JP2015516395A5 - - Google Patents
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- JP2015516395A5 JP2015516395A5 JP2015505971A JP2015505971A JP2015516395A5 JP 2015516395 A5 JP2015516395 A5 JP 2015516395A5 JP 2015505971 A JP2015505971 A JP 2015505971A JP 2015505971 A JP2015505971 A JP 2015505971A JP 2015516395 A5 JP2015516395 A5 JP 2015516395A5
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- Prior art keywords
- pharmaceutical composition
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- 239000008194 pharmaceutical composition Substances 0.000 claims 24
- 150000001875 compounds Chemical class 0.000 claims 12
- 239000003772 serotonin uptake inhibitor Substances 0.000 claims 7
- 230000001430 anti-depressive Effects 0.000 claims 6
- 239000000935 antidepressant agent Substances 0.000 claims 6
- 239000000556 agonist Substances 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 5
- 229940005513 ANTIDEPRESSANTS Drugs 0.000 claims 4
- -1 Indiana Pron Chemical compound 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 229960005426 Doxepin Drugs 0.000 claims 3
- ODQWQRRAPPTVAG-GZTJUZNOSA-N Doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 claims 3
- 206010061215 Impulse-control disease Diseases 0.000 claims 3
- RONZAEMNMFQXRA-UHFFFAOYSA-N Mirtazapine Chemical compound C1C2=CC=CN=C2N2CCN(C)CC2C2=CC=CC=C21 RONZAEMNMFQXRA-UHFFFAOYSA-N 0.000 claims 3
- VRBKIVRKKCLPHA-UHFFFAOYSA-N Nefazodone Chemical compound O=C1N(CCOC=2C=CC=CC=2)C(CC)=NN1CCCN(CC1)CCN1C1=CC=CC(Cl)=C1 VRBKIVRKKCLPHA-UHFFFAOYSA-N 0.000 claims 3
- YLXDSYKOBKBWJQ-LBPRGKRZSA-N Ramelteon Chemical compound C1=C2OCCC2=C2[C@H](CCNC(=O)CC)CCC2=C1 YLXDSYKOBKBWJQ-LBPRGKRZSA-N 0.000 claims 3
- 229960003991 Trazodone Drugs 0.000 claims 3
- PHLBKPHSAVXXEF-UHFFFAOYSA-N Trazodone Chemical compound ClC1=CC=CC(N2CCN(CCCN3C(N4C=CC=CC4=N3)=O)CC2)=C1 PHLBKPHSAVXXEF-UHFFFAOYSA-N 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 230000000051 modifying Effects 0.000 claims 3
- 229960001800 nefazodone Drugs 0.000 claims 3
- 150000003839 salts Chemical group 0.000 claims 3
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 3
- 239000003775 serotonin noradrenalin reuptake inhibitor Substances 0.000 claims 3
- AELCINSCMGFISI-DTWKUNHWSA-N (1R,2S)-2-phenylcyclopropan-1-amine Chemical compound N[C@@H]1C[C@H]1C1=CC=CC=C1 AELCINSCMGFISI-DTWKUNHWSA-N 0.000 claims 2
- 229960000836 Amitriptyline Drugs 0.000 claims 2
- KRMDCWKBEZIMAB-UHFFFAOYSA-N Amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 claims 2
- 229960002519 Amoxapine Drugs 0.000 claims 2
- QWGDMFLQWFTERH-UHFFFAOYSA-N Amoxapine Chemical compound C12=CC(Cl)=CC=C2OC2=CC=CC=C2N=C1N1CCNCC1 QWGDMFLQWFTERH-UHFFFAOYSA-N 0.000 claims 2
