JP2007500743A5 - - Google Patents

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Publication number

JP2007500743A5

JP2007500743A5 JP2006532499A JP2006532499A JP2007500743A5 JP 2007500743 A5 JP2007500743 A5 JP 2007500743A5 JP 2006532499 A JP2006532499 A JP 2006532499A JP 2006532499 A JP2006532499 A JP 2006532499A JP 2007500743 A5 JP2007500743 A5 JP 2007500743A5

Authority

JP

Japan

Prior art keywords

conjugate

compound

formula

independently

conjugate according

Prior art date

2004-04-26

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Withdrawn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 66
• 229910052760 oxygen Inorganic materials 0.000 claims 21
• 229910052757 nitrogen Inorganic materials 0.000 claims 19
• 125000004432 carbon atom Chemical group C* 0.000 claims 11
• 229910052731 fluorine Inorganic materials 0.000 claims 9
• 229910052739 hydrogen Inorganic materials 0.000 claims 9
• 239000000203 mixture Substances 0.000 claims 9
• 125000000217 alkyl group Chemical group 0.000 claims 7
• -1 cyano, methyl Chemical group 0.000 claims 6
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 6
• 229910052717 sulfur Inorganic materials 0.000 claims 6
• 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 6
• 125000004093 cyano group Chemical group *C#N 0.000 claims 5
• 125000004423 acyloxy group Chemical group 0.000 claims 4
• 230000003110 anti-inflammatory effect Effects 0.000 claims 4
• 229910052801 chlorine Inorganic materials 0.000 claims 4
• 239000003814 drug Substances 0.000 claims 4
• 125000005843 halogen group Chemical group 0.000 claims 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
• 125000006239 protecting group Chemical group 0.000 claims 4
• 150000003839 salts Chemical class 0.000 claims 4
• 239000012453 solvate Substances 0.000 claims 4
• 229910052794 bromium Inorganic materials 0.000 claims 3
• 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
• 229940079593 drug Drugs 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
• 239000000546 pharmaceutical excipient Substances 0.000 claims 3
• PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 2
• 206010061218 Inflammation Diseases 0.000 claims 2
• 125000003342 alkenyl group Chemical group 0.000 claims 2
• 125000002947 alkylene group Chemical group 0.000 claims 2
• 125000000304 alkynyl group Chemical group 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 125000002837 carbocyclic group Chemical group 0.000 claims 2
• 229910052799 carbon Inorganic materials 0.000 claims 2
• 239000011737 fluorine Substances 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 125000005842 heteroatom Chemical group 0.000 claims 2
• 150000002430 hydrocarbons Chemical group 0.000 claims 2
• 239000001257 hydrogen Substances 0.000 claims 2
• 238000001727 in vivo Methods 0.000 claims 2
• 230000004054 inflammatory process Effects 0.000 claims 2
• 125000005647 linker group Chemical group 0.000 claims 2
• 125000001424 substituent group Chemical group 0.000 claims 2
• 229960004441 tyrosine Drugs 0.000 claims 2
• ALBODLTZUXKBGZ-JUUVMNCLSA-N (2s)-2-amino-3-phenylpropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CC1=CC=CC=C1 ALBODLTZUXKBGZ-JUUVMNCLSA-N 0.000 claims 1
• 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
• 125000006274 (C1-C3)alkoxy group Chemical group 0.000 claims 1
• 125000004454 (C1-C6) alkoxycarbonyl group Chemical group 0.000 claims 1
• 125000006700 (C1-C6) alkylthio group Chemical group 0.000 claims 1
• 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 1
• 125000000041 C6-C10 aryl group Chemical group 0.000 claims 1
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
• CKLJMWTZIZZHCS-UWTATZPHSA-N D-aspartic acid Chemical compound OC(=O)[C@H](N)CC(O)=O CKLJMWTZIZZHCS-UWTATZPHSA-N 0.000 claims 1
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
• 101710200424 Inosine-5'-monophosphate dehydrogenase Proteins 0.000 claims 1
• HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 1
• AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 1
• OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 1
• 241000124008 Mammalia Species 0.000 claims 1
• 241001465754 Metazoa Species 0.000 claims 1
• ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical group OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 claims 1
