JP2011523949A5 - - Google Patents
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- JP2011523949A5 JP2011523949A5 JP2011511638A JP2011511638A JP2011523949A5 JP 2011523949 A5 JP2011523949 A5 JP 2011523949A5 JP 2011511638 A JP2011511638 A JP 2011511638A JP 2011511638 A JP2011511638 A JP 2011511638A JP 2011523949 A5 JP2011523949 A5 JP 2011523949A5
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- Japan
- Prior art keywords
- composition according
- compound
- formula
- pharmaceutically acceptable
- disorders
- Prior art date
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- 239000000203 mixture Substances 0.000 claims 36
- 150000001875 compounds Chemical class 0.000 claims 18
- 239000003814 drug Substances 0.000 claims 16
- 239000000556 agonist Substances 0.000 claims 14
- -1 aripiparazole Chemical compound 0.000 claims 13
- 150000003839 salts Chemical group 0.000 claims 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 12
- 208000035475 disorder Diseases 0.000 claims 11
- QZAYGJVTTNCVMB-UHFFFAOYSA-N serotonin Chemical compound C1=C(O)C=C2C(CCN)=CNC2=C1 QZAYGJVTTNCVMB-UHFFFAOYSA-N 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 208000019116 sleep disease Diseases 0.000 claims 9
- 239000005557 antagonist Substances 0.000 claims 6
- 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 6
- 229940124597 therapeutic agent Drugs 0.000 claims 6
- 230000000694 effects Effects 0.000 claims 5
- 229960001534 risperidone Drugs 0.000 claims 5
- 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 5
- UGJMXCAKCUNAIE-UHFFFAOYSA-N Gabapentin Chemical compound OC(=O)CC1(CN)CCCCC1 UGJMXCAKCUNAIE-UHFFFAOYSA-N 0.000 claims 4
- YJPIGAIKUZMOQA-UHFFFAOYSA-N Melatonin Natural products COC1=CC=C2N(C(C)=O)C=C(CCN)C2=C1 YJPIGAIKUZMOQA-UHFFFAOYSA-N 0.000 claims 4
- YLXDSYKOBKBWJQ-LBPRGKRZSA-N N-[2-[(8S)-2,6,7,8-tetrahydro-1H-cyclopenta[e]benzofuran-8-yl]ethyl]propanamide Chemical compound C1=C2OCCC2=C2[C@H](CCNC(=O)CC)CCC2=C1 YLXDSYKOBKBWJQ-LBPRGKRZSA-N 0.000 claims 4
- 208000018737 Parkinson disease Diseases 0.000 claims 4
- 208000028017 Psychotic disease Diseases 0.000 claims 4
- VYFYYTLLBUKUHU-UHFFFAOYSA-N dopamine Chemical compound NCCC1=CC=C(O)C(O)=C1 VYFYYTLLBUKUHU-UHFFFAOYSA-N 0.000 claims 4
- 229960005426 doxepin Drugs 0.000 claims 4
- ODQWQRRAPPTVAG-GZTJUZNOSA-N doxepin Chemical compound C1OC2=CC=CC=C2C(=C/CCN(C)C)/C2=CC=CC=C21 ODQWQRRAPPTVAG-GZTJUZNOSA-N 0.000 claims 4
- 229940011871 estrogen Drugs 0.000 claims 4
- 239000000262 estrogen Substances 0.000 claims 4
- 229960003692 gamma aminobutyric acid Drugs 0.000 claims 4
- BTCSSZJGUNDROE-UHFFFAOYSA-N gamma-aminobutyric acid Chemical compound NCCCC(O)=O BTCSSZJGUNDROE-UHFFFAOYSA-N 0.000 claims 4
- 229960003987 melatonin Drugs 0.000 claims 4
- DRLFMBDRBRZALE-UHFFFAOYSA-N melatonin Chemical compound COC1=CC=C2NC=C(CCNC(C)=O)C2=C1 DRLFMBDRBRZALE-UHFFFAOYSA-N 0.000 claims 4
- 229960001800 nefazodone Drugs 0.000 claims 4
- 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 4
- 229960003991 trazodone Drugs 0.000 claims 4
- PHLBKPHSAVXXEF-UHFFFAOYSA-N trazodone Chemical compound ClC1=CC=CC(N2CCN(CCCN3C(N4C=CC=CC4=N3)=O)CC2)=C1 PHLBKPHSAVXXEF-UHFFFAOYSA-N 0.000 claims 4
- WTDRDQBEARUVNC-LURJTMIESA-N L-DOPA Chemical group OC(=O)[C@@H](N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-LURJTMIESA-N 0.000 claims 3
- WTDRDQBEARUVNC-UHFFFAOYSA-N L-Dopa Natural products OC(=O)C(N)CC1=CC=C(O)C(O)=C1 WTDRDQBEARUVNC-UHFFFAOYSA-N 0.000 claims 3
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims 3
- 239000000164 antipsychotic agent Substances 0.000 claims 3
