TW202220650A - 5-甲基-1,2,4-噁二唑-3-基化合物之低劑量療法及調配物 - Google Patents
5-甲基-1,2,4-噁二唑-3-基化合物之低劑量療法及調配物 Download PDFInfo
- Publication number
- TW202220650A TW202220650A TW110126729A TW110126729A TW202220650A TW 202220650 A TW202220650 A TW 202220650A TW 110126729 A TW110126729 A TW 110126729A TW 110126729 A TW110126729 A TW 110126729A TW 202220650 A TW202220650 A TW 202220650A
- Authority
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- Taiwan
- Prior art keywords
- compound
- day
- total dose
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- pharmaceutically acceptable
- Prior art date
Links
- 238000009472 formulation Methods 0.000 title description 5
- 239000000203 mixture Substances 0.000 title description 5
- -1 5-methyl-1,2,4-oxadiazol-3-yl compound Chemical class 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 284
- 150000003839 salts Chemical class 0.000 claims abstract description 73
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 22
- 208000015122 neurodegenerative disease Diseases 0.000 claims abstract description 19
- 230000004770 neurodegeneration Effects 0.000 claims abstract description 18
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims abstract description 12
- 238000000034 method Methods 0.000 claims description 52
- 239000008194 pharmaceutical composition Substances 0.000 claims description 42
- 239000002552 dosage form Substances 0.000 claims description 11
- 208000010877 cognitive disease Diseases 0.000 claims description 10
- 239000002775 capsule Substances 0.000 claims description 9
- 208000027061 mild cognitive impairment Diseases 0.000 claims description 9
- 239000003085 diluting agent Substances 0.000 claims description 5
- 239000003937 drug carrier Substances 0.000 claims description 4
- 239000007937 lozenge Substances 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 4
- 239000007897 gelcap Substances 0.000 claims description 2
- 239000006193 liquid solution Substances 0.000 claims description 2
- 239000006194 liquid suspension Substances 0.000 claims description 2
- 208000034799 Tauopathies Diseases 0.000 abstract description 6
- 201000011240 Frontotemporal dementia Diseases 0.000 abstract description 5
- 208000011580 syndromic disease Diseases 0.000 abstract description 2
- 108010045982 hexosaminidase C Proteins 0.000 description 18
- 238000002600 positron emission tomography Methods 0.000 description 18
- 102100030122 Protein O-GlcNAcase Human genes 0.000 description 16
- 210000004556 brain Anatomy 0.000 description 15
- 239000000902 placebo Substances 0.000 description 13
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- 239000003814 drug Substances 0.000 description 11
- 230000036470 plasma concentration Effects 0.000 description 9
- 229940079593 drug Drugs 0.000 description 7
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 6
- 230000001174 ascending effect Effects 0.000 description 5
- 230000000626 neurodegenerative effect Effects 0.000 description 5
- 239000000700 radioactive tracer Substances 0.000 description 5
- DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 description 4
- 239000008280 blood Substances 0.000 description 4
- 210000004369 blood Anatomy 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 4
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 4
- 239000003112 inhibitor Substances 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 229940100688 oral solution Drugs 0.000 description 4
- 238000002360 preparation method Methods 0.000 description 4
- 108090000790 Enzymes Proteins 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 3
- 238000004458 analytical method Methods 0.000 description 3
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 3
- 238000003384 imaging method Methods 0.000 description 3
