JP2013527158A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013527158A5 JP2013527158A5 JP2013505200A JP2013505200A JP2013527158A5 JP 2013527158 A5 JP2013527158 A5 JP 2013527158A5 JP 2013505200 A JP2013505200 A JP 2013505200A JP 2013505200 A JP2013505200 A JP 2013505200A JP 2013527158 A5 JP2013527158 A5 JP 2013527158A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- agent
- inhibitor
- polysaccharide
- tumor
- Prior art date
- 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.)
- Granted
Links
- 150000004676 glycans Chemical class 0.000 claims description 49
- 239000000203 mixture Substances 0.000 claims description 37
- 206010028980 Neoplasm Diseases 0.000 claims description 31
- 230000000694 effects Effects 0.000 claims description 31
- 229920001282 polysaccharide Polymers 0.000 claims description 28
- 239000005017 polysaccharide Substances 0.000 claims description 28
- 239000002253 acid Substances 0.000 claims description 24
- 239000003795 chemical substances by application Substances 0.000 claims description 23
- 150000004804 polysaccharides Polymers 0.000 claims description 21
- 210000001519 tissue Anatomy 0.000 claims description 21
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 claims description 20
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims description 16
- 239000003112 inhibitor Substances 0.000 claims description 15
- 238000002360 preparation method Methods 0.000 claims description 15
- 230000001858 anti-Xa Effects 0.000 claims description 14
- 239000003814 drug Substances 0.000 claims description 11
- -1 antisense molecule Proteins 0.000 claims description 10
- WGCNASOHLSPBMP-UHFFFAOYSA-N hydroxyacetaldehyde Natural products OCC=O WGCNASOHLSPBMP-UHFFFAOYSA-N 0.000 claims description 10
- 239000012216 imaging agent Substances 0.000 claims description 10
- 230000002757 inflammatory effect Effects 0.000 claims description 10
- 230000003902 lesion Effects 0.000 claims description 10
- 102000004127 Cytokines Human genes 0.000 claims description 9
- 108090000695 Cytokines Proteins 0.000 claims description 9
- IAKHMKGGTNLKSZ-INIZCTEOSA-N (S)-colchicine Chemical compound C1([C@@H](NC(C)=O)CC2)=CC(=O)C(OC)=CC=C1C1=C2C=C(OC)C(OC)=C1OC IAKHMKGGTNLKSZ-INIZCTEOSA-N 0.000 claims description 8
- 229940123237 Taxane Drugs 0.000 claims description 8
- RJURFGZVJUQBHK-UHFFFAOYSA-N actinomycin D Natural products CC1OC(=O)C(C(C)C)N(C)C(=O)CN(C)C(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)NC4C(=O)NC(C(N5CCCC5C(=O)N(C)CC(=O)N(C)C(C(C)C)C(=O)OC4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-UHFFFAOYSA-N 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 claims description 8
- RXWNCPJZOCPEPQ-NVWDDTSBSA-N puromycin Chemical compound C1=CC(OC)=CC=C1C[C@H](N)C(=O)N[C@H]1[C@@H](O)[C@H](N2C3=NC=NC(=C3N=C2)N(C)C)O[C@@H]1CO RXWNCPJZOCPEPQ-NVWDDTSBSA-N 0.000 claims description 8
- 150000008273 hexosamines Chemical group 0.000 claims description 7
- 201000009030 Carcinoma Diseases 0.000 claims description 6
- 229940121363 anti-inflammatory agent Drugs 0.000 claims description 6
- 239000002260 anti-inflammatory agent Substances 0.000 claims description 6
- 208000006673 asthma Diseases 0.000 claims description 6
- 238000009472 formulation Methods 0.000 claims description 6
- 239000000941 radioactive substance Substances 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 206010039491 Sarcoma Diseases 0.000 claims description 5
- 239000002246 antineoplastic agent Substances 0.000 claims description 5
- 206010012601 diabetes mellitus Diseases 0.000 claims description 5
- 230000008685 targeting Effects 0.000 claims description 5
- DKPFODGZWDEEBT-QFIAKTPHSA-N taxane Chemical class C([C@]1(C)CCC[C@@H](C)[C@H]1C1)C[C@H]2[C@H](C)CC[C@@H]1C2(C)C DKPFODGZWDEEBT-QFIAKTPHSA-N 0.000 claims description 5
- 230000001225 therapeutic effect Effects 0.000 claims description 5
- VEEGZPWAAPPXRB-BJMVGYQFSA-N (3e)-3-(1h-imidazol-5-ylmethylidene)-1h-indol-2-one Chemical compound O=C1NC2=CC=CC=C2\C1=C/C1=CN=CN1 VEEGZPWAAPPXRB-BJMVGYQFSA-N 0.000 claims description 4
- FDKXTQMXEQVLRF-ZHACJKMWSA-N (E)-dacarbazine Chemical compound CN(C)\N=N\c1[nH]cnc1C(N)=O FDKXTQMXEQVLRF-ZHACJKMWSA-N 0.000 claims description 4
- VSNHCAURESNICA-NJFSPNSNSA-N 1-oxidanylurea Chemical compound N[14C](=O)NO VSNHCAURESNICA-NJFSPNSNSA-N 0.000 claims description 4
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-VTZDEGQISA-N 0.000 claims description 4
- NMUSYJAQQFHJEW-KVTDHHQDSA-N 5-azacytidine Chemical compound O=C1N=C(N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 NMUSYJAQQFHJEW-KVTDHHQDSA-N 0.000 claims description 4
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims description 4
- 108091023037 Aptamer Proteins 0.000 claims description 4
- NOWKCMXCCJGMRR-UHFFFAOYSA-N Aziridine Chemical compound C1CN1 NOWKCMXCCJGMRR-UHFFFAOYSA-N 0.000 claims description 4
- MLDQJTXFUGDVEO-UHFFFAOYSA-N BAY-43-9006 Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC(=O)NC=3C=C(C(Cl)=CC=3)C(F)(F)F)=CC=2)=C1 MLDQJTXFUGDVEO-UHFFFAOYSA-N 0.000 claims description 4
- GAGWJHPBXLXJQN-UORFTKCHSA-N Capecitabine Chemical compound C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1[C@H]1[C@H](O)[C@H](O)[C@@H](C)O1 GAGWJHPBXLXJQN-UORFTKCHSA-N 0.000 claims description 4
- GAGWJHPBXLXJQN-UHFFFAOYSA-N Capecitabine Natural products C1=C(F)C(NC(=O)OCCCCC)=NC(=O)N1C1C(O)C(O)C(C)O1 GAGWJHPBXLXJQN-UHFFFAOYSA-N 0.000 claims description 4
- 102000019034 Chemokines Human genes 0.000 claims description 4
- 108010012236 Chemokines Proteins 0.000 claims description 4
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims description 4
- 108010092160 Dactinomycin Proteins 0.000 claims description 4
