PE20160044A1 - 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
PE20160044A1
PE20160044A1 PE2015001728A PE2015001728A PE20160044A1 PE 20160044 A1 PE20160044 A1 PE 20160044A1 PE 2015001728 A PE2015001728 A PE 2015001728A PE 2015001728 A PE2015001728 A PE 2015001728A PE 20160044 A1 PE20160044 A1 PE 20160044A1
Authority
PE
Peru
Prior art keywords
methyl
alkyl
compositions
modifying enzymes
modulators
Prior art date
Application number
PE2015001728A
Other languages
English (en)
Inventor
Brian K Albrecht
James Edmund Audia
Andrew S Cook
Les A Dakin
Rishi G Vaswani
Victor S Gehling
Jean-Christophe Harmange
Christopher G Nasveschuk
Martin Duplessis
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=50239937&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20160044(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from PCT/US2013/025639 external-priority patent/WO2013120104A2/en
Application filed by Constellation Pharmaceuticals Inc filed Critical Constellation Pharmaceuticals Inc
Publication of PE20160044A1 publication Critical patent/PE20160044A1/es

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • 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

Abstract

Agentes para modular las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos. Referido a un compuesto caracterizado porque tiene la formula estructural (II): donde A es CH o N; R1a se selecciona entre -C1-C2 alquilo y -O-(C1-C2 alquilo), donde R1a esta opcionalmente sustituido con uno o mas fluoro; R4a se selecciona entre -(C1-C3 alquilen)-O-(C1-C2 alquilo), pipieridin-4-ilo 1-sustituido, C3-C6 cicloalquilo opcionalmente sustituido con uno o mas fluoro, y tetrahidropiranilo; y R13 se selecciona entre el hidrogeno, halo, fenilo, piridinilo, y -O-(C1-C4 alquilo). Los compuestos preferidos son: N-((4-metoxi-6-metil-2-oxo-1,2-dihidropiridin-3-il)-2-metil-1-(1-(1-(2,2,2-trifluoroetil)piperidin-4-il)etil)-1H-indol-3-carboxamida, 1-(1-(1-(2,2-difluoroetil) piperidin-4-il)etil)-N-((4-metoxi-6-metil-2-oxo-1,2-dihidropiridin-3-il)metil)-2-metil-1H-indol-3-carboxamida, o una sal farmaceuticamente aceptable del mismo
PE2015001728A 2013-02-11 2014-02-11 Moduladores de las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos PE20160044A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/US2013/025639 WO2013120104A2 (en) 2012-02-10 2013-02-11 Modulators of methyl modifying enzymes, compositions and uses thereof

Publications (1)

Publication Number Publication Date
PE20160044A1 true PE20160044A1 (es) 2016-02-11

Family

ID=50239937

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015001728A PE20160044A1 (es) 2013-02-11 2014-02-11 Moduladores de las enzimas modificadoras de los metilos, composiciones que los comprenden y sus usos

Country Status (17)

Country Link
EP (1) EP2953941B1 (es)
KR (1) KR102219441B1 (es)
CN (1) CN105102446B (es)
CL (1) CL2015002239A1 (es)
CR (1) CR20150457A (es)
HK (1) HK1218648A1 (es)
IL (1) IL239985B (es)
MA (1) MA38341B1 (es)
ME (1) ME02730B (es)
PE (1) PE20160044A1 (es)
PH (1) PH12015501720A1 (es)
PL (1) PL2953941T3 (es)
RS (1) RS56207B1 (es)
SG (1) SG11201506077XA (es)
SI (1) SI2953941T1 (es)
TW (1) TWI629273B (es)
WO (1) WO2014124418A1 (es)

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US20180037568A1 (en) * 2015-02-13 2018-02-08 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
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
AU2016312514A1 (en) 2015-08-24 2018-03-15 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
WO2017040190A1 (en) * 2015-08-28 2017-03-09 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
CN108699046A (zh) 2015-10-06 2018-10-23 Epizyme股份有限公司 用ezh2抑制剂治疗成神经管细胞瘤的方法
EP3674709A1 (en) 2015-11-05 2020-07-01 Epizyme Inc Flow cytometry for monitoring histone h3 methylation status
US11951108B2 (en) 2016-01-29 2024-04-09 Epizyme, Inc. Combination therapy for treating cancer
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WO2017218953A1 (en) 2016-06-17 2017-12-21 Epizyme, Inc. Ezh2 inhibitors for treating cancer
ES2798424T3 (es) 2016-06-20 2020-12-11 Novartis Ag Compuestos de triazolopiridina y usos de estos
JP2019524872A (ja) 2016-06-20 2019-09-05 ノバルティス アーゲー 癌の治療に有用なイミダゾピリミジン化合物
US11091489B2 (en) 2016-06-20 2021-08-17 Novartis Ag Crystalline forms of a triazolopyrimidine compound
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WO2018102687A2 (en) 2016-12-02 2018-06-07 Epizyme, Inc. Combination therapy for treating cancer
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US20230201212A1 (en) 2017-06-13 2023-06-29 Epizyme, Inc. Inhibitors of ezh2 and methods of use thereof
WO2019014191A1 (en) 2017-07-10 2019-01-17 Constellation Pharmaceuticals, Inc. GENE EXPRESSION INDUCED BY EZH2 INHIBITOR
EP3707136B1 (en) 2017-11-09 2022-05-04 Constellation Pharmaceuticals, Inc. Modulators of methyl modifying enzymes, compositions and uses thereof
TWI698238B (zh) 2017-11-14 2020-07-11 美商輝瑞股份有限公司 Ｅｚｈ２抑制劑組合治療
CN109879790B (zh) * 2017-12-06 2022-09-20 华东师范大学 以吲哚或吲哚类似物为母核结构的酰胺类小分子有机化合物、用途及其制备方法
US20210000815A1 (en) 2017-12-28 2021-01-07 Constellation Pharmaceuticals, Inc. Pharmacokinetic enhancement of ezh2 inhibitors through combination therapies
PT3746446T (pt) 2018-01-31 2022-07-18 Mirati Therapeutics Inc Inibidores de prc2
CN110229157B (zh) * 2018-03-06 2022-06-21 上海海和药物研究开发股份有限公司 嘧啶并五元芳香杂环类化合物、其制备方法及用途
CN110229151B (zh) * 2018-03-06 2021-09-10 上海海和药物研究开发股份有限公司 吲嗪类化合物、其制备方法及用途
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Also Published As

Publication number Publication date
KR20150119201A (ko) 2015-10-23
MA38341B1 (fr) 2018-11-30
RS56207B1 (sr) 2017-11-30
PL2953941T3 (pl) 2017-11-30
EP2953941B1 (en) 2017-04-05
CN105102446B (zh) 2018-01-23
ME02730B (me) 2017-10-20
CR20150457A (es) 2015-10-20
MA38341A1 (fr) 2018-01-31
IL239985A0 (en) 2015-09-24
PH12015501720B1 (en) 2015-11-09
SI2953941T1 (sl) 2017-08-31
WO2014124418A1 (en) 2014-08-14
TWI629273B (zh) 2018-07-11
EP2953941A1 (en) 2015-12-16
CN105102446A (zh) 2015-11-25
KR102219441B1 (ko) 2021-02-23
SG11201506077XA (en) 2015-08-28
TW201443038A (zh) 2014-11-16
HK1218648A1 (zh) 2017-03-03
CL2015002239A1 (es) 2016-02-05
PH12015501720A1 (en) 2015-11-09
IL239985B (en) 2018-11-29

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