BR112021009944A2 - gaboxadol para reduzir risco de suicídio e alívio rápido de depressão - Google Patents
gaboxadol para reduzir risco de suicídio e alívio rápido de depressão Download PDFInfo
- Publication number
- BR112021009944A2 BR112021009944A2 BR112021009944-1A BR112021009944A BR112021009944A2 BR 112021009944 A2 BR112021009944 A2 BR 112021009944A2 BR 112021009944 A BR112021009944 A BR 112021009944A BR 112021009944 A2 BR112021009944 A2 BR 112021009944A2
- Authority
- BR
- Brazil
- Prior art keywords
- gaboxadol
- treatment
- administration
- suicide
- ketamine
- Prior art date
Links
- ZXRVKCBLGJOCEE-UHFFFAOYSA-N Gaboxadol Chemical compound C1NCCC2=C1ONC2=O ZXRVKCBLGJOCEE-UHFFFAOYSA-N 0.000 title claims abstract description 269
- 229950004346 gaboxadol Drugs 0.000 title claims abstract description 262
- 206010010144 Completed suicide Diseases 0.000 title claims abstract description 89
- 238000000034 method Methods 0.000 claims abstract description 79
- 150000003839 salts Chemical class 0.000 claims abstract description 77
- 208000024891 symptom Diseases 0.000 claims abstract description 31
- 230000001154 acute effect Effects 0.000 claims abstract description 17
- 208000028552 Treatment-Resistant Depressive disease Diseases 0.000 claims abstract description 16
- 238000011282 treatment Methods 0.000 claims description 214
- YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 claims description 93
- 229960003299 ketamine Drugs 0.000 claims description 86
- 239000003814 drug Substances 0.000 claims description 70
- 229940079593 drug Drugs 0.000 claims description 62
- 206010042458 Suicidal ideation Diseases 0.000 claims description 55
- 210000004556 brain Anatomy 0.000 claims description 50
- 230000000694 effects Effects 0.000 claims description 49
- 230000004913 activation Effects 0.000 claims description 45
- 239000000935 antidepressant agent Substances 0.000 claims description 35
- 229940005513 antidepressants Drugs 0.000 claims description 35
- 230000004044 response Effects 0.000 claims description 34
- 230000001430 anti-depressive effect Effects 0.000 claims description 22
- 239000002775 capsule Substances 0.000 claims description 21
- 230000002195 synergetic effect Effects 0.000 claims description 19
- 238000012360 testing method Methods 0.000 claims description 19
- 206010054089 Depressive symptom Diseases 0.000 claims description 17
- 230000006872 improvement Effects 0.000 claims description 15
- 238000002582 magnetoencephalography Methods 0.000 claims description 15
- 108010071563 Proto-Oncogene Proteins c-fos Proteins 0.000 claims description 11
- 102000007568 Proto-Oncogene Proteins c-fos Human genes 0.000 claims description 11
- 230000000926 neurological effect Effects 0.000 claims description 10
- HARRKNSQXBRBGZ-GVKWWOCJSA-N zuranolone Chemical compound O=C([C@H]1CC[C@H]2[C@H]3[C@@H]([C@H]4CC[C@@](C)(O)C[C@H]4CC3)CC[C@@]21C)CN1C=C(C#N)C=N1 HARRKNSQXBRBGZ-GVKWWOCJSA-N 0.000 claims description 9
- 102000004300 GABA-A Receptors Human genes 0.000 claims description 8
- 108090000839 GABA-A Receptors Proteins 0.000 claims description 8
- 206010042464 Suicide attempt Diseases 0.000 claims description 8
- 230000036470 plasma concentration Effects 0.000 claims description 8
- 230000036765 blood level Effects 0.000 claims description 7
- 230000009182 swimming Effects 0.000 claims description 7
- DMJHZVARRXJSEG-UHFFFAOYSA-N decoglurant Chemical compound C1=NC(N)=CC=C1C#CC1=C2N=C(C=3C=CC(=CC=3)C(F)(F)F)C=C(C(F)(F)F)N2N=C1 DMJHZVARRXJSEG-UHFFFAOYSA-N 0.000 claims description 6
- AURFZBICLPNKBZ-YZRLXODZSA-N 3alpha-hydroxy-5beta-pregnan-20-one Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-YZRLXODZSA-N 0.000 claims description 5
- 102000027484 GABAA receptors Human genes 0.000 claims description 5
- 108091008681 GABAA receptors Proteins 0.000 claims description 5
- AURFZBICLPNKBZ-UHFFFAOYSA-N Pregnanolone Natural products C1CC2CC(O)CCC2(C)C2C1C1CCC(C(=O)C)C1(C)CC2 AURFZBICLPNKBZ-UHFFFAOYSA-N 0.000 claims description 5
- RECBFDWSXWAXHY-IAGOWNOFSA-N cerc-301 Chemical compound C1=CC(C)=CC=C1COC(=O)N1C[C@@H](F)[C@@H](CNC=2N=CC=CN=2)CC1 RECBFDWSXWAXHY-IAGOWNOFSA-N 0.000 claims description 5
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims description 5
- 229960004170 clozapine Drugs 0.000 claims description 5
- 230000034994 death Effects 0.000 claims description 5
- 239000006186 oral dosage form Substances 0.000 claims description 5
- DVBUEXCIEIAXPM-PJUQSVSOSA-N (2r)-1-[(2s)-1-[(2s,3r)-2-amino-3-hydroxybutanoyl]pyrrolidine-2-carbonyl]-n-[(2s,3r)-1-amino-3-hydroxy-1-oxobutan-2-yl]-2-benzylpyrrolidine-2-carboxamide Chemical compound C[C@@H](O)[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@@](C(=O)N[C@@H]([C@@H](C)O)C(N)=O)(CC=2C=CC=CC=2)CCC1 DVBUEXCIEIAXPM-PJUQSVSOSA-N 0.000 claims description 4
- HQLHZNDJQSRKDT-QMMMGPOBSA-N (2s)-2-amino-4-(2-amino-4-chlorophenyl)-4-oxobutanoic acid Chemical compound OC(=O)[C@@H](N)CC(=O)C1=CC=C(Cl)C=C1N HQLHZNDJQSRKDT-QMMMGPOBSA-N 0.000 claims description 4
- QEMSVZNTSXPFJA-HNAYVOBHSA-N 1-[(1s,2s)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]-4-phenylpiperidin-4-ol Chemical compound C1([C@H](O)[C@H](C)N2CCC(O)(CC2)C=2C=CC=CC=2)=CC=C(O)C=C1 QEMSVZNTSXPFJA-HNAYVOBHSA-N 0.000 claims description 4
- 230000009471 action Effects 0.000 claims description 4
- 238000004519 manufacturing process Methods 0.000 claims description 4
- 150000004682 monohydrates Chemical class 0.000 claims description 4
- 230000000306 recurrent effect Effects 0.000 claims description 4
- PBJUNZJWGZTSKL-MRXNPFEDSA-N tiagabine Chemical compound C1=CSC(C(=CCCN2C[C@@H](CCC2)C(O)=O)C2=C(C=CS2)C)=C1C PBJUNZJWGZTSKL-MRXNPFEDSA-N 0.000 claims description 4
- 229960001918 tiagabine Drugs 0.000 claims description 4
- JWMFYGXQPXQEEM-NUNROCCHSA-N 5β-pregnane Chemical compound C([C@H]1CC2)CCC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](CC)[C@@]2(C)CC1 JWMFYGXQPXQEEM-NUNROCCHSA-N 0.000 claims description 3
- FWUQWDCOOWEXRY-ZDUSSCGKSA-N lanicemine Chemical compound C([C@H](N)C=1C=CC=CC=1)C1=CC=CC=N1 FWUQWDCOOWEXRY-ZDUSSCGKSA-N 0.000 claims description 3
- 238000000386 microscopy Methods 0.000 claims description 3
- VLZBRVJVCCNPRJ-KPHUOKFYSA-N (1S,2S)-2-[(1S)-1-amino-1-carboxy-2-(9H-xanthen-9-yl)ethyl]-1-cyclopropanecarboxylic acid Chemical compound C([C@@H]1[C@](CC2C3=CC=CC=C3OC3=CC=CC=C32)(N)C(O)=O)[C@@H]1C(O)=O VLZBRVJVCCNPRJ-KPHUOKFYSA-N 0.000 claims description 2
- CFBVGSWSOJBYGC-ZYHUDNBSSA-N (2r,6r)-2-amino-2-(2-chlorophenyl)-6-hydroxycyclohexan-1-one Chemical compound C=1C=CC=C(Cl)C=1[C@]1(N)CCC[C@@H](O)C1=O CFBVGSWSOJBYGC-ZYHUDNBSSA-N 0.000 claims description 2
- DUHUCHOQIDJXAT-CSXWOMMHSA-N (3r,5r,8s,9s,10s,13s,14s,17s)-17-acetyl-3-hydroxy-10,13-dimethyl-1,2,3,4,5,6,7,8,9,12,14,15,16,17-tetradecahydrocyclopenta[a]phenanthren-11-one Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1=O DUHUCHOQIDJXAT-CSXWOMMHSA-N 0.000 claims description 2
- DUHUCHOQIDJXAT-OLVMNOGESA-N 3-hydroxy-(3-α,5-α)-Pregnane-11,20-dione Chemical compound C([C@@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1=O DUHUCHOQIDJXAT-OLVMNOGESA-N 0.000 claims description 2
- USPYDUPOCUYHQL-VEVMSBRDSA-N 5beta-dihydrodeoxycorticosterone Chemical compound C1C(=O)CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CC[C@@H]21 USPYDUPOCUYHQL-VEVMSBRDSA-N 0.000 claims description 2
- PGTVWKLGGCQMBR-FLBATMFCSA-N Ganaxolone Chemical compound C([C@@H]1CC2)[C@](C)(O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 PGTVWKLGGCQMBR-FLBATMFCSA-N 0.000 claims description 2