- 229960004170 clozapine Drugs 0.000 claims 3
- QZUDBNBUXVUHMW-UHFFFAOYSA-N clozapine Chemical compound C1CN(C)CCN1C1=NC2=CC(Cl)=CC=C2NC2=CC=CC=C12 QZUDBNBUXVUHMW-UHFFFAOYSA-N 0.000 claims 3
- 239000003085 diluting agent Substances 0.000 claims 3
- 229960004038 fluvoxamine Drugs 0.000 claims 3
- 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 3
- 229960003878 haloperidol Drugs 0.000 claims 3
- 206010022437 insomnia Diseases 0.000 claims 3
- 229960005017 olanzapine Drugs 0.000 claims 3
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims 3
- 229960004431 quetiapine Drugs 0.000 claims 3
- URKOMYMAXPYINW-UHFFFAOYSA-N quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims 3
- 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 2
- 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 2
- WYDUSKDSKCASEF-LJQANCHMSA-N (1s)-1-cyclohexyl-1-phenyl-3-pyrrolidin-1-ylpropan-1-ol Chemical compound C([C@](O)(C1CCCCC1)C=1C=CC=CC=1)CN1CCCC1 WYDUSKDSKCASEF-LJQANCHMSA-N 0.000 claims 2
- 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 2
- 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 2
- 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 2
- 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 2
- 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 claims 2
- YFGHCGITMMYXAQ-UHFFFAOYSA-N 2-[(diphenylmethyl)sulfinyl]acetamide Chemical compound C=1C=CC=CC=1C(S(=O)CC(=O)N)C1=CC=CC=C1 YFGHCGITMMYXAQ-UHFFFAOYSA-N 0.000 claims 2
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 claims 2
- 239000003185 4 aminobutyric acid B receptor stimulating agent Substances 0.000 claims 2
- BQBQAWXALAGUIW-GHVWMZMZSA-N 6-[5-[[(2s)-2-(4-fluorophenyl)-4-methylpiperazin-1-yl]methyl]furan-3-yl]-3h-1,3-benzoxazol-2-one;hydrate;hydrochloride Chemical compound O.Cl.C1([C@@H]2N(CC=3OC=C(C=3)C=3C=C4OC(O)=NC4=CC=3)CCN(C2)C)=CC=C(F)C=C1 BQBQAWXALAGUIW-GHVWMZMZSA-N 0.000 claims 2
- RPUBHMMISKEXSR-MLCLTIQSSA-N 680993-85-5 Chemical compound OC(=O)\C=C/C(O)=O.C1C2=CC=CN=C2N2CCN(C)C[C@@H]2C2=CC=CC=C21 RPUBHMMISKEXSR-MLCLTIQSSA-N 0.000 claims 2
- VMIYHDSEFNYJSL-UHFFFAOYSA-N Bromazepam Chemical compound C12=CC(Br)=CC=C2NC(=O)CN=C1C1=CC=CC=N1 VMIYHDSEFNYJSL-UHFFFAOYSA-N 0.000 claims 2
- GDLIGKIOYRNHDA-UHFFFAOYSA-N Clomipramine Chemical compound C1CC2=CC=C(Cl)C=C2N(CCCN(C)C)C2=CC=CC=C21 GDLIGKIOYRNHDA-UHFFFAOYSA-N 0.000 claims 2
- HCYAFALTSJYZDH-UHFFFAOYSA-N Desimpramine Chemical compound C1CC2=CC=CC=C2N(CCCNC)C2=CC=CC=C21 HCYAFALTSJYZDH-UHFFFAOYSA-N 0.000 claims 2
- 208000012661 Dyskinesia Diseases 0.000 claims 2
- NMYAHEULKSYAPP-UHFFFAOYSA-N Eptapirone Chemical compound O=C1N(C)C(=O)C=NN1CCCCN1CCN(C=2N=CC=CN=2)CC1 NMYAHEULKSYAPP-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 102000019432 Galanin Human genes 0.000 claims 2
- 101800002068 Galanin Proteins 0.000 claims 2
- 102000018997 Growth Hormone Human genes 0.000 claims 2
- 108010051696 Growth Hormone Proteins 0.000 claims 2
- 101000831616 Homo sapiens Protachykinin-1 Proteins 0.000 claims 2
- 102000002265 Human Growth Hormone Human genes 0.000 claims 2
- 108010000521 Human Growth Hormone Proteins 0.000 claims 2
- 239000000854 Human Growth Hormone Substances 0.000 claims 2
- 102000004310 Ion Channels Human genes 0.000 claims 2
- COSPVUFTLGQDQL-UHFFFAOYSA-N Nelotanserin Chemical compound C1=C(C=2N(N=CC=2Br)C)C(OC)=CC=C1NC(=O)NC1=CC=C(F)C=C1F COSPVUFTLGQDQL-UHFFFAOYSA-N 0.000 claims 2
- PHVGLTMQBUFIQQ-UHFFFAOYSA-N Nortryptiline Chemical compound C1CC2=CC=CC=C2C(=CCCNC)C2=CC=CC=C21 PHVGLTMQBUFIQQ-UHFFFAOYSA-N 0.000 claims 2
- 102000002512 Orexin Human genes 0.000 claims 2
