JP2018515570A5 - - Google Patents
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- JP2018515570A5 JP2018515570A5 JP2017560716A JP2017560716A JP2018515570A5 JP 2018515570 A5 JP2018515570 A5 JP 2018515570A5 JP 2017560716 A JP2017560716 A JP 2017560716A JP 2017560716 A JP2017560716 A JP 2017560716A JP 2018515570 A5 JP2018515570 A5 JP 2018515570A5
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- -1 Bizereshin Chemical compound 0.000 claims 43
- 101000984753 Homo sapiens Serine/threonine-protein kinase B-raf Proteins 0.000 claims 32
- 102100027103 Serine/threonine-protein kinase B-raf Human genes 0.000 claims 32
- 239000008194 pharmaceutical composition Substances 0.000 claims 30
- 230000035772 mutation Effects 0.000 claims 29
- 201000010099 disease Diseases 0.000 claims 18
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 18
- 102000043136 MAP kinase family Human genes 0.000 claims 11
- 108091054455 MAP kinase family Proteins 0.000 claims 11
- 230000037361 pathway Effects 0.000 claims 11
- 210000004027 cell Anatomy 0.000 claims 7
- 150000001875 compounds Chemical class 0.000 claims 6
- 230000003213 activating effect Effects 0.000 claims 5
- 208000006990 cholangiocarcinoma Diseases 0.000 claims 5
- 230000004927 fusion Effects 0.000 claims 5
- 230000001939 inductive effect Effects 0.000 claims 5
- 108090000623 proteins and genes Proteins 0.000 claims 5
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 4
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 4
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- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 3
- 229960002170 azathioprine Drugs 0.000 claims 3
- LMEKQMALGUDUQG-UHFFFAOYSA-N azathioprine Chemical compound CN1C=NC([N+]([O-])=O)=C1SC1=NC=NC2=C1NC=N2 LMEKQMALGUDUQG-UHFFFAOYSA-N 0.000 claims 3
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- 238000000034 method Methods 0.000 claims 3
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- 239000003197 protein kinase B inhibitor Substances 0.000 claims 3
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- NNJPGOLRFBJNIW-HNNXBMFYSA-N (-)-demecolcine Chemical compound C1=C(OC)C(=O)C=C2[C@@H](NC)CCC3=CC(OC)=C(OC)C(OC)=C3C2=C1 NNJPGOLRFBJNIW-HNNXBMFYSA-N 0.000 claims 2
- RIWLPSIAFBLILR-WVNGMBSFSA-N (2s)-1-[(2s)-2-[[(2s,3s)-2-[[(2s)-2-[[(2s,3r)-2-[[(2r,3s)-2-[[(2s)-2-[[2-[[2-[acetyl(methyl)amino]acetyl]amino]acetyl]amino]-3-methylbutanoyl]amino]-3-methylpentanoyl]amino]-3-hydroxybutanoyl]amino]pentanoyl]amino]-3-methylpentanoyl]amino]-5-(diaminomethy Chemical compound CC(=O)N(C)CC(=O)NCC(=O)N[C@@H](C(C)C)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCCN=C(N)N)C(=O)N1CCC[C@H]1C(=O)NCC RIWLPSIAFBLILR-WVNGMBSFSA-N 0.000 claims 2
- FPVKHBSQESCIEP-UHFFFAOYSA-N (8S)-3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Natural products C1C(O)C(CO)OC1N1C(NC=NCC2O)=C2N=C1 FPVKHBSQESCIEP-UHFFFAOYSA-N 0.000 claims 2
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- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 claims 2
- VSNHCAURESNICA-NJFSPNSNSA-N 1-oxidanylurea Chemical compound N[14C](=O)NO VSNHCAURESNICA-NJFSPNSNSA-N 0.000 claims 2
