CR20180104A - Inhibidores de ezh2 - Google Patents
Inhibidores de ezh2Info
- Publication number
- CR20180104A CR20180104A CR20180104A CR20180104A CR20180104A CR 20180104 A CR20180104 A CR 20180104A CR 20180104 A CR20180104 A CR 20180104A CR 20180104 A CR20180104 A CR 20180104A CR 20180104 A CR20180104 A CR 20180104A
- Authority
- CR
- Costa Rica
- Prior art keywords
- compounds
- ezh2 inhibitors
- ezh2
- zeste
- hematological
- Prior art date
Links
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 title abstract 2
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 2
- OSXFATOLZGZLSK-UHFFFAOYSA-N 6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-[1-(phenylmethyl)-4-piperidinyl]-4-quinazolinamine Chemical compound C=12C=C(OC)C(OC)=CC2=NC(N2CCN(C)CCC2)=NC=1NC(CC1)CCN1CC1=CC=CC=C1 OSXFATOLZGZLSK-UHFFFAOYSA-N 0.000 abstract 1
- 108010016918 Histone-Lysine N-Methyltransferase Proteins 0.000 abstract 1
- 102000000581 Histone-lysine N-methyltransferase Human genes 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000003623 enhancer Substances 0.000 abstract 1
- QTTMOCOWZLSYSV-QWAPEVOJSA-M equilin sodium sulfate Chemical compound [Na+].[O-]S(=O)(=O)OC1=CC=C2[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4C3=CCC2=C1 QTTMOCOWZLSYSV-QWAPEVOJSA-M 0.000 abstract 1
- 201000005787 hematologic cancer Diseases 0.000 abstract 1
- 230000002489 hematologic effect Effects 0.000 abstract 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
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- 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
- A61K31/28—Compounds containing heavy metals
- A61K31/282—Platinum compounds
-
- 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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/337—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/4738—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems
- A61K31/4745—Quinolines; Isoquinolines ortho- or peri-condensed with heterocyclic ring systems condensed with ring systems having nitrogen as a ring hetero atom, e.g. phenantrolines
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/24—Heavy metals; Compounds thereof
- A61K33/243—Platinum; Compounds thereof
-
- 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
-
- 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
- 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
- A61P19/00—Drugs for skeletal disorders
-
- 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
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/04—Ortho-condensed systems
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Inorganic Chemistry (AREA)
- Molecular Biology (AREA)
- Physical Education & Sports Medicine (AREA)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Epoxy Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente invención se refiere a compuestos que inhiben la actividad de la histona lisina metiltransferasa, Potenciador del Homólogo Zeste 2 (EZH2, por sus siglas en inglés), composiciones farmacéuticas que comprenden los compuestos, y métodos para usar los compuestos para tratar cáncer, tales como tumores hematológicos y sólidos
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15382433 | 2015-08-27 | ||
| EP15382615 | 2015-12-11 | ||