- 229940123730 Orexin receptor antagonist Drugs 0.000 claims 2
- AHOUBRCZNHFOSL-UHFFFAOYSA-N Paroxetine hydrochloride Natural products C1=CC(F)=CC=C1C1C(COC=2C=C3OCOC3=CC=2)CNCC1 AHOUBRCZNHFOSL-UHFFFAOYSA-N 0.000 claims 2
- ZGUGWUXLJSTTMA-UHFFFAOYSA-N Promazinum Chemical compound C1=CC=C2N(CCCN(C)C)C3=CC=CC=C3SC2=C1 ZGUGWUXLJSTTMA-UHFFFAOYSA-N 0.000 claims 2
- 102100024304 Protachykinin-1 Human genes 0.000 claims 2
- PPTYJKAXVCCBDU-UHFFFAOYSA-N Rohypnol Chemical compound N=1CC(=O)N(C)C2=CC=C([N+]([O-])=O)C=C2C=1C1=CC=CC=C1F PPTYJKAXVCCBDU-UHFFFAOYSA-N 0.000 claims 2
- KLBQZWRITKRQQV-UHFFFAOYSA-N Thioridazine Chemical compound C12=CC(SC)=CC=C2SC2=CC=CC=C2N1CCC1CCCCN1C KLBQZWRITKRQQV-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 241001516476 Vanda Species 0.000 claims 2
- 229960004538 alprazolam Drugs 0.000 claims 2
- VREFGVBLTWBCJP-UHFFFAOYSA-N alprazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NN=C2CN=C1C1=CC=CC=C1 VREFGVBLTWBCJP-UHFFFAOYSA-N 0.000 claims 2
- WOLHOYHSEKDWQH-UHFFFAOYSA-N amantadine hydrochloride Chemical compound [Cl-].C1C(C2)CC3CC2CC1([NH3+])C3 WOLHOYHSEKDWQH-UHFFFAOYSA-N 0.000 claims 2
- 229960000836 amitriptyline Drugs 0.000 claims 2
- KRMDCWKBEZIMAB-UHFFFAOYSA-N amitriptyline Chemical compound C1CC2=CC=CC=C2C(=CCCN(C)C)C2=CC=CC=C21 KRMDCWKBEZIMAB-UHFFFAOYSA-N 0.000 claims 2
- 229960002519 amoxapine Drugs 0.000 claims 2
- QWGDMFLQWFTERH-UHFFFAOYSA-N amoxapine Chemical compound C12=CC(Cl)=CC=C2OC2=CC=CC=C2N=C1N1CCNCC1 QWGDMFLQWFTERH-UHFFFAOYSA-N 0.000 claims 2
- 239000000935 antidepressant agent Substances 0.000 claims 2
- 229940005513 antidepressants Drugs 0.000 claims 2
- 229940005529 antipsychotics Drugs 0.000 claims 2
- YFGHCGITMMYXAQ-LJQANCHMSA-N armodafinil Chemical compound C=1C=CC=CC=1C([S@](=O)CC(=O)N)C1=CC=CC=C1 YFGHCGITMMYXAQ-LJQANCHMSA-N 0.000 claims 2
- 229960004823 armodafinil Drugs 0.000 claims 2
- 239000003693 atypical antipsychotic agent Substances 0.000 claims 2
- 229940127236 atypical antipsychotics Drugs 0.000 claims 2
- 150000003936 benzamides Chemical class 0.000 claims 2
- 230000005540 biological transmission Effects 0.000 claims 2
- YSXKPIUOCJLQIE-UHFFFAOYSA-N biperiden Chemical compound C1C(C=C2)CC2C1C(C=1C=CC=CC=1)(O)CCN1CCCCC1 YSXKPIUOCJLQIE-UHFFFAOYSA-N 0.000 claims 2
- 229960002729 bromazepam Drugs 0.000 claims 2
- 229960002802 bromocriptine Drugs 0.000 claims 2
- 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 2
- 229960001058 bupropion Drugs 0.000 claims 2
- SNPPWIUOZRMYNY-UHFFFAOYSA-N bupropion Chemical compound CC(C)(C)NC(C)C(=O)C1=CC=CC(Cl)=C1 SNPPWIUOZRMYNY-UHFFFAOYSA-N 0.000 claims 2
- 229960003778 casopitant Drugs 0.000 claims 2
- XGGTZCKQRWXCHW-WMTVXVAQSA-N casopitant Chemical compound C1([C@H]2C[C@H](CCN2C(=O)N(C)[C@H](C)C=2C=C(C=C(C=2)C(F)(F)F)C(F)(F)F)N2CCN(CC2)C(C)=O)=CC=C(F)C=C1C XGGTZCKQRWXCHW-WMTVXVAQSA-N 0.000 claims 2
- 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 2
- 229960001076 chlorpromazine Drugs 0.000 claims 2
- 229960001653 citalopram Drugs 0.000 claims 2
- 229960001403 clobazam Drugs 0.000 claims 2
- CXOXHMZGEKVPMT-UHFFFAOYSA-N clobazam Chemical compound O=C1CC(=O)N(C)C2=CC=C(Cl)C=C2N1C1=CC=CC=C1 CXOXHMZGEKVPMT-UHFFFAOYSA-N 0.000 claims 2
- 229960004606 clomipramine Drugs 0.000 claims 2
- DGBIGWXXNGSACT-UHFFFAOYSA-N clonazepam Chemical compound C12=CC([N+](=O)[O-])=CC=C2NC(=O)CN=C1C1=CC=CC=C1Cl DGBIGWXXNGSACT-UHFFFAOYSA-N 0.000 claims 2
- 229960003120 clonazepam Drugs 0.000 claims 2
- 229960004362 clorazepate Drugs 0.000 claims 2
- 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 claims 2
- 229960003914 desipramine Drugs 0.000 claims 2
