JP2018507210A5 - - Google Patents
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- JP2018507210A5 JP2018507210A5 JP2017543828A JP2017543828A JP2018507210A5 JP 2018507210 A5 JP2018507210 A5 JP 2018507210A5 JP 2017543828 A JP2017543828 A JP 2017543828A JP 2017543828 A JP2017543828 A JP 2017543828A JP 2018507210 A5 JP2018507210 A5 JP 2018507210A5
- Authority
- JP
- Japan
- Prior art keywords
- deuterium
- compound
- group
- structural formula
- 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
- 150000001875 compounds Chemical class 0.000 claims 39
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 35
- 229910052805 deuterium Inorganic materials 0.000 claims 35
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 6
- -1 R 13 Chemical compound 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 239000001257 hydrogen Substances 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 5
- 208000014094 Dystonic disease Diseases 0.000 claims 4
- 102000010909 Monoamine Oxidase Human genes 0.000 claims 4
- 108010062431 Monoamine oxidase Proteins 0.000 claims 4
- 102000001708 Protein Isoforms Human genes 0.000 claims 4
- 108010029485 Protein Isoforms Proteins 0.000 claims 4
- 230000036470 plasma concentration Effects 0.000 claims 4
- 102100036475 Alanine aminotransferase 1 Human genes 0.000 claims 3
- 108010082126 Alanine transaminase Proteins 0.000 claims 3
- 206010003591 Ataxia Diseases 0.000 claims 3
- 108010081668 Cytochrome P-450 CYP3A Proteins 0.000 claims 3
- 102000018832 Cytochromes Human genes 0.000 claims 3
- 108010052832 Cytochromes Proteins 0.000 claims 3
- 208000012661 Dyskinesia Diseases 0.000 claims 3
- 206010044074 Torticollis Diseases 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000002207 metabolite Substances 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- WEQLWGNDNRARGE-DJIMGWMZSA-N (2R,3R,11bR)-9,10-dimethoxy-3-(2-methylpropyl)-2,3,4,6,7,11b-hexahydro-1H-benzo[a]quinolizin-2-ol Chemical compound C1CN2C[C@@H](CC(C)C)[C@H](O)C[C@@H]2C2=C1C=C(OC)C(OC)=C2 WEQLWGNDNRARGE-DJIMGWMZSA-N 0.000 claims 2
- MKJIEFSOBYUXJB-HOCLYGCPSA-N (3S,11bS)-9,10-dimethoxy-3-isobutyl-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-one Chemical compound C1CN2C[C@H](CC(C)C)C(=O)C[C@H]2C2=C1C=C(OC)C(OC)=C2 MKJIEFSOBYUXJB-HOCLYGCPSA-N 0.000 claims 2
- 102000002260 Alkaline Phosphatase Human genes 0.000 claims 2
- 108020004774 Alkaline Phosphatase Proteins 0.000 claims 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 2
- 108010003415 Aspartate Aminotransferases Proteins 0.000 claims 2
- 102000004625 Aspartate Aminotransferases Human genes 0.000 claims 2
- BPYKTIZUTYGOLE-IFADSCNNSA-N Bilirubin Chemical compound N1C(=O)C(C)=C(C=C)\C1=C\C1=C(C)C(CCC(O)=O)=C(CC2=C(C(C)=C(\C=C/3C(=C(C=C)C(=O)N\3)C)N2)CCC(O)=O)N1 BPYKTIZUTYGOLE-IFADSCNNSA-N 0.000 claims 2
- 108010026925 Cytochrome P-450 CYP2C19 Proteins 0.000 claims 2
- 108010000561 Cytochrome P-450 CYP2C8 Proteins 0.000 claims 2
- 108010000543 Cytochrome P-450 CYP2C9 Proteins 0.000 claims 2
- 108010001237 Cytochrome P-450 CYP2D6 Proteins 0.000 claims 2
- 102100029363 Cytochrome P450 2C19 Human genes 0.000 claims 2
- 102100029359 Cytochrome P450 2C8 Human genes 0.000 claims 2
- 102100029358 Cytochrome P450 2C9 Human genes 0.000 claims 2
- 102100021704 Cytochrome P450 2D6 Human genes 0.000 claims 2
- 102100039205 Cytochrome P450 3A4 Human genes 0.000 claims 2
- 208000023105 Huntington disease Diseases 0.000 claims 2