| PCT/US2016/047989 WO2017035060A1 (en) | 2015-08-27 | 2016-08-22 | Inhibitors of ezh2 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20180104A true CR20180104A (es) | 2018-04-24 |
Family
ID=56801893
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20180104A CR20180104A (es) | 2015-08-27 | 2016-08-22 | Inhibidores de ezh2 |
Country Status (31)
| Country | Link |
|---|---|
| US (1) | US9718838B2 (es) |
| EP (1) | EP3341379B1 (es) |
| JP (1) | JP6704040B2 (es) |
| KR (1) | KR20180030704A (es) |
| CN (1) | CN107922434B (es) |
| AU (1) | AU2016313541A1 (es) |
| BR (1) | BR112018003108A2 (es) |
| CA (1) | CA2994428A1 (es) |
| CO (1) | CO2018002033A2 (es) |
| CR (1) | CR20180104A (es) |
| CY (1) | CY1122364T1 (es) |
| DK (1) | DK3341379T3 (es) |
| DO (1) | DOP2018000058A (es) |
| EC (1) | ECSP18014798A (es) |
| ES (1) | ES2756603T3 (es) |
| HR (1) | HRP20192101T1 (es) |
| HU (1) | HUE047630T2 (es) |
| IL (1) | IL257061A (es) |
| LT (1) | LT3341379T (es) |
| MD (1) | MD3341379T2 (es) |
| ME (1) | ME03650B (es) |
| MX (1) | MX2018002484A (es) |
| PE (1) | PE20181025A1 (es) |
| PH (1) | PH12018500423A1 (es) |
| PL (1) | PL3341379T3 (es) |
| PT (1) | PT3341379T (es) |
| RS (1) | RS59615B1 (es) |
| SI (1) | SI3341379T1 (es) |
| TN (1) | TN2018000058A1 (es) |
| TW (1) | TW201718598A (es) |
| WO (1) | WO2017035060A1 (es) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT1173201E (pt) * | 1999-04-22 | 2005-08-31 | Biogen Idec Inc | Metodo para o tratamento de fibrose utilizando um antagonista da subunidade alfa 4 de integrina |
| 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 |
| SG11201809560QA (en) * | 2016-05-05 | 2018-11-29 | Glaxosmithkline Ip No 2 Ltd | Enhancer of zeste homolog 2 inhibitors |
| CN109312407A (zh) * | 2016-06-08 | 2019-02-05 | 豪夫迈·罗氏有限公司 | 用于癌症的诊断和治疗方法 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| CN109942556A (zh) * | 2017-12-21 | 2019-06-28 | 上海青煜医药科技有限公司 | 嘧啶酮化合物及其应用 |
| NZ766447A (en) | 2018-01-31 | 2021-12-24 | Mirati Therapeutics Inc | Prc2 inhibitors |
| CN111601791B (zh) * | 2018-04-24 | 2022-10-04 | 上海海雁医药科技有限公司 | Ezh2抑制剂及其药学上可接受的盐和多晶型物及其应用 |
| EP3823671B1 (en) | 2018-07-09 | 2024-02-07 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| WO2020219448A1 (en) | 2019-04-22 | 2020-10-29 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as prc2 inhibitors |
| CN111909157B (zh) * | 2019-05-07 | 2023-02-03 | 南京药石科技股份有限公司 | Ezh2抑制剂及其用途 |
| JP7541538B2 (ja) | 2019-06-05 | 2024-08-28 | ミラティ セラピューティクス,インク. | 癌を処置するためのprc2阻害剤としてのイミダゾ[1,2-c]ピリミジン誘導体 |
| CN114269727A (zh) * | 2019-08-16 | 2022-04-01 | 西克拉塞尔有限公司 | 制备嘧啶并二氮杂环庚三烯衍生物的方法 |
| CN116239519A (zh) * | 2023-02-20 | 2023-06-09 | 安徽峆一药业股份有限公司 | 一种(2-苄氧基-4,6-二甲基吡啶-3-基)甲醇的合成方法 |
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| JP2004504342A (ja) * | 2000-07-24 | 2004-02-12 | ファルマシア・アンド・アップジョン・カンパニー | 極めて水不溶性の脂肪親和性薬剤用の自己乳化性ドラッグデリバリーシステム |
| JP2004524277A (ja) * | 2000-10-20 | 2004-08-12 | ブリストル−マイヤーズ スクイブ ファーマ カンパニー | アシルセミカルバジド及びサイクリン依存性キナーゼ(cdk)阻害剤としてのその使用 |
| CN100441176C (zh) * | 2001-09-24 | 2008-12-10 | 杰西·L·S·奥 | 测定联合疗法中使用的苏拉明的化学敏感化剂量的方法和组合物 |
| JP2006521794A (ja) | 2003-02-14 | 2006-09-28 | スミスクライン・ビーチャム・コーポレイション | Ksp発現と相関関係にある示差発現核酸 |
