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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- 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
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- 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
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- 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
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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
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- 206010068100 Vascular parkinsonism Diseases 0.000 description 1
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- 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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- 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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- 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
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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 |
|---|---|---|---|---|
| WO2020072886A1 (en) | 2018-10-05 | 2020-04-09 | Neurocrine Biosciences, Inc. | Methods for the administration of comt inhibitors |
| EP4262798A1 (en) * | 2020-12-17 | 2023-10-25 | Bial-Portela & CA, S.A. | Treatment regimens for early idiopathic parkinson's disease |
| 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 |
|---|---|---|---|---|
| WO2009116882A1 (en) | 2008-03-17 | 2009-09-24 | Portela & Ca., S.A. | Crystal forms of 5- [3- (2, 5-dichloro-4, 6-dimethyl-1-oxy-pyridine-3-yl) [1,2,3] oxadiazol-5-yl] -3-nit robenzene-1, 2-diol |
| PT2413912T (pt) | 2009-04-01 | 2019-06-11 | Bial Portela & Ca Sa | Formulações farmacêuticas compreendendo derivados de nitrocatecol e métodos para as produzir |
| BRPI1016132B8 (pt) | 2009-04-01 | 2021-05-25 | Bial Portela & Ca Sa | composição, formulação farmacêutica, processo de obtenção de uma formulação farmacêutica estável |
| US20140045900A1 (en) * | 2011-02-11 | 2014-02-13 | Bial-Portela & Ca, S.A. | Administration regime for nitrocatechols |
| JP6456143B2 (ja) | 2011-12-13 | 2019-01-23 | ノヴィファーマ，エス．アー． | カテコール−ｏ−メチル転移酵素阻害剤を調製するための中間体として有用な化学的化合物 |
| RU2017120184A (ru) | 2014-11-28 | 2018-12-28 | БИАЛ - ПОРТЕЛА ЭНД Ка, С.А. | Лекарства для замедления течения болезни паркинсона |
| PT3341380T (pt) * | 2015-08-27 | 2019-12-19 | Prexton Therapeutics Sa | Derivado de oxima de cromona penetrante no cérebro para a terapêutica da discinesia induzida por levodopa |
| 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 CN CN202180077619.0A patent/CN116490171A/zh active Pending
- 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 WO PCT/PT2021/050036 patent/WO2022081033A1/en not_active Ceased
- 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 |
|---|---|
| AU2021360114A1 (en) | 2023-06-08 |
| US20230398105A1 (en) | 2023-12-14 |
| WO2022081033A1 (en) | 2022-04-21 |
| CN116490171A (zh) | 2023-07-25 |
| GB202016425D0 (en) | 2020-12-02 |
| AU2021360114A9 (en) | 2024-10-17 |
| JP2023546140A (ja) | 2023-11-01 |
| EP4228618A1 (en) | 2023-08-23 |
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