JP2014509657A5 - - Google Patents
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- Publication number
- JP2014509657A5 JP2014509657A5 JP2014502871A JP2014502871A JP2014509657A5 JP 2014509657 A5 JP2014509657 A5 JP 2014509657A5 JP 2014502871 A JP2014502871 A JP 2014502871A JP 2014502871 A JP2014502871 A JP 2014502871A JP 2014509657 A5 JP2014509657 A5 JP 2014509657A5
- Authority
- JP
- Japan
- Prior art keywords
- vemurafenib
- acceptable salt
- pharmaceutically acceptable
- compound
- medicament
- 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
Links
- GPXBXXGIAQBQNI-UHFFFAOYSA-N vemurafenib Chemical compound CCCS(=O)(=O)NC1=CC=C(F)C(C(=O)C=2C3=CC(=CN=C3NC=2)C=2C=CC(Cl)=CC=2)=C1F GPXBXXGIAQBQNI-UHFFFAOYSA-N 0.000 claims description 44
- 229960003862 vemurafenib Drugs 0.000 claims description 44
- 150000001875 compounds Chemical class 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 31
- 239000011780 sodium chloride Substances 0.000 claims description 31
- 206010025650 Malignant melanoma Diseases 0.000 claims description 24
- 201000001441 melanoma Diseases 0.000 claims description 24
- 239000003814 drug Substances 0.000 claims description 20
- 241000124008 Mammalia Species 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 8
- 102200055464 BRAF V600E Human genes 0.000 claims description 7
- 230000035772 mutation Effects 0.000 claims description 7
- 238000009097 single-agent therapy Methods 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 6
- 108091007934 protein kinase B family Proteins 0.000 claims description 6
- 230000002195 synergetic Effects 0.000 claims description 6
- 230000004913 activation Effects 0.000 claims description 3
- 230000000051 modifying Effects 0.000 claims description 3
- 206010061289 Metastatic neoplasm Diseases 0.000 claims description 2
- 229940079593 drugs Drugs 0.000 claims description 2
- 230000014509 gene expression Effects 0.000 claims description 2
- 230000001394 metastastic Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 description 24
- GRZXWCHAXNAUHY-NSISKUIASA-N (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one Chemical compound C1([C@H](C(=O)N2CCN(CC2)C=2C=3[C@H](C)C[C@@H](O)C=3N=CN=2)CNC(C)C)=CC=C(Cl)C=C1 GRZXWCHAXNAUHY-NSISKUIASA-N 0.000 description 19
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N Docetaxel 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 description 9
- 229960003668 docetaxel Drugs 0.000 description 9
- 206010028980 Neoplasm Diseases 0.000 description 8
- 201000011510 cancer Diseases 0.000 description 7
- 230000000996 additive Effects 0.000 description 5
- 229960004316 cisplatin Drugs 0.000 description 5
- LXZZYRPGZAFOLE-UHFFFAOYSA-L transplatin Chemical compound [H][N]([H])([H])[Pt](Cl)(Cl)[N]([H])([H])[H] LXZZYRPGZAFOLE-UHFFFAOYSA-L 0.000 description 5
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 description 4
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 4
- 230000003463 hyperproliferative Effects 0.000 description 4
- 101700025368 ERBB2 Proteins 0.000 description 3
- 102100016662 ERBB2 Human genes 0.000 description 3
- 210000002307 Prostate Anatomy 0.000 description 3
- 101710037934 QRSL1 Proteins 0.000 description 3
- 230000002611 ovarian Effects 0.000 description 3
- 206010006187 Breast cancer Diseases 0.000 description 2
- 229960001433 Erlotinib Drugs 0.000 description 2
- AAKJLRGGTJKAMG-UHFFFAOYSA-N Erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 description 2
- 239000005551 L01XE03 - Erlotinib Substances 0.000 description 2
- 229940034727 Zelboraf Drugs 0.000 description 2
- 230000030833 cell death Effects 0.000 description 2
- 230000002950 deficient Effects 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 230000002401 inhibitory effect Effects 0.000 description 2
- 230000002018 overexpression Effects 0.000 description 2
- 230000001225 therapeutic Effects 0.000 description 2
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 description 1
- 108040005185 1-phosphatidylinositol-3-kinase activity proteins Proteins 0.000 description 1
- 229940120638 Avastin Drugs 0.000 description 1
- 102100004328 BRAF Human genes 0.000 description 1
- 101700004551 BRAF Proteins 0.000 description 1
