MXPA06013454A - Agonistas inversos del receptor de serotonina selectivos como terapeuticos para enfermedad. - Google Patents
Agonistas inversos del receptor de serotonina selectivos como terapeuticos para enfermedad.Info
- Publication number
- MXPA06013454A MXPA06013454A MXPA06013454A MXPA06013454A MXPA06013454A MX PA06013454 A MXPA06013454 A MX PA06013454A MX PA06013454 A MXPA06013454 A MX PA06013454A MX PA06013454 A MXPA06013454 A MX PA06013454A MX PA06013454 A MXPA06013454 A MX PA06013454A
- Authority
- MX
- Mexico
- Prior art keywords
- compound
- group
- pharmaceutical composition
- drug
- composition according
- Prior art date
Links
- 239000003814 drug Substances 0.000 title claims description 124
- 102000040125 5-hydroxytryptamine receptor family Human genes 0.000 title claims description 34
- 108091032151 5-hydroxytryptamine receptor family Proteins 0.000 title claims description 34
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title description 16
- 201000010099 disease Diseases 0.000 title description 9
- 239000002469 receptor inverse agonist Substances 0.000 title 1
- 238000000034 method Methods 0.000 claims abstract description 67
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 64
- 239000000164 antipsychotic agent Substances 0.000 claims abstract description 35
- 208000028017 Psychotic disease Diseases 0.000 claims abstract description 27
- 150000001875 compounds Chemical class 0.000 claims description 233
- 229940079593 drug Drugs 0.000 claims description 115
- -1 dulexetine Chemical compound 0.000 claims description 53
- 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 description 50
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims description 42
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims description 41
- 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 description 40
- RGCVKNLCSQQDEP-UHFFFAOYSA-N Perphenazine Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 RGCVKNLCSQQDEP-UHFFFAOYSA-N 0.000 claims description 39
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 39
- KLBQZWRITKRQQV-UHFFFAOYSA-N Thioridazine Chemical compound C12=CC(SC)=CC=C2SC2=CC=CC=C2N1CCC1CCCCN1C KLBQZWRITKRQQV-UHFFFAOYSA-N 0.000 claims description 39
- 206010022437 insomnia Diseases 0.000 claims description 39
- 239000005557 antagonist Substances 0.000 claims description 37
- 150000003839 salts Chemical class 0.000 claims description 33
- 230000004075 alteration Effects 0.000 claims description 32
- SLVMESMUVMCQIY-UHFFFAOYSA-N mesoridazine Chemical compound CN1CCCCC1CCN1C2=CC(S(C)=O)=CC=C2SC2=CC=CC=C21 SLVMESMUVMCQIY-UHFFFAOYSA-N 0.000 claims description 32
- XGZVUEUWXADBQD-UHFFFAOYSA-L lithium carbonate Chemical group [Li+].[Li+].[O-]C([O-])=O XGZVUEUWXADBQD-UHFFFAOYSA-L 0.000 claims description 31
- NIJJYAXOARWZEE-UHFFFAOYSA-N Valproic acid Chemical compound CCCC(C(O)=O)CCC NIJJYAXOARWZEE-UHFFFAOYSA-N 0.000 claims description 30
- 229940035004 seroquel Drugs 0.000 claims description 29
- 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 description 28
- KRMDCWKBEZIMAB-UHFFFAOYSA-N amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 claims description 27
- ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 claims description 27
- 229940125425 inverse agonist Drugs 0.000 claims description 27
- XJGVXQDUIWGIRW-UHFFFAOYSA-N loxapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2OC2=CC=C(Cl)C=C12 XJGVXQDUIWGIRW-UHFFFAOYSA-N 0.000 claims description 27
- WEXRUCMBJFQVBZ-UHFFFAOYSA-N pentobarbital Chemical compound CCCC(C)C1(CC)C(=O)NC(=O)NC1=O WEXRUCMBJFQVBZ-UHFFFAOYSA-N 0.000 claims description 27
- PLDUPXSUYLZYBN-UHFFFAOYSA-N Fluphenazine Chemical compound C1CN(CCO)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 PLDUPXSUYLZYBN-UHFFFAOYSA-N 0.000 claims description 26
- 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 description 26
- 229960001076 chlorpromazine Drugs 0.000 claims description 26
- 229940095895 haldol Drugs 0.000 claims description 24
- 229940124834 selective serotonin reuptake inhibitor Drugs 0.000 claims description 24
- 206010034912 Phobia Diseases 0.000 claims description 23
- SNPPWIUOZRMYNY-UHFFFAOYSA-N bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 claims description 23
- 229960004170 clozapine Drugs 0.000 claims description 23
- 229940003380 geodon Drugs 0.000 claims description 23
- 208000019899 phobic disease Diseases 0.000 claims description 23
- 229960004431 quetiapine Drugs 0.000 claims description 23
- URKOMYMAXPYINW-UHFFFAOYSA-N quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims description 23
- 102000049773 5-HT2A Serotonin Receptor Human genes 0.000 claims description 22
- 229910052808 lithium carbonate Inorganic materials 0.000 claims description 22
- 230000003561 anti-manic effect Effects 0.000 claims description 21
- 239000002767 noradrenalin uptake inhibitor Substances 0.000 claims description 21
- 229940127221 norepinephrine reuptake inhibitor Drugs 0.000 claims description 21
- 238000011282 treatment Methods 0.000 claims description 21
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 claims description 20
- 239000003136 dopamine receptor stimulating agent Substances 0.000 claims description 20
- 239000012896 selective serotonin reuptake inhibitor Substances 0.000 claims description 20
- 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 claims description 19
- 229940068796 clozaril Drugs 0.000 claims description 19
- 229940109739 orap Drugs 0.000 claims description 19
- 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 description 19
- 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 description 18
- KTGRHKOEFSJQNS-BDQAORGHSA-N (1s)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-3h-2-benzofuran-5-carbonitrile;oxalic acid Chemical compound OC(=O)C(O)=O.C1([C@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 KTGRHKOEFSJQNS-BDQAORGHSA-N 0.000 claims description 18
- WSEQXVZVJXJVFP-HXUWFJFHSA-N (R)-citalopram Chemical compound C1([C@@]2(C3=CC=C(C=C3CO2)C#N)CCCN(C)C)=CC=C(F)C=C1 WSEQXVZVJXJVFP-HXUWFJFHSA-N 0.000 claims description 18
- WSEQXVZVJXJVFP-UHFFFAOYSA-N 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile Chemical compound O1CC2=CC(C#N)=CC=C2C1(CCCN(C)C)C1=CC=C(F)C=C1 WSEQXVZVJXJVFP-UHFFFAOYSA-N 0.000 claims description 18
- XKFPYPQQHFEXRZ-UHFFFAOYSA-N 5-methyl-N'-(phenylmethyl)-3-isoxazolecarbohydrazide Chemical compound O1C(C)=CC(C(=O)NNCC=2C=CC=CC=2)=N1 XKFPYPQQHFEXRZ-UHFFFAOYSA-N 0.000 claims description 18
- HCYAFALTSJYZDH-UHFFFAOYSA-N Desimpramine Chemical compound C1CC2=CC=CC=C2N(CCCNC)C2=CC=CC=C21 HCYAFALTSJYZDH-UHFFFAOYSA-N 0.000 claims description 18
- LFMYNZPAVPMEGP-PIDGMYBPSA-N Fluvoxamine maleate Chemical compound OC(=O)\C=C/C(O)=O.COCCCC\C(=N/OCCN)C1=CC=C(C(F)(F)F)C=C1 LFMYNZPAVPMEGP-PIDGMYBPSA-N 0.000 claims description 18
- RMUCZJUITONUFY-UHFFFAOYSA-N Phenelzine Chemical compound NNCCC1=CC=CC=C1 RMUCZJUITONUFY-UHFFFAOYSA-N 0.000 claims description 18
- 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 description 18
- 229940047493 celexa Drugs 0.000 claims description 18
- ANTSCNMPPGJYLG-UHFFFAOYSA-N chlordiazepoxide Chemical compound O=N=1CC(NC)=NC2=CC=C(Cl)C=C2C=1C1=CC=CC=C1 ANTSCNMPPGJYLG-UHFFFAOYSA-N 0.000 claims description 18
- 229960001653 citalopram Drugs 0.000 claims description 18
- 229960005426 doxepin Drugs 0.000 claims description 18
- 229960004341 escitalopram Drugs 0.000 claims description 18
- 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 description 18
- 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 description 18
- 229960004038 fluvoxamine Drugs 0.000 claims description 18
- 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 description 18
- ZQDWXGKKHFNSQK-UHFFFAOYSA-N hydroxyzine Chemical compound C1CN(CCOCCO)CCN1C(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 ZQDWXGKKHFNSQK-UHFFFAOYSA-N 0.000 claims description 18
- 229940054157 lexapro Drugs 0.000 claims description 18
- 229940009622 luvox Drugs 0.000 claims description 18
- 229960004090 maprotiline Drugs 0.000 claims description 18
- 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 description 18
- 229960002296 paroxetine Drugs 0.000 claims description 18
- KQPKPCNLIDLUMF-UHFFFAOYSA-N secobarbital Chemical compound CCCC(C)C1(CC=C)C(=O)NC(=O)NC1=O KQPKPCNLIDLUMF-UHFFFAOYSA-N 0.000 claims description 18
- JOFWLTCLBGQGBO-UHFFFAOYSA-N triazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1Cl JOFWLTCLBGQGBO-UHFFFAOYSA-N 0.000 claims description 18
- PNVNVHUZROJLTJ-UHFFFAOYSA-N venlafaxine Chemical compound C1=CC(OC)=CC=C1C(CN(C)C)C1(O)CCCCC1 PNVNVHUZROJLTJ-UHFFFAOYSA-N 0.000 claims description 18
- 229940039925 zyprexa Drugs 0.000 claims description 18
- 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 description 17
- 229940088505 compazine Drugs 0.000 claims description 17
- 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 description 17
- DSKIOWHQLUWFLG-SPIKMXEPSA-N prochlorperazine maleate Chemical compound [H+].[H+].[H+].[H+].[O-]C(=O)\C=C/C([O-])=O.[O-]C(=O)\C=C/C([O-])=O.C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 DSKIOWHQLUWFLG-SPIKMXEPSA-N 0.000 claims description 17
- 229960000607 ziprasidone Drugs 0.000 claims description 17
- BCGWQEUPMDMJNV-UHFFFAOYSA-N imipramine Chemical compound C1CC2=CC=CC=C2N(CCCN(C)C)C2=CC=CC=C21 BCGWQEUPMDMJNV-UHFFFAOYSA-N 0.000 claims description 16
- 229910003002 lithium salt Inorganic materials 0.000 claims description 16
- 159000000002 lithium salts Chemical class 0.000 claims description 16
- 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 description 16
- 229950000688 phenothiazine Drugs 0.000 claims description 15
- RTHCYVBBDHJXIQ-MRXNPFEDSA-N (R)-fluoxetine Chemical compound O([C@H](CCNC)C=1C=CC=CC=1)C1=CC=C(C(F)(F)F)C=C1 RTHCYVBBDHJXIQ-MRXNPFEDSA-N 0.000 claims description 14
- WJFKNYWRSNBZNX-UHFFFAOYSA-N 10H-phenothiazine Chemical compound C1=CC=C2NC3=CC=CC=C3SC2=C1 WJFKNYWRSNBZNX-UHFFFAOYSA-N 0.000 claims description 14
- 229960002464 fluoxetine Drugs 0.000 claims description 14
- 229940089527 loxitane Drugs 0.000 claims description 14
- WSPOMRSOLSGNFJ-AUWJEWJLSA-N (Z)-chlorprothixene Chemical compound C1=C(Cl)C=C2C(=C/CCN(C)C)\C3=CC=CC=C3SC2=C1 WSPOMRSOLSGNFJ-AUWJEWJLSA-N 0.000 claims description 13
- KLPWJLBORRMFGK-UHFFFAOYSA-N Molindone Chemical compound O=C1C=2C(CC)=C(C)NC=2CCC1CN1CCOCC1 KLPWJLBORRMFGK-UHFFFAOYSA-N 0.000 claims description 13
- 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 description 13
- 229960001552 chlorprothixene Drugs 0.000 claims description 13
- 229940075925 depakote Drugs 0.000 claims description 13
- 229940103472 etrafon Drugs 0.000 claims description 13
- 229960003878 haloperidol Drugs 0.000 claims description 13
- 229960000423 loxapine Drugs 0.000 claims description 13
- 229960000300 mesoridazine Drugs 0.000 claims description 13
- IRQVJPHZDYMXNW-UHFFFAOYSA-N metoclopramide dihydrochloride monohydrate Chemical compound O.[Cl-].[Cl-].CC[NH+](CC)CCNC(=O)C1=CC(Cl)=C([NH3+])C=C1OC IRQVJPHZDYMXNW-UHFFFAOYSA-N 0.000 claims description 13
- 229940028394 moban Drugs 0.000 claims description 13
- 229960005017 olanzapine Drugs 0.000 claims description 13