- LBOJYSIDWZQNJS-JKSUJKDBSA-N LSM-5387 Chemical compound C12=CC=CC=C2[C@@]2(C)C3=CC=CC=C3C[C@@H]1N2 LBOJYSIDWZQNJS-JKSUJKDBSA-N 0.000 claims description 2
- WVZSEUPGUDIELE-HTAPYJJXSA-N Ro 25-6981 Chemical compound C([C@H](C)[C@@H](O)C=1C=CC(O)=CC=1)N(CC1)CCC1CC1=CC=CC=C1 WVZSEUPGUDIELE-HTAPYJJXSA-N 0.000 claims description 2
- XWYBFXIUISNTQG-VKMGZQQJSA-N alfadolone Chemical compound C1[C@H](O)CC[C@]2(C)[C@H]3C(=O)C[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CC[C@H]21 XWYBFXIUISNTQG-VKMGZQQJSA-N 0.000 claims description 2
- 229950008709 alfadolone Drugs 0.000 claims description 2
- 229960003305 alfaxalone Drugs 0.000 claims description 2
- 229950003508 apimostinel Drugs 0.000 claims description 2
- 238000007405 data analysis Methods 0.000 claims description 2
- 229950005807 decoglurant Drugs 0.000 claims description 2
- 229950007402 eltanolone Drugs 0.000 claims description 2
- 125000004494 ethyl ester group Chemical group 0.000 claims description 2
- 229950006567 ganaxolone Drugs 0.000 claims description 2
- BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims description 2
- 229960004640 memantine Drugs 0.000 claims description 2
- LFAGGDAZZKUVKO-JAGWWQSPSA-N mgs-0039 Chemical compound O([C@@H]1C[C@@H]2[C@@H]([C@@]2(F)C(O)=O)[C@]1(N)C(O)=O)CC1=CC=C(Cl)C(Cl)=C1 LFAGGDAZZKUVKO-JAGWWQSPSA-N 0.000 claims description 2
- NCGLTZSBTFVVAW-KNXRZYMVSA-N minaxolone Chemical compound C1[C@@H](N(C)C)[C@@H]2[C@@]3(C)C[C@H](OCC)[C@@H](O)C[C@@H]3CC[C@H]2[C@@H]2CC[C@H](C(C)=O)[C@]21C NCGLTZSBTFVVAW-KNXRZYMVSA-N 0.000 claims description 2
- 229960004798 minaxolone Drugs 0.000 claims description 2
- GIBQQARAXHVEGD-BSOLPCOYSA-N rapastinel Chemical compound C[C@@H](O)[C@H](N)C(=O)N1CCC[C@H]1C(=O)N1[C@H](C(=O)N[C@@H]([C@@H](C)O)C(N)=O)CCC1 GIBQQARAXHVEGD-BSOLPCOYSA-N 0.000 claims description 2
- 229950003206 renanolone Drugs 0.000 claims description 2
- 229940070121 rislenemdaz Drugs 0.000 claims description 2
- 229950005135 traxoprodil Drugs 0.000 claims description 2
- XQGZGUOPFIIXCX-UHFFFAOYSA-N NC1=C(C=CC(=C1)NCC1=C(C=C(C=C1C)C)C)NC(O)=O Chemical compound NC1=C(C=CC(=C1)NCC1=C(C=C(C=C1C)C)C)NC(O)=O XQGZGUOPFIIXCX-UHFFFAOYSA-N 0.000 claims 2
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 239000002858 neurotransmitter agent Substances 0.000 claims 1
- 238000012800 visualization Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 abstract description 29
- 208000024714 major depressive disease Diseases 0.000 abstract description 21
- 230000036651 mood Effects 0.000 abstract description 5
- 238000011285 therapeutic regimen Methods 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 description 28
- 239000008194 pharmaceutical composition Substances 0.000 description 21
- 230000000763 evoking effect Effects 0.000 description 19
- 230000001225 therapeutic effect Effects 0.000 description 18
- 238000001802 infusion Methods 0.000 description 17
- 238000009472 formulation Methods 0.000 description 16
- 210000000218 midline thalamic nuclei Anatomy 0.000 description 16
- 239000003826 tablet Substances 0.000 description 16
- 229910052805 deuterium Inorganic materials 0.000 description 15
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 14
- 239000002552 dosage form Substances 0.000 description 14
- 241000282414 Homo sapiens Species 0.000 description 12
- 210000000627 locus coeruleus Anatomy 0.000 description 12
- 238000003556 assay Methods 0.000 description 11
- 238000003745 diagnosis Methods 0.000 description 11
- 210000002509 periaqueductal gray Anatomy 0.000 description 11
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 11
- 241000699670 Mus sp. Species 0.000 description 9
- 210000004727 amygdala Anatomy 0.000 description 9
- 210000003710 cerebral cortex Anatomy 0.000 description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 9
- 239000010408 film Substances 0.000 description 9
- 208000020401 Depressive disease Diseases 0.000 description 8
- 230000006399 behavior Effects 0.000 description 8
- 230000008859 change Effects 0.000 description 8
- 230000001054 cortical effect Effects 0.000 description 8
- 230000001339 gustatory effect Effects 0.000 description 8
- 210000002946 intralaminar thalamic nuclei Anatomy 0.000 description 8
- 230000009467 reduction Effects 0.000 description 8
- 230000003238 somatosensory effect Effects 0.000 description 8
- 230000009278 visceral effect Effects 0.000 description 8
- 230000000007 visual effect Effects 0.000 description 8
- UDHPXYNRXFPDOF-UHFFFAOYSA-N 4,5,6,7-tetrahydro-[1,2]oxazolo[5,4-c]pyridin-6-ium-3-olate;hydrate Chemical compound O.C1NCCC2=C1ON=C2O UDHPXYNRXFPDOF-UHFFFAOYSA-N 0.000 description 7
- -1 NIK-0657 ) Chemical compound 0.000 description 7
- 230000003542 behavioural effect Effects 0.000 description 7
- 201000010099 disease Diseases 0.000 description 7
- 229910052731 fluorine Inorganic materials 0.000 description 7
- 210000000214 mouth Anatomy 0.000 description 7
- 239000006191 orally-disintegrating tablet Substances 0.000 description 7
- 239000000523 sample Substances 0.000 description 7
- 239000000126 substance Substances 0.000 description 7
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 6
- 241000699666 Mus <mouse, genus> Species 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 6
- 239000011737 fluorine Substances 0.000 description 6
- 239000007937 lozenge Substances 0.000 description 6
- 239000000463 material Substances 0.000 description 6
- 238000011160 research Methods 0.000 description 6
- 210000003296 saliva Anatomy 0.000 description 6
- YQEZLKZALYSWHR-ZDUSSCGKSA-N (S)-ketamine Chemical compound C=1C=CC=C(Cl)C=1[C@@]1(NC)CCCCC1=O YQEZLKZALYSWHR-ZDUSSCGKSA-N 0.000 description 5
- 241001465754 Metazoa Species 0.000 description 5
- 238000004458 analytical method Methods 0.000 description 5
- 239000002249 anxiolytic agent Substances 0.000 description 5
- 239000000090 biomarker Substances 0.000 description 5
- 239000008280 blood Substances 0.000 description 5
- 210000004369 blood Anatomy 0.000 description 5
- 210000000133 brain stem Anatomy 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 238000011161 development Methods 0.000 description 5
- 230000018109 developmental process Effects 0.000 description 5
- 238000009826 distribution Methods 0.000 description 5
- 238000001727 in vivo Methods 0.000 description 5
- 238000012423 maintenance Methods 0.000 description 5
- 238000002483 medication Methods 0.000 description 5
- 210000001259 mesencephalon Anatomy 0.000 description 5
- 229940124811 psychiatric drug Drugs 0.000 description 5
- 230000002123 temporal effect Effects 0.000 description 5
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 description 4
- 230000000949 anxiolytic effect Effects 0.000 description 4
- 230000009286 beneficial effect Effects 0.000 description 4
- 239000007963 capsule composition Substances 0.000 description 4
- 238000002648 combination therapy Methods 0.000 description 4
- 230000000875 corresponding effect Effects 0.000 description 4
- 238000001647 drug administration Methods 0.000 description 4
- 238000002635 electroconvulsive therapy Methods 0.000 description 4
- 238000007667 floating Methods 0.000 description 4
- 210000004326 gyrus cinguli Anatomy 0.000 description 4
- 230000002401 inhibitory effect Effects 0.000 description 4
- 230000005764 inhibitory process Effects 0.000 description 4
- 206010022437 insomnia Diseases 0.000 description 4
