KR20190049732A - 5-ht2c 수용체 효능제 및 조성물 및 사용 방법 - Google Patents
5-ht2c 수용체 효능제 및 조성물 및 사용 방법 Download PDFInfo
- Publication number
- KR20190049732A KR20190049732A KR1020197007503A KR20197007503A KR20190049732A KR 20190049732 A KR20190049732 A KR 20190049732A KR 1020197007503 A KR1020197007503 A KR 1020197007503A KR 20197007503 A KR20197007503 A KR 20197007503A KR 20190049732 A KR20190049732 A KR 20190049732A
- Authority
- KR
- South Korea
- Prior art keywords
- pyrazino
- hexahydro
- naphthyridine
- halogen
- optionally substituted
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Withdrawn
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- 239000000203 mixture Substances 0.000 title claims abstract description 39
- 238000000034 method Methods 0.000 title claims description 203
- 239000000018 receptor agonist Substances 0.000 title description 26
- 229940044601 receptor agonist Drugs 0.000 title description 26
- 108010072553 5-HT2C Serotonin Receptor Proteins 0.000 title description 4
- 102000006902 5-HT2C Serotonin Receptor Human genes 0.000 title description 4
- 150000001875 compounds Chemical class 0.000 claims abstract description 489
- 238000011282 treatment Methods 0.000 claims abstract description 192
- 208000008589 Obesity Diseases 0.000 claims abstract description 87
- 235000020824 obesity Nutrition 0.000 claims abstract description 87
- 230000037221 weight management Effects 0.000 claims abstract description 63
- 230000009467 reduction Effects 0.000 claims abstract description 41
- 230000002265 prevention Effects 0.000 claims abstract description 37
- 206010015037 epilepsy Diseases 0.000 claims abstract description 28
- 230000037406 food intake Effects 0.000 claims abstract description 26
- 235000012631 food intake Nutrition 0.000 claims abstract description 25
- 235000019627 satiety Nutrition 0.000 claims abstract description 25
- 230000036186 satiety Effects 0.000 claims abstract description 25
- 208000011580 syndromic disease Diseases 0.000 claims abstract description 23
- 208000007848 Alcoholism Diseases 0.000 claims abstract description 21
- 208000011117 substance-related disease Diseases 0.000 claims abstract description 19
- 206010013663 drug dependence Diseases 0.000 claims abstract description 17
- 230000006698 induction Effects 0.000 claims abstract description 13
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 10
- -1 (Methoxycarbonyl) amino, 2-phenylacetamido Chemical group 0.000 claims description 269
- 229910052736 halogen Inorganic materials 0.000 claims description 222
- 150000002367 halogens Chemical group 0.000 claims description 222
- 239000003814 drug Substances 0.000 claims description 196
- 229940079593 drug Drugs 0.000 claims description 126
- 125000003118 aryl group Chemical group 0.000 claims description 123
- 229910052739 hydrogen Inorganic materials 0.000 claims description 109
- 239000001257 hydrogen Substances 0.000 claims description 108
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims description 92
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 91
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 85
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims description 85
- 150000003839 salts Chemical class 0.000 claims description 76
- 239000012453 solvate Substances 0.000 claims description 75
- 150000004677 hydrates Chemical class 0.000 claims description 72
- 238000004519 manufacturing process Methods 0.000 claims description 61
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 55
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 46
- 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims description 36
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 36
- 229910052757 nitrogen Inorganic materials 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 23
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 21
- 238000002560 therapeutic procedure Methods 0.000 claims description 21
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 20
- 125000002816 methylsulfanyl group Chemical group [H]C([H])([H])S[*] 0.000 claims description 17
