JP2017510602A5 - - Google Patents
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- Publication number
- JP2017510602A5 JP2017510602A5 JP2016561629A JP2016561629A JP2017510602A5 JP 2017510602 A5 JP2017510602 A5 JP 2017510602A5 JP 2016561629 A JP2016561629 A JP 2016561629A JP 2016561629 A JP2016561629 A JP 2016561629A JP 2017510602 A5 JP2017510602 A5 JP 2017510602A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- siponimod
- weight
- form according
- agent
- 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
Links
- 239000002552 dosage form Substances 0.000 claims description 38
- KIHYPELVXPAIDH-HNSNBQBZSA-N 1-[[4-[(e)-n-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-c-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid Chemical compound CCC1=CC(C(\C)=N\OCC=2C=C(C(C3CCCCC3)=CC=2)C(F)(F)F)=CC=C1CN1CC(C(O)=O)C1 KIHYPELVXPAIDH-HNSNBQBZSA-N 0.000 claims description 21
- 229950005693 siponimod Drugs 0.000 claims description 21
- 239000003795 chemical substances by application Substances 0.000 claims description 19
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 18
- 239000000314 lubricant Substances 0.000 claims description 10
- 239000002274 desiccant Substances 0.000 claims description 8
- 238000002156 mixing Methods 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 239000011230 binding agent Substances 0.000 claims description 6
- 150000001875 compounds Chemical class 0.000 claims description 6
- 239000007884 disintegrant Substances 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 5
- KBPLFHHGFOOTCA-UHFFFAOYSA-N caprylic alcohol Natural products CCCCCCCCO KBPLFHHGFOOTCA-UHFFFAOYSA-N 0.000 claims description 4
- OKMWKBLSFKFYGZ-UHFFFAOYSA-N 1-behenoylglycerol Chemical compound CCCCCCCCCCCCCCCCCCCCCC(=O)OCC(O)CO OKMWKBLSFKFYGZ-UHFFFAOYSA-N 0.000 claims description 2
- 239000004359 castor oil Substances 0.000 claims description 2
- 235000019438 castor oil Nutrition 0.000 claims description 2
- 239000012458 free base Substances 0.000 claims description 2
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 2
- 229940049654 glyceryl behenate Drugs 0.000 claims description 2
- FETSQPAGYOVAQU-UHFFFAOYSA-N glyceryl palmitostearate Chemical compound OCC(O)CO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O FETSQPAGYOVAQU-UHFFFAOYSA-N 0.000 claims description 2
- 229940046813 glyceryl palmitostearate Drugs 0.000 claims description 2
- 239000008172 hydrogenated vegetable oil Substances 0.000 claims description 2
- 238000000338 in vitro Methods 0.000 claims description 2
- TVMXDCGIABBOFY-UHFFFAOYSA-N n-Octanol Natural products CCCCCCCC TVMXDCGIABBOFY-UHFFFAOYSA-N 0.000 claims description 2
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 2
- 239000006186 oral dosage form Substances 0.000 claims description 2
- 239000002245 particle Substances 0.000 claims description 2
- 238000005192 partition Methods 0.000 claims description 2
- 239000007787 solid Substances 0.000 claims description 2
- 229940114926 stearate Drugs 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000007888 film coating Substances 0.000 claims 2
- 238000009501 film coating Methods 0.000 claims 2
