JP2014509657A5 - - Google Patents
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- 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 42
- 150000001875 compounds Chemical class 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 31
- 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
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 230000035772 mutation Effects 0.000 claims description 7
- 102200055464 rs113488022 Human genes 0.000 claims description 7
- 238000009097 single-agent therapy Methods 0.000 claims description 7
- 238000002360 preparation method Methods 0.000 claims description 6
- 230000002195 synergetic effect Effects 0.000 claims description 6
- 230000004913 activation Effects 0.000 claims description 3
- 229940079593 drug Drugs 0.000 claims description 2
- 230000014509 gene expression Effects 0.000 claims description 2
- 230000001394 metastastic effect Effects 0.000 claims description 2
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 2
- GRZXWCHAXNAUHY-NSISKUIASA-N (2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]-1-piperazinyl]-3-(propan-2-ylamino)-1-propanone 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 18
- 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 description 9
- 206010028980 Neoplasm Diseases 0.000 description 9
- 229960003668 docetaxel Drugs 0.000 description 9
- 201000011510 cancer Diseases 0.000 description 7
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 6
- 230000000996 additive effect Effects 0.000 description 5
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 description 5
- 229960004316 cisplatin Drugs 0.000 description 5
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 description 4
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 description 4
- 230000003463 hyperproliferative effect Effects 0.000 description 4
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 description 3
- 206010061535 Ovarian neoplasm Diseases 0.000 description 3
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 description 3
- 208000023958 prostate neoplasm Diseases 0.000 description 3
- 239000005551 L01XE03 - Erlotinib Substances 0.000 description 2
- 239000000654 additive Substances 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
- 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
- 230000002496 gastric effect Effects 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- 230000002018 overexpression Effects 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 229940034727 zelboraf Drugs 0.000 description 2
- 229940125431 BRAF inhibitor Drugs 0.000 description 1
- 206010006187 Breast cancer Diseases 0.000 description 1
- 208000026310 Breast neoplasm Diseases 0.000 description 1
- 206010009944 Colon 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
- 102000038030 PI3Ks Human genes 0.000 description 1
- 108091007960 PI3Ks Proteins 0.000 description 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 description 1
- 208000034331 Squamous cell carcinoma of the stomach Diseases 0.000 description 1
- 208000005718 Stomach Neoplasms Diseases 0.000 description 1
- 208000024770 Thyroid neoplasm Diseases 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 229940120638 avastin Drugs 0.000 description 1
- 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 description 1
- 229960004562 carboplatin Drugs 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 208000029742 colonic neoplasm Diseases 0.000 description 1
- 229940126534 drug product Drugs 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
- 229960004671 enzalutamide Drugs 0.000 description 1
- 229960001433 erlotinib Drugs 0.000 description 1
- 206010017758 gastric cancer Diseases 0.000 description 1
- 201000000496 gastric squamous cell carcinoma Diseases 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 230000005764 inhibitory process Effects 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 208000021039 metastatic melanoma 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 prophylactic effect 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
- 229940120982 tarceva Drugs 0.000 description 1
- 201000002510 thyroid cancer Diseases 0.000 description 1
- 208000036907 triple-positive breast carcinoma Diseases 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161470624P | 2011-04-01 | 2011-04-01 | |
| US201161470803P | 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 (enExample) | 2016-09-15 |
