JP2018531963A5 - - Google Patents
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- JP2018531963A5 JP2018531963A5 JP2018521548A JP2018521548A JP2018531963A5 JP 2018531963 A5 JP2018531963 A5 JP 2018531963A5 JP 2018521548 A JP2018521548 A JP 2018521548A JP 2018521548 A JP2018521548 A JP 2018521548A JP 2018531963 A5 JP2018531963 A5 JP 2018531963A5
- Authority
- JP
- Japan
- Prior art keywords
- crystalline form
- form according
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- relative humidity
- crystalline
- 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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- 238000000034 method Methods 0.000 claims description 33
- 238000000113 differential scanning calorimetry Methods 0.000 claims description 32
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 32
- 238000001757 thermogravimetry curve Methods 0.000 claims description 32
- 239000013078 crystal Substances 0.000 claims description 30
- 238000002411 thermogravimetry Methods 0.000 claims description 30
- 239000000203 mixture Substances 0.000 claims description 27
- 150000001875 compounds Chemical class 0.000 claims description 23
- 239000002904 solvent Substances 0.000 claims description 15
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
- 208000013403 hyperactivity Diseases 0.000 claims description 13
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 12
- WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical group CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 12
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 12
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 12
- LRHPLDYGYMQRHN-UHFFFAOYSA-N N-Butanol Chemical compound CCCCO LRHPLDYGYMQRHN-UHFFFAOYSA-N 0.000 claims description 12
- YXFVVABEGXRONW-UHFFFAOYSA-N Toluene Chemical compound CC1=CC=CC=C1 YXFVVABEGXRONW-UHFFFAOYSA-N 0.000 claims description 12
- BDERNNFJNOPAEC-UHFFFAOYSA-N propan-1-ol Chemical compound CCCO BDERNNFJNOPAEC-UHFFFAOYSA-N 0.000 claims description 12
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims description 8
- IMNFDUFMRHMDMM-UHFFFAOYSA-N N-Heptane Chemical compound CCCCCCC IMNFDUFMRHMDMM-UHFFFAOYSA-N 0.000 claims description 8
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims description 8
- 238000001816 cooling Methods 0.000 claims description 8
- RWGFKTVRMDUZSP-UHFFFAOYSA-N cumene Chemical compound CC(C)C1=CC=CC=C1 RWGFKTVRMDUZSP-UHFFFAOYSA-N 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 8
- 239000002002 slurry Substances 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 6
- WSLDOOZREJYCGB-UHFFFAOYSA-N 1,2-Dichloroethane Chemical compound ClCCCl WSLDOOZREJYCGB-UHFFFAOYSA-N 0.000 claims description 4
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims description 4
- XNWFRZJHXBZDAG-UHFFFAOYSA-N 2-METHOXYETHANOL Chemical compound COCCO XNWFRZJHXBZDAG-UHFFFAOYSA-N 0.000 claims description 4
- 206010008748 Chorea Diseases 0.000 claims description 4
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims description 4
- 208000023105 Huntington disease Diseases 0.000 claims description 4
- NTIZESTWPVYFNL-UHFFFAOYSA-N Methyl isobutyl ketone Chemical compound CC(C)CC(C)=O NTIZESTWPVYFNL-UHFFFAOYSA-N 0.000 claims description 4
- BZLVMXJERCGZMT-UHFFFAOYSA-N Methyl tert-butyl ether Chemical compound COC(C)(C)C BZLVMXJERCGZMT-UHFFFAOYSA-N 0.000 claims description 4
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims description 4
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 4
- 208000016620 Tourette disease Diseases 0.000 claims description 4
