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
- 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.)
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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 (enExample) | 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)
| Country | Link |
|---|---|
| US (3) | US9695179B2 (enExample) |
| EP (1) | EP2968360B1 (enExample) |
| JP (1) | JP6464139B2 (enExample) |
| KR (1) | KR20150135359A (enExample) |
| CN (1) | CN105407894A (enExample) |
| AU (1) | AU2014244426B2 (enExample) |
| BR (1) | BR112015022417A2 (enExample) |
| CA (1) | CA2905451A1 (enExample) |
| EA (1) | EA201591746A1 (enExample) |
| HK (1) | HK1222793A1 (enExample) |
| MX (1) | MX367420B (enExample) |
| WO (1) | WO2014159837A1 (enExample) |
Families Citing this family (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK2118074T3 (en) | 2007-02-01 | 2014-03-10 | Resverlogix Corp | Compounds for the prevention and treatment of cardiovascular diseases |
| CN105859639A (zh) | 2009-03-18 | 2016-08-17 | 雷斯韦洛吉克斯公司 | 新的抗炎剂 |
| JP5992049B2 (ja) | 2011-11-01 | 2016-09-14 | レスバーロジックス コーポレイション | 置換されたキナゾリノンのための経口速放性製剤 |
| WO2014080291A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Biaryl derivatives as bromodomain inhibitors |
| WO2014080290A2 (en) | 2012-11-21 | 2014-05-30 | Rvx Therapeutics Inc. | Cyclic amines as bromodomain inhibitors |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| AU2014216178B2 (en) | 2013-02-15 | 2018-06-28 | KALA BIO, 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 |
| EP2958895B1 (en) | 2013-02-20 | 2020-08-19 | Kala Pharmaceuticals, Inc. | Therapeutic compounds and uses thereof |
| BR112015022417A2 (pt) | 2013-03-14 | 2017-07-18 | Convergene Llc | métodos e composições para inibição de proteínas contendo bromodomínio |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| TWI719464B (zh) | 2013-03-15 | 2021-02-21 | 美商英塞特控股公司 | 作為bet蛋白抑制劑之三環雜環 |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
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| CN105102452B (zh) * | 2013-04-26 | 2018-01-26 | 百济神州有限公司 | 取代的5‑(3,5‑二甲基异噁唑‑4‑基)二氢吲哚‑2‑酮类衍生物 |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| ES2661437T3 (es) | 2013-06-21 | 2018-04-02 | Zenith Epigenetics Corp. | Nuevos compuestos bicíclicos sustituidos como inhibidores de bromodominio |
| JP2016523964A (ja) | 2013-07-08 | 2016-08-12 | インサイト・ホールディングス・コーポレイションＩｎｃｙｔｅ Ｈｏｌｄｉｎｇｓ Ｃｏｒｐｏｒａｔｉｏｎ | Ｂｅｔタンパク質阻害剤としての三環式複素環 |
| CN105593224B (zh) | 2013-07-31 | 2021-05-25 | 恒元生物医药科技(苏州)有限公司 | 作为溴结构域抑制剂的新型喹唑啉酮类化合物 |
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| KR20240134245A (ko) | 2014-04-23 | 2024-09-06 | 인사이트 홀딩스 코포레이션 | BET 단백질의 저해제로서의 1H-피롤로[2,3-c]피리딘-7(6H)-온 및 피라졸로[3,4-c]피리딘-7(6H)-온 |
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| CN107207486A (zh) * | 2014-11-13 | 2017-09-26 | 康威基内有限公司 | 用于抑制布罗莫结构域和末端外蛋白质的方法和组合 |
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| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| EA201792214A1 (ru) | 2015-04-10 | 2018-01-31 | Араксис Фарма Ллк | Соединения замещенного хиназолина |
| EP3283462B1 (en) | 2015-04-15 | 2020-12-02 | Araxes Pharma LLC | Fused-tricyclic inhibitors of kras and methods of use thereof |
| KR20180022992A (ko) * | 2015-07-02 | 2018-03-06 | 오리온 코포레이션 | 브로모도메인 억제제로서 바이사이클릭 헤테로사이클 유도체 |
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-
2014
- 2014-03-13 BR BR112015022417A patent/BR112015022417A2/pt not_active IP Right Cessation
- 2014-03-13 US US14/774,387 patent/US9695179B2/en not_active Expired - Fee Related
- 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 KR KR1020157029249A patent/KR20150135359A/ko not_active Abandoned
- 2014-03-13 EA EA201591746A patent/EA201591746A1/ru unknown
- 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 CA CA2905451A patent/CA2905451A1/en not_active Abandoned
- 2014-03-13 HK HK16110964.3A patent/HK1222793A1/zh unknown
- 2014-03-13 AU AU2014244426A patent/AU2014244426B2/en not_active Ceased
- 2014-03-13 WO PCT/US2014/025289 patent/WO2014159837A1/en not_active Ceased
-
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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