HRP20231447T1 - Postupci za povećanje bioraspoloživosti i izloženosti naponski upravljanog otvarača kalijevih kanala - Google Patents
Postupci za povećanje bioraspoloživosti i izloženosti naponski upravljanog otvarača kalijevih kanala Download PDFInfo
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- HRP20231447T1 HRP20231447T1 HRP20231447TT HRP20231447T HRP20231447T1 HR P20231447 T1 HRP20231447 T1 HR P20231447T1 HR P20231447T T HRP20231447T T HR P20231447TT HR P20231447 T HRP20231447 T HR P20231447T HR P20231447 T1 HRP20231447 T1 HR P20231447T1
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- Prior art keywords
- compound
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- use according
- oral administration
- fasting conditions
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- 238000000034 method Methods 0.000 title claims 4
- 102000003734 Voltage-Gated Potassium Channels Human genes 0.000 title 1
- 108090000013 Voltage-Gated Potassium Channels Proteins 0.000 title 1
- 230000002708 enhancing effect Effects 0.000 title 1
- 239000004036 potassium channel stimulating agent Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 55
- 235000020937 fasting conditions Nutrition 0.000 claims 11
- 102000004257 Potassium Channel Human genes 0.000 claims 3
- 206010015037 epilepsy Diseases 0.000 claims 3
- 108020001213 potassium channel Proteins 0.000 claims 3
- 206010001497 Agitation Diseases 0.000 claims 1
- 229940126062 Compound A Drugs 0.000 claims 1
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 1
- 241000282412 Homo Species 0.000 claims 1
- 108010006746 KCNQ2 Potassium Channel Proteins 0.000 claims 1
- 102000005453 KCNQ2 Potassium Channel Human genes 0.000 claims 1
- 108010038888 KCNQ3 Potassium Channel Proteins 0.000 claims 1
- 102000015686 KCNQ3 Potassium Channel Human genes 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 230000002594 corticospinal effect Effects 0.000 claims 1
- FJNPZKZPWVVSON-UHFFFAOYSA-N n-[4-(6-fluoro-3,4-dihydro-1h-isoquinolin-2-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide Chemical compound CC1=C(NC(=O)CC(C)(C)C)C(C)=CC(N2CC3=CC=C(F)C=C3CC2)=C1 FJNPZKZPWVVSON-UHFFFAOYSA-N 0.000 claims 1
- 230000000284 resting effect Effects 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/08—Antiepileptics; Anticonvulsants
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Pain & Pain Management (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (15)
1. Spoj za upotrebu u postupku liječenja terapijom čovjeka kojem je to potrebno; naznačen time što je spoj N-[4-(6-fluor-3,4-dihidro-lH-izokinolin-2-il)-2,6-dimetilfenil]-3,3-dimetilbutanamid; i pri čemu se spoj daje oralno uz uvjet uzimanja hrane.
2. Spoj za upotrebu prema zahtjevu 1, naznačen time što se spoj oralno primjenjuje navedenom čovjeku između 30 minuta prije konzumiranja hrane do 2 sata nakon konzumiranja hrane.
3. Spoj za upotrebu prema zahtjevu 1 ili zahtjevu 2, naznačen time što postupak povećava jedan ili više od Cmax ili AUCinf spoja u usporedbi kada se ista količina Spoja A oralno daje ljudima u uvjetima natašte.
4. Spoj za upotrebu prema bilo kojem od prethodnih zahtjeva, naznačen time što je spoj za upotrebu u liječenju poremećaja napadaja, poželjno pri čemu je poremećaj napadaja epilepsija s žarišnim početkom.
5. Spoj za upotrebu prema bilo kojem od prethodnih zahtjeva, naznačen time što upotreba poboljšava otvaranje Kv7 kalijevog kanala, poželjno pri čemu je Kv7 kalijev kanal odabran od jednog ili više od Kv7.2, Kv7.3, Kv7.4, i Kv7.5, poželjnije kada je uporaba selektivna za povećanje otvaranja Kv7 kalijevog kanala odabranog od jednog ili više Kv7.2, Kv7.3, Kv7.4, i Kv7.5 prema Kv7.1.
