JP2018521143A5 - - Google Patents

Info

Publication number

JP2018521143A5

JP2018521143A5 JP2018522872A JP2018522872A JP2018521143A5 JP 2018521143 A5 JP2018521143 A5 JP 2018521143A5 JP 2018522872 A JP2018522872 A JP 2018522872A JP 2018522872 A JP2018522872 A JP 2018522872A JP 2018521143 A5 JP2018521143 A5 JP 2018521143A5

Authority

JP

Japan

Prior art keywords

serine protease

pharmaceutical composition

polypeptide

protease activity

combination according

Prior art date

2016-07-22

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

• 108010022999 Serine Proteases Proteins 0.000 claims 19
• 102000012479 Serine Proteases Human genes 0.000 claims 19
• 239000008194 pharmaceutical composition Substances 0.000 claims 18
• 229920001184 polypeptide Polymers 0.000 claims 14
• 108090000765 processed proteins & peptides Proteins 0.000 claims 14
• 102000004196 processed proteins & peptides Human genes 0.000 claims 14
• 230000000694 effects Effects 0.000 claims 11
• 108090000631 Trypsin Proteins 0.000 claims 6
• 102000004142 Trypsin Human genes 0.000 claims 6
• 150000001875 compounds Chemical class 0.000 claims 6
• 239000012588 trypsin Substances 0.000 claims 6
• 108090000317 Chymotrypsin Proteins 0.000 claims 5
• 230000001580 bacterial effect Effects 0.000 claims 5
• 230000003115 biocidal effect Effects 0.000 claims 5
• 229960002376 chymotrypsin Drugs 0.000 claims 5
• 239000000203 mixture Substances 0.000 claims 3
• ULGZDMOVFRHVEP-RWJQBGPGSA-N Erythromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)C(=O)[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 ULGZDMOVFRHVEP-RWJQBGPGSA-N 0.000 claims 2
• 241000276438 Gadus morhua Species 0.000 claims 2
• 241000191967 Staphylococcus aureus Species 0.000 claims 2
• MYSWGUAQZAJSOK-UHFFFAOYSA-N ciprofloxacin Chemical compound C12=CC(N3CCNCC3)=C(F)C=C2C(=O)C(C(=O)O)=CN1C1CC1 MYSWGUAQZAJSOK-UHFFFAOYSA-N 0.000 claims 2
• -1 dalasin Chemical compound 0.000 claims 2
• 238000000034 method Methods 0.000 claims 2
• SGKRLCUYIXIAHR-AKNGSSGZSA-N (4s,4ar,5s,5ar,6r,12ar)-4-(dimethylamino)-1,5,10,11,12a-pentahydroxy-6-methyl-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1=CC=C2[C@H](C)[C@@H]([C@H](O)[C@@H]3[C@](C(O)=C(C(N)=O)C(=O)[C@H]3N(C)C)(O)C3=O)C3=C(O)C2=C1O SGKRLCUYIXIAHR-AKNGSSGZSA-N 0.000 claims 1
• FFTVPQUHLQBXQZ-KVUCHLLUSA-N (4s,4as,5ar,12ar)-4,7-bis(dimethylamino)-1,10,11,12a-tetrahydroxy-3,12-dioxo-4a,5,5a,6-tetrahydro-4h-tetracene-2-carboxamide Chemical compound C1C2=C(N(C)C)C=CC(O)=C2C(O)=C2[C@@H]1C[C@H]1[C@H](N(C)C)C(=O)C(C(N)=O)=C(O)[C@@]1(O)C2=O FFTVPQUHLQBXQZ-KVUCHLLUSA-N 0.000 claims 1
• 241000972773 Aulopiformes Species 0.000 claims 1
• 108010001478 Bacitracin Proteins 0.000 claims 1
• 241000894006 Bacteria Species 0.000 claims 1
• 229930186147 Cephalosporin Natural products 0.000 claims 1
• 241000193403 Clostridium Species 0.000 claims 1