- WIKYUJGCLQQFNW-UHFFFAOYSA-N prochlorperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(Cl)=CC=C2SC2=CC=CC=C21 WIKYUJGCLQQFNW-UHFFFAOYSA-N 0.000 claims description 13
- 229960003111 prochlorperazine Drugs 0.000 claims description 13
- XXPDBLUZJRXNNZ-UHFFFAOYSA-N promethazine hydrochloride Chemical compound Cl.C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 XXPDBLUZJRXNNZ-UHFFFAOYSA-N 0.000 claims description 13
- 229940080693 reglan Drugs 0.000 claims description 13
- 229940106887 risperdal Drugs 0.000 claims description 13
- 229960002784 thioridazine Drugs 0.000 claims description 13
- 229960000604 valproic acid Drugs 0.000 claims description 13
- 229940049706 benzodiazepine Drugs 0.000 claims description 11
- 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 description 11
- 229960000394 droperidol Drugs 0.000 claims description 11
- ZEUITGRIYCTCEM-KRWDZBQOSA-N (S)-duloxetine Chemical compound C1([C@@H](OC=2C3=CC=CC=C3C=CC=2)CCNC)=CC=CS1 ZEUITGRIYCTCEM-KRWDZBQOSA-N 0.000 claims description 10
- 239000003085 diluting agent Substances 0.000 claims description 10
- 229960002866 duloxetine Drugs 0.000 claims description 10
- ZEWQUBUPAILYHI-UHFFFAOYSA-N trifluoperazine Chemical compound C1CN(C)CCN1CCCN1C2=CC(C(F)(F)F)=CC=C2SC2=CC=CC=C21 ZEWQUBUPAILYHI-UHFFFAOYSA-N 0.000 claims description 10
- 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 description 10
- 229960004010 zaleplon Drugs 0.000 claims description 10
- 229960001475 zolpidem Drugs 0.000 claims description 10
- IGLYMJRIWWIQQE-QUOODJBBSA-N (1S,2R)-2-phenylcyclopropan-1-amine (1R,2S)-2-phenylcyclopropan-1-amine Chemical compound N[C@H]1C[C@@H]1C1=CC=CC=C1.N[C@@H]1C[C@H]1C1=CC=CC=C1 IGLYMJRIWWIQQE-QUOODJBBSA-N 0.000 claims description 9
- DIWRORZWFLOCLC-HNNXBMFYSA-N (3s)-7-chloro-5-(2-chlorophenyl)-3-hydroxy-1,3-dihydro-1,4-benzodiazepin-2-one Chemical compound N([C@H](C(NC1=CC=C(Cl)C=C11)=O)O)=C1C1=CC=CC=C1Cl DIWRORZWFLOCLC-HNNXBMFYSA-N 0.000 claims description 9
- SVUOLADPCWQTTE-UHFFFAOYSA-N 1h-1,2-benzodiazepine Chemical compound N1N=CC=CC2=CC=CC=C12 SVUOLADPCWQTTE-UHFFFAOYSA-N 0.000 claims description 9
- WKEMJKQOLOHJLZ-UHFFFAOYSA-N Almogran Chemical compound C1=C2C(CCN(C)C)=CNC2=CC=C1CS(=O)(=O)N1CCCC1 WKEMJKQOLOHJLZ-UHFFFAOYSA-N 0.000 claims description 9
- KORNTPPJEAJQIU-KJXAQDMKSA-N Cabaser Chemical compound C1=CC([C@H]2C[C@H](CN(CC=C)[C@@H]2C2)C(=O)N(CCCN(C)C)C(=O)NCC)=C3C2=CNC3=C1 KORNTPPJEAJQIU-KJXAQDMKSA-N 0.000 claims description 9
- 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 description 9
- DYDCUQKUCUHJBH-UWTATZPHSA-N D-Cycloserine Chemical compound N[C@@H]1CONC1=O DYDCUQKUCUHJBH-UWTATZPHSA-N 0.000 claims description 9
- DYDCUQKUCUHJBH-UHFFFAOYSA-N D-Cycloserine Natural products NC1CONC1=O DYDCUQKUCUHJBH-UHFFFAOYSA-N 0.000 claims description 9
- PWWVAXIEGOYWEE-UHFFFAOYSA-N Isophenergan Chemical compound C1=CC=C2N(CC(C)N(C)C)C3=CC=CC=C3SC2=C1 PWWVAXIEGOYWEE-UHFFFAOYSA-N 0.000 claims description 9
- 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 description 9
- 206010026749 Mania Diseases 0.000 claims description 9
- 101800001616 Manserin Proteins 0.000 claims description 9
- 102400000282 Manserin Human genes 0.000 claims description 9
- OCJYIGYOJCODJL-UHFFFAOYSA-N Meclizine Chemical compound CC1=CC=CC(CN2CCN(CC2)C(C=2C=CC=CC=2)C=2C=CC(Cl)=CC=2)=C1 OCJYIGYOJCODJL-UHFFFAOYSA-N 0.000 claims description 9
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 claims description 9
- IKMPWMZBZSAONZ-UHFFFAOYSA-N Quazepam Chemical compound FC1=CC=CC=C1C1=NCC(=S)N(CC(F)(F)F)C2=CC=C(Cl)C=C12 IKMPWMZBZSAONZ-UHFFFAOYSA-N 0.000 claims description 9
- 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 description 9
- BKPRVQDIOGQWTG-ICOOEGOYSA-N [(1s,2r)-2-phenylcyclopropyl]azanium;[(1r,2s)-2-phenylcyclopropyl]azanium;sulfate Chemical compound [O-]S([O-])(=O)=O.[NH3+][C@H]1C[C@@H]1C1=CC=CC=C1.[NH3+][C@@H]1C[C@H]1C1=CC=CC=C1 BKPRVQDIOGQWTG-ICOOEGOYSA-N 0.000 claims description 9
- PWACSDKDOHSSQD-IUTFFREVSA-N acrivastine Chemical compound C1=CC(C)=CC=C1C(\C=1N=C(\C=C\C(O)=O)C=CC=1)=C/CN1CCCC1 PWACSDKDOHSSQD-IUTFFREVSA-N 0.000 claims description 9
- 229960002133 almotriptan Drugs 0.000 claims description 9
- 229960004538 alprazolam Drugs 0.000 claims description 9
- 229960003805 amantadine Drugs 0.000 claims description 9
- DKNWSYNQZKUICI-UHFFFAOYSA-N amantadine Chemical compound C1C(C2)CC3CC2CC1(N)C3 DKNWSYNQZKUICI-UHFFFAOYSA-N 0.000 claims description 9
- 229940094070 ambien Drugs 0.000 claims description 9
- 229960000836 amitriptyline Drugs 0.000 claims description 9
- 229940025141 anafranil Drugs 0.000 claims description 9
- GXDALQBWZGODGZ-UHFFFAOYSA-N astemizole Chemical compound C1=CC(OC)=CC=C1CCN1CCC(NC=2N(C3=CC=CC=C3N=2)CC=2C=CC(F)=CC=2)CC1 GXDALQBWZGODGZ-UHFFFAOYSA-N 0.000 claims description 9
- 229940065779 atarax Drugs 0.000 claims description 9
- 229940072698 ativan Drugs 0.000 claims description 9
- 229960000383 azatadine Drugs 0.000 claims description 9
- SEBMTIQKRHYNIT-UHFFFAOYSA-N azatadine Chemical compound C1CN(C)CCC1=C1C2=NC=CC=C2CCC2=CC=CC=C21 SEBMTIQKRHYNIT-UHFFFAOYSA-N 0.000 claims description 9
- 229960002802 bromocriptine Drugs 0.000 claims description 9
- OZVBMTJYIDMWIL-AYFBDAFISA-N bromocriptine Chemical compound C1=CC(C=2[C@H](N(C)C[C@@H](C=2)C(=O)N[C@]2(C(=O)N3[C@H](C(N4CCC[C@H]4[C@]3(O)O2)=O)CC(C)C)C(C)C)C2)=C3C2=C(Br)NC3=C1 OZVBMTJYIDMWIL-AYFBDAFISA-N 0.000 claims description 9
- ZDIGNSYAACHWNL-UHFFFAOYSA-N brompheniramine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Br)C=C1 ZDIGNSYAACHWNL-UHFFFAOYSA-N 0.000 claims description 9
- 229960000725 brompheniramine Drugs 0.000 claims description 9
- 229960001058 bupropion Drugs 0.000 claims description 9
- 229960004596 cabergoline Drugs 0.000 claims description 9
- 229960000428 carbinoxamine Drugs 0.000 claims description 9
- OJFSXZCBGQGRNV-UHFFFAOYSA-N carbinoxamine Chemical compound C=1C=CC=NC=1C(OCCN(C)C)C1=CC=C(Cl)C=C1 OJFSXZCBGQGRNV-UHFFFAOYSA-N 0.000 claims description 9
- 229960004782 chlordiazepoxide Drugs 0.000 claims description 9
- SOYKEARSMXGVTM-UHFFFAOYSA-N chlorphenamine Chemical compound C=1C=CC=NC=1C(CCN(C)C)C1=CC=C(Cl)C=C1 SOYKEARSMXGVTM-UHFFFAOYSA-N 0.000 claims description 9
- 229960003291 chlorphenamine Drugs 0.000 claims description 9
- 229960002881 clemastine Drugs 0.000 claims description 9
- YNNUSGIPVFPVBX-NHCUHLMSSA-N clemastine Chemical compound CN1CCC[C@@H]1CCO[C@@](C)(C=1C=CC(Cl)=CC=1)C1=CC=CC=C1 YNNUSGIPVFPVBX-NHCUHLMSSA-N 0.000 claims description 9
- 229960004362 clorazepate Drugs 0.000 claims description 9
- 229960001140 cyproheptadine Drugs 0.000 claims description 9
- JJCFRYNCJDLXIK-UHFFFAOYSA-N cyproheptadine Chemical compound C1CN(C)CCC1=C1C2=CC=CC=C2C=CC2=CC=CC=C21 JJCFRYNCJDLXIK-UHFFFAOYSA-N 0.000 claims description 9
- 229960003914 desipramine Drugs 0.000 claims description 9
- 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 description 9
- 229960004993 dimenhydrinate Drugs 0.000 claims description 9
- MZDOIJOUFRQXHC-UHFFFAOYSA-N dimenhydrinate Chemical compound O=C1N(C)C(=O)N(C)C2=NC(Cl)=N[C]21.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 MZDOIJOUFRQXHC-UHFFFAOYSA-N 0.000 claims description 9
- 229960000520 diphenhydramine Drugs 0.000 claims description 9
- QCHSEDTUUKDTIG-UHFFFAOYSA-L dipotassium clorazepate Chemical compound [OH-].[K+].[K+].C12=CC(Cl)=CC=C2NC(=O)C(C(=O)[O-])N=C1C1=CC=CC=C1 QCHSEDTUUKDTIG-UHFFFAOYSA-L 0.000 claims description 9
- 229940075057 doral Drugs 0.000 claims description 9
- 229960005178 doxylamine Drugs 0.000 claims description 9
- HCFDWZZGGLSKEP-UHFFFAOYSA-N doxylamine Chemical compound C=1C=CC=NC=1C(C)(OCCN(C)C)C1=CC=CC=C1 HCFDWZZGGLSKEP-UHFFFAOYSA-N 0.000 claims description 9
- 229940098766 effexor Drugs 0.000 claims description 9
- 229940011681 elavil Drugs 0.000 claims description 9
- 229960002336 estazolam Drugs 0.000 claims description 9
- SIBNYOSJIXCDRI-SECBINFHSA-N frovatriptan Chemical compound C1=C(C(N)=O)[CH]C2=C(C[C@H](NC)CC3)C3=NC2=C1 SIBNYOSJIXCDRI-SECBINFHSA-N 0.000 claims description 9
- 229960002284 frovatriptan Drugs 0.000 claims description 9
- 229940027804 halcion Drugs 0.000 claims description 9
- 229960000930 hydroxyzine Drugs 0.000 claims description 9
- 229960004801 imipramine Drugs 0.000 claims description 9
- 229960002672 isocarboxazid Drugs 0.000 claims description 9
- 229940087372 limbitrol Drugs 0.000 claims description 9
- 229940071264 lithium citrate Drugs 0.000 claims description 9
- WJSIUCDMWSDDCE-UHFFFAOYSA-K lithium citrate (anhydrous) Chemical compound [Li+].[Li+].[Li+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O WJSIUCDMWSDDCE-UHFFFAOYSA-K 0.000 claims description 9
- 229960004391 lorazepam Drugs 0.000 claims description 9
- 229940110127 marplan Drugs 0.000 claims description 9
- 229960001474 meclozine Drugs 0.000 claims description 9
- NDVZIUGCCMZHLG-UHFFFAOYSA-N n-methyl-3-(2-methylsulfanylphenoxy)-3-phenylpropan-1-amine Chemical group C=1C=CC=CC=1C(CCNC)OC1=CC=CC=C1SC NDVZIUGCCMZHLG-UHFFFAOYSA-N 0.000 claims description 9
- 229960005254 naratriptan Drugs 0.000 claims description 9
- 229940087524 nardil Drugs 0.000 claims description 9
- 229960001800 nefazodone Drugs 0.000 claims description 9
- 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 description 9
- DYCKFEBIOUQECE-UHFFFAOYSA-N nefazodone hydrochloride Chemical compound [H+].[Cl-].O=C1N(CCOC=2C=CC=CC=2)C(CC)=NN1CCCN(CC1)CCN1C1=CC=CC(Cl)=C1 DYCKFEBIOUQECE-UHFFFAOYSA-N 0.000 claims description 9
- 229940105631 nembutal Drugs 0.000 claims description 9
- 229940087824 parnate Drugs 0.000 claims description 9
- 229960001412 pentobarbital Drugs 0.000 claims description 9
- 229960004851 pergolide Drugs 0.000 claims description 9
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 9
- 229960000964 phenelzine Drugs 0.000 claims description 9
- 229960003634 pimozide Drugs 0.000 claims description 9
- 229960003089 pramipexole Drugs 0.000 claims description 9
- FASDKYOPVNHBLU-ZETCQYMHSA-N pramipexole Chemical compound C1[C@@H](NCCC)CCC2=C1SC(N)=N2 FASDKYOPVNHBLU-ZETCQYMHSA-N 0.000 claims description 9
- 229960003910 promethazine Drugs 0.000 claims description 9
- 229960002601 protriptyline Drugs 0.000 claims description 9
- BWPIARFWQZKAIA-UHFFFAOYSA-N protriptyline Chemical compound C1=CC2=CC=CC=C2C(CCCNC)C2=CC=CC=C21 BWPIARFWQZKAIA-UHFFFAOYSA-N 0.000 claims description 9
- 229940035613 prozac Drugs 0.000 claims description 9
- 229960001964 quazepam Drugs 0.000 claims description 9
- 229960003770 reboxetine Drugs 0.000 claims description 9
- CBQGYUDMJHNJBX-RTBURBONSA-N reboxetine Chemical compound CCOC1=CC=CC=C1O[C@H](C=1C=CC=CC=1)[C@@H]1OCCNC1 CBQGYUDMJHNJBX-RTBURBONSA-N 0.000 claims description 9
- 229940116246 restoril Drugs 0.000 claims description 9
- 229960000425 rizatriptan Drugs 0.000 claims description 9
- TXHZXHICDBAVJW-UHFFFAOYSA-N rizatriptan Chemical compound C=1[C]2C(CCN(C)C)=CN=C2C=CC=1CN1C=NC=N1 TXHZXHICDBAVJW-UHFFFAOYSA-N 0.000 claims description 9
- 229960001879 ropinirole Drugs 0.000 claims description 9
- UHSKFQJFRQCDBE-UHFFFAOYSA-N ropinirole Chemical compound CCCN(CCC)CCC1=CC=CC2=C1CC(=O)N2 UHSKFQJFRQCDBE-UHFFFAOYSA-N 0.000 claims description 9
- 201000000980 schizophrenia Diseases 0.000 claims description 9
- 229960002060 secobarbital Drugs 0.000 claims description 9