6. Spoj za upotrebu prema zahtjevu 5, naznačen time što upotreba pojačava otvaranje Kv7.2/Kv7.3 kalijevog kanala.
7. Spoj za upotrebu prema bilo kojem od prethodnih zahtjeva, naznačen time što postupak liječenja uključuje davanje čovjeku doze spoja koja je niža od one koja bi bila potrebna za postizanje jednog ili više istih Cmax ili AUCinf spoja kada se oralno daje čovjeku natašte.
8. Spoj za upotrebu prema bilo kojem od zahtjeva 3 do 7 naznačen time što oralna primjena spoja čovjeku povećava Cmax spoja u usporedbi kada se ista količina spoja oralno daje čovjeku u uvjetima natašte, poželjno pri čemu:
(a) omjer Cmax nakon oralne primjene spoja prema Cmax nakon oralne primjene spoja u uvjetima natašte je veći od 1,3, poželjnije veći od 2, još poželjnije veći od 3; ili
(b) oralna primjena spoja čovjeku povećava Cmax spoja za najmanje 50%, poželjnije za najmanje 100%, u usporedbi kada se ista količina spoja oralno daje čovjeku u uvjetima natašte.
9. Spoj za upotrebu prema bilo kojem od zahtjeva 3 do 7, naznačen time što oralna primjena spoja čovjeku povećava Cmax spoja u usporedbi s onom kada se ista količina spoja oralno daje čovjeku u uvjetima natašte i pri čemu je omjer Cmax nakon oralne primjene spoja prema Cmax nakon oralne primjene spoja u uvjetima natašte veći od 1,2, poželjnije veći od 1,3.
10. Spoj za upotrebu prema bilo kojem od zahtjeva 3 do 9, naznačen time što oralna primjena spoja čovjeku povećava AUCinf spoja u usporedbi kada se ista količina spoja oralno daje čovjeku u uvjetima natašte, poželjno pri čemu:
(a) omjer AUCinf nakon oralne primjene spoja prema AUCinf nakon oralne primjene spoja u uvjetima natašte je veći od 1,3, poželjnije veći od 1,5, još poželjnije veći od 1,8; ili
(b) oralna primjena spoja čovjeku povećava AUCinf spoja za najmanje 50%, poželjnije za najmanje 75% u usporedbi kada se ista količina spoja oralno daje čovjeku u uvjetima natašte.
11. Spoj za upotrebu prema bilo kojem od zahtjeva 3 do 9, naznačen time oralna primjena spoja čovjeku povećava AUCinf spoja u usporedbi kada se ista količina spoja oralno daje čovjeku u uvjetima natašte i pri čemu je omjer AUCinf nakon oralne primjene spoja prema AUCinf nakon oralne primjene spoja u uvjetima natašte veći od 1,2, poželjnije veći od 1,3.
12. Spoj za upotrebu prema bilo kojem od prethodnih zahtjeva, naznačen time što je spoj za upotrebu u povećanju motoričkog praga u mirovanju (RMT) ili aktivnog motoričkog praga (AMT) kod čovjeka kojem je to potrebno, poželjno pri čemu je povećanje RMT ili AMT proporcionalno koncentraciji spoja u plazmi.
13. Spoj za upotrebu prema bilo kojem od prethodnih zahtjeva, naznačen time što je spoj za upotrebu u smanjenju kortikospinalne ili kortikalne ekscitabilnosti kod čovjeka kojem je to potrebno.
14. Spoj za upotrebu prema bilo kojem od prethodnih zahtjeva, naznačen time što:
(a) se primjenjuje 2 do 200 mg, poželjno 2 do 100 mg, poželjnije 5 do 50 mg, još poželjnije 10, 20, ili 25 mg, još poželjnije 20 mg spoja;
(b) se primjenjuje 5-500 mg, poželjno 20-150 mg, još poželjnije 100 mg spoja dnevno; ili
(c) 0,1-1,0 mg/kg, poželjno 0,2-0,5 mg/kg spoja.
