JP2016216438A5 - - Google Patents
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- Publication number
- JP2016216438A5 JP2016216438A5 JP2015221719A JP2015221719A JP2016216438A5 JP 2016216438 A5 JP2016216438 A5 JP 2016216438A5 JP 2015221719 A JP2015221719 A JP 2015221719A JP 2015221719 A JP2015221719 A JP 2015221719A JP 2016216438 A5 JP2016216438 A5 JP 2016216438A5
- Authority
- JP
- Japan
- Prior art keywords
- receptor
- formulation
- methyl
- group
- antagonist
- 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
- 238000009472 formulation Methods 0.000 claims 26
- 239000000203 mixture Substances 0.000 claims 26
- 102000005962 receptors Human genes 0.000 claims 18
- 108020003175 receptors Proteins 0.000 claims 18
- 239000000952 serotonin receptor agonist Substances 0.000 claims 13
- 239000003420 antiserotonin agent Substances 0.000 claims 8
- 206010015037 epilepsy Diseases 0.000 claims 7
- 239000005557 antagonist Substances 0.000 claims 6
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 claims 5
- 206010010904 Convulsion Diseases 0.000 claims 5
- 102000014630 G protein-coupled serotonin receptor activity proteins Human genes 0.000 claims 5
- 230000000694 effects Effects 0.000 claims 5
- 239000012634 fragment Substances 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 208000011580 syndromic disease Diseases 0.000 claims 5
- PDWNVVUANMHHOR-UHFFFAOYSA-N 3-bromo-2,5-dimethoxy-N-methylbicyclo[4.2.0]octa-1(6),2,4,7-tetraen-7-amine hydrobromide Chemical compound Br.COC1=CC(Br)=C(OC)C2=C1C(NC)=C2 PDWNVVUANMHHOR-UHFFFAOYSA-N 0.000 claims 4
- 241000004297 Draba Species 0.000 claims 4
- 239000000018 receptor agonist Substances 0.000 claims 4
- 229940044601 receptor agonist Drugs 0.000 claims 4
- BTTOYOKCLDAHHO-HNNXBMFYSA-N (2s)-n,n-dimethyl-5-(1,3,5-trimethylpyrazol-4-yl)-1,2,3,4-tetrahydronaphthalen-2-amine Chemical compound C([C@@H](C1)N(C)C)CC2=C1C=CC=C2C=1C(C)=NN(C)C=1C BTTOYOKCLDAHHO-HNNXBMFYSA-N 0.000 claims 3
- LBVZWEWTNUDWNS-YRNVUSSQSA-N (e)-3-[3-[2-(dimethylamino)ethyl]-1h-indol-5-yl]-n-[(4-methoxyphenyl)methyl]prop-2-enamide Chemical compound C1=CC(OC)=CC=C1CNC(=O)\C=C\C1=CC=C(NC=C2CCN(C)C)C2=C1 LBVZWEWTNUDWNS-YRNVUSSQSA-N 0.000 claims 3
- 239000000969 carrier Substances 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- DBGIVFWFUFKIQN-VIFPVBQESA-N (+)-Fenfluramine Chemical compound CCN[C@@H](C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-VIFPVBQESA-N 0.000 claims 2
- DBGIVFWFUFKIQN-SECBINFHSA-N Levofenfluramine Chemical compound CCN[C@H](C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-SECBINFHSA-N 0.000 claims 2
- 239000000556 agonist Substances 0.000 claims 2
- 229960004597 dexfenfluramine Drugs 0.000 claims 2