• 229940123827 Purine nucleoside phosphorylase inhibitor Drugs 0.000 claims 1
• 239000004473 Threonine Substances 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• 125000004450 alkenylene group Chemical group 0.000 claims 1
• 125000003545 alkoxy group Chemical group 0.000 claims 1
• 125000004419 alkynylene group Chemical group 0.000 claims 1
• IYABWNGZIDDRAK-UHFFFAOYSA-N allene Chemical group C=C=C IYABWNGZIDDRAK-UHFFFAOYSA-N 0.000 claims 1
• 229940024606 amino acid Drugs 0.000 claims 1
• 150000001413 amino acids Chemical class 0.000 claims 1
• 239000012491 analyte Substances 0.000 claims 1
• 230000000340 anti-metabolite Effects 0.000 claims 1
• 229960005475 antiinfective agent Drugs 0.000 claims 1
• 229940100197 antimetabolite Drugs 0.000 claims 1
• 239000002256 antimetabolite Substances 0.000 claims 1
• 239000004599 antimicrobial Substances 0.000 claims 1
• 239000002246 antineoplastic agent Substances 0.000 claims 1
• 239000003443 antiviral agent Substances 0.000 claims 1
• 125000004104 aryloxy group Chemical group 0.000 claims 1
• 229960005261 aspartic acid Drugs 0.000 claims 1
• 125000000852 azido group Chemical group *N=[N+]=[N-] 0.000 claims 1
• 125000000484 butyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• 125000001589 carboacyl group Chemical group 0.000 claims 1
• 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
• 125000001309 chloro group Chemical group Cl* 0.000 claims 1
• 125000000753 cycloalkyl group Chemical group 0.000 claims 1
• 125000002993 cycloalkylene group Chemical group 0.000 claims 1
• 239000002552 dosage form Substances 0.000 claims 1
• 125000005553 heteroaryloxy group Chemical group 0.000 claims 1
• 229960002885 histidine Drugs 0.000 claims 1
• 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
• 238000000338 in vitro Methods 0.000 claims 1
• 230000002757 inflammatory effect Effects 0.000 claims 1
• 239000003112 inhibitor Substances 0.000 claims 1
• 230000002401 inhibitory effect Effects 0.000 claims 1
• 229940043355 kinase inhibitor Drugs 0.000 claims 1
• 230000001404 mediated effect Effects 0.000 claims 1
• 238000013160 medical therapy Methods 0.000 claims 1
• 208000030159 metabolic disease Diseases 0.000 claims 1
• 238000000034 method Methods 0.000 claims 1
• 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
• 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
• 239000002777 nucleoside Substances 0.000 claims 1
• 150000003833 nucleoside derivatives Chemical class 0.000 claims 1
• 125000004043 oxo group Chemical group O=* 0.000 claims 1
• 239000008194 pharmaceutical composition Substances 0.000 claims 1
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
• UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical group [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 1
• 125000004437 phosphorous atom Chemical group 0.000 claims 1
• 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
• 229920000729 poly(L-lysine) polymer Polymers 0.000 claims 1
• 229920002643 polyglutamic acid Polymers 0.000 claims 1
• 108010055896 polyornithine Proteins 0.000 claims 1
• 108010000222 polyserine Proteins 0.000 claims 1
• 108090000765 processed proteins & peptides Proteins 0.000 claims 1
• 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
• QQONPFPTGQHPMA-UHFFFAOYSA-N propylene Natural products CC=C QQONPFPTGQHPMA-UHFFFAOYSA-N 0.000 claims 1
• 125000004805 propylene group Chemical group [H]C([H])([H])C([H])([*:1])C([H])([H])[*:2] 0.000 claims 1
• 239000000784 purine nucleoside phosphorylase inhibitor Substances 0.000 claims 1
• 229920006395 saturated elastomer Polymers 0.000 claims 1
• 229930195734 saturated hydrocarbon Natural products 0.000 claims 1
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
• 229960002898 threonine Drugs 0.000 claims 1
• 229930195735 unsaturated hydrocarbon Natural products 0.000 claims 1
• 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims 1
• 229920002554 vinyl polymer Polymers 0.000 claims 1
• 0 CCC(C)(**(*)*)C(*)(*)*(C*C)C(*)(C#C*)P(N(*)*)OC=C Chemical compound CCC(C)(**(*)*)C(*)(*)*(C*C)C(*)(C#C*)P(N(*)*)OC=C 0.000 description 3
• YNQLUTRBYVCPMQ-UHFFFAOYSA-N CCc1ccccc1 Chemical compound CCc1ccccc1 YNQLUTRBYVCPMQ-UHFFFAOYSA-N 0.000 description 1