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- UEJJHQNACJXSKW-UHFFFAOYSA-N 2-(2,6-dioxopiperidin-3-yl)-1H-isoindole-1,3(2H)-dione Chemical compound O=C1C2=CC=CC=C2C(=O)N1C1CCC(=O)NC1=O UEJJHQNACJXSKW-UHFFFAOYSA-N 0.000 claims 2
- GFMMXOIFOQCCGU-UHFFFAOYSA-N 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide Chemical compound C=1C=C(I)C=C(Cl)C=1NC1=C(F)C(F)=CC=C1C(=O)NOCC1CC1 GFMMXOIFOQCCGU-UHFFFAOYSA-N 0.000 claims 2
- RWEVIPRMPFNTLO-UHFFFAOYSA-N 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-3-pyridinecarboxamide Chemical compound CN1C(=O)C(C)=CC(C(=O)NOCCO)=C1NC1=CC=C(I)C=C1F RWEVIPRMPFNTLO-UHFFFAOYSA-N 0.000 claims 2
- RNAMYOYQYRYFQY-UHFFFAOYSA-N 2-(4,4-difluoropiperidin-1-yl)-6-methoxy-n-(1-propan-2-ylpiperidin-4-yl)-7-(3-pyrrolidin-1-ylpropoxy)quinazolin-4-amine Chemical compound N1=C(N2CCC(F)(F)CC2)N=C2C=C(OCCCN3CCCC3)C(OC)=CC2=C1NC1CCN(C(C)C)CC1 RNAMYOYQYRYFQY-UHFFFAOYSA-N 0.000 claims 2
- MXWHMTNPTTVWDM-UHFFFAOYSA-N 2-[1-(diaminomethylidenehydrazinylidene)propan-2-ylideneamino]guanidine Chemical compound NC(N)=NN=C(C)C=NN=C(N)N MXWHMTNPTTVWDM-UHFFFAOYSA-N 0.000 claims 2
- CQOQDQWUFQDJMK-SSTWWWIQSA-N 2-methoxy-17beta-estradiol Chemical compound C([C@@H]12)C[C@]3(C)[C@@H](O)CC[C@H]3[C@@H]1CCC1=C2C=C(OC)C(O)=C1 CQOQDQWUFQDJMK-SSTWWWIQSA-N 0.000 claims 2
- NDMPLJNOPCLANR-UHFFFAOYSA-N 3,4-dihydroxy-15-(4-hydroxy-18-methoxycarbonyl-5,18-seco-ibogamin-18-yl)-16-methoxy-1-methyl-6,7-didehydro-aspidospermidine-3-carboxylic acid methyl ester Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 NDMPLJNOPCLANR-UHFFFAOYSA-N 0.000 claims 2
- RCLQNICOARASSR-SECBINFHSA-N 3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione Chemical compound FC=1C(=O)N(C)C=2N=CN(C[C@@H](O)CO)C(=O)C=2C=1NC1=CC=C(I)C=C1F RCLQNICOARASSR-SECBINFHSA-N 0.000 claims 2
- WGPXKFOFEXJMBD-UHFFFAOYSA-N 3-[N-[3-[(dimethylamino)methyl]phenyl]-C-phenylcarbonimidoyl]-2-hydroxy-1H-indole-6-carboxamide Chemical compound CN(C)CC1=CC(=CC=C1)N=C(C2=CC=CC=C2)C3=C(NC4=C3C=CC(=C4)C(=O)N)O WGPXKFOFEXJMBD-UHFFFAOYSA-N 0.000 claims 2
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- AKJHMTWEGVYYSE-AIRMAKDCSA-N 4-HPR Chemical compound C=1C=C(O)C=CC=1NC(=O)/C=C(\C)/C=C/C=C(C)C=CC1=C(C)CCCC1(C)C AKJHMTWEGVYYSE-AIRMAKDCSA-N 0.000 claims 2
- TVZGACDUOSZQKY-LBPRGKRZSA-N 4-aminofolic acid Chemical compound C1=NC2=NC(N)=NC(N)=C2N=C1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 TVZGACDUOSZQKY-LBPRGKRZSA-N 0.000 claims 2
- XAUDJQYHKZQPEU-KVQBGUIXSA-N 5-aza-2'-deoxycytidine Chemical compound O=C1N=C(N)N=CN1[C@@H]1O[C@H](CO)[C@@H](O)C1 XAUDJQYHKZQPEU-KVQBGUIXSA-N 0.000 claims 2
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- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 2
- FUXVKZWTXQUGMW-FQEVSTJZSA-N 9-Aminocamptothecin Chemical compound C1=CC(N)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 FUXVKZWTXQUGMW-FQEVSTJZSA-N 0.000 claims 2
- SHGAZHPCJJPHSC-ZVCIMWCZSA-N 9-cis-retinoic acid Chemical compound OC(=O)/C=C(\C)/C=C/C=C(/C)\C=C\C1=C(C)CCCC1(C)C SHGAZHPCJJPHSC-ZVCIMWCZSA-N 0.000 claims 2
