KR20230088753A - 파킨슨병 치료를 위한 오피카폰 및 레보도파 - Google Patents
파킨슨병 치료를 위한 오피카폰 및 레보도파 Download PDFInfo
- Publication number
- KR20230088753A KR20230088753A KR1020237016045A KR20237016045A KR20230088753A KR 20230088753 A KR20230088753 A KR 20230088753A KR 1020237016045 A KR1020237016045 A KR 1020237016045A KR 20237016045 A KR20237016045 A KR 20237016045A KR 20230088753 A KR20230088753 A KR 20230088753A
- Authority
- KR
- South Korea
- Prior art keywords
- levodopa
- opicaphone
- pharmaceutically acceptable
- acceptable derivative
- disease
- 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.)
- Pending
Links
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 title claims abstract description 109
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 title claims abstract description 107
- 229960004502 levodopa Drugs 0.000 title claims abstract description 106
- 208000018737 Parkinson disease Diseases 0.000 title claims abstract description 74
- 238000011282 treatment Methods 0.000 title claims description 59
- 208000024891 symptom Diseases 0.000 claims abstract description 134
- 229940081615 DOPA decarboxylase inhibitor Drugs 0.000 claims description 24
- 239000000534 dopa decarboxylase inhibitor Substances 0.000 claims description 24
- 239000003814 drug Substances 0.000 claims description 16
- 206010030312 On and off phenomenon Diseases 0.000 claims description 10
- 238000000034 method Methods 0.000 claims description 10
- 230000008859 change Effects 0.000 claims description 7
- 238000004519 manufacturing process Methods 0.000 claims description 7
- BNQDCRGUHNALGH-UHFFFAOYSA-N benserazide Chemical compound OCC(N)C(=O)NNCC1=CC=C(O)C(O)=C1O BNQDCRGUHNALGH-UHFFFAOYSA-N 0.000 claims description 4
- 229960000911 benserazide Drugs 0.000 claims description 4
- 229960004205 carbidopa Drugs 0.000 claims description 4
- TZFNLOMSOLWIDK-JTQLQIEISA-N carbidopa (anhydrous) Chemical compound NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 TZFNLOMSOLWIDK-JTQLQIEISA-N 0.000 claims description 4
- 239000000902 placebo Substances 0.000 description 32
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- 208000012661 Dyskinesia Diseases 0.000 description 25
- HVGGGVAREUUJQV-CHHVJCJISA-N (4z)-4-[3-(2,5-dichloro-4,6-dimethyl-1-oxidopyridin-1-ium-3-yl)-2h-1,2,4-oxadiazol-5-ylidene]-2-hydroxy-6-nitrocyclohexa-2,5-dien-1-one Chemical compound CC1=C(Cl)C(C)=[N+]([O-])C(Cl)=C1C(NO1)=N\C1=C\1C=C([N+]([O-])=O)C(=O)C(O)=C/1 HVGGGVAREUUJQV-CHHVJCJISA-N 0.000 description 24
- 229950001673 opicapone Drugs 0.000 description 24
- 238000002560 therapeutic procedure Methods 0.000 description 14
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 description 10
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 description 10
- 230000001684 chronic effect Effects 0.000 description 9
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- 239000003543 catechol methyltransferase inhibitor Substances 0.000 description 5
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- QOSSAOTZNIDXMA-UHFFFAOYSA-N Dicylcohexylcarbodiimide Chemical compound C1CCCCC1N=C=NC1CCCCC1 QOSSAOTZNIDXMA-UHFFFAOYSA-N 0.000 description 3
- 208000014094 Dystonic disease Diseases 0.000 description 3
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- IVTMXOXVAHXCHI-YXLMWLKOSA-N (2s)-2-amino-3-(3,4-dihydroxyphenyl)propanoic acid;(2s)-3-(3,4-dihydroxyphenyl)-2-hydrazinyl-2-methylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1.NN[C@@](C(O)=O)(C)CC1=CC=C(O)C(O)=C1 IVTMXOXVAHXCHI-YXLMWLKOSA-N 0.000 description 2
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- 230000000295 complement effect Effects 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 230000006866 deterioration Effects 0.000 description 2
