JP2018530612A5 - - Google Patents
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- Publication number
- JP2018530612A5 JP2018530612A5 JP2018537734A JP2018537734A JP2018530612A5 JP 2018530612 A5 JP2018530612 A5 JP 2018530612A5 JP 2018537734 A JP2018537734 A JP 2018537734A JP 2018537734 A JP2018537734 A JP 2018537734A JP 2018530612 A5 JP2018530612 A5 JP 2018530612A5
- Authority
- JP
- Japan
- Prior art keywords
- deuterium
- enrichment
- deuterated
- drug
- stereoisomer
- 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
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 33
- 229910052805 deuterium Inorganic materials 0.000 claims description 33
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical class OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims description 23
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims description 12
- 230000007812 deficiency Effects 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 6
- 229960003638 dopamine Drugs 0.000 claims description 6
- 208000018737 Parkinson disease Diseases 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims 28
- 229940079593 drug Drugs 0.000 claims 15
- 229940002612 prodrug Drugs 0.000 claims 11
- 239000000651 prodrug Substances 0.000 claims 11
- 150000003839 salts Chemical class 0.000 claims 11
- 239000012453 solvate Substances 0.000 claims 11
- 229910052739 hydrogen Inorganic materials 0.000 claims 10
- 239000001257 hydrogen Substances 0.000 claims 10
- 239000000203 mixture Substances 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 230000004962 physiological condition Effects 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 102100038238 Aromatic-L-amino-acid decarboxylase Human genes 0.000 claims 2
- 101710151768 Aromatic-L-amino-acid decarboxylase Proteins 0.000 claims 2
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 230000003111 delayed effect Effects 0.000 claims 2
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 238000010521 absorption reaction Methods 0.000 claims 1
- BNQDCRGUHNALGH-UHFFFAOYSA-N benserazide Chemical compound OCC(N)C(=O)NNCC1=CC=C(O)C(O)=C1O BNQDCRGUHNALGH-UHFFFAOYSA-N 0.000 claims 1
- 229960000911 benserazide Drugs 0.000 claims 1
- 229960004205 carbidopa Drugs 0.000 claims 1
- 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 1
- 239000003937 drug carrier Substances 0.000 claims 1
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 description 5
- 229960004502 levodopa Drugs 0.000 description 4
- 230000000694 effects Effects 0.000 description 3
- 238000002560 therapeutic procedure Methods 0.000 description 2
- 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 1
- 241000282567 Macaca fascicularis Species 0.000 description 1
- 206010030312 On and off phenomenon Diseases 0.000 description 1
- 230000003629 anti-akinetic effect Effects 0.000 description 1
- 210000004556 brain Anatomy 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 229950001673 opicapone Drugs 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562284800P | 2015-10-09 | 2015-10-09 | |
| US62/284,800 | 2015-10-09 | ||
| PCT/IB2016/056021 WO2017060870A1 (en) | 2015-10-09 | 2016-10-07 | Combination of deuterated levodopa with carbidopa and opicapone for the treatment of parkinson`s disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018530612A JP2018530612A (ja) | 2018-10-18 |
| JP2018530612A5 true JP2018530612A5 (enExample) | 2019-11-14 |
Family
ID=57209653
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018537734A Pending JP2018530612A (ja) | 2015-10-09 | 2016-10-07 | パーキンソン病の治療のための重水素化レボドパとカルビドパおよびオピカポンとの組合せ |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20170165381A1 (enExample) |
| EP (1) | EP3359148A1 (enExample) |
| JP (1) | JP2018530612A (enExample) |
| AR (1) | AR106313A1 (enExample) |
| BR (1) | BR112018007118A2 (enExample) |
| MX (1) | MX383906B (enExample) |
| TW (1) | TW201720443A (enExample) |
| WO (1) | WO2017060870A1 (enExample) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG11202101817UA (en) * | 2018-09-13 | 2021-03-30 | Univ Canberra | Methods of inhibition |
| CN109293484B (zh) * | 2018-10-22 | 2021-09-28 | 南京大学 | 从羧酸以铱配合物为催化剂蓝光照射下制备氘代醛的方法 |
| GB202016425D0 (en) * | 2020-10-16 | 2020-12-02 | Bial Portela & Ca Sa | Treatment regimens for parkinson's disease |
| WO2022158991A1 (en) * | 2021-01-20 | 2022-07-28 | Bial-Portela & Ca., S.A. | Treatment of pain associated with parkinson's disease with opicapone in combination with levodopa |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2830993A (en) | 1958-04-15 | Quinolizine derivatives | ||
| US3045021A (en) | 1959-09-24 | 1962-07-17 | Hoffmann La Roche | Preparation of substituted 2-oxobenzoquinolizines |
| DE10261807A1 (de) | 2002-12-19 | 2004-07-01 | Turicum Drug Development Ag | Deuterierte Catecholaminderivate sowie diese Verbindungen enthaltende Arzneimittel |
| HUE028777T2 (en) | 2006-02-17 | 2017-01-30 | Ratiopharm Gmbh | Deuterated catecholamine derivatives and medicaments containing these compounds |
| EP2604290A3 (en) | 2006-05-02 | 2013-07-10 | The Trustees of The University of Pennsylvania | Radiolabeled dihydrotetrabenazine derivatives and their use as imaging agents |
| EP2081929B1 (en) | 2006-11-08 | 2013-01-09 | Neurocrine Biosciences, Inc. | Substituted 3-isobutyl-9, 10-dimethoxy-1,3,4,6,7,11b-hexahydro-2h-pyrido[2,1-a]isoquinolin-2-ol compounds and methods relating thereto |
| US20140045900A1 (en) | 2011-02-11 | 2014-02-13 | Bial-Portela & Ca, S.A. | Administration regime for nitrocatechols |
| KR20150115807A (ko) * | 2013-02-05 | 2015-10-14 | 임파 악치엔게젤샤프트 | 위치-특이적 비대칭 중수소 풍부 카테콜아민 유도체 및 상기 화합물을 포함하는 약제 |
-
2016
- 2016-10-07 WO PCT/IB2016/056021 patent/WO2017060870A1/en not_active Ceased
- 2016-10-07 EP EP16788231.5A patent/EP3359148A1/en not_active Withdrawn
- 2016-10-07 AR ARP160103097A patent/AR106313A1/es unknown
- 2016-10-07 BR BR112018007118A patent/BR112018007118A2/pt not_active IP Right Cessation
- 2016-10-07 TW TW105132542A patent/TW201720443A/zh unknown
- 2016-10-07 JP JP2018537734A patent/JP2018530612A/ja active Pending
- 2016-10-07 MX MX2018004339A patent/MX383906B/es unknown
-
2017
- 2017-01-09 US US15/401,270 patent/US20170165381A1/en not_active Abandoned
-
2019
- 2019-08-29 US US16/555,915 patent/US20200121812A1/en not_active Abandoned
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