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- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims 2
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims 2
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- NNJPGOLRFBJNIW-UHFFFAOYSA-N Demecolcine Natural products C1=C(OC)C(=O)C=C2C(NC)CCC3=CC(OC)=C(OC)C(OC)=C3C2=C1 NNJPGOLRFBJNIW-UHFFFAOYSA-N 0.000 claims 2
- RWSOTUBLDIXVET-UHFFFAOYSA-N Dihydrogen sulfide Chemical compound S RWSOTUBLDIXVET-UHFFFAOYSA-N 0.000 claims 2
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- VWUXBMIQPBEWFH-WCCTWKNTSA-N Fulvestrant Chemical compound OC1=CC=C2[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3[C@H](CCCCCCCCCS(=O)CCCC(F)(F)C(F)(F)F)CC2=C1 VWUXBMIQPBEWFH-WCCTWKNTSA-N 0.000 claims 2
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| KR102212923B1 (ko) | 2012-12-21 | 2021-02-04 | 플렉시콘 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| JP6325078B2 (ja) | 2013-03-15 | 2018-05-16 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | ヘテロ環式化合物およびその使用 |
| KR20160013028A (ko) | 2013-05-30 | 2016-02-03 | 플렉시콘, 인코퍼레이티드 | 키나제 조정을 위한 화합물 및 그에 대한 적응증 |
| WO2016164641A1 (en) | 2015-04-08 | 2016-10-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
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| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| SG10201912386RA (en) | 2015-09-21 | 2020-02-27 | Plexxikon Inc | Heterocyclic compounds and uses thereof |
| MX2018006856A (es) | 2015-12-07 | 2018-08-01 | Plexxikon Inc | Compuestos y metodos para modulacion de la quinasa, e indicaciones de los mismos. |
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| WO2018136202A2 (en) | 2016-12-23 | 2018-07-26 | Plexxikon Inc. | Compounds and methods for cdk8 modulation and indications therefor |
| MX393780B (es) | 2017-01-17 | 2025-03-24 | Heparegenix Gmbh | Inhibidores de proteina cinasa para promover la regeneracion hepatica o reducir o prevenir la muerte de hepatocitos |
| ES2896502T3 (es) | 2017-03-20 | 2022-02-24 | Plexxikon Inc | Formas cristalinas de ácido 4-(1-(1,1-di(piridin-2-il) etil)-6-(3,5-dimetilisoxazol-4-il)-1H-pirrolo[3,2-b]piridin-3- il)benzoico que inhiben el bromodominio |
| WO2018218633A1 (en) * | 2017-06-02 | 2018-12-06 | Beijing Percans Oncology Co. Ltd. | Combination therapies for treating cancers |
| US10428067B2 (en) | 2017-06-07 | 2019-10-01 | Plexxikon Inc. | Compounds and methods for kinase modulation |
| KR102615829B1 (ko) | 2017-07-25 | 2023-12-20 | 플렉시콘 인코퍼레이티드 | 키나제를 조정하는 화합물의 제제 |
| EP3694855A1 (en) | 2017-10-13 | 2020-08-19 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
| AU2018354423B2 (en) * | 2017-10-27 | 2024-11-07 | Plexxikon Inc. | Formulations of a compound modulating kinases |
| JP2021518367A (ja) | 2018-03-20 | 2021-08-02 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | Ｉｄｏおよびｔｄｏ調節のための化合物および方法、ならびにそれらのための兆候 |
| WO2019195959A1 (en) | 2018-04-08 | 2019-10-17 | Cothera Biosciences, Inc. | Combination therapy for cancers with braf mutation |
| CN108864060A (zh) * | 2018-06-03 | 2018-11-23 | 刘思良 | 一种重氮类衍生物及其在癌症治疗中的应用 |