- 229960001058 Bupropion Drugs 0.000 claims 2
- SNPPWIUOZRMYNY-UHFFFAOYSA-N Bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 claims 2
- WSEQXVZVJXJVFP-UHFFFAOYSA-N Citalopram Chemical compound O1CC2=CC(C#N)=CC=C2C1(CCCN(C)C)C1=CC=C(F)C=C1 WSEQXVZVJXJVFP-UHFFFAOYSA-N 0.000 claims 2
- GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 claims 2
- HCYAFALTSJYZDH-UHFFFAOYSA-N Desimpramine Chemical compound C1CC2=CC=CC=C2N(CCCNC)C2=CC=CC=C21 HCYAFALTSJYZDH-UHFFFAOYSA-N 0.000 claims 2
- ZEUITGRIYCTCEM-KRWDZBQOSA-N Duloxetine Chemical compound C1([C@@H](OC=2C3=CC=CC=C3C=CC=2)CCNC)=CC=CS1 ZEUITGRIYCTCEM-KRWDZBQOSA-N 0.000 claims 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 claims 2
- GBBSUAFBMRNDJC-INIZCTEOSA-N Eszopiclone Chemical compound C1CN(C)CCN1C(=O)O[C@H]1C2=NC=CN=C2C(=O)N1C1=CC=C(Cl)C=N1 GBBSUAFBMRNDJC-INIZCTEOSA-N 0.000 claims 2
- 229960002464 Fluoxetine Drugs 0.000 claims 2
- 229960004038 Fluvoxamine Drugs 0.000 claims 2
- BCGWQEUPMDMJNV-UHFFFAOYSA-N Imipramine Chemical compound C1CC2=CC=CC=C2N(CCCN(C)C)C2=CC=CC=C21 BCGWQEUPMDMJNV-UHFFFAOYSA-N 0.000 claims 2
- XKFPYPQQHFEXRZ-UHFFFAOYSA-N Isocarboxazid Chemical compound O1C(C)=CC(C(=O)NNCC=2C=CC=CC=2)=N1 XKFPYPQQHFEXRZ-UHFFFAOYSA-N 0.000 claims 2
- QSLMDECMDJKHMQ-GSXCWMCISA-N Maprotiline Chemical compound C12=CC=CC=C2[C@@]2(CCCNC)C3=CC=CC=C3[C@@H]1CC2 QSLMDECMDJKHMQ-GSXCWMCISA-N 0.000 claims 2
- 229960003987 Melatonin Drugs 0.000 claims 2
- 229960001785 Mirtazapine Drugs 0.000 claims 2
- RTHCYVBBDHJXIQ-UHFFFAOYSA-N N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine Chemical compound C=1C=CC=CC=1C(CCNC)OC1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-UHFFFAOYSA-N 0.000 claims 2
- 229960001158 Nortriptyline Drugs 0.000 claims 2
- PHVGLTMQBUFIQQ-UHFFFAOYSA-N Nortryptiline Chemical compound C1CC2=CC=CC=C2C(=CCCNC)C2=CC=CC=C21 PHVGLTMQBUFIQQ-UHFFFAOYSA-N 0.000 claims 2
- 229960001534 Risperidone Drugs 0.000 claims 2
- RAPZEAPATHNIPO-UHFFFAOYSA-N Risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims 2
- ZSCDBOWYZJWBIY-UHFFFAOYSA-N Trimipramine Chemical compound C1CC2=CC=CC=C2N(CC(CN(C)C)C)C2=CC=CC=C21 ZSCDBOWYZJWBIY-UHFFFAOYSA-N 0.000 claims 2
- 230000003042 antagnostic Effects 0.000 claims 2
- 239000005557 antagonist Substances 0.000 claims 2
- 239000000164 antipsychotic agent Substances 0.000 claims 2
- 229960001653 citalopram Drugs 0.000 claims 2
- 229960004606 clomipramine Drugs 0.000 claims 2
- 229960003914 desipramine Drugs 0.000 claims 2
- 229960002866 duloxetine Drugs 0.000 claims 2
- 229960004341 escitalopram Drugs 0.000 claims 2
- 239000000262 estrogen Substances 0.000 claims 2
- CJOFXWAVKWHTFT-XSFVSMFZSA-N fluvoxamine Chemical compound COCCCC\C(=N/OCCN)C1=CC=C(C(F)(F)F)C=C1 CJOFXWAVKWHTFT-XSFVSMFZSA-N 0.000 claims 2
