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 (https=) | 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 (https=) |
| EP (1) | EP2968360B1 (https=) |
| JP (1) | JP6464139B2 (https=) |
| KR (1) | KR20150135359A (https=) |
| CN (1) | CN105407894A (https=) |
| AU (1) | AU2014244426B2 (https=) |
| BR (1) | BR112015022417A2 (https=) |
| CA (1) | CA2905451A1 (https=) |
| EA (1) | EA201591746A1 (https=) |
| HK (1) | HK1222793A1 (https=) |
| MX (1) | MX367420B (https=) |
| WO (1) | WO2014159837A1 (https=) |
Families Citing this family (101)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008092231A1 (en) | 2007-02-01 | 2008-08-07 | Resverlogix Corp. | Compounds for the prevention and treatment of cardiovascular diseases |
| NZ755378A (en) | 2009-03-18 | 2022-07-29 | Resverlogix Corp | Novel quinazolinones and related compounds for use as anti-inflammatory agents |
| RU2640115C2 (ru) | 2011-11-01 | 2017-12-26 | Ресверлоджикс Корп. | Фармацевтические композиции замещенных хиназолинонов |
| 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 |
| AU2013365926B9 (en) | 2012-12-21 | 2019-01-17 | Zenith Epigenetics Ltd. | Novel heterocyclic compounds as bromodomain inhibitors |
| JP6669499B2 (ja) | 2013-02-15 | 2020-03-18 | カラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物 |
| 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 |
| JP2016510000A (ja) | 2013-02-20 | 2016-04-04 | カラ ファーマシューティカルズ インコーポレイテッド | 治療用化合物およびその使用 |
| JP6464139B2 (ja) | 2013-03-14 | 2019-02-06 | コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ | 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 |
| MX366703B (es) | 2013-03-15 | 2019-07-22 | Incyte Holdings Corp | Heterociclos tricíclicos como inhibidores de la proteína bet. |
| US9745319B2 (en) | 2013-03-15 | 2017-08-29 | Araxes Pharma Llc | Irreversible covalent inhibitors of the GTPase K-Ras G12C |
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| 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 |
| EA027139B1 (ru) | 2013-04-26 | 2017-06-30 | Бейджин, Лтд. | Замещенные 5-(3,5-диметилизоксазол-4-ил)индолин-2-оны |
| EP3010918B1 (en) | 2013-06-21 | 2018-08-15 | Zenith Epigenetics Ltd. | Novel substituted bicyclic compounds as bromodomain inhibitors |
| CA2915838C (en) | 2013-06-21 | 2023-04-18 | Zenith Epigenetics Corp. | Bicyclic bromodomain inhibitors |
| AR096837A1 (es) | 2013-07-08 | 2016-02-03 | Incyte Corp | Heterociclos tricíclicos como inhibidores de proteínas bet |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規キナゾリノン |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| NZ719185A (en) | 2013-11-01 | 2017-11-24 | Kala Pharmaceuticals Inc | Crystalline forms of therapeutic compounds and uses thereof |
| US9890173B2 (en) | 2013-11-01 | 2018-02-13 | Kala Pharmaceuticals, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| JP6262363B2 (ja) * | 2013-11-26 | 2018-01-17 | ギリアード サイエンシーズ， インコーポレイテッド | ブロモドメイン阻害剤としてのキノリン誘導体 |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| WO2015095492A1 (en) | 2013-12-19 | 2015-06-25 | Incyte Corporation | Tricyclic heterocycles as bet protein inhibitors |
| MY190835A (en) * | 2014-01-09 | 2022-05-12 | Orion Corp | Bicyclic heterrocyclic derivatives as bromodomain inhibitors |
| EA034972B1 (ru) | 2014-04-23 | 2020-04-13 | Инсайт Корпорейшн | 1h-пирроло[2,3-c]пиридин-7(6h)-оны в качестве ингибиторов белков bet |
