RU2017118165A - Ингибиторы энхансера гомолога 2 zestes - Google Patents
Ингибиторы энхансера гомолога 2 zestes Download PDFInfo
- Publication number
- RU2017118165A RU2017118165A RU2017118165A RU2017118165A RU2017118165A RU 2017118165 A RU2017118165 A RU 2017118165A RU 2017118165 A RU2017118165 A RU 2017118165A RU 2017118165 A RU2017118165 A RU 2017118165A RU 2017118165 A RU2017118165 A RU 2017118165A
- Authority
- RU
- Russia
- Prior art keywords
- methyl
- oxo
- dimethyl
- dihydropyridin
- carboxamide
- Prior art date
Links
- 239000003623 enhancer Substances 0.000 title 1
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 17
- -1 oxazolylmethyl Chemical group 0.000 claims 14
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 210000004907 gland Anatomy 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- DAUYIKBTMNZABP-UHFFFAOYSA-N thiophene-3-carboxamide Chemical compound NC(=O)C=1C=CSC=1 DAUYIKBTMNZABP-UHFFFAOYSA-N 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 208000012609 Cowden disease Diseases 0.000 claims 1
- 206010014967 Ependymoma Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 206010018338 Glioma Diseases 0.000 claims 1
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims 1
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims 1
- 208000005726 Inflammatory Breast Neoplasms Diseases 0.000 claims 1
- 206010021980 Inflammatory carcinoma of the breast Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 208000000172 Medulloblastoma Diseases 0.000 claims 1
- 208000008770 Multiple Hamartoma Syndrome Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 208000008383 Wilms tumor Diseases 0.000 claims 1
- 210000000988 bone and bone Anatomy 0.000 claims 1
- 210000000481 breast Anatomy 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 210000001072 colon Anatomy 0.000 claims 1
- 125000004093 cyano group Chemical group *C#N 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 210000003128 head Anatomy 0.000 claims 1
- 201000004653 inflammatory breast carcinoma Diseases 0.000 claims 1
- 210000003734 kidney Anatomy 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 210000004185 liver Anatomy 0.000 claims 1
- 210000004072 lung Anatomy 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 210000003739 neck Anatomy 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 210000001672 ovary Anatomy 0.000 claims 1
- 210000000496 pancreas Anatomy 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 210000002784 stomach Anatomy 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 210000001685 thyroid gland Anatomy 0.000 claims 1
- 210000003932 urinary bladder Anatomy 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms 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
- A61K31/435—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
- A61K31/4436—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/4535—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a heterocyclic ring having sulfur as a ring hetero atom, e.g. pizotifen
-
- 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
-
- 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
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
-
- 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
- C07D495/06—Peri-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462069438P | 2014-10-28 | 2014-10-28 | |
| US62/069,438 | 2014-10-28 | ||
| US201462075596P | 2014-11-05 | 2014-11-05 | |
| US62/075,596 | 2014-11-05 | ||
| PCT/EP2015/075009 WO2016066697A1 (en) | 2014-10-28 | 2015-10-28 | Enhancer of zeste homolog 2 inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| RU2017118165A true RU2017118165A (ru) | 2018-11-29 |
| RU2017118165A3 RU2017118165A3 (https=) | 2018-12-10 |
Family
ID=54360465
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2017118165A RU2017118165A (ru) | 2014-10-28 | 2015-10-28 | Ингибиторы энхансера гомолога 2 zestes |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20170334891A1 (https=) |
| EP (1) | EP3212639A1 (https=) |
| JP (1) | JP6571180B2 (https=) |
| KR (1) | KR20170068603A (https=) |
| CN (1) | CN107148419A (https=) |
| AU (1) | AU2015340614B2 (https=) |
| BR (1) | BR112017008840A2 (https=) |
| CA (1) | CA2965729A1 (https=) |
| MA (1) | MA40848A (https=) |
| RU (1) | RU2017118165A (https=) |
| WO (1) | WO2016066697A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UY36758A (es) * | 2015-06-30 | 2016-12-30 | Glaxosmithkline Ip No 2 Ltd | Inhibidores del potenciador del homólogo zeste 2 |
| TW201718598A (zh) | 2015-08-27 | 2017-06-01 | 美國禮來大藥廠 | Ｅｚｈ２抑制劑 |