- 235000011475 lollipops Nutrition 0.000 description 4
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 4
- 238000005259 measurement Methods 0.000 description 4
- 238000012986 modification Methods 0.000 description 4
- 230000004048 modification Effects 0.000 description 4
- 238000002610 neuroimaging Methods 0.000 description 4
- 210000001009 nucleus accumben Anatomy 0.000 description 4
- 239000003921 oil Substances 0.000 description 4
- 210000002963 paraventricular hypothalamic nucleus Anatomy 0.000 description 4
- 230000000144 pharmacologic effect Effects 0.000 description 4
- 239000006187 pill Substances 0.000 description 4
- 229940068196 placebo Drugs 0.000 description 4
- 239000000902 placebo Substances 0.000 description 4
- 230000002829 reductive effect Effects 0.000 description 4
- 238000001228 spectrum Methods 0.000 description 4
- 208000011117 substance-related disease Diseases 0.000 description 4
- 229940124597 therapeutic agent Drugs 0.000 description 4
- 239000003981 vehicle Substances 0.000 description 4
- 230000003442 weekly effect Effects 0.000 description 4
- 208000009575 Angelman syndrome Diseases 0.000 description 3
- 208000012239 Developmental disease Diseases 0.000 description 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
- 208000018737 Parkinson disease Diseases 0.000 description 3
- 206010065604 Suicidal behaviour Diseases 0.000 description 3
- 238000010521 absorption reaction Methods 0.000 description 3
- 239000002253 acid Substances 0.000 description 3
- 230000003213 activating effect Effects 0.000 description 3
- 230000002411 adverse Effects 0.000 description 3
- 230000003444 anaesthetic effect Effects 0.000 description 3
- 230000000202 analgesic effect Effects 0.000 description 3
- 238000013459 approach Methods 0.000 description 3
- 230000037007 arousal Effects 0.000 description 3
- 210000004227 basal ganglia Anatomy 0.000 description 3
- 230000008901 benefit Effects 0.000 description 3
- 230000003111 delayed effect Effects 0.000 description 3
- 239000003085 diluting agent Substances 0.000 description 3
- 238000007877 drug screening Methods 0.000 description 3
- 230000008030 elimination Effects 0.000 description 3
- 238000003379 elimination reaction Methods 0.000 description 3
- 229960000450 esketamine Drugs 0.000 description 3
- 239000005090 green fluorescent protein Substances 0.000 description 3
- 238000003384 imaging method Methods 0.000 description 3
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 3
- 238000012744 immunostaining Methods 0.000 description 3
- 230000002045 lasting effect Effects 0.000 description 3
- 238000012417 linear regression Methods 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 230000001537 neural effect Effects 0.000 description 3
- 210000002569 neuron Anatomy 0.000 description 3
- 239000000546 pharmaceutical excipient Substances 0.000 description 3
- 230000003285 pharmacodynamic effect Effects 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 3
- 238000003756 stirring Methods 0.000 description 3
- 201000009032 substance abuse Diseases 0.000 description 3
- 230000005062 synaptic transmission Effects 0.000 description 3
- 239000006188 syrup Substances 0.000 description 3
- 235000020357 syrup Nutrition 0.000 description 3
- 230000000542 thalamic effect Effects 0.000 description 3
- 210000001103 thalamus Anatomy 0.000 description 3
- ZDZDSZQYRBZPNN-UHFFFAOYSA-N 4,5,6,7-tetrahydro-[1,2]oxazolo[5,4-c]pyridin-6-ium-3-olate;hydrochloride Chemical compound Cl.C1NCCC2=C1ONC2=O ZDZDSZQYRBZPNN-UHFFFAOYSA-N 0.000 description 2
- WBZFUFAFFUEMEI-UHFFFAOYSA-M Acesulfame k Chemical compound [K+].CC1=CC(=O)[N-]S(=O)(=O)O1 WBZFUFAFFUEMEI-UHFFFAOYSA-M 0.000 description 2
- 206010067484 Adverse reaction Diseases 0.000 description 2
- 208000024827 Alzheimer disease Diseases 0.000 description 2
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 description 2
- 206010010904 Convulsion Diseases 0.000 description 2
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 2
- 206010012239 Delusion Diseases 0.000 description 2
- 206010012397 Depression suicidal Diseases 0.000 description 2
- 208000001914 Fragile X syndrome Diseases 0.000 description 2
- 108010043121 Green Fluorescent Proteins Proteins 0.000 description 2
- 102000004144 Green Fluorescent Proteins Human genes 0.000 description 2
- 208000023105 Huntington disease Diseases 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 2
- 108700002232 Immediate-Early Genes Proteins 0.000 description 2
- 229930195725 Mannitol Natural products 0.000 description 2
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 description 2
- 208000019022 Mood disease Diseases 0.000 description 2
- 229920000715 Mucilage Polymers 0.000 description 2
- 239000004743 Polypropylene Substances 0.000 description 2
- 239000004372 Polyvinyl alcohol Substances 0.000 description 2
- 201000009916 Postpartum depression Diseases 0.000 description 2
- 208000028017 Psychotic disease Diseases 0.000 description 2
- 241000283984 Rodentia Species 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 229940123445 Tricyclic antidepressant Drugs 0.000 description 2
- 235000010358 acesulfame potassium Nutrition 0.000 description 2
- 229960004998 acesulfame potassium Drugs 0.000 description 2
- 239000000619 acesulfame-K Substances 0.000 description 2
- 239000000853 adhesive Substances 0.000 description 2
- 230000006838 adverse reaction Effects 0.000 description 2
- 238000013019 agitation Methods 0.000 description 2
- 238000000540 analysis of variance Methods 0.000 description 2
- 238000010171 animal model Methods 0.000 description 2
- 229940049706 benzodiazepine Drugs 0.000 description 2
- OSGAYBCDTDRGGQ-UHFFFAOYSA-L calcium sulfate Chemical compound [Ca+2].[O-]S([O-])(=O)=O OSGAYBCDTDRGGQ-UHFFFAOYSA-L 0.000 description 2
- 235000010418 carrageenan Nutrition 0.000 description 2
- 239000000679 carrageenan Substances 0.000 description 2
- 229920001525 carrageenan Polymers 0.000 description 2
- 229940113118 carrageenan Drugs 0.000 description 2
- 238000004140 cleaning Methods 0.000 description 2
- 230000007012 clinical effect Effects 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 231100000868 delusion Toxicity 0.000 description 2
- 230000000994 depressogenic effect Effects 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 238000001514 detection method Methods 0.000 description 2
- 208000035475 disorder Diseases 0.000 description 2
- 238000002001 electrophysiology Methods 0.000 description 2
- 230000007831 electrophysiology Effects 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 2
- 229960004341 escitalopram Drugs 0.000 description 2
- WSEQXVZVJXJVFP-FQEVSTJZSA-N escitalopram Chemical compound C1([C@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-FQEVSTJZSA-N 0.000 description 2
- 201000006517 essential tremor Diseases 0.000 description 2
- 230000007717 exclusion Effects 0.000 description 2
- 238000000799 fluorescence microscopy Methods 0.000 description 2
- 235000013305 food Nutrition 0.000 description 2
- 235000003599 food sweetener Nutrition 0.000 description 2
- 239000007789 gas Substances 0.000 description 2
- 230000002496 gastric effect Effects 0.000 description 2
- 210000001035 gastrointestinal tract Anatomy 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 230000036541 health Effects 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- 238000002952 image-based readout Methods 0.000 description 2