- KXKVLQRXCPHEJC-UHFFFAOYSA-N acetic acid trimethyl ester Natural products COC(C)=O KXKVLQRXCPHEJC-UHFFFAOYSA-N 0.000 claims description 4
- 150000001298 alcohols Chemical class 0.000 claims description 4
- 150000001408 amides Chemical class 0.000 claims description 4
- 150000004649 carbonic acid derivatives Chemical class 0.000 claims description 4
- 150000008280 chlorinated hydrocarbons Chemical class 0.000 claims description 4
- 150000002148 esters Chemical class 0.000 claims description 4
- 150000002170 ethers Chemical class 0.000 claims description 4
- WBJINCZRORDGAQ-UHFFFAOYSA-N formic acid ethyl ester Natural products CCOC=O WBJINCZRORDGAQ-UHFFFAOYSA-N 0.000 claims description 4
- 238000010438 heat treatment Methods 0.000 claims description 4
- 125000000623 heterocyclic group Chemical group 0.000 claims description 4
- 229930195733 hydrocarbon Natural products 0.000 claims description 4
- 150000002430 hydrocarbons Chemical class 0.000 claims description 4
- GJRQTCIYDGXPES-UHFFFAOYSA-N iso-butyl acetate Natural products CC(C)COC(C)=O GJRQTCIYDGXPES-UHFFFAOYSA-N 0.000 claims description 4
- FGKJLKRYENPLQH-UHFFFAOYSA-M isocaproate Chemical compound CC(C)CCC([O-])=O FGKJLKRYENPLQH-UHFFFAOYSA-M 0.000 claims description 4
- JMMWKPVZQRWMSS-UHFFFAOYSA-N isopropanol acetate Natural products CC(C)OC(C)=O JMMWKPVZQRWMSS-UHFFFAOYSA-N 0.000 claims description 4
- 229940011051 isopropyl acetate Drugs 0.000 claims description 4
- GWYFCOCPABKNJV-UHFFFAOYSA-N isovaleric acid Chemical compound CC(C)CC(O)=O GWYFCOCPABKNJV-UHFFFAOYSA-N 0.000 claims description 4
- OQAGVSWESNCJJT-UHFFFAOYSA-N isovaleric acid methyl ester Natural products COC(=O)CC(C)C OQAGVSWESNCJJT-UHFFFAOYSA-N 0.000 claims description 4
- 150000002576 ketones Chemical class 0.000 claims description 4
- 150000002825 nitriles Chemical class 0.000 claims description 4
- 150000002828 nitro derivatives Chemical class 0.000 claims description 4
- LYGJENNIWJXYER-UHFFFAOYSA-N nitromethane Chemical compound C[N+]([O-])=O LYGJENNIWJXYER-UHFFFAOYSA-N 0.000 claims description 4
- 230000009467 reduction Effects 0.000 claims description 4
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Substances C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims description 4
- 208000024891 symptom Diseases 0.000 claims description 3
- 208000014094 Dystonic disease Diseases 0.000 claims description 2
- 108010029485 Protein Isoforms Proteins 0.000 claims description 2
- 102000001708 Protein Isoforms Human genes 0.000 claims description 2
- 102000009659 Vesicular Monoamine Transport Proteins Human genes 0.000 claims description 2
- 108010020033 Vesicular Monoamine Transport Proteins Proteins 0.000 claims description 2
- 208000012601 choreatic disease Diseases 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 208000010118 dystonia Diseases 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- WGFNXGPBPIJYLI-UHFFFAOYSA-N 2,6-difluoro-3-[(3-fluorophenyl)sulfonylamino]-n-(3-methoxy-1h-pyrazolo[3,4-b]pyridin-5-yl)benzamide Chemical compound C1=C2C(OC)=NNC2=NC=C1NC(=O)C(C=1F)=C(F)C=CC=1NS(=O)(=O)C1=CC=CC(F)=C1 WGFNXGPBPIJYLI-UHFFFAOYSA-N 0.000 claims 1
- 0 CC(C)C[C@@](CN(CCc1c2)[C@](C3)c1cc(OC)c2OC)[C@@]3OC([C@@](*)C(C)C)=O Chemical compound CC(C)C[C@@](CN(CCc1c2)[C@](C3)c1cc(OC)c2OC)[C@@]3OC([C@@](*)C(C)C)=O 0.000 description 3
- GEJDGVNQKABXKG-IRIUNPIQSA-N CC(C)CC(CN(CCc1c2)C(C3)c1cc(OC)c2OC)[C@@H]3OC([C@H](C(C)C)N)=O Chemical compound CC(C)CC(CN(CCc1c2)C(C3)c1cc(OC)c2OC)[C@@H]3OC([C@H](C(C)C)N)=O GEJDGVNQKABXKG-IRIUNPIQSA-N 0.000 description 1
- MMQDVRCFNJLGCW-UHFFFAOYSA-N Cc(cc1)ccc1N=[O]=CO Chemical compound Cc(cc1)ccc1N=[O]=CO MMQDVRCFNJLGCW-UHFFFAOYSA-N 0.000 description 1
