JP2020527575A5 - - Google Patents
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- JP2020527575A5 JP2020527575A5 JP2020502346A JP2020502346A JP2020527575A5 JP 2020527575 A5 JP2020527575 A5 JP 2020527575A5 JP 2020502346 A JP2020502346 A JP 2020502346A JP 2020502346 A JP2020502346 A JP 2020502346A JP 2020527575 A5 JP2020527575 A5 JP 2020527575A5
- Authority
- JP
- Japan
- Prior art keywords
- weight
- pharmaceutical composition
- mixture
- composition according
- difluorobenzyl
- 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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- 239000008194 pharmaceutical composition Substances 0.000 claims 28
- 239000000203 mixture Substances 0.000 claims 16
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 10
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 claims 6
- 125000006288 3,5-difluorobenzyl group Chemical group [H]C1=C(F)C([H])=C(C([H])=C1F)C([H])([H])* 0.000 claims 5
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 5
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims 5
- 229960000913 crospovidone Drugs 0.000 claims 5
- 235000019359 magnesium stearate Nutrition 0.000 claims 5
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 claims 5
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 claims 5
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 claims 4
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 4
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 4
- 239000002775 capsule Substances 0.000 claims 4
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 4
- 239000008101 lactose Substances 0.000 claims 4
- 229960001375 lactose Drugs 0.000 claims 4
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 4
- 239000008108 microcrystalline cellulose Substances 0.000 claims 4
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 4
- HAYYBYPASCDWEQ-UHFFFAOYSA-N n-[5-[(3,5-difluorophenyl)methyl]-1h-indazol-3-yl]-4-(4-methylpiperazin-1-yl)-2-(oxan-4-ylamino)benzamide Chemical compound C1CN(C)CCN1C(C=C1NC2CCOCC2)=CC=C1C(=O)NC(C1=C2)=NNC1=CC=C2CC1=CC(F)=CC(F)=C1 HAYYBYPASCDWEQ-UHFFFAOYSA-N 0.000 claims 4
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 3
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 3
- 229960003943 hypromellose Drugs 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 238000002156 mixing Methods 0.000 claims 3
- 229940095064 tartrate Drugs 0.000 claims 3
- SERLAGPUMNYUCK-DCUALPFSSA-N 1-O-alpha-D-glucopyranosyl-D-mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO[C@H]1O[C@H](CO)[C@@H](O)[C@H](O)[C@H]1O SERLAGPUMNYUCK-DCUALPFSSA-N 0.000 claims 2
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 2
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims 2
- 229930195725 Mannitol Natural products 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 229920002472 Starch Polymers 0.000 claims 2
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 2
- 229960004977 anhydrous lactose Drugs 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000000905 isomalt Substances 0.000 claims 2
- 235000010439 isomalt Nutrition 0.000 claims 2
- HPIGCVXMBGOWTF-UHFFFAOYSA-N isomaltol Natural products CC(=O)C=1OC=CC=1O HPIGCVXMBGOWTF-UHFFFAOYSA-N 0.000 claims 2
- 239000000594 mannitol Substances 0.000 claims 2
- 235000010355 mannitol Nutrition 0.000 claims 2
- 239000008107 starch Substances 0.000 claims 2
- 235000019698 starch Nutrition 0.000 claims 2
- 235000002906 tartaric acid Nutrition 0.000 claims 2
- 239000011975 tartaric acid Substances 0.000 claims 2
- -1 4-methyl-piperazine-1-yl Chemical group 0.000 claims 1
