JP2017513908A5 - - Google Patents
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- Publication number
- JP2017513908A5 JP2017513908A5 JP2016564236A JP2016564236A JP2017513908A5 JP 2017513908 A5 JP2017513908 A5 JP 2017513908A5 JP 2016564236 A JP2016564236 A JP 2016564236A JP 2016564236 A JP2016564236 A JP 2016564236A JP 2017513908 A5 JP2017513908 A5 JP 2017513908A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- compound
- ros1
- pharmaceutically acceptable
- administered
- 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.)
- Granted
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- 150000003839 salts Chemical class 0.000 claims description 45
- 150000001875 compounds Chemical class 0.000 claims description 43
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 33
- 229940125904 compound 1 Drugs 0.000 claims description 31
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 31
- 230000004927 fusion Effects 0.000 claims description 25
- 108090000623 proteins and genes Proteins 0.000 claims description 21
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 18
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 18
- 125000001475 halogen functional group Chemical group 0.000 claims description 16
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- 229940049920 malate Drugs 0.000 claims description 12
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 claims description 11
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 claims description 11
- 239000003937 drug carrier Substances 0.000 claims description 11
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 10
- 229960005277 gemcitabine Drugs 0.000 claims description 10
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 8
- BJEPYKJPYRNKOW-UHFFFAOYSA-N malic acid Chemical compound OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 claims description 8
- 239000002146 L01XE16 - Crizotinib Substances 0.000 claims description 6
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims description 6
- 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 description 6
- 229960004562 carboplatin Drugs 0.000 claims description 6
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 6
- 229960004316 cisplatin Drugs 0.000 claims description 6
- KTEIFNKAUNYNJU-GFCCVEGCSA-N crizotinib Chemical compound O([C@H](C)C=1C(=C(F)C=CC=1Cl)Cl)C(C(=NC=1)N)=CC=1C(=C1)C=NN1C1CCNCC1 KTEIFNKAUNYNJU-GFCCVEGCSA-N 0.000 claims description 6
- 229960005061 crizotinib Drugs 0.000 claims description 6
- 238000001514 detection method Methods 0.000 claims description 6
- 229960003668 docetaxel Drugs 0.000 claims description 6
- 208000009956 adenocarcinoma Diseases 0.000 claims description 5
- 201000011510 cancer Diseases 0.000 claims description 5
- 230000002159 abnormal effect Effects 0.000 claims description 4
- 238000003556 assay Methods 0.000 claims description 4
- ONIQOQHATWINJY-UHFFFAOYSA-N cabozantinib Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1)=CC=C1NC(=O)C1(C(=O)NC=2C=CC(F)=CC=2)CC1 ONIQOQHATWINJY-UHFFFAOYSA-N 0.000 claims description 4
- 230000010261 cell growth Effects 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 230000000694 effects Effects 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 238000012163 sequencing technique Methods 0.000 claims description 4
- 102100032218 Cytokine-inducible SH2-containing protein Human genes 0.000 claims description 2
- 101000943420 Homo sapiens Cytokine-inducible SH2-containing protein Proteins 0.000 claims description 2
- 241000124008 Mammalia Species 0.000 claims description 2
- 206010027476 Metastases Diseases 0.000 claims description 2
- 108091000080 Phosphotransferase Proteins 0.000 claims description 2
- 238000003745 diagnosis Methods 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 239000012634 fragment Substances 0.000 claims description 2
- 230000001404 mediated effect Effects 0.000 claims description 2
- 230000009401 metastasis Effects 0.000 claims description 2