| CN108610336A (zh) * | 2018-06-03 | 2018-10-02 | 刘思良 | 一种重氮类衍生物及其在癌症治疗中的应用 |
| CN108586439A (zh) * | 2018-06-03 | 2018-09-28 | 刘思良 | 一种Raf激酶抑制剂及其在癌症治疗中的应用 |
| KR20210044251A (ko) | 2018-08-13 | 2021-04-22 | 베이징 페르칸스 온콜로지 컴퍼니 리미티드 | 암 치료용 바이오마커 |
| WO2020092517A1 (en) | 2018-10-30 | 2020-05-07 | Institute For Cancer Research D/B/A The Research Institute Of Fox Chase Cancer Center | Combination therapies for treating cancer |
| CN113710668B (zh) | 2019-04-09 | 2025-01-07 | Opna生物公司 | 用于ep300或cbp调节及其适应症的缩合吖嗪 |
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| CN111057690A (zh) * | 2019-12-23 | 2020-04-24 | 维塔恩(广州)医药有限公司 | 肿瘤相关基因braf突变相关抗原短肽及其应用 |
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| BR112022021920A2 (pt) | 2020-04-29 | 2023-01-17 | Plexxikon Inc | Síntese de compostos heterocíclicos |
| JP2023530030A (ja) | 2020-06-19 | 2023-07-12 | シーフォー セラピューティクス， インコーポレイテッド | Ｂｒａｆ分解剤 |
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| CN118845777B (zh) * | 2024-06-28 | 2025-02-25 | 遵义医科大学附属医院 | 一种克诺拉尼用作淋巴水肿治疗剂的用途 |
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| PL2395004T3 (pl) | 2005-06-22 | 2016-08-31 | Plexxikon Inc | Pochodne pirolo[2,3-b]pirydyny jako inhibitory kinazy białkowej |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| MX2010000617A (es) | 2007-07-17 | 2010-05-17 | Plexxikon Inc | Compuestos y metodos para modulacion de cinasa, e indicaciones de estos. |
| US8158636B2 (en) | 2008-05-19 | 2012-04-17 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| EA031116B1 (ru) | 2009-04-03 | 2018-11-30 | Ф. Хоффманн-Ля Рош Аг | КРИСТАЛЛИЧЕСКИЕ ПОЛИМОРФНЫЕ ФОРМЫ {3-[5-(4-ХЛОРФЕНИЛ)-1H-ПИРРОЛО[2,3-b]ПИРИДИН-3-КАРБОНИЛ]-2,4-ДИФТОРФЕНИЛ}АМИДА ПРОПАН-1-СУЛЬФОНОВОЙ КИСЛОТЫ |
| KR20120097512A (ko) | 2009-11-18 | 2012-09-04 | 플렉시콘, 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| CN102753549A (zh) | 2009-12-23 | 2012-10-24 | 普莱希科公司 | 用于激酶调节的化合物和方法及其适应症 |
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| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| SI2884979T1 (sl) * | 2012-08-17 | 2019-10-30 | Hoffmann La Roche | Kombinirana zdravljenja melanoma, ki vključujejo dajanje kobimetiniba in vemurafeniba |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| CN112641787A (zh) * | 2013-03-21 | 2021-04-13 | 诺华股份有限公司 | 包含B-Raf抑制剂和第二抑制剂的组合疗法 |
| KR20160013028A (ko) * | 2013-05-30 | 2016-02-03 | 플렉시콘, 인코퍼레이티드 | 키나제 조정을 위한 화합물 및 그에 대한 적응증 |
| US9856259B2 (en) | 2014-09-15 | 2018-01-02 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| WO2016164641A1 (en) | 2015-04-08 | 2016-10-13 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2016179415A1 (en) | 2015-05-06 | 2016-11-10 | Plexxikon Inc. | Solid forms of a compound modulating kinases |
| WO2016191295A1 (en) | 2015-05-22 | 2016-12-01 | Plexxikon Inc. | Solid forms of a compound for modulating kinases |
| US10829484B2 (en) | 2015-07-28 | 2020-11-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| SG10201912386RA (en) | 2015-09-21 | 2020-02-27 | Plexxikon Inc | Heterocyclic compounds and uses thereof |
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