JP2022040131A5 - - Google Patents

Info

Publication number

JP2022040131A5

JP2022040131A5 JP2021202636A JP2021202636A JP2022040131A5 JP 2022040131 A5 JP2022040131 A5 JP 2022040131A5 JP 2021202636 A JP2021202636 A JP 2021202636A JP 2021202636 A JP2021202636 A JP 2021202636A JP 2022040131 A5 JP2022040131 A5 JP 2022040131A5

Authority

JP

Japan

Prior art keywords

formula

cpp

alkyl

compound

ceremony

Prior art date

2021-12-14

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.)

Withdrawn

Links

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• 150000001875 compounds Chemical class 0.000 claims 31
• 125000000217 alkyl group Chemical group 0.000 claims 24
• ISAKRJDGNUQOIC-UHFFFAOYSA-N Uracil Chemical compound O=C1C=CNC(=O)N1 ISAKRJDGNUQOIC-UHFFFAOYSA-N 0.000 claims 16
• RWQNBRDOKXIBIV-UHFFFAOYSA-N thymine Chemical compound CC1=CNC(=O)NC1=O RWQNBRDOKXIBIV-UHFFFAOYSA-N 0.000 claims 16
• 150000003839 salts Chemical class 0.000 claims 14
• 125000002252 acyl group Chemical group 0.000 claims 9
• -1 4-Methoxytrityl Chemical group 0.000 claims 8
• 108010078777 Colistin Proteins 0.000 claims 8
• 125000005647 linker group Chemical group 0.000 claims 8
• JORAUNFTUVJTNG-BSTBCYLQSA-N n-[(2s)-4-amino-1-[[(2s,3r)-1-[[(2s)-4-amino-1-oxo-1-[[(3s,6s,9s,12s,15r,18s,21s)-6,9,18-tris(2-aminoethyl)-3-[(1r)-1-hydroxyethyl]-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-h Polymers CC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@H]([C@@H](C)O)CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O.CCC(C)CCCCC(=O)N[C@@H](CCN)C(=O)N[C@H]([C@@H](C)O)CN[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O JORAUNFTUVJTNG-BSTBCYLQSA-N 0.000 claims 8
• XDJYMJULXQKGMM-UHFFFAOYSA-N polymyxin E1 Natural products CCC(C)CCCCC(=O)NC(CCN)C(=O)NC(C(C)O)C(=O)NC(CCN)C(=O)NC1CCNC(=O)C(C(C)O)NC(=O)C(CCN)NC(=O)C(CCN)NC(=O)C(CC(C)C)NC(=O)C(CC(C)C)NC(=O)C(CCN)NC1=O XDJYMJULXQKGMM-UHFFFAOYSA-N 0.000 claims 8
• 229940113082 thymine Drugs 0.000 claims 8
• 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims 8
• 229940035893 uracil Drugs 0.000 claims 8
• PYHYGIPVYYRJHU-LPGHPFMSSA-N (2s,3r)-2-amino-n-[(2s)-4-amino-1-oxo-1-[[(3s,6s,9s,12s,15s,18s,21s)-6,9,18-tris(2-aminoethyl)-15-benzyl-3-[(1r)-1-hydroxyethyl]-12-(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]-3-hydroxybutanamid Polymers N1C(=O)[C@H](CCN)NC(=O)[C@@H](NC(=O)[C@H](CCN)NC(=O)[C@@H](N)[C@@H](C)O)CCNC(=O)[C@H]([C@@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H]1CC1=CC=CC=C1 PYHYGIPVYYRJHU-LPGHPFMSSA-N 0.000 claims 6
• 239000000203 mixture Substances 0.000 claims 6
• 239000008194 pharmaceutical composition Substances 0.000 claims 6
• 108700026839 polymyxin B nonapeptide Proteins 0.000 claims 6
• 230000008685 targeting Effects 0.000 claims 5
• 125000004485 2-pyrrolidinyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])C1([H])* 0.000 claims 4
• 108010093965 Polymyxin B Proteins 0.000 claims 4
• 210000000170 cell membrane Anatomy 0.000 claims 4
• YKQOSKADJPQZHB-YNWHQGOSSA-N n-[(2s)-4-amino-1-[[(2s,3r)-1-[[(2s)-4-amino-1-oxo-1-[[(3s,6s,9s,12s,15r,18s,21s)-6,9,18-tris(2-aminoethyl)-3-[(1s)-1-hydroxyethyl]-12,15-bis(2-methylpropyl)-2,5,8,11,14,17,20-heptaoxo-1,4,7,10,13,16,19-heptazacyclotricos-21-yl]amino]butan-2-yl]amino]-3-h Polymers CCC(C)CCCC(=O)N[C@@H](CCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCN)C(=O)N[C@H]1CCNC(=O)[C@H]([C@H](C)O)NC(=O)[C@H](CCN)NC(=O)[C@H](CCN)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](CCN)NC1=O YKQOSKADJPQZHB-YNWHQGOSSA-N 0.000 claims 4
• 230000000149 penetrating effect Effects 0.000 claims 4
• 229920000024 polymyxin B Polymers 0.000 claims 4
• 229960005266 polymyxin b Drugs 0.000 claims 4
• 108090000765 processed proteins & peptides Proteins 0.000 claims 4
• 229910052760 oxygen Inorganic materials 0.000 claims 3
• 239000001301 oxygen Substances 0.000 claims 3
• 208000032536 Pseudomonas Infections Diseases 0.000 claims 2
• UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical group NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 2
• 239000003937 drug carrier Substances 0.000 claims 2
• 230000002265 prevention Effects 0.000 claims 2
• SLXKOJJOQWFEFD-UHFFFAOYSA-N 6-aminohexanoic acid Chemical group NCCCCCC(O)=O SLXKOJJOQWFEFD-UHFFFAOYSA-N 0.000 claims 1
• 229960002684 aminocaproic acid Drugs 0.000 claims 1
• 239000003242 anti bacterial agent Substances 0.000 claims 1
• 229940088710 antibiotic agent Drugs 0.000 claims 1
• 230000001580 bacterial effect Effects 0.000 claims 1
• 229940000635 beta-alanine Drugs 0.000 claims 1
• 230000003115 biocidal effect Effects 0.000 claims 1