JPWO2020072773A5 - - Google Patents
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- JPWO2020072773A5 JPWO2020072773A5 JP2021518473A JP2021518473A JPWO2020072773A5 JP WO2020072773 A5 JPWO2020072773 A5 JP WO2020072773A5 JP 2021518473 A JP2021518473 A JP 2021518473A JP 2021518473 A JP2021518473 A JP 2021518473A JP WO2020072773 A5 JPWO2020072773 A5 JP WO2020072773A5
- Authority
- JP
- Japan
- Prior art keywords
- dosage form
- oral dosage
- cav3 antagonist
- plasma concentration
- cav3
- 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
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- 239000006186 oral dosage form Substances 0.000 claims description 101
- 101150110214 Cav3 gene Proteins 0.000 claims description 84
- 239000005557 antagonist Substances 0.000 claims description 84
- 230000036470 plasma concentration Effects 0.000 claims description 32
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 25
- 238000013270 controlled release Methods 0.000 claims description 20
- 150000003839 salts Chemical class 0.000 claims description 10
- 241000282412 Homo Species 0.000 claims description 7
- 208000016285 Movement disease Diseases 0.000 claims description 6
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 claims description 3
- 201000006517 essential tremor Diseases 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 230000002618 waking effect Effects 0.000 claims description 2
- 206010015037 epilepsy Diseases 0.000 claims 1
- 239000002775 capsule Substances 0.000 description 18
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- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 description 4
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- 239000004322 Butylated hydroxytoluene Substances 0.000 description 3
- NLZUEZXRPGMBCV-UHFFFAOYSA-N Butylhydroxytoluene Chemical compound CC1=CC(C(C)(C)C)=C(O)C(C(C)(C)C)=C1 NLZUEZXRPGMBCV-UHFFFAOYSA-N 0.000 description 3
- 206010041349 Somnolence Diseases 0.000 description 3
- 206010044565 Tremor Diseases 0.000 description 3
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- 235000010354 butylated hydroxytoluene Nutrition 0.000 description 3
- 229940095259 butylated hydroxytoluene Drugs 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- 201000010000 Agranulocytosis Diseases 0.000 description 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 2
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 2
- 208000001431 Psychomotor Agitation Diseases 0.000 description 2
- 208000032140 Sleepiness Diseases 0.000 description 2
- 102000003691 T-Type Calcium Channels Human genes 0.000 description 2
- 108090000030 T-Type Calcium Channels Proteins 0.000 description 2
- 235000019282 butylated hydroxyanisole Nutrition 0.000 description 2
- 229960000913 crospovidone Drugs 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 210000003743 erythrocyte Anatomy 0.000 description 2
- 229960001021 lactose monohydrate Drugs 0.000 description 2
- 229920003145 methacrylic acid copolymer Polymers 0.000 description 2
- 229940117841 methacrylic acid copolymer Drugs 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 2
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 2
- 206010001540 Akathisia Diseases 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- WVDDGKGOMKODPV-UHFFFAOYSA-N Benzyl alcohol Chemical compound OCC1=CC=CC=C1 WVDDGKGOMKODPV-UHFFFAOYSA-N 0.000 description 1
- 241000252505 Characidae Species 0.000 description 1
- 206010010774 Constipation Diseases 0.000 description 1
- 206010010904 Convulsion Diseases 0.000 description 1
- 206010013911 Dysgeusia Diseases 0.000 description 1
- 229920003143 Eudragit® FS 30 D Polymers 0.000 description 1
- 241001539473 Euphoria Species 0.000 description 1
- 206010015535 Euphoric mood Diseases 0.000 description 1
- 206010018687 Granulocytopenia Diseases 0.000 description 1
- 208000004547 Hallucinations Diseases 0.000 description 1
- 206010019233 Headaches Diseases 0.000 description 1
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- 206010071081 Idiopathic generalised epilepsy Diseases 0.000 description 1
- 206010022998 Irritability Diseases 0.000 description 1
- 206010024264 Lethargy Diseases 0.000 description 1
- 206010028813 Nausea Diseases 0.000 description 1
- 206010037870 Rash morbilliform Diseases 0.000 description 1
- 206010038743 Restlessness Diseases 0.000 description 1
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 1
- 208000009205 Tinnitus Diseases 0.000 description 1
- DOOTYTYQINUNNV-UHFFFAOYSA-N Triethyl citrate Chemical compound CCOC(=O)CC(O)(C(=O)OCC)CC(=O)OCC DOOTYTYQINUNNV-UHFFFAOYSA-N 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 208000028311 absence seizure Diseases 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 229960004543 anhydrous citric acid Drugs 0.000 description 1