- 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 description 9
- 229940099190 serzone Drugs 0.000 claims description 9
- 229960004425 sibutramine Drugs 0.000 claims description 9
- UNAANXDKBXWMLN-UHFFFAOYSA-N sibutramine Chemical compound C=1C=C(Cl)C=CC=1C1(C(N(C)C)CC(C)C)CCC1 UNAANXDKBXWMLN-UHFFFAOYSA-N 0.000 claims description 9
- 229940061368 sonata Drugs 0.000 claims description 9
- 229960003708 sumatriptan Drugs 0.000 claims description 9
- KQKPFRSPSRPDEB-UHFFFAOYSA-N sumatriptan Chemical compound CNS(=O)(=O)CC1=CC=C2NC=C(CCN(C)C)C2=C1 KQKPFRSPSRPDEB-UHFFFAOYSA-N 0.000 claims description 9
- 229960003188 temazepam Drugs 0.000 claims description 9
- 229940041597 tofranil Drugs 0.000 claims description 9
- 229940063648 tranxene Drugs 0.000 claims description 9
- 229960003741 tranylcypromine Drugs 0.000 claims description 9
- 229960003991 trazodone Drugs 0.000 claims description 9
- PHLBKPHSAVXXEF-UHFFFAOYSA-N trazodone Chemical compound ClC1=CC=CC(N2CCN(CCCN3C(N4C=CC=CC4=N3)=O)CC2)=C1 PHLBKPHSAVXXEF-UHFFFAOYSA-N 0.000 claims description 9
- 229960003386 triazolam Drugs 0.000 claims description 9
- 229960002431 trimipramine Drugs 0.000 claims description 9
- 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 description 9
- 229940072690 valium Drugs 0.000 claims description 9
- 229960004688 venlafaxine Drugs 0.000 claims description 9
- MECHNRXZTMCUDQ-RKHKHRCZSA-N vitamin D2 Chemical compound C1(/[C@@H]2CC[C@@H]([C@]2(CCC1)C)[C@H](C)/C=C/[C@H](C)C(C)C)=C\C=C1\C[C@@H](O)CCC1=C MECHNRXZTMCUDQ-RKHKHRCZSA-N 0.000 claims description 9
- 229940074158 xanax Drugs 0.000 claims description 9
- 229940020965 zoloft Drugs 0.000 claims description 9
- 229940018503 zyban Drugs 0.000 claims description 9
- 206010041250 Social phobia Diseases 0.000 claims description 8
- 229960003528 flurazepam Drugs 0.000 claims description 8
- 229960004372 aripiprazole Drugs 0.000 claims description 7
- 239000000938 histamine H1 antagonist Substances 0.000 claims description 6
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 6
- 238000002360 preparation method Methods 0.000 claims description 6
- 208000019116 sleep disease Diseases 0.000 claims description 6
- 208000022925 sleep disturbance Diseases 0.000 claims description 6
- 208000024827 Alzheimer disease Diseases 0.000 claims description 5
- 208000019901 Anxiety disease Diseases 0.000 claims description 5
- 208000023105 Huntington disease Diseases 0.000 claims description 5
- 229960003792 acrivastine Drugs 0.000 claims description 5
- 230000036506 anxiety Effects 0.000 claims description 5
- 230000036528 appetite Effects 0.000 claims description 5
- 235000019789 appetite Nutrition 0.000 claims description 5
- 229960001128 triprolidine Drugs 0.000 claims description 5
- CBEQULMOCCWAQT-WOJGMQOQSA-N triprolidine Chemical compound C1=CC(C)=CC=C1C(\C=1N=CC=CC=1)=C/CN1CCCC1 CBEQULMOCCWAQT-WOJGMQOQSA-N 0.000 claims description 5
- 229940009065 wellbutrin Drugs 0.000 claims description 5
- JAUOIFJMECXRGI-UHFFFAOYSA-N Neoclaritin Chemical compound C=1C(Cl)=CC=C2C=1CCC1=CC=CN=C1C2=C1CCNCC1 JAUOIFJMECXRGI-UHFFFAOYSA-N 0.000 claims description 4
- 229960001271 desloratadine Drugs 0.000 claims description 4
- 229960003592 fexofenadine Drugs 0.000 claims description 4
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims description 4
- 229960003088 loratadine Drugs 0.000 claims description 4
- JCCNYMKQOSZNPW-UHFFFAOYSA-N loratadine Chemical compound C1CN(C(=O)OCC)CCC1=C1C2=NC=CC=C2CCC2=CC(Cl)=CC=C21 JCCNYMKQOSZNPW-UHFFFAOYSA-N 0.000 claims description 4
- 208000024714 major depressive disease Diseases 0.000 claims description 3
- 201000004311 Gilles de la Tourette syndrome Diseases 0.000 claims description 2
- 208000000323 Tourette Syndrome Diseases 0.000 claims description 2
- 208000016620 Tourette disease Diseases 0.000 claims description 2
- 239000003775 serotonin noradrenalin reuptake inhibitor Substances 0.000 claims 6
- 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 2
- ZZVUWRFHKOJYTH-UHFFFAOYSA-N diphenhydramine Chemical compound C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 ZZVUWRFHKOJYTH-UHFFFAOYSA-N 0.000 claims 2
- XZZXIYZZBJDEEP-UHFFFAOYSA-N imipramine hydrochloride Chemical compound [Cl-].C1CC2=CC=CC=C2N(CCC[NH+](C)C)C2=CC=CC=C21 XZZXIYZZBJDEEP-UHFFFAOYSA-N 0.000 claims 2
- UNHGSHHVDNGCFN-UHFFFAOYSA-N naratriptan Chemical compound C=12[CH]C(CCS(=O)(=O)NC)=CC=C2N=CC=1C1CCN(C)CC1 UNHGSHHVDNGCFN-UHFFFAOYSA-N 0.000 claims 2
- YEHCICAEULNIGD-MZMPZRCHSA-N pergolide Chemical compound C1=CC([C@H]2C[C@@H](CSC)CN([C@@H]2C2)CCC)=C3C2=CNC3=C1 YEHCICAEULNIGD-MZMPZRCHSA-N 0.000 claims 2
- ZTHJULTYCAQOIJ-WXXKFALUSA-N quetiapine fumarate Chemical compound [H+].[H+].[O-]C(=O)\C=C\C([O-])=O.C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12.C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 ZTHJULTYCAQOIJ-WXXKFALUSA-N 0.000 claims 2
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- 239000003420 antiserotonin agent Substances 0.000 abstract description 2
- 239000000952 serotonin receptor agonist Substances 0.000 abstract description 2
- 229940121356 serotonin receptor antagonist Drugs 0.000 abstract description 2
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 description 60
- 230000000694 effects Effects 0.000 description 53
- 102000005962 receptors Human genes 0.000 description 48
- 108020003175 receptors Proteins 0.000 description 48
- 239000000203 mixture Substances 0.000 description 40
- 239000000556 agonist Substances 0.000 description 31
- VRHJBWUIWQOFLF-WLHGVMLRSA-N 2-[2-(4-benzo[b][1,4]benzothiazepin-6-ylpiperazin-1-yl)ethoxy]ethanol;(e)-but-2-enedioic acid Chemical compound OC(=O)\C=C\C(O)=O.C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 VRHJBWUIWQOFLF-WLHGVMLRSA-N 0.000 description 27
- 230000007958 sleep Effects 0.000 description 20
- 229940123685 Monoamine oxidase inhibitor Drugs 0.000 description 17
- 239000002899 monoamine oxidase inhibitor Substances 0.000 description 17
- 229940123445 Tricyclic antidepressant Drugs 0.000 description 16
- 239000003029 tricyclic antidepressant agent Substances 0.000 description 16
- 229940076279 serotonin Drugs 0.000 description 15
- 239000003795 chemical substances by application Substances 0.000 description 13
- 238000009472 formulation Methods 0.000 description 13
- 238000002347 injection Methods 0.000 description 12
- 239000007924 injection Substances 0.000 description 12
- 239000000243 solution Substances 0.000 description 12
- 230000006870 function Effects 0.000 description 11
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 description 10
- 229940002612 prodrug Drugs 0.000 description 10
- 239000000651 prodrug Substances 0.000 description 10
- 108010072553 5-HT2C Serotonin Receptor Proteins 0.000 description 8
- 102000006902 5-HT2C Serotonin Receptor Human genes 0.000 description 8
- 125000000217 alkyl group Chemical group 0.000 description 8
- SPCKHVPPRJWQRZ-UHFFFAOYSA-N 2-benzhydryloxy-n,n-dimethylethanamine;2-hydroxypropane-1,2,3-tricarboxylic acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O.C=1C=CC=CC=1C(OCCN(C)C)C1=CC=CC=C1 SPCKHVPPRJWQRZ-UHFFFAOYSA-N 0.000 description 7
- 230000002411 adverse Effects 0.000 description 7
- 239000002775 capsule Substances 0.000 description 7
- XDDJGVMJFWAHJX-UHFFFAOYSA-N clorazepic acid Chemical compound C12=CC(Cl)=CC=C2NC(=O)C(C(=O)O)N=C1C1=CC=CC=C1 XDDJGVMJFWAHJX-UHFFFAOYSA-N 0.000 description 7
- 208000035475 disorder Diseases 0.000 description 7
- 239000003446 ligand Substances 0.000 description 7
- AMKVXSZCKVJAGH-UHFFFAOYSA-N naratriptan Chemical compound C12=CC(CCS(=O)(=O)NC)=CC=C2NC=C1C1CCN(C)CC1 AMKVXSZCKVJAGH-UHFFFAOYSA-N 0.000 description 7
- YYPWGCZOLGTTER-MZMPZRCHSA-N pergolide Chemical compound C1=CC=C2[C@H]3C[C@@H](CSC)CN(CCC)[C@@H]3CC3=CN=C1[C]32 YYPWGCZOLGTTER-MZMPZRCHSA-N 0.000 description 7
- 230000000862 serotonergic effect Effects 0.000 description 7
- 239000000725 suspension Substances 0.000 description 7
- 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 description 6
- 101710138091 5-hydroxytryptamine receptor 2A Proteins 0.000 description 6
- 239000000969 carrier Substances 0.000 description 6
- 210000004027 cell Anatomy 0.000 description 6
- 229910052757 nitrogen Inorganic materials 0.000 description 6
- 230000002093 peripheral effect Effects 0.000 description 6
- 230000004044 response Effects 0.000 description 6
- 230000002441 reversible effect Effects 0.000 description 6
- 239000000126 substance Substances 0.000 description 6
- 208000024891 symptom Diseases 0.000 description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 6
- 102000003688 G-Protein-Coupled Receptors Human genes 0.000 description 5
- 108090000045 G-Protein-Coupled Receptors Proteins 0.000 description 5
- 239000004480 active ingredient Substances 0.000 description 5
- 230000000561 anti-psychotic effect Effects 0.000 description 5
- 230000004071 biological effect Effects 0.000 description 5
- 239000006184 cosolvent Substances 0.000 description 5
- 239000008298 dragée Substances 0.000 description 5
- 239000004615 ingredient Substances 0.000 description 5
- 238000012423 maintenance Methods 0.000 description 5
- 238000007911 parenteral administration Methods 0.000 description 5
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 5
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 5
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 5
- 239000003826 tablet Substances 0.000 description 5
- 208000020925 Bipolar disease Diseases 0.000 description 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 4
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 4
- 108091006027 G proteins Proteins 0.000 description 4
- 108010010803 Gelatin Proteins 0.000 description 4
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 4
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 4
- 208000019695 Migraine disease Diseases 0.000 description 4
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 4
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 4
- 208000007536 Thrombosis Diseases 0.000 description 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 4
- 239000002253 acid Substances 0.000 description 4
- 230000004913 activation Effects 0.000 description 4
- 230000008485 antagonism Effects 0.000 description 4
- 229940005529 antipsychotics Drugs 0.000 description 4
- 230000006399 behavior Effects 0.000 description 4
- 229910052799 carbon Inorganic materials 0.000 description 4
- 230000037011 constitutive activity Effects 0.000 description 4
- 238000009826 distribution Methods 0.000 description 4
- 230000002526 effect on cardiovascular system Effects 0.000 description 4
- 125000005678 ethenylene group Chemical group [H]C([*:1])=C([H])[*:2] 0.000 description 4
- 229940104076 fluoxetine / olanzapine Drugs 0.000 description 4
- 239000008273 gelatin Substances 0.000 description 4
- 229920000159 gelatin Polymers 0.000 description 4
- 235000019322 gelatine Nutrition 0.000 description 4
- 235000011852 gelatine desserts Nutrition 0.000 description 4
- 125000001072 heteroaryl group Chemical group 0.000 description 4
- 230000002209 hydrophobic effect Effects 0.000 description 4
