JP2015530389A5 - - Google Patents
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- JP2015530389A5 JP2015530389A5 JP2015531283A JP2015531283A JP2015530389A5 JP 2015530389 A5 JP2015530389 A5 JP 2015530389A5 JP 2015531283 A JP2015531283 A JP 2015531283A JP 2015531283 A JP2015531283 A JP 2015531283A JP 2015530389 A5 JP2015530389 A5 JP 2015530389A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- medicament
- pharmaceutically acceptable
- medicament according
- lung adenocarcinoma
- 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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- 239000003814 drug Substances 0.000 claims 16
- 229940125904 compound 1 Drugs 0.000 claims 11
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims 8
- 201000005249 lung adenocarcinoma Diseases 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 7
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 6
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 6
- 230000004927 fusion Effects 0.000 claims 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 3
- 229940049920 malate Drugs 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 230000002159 abnormal effect Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 2
- 229960004316 cisplatin Drugs 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 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 2
- 229960005277 gemcitabine Drugs 0.000 claims 2
- BJEPYKJPYRNKOW-UHFFFAOYSA-L malate(2-) Chemical compound [O-]C(=O)C(O)CC([O-])=O BJEPYKJPYRNKOW-UHFFFAOYSA-L 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 241000124008 Mammalia Species 0.000 claims 1
- 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 1
- 230000010261 cell growth Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000012010 growth Effects 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261698143P | 2012-09-07 | 2012-09-07 | |
| US61/698,143 | 2012-09-07 | ||
| PCT/US2013/058768 WO2014039971A1 (en) | 2012-09-07 | 2013-09-09 | Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018103041A Division JP2018203727A (ja) | 2012-09-07 | 2018-05-30 | 肺腺癌の治療で使用するためのmet、vegfr、およびretの阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015530389A JP2015530389A (ja) | 2015-10-15 |
| JP2015530389A5 true JP2015530389A5 (enExample) | 2017-03-09 |
| JP6513567B2 JP6513567B2 (ja) | 2019-05-15 |
Family
ID=49226556
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015531283A Active JP6513567B2 (ja) | 2012-09-07 | 2013-09-09 | 肺腺癌の治療で使用するためのmet、vegfr、およびretの阻害剤 |
| JP2018103041A Pending JP2018203727A (ja) | 2012-09-07 | 2018-05-30 | 肺腺癌の治療で使用するためのmet、vegfr、およびretの阻害剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018103041A Pending JP2018203727A (ja) | 2012-09-07 | 2018-05-30 | 肺腺癌の治療で使用するためのmet、vegfr、およびretの阻害剤 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US20140121239A1 (enExample) |
| EP (1) | EP2892532B1 (enExample) |
| JP (2) | JP6513567B2 (enExample) |
| CN (2) | CN114129566A (enExample) |
| ES (1) | ES2726605T3 (enExample) |
| WO (1) | WO2014039971A1 (enExample) |