- 230000002068 genetic effect Effects 0.000 claims 2
- XTTZERNUQAFMOF-QMMMGPOBSA-N lorcaserin Chemical compound C[C@H]1CNCCC2=CC=C(Cl)C=C12 XTTZERNUQAFMOF-QMMMGPOBSA-N 0.000 claims 2
- DBGIVFWFUFKIQN-UHFFFAOYSA-N (+-)-Fenfluramine Chemical group CCNC(C)CC1=CC=CC(C(F)(F)F)=C1 DBGIVFWFUFKIQN-UHFFFAOYSA-N 0.000 claims 1
- USFUFHFQWXDVMH-UHFFFAOYSA-N 1-(1-methylindol-5-yl)-3-(3-methyl-1,2-thiazol-5-yl)urea Chemical compound S1N=C(C)C=C1NC(=O)NC1=CC=C(N(C)C=C2)C2=C1 USFUFHFQWXDVMH-UHFFFAOYSA-N 0.000 claims 1
- KPXKZZURYAXZQE-UHFFFAOYSA-N 1-[(2-chloro-3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole;hydrochloride Chemical compound Cl.ClC1=C(OC)C(OC)=CC=C1CC1C(NC=2C3=CC(C)=CC=2)=C3CCN1 KPXKZZURYAXZQE-UHFFFAOYSA-N 0.000 claims 1
- BKAZOTIBKRWLQA-UHFFFAOYSA-N 1-[(3,4-dimethoxyphenyl)methyl]-6-methyl-2,3,4,9-tetrahydro-1h-pyrido[3,4-b]indole;hydrochloride Chemical compound Cl.C1=C(OC)C(OC)=CC=C1CC1C(NC=2C3=CC(C)=CC=2)=C3CCN1 BKAZOTIBKRWLQA-UHFFFAOYSA-N 0.000 claims 1
- VGEMBOFBPSNOIO-UHFFFAOYSA-N 1-methyl-n-pyridin-3-yl-6,7-dihydropyrrolo[2,3-f]indole-5-carboxamide;hydrochloride Chemical compound Cl.C1CC=2C=C3N(C)C=CC3=CC=2N1C(=O)NC1=CC=CN=C1 VGEMBOFBPSNOIO-UHFFFAOYSA-N 0.000 claims 1
- MKJPYBJBPRFMHL-UHFFFAOYSA-N 4-(4-fluoronaphthalen-1-yl)-6-propan-2-ylpyrimidin-2-amine;hydrochloride Chemical compound Cl.NC1=NC(C(C)C)=CC(C=2C3=CC=CC=C3C(F)=CC=2)=N1 MKJPYBJBPRFMHL-UHFFFAOYSA-N 0.000 claims 1
- 229940127239 5 Hydroxytryptamine receptor antagonist Drugs 0.000 claims 1
- LMIQERWZRIFWNZ-UHFFFAOYSA-N 5-hydroxyindole Chemical compound OC1=CC=C2NC=CC2=C1 LMIQERWZRIFWNZ-UHFFFAOYSA-N 0.000 claims 1
- MSXFEKRSKBQMGJ-QMMMGPOBSA-N C[C@H]1CNCCC2=C1C(=CC=C2)Cl Chemical compound C[C@H]1CNCCC2=C1C(=CC=C2)Cl MSXFEKRSKBQMGJ-QMMMGPOBSA-N 0.000 claims 1
- HUUPKFUYSQNNLO-FAESNJTISA-N Cl.N([C@H]1CC[C@H](CC1)NC=1N=C(C2=CC=CC=C2N=1)N(C)C)C(=O)C1=CC=C(F)C(F)=C1 Chemical compound Cl.N([C@H]1CC[C@H](CC1)NC=1N=C(C2=CC=CC=C2N=1)N(C)C)C(=O)C1=CC=C(F)C(F)=C1 HUUPKFUYSQNNLO-FAESNJTISA-N 0.000 claims 1
- OJZZJTLBYXHUSJ-UHFFFAOYSA-N SB 200646 Chemical compound C=1C=C2N(C)C=CC2=CC=1NC(=O)NC1=CC=CN=C1 OJZZJTLBYXHUSJ-UHFFFAOYSA-N 0.000 claims 1
- OQZOXHCRSXYSPM-UHFFFAOYSA-N SB 221284 Chemical compound C1=2C=C(C(F)(F)F)C(SC)=CC=2CCN1C(=O)NC1=CC=CN=C1 OQZOXHCRSXYSPM-UHFFFAOYSA-N 0.000 claims 1
- RRJLJKRFFRZRAF-UHFFFAOYSA-N SB 228357 Chemical compound C1=2C=C(C(F)(F)F)C(OC)=CC=2CCN1C(=O)NC(C=1)=CC(F)=CC=1C1=CC=CN=C1 RRJLJKRFFRZRAF-UHFFFAOYSA-N 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960001582 fenfluramine Drugs 0.000 claims 1
- DXUZZRDHJMOLTN-MRYVXRNOSA-N ser-082 Chemical compound OC(=O)\C=C\C(O)=O.C1CC2=CC=CC3=C2N1C[C@H]1CCN(C)C[C@H]13 DXUZZRDHJMOLTN-MRYVXRNOSA-N 0.000 claims 1