| KR20190003699A (ko) * | 2016-05-05 | 2019-01-09 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | 제스트 인핸서 상동체 2 억제제 |
| TW201831181A (zh) | 2017-01-19 | 2018-09-01 | 日商第一三共股份有限公司 | 用以用於治療ｈｔｌｖ－１相關脊髓病之醫藥組成物 |
| US10266542B2 (en) | 2017-03-15 | 2019-04-23 | Mirati Therapeutics, Inc. | EZH2 inhibitors |
| WO2018177993A1 (de) | 2017-03-31 | 2018-10-04 | Bayer Cropscience Aktiengesellschaft | Pyrazole zur bekämpfung von arthropoden |
| MX2020007974A (es) | 2018-01-31 | 2020-09-07 | Mirati Therapeutics Inc | Inhibidores de complejo represivo polycomb 2 (prc2). |
| HRP20240793T1 (hr) | 2018-04-18 | 2024-09-13 | Constellation Pharmaceuticals, Inc. | Modulatori enzima koji modificiraju metil, njihovi pripravci i upotreba |
| EP3797108B1 (en) | 2018-05-21 | 2022-07-20 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| EP3823671B1 (en) | 2018-07-09 | 2024-02-07 | Fondation Asile Des Aveugles | Inhibition of prc2 subunits to treat eye disorders |
| US12421228B2 (en) | 2019-04-22 | 2025-09-23 | Mirati Therapeutics, Inc. | Naphthyridine derivatives as PRC2 inhibitors |
| EP3980422A1 (en) | 2019-06-05 | 2022-04-13 | Mirati Therapeutics, Inc. | Imidazo[1,2-c]pyrimidine derivatives as prc2 inhibitors for treating cancer |
| MX2022000933A (es) * | 2019-07-24 | 2022-05-06 | Constellation Pharmaceuticals Inc | Inhibición de ezh2 en tratamientos combinados para el tratamiento del cáncer. |
| LT4003532T (lt) | 2019-07-24 | 2024-11-11 | Constellation Pharmaceuticals, Inc. | 7-chlor-2- (4-(3-metoksiazetidin-1-il)cikloheksil)-2,4-dimetil-n-((6-metil-4-(metiltio)-2-okso-1,2-dihidropiridin-3-il)metil)benzo[d][1,3]dioksol-5-karboksamido kristalinės formos |
| CN114555112A (zh) | 2019-08-22 | 2022-05-27 | 朱诺治疗学股份有限公司 | T细胞疗法和zeste增强子同源物2(ezh2)抑制剂的组合疗法及相关方法 |
| CN110950834A (zh) * | 2019-11-26 | 2020-04-03 | 济南大学 | 新型eed-ezh2相互作用小分子抑制剂的确定和评价 |
| EP4514391A1 (en) | 2022-04-27 | 2025-03-05 | Daiichi Sankyo Company, Limited | Combination of antibody-drug conjugate with ezh1 and/or ezh2 inhibitor |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA023788B1 (ru) * | 2010-05-07 | 2016-07-29 | ГЛЭКСОСМИТКЛАЙН ЭлЭлСи | Производные индола и фармацевтические композиции на их основе |
| TW201733984A (zh) * | 2011-04-13 | 2017-10-01 | 雅酶股份有限公司 | 經取代之苯化合物 |
| JO3363B1 (ar) * | 2011-04-13 | 2019-03-13 | Epizyme Inc | مركبات بنزين مستبدلة بأريل أو أريل غير متجانس |
| CN104039956A (zh) * | 2011-11-04 | 2014-09-10 | 葛兰素史密斯克莱知识产权（第2号）有限公司 | 治疗方法 |
| JP5989805B2 (ja) * | 2012-02-10 | 2016-09-07 | コンステレーション・ファーマシューティカルズ・インコーポレイテッドＣｏｎｓｔｅｌｌａｔｉｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ，Ｉｎｃ． | メチル基変更酵素の調節物質、組成物及びその使用 |
| UA111305C2 (uk) * | 2012-12-21 | 2016-04-11 | Пфайзер Інк. | Конденсовані лактами арилу та гетероарилу |
| WO2014177982A1 (en) * | 2013-04-30 | 2014-11-06 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of zeste homolog 2 inhibitors |
| AU2014288839B2 (en) * | 2013-07-10 | 2017-02-02 | Glaxosmithkline Intellectual Property (No.2) Limited | Enhancer of Zeste Homolog 2 inhibitors |
-
2015
- 2015-10-28 BR BR112017008840A patent/BR112017008840A2/pt not_active Application Discontinuation
- 2015-10-28 CA CA2965729A patent/CA2965729A1/en not_active Abandoned
- 2015-10-28 EP EP15786958.7A patent/EP3212639A1/en not_active Withdrawn
- 2015-10-28 CN CN201580058856.7A patent/CN107148419A/zh active Pending
- 2015-10-28 KR KR1020177014034A patent/KR20170068603A/ko not_active Withdrawn
- 2015-10-28 AU AU2015340614A patent/AU2015340614B2/en not_active Ceased
- 2015-10-28 JP JP2017522890A patent/JP6571180B2/ja not_active Expired - Fee Related
- 2015-10-28 US US15/522,373 patent/US20170334891A1/en not_active Abandoned
- 2015-10-28 WO PCT/EP2015/075009 patent/WO2016066697A1/en not_active Ceased
- 2015-10-28 MA MA040848A patent/MA40848A/fr unknown
- 2015-10-28 RU RU2017118165A patent/RU2017118165A/ru not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20170334891A1 (en) | 2017-11-23 |
| BR112017008840A2 (pt) | 2017-12-19 |
| WO2016066697A1 (en) | 2016-05-06 |
| JP6571180B2 (ja) | 2019-09-04 |
| MA40848A (fr) | 2021-05-05 |
| CA2965729A1 (en) | 2016-05-06 |
| AU2015340614B2 (en) | 2018-07-19 |
| EP3212639A1 (en) | 2017-09-06 |
| CN107148419A (zh) | 2017-09-08 |
| JP2017532360A (ja) | 2017-11-02 |
| AU2015340614A1 (en) | 2017-05-18 |
| RU2017118165A3 (https=) | 2018-12-10 |
| KR20170068603A (ko) | 2017-06-19 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA94 | Acknowledgement of application withdrawn (non-payment of fees) |
Effective date: 20200825 |