- 229960003529 diazepam Drugs 0.000 claims 2
- 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 2
- 229960003638 dopamine Drugs 0.000 claims 2
- 239000002552 dosage form Substances 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 229960002866 duloxetine Drugs 0.000 claims 2
- 229960003337 entacapone Drugs 0.000 claims 2
- JRURYQJSLYLRLN-BJMVGYQFSA-N entacapone Chemical compound CCN(CC)C(=O)C(\C#N)=C\C1=CC(O)=C(O)C([N+]([O-])=O)=C1 JRURYQJSLYLRLN-BJMVGYQFSA-N 0.000 claims 2
- 229950002850 eptapirone Drugs 0.000 claims 2
- 229960002336 estazolam Drugs 0.000 claims 2
- 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 2
- JCYLWUVDHLVGER-UHFFFAOYSA-N evt-201 Chemical compound O1C(CN(C)C)=NC(C2=C3N(C4=CC=CC(Cl)=C4C(=O)N(C)C3)C=N2)=N1 JCYLWUVDHLVGER-UHFFFAOYSA-N 0.000 claims 2
- 229960002200 flunitrazepam Drugs 0.000 claims 2
- 229960002464 fluoxetine Drugs 0.000 claims 2
- 229960002690 fluphenazine Drugs 0.000 claims 2
- 229960003528 flurazepam Drugs 0.000 claims 2
- 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 2
- 229960002870 gabapentin Drugs 0.000 claims 2
- 239000000122 growth hormone Substances 0.000 claims 2
- 229960005417 ketanserin Drugs 0.000 claims 2
- FPCCSQOGAWCVBH-UHFFFAOYSA-N ketanserin Chemical compound C1=CC(F)=CC=C1C(=O)C1CCN(CCN2C(C3=CC=CC=C3NC2=O)=O)CC1 FPCCSQOGAWCVBH-UHFFFAOYSA-N 0.000 claims 2
- 229960001848 lamotrigine Drugs 0.000 claims 2
- PYZRQGJRPPTADH-UHFFFAOYSA-N lamotrigine Chemical compound NC1=NC(N)=NN=C1C1=CC=CC(Cl)=C1Cl PYZRQGJRPPTADH-UHFFFAOYSA-N 0.000 claims 2
- 229960004391 lorazepam Drugs 0.000 claims 2
- 229960000423 loxapine Drugs 0.000 claims 2
- XJGVXQDUIWGIRW-UHFFFAOYSA-N loxapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2OC2=CC=C(Cl)C=C12 XJGVXQDUIWGIRW-UHFFFAOYSA-N 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 229960004090 maprotiline Drugs 0.000 claims 2
- QSLMDECMDJKHMQ-GSXCWMCISA-N maprotiline Chemical compound C12=CC=CC=C2[C@@]2(CCCNC)C3=CC=CC=C3[C@@H]1CC2 QSLMDECMDJKHMQ-GSXCWMCISA-N 0.000 claims 2
- 229960003793 midazolam Drugs 0.000 claims 2
- DDLIGBOFAVUZHB-UHFFFAOYSA-N midazolam Chemical compound C12=CC(Cl)=CC=C2N2C(C)=NC=C2CN=C1C1=CC=CC=C1F DDLIGBOFAVUZHB-UHFFFAOYSA-N 0.000 claims 2
- 229960001785 mirtazapine Drugs 0.000 claims 2
- RONZAEMNMFQXRA-UHFFFAOYSA-N mirtazapine Chemical compound C1C2=CC=CN=C2N2CCN(C)CC2C2=CC=CC=C21 RONZAEMNMFQXRA-UHFFFAOYSA-N 0.000 claims 2
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Families Citing this family (74)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2008070795A2 (en) * | 2006-12-06 | 2008-06-12 | Somaxon Pharmaceuticals, Inc. | Combination therapy using low-dose doxepin for the improvement of sleep |
| KR102107954B1 (ko) | 2007-03-12 | 2020-05-07 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 치환된 헤테로환 융합 감마-카르볼린 합성 |
| AU2009223701B2 (en) | 2008-03-12 | 2015-04-16 | Intra-Cellular Therapies, Inc. | Substituted heterocycle fused gamma-carbolines solid |
| EP3085231A1 (en) | 2008-05-27 | 2016-10-26 | Intra-Cellular Therapies, Inc. | Method and compositions for sleep disorders and other disorders |
| ME03452B (me) | 2009-10-23 | 2020-01-20 | Janssen Pharmaceutica Nv | Disupstituisani oktahi-dropirolo[3,4-c]piroli kao modulatori oreksin receptora |
| CA2796756A1 (en) * | 2010-04-22 | 2011-10-27 | Intra-Cellular Therapies, Inc. | Substituted pyrido(3',4':4,5)pyrrolo(1,2,3-de)quinoxalines for the treatment of central nervous system disorders |
| US8741888B2 (en) * | 2010-11-09 | 2014-06-03 | Carl A. Forest | Sleep aid composition and method |