- 230000006698 induction Effects 0.000 description 2
- 230000000977 initiatory effect Effects 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 150000002500 ions Chemical class 0.000 description 2
- 230000000670 limiting effect Effects 0.000 description 2
- 239000012669 liquid formulation Substances 0.000 description 2
- 235000019359 magnesium stearate Nutrition 0.000 description 2
- 238000002595 magnetic resonance imaging Methods 0.000 description 2
- 239000000594 mannitol Substances 0.000 description 2
- 235000010355 mannitol Nutrition 0.000 description 2
- 239000012907 medicinal substance Substances 0.000 description 2
- 239000002899 monoamine oxidase inhibitor Substances 0.000 description 2
- 230000008555 neuronal activation Effects 0.000 description 2
- 239000002547 new drug Substances 0.000 description 2
- 230000001766 physiological effect Effects 0.000 description 2
- 229920001223 polyethylene glycol Polymers 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229920001155 polypropylene Polymers 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 229920002451 polyvinyl alcohol Polymers 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 238000012545 processing Methods 0.000 description 2
- 208000020016 psychiatric disease Diseases 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 102000005962 receptors Human genes 0.000 description 2
- 108020003175 receptors Proteins 0.000 description 2
- 238000005070 sampling Methods 0.000 description 2
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 2
- 230000007781 signaling event Effects 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000007909 solid dosage form Substances 0.000 description 2
- 238000007619 statistical method Methods 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 231100000736 substance abuse Toxicity 0.000 description 2
- 239000000725 suspension Substances 0.000 description 2
- 239000003765 sweetening agent Substances 0.000 description 2
- 230000008961 swelling Effects 0.000 description 2
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 2
- 210000002700 urine Anatomy 0.000 description 2
- UHVMMEOXYDMDKI-JKYCWFKZSA-L zinc;1-(5-cyanopyridin-2-yl)-3-[(1s,2s)-2-(6-fluoro-2-hydroxy-3-propanoylphenyl)cyclopropyl]urea;diacetate Chemical compound [Zn+2].CC([O-])=O.CC([O-])=O.CCC(=O)C1=CC=C(F)C([C@H]2[C@H](C2)NC(=O)NC=2N=CC(=CC=2)C#N)=C1O UHVMMEOXYDMDKI-JKYCWFKZSA-L 0.000 description 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 description 1
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 description 1
- HCYFGRCYSCXKNQ-UHFFFAOYSA-N 2-(1,3-dimethyl-2,6-dioxo-7-purinyl)acetic acid Chemical compound O=C1N(C)C(=O)N(C)C2=C1N(CC(O)=O)C=N2 HCYFGRCYSCXKNQ-UHFFFAOYSA-N 0.000 description 1
- JAHNSTQSQJOJLO-UHFFFAOYSA-N 2-(3-fluorophenyl)-1h-imidazole Chemical compound FC1=CC=CC(C=2NC=CN=2)=C1 JAHNSTQSQJOJLO-UHFFFAOYSA-N 0.000 description 1
- OZDAOHVKBFBBMZ-UHFFFAOYSA-N 2-aminopentanedioic acid;hydrate Chemical compound O.OC(=O)C(N)CCC(O)=O OZDAOHVKBFBBMZ-UHFFFAOYSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- GRFNBEZIAWKNCO-UHFFFAOYSA-N 3-pyridinol Chemical compound OC1=CC=CN=C1 GRFNBEZIAWKNCO-UHFFFAOYSA-N 0.000 description 1
- 239000003483 4 aminobutyric acid A receptor stimulating agent Substances 0.000 description 1
- UPXRTVAIJMUAQR-UHFFFAOYSA-N 4-(9h-fluoren-9-ylmethoxycarbonylamino)-1-[(2-methylpropan-2-yl)oxycarbonyl]pyrrolidine-2-carboxylic acid Chemical compound C1C(C(O)=O)N(C(=O)OC(C)(C)C)CC1NC(=O)OCC1C2=CC=CC=C2C2=CC=CC=C21 UPXRTVAIJMUAQR-UHFFFAOYSA-N 0.000 description 1
- ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 1
- TWQHGBJNKVFWIU-UHFFFAOYSA-N 8-[4-(4-quinolin-2-ylpiperazin-1-yl)butyl]-8-azaspiro[4.5]decane-7,9-dione Chemical compound C1C(=O)N(CCCCN2CCN(CC2)C=2N=C3C=CC=CC3=CC=2)C(=O)CC21CCCC2 TWQHGBJNKVFWIU-UHFFFAOYSA-N 0.000 description 1
- SKTFQHRVFFOHTQ-UHFFFAOYSA-N 8-bromo-1,3-dimethyl-7h-purine-2,6-dione Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC(Br)=N2 SKTFQHRVFFOHTQ-UHFFFAOYSA-N 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 208000007848 Alcoholism Diseases 0.000 description 1
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 206010002869 Anxiety symptoms Diseases 0.000 description 1
- 108010011485 Aspartame Proteins 0.000 description 1
- CKLJMWTZIZZHCS-UHFFFAOYSA-N Aspartic acid Chemical compound OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 description 1
- 208000020925 Bipolar disease Diseases 0.000 description 1
- 201000004569 Blindness Diseases 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- 244000298643 Cassia fistula Species 0.000 description 1
- 235000007631 Cassia fistula Nutrition 0.000 description 1
- 229920001661 Chitosan Polymers 0.000 description 1
- WBYWAXJHAXSJNI-SREVYHEPSA-N Cinnamic acid Chemical compound OC(=O)\C=C/C1=CC=CC=C1 WBYWAXJHAXSJNI-SREVYHEPSA-N 0.000 description 1
- 206010010219 Compulsions Diseases 0.000 description 1
- 229920000742 Cotton Polymers 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 206010012218 Delirium Diseases 0.000 description 1
- 206010013470 Dissociative states Diseases 0.000 description 1
- 206010013654 Drug abuse Diseases 0.000 description 1
- 208000012661 Dyskinesia Diseases 0.000 description 1
- 206010014357 Electric shock Diseases 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- OTMSDBZUPAUEDD-UHFFFAOYSA-N Ethane Chemical compound CC OTMSDBZUPAUEDD-UHFFFAOYSA-N 0.000 description 1
- 229940124602 FDA-approved drug Drugs 0.000 description 1
- 238000000729 Fisher's exact test Methods 0.000 description 1
- 229940121869 GABA A receptor agonist Drugs 0.000 description 1
- 102000005915 GABA Receptors Human genes 0.000 description 1
- 108010005551 GABA Receptors Proteins 0.000 description 1
- 239000001828 Gelatine Substances 0.000 description 1
- 241000206671 Gelidium amansii Species 0.000 description 1
- 229920002148 Gellan gum Polymers 0.000 description 1
- 102000018899 Glutamate Receptors Human genes 0.000 description 1
- 108010027915 Glutamate Receptors Proteins 0.000 description 1
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 1
- 206010018671 Grandiosity Diseases 0.000 description 1
- 229920002907 Guar gum Polymers 0.000 description 1
- 229920000569 Gum karaya Polymers 0.000 description 1
- 208000004547 Hallucinations Diseases 0.000 description 1
- 241000282412 Homo Species 0.000 description 1
- 206010020751 Hypersensitivity Diseases 0.000 description 1
- 244000211187 Lepidium sativum Species 0.000 description 1
- 235000007849 Lepidium sativum Nutrition 0.000 description 1
- 229920000161 Locust bean gum Polymers 0.000 description 1
- 240000007228 Mangifera indica Species 0.000 description 1
- 235000014826 Mangifera indica Nutrition 0.000 description 1
- 206010026749 Mania Diseases 0.000 description 1
- 244000246386 Mentha pulegium Species 0.000 description 1
- 235000016257 Mentha pulegium Nutrition 0.000 description 1
- 235000004357 Mentha x piperita Nutrition 0.000 description 1
- 229920000168 Microcrystalline cellulose Polymers 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- ILRKKHJEINIICQ-OOFFSTKBSA-N Monoammonium glycyrrhizinate Chemical compound N.O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O ILRKKHJEINIICQ-OOFFSTKBSA-N 0.000 description 1
- 101100381510 Mus musculus Bcl10 gene Proteins 0.000 description 1
- 240000008790 Musa x paradisiaca Species 0.000 description 1
- 235000018290 Musa x paradisiaca Nutrition 0.000 description 1
