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 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 |
|---|---|---|---|
| US201161470803P | 2011-04-01 | 2011-04-01 | |
| US201161470624P | 2011-04-01 | 2011-04-01 | |
| US61/470,624 | 2011-04-01 | ||
| US61/470,803 | 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 |
| 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 |
| 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 |
| 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 (2)
| 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 |
| 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 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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) | US20150064171A1 (enExample) |
| EP (4) | EP2694072B2 (enExample) |
| JP (4) | JP6239497B2 (enExample) |
| KR (4) | KR101950044B1 (enExample) |
| CN (8) | CN104586861A (enExample) |
| AU (4) | AU2012236135A1 (enExample) |
| BR (4) | BR112013025386B1 (enExample) |
| CA (4) | CA2831937A1 (enExample) |
| DK (1) | DK2694072T4 (enExample) |
| ES (3) | ES2660263T5 (enExample) |
| FI (1) | FI2694072T4 (enExample) |
| HK (1) | HK1204575A1 (enExample) |
| HR (1) | HRP20180223T4 (enExample) |
| HU (1) | HUE036513T2 (enExample) |
| IL (4) | IL228638A0 (enExample) |
| LT (1) | LT2694072T (enExample) |
| ME (1) | ME02998B (enExample) |
| MX (4) | MX354509B (enExample) |
| MY (1) | MY179607A (enExample) |
| PL (2) | PL2694072T5 (enExample) |
| PT (1) | PT2694072T (enExample) |
| RS (1) | RS56759B2 (enExample) |
| RU (4) | RU2013148721A (enExample) |
| SG (5) | SG10201504303SA (enExample) |
| SI (1) | SI2694072T2 (enExample) |
| SM (1) | SMT201800250T1 (enExample) |
| TR (1) | TR201802093T4 (enExample) |
| WO (4) | WO2012135750A1 (enExample) |
| ZA (4) | ZA201308062B (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| KR101660050B1 (ko) | 2008-01-04 | 2016-09-26 | 인텔리카인, 엘엘씨 | 특정 화학 물질, 조성물 및 방법 |
| US9447049B2 (en) | 2010-03-01 | 2016-09-20 | University Of Tennessee Research Foundation | Compounds for treatment of cancer |
| HUE034598T2 (en) | 2008-06-16 | 2018-02-28 | Univ Tennessee Res Found | Compound for cancer treatment |
| US11084811B2 (en) | 2010-03-01 | 2021-08-10 | Oncternal Therapeutics, Inc. | Compounds for treatment of cancer |
| NZ612909A (en) | 2011-01-10 | 2015-09-25 | Infinity Pharmaceuticals Inc | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
| MX356704B (es) | 2011-01-11 | 2018-06-11 | Novartis Ag | Combinación. |
| JP6239497B2 (ja) | 2011-04-01 | 2017-11-29 | ジェネンテック， インコーポレイテッド | 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 |
| US9216170B2 (en) | 2012-03-19 | 2015-12-22 | Hoffmann-La Roche Inc. | Combination therapy for proliferative disorders |
| EP2827903A4 (en) * | 2012-03-23 | 2016-02-10 | Sloan Kettering Inst Cancer | POTENTIATION OF ANTIBODY-INDUCED COMPLEMENT-MEDIATED CYTOTOXICITY BY PI3K INHIBITION |
| CN109568312A (zh) | 2013-03-05 | 2019-04-05 | 田纳西大学研究基金会 | 用于治疗癌症的化合物 |
| 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 |
| EP4265300B1 (en) * | 2013-10-01 | 2025-12-10 | Novartis AG | Composition comprising a 17 a-hydroxylase/c17,20 lyase (cyp17a1) inhibitor and an akt inhibitor |
| MX367620B (es) * | 2013-11-15 | 2019-08-28 | Hoffmann La Roche | Procesos para la preparación de compuestos de pirimidinilciclopentano. |
| 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 |
| EP3280448B1 (en) | 2015-04-10 | 2020-12-30 | 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 |
| US11621057B2 (en) * | 2016-04-08 | 2023-04-04 | Biodesix, Inc. | Classifier generation methods and predictive test for ovarian cancer patient prognosis under platinum chemotherapy |
| BR112018077021A2 (pt) | 2016-06-24 | 2019-04-02 | Infinity Pharmaceuticals, Inc. | terapias de combinação |
| JP7300394B2 (ja) | 2017-01-17 | 2023-06-29 | ヘパリジェニックス ゲーエムベーハー | 肝再生の促進又は肝細胞死の低減もしくは予防のためのプロテインキナーゼ阻害 |
| EP3807248A4 (en) * | 2018-05-29 | 2021-10-27 | Council of Scientific and Industrial Research | BICYCLIC TOPOISOMERASE I INHIBITOR COMPOUNDS, THEIR PREPARATION AND USE |
| 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 |
| US11576919B2 (en) * | 2019-08-12 | 2023-02-14 | Genentech, Inc. | Treatment of breast cancer using combination therapies comprising an ATP competitive AKT inhibitor, a CDK4/6 inhibitor, and fulvestrant |
| CA3144088C (en) | 2019-09-13 | 2024-01-23 | Praxair S. T. Technology, Inc. | Methods for producing increased crystalline and dense improved coatings |
| US20230190718A1 (en) * | 2020-05-19 | 2023-06-22 | 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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- 2012-03-30 SG SG2013073788A patent/SG194052A1/en unknown
-
2013
- 2013-09-30 IL IL228638A patent/IL228638A0/en unknown
- 2013-09-30 IL IL228641A patent/IL228641A0/en unknown
- 2013-09-30 IL IL228642A patent/IL228642A0/en unknown
- 2013-09-30 IL IL228637A patent/IL228637B/en active IP Right Grant
- 2013-10-29 ZA ZA2013/08062A patent/ZA201308062B/en unknown
- 2013-10-29 ZA ZA2013/08065A patent/ZA201308065B/en unknown
- 2013-10-29 ZA ZA2013/08064A patent/ZA201308064B/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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