- 208000000409 Breast Neoplasms Diseases 0.000 description 1
- 229960004562 Carboplatin Drugs 0.000 description 1
- OLESAACUTLOWQZ-UHFFFAOYSA-L Carboplatin Chemical compound O=C1O[Pt]([N]([H])([H])[H])([N]([H])([H])[H])OC(=O)C11CCC1 OLESAACUTLOWQZ-UHFFFAOYSA-L 0.000 description 1
- 206010009944 Colon cancer Diseases 0.000 description 1
- WXCXUHSOUPDCQV-UHFFFAOYSA-N Enzalutamide Chemical compound C1=C(F)C(C(=O)NC)=CC=C1N1C(C)(C)C(=O)N(C=2C=C(C(C#N)=CC=2)C(F)(F)F)C1=S WXCXUHSOUPDCQV-UHFFFAOYSA-N 0.000 description 1
- 206010017758 Gastric cancer Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 206010027480 Metastatic malignant melanoma Diseases 0.000 description 1
- 206010025310 Other lymphomas Diseases 0.000 description 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 description 1
- 229940120982 Tarceva Drugs 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 229960004671 enzalutamide Drugs 0.000 description 1
- 230000002496 gastric Effects 0.000 description 1
- 201000000496 gastric squamous cell carcinoma Diseases 0.000 description 1
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 238000003199 nucleic acid amplification method Methods 0.000 description 1
- 230000037361 pathway Effects 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- 230000000069 prophylaxis Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 201000011549 stomach cancer Diseases 0.000 description 1
- 239000011885 synergistic combination Substances 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 231100000730 tolerability Toxicity 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161470803P | 2011-04-01 | 2011-04-01 | |
| US201161470624P | 2011-04-01 | 2011-04-01 | |
| US61/470,803 | 2011-04-01 | ||
| US61/470,624 | 2011-04-01 | ||
| PCT/US2012/031665 WO2012135750A1 (en) | 2011-04-01 | 2012-03-30 | Combinations of akt inhibitor compounds and vemurafenib, and methods of use |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014509657A JP2014509657A (ja) | 2014-04-21 |
| JP2014509657A5 true JP2014509657A5 (pt-PT) | 2016-09-15 |
| JP6143739B2 JP6143739B2 (ja) | 2017-06-07 |
Family
ID=46931958
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014502871A Active JP6143739B2 (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及びベムラフェニブの組み合わせ、及び使用方法 |
| JP2014502886A Pending JP2014512356A (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及び化学療法剤の組み合わせ、及び使用方法 |
| JP2014502873A Pending JP2014512354A (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及びエルロチニブの組み合わせ、及び使用方法 |
| JP2014502876A Active JP6239497B2 (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及びアビラテロンの組み合わせ、及び使用方法 |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014502886A Pending JP2014512356A (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及び化学療法剤の組み合わせ、及び使用方法 |
| JP2014502873A Pending JP2014512354A (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及びエルロチニブの組み合わせ、及び使用方法 |
| JP2014502876A Active JP6239497B2 (ja) | 2011-04-01 | 2012-03-30 | Ａｋｔ阻害剤化合物及びアビラテロンの組み合わせ、及び使用方法 |
Country Status (28)
| Country | Link |
|---|---|
| US (7) | US9150549B2 (pt-PT) |
| EP (4) | EP2694072B2 (pt-PT) |
| JP (4) | JP6143739B2 (pt-PT) |
| KR (4) | KR102021157B1 (pt-PT) |
| CN (8) | CN103635192B (pt-PT) |
| AU (4) | AU2012236144B2 (pt-PT) |
| BR (4) | BR112013025355B1 (pt-PT) |
| CA (4) | CA2844699C (pt-PT) |
| DK (1) | DK2694072T4 (pt-PT) |
| ES (3) | ES2660263T3 (pt-PT) |
| FI (1) | FI2694072T4 (pt-PT) |
| HK (2) | HK1199244A1 (pt-PT) |
| HR (1) | HRP20180223T4 (pt-PT) |
| HU (1) | HUE036513T2 (pt-PT) |
| IL (4) | IL228641A0 (pt-PT) |
| LT (1) | LT2694072T (pt-PT) |
| ME (1) | ME02998B (pt-PT) |
| MX (4) | MX2013011327A (pt-PT) |
| MY (1) | MY179607A (pt-PT) |
| PL (2) | PL2694072T3 (pt-PT) |
| PT (1) | PT2694072T (pt-PT) |
| RS (1) | RS56759B1 (pt-PT) |
| RU (4) | RU2631240C2 (pt-PT) |
| SG (5) | SG194051A1 (pt-PT) |
| SI (1) | SI2694072T1 (pt-PT) |
| TR (1) | TR201802093T4 (pt-PT) |
| WO (4) | WO2012135753A1 (pt-PT) |
| ZA (4) | ZA201308064B (pt-PT) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
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| KR101897881B1 (ko) | 2008-01-04 | 2018-09-12 | 인텔리카인, 엘엘씨 | 특정 화학 물질, 조성물 및 방법 |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| RU2514427C2 (ru) | 2008-06-16 | 2014-04-27 | Юниверсити Оф Теннесси Рисёч Фаундейшн | Соединения для лечения рака |