- BXGKAGLZHGYAMW-TZYFFPFWSA-N [(2R,3R,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-yl] (2S)-2-amino-3-methylbutanoate 4-methylbenzenesulfonic acid Chemical compound Cc1ccc(cc1)S(O)(=O)=O.Cc1ccc(cc1)S(O)(=O)=O.COc1cc2CCN3C[C@@H](CC(C)C)[C@@H](C[C@@H]3c2cc1OC)OC(=O)[C@@H](N)C(C)C BXGKAGLZHGYAMW-TZYFFPFWSA-N 0.000 description 1
- 230000000155 isotopic effect Effects 0.000 description 1
- 239000012453 solvate Substances 0.000 description 1
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022114755A JP2022141821A (ja) | 2015-10-30 | 2022-07-19 | バルベナジン塩およびその多形体 |
| JP2024095055A JP2024107365A (ja) | 2015-10-30 | 2024-06-12 | バルベナジン塩およびその多形体 |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562249074P | 2015-10-30 | 2015-10-30 | |
| US62/249,074 | 2015-10-30 | ||
| PCT/US2016/059306 WO2017075340A1 (en) | 2015-10-30 | 2016-10-28 | Valbenazine salts and polymorphs thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022114755A Division JP2022141821A (ja) | 2015-10-30 | 2022-07-19 | バルベナジン塩およびその多形体 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018531963A JP2018531963A (ja) | 2018-11-01 |
| JP2018531963A5 true JP2018531963A5 (enExample) | 2019-12-05 |
| JP7109360B2 JP7109360B2 (ja) | 2022-07-29 |
Family
ID=57281297
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018521548A Active JP7109360B2 (ja) | 2015-10-30 | 2016-10-28 | バルベナジン塩およびその多形体 |
| JP2022114755A Withdrawn JP2022141821A (ja) | 2015-10-30 | 2022-07-19 | バルベナジン塩およびその多形体 |
| JP2024095055A Pending JP2024107365A (ja) | 2015-10-30 | 2024-06-12 | バルベナジン塩およびその多形体 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022114755A Withdrawn JP2022141821A (ja) | 2015-10-30 | 2022-07-19 | バルベナジン塩およびその多形体 |
| JP2024095055A Pending JP2024107365A (ja) | 2015-10-30 | 2024-06-12 | バルベナジン塩およびその多形体 |
Country Status (31)
| Country | Link |
|---|---|
| US (4) | US10065952B2 (enExample) |
| EP (3) | EP3368534B1 (enExample) |
| JP (3) | JP7109360B2 (enExample) |
| KR (2) | KR102736973B1 (enExample) |
| CN (3) | CN115322188A (enExample) |
| AU (1) | AU2016343633B2 (enExample) |
| CA (1) | CA3002074A1 (enExample) |
| CL (1) | CL2018001089A1 (enExample) |
| CO (1) | CO2018004589A2 (enExample) |
| CY (1) | CY1124002T1 (enExample) |
| DK (2) | DK3368534T3 (enExample) |
| EA (1) | EA201890852A1 (enExample) |
| ES (2) | ES2972600T3 (enExample) |
| FI (1) | FI3875459T3 (enExample) |
| HR (2) | HRP20210469T1 (enExample) |
| HU (2) | HUE053872T2 (enExample) |
| IL (2) | IL284874B2 (enExample) |
| LT (2) | LT3875459T (enExample) |
| MA (2) | MA56137B1 (enExample) |
| MX (1) | MX381258B (enExample) |
| MY (2) | MY209348A (enExample) |
| PH (1) | PH12018500900A1 (enExample) |
| PL (2) | PL3875459T3 (enExample) |
| PT (2) | PT3875459T (enExample) |
| RS (2) | RS65154B1 (enExample) |
| SA (1) | SA518391477B1 (enExample) |
| SG (1) | SG11201803408PA (enExample) |
| SI (2) | SI3368534T1 (enExample) |
| SM (1) | SMT202400177T1 (enExample) |
| TN (1) | TN2018000121A1 (enExample) |
| WO (1) | WO2017075340A1 (enExample) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3875459T (lt) | 2015-10-30 | 2024-02-26 | Neurocrine Biosciences, Inc. | Valbenazino dihidrochlorido druskos ir jų polimorfai |
| CA3009169A1 (en) * | 2015-12-23 | 2017-06-29 | Neurocrine Biosciences, Inc. | Synthetic methods for preparation of (s)-(2r,3r,11br)-3-isobutyl-9,10-dimethoxy-2,3,4,6,7,11b-hexahydro-1h-pyrido[2,1-a]isoquinolin-2-yl 2-amino-3-methylbutanoate di(4-methylbenzenesulfonate) |
| RU2019110048A (ru) | 2016-10-06 | 2020-11-06 | Ассиа Кемикал Индастрис Лтд. | Твердые формы валбеназина |
| JP2020500875A (ja) * | 2016-12-02 | 2020-01-16 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | 統合失調症または統合失調感情障害を処置するためのバルベナジンの使用 |