| AU2012283035B2 (en) * | 2011-07-08 | 2015-07-30 | Eli Lilly & Company | (thieno[2,3-b][1,5]benzoxazepin-4-yl)piperazin-1-yl compounds as dual activity H1 inverse agonists/5-HT2A antagonists |
| KR20140146192A (ko) | 2012-04-14 | 2014-12-24 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| CN103175973B (zh) * | 2013-02-26 | 2015-05-13 | 首都医科大学 | 甘丙肽在制备女性抑郁症检测工具中的应用 |
| WO2014159720A1 (en) * | 2013-03-13 | 2014-10-02 | The University Of Chicago | Methods and compositions for inhibiting glyoxalase 1 (glo1) |
| WO2014152804A1 (en) * | 2013-03-14 | 2014-09-25 | Hyperion Biotechnology | Methods and compositions for biomarkers of fatigue, fitness and physical performance capacity |
| US9708322B2 (en) | 2013-03-15 | 2017-07-18 | Intra-Cellular Therapies, Inc. | Substituted pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines for inhibiting serotonin reuptake transporter activity |
| KR102373288B1 (ko) | 2013-12-03 | 2022-03-10 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 신규한 방법 |
| US10077267B2 (en) | 2014-04-04 | 2018-09-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA2944755A1 (en) | 2014-04-04 | 2015-10-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CN107206093A (zh) * | 2015-01-28 | 2017-09-26 | 韩国真耐瑞斯有限公司 | 用于治疗神经精神类障碍的组合物及方法 |
| WO2017117514A1 (en) * | 2015-12-31 | 2017-07-06 | Tung Roger D | Deuterated iti-007 |
| PL3838274T3 (pl) * | 2016-01-26 | 2024-04-02 | Intra-Cellular Therapies, Inc. | Pochodna pirydo[3',4':4,5]pirolo[1,2,3-DE]chinoksaliny do zastosowania w leczeniu zaburzeń OUN |
| MD3426251T2 (ro) | 2016-03-10 | 2022-09-30 | Janssen Pharmaceutica Nv | Metode de tratament al depresiei utilizând antagoniști ai receptorului orexină-2 |
| DK3407889T3 (da) | 2016-03-25 | 2021-08-09 | Intra Cellular Therapies Inc | Organiske forbindelser og deres anvendelse til behandling og forebyggelse af lidelser i centralnervesystemet |
| US10682354B2 (en) | 2016-03-28 | 2020-06-16 | Intra-Cellular Therapies, Inc. | Compositions and methods |
| US11014925B2 (en) | 2016-03-28 | 2021-05-25 | Intra-Cellular Therapies, Inc. | Co-crystals of 1-(4-fluoro-phenyl)-4-((6bR,1OaS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H- pyrido[3′,4′:4,51_pyrrolo [1,2,3-delqcuinoxalin-8-yl)-butan-1-one with nicotinamide or isonicotinamide |
| EP3436455A4 (en) * | 2016-03-28 | 2019-09-04 | Intra-Cellular Therapies, Inc. | NOVEL SALTS AND CRYSTALS |
| EP3525763B1 (en) | 2016-10-12 | 2025-03-05 | Intra-Cellular Therapies, Inc. | Amorphous solid dispersions |
| WO2018126140A1 (en) | 2016-12-29 | 2018-07-05 | Intra-Cellular Therapies, Inc. | Organic compounds |
| EP3562484B1 (en) | 2016-12-29 | 2021-08-25 | Intra-Cellular Therapies, Inc. | Pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxaline derivatives useful in the treatment of cns disorders |
| RU2767410C2 (ru) | 2017-03-24 | 2022-03-17 | Интра-Селлулар Терапиз, Инк. | Новые композиции и способы |
| EP3609501A4 (en) * | 2017-04-10 | 2020-08-19 | Dr. Reddy's Laboratories Limited | AMORPHIC FORM AND SOLID DISPERSIONS OF LUMATEPERONE P-TOSYLATE |
| US9993486B1 (en) | 2017-06-19 | 2018-06-12 | Tlc Therapeutics, Llc | Oral quetiapine suspension formulations with extended shelf life and enhanced bioavailability |
| WO2019023062A1 (en) | 2017-07-26 | 2019-01-31 | Intra-Cellular Therapies, Inc. | ORGANIC COMPOUNDS |
| EP3658144B1 (en) | 2017-07-26 | 2022-01-26 | Intra-Cellular Therapies, Inc. | Pyridopyrroloquinoxaline compounds, their compositions and uses in therapy |
| US11440911B2 (en) | 2017-09-26 | 2022-09-13 | Intra-Cellular Therapies, Inc. | Salts and crystals |