- ZBNZXTGUTAYRHI-UHFFFAOYSA-N Dasatinib Chemical compound C=1C(N2CCN(CCO)CC2)=NC(C)=NC=1NC(S1)=NC=C1C(=O)NC1=C(C)C=CC=C1Cl ZBNZXTGUTAYRHI-UHFFFAOYSA-N 0.000 claims description 4
- 201000004624 Dermatitis Diseases 0.000 claims description 4
- MBYXEBXZARTUSS-QLWBXOBMSA-N Emetamine Natural products O(C)c1c(OC)cc2c(c(C[C@@H]3[C@H](CC)CN4[C@H](c5c(cc(OC)c(OC)c5)CC4)C3)ncc2)c1 MBYXEBXZARTUSS-QLWBXOBMSA-N 0.000 claims description 4
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims description 4
- HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims description 4
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 4
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 4
- 102000003964 Histone deacetylase Human genes 0.000 claims description 4
- 108090000353 Histone deacetylase Proteins 0.000 claims description 4
- 102000008394 Immunoglobulin Fragments Human genes 0.000 claims description 4
- 108010021625 Immunoglobulin Fragments Proteins 0.000 claims description 4
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 4
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims description 4
- 239000005517 L01XE01 - Imatinib Substances 0.000 claims description 4
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims description 4
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims description 4
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims description 4
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims description 4
- 239000002067 L01XE06 - Dasatinib Substances 0.000 claims description 4
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims description 4
- 239000005536 L01XE08 - Nilotinib Substances 0.000 claims description 4
- NNJVILVZKWQKPM-UHFFFAOYSA-N Lidocaine Chemical compound CCN(CC)CC(=O)NC1=C(C)C=CC=C1C NNJVILVZKWQKPM-UHFFFAOYSA-N 0.000 claims description 4
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 4
- 239000004472 Lysine Substances 0.000 claims description 4
- 229940122255 Microtubule inhibitor Drugs 0.000 claims description 4
- 229930192392 Mitomycin Natural products 0.000 claims description 4
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims description 4
- 229930012538 Paclitaxel Natural products 0.000 claims description 4
- 229940124158 Protease/peptidase inhibitor Drugs 0.000 claims description 4
- 229940079156 Proteasome inhibitor Drugs 0.000 claims description 4
- AUVVAXYIELKVAI-UHFFFAOYSA-N SJ000285215 Natural products N1CCC2=CC(OC)=C(OC)C=C2C1CC1CC2C3=CC(OC)=C(OC)C=C3CCN2CC1CC AUVVAXYIELKVAI-UHFFFAOYSA-N 0.000 claims description 4
- 108020004459 Small interfering RNA Proteins 0.000 claims description 4
- CBPNZQVSJQDFBE-FUXHJELOSA-N Temsirolimus Chemical compound C1C[C@@H](OC(=O)C(C)(CO)CO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 CBPNZQVSJQDFBE-FUXHJELOSA-N 0.000 claims description 4
- JXLYSJRDGCGARV-WWYNWVTFSA-N Vinblastine Natural products O=C(O[C@H]1[C@](O)(C(=O)OC)[C@@H]2N(C)c3c(cc(c(OC)c3)[C@]3(C(=O)OC)c4[nH]c5c(c4CCN4C[C@](O)(CC)C[C@H](C3)C4)cccc5)[C@@]32[C@H]2[C@@]1(CC)C=CCN2CC3)C JXLYSJRDGCGARV-WWYNWVTFSA-N 0.000 claims description 4
- 229940122803 Vinca alkaloid Drugs 0.000 claims description 4
- RJURFGZVJUQBHK-IIXSONLDSA-N actinomycin D Chemical compound C[C@H]1OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C(=O)[C@@H]2CCCN2C(=O)[C@@H](C(C)C)NC(=O)[C@H]1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)N[C@@H]4C(=O)N[C@@H](C(N5CCC[C@H]5C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-IIXSONLDSA-N 0.000 claims description 4
- 229940009456 adriamycin Drugs 0.000 claims description 4
- 150000008052 alkyl sulfonates Chemical class 0.000 claims description 4
- 229940100198 alkylating agent Drugs 0.000 claims description 4
- 239000002168 alkylating agent Substances 0.000 claims description 4
- 210000002255 anal canal Anatomy 0.000 claims description 4
- 239000004037 angiogenesis inhibitor Substances 0.000 claims description 4
- 229940121369 angiogenesis inhibitor Drugs 0.000 claims description 4
- 229940045799 anthracyclines and related substance Drugs 0.000 claims description 4
- 230000000340 anti-metabolite Effects 0.000 claims description 4
- 230000000692 anti-sense effect Effects 0.000 claims description 4
- 229940100197 antimetabolite Drugs 0.000 claims description 4
- 239000002256 antimetabolite Substances 0.000 claims description 4
- 239000002257 antimetastatic agent Substances 0.000 claims description 4
- 230000006907 apoptotic process Effects 0.000 claims description 4
- 229960002756 azacitidine Drugs 0.000 claims description 4
- RSIHSRDYCUFFLA-DYKIIFRCSA-N boldenone Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)O)[C@@H]4[C@@H]3CCC2=C1 RSIHSRDYCUFFLA-DYKIIFRCSA-N 0.000 claims description 4
- 229960001467 bortezomib Drugs 0.000 claims description 4
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims description 4
- 210000000481 breast Anatomy 0.000 claims description 4
- 229940124630 bronchodilator Drugs 0.000 claims description 4
- 229960004117 capecitabine Drugs 0.000 claims description 4
- 210000003679 cervix uteri Anatomy 0.000 claims description 4
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims description 4
- 229960004316 cisplatin Drugs 0.000 claims description 4
- 229960001338 colchicine Drugs 0.000 claims description 4
- 210000001072 colon Anatomy 0.000 claims description 4
- 229960004397 cyclophosphamide Drugs 0.000 claims description 4
- 102000003675 cytokine receptors Human genes 0.000 claims description 4
- 108010057085 cytokine receptors Proteins 0.000 claims description 4
- 229940127089 cytotoxic agent Drugs 0.000 claims description 4
- 239000002254 cytotoxic agent Substances 0.000 claims description 4
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 4