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 2
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 2
- 102000002704 Leucyl aminopeptidase Human genes 0.000 claims 2
- 108010004098 Leucyl aminopeptidase Proteins 0.000 claims 2
- 208000001089 Multiple system atrophy Diseases 0.000 claims 2
- 208000018737 Parkinson disease Diseases 0.000 claims 2
- 102100033075 Prostacyclin synthase Human genes 0.000 claims 2
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims 2
- 208000010118 dystonia Diseases 0.000 claims 2
- 208000016570 early-onset generalized limb-onset dystonia Diseases 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- 208000018197 inherited torticollis Diseases 0.000 claims 2
- 229960004502 levodopa Drugs 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 201000007601 neurodegeneration with brain iron accumulation Diseases 0.000 claims 2
- 108010064377 prostacyclin synthetase Proteins 0.000 claims 2
- 210000002966 serum Anatomy 0.000 claims 2
- 229960005333 tetrabenazine Drugs 0.000 claims 2
- 108010073030 25-Hydroxyvitamin D3 1-alpha-Hydroxylase Proteins 0.000 claims 1
- 102100036285 25-hydroxyvitamin D-1 alpha hydroxylase, mitochondrial Human genes 0.000 claims 1
- 102000004008 5'-Nucleotidase Human genes 0.000 claims 1
- 102100032645 7-alpha-hydroxycholest-4-en-3-one 12-alpha-hydroxylase Human genes 0.000 claims 1
- 206010000117 Abnormal behaviour Diseases 0.000 claims 1
- 102000014461 Ataxins Human genes 0.000 claims 1
- 108010078286 Ataxins Proteins 0.000 claims 1
- 208000009017 Athetosis Diseases 0.000 claims 1
- 206010003694 Atrophy Diseases 0.000 claims 1
- 101000856500 Bacillus subtilis subsp. natto Glutathione hydrolase proenzyme Proteins 0.000 claims 1
- 208000035183 Benign hereditary chorea Diseases 0.000 claims 1
- 102000004506 Blood Proteins Human genes 0.000 claims 1
- 108010017384 Blood Proteins Proteins 0.000 claims 1
- 206010008025 Cerebellar ataxia Diseases 0.000 claims 1
- 206010008748 Chorea Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 102000012437 Copper-Transporting ATPases Human genes 0.000 claims 1
- 108010074918 Cytochrome P-450 CYP1A1 Proteins 0.000 claims 1
- 108010074922 Cytochrome P-450 CYP1A2 Proteins 0.000 claims 1
- 108010020070 Cytochrome P-450 CYP2B6 Proteins 0.000 claims 1
- 108010001202 Cytochrome P-450 CYP2E1 Proteins 0.000 claims 1
- 102100031476 Cytochrome P450 1A1 Human genes 0.000 claims 1
- 102100026533 Cytochrome P450 1A2 Human genes 0.000 claims 1
- 102100027417 Cytochrome P450 1B1 Human genes 0.000 claims 1
- 102100038742 Cytochrome P450 2A13 Human genes 0.000 claims 1
- 102100036194 Cytochrome P450 2A6 Human genes 0.000 claims 1
- 102100038739 Cytochrome P450 2B6 Human genes 0.000 claims 1
- 102100029368 Cytochrome P450 2C18 Human genes 0.000 claims 1
- 102100024889 Cytochrome P450 2E1 Human genes 0.000 claims 1
- 102100031461 Cytochrome P450 2J2 Human genes 0.000 claims 1
- 102100026515 Cytochrome P450 2S1 Human genes 0.000 claims 1
- 102100039208 Cytochrome P450 3A5 Human genes 0.000 claims 1
- 102100039203 Cytochrome P450 3A7 Human genes 0.000 claims 1
- 102100027567 Cytochrome P450 4A11 Human genes 0.000 claims 1
- 102100027419 Cytochrome P450 4B1 Human genes 0.000 claims 1
- 102100024916 Cytochrome P450 4F11 Human genes 0.000 claims 1
- 102100024918 Cytochrome P450 4F12 Human genes 0.000 claims 1
- 102100024902 Cytochrome P450 4F2 Human genes 0.000 claims 1