- 101000686031 Homo sapiens Proto-oncogene tyrosine-protein kinase ROS Proteins 0.000 claims 1
- 101150111783 NTRK1 gene Proteins 0.000 claims 1
- 101150117329 NTRK3 gene Proteins 0.000 claims 1
- 101150056950 Ntrk2 gene Proteins 0.000 claims 1
- 102100023347 Proto-oncogene tyrosine-protein kinase ROS Human genes 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 238000004090 dissolution Methods 0.000 claims 1
- 230000009246 food effect Effects 0.000 claims 1
- 235000021471 food effect Nutrition 0.000 claims 1
- 229940057948 magnesium stearate Drugs 0.000 claims 1
- 239000007974 sodium acetate buffer Substances 0.000 claims 1
- 239000008247 solid mixture Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762534585P | 2017-07-19 | 2017-07-19 | |
| US62/534,585 | 2017-07-19 | ||
| PCT/US2018/042756 WO2019018570A1 (en) | 2017-07-19 | 2018-07-18 | PHARMACEUTICAL COMPOSITIONS CONTAINING ENTRECTINIB |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020527575A JP2020527575A (ja) | 2020-09-10 |
| JP2020527575A5 true JP2020527575A5 (enExample) | 2021-08-26 |
| JP7203083B2 JP7203083B2 (ja) | 2023-01-12 |
Family
ID=63254769
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020502346A Active JP7203083B2 (ja) | 2017-07-19 | 2018-07-18 | エントレクチニブを含む薬学的組成物 |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US10398693B2 (enExample) |
| EP (1) | EP3654952A1 (enExample) |
| JP (1) | JP7203083B2 (enExample) |
| KR (1) | KR102718538B1 (enExample) |
| CN (1) | CN110913842A (enExample) |
| AU (1) | AU2018302170B2 (enExample) |
| BR (1) | BR112020000793A2 (enExample) |
| CA (1) | CA3069339A1 (enExample) |
| IL (1) | IL271759B2 (enExample) |
| TW (1) | TWI785074B (enExample) |
| WO (1) | WO2019018570A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
| US10085979B2 (en) | 2014-12-02 | 2018-10-02 | Ignyta, Inc. | Combinations for the treatment of neuroblastoma |
| WO2017106492A1 (en) | 2015-12-18 | 2017-06-22 | Ignyta, Inc. | Combinations for the treatment of cancer |
| JP7203083B2 (ja) | 2017-07-19 | 2023-01-12 | イグナイタ インコーポレイテッド | エントレクチニブを含む薬学的組成物 |
| EP3697390A1 (en) | 2017-10-17 | 2020-08-26 | Ignyta, Inc. | Pharmaceutical compositions and dosage forms |
| CN119909073A (zh) * | 2019-07-31 | 2025-05-02 | 豪夫迈·罗氏有限公司 | 新型药物制剂 |
| CN116744931A (zh) * | 2020-12-31 | 2023-09-12 | 石药集团中奇制药技术(石家庄)有限公司 | 一种多靶点蛋白激酶抑制剂的药物组合物及其应用 |
| WO2023230454A1 (en) * | 2022-05-24 | 2023-11-30 | Icahn School Of Medicine At Mount Sinai | Neurotrophic tyrosine receptor kinase inhibitors as therapeutics for liver disease |
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| JPS6041489A (ja) | 1983-08-12 | 1985-03-05 | Kyowa Hakko Kogyo Co Ltd | 新規生理活性物質k―252 |
| US5736158A (en) * | 1996-03-27 | 1998-04-07 | The Block Drug Company | Partial denture cleanser with fluoride |
| JP3529102B2 (ja) * | 1997-07-11 | 2004-05-24 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノート シヤツプ | 5−ht3および5−ht4介在性障害に有用な(+)−ノルシサプリド |
| WO1999043302A1 (en) * | 1998-02-27 | 1999-09-02 | Watson Pharmaceuticals, Inc. | Stabilizing composition for pharmaceutical dosage forms |
| JP2002275068A (ja) | 2001-03-16 | 2002-09-25 | Kyowa Hakko Kogyo Co Ltd | アポトーシス誘導剤 |
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| WO2003051847A1 (en) | 2001-12-19 | 2003-06-26 | Smithkline Beecham P.L.C. | (1-h-indazol-3-yl) -amide derivatives as gsk-3 inhibitors |
| FR2836915B1 (fr) | 2002-03-11 | 2008-01-11 | Aventis Pharma Sa | Derives d'aminoindazoles, procede de preparation et intermediaires de ce procede a titre de medicaments et compositions pharmaceutiques les renfermant |
| WO2004007676A2 (en) | 2002-07-15 | 2004-01-22 | Combinatorx, Incorporated | Combination therapy for the treatment of neoplasms |
