JP2017521489A5 - - Google Patents
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- Publication number
- JP2017521489A5 JP2017521489A5 JP2017518041A JP2017518041A JP2017521489A5 JP 2017521489 A5 JP2017521489 A5 JP 2017521489A5 JP 2017518041 A JP2017518041 A JP 2017518041A JP 2017518041 A JP2017518041 A JP 2017518041A JP 2017521489 A5 JP2017521489 A5 JP 2017521489A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- methyl
- chloro
- ethyl
- alkyl
- Prior art date
- Legal status (The legal status 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 status listed.)
- Granted
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- -1 cyanomethoxy Chemical group 0.000 claims description 156
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 104
- 125000000217 alkyl group Chemical group 0.000 claims description 81
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 76
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical group N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 42
- 229910052736 halogen Inorganic materials 0.000 claims description 38
- 150000002367 halogens Chemical class 0.000 claims description 38
- 150000001875 compounds Chemical class 0.000 claims description 37
- 125000003545 alkoxy group Chemical group 0.000 claims description 35
- 125000001246 bromo group Chemical group Br* 0.000 claims description 24
- 229910052757 nitrogen Chemical group 0.000 claims description 24
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 22
- 125000005119 alkyl cycloalkyl group Chemical group 0.000 claims description 21
- 125000004429 atom Chemical group 0.000 claims description 21
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 20
- 125000003118 aryl group Chemical group 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 18
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 18
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 16
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 16
- 229910052717 sulfur Inorganic materials 0.000 claims description 16
- 239000011593 sulfur Substances 0.000 claims description 16
- 125000000623 heterocyclic group Chemical group 0.000 claims description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims description 15
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 14
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 229910052760 oxygen Inorganic materials 0.000 claims description 14
- 239000001301 oxygen Chemical group 0.000 claims description 14
- 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims description 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 12
- 125000005842 heteroatom Chemical group 0.000 claims description 12
- 208000015181 infectious disease Diseases 0.000 claims description 12
- 125000002252 acyl group Chemical group 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 10
- 125000005309 thioalkoxy group Chemical group 0.000 claims description 8
- 241000124008 Mammalia Species 0.000 claims description 7
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims description 6
- 125000001340 2-chloroethyl group Chemical group [H]C([H])(Cl)C([H])([H])* 0.000 claims description 6
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 6
- 125000006479 2-pyridyl methyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims description 6
- QOXOZONBQWIKDA-UHFFFAOYSA-N 3-hydroxypropyl Chemical group [CH2]CCO QOXOZONBQWIKDA-UHFFFAOYSA-N 0.000 claims description 6
- 102100034051 Heat shock protein HSP 90-alpha Human genes 0.000 claims description 6
- 101001016865 Homo sapiens Heat shock protein HSP 90-alpha Proteins 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 6
- 125000001028 difluoromethyl group Chemical group [H]C(F)(F)* 0.000 claims description 6
- 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims description 6
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 6
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 6
- 230000004770 neurodegeneration Effects 0.000 claims description 6
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 6
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000035473 Communicable disease Diseases 0.000 claims description 4
- 241000711950 Filoviridae Species 0.000 claims description 4
- 201000011240 Frontotemporal dementia Diseases 0.000 claims description 4
- 241000712907 Retroviridae Species 0.000 claims description 4
- 241000711931 Rhabdoviridae Species 0.000 claims description 4
- 125000000051 benzyloxy group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])O* 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 0.000 claims description 4
- 230000002757 inflammatory effect Effects 0.000 claims description 4
- 125000004001 thioalkyl group Chemical group 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 241000700739 Hepadnaviridae Species 0.000 claims description 3
- 241000709664 Picornaviridae Species 0.000 claims description 3
- 241000700605 Viruses Species 0.000 claims description 3
- 230000002062 proliferating effect Effects 0.000 claims description 3
- 230000003612 virological effect Effects 0.000 claims description 3
- 125000000979 2-amino-2-oxoethyl group Chemical group [H]C([*])([H])C(=O)N([H])[H] 0.000 claims description 2
- 241000712892 Arenaviridae Species 0.000 claims description 2
- 201000001320 Atherosclerosis Diseases 0.000 claims description 2
- 208000035143 Bacterial infection Diseases 0.000 claims description 2
- 208000004051 Chronic Traumatic Encephalopathy Diseases 0.000 claims description 2
- 241000710781 Flaviviridae Species 0.000 claims description 2
- 206010017533 Fungal infection Diseases 0.000 claims description 2
- 101710113864 Heat shock protein 90 Proteins 0.000 claims description 2
- 241001122120 Hepeviridae Species 0.000 claims description 2
- 241000700586 Herpesviridae Species 0.000 claims description 2
- 208000023105 Huntington disease Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 208000031888 Mycoses Diseases 0.000 claims description 2
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 206010033799 Paralysis Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 208000000609 Pick Disease of the Brain Diseases 0.000 claims description 2
- 241001631648 Polyomaviridae Species 0.000 claims description 2
- 241000700625 Poxviridae Species 0.000 claims description 2
- 241000702247 Reoviridae Species 0.000 claims description 2
- 208000034799 Tauopathies Diseases 0.000 claims description 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 2
- 208000026935 allergic disease Diseases 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 125000004103 aminoalkyl group Chemical group 0.000 claims description 2
- 208000006673 asthma Diseases 0.000 claims description 2
- 208000022362 bacterial infectious disease Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 208000017004 dementia pugilistica Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 230000000750 progressive effect Effects 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims description 2
- 230000009529 traumatic brain injury Effects 0.000 claims description 2
- XLSZMDLNRCVEIJ-UHFFFAOYSA-N 4-methylimidazole Chemical compound CC1=CNC=N1 XLSZMDLNRCVEIJ-UHFFFAOYSA-N 0.000 claims 6
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 5
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 3
- 125000000547 substituted alkyl group Chemical group 0.000 claims 3
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
- 241000702628 Birnaviridae Species 0.000 claims 1
- 241000712464 Orthomyxoviridae Species 0.000 claims 1
- 210000004227 basal ganglia Anatomy 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 24
- 0 C=C(C1)C1NC(C(S)=*)=O Chemical compound C=C(C1)C1NC(C(S)=*)=O 0.000 description 3
- 125000001539 acetonyl group Chemical group [H]C([H])([H])C(=O)C([H])([H])* 0.000 description 3
- FXBQZODCHGJETH-DAXSKMNVSA-N CC(C)/C=C(/C(C)=O)\N Chemical compound CC(C)/C=C(/C(C)=O)\N FXBQZODCHGJETH-DAXSKMNVSA-N 0.000 description 1
- 208000011990 Corticobasal Degeneration Diseases 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- 208000036142 Viral infection Diseases 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000007917 intracranial administration Methods 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 238000007913 intrathecal administration Methods 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 230000009385 viral infection Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462012152P | 2014-06-13 | 2014-06-13 | |
| US62/012,152 | 2014-06-13 | ||
| PCT/US2015/035735 WO2015192119A1 (en) | 2014-06-13 | 2015-06-15 | Pyrimidine compounds and methods using the same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017521489A JP2017521489A (ja) | 2017-08-03 |
| JP2017521489A5 true JP2017521489A5 (enExample) | 2018-07-26 |
| JP6779867B2 JP6779867B2 (ja) | 2020-11-04 |
Family
ID=54834482
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017518041A Active JP6779867B2 (ja) | 2014-06-13 | 2015-06-15 | ピリミジン化合物およびその使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US10336768B2 (enExample) |
| EP (1) | EP3154547B1 (enExample) |
| JP (1) | JP6779867B2 (enExample) |
| CN (1) | CN106687114B (enExample) |
| AU (1) | AU2015274285C1 (enExample) |
| CA (1) | CA2952230C (enExample) |
| ES (1) | ES2954453T3 (enExample) |
| WO (1) | WO2015192119A1 (enExample) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3154547B1 (en) * | 2014-06-13 | 2023-06-07 | Yuma Therapeutics, Inc. | Pyrimidine compounds and methods using the same |
| KR20190043437A (ko) | 2017-10-18 | 2019-04-26 | 씨제이헬스케어 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| KR102195348B1 (ko) | 2018-11-15 | 2020-12-24 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물 |
| JP7156154B2 (ja) * | 2019-04-18 | 2022-10-19 | 株式会社島津製作所 | 培地処理システム及び培地処理方法 |
| KR102112336B1 (ko) * | 2019-08-12 | 2020-05-18 | 에이치케이이노엔 주식회사 | 단백질 키나제 억제제로서의 헤테로고리 화합물 |
| US20230390416A1 (en) * | 2020-10-16 | 2023-12-07 | The Brigham And Women's Hospital, Inc. | Compositions for inducing tumor immunity and reducing drug tolerance |
Family Cites Families (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2691655A (en) * | 1952-05-24 | 1954-10-12 | Burroughs Wellcome Co | 2-amino-4-substituted amino-6-aryl pyrimidines and process of preparing same |
| DE3815221C2 (de) | 1988-05-04 | 1995-06-29 | Gradinger F Hermes Pharma | Verwendung einer Retinol- und/oder Retinsäureester enthaltenden pharmazeutischen Zubereitung zur Inhalation zur Einwirkung auf die Schleimhäute des Tracheo-Bronchialtraktes einschließlich der Lungenalveolen |
| TW440563B (en) * | 1996-05-23 | 2001-06-16 | Hoffmann La Roche | Aryl pyrimidine derivatives and a pharmaceutical composition thereof |
| DE19735800A1 (de) * | 1997-08-18 | 1999-02-25 | Boehringer Ingelheim Pharma | Triazine mit adenosinantagonistischer Wirkung |
| ES2559779T3 (es) | 2003-08-29 | 2016-02-15 | Vernalis (R&D) Limited | Compuestos de pirimidotiofeno |
| GB0416168D0 (en) * | 2004-07-20 | 2004-08-18 | Vernalis Cambridge Ltd | Pyrmidothiophene compounds |
| WO2006090094A1 (en) | 2005-02-28 | 2006-08-31 | Vernalis R & D Ltd | Pyrimidothiophene compounds for use as hsp90 inhibitors |
| DE102005022977A1 (de) * | 2005-05-19 | 2006-12-07 | Merck Patent Gmbh | Phenylchinazolinderivate |
| WO2006123165A2 (en) * | 2005-05-19 | 2006-11-23 | Astex Therapeutics Limited | Pyrimidine derivatives as hsp90 inhibitors |
| DE102006008880A1 (de) * | 2006-02-27 | 2007-09-06 | Merck Patent Gmbh | Aminopyrimidinderivate |
| CA2645343A1 (en) | 2006-03-11 | 2007-09-20 | Vernalis (R&D) Limited | Pyrrolopyrimidine derivatives used as hsp90 inhibitors |
| AR061185A1 (es) | 2006-05-26 | 2008-08-13 | Chugai Pharmaceutical Co Ltd | Compuestos heterociclicos como inhibidores de hsp90. composiciones farmaceuticas. |
| WO2008059368A2 (en) * | 2006-11-17 | 2008-05-22 | Pfizer Products Inc. | Fused 2-amino pyrimidine compounds and their use for the treatment of cancer |
| WO2008096218A1 (en) * | 2007-02-06 | 2008-08-14 | Pfizer Inc. | 2-amin0-5, 7-dihydr0-6h- pyrrolo [3, 4-d] pyrimidine derivatives as hsp-90 inhibitors for treating cancer |
| JP2009067729A (ja) * | 2007-09-14 | 2009-04-02 | Kyowa Hakko Kirin Co Ltd | Ｈｓｐ９０ファミリー蛋白質阻害剤 |
| US20110201587A1 (en) | 2010-02-16 | 2011-08-18 | Bio Holding, Inc. | Hsp90 inhibitors and methods of use |
| US9481670B2 (en) | 2011-01-25 | 2016-11-01 | Sphaera Pharma Pte. Ltd. | Triazine compounds |
| WO2013157021A1 (en) * | 2012-04-20 | 2013-10-24 | Advinus Therapeutics Limited | Bicyclic compounds, compositions and medicinal applications thereof |
| EA201492184A1 (ru) * | 2012-05-25 | 2015-07-30 | Берг Ллк | Способы лечения метаболического синдрома путем модулирования белка теплового шока (hsp) 90-бета |
| PE20151412A1 (es) * | 2012-11-27 | 2015-10-10 | Thomas Helledays Stiftelse For Medicinsk Forskning | Derivados de pirimidin-2,4-diamina para el tratamiento de cancer |
| CN106794181A (zh) | 2014-06-04 | 2017-05-31 | 托马斯·黑勒戴药物研究基金会 | 用于治疗炎性和自身免疫性病况的mth1抑制剂 |
| EP3154547B1 (en) * | 2014-06-13 | 2023-06-07 | Yuma Therapeutics, Inc. | Pyrimidine compounds and methods using the same |
| WO2016044781A1 (en) * | 2014-09-19 | 2016-03-24 | Forma Therapeutics, Inc. | Quinolinone pyrimidines compositions as mutant-isocitrate dehydrogenase inhibitors |
-
2015
- 2015-06-15 EP EP15806816.3A patent/EP3154547B1/en active Active
- 2015-06-15 WO PCT/US2015/035735 patent/WO2015192119A1/en not_active Ceased
- 2015-06-15 US US15/317,999 patent/US10336768B2/en active Active
- 2015-06-15 JP JP2017518041A patent/JP6779867B2/ja active Active
- 2015-06-15 CN CN201580043036.0A patent/CN106687114B/zh active Active
- 2015-06-15 AU AU2015274285A patent/AU2015274285C1/en active Active
- 2015-06-15 CA CA2952230A patent/CA2952230C/en active Active
- 2015-06-15 ES ES15806816T patent/ES2954453T3/es active Active
-
2019
- 2019-07-01 US US16/459,138 patent/US10961254B2/en active Active
-
2021
- 2021-03-29 US US17/216,076 patent/US20210363154A1/en not_active Abandoned
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