AR123185A1 - Compuestos y composiciones para inhibir ezh2 - Google Patents

Compuestos y composiciones para inhibir ezh2

Info

Publication number
AR123185A1
AR123185A1 ARP210102216A ARP210102216A AR123185A1 AR 123185 A1 AR123185 A1 AR 123185A1 AR P210102216 A ARP210102216 A AR P210102216A AR P210102216 A ARP210102216 A AR P210102216A AR 123185 A1 AR123185 A1 AR 123185A1
Authority
AR
Argentina
Prior art keywords
alkyl
4alkyl
4alkylene
hydroxyc1
4alkoxy
Prior art date
Application number
ARP210102216A
Other languages
English (en)
Inventor
Xuan Dai
Michael Dore
Xiang Gu
Justin - Li Ling Ju
Kevin Kun Chin Liu
Sing Yeung Frankie Mak
Yuan Mi
Counde Oyang
Julien Papillon
Wei Qi
Xiaoxia Yan
Zhengtian Yu
Ji Yue Zhang
Kehao Zhao
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of AR123185A1 publication Critical patent/AR123185A1/es

Links

Classifications

    • 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
    • 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
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—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 three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Abstract

La invención dada a conocer en la presente se refiere a compuestos de azaquinolina de fórmula (1), composiciones farmacéuticas que comprenden tales compuestos; y el uso de tales compuestos para tratar una enfermedad o afección mediada por el potenciador del homólogo Zeste 2 (EZH2), complejo represor Polycomb 2 (PRC2) o una combinación de estos. Reivindicación 1: Un compuesto que tiene la estructura de fórmula (1) o un estereoisómero, enantiómero, mezcla enantiomérica o sal farmacéuticamente aceptable de este; en donde: Y es N o CRᵃ; Rᵃ, R¹, R³, R⁵, R⁶, R⁷, R⁸ y R⁹ son independientemente es H, halógeno o -alquilo C₁₋₄; R² es -CN, -alquilo C₁₋₆, -hidroxialquileno C₁₋₄, -alcoxi C₁₋₄, -alcoxi C₂₋₄ sustituido con 1 - 2 hidroxilo; -(CR¹³R¹⁴)ₙC(=O)NR¹¹R¹², -(CR¹³R¹⁴)ₙC(=O)NR¹¹R¹⁵; -(CR¹³R¹⁴)ₙC(=O)R¹⁵; -(CR₂)ₙNR¹¹C(=O)R¹⁵, -(CR₂)ₙNR¹¹(CR₂)₂C(=O)R¹⁵; -(CR₂)ₙNR-C(=O)OR¹¹,-(CR₂)ₙNR-C(=O)O-(CR₂)-R¹⁵; -NR-C(=O)(CR₂)₂C(=O)R¹⁵, -NR-C(=O)R¹¹; -(CR₂)ₙNR¹¹R¹², -(CR₂)ₙNR¹¹(CR₂)ₙR¹⁵; -(CR₂)ₙOR¹⁵, -(CR₂)ₙR¹⁵; un compuesto de fórmula (2), o un heteroarilo de 5 a 6 miembros que tiene de 1 a 4 heteroátomos seleccionados independientemente de O, S y N; R⁴ᵃ, R⁴ᵇ, R⁴ᶜ y R⁴ᵈ son independientemente H o -alquilo C₁₋₄; R¹⁰ es H, halógeno, -alquilo C₁₋₄, -alcoxi C₁₋₄, -haloalcoxi C₁₋₄ o -NH(alquilo C₁₋₄); R¹¹ es H, -alquilo C₁₋₄, -hidroxialquileno C₁₋₄, -cianoalquileno C₁₋₄ o -alquilo C₁₋₄ sustituido con -alcoxi C₁₋₄; R¹² es H o -alquilo C₁₋₄; R¹³ es H, halógeno, -CN, -OH, -alquilo C₁₋₄ o -hidroxialquileno C₁₋₄; R¹⁴ es H, halógeno o -alquilo C₁₋₄; R¹⁵ es un compuesto de fórmula (3), cicloalquilo C₃₋₆ o un heterocicloalquilo de 4 a 6 miembros que tiene 1 - 2 heteroátomos seleccionados independientemente de O, S, S(=O)₂ y N; en donde dicho -cicloalquilo C₃₋₆ o heterocicloalquilo de 4 a 6 miembros de R¹⁵ no está sustituido o está sustituido con 1 - 2 sustituyentes seleccionados de -OH, -alquilo C₁₋₄, -hidroxialquileno C₁₋₄, -alcoxi C₁₋₄, -SO₂(alquilo C₁₋₄) y -N(alquilo C₁₋₄)₂; R¹⁶, si está presente, es un sustituyente seleccionado de halógeno, -CN, -OH, -alquilo C₁₋₄ e -hidroxialquileno C₁₋₄; cada R es independientemente H o -alquilo C₁₋₄; m es 0, 1 ó 2; y cada n se selecciona independientemente de 0, 1 y 2.
ARP210102216A 2020-08-10 2021-08-09 Compuestos y composiciones para inhibir ezh2 AR123185A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2020108213 2020-08-10