| KR102036909B1 (ko) * | 2017-11-28 | 2019-10-25 | 한국과학기술원 | 신규 디스토니아 치료용 약학적 조성물 |
| WO2019178484A1 (en) | 2018-03-16 | 2019-09-19 | Intra-Cellular Therapies, Inc. | Novel methods |
| CN112040940A (zh) | 2018-03-23 | 2020-12-04 | 细胞内治疗公司 | 有机化合物 |
| US20210008065A1 (en) | 2018-03-23 | 2021-01-14 | Intra-Cellular Therapies, Inc. | Organic compounds |
| AU2019280850C1 (en) | 2018-06-06 | 2025-02-13 | Intra-Cellular Therapies, Inc. | Novel salts and crystals |
| EP3801527B1 (en) | 2018-06-08 | 2025-02-19 | Intra-Cellular Therapies, Inc. | Fused gamma-carbolines for acute treatment of anxiety or depression |
| CA3240552A1 (en) | 2018-06-11 | 2019-12-19 | Intra-Cellular Therapies, Inc. | Substituted heterocycle fused gamma-carbolines synthesis |
| US11806311B2 (en) | 2018-06-21 | 2023-11-07 | Aquestive Therapeutics, Inc. | System and method for making personalized individual unit doses containing pharmaceutical actives |
| US12144808B2 (en) | 2018-08-29 | 2024-11-19 | Intra-Cellular Therapies, Inc. | Compositions and methods |
| BR112021003655A2 (pt) | 2018-08-31 | 2021-05-18 | Intra-Cellular Therapies, Inc. | métodos novos |
| WO2020047408A1 (en) | 2018-08-31 | 2020-03-05 | Intra-Cellular Therapies, Inc. | Novel methods |
| CA3110997A1 (en) | 2018-09-07 | 2020-03-12 | Aquestive Therapeutics, Inc. | Oral film compositions and dosage forms having precise active dissolution profiles |
| US20210393621A1 (en) | 2018-10-26 | 2021-12-23 | The Research Foundation For The State University Of New York | Combination serotonin specific reuptake inhibitor and serotonin 1a receptor partial agonist for reducing l-dopa-induced dyskinesia |
| JP7520013B2 (ja) | 2018-12-17 | 2024-07-22 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 置換複素環縮合γ－カルボリンの合成 |
| IL315005B2 (en) | 2018-12-17 | 2026-04-01 | Intra Cellular Therapies Inc | Synthesis of condensed gamma-carbolines and converted heterocycles |
| WO2020131899A1 (en) | 2018-12-17 | 2020-06-25 | Intra-Cellular Therapies, Inc. | Organic compound |
| US12195463B2 (en) | 2018-12-21 | 2025-01-14 | Intra-Cellular Therapies, Inc. | Organic compounds |
| JP7649743B2 (ja) * | 2018-12-21 | 2025-03-21 | イントラ－セルラー・セラピーズ・インコーポレイテッド | 有機化合物 |
| WO2021007245A1 (en) | 2019-07-07 | 2021-01-14 | Intra-Cellular Therapies, Inc. | Novel methods |
| US12478623B2 (en) | 2019-09-25 | 2025-11-25 | Intra-Cellular Therapies, Inc. | Methods of treating central nervous system disorders comprising administering lumateperone and a nitric oxide donor |
| KR102227268B1 (ko) * | 2019-10-07 | 2021-03-12 | 한국과학기술원 | 디스토니아 치료 후보 약물의 신규 스크리닝 방법 |
| KR20220126286A (ko) | 2019-11-01 | 2022-09-15 | 어퀘스티브 테라퓨틱스, 아이엔씨. | 전구약물 조성물 및 치료 방법 |
| KR20220126287A (ko) | 2019-11-14 | 2022-09-15 | 어퀘스티브 테라퓨틱스, 아이엔씨. | 멀티모달 조성물 및 치료 방법 |
| EP4072554A4 (en) | 2019-12-11 | 2023-12-20 | Intra-Cellular Therapies, Inc. | ORGANIC CONNECTION |
| WO2021127572A1 (en) | 2019-12-19 | 2021-06-24 | Intra-Cellular Therapies, Inc. | Methods of schizophrenia treatment |
| MX2023004102A (es) * | 2020-10-09 | 2023-04-27 | Shujing Biopharma Co Ltd | Derivado de gamma-carbolina fusionado sustituido con heterociclo, metodo de preparacion del mismo, intermediarios del mismo y uso del mismo. |
| EP4277611A1 (en) | 2021-01-15 | 2023-11-22 | Aquestive Therapeutics, Inc. | Prodrug compositions and methods of treatment |
| CA3210706A1 (en) | 2021-03-09 | 2022-09-15 | Alexander Mark Schobel | Dosage forms having equivalent biocomparable profiles |
| US20250025572A1 (en) * | 2021-11-29 | 2025-01-23 | Editas Medicine, Inc. | Engineered crispr/cas12a effector proteins, and uses thereof |