- 239000011248 coating agent Substances 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 230000004888 barrier function Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461977806P | 2014-04-10 | 2014-04-10 | |
| US61/977,806 | 2014-04-10 | ||
| PCT/IB2015/052552 WO2015155711A1 (en) | 2014-04-10 | 2015-04-08 | Immunosuppressant formulation |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020009871A Division JP2020097591A (ja) | 2014-04-10 | 2020-01-24 | 免疫抑制製剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017510602A JP2017510602A (ja) | 2017-04-13 |
| JP2017510602A5 true JP2017510602A5 (enExample) | 2018-05-17 |
| JP6679495B2 JP6679495B2 (ja) | 2020-04-15 |
Family
ID=53525213
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016561629A Active JP6679495B2 (ja) | 2014-04-10 | 2015-04-08 | 免疫抑制製剤 |
| JP2020009871A Withdrawn JP2020097591A (ja) | 2014-04-10 | 2020-01-24 | 免疫抑制製剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020009871A Withdrawn JP2020097591A (ja) | 2014-04-10 | 2020-01-24 | 免疫抑制製剤 |
Country Status (23)
| Country | Link |
|---|---|
| US (5) | US20170027906A1 (enExample) |
| EP (1) | EP3129006B1 (enExample) |
| JP (2) | JP6679495B2 (enExample) |
| KR (1) | KR102466348B1 (enExample) |
| CN (1) | CN106163502B (enExample) |
| AR (1) | AR100002A1 (enExample) |
| AU (1) | AU2015246038C1 (enExample) |
| CA (1) | CA2942236C (enExample) |
| CL (1) | CL2016002560A1 (enExample) |
| DK (1) | DK3129006T3 (enExample) |
| EA (1) | EA201692043A1 (enExample) |
| ES (1) | ES2865451T3 (enExample) |
| HU (1) | HUE054245T2 (enExample) |
| IL (1) | IL247599B (enExample) |
| MX (1) | MX2016013236A (enExample) |
| PE (1) | PE20161385A1 (enExample) |
| PH (1) | PH12016501841A1 (enExample) |
| PL (1) | PL3129006T3 (enExample) |
| PT (1) | PT3129006T (enExample) |
| SG (1) | SG11201607354PA (enExample) |
| SI (1) | SI3129006T1 (enExample) |
| TW (1) | TW201622707A (enExample) |
| WO (1) | WO2015155711A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6111202B2 (ja) | 2011-01-07 | 2017-04-05 | ノバルティス アーゲー | 免疫抑制製剤 |
| EP3129006B1 (en) * | 2014-04-10 | 2021-01-27 | Novartis AG | Immunosuppressant formulation |
| US11629124B2 (en) | 2017-03-09 | 2023-04-18 | Novartis Ag | Solid forms comprising an oxime ether compound, compositions and methods of use thereof |
| US11434200B2 (en) | 2017-03-09 | 2022-09-06 | Novartis Ag | Solid forms comprising an oxime ether compound and a coformer, compositions and methods of use thereof |
| KR20200059221A (ko) | 2017-09-27 | 2020-05-28 | 노파르티스 아게 | 시포니모드를 포함하는 비경구 제형 |
| CA3074416A1 (en) | 2017-09-29 | 2019-04-04 | Novartis Ag | Dosing regimen of siponimod |
| MX2020007268A (es) | 2017-09-29 | 2020-08-17 | Novartis Ag | Regimen de dosificacion de siponimod. |
| WO2019144094A1 (en) * | 2018-01-22 | 2019-07-25 | Teva Pharmaceuticals International Gmbh | Crystalline siponimod fumaric acid and polymorphs thereof |
| CN109908095A (zh) * | 2019-04-08 | 2019-06-21 | 肇庆学院 | 一种西尼莫德片剂及制备方法 |
| WO2021214717A1 (en) | 2020-04-23 | 2021-10-28 | Novartis Ag | Dosing regimen for the use of siponimod for the treatment of acute respiratory distress syndrome |
| CN113633632A (zh) * | 2021-09-09 | 2021-11-12 | 暨南大学附属第一医院（广州华侨医院） | siponimod在制备抗肿瘤转移药物中的应用 |
