JP2020530007A5 - - Google Patents

Info

Publication number

JP2020530007A5

JP2020530007A5 JP2020506300A JP2020506300A JP2020530007A5 JP 2020530007 A5 JP2020530007 A5 JP 2020530007A5 JP 2020506300 A JP2020506300 A JP 2020506300A JP 2020506300 A JP2020506300 A JP 2020506300A JP 2020530007 A5 JP2020530007 A5 JP 2020530007A5

Authority

JP

Japan

Prior art keywords

psma

alkyl

drug composition

group

independently

Prior art date

2018-04-11

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

• 239000003814 drug Substances 0.000 claims 18
• 229940079593 drug Drugs 0.000 claims 12
• 239000000203 mixture Substances 0.000 claims 12
• 125000000217 alkyl group Chemical group 0.000 claims 10
• ISEYJGQFXSTPMQ-UHFFFAOYSA-N 2-(phosphonomethyl)pentanedioic acid Chemical compound OC(=O)CCC(C(O)=O)CP(O)(O)=O ISEYJGQFXSTPMQ-UHFFFAOYSA-N 0.000 claims 9
• 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 8
• 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 8
• 229940002612 prodrug Drugs 0.000 claims 7
• 239000000651 prodrug Substances 0.000 claims 7
• 239000008194 pharmaceutical composition Substances 0.000 claims 6
• 238000003384 imaging method Methods 0.000 claims 5
• 229940124597 therapeutic agent Drugs 0.000 claims 5
• 125000001072 heteroaryl group Chemical group 0.000 claims 4
• 239000012216 imaging agent Substances 0.000 claims 4
• 206010028980 Neoplasm Diseases 0.000 claims 3
• 201000011510 cancer Diseases 0.000 claims 3
• 150000001875 compounds Chemical class 0.000 claims 3
• 210000003079 salivary gland Anatomy 0.000 claims 3
• 210000001519 tissue Anatomy 0.000 claims 3
• 125000002877 alkyl aryl group Chemical group 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 239000003795 chemical substances by application Substances 0.000 claims 2
• 210000003734 kidney Anatomy 0.000 claims 2
• 210000004561 lacrimal apparatus Anatomy 0.000 claims 2
• 210000003296 saliva Anatomy 0.000 claims 2
• 150000003839 salts Chemical class 0.000 claims 2
• 125000003107 substituted aryl group Chemical group 0.000 claims 2
• LFEGKCKGGNXWDV-LUOJOMRDSA-N (2S)-2-[[(1S)-1-carboxy-5-[(4-(131I)iodanylphenyl)carbamoylamino]pentyl]carbamoylamino]pentanedioic acid Chemical compound C(=O)(O)[C@H](CCCCNC(=O)NC1=CC=C(C=C1)[131I])NC(N[C@H](C(=O)O)CCC(=O)O)=O LFEGKCKGGNXWDV-LUOJOMRDSA-N 0.000 claims 1
• OLWVRJUNLXQDSP-MVBOSPHXSA-N (2s)-2-[[(1s)-1-carboxy-5-[(6-fluoranylpyridine-3-carbonyl)amino]pentyl]carbamoylamino]pentanedioic acid Chemical compound OC(=O)CC[C@@H](C(O)=O)NC(=O)N[C@H](C(O)=O)CCCCNC(=O)C1=CC=C([18F])N=C1 OLWVRJUNLXQDSP-MVBOSPHXSA-N 0.000 claims 1
• QJUIUFGOTBRHKP-LQJZCPKCSA-N (2s)-2-[[(1s)-1-carboxy-5-[6-[3-[3-[[2-[[5-(2-carboxyethyl)-2-hydroxyphenyl]methyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]methyl]-4-hydroxyphenyl]propanoylamino]hexanoylamino]pentyl]carbamoylamino]pentanedioic acid Chemical compound OC(=O)CC[C@@H](C(O)=O)NC(=O)N[C@H](C(O)=O)CCCCNC(=O)CCCCCNC(=O)CCC1=CC=C(O)C(CN(CCN(CC(O)=O)CC=2C(=CC=C(CCC(O)=O)C=2)O)CC(O)=O)=C1 QJUIUFGOTBRHKP-LQJZCPKCSA-N 0.000 claims 1
• IZLOSIXADNUSCM-ACRUOGEOSA-N (2s)-2-[[[(4s)-4-carboxy-4-[[(4s)-4-carboxy-4-[6-[(4-fluorobenzoyl)amino]hexanoylamino]butanoyl]amino]butoxy]-hydroxyphosphoryl]amino]pentanedioic acid Chemical compound OC(=O)CC[C@@H](C(O)=O)NP(O)(=O)OCCC[C@@H](C(O)=O)NC(=O)CC[C@@H](C(O)=O)NC(=O)CCCCCNC(=O)C1=CC=C(F)C=C1 IZLOSIXADNUSCM-ACRUOGEOSA-N 0.000 claims 1
• 208000010470 Ageusia Diseases 0.000 claims 1
• 208000019505 Deglutition disease Diseases 0.000 claims 1
• 206010013952 Dysphonia Diseases 0.000 claims 1
• 108010048963 Glutamate carboxypeptidase Proteins 0.000 claims 1
• 208000010473 Hoarseness Diseases 0.000 claims 1
• WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
• 108010037516 PSMA-617 Proteins 0.000 claims 1
• 206010060862 Prostate cancer Diseases 0.000 claims 1
• 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
• 208000027418 Wounds and injury Diseases 0.000 claims 1
• 235000019666 ageusia Nutrition 0.000 claims 1
• 230000001186 cumulative effect Effects 0.000 claims 1
• 230000006378 damage Effects 0.000 claims 1
• 230000003247 decreasing effect Effects 0.000 claims 1
• 206010013781 dry mouth Diseases 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 229930195712 glutamate Natural products 0.000 claims 1
• 239000003112 inhibitor Substances 0.000 claims 1
• 208000014674 injury Diseases 0.000 claims 1
• 210000000056 organ Anatomy 0.000 claims 1
• 230000003439 radiotherapeutic effect Effects 0.000 claims 1
• 238000001959 radiotherapy Methods 0.000 claims 1
• 150000003384 small molecules Chemical class 0.000 claims 1
• 208000003265 stomatitis Diseases 0.000 claims 1
• 239000000126 substance Substances 0.000 claims 1
• 230000008685 targeting Effects 0.000 claims 1
• 229940126585 therapeutic drug Drugs 0.000 claims 1
• 230000000451 tissue damage Effects 0.000 claims 1
• 231100000827 tissue damage Toxicity 0.000 claims 1
• JBHPLHATEXGMQR-LFWIOBPJSA-N vipivotide tetraxetan Chemical compound OC(=O)CC[C@H](NC(=O)N[C@@H](CCCCNC(=O)[C@H](CC1=CC=C2C=CC=CC2=C1)NC(=O)[C@H]1CC[C@H](CNC(=O)CN2CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC2)CC1)C(O)=O)C(O)=O JBHPLHATEXGMQR-LFWIOBPJSA-N 0.000 claims 1