| US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
| ES2637113T3 (es) | 2011-01-10 | 2017-10-10 | Infinity Pharmaceuticals, Inc. | Procedimientos para preparar isoquinolinonas y formas sólidas de isoquinolinonas |
| SG191724A1 (en) | 2011-01-11 | 2013-08-30 | Glaxosmithkline Llc | Combination |
| HUE036513T2 (hu) | 2011-04-01 | 2018-07-30 | Genentech Inc | AKT inhibitor vegyület és abirateron kombinációja terápiás kezelésekben való alkalmazásra |
| US9216170B2 (en) | 2012-03-19 | 2015-12-22 | Hoffmann-La Roche Inc. | Combination therapy for proliferative disorders |
| CA2867700A1 (en) * | 2012-03-23 | 2013-09-26 | Memorial Sloan-Kettering Cancer Center | Potentiating antibody-induced complement-mediated cytotoxicity via pi3k inhibition |
| RU2708247C2 (ru) | 2013-03-05 | 2019-12-05 | Юниверсити Оф Теннесси Рисерч Фаундейшн | Соединение для лечения рака |
| CN103304404B (zh) * | 2013-05-30 | 2015-07-29 | 万华化学集团股份有限公司 | 一种2,2-二羟甲基丁酸的制备方法 |
| RU2016116915A (ru) * | 2013-10-01 | 2017-11-13 | Новартис Аг | Комбинация |
| ES2765511T3 (es) * | 2013-11-15 | 2020-06-09 | Hoffmann La Roche | Procesos para la preparación de compuestos de pirimidinilciclopentano |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2015160986A2 (en) * | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2016001830A1 (en) * | 2014-07-01 | 2016-01-07 | Friedrich Miescher Institute For Biomedical Research | Combination of a brafv600e inhibitor and mertk inhibitor to treat melanoma |
| KR101689542B1 (ko) | 2015-01-15 | 2016-12-26 | 숭실대학교산학협력단 | 폐암치료 향상을 위한 제피티닙 또는 에를로티닙 나노복합체 |
| EP3072528B1 (en) * | 2015-03-26 | 2017-07-05 | ratiopharm GmbH | Composition comprising vemurafenib and cationic copolymer based on methacrylates |
| US10722527B2 (en) | 2015-04-10 | 2020-07-28 | Capsugel Belgium Nv | Abiraterone acetate lipid formulations |
| WO2017095826A1 (en) * | 2015-11-30 | 2017-06-08 | The Regents Of The University Of California | Combination therapy for treatment of melanoma |
| WO2017120218A1 (en) * | 2016-01-04 | 2017-07-13 | The Regents Of The University Of Colorado, A Body Corporate | Treatment of prostate cancer cells with fat oxidation inhibitors and enzalutamide |
| WO2017176423A1 (en) * | 2016-04-08 | 2017-10-12 | Biodesix, Inc. | Classifier generation methods and predictive test for ovarian cancer patient prognosis under platinum chemotherapy |
| EP3474856B1 (en) | 2016-06-24 | 2022-09-14 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| CA3049926A1 (en) | 2017-01-17 | 2018-07-26 | Heparegenix Gmbh | Protein kinase inhibitors for promoting liver regeneration or reducing or preventing hepatocyte death |
| WO2019229765A1 (en) * | 2018-05-29 | 2019-12-05 | Council Of Scientific & Industrial Research, India | Bicycle topoisomerase i inhibiting compounds, process for preparation and use thereof |
| JP2022515371A (ja) | 2018-12-19 | 2022-02-18 | ジェネンテック， インコーポレイテッド | Ａｋｔ阻害剤、タキサンおよびｐｄ－ｌ１阻害剤を含む併用療法を用いた乳癌の処置 |
| TW202120096A (zh) * | 2019-08-12 | 2021-06-01 | 美商建南德克公司 | 使用包含atp競爭性akt抑制劑、cdk4/6抑制劑及氟維司群之組合療法治療乳癌 |
| JP7383734B2 (ja) | 2019-09-13 | 2023-11-20 | プラクスエア エス．ティ．テクノロジー、インコーポレイテッド | 結晶性が増加し、かつ高密度の改善されたコーティングを生成するための方法 |
| AU2021275052A1 (en) * | 2020-05-19 | 2022-12-15 | Board Of Regents, The University Of Texas System | Methods for the treatment of pancreatitis and prevention of pancreatic cancer |
| CN117677614A (zh) * | 2021-12-17 | 2024-03-08 | 中国医药研究开发中心有限公司 | 具有akt激酶抑制活性的杂环化合物及其制备方法和医药用途 |
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2014
- 2014-12-18 HK HK14112699.3A patent/HK1199244A1/zh unknown
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2015
- 2015-06-01 HK HK15105215.1A patent/HK1204575A1/xx unknown
- 2015-08-26 US US14/836,827 patent/US9610289B2/en active Active
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2016
- 2016-02-05 US US15/017,315 patent/US9717730B2/en active Active
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2017
- 2017-02-21 US US15/438,277 patent/US10092567B2/en active Active
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