- JRURYQJSLYLRLN-BJMVGYQFSA-N entacapone Chemical compound CCN(CC)C(=O)C(\C#N)=C\C1=CC(O)=C(O)C([N+]([O-])=O)=C1 JRURYQJSLYLRLN-BJMVGYQFSA-N 0.000 description 2
- 229960003337 entacapone Drugs 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
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- 230000004580 weight loss Effects 0.000 description 2
- PFDUUKDQEHURQC-ZETCQYMHSA-N 3-O-methyldopa Chemical compound COC1=CC(C[C@H](N)C(O)=O)=CC=C1O PFDUUKDQEHURQC-ZETCQYMHSA-N 0.000 description 1
- 206010001540 Akathisia Diseases 0.000 description 1
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- 229940123736 Decarboxylase inhibitor Drugs 0.000 description 1
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- PFDUUKDQEHURQC-UHFFFAOYSA-N L-3-methoxytyrosine Natural products COC1=CC(CC(N)C(O)=O)=CC=C1O PFDUUKDQEHURQC-UHFFFAOYSA-N 0.000 description 1
- 101710096582 L-tyrosine decarboxylase Proteins 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- 208000001089 Multiple system atrophy Diseases 0.000 description 1
- 206010052904 Musculoskeletal stiffness Diseases 0.000 description 1
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- 238000000692 Student's t-test Methods 0.000 description 1
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- 206010068100 Vascular parkinsonism Diseases 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 102000003802 alpha-Synuclein Human genes 0.000 description 1
- 108090000185 alpha-Synuclein Proteins 0.000 description 1
- VMWNQDUVQKEIOC-CYBMUJFWSA-N apomorphine Chemical compound C([C@H]1N(C)CC2)C3=CC=C(O)C(O)=C3C3=C1C2=CC=C3 VMWNQDUVQKEIOC-CYBMUJFWSA-N 0.000 description 1
- 229960004046 apomorphine Drugs 0.000 description 1
- 238000011888 autopsy Methods 0.000 description 1
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- 208000012601 choreatic disease Diseases 0.000 description 1
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- 230000003111 delayed effect Effects 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- MHUWZNTUIIFHAS-CLFAGFIQSA-N dioleoyl phosphatidic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(COP(O)(O)=O)OC(=O)CCCCCCC\C=C/CCCCCCCC MHUWZNTUIIFHAS-CLFAGFIQSA-N 0.000 description 1
- 208000002173 dizziness Diseases 0.000 description 1
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- 230000002497 edematous effect Effects 0.000 description 1
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- 210000002569 neuron Anatomy 0.000 description 1
- 201000003077 normal pressure hydrocephalus Diseases 0.000 description 1
- ASOADIZOVZTJSR-UHFFFAOYSA-N opicapone Chemical compound CC1=C(Cl)C(C)=[N+]([O-])C(Cl)=C1C1=NOC(C=2C=C(C(O)=C(O)C=2)[N+]([O-])=O)=N1 ASOADIZOVZTJSR-UHFFFAOYSA-N 0.000 description 1
- 238000013386 optimize process Methods 0.000 description 1
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- 239000007858 starting material Substances 0.000 description 1
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- 208000019206 urinary tract infection Diseases 0.000 description 1
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Images
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
- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/19—Carboxylic acids, e.g. valproic acid
- A61K31/195—Carboxylic acids, e.g. valproic acid having an amino group
- A61K31/197—Carboxylic acids, e.g. valproic acid having an amino group the amino and the carboxyl groups being attached to the same acyclic carbon chain, e.g. gamma-aminobutyric acid [GABA], beta-alanine, epsilon-aminocaproic acid or pantothenic acid
- A61K31/198—Alpha-amino acids, e.g. alanine or edetic acid [EDTA]
-
- 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
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- 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
