JP2005504734A5 - - Google Patents

Info

Publication number

JP2005504734A5

JP2005504734A5 JP2003508926A JP2003508926A JP2005504734A5 JP 2005504734 A5 JP2005504734 A5 JP 2005504734A5 JP 2003508926 A JP2003508926 A JP 2003508926A JP 2003508926 A JP2003508926 A JP 2003508926A JP 2005504734 A5 JP2005504734 A5 JP 2005504734A5

Authority

JP

Japan

Prior art keywords

compound

diaza

hydrogen atom

alkyl

methoxycarbonyl

Prior art date

2002-06-28

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.)

Granted

Links

• Espacenet
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• 150000001875 compounds Chemical class 0.000 claims 24
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 21
• VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 14
• 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 11
• PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 11
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 11
• 125000001424 substituent group Chemical group 0.000 claims 11
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
• 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 6
• 125000003974 3-carbamimidamidopropyl group Chemical group C(N)(=N)NCCC* 0.000 claims 6
• 125000004042 4-aminobutyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])N([H])[H] 0.000 claims 5
• UJOBWOGCFQCDNV-UHFFFAOYSA-N 9H-carbazole Chemical compound C1=CC=C2C3=CC=CC=C3NC2=C1 UJOBWOGCFQCDNV-UHFFFAOYSA-N 0.000 claims 4
• 208000035143 Bacterial infection Diseases 0.000 claims 4
• 208000022362 bacterial infectious disease Diseases 0.000 claims 4
• NIHNNTQXNPWCJQ-UHFFFAOYSA-N fluorene Chemical compound C1=CC=C2CC3=CC=CC=C3C2=C1 NIHNNTQXNPWCJQ-UHFFFAOYSA-N 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• -1 4-{[(t-butoxy) carbonyl] amino} butyl Chemical group 0.000 claims 3
• 125000003277 amino group Chemical group 0.000 claims 3
• 125000001072 heteroaryl group Chemical group 0.000 claims 3
• 125000006619 (C1-C6) dialkylamino group Chemical group 0.000 claims 2
• 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
• 125000000041 C6-C10 aryl group Chemical group 0.000 claims 2
• SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 2
• 241000124008 Mammalia Species 0.000 claims 2
• ZTVJJAASXFPCHR-UHFFFAOYSA-N O=S(=O)N=S(=O)=O Chemical compound O=S(=O)N=S(=O)=O ZTVJJAASXFPCHR-UHFFFAOYSA-N 0.000 claims 2
• SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims 2
• 125000004390 alkyl sulfonyl group Chemical group 0.000 claims 2
• 125000003710 aryl alkyl group Chemical group 0.000 claims 2
• 125000004391 aryl sulfonyl group Chemical group 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
• 229910052799 carbon Inorganic materials 0.000 claims 2
• 125000004432 carbon atom Chemical group C* 0.000 claims 2
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
• ZUOUZKKEUPVFJK-UHFFFAOYSA-N diphenyl Chemical compound C1=CC=CC=C1C1=CC=CC=C1 ZUOUZKKEUPVFJK-UHFFFAOYSA-N 0.000 claims 2
• 125000001475 halogen functional group Chemical group 0.000 claims 2
• AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims 2
• YCWSUKQGVSGXJO-NTUHNPAUSA-N nifuroxazide Chemical group C1=CC(O)=CC=C1C(=O)N\N=C\C1=CC=C([N+]([O-])=O)O1 YCWSUKQGVSGXJO-NTUHNPAUSA-N 0.000 claims 2
• 150000002825 nitriles Chemical class 0.000 claims 2
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 2
