JP2020172531A5 - - Google Patents
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- JP2020172531A5 JP2020172531A5 JP2020116157A JP2020116157A JP2020172531A5 JP 2020172531 A5 JP2020172531 A5 JP 2020172531A5 JP 2020116157 A JP2020116157 A JP 2020116157A JP 2020116157 A JP2020116157 A JP 2020116157A JP 2020172531 A5 JP2020172531 A5 JP 2020172531A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- pharmaceutical preparation
- polymorph
- hcl
- preparation 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.)
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- 150000001875 compounds Chemical class 0.000 claims 9
- 239000000825 pharmaceutical preparation Substances 0.000 claims 7
- VEXZGXHMUGYJMC-UHFFFAOYSA-N HCl Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 3
- 229910000041 hydrogen chloride Inorganic materials 0.000 claims 3
- 239000000945 filler Substances 0.000 claims 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims 2
- 229960003943 hypromellose Drugs 0.000 claims 2
- 239000000314 lubricant Substances 0.000 claims 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical group [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000037242 Cmax Effects 0.000 claims 1
- GUBGYTABKSRVRQ-UUNJERMWSA-N Lactose Natural products O([C@@H]1[C@H](O)[C@H](O)[C@H](O)O[C@@H]1CO)[C@H]1[C@@H](O)[C@@H](O)[C@H](O)[C@H](CO)O1 GUBGYTABKSRVRQ-UUNJERMWSA-N 0.000 claims 1
- 230000035888 Maximum plasma concentration Effects 0.000 claims 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims 1
- 239000004359 castor oil Substances 0.000 claims 1
- 235000019438 castor oil Nutrition 0.000 claims 1
- 239000008119 colloidal silica Substances 0.000 claims 1
- 239000008101 lactose Substances 0.000 claims 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N 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 1
- 235000019359 magnesium stearate Nutrition 0.000 claims 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims 1
- 239000008108 microcrystalline cellulose Substances 0.000 claims 1
- 229940016286 microcrystalline cellulose Drugs 0.000 claims 1
- 230000001105 regulatory Effects 0.000 claims 1
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims 1
- 229940045902 sodium stearyl fumarate Drugs 0.000 claims 1
- STFSJTPVIIDAQX-LTRPLHCISA-M sodium;(E)-4-octadecoxy-4-oxobut-2-enoate Chemical compound [Na+].CCCCCCCCCCCCCCCCCCOC(=O)\C=C\C([O-])=O STFSJTPVIIDAQX-LTRPLHCISA-M 0.000 claims 1
Claims (8)
- 化合物(I)：
を含む医薬製剤であって、約1-40mgの用量でヒトに投与される場合に、50ng/mL未満の化合物（Ｉ）の最大血漿濃度(Cmax)を提供し、放出調節剤としてヒプロメロースを、化合物（Ｉ）：ヒプロメロース＝1：１．４〜1：６．７５の割合で含有する、放出調節型の医薬製剤。
- 化合物（Ｉ）が、化合物（Ｉ）・ＨＣｌ・２Ｈ２Ｏの多形体(A)として存在する、請求項１に記載の医薬製剤。
- 約16mg、32mg、または40mgの化合物（Ｉ）または化合物（Ｉ）・ＨＣｌ・２Ｈ２Ｏの多形体(A)を含む、請求項１に記載の医薬製剤。
- 充填剤、流動促進剤、および滑沢剤をさらに含む、請求項１〜３のいずれかに記載の医薬製剤。
- 充填剤が、微結晶セルロース、ラクトース、またはそれらの組み合わせである、請求項４に記載の医薬製剤。
- 流動促進剤が、無水コロイダルシリカである、請求項４に記載の医薬製剤。
- 滑沢剤が、ステアリン酸マグネシウム、硬化ヒマシ油〔Kolliwax HCO（登録商標）〕、ステアリルフマル酸ナトリウム、またはそれらの組み合わせである、請求項４に記載の医薬製剤。
- 化合物（Ｉ）または化合物（Ｉ）・ＨＣｌ・２Ｈ２Ｏの多形体(A)の投与用量の実質的にすべてが、16-24時間にわたって医薬製剤から放出される、請求項１〜７のいずれかに記載の医薬製剤。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022076280A JP2022105159A (ja) | 2014-12-02 | 2022-05-02 | 統合失調症を治療するための２－（（１－（２（４－フルオロフェニル）－２－オキソエチル）ピペリジン－４－イル）メチル）イソインドリン－１－オン |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462086691P | 2014-12-02 | 2014-12-02 | |