- 229960002672 isocarboxazid Drugs 0.000 claims 2
- 229960004090 maprotiline Drugs 0.000 claims 2
- DRLFMBDRBRZALE-UHFFFAOYSA-N melatonin Chemical compound COC1=CC=C2NC=C(CCNC(C)=O)C2=C1 DRLFMBDRBRZALE-UHFFFAOYSA-N 0.000 claims 2
- 201000008839 post-traumatic stress disease Diseases 0.000 claims 2
- 229960001150 ramelteon Drugs 0.000 claims 2
- 229960003741 tranylcypromine Drugs 0.000 claims 2
- 239000003029 tricyclic antidepressant agent Substances 0.000 claims 2
- 229960002431 trimipramine Drugs 0.000 claims 2
- 229960004688 venlafaxine Drugs 0.000 claims 2
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 claims 2
- SFLSHLFXELFNJZ-QMMMGPOBSA-N (-)-norepinephrine Chemical compound NC[C@H](O)C1=CC=C(O)C(O)=C1 SFLSHLFXELFNJZ-QMMMGPOBSA-N 0.000 claims 1
- AYXYPKUFHZROOJ-ZETCQYMHSA-N (3S)-3-(aminomethyl)-5-methylhexanoic acid Chemical compound CC(C)C[C@H](CN)CC(O)=O AYXYPKUFHZROOJ-ZETCQYMHSA-N 0.000 claims 1
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 claims 1
- 239000003185 4 aminobutyric acid B receptor stimulating agent Substances 0.000 claims 1
- BQBQAWXALAGUIW-GHVWMZMZSA-N 6-[5-[[(2S)-2-(4-fluorophenyl)-4-methylpiperazin-1-yl]methyl]furan-3-yl]-3H-1,3-benzoxazol-2-one;hydrate;hydrochloride Chemical compound O.Cl.C1([C@@H]2N(CC=3OC=C(C=3)C=3C=C4OC(O)=NC4=CC=3)CCN(C2)C)=CC=C(F)C=C1 BQBQAWXALAGUIW-GHVWMZMZSA-N 0.000 claims 1
- 206010001488 Aggression Diseases 0.000 claims 1
- 206010001497 Agitation Diseases 0.000 claims 1
- YJYPHIXNFHFHND-UHFFFAOYSA-N Agomelatine Chemical compound C1=CC=C(CCNC(C)=O)C2=CC(OC)=CC=C21 YJYPHIXNFHFHND-UHFFFAOYSA-N 0.000 claims 1
- VREFGVBLTWBCJP-UHFFFAOYSA-N Alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 claims 1
- CEUORZQYGODEFX-UHFFFAOYSA-N Aripirazole Chemical compound ClC1=CC=CC(N2CCN(CCCCOC=3C=C4NC(=O)CCC4=CC=3)CC2)=C1Cl CEUORZQYGODEFX-UHFFFAOYSA-N 0.000 claims 1
- 102100010720 BATF2 Human genes 0.000 claims 1
- 101700013168 BATF2 Proteins 0.000 claims 1
- VMIYHDSEFNYJSL-UHFFFAOYSA-N Bromazepam Chemical compound C12=CC(Br)=CC=C2NC(=O)CN=C1C1=CC=CC=N1 VMIYHDSEFNYJSL-UHFFFAOYSA-N 0.000 claims 1
- QWCRAEMEVRGPNT-UHFFFAOYSA-N Buspirone Chemical compound C1C(=O)N(CCCCN2CCN(CC2)C=2N=CC=CN=2)C(=O)CC21CCCC2 QWCRAEMEVRGPNT-UHFFFAOYSA-N 0.000 claims 1
- AHOUBRCZNHFOSL-YOEHRIQHSA-N Casbol Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-YOEHRIQHSA-N 0.000 claims 1
- XGGTZCKQRWXCHW-WMTVXVAQSA-N Casopitant Chemical compound C1([C@H]2C[C@H](CCN2C(=O)N(C)[C@H](C)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)N2CCN(CC2)C(C)=O)=CC=C(F)C=C1C XGGTZCKQRWXCHW-WMTVXVAQSA-N 0.000 claims 1
- 229960001076 Chlorpromazine Drugs 0.000 claims 1