Families Citing this family (57)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS53350B (sr) | 2008-09-22 | 2014-10-31 | Array Biopharma, Inc. | Supstituisana jedinjenja imidazo[1,2-b]piridazina kao inhibitori trk kinaze |
| TWI511956B (zh) | 2009-01-16 | 2015-12-11 | Exelixis Inc | 製備n-(4-{〔6,7-雙(甲氧基)喹啉-4-基〕氧基}苯基)-n’-(4-氟苯基)環丙烷-1,1-二甲醯胺之方法 |
| AR077468A1 (es) | 2009-07-09 | 2011-08-31 | Array Biopharma Inc | Compuestos de pirazolo (1,5 -a) pirimidina sustituidos como inhibidores de trk- quinasa |
| UA108618C2 (uk) | 2009-08-07 | 2015-05-25 | Застосування c-met-модуляторів в комбінації з темозоломідом та/або променевою терапією для лікування раку | |
| PL3205654T3 (pl) | 2010-05-20 | 2019-08-30 | Array Biopharma, Inc. | Związki makrocykliczne jako inhibitory kinazy TRK |
| PT2621481T (pt) | 2010-09-27 | 2019-11-19 | Exelixis Inc | Inibidores duplos de met e vegf para o tratamento de cancro da próstata resistente à castração e metástases ósseas osteoblásticas |
| PL2673262T3 (pl) | 2011-02-10 | 2022-04-11 | Exelixis, Inc. | Sposoby wytwarzania związków chinolinowych i kompozycje farmaceutyczne zawierające takie związki |
| ES2639093T3 (es) | 2011-09-22 | 2017-10-25 | Exelixis, Inc. | Procedimiento para el tratamiento de la osteoporosis |
| JP6208140B2 (ja) | 2011-10-20 | 2017-10-04 | エクセリクシス, インク. | キノリン誘導体の調製プロセス |
| WO2013166296A1 (en) | 2012-05-02 | 2013-11-07 | Exelixis, Inc. | A dual met - vegf modulator for treating osteolytic bone metastases |
| EP2892532B1 (en) * | 2012-09-07 | 2019-02-13 | Exelixis, Inc. | Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma |
| CA2907334C (en) | 2013-03-15 | 2021-12-07 | Exelixis, Inc. | Metabolites of n-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-n'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| US11564915B2 (en) | 2013-04-04 | 2023-01-31 | Exelixis, Inc. | Cabozantinib dosage form and use in the treatment of cancer |
| KR102354963B1 (ko) | 2014-02-14 | 2022-01-21 | 엑셀리시스, 인코포레이티드 | N-{4-[(6,7-다이메톡시퀴놀린-4-일)옥시]페닐}-n'-(4-플루오로페닐) 사이클로프로판-1,1-다이카복스아마이드의 결정질 고체 형태, 제조 방법 및 사용 방법 |
| US10159666B2 (en) | 2014-03-17 | 2018-12-25 | Exelixis, Inc. | Dosing of cabozantinib formulations |
| WO2015161277A1 (en) * | 2014-04-18 | 2015-10-22 | Blueprint Medicines Corporation | Met fusions |
| MX375716B (es) * | 2014-04-25 | 2025-03-06 | Exelixis Inc | Método para tratar adenocarcinoma de pulmón. |
| CN104788372B (zh) * | 2014-07-25 | 2018-01-30 | 上海圣考医药科技有限公司 | 一种氘代卡博替尼衍生物、其制备方法、应用及其中间体 |
| JP6789923B2 (ja) | 2014-07-31 | 2020-11-25 | エグゼリクシス, インコーポレイテッド | フッ素18標識化カボザンチニブ及びその類似体の調製方法 |
| AU2015301097B2 (en) | 2014-08-05 | 2021-03-04 | Exelixis, Inc. | Drug combinations to treat multiple myeloma |
| CN107428760B (zh) | 2014-11-16 | 2021-04-27 | 阵列生物制药公司 | (s)-n-(5-((r)-2-(2,5-二氟苯基)-吡咯烷-1-基)-吡唑并[1,5-a]嘧啶-3-基)-3-羟基吡咯烷-1-甲酰胺硫酸氢盐的晶型 |
| US10202365B2 (en) | 2015-02-06 | 2019-02-12 | Blueprint Medicines Corporation | 2-(pyridin-3-yl)-pyrimidine derivatives as RET inhibitors |
| BR112018000808A2 (pt) | 2015-07-16 | 2018-09-04 | Array Biopharma Inc | compostos de pirazolo[1,5-a]piridina substituída como inibidores de ret cinase |
