JP2016527486A5 - - Google Patents
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- JP2016527486A5 JP2016527486A5 JP2016519703A JP2016519703A JP2016527486A5 JP 2016527486 A5 JP2016527486 A5 JP 2016527486A5 JP 2016519703 A JP2016519703 A JP 2016519703A JP 2016519703 A JP2016519703 A JP 2016519703A JP 2016527486 A5 JP2016527486 A5 JP 2016527486A5
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- 238000000034 method Methods 0.000 claims description 77
- 229940000406 drug candidate Drugs 0.000 claims description 33
- 102000004169 proteins and genes Human genes 0.000 claims description 20
- 108090000623 proteins and genes Proteins 0.000 claims description 20
- 230000000144 pharmacologic effect Effects 0.000 claims description 10
- 230000000694 effects Effects 0.000 claims description 9
- 125000004429 atom Chemical group 0.000 claims description 8
- 239000000126 substance Substances 0.000 claims description 8
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 125000004122 cyclic group Chemical group 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 4
- 125000004434 sulfur atom Chemical group 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 3
- 238000005192 partition Methods 0.000 claims description 3
- 238000012216 screening Methods 0.000 claims description 3
- 102000003802 alpha-Synuclein Human genes 0.000 claims description 2
- 108090000185 alpha-Synuclein Proteins 0.000 claims description 2
- 230000009021 linear effect Effects 0.000 claims 9
- 230000009022 nonlinear effect Effects 0.000 claims 5
- 230000003287 optical effect Effects 0.000 claims 3
- HMWAJFNEGAJETK-UHFFFAOYSA-N 1-[6-(dimethylamino)naphthalen-2-yl]prop-2-en-1-one Chemical compound C1=C(C(=O)C=C)C=CC2=CC(N(C)C)=CC=C21 HMWAJFNEGAJETK-UHFFFAOYSA-N 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- DENNAQTZCPWYSQ-UHFFFAOYSA-M (2,5-dioxopyrrolidin-1-yl) 3-[[4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]pyridin-1-ium-1-yl]methyl]benzoate;bromide Chemical compound [Br-].C1=CC(OC)=CC=C1C1=CN=C(C=2C=C[N+](CC=3C=C(C=CC=3)C(=O)ON3C(CCC3=O)=O)=CC=2)O1 DENNAQTZCPWYSQ-UHFFFAOYSA-M 0.000 claims 1
- ZEIHZWQYRTVVMA-UHFFFAOYSA-N 2-bromo-1-[6-(dimethylamino)naphthalen-2-yl]ethanone Chemical compound C1=C(C(=O)CBr)C=CC2=CC(N(C)C)=CC=C21 ZEIHZWQYRTVVMA-UHFFFAOYSA-N 0.000 claims 1
- CDSULTPOCMWJCM-UHFFFAOYSA-N 4h-chromene-2,3-dione Chemical compound C1=CC=C2OC(=O)C(=O)CC2=C1 CDSULTPOCMWJCM-UHFFFAOYSA-N 0.000 claims 1
- 235000014785 Bergenia crassifolia Nutrition 0.000 claims 1
- 240000004972 Bergenia crassifolia Species 0.000 claims 1
- 230000002596 correlated effect Effects 0.000 claims 1
- WLUHMAZNVINQRC-UHFFFAOYSA-M methanesulfonate;1-[2-[4-[5-(4-methoxyphenyl)-1,3-oxazol-2-yl]pyridin-1-ium-1-yl]ethyl]pyrrole-2,5-dione Chemical compound CS([O-])(=O)=O.C1=CC(OC)=CC=C1C1=CN=C(C=2C=C[N+](CCN3C(C=CC3=O)=O)=CC=2)O1 WLUHMAZNVINQRC-UHFFFAOYSA-M 0.000 claims 1
- 229940126586 small molecule drug Drugs 0.000 claims 1
- 238000005556 structure-activity relationship Methods 0.000 description 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000003596 drug target Substances 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361834782P | 2013-06-13 | 2013-06-13 | |
| US61/834,782 | 2013-06-13 | ||