| US9527864B2 (en) | 2014-09-15 | 2016-12-27 | Incyte Corporation | Tricyclic heterocycles as BET protein inhibitors |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| ES2826443T3 (es) | 2014-09-25 | 2021-05-18 | Araxes Pharma Llc | Inhibidores de proteínas mutantes KRAS G12C |
| CA2966908A1 (en) * | 2014-11-13 | 2016-05-19 | Convergene Llc | Methods and compositions for inhibition of bromodomain and extraterminal proteins |
| HK1246273B (en) | 2014-12-01 | 2019-12-06 | 恒翼生物医药(上海)股份有限公司 | Substituted pyridines as bromodomain inhibitors |
| EP3227281A4 (en) | 2014-12-01 | 2018-05-30 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| JP2017537940A (ja) * | 2014-12-10 | 2017-12-21 | マサチューセッツ インスティテュート オブ テクノロジー | 増殖性疾患の処置に有用な融合１，３−アゾール誘導体 |
| EP3230277B1 (en) | 2014-12-11 | 2019-09-18 | Zenith Epigenetics Ltd. | Substituted heterocycles as bromodomain inhibitors |
| HK1245247A1 (zh) | 2014-12-17 | 2018-08-24 | 恒翼生物医药科技(上海)有限公司 | 溴结构域的抑制剂 |
| US10577349B2 (en) | 2015-03-02 | 2020-03-03 | Sanford Burnham Prebys Medical Discovery Institute | Quinolinones as inhibitors of translation initiation complex |
| JO3789B1 (ar) | 2015-03-13 | 2021-01-31 | Resverlogix Corp | التراكيب والوسائل العلاجية المعتمدة لمعالجة الامراض المتعلقة بالمتممة |
| GB201504694D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Covalent conjugates |
| JP2018513853A (ja) | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| JP6789239B2 (ja) | 2015-04-15 | 2020-11-25 | アラクセス ファーマ エルエルシー | Ｋｒａｓの縮合三環系インヒビターおよびその使用の方法 |
| US20180312496A1 (en) * | 2015-07-02 | 2018-11-01 | Orion Corporation | Bicyclic heterocycle derivatives as bromodomain inhibitors |
| HK1249105A1 (zh) | 2015-07-17 | 2018-10-26 | 富士胶片富山化学株式会社 | 含氮杂环化合物 |
| CN108026046B (zh) * | 2015-07-22 | 2021-12-21 | 亚瑞克西斯制药公司 | 取代的喹唑啉化合物及其作为g12c突变体kras、hras和/或nras蛋白质的抑制剂的用途 |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| MX388781B (es) * | 2015-07-22 | 2025-03-20 | Araxes Pharma Llc | Compuestos de quinazolina sustituido y su uso como inhibidores de proteínas kras, hras y/o nras mutantes g12c. |
| PE20181366A1 (es) | 2015-08-03 | 2018-08-27 | Bristol Myers Squibb Co | Compuestos heterociclicos utiles como moduladores de factor de necrosis tumoral (tnf) alfa |
| US10836742B2 (en) | 2015-08-11 | 2020-11-17 | Neomed Institute | N-substituted bicyclic lactams, their preparation and their use as pharmaceuticals |
| WO2017024408A1 (en) | 2015-08-11 | 2017-02-16 | Neomed Institute | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
| CN108137539B (zh) | 2015-08-12 | 2022-01-11 | 尼奥迈德研究所 | 取代的苯并咪唑、它们的制备和它们作为药物的用途 |
| EP3356354A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| EP3356353A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058915A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10882847B2 (en) | 2015-09-28 | 2021-01-05 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| US10647703B2 (en) | 2015-09-28 | 2020-05-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| WO2017058807A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| JP2018533939A (ja) | 2015-10-19 | 2018-11-22 | アラクセス ファーマ エルエルシー | Ｒａｓの阻害剤をスクリーニングするための方法 |
| US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
| TW201722966A (zh) | 2015-10-29 | 2017-07-01 | 英塞特公司 | Bet蛋白質抑制劑之非晶固體形式 |