- 239000002502 liposome Substances 0.000 description 4
- 206010027599 migraine Diseases 0.000 description 4
- 239000002858 neurotransmitter agent Substances 0.000 description 4
- 229910052760 oxygen Inorganic materials 0.000 description 4
- 230000000144 pharmacologic effect Effects 0.000 description 4
- 229920001223 polyethylene glycol Polymers 0.000 description 4
- 108090000623 proteins and genes Proteins 0.000 description 4
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 4
- 239000002400 serotonin 2A antagonist Substances 0.000 description 4
- 239000003381 stabilizer Substances 0.000 description 4
- 229910052717 sulfur Inorganic materials 0.000 description 4
- 238000013268 sustained release Methods 0.000 description 4
- 239000012730 sustained-release form Substances 0.000 description 4
- 229940034173 symbyax Drugs 0.000 description 4
- 210000001519 tissue Anatomy 0.000 description 4
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 4
- 230000002792 vascular Effects 0.000 description 4
- 102000056834 5-HT2 Serotonin Receptors Human genes 0.000 description 3
- 108091005479 5-HT2 receptors Proteins 0.000 description 3
- 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 3
- 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 3
- 102000030782 GTP binding Human genes 0.000 description 3
- 108091000058 GTP-Binding Proteins 0.000 description 3
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 3
- 101150104779 HTR2A gene Proteins 0.000 description 3
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 3
- 241000124008 Mammalia Species 0.000 description 3
- 241001465754 Metazoa Species 0.000 description 3
- 239000002202 Polyethylene glycol Substances 0.000 description 3
- 229940121991 Serotonin and norepinephrine reuptake inhibitor Drugs 0.000 description 3
- 230000001800 adrenalinergic effect Effects 0.000 description 3
- 239000000443 aerosol Substances 0.000 description 3
- 150000001408 amides Chemical class 0.000 description 3
- 230000001430 anti-depressive effect Effects 0.000 description 3
- 239000000935 antidepressant agent Substances 0.000 description 3
- 150000004030 azacyclic compounds Chemical class 0.000 description 3
- 239000002585 base Substances 0.000 description 3
- 230000005540 biological transmission Effects 0.000 description 3
- 210000004556 brain Anatomy 0.000 description 3
- 210000003169 central nervous system Anatomy 0.000 description 3
- 230000007423 decrease Effects 0.000 description 3
- 230000003291 dopaminomimetic effect Effects 0.000 description 3
- 239000003937 drug carrier Substances 0.000 description 3
- 239000000839 emulsion Substances 0.000 description 3
- 150000002148 esters Chemical class 0.000 description 3
- 230000000742 histaminergic effect Effects 0.000 description 3
- 230000006698 induction Effects 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 239000008101 lactose Substances 0.000 description 3
- 239000007788 liquid Substances 0.000 description 3
- 230000001730 monoaminergic effect Effects 0.000 description 3
- 239000006187 pill Substances 0.000 description 3
- 239000000843 powder Substances 0.000 description 3
- 230000008569 process Effects 0.000 description 3
- 108090000765 processed proteins & peptides Proteins 0.000 description 3
- 102000004169 proteins and genes Human genes 0.000 description 3
- 208000020016 psychiatric disease Diseases 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- 230000001624 sedative effect Effects 0.000 description 3
- 239000000600 sorbitol Substances 0.000 description 3
- 235000000346 sugar Nutrition 0.000 description 3
- 239000004094 surface-active agent Substances 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 3
- 239000003981 vehicle Substances 0.000 description 3
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 description 2
- 206010001488 Aggression Diseases 0.000 description 2
- 206010001497 Agitation Diseases 0.000 description 2
- 208000007848 Alcoholism Diseases 0.000 description 2
- 208000032841 Bulimia Diseases 0.000 description 2
- 206010006550 Bulimia nervosa Diseases 0.000 description 2
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 2
- IVOMOUWHDPKRLL-KQYNXXCUSA-N Cyclic adenosine monophosphate Chemical compound C([C@H]1O2)OP(O)(=O)O[C@H]1[C@@H](O)[C@@H]2N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-KQYNXXCUSA-N 0.000 description 2
- 102000004980 Dopamine D2 Receptors Human genes 0.000 description 2
- 108090001111 Dopamine D2 Receptors Proteins 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- VGGSQFUCUMXWEO-UHFFFAOYSA-N Ethene Chemical compound C=C VGGSQFUCUMXWEO-UHFFFAOYSA-N 0.000 description 2
- 239000005977 Ethylene Substances 0.000 description 2
- 102000005915 GABA Receptors Human genes 0.000 description 2
- 108010005551 GABA Receptors Proteins 0.000 description 2
- SQUHHTBVTRBESD-UHFFFAOYSA-N Hexa-Ac-myo-Inositol Natural products CC(=O)OC1C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C(OC(C)=O)C1OC(C)=O SQUHHTBVTRBESD-UHFFFAOYSA-N 0.000 description 2
- 241000282412 Homo Species 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- 102000004310 Ion Channels Human genes 0.000 description 2
- 102000004108 Neurotransmitter Receptors Human genes 0.000 description 2
- 108090000590 Neurotransmitter Receptors Proteins 0.000 description 2
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 2
- 208000021384 Obsessive-Compulsive disease Diseases 0.000 description 2
- 229910019142 PO4 Inorganic materials 0.000 description 2
- 208000002193 Pain Diseases 0.000 description 2
- 206010033664 Panic attack Diseases 0.000 description 2
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- ZGUGWUXLJSTTMA-UHFFFAOYSA-N Promazinum Chemical compound C1=CC=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZGUGWUXLJSTTMA-UHFFFAOYSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 208000006011 Stroke Diseases 0.000 description 2
- GWEVSGVZZGPLCZ-UHFFFAOYSA-N Titan oxide Chemical compound O=[Ti]=O GWEVSGVZZGPLCZ-UHFFFAOYSA-N 0.000 description 2
- 206010044565 Tremor Diseases 0.000 description 2
- IVOMOUWHDPKRLL-UHFFFAOYSA-N UNPD107823 Natural products O1C2COP(O)(=O)OC2C(O)C1N1C(N=CN=C2N)=C2N=C1 IVOMOUWHDPKRLL-UHFFFAOYSA-N 0.000 description 2
- 206010047163 Vasospasm Diseases 0.000 description 2
- 238000010521 absorption reaction Methods 0.000 description 2
- 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 2
- 230000002776 aggregation Effects 0.000 description 2
- 238000004220 aggregation Methods 0.000 description 2
- 201000007930 alcohol dependence Diseases 0.000 description 2
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 125000004103 aminoalkyl group Chemical group 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 208000022531 anorexia Diseases 0.000 description 2
- 229940005513 antidepressants Drugs 0.000 description 2
- 239000000228 antimanic agent Substances 0.000 description 2
- 239000007864 aqueous solution Substances 0.000 description 2
- 125000003710 aryl alkyl group Chemical group 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- 150000001557 benzodiazepines Chemical class 0.000 description 2
- 208000028683 bipolar I disease Diseases 0.000 description 2
- 208000025307 bipolar depression Diseases 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 230000036760 body temperature Effects 0.000 description 2
- SXDBWCPKPHAZSM-UHFFFAOYSA-N bromic acid Chemical compound OBr(=O)=O SXDBWCPKPHAZSM-UHFFFAOYSA-N 0.000 description 2
- 239000007853 buffer solution Substances 0.000 description 2
- 239000004202 carbamide Substances 0.000 description 2
- 235000013877 carbamide Nutrition 0.000 description 2
- 239000001768 carboxy methyl cellulose Substances 0.000 description 2
- 210000000748 cardiovascular system Anatomy 0.000 description 2
- 230000001413 cellular effect Effects 0.000 description 2
- 230000005754 cellular signaling Effects 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 238000006243 chemical reaction Methods 0.000 description 2
- 238000000576 coating method Methods 0.000 description 2
- 230000001149 cognitive effect Effects 0.000 description 2
- 230000001054 cortical effect Effects 0.000 description 2
- 229940095074 cyclic amp Drugs 0.000 description 2
- 125000004122 cyclic group Chemical group 0.000 description 2
- 125000000753 cycloalkyl group Chemical group 0.000 description 2
- 206010061428 decreased appetite Diseases 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 150000001982 diacylglycerols Chemical class 0.000 description 2
- 239000002552 dosage form Substances 0.000 description 2
- 201000002545 drug psychosis Diseases 0.000 description 2
- 230000007937 eating Effects 0.000 description 2
- 239000006274 endogenous ligand Substances 0.000 description 2
- 238000005516 engineering process Methods 0.000 description 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 description 2
- CCIVGXIOQKPBKL-UHFFFAOYSA-M ethanesulfonate Chemical compound CCS([O-])(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-M 0.000 description 2
- 239000000945 filler Substances 0.000 description 2
- 210000005095 gastrointestinal system Anatomy 0.000 description 2
- 239000000499 gel Substances 0.000 description 2
- 230000002489 hematologic effect Effects 0.000 description 2
- 210000005096 hematological system Anatomy 0.000 description 2
- 125000004475 heteroaralkyl group Chemical group 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 150000002431 hydrogen Chemical group 0.000 description 2
- 125000002768 hydroxyalkyl group Chemical group 0.000 description 2
- 238000000338 in vitro Methods 0.000 description 2
- 238000001727 in vivo Methods 0.000 description 2
- 238000001802 infusion Methods 0.000 description 2
- 230000005764 inhibitory process Effects 0.000 description 2
- 229960000367 inositol Drugs 0.000 description 2
- 230000035992 intercellular communication Effects 0.000 description 2
- 230000003834 intracellular effect Effects 0.000 description 2
- 238000007918 intramuscular administration Methods 0.000 description 2
- 238000001990 intravenous administration Methods 0.000 description 2
- 238000003874 inverse correlation nuclear magnetic resonance spectroscopy Methods 0.000 description 2
- 208000028867 ischemia Diseases 0.000 description 2
- 230000002197 limbic effect Effects 0.000 description 2
- 230000033001 locomotion Effects 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 239000000463 material Substances 0.000 description 2
- 238000002483 medication Methods 0.000 description 2
- 239000012528 membrane Substances 0.000 description 2
- 230000003340 mental effect Effects 0.000 description 2
- 229940098779 methanesulfonic acid Drugs 0.000 description 2
- 150000007522 mineralic acids Chemical class 0.000 description 2
- 238000002156 mixing Methods 0.000 description 2
- 230000009456 molecular mechanism Effects 0.000 description 2
- 230000003551 muscarinic effect Effects 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- 229910017604 nitric acid Inorganic materials 0.000 description 2
- 210000000929 nociceptor Anatomy 0.000 description 2
- 108091008700 nociceptors Proteins 0.000 description 2
- 239000003921 oil Substances 0.000 description 2
- 235000019198 oils Nutrition 0.000 description 2