- 229960003901 dacarbazine Drugs 0.000 claims description 4
- 229960000640 dactinomycin Drugs 0.000 claims description 4
- 229960002448 dasatinib Drugs 0.000 claims description 4
- 229960000975 daunorubicin Drugs 0.000 claims description 4
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims description 4
- 238000006731 degradation reaction Methods 0.000 claims description 4
- RSIHSRDYCUFFLA-UHFFFAOYSA-N dehydrotestosterone Natural products O=C1C=CC2(C)C3CCC(C)(C(CC4)O)C4C3CCC2=C1 RSIHSRDYCUFFLA-UHFFFAOYSA-N 0.000 claims description 4
- 125000000600 disaccharide group Chemical group 0.000 claims description 4
- 239000003968 dna methyltransferase inhibitor Substances 0.000 claims description 4
- 239000003534 dna topoisomerase inhibitor Substances 0.000 claims description 4
- 229960004679 doxorubicin Drugs 0.000 claims description 4
- AUVVAXYIELKVAI-CKBKHPSWSA-N emetine Chemical compound N1CCC2=CC(OC)=C(OC)C=C2[C@H]1C[C@H]1C[C@H]2C3=CC(OC)=C(OC)C=C3CCN2C[C@@H]1CC AUVVAXYIELKVAI-CKBKHPSWSA-N 0.000 claims description 4
- 229960002694 emetine Drugs 0.000 claims description 4
- AUVVAXYIELKVAI-UWBTVBNJSA-N emetine Natural products N1CCC2=CC(OC)=C(OC)C=C2[C@H]1C[C@H]1C[C@H]2C3=CC(OC)=C(OC)C=C3CCN2C[C@H]1CC AUVVAXYIELKVAI-UWBTVBNJSA-N 0.000 claims description 4
- 210000004696 endometrium Anatomy 0.000 claims description 4
- 229960001904 epirubicin Drugs 0.000 claims description 4
- 229930013356 epothilone Natural products 0.000 claims description 4
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims description 4
- 229960001433 erlotinib Drugs 0.000 claims description 4
- 210000003238 esophagus Anatomy 0.000 claims description 4
- ZMMJGEGLRURXTF-UHFFFAOYSA-N ethidium bromide Chemical compound [Br-].C12=CC(N)=CC=C2C2=CC=C(N)C=C2[N+](CC)=C1C1=CC=CC=C1 ZMMJGEGLRURXTF-UHFFFAOYSA-N 0.000 claims description 4
- 229960005542 ethidium bromide Drugs 0.000 claims description 4
- 229960005420 etoposide Drugs 0.000 claims description 4
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims description 4
- 229960005167 everolimus Drugs 0.000 claims description 4
- 229960002949 fluorouracil Drugs 0.000 claims description 4
- 150000002224 folic acids Chemical class 0.000 claims description 4
- 102000037865 fusion proteins Human genes 0.000 claims description 4
- 108020001507 fusion proteins Proteins 0.000 claims description 4
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims description 4
- 229960002584 gefitinib Drugs 0.000 claims description 4
- SDUQYLNIPVEERB-QPPQHZFASA-N gemcitabine Chemical compound O=C1N=C(N)C=CN1[C@H]1C(F)(F)[C@H](O)[C@@H](CO)O1 SDUQYLNIPVEERB-QPPQHZFASA-N 0.000 claims description 4
- 229960005277 gemcitabine Drugs 0.000 claims description 4
- 210000004392 genitalia Anatomy 0.000 claims description 4
- 239000003862 glucocorticoid Substances 0.000 claims description 4
- 210000003128 head Anatomy 0.000 claims description 4
- 238000003384 imaging method Methods 0.000 claims description 4
- KTUFNOKKBVMGRW-UHFFFAOYSA-N imatinib Chemical compound C1CN(C)CCN1CC1=CC=C(C(=O)NC=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)C=C1 KTUFNOKKBVMGRW-UHFFFAOYSA-N 0.000 claims description 4
- 229960002411 imatinib Drugs 0.000 claims description 4
- 239000002955 immunomodulating agent Substances 0.000 claims description 4
- 229940121354 immunomodulator Drugs 0.000 claims description 4
- 230000002584 immunomodulator Effects 0.000 claims description 4
- 239000000138 intercalating agent Substances 0.000 claims description 4
- 229960004768 irinotecan Drugs 0.000 claims description 4
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims description 4
- 229960002014 ixabepilone Drugs 0.000 claims description 4
- FABUFPQFXZVHFB-CFWQTKTJSA-N ixabepilone Chemical compound C/C([C@@H]1C[C@@H]2O[C@]2(C)CCC[C@@H]([C@@H]([C@H](C)C(=O)C(C)(C)[C@H](O)CC(=O)N1)O)C)=C\C1=CSC(C)=N1 FABUFPQFXZVHFB-CFWQTKTJSA-N 0.000 claims description 4
- 210000003734 kidney Anatomy 0.000 claims description 4
- 229960004891 lapatinib Drugs 0.000 claims description 4
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims description 4
- 229960004194 lidocaine Drugs 0.000 claims description 4
- 210000004185 liver Anatomy 0.000 claims description 4
- 210000004072 lung Anatomy 0.000 claims description 4
- 229960003646 lysine Drugs 0.000 claims description 4
- HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical class ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims description 4
- 229960004961 mechlorethamine Drugs 0.000 claims description 4
- 229960000485 methotrexate Drugs 0.000 claims description 4
- 231100000782 microtubule inhibitor Toxicity 0.000 claims description 4
- CFCUWKMKBJTWLW-BKHRDMLASA-N mithramycin Chemical compound O([C@@H]1C[C@@H](O[C@H](C)[C@H]1O)OC=1C=C2C=C3C[C@H]([C@@H](C(=O)C3=C(O)C2=C(O)C=1C)O[C@@H]1O[C@H](C)[C@@H](O)[C@H](O[C@@H]2O[C@H](C)[C@H](O)[C@H](O[C@@H]3O[C@H](C)[C@@H](O)[C@@](C)(O)C3)C2)C1)[C@H](OC)C(=O)[C@@H](O)[C@@H](C)O)[C@H]1C[C@@H](O)[C@H](O)[C@@H](C)O1 CFCUWKMKBJTWLW-BKHRDMLASA-N 0.000 claims description 4
- 229960004857 mitomycin Drugs 0.000 claims description 4
- 229960001156 mitoxantrone Drugs 0.000 claims description 4
- KKZJGLLVHKMTCM-UHFFFAOYSA-N mitoxantrone Chemical compound O=C1C2=C(O)C=CC(O)=C2C(=O)C2=C1C(NCCNCCO)=CC=C2NCCNCCO KKZJGLLVHKMTCM-UHFFFAOYSA-N 0.000 claims description 4
- 210000000214 mouth Anatomy 0.000 claims description 4
- 210000003739 neck Anatomy 0.000 claims description 4
- 210000002569 neuron Anatomy 0.000 claims description 4
- HHZIURLSWUIHRB-UHFFFAOYSA-N nilotinib Chemical compound C1=NC(C)=CN1C1=CC(NC(=O)C=2C=C(NC=3N=C(C=CN=3)C=3C=NC=CC=3)C(C)=CC=2)=CC(C(F)(F)F)=C1 HHZIURLSWUIHRB-UHFFFAOYSA-N 0.000 claims description 4
- 229960001346 nilotinib Drugs 0.000 claims description 4
