JP2015512942A5 - - Google Patents
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- JP2015512942A5 JP2015512942A5 JP2015505912A JP2015505912A JP2015512942A5 JP 2015512942 A5 JP2015512942 A5 JP 2015512942A5 JP 2015505912 A JP2015505912 A JP 2015505912A JP 2015505912 A JP2015505912 A JP 2015505912A JP 2015512942 A5 JP2015512942 A5 JP 2015512942A5
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- JP
- Japan
- Prior art keywords
- polymorph
- methyl
- ray powder
- powder diffraction
- expressed
- 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.)
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- 238000000634 powder X-ray diffraction Methods 0.000 claims description 24
- 150000001875 compounds Chemical class 0.000 claims description 23
- 238000000034 method Methods 0.000 claims description 17
- 206010028980 Neoplasm Diseases 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 11
- 239000000203 mixture Substances 0.000 claims description 10
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical group CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 8
- 238000004519 manufacturing process Methods 0.000 claims description 8
- 239000002904 solvent Substances 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- -1 pyran-4-yl Chemical group 0.000 claims description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 101000882127 Homo sapiens Histone-lysine N-methyltransferase EZH2 Proteins 0.000 claims description 5
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical compound Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 claims description 5
- 230000000694 effects Effects 0.000 claims description 5
- KLYFLPQLTNAFGR-UHFFFAOYSA-N 3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzoic acid Chemical compound C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(O)=O)=C(C)C=1N(CC)C1CCOCC1 KLYFLPQLTNAFGR-UHFFFAOYSA-N 0.000 claims description 4
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 claims description 4
- 108010036115 Histone Methyltransferases Proteins 0.000 claims description 4
- 102000011787 Histone Methyltransferases Human genes 0.000 claims description 4
- 102100038970 Histone-lysine N-methyltransferase EZH2 Human genes 0.000 claims description 4
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical group COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims description 4
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 4
- 239000003085 diluting agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 4
- 239000002244 precipitate Substances 0.000 claims description 4
- 238000001757 thermogravimetry curve Methods 0.000 claims description 4
- 230000002401 inhibitory effect Effects 0.000 claims description 3
- 230000005764 inhibitory process Effects 0.000 claims description 3
- FSPIBFKGESGOLU-UHFFFAOYSA-N 4,6-dimethyl-1h-pyridin-2-one Chemical compound CC1=CC(C)=NC(O)=C1 FSPIBFKGESGOLU-UHFFFAOYSA-N 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims description 2
- 238000001914 filtration Methods 0.000 claims description 2
- 239000012535 impurity Substances 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- UQRICAQPWZSJNF-UHFFFAOYSA-N n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide;hydrobromide Chemical compound Br.C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCOCC1 UQRICAQPWZSJNF-UHFFFAOYSA-N 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 238000001953 recrystallisation Methods 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 230000001747 exhibiting effect Effects 0.000 claims 2
- WVYJQDGOYSNTQB-UHFFFAOYSA-N Br.C(C)N(C1CCOCC1)C1=C(C=CC(=C1C(=O)N)C)C1=CC=C(C=C1)CN1CCOCC1 Chemical compound Br.C(C)N(C1CCOCC1)C1=C(C=CC(=C1C(=O)N)C)C1=CC=C(C=C1)CN1CCOCC1 WVYJQDGOYSNTQB-UHFFFAOYSA-N 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- BBCSKDZLEVADMO-UHFFFAOYSA-N 2-[ethyl(oxan-4-yl)amino]-6-methyl-3-[4-(morpholin-4-ylmethyl)phenyl]benzamide Chemical compound C(C)N(C1CCOCC1)C1=C(C=CC(=C1C(=O)N)C)C1=CC=C(C=C1)CN1CCOCC1 BBCSKDZLEVADMO-UHFFFAOYSA-N 0.000 description 1
- IHTNRDIBNXBSIF-UHFFFAOYSA-N 2-ethyloxane Chemical compound CCC1CCCCO1 IHTNRDIBNXBSIF-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261624215P | 2012-04-13 | 2012-04-13 | |
| US61/624,215 | 2012-04-13 | ||
| PCT/US2013/036193 WO2013155317A1 (en) | 2012-04-13 | 2013-04-11 | Salt form of a human hi stone methyltransf erase ezh2 inhibitor |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017198642A Division JP6634058B2 (ja) | 2012-04-13 | 2017-10-12 | ヒトヒストンメチルトランスフェラーゼｅｚｈ２阻害剤の塩形態 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015512942A JP2015512942A (ja) | 2015-04-30 |
| JP2015512942A5 true JP2015512942A5 (enExample) | 2016-06-09 |
| JP6255382B2 JP6255382B2 (ja) | 2017-12-27 |
Family
ID=49328166
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015505912A Active JP6255382B2 (ja) | 2012-04-13 | 2013-04-11 | ヒトヒストンメチルトランスフェラーゼｅｚｈ２阻害剤の塩形態 |
| JP2017198642A Active JP6634058B2 (ja) | 2012-04-13 | 2017-10-12 | ヒトヒストンメチルトランスフェラーゼｅｚｈ２阻害剤の塩形態 |
| JP2018187463A Pending JP2018199740A (ja) | 2012-04-13 | 2018-10-02 | ヒトヒストンメチルトランスフェラーゼｅｚｈ２阻害剤の塩形態 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017198642A Active JP6634058B2 (ja) | 2012-04-13 | 2017-10-12 | ヒトヒストンメチルトランスフェラーゼｅｚｈ２阻害剤の塩形態 |
| JP2018187463A Pending JP2018199740A (ja) | 2012-04-13 | 2018-10-02 | ヒトヒストンメチルトランスフェラーゼｅｚｈ２阻害剤の塩形態 |
Country Status (26)
| Country | Link |
|---|---|
| US (7) | US9394283B2 (enExample) |
| EP (4) | EP3184523B1 (enExample) |
| JP (3) | JP6255382B2 (enExample) |
| KR (4) | KR20250005505A (enExample) |
| CN (2) | CN104603130B (enExample) |
| AU (2) | AU2013245878B2 (enExample) |
| BR (1) | BR112014025508B1 (enExample) |
| CA (1) | CA2870005C (enExample) |
| CY (2) | CY1119383T1 (enExample) |
| DK (3) | DK3628670T3 (enExample) |
| ES (3) | ES2745016T3 (enExample) |
| HR (2) | HRP20170295T1 (enExample) |
| HU (3) | HUE031976T2 (enExample) |
| IL (4) | IL296199B2 (enExample) |
| IN (1) | IN2014DN09068A (enExample) |
| LT (2) | LT3184523T (enExample) |
| MX (2) | MX384641B (enExample) |
| NZ (1) | NZ700761A (enExample) |
| PL (3) | PL3184523T3 (enExample) |
| PT (3) | PT2836491T (enExample) |
| RS (2) | RS55690B1 (enExample) |
| RU (1) | RU2658911C2 (enExample) |
| SG (3) | SG10201608577RA (enExample) |
| SI (2) | SI2836491T1 (enExample) |
| SM (2) | SMT201700132T1 (enExample) |
| WO (1) | WO2013155317A1 (enExample) |
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| AU2014337300B2 (en) | 2013-10-16 | 2019-01-03 | Eisai R&D Management Co., Ltd. | Hydrochloride salt form for EZH2 inhibition |
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