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
Landscapes
- 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)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB2016425.7A GB202016425D0 (en) | 2020-10-16 | 2020-10-16 | Treatment regimens for parkinson's disease |
| GB2016425.7 | 2020-10-16 | ||
| PCT/PT2021/050036 WO2022081033A1 (en) | 2020-10-16 | 2021-10-14 | Opicapone and levodopa for the treatment of parkinson's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| KR20230088753A true KR20230088753A (ko) | 2023-06-20 |
Family
ID=73598546
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| KR1020237016045A Pending KR20230088753A (ko) | 2020-10-16 | 2021-10-14 | 파킨슨병 치료를 위한 오피카폰 및 레보도파 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20230398105A1 (https=) |
| EP (1) | EP4228618A1 (https=) |
| JP (1) | JP2023546140A (https=) |
| KR (1) | KR20230088753A (https=) |
| CN (1) | CN116490171A (https=) |
| AU (1) | AU2021360114A1 (https=) |
| GB (1) | GB202016425D0 (https=) |
| WO (1) | WO2022081033A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3860603A1 (en) | 2018-10-05 | 2021-08-11 | Neurocrine Biosciences, Inc. | Methods for the administration of comt inhibitors |
| JP2024500754A (ja) * | 2020-12-17 | 2024-01-10 | ビアル－ポルテラ エ コンパニア，ソシエダッド アノニマ | 早期特発性パーキンソン病のための治療レジメン |
| GB202212082D0 (en) * | 2022-08-18 | 2022-10-05 | Bial Portela & Ca Sa | Treatment regimens for parkinson's disease |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20110002462A (ko) | 2008-03-17 | 2011-01-07 | 바이알 - 포르텔라 앤드 씨에이 에스에이 | 5-[3-(2,5-디클로로-4,6-디메틸-1-옥시-피리딘-3-일)-[1,2,4]옥사디아졸-5-일]-3-나이트로벤젠-1,2-디올의 결정형 |
| AU2010231961B2 (en) | 2009-04-01 | 2015-05-21 | Bial - Portela & Ca., S.A. | Pharmaceutical formulations comprising nitrocatechol derivatives and methods of making thereof |
| RU2550133C2 (ru) | 2009-04-01 | 2015-05-10 | БИАЛ-ПОРТЕЛА энд КА., С.А. | Фармацевтические составы, включающие производные нитрокатехола, и способы их получения |
| US20140045900A1 (en) * | 2011-02-11 | 2014-02-13 | Bial-Portela & Ca, S.A. | Administration regime for nitrocatechols |
| WO2013089573A1 (en) | 2011-12-13 | 2013-06-20 | BIAL - PORTELA & Cª., S.A. | Chemical compound useful as intermediate for preparing a catechol-o-methyltransferase inhibitor |
| JP2018500300A (ja) * | 2014-11-28 | 2018-01-11 | ノヴィファーマ，エス．アー． | パーキンソン病を遅延させるための医薬 |
| RU2018110580A (ru) * | 2015-08-27 | 2019-09-30 | Прекстон Терапьютикс Са | Проникающее в мозг производное оксима хромона для терапии леводопа-индуцированной дискинезии |
| MX383906B (es) * | 2015-10-09 | 2025-03-14 | Teva Pharmaceuticals Int Gmbh | Combinación de levodopa deuterado con carbidopa y opicapona para el tratamiento del mal de parkinson |
| JP2020023540A (ja) * | 2019-10-11 | 2020-02-13 | ノヴィファーマ，エス．アー． | パーキンソン病を遅延させるための医薬 |
-
2020
- 2020-10-16 GB GBGB2016425.7A patent/GB202016425D0/en not_active Ceased
-
2021
- 2021-10-14 WO PCT/PT2021/050036 patent/WO2022081033A1/en not_active Ceased
- 2021-10-14 JP JP2023523099A patent/JP2023546140A/ja active Pending
- 2021-10-14 KR KR1020237016045A patent/KR20230088753A/ko active Pending
- 2021-10-14 EP EP21801249.0A patent/EP4228618A1/en active Pending
- 2021-10-14 CN CN202180077619.0A patent/CN116490171A/zh active Pending
- 2021-10-14 AU AU2021360114A patent/AU2021360114A1/en active Pending
- 2021-10-14 US US18/032,034 patent/US20230398105A1/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| GB202016425D0 (en) | 2020-12-02 |
| AU2021360114A9 (en) | 2024-10-17 |
| EP4228618A1 (en) | 2023-08-23 |
| JP2023546140A (ja) | 2023-11-01 |
| AU2021360114A1 (en) | 2023-06-08 |
| WO2022081033A1 (en) | 2022-04-21 |
| US20230398105A1 (en) | 2023-12-14 |
| CN116490171A (zh) | 2023-07-25 |
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