- 125000004210 cyclohexylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 16
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 16
- 230000001939 inductive effect Effects 0.000 claims description 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 15
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 14
- 125000005418 aryl aryl group Chemical group 0.000 claims description 13
- 125000001731 2-cyanoethyl group Chemical group [H]C([H])(*)C([H])([H])C#N 0.000 claims description 11
- 125000006284 3-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C(F)=C1[H])C([H])([H])* 0.000 claims description 11
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 11
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 11
- 125000001972 isopentyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])C([H])([H])* 0.000 claims description 11
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 11
- 125000004847 2-fluorobenzyl group Chemical group [H]C1=C([H])C(F)=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 10
- 125000004851 cyclopentylmethyl group Chemical group C1(CCCC1)C* 0.000 claims description 10
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 10
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 10
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 10
- 125000000094 2-phenylethyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])C([H])([H])* 0.000 claims description 9
- 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 125000004176 4-fluorobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1F)C([H])([H])* 0.000 claims description 7
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims description 7
- 241001465754 Metazoa Species 0.000 claims description 7
- 125000003548 sec-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 7
- 125000000175 2-thienyl group Chemical group S1C([*])=C([H])C([H])=C1[H] 0.000 claims description 6
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 6
- 125000004850 cyclobutylmethyl group Chemical group C1(CCC1)C* 0.000 claims description 6
- 239000003937 drug carrier Substances 0.000 claims description 6
- 125000004974 2-butenyl group Chemical group C(C=CC)* 0.000 claims description 5
- ZUSWDTWYONAOPH-UHFFFAOYSA-N [2-(trifluoromethyl)phenyl]hydrazine;hydrochloride Chemical group [Cl-].[NH3+]NC1=CC=CC=C1C(F)(F)F ZUSWDTWYONAOPH-UHFFFAOYSA-N 0.000 claims description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 5
- 206010001605 Alcohol poisoning Diseases 0.000 claims description 3
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims description 3
- 206010070863 Toxicity to various agents Diseases 0.000 claims description 3
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims description 3
- 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 2
- 125000005605 benzo group Chemical group 0.000 claims description 2
- 150000002431 hydrogen Chemical class 0.000 claims 4
- FLBAYUMRQUHISI-UHFFFAOYSA-N 1,8-naphthyridine Chemical compound N1=CC=CC2=CC=CN=C21 FLBAYUMRQUHISI-UHFFFAOYSA-N 0.000 claims 2
- PRCYDMDJOWSMFR-UHFFFAOYSA-N C1=CN=C2N3CC=NC=C3C=CC2=C1 Chemical compound C1=CN=C2N3CC=NC=C3C=CC2=C1 PRCYDMDJOWSMFR-UHFFFAOYSA-N 0.000 claims 2
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 2
- NVIQIDULVIDTHT-MRVPVSSYSA-N (10R)-6-chloro-1,3,5,12-tetrazatricyclo[8.5.0.02,7]pentadeca-2(7),3,5-triene Chemical compound ClC1=NC=NC2=C1CC[C@H]1N2CCCNC1 NVIQIDULVIDTHT-MRVPVSSYSA-N 0.000 claims 1
- RHUYPYGEUQRZCB-SNVBAGLBSA-N (4aR)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a][1,6]naphthyridine Chemical compound C1CNC[C@@H]2N1C1=CC=NC=C1CC2 RHUYPYGEUQRZCB-SNVBAGLBSA-N 0.000 claims 1
- XTFPZVLQJQUVFI-CYBMUJFWSA-N (4aR)-7-(cyclobutylmethyl)-2,3,4,4a,5,6-hexahydro-1H-pyrazino[1,2-a][1,6]naphthyridine Chemical compound C1(CCC1)CC1=C2CC[C@H]3N(C2=CC=N1)CCNC3 XTFPZVLQJQUVFI-CYBMUJFWSA-N 0.000 claims 1
- VDZXAROYSVTVCJ-QGZVFWFLSA-N (6aR)-3-(cyclohexylmethyl)-4-ethyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C1(CCCCC1)CC1=C(C=2CC[C@H]3N(C=2N=C1)CCNC3)CC VDZXAROYSVTVCJ-QGZVFWFLSA-N 0.000 claims 1