15. Spoj za upotrebu prema bilo kojem od zahtjeva 1-13, naznačen time što se primjenjuje 0,05-2,0 mg/kg spoja.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862670253P | 2018-05-11 | 2018-05-11 | |
| EP19727216.4A EP3790548B1 (en) | 2018-05-11 | 2019-05-10 | Methods for enhancing the bioavailability and exposure of a voltage-gated potassium channel opener |
| PCT/US2019/031872 WO2019217924A1 (en) | 2018-05-11 | 2019-05-10 | Methods for enhancing the bioavailability and exposure of a voltage-gated potassium channel opener |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20231447T1 true HRP20231447T1 (hr) | 2024-03-01 |
Family
ID=66669101
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20231447TT HRP20231447T1 (hr) | 2018-05-11 | 2019-05-10 | Postupci za povećanje bioraspoloživosti i izloženosti naponski upravljanog otvarača kalijevih kanala |
Country Status (30)
| Country | Link |
|---|---|
| US (4) | US11135214B2 (hr) |
| EP (2) | EP3790548B1 (hr) |
| KR (1) | KR20210020892A (hr) |
| CN (1) | CN112384216A (hr) |
| AU (2) | AU2019265002B2 (hr) |
| BR (1) | BR112020022713A2 (hr) |
| CA (1) | CA3099292A1 (hr) |
| CL (1) | CL2020002932A1 (hr) |
| CO (1) | CO2020015476A2 (hr) |
| CR (1) | CR20200602A (hr) |
| DK (1) | DK3790548T3 (hr) |
| EA (1) | EA202092720A1 (hr) |
| ES (1) | ES2964409T3 (hr) |
| FI (1) | FI3790548T3 (hr) |
| GE (1) | GEP20237527B (hr) |
| HR (1) | HRP20231447T1 (hr) |
| HU (1) | HUE064326T2 (hr) |
| LT (1) | LT3790548T (hr) |
| MA (1) | MA52569B1 (hr) |
| MD (1) | MD3790548T2 (hr) |
| MX (2) | MX2020012008A (hr) |
| PE (1) | PE20211211A1 (hr) |
| PH (1) | PH12020551898A1 (hr) |
| PL (1) | PL3790548T3 (hr) |
| PT (1) | PT3790548T (hr) |
| RS (1) | RS64922B1 (hr) |
| SG (1) | SG11202011102TA (hr) |
| SI (1) | SI3790548T1 (hr) |
| UA (1) | UA127229C2 (hr) |
| WO (1) | WO2019217924A1 (hr) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI3790548T1 (sl) | 2018-05-11 | 2024-02-29 | Xenon Pharmaceuticals Inc. | Postopek za povečanje biološke razpoložljivosti in izpostavljenosti napetostno odvisnih odpiralcev kalijevih kanalačkov |
| TW202128627A (zh) | 2019-10-10 | 2021-08-01 | 加拿大商再諾製藥公司 | 選擇性鉀通道調節劑之固態晶型 |
| TW202133847A (zh) * | 2019-12-06 | 2021-09-16 | 加拿大商再諾製藥公司 | 治療疼痛的方法 |
| AU2022218962A1 (en) * | 2021-02-09 | 2023-09-14 | Xenon Pharmaceuticals Inc. | Conjoint therapy for treating seizure disorders |
| JP2024508660A (ja) * | 2021-02-09 | 2024-02-28 | 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 | 快感消失の治療に使用するための電位依存性カリウムチャネル開口薬 |
| CN113698345B (zh) * | 2021-10-27 | 2022-02-01 | 上海挚盟医药科技有限公司 | 作为钾通道调节剂的化合物及其制备和应用 |
| EP4074696A4 (en) * | 2021-10-27 | 2024-01-31 | Shanghai Zhimeng Biopharma, Inc. | POTASSIUM CHANNEL REGULATOR COMPOUND, PRODUCTION AND USE THEREOF |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8236861B2 (en) | 2004-02-13 | 2012-08-07 | Hormos Medical Corporation | Method for enhancing the bioavailablity of ospemifene |
| NZ563361A (en) | 2005-06-02 | 2011-02-25 | Schering Corp | HCV protease inhibitors in combination with food |
| US20090318507A2 (en) | 2006-05-02 | 2009-12-24 | Chris Rundfeldt | Potassium Channel Activators for the Prevention and Treatment of Dystonia and Dystonia Like Symptoms |