• YNPNZTXNASCQKK-UHFFFAOYSA-N phenanthrene Chemical compound C1=CC=C2C3=CC=CC=C3C=CC2=C1 YNPNZTXNASCQKK-UHFFFAOYSA-N 0.000 claims 2
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
• QUOGESRFPZDMMT-RXMQYKEDSA-N (2r)-2-amino-6-(diaminomethylideneamino)hexanoic acid Chemical group OC(=O)[C@H](N)CCCCNC(N)=N QUOGESRFPZDMMT-RXMQYKEDSA-N 0.000 claims 1
• 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
• HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 1
• BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims 1
• LCGTWRLJTMHIQZ-UHFFFAOYSA-N 5H-dibenzo[b,f]azepine Chemical compound C1=CC2=CC=CC=C2NC2=CC=CC=C21 LCGTWRLJTMHIQZ-UHFFFAOYSA-N 0.000 claims 1
• 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 1
• 125000002038 D-arginyl group Chemical group N[C@@H](C(=O)*)CCCNC(=N)N 0.000 claims 1
• KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine group Chemical group N[C@H](CCCCN)C(=O)O KDXKERNSBIXSRK-RXMQYKEDSA-N 0.000 claims 1
• 241000192125 Firmicutes Species 0.000 claims 1
• 125000003412 L-alanyl group Chemical group [H]N([H])[C@@](C([H])([H])[H])(C(=O)[*])[H] 0.000 claims 1
• 241000191967 Staphylococcus aureus Species 0.000 claims 1
• 108010059993 Vancomycin Proteins 0.000 claims 1
• 239000002671 adjuvant Substances 0.000 claims 1
• 125000003282 alkyl amino group Chemical group 0.000 claims 1
• 125000003275 alpha amino acid group Chemical group 0.000 claims 1
• 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 1
• 235000008206 alpha-amino acids Nutrition 0.000 claims 1
• 125000000539 amino acid group Chemical group 0.000 claims 1
• 125000003118 aryl group Chemical group 0.000 claims 1
• 230000001580 bacterial effect Effects 0.000 claims 1
• 150000001576 beta-amino acids Chemical group 0.000 claims 1
• ZDZHCHYQNPQSGG-UHFFFAOYSA-N binaphthyl group Chemical group C1(=CC=CC2=CC=CC=C12)C1=CC=CC2=CC=CC=C12 ZDZHCHYQNPQSGG-UHFFFAOYSA-N 0.000 claims 1
• 235000010290 biphenyl Nutrition 0.000 claims 1
• 239000004305 biphenyl Substances 0.000 claims 1
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
• 125000000753 cycloalkyl group Chemical group 0.000 claims 1
• 150000002016 disaccharides Chemical group 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 125000002795 guanidino group Chemical group C(N)(=N)N* 0.000 claims 1
• 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 1
• PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 1
• RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 150000002772 monosaccharides Chemical group 0.000 claims 1
• MYPYJXKWCTUITO-LYRMYLQWSA-N vancomycin Chemical compound O([C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@H]1OC1=C2C=C3C=C1OC1=CC=C(C=C1Cl)[C@@H](O)[C@H](C(N[C@@H](CC(N)=O)C(=O)N[C@H]3C(=O)N[C@H]1C(=O)N[C@H](C(N[C@@H](C3=CC(O)=CC(O)=C3C=3C(O)=CC=C1C=3)C(O)=O)=O)[C@H](O)C1=CC=C(C(=C1)Cl)O2)=O)NC(=O)[C@@H](CC(C)C)NC)[C@H]1C[C@](C)(N)[C@H](O)[C@H](C)O1 MYPYJXKWCTUITO-LYRMYLQWSA-N 0.000 claims 1
• 229960003165 vancomycin Drugs 0.000 claims 1
• MYPYJXKWCTUITO-UHFFFAOYSA-N vancomycin Natural products O1C(C(=C2)Cl)=CC=C2C(O)C(C(NC(C2=CC(O)=CC(O)=C2C=2C(O)=CC=C3C=2)C(O)=O)=O)NC(=O)C3NC(=O)C2NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(CC(C)C)NC)C(O)C(C=C3Cl)=CC=C3OC3=CC2=CC1=C3OC1OC(CO)C(O)C(O)C1OC1CC(C)(N)C(O)C(C)O1 MYPYJXKWCTUITO-UHFFFAOYSA-N 0.000 claims 1