| US12414948B2 (en) | 2022-05-18 | 2025-09-16 | Intra-Cellular Therapies, Inc. | Methods |
| CN119486738A (zh) | 2022-05-18 | 2025-02-18 | 细胞内治疗公司 | 新方法 |
| CN115067220B (zh) * | 2022-06-16 | 2023-04-25 | 中国人民解放军军事科学院军事医学研究院 | 一种双通道小动物恐惧共情行为检测系统 |
| CN120282964A (zh) * | 2022-10-26 | 2025-07-08 | 上海枢境生物科技有限公司 | 一种杂环取代的稠合γ-咔啉类衍生物的甲磺酸盐、晶型及其制备方法和应用 |
| WO2024145659A1 (en) | 2022-12-30 | 2024-07-04 | Intra-Cellular Therapies, Inc. | Heterocycle fused gamma-carbolines acting on the serotonine 5-ht2a receptor |
| WO2024173901A1 (en) | 2023-02-17 | 2024-08-22 | Intra-Cellular Therapies, Inc. | Lumateperone and derivatives thereof for modulating the nervous system |
| WO2025111568A1 (en) | 2023-11-22 | 2025-05-30 | Intra-Cellular Therapies, Inc. | Lumateperone and analogues, as 5-ht2a or 5-ht2a/d2 receptor modulators, for use in the treatment of psychiatric disorders caused by viral, bacterial, or autoimmune encephalitis, and of psychiatric symptoms thereof |
| KR20250129554A (ko) | 2024-02-22 | 2025-08-29 | 단국대학교 천안캠퍼스 산학협력단 | 드로페리돌을 유효성분으로 포함하는 신경 질환 예방 또는 치료용 약학 조성물 |
| US20250352469A1 (en) | 2024-05-16 | 2025-11-20 | Intra-Cellular Therapies, Inc. | Novel compositions, devices, and methods |
| WO2026011166A1 (en) | 2024-07-03 | 2026-01-08 | Intra-Cellular Therapies, Inc. | Substituted heterocycles for use in the treatment of diseases involving the 5-ht2a receptor |
| WO2026011136A1 (en) | 2024-07-03 | 2026-01-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4162318A (en) * | 1976-05-05 | 1979-07-24 | Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.P.A. | Use of trazodone and etoperidone in Parkinsonism and in other extrapyramidal syndromes characterized by tremors |
| HU208484B (en) | 1988-08-17 | 1993-11-29 | Chinoin Gyogyszer Es Vegyeszet | Process for producing pharmaceutical composition containing acid additional salt of selegilin as active component for treating schisofrenia |
| US5114976A (en) | 1989-01-06 | 1992-05-19 | Norden Michael J | Method for treating certain psychiatric disorders and certain psychiatric symptoms |
| ATE277048T1 (de) | 1999-06-15 | 2004-10-15 | Bristol Myers Squibb Pharma Co | Substituierte hetercyclisch kondensierte gamma carboline |
| US6713471B1 (en) | 1999-06-15 | 2004-03-30 | Bristol-Myers Squibb Pharma Company | Substituted heterocycle fused gamma-carbolines |
| US7071186B2 (en) * | 1999-06-15 | 2006-07-04 | Bristol-Myers Squibb Pharma Co. | Substituted heterocycle fused gamma-carbolines |
| US20050222209A1 (en) | 2004-04-01 | 2005-10-06 | Zeldis Jerome B | Methods and compositions for the treatment, prevention or management of dysfunctional sleep and dysfunctional sleep associated with disease |
| EP1848433A2 (en) | 2005-01-25 | 2007-10-31 | Celgene Corporation | Methods and compositions using 4-amino-2-(3-methyl-2,6-dioxopiperidin-3-yl)-isoindole-1-3-dione |
| US20080194592A1 (en) | 2005-08-23 | 2008-08-14 | Intra-Cellular Therapies, Inc. | Organic Compounds |
| US7645752B2 (en) | 2006-01-13 | 2010-01-12 | Wyeth Llc | Sulfonyl substituted 1H-indoles as ligands for the 5-hydroxytryptamine receptors |
| AU2007292848A1 (en) | 2006-09-08 | 2008-03-13 | Braincells, Inc. | Combinations containing a 4-acylaminopyridine derivative |
| KR102107954B1 (ko) | 2007-03-12 | 2020-05-07 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 치환된 헤테로환 융합 감마-카르볼린 합성 |
| MX2010001218A (es) | 2007-08-01 | 2010-04-07 | Medivation Neurology Inc | Metodos y composiciones para tratamiento contra esquizofrenia mediante uso de terapia combinada de agentes antipsicoticos. |