| US62/086,691 | 2014-12-02 | ||
| US201562248071P | 2015-10-29 | 2015-10-29 | |
| US62/248,071 | 2015-10-29 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017529388A Division JP2018501217A (ja) | 2014-12-02 | 2015-11-30 | 統合失調症を治療するための２−（（１−（２（４−フルオロフェニル）−２−オキソエチル）ピペリジン−４−イル）メチル）イソインドリン−１−オン |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022076280A Division JP2022105159A (ja) | 2014-12-02 | 2022-05-02 | 統合失調症を治療するための２－（（１－（２（４－フルオロフェニル）－２－オキソエチル）ピペリジン－４－イル）メチル）イソインドリン－１－オン |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020172531A JP2020172531A (ja) | 2020-10-22 |
| JP2020172531A5 true JP2020172531A5 (ja) | 2021-04-01 |
| JP7069253B2 JP7069253B2 (ja) | 2022-05-17 |
Family
ID=54848909
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017529388A Pending JP2018501217A (ja) | 2014-12-02 | 2015-11-30 | 統合失調症を治療するための２−（（１−（２（４−フルオロフェニル）−２−オキソエチル）ピペリジン−４−イル）メチル）イソインドリン−１−オン |
| JP2020116157A Active JP7069253B2 (ja) | 2014-12-02 | 2020-07-06 | 統合失調症を治療するための２－（（１－（２（４－フルオロフェニル）－２－オキソエチル）ピペリジン－４－イル）メチル）イソインドリン－１－オン |
| JP2022076280A Pending JP2022105159A (ja) | 2014-12-02 | 2022-05-02 | 統合失調症を治療するための２－（（１－（２（４－フルオロフェニル）－２－オキソエチル）ピペリジン－４－イル）メチル）イソインドリン－１－オン |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017529388A Pending JP2018501217A (ja) | 2014-12-02 | 2015-11-30 | 統合失調症を治療するための２−（（１−（２（４−フルオロフェニル）−２−オキソエチル）ピペリジン−４−イル）メチル）イソインドリン−１−オン |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022076280A Pending JP2022105159A (ja) | 2014-12-02 | 2022-05-02 | 統合失調症を治療するための２－（（１－（２（４－フルオロフェニル）－２－オキソエチル）ピペリジン－４－イル）メチル）イソインドリン－１－オン |
Country Status (26)
| Country | Link |
|---|---|
| US (6) | US9458130B2 (ja) |
| EP (2) | EP3227273B1 (ja) |
| JP (3) | JP2018501217A (ja) |
| KR (1) | KR102620681B1 (ja) |
| CN (2) | CN111110677A (ja) |
| AU (4) | AU2015355226B2 (ja) |
| BR (1) | BR112017011555B1 (ja) |
| CA (1) | CA2968977A1 (ja) |
| CL (2) | CL2017001376A1 (ja) |
| CO (1) | CO2017005498A2 (ja) |
| DK (1) | DK3227273T3 (ja) |
| EA (1) | EA201791226A1 (ja) |
| ES (1) | ES2910528T3 (ja) |
| HU (1) | HUE058212T2 (ja) |
| IL (3) | IL280052B2 (ja) |
| MX (1) | MX2017007065A (ja) |
| MY (1) | MY185516A (ja) |
| PE (1) | PE20171646A1 (ja) |
| PH (1) | PH12017501007A1 (ja) |
| PL (1) | PL3227273T3 (ja) |
| PT (1) | PT3227273T (ja) |
| SG (1) | SG11201704332YA (ja) |
| TW (1) | TWI694069B (ja) |
| UA (1) | UA122780C2 (ja) |
| WO (1) | WO2016089766A1 (ja) |
| ZA (1) | ZA201703481B (ja) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016089766A1 (en) * | 2014-12-02 | 2016-06-09 | Minerva Neurosciences, Inc. | Compositions comprising 2-((1-(2(4-fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one for treating schizophrenia |
| JP2019516756A (ja) * | 2016-05-25 | 2019-06-20 | 田辺三菱製薬株式会社 | 非統合失調症患者の陰性症状を治療するための方法および組成物 |
| UA127349C2 (uk) | 2017-06-21 | 2023-07-26 | Мінерва Ньюросаєнсиз, Інк. | Кишковорозчинна лікарська форма для перорального застосування з контрольованим вивільненням |
| CN107721988A (zh) * | 2017-10-31 | 2018-02-23 | 无锡福祈制药有限公司 | 具有抗炎活性的异吲哚‑1‑酮类化合物 |