- 239000003960 organic solvent Substances 0.000 description 2
- 239000001301 oxygen Substances 0.000 description 2
- 208000019906 panic disease Diseases 0.000 description 2
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-UHFFFAOYSA-N 0.000 description 2
- 230000001575 pathological effect Effects 0.000 description 2
- 230000000149 penetrating effect Effects 0.000 description 2
- 239000000825 pharmaceutical preparation Substances 0.000 description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 description 2
- WVDDGKGOMKODPV-ZQBYOMGUSA-N phenyl(114C)methanol Chemical compound O[14CH2]C1=CC=CC=C1 WVDDGKGOMKODPV-ZQBYOMGUSA-N 0.000 description 2
- 235000021317 phosphate Nutrition 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 2
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 2
- 229940068968 polysorbate 80 Drugs 0.000 description 2
- 229920000053 polysorbate 80 Polymers 0.000 description 2
- 238000012545 processing Methods 0.000 description 2
- 210000004129 prosencephalon Anatomy 0.000 description 2
- 229960004889 salicylic acid Drugs 0.000 description 2
- CDAISMWEOUEBRE-UHFFFAOYSA-N scyllo-inosotol Natural products OC1C(O)C(O)C(O)C(O)C1O CDAISMWEOUEBRE-UHFFFAOYSA-N 0.000 description 2
- 230000003248 secreting effect Effects 0.000 description 2
- 229940126570 serotonin reuptake inhibitor Drugs 0.000 description 2
- 239000003772 serotonin uptake inhibitor Substances 0.000 description 2
- 230000009329 sexual behaviour Effects 0.000 description 2
- 230000011664 signaling Effects 0.000 description 2
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 2
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 125000003107 substituted aryl group Chemical group 0.000 description 2
- 150000008163 sugars Chemical class 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 239000000454 talc Substances 0.000 description 2
- 229910052623 talc Inorganic materials 0.000 description 2
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 230000025102 vascular smooth muscle contraction Effects 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
- LNAZSHAWQACDHT-XIYTZBAFSA-N (2r,3r,4s,5r,6s)-4,5-dimethoxy-2-(methoxymethyl)-3-[(2s,3r,4s,5r,6r)-3,4,5-trimethoxy-6-(methoxymethyl)oxan-2-yl]oxy-6-[(2r,3r,4s,5r,6r)-4,5,6-trimethoxy-2-(methoxymethyl)oxan-3-yl]oxyoxane Chemical compound CO[C@@H]1[C@@H](OC)[C@H](OC)[C@@H](COC)O[C@H]1O[C@H]1[C@H](OC)[C@@H](OC)[C@H](O[C@H]2[C@@H]([C@@H](OC)[C@H](OC)O[C@@H]2COC)OC)O[C@@H]1COC LNAZSHAWQACDHT-XIYTZBAFSA-N 0.000 description 1
- GBBSUAFBMRNDJC-MRXNPFEDSA-N (5R)-zopiclone Chemical compound C1CN(C)CCN1C(=O)O[C@@H]1C2=NC=CN=C2C(=O)N1C1=CC=C(Cl)C=N1 GBBSUAFBMRNDJC-MRXNPFEDSA-N 0.000 description 1
- HXTGXYRHXAGCFP-OAQYLSRUSA-N (r)-(2,3-dimethoxyphenyl)-[1-[2-(4-fluorophenyl)ethyl]piperidin-4-yl]methanol Chemical compound COC1=CC=CC([C@H](O)C2CCN(CCC=3C=CC(F)=CC=3)CC2)=C1OC HXTGXYRHXAGCFP-OAQYLSRUSA-N 0.000 description 1
- DDMOUSALMHHKOS-UHFFFAOYSA-N 1,2-dichloro-1,1,2,2-tetrafluoroethane Chemical compound FC(F)(Cl)C(F)(F)Cl DDMOUSALMHHKOS-UHFFFAOYSA-N 0.000 description 1
- QVZXBANNBNDOFW-UHFFFAOYSA-N 1-(4-phenylbutyl)piperidine Chemical compound C1CCCCN1CCCCC1=CC=CC=C1 QVZXBANNBNDOFW-UHFFFAOYSA-N 0.000 description 1
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 1
- HZLCGUXUOFWCCN-UHFFFAOYSA-N 2-hydroxynonadecane-1,2,3-tricarboxylic acid Chemical compound CCCCCCCCCCCCCCCCC(C(O)=O)C(O)(C(O)=O)CC(O)=O HZLCGUXUOFWCCN-UHFFFAOYSA-N 0.000 description 1
- 239000003477 4 aminobutyric acid receptor stimulating agent Substances 0.000 description 1
- 102100024959 5-hydroxytryptamine receptor 2C Human genes 0.000 description 1
- 101710138093 5-hydroxytryptamine receptor 2C Proteins 0.000 description 1
- 244000215068 Acacia senegal Species 0.000 description 1
- 108060003345 Adrenergic Receptor Proteins 0.000 description 1
- 102000017910 Adrenergic receptor Human genes 0.000 description 1
- 229920001817 Agar Polymers 0.000 description 1
- 206010001540 Akathisia Diseases 0.000 description 1
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound 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 GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 1
- 206010002942 Apathy Diseases 0.000 description 1
- 239000004475 Arginine Substances 0.000 description 1
- 241000283690 Bos taurus Species 0.000 description 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000283707 Capra Species 0.000 description 1
- 241000700198 Cavia Species 0.000 description 1
- 241000282693 Cercopithecidae Species 0.000 description 1
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 206010010744 Conjunctivitis allergic Diseases 0.000 description 1
- 229920002261 Corn starch Polymers 0.000 description 1
- 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 1
- 101150049660 DRD2 gene Proteins 0.000 description 1
- 208000020401 Depressive disease Diseases 0.000 description 1
- 229920002307 Dextran Polymers 0.000 description 1
- 239000004338 Dichlorodifluoromethane Substances 0.000 description 1
- XBPCUCUWBYBCDP-UHFFFAOYSA-N Dicyclohexylamine Chemical compound C1CCCCC1NC1CCCCC1 XBPCUCUWBYBCDP-UHFFFAOYSA-N 0.000 description 1
- LVGKNOAMLMIIKO-UHFFFAOYSA-N Elaidinsaeure-aethylester Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC LVGKNOAMLMIIKO-UHFFFAOYSA-N 0.000 description 1
- 206010014557 Emotional poverty Diseases 0.000 description 1
- 241000792859 Enema Species 0.000 description 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 102000034286 G proteins Human genes 0.000 description 1
- ZXRVKCBLGJOCEE-UHFFFAOYSA-N Gaboxadol Chemical compound C1NCCC2=C1ONC2=O ZXRVKCBLGJOCEE-UHFFFAOYSA-N 0.000 description 1
- WQZGKKKJIJFFOK-GASJEMHNSA-N Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- 229920000084 Gum arabic Polymers 0.000 description 1
- 208000004547 Hallucinations Diseases 0.000 description 1
- 102000000543 Histamine Receptors Human genes 0.000 description 1
- 108010002059 Histamine Receptors Proteins 0.000 description 1
- 229940122236 Histamine receptor antagonist Drugs 0.000 description 1
- 241001272567 Hominoidea Species 0.000 description 1
- 208000001953 Hypotension Diseases 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- CBIAWPMZSFFRGN-UHFFFAOYSA-N Indiplon Chemical compound CC(=O)N(C)C1=CC=CC(C=2N3N=CC(=C3N=CC=2)C(=O)C=2SC=CC=2)=C1 CBIAWPMZSFFRGN-UHFFFAOYSA-N 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 1
- 229930195725 Mannitol Natural products 0.000 description 1
- 102000010909 Monoamine Oxidase Human genes 0.000 description 1
- 108010062431 Monoamine oxidase Proteins 0.000 description 1
- 208000019022 Mood disease Diseases 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 description 1
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 description 1
- HSHXDCVZWHOWCS-UHFFFAOYSA-N N'-hexadecylthiophene-2-carbohydrazide Chemical compound CCCCCCCCCCCCCCCCNNC(=O)c1cccs1 HSHXDCVZWHOWCS-UHFFFAOYSA-N 0.000 description 1
- MBBZMMPHUWSWHV-BDVNFPICSA-N N-methylglucamine Chemical compound CNC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO MBBZMMPHUWSWHV-BDVNFPICSA-N 0.000 description 1
- 229940121985 Non-benzodiazepine hypnotic Drugs 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 241000282579 Pan Species 0.000 description 1
- 208000027089 Parkinsonian disease Diseases 0.000 description 1
- 206010034010 Parkinsonism Diseases 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 208000001431 Psychomotor Agitation Diseases 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 230000010799 Receptor Interactions Effects 0.000 description 1
- 206010039085 Rhinitis allergic Diseases 0.000 description 1
- 206010039897 Sedation Diseases 0.000 description 1
- 208000032140 Sleepiness Diseases 0.000 description 1
- 206010041243 Social avoidant behaviour Diseases 0.000 description 1
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 1
- 229920002125 Sokalan® Polymers 0.000 description 1
- 206010041349 Somnolence Diseases 0.000 description 1
- 208000011963 Substance-induced psychotic disease Diseases 0.000 description 1
- 231100000393 Substance-induced psychotic disorder Toxicity 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- 206010043118 Tardive Dyskinesia Diseases 0.000 description 1
- 229920001615 Tragacanth Polymers 0.000 description 1
- 208000024780 Urticaria Diseases 0.000 description 1
- RLFKILXOLJVUNF-UHFFFAOYSA-N abecarnil Chemical compound C1=C2C=3C(COC)=C(C(=O)OC(C)C)N=CC=3NC2=CC=C1OCC1=CC=CC=C1 RLFKILXOLJVUNF-UHFFFAOYSA-N 0.000 description 1
- 229950000552 abecarnil Drugs 0.000 description 1
- 235000010489 acacia gum Nutrition 0.000 description 1
- 239000000205 acacia gum Substances 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 230000001154 acute effect Effects 0.000 description 1
- 125000002015 acyclic group Chemical group 0.000 description 1
- 239000008272 agar Substances 0.000 description 1
- 235000010419 agar Nutrition 0.000 description 1
- 229940040563 agaric acid Drugs 0.000 description 1
- 230000008484 agonism Effects 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
- 229910052783 alkali metal Inorganic materials 0.000 description 1
- 229910052784 alkaline earth metal Inorganic materials 0.000 description 1
- 208000002205 allergic conjunctivitis Diseases 0.000 description 1
- 201000010105 allergic rhinitis Diseases 0.000 description 1
- 201000010435 allergic urticaria Diseases 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 150000001412 amines Chemical group 0.000 description 1
- 150000003863 ammonium salts Chemical class 0.000 description 1
- 230000003321 amplification Effects 0.000 description 1
- 239000008346 aqueous phase Substances 0.000 description 1
- 239000003125 aqueous solvent Substances 0.000 description 1
- 239000008135 aqueous vehicle Substances 0.000 description 1
- ODKSFYDXXFIFQN-UHFFFAOYSA-N arginine Natural products OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 description 1
- 239000000305 astragalus gummifer gum Substances 0.000 description 1
- 208000024998 atopic conjunctivitis Diseases 0.000 description 1
- 229940125717 barbiturate Drugs 0.000 description 1
- 230000004888 barrier function Effects 0.000 description 1
- 230000008901 benefit Effects 0.000 description 1
- 102000014974 beta2-adrenergic receptor activity proteins Human genes 0.000 description 1
- 108040006828 beta2-adrenergic receptor activity proteins Proteins 0.000 description 1
- 239000011230 binding agent Substances 0.000 description 1
- 238000011953 bioanalysis Methods 0.000 description 1
- 229920000249 biocompatible polymer Polymers 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000037396 body weight Effects 0.000 description 1
- 229910052791 calcium Inorganic materials 0.000 description 1
- 239000011575 calcium Substances 0.000 description 1
- 239000001569 carbon dioxide Substances 0.000 description 1
- 229910002092 carbon dioxide Inorganic materials 0.000 description 1
- 229960004424 carbon dioxide Drugs 0.000 description 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 description 1
- 230000000747 cardiac effect Effects 0.000 description 1
- 210000000170 cell membrane Anatomy 0.000 description 1
- 239000001913 cellulose Substances 0.000 description 1
- 229920002678 cellulose Polymers 0.000 description 1