- ZPEIMTDSQAKGNT-UHFFFAOYSA-N Chlorpromazine Chemical compound C1=C(Cl)C=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZPEIMTDSQAKGNT-UHFFFAOYSA-N 0.000 claims 1
- CXOXHMZGEKVPMT-UHFFFAOYSA-N Clobazam Chemical compound O=C1CC(=O)N(C)C2=CC=C(Cl)C=C2N1C1=CC=CC=C1 CXOXHMZGEKVPMT-UHFFFAOYSA-N 0.000 claims 1
- DGBIGWXXNGSACT-UHFFFAOYSA-N Clonazepam Chemical compound C12=CC([N+](=O)[O-])=CC=C2NC(=O)CN=C1C1=CC=CC=C1Cl DGBIGWXXNGSACT-UHFFFAOYSA-N 0.000 claims 1
- QZUDBNBUXVUHMW-UHFFFAOYSA-N Clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims 1
- AAOVKJBEBIDNHE-UHFFFAOYSA-N Diazepam Chemical compound N=1CC(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 AAOVKJBEBIDNHE-UHFFFAOYSA-N 0.000 claims 1
- 229960000394 Droperidol Drugs 0.000 claims 1
- RMEDXOLNCUSCGS-UHFFFAOYSA-N Droperidol Chemical compound C1=CC(F)=CC=C1C(=O)CCCN1CC=C(N2C(NC3=CC=CC=C32)=O)CC1 RMEDXOLNCUSCGS-UHFFFAOYSA-N 0.000 claims 1
- 229960002336 Estazolam Drugs 0.000 claims 1
- CDCHDCWJMGXXRH-UHFFFAOYSA-N Estazolam Chemical compound C=1C(Cl)=CC=C(N2C=NN=C2CN=2)C=1C=2C1=CC=CC=C1 CDCHDCWJMGXXRH-UHFFFAOYSA-N 0.000 claims 1
- 229960001578 Eszopiclone Drugs 0.000 claims 1
- 229960002200 Flunitrazepam Drugs 0.000 claims 1
- 229960003528 Flurazepam Drugs 0.000 claims 1
- SAADBVWGJQAEFS-UHFFFAOYSA-N Flurazepam Chemical compound N=1CC(=O)N(CCN(CC)CC)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1F SAADBVWGJQAEFS-UHFFFAOYSA-N 0.000 claims 1
- BTCSSZJGUNDROE-UHFFFAOYSA-N GABA Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 1
- 101700002119 GAL Proteins 0.000 claims 1
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapen Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 1
- ZXRVKCBLGJOCEE-UHFFFAOYSA-N Gaboxadol Chemical compound C1NCCC2=C1ONC2=O ZXRVKCBLGJOCEE-UHFFFAOYSA-N 0.000 claims 1
- 229950004346 Gaboxadol Drugs 0.000 claims 1
- 102000018997 Growth Hormone Human genes 0.000 claims 1
- 108010051696 Growth Hormone Proteins 0.000 claims 1
- 102100013818 HCRT Human genes 0.000 claims 1
- 101710023151 HCRT Proteins 0.000 claims 1
- LNEPOXFFQSENCJ-UHFFFAOYSA-N Haloperidol Chemical compound C1CC(O)(C=2C=CC(Cl)=CC=2)CCN1CCCC(=O)C1=CC=C(F)C=C1 LNEPOXFFQSENCJ-UHFFFAOYSA-N 0.000 claims 1
- 102000002265 Human Growth Hormone Human genes 0.000 claims 1
- 108010000521 Human Growth Hormone Proteins 0.000 claims 1
- 239000000854 Human Growth Hormone Substances 0.000 claims 1
- 206010022568 Intermittent explosive disease Diseases 0.000 claims 1
- 102000004310 Ion Channels Human genes 0.000 claims 1
- 108090000862 Ion Channels Proteins 0.000 claims 1
- FPCCSQOGAWCVBH-UHFFFAOYSA-N Ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 claims 1
- PYZRQGJRPPTADH-UHFFFAOYSA-N Lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 claims 1
