JP2018511628A5 - - Google Patents

Info

Publication number

JP2018511628A5

JP2018511628A5 JP2017553879A JP2017553879A JP2018511628A5 JP 2018511628 A5 JP2018511628 A5 JP 2018511628A5 JP 2017553879 A JP2017553879 A JP 2017553879A JP 2017553879 A JP2017553879 A JP 2017553879A JP 2018511628 A5 JP2018511628 A5 JP 2018511628A5

Authority

JP

Japan

Prior art keywords

seq

group

alkyl

formula

antibody

Prior art date

2016-04-15

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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• 125000000217 alkyl group Chemical group 0.000 claims 18
• 229910052799 carbon Inorganic materials 0.000 claims 13
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 13
• 125000003342 alkenyl group Chemical group 0.000 claims 12
• 150000001413 amino acids Chemical group 0.000 claims 12
• 125000003118 aryl group Chemical group 0.000 claims 9
• 235000018417 cysteine Nutrition 0.000 claims 9
• XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 8
• 125000005843 halogen group Chemical group 0.000 claims 8
• 229910052739 hydrogen Inorganic materials 0.000 claims 8
• 125000005647 linker group Chemical group 0.000 claims 8
• 235000001014 amino acid Nutrition 0.000 claims 7
• 125000004432 carbon atom Chemical group C* 0.000 claims 7
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 6
• 238000006467 substitution reaction Methods 0.000 claims 6
• 125000001544 thienyl group Chemical group 0.000 claims 6
• 125000002947 alkylene group Chemical group 0.000 claims 5
• 229940024606 amino acid Drugs 0.000 claims 5
• 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 5
• 229940079593 drug Drugs 0.000 claims 5
• 239000003814 drug Substances 0.000 claims 5
• 239000012634 fragment Substances 0.000 claims 5
• 229910052760 oxygen Inorganic materials 0.000 claims 5
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 5
• NFGXHKASABOEEW-UHFFFAOYSA-N 1-methylethyl 11-methoxy-3,7,11-trimethyl-2,4-dodecadienoate Chemical compound COC(C)(C)CCCC(C)CC=CC(C)=CC(=O)OC(C)C NFGXHKASABOEEW-UHFFFAOYSA-N 0.000 claims 4
• 125000005907 alkyl ester group Chemical group 0.000 claims 4
• 125000000304 alkynyl group Chemical group 0.000 claims 4
• -1 methoxy, pyridyl Chemical group 0.000 claims 4
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
• UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 claims 3
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
• 125000000623 heterocyclic group Chemical group 0.000 claims 3
• 229910052757 nitrogen Inorganic materials 0.000 claims 3
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
• 229910052717 sulfur Inorganic materials 0.000 claims 3
• 108010016626 Dipeptides Proteins 0.000 claims 2
• DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 2
• JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
• 125000001309 chloro group Chemical group Cl* 0.000 claims 2
• 239000002131 composite material Substances 0.000 claims 2
• IBAHLNWTOIHLKE-UHFFFAOYSA-N cyano cyanate Chemical compound N#COC#N IBAHLNWTOIHLKE-UHFFFAOYSA-N 0.000 claims 2
• 125000004093 cyano group Chemical group *C#N 0.000 claims 2
• 125000000753 cycloalkyl group Chemical group 0.000 claims 2
• 201000010099 disease Diseases 0.000 claims 2
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
• 150000002148 esters Chemical class 0.000 claims 2
• 229910052731 fluorine Inorganic materials 0.000 claims 2
• 125000001153 fluoro group Chemical group F* 0.000 claims 2
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
• 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
• 150000002825 nitriles Chemical group 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 2
• 125000004076 pyridyl group Chemical group 0.000 claims 2
• 125000001424 substituent group Chemical group 0.000 claims 2
• 125000004400 (C1-C12) alkyl group Chemical group 0.000 claims 1
• 125000000229 (C1-C4)alkoxy group Chemical group 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 compound 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
• 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 1
• 239000004471 Glycine Substances 0.000 claims 1
• 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 1
• QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 1
• AGPKZVBTJJNPAG-WHFBIAKZSA-N L-isoleucine Chemical compound CC[C@H](C)[C@H](N)C(O)=O AGPKZVBTJJNPAG-WHFBIAKZSA-N 0.000 claims 1
• KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
• 206010028980 Neoplasm Diseases 0.000 claims 1
• KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
• 235000004279 alanine Nutrition 0.000 claims 1
• 239000002246 antineoplastic agent Substances 0.000 claims 1
• 201000011510 cancer Diseases 0.000 claims 1
• 150000001768 cations Chemical class 0.000 claims 1
• 230000021615 conjugation Effects 0.000 claims 1
• 150000001945 cysteines Chemical group 0.000 claims 1
• 229940127089 cytotoxic agent Drugs 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 125000005842 heteroatom Chemical group 0.000 claims 1
• 229960000310 isoleucine Drugs 0.000 claims 1
• AGPKZVBTJJNPAG-UHFFFAOYSA-N isoleucine Natural products CCC(C)C(N)C(O)=O AGPKZVBTJJNPAG-UHFFFAOYSA-N 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 229920001481 poly(stearyl methacrylate) Polymers 0.000 claims 1
• 230000002062 proliferating effect Effects 0.000 claims 1
• UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
• 238000002560 therapeutic procedure Methods 0.000 claims 1
• 239000004474 valine Substances 0.000 claims 1
• 0 N=C(CC(CC1)=O)C1*1=CC=CC=CC1 Chemical compound N=C(CC(CC1)=O)C1*1=CC=CC=CC1 0.000 description 1