- OSTGTTZJOCZWJG-UHFFFAOYSA-N nitrosourea Chemical compound NC(=O)N=NO OSTGTTZJOCZWJG-UHFFFAOYSA-N 0.000 claims description 4
- 239000003865 nucleic acid synthesis inhibitor Substances 0.000 claims description 4
- 210000001672 ovary Anatomy 0.000 claims description 4
- 229960001592 paclitaxel Drugs 0.000 claims description 4
- 210000000496 pancreas Anatomy 0.000 claims description 4
- 239000000137 peptide hydrolase inhibitor Substances 0.000 claims description 4
- 210000003800 pharynx Anatomy 0.000 claims description 4
- 229960003171 plicamycin Drugs 0.000 claims description 4
- 229960004919 procaine Drugs 0.000 claims description 4
- MFDFERRIHVXMIY-UHFFFAOYSA-N procaine Chemical compound CCN(CC)CCOC(=O)C1=CC=C(N)C=C1 MFDFERRIHVXMIY-UHFFFAOYSA-N 0.000 claims description 4
- 229960003712 propranolol Drugs 0.000 claims description 4
- 210000002307 prostate Anatomy 0.000 claims description 4
- 239000003207 proteasome inhibitor Substances 0.000 claims description 4
- 238000001243 protein synthesis Methods 0.000 claims description 4
- 230000017854 proteolysis Effects 0.000 claims description 4
- 229950010131 puromycin Drugs 0.000 claims description 4
- ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims description 4
- 210000000664 rectum Anatomy 0.000 claims description 4
- QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims description 4
- 229960002930 sirolimus Drugs 0.000 claims description 4
- 210000000813 small intestine Anatomy 0.000 claims description 4
- 229960003787 sorafenib Drugs 0.000 claims description 4
- 150000003431 steroids Chemical class 0.000 claims description 4
- 210000002784 stomach Anatomy 0.000 claims description 4
- WINHZLLDWRZWRT-ATVHPVEESA-N sunitinib Chemical compound CCN(CC)CCNC(=O)C1=C(C)NC(\C=C/2C3=CC(F)=CC=C3NC\2=O)=C1C WINHZLLDWRZWRT-ATVHPVEESA-N 0.000 claims description 4
- 229960001796 sunitinib Drugs 0.000 claims description 4
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims description 4
- 229960000235 temsirolimus Drugs 0.000 claims description 4
- QFJCIRLUMZQUOT-UHFFFAOYSA-N temsirolimus Natural products C1CC(O)C(OC)CC1CC(C)C1OC(=O)C2CCCCN2C(=O)C(=O)C(O)(O2)C(C)CCC2CC(OC)C(C)=CC=CC=CC(C)CC(C)C(=O)C(OC)C(O)C(C)=CC(C)C(=O)C1 QFJCIRLUMZQUOT-UHFFFAOYSA-N 0.000 claims description 4
- 229960001278 teniposide Drugs 0.000 claims description 4
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims description 4
- 210000001550 testis Anatomy 0.000 claims description 4
- 229960002372 tetracaine Drugs 0.000 claims description 4
- GKCBAIGFKIBETG-UHFFFAOYSA-N tetracaine Chemical compound CCCCNC1=CC=C(C(=O)OCCN(C)C)C=C1 GKCBAIGFKIBETG-UHFFFAOYSA-N 0.000 claims description 4
- 210000001685 thyroid gland Anatomy 0.000 claims description 4
- 229940044693 topoisomerase inhibitor Drugs 0.000 claims description 4
- 229960000303 topotecan Drugs 0.000 claims description 4
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims description 4
- 230000014616 translation Effects 0.000 claims description 4
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims description 4
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims description 4
- 150000004917 tyrosine kinase inhibitor derivatives Chemical class 0.000 claims description 4
- 210000003932 urinary bladder Anatomy 0.000 claims description 4
- 210000004291 uterus Anatomy 0.000 claims description 4
- 229960005486 vaccine Drugs 0.000 claims description 4
- 229960003048 vinblastine Drugs 0.000 claims description 4
- JXLYSJRDGCGARV-XQKSVPLYSA-N vincaleukoblastine Chemical compound C([C@@H](C[C@]1(C(=O)OC)C=2C(=CC3=C([C@]45[C@H]([C@@]([C@H](OC(C)=O)[C@]6(CC)C=CCN([C@H]56)CC4)(O)C(=O)OC)N3C)C=2)OC)C[C@@](C2)(O)CC)N2CCC2=C1NC1=CC=CC=C21 JXLYSJRDGCGARV-XQKSVPLYSA-N 0.000 claims description 4
- 229960004528 vincristine Drugs 0.000 claims description 4
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims description 4
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims description 4
- 229960002066 vinorelbine Drugs 0.000 claims description 4
- GBABOYUKABKIAF-GHYRFKGUSA-N vinorelbine Chemical compound C1N(CC=2C3=CC=CC=C3NC=22)CC(CC)=C[C@H]1C[C@]2(C(=O)OC)C1=CC([C@]23[C@H]([C@]([C@H](OC(C)=O)[C@]4(CC)C=CCN([C@H]34)CC2)(O)C(=O)OC)N2C)=C2C=C1OC GBABOYUKABKIAF-GHYRFKGUSA-N 0.000 claims description 4
- 229960000237 vorinostat Drugs 0.000 claims description 4
- WAEXFXRVDQXREF-UHFFFAOYSA-N vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims description 4
- 208000010668 atopic eczema Diseases 0.000 claims description 3
- 206010006451 bronchitis Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- HESCAJZNRMSMJG-KKQRBIROSA-N epothilone A Chemical class C/C([C@@H]1C[C@@H]2O[C@@H]2CCC[C@@H]([C@@H]([C@@H](C)C(=O)C(C)(C)[C@@H](O)CC(=O)O1)O)C)=C\C1=CSC(C)=N1 HESCAJZNRMSMJG-KKQRBIROSA-N 0.000 claims description 3
- 230000003176 fibrotic effect Effects 0.000 claims description 3
- 210000005095 gastrointestinal system Anatomy 0.000 claims description 3
- 210000002751 lymph Anatomy 0.000 claims description 3
- 206010061289 metastatic neoplasm Diseases 0.000 claims description 3
- 201000008261 skin carcinoma Diseases 0.000 claims description 3
- 210000003741 urothelium Anatomy 0.000 claims description 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 2
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 2
- 208000011231 Crohn disease Diseases 0.000 claims description 2
- 229940126190 DNA methyltransferase inhibitor Drugs 0.000 claims description 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims description 2
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims description 2
- 206010020751 Hypersensitivity Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 206010029164 Nephrotic syndrome Diseases 0.000 claims description 2