- 238000012512 characterization method Methods 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- 229940110456 cocoa butter Drugs 0.000 description 1
- 235000019868 cocoa butter Nutrition 0.000 description 1
- 208000010877 cognitive disease Diseases 0.000 description 1
- 230000003920 cognitive function Effects 0.000 description 1
- 238000002648 combination therapy Methods 0.000 description 1
- 230000002860 competitive effect Effects 0.000 description 1
- 238000011340 continuous therapy Methods 0.000 description 1
- 239000008120 corn starch Substances 0.000 description 1
- 229940099112 cornstarch Drugs 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 230000002950 deficient Effects 0.000 description 1
- 239000003405 delayed action preparation Substances 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 230000001627 detrimental effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- 239000008121 dextrose Substances 0.000 description 1
- 238000003745 diagnosis Methods 0.000 description 1
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 description 1
- 235000019404 dichlorodifluoromethane Nutrition 0.000 description 1
- 229940042935 dichlorodifluoromethane Drugs 0.000 description 1
- 229940087091 dichlorotetrafluoroethane Drugs 0.000 description 1
- 235000014113 dietary fatty acids Nutrition 0.000 description 1
- LOKCTEFSRHRXRJ-UHFFFAOYSA-I dipotassium trisodium dihydrogen phosphate hydrogen phosphate dichloride Chemical compound P(=O)(O)(O)[O-].[K+].P(=O)(O)([O-])[O-].[Na+].[Na+].[Cl-].[K+].[Cl-].[Na+] LOKCTEFSRHRXRJ-UHFFFAOYSA-I 0.000 description 1
- 239000002270 dispersing agent Substances 0.000 description 1
- 238000012377 drug delivery Methods 0.000 description 1
- 238000009509 drug development Methods 0.000 description 1
- 239000000975 dye Substances 0.000 description 1
- 230000001804 emulsifying effect Effects 0.000 description 1
- 239000007920 enema Substances 0.000 description 1
- 229940079360 enema for constipation Drugs 0.000 description 1
- VAIOZOCLKVMIMN-PRJWTAEASA-N eplivanserin Chemical compound C=1C=CC=C(F)C=1\C(=N/OCCN(C)C)\C=C\C1=CC=C(O)C=C1 VAIOZOCLKVMIMN-PRJWTAEASA-N 0.000 description 1
- 229950000789 eplivanserin Drugs 0.000 description 1
- 229960001578 eszopiclone Drugs 0.000 description 1
- LVGKNOAMLMIIKO-QXMHVHEDSA-N ethyl oleate Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC LVGKNOAMLMIIKO-QXMHVHEDSA-N 0.000 description 1
- 229940093471 ethyl oleate Drugs 0.000 description 1
- 238000002474 experimental method Methods 0.000 description 1
- 239000000194 fatty acid Substances 0.000 description 1
- 229930195729 fatty acid Natural products 0.000 description 1
- 239000010685 fatty oil Substances 0.000 description 1
- 210000002950 fibroblast Anatomy 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 239000012458 free base Substances 0.000 description 1
- 230000004927 fusion Effects 0.000 description 1
- 229950004346 gaboxadol Drugs 0.000 description 1
- 239000007789 gas Substances 0.000 description 1
- 229940014259 gelatin Drugs 0.000 description 1
- 230000002068 genetic effect Effects 0.000 description 1
- 125000005456 glyceride group Chemical group 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 238000000227 grinding Methods 0.000 description 1
- UYTPUPDQBNUYGX-UHFFFAOYSA-N guanine Chemical class O=C1NC(N)=NC2=C1N=CN2 UYTPUPDQBNUYGX-UHFFFAOYSA-N 0.000 description 1
- 230000036541 health Effects 0.000 description 1
- 238000004128 high performance liquid chromatography Methods 0.000 description 1
- 231100000171 higher toxicity Toxicity 0.000 description 1
- 229920001600 hydrophobic polymer Polymers 0.000 description 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 description 1
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 description 1
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 description 1
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 description 1
- 208000021822 hypotensive Diseases 0.000 description 1
- 230000001077 hypotensive effect Effects 0.000 description 1
- 230000001771 impaired effect Effects 0.000 description 1
- 239000007943 implant Substances 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 229950003867 indiplon Drugs 0.000 description 1
- 230000001939 inductive effect Effects 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000000968 intestinal effect Effects 0.000 description 1
- 238000010255 intramuscular injection Methods 0.000 description 1
- 239000007927 intramuscular injection Substances 0.000 description 1
- 238000007912 intraperitoneal administration Methods 0.000 description 1
- 238000007913 intrathecal administration Methods 0.000 description 1
- 238000010253 intravenous injection Methods 0.000 description 1
- 238000007914 intraventricular administration Methods 0.000 description 1
- 239000003456 ion exchange resin Substances 0.000 description 1
- 229920003303 ion-exchange polymer Polymers 0.000 description 1
- 230000007794 irritation Effects 0.000 description 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 description 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 description 1
- 229960005417 ketanserin Drugs 0.000 description 1
- 239000004922 lacquer Substances 0.000 description 1
- 229940057995 liquid paraffin Drugs 0.000 description 1
- 231100000053 low toxicity Toxicity 0.000 description 1
- 239000000314 lubricant Substances 0.000 description 1
- 229940012618 lunesta Drugs 0.000 description 1
- 159000000003 magnesium salts Chemical class 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 230000003211 malignant effect Effects 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 230000010534 mechanism of action Effects 0.000 description 1
- 229910052751 metal Inorganic materials 0.000 description 1
- 239000002184 metal Substances 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 238000010369 molecular cloning Methods 0.000 description 1
- 230000007659 motor function Effects 0.000 description 1
- 239000006199 nebulizer Substances 0.000 description 1
- 239000003176 neuroleptic agent Substances 0.000 description 1
- 230000000701 neuroleptic 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
- 238000003199 nucleic acid amplification method Methods 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- 150000007530 organic bases Chemical class 0.000 description 1
- 150000002894 organic compounds Chemical class 0.000 description 1
- 229920000620 organic polymer Polymers 0.000 description 1
- 239000003791 organic solvent mixture Substances 0.000 description 1
- 125000001190 organyl group Chemical group 0.000 description 1
- 230000001991 pathophysiological effect Effects 0.000 description 1
- 239000008177 pharmaceutical agent Substances 0.000 description 1
- 238000001050 pharmacotherapy Methods 0.000 description 1
- 150000002990 phenothiazines Chemical class 0.000 description 1
- 239000002953 phosphate buffered saline Substances 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 239000002504 physiological saline solution Substances 0.000 description 1
- 239000000049 pigment Substances 0.000 description 1
- 230000036470 plasma concentration Effects 0.000 description 1
- 229920003023 plastic Polymers 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000004014 plasticizer Substances 0.000 description 1
- 229940068886 polyethylene glycol 300 Drugs 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
- 238000010837 poor prognosis Methods 0.000 description 1
- XAEFZNCEHLXOMS-UHFFFAOYSA-M potassium benzoate Chemical compound [K+].[O-]C(=O)C1=CC=CC=C1 XAEFZNCEHLXOMS-UHFFFAOYSA-M 0.000 description 1
- 229920001592 potato starch Polymers 0.000 description 1
- 229940116317 potato starch Drugs 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 239000003755 preservative agent Substances 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 239000003380 propellant Substances 0.000 description 1
- 125000006239 protecting group Chemical group 0.000 description 1
- 230000029983 protein stabilization Effects 0.000 description 1
- 230000004461 rapid eye movement Effects 0.000 description 1
- 239000000018 receptor agonist Substances 0.000 description 1
- 229940044601 receptor agonist Drugs 0.000 description 1
- 230000000306 recurrent effect Effects 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- 238000011160 research Methods 0.000 description 1
- 230000029058 respiratory gaseous exchange Effects 0.000 description 1
- 229940100486 rice starch Drugs 0.000 description 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 description 1
- 229950009626 ritanserin Drugs 0.000 description 1
- 230000036280 sedation Effects 0.000 description 1
- 239000000932 sedative agent Substances 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
- 230000004620 sleep latency Effects 0.000 description 1
- 230000037321 sleepiness Effects 0.000 description 1
- 230000037322 slow-wave sleep Effects 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- 239000011780 sodium chloride Substances 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000012439 solid excipient Substances 0.000 description 1
- 230000002269 spontaneous effect Effects 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 239000002511 suppository base Substances 0.000 description 1
- 230000004083 survival effect Effects 0.000 description 1
- 239000000375 suspending agent Substances 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000004408 titanium dioxide Substances 0.000 description 1
- 238000011200 topical administration Methods 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 231100000041 toxicology testing Toxicity 0.000 description 1
- 238000012549 training Methods 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 description 1
- 229940029284 trichlorofluoromethane Drugs 0.000 description 1
- LENZDBCJOHFCAS-UHFFFAOYSA-N tris Chemical compound OCC(N)(CO)CO LENZDBCJOHFCAS-UHFFFAOYSA-N 0.000 description 1
- 229940100445 wheat starch Drugs 0.000 description 1
- 229960000820 zopiclone Drugs 0.000 description 1
- AIFRHYZBTHREPW-UHFFFAOYSA-N β-carboline Chemical class N1=CC=C2C3=CC=CC=C3NC2=C1 AIFRHYZBTHREPW-UHFFFAOYSA-N 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
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
- A61K31/138—Aryloxyalkylamines, e.g. propranolol, tamoxifen, phenoxybenzamine
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4468—Non condensed piperidines, e.g. piperocaine having a nitrogen directly attached in position 4, e.g. clebopride, fentanyl
-
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- 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
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- 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
- A61P25/20—Hypnotics; Sedatives
-
- 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
- A61P25/22—Anxiolytics
-
- 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
-
- 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
- A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
- A61P25/36—Opioid-abuse
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Psychiatry (AREA)
- Dermatology (AREA)
- Addiction (AREA)
- Psychology (AREA)
