JP2019510039A5 - - Google Patents

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Publication number

JP2019510039A5

JP2019510039A5 JP2018550673A JP2018550673A JP2019510039A5 JP 2019510039 A5 JP2019510039 A5 JP 2019510039A5 JP 2018550673 A JP2018550673 A JP 2018550673A JP 2018550673 A JP2018550673 A JP 2018550673A JP 2019510039 A5 JP2019510039 A5 JP 2019510039A5

Authority

JP

Japan

Prior art keywords

pharmaceutical composition

formula

composition according

dementia

ht2a

Prior art date

2017-03-28

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.)

Pending

Links

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• 239000008194 pharmaceutical composition Substances 0.000 claims description 27
• 150000001875 compounds Chemical class 0.000 claims description 26
• 125000000217 alkyl group Chemical group 0.000 claims description 23
• 102100036321 5-hydroxytryptamine receptor 2A Human genes 0.000 claims description 16
• 150000003839 salts Chemical group 0.000 claims description 15
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
• 208000035475 disorder Diseases 0.000 claims description 14
• 239000012458 free base Substances 0.000 claims description 14
• 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 claims description 11
• 206010012289 Dementia Diseases 0.000 claims description 10
• 108010072564 5-HT2A Serotonin Receptor Proteins 0.000 claims description 8
• 101710138091 5-hydroxytryptamine receptor 2A Proteins 0.000 claims description 8
• 101150049660 DRD2 gene Proteins 0.000 claims description 8
• 229940121836 Phosphodiesterase 1 inhibitor Drugs 0.000 claims description 8
• 239000003446 ligand Substances 0.000 claims description 8
• 208000024827 Alzheimer disease Diseases 0.000 claims description 6
• 239000002775 capsule Substances 0.000 claims description 6
• 125000001475 halogen functional group Chemical group 0.000 claims description 5
• 201000011240 Frontotemporal dementia Diseases 0.000 claims description 4
• 230000019771 cognition Effects 0.000 claims description 4
• 239000003085 diluting agent Substances 0.000 claims description 4
• -1 monophosphate salt Chemical class 0.000 claims description 4
• 125000002490 anilino group Chemical group [H]N(*)C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 3
• 125000000440 benzylamino group Chemical group [H]N(*)C([H])([H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 3
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 3
• 239000000651 prodrug Chemical group 0.000 claims description 3
• 229940002612 prodrug Drugs 0.000 claims description 3
• 201000010374 Down Syndrome Diseases 0.000 claims description 2
• 208000023105 Huntington disease Diseases 0.000 claims description 2
• 208000006264 Korsakoff syndrome Diseases 0.000 claims description 2
• 208000009829 Lewy Body Disease Diseases 0.000 claims description 2
• 201000002832 Lewy body dementia Diseases 0.000 claims description 2
• 208000019022 Mood disease Diseases 0.000 claims description 2
• 206010033799 Paralysis Diseases 0.000 claims description 2
• 208000018737 Parkinson disease Diseases 0.000 claims description 2
• 208000000609 Pick Disease of the Brain Diseases 0.000 claims description 2
• 208000024777 Prion disease Diseases 0.000 claims description 2
• 208000028017 Psychotic disease Diseases 0.000 claims description 2
• 206010039966 Senile dementia Diseases 0.000 claims description 2
• 201000004810 Vascular dementia Diseases 0.000 claims description 2
• 201000008485 Wernicke-Korsakoff syndrome Diseases 0.000 claims description 2
• 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 2
• 230000003542 behavioural effect Effects 0.000 claims description 2
• 239000003795 chemical substances by application Substances 0.000 claims description 2
• 208000013044 corticobasal degeneration disease Diseases 0.000 claims description 2
• 239000012895 dilution Substances 0.000 claims description 2
• 238000010790 dilution Methods 0.000 claims description 2
• 239000002552 dosage form Substances 0.000 claims description 2
• 239000011159 matrix material Substances 0.000 claims description 2
• 201000006417 multiple sclerosis Diseases 0.000 claims description 2
• 208000021090 palsy Diseases 0.000 claims description 2
• 208000019116 sleep disease Diseases 0.000 claims description 2
• 208000024891 symptom Diseases 0.000 claims description 2
• JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
• UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
• 125000005490 tosylate group Chemical class 0.000 claims 1
• 238000000034 method Methods 0.000 description 20
• POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 4
• IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 4
• WWZKQHOCKIZLMA-UHFFFAOYSA-N octanoic acid Chemical compound CCCCCCCC(O)=O WWZKQHOCKIZLMA-UHFFFAOYSA-N 0.000 description 4
• 229920006395 saturated elastomer Polymers 0.000 description 4
• TUNFSRHWOTWDNC-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O TUNFSRHWOTWDNC-UHFFFAOYSA-N 0.000 description 4
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 3
• 229910052799 carbon Inorganic materials 0.000 description 3
• 239000000203 mixture Substances 0.000 description 3
• 125000004076 pyridyl group Chemical group 0.000 description 3
• JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical group CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 3
• UGUHFDPGDQDVGX-UHFFFAOYSA-N 1,2,3-thiadiazole Chemical compound C1=CSN=N1 UGUHFDPGDQDVGX-UHFFFAOYSA-N 0.000 description 2
• GYSCBCSGKXNZRH-UHFFFAOYSA-N 1-benzothiophene-2-carboxamide Chemical compound C1=CC=C2SC(C(=O)N)=CC2=C1 GYSCBCSGKXNZRH-UHFFFAOYSA-N 0.000 description 2
• GHVNFZFCNZKVNT-UHFFFAOYSA-N Decanoic acid Natural products CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 2
• 235000021314 Palmitic acid Nutrition 0.000 description 2
• 125000003545 alkoxy group Chemical group 0.000 description 2
• OBETXYAYXDNJHR-UHFFFAOYSA-N alpha-ethylcaproic acid Natural products CCCCC(CC)C(O)=O OBETXYAYXDNJHR-UHFFFAOYSA-N 0.000 description 2
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 description 2
• 150000002440 hydroxy compounds Chemical class 0.000 description 2
• 125000004356 hydroxy functional group Chemical group O* 0.000 description 2
• 150000004712 monophosphates Chemical group 0.000 description 2
• 150000004671 saturated fatty acids Chemical class 0.000 description 2
• 125000001113 thiadiazolyl group Chemical group 0.000 description 2
• 125000003258 trimethylene group Chemical group [H]C([H])([*:2])C([H])([H])C([H])([H])[*:1] 0.000 description 2
• 235000021122 unsaturated fatty acids Nutrition 0.000 description 2
• 150000004670 unsaturated fatty acids Chemical class 0.000 description 2
• 230000016571 aggressive behavior Effects 0.000 description 1
• 238000013019 agitation Methods 0.000 description 1
• 229920001577 copolymer Polymers 0.000 description 1
• 230000002708 enhancing effect Effects 0.000 description 1
• 239000006186 oral dosage form Substances 0.000 description 1
• 239000000546 pharmaceutical excipient Substances 0.000 description 1
• 230000002265 prevention Effects 0.000 description 1
• 239000000243 solution Substances 0.000 description 1
• 239000000725 suspension Substances 0.000 description 1
• 239000003826 tablet Substances 0.000 description 1