| BR112018008357A2 (en) | 2015-10-26 | 2018-11-27 | Loxo Oncology, Inc. | dot mutations in trk inhibitor resistant cancer and related methods |
| EA038890B1 (ru) | 2015-11-02 | 2021-11-03 | Блюпринт Медсинс Корпорейшн | Ингибиторы ret |
| US10183928B2 (en) | 2016-03-17 | 2019-01-22 | Blueprint Medicines Corporation | Inhibitors of RET |
| US10045991B2 (en) | 2016-04-04 | 2018-08-14 | Loxo Oncology, Inc. | Methods of treating pediatric cancers |
| RS65988B1 (sr) | 2016-04-04 | 2024-10-31 | Loxo Oncology Inc | Postupak lečenja pedijatrijskih karcinoma |
| FI3439662T3 (fi) | 2016-04-04 | 2024-09-04 | Loxo Oncology Inc | (s)-n-(5-((r)-2-(2,5-difluorifenyyli)pyrrolidin-1-yyli)pyratsolo[1,5-a]pyrimidin-3-yyli)-3-hydroksipyrrolidiini-1-karboksamidin nesteformulaatioita |
| 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 |
| EP3454886A1 (en) | 2016-05-13 | 2019-03-20 | Instituto de Medicina Molecular | Methods of treating diseases associated with ilc3 cells |
| HRP20201984T1 (hr) | 2016-05-18 | 2021-04-16 | Loxo Oncology, Inc. | Priprema (s)-n-(5-((r)-2-(2,5-difluorofenil)pirolidin-1-il)pirazolo[1,5-a]pirimidin-3-il)-3-hidroksipirolidin-1-karboksamida |
| US10227329B2 (en) | 2016-07-22 | 2019-03-12 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| US10035789B2 (en) | 2016-07-27 | 2018-07-31 | Blueprint Medicines Corporation | Compounds useful for treating disorders related to RET |
| TWI704148B (zh) | 2016-10-10 | 2020-09-11 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑并[1,5-a]吡啶化合物 |
| JOP20190077A1 (ar) | 2016-10-10 | 2019-04-09 | Array Biopharma Inc | مركبات بيرازولو [1، 5-a]بيريدين بها استبدال كمثبطات كيناز ret |
| JOP20190092A1 (ar) | 2016-10-26 | 2019-04-25 | Array Biopharma Inc | عملية لتحضير مركبات بيرازولو[1، 5-a]بيريميدين وأملاح منها |
| WO2018136661A1 (en) | 2017-01-18 | 2018-07-26 | Andrews Steven W | SUBSTITUTED PYRAZOLO[1,5-a]PYRAZINE COMPOUNDS AS RET KINASE INHIBITORS |
| WO2018136663A1 (en) | 2017-01-18 | 2018-07-26 | Array Biopharma, Inc. | Ret inhibitors |
| JOP20190213A1 (ar) | 2017-03-16 | 2019-09-16 | Array Biopharma Inc | مركبات حلقية ضخمة كمثبطات لكيناز ros1 |
| MY201941A (en) | 2017-08-21 | 2024-03-25 | Taiho Pharmaceutical Co Ltd | Fusion protein of dctn1 protein with ret protein |
| TWI791053B (zh) | 2017-10-10 | 2023-02-01 | 美商亞雷生物製藥股份有限公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之結晶形式及其醫藥組合物 |
| TWI876442B (zh) | 2017-10-10 | 2025-03-11 | 美商絡速藥業公司 | 6-(2-羥基-2-甲基丙氧基)-4-(6-(6-((6-甲氧基吡啶-3-基)甲基)-3,6-二氮雜雙環[3.1.1]庚-3-基)吡啶-3-基)吡唑并[1,5-a]吡啶-3-甲腈之調配物 |
| WO2019143977A1 (en) | 2018-01-18 | 2019-07-25 | Array Biopharma Inc. | Substituted pyrrolo[2,3-d]pyrimidines compounds as ret kinase inhibitors |
| TW201932464A (zh) | 2018-01-18 | 2019-08-16 | 美商亞雷生物製藥股份有限公司 | 作為ret激酶抑制劑之經取代吡唑基[4,3-c]吡啶化合物 |
| CN111630054B (zh) | 2018-01-18 | 2023-05-09 | 奥瑞生物药品公司 | 作为RET激酶抑制剂的取代的吡唑并[3,4-d]嘧啶化合物 |
| MX2020007765A (es) | 2018-01-26 | 2020-09-25 | Exelixis Inc | Compuestos para el tratamiento de trastornos dependientes de cinasas. |