- 102100024901 Cytochrome P450 4F3 Human genes 0.000 claims 1
- 102100024899 Cytochrome P450 4F8 Human genes 0.000 claims 1
- 102100022027 Cytochrome P450 4X1 Human genes 0.000 claims 1
- 102100022034 Cytochrome P450 4Z1 Human genes 0.000 claims 1
- 102100038637 Cytochrome P450 7A1 Human genes 0.000 claims 1
- 102100038698 Cytochrome P450 7B1 Human genes 0.000 claims 1
- 108010036233 Cytochrome P450 Family 46 Proteins 0.000 claims 1
- 102000023526 Cytochrome P450 Family 46 Human genes 0.000 claims 1
- 206010012559 Developmental delay Diseases 0.000 claims 1
- 201000010374 Down Syndrome Diseases 0.000 claims 1
- 206010013801 Duchenne Muscular Dystrophy Diseases 0.000 claims 1
- 208000024412 Friedreich ataxia Diseases 0.000 claims 1
- 102000001390 Fructose-Bisphosphate Aldolase Human genes 0.000 claims 1
- 108010068561 Fructose-Bisphosphate Aldolase Proteins 0.000 claims 1
- 108020004206 Gamma-glutamyltransferase Proteins 0.000 claims 1
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims 1
- 208000002972 Hepatolenticular Degeneration Diseases 0.000 claims 1
- 101000725164 Homo sapiens Cytochrome P450 1B1 Proteins 0.000 claims 1
- 101000957389 Homo sapiens Cytochrome P450 2A13 Proteins 0.000 claims 1
- 101000875170 Homo sapiens Cytochrome P450 2A6 Proteins 0.000 claims 1
- 101000919360 Homo sapiens Cytochrome P450 2C18 Proteins 0.000 claims 1
- 101000941723 Homo sapiens Cytochrome P450 2J2 Proteins 0.000 claims 1
- 101000855328 Homo sapiens Cytochrome P450 2S1 Proteins 0.000 claims 1
- 101000745715 Homo sapiens Cytochrome P450 3A7 Proteins 0.000 claims 1
- 101000725111 Homo sapiens Cytochrome P450 4A11 Proteins 0.000 claims 1
- 101000909111 Homo sapiens Cytochrome P450 4F11 Proteins 0.000 claims 1
- 101000909108 Homo sapiens Cytochrome P450 4F12 Proteins 0.000 claims 1
- 101000909122 Homo sapiens Cytochrome P450 4F2 Proteins 0.000 claims 1
- 101000909121 Homo sapiens Cytochrome P450 4F3 Proteins 0.000 claims 1
- 101000909112 Homo sapiens Cytochrome P450 4F8 Proteins 0.000 claims 1
- 101000896935 Homo sapiens Cytochrome P450 4Z1 Proteins 0.000 claims 1
- 101000957672 Homo sapiens Cytochrome P450 7A1 Proteins 0.000 claims 1
- 101000957674 Homo sapiens Cytochrome P450 7B1 Proteins 0.000 claims 1
- 101000875401 Homo sapiens Sterol 26-hydroxylase, mitochondrial Proteins 0.000 claims 1
- 101000653005 Homo sapiens Thromboxane-A synthase Proteins 0.000 claims 1
- 101000855326 Homo sapiens Vitamin D 25-hydroxylase Proteins 0.000 claims 1
- 208000010152 Huntington disease-like 3 Diseases 0.000 claims 1
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 1
- 102100021695 Lanosterol 14-alpha demethylase Human genes 0.000 claims 1
- 101710146773 Lanosterol 14-alpha demethylase Proteins 0.000 claims 1
- 208000008238 Muscle Spasticity Diseases 0.000 claims 1
- 208000002033 Myoclonus Diseases 0.000 claims 1
- 108010045510 NADPH-Ferrihemoprotein Reductase Proteins 0.000 claims 1
- 108090000279 Peptidyltransferases Proteins 0.000 claims 1
- 208000008601 Polycythemia Diseases 0.000 claims 1
- 101710098398 Probable alanine aminotransferase, mitochondrial Proteins 0.000 claims 1
- 102100026372 Putative inactive cytochrome P450 2G1 Human genes 0.000 claims 1
- 208000005793 Restless legs syndrome Diseases 0.000 claims 1
- 208000006289 Rett Syndrome Diseases 0.000 claims 1
- 206010067672 Spasmodic dysphonia Diseases 0.000 claims 1
- 208000009415 Spinocerebellar Ataxias Diseases 0.000 claims 1