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| EA023788B1 (ru) | 2010-05-07 | 2016-07-29 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Производные индола и фармацевтические композиции на их основе |
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| EA036889B1 (ru) | 2014-06-19 | 2021-01-12 | Мемориал Слоан-Кеттеринг Кэнсер Сентер | Биомаркеры ответа на ингибиторы ezh2 |
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| CN107148419A (zh) | 2014-10-28 | 2017-09-08 | 葛兰素史密斯克莱知识产权(第2 号)有限公司 | Zeste增强子同源物2抑制剂 |
| AR102767A1 (es) | 2014-12-05 | 2017-03-22 | Lilly Co Eli | Inhibidores de ezh2 |
| WO2016102493A1 (en) | 2014-12-22 | 2016-06-30 | Bayer Pharma Aktiengesellschaft | Imidazopyridine ezh2 inhibitors |
| WO2016130396A1 (en) | 2015-02-13 | 2016-08-18 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| WO2016140501A1 (en) | 2015-03-04 | 2016-09-09 | Kainos Medicine, Inc. | Pyridine n-oxide for enhancer of zeste homolog 2 inhibitors |
| 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 |
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2016
- 2016-08-11 TW TW105125679A patent/TW201718598A/zh unknown
- 2016-08-22 PL PL16757513T patent/PL3341379T3/pl unknown
- 2016-08-22 EP EP16757513.3A patent/EP3341379B1/en active Active
- 2016-08-22 SI SI201630453T patent/SI3341379T1/sl unknown
- 2016-08-22 HR HRP20192101TT patent/HRP20192101T1/hr unknown
- 2016-08-22 WO PCT/US2016/047989 patent/WO2017035060A1/en not_active Ceased
- 2016-08-22 PT PT167575133T patent/PT3341379T/pt unknown
- 2016-08-22 RS RS20191526A patent/RS59615B1/sr unknown
- 2016-08-22 CN CN201680049957.2A patent/CN107922434B/zh active Active
- 2016-08-22 CR CR20180104A patent/CR20180104A/es unknown
- 2016-08-22 KR KR1020187005603A patent/KR20180030704A/ko not_active Withdrawn
- 2016-08-22 HU HUE16757513A patent/HUE047630T2/hu unknown
- 2016-08-22 US US15/242,638 patent/US9718838B2/en active Active
- 2016-08-22 MD MDE20180644T patent/MD3341379T2/ro unknown
- 2016-08-22 PE PE2018000313A patent/PE20181025A1/es not_active Application Discontinuation
- 2016-08-22 ES ES16757513T patent/ES2756603T3/es active Active
- 2016-08-22 ME MEP-2019-322A patent/ME03650B/me unknown
- 2016-08-22 JP JP2018510778A patent/JP6704040B2/ja active Active
- 2016-08-22 BR BR112018003108-9A patent/BR112018003108A2/pt not_active Application Discontinuation
- 2016-08-22 TN TNP/2018/000058A patent/TN2018000058A1/en unknown
- 2016-08-22 DK DK16757513T patent/DK3341379T3/da active
- 2016-08-22 AU AU2016313541A patent/AU2016313541A1/en not_active Abandoned
- 2016-08-22 CA CA2994428A patent/CA2994428A1/en not_active Abandoned
- 2016-08-22 MX MX2018002484A patent/MX2018002484A/es unknown
- 2016-08-22 LT LT16757513T patent/LT3341379T/lt unknown
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2018
- 2018-01-21 IL IL257061A patent/IL257061A/en unknown
- 2018-02-22 DO DO2018000058A patent/DOP2018000058A/es unknown
- 2018-02-23 CO CONC2018/0002033A patent/CO2018002033A2/es unknown
- 2018-02-26 EC ECIEPI201814798A patent/ECSP18014798A/es unknown
- 2018-02-26 PH PH12018500423A patent/PH12018500423A1/en unknown
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2019
- 2019-12-04 CY CY20191101284T patent/CY1122364T1/el unknown
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