2009073772A1 (en) 2007-12-06 2009-06-11 Smithkline Beecham Corporation Novel seh inhibitors and their use
AR071069A1 (es) 2008-03-26 2010-05-26 Takeda Pharmaceutical Derivados sustituidos de pirazol y su uso para la prevencion o el tratamiento de cancer
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
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
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
US8846935B2 (en) 2010-05-07 2014-09-30 Glaxosmithkline Llc Indazoles
EP2566479B1 (en) 2010-05-07 2014-12-24 GlaxoSmithKline LLC Azaindazoles
SI2566327T1 (sl) 2010-05-07 2017-07-31 Glaxosmithkline Llc Indoli
AU2011291599B2 (en) 2010-08-18 2015-09-10 Caris Life Sciences Switzerland Holdings Gmbh Circulating biomarkers for disease
KR102061353B1 (ko) * 2010-09-10 2020-01-02 에피자임, 인코포레이티드 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
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
US8765792B2 (en) 2010-12-01 2014-07-01 Glaxosmithkline Llc Indoles
WO2012115885A1 (en) 2011-02-22 2012-08-30 Caris Life Sciences Luxembourg Holdings, S.A.R.L. Circulating biomarkers
AU2012223448B2 (en) 2011-02-28 2017-03-16 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
ES2624986T3 (es) * 2011-09-13 2017-07-18 Glaxosmithkline Llc Azaindazoles
AU2012315566A1 (en) 2011-09-30 2014-04-17 Glaxosmithkline Llc Methods of treating cancer
WO2013067302A1 (en) * 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
WO2013067300A1 (en) 2011-11-04 2013-05-10 Glaxosmithkline Intellectual Property (No. 2) Limited Method of treatment
BR112014010803A2 (pt) * 2011-11-04 2017-04-25 Glaxosmithkline Intellectual Property (No 2) Ltd método de tratamento
US9206128B2 (en) 2011-11-18 2015-12-08 Constellation Pharmaceuticals, Inc. 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
WO2014124418A1 (en) 2013-02-11 2014-08-14 Constellation Pharmaceuticals, Inc. 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
KR102453519B1 (ko) 2012-03-12 2022-10-11 에피자임, 인코포레이티드 인간 ｅｚｈ2의 억제제 및 이의 사용 방법
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.
IL289300B1 (en) 2012-04-13 2024-01-01 Epizyme Inc Combined treatment for cancer
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
UA115074C2 (uk) 2012-10-15 2017-09-11 Епізайм, Інк. Бензольні сполуки, що містять замісники
LT2908823T (lt) 2012-10-15 2019-10-25 Epizyme Inc Vėžio gydymo būdai
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
HUE040126T2 (hu) 2012-11-01 2019-02-28 Infinity Pharmaceuticals Inc Rákok kezelése PI3 kináz izoform modulátorok alkalmazásával
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
WO2014151142A1 (en) * 2013-03-15 2014-09-25 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
EA030196B1 (ru) * 2013-04-30 2018-07-31 Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед Ингибиторы энхансера zeste гомолога 2
US9624205B2 (en) * 2013-07-19 2017-04-18 Epizyme, Inc. Substituted 6,5-fused bicyclic heteroaryl compounds
WO2015023915A1 (en) * 2013-08-15 2015-02-19 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
CA2862289A1 (en) 2013-08-15
MY172156A (en) 2019-11-15