| AU2003278249B8 (en) | 2002-09-05 | 2010-11-18 | Aventis Pharma S.A. | Novel aminoindazole derivatives as medicines and pharmaceutical compositions containing same |
| PL376789A1 (pl) | 2002-12-12 | 2006-01-09 | Aventis Pharma S.A. | Pochodne aminoindazoli i ich zastosowanie jako inhibitorów kinazy |
| TW200423938A (en) | 2003-02-21 | 2004-11-16 | Wyeth Corp | 4-[(2,4-dichloro-5-methoxyphenyl)amino]-6-alkoxy-3-quinolinecarbonitriles for the treatment of ischemic injury |
| DK1603570T5 (da) | 2003-02-26 | 2013-12-09 | Sugen Inc | Aminoheteroarylforbindelser som proteinkinaseinhibitorer |
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| GB0305929D0 (en) | 2003-03-14 | 2003-04-23 | Novartis Ag | Organic compounds |
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| AU2006248780B2 (en) | 2005-05-16 | 2010-06-03 | Astrazeneca Ab | Pyrazolylaminopyrimidine derivatives useful as tyrosine kinase inhibitors |
| JP2009504608A (ja) | 2005-08-09 | 2009-02-05 | ヨハネス・グーテンベルク−ウニヴェルジテート・マインツ | 薬剤耐性肺癌のタンパク質キナーゼ阻害剤への感作 |
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| CN102924479A (zh) | 2011-08-09 | 2013-02-13 | 山东鲁北药业有限公司 | 一种星孢菌素类衍生物的半合成方法 |
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| US10231965B2 (en) | 2014-02-20 | 2019-03-19 | Ignyta, Inc. | Molecules for administration to ROS1 mutant cancer cells |
| PT3154959T (pt) | 2014-05-15 | 2019-09-24 | Array Biopharma Inc | 1-((3s,4r)-4-(3-fluorofenil)-1-(2-metoxietil)-pirrolidin-3-il)-3-(4-metil-3-(2-metilpirimidin-5-il)-1-fenil-1h-pirazol-5-il)ureia como inibidor da cinase trka |
| US9901583B2 (en) | 2014-06-13 | 2018-02-27 | Oncoethix Gmbh | Method of treating non-small cell lung cancer and/or small cell lung cancer using thienotriazolodiazepine compounds |
| US10085979B2 (en) | 2014-12-02 | 2018-10-02 | Ignyta, Inc. | Combinations for the treatment of neuroblastoma |
| US20170356918A1 (en) | 2014-12-03 | 2017-12-14 | Ignyta, Inc. | Multiplexed immunohistochemistry assays for diagnosis and treatment of cancer |
| EP3303382A4 (en) | 2015-05-29 | 2018-12-19 | Ignyta, Inc. | Compositions and methods for treating patients with rtk mutant cells |
| EP3722441A1 (en) | 2015-06-01 | 2020-10-14 | Loxo Oncology Inc. | Method of diagnosing a cancer for a treatment with a trk inhibitor |
| JP2018534296A (ja) | 2015-10-26 | 2018-11-22 | ロクソ オンコロジー, インコーポレイテッドLoxo Oncology, Inc. | Trk阻害薬耐性がんにおける点変異およびそれに関連する方法 |
| WO2017106492A1 (en) * | 2015-12-18 | 2017-06-22 | Ignyta, Inc. | Combinations for the treatment of cancer |
| JP7203083B2 (ja) | 2017-07-19 | 2023-01-12 | イグナイタ インコーポレイテッド | エントレクチニブを含む薬学的組成物 |
| EP3697390A1 (en) | 2017-10-17 | 2020-08-26 | Ignyta, Inc. | Pharmaceutical compositions and dosage forms |
-
2018
- 2018-07-18 JP JP2020502346A patent/JP7203083B2/ja active Active
- 2018-07-18 CA CA3069339A patent/CA3069339A1/en active Pending
- 2018-07-18 US US16/039,196 patent/US10398693B2/en active Active
- 2018-07-18 EP EP18756313.5A patent/EP3654952A1/en active Pending
- 2018-07-18 AU AU2018302170A patent/AU2018302170B2/en active Active
- 2018-07-18 WO PCT/US2018/042756 patent/WO2019018570A1/en not_active Ceased
- 2018-07-18 IL IL271759A patent/IL271759B2/en unknown
- 2018-07-18 BR BR112020000793-5A patent/BR112020000793A2/pt unknown
- 2018-07-18 KR KR1020207002728A patent/KR102718538B1/ko active Active
- 2018-07-18 CN CN201880047029.1A patent/CN110913842A/zh active Pending
- 2018-07-19 TW TW107125013A patent/TWI785074B/zh active
-
2020
- 2020-01-17 US US16/746,644 patent/US11253515B2/en active Active
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