- DIWRORZWFLOCLC-UHFFFAOYSA-N Lorazepam Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(O)N=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-UHFFFAOYSA-N 0.000 claims 1
- XJGVXQDUIWGIRW-UHFFFAOYSA-N Loxapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2OC2=CC=C(Cl)C=C12 XJGVXQDUIWGIRW-UHFFFAOYSA-N 0.000 claims 1
- 229960003793 Midazolam Drugs 0.000 claims 1
- DDLIGBOFAVUZHB-UHFFFAOYSA-N Midazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NC=C2CN=C1C1=CC=CC=C1F DDLIGBOFAVUZHB-UHFFFAOYSA-N 0.000 claims 1
- YFGHCGITMMYXAQ-UHFFFAOYSA-N Modafinil Chemical compound C=1C=CC=CC=1C(S(=O)CC(=O)N)C1=CC=CC=C1 YFGHCGITMMYXAQ-UHFFFAOYSA-N 0.000 claims 1
- COSPVUFTLGQDQL-UHFFFAOYSA-N Nelotanserin Chemical compound C1=C(C=2N(N=CC=2Br)C)C(OC)=CC=C1NC(=O)NC1=CC=C(F)C=C1F COSPVUFTLGQDQL-UHFFFAOYSA-N 0.000 claims 1
- 229960001454 Nitrazepam Drugs 0.000 claims 1
- KJONHKAYOJNZEC-UHFFFAOYSA-N Nitrazepam Chemical compound C12=CC([N+](=O)[O-])=CC=C2NC(=O)CN=C1C1=CC=CC=C1 KJONHKAYOJNZEC-UHFFFAOYSA-N 0.000 claims 1
- 229960002748 Norepinephrine Drugs 0.000 claims 1
- KVWDHTXUZHCGIO-UHFFFAOYSA-N Olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims 1
- 102000008834 Orexin receptor family Human genes 0.000 claims 1
- 108050000742 Orexin receptor family Proteins 0.000 claims 1
- 229940053544 Other antidepressants in ATC Drugs 0.000 claims 1
- ADIMAYPTOBDMTL-UHFFFAOYSA-N Oxazepam Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(O)N=C1C1=CC=CC=C1 ADIMAYPTOBDMTL-UHFFFAOYSA-N 0.000 claims 1
- 229960000762 Perphenazine Drugs 0.000 claims 1
- 229960004790 Phenelzine Sulfate Drugs 0.000 claims 1
- RXBKMJIPNDOHFR-UHFFFAOYSA-N Phenelzine sulfate Chemical compound OS(O)(=O)=O.NNCCC1=CC=CC=C1 RXBKMJIPNDOHFR-UHFFFAOYSA-N 0.000 claims 1
- YVUQSNJEYSNKRX-UHFFFAOYSA-N Pimozide Chemical compound C1=CC(F)=CC=C1C(C=1C=CC(F)=CC=1)CCCN1CCC(N2C(NC3=CC=CC=C32)=O)CC1 YVUQSNJEYSNKRX-UHFFFAOYSA-N 0.000 claims 1
- WIKYUJGCLQQFNW-UHFFFAOYSA-N Prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 claims 1
- ZGUGWUXLJSTTMA-UHFFFAOYSA-N Promazinum Chemical compound C1=CC=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZGUGWUXLJSTTMA-UHFFFAOYSA-N 0.000 claims 1
- BWPIARFWQZKAIA-UHFFFAOYSA-N Protriptyline Chemical compound C1=CC2=CC=CC=C2C(CCCNC)C2=CC=CC=C21 BWPIARFWQZKAIA-UHFFFAOYSA-N 0.000 claims 1
- URKOMYMAXPYINW-UHFFFAOYSA-N Quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims 1
- YGYBFMRFXNDIPO-QGZVFWFLSA-N Repinotan Chemical compound O=S1(=O)C2=CC=CC=C2C(=O)N1CCCCNC[C@@H]1OC2=CC=CC=C2CC1 YGYBFMRFXNDIPO-QGZVFWFLSA-N 0.000 claims 1
- 229950009693 Repinotan Drugs 0.000 claims 1
- 229950009626 Ritanserin Drugs 0.000 claims 1
