JP2017518304A5 - - Google Patents

Info

Publication number

JP2017518304A5

JP2017518304A5 JP2016570835A JP2016570835A JP2017518304A5 JP 2017518304 A5 JP2017518304 A5 JP 2017518304A5 JP 2016570835 A JP2016570835 A JP 2016570835A JP 2016570835 A JP2016570835 A JP 2016570835A JP 2017518304 A5 JP2017518304 A5 JP 2017518304A5

Authority

JP

Japan

Prior art keywords

compound

conjugate

antibody

formula

antigen

Prior art date

2015-06-01

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
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• 150000001875 compounds Chemical class 0.000 claims 37
• 239000000562 conjugate Substances 0.000 claims 26
• 239000000427 antigen Substances 0.000 claims 12
• 102000036639 antigens Human genes 0.000 claims 12
• 108091007433 antigens Proteins 0.000 claims 12
• 239000012634 fragment Substances 0.000 claims 12
• 235000018417 cysteine Nutrition 0.000 claims 8
• XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 8
• 229910052717 sulfur Inorganic materials 0.000 claims 8
• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 7
• 108010044540 auristatin Proteins 0.000 claims 6
• 125000000217 alkyl group Chemical group 0.000 claims 4
• 235000001014 amino acid Nutrition 0.000 claims 4
• 150000001413 amino acids Chemical class 0.000 claims 4
• 239000008194 pharmaceutical composition Substances 0.000 claims 4
• 108090000765 processed proteins & peptides Proteins 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• MFRNYXJJRJQHNW-DEMKXPNLSA-N (2s)-2-[[(2r,3r)-3-methoxy-3-[(2s)-1-[(3r,4s,5s)-3-methoxy-5-methyl-4-[methyl-[(2s)-3-methyl-2-[[(2s)-3-methyl-2-(methylamino)butanoyl]amino]butanoyl]amino]heptanoyl]pyrrolidin-2-yl]-2-methylpropanoyl]amino]-3-phenylpropanoic acid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C(O)=O)CC1=CC=CC=C1 MFRNYXJJRJQHNW-DEMKXPNLSA-N 0.000 claims 2
• BLUGYPPOFIHFJS-UUFHNPECSA-N (2s)-n-[(2s)-1-[[(3r,4s,5s)-3-methoxy-1-[(2s)-2-[(1r,2r)-1-methoxy-2-methyl-3-oxo-3-[[(1s)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]-3-methyl-2-(methylamino)butanamid Chemical compound CN[C@@H](C(C)C)C(=O)N[C@@H](C(C)C)C(=O)N(C)[C@@H]([C@@H](C)CC)[C@H](OC)CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C=1SC=CN=1)CC1=CC=CC=C1 BLUGYPPOFIHFJS-UUFHNPECSA-N 0.000 claims 2
• 208000007934 ACTH-independent macronodular adrenal hyperplasia Diseases 0.000 claims 2
• IEDXPSOJFSVCKU-HOKPPMCLSA-N [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[6-(2,5-dioxopyrrolidin-1-yl)hexanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-1-[(2S)-2-[(1R,2R)-3-[[(1S,2R)-1-hydroxy-1-phenylpropan-2-yl]amino]-1-methoxy-2-methyl-3-oxopropyl]pyrrolidin-1-yl]-3-methoxy-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate Chemical compound CC[C@H](C)[C@@H]([C@@H](CC(=O)N1CCC[C@H]1[C@H](OC)[C@@H](C)C(=O)N[C@H](C)[C@@H](O)c1ccccc1)OC)N(C)C(=O)[C@@H](NC(=O)[C@H](C(C)C)N(C)C(=O)OCc1ccc(NC(=O)[C@H](CCCNC(N)=O)NC(=O)[C@@H](NC(=O)CCCCCN2C(=O)CCC2=O)C(C)C)cc1)C(C)C IEDXPSOJFSVCKU-HOKPPMCLSA-N 0.000 claims 2
• 230000000975 bioactive effect Effects 0.000 claims 2
• 210000004027 cell Anatomy 0.000 claims 2
• 125000006850 spacer group Chemical group 0.000 claims 2
• 206010028980 Neoplasm Diseases 0.000 claims 1
• 230000002159 abnormal effect Effects 0.000 claims 1
• 239000000611 antibody drug conjugate Substances 0.000 claims 1
• 229940049595 antibody-drug conjugate Drugs 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• 230000010261 cell growth Effects 0.000 claims 1
• 150000004820 halides Chemical class 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 210000004881 tumor cell Anatomy 0.000 claims 1
• 0 CCC(C*(C)(C)C*C)C(NC)=O Chemical compound CCC(C*(C)(C)C*C)C(NC)=O 0.000 description 1