| US10703750B2 (en) | 2017-01-10 | 2020-07-07 | Sandoz Ag | Crystalline valbenazine free base |
| JP7090151B2 (ja) | 2017-01-27 | 2022-06-23 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | 特定のｖｍａｔ２インヒビターを投与するための方法 |
| US10954235B2 (en) * | 2017-02-27 | 2021-03-23 | Sandoz Ag | Crystalline forms of valbenazine salts |
| WO2018200605A1 (en) * | 2017-04-26 | 2018-11-01 | Neurocrine Biosciences, Inc. | Use of valbenazine for treating levodopa-induced dyskinesia |
| MA50175B1 (fr) | 2017-09-21 | 2025-05-30 | Neurocrine Biosciences, Inc. | Formulation de valbenazine à dosage élevé et compositions, procédés et kits associés |
| AU2017435893B2 (en) * | 2017-10-10 | 2023-06-29 | Neurocrine Biosciences, Inc | Methods for the administration of certain VMAT2 inhibitors |
| KR20250070134A (ko) | 2017-10-10 | 2025-05-20 | 뉴로크린 바이오사이언시즈 인코퍼레이티드 | 특정 vmat2 억제제의 투여 방법 |
| KR102776189B1 (ko) * | 2017-11-22 | 2025-03-04 | 아시아 케미컬 인더스트리스 리미티드 | 발베나진의 고상 형태 |
| CA3086611C (en) * | 2017-12-26 | 2023-07-25 | Crystal Pharmaceutical (Suzhou) Co., Ltd. | A crystalline form of valbenazine ditosylate, processes for preparation thereof and use thereof |
| CN110818705A (zh) * | 2018-08-14 | 2020-02-21 | 苏州鹏旭医药科技有限公司 | 缬苯那嗪的盐型和相应晶型与其制备方法 |
| SG11202100303QA (en) | 2018-08-15 | 2021-02-25 | Neurocrine Biosciences Inc | Methods for the administration of certain vmat2 inhibitors |
| CA3065236A1 (en) | 2018-12-27 | 2020-06-27 | Apotex Inc. | Novel crystalline form of valbenazine dibesylate |
| WO2020213014A1 (en) | 2019-04-19 | 2020-10-22 | Mylan Laboratories Limited | An improved process for the preparation of valbenazine and its salts |
| US10689380B1 (en) * | 2019-07-30 | 2020-06-23 | Farmhispania S.A. | Crystalline forms of valbenazine ditosylate |
| US10940141B1 (en) | 2019-08-23 | 2021-03-09 | Neurocrine Biosciences, Inc. | Methods for the administration of certain VMAT2 inhibitors |
| CN114423755A (zh) | 2019-09-13 | 2022-04-29 | 纽罗克里生物科学有限公司 | 用于合成缬苯那嗪的方法 |
| SMT202500315T1 (it) * | 2020-09-09 | 2025-11-10 | Crinetics Pharmaceuticals Inc | Formulazioni di un modulatore della somatostatina |
| CN112569465B (zh) * | 2020-12-29 | 2022-07-19 | 华东理工大学 | 一种微针贴片的制备方法 |
| HRP20250868T1 (hr) * | 2021-03-22 | 2025-09-26 | Neurocrine Biosciences, Inc. | Vmat2 inhibitori i postupci za uporabu |
| IL307826A (en) | 2021-04-26 | 2023-12-01 | Neurocrine Biosciences Inc | Processes for the synthesis of valbanazine |
| EP4362942A1 (en) * | 2021-06-30 | 2024-05-08 | Neurocrine Biosciences, Inc. | Valbenazine for use in the treatment of dyskinesia due to cerebral palsy |
| JP2024524324A (ja) | 2021-06-30 | 2024-07-05 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | 統合失調症のアドオン処置において使用するためのバルベナジン |
| US20250064990A1 (en) | 2021-08-20 | 2025-02-27 | Neurocrine Biosciences, Inc. | Methods of screening for vmat2 inhibitors |
| EP4422603A1 (en) * | 2021-10-29 | 2024-09-04 | Neurocrine Biosciences, Inc. | Valbenazine compositions |
| WO2025038959A1 (en) | 2023-08-17 | 2025-02-20 | Neurocrine Biosciences, Inc. | Methods for the administration of certain vmat2 inhibitors |
| TW202521119A (zh) | 2023-08-17 | 2025-06-01 | 美商紐羅克里生物科學有限公司 | 用於投與特定vmat2抑制劑之方法 |
| WO2025096823A1 (en) | 2023-11-01 | 2025-05-08 | Neurocrine Biosciences, Inc. | Improvement, maintenance or reduction of decline of motor function associated with huntington disease using valbenazine |
| WO2025188830A1 (en) * | 2024-03-06 | 2025-09-12 | Neurocrine Biosciences, Inc. | Methods for the administration of certain vmat2 inhibitors |
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