| US8993593B2 (en) * | 2006-08-23 | 2015-03-31 | Valeant Pharmaceuticals International | N-(4-(6-fluoro-3,4-dihydroisoquinolin-2(1H)-yl)-2,6-dimethylphenyl)-3,3-dimethylbutanamide as potassium channel modulators |
| PT2061465E (pt) | 2006-08-23 | 2013-07-15 | Valeant Pharmaceuticals Int | Derivados de 4-(n-azacicloalquil)anilidas como moduladores do canal de potássio |
| US10500216B2 (en) | 2011-11-18 | 2019-12-10 | Corcept Therapeutics, Inc. | Optimizing mifepristone absorption |
| SI3790548T1 (sl) | 2018-05-11 | 2024-02-29 | Xenon Pharmaceuticals Inc. | Postopek za povečanje biološke razpoložljivosti in izpostavljenosti napetostno odvisnih odpiralcev kalijevih kanalačkov |
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2019
- 2019-05-10 SI SI201930665T patent/SI3790548T1/sl unknown
- 2019-05-10 EP EP19727216.4A patent/EP3790548B1/en active Active
- 2019-05-10 PT PT197272164T patent/PT3790548T/pt unknown
- 2019-05-10 SG SG11202011102TA patent/SG11202011102TA/en unknown
- 2019-05-10 EA EA202092720A patent/EA202092720A1/ru unknown
- 2019-05-10 BR BR112020022713-7A patent/BR112020022713A2/pt unknown
- 2019-05-10 EP EP23185386.2A patent/EP4279133A3/en active Pending
- 2019-05-10 PE PE2020001843A patent/PE20211211A1/es unknown
- 2019-05-10 PL PL19727216.4T patent/PL3790548T3/pl unknown
- 2019-05-10 CR CR20200602A patent/CR20200602A/es unknown
- 2019-05-10 AU AU2019265002A patent/AU2019265002B2/en active Active
- 2019-05-10 HR HRP20231447TT patent/HRP20231447T1/hr unknown
- 2019-05-10 CN CN201980046273.0A patent/CN112384216A/zh active Pending
- 2019-05-10 MA MA52569A patent/MA52569B1/fr unknown
- 2019-05-10 UA UAA202007781A patent/UA127229C2/uk unknown
- 2019-05-10 LT LTEPPCT/US2019/031872T patent/LT3790548T/lt unknown
- 2019-05-10 FI FIEP19727216.4T patent/FI3790548T3/fi active
- 2019-05-10 MX MX2020012008A patent/MX2020012008A/es unknown
- 2019-05-10 CA CA3099292A patent/CA3099292A1/en active Pending
- 2019-05-10 HU HUE19727216A patent/HUE064326T2/hu unknown
- 2019-05-10 WO PCT/US2019/031872 patent/WO2019217924A1/en active Application Filing
- 2019-05-10 DK DK19727216.4T patent/DK3790548T3/da active
- 2019-05-10 GE GEAP201915508A patent/GEP20237527B/en unknown
- 2019-05-10 RS RS20231089A patent/RS64922B1/sr unknown
- 2019-05-10 MD MDE20210233T patent/MD3790548T2/ro unknown
- 2019-05-10 KR KR1020207035334A patent/KR20210020892A/ko unknown
- 2019-05-10 ES ES19727216T patent/ES2964409T3/es active Active
- 2019-05-13 US US16/410,851 patent/US11135214B2/en active Active
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2020
- 2020-11-09 PH PH12020551898A patent/PH12020551898A1/en unknown
- 2020-11-10 MX MX2023013247A patent/MX2023013247A/es unknown
- 2020-11-11 CL CL2020002932A patent/CL2020002932A1/es unknown
- 2020-12-11 CO CONC2020/0015476A patent/CO2020015476A2/es unknown
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2021
- 2021-10-01 US US17/449,785 patent/US20220062266A1/en active Pending
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2024
- 2024-04-26 US US18/648,049 patent/US20240316032A1/en active Pending
- 2024-05-30 US US18/679,045 patent/US20240316033A1/en active Pending
- 2024-09-17 AU AU2024219794A patent/AU2024219794A1/en active Pending
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