- 108010058254 Steroid 12-alpha-Hydroxylase Proteins 0.000 claims 1
- 102100036325 Sterol 26-hydroxylase, mitochondrial Human genes 0.000 claims 1
- 208000006011 Stroke Diseases 0.000 claims 1
- 206010043189 Telangiectasia Diseases 0.000 claims 1
- 102100030973 Thromboxane-A synthase Human genes 0.000 claims 1
- 208000000323 Tourette Syndrome Diseases 0.000 claims 1
- 208000016620 Tourette disease Diseases 0.000 claims 1
- 206010044688 Trisomy 21 Diseases 0.000 claims 1
- 102100026523 Vitamin D 25-hydroxylase Human genes 0.000 claims 1
- 208000018839 Wilson disease Diseases 0.000 claims 1
- 208000013142 Writer cramp Diseases 0.000 claims 1
- 230000002411 adverse Effects 0.000 claims 1
- 229910021529 ammonia Inorganic materials 0.000 claims 1
- 230000037444 atrophy Effects 0.000 claims 1
- 208000015802 attention deficit-hyperactivity disease Diseases 0.000 claims 1
- 201000004562 autosomal dominant cerebellar ataxia Diseases 0.000 claims 1
- 210000004227 basal ganglia Anatomy 0.000 claims 1
- 230000006931 brain damage Effects 0.000 claims 1
- 231100000874 brain damage Toxicity 0.000 claims 1
- 208000029028 brain injury Diseases 0.000 claims 1
- 210000003710 cerebral cortex Anatomy 0.000 claims 1
- 206010008129 cerebral palsy Diseases 0.000 claims 1
- 201000002866 cervical dystonia Diseases 0.000 claims 1
- 208000012601 choreatic disease Diseases 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000007012 clinical effect Effects 0.000 claims 1
- 208000022124 combined dystonia Diseases 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 230000002920 convulsive effect Effects 0.000 claims 1
- 108010026647 cytochrome P-450 4X1 Proteins 0.000 claims 1
- 108010062869 cytochrome P-450 CYP2G1 Proteins 0.000 claims 1
- 108010018719 cytochrome P-450 CYP4B1 Proteins 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 201000006517 essential tremor Diseases 0.000 claims 1
- 230000004424 eye movement Effects 0.000 claims 1
- 201000002904 focal dystonia Diseases 0.000 claims 1
- 201000002865 focal hand dystonia Diseases 0.000 claims 1
- 102000006640 gamma-Glutamyltransferase Human genes 0.000 claims 1
- 125000002642 gamma-glutamyl group Chemical group 0.000 claims 1
- 208000008675 hereditary spastic paraplegia Diseases 0.000 claims 1
- 208000035231 inattentive type attention deficit hyperactivity disease Diseases 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 238000012317 liver biopsy Methods 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000001898 pallidal effect Effects 0.000 claims 1
- 230000001314 paroxysmal effect Effects 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 108010043671 prostatic acid phosphatase Proteins 0.000 claims 1
- 210000000463 red nucleus Anatomy 0.000 claims 1
- 201000002849 spasmodic dystonia Diseases 0.000 claims 1
- 230000001148 spastic effect Effects 0.000 claims 1
- 208000018198 spasticity Diseases 0.000 claims 1
- 210000000278 spinal cord Anatomy 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 208000009056 telangiectasis Diseases 0.000 claims 1
- 238000002604 ultrasonography Methods 0.000 claims 1
- 0 C*(C)(CCc(cc1OO*)ccc1O*)C(C(C(O)(O)Oc1cc(C)ccc1)(O)OC)(O)O Chemical compound C*(C)(CCc(cc1OO*)ccc1O*)C(C(C(O)(O)Oc1cc(C)ccc1)(O)OC)(O)O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562117654P | 2015-02-18 | 2015-02-18 | |
| US62/117,654 | 2015-02-18 | ||