• 108010013198 Daptomycin Proteins 0.000 claims 1
• 241000239366 Euphausiacea Species 0.000 claims 1
• 241001313700 Gadus chalcogrammus Species 0.000 claims 1
• 241000606768 Haemophilus influenzae Species 0.000 claims 1
• JUZNIMUFDBIJCM-ANEDZVCMSA-N Invanz Chemical compound O=C([C@H]1NC[C@H](C1)SC=1[C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)NC1=CC=CC(C(O)=O)=C1 JUZNIMUFDBIJCM-ANEDZVCMSA-N 0.000 claims 1
• 241000589242 Legionella pneumophila Species 0.000 claims 1
• 229930182555 Penicillin Natural products 0.000 claims 1
• JGSARLDLIJGVTE-MBNYWOFBSA-N Penicillin G Chemical compound N([C@H]1[C@H]2SC([C@@H](N2C1=O)C(O)=O)(C)C)C(=O)CC1=CC=CC=C1 JGSARLDLIJGVTE-MBNYWOFBSA-N 0.000 claims 1
• 108010093965 Polymyxin B Proteins 0.000 claims 1
• 241000589517 Pseudomonas aeruginosa Species 0.000 claims 1
• 101710151387 Serine protease 1 Proteins 0.000 claims 1
• 102100032491 Serine protease 1 Human genes 0.000 claims 1
• 241001134658 Streptococcus mitis Species 0.000 claims 1
• 241000193998 Streptococcus pneumoniae Species 0.000 claims 1
• 108010053950 Teicoplanin Proteins 0.000 claims 1
• 239000004098 Tetracycline Substances 0.000 claims 1
• 101710119665 Trypsin-1 Proteins 0.000 claims 1
• 229960003022 amoxicillin Drugs 0.000 claims 1
• LSQZJLSUYDQPKJ-NJBDSQKTSA-N amoxicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=C(O)C=C1 LSQZJLSUYDQPKJ-NJBDSQKTSA-N 0.000 claims 1
• 229960000723 ampicillin Drugs 0.000 claims 1
• AVKUERGKIZMTKX-NJBDSQKTSA-N ampicillin Chemical compound C1([C@@H](N)C(=O)N[C@H]2[C@H]3SC([C@@H](N3C2=O)C(O)=O)(C)C)=CC=CC=C1 AVKUERGKIZMTKX-NJBDSQKTSA-N 0.000 claims 1
• 239000003242 anti bacterial agent Substances 0.000 claims 1
• 229940088710 antibiotic agent Drugs 0.000 claims 1
• 229960004099 azithromycin Drugs 0.000 claims 1
• MQTOSJVFKKJCRP-BICOPXKESA-N azithromycin Chemical compound O([C@@H]1[C@@H](C)C(=O)O[C@@H]([C@@]([C@H](O)[C@@H](C)N(C)C[C@H](C)C[C@@](C)(O)[C@H](O[C@H]2[C@@H]([C@H](C[C@@H](C)O2)N(C)C)O)[C@H]1C)(C)O)CC)[C@H]1C[C@@](C)(OC)[C@@H](O)[C@H](C)O1 MQTOSJVFKKJCRP-BICOPXKESA-N 0.000 claims 1
• 229960003071 bacitracin Drugs 0.000 claims 1
• 229930184125 bacitracin Natural products 0.000 claims 1
• CLKOFPXJLQSYAH-ABRJDSQDSA-N bacitracin A Chemical compound C1SC([C@@H](N)[C@@H](C)CC)=N[C@@H]1C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]1C(=O)N[C@H](CCCN)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CC=2N=CNC=2)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CC(N)=O)C(=O)NCCCC1 CLKOFPXJLQSYAH-ABRJDSQDSA-N 0.000 claims 1
• YZBQHRLRFGPBSL-RXMQYKEDSA-N carbapenem Chemical compound C1C=CN2C(=O)C[C@H]21 YZBQHRLRFGPBSL-RXMQYKEDSA-N 0.000 claims 1
• 229960004261 cefotaxime Drugs 0.000 claims 1
• GPRBEKHLDVQUJE-VINNURBNSA-N cefotaxime Chemical compound N([C@@H]1C(N2C(=C(COC(C)=O)CS[C@@H]21)C(O)=O)=O)C(=O)/C(=N/OC)C1=CSC(N)=N1 GPRBEKHLDVQUJE-VINNURBNSA-N 0.000 claims 1
• 229960004755 ceftriaxone Drugs 0.000 claims 1