- 230000001575 pathological effect Effects 0.000 claims description 2
- 102000020233 phosphotransferase Human genes 0.000 claims description 2
- 229920001184 polypeptide Polymers 0.000 claims description 2
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 2
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 2
- 238000003757 reverse transcription PCR Methods 0.000 claims description 2
- 230000001225 therapeutic effect Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 68
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 51
- 210000004027 cell Anatomy 0.000 description 7
- 102000037865 fusion proteins Human genes 0.000 description 2
- 108020001507 fusion proteins Proteins 0.000 description 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 description 1
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 description 1
- 101150035397 Ros1 gene Proteins 0.000 description 1
- 210000003917 human chromosome Anatomy 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461984599P | 2014-04-25 | 2014-04-25 | |
| US61/984,599 | 2014-04-25 | ||
| PCT/US2015/027800 WO2015164869A1 (en) | 2014-04-25 | 2015-04-27 | Method of treating lung adenocarcinoma |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019126230A Division JP2019189646A (ja) | 2014-04-25 | 2019-07-05 | 肺腺癌の治療方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017513908A JP2017513908A (ja) | 2017-06-01 |
| JP2017513908A5 true JP2017513908A5 (enExample) | 2018-06-14 |
| JP6696908B2 JP6696908B2 (ja) | 2020-05-20 |
Family
ID=53055132
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016564236A Active JP6696908B2 (ja) | 2014-04-25 | 2015-04-27 | 肺腺癌の治療方法 |
| JP2019126230A Pending JP2019189646A (ja) | 2014-04-25 | 2019-07-05 | 肺腺癌の治療方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019126230A Pending JP2019189646A (ja) | 2014-04-25 | 2019-07-05 | 肺腺癌の治療方法 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20170042880A1 (enExample) |
| EP (2) | EP3906921A1 (enExample) |
| JP (2) | JP6696908B2 (enExample) |
| KR (1) | KR102474701B1 (enExample) |
| CN (1) | CN106488768A (enExample) |
| AR (1) | AR100191A1 (enExample) |
| AU (1) | AU2015249232B2 (enExample) |
| BR (1) | BR112016024672A2 (enExample) |
| CA (1) | CA2946416C (enExample) |
| DK (1) | DK3134084T3 (enExample) |
| EA (1) | EA035223B1 (enExample) |
| ES (1) | ES2874875T3 (enExample) |
| HU (1) | HUE054557T2 (enExample) |
| IL (1) | IL248408B (enExample) |
| MX (1) | MX375716B (enExample) |
| PL (1) | PL3134084T3 (enExample) |
| PT (1) | PT3134084T (enExample) |
| SG (1) | SG11201608657QA (enExample) |
| TW (1) | TWI724988B (enExample) |
| UA (1) | UA121655C2 (enExample) |
| WO (1) | WO2015164869A1 (enExample) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103717221A (zh) | 2011-05-02 | 2014-04-09 | 埃克塞里艾克西斯公司 | 治疗癌症和骨癌疼痛的方法 |
| EP3119476A1 (en) | 2014-03-17 | 2017-01-25 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| CN106715397B (zh) | 2014-07-31 | 2021-07-23 | 埃克塞里艾克西斯公司 | 制备氟-18标记的卡博替尼及其类似物的方法 |
| MA40457A (fr) | 2014-08-05 | 2017-06-14 | Exelixis Inc | Combinaison de médicaments pour traiter le myélome multiple |
| US11141413B2 (en) | 2016-04-15 | 2021-10-12 | Exelixis, Inc. | Method of treating renal cell carcinoma using N-(4-(6,7-dimethoxyquinolin-4-yloxy)phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, (2S)-hydroxybutanedioate |
| CN107353246A (zh) * | 2016-12-27 | 2017-11-17 | 辅仁药业集团熙德隆肿瘤药品有限公司 | 一种制备抗肿瘤药物卡博替尼的方法 |
| CN110691852A (zh) | 2017-05-31 | 2020-01-14 | 豪夫迈·罗氏有限公司 | Alk、ret和ros融合物的多重pcr检测 |
| WO2018227119A1 (en) | 2017-06-09 | 2018-12-13 | Exelixis, Inc. | Liquid dosage forms to treat cancer |
| CN107541550A (zh) * | 2017-08-21 | 2018-01-05 | 上海派森诺生物科技股份有限公司 | 人ros1融合基因检测方法 |
| KR20200055770A (ko) * | 2017-09-20 | 2020-05-21 | 메르사나 테라퓨틱스, 인코포레이티드 | Napi2b 표적 요법에 대한 반응을 예측하기 위한 조성물 및 방법 |
| UA128348C2 (uk) | 2018-01-26 | 2024-06-19 | Екселіксіс, Інк. | Сполуки для лікування кіназозалежних розладів |