- 238000001802 infusion Methods 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 239000002287 radioligand Substances 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- 238000011285 therapeutic regimen Methods 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- FRVXHWNHGWUTQO-CABZTGNLSA-N N-[4-fluoro-5-[[(2S,4S)-2-methyl-4-[(5-methyl-1,2,4-oxadiazol-3-yl)methoxy]piperidin-1-yl]methyl]-1,3-thiazol-2-yl]acetamide Chemical compound FC=1N=C(SC=1CN1[C@H](C[C@H](CC1)OCC1=NOC(=N1)C)C)NC(C)=O FRVXHWNHGWUTQO-CABZTGNLSA-N 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 239000012458 free base Substances 0.000 description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 2
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 2
- 229940100691 oral capsule Drugs 0.000 description 2
- 230000035515 penetration Effects 0.000 description 2
- 239000002243 precursor Substances 0.000 description 2
- 230000000750 progressive effect Effects 0.000 description 2
- 239000012217 radiopharmaceutical Substances 0.000 description 2
- 229940121896 radiopharmaceutical Drugs 0.000 description 2
- 230000002799 radiopharmaceutical effect Effects 0.000 description 2
- 235000010378 sodium ascorbate Nutrition 0.000 description 2
- 229960005055 sodium ascorbate Drugs 0.000 description 2
- PPASLZSBLFJQEF-RKJRWTFHSA-M sodium ascorbate Substances [Na+].OC[C@@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RKJRWTFHSA-M 0.000 description 2
- PPASLZSBLFJQEF-RXSVEWSESA-M sodium-L-ascorbate Chemical compound [Na+].OC[C@H](O)[C@H]1OC(=O)C(O)=C1[O-] PPASLZSBLFJQEF-RXSVEWSESA-M 0.000 description 2
- 238000004885 tandem mass spectrometry Methods 0.000 description 2
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 description 2
- 231100000027 toxicology Toxicity 0.000 description 2
- 239000003981 vehicle Substances 0.000 description 2
- 201000004569 Blindness Diseases 0.000 description 1
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 208000019505 Deglutition disease Diseases 0.000 description 1
- 206010012289 Dementia Diseases 0.000 description 1
- 208000031124 Dementia Alzheimer type Diseases 0.000 description 1
- 238000012879 PET imaging Methods 0.000 description 1
- 206010033799 Paralysis Diseases 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 210000004227 basal ganglia Anatomy 0.000 description 1
- 239000007963 capsule composition Substances 0.000 description 1
- 210000001638 cerebellum Anatomy 0.000 description 1
- 210000003710 cerebral cortex Anatomy 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000001747 exhibiting effect Effects 0.000 description 1
- 210000000609 ganglia Anatomy 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
- 229960003943 hypromellose Drugs 0.000 description 1
- 238000011503 in vivo imaging Methods 0.000 description 1
- 239000005414 inactive ingredient Substances 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 238000012933 kinetic analysis Methods 0.000 description 1
- 238000012417 linear regression Methods 0.000 description 1
- 230000007774 longterm Effects 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 230000002285 radioactive effect Effects 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000008227 sterile water for injection Substances 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 230000002123 temporal effect Effects 0.000 description 1
- 210000001103 thalamus Anatomy 0.000 description 1
- 210000002700 urine Anatomy 0.000 description 1
Classifications
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
-
- 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
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Pharmacology & Pharmacy (AREA)
- Neurology (AREA)
- Organic Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063055362P | 2020-07-23 | 2020-07-23 | |
| US63/055,362 | 2020-07-23 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| TW202220650A true TW202220650A (zh) | 2022-06-01 |
Family
