JP2016521755A5 - - Google Patents
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- JP2016521755A5 JP2016521755A5 JP2016519696A JP2016519696A JP2016521755A5 JP 2016521755 A5 JP2016521755 A5 JP 2016521755A5 JP 2016519696 A JP2016519696 A JP 2016519696A JP 2016519696 A JP2016519696 A JP 2016519696A JP 2016521755 A5 JP2016521755 A5 JP 2016521755A5
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- Prior art keywords
- metabolic disorder
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- antagonist
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- sumn
- Prior art date
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- 239000000203 mixture Substances 0.000 claims description 22
- 239000003795 chemical substances by application Substances 0.000 claims description 17
- 230000000694 effects Effects 0.000 claims description 13
- 102000005962 receptors Human genes 0.000 claims description 11
- 108020003175 receptors Proteins 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 239000000556 agonist Substances 0.000 claims description 7
- 102000003678 AMPA Receptors Human genes 0.000 claims description 4
- 108090000078 AMPA Receptors Proteins 0.000 claims description 4
- 239000005557 antagonist Substances 0.000 claims description 4
- 229940044601 receptor agonist Drugs 0.000 claims description 4
- 239000000018 receptor agonist Substances 0.000 claims description 4
- 239000003148 4 aminobutyric acid receptor blocking agent Substances 0.000 claims description 3
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims description 2
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims 31
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims 22
- 239000000774 AMPA receptor agonist Substances 0.000 claims 14
- 239000003140 4 aminobutyric acid A receptor blocking agent Substances 0.000 claims 12
- 239000003706 n methyl dextro aspartic acid receptor stimulating agent Substances 0.000 claims 12
- 229940124118 AMPA receptor agonist Drugs 0.000 claims 11
- 229960003638 dopamine Drugs 0.000 claims 9
- 206010018429 Glucose tolerance impaired Diseases 0.000 claims 7
- 208000008589 Obesity Diseases 0.000 claims 7
- 208000001280 Prediabetic State Diseases 0.000 claims 7
- 235000020824 obesity Nutrition 0.000 claims 7
- 201000009104 prediabetes syndrome Diseases 0.000 claims 7
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 7
- 208000024172 Cardiovascular disease Diseases 0.000 claims 6
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 claims 6
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 claims 6
- 210000005064 dopaminergic neuron Anatomy 0.000 claims 5
- 230000008499 blood brain barrier function Effects 0.000 claims 4
- 210000001218 blood-brain barrier Anatomy 0.000 claims 4
- 210000002569 neuron Anatomy 0.000 claims 4
- 230000033764 rhythmic process Effects 0.000 claims 4
- 230000037007 arousal Effects 0.000 claims 3
- 230000003371 gabaergic effect Effects 0.000 claims 3
- 210000000221 suprachiasmatic nucleus Anatomy 0.000 claims 3
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- 210000003169 central nervous system Anatomy 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
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- -1 amide phosphate derivatives Chemical class 0.000 description 3
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- SULXXKLCQRXMHP-UHFFFAOYSA-N 4-[1-hydroxy-5-(3-phenylphenyl)pyrazol-4-yl]piperidine;2,2,2-trifluoroacetic acid Chemical compound OC(=O)C(F)(F)F.C=1C=CC(C=2C=CC=CC=2)=CC=1C=1N(O)N=CC=1C1CCNCC1 SULXXKLCQRXMHP-UHFFFAOYSA-N 0.000 description 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 description 2
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- MOLPUWBMSBJXER-YDGSQGCISA-N bilobalide Chemical compound O([C@H]1OC2=O)C(=O)[C@H](O)[C@@]11[C@@](C(C)(C)C)(O)C[C@H]3[C@@]21CC(=O)O3 MOLPUWBMSBJXER-YDGSQGCISA-N 0.000 description 2
- OMCYEZUIYGPHDJ-OQLLNIDSSA-N chembl354261 Chemical compound OC1=CC=CC=C1\C=N\NC(=O)C1=CC=CC=C1O OMCYEZUIYGPHDJ-OQLLNIDSSA-N 0.000 description 2
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 description 2