• VAAUVRVFOQPIGI-SPQHTLEESA-N ceftriaxone Chemical compound S([C@@H]1[C@@H](C(N1C=1C(O)=O)=O)NC(=O)\C(=N/OC)C=2N=C(N)SC=2)CC=1CSC1=NC(=O)C(=O)NN1C VAAUVRVFOQPIGI-SPQHTLEESA-N 0.000 claims 1
• 229960001668 cefuroxime Drugs 0.000 claims 1
• JFPVXVDWJQMJEE-IZRZKJBUSA-N cefuroxime Chemical compound N([C@@H]1C(N2C(=C(COC(N)=O)CS[C@@H]21)C(O)=O)=O)C(=O)\C(=N/OC)C1=CC=CO1 JFPVXVDWJQMJEE-IZRZKJBUSA-N 0.000 claims 1
• 229940124587 cephalosporin Drugs 0.000 claims 1
• 150000001780 cephalosporins Chemical class 0.000 claims 1
• DDTDNCYHLGRFBM-YZEKDTGTSA-N chembl2367892 Chemical compound CC(=O)N[C@H]1[C@@H](O)[C@H](O)[C@H](CO)O[C@H]1O[C@@H]([C@H]1C(N[C@@H](C2=CC(O)=CC(O[C@@H]3[C@H]([C@H](O)[C@H](O)[C@@H](CO)O3)O)=C2C=2C(O)=CC=C(C=2)[C@@H](NC(=O)[C@@H]2NC(=O)[C@@H]3C=4C=C(O)C=C(C=4)OC=4C(O)=CC=C(C=4)[C@@H](N)C(=O)N[C@H](CC=4C=C(Cl)C(O5)=CC=4)C(=O)N3)C(=O)N1)C(O)=O)=O)C(C=C1Cl)=CC=C1OC1=C(O[C@H]3[C@H]([C@@H](O)[C@H](O)[C@H](CO)O3)NC(C)=O)C5=CC2=C1 DDTDNCYHLGRFBM-YZEKDTGTSA-N 0.000 claims 1
• 229960005091 chloramphenicol Drugs 0.000 claims 1
• WIIZWVCIJKGZOK-RKDXNWHRSA-N chloramphenicol Chemical compound ClC(Cl)C(=O)N[C@H](CO)[C@H](O)C1=CC=C([N+]([O-])=O)C=C1 WIIZWVCIJKGZOK-RKDXNWHRSA-N 0.000 claims 1
• 229960003405 ciprofloxacin Drugs 0.000 claims 1
• 229960002227 clindamycin Drugs 0.000 claims 1
• KDLRVYVGXIQJDK-AWPVFWJPSA-N clindamycin Chemical compound CN1C[C@H](CCC)C[C@H]1C(=O)N[C@H]([C@H](C)Cl)[C@@H]1[C@H](O)[C@H](O)[C@@H](O)[C@@H](SC)O1 KDLRVYVGXIQJDK-AWPVFWJPSA-N 0.000 claims 1
• 229960002615 dalfopristin Drugs 0.000 claims 1
• 108700028430 dalfopristin Proteins 0.000 claims 1
• SUYRLXYYZQTJHF-VMBLUXKRSA-N dalfopristin Chemical compound O=C([C@@H]1N(C2=O)CC[C@H]1S(=O)(=O)CCN(CC)CC)O[C@H](C(C)C)[C@H](C)\C=C\C(=O)NC\C=C\C(\C)=C\[C@@H](O)CC(=O)CC1=NC2=CO1 SUYRLXYYZQTJHF-VMBLUXKRSA-N 0.000 claims 1
• 229960005484 daptomycin Drugs 0.000 claims 1
• DOAKLVKFURWEDJ-QCMAZARJSA-N daptomycin Chemical compound C([C@H]1C(=O)O[C@H](C)[C@@H](C(NCC(=O)N[C@@H](CCCN)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@H](C)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@H](CO)C(=O)N[C@H](C(=O)N1)[C@H](C)CC(O)=O)=O)NC(=O)[C@H](CC(O)=O)NC(=O)[C@@H](CC(N)=O)NC(=O)[C@H](CC=1C2=CC=CC=C2NC=1)NC(=O)CCCCCCCCC)C(=O)C1=CC=CC=C1N DOAKLVKFURWEDJ-QCMAZARJSA-N 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 229960003722 doxycycline Drugs 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 229960002770 ertapenem Drugs 0.000 claims 1
• 229960003276 erythromycin Drugs 0.000 claims 1
• 229940124307 fluoroquinolone Drugs 0.000 claims 1
• 229940047650 haemophilus influenzae Drugs 0.000 claims 1
• 238000000338 in vitro Methods 0.000 claims 1
• 230000002401 inhibitory effect Effects 0.000 claims 1
• 229940115932 legionella pneumophila Drugs 0.000 claims 1
• 229960002260 meropenem Drugs 0.000 claims 1