| CA3108882A1 (en) | 2018-08-21 | 2020-02-27 | Minerva Neurosciences, Inc. | Use of roluperidone to treat negative symptoms and disorders, increase neuroplasticity, and promote neuroprotection |
| WO2020264486A1 (en) | 2019-06-28 | 2020-12-30 | Teva Czech Industries S.R.O | Solid state forms of roluperidone and salts thereof |
| IL298323B2 (en) | 2020-05-20 | 2023-10-01 | Univ Illinois | A method for treating lysosomal storage disease using histatin peptides |
| WO2023154927A1 (en) | 2022-02-14 | 2023-08-17 | Minerva Neurosciences, Inc. | Use of roluperidone in preventing relapse in schizophrenia patients |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4522811A (en) | 1982-07-08 | 1985-06-11 | Syntex (U.S.A.) Inc. | Serial injection of muramyldipeptides and liposomes enhances the anti-infective activity of muramyldipeptides |
| ATE102482T1 (de) | 1988-01-21 | 1994-03-15 | Merrell Dow Pharma | Verwendung von 1,4-disubstituierten-piperidinyl- verbindungen zur herstellung eines arzneimittels zur behandlung von schlaflosigkeit. |
| CA2069318A1 (en) | 1989-10-27 | 1991-04-28 | Engelbert Ciganek | (n-phthalimidoalkyl) piperidines |
| FR2797643B1 (fr) | 1999-08-17 | 2003-06-06 | Rhodia Chimie Sa | Utilisation composes terpeniques polyoxypropylenes/ polyoxyethylenes comme agent de degraissage de surfaces dures |
| KR100815772B1 (ko) * | 2000-02-29 | 2008-03-20 | 미쯔비시 웰 파마 가부시키가이샤 | 신규 고리상 아미드 유도체 |
| CA2439097C (en) * | 2001-03-26 | 2010-10-12 | Novartis Ag | Pharmaceutical compositions |
| JP5281395B2 (ja) | 2005-06-06 | 2013-09-04 | メルク シャープ エンド ドーム リミテッド | 統合失調症の治療用のｇｌｙｔ１阻害剤としてのシクロヘキサンスルホニル誘導体 |
| CA2569776A1 (en) * | 2006-02-17 | 2007-08-17 | Kos Life Sciences, Inc. | Low flush niacin formulation |
| GB2462611A (en) * | 2008-08-12 | 2010-02-17 | Cambridge Lab | Pharmaceutical composition comprising tetrabenazine |
| US8937900B2 (en) * | 2010-07-20 | 2015-01-20 | Qualcomm Incorporated | Enhancing pilot channel transmission in TD-SCDMA multicarrier systems using secondary carrier frequencies |
| ES2914120T3 (es) * | 2010-07-20 | 2022-06-07 | Minerva Neurosciences Inc | Procedimientos de uso de derivados de amida cíclicos para tratar trastornos mediados por el receptor sigma |
| EP2595484B1 (en) * | 2010-07-20 | 2017-10-18 | Minerva Neurosciences, Inc. | Use of cyclic amide derivatives to treat sleep disorders |
| EP2468264A1 (en) | 2010-12-27 | 2012-06-27 | Laboratorios Liconsa, S.A. | Oral pharmaceutical tablet for controled release of mesalazine and process for obtaining it |
| US9737531B2 (en) * | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| US20140010883A1 (en) * | 2011-03-17 | 2014-01-09 | Lupin Limited | Controlled release pharmaceutical compositions of selective serotonin reuptake inhibitor |
| WO2015191554A1 (en) * | 2014-06-09 | 2015-12-17 | Intra-Cellular Therapies, Inc. | Compounds and methods of use to treat schizophrenia |
| WO2016089766A1 (en) * | 2014-12-02 | 2016-06-09 | Minerva Neurosciences, Inc. | Compositions comprising 2-((1-(2(4-fluorophenyl)-2-oxoethyl)piperidin-4-yl)methyl)isoindolin-1-one for treating schizophrenia |
| JP2019516756A (ja) | 2016-05-25 | 2019-06-20 | 田辺三菱製薬株式会社 | 非統合失調症患者の陰性症状を治療するための方法および組成物 |