| WO2019195471A1 (en) | 2018-04-03 | 2019-10-10 | Blueprint Medicines Corporation | Ret inhibitor for use in treating cancer having a ret alteration |
| TWI770624B (zh) | 2018-06-15 | 2022-07-11 | 漢達生技醫藥股份有限公司 | 尼洛替尼十二烷基硫酸鹽在製備用於治療慢性骨髓性白血病之劑型的用途 |
| CN110862397A (zh) * | 2018-08-27 | 2020-03-06 | 北京赛特明强医药科技有限公司 | 二噁烷并喹唑啉与二噁烷并喹啉类化合物及其制备方法与应用 |
| WO2020055672A1 (en) | 2018-09-10 | 2020-03-19 | Array Biopharma Inc. | Fused heterocyclic compounds as ret kinase inhibitors |
| WO2021243192A1 (en) | 2020-05-29 | 2021-12-02 | Blueprint Medicines Corporation | Solid forms of pralsetinib |
| DE102020005002A1 (de) * | 2020-08-17 | 2022-02-17 | Epo Experimentelle Pharmakologie & Onkologie Berlin-Buch Gmbh | Mittel zur Therapie von Tumorerkrankungen |
| EP4347645A1 (en) | 2021-06-03 | 2024-04-10 | Fundação D. Anna de Sommer Champalimaud e Dr. Carlos Montez Champalimaud Foundation | Neuro-mesenchyme units control ilc2 and obesity via a brain-adipose circuit |
| CN114354789B (zh) * | 2021-12-27 | 2023-08-29 | 深圳海王医药科技研究院有限公司 | 一种同时测定卡博替尼类似物及其有关物质的方法 |
| WO2023230770A1 (en) * | 2022-05-30 | 2023-12-07 | Suzhou Singleron Biotechnologies Co., Ltd. | Methods of lung adenocarcinoma treatment with non anti-luad drugs or compounds |
| CN120417903A (zh) | 2023-01-31 | 2025-08-01 | 汉达癌症医药责任有限公司 | 改良的卡博替尼组合物及其使用方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2338488A1 (en) * | 2006-05-26 | 2011-06-29 | Bayer HealthCare, LLC | Drug combinations with substituted diaryl ureas for the treatment of cancer |
| MX2011003363A (es) * | 2008-10-01 | 2011-04-27 | Ludwig Inst Cancer Res | Metodos para el tratamiento de cancer. |
| TWI511956B (zh) * | 2009-01-16 | 2015-12-11 | Exelixis Inc | 製備n-(4-{〔6,7-雙(甲氧基)喹啉-4-基〕氧基}苯基)-n’-(4-氟苯基)環丙烷-1,1-二甲醯胺之方法 |
| US20120070368A1 (en) * | 2010-04-16 | 2012-03-22 | Exelixis, Inc. | Methods of Using C-Met Modulators |
| JP2014005206A (ja) * | 2010-10-22 | 2014-01-16 | Astellas Pharma Inc | アリールアミノヘテロ環カルボキサミド化合物 |
| US10023855B2 (en) * | 2011-10-31 | 2018-07-17 | Macrogen, Inc. | Fusion protein comprising C-terminal domain of RET protein and use thereof as a diagnosing marker |
| WO2013163428A1 (en) * | 2012-04-25 | 2013-10-31 | The Regents Of The University Of Colorado | Detection of ret fusions in cancer |
| EP2892532B1 (en) * | 2012-09-07 | 2019-02-13 | Exelixis, Inc. | Inhibitors of met, vegfr and ret for use in the treatment of lung adenocarcinoma |
-
2013
- 2013-09-09 EP EP13765886.0A patent/EP2892532B1/en active Active
- 2013-09-09 CN CN202111124139.3A patent/CN114129566A/zh active Pending
- 2013-09-09 US US14/021,614 patent/US20140121239A1/en not_active Abandoned
- 2013-09-09 US US14/426,580 patent/US20150238477A1/en not_active Abandoned
- 2013-09-09 ES ES13765886T patent/ES2726605T3/es active Active
- 2013-09-09 JP JP2015531283A patent/JP6513567B2/ja active Active
- 2013-09-09 WO PCT/US2013/058768 patent/WO2014039971A1/en not_active Ceased
- 2013-09-09 CN CN201380052164.2A patent/CN104703600A/zh active Pending
-
2018
- 2018-05-30 JP JP2018103041A patent/JP2018203727A/ja active Pending
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