- 201000004681 Psoriasis Diseases 0.000 claims description 2
- 108091028664 Ribonucleotide Proteins 0.000 claims description 2
- 208000021386 Sjogren Syndrome Diseases 0.000 claims description 2
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 2
- 208000024780 Urticaria Diseases 0.000 claims description 2
- 206010046851 Uveitis Diseases 0.000 claims description 2
- 229940045714 alkyl sulfonate alkylating agent Drugs 0.000 claims description 2
- 230000000172 allergic effect Effects 0.000 claims description 2
- 230000007815 allergy Effects 0.000 claims description 2
- 230000003510 anti-fibrotic effect Effects 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 210000004369 blood Anatomy 0.000 claims description 2
- 239000008280 blood Substances 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 230000005713 exacerbation Effects 0.000 claims description 2
- 208000024908 graft versus host disease Diseases 0.000 claims description 2
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims description 2
- 229940121372 histone deacetylase inhibitor Drugs 0.000 claims description 2
- 239000000411 inducer Substances 0.000 claims description 2
- 230000001939 inductive effect Effects 0.000 claims description 2
- 206010025135 lupus erythematosus Diseases 0.000 claims description 2
- 230000001394 metastastic effect Effects 0.000 claims description 2
- 230000011278 mitosis Effects 0.000 claims description 2
- 230000000394 mitotic effect Effects 0.000 claims description 2
- 201000006417 multiple sclerosis Diseases 0.000 claims description 2
- 239000002777 nucleoside Substances 0.000 claims description 2
- 229940127073 nucleoside analogue Drugs 0.000 claims description 2
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 2
- 239000002773 nucleotide Substances 0.000 claims description 2
- 125000003729 nucleotide group Chemical group 0.000 claims description 2
- 206010039083 rhinitis Diseases 0.000 claims description 2
- 239000002336 ribonucleotide Substances 0.000 claims description 2
- 125000002652 ribonucleotide group Chemical group 0.000 claims description 2
- 230000019491 signal transduction Effects 0.000 claims description 2
- 230000011664 signaling Effects 0.000 claims description 2
- AYNNSCRYTDRFCP-UHFFFAOYSA-N triazene Chemical compound NN=N AYNNSCRYTDRFCP-UHFFFAOYSA-N 0.000 claims description 2
- 150000004654 triazenes Chemical class 0.000 claims description 2
- 210000004027 cell Anatomy 0.000 claims 2
- 210000003169 central nervous system Anatomy 0.000 claims 2
- 210000001635 urinary tract Anatomy 0.000 claims 2
- MCHWWJLLPNDHGL-KVTDHHQDSA-N (2r,3s,4s,5r)-2,5-bis(hydroxymethyl)oxolane-3,4-diol Chemical group OC[C@H]1O[C@H](CO)[C@@H](O)[C@@H]1O MCHWWJLLPNDHGL-KVTDHHQDSA-N 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- 201000009961 allergic asthma Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000007850 fluorescent dye Substances 0.000 claims 1
- 230000002496 gastric effect Effects 0.000 claims 1
- 201000010659 intrinsic asthma Diseases 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000004477 skin sarcoma Diseases 0.000 claims 1
- 230000002485 urinary effect Effects 0.000 claims 1
- HTTJABKRGRZYRN-UHFFFAOYSA-N Heparin Chemical compound OC1C(NC(=O)C)C(O)OC(COS(O)(=O)=O)C1OC1C(OS(O)(=O)=O)C(O)C(OC2C(C(OS(O)(=O)=O)C(OC3C(C(O)C(O)C(O3)C(O)=O)OS(O)(=O)=O)C(CO)O2)NS(O)(=O)=O)C(C(O)=O)O1 HTTJABKRGRZYRN-UHFFFAOYSA-N 0.000 description 28
- 238000000034 method Methods 0.000 description 22
- 230000014508 negative regulation of coagulation Effects 0.000 description 6
- 0 *C(C(CC*=C)CO)OCC(CCN)CO Chemical compound *C(C(CC*=C)CO)OCC(CCN)CO 0.000 description 4
- 206010027476 Metastases Diseases 0.000 description 3
- 230000002401 inhibitory effect Effects 0.000 description 3
- 230000009401 metastasis Effects 0.000 description 3
- 208000032612 Glial tumor Diseases 0.000 description 2
- 206010018338 Glioma Diseases 0.000 description 2
- 241001465754 Metazoa Species 0.000 description 2
- 206010029260 Neuroblastoma Diseases 0.000 description 2
- 102100040247 Tumor necrosis factor Human genes 0.000 description 2
- 201000001441 melanoma Diseases 0.000 description 2
- 210000004498 neuroglial cell Anatomy 0.000 description 2
- 241000283690 Bos taurus Species 0.000 description 1
- 206010006458 Bronchitis chronic Diseases 0.000 description 1
- 241000282472 Canis lupus familiaris Species 0.000 description 1
- 241000283707 Capra Species 0.000 description 1
- 241000700198 Cavia Species 0.000 description 1
- 241000283086 Equidae Species 0.000 description 1
- 241000282326 Felis catus Species 0.000 description 1
- 102000014150 Interferons Human genes 0.000 description 1
- 108010050904 Interferons Proteins 0.000 description 1
- 241000699670 Mus sp. Species 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 241001494479 Pecora Species 0.000 description 1
- 241000288906 Primates Species 0.000 description 1
- 241000700159 Rattus Species 0.000 description 1
- 229940123934 Reductase inhibitor Drugs 0.000 description 1
- 101000935814 Salmonella typhimurium (strain LT2 / SGSC1412 / ATCC 700720) Periplasmic beta-glucosidase Proteins 0.000 description 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 1
- 241000282887 Suidae Species 0.000 description 1
- 229940123155 T cell inhibitor Drugs 0.000 description 1
- 108060008683 Tumor Necrosis Factor Receptor Proteins 0.000 description 1
- 208000024716 acute asthma Diseases 0.000 description 1
- 208000009956 adenocarcinoma Diseases 0.000 description 1
- 208000026935 allergic disease Diseases 0.000 description 1
- 238000010171 animal model Methods 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000000903 blocking effect Effects 0.000 description 1