- CMOXGSMXWFCHLU-MRXNPFEDSA-N (6aR)-3-(cyclopentylmethyl)-4-ethyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C1(CCCC1)CC1=C(C=2CC[C@H]3N(C=2N=C1)CCNC3)CC CMOXGSMXWFCHLU-MRXNPFEDSA-N 0.000 claims 1
- NZMUSZUGSVODII-QGZVFWFLSA-N (6aR)-3-benzyl-4-ethyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(C1=CC=CC=C1)C1=C(C=2CC[C@H]3N(C=2N=C1)CCNC3)CC NZMUSZUGSVODII-QGZVFWFLSA-N 0.000 claims 1
- VNFDDQKZHIOOLW-SECBINFHSA-N (6aR)-3-chloro-4-(3,3,3-trifluoropropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound ClC1=C(C=2CC[C@H]3N(C=2N=C1)CCNC3)CCC(F)(F)F VNFDDQKZHIOOLW-SECBINFHSA-N 0.000 claims 1
- HQAWHPVYGMEWPU-CYBMUJFWSA-N (6aR)-3-cyclobutyl-4-ethyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C1(CCC1)C1=C(C=2CC[C@H]3N(C=2N=C1)CCNC3)CC HQAWHPVYGMEWPU-CYBMUJFWSA-N 0.000 claims 1
- XTWJJKFHLIDCOK-CYBMUJFWSA-N (6aR)-3-propyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(CC)C1=CC=2CC[C@H]3N(C=2N=C1)CCNC3 XTWJJKFHLIDCOK-CYBMUJFWSA-N 0.000 claims 1
- SUFPITAQEZLQHL-CYBMUJFWSA-N (6aR)-4-(1,3-benzodioxol-5-yl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound O1COC2=C1C=CC(=C2)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 SUFPITAQEZLQHL-CYBMUJFWSA-N 0.000 claims 1
- IGPVFLAKJJQRDS-CYBMUJFWSA-N (6aR)-4-(2,2-dimethylpropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(C(C)(C)C)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 IGPVFLAKJJQRDS-CYBMUJFWSA-N 0.000 claims 1
- QFCTXPYSZGPYAK-GFCCVEGCSA-N (6aR)-4-(2-methoxyethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound COCCC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 QFCTXPYSZGPYAK-GFCCVEGCSA-N 0.000 claims 1
- FFLMKLHRNAKIDD-CYBMUJFWSA-N (6aR)-4-(2-methylpropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(C(C)C)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 FFLMKLHRNAKIDD-CYBMUJFWSA-N 0.000 claims 1
- PQVMQEUTSZUZCU-QGZVFWFLSA-N (6aR)-4-(2-phenylethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C1(=CC=CC=C1)CCC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 PQVMQEUTSZUZCU-QGZVFWFLSA-N 0.000 claims 1
- ZLOMTQBPDHCEQU-LLVKDONJSA-N (6aR)-4-(3,3,3-trifluoropropyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound FC(CCC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3)(F)F ZLOMTQBPDHCEQU-LLVKDONJSA-N 0.000 claims 1
- HACPNJTWKCOJIE-CQSZACIVSA-N (6aR)-4-(3-methylbutyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(CC(C)C)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 HACPNJTWKCOJIE-CQSZACIVSA-N 0.000 claims 1
- XRKGPWHXUPXFEO-CQSZACIVSA-N (6aR)-4-(4-methoxyphenyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound COC1=CC=C(C=C1)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 XRKGPWHXUPXFEO-CQSZACIVSA-N 0.000 claims 1
- UXZDAOLWIVIKNR-MRXNPFEDSA-N (6aR)-4-(cyclohexylmethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,7]naphthyridine Chemical compound C1(CCCCC1)CC=1C=2CC[C@H]3N(C=2C=NC=1)CCNC3 UXZDAOLWIVIKNR-MRXNPFEDSA-N 0.000 claims 1
- YWNMUBLSJLIWPI-MRXNPFEDSA-N (6aR)-4-(cyclohexylmethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C1(CCCCC1)CC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 YWNMUBLSJLIWPI-MRXNPFEDSA-N 0.000 claims 1
- VLNBXOFFUSACLM-OAHLLOKOSA-N (6aR)-4-(cyclopentylmethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C1(CCCC1)CC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 VLNBXOFFUSACLM-OAHLLOKOSA-N 0.000 claims 1
- JZNPRZRCDYEBIG-LLVKDONJSA-N (6aR)-4-(methoxymethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound COCC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 JZNPRZRCDYEBIG-LLVKDONJSA-N 0.000 claims 1
- MMTJSSRLSCOMQV-GICMACPYSA-N (6aR)-4-(oxan-2-ylmethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound O1C(CCCC1)CC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 MMTJSSRLSCOMQV-GICMACPYSA-N 0.000 claims 1
- KRIAGOUOSDKANC-MRXNPFEDSA-N (6aR)-4-(oxan-4-ylmethoxymethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound O1CCC(CC1)COCC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 KRIAGOUOSDKANC-MRXNPFEDSA-N 0.000 claims 1
- ZFNONDAYGNEJHH-CYBMUJFWSA-N (6aR)-4-(propan-2-yloxymethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(C)(C)OCC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 ZFNONDAYGNEJHH-CYBMUJFWSA-N 0.000 claims 1