- 208000022531 anorexia Diseases 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 229960004217 benzyl alcohol Drugs 0.000 description 1
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 206010061428 decreased appetite Diseases 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 206010013781 dry mouth Diseases 0.000 description 1
- 235000019564 dysgeusia Nutrition 0.000 description 1
- 230000004970 emotional disturbance Effects 0.000 description 1
- 206010016256 fatigue Diseases 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 231100000869 headache Toxicity 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 description 1
- 208000034783 hypoesthesia Diseases 0.000 description 1
- 201000001993 idiopathic generalized epilepsy Diseases 0.000 description 1
- 201000001881 impotence Diseases 0.000 description 1
- 239000004615 ingredient Substances 0.000 description 1
- 206010022437 insomnia Diseases 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 239000007791 liquid phase Substances 0.000 description 1
- 206010027175 memory impairment Diseases 0.000 description 1
- 239000011859 microparticle Substances 0.000 description 1
- 239000002105 nanoparticle Substances 0.000 description 1
- 230000008693 nausea Effects 0.000 description 1
- 206010029864 nystagmus Diseases 0.000 description 1
- 208000035824 paresthesia Diseases 0.000 description 1
- 239000012071 phase Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 208000019116 sleep disease Diseases 0.000 description 1
- 208000022925 sleep disturbance Diseases 0.000 description 1
- 230000037321 sleepiness Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 206010042772 syncope Diseases 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 231100000886 tinnitus Toxicity 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
- 230000008673 vomiting Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024070307A JP2024102139A (ja) | 2018-10-03 | 2024-04-24 | （ｒ）－２－（４－イソプロピルフェニル）－ｎ－（１－（５－（２，２，２－トリフルオロエトキシ）ピリジン－２－イル）エチル）アセトアミドを使用した本態性振戦の処置 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862740755P | 2018-10-03 | 2018-10-03 | |
| US62/740,755 | 2018-10-03 | ||
| US201862780049P | 2018-12-14 | 2018-12-14 | |
| US62/780,049 | 2018-12-14 | ||
| PCT/US2019/054498 WO2020072773A1 (en) | 2018-10-03 | 2019-10-03 | Treating essential tremor using (r)-2-(4-isopropylphenyl)-n-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024070307A Division JP2024102139A (ja) | 2018-10-03 | 2024-04-24 | （ｒ）－２－（４－イソプロピルフェニル）－ｎ－（１－（５－（２，２，２－トリフルオロエトキシ）ピリジン－２－イル）エチル）アセトアミドを使用した本態性振戦の処置 |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022504182A JP2022504182A (ja) | 2022-01-13 |
| JP2022504182A5 JP2022504182A5 (https=) | 2022-10-12 |
| JPWO2020072773A5 true JPWO2020072773A5 (https=) | 2022-10-12 |
| JP7480131B2 JP7480131B2 (ja) | 2024-05-09 |
Family
ID=70055875
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021518473A Active JP7480131B2 (ja) | 2018-10-03 | 2019-10-03 | （ｒ）－２－（４－イソプロピルフェニル）－ｎ－（１－（５－（２，２，２－トリフルオロエトキシ）ピリジン－２－イル）エチル）アセトアミドを使用した本態性振戦の処置 |
| JP2024070307A Pending JP2024102139A (ja) | 2018-10-03 | 2024-04-24 | （ｒ）－２－（４－イソプロピルフェニル）－ｎ－（１－（５－（２，２，２－トリフルオロエトキシ）ピリジン－２－イル）エチル）アセトアミドを使用した本態性振戦の処置 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024070307A Pending JP2024102139A (ja) | 2018-10-03 | 2024-04-24 | （ｒ）－２－（４－イソプロピルフェニル）－ｎ－（１－（５－（２，２，２－トリフルオロエトキシ）ピリジン－２－イル）エチル）アセトアミドを使用した本態性振戦の処置 |
Country Status (12)
| Country | Link |
|---|---|
| US (3) | US12383539B2 (https=) |
| EP (1) | EP3860571A4 (https=) |
| JP (2) | JP7480131B2 (https=) |
| KR (1) | KR102946985B1 (https=) |
| CN (1) | CN113164393A (https=) |
| AU (2) | AU2019355021B2 (https=) |
| BR (1) | BR112021006398A2 (https=) |
| CA (1) | CA3115235A1 (https=) |
| IL (2) | IL300798B2 (https=) |
| MX (2) | MX2021003706A (https=) |
| TW (2) | TWI879741B (https=) |
| WO (1) | WO2020072773A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6957460B2 (ja) | 2015-10-22 | 2021-11-02 | カビオン・インコーポレイテッドＣａｖｉｏｎ， Ｉｎｃ． | アンジェルマン症候群および関連する障害の処置方法 |
| JP7321097B2 (ja) | 2017-04-26 | 2023-08-04 | カビオン・インコーポレイテッド | 記憶および認知を改善する、ならびに記憶および認知障害を処置するための方法 |
| IL300798B2 (en) | 2018-10-03 | 2025-09-01 | Cavion Inc | Treatment of skeletal tremor with (r)–2-(4–isopropylphenyl)–n-(1-(5-(2,2,2–trifluoroethoxy)pyridin-2-yl)ethyl)acetamide |
| CN114340670B (zh) | 2019-07-11 | 2026-02-17 | 普拉克西斯精密药物股份有限公司 | T-型钙通道调节剂的制剂及其使用方法 |
| TWI870475B (zh) * | 2019-10-02 | 2025-01-21 | 美商卡凡恩公司 | 用於治療神經毒性之方法及材料 |
| CN115776894A (zh) * | 2020-04-29 | 2023-03-10 | 普拉西斯精密医药公司 | T型钙通道调节剂的使用方法 |
| BR112023024354A2 (pt) * | 2021-05-24 | 2024-02-06 | Cavion Inc | Método de tratamento de tremor essencial |
| CN121013719A (zh) * | 2023-03-02 | 2025-11-25 | 普拉西斯精密医药公司 | 治疗特发性震颤的方法 |
| WO2024182654A1 (en) * | 2023-03-02 | 2024-09-06 | Praxis Precision Medicines, Inc. | High strength single unit dose formulations and methods of use thereof |
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