- Anesthesiology (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US10/850,819 US7820695B2 (en) | 2004-05-21 | 2004-05-21 | Selective serotonin receptor inverse agonists as therapeutics for disease |
| US10/854,035 US20050261278A1 (en) | 2004-05-21 | 2004-05-24 | Selective serotonin receptor inverse agonists as therapeutics for disease |
| PCT/US2005/017808 WO2005112927A1 (en) | 2004-05-21 | 2005-05-20 | Selective serotonin receptor inverse agonists as therapeutics for disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| MXPA06013454A true MXPA06013454A (es) | 2007-03-01 |
Family
ID=34970819
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MXPA06013454A MXPA06013454A (es) | 2004-05-21 | 2005-05-20 | Agonistas inversos del receptor de serotonina selectivos como terapeuticos para enfermedad. |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US20050261278A1 (cg-RX-API-DMAC7.html) |
| EP (2) | EP1750705A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2008500390A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2005244982B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2567704C (cg-RX-API-DMAC7.html) |
| MX (1) | MXPA06013454A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2442607C2 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2005112927A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE348808T1 (de) | 2000-03-06 | 2007-01-15 | Acadia Pharm Inc | Azacyclische verbindungen zur verwendung in der behandlung von mit serotonin verwandten krankheiten |
| US6911452B2 (en) | 2001-12-28 | 2005-06-28 | Acadia Pharmaceuticals Inc. | Spiroazacyclic compounds as monoamine receptor modulators |
| US7253186B2 (en) | 2002-06-24 | 2007-08-07 | Carl-Magnus Andersson | N-substituted piperidine derivatives as serotonin receptor agents |
| US7538222B2 (en) | 2002-06-24 | 2009-05-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| AU2003247615B2 (en) | 2002-06-24 | 2007-08-09 | Acadia Pharmaceuticals Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| NZ541146A (en) | 2003-01-16 | 2009-04-30 | Acadia Pharm Inc | N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide, also known as ACP-103, and its tartrate salt as therapeutics for neurodegenerative diseases |
| US7884096B2 (en) * | 2003-12-02 | 2011-02-08 | Pharmaneuroboost N.V. | Method of treating mental disorders using of D4 and 5-HT2A antagonists, inverse agonists or partial agonists |
| US20050203130A1 (en) * | 2003-12-02 | 2005-09-15 | Erik Buntinx | Use of D4 and 5-HT2A antagonists, inverse agonists or partial agonists |
| PL1708790T3 (pl) * | 2003-12-02 | 2010-10-29 | Pharmaneuroboost N V | Zastosowanie pipamperonu oraz antagonisty receptora D2 lub antagonisty receptora serotoniny/dopaminy do leczenia zaburzeń psychotycznych |
| US7855195B2 (en) * | 2003-12-02 | 2010-12-21 | Pharmaneuroboost N.V. | Method of treating mental disorders using D4 and 5-HT2A antagonists, inverse agonists or partial agonists |
| US20050119249A1 (en) * | 2003-12-02 | 2005-06-02 | Erik Buntinx | Method of treating neurodegenerative diseases using D4 and 5-HT2A antagonists, inverse agonists or partial agonists |
| US20050171088A1 (en) * | 2004-01-30 | 2005-08-04 | Astrazeneca Ab | Treatment of psychoses with dibenzothiazepine antipsychotic |
| US7868176B2 (en) * | 2004-09-27 | 2011-01-11 | Acadia Pharmaceuticals, Inc. | Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-y1)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation |
| US7790899B2 (en) | 2004-09-27 | 2010-09-07 | Acadia Pharmaceuticals, Inc. | Synthesis of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-yl)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and its tartrate salt and crystalline forms |
| WO2006093192A1 (ja) * | 2005-03-04 | 2006-09-08 | Tokyo Medical And Dental University | 覚醒剤精神病及び統合失調症の再発防止治療薬 |
| NZ568720A (en) | 2005-12-01 | 2011-06-30 | Auspex Pharmaceuticals Inc | Substituted phenethylamines with serotoninergic and/or norepinephrinergic acitivity |
| WO2007124136A1 (en) * | 2006-04-19 | 2007-11-01 | Acadia Pharmaceuticals, Inc. | Use of 4-amino-piperidines for treating sleep disorders |
| US20080051429A1 (en) * | 2006-04-19 | 2008-02-28 | Van Kammen Daniel | Use of 4-amino-piperidines for treating sleep disorders |
| JP2009537538A (ja) * | 2006-05-15 | 2009-10-29 | アカドイア プハルマセウチカルス インコーポレーテッド | ピマバンセリン医薬製剤 |
| JP2010522135A (ja) | 2006-10-09 | 2010-07-01 | チャールストン ラボラトリーズ，インコーポレイテッド | 医薬組成物 |
| WO2008052139A2 (en) | 2006-10-25 | 2008-05-02 | Somaxon Pharmaceuticals, Inc. | Ultra low dose doxepin and methods of using the same to treat sleep disorders |
| US20110077200A1 (en) * | 2006-12-06 | 2011-03-31 | Somaxon Pharmaceuticals, Inc. | Combination therapy using low-dose doxepin for the improvement of sleep |
| HRP20161581T1 (hr) | 2007-03-15 | 2016-12-30 | Auspex Pharmaceuticals, Inc. | DEUTERIRANI d9-VENLAFAKSI |
| CN101677971A (zh) * | 2007-03-19 | 2010-03-24 | 阿卡蒂亚药品公司 | 5-ht2a反向激动剂和拮抗剂与抗精神病药物的组合 |
| DK2200610T3 (en) * | 2007-09-21 | 2018-04-23 | Acadia Pharm Inc | ADMINISTRATION OF PIMAVANSERIN WITH OTHER AGENTS |
| WO2009039461A2 (en) * | 2007-09-21 | 2009-03-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| JP5714910B2 (ja) | 2008-01-09 | 2015-05-07 | チャールストン ラボラトリーズ，インコーポレイテッド | 薬学的組成物 |
| EP3311667A1 (en) | 2009-07-08 | 2018-04-25 | Charleston Laboratories, Inc. | Pharmaceutical compositions |
| TWI471146B (zh) | 2009-12-02 | 2015-02-01 | Aptalis Pharma Ltd | 菲索特芬那定（ｆｅｘｏｆｅｎａｄｉｎｅ）微膠囊及包含其之組合物 |
| US9737531B2 (en) | 2012-07-12 | 2017-08-22 | Glytech, Llc | Composition and method for treatment of depression and psychosis in humans |
| WO2012113103A1 (en) | 2011-02-25 | 2012-08-30 | Helsinn Healthcare S.A. | Asymmetric ureas and medical uses thereof |
| WO2014085362A1 (en) | 2012-11-27 | 2014-06-05 | Acadia Pharmaceuticals Inc. | Methods for the treatment of parkinson's disease psychosis using pimavanserin |
| EP3316865A4 (en) | 2015-07-02 | 2019-01-23 | Civitas Therapeutics, Inc. | TRIPTAN POWDER FOR PULMONARY ADMINISTRATION |
| JP6850282B2 (ja) | 2015-07-20 | 2021-03-31 | アカディア ファーマシューティカルズ インコーポレーテッド | Ｎ−（４−フルオロベンジル）−ｎ−（１−メチルピペリジン−４−イル）−ｎ’−（４−（２−メチルプロピルオキシ）フェニルメチル）カルバミドならびにその酒石酸塩および多形形態ｃを調製する方法 |
| US10179109B2 (en) | 2016-03-04 | 2019-01-15 | Charleston Laboratories, Inc. | Pharmaceutical compositions comprising 5HT receptor agonist and antiemetic particulates |
| MY198885A (en) | 2016-03-22 | 2023-10-02 | Helsinn Healthcare Sa | Benzenesulfonyl-asymmetric ureas and medical uses thereof |
| US10953000B2 (en) | 2016-03-25 | 2021-03-23 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome P450 modulators |
| WO2017165635A1 (en) | 2016-03-25 | 2017-09-28 | Acadia Pharmaceuticals Inc. | Combination of pimavanserin and cytochrome p450 modulators |
| EP3558311A1 (en) | 2016-12-20 | 2019-10-30 | Acadia Pharmaceuticals Inc. | Pimavanserin alone or in combination for use in the treatment of alzheimer's disease psychosis |
| SG10201912846PA (en) | 2017-01-13 | 2020-02-27 | Sumitomo Dainippon Pharma Co Ltd | Therapeutic agent for non-motor symptoms associated with parkinson's disease |
| US11135211B2 (en) | 2017-04-28 | 2021-10-05 | Acadia Pharmaceuticals Inc. | Pimavanserin for treating impulse control disorder |
| MX394875B (es) | 2017-05-25 | 2025-03-24 | Glytech Llc | Terapia combinada para trastornos neuropsiquiatricos sensibles al antagonista de nmdar. |
| BR112019024987A2 (pt) * | 2017-06-02 | 2020-06-16 | Xeris Pharmaceuticals, Inc. | Formulações de fármaco de molécula pequena resistente à precipitação |
| WO2018229744A1 (en) | 2017-06-12 | 2018-12-20 | Glytech Llc. | Treatment of depression with nmda antagonists and d2/5ht2a or selective 5ht2a antagonists |
| EP3675827A1 (en) | 2017-08-30 | 2020-07-08 | Acadia Pharmaceuticals Inc. | Formulations of pimavanserin |
| US12459965B2 (en) | 2017-10-09 | 2025-11-04 | Compass Pathfinder Limited | Preparation of psilocybin, different polymorphic forms, intermediates, formulations and their use |
| GB2571696B (en) | 2017-10-09 | 2020-05-27 | Compass Pathways Ltd | Large scale method for the preparation of Psilocybin and formulations of Psilocybin so produced |
| US20220016101A1 (en) * | 2018-10-30 | 2022-01-20 | Acadia Pharmaceuticals Inc. | Methods of treating depression, anxiety and sexual dysfunction using the compound pimavanserin |
| JP2022529781A (ja) | 2019-04-17 | 2022-06-24 | コンパス パスファインダー リミテッド | サイロシビンによるうつ病及び他の様々な障害の治療 |
| CN114786668B (zh) * | 2019-11-27 | 2024-07-16 | 诺罗瑞韦有限公司 | 用于治疗抑郁症的环丝氨酸和锂的组合疗法 |
| JPWO2021193790A1 (cg-RX-API-DMAC7.html) * | 2020-03-26 | 2021-09-30 | ||
| WO2022094230A1 (en) * | 2020-11-02 | 2022-05-05 | Acadia Pharmaceuticals Inc. | Compounds for treating psychosis or depression |
| KR102397333B1 (ko) * | 2020-12-21 | 2022-05-13 | 주식회사 스탠다임 | 클레마스틴을 포함하는 강박장애, 틱 장애 또는 뚜렛 증후군 예방 또는 치료용 약학 조성물 |
Family Cites Families (76)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE794333A (fr) | 1972-01-20 | 1973-07-19 | Wyeth John & Brother Ltd | Composes heterocycliques azotes therapeutiques |
| GB1507462A (en) * | 1974-03-21 | 1978-04-12 | Gallardo Antonio Sa | N-heterocyclic substituted benzamides methods for their preparation and compositions containing them |
| US3983234A (en) * | 1974-07-04 | 1976-09-28 | Sandoz Ltd. | Treatment of dyskinesias |
| JPS5152176A (cg-RX-API-DMAC7.html) | 1974-10-12 | 1976-05-08 | Yoshitomi Pharmaceutical | |
| JPS528517A (en) | 1975-07-09 | 1977-01-22 | Toyo Autom Kk | Fluid line automatic closing system at an earthquake |
| GB1586468A (en) * | 1976-10-29 | 1981-03-18 | Anphar Sa | Piperidine derivatives |
| CA1140119A (en) | 1978-04-03 | 1983-01-25 | Joseph Torremans | N-heterocyclyl-4-piperidinamines |
| US4255432A (en) * | 1979-09-06 | 1981-03-10 | Syntex (U.S.A.) Inc. | 8-[2-3-Indolyl)ethyl]-1-oxa-3-,8-diazaspiro[4.5]decan-2-ones, pharmaceutical compositions thereof and methods of use thereof |
| DE3100535A1 (de) | 1981-01-10 | 1982-08-12 | Dr. Karl Thomae Gmbh, 7950 Biberach | "neue carbonsaeure-derivate, ihre herstellung und ihre verwendung als arzneimittel" |
| US4332804A (en) | 1981-03-23 | 1982-06-01 | Syntex (U.S.A.) Inc. | 9-[2-(3-Indolyl)ethyl]-1oxa-4,9-diazaspiro[5.5]undecan-3-ones |
| US4401665A (en) * | 1981-04-14 | 1983-08-30 | Bristol-Myers Company | Sleep-aid composition containing an analgesic and diphenhydramine dihydrogencitrate, and method of use |
| US4353900A (en) * | 1981-10-19 | 1982-10-12 | Syntex (U.S.A.) Inc. | 9-(Arylalkyl or aroylalkyl)-1-oxa-4,9-diazaspiro(5.5)undecan-3-ones |
| US4353901A (en) * | 1981-10-19 | 1982-10-12 | Syntex (U.S.A.) Inc. | 9-(1,4-Benzodioxan-2-ylalkyl and hydroxyalkyl)-1-oxa-4,9-diazaspiro[5.5]undecan-3-ones |
| GB8527052D0 (en) * | 1985-11-02 | 1985-12-04 | Beecham Group Plc | Compounds |
| GB8621892D0 (en) | 1986-09-11 | 1986-10-15 | Lundbeck & Co As H | Organic compound |
| ATE102482T1 (de) * | 1988-01-21 | 1994-03-15 | Merrell Dow Pharma | Verwendung von 1,4-disubstituierten-piperidinyl- verbindungen zur herstellung eines arzneimittels zur behandlung von schlaflosigkeit. |
| FR2642069B1 (fr) * | 1989-01-20 | 1991-04-12 | Rhone Poulenc Sante | Nouveaux derives du benzopyranne, leur preparation et les compositions pharmaceutiques qui les contiennent |
| GB8906324D0 (en) * | 1989-03-20 | 1989-05-04 | Pfizer Ltd | 1,4-dihydropyridines |