| JP6143739B2 JP6143739B2 (ja) | 2017-06-07 |
Family
ID=46931958
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
| 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 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 (2)
| 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 |
Country Status (29)
| Country | Link |
|---|---|
| US (7) | US9346789B2 (enExample) |
| EP (4) | EP2694070A4 (enExample) |
| JP (4) | JP6239497B2 (enExample) |
| KR (4) | KR102021157B1 (enExample) |
| CN (8) | CN103857395A (enExample) |
| AU (4) | AU2012236144B2 (enExample) |
| BR (4) | BR112013025354A2 (enExample) |
| CA (4) | CA2844699C (enExample) |
| DK (1) | DK2694072T4 (enExample) |
| ES (3) | ES2657750T3 (enExample) |
| FI (1) | FI2694072T4 (enExample) |
| HK (1) | HK1204575A1 (enExample) |
| HR (1) | HRP20180223T4 (enExample) |
| HU (1) | HUE036513T2 (enExample) |
| IL (4) | IL228642A0 (enExample) |
| LT (1) | LT2694072T (enExample) |
| ME (1) | ME02998B (enExample) |
| MX (4) | MX354509B (enExample) |
| MY (1) | MY179607A (enExample) |
| PL (2) | PL2694485T3 (enExample) |
| PT (1) | PT2694072T (enExample) |
| RS (1) | RS56759B2 (enExample) |
| RU (4) | RU2013148732A (enExample) |
| SG (5) | SG194048A1 (enExample) |
| SI (1) | SI2694072T2 (enExample) |
| SM (1) | SMT201800250T1 (enExample) |
| TR (1) | TR201802093T4 (enExample) |
| WO (4) | WO2012135759A1 (enExample) |
| ZA (4) | ZA201308064B (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR101660050B1 (ko) | 2008-01-04 | 2016-09-26 | 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 |
| PT3289876T (pt) | 2008-06-16 | 2022-10-28 | Univ Tennessee Res Found | Compostos para o tratamento do câncer |
| US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
| EP3238722B1 (en) | 2011-01-10 | 2019-03-13 | Infinity Pharmaceuticals, Inc. | Solid forms of isoquinolinones |
| CN103298345B (zh) | 2011-01-11 | 2016-12-14 | 诺瓦蒂斯公司 | 组合 |
| CN103857395A (zh) | 2011-04-01 | 2014-06-11 | 基因泰克公司 | Akt抑制剂化合物和阿比特龙的组合及使用方法 |
| US9216170B2 (en) | 2012-03-19 | 2015-12-22 | Hoffmann-La Roche Inc. | Combination therapy for proliferative disorders |
| US20150023954A1 (en) * | 2012-03-23 | 2015-01-22 | Memorial Sloan-Kettering Cancer Center | Potentiating antibody-induced complement-mediated cytotoxicity via pi3k inhibition |
| CA2904338C (en) | 2013-03-05 | 2022-07-05 | University Of Tennessee Research Foundation | Use of imidazole derivatives in combination with a braf inhibitor or mek inhibitor in the treatment of cancer |
| 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 |
| CN109674801A (zh) * | 2013-10-01 | 2019-04-26 | 诺华股份有限公司 | 组合 |
| SI3068770T1 (sl) * | 2013-11-15 | 2020-02-28 | F. Hoffmann-La Roche Ag | Postopki za pripravo pirimidinilciklopentanskih spojin |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| US20150320754A1 (en) * | 2014-04-16 | 2015-11-12 | 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 |
| ES2863500T3 (es) | 2015-04-10 | 2021-10-11 | Capsugel Belgium Nv | Formulaciones lipídicas de acetato de abiraterona |
| US20180369195A1 (en) * | 2015-11-30 | 2018-12-27 | 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 |
| AU2017281797A1 (en) | 2016-06-24 | 2019-01-24 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| US11040027B2 (en) | 2017-01-17 | 2021-06-22 | 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 |
| WO2020131765A1 (en) | 2018-12-19 | 2020-06-25 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising an akt inhibitor, a taxane, and a pd-l1 inhibitor |
| 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 |
| SG11202113363QA (en) | 2019-09-13 | 2021-12-30 | Praxair Technology Inc | Methods for producing increased crystalline and dense improved coatings |
| CA3183401A1 (en) * | 2020-05-19 | 2021-11-25 | Board Of Regents, The University Of Texas System | Methods for the treatment of pancreatitis and prevention of pancreatic cancer |
| WO2023109540A1 (zh) * | 2021-12-17 | 2023-06-22 | 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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- 2013-09-30 IL IL228637A patent/IL228637B/en active IP Right Grant
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- 2013-10-29 ZA ZA2013/08062A patent/ZA201308062B/en unknown
- 2013-11-01 ZA ZA2013/08198A patent/ZA201308198B/en 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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