| EP2250199B1 (en) | 2008-02-07 | 2015-09-02 | Merck Sharp & Dohme Corp. | Engineered anti-tslpr antibodies |
| AU2009223701B2 (en) | 2008-03-12 | 2015-04-16 | Intra-Cellular Therapies, Inc. | Substituted heterocycle fused gamma-carbolines solid |
| EP3085231A1 (en) * | 2008-05-27 | 2016-10-26 | Intra-Cellular Therapies, Inc. | Method and compositions for sleep disorders and other disorders |
| CA2796756A1 (en) | 2010-04-22 | 2011-10-27 | Intra-Cellular Therapies, Inc. | Substituted pyrido(3',4':4,5)pyrrolo(1,2,3-de)quinoxalines for the treatment of central nervous system disorders |
| KR20140146192A (ko) | 2012-04-14 | 2014-12-24 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 유기 화합물 |
| US9708322B2 (en) * | 2013-03-15 | 2017-07-18 | Intra-Cellular Therapies, Inc. | Substituted pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines for inhibiting serotonin reuptake transporter activity |
| KR102373288B1 (ko) * | 2013-12-03 | 2022-03-10 | 인트라-셀룰라 써래피스, 인코퍼레이티드. | 신규한 방법 |
| US10077267B2 (en) * | 2014-04-04 | 2018-09-18 | Intra-Cellular Therapies, Inc. | Organic compounds |
| CA2944755A1 (en) * | 2014-04-04 | 2015-10-08 | Intra-Cellular Therapies, Inc. | Organic compounds |
| PL3838274T3 (pl) * | 2016-01-26 | 2024-04-02 | Intra-Cellular Therapies, Inc. | Pochodna pirydo[3',4':4,5]pirolo[1,2,3-DE]chinoksaliny do zastosowania w leczeniu zaburzeń OUN |
| US11014925B2 (en) * | 2016-03-28 | 2021-05-25 | Intra-Cellular Therapies, Inc. | Co-crystals of 1-(4-fluoro-phenyl)-4-((6bR,1OaS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H- pyrido[3′,4′:4,51_pyrrolo [1,2,3-delqcuinoxalin-8-yl)-butan-1-one with nicotinamide or isonicotinamide |
| EP3436455A4 (en) * | 2016-03-28 | 2019-09-04 | Intra-Cellular Therapies, Inc. | NOVEL SALTS AND CRYSTALS |
| EP3525763B1 (en) * | 2016-10-12 | 2025-03-05 | Intra-Cellular Therapies, Inc. | Amorphous solid dispersions |
| EP3658144B1 (en) * | 2017-07-26 | 2022-01-26 | Intra-Cellular Therapies, Inc. | Pyridopyrroloquinoxaline compounds, their compositions and uses in therapy |
| WO2020047408A1 (en) * | 2018-08-31 | 2020-03-05 | Intra-Cellular Therapies, Inc. | Novel methods |
-
2009
- 2009-05-27 EP EP16151760.2A patent/EP3085231A1/en not_active Withdrawn
- 2009-05-27 US US12/994,560 patent/US8598119B2/en not_active Ceased
- 2009-05-27 CN CN200980128888.4A patent/CN102105059B/zh active Active
- 2009-05-27 KR KR1020107029327A patent/KR20110022631A/ko not_active Ceased
- 2009-05-27 AU AU2009251816A patent/AU2009251816B2/en active Active
- 2009-05-27 KR KR1020167032085A patent/KR102133073B1/ko active Active
- 2009-05-27 MX MX2015004044A patent/MX377802B/es unknown
- 2009-05-27 EP EP09755263A patent/EP2320731A4/en not_active Ceased
- 2009-05-27 US US16/784,112 patent/USRE48839E1/en active Active
- 2009-05-27 CN CN201510553160.3A patent/CN105168219B/zh active Active
- 2009-05-27 KR KR1020207033595A patent/KR102317698B1/ko active Active
- 2009-05-27 WO PCT/US2009/003261 patent/WO2009145900A1/en not_active Ceased
- 2009-05-27 KR KR1020197000911A patent/KR102184038B1/ko active Active
- 2009-05-27 MX MX2010013020A patent/MX2010013020A/es active IP Right Grant
- 2009-05-27 CA CA2725342A patent/CA2725342C/en active Active
- 2009-05-27 JP JP2011511638A patent/JP6106361B2/ja active Active
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2010
- 2010-11-26 MX MX2020012868A patent/MX2020012868A/es unknown
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2023
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- 2023-10-04 US US18/481,170 patent/US20240041871A1/en not_active Abandoned
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