PE20181025A1 - Inhibidores de ezh2 - Google Patents
Inhibidores de ezh2Info
- Publication number
- PE20181025A1 PE20181025A1 PE2018000313A PE2018000313A PE20181025A1 PE 20181025 A1 PE20181025 A1 PE 20181025A1 PE 2018000313 A PE2018000313 A PE 2018000313A PE 2018000313 A PE2018000313 A PE 2018000313A PE 20181025 A1 PE20181025 A1 PE 20181025A1
- Authority
- PE
- Peru
- Prior art keywords
- methyl
- compounds
- cyclohexyl
- ethyl
- refers
- Prior art date
Links
Classifications
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- 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
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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
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)
- Endocrinology (AREA)
- Pulmonology (AREA)
- Reproductive Health (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Saccharide Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Epoxy Compounds (AREA)
Abstract
Se refiere a compuestos que inhiben la actividad de la histona lisina metiltransferasa, potenciador del homologo de Zeste 2 (EZH2), donde: X es -CH2- o -CH2-CH2-; Y' es -NR4R5, -CH(CH3)-ciclohexil-4-il-N-metil-N-metoxietilo, entre otros; R4 es ciclohex-4-il sustituido con N-metil-N-metoxietilamino, N-metil-N-ciclopropilamino, entre otros; R5 es metilo o etilo; R6 es metilo o cloro. Tambien se refiere a una composicion y a una combinacion que comprende a dichos compuestos. Un compuesto preferido es 5-[(4,6-dimetil-2-oxo-1,2-dihidropiridin-3-il)metil]-2-{(1R)-1-[4-(3-metoxiazetidin-1-il)ciclohexil]etil}-3-metil-5,6,7,8-tetrahidro-4H-tieno[3,2-c]azepin-4-ona. Dichos compuestos son utiles para el tratamiento del cancer tales como cancer de ovario, gastrico, colorrectal, entre otros
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP15382433 | 2015-08-27 | ||
EP15382615 | 2015-12-11 |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20181025A1 true PE20181025A1 (es) | 2018-06-27 |
Family
ID=56801893
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2018000313A PE20181025A1 (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 (10)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN100360183C (zh) * | 1999-04-22 | 2008-01-09 | 比奥根艾迪克Ma公司 | 整联蛋白α4亚单位的拮抗剂在制备治疗纤维变性的药物中的用途 |
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 |
CN109328188A (zh) * | 2016-05-05 | 2019-02-12 | 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 |
JP2019527037A (ja) * | 2016-06-08 | 2019-09-26 | ジェネンテック, インコーポレイテッド | がんのための診断及び治療方法 |
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 |
CA3089639C (en) | 2018-01-31 | 2024-06-18 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidinyl compounds as prc2 inhibitors |
WO2019206155A1 (zh) * | 2018-04-24 | 2019-10-31 | 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 |
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 |
Family Cites Families (60)
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EP1303261B1 (en) * | 2000-07-24 | 2005-03-09 | Pharmacia & Upjohn Company | Self-emulsifying drug delivery systems for extremely water-insoluble, lipophilic drugs |
EP1414804A1 (en) * | 2000-10-20 | 2004-05-06 | Bristol-Myers Squibb Pharma Company | Acylsemicarbazides and their use as cyclin dependent kinase (cdk) inhibitors |
WO2003026574A2 (en) * | 2001-09-24 | 2003-04-03 | Au Jessie L-S | Methods and compositions to determine the chemosensitizing dose of suramin used in combination therapy |
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 |
WO2011140325A1 (en) | 2010-05-07 | 2011-11-10 | Glaxosmithkline Llc | Indazoles |
MX2012012966A (es) | 2010-05-07 | 2013-01-22 | Glaxosmithkline Llc | Indoles. |
US8637509B2 (en) | 2010-05-07 | 2014-01-28 | Glaxosmithkline Llc | Azaindazoles |
RU2765155C2 (ru) | 2010-09-10 | 2022-01-26 | Эпизайм, Инк. | Ингибиторы ezh2 человека и способы их применения |
US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
WO2012068589A2 (en) | 2010-11-19 | 2012-05-24 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
US8765792B2 (en) | 2010-12-01 | 2014-07-01 | Glaxosmithkline Llc | Indoles |
