JP2016514147A5 - - Google Patents
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- JP2016514147A5 JP2016514147A5 JP2016501811A JP2016501811A JP2016514147A5 JP 2016514147 A5 JP2016514147 A5 JP 2016514147A5 JP 2016501811 A JP2016501811 A JP 2016501811A JP 2016501811 A JP2016501811 A JP 2016501811A JP 2016514147 A5 JP2016514147 A5 JP 2016514147A5
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- Prior art keywords
- substituted
- unsubstituted
- hydrogen
- alkyl
- compound
- Prior art date
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- 229910052739 hydrogen Inorganic materials 0.000 claims 68
- 239000001257 hydrogen Substances 0.000 claims 68
- 125000000217 alkyl group Chemical group 0.000 claims 57
- 150000001875 compounds Chemical class 0.000 claims 51
- 125000001072 heteroaryl group Chemical group 0.000 claims 45
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 42
- 125000003118 aryl group Chemical group 0.000 claims 36
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 29
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 26
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 26
- 125000005842 heteroatom Chemical group 0.000 claims 22
- 125000003545 alkoxy group Chemical group 0.000 claims 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 21
- 125000005309 thioalkoxy group Chemical group 0.000 claims 21
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 20
- 150000002367 halogens Chemical class 0.000 claims 20
- 229910052760 oxygen Inorganic materials 0.000 claims 20
- 229910052717 sulfur Inorganic materials 0.000 claims 19
- 125000001424 substituent group Chemical group 0.000 claims 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims 17
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 14
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- 239000001301 oxygen Substances 0.000 claims 14
- 239000011593 sulfur Substances 0.000 claims 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- 125000003710 aryl alkyl group Chemical group 0.000 claims 8
- 125000004404 heteroalkyl group Chemical group 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 4
- 125000002950 monocyclic group Chemical group 0.000 claims 4
- 108091005646 acetylated proteins Proteins 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 108091005575 Bromodomain-containing proteins Proteins 0.000 claims 2
- 102000001805 Bromodomains Human genes 0.000 claims 2
- 125000004122 cyclic group Chemical group 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 230000002401 inhibitory effect Effects 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- YTDWXVPNUKQSOW-UHFFFAOYSA-N 4-(benzylamino)-1-benzylsulfonyl-6-(3,5-dimethyl-1,2-oxazol-4-yl)quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2n(c(=O)cc(NCc3ccccc3)c2c1)S(=O)(=O)Cc1ccccc1 YTDWXVPNUKQSOW-UHFFFAOYSA-N 0.000 claims 1
- ZZEQMSXTKAJTLH-UHFFFAOYSA-N 4-(benzylamino)-6-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2[nH]c(=O)cc(NCc3ccccc3)c2c1 ZZEQMSXTKAJTLH-UHFFFAOYSA-N 0.000 claims 1
- ZLSFHNBGYXITTM-UHFFFAOYSA-N 4-[(2-chlorophenyl)methylamino]-6-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2[nH]c(=O)cc(NCc3ccccc3Cl)c2c1 ZLSFHNBGYXITTM-UHFFFAOYSA-N 0.000 claims 1
- JZMJFRBVEUASSI-UHFFFAOYSA-N 4-chloro-6-(3,5-dimethyl-1,2-oxazol-4-yl)-1H-quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2[nH]c(=O)cc(Cl)c2c1 JZMJFRBVEUASSI-UHFFFAOYSA-N 0.000 claims 1
- GUINEUSEISTICJ-UHFFFAOYSA-N 6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-hydroxy-1H-quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2[nH]c(=O)cc(O)c2c1 GUINEUSEISTICJ-UHFFFAOYSA-N 0.000 claims 1
- CQBPUBOCBYCHQV-UHFFFAOYSA-N 6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-morpholin-4-yl-1H-quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2[nH]c(=O)cc(N3CCOCC3)c2c1 CQBPUBOCBYCHQV-UHFFFAOYSA-N 0.000 claims 1
- MXIMZZRBWSDGFZ-UHFFFAOYSA-N 6-(3,5-dimethyl-1,2-oxazol-4-yl)-4-piperidin-1-yl-1H-quinolin-2-one Chemical compound Cc1noc(C)c1-c1ccc2[nH]c(=O)cc(N3CCCCC3)c2c1 MXIMZZRBWSDGFZ-UHFFFAOYSA-N 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000011691 Burkitt lymphomas Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 108010033040 Histones Proteins 0.000 claims 1
- 101001122114 Homo sapiens NUT family member 1 Proteins 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- LDOIFKDOYRRTCR-UHFFFAOYSA-N N,N'-bis[4-(3,5-dimethyl-1,2-oxazol-4-yl)phenyl]propanediamide Chemical compound CC1=NOC(=C1C1=CC=C(C=C1)NC(CC(=O)NC1=CC=C(C=C1)C=1C(=NOC1C)C)=O)C LDOIFKDOYRRTCR-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010039491 Sarcoma Diseases 0.000 claims 1
- 210000001744 T-lymphocyte Anatomy 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 1
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 1
- 102000057037 human NUTM1 Human genes 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000003747 lymphoid leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 208000025113 myeloid leukemia Diseases 0.000 claims 1
- PRVAKTGWODYESP-UHFFFAOYSA-N n,n'-bis(4-bromophenyl)propanediamide Chemical compound C1=CC(Br)=CC=C1NC(=O)CC(=O)NC1=CC=C(Br)C=C1 PRVAKTGWODYESP-UHFFFAOYSA-N 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 230000014493 regulation of gene expression Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 0 *C(*)=C(C(*)=N)c(c(*)cc1c2N3*)cc1ncc2N(*)C3=* Chemical compound *C(*)=C(C(*)=N)c(c(*)cc1c2N3*)cc1ncc2N(*)C3=* 0.000 description 3
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361781988P | 2013-03-14 | 2013-03-14 | |
| US61/781,988 | 2013-03-14 | ||
| PCT/US2014/025289 WO2014159837A1 (en) | 2013-03-14 | 2014-03-13 | Methods and compositions for inhibition of bromodomain-containing proteins |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016514147A JP2016514147A (ja) | 2016-05-19 |
| JP2016514147A5 true JP2016514147A5 (cg-RX-API-DMAC10.html) | 2017-04-13 |
| JP6464139B2 JP6464139B2 (ja) | 2019-02-06 |
Family
ID=51625268
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016501811A Expired - Fee Related JP6464139B2 (ja) | 2013-03-14 | 2014-03-13 | ブロモドメイン含有タンパク質の阻害のための方法および組成物 |
Country Status (12)
Families Citing this family (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2118074E (pt) | 2007-02-01 | 2014-03-20 | Resverlogix Corp | Compostos para a prevenção e tratamento de doenças cardiovasculares |
| NZ617779A (en) | 2009-03-18 | 2015-08-28 | Resverlogix Corp | Novel anti-inflammatory agents |
| PT2773354T (pt) | 2011-11-01 | 2019-07-17 | Resverlogix Corp | Formulações orais de libertação imediata para quinazolinonas substituídas |
| US9765039B2 (en) | 2012-11-21 | 2017-09-19 | Zenith Epigenetics Ltd. | Biaryl derivatives as bromodomain inhibitors |
| US9073878B2 (en) | 2012-11-21 | 2015-07-07 | Zenith Epigenetics Corp. | Cyclic amines as bromodomain inhibitors |
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| US9353122B2 (en) | 2013-02-15 | 2016-05-31 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| US9688688B2 (en) | 2013-02-20 | 2017-06-27 | Kala Pharmaceuticals, Inc. | Crystalline forms of 4-((4-((4-fluoro-2-methyl-1H-indol-5-yl)oxy)-6-methoxyquinazolin-7-yl)oxy)-1-(2-oxa-7-azaspiro[3.5]nonan-7-yl)butan-1-one and uses thereof |
| US9353123B2 (en) | 2013-02-20 | 2016-05-31 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| EA201591746A1 (ru) | 2013-03-14 | 2016-08-31 | КОНВЕРДЖЕН ЭлЭлСи | Способы и композиции для ингибирования бромодомен-содержащих белков |
| WO2014143659A1 (en) | 2013-03-15 | 2014-09-18 | Araxes Pharma Llc | Irreversible covalent inhibitors of the gtpase k-ras g12c |
| EA035469B1 (ru) | 2013-03-15 | 2020-06-22 | Инсайт Холдингс Корпорейшн | Трициклические гетероциклы как ингибиторы белков бэт |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| EA027139B1 (ru) * | 2013-04-26 | 2017-06-30 | Бейджин, Лтд. | Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны |
| KR102307566B1 (ko) | 2013-06-21 | 2021-10-05 | 제니쓰 에피제네틱스 리미티드 | 신규한 바이사이클릭 브로모도메인 억제제 |
| CN105473581B (zh) | 2013-06-21 | 2019-04-23 | 齐尼思表观遗传学有限公司 | 作为溴结构域抑制剂的新取代的双环化合物 |
| EP3019502B1 (en) | 2013-07-08 | 2017-05-17 | Incyte Holdings Corporation | Tricyclic heterocycles as bet protein inhibitors |
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| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| KR20160099084A (ko) | 2013-11-01 | 2016-08-19 | 칼라 파마슈티컬스, 인크. | 치료 화합물의 결정질 형태 및 그의 용도 |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| US9315501B2 (en) | 2013-11-26 | 2016-04-19 | Incyte Corporation | Bicyclic heterocycles as BET protein inhibitors |
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| ES2750452T3 (es) * | 2013-11-26 | 2020-03-25 | Gilead Sciences Inc | Derivados de quinolina como inhibidores del bromodominio |
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| CN108137547B (zh) | 2015-08-03 | 2021-11-12 | 百时美施贵宝公司 | 可用作TNFα调节剂的杂环化合物 |
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2014
- 2014-03-13 EA EA201591746A patent/EA201591746A1/ru unknown
- 2014-03-13 BR BR112015022417A patent/BR112015022417A2/pt not_active IP Right Cessation
- 2014-03-13 EP EP14776141.5A patent/EP2968360B1/en not_active Not-in-force
- 2014-03-13 MX MX2015012478A patent/MX367420B/es active IP Right Grant
- 2014-03-13 CN CN201480028551.7A patent/CN105407894A/zh active Pending
- 2014-03-13 JP JP2016501811A patent/JP6464139B2/ja not_active Expired - Fee Related
- 2014-03-13 US US14/774,387 patent/US9695179B2/en not_active Expired - Fee Related
- 2014-03-13 WO PCT/US2014/025289 patent/WO2014159837A1/en not_active Ceased
- 2014-03-13 KR KR1020157029249A patent/KR20150135359A/ko not_active Abandoned
- 2014-03-13 AU AU2014244426A patent/AU2014244426B2/en not_active Ceased
- 2014-03-13 CA CA2905451A patent/CA2905451A1/en not_active Abandoned
- 2014-03-13 HK HK16110964.3A patent/HK1222793A1/zh unknown
-
2017
- 2017-06-27 US US15/634,768 patent/US10266536B2/en not_active Expired - Fee Related
-
2019
- 2019-04-16 US US16/385,606 patent/US10717739B2/en not_active Expired - Fee Related
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