- PBLXOWHPHSPXLH-OAHLLOKOSA-N (6aR)-4-(pyridin-2-ylmethyl)-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound N1=C(C=CC=C1)CC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 PBLXOWHPHSPXLH-OAHLLOKOSA-N 0.000 claims 1
- DVGKKRBHJDLRAB-OAHLLOKOSA-N (6aR)-4-[(2-fluorophenyl)methyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound FC1=C(CC=2C=3CC[C@H]4N(C=3N=CC=2)CCNC4)C=CC=C1 DVGKKRBHJDLRAB-OAHLLOKOSA-N 0.000 claims 1
- LXJQUSCIXJJMCJ-MRXNPFEDSA-N (6aR)-4-[(3-fluorophenyl)methyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound FC=1C=C(CC=2C=3CC[C@H]4N(C=3N=CC=2)CCNC4)C=CC=1 LXJQUSCIXJJMCJ-MRXNPFEDSA-N 0.000 claims 1
- PUZQIEAXLJCDIM-MRXNPFEDSA-N (6aR)-4-[(4-fluorophenyl)methyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound FC1=CC=C(CC=2C=3CC[C@H]4N(C=3N=CC=2)CCNC4)C=C1 PUZQIEAXLJCDIM-MRXNPFEDSA-N 0.000 claims 1
- IXPAHOYPEONZOP-CYBMUJFWSA-N (6aR)-4-[3-(trifluoromethoxy)phenyl]-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound FC(OC=1C=C(C=CC=1)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3)(F)F IXPAHOYPEONZOP-CYBMUJFWSA-N 0.000 claims 1
- YEAATRDZIJRTNR-MRXNPFEDSA-N (6aR)-4-benzyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,7]naphthyridine Chemical compound C(C1=CC=CC=C1)C=1C=2CC[C@H]3N(C=2C=NC=1)CCNC3 YEAATRDZIJRTNR-MRXNPFEDSA-N 0.000 claims 1
- BCRYOGOFXLRJPN-MRXNPFEDSA-N (6aR)-4-benzyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(C1=CC=CC=C1)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 BCRYOGOFXLRJPN-MRXNPFEDSA-N 0.000 claims 1
- RWJBCAMNHPNRNP-SECBINFHSA-N (6aR)-4-bromo-5,6,6a,7,8,9,10,11-octahydro-[1,4]diazepino[1,2-a][1,8]naphthyridine Chemical compound BrC=1C=2CC[C@H]3N(C=2N=CC=1)CCCNC3 RWJBCAMNHPNRNP-SECBINFHSA-N 0.000 claims 1
- NPSWEGDJUDVYGS-MRVPVSSYSA-N (6aR)-4-bromo-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,7]naphthyridine Chemical compound BrC=1C=2CC[C@H]3N(C=2C=NC=1)CCNC3 NPSWEGDJUDVYGS-MRVPVSSYSA-N 0.000 claims 1
- KXNZVLXXOMNAOM-CYBMUJFWSA-N (6aR)-4-butyl-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound C(CCC)C=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 KXNZVLXXOMNAOM-CYBMUJFWSA-N 0.000 claims 1
- XNITVWNCNFQVDG-MRVPVSSYSA-N (6aR)-4-chloro-6,6a,7,8,9,10-hexahydro-5H-pyrazino[1,2-a][1,8]naphthyridine Chemical compound ClC=1C=2CC[C@H]3N(C=2N=CC=1)CCNC3 XNITVWNCNFQVDG-MRVPVSSYSA-N 0.000 claims 1
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| 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 |
| WO2019131902A1 (ja) | 2017-12-27 | 2019-07-04 | 武田薬品工業株式会社 | 腹圧性尿失禁および便失禁の治療薬 |
| CA3113234A1 (en) | 2018-09-18 | 2020-03-26 | Nikang Therapeutics, Inc. | Tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors |
| WO2020072675A1 (en) | 2018-10-02 | 2020-04-09 | Northwestern University | Beta-carbolines as positive allosteric modulators of the human serotonin receptor 2c (5-ht2c) |
| CN113993523A (zh) | 2019-04-17 | 2022-01-28 | 指南针探路者有限公司 | 用赛洛西宾治疗抑郁症和其他各种病症 |
| WO2022011350A1 (en) * | 2020-07-10 | 2022-01-13 | Eleusis Therapeutics Us, Inc. | Method of treatment for psilocybin or psilocin infusion |
| US11312684B1 (en) | 2021-02-10 | 2022-04-26 | Eleusis Therapeutics Us, Inc. | Pharmaceutically acceptable salts of psilocin and uses thereof |
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| KR101913442B1 (ko) * | 2010-09-01 | 2018-10-30 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 체중 관리에 유용한 5-ｈｔ2ｃ 작동제의 변형-방출 투여 형태 |
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| US20190225612A1 (en) | 2019-07-25 |
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| CA3033142A1 (en) | 2018-02-22 |
| EP3500570A1 (en) | 2019-06-26 |
| CN109952301A (zh) | 2019-06-28 |
| BR112019003142A2 (pt) | 2019-05-21 |
| AU2017313908A1 (en) | 2019-02-28 |
| EA201990527A1 (ru) | 2019-07-31 |
| NZ750469A (en) | 2023-03-31 |
| MA45987A (fr) | 2019-06-26 |
| JP2019524844A (ja) | 2019-09-05 |
| US20210214355A1 (en) | 2021-07-15 |
| MX2019002020A (es) | 2019-11-25 |
| CN109952301B (zh) | 2022-03-25 |
| AU2017313908B2 (en) | 2021-10-21 |
| EA038219B1 (ru) | 2021-07-26 |
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