- 208000008238 Muscle Spasticity Diseases 0.000 description 1
- 102000004868 N-Methyl-D-Aspartate Receptors Human genes 0.000 description 1
- 108090001041 N-Methyl-D-Aspartate Receptors Proteins 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 238000005481 NMR spectroscopy Methods 0.000 description 1
- 208000012902 Nervous system disease Diseases 0.000 description 1
- 208000025966 Neurological disease Diseases 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- BRUQQQPBMZOVGD-XFKAJCMBSA-N Oxycodone Chemical compound O=C([C@@H]1O2)CC[C@@]3(O)[C@H]4CC5=CC=C(OC)C2=C5[C@@]13CCN4C BRUQQQPBMZOVGD-XFKAJCMBSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 1
- 239000002202 Polyethylene glycol Substances 0.000 description 1
- 208000027030 Premenstrual dysphoric disease Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 241000206572 Rhodophyta Species 0.000 description 1
- 241000934878 Sterculia Species 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- 230000002159 abnormal effect Effects 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 229950003769 acefylline Drugs 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 239000002671 adjuvant Substances 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 239000000556 agonist Substances 0.000 description 1
- 201000007930 alcohol dependence Diseases 0.000 description 1
- 235000010443 alginic acid Nutrition 0.000 description 1
- 239000000783 alginic acid Substances 0.000 description 1
- 229920000615 alginic acid Polymers 0.000 description 1
- 229960001126 alginic acid Drugs 0.000 description 1
- 150000004781 alginic acids Chemical class 0.000 description 1
- 208000030961 allergic reaction Diseases 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 description 1
- 210000003484 anatomy Anatomy 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 239000000730 antalgic agent Substances 0.000 description 1
- 230000003466 anti-cipated effect Effects 0.000 description 1
- 239000000164 antipsychotic agent Substances 0.000 description 1
- 229940005529 antipsychotics Drugs 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 229940005530 anxiolytics Drugs 0.000 description 1
- 230000001174 ascending effect Effects 0.000 description 1
- 239000000605 aspartame Substances 0.000 description 1
- 229960003438 aspartame Drugs 0.000 description 1
- 235000010357 aspartame Nutrition 0.000 description 1
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- 229940092714 benzenesulfonic acid Drugs 0.000 description 1
- 150000001557 benzodiazepines Chemical class 0.000 description 1
- WPYMKLBDIGXBTP-UHFFFAOYSA-N benzoic acid group Chemical group C(C1=CC=CC=C1)(=O)O WPYMKLBDIGXBTP-UHFFFAOYSA-N 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 229920001222 biopolymer Polymers 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 230000036772 blood pressure Effects 0.000 description 1
- 208000030963 borderline personality disease Diseases 0.000 description 1
- 230000007177 brain activity Effects 0.000 description 1
- 210000005013 brain tissue Anatomy 0.000 description 1
- AURFZBICLPNKBZ-SYBPFIFISA-N brexanolone Chemical compound C([C@@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)C)[C@@]2(C)CC1 AURFZBICLPNKBZ-SYBPFIFISA-N 0.000 description 1
- 229950009652 brexanolone Drugs 0.000 description 1
- 238000011094 buffer selection Methods 0.000 description 1
- 229910000019 calcium carbonate Inorganic materials 0.000 description 1
- 235000010216 calcium carbonate Nutrition 0.000 description 1
- 235000011132 calcium sulphate Nutrition 0.000 description 1
- 238000004364 calculation method Methods 0.000 description 1
- 230000002802 cardiorespiratory effect Effects 0.000 description 1
- 239000002771 cell marker Substances 0.000 description 1
- 230000001413 cellular effect Effects 0.000 description 1
- 238000000546 chi-square test Methods 0.000 description 1
- HNEGQIOMVPPMNR-IHWYPQMZSA-N citraconic acid Chemical compound OC(=O)C(/C)=C\C(O)=O HNEGQIOMVPPMNR-IHWYPQMZSA-N 0.000 description 1
- 238000011260 co-administration Methods 0.000 description 1
- 239000008199 coating composition Substances 0.000 description 1
- 235000009508 confectionery Nutrition 0.000 description 1
- 238000012790 confirmation Methods 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 230000002596 correlated effect Effects 0.000 description 1
- 239000002537 cosmetic Substances 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 238000009109 curative therapy Methods 0.000 description 1
- WZHCOOQXZCIUNC-UHFFFAOYSA-N cyclandelate Chemical compound C1C(C)(C)CC(C)CC1OC(=O)C(O)C1=CC=CC=C1 WZHCOOQXZCIUNC-UHFFFAOYSA-N 0.000 description 1
- 238000009792 diffusion process Methods 0.000 description 1
- FSBVERYRVPGNGG-UHFFFAOYSA-N dimagnesium dioxido-bis[[oxido(oxo)silyl]oxy]silane hydrate Chemical compound O.[Mg+2].[Mg+2].[O-][Si](=O)O[Si]([O-])([O-])O[Si]([O-])=O FSBVERYRVPGNGG-UHFFFAOYSA-N 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 239000007884 disintegrant Substances 0.000 description 1
- 238000004090 dissolution Methods 0.000 description 1
- 231100000673 dose–response relationship Toxicity 0.000 description 1
- 229940000406 drug candidate Drugs 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000009509 drug development Methods 0.000 description 1
- 230000008482 dysregulation Effects 0.000 description 1
- 208000024732 dysthymic disease Diseases 0.000 description 1
- 238000000537 electroencephalography Methods 0.000 description 1
- 239000003623 enhancer Substances 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
- 210000003238 esophagus Anatomy 0.000 description 1
- 238000011156 evaluation Methods 0.000 description 1
- 230000002964 excitative effect Effects 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 239000000945 filler Substances 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 235000019634 flavors Nutrition 0.000 description 1
- 238000003682 fluorination reaction Methods 0.000 description 1
- 238000012048 forced swim test Methods 0.000 description 1
- 108700025906 fos Genes Proteins 0.000 description 1
- 238000004108 freeze drying Methods 0.000 description 1
- 210000005153 frontal cortex Anatomy 0.000 description 1
- 238000002599 functional magnetic resonance imaging Methods 0.000 description 1
- 230000003371 gabaergic effect Effects 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 238000001879 gelation Methods 0.000 description 1
- 235000010492 gellan gum Nutrition 0.000 description 1
- 239000000216 gellan gum Substances 0.000 description 1
- 239000003349 gelling agent Substances 0.000 description 1
- 235000021474 generally recognized As safe (food) Nutrition 0.000 description 1
- 235000021473 generally recognized as safe (food ingredients) Nutrition 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 230000000848 glutamatergic effect Effects 0.000 description 1
- 229920000578 graft copolymer Polymers 0.000 description 1
- 235000010417 guar gum Nutrition 0.000 description 1
- 239000000665 guar gum Substances 0.000 description 1
- 229960002154 guar gum Drugs 0.000 description 1
- 210000003128 head Anatomy 0.000 description 1
- 229920000669 heparin Polymers 0.000 description 1
- ZFGMDIBRIDKWMY-PASTXAENSA-N heparin Chemical compound CC(O)=N[C@@H]1[C@@H](O)[C@H](O)[C@@H](COS(O)(=O)=O)O[C@@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O[C@H]2[C@@H]([C@@H](OS(O)(=O)=O)[C@@H](O[C@@H]3[C@@H](OC(O)[C@H](OS(O)(=O)=O)[C@H]3O)C(O)=O)O[C@@H]2O)CS(O)(=O)=O)[C@H](O)[C@H]1O ZFGMDIBRIDKWMY-PASTXAENSA-N 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 1