| JP7480048B2 (ja) | 2018-01-26 | 2024-05-09 | エグゼリクシス， インコーポレイテッド | キナーゼ依存的障害を処置するための化合物 |
| IL321138A (en) | 2018-01-26 | 2025-07-01 | Exelixis Inc | Compounds for the treatment of kinase-dependent disorders |
| AR119069A1 (es) * | 2019-06-04 | 2021-11-24 | Exelixis Inc | Compuestos para el tratamiento de trastornos dependientes de quinasas |
| DE102020005002A1 (de) * | 2020-08-17 | 2022-02-17 | Epo Experimentelle Pharmakologie & Onkologie Berlin-Buch Gmbh | Mittel zur Therapie von Tumorerkrankungen |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4107288A (en) | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| US5447841A (en) | 1986-01-16 | 1995-09-05 | The Regents Of The Univ. Of California | Methods for chromosome-specific staining |
| US5756696A (en) | 1986-01-16 | 1998-05-26 | Regents Of The University Of California | Compositions for chromosome-specific staining |
| US5491224A (en) | 1990-09-20 | 1996-02-13 | Bittner; Michael L. | Direct label transaminated DNA probe compositions for chromosome identification and methods for their manufacture |
| US5145684A (en) | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| US6573043B1 (en) | 1998-10-07 | 2003-06-03 | Genentech, Inc. | Tissue analysis and kits therefor |
| EP2210607B1 (en) | 2003-09-26 | 2011-08-17 | Exelixis Inc. | N-[3-fluoro-4-({6-(methyloxy)-7-[(3-morpholin-4-ylpropyl)oxy]quinolin-4-yl}oxy)phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide for the treatment of cancer |
| US20100143918A1 (en) | 2007-01-19 | 2010-06-10 | Cell Signaling Technology, Inc. | Translocation and mutant ros kinase in human non-small cell lung carcinoma |
| US20080200515A1 (en) | 2006-12-29 | 2008-08-21 | Tap Pharmaceutical Products Inc. | Solid state forms of enantiopure ilaprazole |
| EP3741851A1 (en) | 2007-10-18 | 2020-11-25 | Cell Signaling Technology, Inc. | Translocation and mutant ros kinase in human non-small cell lung carcinoma |
| TW202112751A (zh) * | 2009-01-16 | 2021-04-01 | 美商艾克塞里克斯公司 | 包含n-(4-{[6,7-雙(甲氧基)喹啉-4-基]氧基}苯基)-n'-(4-氟苯基)環丙烷-1,1-二甲醯胺之蘋果酸鹽之醫藥組合物及其用途 |
| JP5979877B2 (ja) | 2009-02-12 | 2016-08-31 | セル・シグナリング・テクノロジー・インコーポレイテツド | ヒト癌における変異ｒｏｓ発現 |
| TWI585088B (zh) * | 2012-06-04 | 2017-06-01 | 第一三共股份有限公司 | 作爲激酶抑制劑之咪唑并［１，２－ｂ］嗒衍生物 |
| CN114129566A (zh) * | 2012-09-07 | 2022-03-04 | 埃克塞里艾克西斯公司 | 用于治疗肺腺癌的met、vegfr和ret的抑制剂 |
-
2015
- 2015-04-27 EP EP21162169.3A patent/EP3906921A1/en not_active Withdrawn
- 2015-04-27 SG SG11201608657QA patent/SG11201608657QA/en unknown
- 2015-04-27 AU AU2015249232A patent/AU2015249232B2/en active Active
- 2015-04-27 WO PCT/US2015/027800 patent/WO2015164869A1/en not_active Ceased
- 2015-04-27 ES ES15721100T patent/ES2874875T3/es active Active
- 2015-04-27 EP EP15721100.4A patent/EP3134084B1/en not_active Revoked
- 2015-04-27 CA CA2946416A patent/CA2946416C/en active Active
- 2015-04-27 US US15/305,854 patent/US20170042880A1/en not_active Abandoned
- 2015-04-27 KR KR1020167033010A patent/KR102474701B1/ko active Active
- 2015-04-27 PL PL15721100T patent/PL3134084T3/pl unknown
- 2015-04-27 HU HUE15721100A patent/HUE054557T2/hu unknown
- 2015-04-27 IL IL248408A patent/IL248408B/en unknown
- 2015-04-27 TW TW104113427A patent/TWI724988B/zh active
- 2015-04-27 UA UAA201611881A patent/UA121655C2/uk unknown
- 2015-04-27 MX MX2016013600A patent/MX375716B/es active IP Right Grant
- 2015-04-27 AR ARP150101255A patent/AR100191A1/es unknown
- 2015-04-27 BR BR112016024672-1A patent/BR112016024672A2/pt not_active Application Discontinuation
- 2015-04-27 JP JP2016564236A patent/JP6696908B2/ja active Active
- 2015-04-27 DK DK15721100.4T patent/DK3134084T3/da active
- 2015-04-27 EA EA201692150A patent/EA035223B1/ru not_active IP Right Cessation
- 2015-04-27 CN CN201580022580.7A patent/CN106488768A/zh active Pending
- 2015-04-27 PT PT157211004T patent/PT3134084T/pt unknown
-
2019
- 2019-07-05 JP JP2019126230A patent/JP2019189646A/ja active Pending
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