| KR20180081596A (ko) | 2015-11-16 | 2018-07-16 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| CA3006300C (en) * | 2015-11-25 | 2024-02-27 | Convergene Llc | Bicyclic bet bromodomain inhibitors and uses thereof |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017127930A1 (en) | 2016-01-28 | 2017-08-03 | Neomed Institute | Substituted [1,2,4]triazolo[4,3-a]pyridines, their preparation and their use as pharmaceuticals |
| CN109071456A (zh) | 2016-02-16 | 2018-12-21 | 麻省理工学院 | 作为myc调节剂的max结合剂及其用途 |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| KR102643344B1 (ko) | 2016-06-20 | 2024-03-07 | 인사이트 코포레이션 | Bet 저해제의 결정질 고체 형태 |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| EP3509423A4 (en) | 2016-09-08 | 2020-05-13 | Kala Pharmaceuticals, Inc. | CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF |
| AU2017324713B2 (en) | 2016-09-08 | 2020-08-13 | KALA BIO, Inc. | Crystalline forms of therapeutic compounds and uses thereof |
| KR20190051010A (ko) | 2016-09-08 | 2019-05-14 | 칼라 파마슈티컬스, 인크. | 치료 화합물의 결정형 및 그의 용도 |
| US10280172B2 (en) | 2016-09-29 | 2019-05-07 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
| CA3047098A1 (en) | 2016-12-16 | 2018-06-21 | Jia Zhou | Inhibitors of bromodomain-containing protein 4 (brd4) |
| KR102271111B1 (ko) | 2016-12-27 | 2021-06-29 | 후지필름 가부시키가이샤 | 항종양제 및 브로모도메인 저해제 |
| CN108314680A (zh) * | 2017-01-16 | 2018-07-24 | 凯惠科技发展(上海)有限公司 | 一种含芳环化合物、其制备方法、药物组合物及应用 |
| EP3573954A1 (en) | 2017-01-26 | 2019-12-04 | Araxes Pharma LLC | Fused bicyclic benzoheteroaromatic compounds and methods of use thereof |
| WO2018140599A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | Benzothiophene and benzothiazole compounds and methods of use thereof |
| CN110382482A (zh) | 2017-01-26 | 2019-10-25 | 亚瑞克西斯制药公司 | 稠合的杂-杂二环化合物及其使用方法 |
| WO2018140513A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(3-(6-(3-hydroxynaphthalen-1-yl)benzofuran-2-yl)azetidin-1yl)prop-2-en-1-one derivatives and similar compounds as kras g12c modulators for treating cancer |
| WO2018140514A1 (en) | 2017-01-26 | 2018-08-02 | Araxes Pharma Llc | 1-(6-(3-hydroxynaphthalen-1-yl)quinazolin-2-yl)azetidin-1-yl)prop-2-en-1-one derivatives and similar compounds as kras g12c inhibitors for the treatment of cancer |
| CN108658972A (zh) * | 2017-03-28 | 2018-10-16 | 中国海洋大学 | 一种取代内酰胺类化合物及其制备方法和用途 |
| CN108658855A (zh) * | 2017-03-28 | 2018-10-16 | 中国海洋大学 | 一种含氮双环化合物及其制备方法和用途 |
| JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| AU2018271990A1 (en) | 2017-05-25 | 2019-12-12 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| US11639346B2 (en) | 2017-05-25 | 2023-05-02 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant KRAS, HRAS or NRAS |
| US11389433B2 (en) | 2018-06-18 | 2022-07-19 | Board Of Regents, The University Of Texas System | BRD4 inhibitor treatment of IgE-mediated diseases |
| MX2021000887A (es) | 2018-08-01 | 2021-03-31 | Araxes Pharma Llc | Compuestos espiroheterociclicos y metodos de uso de los mismos para el tratamiento de cancer. |
| WO2020123395A1 (en) | 2018-12-10 | 2020-06-18 | Ideaya Biosciences, Inc. | 2-oxoquinazoline derivatives as methionine adenosyltransferase 2a inhibitors |
| EP4424379A3 (en) | 2019-04-24 | 2024-10-30 | Convergene Llc | Small molecule bromodomain inhibitors and uses thereof |