- 235000001050 hortel pimenta Nutrition 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 210000003016 hypothalamus Anatomy 0.000 description 1
- 238000012151 immunohistochemical method Methods 0.000 description 1
- 238000007901 in situ hybridization Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000005462 in vivo assay Methods 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 238000010988 intraclass correlation coefficient Methods 0.000 description 1
- 238000007918 intramuscular administration Methods 0.000 description 1
- 235000010494 karaya gum Nutrition 0.000 description 1
- 239000000231 karaya gum Substances 0.000 description 1
- 229940039371 karaya gum Drugs 0.000 description 1
- 229960004184 ketamine hydrochloride Drugs 0.000 description 1
- 230000006651 lactation Effects 0.000 description 1
- 229960001021 lactose monohydrate Drugs 0.000 description 1
- 229950003165 lanicemine Drugs 0.000 description 1
- 229940069445 licorice extract Drugs 0.000 description 1
- 239000002502 liposome Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 235000010420 locust bean gum Nutrition 0.000 description 1
- 239000000711 locust bean gum Substances 0.000 description 1
- 238000007477 logistic regression Methods 0.000 description 1
- 229940031703 low substituted hydroxypropyl cellulose Drugs 0.000 description 1
- 238000010801 machine learning Methods 0.000 description 1
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 description 1
- 239000001095 magnesium carbonate Substances 0.000 description 1
- 229910000021 magnesium carbonate Inorganic materials 0.000 description 1
- 235000014380 magnesium carbonate Nutrition 0.000 description 1
- 239000000391 magnesium silicate Substances 0.000 description 1
- 235000019793 magnesium trisilicate Nutrition 0.000 description 1
- 229940099273 magnesium trisilicate Drugs 0.000 description 1
- 229910000386 magnesium trisilicate Inorganic materials 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 238000013507 mapping Methods 0.000 description 1
- 239000003550 marker Substances 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 238000007909 melt granulation Methods 0.000 description 1
- 230000006996 mental state Effects 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 239000004530 micro-emulsion Substances 0.000 description 1
- 235000019813 microcrystalline cellulose Nutrition 0.000 description 1
- 239000008108 microcrystalline cellulose Substances 0.000 description 1
- 229940016286 microcrystalline cellulose Drugs 0.000 description 1
- DDLIGBOFAVUZHB-UHFFFAOYSA-N midazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NC=C2CN=C1C1=CC=CC=C1F DDLIGBOFAVUZHB-UHFFFAOYSA-N 0.000 description 1
- 229960003793 midazolam Drugs 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 238000002156 mixing Methods 0.000 description 1
- 238000012544 monitoring process Methods 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- LNOPIUAQISRISI-UHFFFAOYSA-N n'-hydroxy-2-propan-2-ylsulfonylethanimidamide Chemical compound CC(C)S(=O)(=O)CC(N)=NO LNOPIUAQISRISI-UHFFFAOYSA-N 0.000 description 1
- 239000007908 nanoemulsion Substances 0.000 description 1
- 210000003928 nasal cavity Anatomy 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 description 1
- 230000002474 noradrenergic effect Effects 0.000 description 1
- 229960002748 norepinephrine Drugs 0.000 description 1
- SFLSHLFXELFNJZ-UHFFFAOYSA-N norepinephrine Natural products NCC(O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-UHFFFAOYSA-N 0.000 description 1
- 229940127221 norepinephrine reuptake inhibitor Drugs 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- 229940100691 oral capsule Drugs 0.000 description 1
- 230000008520 organization Effects 0.000 description 1
- 229960002085 oxycodone Drugs 0.000 description 1
- 238000007427 paired t-test Methods 0.000 description 1
- 239000002245 particle Substances 0.000 description 1
- 230000035515 penetration Effects 0.000 description 1
- 239000007967 peppermint flavor Substances 0.000 description 1
- 230000002085 persistent effect Effects 0.000 description 1
- 238000011458 pharmacological treatment Methods 0.000 description 1
- 210000003800 pharynx Anatomy 0.000 description 1
- 238000009520 phase I clinical trial Methods 0.000 description 1
- 238000009521 phase II clinical trial Methods 0.000 description 1
- 229940023488 pill Drugs 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229920000728 polyester Polymers 0.000 description 1
- 229920001282 polysaccharide Polymers 0.000 description 1
- 239000005017 polysaccharide Substances 0.000 description 1
- 150000004804 polysaccharides Chemical class 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 229940126027 positive allosteric modulator Drugs 0.000 description 1
- 230000008092 positive effect Effects 0.000 description 1
- 230000035935 pregnancy Effects 0.000 description 1
- 230000002035 prolonged effect Effects 0.000 description 1
- 229940001470 psychoactive drug Drugs 0.000 description 1
- 230000002385 psychotomimetic effect Effects 0.000 description 1
- 239000004089 psychotropic agent Substances 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 238000011002 quantification Methods 0.000 description 1
- 229940121896 radiopharmaceutical Drugs 0.000 description 1
- 239000012217 radiopharmaceutical Substances 0.000 description 1
- 230000002799 radiopharmaceutical effect Effects 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 238000011084 recovery Methods 0.000 description 1
- 230000007115 recruitment Effects 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 239000011347 resin Substances 0.000 description 1
- 229920005989 resin Polymers 0.000 description 1
- 230000036387 respiratory rate Effects 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 235000002020 sage Nutrition 0.000 description 1
- 201000000980 schizophrenia Diseases 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 229940076279 serotonin Drugs 0.000 description 1
- 239000003772 serotonin uptake inhibitor Substances 0.000 description 1
- 210000002966 serum Anatomy 0.000 description 1
- 230000035939 shock Effects 0.000 description 1
- 238000002633 shock therapy Methods 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 230000000392 somatic effect Effects 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 235000010356 sorbitol Nutrition 0.000 description 1
- 208000018198 spasticity Diseases 0.000 description 1
- 230000003595 spectral effect Effects 0.000 description 1
- 238000001694 spray drying Methods 0.000 description 1
- 238000010561 standard procedure Methods 0.000 description 1
- 239000000021 stimulant Substances 0.000 description 1
- 238000013517 stratification Methods 0.000 description 1
- 238000000859 sublimation Methods 0.000 description 1
- 230000008022 sublimation Effects 0.000 description 1
- 201000006152 substance dependence Diseases 0.000 description 1
- 230000009747 swallowing Effects 0.000 description 1
- 230000001360 synchronised effect Effects 0.000 description 1
- 230000009897 systematic effect Effects 0.000 description 1
- 230000009885 systemic effect Effects 0.000 description 1
- 238000012353 t test Methods 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 238000010998 test method Methods 0.000 description 1
- 239000010409 thin film Substances 0.000 description 1
- 229940098465 tincture Drugs 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