MX2015010377A (es) 2015-10-29
AR094755A1 (es) 2015-08-26
US20150368229A1 (en) 2015-12-24
JP5989805B2 (ja) 2016-09-07
EA201591474A1 (ru) 2016-01-29
NZ628762A (en) 2016-07-29
US9980952B2 (en) 2018-05-29
AU2013216721B2 (en) 2017-09-28
US20190125737A1 (en) 2019-05-02
EA029089B9 (ru) 2019-01-31
USRE47428E1 (en) 2019-06-11
JP2015506985A (ja) 2015-03-05
US9371331B2 (en) 2016-06-21
ES2632241T3 (es) 2017-09-12
AU2013216721A1 (en) 2014-09-04
US20150259351A1 (en) 2015-09-17
JP2016507573A (ja) 2016-03-10
US9469646B2 (en) 2016-10-18
EA029089B1 (ru) 2018-02-28
BR112015018508B1 (pt) 2021-08-24
HRP20171030T1 (hr) 2017-10-06
US20170056388A1 (en) 2017-03-02
EP2812001A2 (en) 2014-12-17
PT2953941T (pt) 2017-07-13
CA2862289C (en) 2019-11-26
WO2013120104A3 (en) 2014-03-06
US20150011546A1 (en) 2015-01-08
LT2953941T (lt) 2017-09-11
US20170312262A9 (en) 2017-11-02
EP2812001B1 (en) 2017-06-14
US10016405B2 (en) 2018-07-10
EP2812001A4 (en) 2015-09-02
MX363392B (es) 2019-03-20
BR112015018508A2 (pt) 2017-07-18
US20150376190A1 (en) 2015-12-31
US9085583B2 (en) 2015-07-21
US20160333016A1 (en) 2016-11-17
WO2013120104A2 (en) 2013-08-15
UA117362C2 (uk) 2018-07-25
DK2953941T3 (en) 2017-07-24
JP5989923B2 (ja) 2016-09-07

Similar Documents

Publication Publication Date Title
CY1119060T1 (el) Ρυθμιστες ενζυμων μεθυλικης τροποποιησης, συνθεσεις και χρησεις αυτων
CY1123407T1 (el) Σταθερες υδατικες φαρμακοτεχνικες μορφες της αδαλιμουμαμπης
CY1118860T1 (el) Νεα διαζασπειροκυκλοαλκανια και αζασπειροκυκλοαλκανια
PH12015501720A1 (en) Modulators of methyl modifying enzymes, compositions and uses thereof
CY1117956T1 (el) N3-αντικατεστημενα-n1-sulfonyl-5-fluoropyrimidinone παραγωγα
CO2018005381A2 (es) Inhibidores éster de acc y usos de los mismos
TR201900038T4 (tr) GPR6'nın tetrahidropiridopirazin modülatörleri.
CY1119762T1 (el) C-17-ετεροαρυλικα παραγωγα ελαιολικου οξεος και μεθοδοι χρησης αυτων
EA201590534A1 (ru) Новые бициклические производные
EA201691794A1 (ru) Конденсированные [1,4]диазепиновые соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa)
EA201591961A1 (ru) Ингибиторы акк и их применение
EA201401054A1 (ru) N-циклиламиды в качестве нематоцидов
EA201391602A1 (ru) Контролируемое высвобождение иммунодепрессантов из синтетических наноносителей
EA201591959A1 (ru) Ингибиторы акк и их применение
EA201690473A1 (ru) Комбинированный состав двух противовирусных соединений
EA201591960A1 (ru) Ингибиторы акк и их применение
CR20140468A (es) Inhibidores de diacilglicerol aciltransferasa 2
UA111626C2 (uk) Похідні дигідрохінолін-2-ону
EA201591962A1 (ru) Ингибиторы акк и их применение
EA201591805A1 (ru) Оксабицикло [2.2.2] кислоты - модуляторы gpr120
CY1120759T1 (el) Παρασκευη διγλυκοζιτη (s,s)-σεκοϊσολαρικιρεσινολης και διγλυκοζιτη (r,r)-σεκοϊσολαρικιρεσινολης
EA201490846A1 (ru) Новые производные арилхинолина
EA201600124A1 (ru) Новые индолизиновые соединения, способ их получения и фармацевтические композиции, содержащие их
WO2013072528A3 (en) Substituted n-(tetrazol-5-yl)- and n-(triazol-5-yl)pyridin-3-yl-carboxamide compounds and their use as herbicides
EA201591451A1 (ru) Модуляторы flap