| PCT/US2014/042428 WO2014201435A1 (en) | 2013-06-13 | 2014-06-13 | Method of screening candidate biochemical entities targeting a target biochemical entity |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019081077A Division JP2019135498A (ja) | 2013-06-13 | 2019-04-22 | 標的生体実体を標的にする生化学実体候補をスクリーニングする方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016527486A JP2016527486A (ja) | 2016-09-08 |
| JP2016527486A5 true JP2016527486A5 (enExample) | 2017-07-27 |
| JP6518656B2 JP6518656B2 (ja) | 2019-05-22 |
Family
ID=52022828
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016519703A Active JP6518656B2 (ja) | 2013-06-13 | 2014-06-13 | 標的生体実体を標的にする生化学実体候補をスクリーニングする方法 |
| JP2019081077A Pending JP2019135498A (ja) | 2013-06-13 | 2019-04-22 | 標的生体実体を標的にする生化学実体候補をスクリーニングする方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019081077A Pending JP2019135498A (ja) | 2013-06-13 | 2019-04-22 | 標的生体実体を標的にする生化学実体候補をスクリーニングする方法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20150330990A1 (enExample) |
| EP (1) | EP3008465B1 (enExample) |
| JP (2) | JP6518656B2 (enExample) |
| CN (1) | CN105659087B (enExample) |
| GB (1) | GB2538216A (enExample) |
| WO (1) | WO2014201435A1 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9182406B2 (en) | 2008-08-04 | 2015-11-10 | Biodesy, Inc. | Nonlinear optical detection of molecules comprising an unnatural amino acid possessing a hyperpolarizability |
| GB2503604B (en) | 2011-03-21 | 2020-04-22 | Biodesy Llc | Classification of kinase inhibitors using second harmonic optical techniques |
| US9395358B2 (en) | 2012-02-05 | 2016-07-19 | Biodesy, Inc. | Methods for detecting allosteric modulators of protein |
| US20130288271A1 (en) | 2012-04-25 | 2013-10-31 | Biodesy, Llc | Methods for detecting allosteric modulators of protein |
| US9938560B2 (en) | 2012-02-05 | 2018-04-10 | Biodesy, Inc. | Methods for identifying modulators of Ras using nonlinear techniques |
| US9227978B2 (en) | 2013-03-15 | 2016-01-05 | Araxes Pharma Llc | Covalent inhibitors of Kras G12C |
| TWI659021B (zh) | 2013-10-10 | 2019-05-11 | 亞瑞克西斯製藥公司 | Ｋｒａｓ ｇ１２ｃ之抑制劑 |
| GB2531213B (en) * | 2014-06-30 | 2020-09-16 | Biodesy Inc | Systems and methods for high throughput analysis of conformation in biological entities |
| JO3556B1 (ar) | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| US9862701B2 (en) | 2014-09-25 | 2018-01-09 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10011600B2 (en) | 2014-09-25 | 2018-07-03 | Araxes Pharma Llc | Methods and compositions for inhibition of Ras |
| EP3237906B8 (en) * | 2014-12-23 | 2020-10-28 | Bluelight Therapeutics, Inc. | Attachment of proteins to interfaces for use in nonlinear optical detection |
| US10672502B2 (en) | 2015-04-02 | 2020-06-02 | Biodesy, Inc. | Methods for determining protein structure using a surface-selective nonlinear optical technique |
| AU2016245864C1 (en) | 2015-04-10 | 2021-09-09 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| ES2856880T3 (es) | 2015-04-15 | 2021-09-28 | Araxes Pharma Llc | Inhibidores tricíclicos condensados de KRAS y métodos de uso de los mismos |
| US10144724B2 (en) | 2015-07-22 | 2018-12-04 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use thereof |