| US5214055A (en) * | 1990-05-18 | 1993-05-25 | Adir Et Compagnie | Aminopiperidine 4-oxo-4H-chromen-2-yl compounds |
| WO1991018602A1 (en) * | 1990-06-01 | 1991-12-12 | Merrell Dow Pharmaceuticals Inc. | (+)-α-(2,3-DIMETHOXYPHENYL)-1-[2-(4-FLUOROPHENYL)ETHYL]-4-PIPERIDINEMETHANOL |
| US5216165A (en) * | 1990-10-03 | 1993-06-01 | American Home Products Corporation | N-substituted aminoquinolines as analgesic agents |
| IT1252227B (it) | 1991-12-17 | 1995-06-05 | Ciba Geigy Spa | Composti tetrametilpiperidinici atti all'impiego come stabilizzanti per materiali organici |
| JPH05208517A (ja) | 1992-01-31 | 1993-08-20 | Nec Corp | 印字制御回路 |
| US5595872A (en) * | 1992-03-06 | 1997-01-21 | Bristol-Myers Squibb Company | Nucleic acids encoding microsomal trigyceride transfer protein |
| CA2123728A1 (en) | 1993-05-21 | 1994-11-22 | Noriyoshi Sueda | Urea derivatives and their use as acat inhibitors |
| WO1994027967A1 (en) | 1993-05-26 | 1994-12-08 | Smithkline Beecham Laboratoires Pharmaceutiques | Novel compounds |
| US5707798A (en) * | 1993-07-13 | 1998-01-13 | Novo Nordisk A/S | Identification of ligands by selective amplification of cells transfected with receptors |
| DE4404183A1 (de) * | 1994-02-10 | 1995-08-17 | Merck Patent Gmbh | 4-Amino-1-piperidylbenzoylguanidine |
| PT792273E (pt) * | 1994-11-15 | 2003-06-30 | Upjohn Co | Produtos antibacterianos de oxazolidinona substituida com oxazina e tiazina biciclicas |
| US5795894A (en) * | 1995-05-02 | 1998-08-18 | Schering Corporation | Piperazino derivatives as neurokinn antagonists |
| BR9610277A (pt) | 1995-08-31 | 1999-07-06 | Schering Corp | Derivados de piperazino como antagonistas de neurowuinina |
| JPH11512723A (ja) | 1995-09-29 | 1999-11-02 | イーライ リリー アンド カンパニー | フィブリノゲン依存血小板凝集抑制物質としてのスピロ化合物 |
| JPH09231567A (ja) * | 1996-02-28 | 1997-09-05 | Sony Corp | 光デイスク装置、光デイスク及び記録方法 |
| WO1997038665A2 (en) | 1996-04-03 | 1997-10-23 | Merck & Co., Inc. | Inhibitors of farnesyl-protein transferase |
| WO1997038984A1 (en) | 1996-04-17 | 1997-10-23 | Du Pont Pharmaceuticals Company | N-(amidinophenyl)-n'-(subst.)-3h-2,4-benzodiazepin-3-one derivatives as factor xa inhibitors |
| AT403803B (de) * | 1996-04-19 | 1998-05-25 | Sanochemia Ltd | Neue benzazepinderivate, diese enthaltende arzneimittel und verwendung derselben zum herstellen von arzneimitteln |
| US5869488A (en) * | 1996-05-01 | 1999-02-09 | Schering Corporation | Piperazino derivatives as neurokinin antagonists |
| US5877173A (en) * | 1996-08-28 | 1999-03-02 | Washington University | Preventing neuronal degeneration in Alzheimer's disease |
| CA2262818A1 (en) | 1996-09-10 | 1998-03-19 | Dr. Karl Thomae Gesellschaft Mit Beschrankter Haftung | Modified amino acids, pharmaceuticals containing these compounds and methods for their production |
| DE19643331A1 (de) | 1996-10-21 | 1998-04-23 | Thomae Gmbh Dr K | 1-(4-Piperidinyl)-piperidinylene, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| US6057338A (en) | 1997-04-04 | 2000-05-02 | Merck & Co., Inc. | Somatostatin agonists |
| CA2289010A1 (en) | 1997-05-08 | 1998-11-12 | Daniel F. Veber | Protease inhibitors |
| GB9718833D0 (en) * | 1997-09-04 | 1997-11-12 | Merck Sharp & Dohme | Therapeutic agents |
| WO1999052927A1 (en) | 1998-04-14 | 1999-10-21 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof |
| AU765603C (en) * | 1998-04-14 | 2004-08-05 | General Hospital Corporation, The | Methods for treating neuropsychiatric disorders |
| IL140084A0 (en) * | 1998-06-05 | 2002-02-10 | Astra Ab | Oxazolidinone derivatives, process for their preparation and pharmaceutical compositions containing them |
| US6140509A (en) * | 1998-06-26 | 2000-10-31 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human serotonin receptors and small molecule modulators thereof |
| GB9816263D0 (en) * | 1998-07-24 | 1998-09-23 | Merck Sharp & Dohme | Therapeutic agents |
| US6358698B1 (en) * | 1998-10-07 | 2002-03-19 | Acadia Pharmacueticals Inc. | Methods of identifying inverse agonists of the serotonin 2A receptor |
| JP2002527477A (ja) | 1998-10-16 | 2002-08-27 | サントリー株式会社 | 神経細胞保護作用物質としてのアミノフェノキシ酢酸誘導体 |
| US6150393A (en) * | 1998-12-18 | 2000-11-21 | Arena Pharmaceuticals, Inc. | Small molecule modulators of non-endogenous, constitutively activated human serotonin receptors |
| EP1013276A1 (en) * | 1998-12-23 | 2000-06-28 | Pfizer Inc. | Aminoazacycloalkanes as CCR5 modulators |
| CA2367112A1 (en) | 1999-03-24 | 2000-09-28 | The Regents Of The University Of California | Methods for treating neurodegenerative disorders using aspartyl protease inhibitors |
| US6399619B1 (en) | 1999-04-06 | 2002-06-04 | Merck & Co., Inc. | Pyrrolidine modulators of chemokine receptor activity |
| BR0010651A (pt) | 1999-05-17 | 2002-03-19 | Novo Nordisk As | Composto, uso de um composto, composição farmacêutica, e, método para o tratamento e/ou prevenção de distúrbios ou de doenças mediadas por uma ação antagonìstica de glucagon |
| US20050148018A1 (en) * | 1999-10-07 | 2005-07-07 | David Weiner | Methods of identifying inverse agonists of the serotonin 2A receptor |
| FR2802206B1 (fr) | 1999-12-14 | 2005-04-22 | Sod Conseils Rech Applic | Derives de 4-aminopiperidine et leur utilisation en tant que medicament |
| US7022698B2 (en) * | 1999-12-28 | 2006-04-04 | U & I Pharmaceuticals, Ltd. | Pharmaceutical compositions containing new polymorphic forms of olanzapine and uses thereof |
| ATE348808T1 (de) | 2000-03-06 | 2007-01-15 | Acadia Pharm Inc | Azacyclische verbindungen zur verwendung in der behandlung von mit serotonin verwandten krankheiten |
| GB0011838D0 (en) * | 2000-05-17 | 2000-07-05 | Astrazeneca Ab | Chemical compounds |
| EP1656938A1 (en) | 2000-07-06 | 2006-05-17 | Wyeth | Combinations of SSRI and estrogenic agents |
| US20040102431A1 (en) | 2000-09-25 | 2004-05-27 | Christoph Boss | Substituted amino-aza-cycloalkanes useful against malaria |
| WO2002076464A1 (en) | 2001-03-22 | 2002-10-03 | Arena Pharmaceuticals, Inc. | Anti-psychosis combination |
| GB0108099D0 (en) | 2001-03-30 | 2001-05-23 | Hoffmann La Roche | Aminopiperidine derivatives |
| US6911452B2 (en) * | 2001-12-28 | 2005-06-28 | Acadia Pharmaceuticals Inc. | Spiroazacyclic compounds as monoamine receptor modulators |
| US7538222B2 (en) * | 2002-06-24 | 2009-05-26 | Acadia Pharmaceuticals, Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| US7253186B2 (en) * | 2002-06-24 | 2007-08-07 | Carl-Magnus Andersson | N-substituted piperidine derivatives as serotonin receptor agents |
| AU2003247615B2 (en) * | 2002-06-24 | 2007-08-09 | Acadia Pharmaceuticals Inc. | N-substituted piperidine derivatives as serotonin receptor agents |
| WO2004039322A2 (en) | 2002-10-29 | 2004-05-13 | Miicro, Inc. | Novel combination therapy for schizophrenia focused on improved cognition: 5-ht-2a/d2 blockade with adjunctive blockade of prefrontal da reuptake |
| NZ541146A (en) * | 2003-01-16 | 2009-04-30 | Acadia Pharm Inc | N-(1-methylpiperidin-4-yl)-N-(4-fluorophenylmethyl)-N'-(4-(2-methylpropyloxy)phenylmethyl)carbamide, also known as ACP-103, and its tartrate salt as therapeutics for neurodegenerative diseases |
| AU2004206931A1 (en) * | 2003-01-23 | 2004-08-05 | Acadia Pharmaceuticals Inc. | Use of N-desmethylclozapine to treat human neuropsychiatric disease |
| GB0324790D0 (en) | 2003-10-24 | 2003-11-26 | Astrazeneca Ab | Amide derivatives |
| PL1708790T3 (pl) | 2003-12-02 | 2010-10-29 | Pharmaneuroboost N V | Zastosowanie pipamperonu oraz antagonisty receptora D2 lub antagonisty receptora serotoniny/dopaminy do leczenia zaburzeń psychotycznych |
| PL1696931T3 (pl) * | 2003-12-22 | 2009-10-30 | Acadia Pharm Inc | Aminopodstawione analogi diarylo[A,D]cykloheptenowe jako agoniści receptorów muskarynowych i sposoby leczenia chorób neuropsychiatrycznych |
| US7868176B2 (en) * | 2004-09-27 | 2011-01-11 | Acadia Pharmaceuticals, Inc. | Salts of N-(4-fluorobenzyl)-N-(1-methylpiperidin-4-y1)-N′-(4-(2-methylpropyloxy)phenylmethyl)carbamide and their preparation |
| US8572080B2 (en) | 2010-06-04 | 2013-10-29 | Salesforce.Com, Inc. | Methods and systems for analyzing a network feed in a multi-tenant database system environment |
-
2004
- 2004-05-24 US US10/854,035 patent/US20050261278A1/en not_active Abandoned
-
2005
- 2005-05-20 JP JP2007527488A patent/JP2008500390A/ja active Pending
- 2005-05-20 AU AU2005244982A patent/AU2005244982B2/en not_active Expired
- 2005-05-20 CA CA2567704A patent/CA2567704C/en not_active Expired - Lifetime
- 2005-05-20 MX MXPA06013454A patent/MXPA06013454A/es active IP Right Grant
- 2005-05-20 RU RU2006145433/15A patent/RU2442607C2/ru active
- 2005-05-20 EP EP05753034A patent/EP1750705A1/en not_active Withdrawn
- 2005-05-20 EP EP10180326A patent/EP2283841A1/en not_active Withdrawn
- 2005-05-20 US US11/134,769 patent/US7863296B2/en active Active
- 2005-05-20 WO PCT/US2005/017808 patent/WO2005112927A1/en not_active Ceased
-
2009
- 2009-02-11 US US12/378,385 patent/US7875632B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US7863296B2 (en) | 2011-01-04 |
| RU2006145433A (ru) | 2008-06-27 |
| RU2442607C2 (ru) | 2012-02-20 |
| EP2283841A1 (en) | 2011-02-16 |
| AU2005244982B2 (en) | 2011-01-27 |
| JP2008500390A (ja) | 2008-01-10 |
| CA2567704C (en) | 2013-09-03 |
| WO2005112927A1 (en) | 2005-12-01 |
| AU2005244982A1 (en) | 2005-12-01 |
| US7875632B2 (en) | 2011-01-25 |
| CA2567704A1 (en) | 2005-12-01 |
| US20090155389A1 (en) | 2009-06-18 |
| US20050261278A1 (en) | 2005-11-24 |
| EP1750705A1 (en) | 2007-02-14 |
| US20050288328A1 (en) | 2005-12-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AU2005244982B2 (en) | Selective serotonin receptor inverse agonists as therapeutics for disease | |
| US7820695B2 (en) | Selective serotonin receptor inverse agonists as therapeutics for disease | |
| US7429580B2 (en) | Compositions of an anticonvulsant and an antipsychotic drug and methods of using the same for affecting weight loss | |
| US20100179129A1 (en) | Compositions of an anticonvulsant and mirtazapine to prevent weight gain | |
| AU2006323048B2 (en) | Compositions and methods for increasing insulin sensitivity | |
| US20080214592A1 (en) | Methods of treating anxiety disorders | |
| MX2007015052A (es) | Metodos y composiciones para manejar trastornos psicoticos. | |
| JP2021080288A (ja) | 吃音を治療するための融合ベンズアゼピン | |
| CA2879020C (en) | Fused benzazepines for treatment of tourette's syndrome | |
| PL207738B1 (pl) | Zastosowanie 2-(7-chloro-1,8-naftyrydyn-2-ylo)-3-(5-metylo-2-oksoheksylo)-1-izoindolinonu lub 2-(7-chloro-1,8-naftyrydyn-2-ylo)-3- (5-metylo-5-hydroksy-2-oksoheksylo)-1-izoindolinonu albo ich farmaceutycznie dopuszczalnej soli lub izomeru optycznego do wytwarzania leku | |
| JP2007506784A (ja) | 双極性障害およびその他の認知障害の治療における、ケレリトリン、その類似体およびそれらの使用 | |
| HK1116663A (en) | Selective serotonin receptor inverse agonists as therapeutics for disease | |
| Prasad | Chemistry and Synthesis of Medicinal Agents:(Expanding Knowledge of Drug Chemistry) | |
| CN1909903A (zh) | 用于影响体重减轻的抗惊厥药和抗精神病药的组合物 | |
| MXPA06007770A (en) | Compositions of an anticonvulsant and an antipsychotic drug for affecting weight loss |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |