HRP20240012T1 - Derivati 1-((2-(2,2,2-trifluoroetoksi)piridin-4-il)metil)uree kao kcnq potencijatori - Google Patents
Derivati 1-((2-(2,2,2-trifluoroetoksi)piridin-4-il)metil)uree kao kcnq potencijatori Download PDFInfo
- Publication number
- HRP20240012T1 HRP20240012T1 HRP20240012TT HRP20240012T HRP20240012T1 HR P20240012 T1 HRP20240012 T1 HR P20240012T1 HR P20240012T T HRP20240012T T HR P20240012TT HR P20240012 T HRP20240012 T HR P20240012T HR P20240012 T1 HRP20240012 T1 HR P20240012T1
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- Croatia
- Prior art keywords
- pharmaceutically acceptable
- acceptable salt
- compound according
- image
- compound
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Links
- VDRSSRINXUQZRZ-UHFFFAOYSA-N [2-(2,2,2-trifluoroethoxy)pyridin-4-yl]methylurea Chemical class FC(COC1=NC=CC(=C1)CNC(=O)N)(F)F VDRSSRINXUQZRZ-UHFFFAOYSA-N 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 17
- 150000003839 salts Chemical class 0.000 claims 16
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 6
- 239000000825 pharmaceutical preparation Substances 0.000 claims 4
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 230000003287 optical effect Effects 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 230000000750 progressive effect Effects 0.000 claims 2
- 206010001497 Agitation Diseases 0.000 claims 1
- 206010006542 Bulbar palsy Diseases 0.000 claims 1
- 206010028289 Muscle atrophy Diseases 0.000 claims 1
- 208000029578 Muscle disease Diseases 0.000 claims 1
- 208000021642 Muscular disease Diseases 0.000 claims 1
- 208000032319 Primary lateral sclerosis Diseases 0.000 claims 1
- 206010046298 Upper motor neurone lesion Diseases 0.000 claims 1
- 206010015037 epilepsy Diseases 0.000 claims 1
- 201000010901 lateral sclerosis Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 208000005264 motor neuron disease Diseases 0.000 claims 1
- 230000020763 muscle atrophy Effects 0.000 claims 1
- 201000000585 muscular atrophy Diseases 0.000 claims 1
- 210000000578 peripheral nerve Anatomy 0.000 claims 1
- 201000002241 progressive bulbar palsy Diseases 0.000 claims 1
- 201000000196 pseudobulbar palsy Diseases 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/38—Radicals substituted by singly-bound nitrogen atoms having only hydrogen or hydrocarbon radicals attached to the substituent nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D213/62—Oxygen or sulfur atoms
- C07D213/63—One oxygen atom
- C07D213/64—One oxygen atom attached in position 2 or 6
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4412—Non condensed pyridines; Hydrogenated derivatives thereof having oxo groups directly attached to the heterocyclic ring
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
-
- 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
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Pyridine Compounds (AREA)
Claims (15)
1. Spoj formule:
[image]
pri čemu R1 je
[image]
ili
[image]
i pri čemu R2 je H ili OH,
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema patentnom zahtjevu 1, naznačen time što R1 je:
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema patentnom zahtjevu 2, naznačen time što je R2 jednako OH, ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema patentnom zahtjevu 3 formule:
[image]
pri čemu spoj sadrži jedan enantiomer koji ima (+) optičku rotaciju kada se mjeri na 20°C i 589 nm u koncentraciji od 0.20 g/100 mL u metanolu, ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema patentnom zahtjevu 3 formule:
[image]
pri čemu spoj sadrži jedan enantiomer koji ima (-) optičku rotaciju kada se mjeri na 20°C i 589 nm u koncentraciji od 0.20 g/100 mL u metanolu, ili njegova farmaceutski prihvatljiva sol.
6. Spoj prema patentnom zahtjevu 1, naznačen time što R1 je
[image]
ili njegova farmaceutski prihvatljiva sol.
7. Spoj prema patentnom zahtjevu 6, naznačen time što R2 je H, ili njegova farmaceutski prihvatljiva sol.
8. Spoj prema patentnom zahtjevu 6, naznačen time što R2 je OH, ili njegova farmaceutski prihvatljiva sol.
9. Spoj prema patentnom zahtjevu 8 formule:
[image]
ili njegova farmaceutski prihvatljiva sol; ili
formule:
[image]
ili njegova farmaceutski prihvatljiva sol.
10. Spoj prema patentnom zahtjevu 1 formule:
[image]
ili njegova farmaceutski prihvatljiva sol.
11. Farmaceutski pripravak koji sadrži spoj prema bilo kojem od patentnih zahtjeva 1-10, ili njegovu farmaceutski prihvatljivu sol, sa jednim ili više farmaceutski prihvatljivih nosača, razblaživača ili ekscipijenasa.
12. Spoj prema bilo kojem od patentnih zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol, za uporabu u terapiji.
13. Spoj prema bilo kojem od patentnih zahtjeva 1-10, ili njegova farmaceutski prihvatljiva sol, ili farmaceutski pripravak prema patentnom zahtjevu 11, za uporabu u liječenju bolesti izabrane iz grupe koja se sastoji od ALS, primarne lateralne skleroze, pseudobulbarne paralize, progresivne bulbarne paralize, epilepsije, progresivne mišićne atrofije i poremećaja hiper ekscitabilnosti perifernih živaca.
14. Spoj, ili njegova farmaceutski prihvatljiva sol, za uporabu prema patentnom zahtjevu 13, ili farmaceutski pripravak za uporabu prema patentnom zahtjevu 13, naznačen time što bolest je ALS.
15. Postupak za pripremu farmaceutskog pripravka, koji sadrži miješanje spojeva prema bilo kojem od patentnih zahtjeva 1-10, ili njegove farmaceutski prihvatljive soli, sa jednim ili više farmaceutski prihvatljivih nosača, razblaživača ili ekscipijenata.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962801716P | 2019-02-06 | 2019-02-06 | |
| US201962811038P | 2019-02-27 | 2019-02-27 | |
| EP20709409.5A EP3921030B1 (en) | 2019-02-06 | 2020-02-04 | 1-((2-(2,2,2-trifluoroethoxy)pyridin-4-yl)methyl)urea derivatives as kcnq potentiators |
| PCT/US2020/016499 WO2020163268A1 (en) | 2019-02-06 | 2020-02-04 | 1-((2-(2,2,2-trifluoroethoxy)pyridin-4-yl)methyl)urea derivatives as kcnq potentiators |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| HRP20240012T1 true HRP20240012T1 (hr) | 2024-03-29 |
Family
ID=69743945
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HRP20240012TT HRP20240012T1 (hr) | 2019-02-06 | 2020-02-04 | Derivati 1-((2-(2,2,2-trifluoroetoksi)piridin-4-il)metil)uree kao kcnq potencijatori |
Country Status (22)
| Country | Link |
|---|---|
| US (3) | US11208383B2 (hr) |
| EP (1) | EP3921030B1 (hr) |
| JP (2) | JP7451543B2 (hr) |
| KR (1) | KR20210126040A (hr) |
| CN (1) | CN113692304A (hr) |
| AU (1) | AU2020218180A1 (hr) |
| BR (1) | BR112021015544A2 (hr) |
| CA (1) | CA3128975A1 (hr) |
| DK (1) | DK3921030T3 (hr) |
| ES (1) | ES2968807T3 (hr) |
| FI (1) | FI3921030T3 (hr) |
| HR (1) | HRP20240012T1 (hr) |
| HU (1) | HUE064734T2 (hr) |
| IL (1) | IL285113A (hr) |
| LT (1) | LT3921030T (hr) |
| MX (1) | MX2021009396A (hr) |
| PL (1) | PL3921030T3 (hr) |
| PT (1) | PT3921030T (hr) |
| RS (1) | RS65040B1 (hr) |
| SG (1) | SG11202108599SA (hr) |
| SI (1) | SI3921030T1 (hr) |
| WO (1) | WO2020163268A1 (hr) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| LT3921030T (lt) * | 2019-02-06 | 2024-01-25 | Eli Lilly And Company | 1-((2-(2,2,2-trifluoroetoksi)piridin-4-il)metil)karbamido dariniai, kaip kcnq stiprikliai |
| AR122739A1 (es) | 2020-06-25 | 2022-10-05 | Idorsia Pharmaceuticals Ltd | Derivados de ciclobutil-urea |
| TW202330471A (zh) * | 2021-09-30 | 2023-08-01 | 日商住友製藥股份有限公司 | 環丙醯胺衍生物 |
| AU2022390453A1 (en) | 2021-11-19 | 2024-05-30 | F. Hoffmann-La Roche Ag | Novel heteroaryl-urea compounds as kv7.2 inhibitors |
| WO2023091461A1 (en) | 2021-11-19 | 2023-05-25 | Icagen, Llc | Pyridine compounds as kv7.2 enhancers |
| WO2023121992A1 (en) | 2021-12-22 | 2023-06-29 | Icagen, Llc | Cyclopropyl compounds |
| WO2023158584A1 (en) | 2022-02-15 | 2023-08-24 | Icagen, Llc | New bicyclopentane derivatives |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2005100349A2 (en) | 2004-04-13 | 2005-10-27 | Icagen, Inc. | Polycyclic pyridines as potassium ion channel modulators |
| WO2010036316A1 (en) | 2008-09-24 | 2010-04-01 | Yangbo Feng | Urea and carbamate compounds and analogs as kinase inhibitors |
| AR090151A1 (es) | 2012-03-07 | 2014-10-22 | Lilly Co Eli | Compuestos inhibidores de raf |
| CN103709097A (zh) | 2012-09-28 | 2014-04-09 | 中国科学院上海药物研究所 | 1,3-取代脲或硫脲化合物、其制备方法、药物组合物和应用 |
| WO2014145028A2 (en) | 2013-03-15 | 2014-09-18 | Deciphera Pharmaceuticals, Llc | N-acyl-n'-(pyridin-2-yl) ureas and analogs exhibiting anti-cancer and anti-proliferative activities |
| JP6577479B2 (ja) | 2014-02-27 | 2019-09-18 | メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツングＭｅｒｃｋ Ｐａｔｅｎｔ Ｇｅｓｅｌｌｓｃｈａｆｔ ｍｉｔ ｂｅｓｃｈｒａｅｎｋｔｅｒ Ｈａｆｔｕｎｇ | Ｎａｖ チャンネル阻害剤としてのヘテロ環化合物及びその使用 |
| EP3210969B1 (en) | 2014-10-24 | 2021-04-28 | ONO Pharmaceutical Co., Ltd. | Kcnq2-5 channel activator |
| ES2866324T3 (es) | 2016-04-22 | 2021-10-19 | Ono Pharmaceutical Co | Derivados de 1-(1-hidroxi-2,3-dihidro-1H-inden5-il)-urea y compuestos similares como activadores del canal KCNQ2-5 para el tratamiento de la disuria |
| LT3921030T (lt) * | 2019-02-06 | 2024-01-25 | Eli Lilly And Company | 1-((2-(2,2,2-trifluoroetoksi)piridin-4-il)metil)karbamido dariniai, kaip kcnq stiprikliai |
-
2020
- 2020-02-04 LT LTEPPCT/US2020/016499T patent/LT3921030T/lt unknown
- 2020-02-04 EP EP20709409.5A patent/EP3921030B1/en active Active
- 2020-02-04 SI SI202030316T patent/SI3921030T1/sl unknown
- 2020-02-04 WO PCT/US2020/016499 patent/WO2020163268A1/en active Application Filing
- 2020-02-04 HU HUE20709409A patent/HUE064734T2/hu unknown
- 2020-02-04 PL PL20709409.5T patent/PL3921030T3/pl unknown
- 2020-02-04 US US16/781,148 patent/US11208383B2/en active Active
- 2020-02-04 CA CA3128975A patent/CA3128975A1/en active Pending
- 2020-02-04 HR HRP20240012TT patent/HRP20240012T1/hr unknown
- 2020-02-04 MX MX2021009396A patent/MX2021009396A/es unknown
- 2020-02-04 AU AU2020218180A patent/AU2020218180A1/en active Pending
- 2020-02-04 RS RS20240009A patent/RS65040B1/sr unknown
- 2020-02-04 ES ES20709409T patent/ES2968807T3/es active Active
- 2020-02-04 CN CN202080012797.0A patent/CN113692304A/zh active Pending
- 2020-02-04 KR KR1020217028040A patent/KR20210126040A/ko unknown
- 2020-02-04 BR BR112021015544-9A patent/BR112021015544A2/pt unknown
- 2020-02-04 DK DK20709409.5T patent/DK3921030T3/da active
- 2020-02-04 FI FIEP20709409.5T patent/FI3921030T3/fi active
- 2020-02-04 JP JP2021546360A patent/JP7451543B2/ja active Active
- 2020-02-04 SG SG11202108599SA patent/SG11202108599SA/en unknown
- 2020-02-04 PT PT207094095T patent/PT3921030T/pt unknown
-
2021
- 2021-07-25 IL IL285113A patent/IL285113A/en unknown
- 2021-11-19 US US17/531,000 patent/US11840516B2/en active Active
-
2023
- 2023-11-09 US US18/388,299 patent/US20240076269A1/en active Pending
-
2024
- 2024-03-06 JP JP2024033668A patent/JP2024063191A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20220073464A1 (en) | 2022-03-10 |
| PT3921030T (pt) | 2024-01-12 |
| JP7451543B2 (ja) | 2024-03-18 |
| DK3921030T3 (da) | 2024-01-02 |
| HUE064734T2 (hu) | 2024-04-28 |
| US11840516B2 (en) | 2023-12-12 |
| RS65040B1 (sr) | 2024-02-29 |
| LT3921030T (lt) | 2024-01-25 |
| WO2020163268A1 (en) | 2020-08-13 |
| MX2021009396A (es) | 2021-09-10 |
| PL3921030T3 (pl) | 2024-05-06 |
| BR112021015544A2 (pt) | 2021-10-26 |
| SI3921030T1 (sl) | 2024-03-29 |
| FI3921030T3 (fi) | 2024-01-08 |
| EP3921030B1 (en) | 2023-10-11 |
| EP3921030A1 (en) | 2021-12-15 |
| SG11202108599SA (en) | 2021-09-29 |
| AU2020218180A1 (en) | 2021-08-19 |
| US11208383B2 (en) | 2021-12-28 |
| KR20210126040A (ko) | 2021-10-19 |
| CA3128975A1 (en) | 2020-08-13 |
| ES2968807T3 (es) | 2024-05-14 |
| JP2022519744A (ja) | 2022-03-24 |
| US20200247752A1 (en) | 2020-08-06 |
| IL285113A (en) | 2021-09-30 |
| CN113692304A (zh) | 2021-11-23 |
| US20240076269A1 (en) | 2024-03-07 |
| JP2024063191A (ja) | 2024-05-10 |
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