Priority Applications (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US15/265,062 US20170071949A1 (en) | 2015-09-14 | 2016-09-14 | Combination treatment of specific forms of epilepsy |
| US15/989,812 US20180325909A1 (en) | 2015-09-14 | 2018-05-25 | Combination treatment of specific forms of epilepsy |
| US17/579,135 US20220193082A1 (en) | 2015-09-14 | 2022-01-19 | Combination treatment of specific forms of epilepsy |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562162544P | 2015-05-15 | 2015-05-15 | |
| US62/162,544 | 2015-05-15 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016216438A JP2016216438A (ja) | 2016-12-22 |
| JP2016216438A5 true JP2016216438A5 (enExample) | 2018-07-26 |
| JP6668045B2 JP6668045B2 (ja) | 2020-03-18 |
Family
ID=57579762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015221719A Expired - Fee Related JP6668045B2 (ja) | 2015-05-15 | 2015-11-12 | ドラベ症候群を処置するための選択的５−ｈｔ受容体アゴニストおよびアンタゴニスト |
Country Status (1)
| Country | Link |
|---|---|
| JP (1) | JP6668045B2 (enExample) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9549909B2 (en) | 2013-05-03 | 2017-01-24 | The Katholieke Universiteit Leuven | Method for the treatment of dravet syndrome |
| JP2019507111A (ja) | 2015-12-22 | 2019-03-14 | ゾゲニクス インターナショナル リミテッド | 代謝抵抗性フェンフルラミン類縁体およびその使用法 |
| KR102688278B1 (ko) | 2015-12-22 | 2024-07-26 | 조게닉스 인터내셔널 리미티드 | 펜플루라민 조성물 및 그 제조 방법 |
| CA3032996C (en) | 2016-08-24 | 2025-05-06 | Zogenix International Ltd | Formulation for inhibiting formation of 5-ht 2b agonists and methods of using same |
| US20190091179A1 (en) * | 2017-09-26 | 2019-03-28 | Zogenix International Limited | Congnitive function with fenfluramine |
| JP2021530541A (ja) * | 2018-07-27 | 2021-11-11 | ゼノン・ファーマシューティカルズ・インコーポレイテッドXenon Pharmaceuticals Inc. | てんかんの治療方法 |
| AU2019384963B2 (en) | 2018-11-19 | 2022-05-26 | Zogenix International Limited | Methods of treating Rett syndrome using fenfluramine |
| WO2020112460A1 (en) * | 2018-11-30 | 2020-06-04 | Zogenix International Limited | A method of treating refractory epilepsy syndromes using fenfluramine enantiomers |
| CN113897399A (zh) * | 2021-08-31 | 2022-01-07 | 浙江赛微思生物科技有限公司 | 一种scn1lab基因敲除斑马鱼癫痫模型及其应用 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009051747A1 (en) * | 2007-10-15 | 2009-04-23 | Concert Pharmaceuticals, Inc. | Deuterated lorcaserin |
| US9549909B2 (en) * | 2013-05-03 | 2017-01-24 | The Katholieke Universiteit Leuven | Method for the treatment of dravet syndrome |
| WO2015066344A1 (en) * | 2013-11-01 | 2015-05-07 | Arena Pharmaceuticals, Inc. | 5-ht2c receptor agonists and compositions and methods of use |
-
2015
- 2015-11-12 JP JP2015221719A patent/JP6668045B2/ja not_active Expired - Fee Related
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