JP2020510027A5 - - Google Patents
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- JP2020510027A5 JP2020510027A5 JP2019548708A JP2019548708A JP2020510027A5 JP 2020510027 A5 JP2020510027 A5 JP 2020510027A5 JP 2019548708 A JP2019548708 A JP 2019548708A JP 2019548708 A JP2019548708 A JP 2019548708A JP 2020510027 A5 JP2020510027 A5 JP 2020510027A5
- Authority
- JP
- Japan
- Prior art keywords
- weight
- pharmaceutical composition
- brigatinib
- tablet
- composition according
- 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.)
- Pending
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 81
- AILRADAXUVEEIR-UHFFFAOYSA-N 5-chloro-4-n-(2-dimethylphosphorylphenyl)-2-n-[2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrimidine-2,4-diamine Chemical compound COC1=CC(N2CCC(CC2)N2CCN(C)CC2)=CC=C1NC(N=1)=NC=C(Cl)C=1NC1=CC=CC=C1P(C)(C)=O AILRADAXUVEEIR-UHFFFAOYSA-N 0.000 claims description 65
- 229950004272 brigatinib Drugs 0.000 claims description 53
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims description 30
- 238000000034 method Methods 0.000 claims description 28
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 22
- 239000008119 colloidal silica Substances 0.000 claims description 21
- 230000002209 hydrophobic effect Effects 0.000 claims description 21
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 19
- 229960001021 lactose monohydrate Drugs 0.000 claims description 19
- 229940079832 sodium starch glycolate Drugs 0.000 claims description 19
- 229920003109 sodium starch glycolate Polymers 0.000 claims description 19
- 239000008109 sodium starch glycolate Substances 0.000 claims description 19
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 18
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 18
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 18
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 18
- 235000019359 magnesium stearate Nutrition 0.000 claims description 15
- 239000002245 particle Substances 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 8
- 239000011248 coating agent Substances 0.000 claims description 7
- 238000000576 coating method Methods 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 5
- 208000035475 disorder Diseases 0.000 claims description 5
- 230000005764 inhibitory process Effects 0.000 claims description 5
- 239000012458 free base Substances 0.000 claims description 3
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 3
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 3
- 238000009492 tablet coating Methods 0.000 claims description 2
- 239000002700 tablet coating Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 description 6
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- 238000002156 mixing Methods 0.000 description 3
- 229920000642 polymer Polymers 0.000 description 3
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 description 3
- 235000010980 cellulose Nutrition 0.000 description 2
- 229920002678 cellulose Polymers 0.000 description 2
- 239000001913 cellulose Substances 0.000 description 2
- 238000011278 co-treatment Methods 0.000 description 2
- 239000013078 crystal Substances 0.000 description 2
- 238000012216 screening Methods 0.000 description 2
- JLVVSXFLKOJNIY-UHFFFAOYSA-N Magnesium ion Chemical compound [Mg+2] JLVVSXFLKOJNIY-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 239000004372 Polyvinyl alcohol Substances 0.000 description 1
- 229920006243 acrylic copolymer Polymers 0.000 description 1