• DMJNNHOOLUXYBV-PQTSNVLCSA-N meropenem Chemical compound C=1([C@H](C)[C@@H]2[C@H](C(N2C=1C(O)=O)=O)[C@H](O)C)S[C@@H]1CN[C@H](C(=O)N(C)C)C1 DMJNNHOOLUXYBV-PQTSNVLCSA-N 0.000 claims 1
• 229960000282 metronidazole Drugs 0.000 claims 1
• VAOCPAMSLUNLGC-UHFFFAOYSA-N metronidazole Chemical compound CC1=NC=C([N+]([O-])=O)N1CCO VAOCPAMSLUNLGC-UHFFFAOYSA-N 0.000 claims 1
• 229960004023 minocycline Drugs 0.000 claims 1
• 229960003702 moxifloxacin Drugs 0.000 claims 1
• FABPRXSRWADJSP-MEDUHNTESA-N moxifloxacin Chemical compound COC1=C(N2C[C@H]3NCCC[C@H]3C2)C(F)=CC(C(C(C(O)=O)=C2)=O)=C1N2C1CC1 FABPRXSRWADJSP-MEDUHNTESA-N 0.000 claims 1
• 229960000515 nafcillin Drugs 0.000 claims 1
• GPXLMGHLHQJAGZ-JTDSTZFVSA-N nafcillin Chemical compound C1=CC=CC2=C(C(=O)N[C@@H]3C(N4[C@H](C(C)(C)S[C@@H]43)C(O)=O)=O)C(OCC)=CC=C21 GPXLMGHLHQJAGZ-JTDSTZFVSA-N 0.000 claims 1
• 239000007922 nasal spray Substances 0.000 claims 1
• 229940097496 nasal spray Drugs 0.000 claims 1
• 229960001019 oxacillin Drugs 0.000 claims 1
• UWYHMGVUTGAWSP-JKIFEVAISA-N oxacillin Chemical compound N([C@@H]1C(N2[C@H](C(C)(C)S[C@@H]21)C(O)=O)=O)C(=O)C1=C(C)ON=C1C1=CC=CC=C1 UWYHMGVUTGAWSP-JKIFEVAISA-N 0.000 claims 1
• LSQZJLSUYDQPKJ-UHFFFAOYSA-N p-Hydroxyampicillin Natural products O=C1N2C(C(O)=O)C(C)(C)SC2C1NC(=O)C(N)C1=CC=C(O)C=C1 LSQZJLSUYDQPKJ-UHFFFAOYSA-N 0.000 claims 1
• 229940049954 penicillin Drugs 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 229920000024 polymyxin B Polymers 0.000 claims 1
• 229960005266 polymyxin b Drugs 0.000 claims 1
• 229960005442 quinupristin Drugs 0.000 claims 1
• WTHRRGMBUAHGNI-LCYNINFDSA-N quinupristin Chemical compound N([C@@H]1C(=O)N[C@@H](C(N2CCC[C@H]2C(=O)N(C)[C@@H](CC=2C=CC(=CC=2)N(C)C)C(=O)N2C[C@@H](CS[C@H]3C4CCN(CC4)C3)C(=O)C[C@H]2C(=O)N[C@H](C(=O)O[C@@H]1C)C=1C=CC=CC=1)=O)CC)C(=O)C1=NC=CC=C1O WTHRRGMBUAHGNI-LCYNINFDSA-N 0.000 claims 1
• 108700028429 quinupristin Proteins 0.000 claims 1
• 210000002345 respiratory system Anatomy 0.000 claims 1
• 229960001225 rifampicin Drugs 0.000 claims 1
• JQXXHWHPUNPDRT-WLSIYKJHSA-N rifampicin Chemical compound O([C@](C1=O)(C)O/C=C/[C@@H]([C@H]([C@@H](OC(C)=O)[C@H](C)[C@H](O)[C@H](C)[C@@H](O)[C@@H](C)\C=C\C=C(C)/C(=O)NC=2C(O)=C3C([O-])=C4C)C)OC)C4=C1C3=C(O)C=2\C=N\N1CC[NH+](C)CC1 JQXXHWHPUNPDRT-WLSIYKJHSA-N 0.000 claims 1
• 235000019515 salmon Nutrition 0.000 claims 1
• 239000007921 spray Substances 0.000 claims 1
• 229940031000 streptococcus pneumoniae Drugs 0.000 claims 1
• 229960005404 sulfamethoxazole Drugs 0.000 claims 1
• JLKIGFTWXXRPMT-UHFFFAOYSA-N sulphamethoxazole Chemical compound O1C(C)=CC(NS(=O)(=O)C=2C=CC(N)=CC=2)=N1 JLKIGFTWXXRPMT-UHFFFAOYSA-N 0.000 claims 1
• 229960001608 teicoplanin Drugs 0.000 claims 1
• 229960002180 tetracycline Drugs 0.000 claims 1
• 229930101283 tetracycline Natural products 0.000 claims 1
• 235000019364 tetracycline Nutrition 0.000 claims 1
• 150000003522 tetracyclines Chemical class 0.000 claims 1