| WO2021021986A1 (en) | 2019-07-31 | 2021-02-04 | Ribon Therapeutics, Inc. | Heterobicyclic amides as inhibitors of cd38 |
| KR20220119456A (ko) * | 2019-12-23 | 2022-08-29 | 브리스톨-마이어스 스큅 컴퍼니 | T 세포 활성화제로서 유용한 치환된 퀴놀리노닐 피페라진 화합물 |
| IL294273A (en) * | 2019-12-23 | 2022-08-01 | Bristol Myers Squibb Co | Substituted heteroaryl compounds are useful as t-cell activators |
| US20210269434A1 (en) * | 2020-01-10 | 2021-09-02 | Incyte Corporation | Tricyclic compounds as inhibitors of kras |
| CN113549010B (zh) * | 2020-04-26 | 2023-10-20 | 中国科学院上海药物研究所 | 一种具有ampk激动活性的化合物及其前药的制备和应用 |
| US11833155B2 (en) | 2020-06-03 | 2023-12-05 | Incyte Corporation | Combination therapy for treatment of myeloproliferative neoplasms |
| US20230227409A1 (en) * | 2020-06-10 | 2023-07-20 | Ideaya Biosciences, Inc. | Quinolinone derivatives as methionine adenosyltransferase 2a inhibitors |
| IL301225A (en) * | 2020-09-09 | 2023-05-01 | Aurigene Oncology Ltd | Heterocyclic compounds as CBP/EP300 bromodomain inhibitors |
| HRP20251111T1 (hr) * | 2021-01-29 | 2025-11-21 | Boehringer Ingelheim International Gmbh | Azakinolini kao inhibitori cd38 |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE636867A (https=) * | 1963-08-30 | |||
| US3755332A (en) | 1971-07-01 | 1973-08-28 | Ciba Geigy Corp | Substituted 4 indazolaminoquinolines |
| GB8908229D0 (en) | 1989-04-12 | 1989-05-24 | Smithkline Beckman Intercredit | Compounds |
| US5430153A (en) | 1991-04-03 | 1995-07-04 | Korea Research Institute Of Chemical Technology | 2-quinolinone derivatives |
| FI940469L (fi) | 1991-08-02 | 1994-02-01 | Pfizer | Kinoliinijohdannaisia immunostimulantteina |
| WO1999011658A1 (en) | 1997-08-29 | 1999-03-11 | Proteus Molecular Design Ltd. | Meta-benzamidine derivatives as serin protease inhibitors |
| SE0102858D0 (sv) | 2001-08-27 | 2001-08-27 | Astrazeneca Ab | N-type calcium channel antagonists for the treatment of pain |
| CA2488635C (en) * | 2002-06-12 | 2012-10-23 | Abbott Laboratories | Antagonists of melanin concentrating hormone receptor |
| JP4934432B2 (ja) | 2004-02-19 | 2012-05-16 | レクサン ファーマシューティカルズ インコーポレイテッド | キナゾリン誘導体およびキナゾリン誘導体の治療への使用 |
| KR100910333B1 (ko) | 2005-02-23 | 2009-07-31 | 시오노기세이야쿠가부시키가이샤 | 타이로신 키나아제 억제 활성을 갖는 퀴나졸린 유도체 |
| CR9465A (es) | 2005-03-25 | 2008-06-19 | Surface Logix Inc | Compuestos mejorados farmacocineticamente |
| WO2006121767A2 (en) | 2005-05-06 | 2006-11-16 | Apath, Llc | 4-aminoquinoline compounds for treating virus-related conditions |
| GB0605689D0 (en) * | 2006-03-21 | 2006-05-03 | Novartis Ag | Organic compounds |
| WO2008054599A2 (en) | 2006-09-27 | 2008-05-08 | Surface Logix, Inc. | Rho kinase inhibitors |
| GB0705915D0 (en) | 2007-03-28 | 2007-05-09 | Helperby Therapeutics Ltd | New use |
| EP2152672A1 (en) | 2007-05-24 | 2010-02-17 | Bayer Schering Pharma Aktiengesellschaft | Novel sulphoximine-substituted quinazoline and quinazoline derivatives as kinase inhibitors |
| JP5301456B2 (ja) | 2007-11-12 | 2013-09-25 | Ｍｓｄ株式会社 | ヘテロアリールオキシキナゾリン誘導体 |
| EP2072502A1 (de) | 2007-12-20 | 2009-06-24 | Bayer Schering Pharma Aktiengesellschaft | Sulfoximid-substituierte Chinolin- und Chinazolinderivate als Kinase-Inhibitoren |
| WO2009084693A1 (ja) | 2007-12-28 | 2009-07-09 | Mitsubishi Tanabe Pharma Corporation | 抗癌剤 |
