JP2012503010A5 - - Google Patents
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- JP2012503010A5 JP2012503010A5 JP2011527995A JP2011527995A JP2012503010A5 JP 2012503010 A5 JP2012503010 A5 JP 2012503010A5 JP 2011527995 A JP2011527995 A JP 2011527995A JP 2011527995 A JP2011527995 A JP 2011527995A JP 2012503010 A5 JP2012503010 A5 JP 2012503010A5
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- 150000001875 compounds Chemical class 0.000 claims 33
- 239000008194 pharmaceutical composition Substances 0.000 claims 10
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 6
- 102000001708 Protein Isoforms Human genes 0.000 claims 6
- 108010029485 Protein Isoforms Proteins 0.000 claims 6
- 229910052805 deuterium Inorganic materials 0.000 claims 6
- 102000018832 Cytochromes Human genes 0.000 claims 4
- 108010052832 Cytochromes Proteins 0.000 claims 4
- 102000010909 Monoamine Oxidase Human genes 0.000 claims 4
- 108010062431 Monoamine oxidase Proteins 0.000 claims 4
- 230000036470 plasma concentration Effects 0.000 claims 4
- 230000005764 inhibitory process Effects 0.000 claims 3
- 239000002207 metabolite Substances 0.000 claims 3
- 108010082126 Alanine transaminase 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
- 108010081668 Cytochrome P-450 CYP3A 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
- 108010022037 Retinoic Acid 4-Hydroxylase Proteins 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 210000004185 liver Anatomy 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 210000002966 serum Anatomy 0.000 claims 2
- 102100027518 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial Human genes 0.000 claims 1
- 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
- 102100036475 Alanine aminotransferase 1 Human genes 0.000 claims 1
- 102000002260 Alkaline Phosphatase Human genes 0.000 claims 1
- 108020004774 Alkaline Phosphatase Proteins 0.000 claims 1
- 108010078554 Aromatase Proteins 0.000 claims 1
- 102100029361 Aromatase Human genes 0.000 claims 1
- 101000856500 Bacillus subtilis subsp. natto Glutathione hydrolase proenzyme Proteins 0.000 claims 1
- 102000004506 Blood Proteins Human genes 0.000 claims 1
- 108010017384 Blood Proteins Proteins 0.000 claims 1
- 101150051438 CYP gene Proteins 0.000 claims 1
- -1 CYP39 Proteins 0.000 claims 1
- 108010084976 Cholesterol Side-Chain Cleavage Enzyme Proteins 0.000 claims 1
- 102100027516 Cholesterol side-chain cleavage enzyme, mitochondrial Human genes 0.000 claims 1
- 108010009911 Cytochrome P-450 CYP11B2 Proteins 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
- 102100024332 Cytochrome P450 11B1, mitochondrial Human genes 0.000 claims 1
- 102100024329 Cytochrome P450 11B2, mitochondrial Human genes 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
- 102100039282 Cytochrome P450 26A1 Human genes 0.000 claims 1
- 102100039281 Cytochrome P450 26B1 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
- 102100039205 Cytochrome P450 3A4 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
- 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
- 101000861278 Homo sapiens 1,25-dihydroxyvitamin D(3) 24-hydroxylase, mitochondrial Proteins 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
- 208000023105 Huntington disease Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-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
- 102000002704 Leucyl aminopeptidase Human genes 0.000 claims 1
- 108010004098 Leucyl aminopeptidase Proteins 0.000 claims 1
- 101150053185 P450 gene Proteins 0.000 claims 1
- 108090000279 Peptidyltransferases Proteins 0.000 claims 1
- 101710098398 Probable alanine aminotransferase, mitochondrial Proteins 0.000 claims 1
- 102100033075 Prostacyclin synthase Human genes 0.000 claims 1
- 102100026372 Putative inactive cytochrome P450 2G1 Human genes 0.000 claims 1
- 108010049356 Steroid 11-beta-Hydroxylase Proteins 0.000 claims 1
- 108010058254 Steroid 12-alpha-Hydroxylase Proteins 0.000 claims 1
- 108010015330 Steroid 17-alpha-Hydroxylase Proteins 0.000 claims 1
- 102100021719 Steroid 17-alpha-hydroxylase/17,20 lyase Human genes 0.000 claims 1
- 102100036325 Sterol 26-hydroxylase, mitochondrial Human genes 0.000 claims 1
- 102100030973 Thromboxane-A synthase Human genes 0.000 claims 1
- 102100026523 Vitamin D 25-hydroxylase Human genes 0.000 claims 1
- 229910021529 ammonia Inorganic materials 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