- 208000007451 chronic bronchitis Diseases 0.000 description 1
- 230000000779 depleting effect Effects 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 150000003883 epothilone derivatives Chemical class 0.000 description 1
- 239000003102 growth factor Substances 0.000 description 1
- 210000003494 hepatocyte Anatomy 0.000 description 1
- 229940079322 interferon Drugs 0.000 description 1
- 208000011645 metastatic carcinoma Diseases 0.000 description 1
- 230000001537 neural effect Effects 0.000 description 1
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 description 1
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
- 206010041823 squamous cell carcinoma Diseases 0.000 description 1
- 229940046728 tumor necrosis factor alpha inhibitor Drugs 0.000 description 1
- 239000002451 tumor necrosis factor inhibitor Substances 0.000 description 1
- 102000003298 tumor necrosis factor receptor Human genes 0.000 description 1
- 208000010576 undifferentiated carcinoma Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US32514610P | 2010-04-16 | 2010-04-16 | |
| US61/325,146 | 2010-04-16 | ||
| PCT/US2011/032771 WO2011130697A2 (en) | 2010-04-16 | 2011-04-15 | Tissue targeting |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013527158A JP2013527158A (ja) | 2013-06-27 |
| JP2013527158A5 true JP2013527158A5 (https=) | 2014-05-29 |
| JP5982361B2 JP5982361B2 (ja) | 2016-08-31 |
Family
ID=44799366
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013505200A Active JP5982361B2 (ja) | 2010-04-16 | 2011-04-15 | 組織標的化方法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US9387256B2 (https=) |
| EP (1) | EP2558506B1 (https=) |
| JP (1) | JP5982361B2 (https=) |
| CN (1) | CN102985443B (https=) |
| BR (1) | BR112012026542A2 (https=) |
| CA (1) | CA2795360A1 (https=) |
| WO (1) | WO2011130697A2 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104142405A (zh) * | 2014-07-31 | 2014-11-12 | 温州市中心医院 | 硼替佐米对k562细胞株中dna甲基转移酶表达的检测方法 |
| CN107802833A (zh) * | 2016-09-09 | 2018-03-16 | 埃提斯生物技术(上海)有限公司 | 赫赛汀、依维莫司和长春瑞滨的药物组合 |
| WO2019222272A1 (en) | 2018-05-14 | 2019-11-21 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| CN113811333B (zh) | 2019-05-14 | 2024-03-12 | 诺维逊生物股份有限公司 | 靶向抗癌核激素受体的化合物 |
| WO2021097046A1 (en) | 2019-11-13 | 2021-05-20 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
| KR20230160299A (ko) | 2021-03-23 | 2023-11-23 | 누베이션 바이오 인크. | 항암 핵 호르몬 수용체 표적화 화합물 |
| US12006314B2 (en) | 2021-05-03 | 2024-06-11 | Nuvation Bio Inc. | Anti-cancer nuclear hormone receptor-targeting compounds |
Family Cites Families (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BE620906A (https=) | ||||
| US3118816A (en) | 1962-04-03 | 1964-01-21 | Abbott Lab | N-succinyl heparin and process |
| US4235871A (en) | 1978-02-24 | 1980-11-25 | Papahadjopoulos Demetrios P | Method of encapsulating biologically active materials in lipid vesicles |
| CA1136620A (en) | 1979-01-08 | 1982-11-30 | Ulf P.F. Lindahl | Heparin fragments having selective anticoagulation activity |
| FR2538404B1 (https=) | 1982-12-28 | 1985-08-23 | Anic Spa | |
| IT1195497B (it) | 1983-03-08 | 1988-10-19 | Opocrin Spa | Procedimento per la preparazione di frazioni oligosaccaridiche dotate di proprieta' farmacologiche per degradazione chimica di eparina |
| FR2553287B1 (fr) | 1983-10-18 | 1986-09-12 | Choay Sa | Compositions a base de mucopolysaccharides ou d'oligosaccharides, notamment a base de fractions ou fragments d'heparine, appropriees au traitement de desordres de la proliferation cellulaire |
| IT1169888B (it) | 1983-10-25 | 1987-06-03 | Italfarmaco Spa | Glicosaminoglicani modificati dotati di attivita' antitrombotica |
| US4916219A (en) | 1985-03-28 | 1990-04-10 | University Of Iowa Research Foundation | Oligosaccharide heparin fragments as inhibitors of complement cascade |
| US4847338A (en) | 1985-03-28 | 1989-07-11 | University Of Iowa Research Foundation | Low molecular weight heparin fragments as inhibitors of complement activation |
| US4868103A (en) | 1986-02-19 | 1989-09-19 | Enzo Biochem, Inc. | Analyte detection by means of energy transfer |
| US5262403A (en) | 1986-03-10 | 1993-11-16 | Board Of Regents, The University Of Texas System | Glycosaminoglycan derivatives and their use as inhibitors of tumor invasiveness of metastatic profusion-II |
| US5541166A (en) | 1987-01-23 | 1996-07-30 | The Australian National University | Sulphated polysaccharides having anti-metastatic and/or anti-inflammatory activity |
| US5668116A (en) | 1987-03-19 | 1997-09-16 | Anthropharm Pty. Limited | Anti-inflammatory compounds and compositions |
| FR2614026B1 (fr) | 1987-04-16 | 1992-04-17 | Sanofi Sa | Heparines de bas poids moleculaire, a structure reguliere, leur preparation et leurs applications biologiques |
| US5264425A (en) | 1988-06-03 | 1993-11-23 | Italfarmaco S.P.A. | Glycosaminoglycan salts and pharmaceutical compositions containing them |
| IL86753A0 (en) | 1988-06-15 | 1988-11-30 | Hadassah Med Org | Pharmaceutical compositions for treatment of lupus |
| US5308617A (en) | 1988-08-10 | 1994-05-03 | Halzyme Ltd. | Protein heparin conjugates |
| DK191889D0 (da) | 1989-04-20 | 1989-04-20 | Bukh Meditec | Kosmetisk middel |
| SE9002550D0 (sv) | 1990-08-01 | 1990-08-01 | Kabivitrum Ab | Heparinfragment |
| IT1243987B (it) | 1990-10-29 | 1994-06-28 | Derivati Organici Lab | Procedimento per la preparazione di epossi-eparidi prodotti ottenuti ecomposizioni farmaceutiche che li contengono |
| US5250519A (en) | 1991-03-29 | 1993-10-05 | Glycomed Incorporated | Non-anticoagulant heparin derivatives |
| US5280016A (en) | 1991-03-29 | 1994-01-18 | Glycomed Incorporated | Non-anticoagulant heparin derivatives |