| PCT/US2016/018222 WO2016133989A1 (en) | 2015-02-18 | 2016-02-17 | Dimethoxyphenyl inhibitors of vesicular monoamine transporter 2 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2018507210A JP2018507210A (ja) | 2018-03-15 |
| JP2018507210A5 true JP2018507210A5 (https=) | 2019-03-22 |
Family
ID=56692737
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017543828A Pending JP2018507210A (ja) | 2015-02-18 | 2016-02-17 | 小胞モノアミン輸送体２のジメトキシフェニル系阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US10722479B2 (https=) |
| EP (1) | EP3258926A4 (https=) |
| JP (1) | JP2018507210A (https=) |
| AR (1) | AR103728A1 (https=) |
| BR (1) | BR112017017673A2 (https=) |
| CA (1) | CA2976229A1 (https=) |
| EA (1) | EA201791839A1 (https=) |
| IL (1) | IL253901A0 (https=) |
| MA (1) | MA41557A (https=) |
| MX (1) | MX2017010567A (https=) |
| TW (1) | TW201630871A (https=) |
| WO (1) | WO2016133989A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017180794A1 (en) | 2016-04-13 | 2017-10-19 | Skyline Antiinfectives, Inc. | Deuterated o-sulfated beta-lactam hydroxamic acids and deuterated n-sulfated beta-lactams |
| KR20240096817A (ko) | 2020-05-19 | 2024-06-26 | 사이빈 아이알엘 리미티드 | 중수소화된 트립타민 유도체 및 사용 방법 |
| WO2026050236A1 (en) | 2024-08-27 | 2026-03-05 | Neurocrine Biosciences, Inc. | Muscarinic receptor agonist in combination with a vesicular monoamine transporter 2 inhibitor, for use in the treatment of a neurological or psychiatric disorder |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ211815A (en) | 1984-05-15 | 1988-11-29 | Warner Lambert Co | Preparation of 1-((3,4-dimethoxyphenethyl)amino)-3- (3-tolyloxy)-2-propanol |
| CA2653209A1 (en) * | 2006-05-26 | 2007-12-06 | Auspex Pharmaceuticals, Inc. | Deuterated aminoglycidyl compounds |
| CA2701638A1 (en) | 2007-04-02 | 2008-10-09 | Concert Pharmaceuticals Inc. | Pharmaceutical calcimimetics |
| US20100009950A1 (en) * | 2008-06-30 | 2010-01-14 | Auspex Pharmaceuticals, Inc. | Substituted ethanolamines |
| WO2010044981A2 (en) * | 2008-09-18 | 2010-04-22 | Auspex Pharmaceutical ,Inc. | Benzoquinoline inhibitors of vesicular monoamine transporter 2 |
| US20100143287A1 (en) | 2008-12-09 | 2010-06-10 | Auspex Pharmaceuticals, Inc. | Trifluoromethylphenyl modulators of calcium-sensing receptor |
| CA2801061A1 (en) * | 2010-06-01 | 2011-12-08 | Auspex Pharmaceuticals, Inc. | Benzoquinolone inhibitors of vmat2 |
| CN104684555A (zh) | 2012-09-18 | 2015-06-03 | 奥斯拜客斯制药有限公司 | 囊泡单胺转运体2的氘化苯并喹啉抑制剂的制剂药代动力学 |
| JP6476174B2 (ja) | 2013-06-19 | 2019-02-27 | ソム イノヴェーション バイオテック、ソシエダッド リミターダ | 運動過剰障害の予防および／または治療における使用のための治療剤 |
-
2016
- 2016-02-16 MA MA041557A patent/MA41557A/fr unknown
- 2016-02-17 WO PCT/US2016/018222 patent/WO2016133989A1/en not_active Ceased
- 2016-02-17 EP EP16752959.3A patent/EP3258926A4/en not_active Withdrawn
- 2016-02-17 EA EA201791839A patent/EA201791839A1/ru unknown
- 2016-02-17 JP JP2017543828A patent/JP2018507210A/ja active Pending
- 2016-02-17 MX MX2017010567A patent/MX2017010567A/es unknown
- 2016-02-17 US US15/550,152 patent/US10722479B2/en active Active
- 2016-02-17 CA CA2976229A patent/CA2976229A1/en not_active Abandoned
- 2016-02-17 BR BR112017017673A patent/BR112017017673A2/pt not_active Application Discontinuation
- 2016-02-18 AR ARP160100435A patent/AR103728A1/es unknown
- 2016-02-18 TW TW105104725A patent/TW201630871A/zh unknown
-
2017
- 2017-08-08 IL IL253901A patent/IL253901A0/en unknown
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