- JUQLTPCYUFPYKE-UHFFFAOYSA-N Ritanserin Chemical compound CC=1N=C2SC=CN2C(=O)C=1CCN(CC1)CCC1=C(C=1C=CC(F)=CC=1)C1=CC=C(F)C=C1 JUQLTPCYUFPYKE-UHFFFAOYSA-N 0.000 claims 1
- PPTYJKAXVCCBDU-UHFFFAOYSA-N Rohypnol Chemical compound N=1CC(=O)N(C)C2=CC=C([N+]([O-])=O)C=C2C=1C1=CC=CC=C1F PPTYJKAXVCCBDU-UHFFFAOYSA-N 0.000 claims 1
- 229940071773 Rozerem Drugs 0.000 claims 1
- 229940076279 Serotonin Drugs 0.000 claims 1
- 229960002073 Sertraline Drugs 0.000 claims 1
- VGKDLMBJGBXTGI-SJCJKPOMSA-N Sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 claims 1
- 102100002996 TAC1 Human genes 0.000 claims 1
- 101700065588 TAC1 Proteins 0.000 claims 1
- PTOIAAWZLUQTIO-GXFFZTMASA-N Tasimelteon Chemical compound CCC(=O)NC[C@@H]1C[C@H]1C1=CC=CC2=C1CCO2 PTOIAAWZLUQTIO-GXFFZTMASA-N 0.000 claims 1
- 229960003188 Temazepam Drugs 0.000 claims 1
- SEQDDYPDSLOBDC-UHFFFAOYSA-N Temazepam Chemical compound N=1C(O)C(=O)N(C)C2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 SEQDDYPDSLOBDC-UHFFFAOYSA-N 0.000 claims 1
- GFBKORZTTCHDGY-UWVJOHFNSA-N Thiothixene Chemical compound C12=CC(S(=O)(=O)N(C)C)=CC=C2SC2=CC=CC=C2\C1=C\CCN1CCN(C)CC1 GFBKORZTTCHDGY-UWVJOHFNSA-N 0.000 claims 1
- RGCVKNLCSQQDEP-UHFFFAOYSA-N Tranquisan Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 RGCVKNLCSQQDEP-UHFFFAOYSA-N 0.000 claims 1
- JOFWLTCLBGQGBO-UHFFFAOYSA-N Triazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1Cl JOFWLTCLBGQGBO-UHFFFAOYSA-N 0.000 claims 1
- 241001516476 Vanda Species 0.000 claims 1
- PJDFLNIOAUIZSL-UHFFFAOYSA-N Vigabatrin Chemical compound C=CC(N)CCC(O)=O PJDFLNIOAUIZSL-UHFFFAOYSA-N 0.000 claims 1
- HUNXMJYCHXQEGX-UHFFFAOYSA-N Zaleplon Chemical compound CCN(C(C)=O)C1=CC=CC(C=2N3N=CC(=C3N=CC=2)C#N)=C1 HUNXMJYCHXQEGX-UHFFFAOYSA-N 0.000 claims 1
- MVWVFYHBGMAFLY-UHFFFAOYSA-N Ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 claims 1
- ZAFYATHCZYHLPB-UHFFFAOYSA-N Zolpidem Chemical compound N1=C2C=CC(C)=CN2C(CC(=O)N(C)C)=C1C1=CC=C(C)C=C1 ZAFYATHCZYHLPB-UHFFFAOYSA-N 0.000 claims 1
- 229960000820 Zopiclone Drugs 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 230000016571 aggressive behavior Effects 0.000 claims 1
- 229960002629 agomelatine Drugs 0.000 claims 1
- 229960004538 alprazolam Drugs 0.000 claims 1
- 229960003692 aminobutyric acid Drugs 0.000 claims 1
- 229960004372 aripiprazole Drugs 0.000 claims 1
- YFGHCGITMMYXAQ-LJQANCHMSA-N armodafinil Chemical compound C=1C=CC=CC=1C([S@](=O)CC(=O)N)C1=CC=CC=C1 YFGHCGITMMYXAQ-LJQANCHMSA-N 0.000 claims 1
- 229960004823 armodafinil Drugs 0.000 claims 1
- 150000003936 benzamides Chemical class 0.000 claims 1
- 229960002729 bromazepam Drugs 0.000 claims 1
- 229960002495 buspirone Drugs 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 239000000969 carrier Substances 0.000 claims 1