| SE9101155D0 (sv) | 1991-04-18 | 1991-04-18 | Kabi Pharmacia Ab | Novel heparin derivatives |
| IT1254216B (it) | 1992-02-25 | 1995-09-14 | Opocrin Spa | Derivati polisaccaridici di eparina, eparan solfato, loro frazioni e frammenti, procedimento per la loro preparazione e composizioni farmaceutiche che li contengono |
| US5668118A (en) | 1992-07-24 | 1997-09-16 | Cavalier Pharmaceuticals | Method of synthesis of 2-O-desulfated Heparin and use thereof for inhibition of elastase and Cathepspin G |
| US5696100A (en) | 1992-12-22 | 1997-12-09 | Glycomed Incorporated | Method for controlling O-desulfation of heparin and compositions produced thereby |
| US5296471A (en) | 1992-12-22 | 1994-03-22 | Glycomed Incorporated | Method for controlling o-desulfation of heparin and compositions produced thereby |
| EP0690720B1 (en) | 1993-03-12 | 2001-06-27 | XOMA Technology Ltd. | Therapeutic uses of bactericidal/permeability increasing protein products |
| IT1264709B1 (it) | 1993-07-12 | 1996-10-04 | Italfarmaco Spa | Derivati eparinici ad attivita' antimetastatica |
| US5583121A (en) | 1994-01-12 | 1996-12-10 | Michigan State University | Non-anticoagulant chemically modified heparinoids for treating hypovolemic shock and related shock syndromes |
| US6127347A (en) | 1994-01-12 | 2000-10-03 | Univ Michigan | Non-anticoagulant chemically modified heparinoids for treating hypovolemic shock and related shock syndromes |
| AU2435795A (en) | 1994-05-06 | 1995-11-29 | Glycomed Incorporated | O-desulfated heparin derivatives, methods of making and uses thereof |
| US6140481A (en) | 1994-07-01 | 2000-10-31 | Seikagaku Corporation | Process for producing desulfated polysaccharide, and desulfated heparin |
| US5733893A (en) | 1995-03-15 | 1998-03-31 | Washington University | Method of identifying molecules that regulate FGF activity |
| US6001820A (en) | 1995-03-31 | 1999-12-14 | Hamilton Civic Hospitals Research Development Inc. | Compositions and methods for inhibiting thrombogenesis |
| EP0735050B1 (en) | 1995-03-31 | 2002-09-25 | Hamilton Civic Hospitals Research Development, Inc. | Compositions for inhibiting thrombogenesis |
| US5744457A (en) | 1995-03-31 | 1998-04-28 | Hamilton Civic Hospitals Research Development Inc. | Compositions and methods for inhibiting thrombogenesis |
| US5690910A (en) | 1995-08-18 | 1997-11-25 | Baker Norton Pharmaceuticals, Inc. | Method for treating asthma |
| ES2231880T3 (es) | 1996-07-29 | 2005-05-16 | Paringenix, Inc. | Procedimiento para tratar el asma con heparina o-desulfatada. |
| US5767269A (en) | 1996-10-01 | 1998-06-16 | Hamilton Civic Hospitals Research Development Inc. | Processes for the preparation of low-affinity, low molecular weight heparins useful as antithrombotics |
| US6248334B1 (en) | 1997-01-08 | 2001-06-19 | Henry M. Jackson Foundation For The Advancement Of Military Medicine | Process for preparing conjugate vaccines including free protein and the conjugate vaccines, immunogens, and immunogenic reagents produced by this process |
| AUPO573697A0 (en) | 1997-03-20 | 1997-04-10 | Prince Henry's Institute Of Medical Research | Diagnosis of endometrial cancer |
| US6596705B1 (en) | 1998-02-09 | 2003-07-22 | The Regents Of The University Of California | Inhibition of L-selectin and P-selection mediated binding using heparin |
| US6656922B2 (en) | 1998-05-28 | 2003-12-02 | Mediplex Corporation, Korea | Oral delivery of macromolecules |
| KR100314496B1 (ko) | 1998-05-28 | 2001-11-22 | 윤동진 | 항혈전성이 있는 헤파린 유도체, 그의 제조방법 및 용도 |
| US7781416B2 (en) | 2000-01-25 | 2010-08-24 | Sigma-Tau Research Switzerland S.A. | Derivatives of partially desulphated glycosaminoglycans as heparanase inhibitors, endowed with antiangiogenic activity and devoid of anticoagulating effect |
| IT1316986B1 (it) | 2000-01-25 | 2003-05-26 | Sigma Tau Ind Farmaceuti | Derivati glicosamminoglicani parzialmente desolfatati nonanticoagulanti ad attivita' antiangiogenica. |
| US6749865B2 (en) | 2000-02-15 | 2004-06-15 | Genzyme Corporation | Modification of biopolymers for improved drug delivery |
| CN1197587C (zh) | 2000-06-09 | 2005-04-20 | 中国科学院上海细胞生物学研究所 | N-位脱硫酸肝素在预防和治疗炎症中的应用 |
| US6514866B2 (en) | 2001-01-12 | 2003-02-04 | North Carolina State University | Chemically enhanced focused ion beam micro-machining of copper |
| BRPI0101486B1 (pt) | 2001-04-17 | 2017-09-19 | Cristália Produtos Químicos Farmacêuticos Ltda. | Pharmaceutical composition for topic use containing heparin for the treatment of skin or mucosal injuries caused by burns |
| SK288335B6 (sk) | 2001-09-12 | 2016-02-02 | Sigma-Tau Research Switzerland S.A. | Čiastočne alebo úplne N-desulfatovaný, N-reacetylovaný heparín, spôsob jeho prípravy, jeho použitie na prípravu liečiva s inhibičným účinkom na heparanázu, s antiangiogénnym a protizápalovým účinkom a farmaceutický prostriedok s jeho obsahom |
| US7575886B2 (en) | 2002-03-11 | 2009-08-18 | Momenta Pharmaceuticals, Inc. | Analysis of sulfated polysaccharides |
| EP1551852A4 (en) * | 2002-04-25 | 2007-03-21 | Momenta Pharmaceuticals Inc | METHOD AND PRODUCTS FOR MUCOSAL DELIVERY |
| US8071569B2 (en) | 2002-09-20 | 2011-12-06 | Mousa Shaker A | Oxidized heparin fractions and their use in inhibiting angiogenesis |
| US7964439B2 (en) | 2002-12-20 | 2011-06-21 | The Trustees Of Princeton University | Methods of fabricating devices by transfer of organic material |
| WO2004113278A2 (en) | 2003-05-20 | 2004-12-29 | Genentech, Inc. | Acylsulfamide inhibitors of factor viia |
| US7560444B2 (en) * | 2003-10-01 | 2009-07-14 | Momenta Pharmaceuticals, Inc. | Polysaccharides for pulmonary delivery of active agents |