- 239000008186 active pharmaceutical agent Substances 0.000 description 1
- 229920003086 cellulose ether Polymers 0.000 description 1
- 229920001688 coating polymer Polymers 0.000 description 1
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 229920001577 copolymer Polymers 0.000 description 1
- 238000002425 crystallisation Methods 0.000 description 1
- 230000008025 crystallization Effects 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940057948 magnesium stearate Drugs 0.000 description 1
- 125000005395 methacrylic acid group Chemical group 0.000 description 1
- 239000012452 mother liquor Substances 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 229920000058 polyacrylate Polymers 0.000 description 1
- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 229920002451 polyvinyl alcohol Polymers 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000009495 sugar coating Methods 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 238000001238 wet grinding Methods 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022201704A JP2023027312A (ja) | 2017-03-08 | 2022-12-19 | ５－クロロ－ｎ４－［２－（ジメチルホスホリル）フェニル］－ｎ２－｛２－メトキシ－４－［４－（４－メチルピペラジン－１－イル）ピペリジン－１－イル］フェニル｝ピリミジン－２，４－ジアミンを含む医薬製剤 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762468696P | 2017-03-08 | 2017-03-08 | |
| US62/468,696 | 2017-03-08 | ||
| US201762491179P | 2017-04-27 | 2017-04-27 | |
| US62/491,179 | 2017-04-27 | ||
| US201762569954P | 2017-10-09 | 2017-10-09 | |
| US62/569,954 | 2017-10-09 | ||
| PCT/US2018/021128 WO2018165145A1 (en) | 2017-03-08 | 2018-03-06 | Pharmaceutical formulations comprising 5-chloro-n4-[2-(dimethylphosphoryl) phenyl]-n2-{2-methoxy-4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl} pyrimidine-2,4-diamine |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022201704A Division JP2023027312A (ja) | 2017-03-08 | 2022-12-19 | ５－クロロ－ｎ４－［２－（ジメチルホスホリル）フェニル］－ｎ２－｛２－メトキシ－４－［４－（４－メチルピペラジン－１－イル）ピペリジン－１－イル］フェニル｝ピリミジン－２，４－ジアミンを含む医薬製剤 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020510027A JP2020510027A (ja) | 2020-04-02 |
| JP2020510027A5 true JP2020510027A5 (enExample) | 2021-04-30 |
Family
ID=61750531
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019548708A Pending JP2020510027A (ja) | 2017-03-08 | 2018-03-06 | ５−クロロ−ｎ４−［２−（ジメチルホスホリル）フェニル］−ｎ２−｛２−メトキシ−４−［４−（４−メチルピペラジン−１−イル）ピペリジン−１−イル］フェニル｝ピリミジン−２，４−ジアミンを含む医薬製剤 |
| JP2022201704A Pending JP2023027312A (ja) | 2017-03-08 | 2022-12-19 | ５－クロロ－ｎ４－［２－（ジメチルホスホリル）フェニル］－ｎ２－｛２－メトキシ－４－［４－（４－メチルピペラジン－１－イル）ピペリジン－１－イル］フェニル｝ピリミジン－２，４－ジアミンを含む医薬製剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022201704A Pending JP2023027312A (ja) | 2017-03-08 | 2022-12-19 | ５－クロロ－ｎ４－［２－（ジメチルホスホリル）フェニル］－ｎ２－｛２－メトキシ－４－［４－（４－メチルピペラジン－１－イル）ピペリジン－１－イル］フェニル｝ピリミジン－２，４－ジアミンを含む医薬製剤 |
Country Status (7)
| Country | Link |
|---|---|
| US (5) | US20180256610A1 (enExample) |
| EP (1) | EP3592338A1 (enExample) |
| JP (2) | JP2020510027A (enExample) |
| CN (1) | CN110520110A (enExample) |
| CA (1) | CA3055109A1 (enExample) |
| TW (1) | TWI794214B (enExample) |
| WO (1) | WO2018165145A1 (enExample) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019182936A1 (en) * | 2018-03-19 | 2019-09-26 | Ariad Pharmaceuticals, Inc. | Methods of treating cancer in pediatric patients |
| TW202207940A (zh) * | 2020-04-14 | 2022-03-01 | 美商健生生物科技公司 | 包含胺基嘧啶衍生物或其醫藥上可接受之鹽、水合物、或溶劑化物之用於經口投予之醫藥組成物 |
| AU2022306151B2 (en) * | 2021-07-05 | 2024-11-14 | Qilu Pharmaceutical Co., Ltd. | Pharmaceutical composition, and preparation method therefor and application thereof |