| ES2563057T3 (es) | 2009-11-05 | 2016-03-10 | Glaxosmithkline Llc | Inhibidor de bromodominio de benzodiazepina |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| RS54645B1 (sr) * | 2009-11-05 | 2016-08-31 | Glaxosmithkline Llc | Benzodiazepin kao inhibitor bromodomena |
| GB0919426D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919423D0 (en) * | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| AR079814A1 (es) | 2009-12-31 | 2012-02-22 | Otsuka Pharma Co Ltd | Compuestos heterociclicos, composiciones farmaceuticas que los contienen y sus usos |
| EP2566477B1 (en) | 2010-05-07 | 2015-09-02 | GlaxoSmithKline Intellectual Property Development Limited | Amino-quinolines as kinase inhibitors |
| WO2011143651A1 (en) | 2010-05-14 | 2011-11-17 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for modulating metabolism |
| WO2012040499A2 (en) | 2010-09-22 | 2012-03-29 | Surface Logix, Inc. | Metabolic inhibitors |
| AR084070A1 (es) * | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| WO2012125913A1 (en) | 2011-03-17 | 2012-09-20 | The Trustees Of The University Of Pennsylvania | Methods and use of bifunctional enzyme-building clamp-shaped molecules |
| GB201106799D0 (en) | 2011-04-21 | 2011-06-01 | Glaxosmithkline Llc | Novel compounds |
| KR20140048216A (ko) | 2011-06-29 | 2014-04-23 | 오츠카 세이야쿠 가부시키가이샤 | 치료 화합물로서의 퀴나졸린 및 관련된 사용 방법 |
| WO2013027168A1 (en) * | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| US9977024B2 (en) | 2012-12-09 | 2018-05-22 | The Scripps Research Institute | Targeted covalent probes and inhibitors of proteins containing redox-sensitive cysteines |
| JP6464139B2 (ja) * | 2013-03-14 | 2019-02-06 | コンバージーン・リミテッド・ライアビリティ・カンパニーＣｏｎｖｅｒｇｅｎｅ Ｌｌｃ | 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 |
| JP6542212B2 (ja) | 2013-07-31 | 2019-07-10 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規キナゾリノン |
| CA2966908A1 (en) | 2014-11-13 | 2016-05-19 | Convergene Llc | Methods and compositions for inhibition of bromodomain and extraterminal proteins |
| WO2016120808A1 (en) | 2015-01-28 | 2016-08-04 | Minoryx Therapeutics S.L. | Heteroarylaminoisoquinolines, methods for their preparation and therapeutic uses thereof |
-
2014
- 2014-03-13 JP JP2016501811A patent/JP6464139B2/ja not_active Expired - Fee Related
- 2014-03-13 AU AU2014244426A patent/AU2014244426B2/en not_active Ceased
- 2014-03-13 EA EA201591746A patent/EA201591746A1/ru unknown
- 2014-03-13 WO PCT/US2014/025289 patent/WO2014159837A1/en not_active Ceased
- 2014-03-13 CA CA2905451A patent/CA2905451A1/en not_active Abandoned
- 2014-03-13 CN CN201480028551.7A patent/CN105407894A/zh active Pending
- 2014-03-13 EP EP14776141.5A patent/EP2968360B1/en not_active Not-in-force
- 2014-03-13 BR BR112015022417A patent/BR112015022417A2/pt not_active IP Right Cessation
- 2014-03-13 KR KR1020157029249A patent/KR20150135359A/ko not_active Abandoned
- 2014-03-13 HK HK16110964.3A patent/HK1222793A1/zh unknown
- 2014-03-13 MX MX2015012478A patent/MX367420B/es active IP Right Grant
- 2014-03-13 US US14/774,387 patent/US9695179B2/en not_active Expired - Fee Related
-
2017
- 2017-06-27 US US15/634,768 patent/US10266536B2/en not_active Expired - Fee Related
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- 2019-04-16 US US16/385,606 patent/US10717739B2/en not_active Expired - Fee Related
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