JP2017529386A5 - - Google Patents

Info

Publication number

JP2017529386A5

JP2017529386A5 JP2017526762A JP2017526762A JP2017529386A5 JP 2017529386 A5 JP2017529386 A5 JP 2017529386A5 JP 2017526762 A JP2017526762 A JP 2017526762A JP 2017526762 A JP2017526762 A JP 2017526762A JP 2017529386 A5 JP2017529386 A5 JP 2017529386A5

Authority

JP

Japan

Prior art keywords

pro

arg

nap

trp

hca

Prior art date

2015-08-05

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

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• 125000000539 amino acid group Chemical group 0.000 claims 8
• 239000008194 pharmaceutical composition Substances 0.000 claims 8
• 239000002253 acid Substances 0.000 claims 6
• 239000003814 drug Substances 0.000 claims 4
• 229940124597 therapeutic agent Drugs 0.000 claims 4
• 230000006536 aerobic glycolysis Effects 0.000 claims 3
• 239000003112 inhibitor Substances 0.000 claims 3
• -1 1,2-dihydronaphthyl group Chemical group 0.000 claims 2
• 206010028980 Neoplasm Diseases 0.000 claims 2
• 230000002378 acidificating effect Effects 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 201000011510 cancer Diseases 0.000 claims 2
• 239000000203 mixture Substances 0.000 claims 2
• 229940002612 prodrug Drugs 0.000 claims 2
• 239000000651 prodrug Substances 0.000 claims 2
• 150000003839 salts Chemical class 0.000 claims 2
• MJIDYLIDXWGFRN-QMMMGPOBSA-N (2s)-2-[2-(diaminomethylidene)hydrazinyl]-3-phenylpropanoic acid Chemical compound NC(=N)NN[C@H](C(O)=O)CC1=CC=CC=C1 MJIDYLIDXWGFRN-QMMMGPOBSA-N 0.000 claims 1
• NNWQLZWAZSJGLY-VKHMYHEASA-N (2s)-2-azaniumyl-4-azidobutanoate Chemical compound OC(=O)[C@@H](N)CCN=[N+]=[N-] NNWQLZWAZSJGLY-VKHMYHEASA-N 0.000 claims 1
• VRYALKFFQXWPIH-PBXRRBTRSA-N (3r,4s,5r)-3,4,5,6-tetrahydroxyhexanal Chemical group OC[C@@H](O)[C@@H](O)[C@H](O)CC=O VRYALKFFQXWPIH-PBXRRBTRSA-N 0.000 claims 1
• JASNXOXPNZWQRV-UHFFFAOYSA-N 3-azaniumyl-3-naphthalen-2-ylpropanoate Chemical compound C1=CC=CC2=CC(C(CC(O)=O)N)=CC=C21 JASNXOXPNZWQRV-UHFFFAOYSA-N 0.000 claims 1
• FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical group C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims 1
• OMLWNBVRVJYMBQ-YUMQZZPRSA-N Arg-Arg Chemical group NC(N)=NCCC[C@H](N)C(=O)N[C@@H](CCCN=C(N)N)C(O)=O OMLWNBVRVJYMBQ-YUMQZZPRSA-N 0.000 claims 1
• 206010005003 Bladder cancer Diseases 0.000 claims 1
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• 125000000998 L-alanino group Chemical group [H]N([*])[C@](C([H])([H])[H])([H])C(=O)O[H] 0.000 claims 1
• VBOQYPQEPHKASR-VKHMYHEASA-N L-homocysteic acid Chemical compound OC(=O)[C@@H](N)CCS(O)(=O)=O VBOQYPQEPHKASR-VKHMYHEASA-N 0.000 claims 1
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• 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
• NQIHMZLGCZNZBN-PXNSSMCTSA-N Trp-Trp Chemical group C1=CC=C2C(C[C@H](NC(=O)[C@H](CC=3C4=CC=CC=C4NC=3)N)C(O)=O)=CNC2=C1 NQIHMZLGCZNZBN-PXNSSMCTSA-N 0.000 claims 1
• 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
• 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
• PMMURAAUARKVCB-UHFFFAOYSA-N alpha-D-ara-dHexp Natural products OCC1OC(O)CC(O)C1O PMMURAAUARKVCB-UHFFFAOYSA-N 0.000 claims 1
• 108010068380 arginylarginine Proteins 0.000 claims 1
• 201000010881 cervical cancer Diseases 0.000 claims 1
• 238000003776 cleavage reaction Methods 0.000 claims 1
• 208000035250 cutaneous malignant susceptibility to 1 melanoma Diseases 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 230000000694 effects Effects 0.000 claims 1
• 201000004101 esophageal cancer Diseases 0.000 claims 1
• 206010017758 gastric cancer Diseases 0.000 claims 1
• 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
• 201000010536 head and neck cancer Diseases 0.000 claims 1
• 208000014829 head and neck neoplasm Diseases 0.000 claims 1
• 230000002401 inhibitory effect Effects 0.000 claims 1
• 208000032839 leukemia Diseases 0.000 claims 1
• 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
• 201000001441 melanoma Diseases 0.000 claims 1
• 125000001624 naphthyl group Chemical group 0.000 claims 1
• 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
• 201000002528 pancreatic cancer Diseases 0.000 claims 1
• 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 108090000765 processed proteins & peptides Proteins 0.000 claims 1
• 238000001959 radiotherapy Methods 0.000 claims 1
• FSYKKLYZXJSNPZ-UHFFFAOYSA-N sarcosine Chemical group C[NH2+]CC([O-])=O FSYKKLYZXJSNPZ-UHFFFAOYSA-N 0.000 claims 1
• 230000007017 scission Effects 0.000 claims 1
• 208000000587 small cell lung carcinoma Diseases 0.000 claims 1
• 201000011549 stomach cancer Diseases 0.000 claims 1
• 238000001356 surgical procedure Methods 0.000 claims 1
• 108010045269 tryptophyltryptophan Proteins 0.000 claims 1
• 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 1
• 201000005112 urinary bladder cancer Diseases 0.000 claims 1
• 0 CCC(C)(C)N1[C@](CCCC(CCS(O)(=O)=O)C(CC*N(CCC2)[C@@]2C(N[C@@](CCS(O)(=O)=O)C(N(CCC2)[C@]2C(OC(C)(C)CC)=[U])=C)=C)=[U])CCC1 Chemical compound CCC(C)(C)N1[C@](CCCC(CCS(O)(=O)=O)C(CC*N(CCC2)[C@@]2C(N[C@@](CCS(O)(=O)=O)C(N(CCC2)[C@]2C(OC(C)(C)CC)=[U])=C)=C)=[U])CCC1 0.000 description 1