JP2021505568A5 - - Google Patents

Info

Publication number

JP2021505568A5

JP2021505568A5 JP2020530502A JP2020530502A JP2021505568A5 JP 2021505568 A5 JP2021505568 A5 JP 2021505568A5 JP 2020530502 A JP2020530502 A JP 2020530502A JP 2020530502 A JP2020530502 A JP 2020530502A JP 2021505568 A5 JP2021505568 A5 JP 2021505568A5

Authority

JP

Japan

Prior art keywords

methyl

hydrogen

membered

optionally

substituted

Prior art date

2018-11-30

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.)

Granted

Links

• Espacenet
• Global Dossier
• Discuss

• -1 C 1 -C 3 alkoxy Chemical group 0.000 claims 95
• 229910052739 hydrogen Inorganic materials 0.000 claims 42
• 239000001257 hydrogen Substances 0.000 claims 42
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 33
• 150000001875 compounds Chemical class 0.000 claims 29
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 23
• 125000001424 substituent group Chemical group 0.000 claims 20
• 150000002431 hydrogen Chemical class 0.000 claims 19
• 125000001153 fluoro group Chemical group F* 0.000 claims 17
• 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 14
• 125000000623 heterocyclic group Chemical group 0.000 claims 11
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
• 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 8
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 8
• 125000005843 halogen group Chemical group 0.000 claims 8
• 125000004043 oxo group Chemical group O=* 0.000 claims 8
• 150000003839 salts Chemical class 0.000 claims 7
• 239000012453 solvate Substances 0.000 claims 7
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 6
• 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 6
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
• 125000004432 carbon atom Chemical group C* 0.000 claims 5
• FXHOOIRPVKKKFG-UHFFFAOYSA-N N,N-Dimethylacetamide Chemical compound CN(C)C(C)=O FXHOOIRPVKKKFG-UHFFFAOYSA-N 0.000 claims 4
• 125000001309 chloro group Chemical group Cl* 0.000 claims 4
• 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims 4
• 125000004076 pyridyl group Chemical group 0.000 claims 4
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 4
• 125000004214 1-pyrrolidinyl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 3
• 229910052799 carbon Inorganic materials 0.000 claims 3
• 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims 3
• 125000004093 cyano group Chemical group *C#N 0.000 claims 3
• 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 3
• 125000000719 pyrrolidinyl group Chemical group 0.000 claims 3
• 125000004568 thiomorpholinyl group Chemical group 0.000 claims 3
• 125000004206 2,2,2-trifluoroethyl group Chemical group [H]C([H])(*)C(F)(F)F 0.000 claims 2
• 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
• 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 2
• 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 2
• DLFVBJFMPXGRIB-UHFFFAOYSA-N Acetamide Chemical compound CC(N)=O DLFVBJFMPXGRIB-UHFFFAOYSA-N 0.000 claims 2
• XZMCDFZZKTWFGF-UHFFFAOYSA-N Cyanamide Chemical compound NC#N XZMCDFZZKTWFGF-UHFFFAOYSA-N 0.000 claims 2
• 108010015720 Dopamine beta-Hydroxylase Proteins 0.000 claims 2
• 102100033156 Dopamine beta-hydroxylase Human genes 0.000 claims 2
• 125000003545 alkoxy group Chemical group 0.000 claims 2
• 230000001668 ameliorated effect Effects 0.000 claims 2
• 150000001408 amides Chemical class 0.000 claims 2
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
• 125000001246 bromo group Chemical group Br* 0.000 claims 2
• 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• 210000003169 central nervous system Anatomy 0.000 claims 2
• 125000000753 cycloalkyl group Chemical group 0.000 claims 2
• 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
• 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 2
• 125000004186 cyclopropylmethyl group Chemical group [H]C([H])(*)C1([H])C([H])([H])C1([H])[H] 0.000 claims 2
• 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 2
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
• 125000002541 furyl group Chemical group 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
• 230000005764 inhibitory process Effects 0.000 claims 2
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
• 125000002757 morpholinyl group Chemical group 0.000 claims 2
• 125000003386 piperidinyl group Chemical group 0.000 claims 2
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
• 125000001544 thienyl group Chemical group 0.000 claims 2
• GSJJVNAPLSISFR-CQSZACIVSA-N (6S)-1-benzyl-6-(3,5-difluorophenyl)-2,5,6,7-tetrahydropyrrolo[1,2-c]imidazole-3-thione Chemical compound C(C1=CC=CC=C1)C1=C2N(C(N1)=S)C[C@@H](C2)C1=CC(=CC(=C1)F)F GSJJVNAPLSISFR-CQSZACIVSA-N 0.000 claims 1
• 125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims 1
• 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 1
• 239000000654 additive Substances 0.000 claims 1
• 230000000996 additive effect Effects 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 125000003754 ethoxycarbonyl group Chemical group C(=O)(OCC)* 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 125000005322 morpholin-1-yl group Chemical group 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 125000004193 piperazinyl group Chemical group 0.000 claims 1
• 238000007493 shaping process Methods 0.000 claims 1
• 230000001225 therapeutic effect Effects 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• 125000000437 thiazol-2-yl group Chemical group [H]C1=C([H])N=C(*)S1 0.000 claims 1