WO2016044641A3 - Inhibiteurs de carm1 et leurs utilisations - Google Patents

Inhibiteurs de carm1 et leurs utilisations Download PDF

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Publication number
WO2016044641A3
WO2016044641A3 PCT/US2015/050776 US2015050776W WO2016044641A3 WO 2016044641 A3 WO2016044641 A3 WO 2016044641A3 US 2015050776 W US2015050776 W US 2015050776W WO 2016044641 A3 WO2016044641 A3 WO 2016044641A3
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compounds
formula
carml
carm1
inhibitors
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PCT/US2015/050776
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English (en)
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WO2016044641A2 (fr
Inventor
Richard Chesworth
Oscar Miguel Moradei
Gideon Shapiro
Lei Jin
Robert E. Babine
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Epizyme, Inc.
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Publication of WO2016044641A2 publication Critical patent/WO2016044641A2/fr
Publication of WO2016044641A3 publication Critical patent/WO2016044641A3/fr

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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
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    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/04—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 two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07D405/12—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 two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • 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
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04—Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C—CHEMISTRY; METALLURGY
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    • 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
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    • 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
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Abstract

La présente invention concerne des composés de formule (I) et leurs sels pharmaceutiquement acceptables, ainsi que des compositions pharmaceutiques à base desdits composés ; dans la formule, X, R1, R1a, R2a, R2b, R2c, R2d, sont tels que définis dans la description, et le noyau HET est un système à noyau hétéroaryle monocyclique à 6 chaînons de formule () dans laquelle L2, R13, G8, G10, G11, et G12 sont tels que définis dans la description. Les composés de la présente invention sont utiles pour inhiber l'activité de CARM1. L'invention concerne également des procédés d'utilisation desdits composés pour le traitement de troubles médiés par CARM1.
PCT/US2015/050776 2014-09-17 2015-09-17 Inhibiteurs de carm1 et leurs utilisations WO2016044641A2 (fr)

Applications Claiming Priority (2)

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US201462051654P 2014-09-17 2014-09-17
US62/051,654 2014-09-17

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WO2016044641A2 WO2016044641A2 (fr) 2016-03-24
WO2016044641A3 true WO2016044641A3 (fr) 2016-09-29

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Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6678455B2 (ja) 2012-12-21 2020-04-08 エピザイム，インコーポレイティド Ｐｒｍｔ５阻害剤およびその使用
WO2014100716A1 (fr) 2012-12-21 2014-06-26 Epizyme, Inc. Inhibiteurs de prmt5 et leurs utilisations
WO2014100730A1 (fr) 2012-12-21 2014-06-26 Epizyme, Inc. Inhibiteurs de la prmt5 contenant une dihydro- ou tétrahydro-isoquinoléine et leurs utilisations
US9221794B2 (en) 2012-12-21 2015-12-29 Epizyme, Inc. PRMT5 inhibitors and uses thereof
JP2016505000A (ja) 2012-12-21 2016-02-18 エピザイム，インコーポレイティド Ｐｒｍｔ５阻害剤およびその使用
US9120757B2 (en) 2013-03-14 2015-09-01 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
US9023883B2 (en) 2013-03-14 2015-05-05 Epizyme, Inc. PRMT1 inhibitors and uses thereof
BR112015022785A2 (pt) 2013-03-14 2017-07-18 Epizyme Inc composto; composição farmacêutica; kit ou artigo farmacêutico embalado; método de inibição de uma arginina metil transferase (rmt); método de modulação da expressão genética; método de modulação da transcrição; e método de tratamento de um distúrbio mediado por rmt
WO2014153214A1 (fr) 2013-03-14 2014-09-25 Epizyme, Inc. Inhibteurs de l'arginine méthyltransférase et utilisations de ceux-ci
US9346761B2 (en) 2013-03-14 2016-05-24 Epizyme, Inc. Arginine methyltransferase inhibitors and uses thereof
EP2970181B1 (fr) 2013-03-14 2017-06-07 Epizyme, Inc. Inhibiteurs d'arginine méthyltransférase et leurs utilisations
WO2014144455A1 (fr) 2013-03-15 2014-09-18 Epizyme, Inc. Dérivés de 1-phénoxy-3-(alkylamino)-propan-2-ol en tant qu'inhibiteurs de carm1 et leurs utilisations
EP2970219B1 (fr) 2013-03-15 2019-02-27 Epizyme, Inc. Inhibiteurs de carm1 et leurs utilisations
CA2953572A1 (fr) 2014-08-04 2016-02-11 Epizyme, Inc. Inhibiteurs de prmt5 et leurs utilisations
JP2017530959A (ja) * 2014-09-17 2017-10-19 エピザイム，インコーポレイティド Ｃａｒｍ１阻害剤およびその使用
CA3042700A1 (fr) 2016-11-07 2018-05-11 University Of Massachusetts Cibles therapeutiques pour dystrophie musculaire facio-scapulo-humerale
CN107200744A (zh) * 2017-05-31 2017-09-26 湖南华腾制药有限公司 一种制备吡咯并嘧啶盐酸盐的方法
JP2022539556A (ja) 2019-06-28 2022-09-12 エイエルエス・セラピー・デベロップメント・インスティテュート ジペプチドリピートタンパク質の阻害
JPWO2022059779A1 (fr) 2020-09-18 2022-03-24

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US20110065681A1 (en) * 2008-02-29 2011-03-17 Zhi-Liang Wei Amide compounds, compositions and uses thereof
US20140221310A1 (en) * 2013-02-04 2014-08-07 Janssen Pharmaceutica Nv Flap modulators
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