- 229960003778 casopitant Drugs 0.000 claims 1
- 229960001403 clobazam Drugs 0.000 claims 1
- 229960003120 clonazepam Drugs 0.000 claims 1
- 229960004362 clorazepate Drugs 0.000 claims 1
- XDDJGVMJFWAHJX-UHFFFAOYSA-M clorazepic acid anion Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(C(=O)[O-])N=C1C1=CC=CC=C1 XDDJGVMJFWAHJX-UHFFFAOYSA-M 0.000 claims 1
- 229960004170 clozapine Drugs 0.000 claims 1
- 229960003529 diazepam Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- KLBQZWRITKRQQV-UHFFFAOYSA-N dl-Thioridazine Chemical compound C12=CC(SC)=CC=C2SC2=CC=CC=C2N1CCC1CCCCN1C KLBQZWRITKRQQV-UHFFFAOYSA-N 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229960002870 gabapentin Drugs 0.000 claims 1
- 239000000122 growth hormone Substances 0.000 claims 1
- 229960003878 haloperidol Drugs 0.000 claims 1
- 229960004801 imipramine Drugs 0.000 claims 1
- 229960005417 ketanserin Drugs 0.000 claims 1
- 229960001848 lamotrigine Drugs 0.000 claims 1
- 229960004391 lorazepam Drugs 0.000 claims 1
- 229960000423 loxapine Drugs 0.000 claims 1
- 229960001165 modafinil Drugs 0.000 claims 1
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 claims 1
- 229960005017 olanzapine Drugs 0.000 claims 1
- 229960004535 oxazepam Drugs 0.000 claims 1
- 229960001057 paliperidone Drugs 0.000 claims 1
- 229960002296 paroxetine Drugs 0.000 claims 1
- 229960003634 pimozide Drugs 0.000 claims 1
- 229960001233 pregabalin Drugs 0.000 claims 1
- 229960003111 prochlorperazine Drugs 0.000 claims 1
- 229960003598 promazine Drugs 0.000 claims 1
- 229960002601 protriptyline Drugs 0.000 claims 1
- 229960004431 quetiapine Drugs 0.000 claims 1
- 239000002464 receptor antagonist Substances 0.000 claims 1
- 239000003215 serotonin 5-HT2 receptor antagonist Substances 0.000 claims 1
- QAOWNCQODCNURD-UHFFFAOYSA-L sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 claims 1
- 230000000576 supplementary Effects 0.000 claims 1
- 229960000660 tasimelteon Drugs 0.000 claims 1
- 229960002784 thioridazine Drugs 0.000 claims 1
- 229960004660 thiothixene Drugs 0.000 claims 1
- 229960003386 triazolam Drugs 0.000 claims 1
- 229960005318 vigabatrin Drugs 0.000 claims 1
- 229960004010 zaleplon Drugs 0.000 claims 1
- 229960000607 ziprasidone Drugs 0.000 claims 1
- 229960001475 zolpidem Drugs 0.000 claims 1
Claims (23)
- 式Iの化合物が、
Xが−O−であり、Yが−C(H)(OH)−である、
Xが−NH−であり、Yが−C(H)(OH)−である、
Xが−N(CH3)−であり、Yが−C(H)(OH)−である、
Xが−O−であり、Yが−C(O)−である、
Xが−O−であり、Yが−O−である、
Xが−N(CH3)−であり、Yが−C(O)−である、
Xが−N(CH3)−であり、Yが−O−である、
Xが−NH−であり、Yが−C(O)−であるおよび
Xが−NH−であり、Yが−O−である、
式Iの化合物から成る群から選択される、請求項1に記載の医薬組成物。 - Xが−N(CH3)−であり、Yが−C(O)−である、請求項1に記載の医薬組成物。
- 障害が外傷後ストレス障害である、請求項1〜3のいずれかに記載の医薬組成物。
- 障害が衝動制御障害である、請求項1〜4のいずれかに記載の医薬組成物。
