AR123185A1 - Compuestos y composiciones para inhibir ezh2 - Google Patents
Compuestos y composiciones para inhibir ezh2Info
- 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
Links
Classifications
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- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
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.
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 (12)
| Country | Link |
|---|---|
| US (1) | US12473273B2 (es) |
| EP (1) | EP4041725B1 (es) |
| JP (1) | JP7768880B2 (es) |
| KR (1) | KR20230051116A (es) |
| CN (2) | CN119431341A (es) |
| AR (1) | AR123185A1 (es) |
| AU (1) | AU2021323828A1 (es) |
| CA (1) | CA3180139A1 (es) |
| ES (1) | ES2985111T3 (es) |
| IL (1) | IL297332B1 (es) |
| TW (1) | TW202220979A (es) |
| WO (1) | WO2022033492A1 (es) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR123185A1 (es) | 2020-08-10 | 2022-11-09 | Novartis Ag | Compuestos y composiciones para inhibir ezh2 |
| CA3243621A1 (en) * | 2022-02-01 | 2023-08-10 | Eli Lilly And Company | METHODS FOR PREPARING SELECTIVE ESTROGEN RECEPTOR DEGRADING AGENTS |
| 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 |
| CN118515653B (zh) * | 2024-07-23 | 2024-12-10 | 西湖制药(杭州)有限公司 | 一种ezh2特异性抑制剂及其制备方法和用途 |
Family Cites Families (21)
| 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 |
| IL143236A0 (en) | 1998-12-16 | 2002-04-21 | Warner Lambert Co | Treatment of arthritis with mek inhibitors |
| DZ3401A1 (fr) | 2000-07-19 | 2002-01-24 | Warner Lambert Co | Esters oxygenes d'acides 4-iodophenylamino benzhydroxamiques |
| CN104876904A (zh) | 2002-03-08 | 2015-09-02 | 卫材R&D管理株式会社 | 用作医药品的大环化合物 |
| TWI338685B (en) | 2002-03-13 | 2011-03-11 | Array Biopharma Inc | N3 alkylated benzimid azole derivatives as mek inhibitors |
| SE0202134D0 (sv) | 2002-07-08 | 2002-07-08 | Astrazeneca Ab | Therapeutic agents |
| JP2006124387A (ja) | 2004-09-30 | 2006-05-18 | Taisho Pharmaceut Co Ltd | 新規なキノリン、テトラヒドロキナゾリン、及びピリミジン誘導体と、これらを使用することに関連した治療方法 |
| 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 |
| CA2699202C (en) | 2007-09-12 | 2016-09-27 | F. Hoffmann-La Roche Ag | Combinations of phosphoinositide 3-kinase inhibitor compounds and chemotherapeutic agents, and methods of use |
| 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 |
| WO2012068589A2 (en) * | 2010-11-19 | 2012-05-24 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| AP2016009605A0 (en) | 2014-06-17 | 2016-12-31 | Pfizer | Substituted dihydroisoquinolinone compounds |
| 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 |
| US11672800B2 (en) | 2017-04-21 | 2023-06-13 | Epizyme, Inc. | Combination therapies with EHMT2 inhibitors |
| CN109912576B (zh) | 2019-03-20 | 2021-11-19 | 华东理工大学 | 环状或螺环二胺类嘧啶-异羟肟酸及其用途 |
| CN114746414B (zh) * | 2019-09-26 | 2024-10-18 | 诺华公司 | 氮杂-喹啉化合物及其用途 |
| AR123185A1 (es) | 2020-08-10 | 2022-11-09 | Novartis Ag | Compuestos y composiciones para inhibir ezh2 |
-
2021
- 2021-08-09 AR ARP210102216A patent/AR123185A1/es unknown
- 2021-08-10 WO PCT/CN2021/111910 patent/WO2022033492A1/en not_active Ceased
- 2021-08-10 EP EP21762334.7A patent/EP4041725B1/en active Active
- 2021-08-10 KR KR1020227019646A patent/KR20230051116A/ko active Pending
- 2021-08-10 IL IL297332A patent/IL297332B1/en unknown
- 2021-08-10 TW TW110129535A patent/TW202220979A/zh unknown
- 2021-08-10 AU AU2021323828A patent/AU2021323828A1/en active Pending
- 2021-08-10 CN CN202411371645.6A patent/CN119431341A/zh active Pending
- 2021-08-10 JP JP2022530800A patent/JP7768880B2/ja active Active
- 2021-08-10 CN CN202180005903.7A patent/CN114555589B/zh active Active
- 2021-08-10 US US17/919,490 patent/US12473273B2/en active Active
- 2021-08-10 ES ES21762334T patent/ES2985111T3/es active Active
- 2021-08-10 CA CA3180139A patent/CA3180139A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| EP4041725A1 (en) | 2022-08-17 |
| JP7768880B2 (ja) | 2025-11-12 |
| IL297332B1 (en) | 2025-10-01 |
| TW202220979A (zh) | 2022-06-01 |
| CN114555589B (zh) | 2024-10-25 |
| WO2022033492A1 (en) | 2022-02-17 |
| US12473273B2 (en) | 2025-11-18 |
| AU2021323828A1 (en) | 2022-05-19 |
| CN119431341A (zh) | 2025-02-14 |
| ES2985111T3 (es) | 2024-11-04 |
| IL297332A (en) | 2022-12-01 |
| CN114555589A (zh) | 2022-05-27 |
| KR20230051116A (ko) | 2023-04-17 |
| JP2023538159A (ja) | 2023-09-07 |
| US20230167100A1 (en) | 2023-06-01 |
| EP4041725B1 (en) | 2024-03-27 |
| CA3180139A1 (en) | 2022-02-17 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FB | Suspension of granting procedure |