| US11001872B2 (en) * | 2015-09-22 | 2021-05-11 | Shawn Clark | Designing customized protein-specific buffer system |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | 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 |
| EP3356347A1 (en) | 2015-09-28 | 2018-08-08 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| US10975071B2 (en) | 2015-09-28 | 2021-04-13 | Araxes Pharma Llc | Inhibitors of KRAS G12C mutant proteins |
| US10730867B2 (en) | 2015-09-28 | 2020-08-04 | 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 |
| KR102932353B1 (ko) | 2015-11-16 | 2026-02-27 | 아락세스 파마 엘엘씨 | 치환된 헤테로사이클릭 그룹을 포함하는 2-치환된 퀴나졸린 화합물 및 이의 사용 방법 |
| WO2017100546A1 (en) | 2015-12-09 | 2017-06-15 | Araxes Pharma Llc | Methods for preparation of quinazoline derivatives |
| WO2017172979A1 (en) | 2016-03-30 | 2017-10-05 | Araxes Pharma Llc | Substituted quinazoline compounds and methods of use |
| WO2017196891A1 (en) | 2016-05-09 | 2017-11-16 | Biodesy, Inc. | Methods and devices for detection of peripheral membrane protein interactions using nonlinear optical techniques |
| 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 |
| JP2019529484A (ja) | 2016-09-29 | 2019-10-17 | アラクセス ファーマ エルエルシー | Ｋｒａｓ ｇ１２ｃ変異体タンパク質の阻害剤 |
| CN106650209B (zh) * | 2016-09-30 | 2020-07-07 | 中车南京浦镇车辆有限公司 | 一种车辆应用实时信息确定可靠性增长趋势及参数的方法 |
| US10377743B2 (en) | 2016-10-07 | 2019-08-13 | Araxes Pharma Llc | Inhibitors of RAS and methods of use thereof |
| CN106650317B (zh) * | 2016-10-09 | 2019-04-16 | 南京双运生物技术有限公司 | 一种通过协同过滤公共数据库发现肿瘤潜在基因标靶的方法 |
| EP3573971A1 (en) | 2017-01-26 | 2019-12-04 | 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 |
| 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 |
| US11136308B2 (en) | 2017-01-26 | 2021-10-05 | Araxes Pharma Llc | Substituted quinazoline and quinazolinone compounds and methods of use thereof |
| JP7327802B2 (ja) | 2017-01-26 | 2023-08-16 | アラクセス ファーマ エルエルシー | 縮合ヘテロ－ヘテロ二環式化合物およびその使用方法 |
| CN110730822B (zh) * | 2017-04-18 | 2024-03-08 | X-化学有限公司 | 鉴定化合物的方法 |
| TW201906832A (zh) | 2017-05-25 | 2019-02-16 | 美商亞瑞克西斯製藥公司 | 用於癌症治療之化合物及其使用方法 |
| WO2018218069A1 (en) | 2017-05-25 | 2018-11-29 | Araxes Pharma Llc | Quinazoline derivatives as modulators of mutant kras, hras or nras |
| CN110869358A (zh) | 2017-05-25 | 2020-03-06 | 亚瑞克西斯制药公司 | Kras的共价抑制剂 |
| US10657525B2 (en) | 2017-06-27 | 2020-05-19 | Kasisto, Inc. | Method and apparatus for determining expense category distance between transactions via transaction signatures |
| BR112021001709A2 (pt) | 2018-08-01 | 2021-05-04 | Araxes Pharma Llc | compostos espiro heterocíclicos e métodos de uso dos mesmos para o tratamento de câncer |
| CN114787632A (zh) * | 2019-10-15 | 2022-07-22 | 杰那医疗公司 | 反应性亲和探针相互作用发现平台 |
| CN112630444B (zh) * | 2020-12-11 | 2024-05-24 | 深圳碳云智肽药物科技有限公司 | 基于靶点蛋白的多肽筛选方法 |
| CN113963745A (zh) * | 2021-12-07 | 2022-01-21 | 国际竹藤中心 | 一种构建植物发育分子调控网络的方法及其应用 |
| CN114317669A (zh) * | 2022-01-04 | 2022-04-12 | 北京大学 | 一种基于细胞内蛋白激酶c激活状态筛选药物的方法及高通量筛选装置 |
| WO2024129721A1 (en) * | 2022-12-13 | 2024-06-20 | Lafond David | Systems and methods to predict biological receptor signal response |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0877759A1 (en) * | 1996-02-01 | 1998-11-18 | Neurocrine Biosciences, Inc. | Methods for increasing endogenous levels of corticotropin-releasing factor |