- 衝動制御障害が間欠性爆発性障害である、請求項5に記載の医薬組成物。
- 式Iの化合物を含む組成物が1種以上のさらなる抗鬱剤に補助的である、請求項1〜6に記載の医薬組成物。
- 1種以上のさらなる抗鬱剤が式Iの化合物を含む組成物に補助的である、請求項1〜6のいずれかに記載の医薬組成物。
- 抗鬱剤がアミトリプチリン、アモキサピン、ブプロピオン、シタロプラム、クロミプラミン、デシプラミン、ドキセピン、デュロキセチン、エスシタロプラム、フルオキセチン、フルボキサミン、イミプラミン、イソカルボキサジド、マプロチリン、ミルタザピン、ネファゾドン、ノルトリプチリン、パロキセチン、硫酸フェネルジン、プロトリプチリン、セルトラリン、トラニルシプロミン、トラゾドン、トリミプラミンおよびベンラフェキシンの1種以上から選択される、請求項7または8に記載の医薬組成物。
- 抗鬱剤が選択的セロトニン再取り込み阻害剤(SSRI)、セロトニン−ノルエピネフリン再取り込み阻害剤(SNRI)および三環系抗鬱剤から選択される1種以上の抗鬱剤である、請求項7、8または9に記載の医薬組成物。
- 抗鬱剤がSSRIである、請求項10に記載の医薬組成物。
- 錠剤またはカプセル剤である経口単位投与量形態として薬学的に許容される希釈剤または担体を含む組成物として経口用である、請求項1〜11のいずれかに記載の医薬組成物。
- 式Iの化合物の有効量が約1mg〜約140mgの1日投与量である、請求項1〜12のいずれかに記載の医薬組成物。
- 式Iの化合物を1mg〜100mgの1日投与量で投与する、請求項1〜13のいずれかに記載の医薬組成物。
- 式Iの化合物を10mg〜100mgの1日投与量で投与する、請求項1〜14のいずれかに記載の医薬組成物。
- 式Iの化合物を10mg〜50mgの1日投与量で投与する、請求項1〜15のいずれかに記載の医薬組成物。
- 式Iの化合物を20mg〜40mgの1日投与量で投与する、請求項1〜16のいずれかに記載の医薬組成物。
- 式Iの化合物を1mg〜10mgの1日投与量で投与する、請求項1〜17のいずれかに記載の医薬組成物。
- 遊離形または薬学的に許容される塩形のGABA活性を調節する化合物、GABA−Bアゴニスト、5−HTモジュレーター、メラトニンアゴニスト、イオンチャネルモジュレーター、セロトニン−2アンタゴニスト/再取り込み阻害剤(SARI)、オレキシン受容体アンタゴニスト、H3アゴニスト、ノルアドレナリンアンタゴニスト、ガラニンアゴニスト、CRHアンタゴニスト、ヒト成長ホルモン、成長ホルモンアゴニスト、エストロゲン、エストロゲンアゴニスト、ニューロキニン−1剤および抗精神病剤、例えば、典型的抗精神病剤から選択される1種以上のさらなる治療剤と投与することを特徴とする、請求項1〜18のいずれかに記載の医薬組成物。
- 遊離形または薬学的に許容される塩形のモダフィニル、アルモダフィニル、ドキセピン、アルプラゾラム、ブロマゼパム、クロバザム、クロナゼパム、クロラゼプ酸、ジアゼパム、フルニトラゼパム、フルラゼパム、ロラゼパム、ミダゾラム、ニトラゼパム、オキサゼパム、テマゼパム、トリアゾラム、インディプロン、ゾピクロン、エスゾピクロン、ザレプロン、ゾルピデム、ガボキサドール、ビガバトリン、チアギャビン、EVT 201(Evotec Pharmaceuticals)、エスタゾラム、ケタンセリン、リスペリドン、エプリバンセリン、ボリナンセリン(Sanofi-Aventis, France)、プルバンセリン、MDL 100907(Sanofi-Aventis, France)、HY10275(Eli Lilly)、APD125(Arena Pharmaceuticals, San Diego, CA)、AVE8488(Sanofi-Aventis, France)、レピノタン、サリゾタン、エプタピロン、ブスピロン、MN−305(MediciNova, San Diego, CA)、メラトニン、ラメルテオン(ロゼレム(登録商標)、武田薬品、日本)、VEC−162(Vanda Pharmaceuticals, Rockville, MD)、PD−6735(Phase II Discovery))、アゴメラチン、ラモトリジン、ギャバペンチン、プレガバリン、オレキシン、1,3−ビアリールウレア、SB−334867−a(GlaxoSmithKline, UK)、GW649868(GlaxoSmithKline)、ベンズアミド誘導体、Org 50081(Organon - Netherlands)、リタンセリン、ネファゾドン、サーゾーン、トラゾドン、カソピタント(GlaxoSmithKline)、アミトリプチリン、アモキサピン、ブプロピオン、シタロプラム、クロミプラミン、デシプラミン、ドキセピン、デュロキセチン、エスシタロプラム、フルオキセチン、フルボキサミン、イミプラミン、イソカルボキサジド、マプロチリン、ミルタザピン、ネファゾドン、ノルトリプチリン、パロキセチン、硫酸フェネルジン、プロトリプチリン、セルトラリン、トラニルシプロミン、トラゾドン、トリミプラミン、ベンラファキシン、クロルプロマジン、ハロペリドール、ドロペリドール、フルフェナジン、ロキサピン、メソリダジン、モリンドン、ペルフェナジン、ピモジド、プロクロルペラジン、プロマジン、チオリダジン、チオチキセン、トリフロペラジン、クロザピン、アリピプラゾール、オランザピン、クエチアピン、リスペリドン、ジプラシドンおよびパリペリドンから成る群から選択される1種以上のさらなる治療剤と投与することを特徴とする、請求項1〜19のいずれかに記載の医薬組成物。
- 他の抗鬱剤または複数抗鬱剤の組み合わせでの処置に十分に応答していない患者に使用する、請求項1〜20のいずれかに記載の医薬組成物。
- 患者が選択的セロトニン再取り込み阻害剤(SSRI)、セロトニン−ノルエピネフリン再取り込み阻害剤(SNRI)および三環系抗鬱剤から選択される1種以上の抗鬱剤での処置に応答していない、請求項20に記載の医薬組成物。
- 患者がSSRIでの処置に応答していない、請求項22に記載の医薬組成物。
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