- 235000009200 high fat diet Nutrition 0.000 description 2
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical compound N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 description 2
- 238000000034 method Methods 0.000 description 2
- ZJQHPWUVQPJPQT-UHFFFAOYSA-N muscimol Chemical compound NCC1=CC(=O)NO1 ZJQHPWUVQPJPQT-UHFFFAOYSA-N 0.000 description 2
- RLJKFAMYSYWMND-GRTNUQQKSA-M (6r)-6-[(5s)-6,6-dimethyl-7,8-dihydro-5h-[1,3]dioxolo[4,5-g]isoquinolin-6-ium-5-yl]-6h-furo[3,4-g][1,3]benzodioxol-8-one;chloride Chemical compound [Cl-].O([C@H]1[C@@H]2C3=CC=4OCOC=4C=C3CC[N+]2(C)C)C(=O)C2=C1C=CC1=C2OCO1 RLJKFAMYSYWMND-GRTNUQQKSA-M 0.000 description 1
- HKJKCPKPSSVUHY-GRTNUQQKSA-M (6r)-6-[(5s)-6,6-dimethyl-7,8-dihydro-5h-[1,3]dioxolo[4,5-g]isoquinolin-6-ium-5-yl]-6h-furo[3,4-g][1,3]benzodioxol-8-one;iodide Chemical compound [I-].O([C@H]1[C@@H]2C3=CC=4OCOC=4C=C3CC[N+]2(C)C)C(=O)C2=C1C=CC1=C2OCO1 HKJKCPKPSSVUHY-GRTNUQQKSA-M 0.000 description 1
- MGRVRXRGTBOSHW-UHFFFAOYSA-N (aminomethyl)phosphonic acid Chemical compound NCP(O)(O)=O MGRVRXRGTBOSHW-UHFFFAOYSA-N 0.000 description 1
- ZCXLTWVZYXBHJS-UHFFFAOYSA-N 1,2-benzoxazepine Chemical class O1N=CC=CC2=CC=CC=C12 ZCXLTWVZYXBHJS-UHFFFAOYSA-N 0.000 description 1
- IAWXTSMHXFRLQR-UHFFFAOYSA-N 2,3-bis($l^{1}-oxidanyl)-7-nitroquinoxaline-6-carbonitrile Chemical compound O=C1C(=O)N=C2C=C(C#N)C([N+](=O)[O-])=CC2=N1 IAWXTSMHXFRLQR-UHFFFAOYSA-N 0.000 description 1
- ZZYJIEWWTWIQGM-UHFFFAOYSA-N 3-ethoxy-4-[4-[3-(propan-2-ylsulfonylamino)thiophen-2-yl]phenyl]benzoic acid Chemical compound CCOC1=CC(C(O)=O)=CC=C1C1=CC=C(C2=C(C=CS2)NS(=O)(=O)C(C)C)C=C1 ZZYJIEWWTWIQGM-UHFFFAOYSA-N 0.000 description 1
- 239000003477 4 aminobutyric acid receptor stimulating agent Substances 0.000 description 1
- BWXCECYGGMGBHD-UHFFFAOYSA-M 6-(6,6-dimethyl-7,8-dihydro-5h-[1,3]dioxolo[4,5-g]isoquinolin-6-ium-5-yl)-6h-furo[3,4-g][1,3]benzodioxol-8-one;bromide Chemical compound [Br-].C[N+]1(C)CCC2=CC=3OCOC=3C=C2C1C1OC(=O)C2=C1C=CC1=C2OCO1 BWXCECYGGMGBHD-UHFFFAOYSA-M 0.000 description 1
- 229940098747 AMPA receptor antagonist Drugs 0.000 description 1
- 239000000775 AMPA receptor antagonist Substances 0.000 description 1
- 102000005915 GABA Receptors Human genes 0.000 description 1
- 108010005551 GABA Receptors Proteins 0.000 description 1
- 229940098788 GABA receptor antagonist Drugs 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 102000004877 Insulin Human genes 0.000 description 1
- 108090001061 Insulin Proteins 0.000 description 1
- 241001465754 Metazoa Species 0.000 description 1
- CWRVKFFCRWGWCS-UHFFFAOYSA-N Pentrazole Chemical compound C1CCCCC2=NN=NN21 CWRVKFFCRWGWCS-UHFFFAOYSA-N 0.000 description 1
- PIMZUZSSNYHVCU-OMKDEKJRSA-N Picrotoxinin Natural products O=C1O[C@@H]2[C@@H](C(=C)C)[C@H]1[C@@]1(O)[C@@]3(C)[C@@H]2OC(=O)[C@@]23O[C@H]2C1 PIMZUZSSNYHVCU-OMKDEKJRSA-N 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 description 1
- WQZGKKKJIJFFOK-VFUOTHLCSA-N beta-D-glucose Chemical compound OC[C@H]1O[C@@H](O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-VFUOTHLCSA-N 0.000 description 1
- IYGYMKDQCDOMRE-ZWKOTPCHSA-N bicuculline Chemical compound O([C@H]1[C@@H]2C3=CC=4OCOC=4C=C3CCN2C)C(=O)C2=C1C=CC1=C2OCO1 IYGYMKDQCDOMRE-ZWKOTPCHSA-N 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 229940000425 combination drug Drugs 0.000 description 1
- OFBIFZUFASYYRE-UHFFFAOYSA-N flumazenil Chemical compound C1N(C)C(=O)C2=CC(F)=CC=C2N2C=NC(C(=O)OCC)=C21 OFBIFZUFASYYRE-UHFFFAOYSA-N 0.000 description 1
- 229960004381 flumazenil Drugs 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 235000012631 food intake Nutrition 0.000 description 1
- 229960003883 furosemide Drugs 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 229940125396 insulin Drugs 0.000 description 1
- 210000001596 intra-abdominal fat Anatomy 0.000 description 1
- SHLPPXXKRFINFY-UHFFFAOYSA-N isoquinolin-2-ium;bromide Chemical compound Br.C1=NC=CC2=CC=CC=C21 SHLPPXXKRFINFY-UHFFFAOYSA-N 0.000 description 1
- 231100000053 low toxicity Toxicity 0.000 description 1
- PIMZUZSSNYHVCU-YKWPQBAZSA-N picrotoxinin Chemical compound O=C([C@@]12O[C@@H]1C[C@]1(O)[C@@]32C)O[C@@H]3[C@H]2[C@@H](C(=C)C)[C@@H]1C(=O)O2 PIMZUZSSNYHVCU-YKWPQBAZSA-N 0.000 description 1
