JP2008115166A5 - - Google Patents

Info

Publication number

JP2008115166A5

JP2008115166A5 JP2007262868A JP2007262868A JP2008115166A5 JP 2008115166 A5 JP2008115166 A5 JP 2008115166A5 JP 2007262868 A JP2007262868 A JP 2007262868A JP 2007262868 A JP2007262868 A JP 2007262868A JP 2008115166 A5 JP2008115166 A5 JP 2008115166A5

Authority

JP

Japan

Prior art keywords

group

methyl

salt

active ingredient

solvate

Prior art date

2007-10-09

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

• Espacenet
• Global Dossier
• Discuss

• -1 2, 5- difluorophenyl group Chemical group 0.000 claims 74
• 150000003839 salts Chemical class 0.000 claims 37
• 239000011780 sodium chloride Substances 0.000 claims 37
• 239000012453 solvate Substances 0.000 claims 37
• 239000004480 active ingredient Substances 0.000 claims 36
• 125000001424 substituent group Chemical group 0.000 claims 24
• 150000001875 compounds Chemical class 0.000 claims 21
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 21
• 239000003814 drug Substances 0.000 claims 12
• 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 11
• 125000000623 heterocyclic group Chemical group 0.000 claims 9
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
• 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 7
• 125000000217 alkyl group Chemical group 0.000 claims 7
• 125000004430 oxygen atoms Chemical group O* 0.000 claims 7
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 7
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 7
• 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 5
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
• 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 3
• 125000003277 amino group Chemical group 0.000 claims 3
• 229910052757 nitrogen Inorganic materials 0.000 claims 3
• 125000004433 nitrogen atoms Chemical group N* 0.000 claims 3
• 125000000954 2-hydroxyethyl group Chemical group [H]C([*])([H])C([H])([H])O[H] 0.000 claims 2
• 102000013455 Amyloid beta-Peptides Human genes 0.000 claims 2
• 108010090849 Amyloid beta-Peptides Proteins 0.000 claims 2
• 230000002159 abnormal effect Effects 0.000 claims 2
• 125000002252 acyl group Chemical group 0.000 claims 2
• 125000003545 alkoxy group Chemical group 0.000 claims 2
• 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 2
• 150000003857 carboxamides Chemical class 0.000 claims 2
• 125000006222 dimethylaminomethyl group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])* 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 229940079593 drugs Drugs 0.000 claims 2
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 2
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
• 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 2
• 125000001476 phosphono group Chemical group [H]OP(*)(=O)O[H] 0.000 claims 2
• 230000028327 secretion Effects 0.000 claims 2
• FFDGPVCHZBVARC-UHFFFAOYSA-M 2-(dimethylamino)acetate Chemical compound CN(C)CC([O-])=O FFDGPVCHZBVARC-UHFFFAOYSA-M 0.000 claims 1
• 125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 claims 1
• 125000001340 2-chloroethyl group Chemical group [H]C([H])(Cl)C([H])([H])* 0.000 claims 1
• 125000004211 3,5-difluorophenyl group Chemical group [H]C1=C(F)C([H])=C(*)C([H])=C1F 0.000 claims 1
• 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
• 125000000590 4-methylphenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
• PUJYWJMTQHYWQY-UHFFFAOYSA-N 5-[(2,5-difluorophenyl)-(4-fluorophenyl)sulfinylmethyl]-N,N,4-trimethylpyridine-2-carboxamide Chemical compound C1=NC(C(=O)N(C)C)=CC(C)=C1C(S(=O)C=1C=CC(F)=CC=1)C1=CC(F)=CC=C1F PUJYWJMTQHYWQY-UHFFFAOYSA-N 0.000 claims 1
• QYTZOANRZCUFRE-UHFFFAOYSA-N 5-[(2,5-difluorophenyl)-(4-fluorophenyl)sulfonylmethyl]-N-(hydroxymethyl)-4-methylpyridine-2-carboxamide Chemical compound CC1=CC(C(=O)NCO)=NC=C1C(S(=O)(=O)C=1C=CC(F)=CC=1)C1=CC(F)=CC=C1F QYTZOANRZCUFRE-UHFFFAOYSA-N 0.000 claims 1
• HIQHKJUWHPLGPM-UHFFFAOYSA-N 5-[(4-fluorophenyl)sulfonyl-(2,3,6-trifluorophenyl)methyl]-N-(hydroxymethyl)-4-methylpyridine-2-carboxamide Chemical compound CC1=CC(C(=O)NCO)=NC=C1C(S(=O)(=O)C=1C=CC(F)=CC=1)C1=C(F)C=CC(F)=C1F HIQHKJUWHPLGPM-UHFFFAOYSA-N 0.000 claims 1
• WMCPAYAILCFLSN-UHFFFAOYSA-N 5-[benzenesulfonyl-(2,3,6-trifluorophenyl)methyl]-N-(hydroxymethyl)-4-methylpyridine-2-carboxamide Chemical compound CC1=CC(C(=O)NCO)=NC=C1C(S(=O)(=O)C=1C=CC=CC=1)C1=C(F)C=CC(F)=C1F WMCPAYAILCFLSN-UHFFFAOYSA-N 0.000 claims 1
• 206010001897 Alzheimer's disease Diseases 0.000 claims 1
• OVAHWBMWJHSLJB-UHFFFAOYSA-N C(C)(=O)OOCC1=CC=C(C=C1)OC Chemical compound C(C)(=O)OOCC1=CC=C(C=C1)OC OVAHWBMWJHSLJB-UHFFFAOYSA-N 0.000 claims 1
• 201000010374 Down syndrome Diseases 0.000 claims 1
• VMWJCFLUSKZZDX-UHFFFAOYSA-N N,N-dimethylmethanamine Chemical group [CH2]N(C)C VMWJCFLUSKZZDX-UHFFFAOYSA-N 0.000 claims 1
• 206010044688 Trisomy 21 Diseases 0.000 claims 1
• 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
• 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 1
• 125000004429 atoms Chemical group 0.000 claims 1
• 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
• 125000002147 dimethylamino group Chemical group [H]C([H])([H])N(*)C([H])([H])[H] 0.000 claims 1
• AEMRFAOFKBGASW-UHFFFAOYSA-M glycolate Chemical compound OCC([O-])=O AEMRFAOFKBGASW-UHFFFAOYSA-M 0.000 claims 1
• 125000005843 halogen group Chemical group 0.000 claims 1
• 239000004615 ingredient Substances 0.000 claims 1
• GSJFXBNYJCXDGI-UHFFFAOYSA-N methyl 2-hydroxyacetate Chemical compound COC(=O)CO GSJFXBNYJCXDGI-UHFFFAOYSA-N 0.000 claims 1
• 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
• 125000004373 methylthiopropyl group Chemical group [H]C([H])([H])SC([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
• 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 1
• 229910052760 oxygen Inorganic materials 0.000 claims 1
• 239000001301 oxygen Substances 0.000 claims 1
• MYMOFIZGZYHOMD-UHFFFAOYSA-N oxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
• 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
• IBBMAWULFFBRKK-UHFFFAOYSA-N picolinamide Chemical compound NC(=O)C1=CC=CC=N1 IBBMAWULFFBRKK-UHFFFAOYSA-N 0.000 claims 1
• 229910052717 sulfur Inorganic materials 0.000 claims 1
• 125000004434 sulfur atoms Chemical group 0.000 claims 1
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
• 125000003944 tolyl group Chemical group 0.000 claims 1