- 231100000440 toxicity profile Toxicity 0.000 description 1
- 230000007704 transition Effects 0.000 description 1
- 238000011277 treatment modality Methods 0.000 description 1
- 230000036325 urinary excretion Effects 0.000 description 1
- 238000010200 validation analysis Methods 0.000 description 1
- 230000017260 vegetative to reproductive phase transition of meristem Effects 0.000 description 1
- 210000001030 ventral striatum Anatomy 0.000 description 1
- 239000000341 volatile oil Substances 0.000 description 1
- 230000002747 voluntary effect Effects 0.000 description 1
- 229920001285 xanthan gum Polymers 0.000 description 1
- 235000010493 xanthan gum Nutrition 0.000 description 1
- 239000000230 xanthan gum Substances 0.000 description 1
- 229940082509 xanthan gum Drugs 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
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
- A61K31/33—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
- A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
-
- 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
-
- 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
- A61P25/24—Antidepressants
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862770287P | 2018-11-21 | 2018-11-21 | |
| US62/770,287 | 2018-11-21 | ||
| PCT/US2019/062554 WO2020106927A1 (en) | 2018-11-21 | 2019-11-21 | Gaboxadol for reducing risk of suicide and rapid relief of depression |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112021009944A2 true BR112021009944A2 (pt) | 2021-08-17 |
Family
ID=70728606
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112021009944-1A BR112021009944A2 (pt) | 2018-11-21 | 2019-11-21 | gaboxadol para reduzir risco de suicídio e alívio rápido de depressão |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US20220008398A1 (https=) |
| EP (1) | EP3883566A4 (https=) |
| JP (1) | JP2022514194A (https=) |
| KR (1) | KR20210110585A (https=) |
| CN (1) | CN113395962A (https=) |
| AU (1) | AU2019384157A1 (https=) |
| BR (1) | BR112021009944A2 (https=) |
| CA (1) | CA3120856A1 (https=) |
| GB (1) | GB2594616A (https=) |
| IL (1) | IL283311A (https=) |
| MX (1) | MX2021005992A (https=) |
| SG (1) | SG11202105358RA (https=) |
| WO (1) | WO2020106927A1 (https=) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2882708A1 (en) | 2012-08-21 | 2014-02-27 | Sage Therapeutics, Inc. | Methods of treating epilepsy or status epilepticus |
| JOP20200195A1 (ar) | 2014-09-08 | 2017-06-16 | Sage Therapeutics Inc | سترويدات وتركيبات نشطة عصبياً، واستخداماتها |
| KR20240157128A (ko) | 2016-03-08 | 2024-10-31 | 세이지 테라퓨틱스, 인크. | 신경활성 스테로이드, 조성물, 및 그의 용도 |
| EP3481387A4 (en) * | 2016-08-11 | 2020-04-08 | Ovid Therapeutics Inc | METHOD AND COMPOSITIONS FOR TREATING EPILEPTIC DISEASES |
| US10071083B2 (en) * | 2017-02-03 | 2018-09-11 | Ovid Therapeutics Inc | Use of gaboxadol in the treatment of tinnitus |
| ES2907692T3 (es) | 2017-12-29 | 2022-04-26 | Celon Pharma Sa | Composición de ketamina de polvo seco para su administración por vía pulmonar en la depresión resistente al tratamiento |
| JP2022514194A (ja) * | 2018-11-21 | 2022-02-10 | セルテゴ セラピューティクス インコーポレイテッド | 自殺のリスクを低減し、うつ病を迅速に軽減するためのガボキサドール |
| MX2022014599A (es) | 2020-05-20 | 2022-12-16 | Certego Therapeutics Inc | Gaboxadol deuterado en anillo y su uso para el tratamiento de trastornos psiquiatricos. |
| JP2024020037A (ja) * | 2022-08-01 | 2024-02-14 | 学校法人順天堂 | 痛みと痒みのバイオマーカー |
Family Cites Families (60)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK270378A (da) | 1977-06-20 | 1978-12-21 | Krogsgaard Larsen P | Isoxazolderivater |
| US4362731A (en) | 1980-09-01 | 1982-12-07 | Sandoz Ltd. | Myotonolytic use of 4,5,6,7-tetrahydroisoxazolo [5,4-c] pyridin-3-ol and derivatives thereof |
| US4353910A (en) | 1981-11-27 | 1982-10-12 | Kefalas A/S | Derivatives of 4,5,6,7-tetrahydroisoxazolo [5,4-c] pyridine-3-one, pharmaceutical compositions and methods of treatment |
| DE19525598C2 (de) | 1995-07-13 | 1997-09-25 | Max Planck Gesellschaft | Schlafmittel |
| AR031473A1 (es) | 2000-11-20 | 2003-09-24 | Lundbeck & Co As H | Intensificadores de gaba en el tratamiento de enfermedades relacionadas con una reducida actividad neuroesteroide |
| US20020165217A1 (en) | 2001-05-01 | 2002-11-07 | Pfizer Inc. | Combination treatment for anxiety and depression |
| CL2004001603A1 (es) | 2003-06-25 | 2005-05-27 | Lundbeck & Co As H | Uso de gabaxadol para preparar un medicamento util para el tratamiento del dolor neuropatico. |
| TW200509918A (en) | 2003-06-25 | 2005-03-16 | Lundbeck & Co As H | Treatment of depression and other affective disorders |
| TW200501951A (en) | 2003-06-25 | 2005-01-16 | Lundbeck & Co As H | Treatment of neuropathic pain, fibromyalgia or rheumatoid arthritis |
| BRPI0410857A (pt) | 2003-06-25 | 2006-07-04 | Lundbeck & Co As H | método para o tratamento de depressão, uso de gaboxadol, e, composição farmacêutica |
| US20050234093A1 (en) | 2003-06-25 | 2005-10-20 | H. Lundbeck A/S | Treatment of depression and other affective disorders |
| AR045540A1 (es) | 2003-09-05 | 2005-11-02 | Lundbeck & Co As H | Metodo de elaboracion de 4,5,6,7 tetrahidroisoxazol [5,4-c] piridin-3-ol (thip) |
| UY28650A1 (es) * | 2003-12-05 | 2005-02-28 | Forest Laboratories | Memantina para la prevencion o disminucion de la conducta suicida y para el tratamiento de la depresion mayor asociada con esta conducta |
| US20050137222A1 (en) | 2003-12-18 | 2005-06-23 | H. Lundbeck A/S | Treatment of insomnia in human patients |
| GB0402118D0 (en) | 2004-01-30 | 2004-03-03 | Merck Sharp & Dohme | Polymorphic forms of a GABAA agonist |
| JP2007530604A (ja) | 2004-04-02 | 2007-11-01 | ハー・ルンドベック・アクチエゼルスカベット | 呼吸機能障害の治療 |
| ZA200607427B (en) | 2004-04-02 | 2009-02-25 | Lundbeck & Co As H | Treatment of impaired respiratory function with gaboxadol |
| GB0417558D0 (en) | 2004-08-06 | 2004-09-08 | Merck Sharp & Dohme | Novel combination therapy |
| EP1848420A4 (en) | 2005-01-28 | 2008-01-23 | Merck & Co Inc | POLYMORPH SHAPES OF A GABAA AGONIST |
| US20080262029A1 (en) | 2005-04-29 | 2008-10-23 | H. Lundbeck A/S | Acid and Base Salt Forms of Gaboxadol |
| DE102005020882A1 (de) | 2005-05-04 | 2006-11-09 | Dömling, Alexander, Dr. | Verwendung von Gaboxadol und Derivaten zur Behandlung von Kinase-induzierten Krankheiten |
| FR2889811B1 (fr) | 2005-08-19 | 2009-10-09 | Sanofi Aventis Sa | Association d'un agent hypnotique a duree d'action longue et d'un agent hypnotique a duree d'action courte, composition pharmaceutique la contenant et son application en therapeutique. |
| AU2007229866A1 (en) * | 2006-03-22 | 2007-10-04 | Mount Sinai School Of Medicine | Intranasal administration of ketamine to treat depression |
| US20080159958A1 (en) | 2006-12-27 | 2008-07-03 | Abbott Laboratories | Determination of histamine-3 bioactivity |
| TW200920358A (en) | 2007-08-13 | 2009-05-16 | Lundbeck & Co As H | Method of treating stress-mediated depression |
| US20090048288A1 (en) | 2007-08-13 | 2009-02-19 | H. Lundbeck A/S | Method of treating stress-mediated depression |
| US20090143335A1 (en) | 2007-10-29 | 2009-06-04 | H. Lundbeck A/S | Modified absorption formulation of gaboxadol |
| GB0810063D0 (en) | 2008-06-03 | 2008-07-09 | Renovo Ltd | Medicaments and methods for inhibition of scarring |
| EP2334299A1 (en) | 2008-09-01 | 2011-06-22 | H. Lundbeck A/S | Pharmaceutical composition comprising gaboxadol and an inhibitor of patl or oat |