| FR2866650B1 (fr) | 2004-02-24 | 2006-04-28 | Aventis Pharma Sa | Oligosaccharides, procede de preparation, utilisation et compositions pharmaceutiques les renfermant |
| US20050282775A1 (en) | 2004-06-16 | 2005-12-22 | Paringenix, Inc. | Method and medicament for sulfated polysaccharide treatment of inflammation without inducing platelet activation and heparin-induced thrombocytopenia syndrome |
| US20060040896A1 (en) | 2004-08-18 | 2006-02-23 | Paringenix, Inc. | Method and medicament for anticoagulation using a sulfated polysaccharide with enhanced anti-inflammatory activity |
| ZA200801696B (en) | 2005-07-22 | 2009-08-26 | Univ California | Heparin compositions and selection inhibition |
| US7517856B2 (en) | 2005-10-11 | 2009-04-14 | Ben-Gurion University Of The Negev Research And Development Authority | Bioconjugates comprising sulfated polysaccharides and their uses |
| US7767420B2 (en) | 2005-11-03 | 2010-08-03 | Momenta Pharmaceuticals, Inc. | Heparan sulfate glycosaminoglycan lyase and uses thereof |
| AU2006315348A1 (en) | 2005-11-16 | 2007-05-24 | Beth Israel Deaconess Medical Center | Method to assess breast cancer risk |
| CN101495517B (zh) * | 2006-05-25 | 2012-10-10 | 莫曼塔医药品有限公司 | 低分子量肝素及其用途 |
| EP1867995A1 (en) | 2006-06-15 | 2007-12-19 | Cézanne S.A.S. | In vitro method for diagnosing and monitoring metastasized bladder cancer using the determination of MMP-7 in the circulation of patients |
| US10166271B2 (en) | 2006-06-21 | 2019-01-01 | The Regents Of The University Of California | Methods for promoting hair growth |
| JP4964577B2 (ja) | 2006-12-15 | 2012-07-04 | 有限会社応用糖質化学研究所 | 親脂質性ヘパリン修飾体、その製造方法及び毛髪成長促進剤 |
| FR2912409B1 (fr) | 2007-02-14 | 2012-08-24 | Sanofi Aventis | Heparines de bas poids moleculaire comprenant au moins une liaison covalente avec la biotine ou un derive de la biotine leur procede de preparation,leur utilisation |
| US8088753B2 (en) | 2007-06-29 | 2012-01-03 | Mediplex Corporation, Korea | Heparin conjugates and methods |
| US20090012165A1 (en) | 2007-07-03 | 2009-01-08 | Sucampo Ag | Pharmaceutical combination of nsaid and prostaglandin compound |
| WO2009007224A1 (en) | 2007-07-10 | 2009-01-15 | Sigma-Tau Industrie Farmaceutiche Riunite S.P.A. | Low molecular weight heparin derivatives having neuroprotective activity |
| US8592393B2 (en) | 2007-11-02 | 2013-11-26 | Momenta Pharmaceuticals, Inc. | Polysaccharide compositions and methods of use for the treatment and prevention of disorders associated with progenitor cell mobilization |
| US8569262B2 (en) | 2007-11-02 | 2013-10-29 | Momenta Pharmaceuticals, Inc. | Polysaccharide compositions and methods of use for the treatment and prevention of disorders associated with progenitor cell mobilization |
| EP2207811B1 (en) * | 2007-11-02 | 2017-01-04 | Momenta Pharmaceuticals, Inc. | Non-anticoagulant polysaccharide compositions |
| WO2009105522A1 (en) | 2008-02-20 | 2009-08-27 | Momenta Pharmaceuticals, Inc. | Methods of making low molecular weight heparin compositions |
| JP5421366B2 (ja) | 2008-07-21 | 2014-02-19 | オトノミ―,インク. | 制御放出性の耳の構造体調節および生来の免疫システム調節化合物および耳の障害の処置のための方法 |
| US20100331746A1 (en) | 2009-02-20 | 2010-12-30 | Aventis Pharma S.A. | Method of using enoxaparin for reducing the risk of death in acutely ill medical patients |
| US8435795B2 (en) | 2010-01-19 | 2013-05-07 | Momenta Pharmaceuticals, Inc. | Evaluating heparin preparations |
-
2011
- 2011-04-15 BR BR112012026542A patent/BR112012026542A2/pt not_active Application Discontinuation
- 2011-04-15 CN CN201180019382.7A patent/CN102985443B/zh not_active Expired - Fee Related
- 2011-04-15 CA CA2795360A patent/CA2795360A1/en not_active Abandoned
- 2011-04-15 EP EP11769718.5A patent/EP2558506B1/en active Active
- 2011-04-15 US US13/641,278 patent/US9387256B2/en active Active
- 2011-04-15 JP JP2013505200A patent/JP5982361B2/ja active Active
- 2011-04-15 WO PCT/US2011/032771 patent/WO2011130697A2/en not_active Ceased
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013527158A5 (https=) | ||
| IL277783B1 (en) | Shp2 inhibitor compositions, methods for treating cancer and methods for identifying a subject with shp2 mutations | |
| ES2688938T3 (es) | Combinaciones de agente antifolato y metoxiamina en el tratamiento del cáncer | |
| JP5860874B2 (ja) | 核酸コンジュゲートのためのエンドソーム溶解剤を用いた最適化invivo送達システム | |
| TW202216208A (zh) | 抗體-藥物結合物及atr抑制劑之組合 | |
| HRP20181646T2 (hr) | Konjugati pirolobenzodiazepin - anti-psma protutijela | |
| JP2015534577A5 (https=) | ||
| JP2015534578A5 (https=) | ||
| EP2953938B1 (en) | Functionalised benzopyran compounds and use thereof | |
| US20250249114A1 (en) | Method for treating her2-positive solid tumor | |
| TW202042844A (zh) | 模式辨別受體(pattern recognition receptor)促效劑的共軛物 | |
| CN111936143A (zh) | 用于治疗癌症的微管蛋白聚合抑制剂和聚(adp-核糖)聚合酶(parp)抑制剂的新型联用药品 | |
| JP5982361B2 (ja) | 組織標的化方法 | |
| CN108348599A (zh) | 包含金属纳米粒子、连接物及抗体的复合物 | |
| CN113316452A (zh) | 先天性免疫激动剂的持续局部药物水平 | |
| TW202327652A (zh) | 抗trop-2抗體及parp抑制劑之組合療法 | |
| WO2020010900A1 (zh) | 化合物用于制备预防、治疗或改善疼痛的药物的用途 | |
| US20220054478A1 (en) | Minimization of systemic inflammation | |
| AU2020215801B2 (en) | Deoxy- cytidine or uridine derivatives for use in cancer therapies | |
| ES2784182T3 (es) | Composiciones y métodos para inducir la apoptosis | |
| Yi et al. | Folate-targeted hapten immunotherapy of adjuvant-induced arthritis: comparison of hapten potencies | |
| US20160193233A1 (en) | Dendrogenin a and antineoplastic agents for the treatment of chemosensitive or chemoresistant tumors | |
| CN106714795A (zh) | 用于治疗尤因家族肿瘤的组合物及方法 | |
| TW202317128A (zh) | 治療化療相關的胃腸道副作用的化合物和方法 | |
| US20190381026A1 (en) | In vivo amelioration of endogenous anti-tumor autoantibodies targeting surface tumor antigens via low-dose p4n |