| CN116407512A (zh) * | 2021-12-31 | 2023-07-11 | 南京艾德凯腾生物医药有限责任公司 | 一种布格替尼冻干口崩片及其制备方法 |
| CN115154473A (zh) * | 2022-08-04 | 2022-10-11 | 中国人民解放军陆军特色医学中心 | 布格替尼作为axl、c-met、st3gal4抑制剂的新应用 |
Family Cites Families (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20120208824A1 (en) * | 2006-01-20 | 2012-08-16 | Cell Signaling Technology, Inc. | ROS Kinase in Lung Cancer |
| CN102105150B (zh) | 2008-05-21 | 2014-03-12 | 阿里亚德医药股份有限公司 | 用作激酶抑制剂的磷衍生物 |
| RU2011137516A (ru) * | 2009-02-13 | 2013-03-20 | Ипсен Фарма С.А.С. | ТВЕРДАЯ ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, СОДЕРЖАЩАЯ 6-ОКСО-6,7,8,9,10,11-ГЕКСАГИДРОЦИКЛОГЕПТА[c]ХРОМЕН-3-ИЛСУЛЬФАМАТ И ЕГО ПОЛИФОРМЫ |
| US8691281B2 (en) * | 2009-02-13 | 2014-04-08 | Ipsen Pharma S.A.S. | Solid pharmaceutical composition containing 6-oxo-6,7,8,9,10,11-hexahydrocyclohepta (C)chromen-3-yl sulfamate and polymorphs thereof |
| EP2627179A4 (en) * | 2010-10-14 | 2014-04-02 | Ariad Pharma Inc | METHODS OF INHIBITING CELL PROLIFERATION IN EGFR-INDUCED CANCERS |
| WO2013008253A2 (en) * | 2011-07-11 | 2013-01-17 | Dr. Reddys Laboratories Limited | Imatinib formulations |
| TWI589576B (zh) * | 2011-07-15 | 2017-07-01 | 諾華公司 | 氮雜－雙環二芳基醚之鹽類及製造彼等或其前驅物之方法 |
| EP2753312B1 (en) * | 2011-09-08 | 2016-12-14 | Mereo BioPharma 2 Limited | Use of an aromatase inhibitor for the treatment of hypogonadism and related diseases |
| HK1202377A1 (en) * | 2011-11-14 | 2015-10-02 | Tesaro Inc. | Modulating certain tyrosine kinases |
| JP2015501645A (ja) * | 2011-12-10 | 2015-01-19 | オハイオ・ステイト・イノベーション・ファウンデーション | 肺がんの腫瘍発生および化学療法耐性を低減するために有用なｍｉＲＮＡならびに関連する組成物および方法 |
| CN102600146B (zh) * | 2012-04-11 | 2014-10-08 | 兆科药业（合肥）有限公司 | 一种盐酸乐卡地平和氯沙坦钾复方制剂及其制备方法 |
| BR112015023020A2 (pt) * | 2013-03-14 | 2017-07-18 | Pfizer | combinação de inibidor de egfr t790m e inibidor de egfr para o tratamento de câncer pulmonar de células não-pequenas |
| US9474761B2 (en) * | 2014-06-10 | 2016-10-25 | The George Washington University | Use of NK-1 receptor antagonists for treating hypomagnesemia, neurogenic inflammation, and cardiac dysfunction associated with EGFR-blocking drugs |
| HRP20201343T1 (hr) * | 2014-10-21 | 2020-11-27 | Ariad Pharmaceuticals, Inc. | Kristalni oblici 5-kloro-n4-[-2-(dimetilfosforil)fenil]-n2-{2-metoksi-4-[4-(4-metilpiperazin-1-il)piperidin-1-il]pirimidin-2,4-diamina |
| CN105061506B (zh) * | 2015-07-27 | 2017-08-29 | 苏州明锐医药科技有限公司 | 抗肿瘤药物ap26113的制备方法 |
| US10813935B2 (en) * | 2017-02-23 | 2020-10-27 | Transgenex Nanobiotech, Inc. | Methods and compositions for treating drug resistance in cancer |
-
2018
- 2018-03-06 WO PCT/US2018/021128 patent/WO2018165145A1/en not_active Ceased
- 2018-03-06 JP JP2019548708A patent/JP2020510027A/ja active Pending
- 2018-03-06 CN CN201880021866.7A patent/CN110520110A/zh active Pending
- 2018-03-06 CA CA3055109A patent/CA3055109A1/en active Pending
- 2018-03-06 EP EP18712759.2A patent/EP3592338A1/en not_active Withdrawn
- 2018-03-07 US US15/914,899 patent/US20180256610A1/en not_active Abandoned
- 2018-03-08 TW TW107107838A patent/TWI794214B/zh active
-
2021
- 2021-03-05 US US17/193,502 patent/US20210186994A1/en not_active Abandoned
- 2021-09-14 US US17/474,246 patent/US20210401860A1/en not_active Abandoned
-
2022
- 2022-04-22 US US17/726,736 patent/US20220249524A1/en not_active Abandoned
- 2022-12-19 JP JP2022201704A patent/JP2023027312A/ja active Pending
-
2023
- 2023-11-14 US US18/508,499 patent/US20240082275A1/en not_active Abandoned
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