| US11083732B2 (en) | 2014-03-31 | 2021-08-10 | University Of Maryland, Baltimore | Use of negative modulators of GABA receptors containing alpha5 subunits as fast acting antidepressants |
| WO2015171547A1 (en) | 2014-05-05 | 2015-11-12 | Ovid Therapeutics Inc. | Methods of treating cognitive impairment associated with neurodegenerative disorders |
| RS62007B1 (sr) | 2014-06-06 | 2021-07-30 | Ovid Therapeutics Inc | Postupci pojačavanja tonične inhibicije i lečenja angelmanovog sindroma |
| US20170304358A1 (en) | 2014-10-06 | 2017-10-26 | Seyyed Nassir GHAEMI | Primary and secondary prevention of dementias and suicide with trace dose lithium |
| LT3274331T (lt) | 2015-03-24 | 2020-04-10 | H. Lundbeck A/S | 4,5,6,7-tetrahidroizozaksolo[5,4-c]piridin-3-olio gamybos būdas |
| WO2016176609A1 (en) | 2015-04-30 | 2016-11-03 | Ovid Therapeutics Inc | Methods of treating prader-willi syndrome |
| US20170348232A1 (en) | 2016-06-07 | 2017-12-07 | Ovid Therapeutics Inc. | Formulations of gaboxadol for treatment of angelman syndrome, fragile x syndrome and fragile x-associated tremor/ataxia syndrome |
| AR105378A1 (es) | 2015-07-17 | 2017-09-27 | Ovid Therapeutics Inc | Métodos de tratamiento de trastornos del desarrollo con gaboxadol |
| EP4541420A3 (en) | 2015-07-17 | 2025-06-25 | Ovid Therapeutics Inc. | Methods of treating developmental disorders with gaboxadol |
| US9682069B2 (en) | 2015-07-17 | 2017-06-20 | Ovid Therapeutics Inc | Methods of treating Dravet syndrome |
| AR105670A1 (es) | 2015-08-11 | 2017-10-25 | Ovid Therapeutics Inc | Métodos de sedación parenteral para usar durante el tratamiento de cuidados intensivos |
| US9399034B1 (en) | 2015-08-11 | 2016-07-26 | Ovid Therapeutics Inc | Methods of sedation during critical care treatment |
| WO2017027249A1 (en) * | 2015-08-11 | 2017-02-16 | Ovid Therapeutics Inc. | Methods of sedation and parenteral formulation for use during critical care treatment |
| JP6857647B2 (ja) | 2015-08-11 | 2021-04-14 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | クリティカル・ケア処置中に用いるための鎮静方法および非経腸製剤 |
| US9351968B1 (en) | 2015-09-09 | 2016-05-31 | Ovid Therapeutics Inc | Methods of treating developmental disorders using pipradrol |
| US20170119704A1 (en) | 2015-10-13 | 2017-05-04 | Ovid Therapeutics Inc. | Treatment of cognitive impairment |
| WO2017205606A1 (en) | 2016-05-26 | 2017-11-30 | Ovid Therapeutics Inc. | Methods of treating behavioral syndromes using pipradrol |
| EP3481387A4 (en) | 2016-08-11 | 2020-04-08 | Ovid Therapeutics Inc | METHOD AND COMPOSITIONS FOR TREATING EPILEPTIC DISEASES |
| CN110225754A (zh) | 2016-11-22 | 2019-09-10 | 奥维德医疗公司 | 用氟吡汀治疗发育障碍和/或癫痫发作紊乱的方法 |
| US10737984B2 (en) | 2016-11-30 | 2020-08-11 | Hrl Laboratories, Llc | Formulations and methods for 3D printing of ceramic matrix composites |
| US10071083B2 (en) | 2017-02-03 | 2018-09-11 | Ovid Therapeutics Inc | Use of gaboxadol in the treatment of tinnitus |
| CN110621318A (zh) | 2017-03-15 | 2019-12-27 | 奥维德医疗公司 | 排他地由设计者药物激活的设计者受体在治疗癫痫发作紊乱中的用途 |
| US20180338959A1 (en) | 2017-05-24 | 2018-11-29 | Ovid Therapeutics Inc. | Treatment of depressive disorders |
| WO2018222957A1 (en) | 2017-06-01 | 2018-12-06 | Ovid Therapeutics Inc. | Treatment of developmental disorders with imidazolone derivatives |
| WO2019006161A1 (en) | 2017-06-28 | 2019-01-03 | Ovid Therapeutics Inc. | TREATMENT OF DEVELOPMENT SYNDROMES |
| JP2020529440A (ja) | 2017-08-04 | 2020-10-08 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | 糖尿病および関連する状態の処置におけるガボキサドールの使用 |
| AU2018320849A1 (en) | 2017-08-25 | 2020-03-05 | Ovid Therapeutics Inc. | Recombinant adeno-associated vectors |
| JP2020533415A (ja) | 2017-09-12 | 2020-11-19 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | ナルコレプシーの処置におけるガボキサドールの使用 |
| CN107595850A (zh) | 2017-10-25 | 2018-01-19 | 桂林浩新科技服务有限公司 | 一种有效提高睡眠质量的药物组合物及其用途 |
| JP2021521103A (ja) | 2018-04-06 | 2021-08-26 | オービッド・セラピューティクス・インコーポレイテッドＯｖｉｄ Ｔｈｅｒａｐｅｕｔｉｃｓ Ｉｎｃ． | 物質使用障害の処置におけるガボキサドールの使用 |
| JP2022514194A (ja) * | 2018-11-21 | 2022-02-10 | セルテゴ セラピューティクス インコーポレイテッド | 自殺のリスクを低減し、うつ病を迅速に軽減するためのガボキサドール |
-
2019
- 2019-11-21 JP JP2021529111A patent/JP2022514194A/ja active Pending
- 2019-11-21 US US17/295,845 patent/US20220008398A1/en not_active Abandoned
- 2019-11-21 CN CN201980089656.6A patent/CN113395962A/zh active Pending
- 2019-11-21 SG SG11202105358RA patent/SG11202105358RA/en unknown
- 2019-11-21 BR BR112021009944-1A patent/BR112021009944A2/pt not_active IP Right Cessation
- 2019-11-21 AU AU2019384157A patent/AU2019384157A1/en not_active Abandoned
- 2019-11-21 US US16/691,049 patent/US11123332B2/en not_active Expired - Fee Related
- 2019-11-21 KR KR1020217019089A patent/KR20210110585A/ko not_active Ceased
- 2019-11-21 CA CA3120856A patent/CA3120856A1/en active Pending
- 2019-11-21 MX MX2021005992A patent/MX2021005992A/es unknown
- 2019-11-21 EP EP19886329.2A patent/EP3883566A4/en not_active Withdrawn
- 2019-11-21 WO PCT/US2019/062554 patent/WO2020106927A1/en not_active Ceased
- 2019-11-21 GB GB2108720.0A patent/GB2594616A/en not_active Withdrawn
-
2021
- 2021-04-02 US US17/221,178 patent/US20220054461A1/en not_active Abandoned
- 2021-05-20 IL IL283311A patent/IL283311A/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| GB202108720D0 (en) | 2021-08-04 |
| US20200155522A1 (en) | 2020-05-21 |
| JP2022514194A (ja) | 2022-02-10 |
| KR20210110585A (ko) | 2021-09-08 |
| US20220054461A1 (en) | 2022-02-24 |
| AU2019384157A1 (en) | 2021-06-17 |
| US20220008398A1 (en) | 2022-01-13 |
| CA3120856A1 (en) | 2020-05-28 |
| CN113395962A (zh) | 2021-09-14 |
| EP3883566A1 (en) | 2021-09-29 |
| GB2594616A (en) | 2021-11-03 |
| WO2020106927A1 (en) | 2020-05-28 |
| SG11202105358RA (en) | 2021-06-29 |
| IL283311A (en) | 2021-07-29 |
| US11123332B2 (en) | 2021-09-21 |
| MX2021005992A (es) | 2021-09-14 |
| EP3883566A4 (en) | 2022-09-07 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| US11123332B2 (en) | Gaboxadol for reducing risk of suicide and rapid relief of depression | |
| AU2024227357A1 (en) | Ganaxolone For Use In Treating Genetic Epileptic Disorders | |
| US11918551B2 (en) | Methods of treating seizure disorders and Prader-Willi syndrome | |
| US11597726B2 (en) | Ring deuterated gaboxadol and its use for the treatment of psychiatric disorders | |
| BR112020011345A2 (pt) | tratamento com ciclobenzaprina para agitação, psicose e declínio cognitivo na demência e condições neurodegenerativas | |
| BR112021000768A2 (pt) | uso de pró-medicamentos de riluzol para tratar a doença de alzheimer | |
| BR112021011386A2 (pt) | Deutetrabenazina para o tratamento da discinesia na paralisia cerebral | |
| HK40061974A (en) | Gaboxadol for reducing risk of suicide and rapid relief of depression | |
| HK40051546A (en) | Gaboxadol for reducing risk of suicide and rapid relief of depression | |
| JP2022511755A (ja) | 精神障害の治療のためのガボキサドールとリチウムとの組み合わせ | |
| EA052165B1 (ru) | Ганаксолон для использования в лечении наследственных эпилептических заболеваний | |
| HK40016106A (en) | Methods of treating seizure disorders and prader-willi syndrome | |
| Lalasa et al. | Psychopharmacology of schizophrenia |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] | ||
| B08F | Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette] |
Free format text: REFERENTE A 5A ANUIDADE. |
|
| B08K | Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette] |
Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2802 DE 17/09/2024. |