ID=77338898
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| TW110126729A TW202220650A (zh) | 2020-07-23 | 2021-07-21 | 5-甲基-1,2,4-噁二唑-3-基化合物之低劑量療法及調配物 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US20230338349A1 (https=) |
| EP (1) | EP4185291B1 (https=) |
| JP (1) | JP2023535034A (https=) |
| KR (1) | KR20230043905A (https=) |
| CN (1) | CN116323604A (https=) |
| AR (1) | AR123031A1 (https=) |
| AU (1) | AU2021312894B2 (https=) |
| BR (1) | BR112023000975A2 (https=) |
| CA (1) | CA3186808A1 (https=) |
| CL (1) | CL2023000194A1 (https=) |
| CO (1) | CO2023000594A2 (https=) |
| DO (1) | DOP2023000009A (https=) |
| EC (1) | ECSP23005057A (https=) |
| ES (1) | ES3039536T3 (https=) |
| IL (1) | IL300023A (https=) |
| JO (1) | JOP20230018A1 (https=) |
| MX (1) | MX2023000993A (https=) |
| PE (1) | PE20231031A1 (https=) |
| PH (1) | PH12023550177A1 (https=) |
| TW (1) | TW202220650A (https=) |
| WO (1) | WO2022020663A1 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA3243602A1 (en) | 2022-02-03 | 2023-08-10 | Eli Lilly And Company | Regional Tau Imaging for the Diagnosis and Treatment of Alzheimer's Disease |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018014331A1 (zh) * | 2016-07-22 | 2018-01-25 | 深圳市大富科技股份有限公司 | Usb金属管件加工设备及其上模板 |
| TWI654978B (zh) * | 2017-01-27 | 2019-04-01 | 美商美國禮來大藥廠 | 5－甲基－1,2,4－二唑－3－基化合物 |
| CA3107788A1 (en) * | 2018-07-31 | 2020-02-06 | Eli Lilly And Company | Combination of anti-tau antibody and oga inhibitor for treatment of diseases characterized by aberrant tau aggregation |
-
2021
- 2021-07-21 TW TW110126729A patent/TW202220650A/zh unknown
- 2021-07-21 AR ARP210102050A patent/AR123031A1/es unknown
- 2021-07-23 ES ES21755253T patent/ES3039536T3/es active Active
- 2021-07-23 PH PH1/2023/550177A patent/PH12023550177A1/en unknown
- 2021-07-23 JP JP2023504346A patent/JP2023535034A/ja active Pending
- 2021-07-23 PE PE2023000107A patent/PE20231031A1/es unknown
- 2021-07-23 BR BR112023000975A patent/BR112023000975A2/pt unknown
- 2021-07-23 CN CN202180063288.5A patent/CN116323604A/zh active Pending
- 2021-07-23 AU AU2021312894A patent/AU2021312894B2/en active Active
- 2021-07-23 CA CA3186808A patent/CA3186808A1/en active Pending
- 2021-07-23 WO PCT/US2021/042877 patent/WO2022020663A1/en not_active Ceased
- 2021-07-23 IL IL300023A patent/IL300023A/en unknown
- 2021-07-23 US US18/005,245 patent/US20230338349A1/en active Pending
- 2021-07-23 KR KR1020237005839A patent/KR20230043905A/ko active Pending
- 2021-07-23 EP EP21755253.8A patent/EP4185291B1/en active Active
- 2021-07-23 MX MX2023000993A patent/MX2023000993A/es unknown
-
2023
- 2023-01-19 CL CL2023000194A patent/CL2023000194A1/es unknown
- 2023-01-19 CO CONC2023/0000594A patent/CO2023000594A2/es unknown
- 2023-01-20 DO DO2023000009A patent/DOP2023000009A/es unknown
- 2023-01-23 JO JOJO/P/2023/0018A patent/JOP20230018A1/ar unknown
- 2023-01-23 EC ECSENADI20235057A patent/ECSP23005057A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP4185291B1 (en) | 2025-07-09 |
| AU2021312894B2 (en) | 2025-09-11 |
| WO2022020663A1 (en) | 2022-01-27 |
| MX2023000993A (es) | 2023-03-01 |
| CO2023000594A2 (es) | 2023-01-26 |
| PE20231031A1 (es) | 2023-07-10 |
| CL2023000194A1 (es) | 2023-07-21 |
| CN116323604A (zh) | 2023-06-23 |
| ECSP23005057A (es) | 2023-02-28 |
| JP2023535034A (ja) | 2023-08-15 |
| EP4185291A1 (en) | 2023-05-31 |
| CA3186808A1 (en) | 2022-01-27 |
| IL300023A (en) | 2023-03-01 |
| AR123031A1 (es) | 2022-10-26 |
| KR20230043905A (ko) | 2023-03-31 |
| EP4185291C0 (en) | 2025-07-09 |
| BR112023000975A2 (pt) | 2023-02-07 |
| DOP2023000009A (es) | 2023-02-15 |
| JOP20230018A1 (ar) | 2023-01-23 |
| PH12023550177A1 (en) | 2024-03-18 |
| US20230338349A1 (en) | 2023-10-26 |
| ES3039536T3 (en) | 2025-10-22 |
| AU2021312894A1 (en) | 2023-02-23 |
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