Publications (1)

Publication Number Publication Date
AR123185A1 true AR123185A1 (es) 2022-11-09

Family

ID=77520462

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP210102216A AR123185A1 (es) 2020-08-10 2021-08-09 Compuestos y composiciones para inhibir ezh2

Country Status (11)

Country Link
US (1) US20230167100A1 (es)
EP (1) EP4041725B1 (es)
JP (1) JP2023538159A (es)
KR (1) KR20230051116A (es)
CN (1) CN114555589A (es)
AR (1) AR123185A1 (es)
AU (1) AU2021323828A1 (es)
CA (1) CA3180139A1 (es)
IL (1) IL297332A (es)
TW (1) TW202220979A (es)
WO (1) WO2022033492A1 (es)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN117384153A (zh) * 2022-07-12 2024-01-12 上海赛岚生物科技有限公司 一类甲基转移酶抑制剂及其用途

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2779780A (en) 1955-03-01 1957-01-29 Du Pont 1, 4-diamino-2, 3-dicyano-1, 4-bis (substituted mercapto) butadienes and their preparation
EP0647450A1 (en) 1993-09-09 1995-04-12 BEHRINGWERKE Aktiengesellschaft Improved prodrugs for enzyme mediated activation
HUP0104693A3 (en) 1998-12-16 2003-12-29 Warner Lambert Co Treatment of arthritis with mek inhibitors
EE05450B1 (et) 2000-07-19 2011-08-15 Warner-Lambert Company 4-jodofenlaminobenshdroksaamhapete oksgeenitud estrid, nende kristallvormid ja farmatseutilised kompositsioonid ning kasutamine
PL221491B1 (pl) 2002-03-08 2016-04-29 Eisai R&D Man Co Związki makrocykliczne, środek farmaceutyczny zawierający te związki oraz zastosowanie tych związków
PL401637A1 (pl) 2002-03-13 2013-05-27 Array Biopharma Inc. N3 alkilowane pochodne benzimidazolu jako inhibitory MEK
GB0510390D0 (en) 2005-05-20 2005-06-29 Novartis Ag Organic compounds
CA2618218C (en) 2005-07-21 2015-06-30 Ardea Biosciences, Inc. N-(arylamino)-sulfonamide inhibitors of mek
JO2660B1 (en) 2006-01-20 2012-06-17 نوفارتيس ايه جي Pi-3 inhibitors and methods of use
KR101584823B1 (ko) 2007-09-12 2016-01-22 제넨테크, 인크. 포스포이노시타이드 3-키나제 저해제 화합물과 화학치료제의 배합물 및 이의 사용방법
US8354528B2 (en) 2007-10-25 2013-01-15 Genentech, Inc. Process for making thienopyrimidine compounds
US8168784B2 (en) 2008-06-20 2012-05-01 Abbott Laboratories Processes to make apoptosis promoters
US20130310379A1 (en) * 2010-11-19 2013-11-21 Constellation Pharmaceuticals Modulators of methyl modifying enzymes, compositions and uses thereof
WO2018195450A1 (en) * 2017-04-21 2018-10-25 Epizyme, Inc. Combination therapies with ehmt2 inhibitors
KR20220070229A (ko) * 2019-09-26 2022-05-30 노파르티스 아게 아자-퀴놀린 화합물 및 그의 용도

Also Published As

Publication number Publication date
CA3180139A1 (en) 2022-02-17
US20230167100A1 (en) 2023-06-01
AU2021323828A1 (en) 2022-05-19
EP4041725A1 (en) 2022-08-17
WO2022033492A1 (en) 2022-02-17
IL297332A (en) 2022-12-01
JP2023538159A (ja) 2023-09-07
TW202220979A (zh) 2022-06-01
KR20230051116A (ko) 2023-04-17
EP4041725B1 (en) 2024-03-27
CN114555589A (zh) 2022-05-27

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