JP2018516946A5 - - Google Patents
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- JP2018516946A5 JP2018516946A5 JP2017563542A JP2017563542A JP2018516946A5 JP 2018516946 A5 JP2018516946 A5 JP 2018516946A5 JP 2017563542 A JP2017563542 A JP 2017563542A JP 2017563542 A JP2017563542 A JP 2017563542A JP 2018516946 A5 JP2018516946 A5 JP 2018516946A5
- Authority
- JP
- Japan
- Prior art keywords
- oxoheptyl
- hydroxyamino
- chlorophenyl
- pyrimidine
- phenyl
- 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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- VLIUIBXPEDFJRF-UHFFFAOYSA-N 2-(N-(2-chlorophenyl)anilino)-N-[7-(hydroxyamino)-7-oxoheptyl]pyrimidine-5-carboxamide Chemical compound N1=CC(C(=O)NCCCCCCC(=O)NO)=CN=C1N(C=1C(=CC=CC=1)Cl)C1=CC=CC=C1 VLIUIBXPEDFJRF-UHFFFAOYSA-N 0.000 claims 9
- 239000000203 mixture Substances 0.000 claims 7
- 238000000634 powder X-ray diffraction Methods 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 2
- 238000002844 melting Methods 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 239000002244 precipitate Substances 0.000 claims 2
- 239000002002 slurry Substances 0.000 claims 2
- -1 7- (hydroxyamino) -7-oxoheptyl Chemical group 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 238000002441 X-ray diffraction Methods 0.000 claims 1
- 150000003857 carboxamides Chemical class 0.000 claims 1
- 238000001816 cooling Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000001914 filtration Methods 0.000 claims 1
- 238000010438 heat treatment Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000009251 multiple myeloma Diseases 0.000 claims 1
- 239000000843 powder Substances 0.000 claims 1
- 239000007787 solid Substances 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
Claims (11)
- 結晶形態の２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドであって、２θ（度）で表され、角度８．３±０．２°、１０．６±０．２°、１６．６±０．２°、２１．３±０．２°、及び２５．０±０．２°のピークを有する粉末Ｘ線回折パターンによって特徴づけられる（形態Ｉ）、結晶形態。
- 前記結晶形態が、約１７３°Ｃの融点によって特徴づけられる、請求項１に記載の結晶形態。
- 前記結晶形態が、１７３±２°Ｃの融点によって特徴づけられる、請求項１に記載の結晶形態。
- 結晶形態の２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミド、及び製薬上許容できるキャリアを含む、薬学的組成物であって、前記結晶形態が、２θ（度）で表され、角度８．３±０．２°、１０．６±０．２°、１６．６±０．２°、２１．３±０．２°、及び２５．０±０．２°のピークを有する粉末Ｘ線回折パターンによって特徴づけられる（形態Ｉ）、薬学的組成物。
- がんの治療のための医薬の製造における、結晶形態の２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドの使用であって、結晶形態が、２θ（度）で表され、角度８．３±０．２°、１０．６±０．２°、１６．６±０．２°、２１．３±０．２°、及び２５．０±０．２°のピークを有する粉末Ｘ線回折パターンによって特徴づけられる（形態Ｉ）、使用。
- 前記がんが多発性骨髄腫である、請求項５に記載の使用。
- （ａ）２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドを含む組成物を溶媒に懸濁しスラリーを形成すること、；
（ｂ）前記固体が溶解するまで前記スラリーを加熱すること、；
（ｃ）工程（ｂ）において形成される前記溶液に形態Ｉの２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドにおける結晶の種結晶を添加すること、；
（ｄ）沈殿物を形成するまで前記溶液を冷却すること、；及び
（ｅ）前記沈殿物をろ過することを含むプロセスによって形成される形態Ｉの２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドを含み、
形態Ｉが、２θ（度）で表され、角度８．３±０．２°、１０．６±０．２°、１６．６±０．２°、２１．３±０．２°、及び２５．０±０．２°のピークを有する粉末Ｘ線回折パターンによって特徴づけられる組成物。 - 前記組成物が、その他の結晶形の２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドを実質的に含まない、形態Ｉの２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドを含む、請求項７に記載の組成物。
- 前記２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドが、純度が９０％超である、請求項７に記載の組成物。
- 前記２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドが、純度が９５％超である、請求項７に記載の組成物。
- 前記２−（（２−クロロフェニル）（フェニル）アミノ）−Ｎ−（７−（ヒドロキシアミノ）−７−オキソヘプチル）ピリミジン−５−カルボキサミドが、純度が９９％超である、請求項７に記載の組成物。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562172629P | 2015-06-08 | 2015-06-08 | |
| US62/172,629 | 2015-06-08 | ||
| PCT/US2016/036422 WO2016200919A1 (en) | 2015-06-08 | 2016-06-08 | Crystalline forms of a histone deacetylase inhibitor |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018516946A JP2018516946A (ja) | 2018-06-28 |
| JP2018516946A5 true JP2018516946A5 (ja) | 2019-07-04 |
| JP6816036B2 JP6816036B2 (ja) | 2021-01-20 |
Family
ID=56178492
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017563542A Active JP6816036B2 (ja) | 2015-06-08 | 2016-06-08 | ヒストン脱アセチル化阻害剤の結晶形態 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10464906B2 (ja) |
| EP (1) | EP3303306B1 (ja) |
| JP (1) | JP6816036B2 (ja) |
| AR (1) | AR104935A1 (ja) |
| TW (1) | TW201718516A (ja) |
| WO (1) | WO2016200919A1 (ja) |
Families Citing this family (5)
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|---|---|---|---|---|
| WO2013158984A1 (en) | 2012-04-19 | 2013-10-24 | Acetylon Pharmaceuticals, Inc. | Biomarkers to identify patients that will respond to treatment and treating such patients |
| CN107922352B (zh) | 2015-06-08 | 2021-08-06 | 埃斯泰隆制药公司 | 制备蛋白质脱乙酰酶抑制剂的方法 |
| AR109250A1 (es) * | 2016-06-09 | 2018-11-14 | Acetylon Pharmaceuticals Inc | Métodos de uso y combinaciones farmacéuticas de inhibidores de hdac con inhibidores de proteínas bet |
| ES2929032T3 (es) | 2016-08-08 | 2022-11-24 | Acetylon Pharmaceuticals Inc | Combinaciones farmacéuticas de inhibidores de histona desacetilasa 6 y anticuerpos inhibidores de CD20 y usos de los mismos |
| WO2018098168A1 (en) | 2016-11-23 | 2018-05-31 | Acetylon Pharmaceuticals, Inc. | Pharmaceutical combinations comprising a histone deacetylase inhibitor and a programmed death-ligand 1 (pd-l1) inhibitor and methods of use thereof |
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-
2016
- 2016-06-08 US US15/176,788 patent/US10464906B2/en active Active
- 2016-06-08 JP JP2017563542A patent/JP6816036B2/ja active Active
- 2016-06-08 AR ARP160101702A patent/AR104935A1/es unknown
- 2016-06-08 EP EP16731454.1A patent/EP3303306B1/en active Active
- 2016-06-08 WO PCT/US2016/036422 patent/WO2016200919A1/en active Application Filing
- 2016-06-08 TW TW105118206A patent/TW201718516A/zh unknown
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