| UA127349C2 (uk) | 2017-06-21 | 2023-07-26 | Мінерва Ньюросаєнсиз, Інк. | Кишковорозчинна лікарська форма для перорального застосування з контрольованим вивільненням |
| CA3108882A1 (en) | 2018-08-21 | 2020-02-27 | Minerva Neurosciences, Inc. | Use of roluperidone to treat negative symptoms and disorders, increase neuroplasticity, and promote neuroprotection |
-
2015
- 2015-11-30 WO PCT/US2015/062985 patent/WO2016089766A1/en active Application Filing
- 2015-11-30 KR KR1020177018088A patent/KR102620681B1/ko active IP Right Grant
- 2015-11-30 BR BR112017011555-7A patent/BR112017011555B1/pt active IP Right Grant
- 2015-11-30 US US14/954,264 patent/US9458130B2/en active Active
- 2015-11-30 JP JP2017529388A patent/JP2018501217A/ja active Pending
- 2015-11-30 MX MX2017007065A patent/MX2017007065A/es unknown
- 2015-11-30 CN CN202010012498.9A patent/CN111110677A/zh active Pending
- 2015-11-30 EP EP15808314.7A patent/EP3227273B1/en active Active
- 2015-11-30 MY MYPI2017701998A patent/MY185516A/en unknown
- 2015-11-30 CN CN201580065471.3A patent/CN107567444A/zh active Pending
- 2015-11-30 EA EA201791226A patent/EA201791226A1/ru unknown
- 2015-11-30 SG SG11201704332YA patent/SG11201704332YA/en unknown
- 2015-11-30 PE PE2017000948A patent/PE20171646A1/es unknown
- 2015-11-30 PT PT158083147T patent/PT3227273T/pt unknown
- 2015-11-30 TW TW104139904A patent/TWI694069B/zh active
- 2015-11-30 IL IL280052A patent/IL280052B2/en unknown
- 2015-11-30 CA CA2968977A patent/CA2968977A1/en active Pending
- 2015-11-30 DK DK15808314.7T patent/DK3227273T3/da active
- 2015-11-30 ES ES15808314T patent/ES2910528T3/es active Active
- 2015-11-30 PL PL15808314T patent/PL3227273T3/pl unknown
- 2015-11-30 EP EP22155504.8A patent/EP4063357A1/en active Pending
- 2015-11-30 UA UAA201706785A patent/UA122780C2/uk unknown
- 2015-11-30 HU HUE15808314A patent/HUE058212T2/hu unknown
- 2015-11-30 AU AU2015355226A patent/AU2015355226B2/en active Active
-
2016
- 2016-09-28 US US15/278,421 patent/US9730920B2/en active Active
-
2017
- 2017-05-17 IL IL252347A patent/IL252347B/en active IP Right Grant
- 2017-05-19 ZA ZA2017/03481A patent/ZA201703481B/en unknown
- 2017-05-30 CL CL2017001376A patent/CL2017001376A1/es unknown
- 2017-05-31 PH PH12017501007A patent/PH12017501007A1/en unknown
- 2017-05-31 CO CONC2017/0005498A patent/CO2017005498A2/es unknown
- 2017-07-17 US US15/651,065 patent/US10258614B2/en active Active
-
2019
- 2019-03-01 US US16/290,234 patent/US10799493B2/en active Active
-
2020
- 2020-06-26 AU AU2020204286A patent/AU2020204286B2/en active Active
- 2020-07-06 JP JP2020116157A patent/JP7069253B2/ja active Active
- 2020-09-11 US US17/017,816 patent/US20210228561A1/en not_active Abandoned
-
2021
- 2021-01-07 CL CL2021000044A patent/CL2021000044A1/es unknown
- 2021-09-10 AU AU2021229240A patent/AU2021229240B2/en active Active
-
2022
- 2022-05-02 JP JP2022076280A patent/JP2022105159A/ja active Pending
-
2023
- 2023-02-17 US US18/111,072 patent/US20230201184A1/en active Pending
- 2023-03-12 IL IL301320A patent/IL301320B1/en unknown
- 2023-11-01 AU AU2023258386A patent/AU2023258386A1/en active Pending
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