- 150000003217 pyrazoles Chemical class 0.000 description 1
- 150000003246 quinazolines Chemical class 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 238000013223 sprague-dawley female rat Methods 0.000 description 1
- 150000008334 thiadiazines Chemical class 0.000 description 1
- USMNOWBWPHYOEA-MRTMQBJTSA-N α-thujone Chemical compound O=C([C@@H]1C)C[C@@]2(C(C)C)[C@@H]1C2 USMNOWBWPHYOEA-MRTMQBJTSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361834864P | 2013-06-13 | 2013-06-13 | |
| US61/834,864 | 2013-06-13 | ||
| PCT/US2014/042397 WO2014201411A1 (en) | 2013-06-13 | 2014-06-13 | Compositions and methods for treating metabolic disorders |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2016521755A JP2016521755A (ja) | 2016-07-25 |
| JP2016521755A5 true JP2016521755A5 (enExample) | 2017-07-27 |
Family
ID=52022819
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016519696A Pending JP2016521755A (ja) | 2013-06-13 | 2014-06-13 | 代謝障害を治療するための組成物および方法 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US20150011554A1 (enExample) |
| EP (2) | EP3311842A1 (enExample) |
| JP (1) | JP2016521755A (enExample) |
| CN (1) | CN105579575A (enExample) |
| AU (1) | AU2014277952A1 (enExample) |
| BR (1) | BR112015031249A2 (enExample) |
| CA (1) | CA2915405A1 (enExample) |
| MX (1) | MX2015017253A (enExample) |
| WO (1) | WO2014201411A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9655865B2 (en) | 2002-07-29 | 2017-05-23 | Veroscience, Llc | Therapeutic treatment for metabolic syndrome, type 2 diabetes, obesity, or prediabetes |
| US8821915B2 (en) | 2002-08-09 | 2014-09-02 | Veroscience, Llc | Therapeutic process for the treatment of the metabolic syndrome and associated metabolic disorders |
| EP2217073B1 (en) | 2007-06-21 | 2019-10-09 | VeroScience LLC | Method of treating metabolic disorders and depression with dopamine receptor agonists |
| US20100035886A1 (en) | 2007-06-21 | 2010-02-11 | Veroscience, Llc | Parenteral formulations of dopamine agonists |
| US8741918B2 (en) | 2007-06-21 | 2014-06-03 | Veroscience Llc | Parenteral formulations of dopamine agonists |
| US9352025B2 (en) | 2009-06-05 | 2016-05-31 | Veroscience Llc | Combination of dopamine agonists plus first phase insulin secretagogues for the treatment of metabolic disorders |
| US8431155B1 (en) | 2012-04-30 | 2013-04-30 | Veroscience Llc | Bromocriptine formulations |
| EP3925610A1 (en) | 2016-04-20 | 2021-12-22 | VeroScience LLC | Composition and method for treating metabolic disorders |
| HRP20241365T1 (hr) | 2017-10-18 | 2024-12-20 | Veroscience Llc | Poboljšane formulacije bromokriptina |
| WO2019113110A2 (en) * | 2017-12-05 | 2019-06-13 | Peter Vanderklish | Modulation of ampa/kainate receptors for the treatment of hypoglycemia |
| WO2020236696A1 (en) * | 2019-05-23 | 2020-11-26 | Dignity Health | Inhibitory interneuron treatment methods, uses and compositions for diabetes |
| US11607455B2 (en) | 2019-09-23 | 2023-03-21 | Veroscience Llc | Method for inducing tumor regression |
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-
2014
- 2014-06-13 CA CA2915405A patent/CA2915405A1/en not_active Abandoned
- 2014-06-13 WO PCT/US2014/042397 patent/WO2014201411A1/en not_active Ceased
- 2014-06-13 EP EP17206128.5A patent/EP3311842A1/en not_active Withdrawn
- 2014-06-13 CN CN201480044899.5A patent/CN105579575A/zh active Pending
- 2014-06-13 EP EP14811295.6A patent/EP3008167A4/en not_active Withdrawn
- 2014-06-13 JP JP2016519696A patent/JP2016521755A/ja active Pending
- 2014-06-13 AU AU2014277952A patent/AU2014277952A1/en not_active Abandoned
- 2014-06-13 BR BR112015031249A patent/BR112015031249A2/pt not_active Application Discontinuation
- 2014-06-13 US US14/304,659 patent/US20150011554A1/en not_active Abandoned
- 2014-06-13 MX MX2015017253A patent/MX2015017253A/es unknown
-
2018
- 2018-11-16 US US16/193,193 patent/US20190160059A1/en not_active Abandoned
-
2022
- 2022-01-04 US US17/568,560 patent/US20220142960A1/en not_active Abandoned
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