BR112019022902A2 - composição, composição farmacêutica, uso da composição terapeuticamente eficaz, método e uso de uma composição terapeuticamente eficaz em um método de tratamento - Google Patents

Info

Publication number

BR112019022902A2

BR112019022902A2 BR112019022902A BR112019022902A BR112019022902A2 BR 112019022902 A2 BR112019022902 A2 BR 112019022902A2 BR 112019022902 A BR112019022902 A BR 112019022902A BR 112019022902 A BR112019022902 A BR 112019022902A BR 112019022902 A2 BR112019022902 A2 BR 112019022902A2

Authority

BR

Brazil

Prior art keywords

phenoxy

methyl

oxy

propan

dimethylamino

Prior art date

2017-05-04

Links

• Espacenet
• Global Dossier
• Discuss

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• 238000000034 method Methods 0.000 title claims abstract description 96
• 239000008194 pharmaceutical composition Substances 0.000 title claims abstract description 15
• 238000011282 treatment Methods 0.000 title claims description 106
• 150000001875 compounds Chemical class 0.000 claims abstract description 413
• 150000003839 salts Chemical class 0.000 claims abstract description 73
• 239000002253 acid Substances 0.000 claims abstract description 60
• 229940002612 prodrug Drugs 0.000 claims abstract description 52
• 239000000651 prodrug Substances 0.000 claims abstract description 52
• 239000002207 metabolite Substances 0.000 claims abstract description 31
• 239000003795 chemical substances by application Substances 0.000 claims abstract description 26
• HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims abstract description 21
• 108010001237 Cytochrome P-450 CYP2D6 Proteins 0.000 claims abstract description 19
• -1 acyl radical Chemical class 0.000 claims description 533
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• 208000024891 symptom Diseases 0.000 claims description 97
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 82
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 81
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• BUGYDGFZZOZRHP-UHFFFAOYSA-N memantine Chemical compound C1C(C2)CC3(C)CC1(C)CC2(N)C3 BUGYDGFZZOZRHP-UHFFFAOYSA-N 0.000 claims description 47
• LOUPRKONTZGTKE-LHHVKLHASA-N quinidine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@H]2[C@@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-LHHVKLHASA-N 0.000 claims description 42
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• 239000002400 serotonin 2A antagonist Substances 0.000 claims description 39
• 229910052739 hydrogen Inorganic materials 0.000 claims description 38
• ITPDYQOUSLNIHG-UHFFFAOYSA-N Amiodarone hydrochloride Chemical compound [Cl-].CCCCC=1OC2=CC=CC=C2C=1C(=O)C1=CC(I)=C(OCC[NH+](CC)CC)C(I)=C1 ITPDYQOUSLNIHG-UHFFFAOYSA-N 0.000 claims description 37
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• 125000000623 heterocyclic group Chemical group 0.000 claims description 23
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• 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 17
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• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 13
• YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 claims description 12
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• 230000002441 reversible effect Effects 0.000 claims description 12
• KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 12
• 239000000556 agonist Substances 0.000 claims description 11
• 125000005842 heteroatom Chemical group 0.000 claims description 11
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• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
• XNGIFLGASWRNHJ-UHFFFAOYSA-L phthalate(2-) Chemical compound [O-]C(=O)C1=CC=CC=C1C([O-])=O XNGIFLGASWRNHJ-UHFFFAOYSA-L 0.000 claims description 11
• 229960001860 salicylate Drugs 0.000 claims description 11
• QIVBCDIJIAJPQS-UHFFFAOYSA-M tryptophanate Chemical compound C1=CC=C2C(CC(N)C([O-])=O)=CNC2=C1 QIVBCDIJIAJPQS-UHFFFAOYSA-M 0.000 claims description 11
• 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 10
• RGHNJXZEOKUKBD-MGCNEYSASA-N D-galactonic acid Chemical compound OC[C@@H](O)[C@H](O)[C@H](O)[C@@H](O)C(O)=O RGHNJXZEOKUKBD-MGCNEYSASA-N 0.000 claims description 10
• FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims description 10
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• USSIQXCVUWKGNF-UHFFFAOYSA-N 6-(dimethylamino)-4,4-diphenylheptan-3-one Chemical compound C=1C=CC=CC=1C(CC(C)N(C)C)(C(=O)CC)C1=CC=CC=C1 USSIQXCVUWKGNF-UHFFFAOYSA-N 0.000 claims description 9
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• 150000001602 bicycloalkyls Chemical group 0.000 claims description 8
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