AU2012223448B2 (en) | 2011-02-28 | 2017-03-16 | Epizyme, Inc. | Substituted 6,5-fused bicyclic heteroaryl compounds |
JO3438B1 (ar) | 2011-04-13 | 2019-10-20 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
TWI598336B (zh) | 2011-04-13 | 2017-09-11 | 雅酶股份有限公司 | 經取代之苯化合物 |
US9073924B2 (en) | 2011-09-13 | 2015-07-07 | Glaxosmithkline Llc | Azaindazoles |
EP2760452A4 (en) | 2011-09-30 | 2015-04-01 | Glaxosmithkline Llc | METHODS OF TREATING CANCER |
WO2013067302A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
WO2013067300A1 (en) | 2011-11-04 | 2013-05-10 | Glaxosmithkline Intellectual Property (No. 2) Limited | Method of treatment |
AU2012332297B2 (en) | 2011-11-04 | 2016-01-07 | Glaxosmithkline Intellectual Property (No.2) Limited | Method of treatment |
US9206128B2 (en) | 2011-11-18 | 2015-12-08 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
US9051269B2 (en) | 2011-11-18 | 2015-06-09 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
WO2013078320A1 (en) | 2011-11-21 | 2013-05-30 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
NZ628762A (en) | 2012-02-10 | 2016-07-29 | Constellation Pharmaceuticals Inc | Modulators of methyl modifying enzymes, compositions and uses thereof |
CA2867282C (en) | 2012-03-12 | 2024-04-02 | Epizyme, Inc. | Inhibitors of human ezh2, and methods of use thereof |
JP6250633B2 (ja) | 2012-04-12 | 2017-12-20 | ザ ケマーズ カンパニー エフシー リミテッド ライアビリティ カンパニー | 缶のタップ |
KR20220123339A (ko) | 2012-04-13 | 2022-09-06 | 에피자임, 인코포레이티드 | 인간 히스톤 메틸트랜스퍼라제 ezh2 억제제의 염 형태 |
JP6340361B2 (ja) | 2012-04-13 | 2018-06-06 | エピザイム,インコーポレイティド | がんを処置するための組合せ治療 |
WO2013173441A2 (en) | 2012-05-16 | 2013-11-21 | Glaxosmithkline Llc | Enhancer of zeste homolog 2 inhibitors |
JP2015518053A (ja) * | 2012-05-31 | 2015-06-25 | アムジエン・インコーポレーテツド | 癌の治療のためのamg900の使用 |
EP2900653A1 (en) | 2012-09-28 | 2015-08-05 | Pfizer Inc. | Benzamide and heterobenzamide compounds |
RU2658919C2 (ru) | 2012-10-15 | 2018-06-26 | Эпизайм, Инк. | Замещенные бензольные соединения |
NZ746054A (en) | 2012-10-15 | 2020-07-31 | Epizyme Inc | Methods of treating cancer |
EP2931707A4 (en) | 2012-12-13 | 2016-07-20 | Glaxosmithkline Llc | AMPLIFIER OF ZEST HOMOLOG 2 INHIBITORS |
US20150313906A1 (en) | 2012-12-19 | 2015-11-05 | Glaxosmithkline Llc | Combination |
WO2014100646A1 (en) | 2012-12-21 | 2014-06-26 | Epizyme, Inc. | 1,4-pyridone compounds |
UA111305C2 (uk) * | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
US9701666B2 (en) | 2012-12-21 | 2017-07-11 | Epizyme, Inc. | 1,4-pyridone bicyclic heteroaryl compounds |
KR102219441B1 (ko) | 2013-02-11 | 2021-02-23 | 콘스텔레이션 파마슈티칼스, 인크. | 메틸 변형 효소 조절제, 이의 조성물 및 용도 |
EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
EA030196B1 (ru) * | 2013-04-30 | 2018-07-31 | Глэксосмитклайн Интеллекчуал Проперти (No.2) Лимитед | Ингибиторы энхансера zeste гомолога 2 |
RU2016104044A (ru) | 2013-07-10 | 2017-08-15 | Глэксосмитклайн Интеллекчуал Проперти (Nо.2) Лимитед | Ингибиторы усилителя zeste гомолога 2 |
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TW201636344A (zh) | 2014-12-05 | 2016-10-16 | 美國禮來大藥廠 | Ezh2抑制劑 |
WO2016102493A1 (en) | 2014-12-22 | 2016-06-30 | Bayer Pharma Aktiengesellschaft | Imidazopyridine ezh2 inhibitors |
US20180037568A1 (en) | 2015-02-13 | 2018-02-08 | 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 SI SI201630453T patent/SI3341379T1/sl unknown
- 2016-08-22 ES ES16757513T patent/ES2756603T3/es active Active
- 2016-08-22 US US15/242,638 patent/US9718838B2/en active Active
- 2016-08-22 BR BR112018003108-9A patent/BR112018003108A2/pt not_active Application Discontinuation
- 2016-08-22 RS RS20191526A patent/RS59615B1/sr unknown
- 2016-08-22 TN TNP/2018/000058A patent/TN2018000058A1/en unknown
- 2016-08-22 LT LT16757513T patent/LT3341379T/lt unknown
- 2016-08-22 DK DK16757513T patent/DK3341379T3/da active
- 2016-08-22 ME MEP-2019-322A patent/ME03650B/me unknown
- 2016-08-22 WO PCT/US2016/047989 patent/WO2017035060A1/en active Application Filing
- 2016-08-22 HU HUE16757513A patent/HUE047630T2/hu unknown
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