- 230000006866 deterioration Effects 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 102000006640 gamma-Glutamyltransferase Human genes 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 238000012317 liver biopsy Methods 0.000 claims 1
- 230000004060 metabolic process Effects 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 108010064377 prostacyclin synthetase Proteins 0.000 claims 1
- 108010043671 prostatic acid phosphatase Proteins 0.000 claims 1
- 238000002604 ultrasonography Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US9789608P | 2008-09-18 | 2008-09-18 | |
| US61/097,896 | 2008-09-18 | ||
| PCT/US2009/057480 WO2010044981A2 (en) | 2008-09-18 | 2009-09-18 | Benzoquinoline inhibitors of vesicular monoamine transporter 2 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014185634A Division JP5970037B2 (ja) | 2008-09-18 | 2014-09-11 | 小胞モノアミン輸送体２のベンゾキノリン阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2012503010A JP2012503010A (ja) | 2012-02-02 |
| JP2012503010A5 true JP2012503010A5 (cg-RX-API-DMAC7.html) | 2012-11-01 |
| JP5616345B2 JP5616345B2 (ja) | 2014-10-29 |
Family
ID=42107127
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011527995A Active JP5616345B2 (ja) | 2008-09-18 | 2009-09-18 | 小胞モノアミン輸送体２のベンゾキノリン阻害剤 |
| JP2014185634A Active JP5970037B2 (ja) | 2008-09-18 | 2014-09-11 | 小胞モノアミン輸送体２のベンゾキノリン阻害剤 |
| JP2016136178A Active JP6138322B2 (ja) | 2008-09-18 | 2016-07-08 | 小胞モノアミン輸送体２のベンゾキノリン阻害剤 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014185634A Active JP5970037B2 (ja) | 2008-09-18 | 2014-09-11 | 小胞モノアミン輸送体２のベンゾキノリン阻害剤 |
| JP2016136178A Active JP6138322B2 (ja) | 2008-09-18 | 2016-07-08 | 小胞モノアミン輸送体２のベンゾキノリン阻害剤 |
Country Status (20)
| Country | Link |
|---|---|
| US (16) | US8524733B2 (cg-RX-API-DMAC7.html) |
| EP (4) | EP3061760B1 (cg-RX-API-DMAC7.html) |
| JP (3) | JP5616345B2 (cg-RX-API-DMAC7.html) |
| CN (2) | CN102186848B (cg-RX-API-DMAC7.html) |
| AU (1) | AU2009303758B8 (cg-RX-API-DMAC7.html) |
| BR (1) | BRPI0913457B8 (cg-RX-API-DMAC7.html) |
| CA (2) | CA2972242A1 (cg-RX-API-DMAC7.html) |
| CY (1) | CY1120060T1 (cg-RX-API-DMAC7.html) |
| DK (2) | DK2326643T3 (cg-RX-API-DMAC7.html) |
| ES (4) | ES2425623T3 (cg-RX-API-DMAC7.html) |
| HR (1) | HRP20180239T1 (cg-RX-API-DMAC7.html) |
| HU (1) | HUE038158T2 (cg-RX-API-DMAC7.html) |
| LT (1) | LT3061760T (cg-RX-API-DMAC7.html) |
| NO (1) | NO3061760T3 (cg-RX-API-DMAC7.html) |
| NZ (1) | NZ591615A (cg-RX-API-DMAC7.html) |
| PL (1) | PL3061760T3 (cg-RX-API-DMAC7.html) |
| PT (1) | PT3061760T (cg-RX-API-DMAC7.html) |
| SI (1) | SI3061760T1 (cg-RX-API-DMAC7.html) |
| SM (1) | SMT201800067T1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2010044981A2 (cg-RX-API-DMAC7.html) |
Families Citing this family (63)
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| NO3061760T3 (cg-RX-API-DMAC7.html) * | 2008-09-18 | 2018-04-07 | ||
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| CA2801061A1 (en) * | 2010-06-01 | 2011-12-08 | Auspex Pharmaceuticals, Inc. | Benzoquinolone inhibitors of vmat2 |
| PL3222266T3 (pl) | 2010-08-27 | 2018-10-31 | Sienna Biopharmaceuticals, Inc. | Kompozycje i sposoby do termomodulacji celowanej |
| US9572880B2 (en) | 2010-08-27 | 2017-02-21 | Sienna Biopharmaceuticals, Inc. | Ultrasound delivery of nanoparticles |
| WO2012081031A1 (en) * | 2010-12-15 | 2012-06-21 | Enaltec Labs Pvt. Ltd. | Process for preparing tetrabenazine |
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| NZ705372A (en) * | 2012-09-18 | 2018-07-27 | Auspex Pharmaceuticals Inc | Formulations pharmacokinetics of deuterated benzoquinoline inhibitors of vesicular monoamine transporter 2 |
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| JP6635945B2 (ja) | 2014-05-06 | 2020-01-29 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | 多動性運動障害を処置するためのｖｍａｔ２インヒビター |
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| JP7109360B2 (ja) | 2015-10-30 | 2022-07-29 | ニューロクライン バイオサイエンシーズ，インコーポレイテッド | バルベナジン塩およびその多形体 |
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| US10479787B2 (en) | 2016-04-22 | 2019-11-19 | Lupin Limited | Process for preparation of tetrabenazine and deutetrabenazine |
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| CN107936008B (zh) * | 2016-10-13 | 2022-06-14 | 泰州华元医药科技有限公司 | 氘代化合物及其医药用途 |
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| CN108794337A (zh) * | 2018-07-10 | 2018-11-13 | 上海华堇生物技术有限责任公司 | 一种3,4-二羟基-β-硝基苯乙烯的新制备方法 |
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