| AU2001278901A1 (en) * | 2000-07-12 | 2002-01-21 | Karo Bio Ab | Method of identifying conformation-sensitive binding peptides and uses thereof |
| US20020094528A1 (en) * | 2000-11-29 | 2002-07-18 | Salafsky Joshua S. | Method and apparatus using a surface-selective nonlinear optical technique for detection of probe-target interations |
| US20030129649A1 (en) * | 2001-04-24 | 2003-07-10 | Kobilka Brian K. | Conformational assays to detect binding to G protein-coupled receptors |
| US7384773B1 (en) | 2001-05-10 | 2008-06-10 | Pfizer Inc | Crystal of HIV protease-cleaved human beta secretase and method for crystallization thereof |
| GB0117326D0 (en) * | 2001-07-16 | 2001-09-05 | Univ Aberdeen | Napthoquinone-type inhibitors of protein aggregation |
| US20030148391A1 (en) * | 2002-01-24 | 2003-08-07 | Salafsky Joshua S. | Method using a nonlinear optical technique for detection of interactions involving a conformational change |
| US7358331B2 (en) * | 2003-05-19 | 2008-04-15 | Elan Pharmaceuticals, Inc. | Truncated fragments of alpha-synuclein in Lewy body disease |
| US7342093B2 (en) * | 2004-07-23 | 2008-03-11 | University Of Massachusetts | Compounds that inhibit Hsp90 protein-protein interactions with IAP proteins |
| EP1637885A1 (en) | 2004-09-16 | 2006-03-22 | Vivalis | Method of screening by using conformation sensitive peptides |
| EP2954903A1 (en) * | 2005-02-16 | 2015-12-16 | The General Hospital Corporation | Use of bmp antagonists to regulate hepcidin-mediated iron metabolism |
| JP2008544252A (ja) * | 2005-06-16 | 2008-12-04 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニア | 神経変性疾患のための潜在的薬物分子の同定における、アミロイドベータタンパク質チャネルその、構造および使用 |
| US20090010894A1 (en) * | 2005-12-23 | 2009-01-08 | The Parkinson's Institute | Methods and systems for identifying compounds that modulate alpha-synuclein aggregation |
| JP5097206B2 (ja) * | 2006-07-28 | 2012-12-12 | エイディーライフ インコーポレイティッド | 診断および治療のためのペプチドプローブ |
| AU2009273465A1 (en) * | 2008-07-24 | 2010-01-28 | Max-Planck-Gesellschaft Zur Forderung Der Wissenschaften E.V. | Fluorescently or spin-labeled kinases for rapid screening and identification of novel kinase inhibitor scaffolds |
| US9182406B2 (en) * | 2008-08-04 | 2015-11-10 | Biodesy, Inc. | Nonlinear optical detection of molecules comprising an unnatural amino acid possessing a hyperpolarizability |
| WO2010031185A1 (en) * | 2008-09-19 | 2010-03-25 | Protox Therapeutics Inc. | Treating cancer stem cells using targeted cargo proteins |
| GB2503604B (en) * | 2011-03-21 | 2020-04-22 | Biodesy Llc | Classification of kinase inhibitors using second harmonic optical techniques |
| GB2517857A (en) * | 2012-04-25 | 2015-03-04 | Biodesy Inc | Methods for detecting allosteric modulators of proteins |
-
2014
- 2014-06-13 CN CN201480045112.7A patent/CN105659087B/zh active Active
- 2014-06-13 GB GB1422724.3A patent/GB2538216A/en not_active Withdrawn
- 2014-06-13 WO PCT/US2014/042428 patent/WO2014201435A1/en not_active Ceased
- 2014-06-13 JP JP2016519703A patent/JP6518656B2/ja active Active
- 2014-06-13 US US14/367,876 patent/US20150330990A1/en not_active Abandoned
- 2014-06-13 EP EP14810249.4A patent/EP3008465B1/en active Active
-
2019
- 2019-04-22 JP JP2019081077A patent/JP2019135498A/ja active Pending
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