| WO2024126409A1 (en) | 2022-12-12 | 2024-06-20 | Synthon B.V. | Pharmaceutical composition of siponimod |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT2465492E (pt) * | 2007-10-12 | 2015-10-15 | Novartis Ag | Composições que compreendem moduladores de receptores de esfingosina-1-fosfato (s1p) |
| WO2010008045A1 (ja) | 2008-07-16 | 2010-01-21 | 日本電気株式会社 | Ｉｕ－ＵＰプロトコルのネゴシエーション結果情報の通知方法、プロトコル変換方法、通信ネットワークシステム、インターワーキング装置、ＩｕＵＰネゴシエーション結果情報取得装置及びコンピュータ読み取り可能な情報記録媒体 |
| RS53041B (sr) | 2008-12-18 | 2014-04-30 | Novartis Ag | Hemifumaratna so 1-[4-[1-(4-cikloheksil-3-trifluorometil-benziloksiimino)-etil]-2-etil-benzil]-azetidin-3-karboksilne kiseline |
| AU2009327405A1 (en) | 2008-12-18 | 2011-06-30 | Novartis Ag | New polymorphic form of 1- (4- { l- [ (E) -4-cyclohexyl--3-trifluoromethyl-benzyloxyimino] -ethyl) -2-ethyl-benzy l) -azetidine-3-carboxylic |
| WO2010072703A1 (en) * | 2008-12-22 | 2010-07-01 | Novartis Ag | Dosage regimen of an s1p receptor agonist |
| CN101480374A (zh) * | 2009-01-20 | 2009-07-15 | 苏州中化药品工业有限公司 | 一种稳定的固体药物组合物 |
| JP6111202B2 (ja) * | 2011-01-07 | 2017-04-05 | ノバルティス アーゲー | 免疫抑制製剤 |
| WO2012095853A1 (en) * | 2011-01-10 | 2012-07-19 | Novartis Pharma Ag | Modified release formulations comprising sip receptor modulators |
| EP3129006B1 (en) * | 2014-04-10 | 2021-01-27 | Novartis AG | Immunosuppressant formulation |
-
2015
- 2015-04-08 EP EP15735733.6A patent/EP3129006B1/en active Active
- 2015-04-08 KR KR1020167027528A patent/KR102466348B1/ko active Active
- 2015-04-08 WO PCT/IB2015/052552 patent/WO2015155711A1/en not_active Ceased
- 2015-04-08 MX MX2016013236A patent/MX2016013236A/es unknown
- 2015-04-08 SG SG11201607354PA patent/SG11201607354PA/en unknown
- 2015-04-08 DK DK15735733.6T patent/DK3129006T3/da active
- 2015-04-08 EA EA201692043A patent/EA201692043A1/ru unknown
- 2015-04-08 AU AU2015246038A patent/AU2015246038C1/en active Active
- 2015-04-08 PE PE2016001740A patent/PE20161385A1/es not_active Application Discontinuation
- 2015-04-08 ES ES15735733T patent/ES2865451T3/es active Active
- 2015-04-08 SI SI201531566T patent/SI3129006T1/sl unknown
- 2015-04-08 HU HUE15735733A patent/HUE054245T2/hu unknown
- 2015-04-08 CA CA2942236A patent/CA2942236C/en active Active
- 2015-04-08 JP JP2016561629A patent/JP6679495B2/ja active Active
- 2015-04-08 CN CN201580018811.7A patent/CN106163502B/zh active Active
- 2015-04-08 PT PT157357336T patent/PT3129006T/pt unknown
- 2015-04-08 US US15/300,968 patent/US20170027906A1/en not_active Abandoned
- 2015-04-08 PL PL15735733T patent/PL3129006T3/pl unknown
- 2015-04-09 TW TW104111464A patent/TW201622707A/zh unknown
- 2015-04-10 AR ARP150101084A patent/AR100002A1/es unknown
-
2016
- 2016-09-01 IL IL247599A patent/IL247599B/en active IP Right Grant
- 2016-09-20 PH PH12016501841A patent/PH12016501841A1/en unknown
- 2016-10-07 CL CL2016002560A patent/CL2016002560A1/es unknown
-
2018
- 2018-03-20 US US15/926,699 patent/US20180207128A1/en not_active Abandoned
-
2019
- 2019-03-21 US US16/360,696 patent/US20190328705A1/en not_active Abandoned
-
2020
- 2020-01-24 JP JP2020009871A patent/JP2020097591A/ja not_active Withdrawn
-
2021
- 2021-02-04 US US17/167,635 patent/US20210161860A1/en not_active Abandoned
-
2024
- 2024-03-14 US US18/605,259 patent/US20250073203A1/en active Pending
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