HUE034923T2 - Makromolekuláris adagoló rendszerek artritisz és más gyulladásos betegségek nem-invazív leképezésére, kiértékelésére és kezelésére - Google Patents
Makromolekuláris adagoló rendszerek artritisz és más gyulladásos betegségek nem-invazív leképezésére, kiértékelésére és kezelésére Download PDFInfo
- Publication number
- HUE034923T2 HUE034923T2 HUE05732710A HUE05732710A HUE034923T2 HU E034923 T2 HUE034923 T2 HU E034923T2 HU E05732710 A HUE05732710 A HU E05732710A HU E05732710 A HUE05732710 A HU E05732710A HU E034923 T2 HUE034923 T2 HU E034923T2
- Authority
- HU
- Hungary
- Prior art keywords
- imaging
- composition
- targeting
- agent
- pharmaceutical composition
- Prior art date
Links
- 238000003384 imaging method Methods 0.000 title claims abstract description 41
- 208000027866 inflammatory disease Diseases 0.000 title claims abstract description 22
- 206010003246 arthritis Diseases 0.000 title claims description 33
- 238000011282 treatment Methods 0.000 title abstract description 27
- 238000011156 evaluation Methods 0.000 title abstract description 15
- 229920000642 polymer Polymers 0.000 claims abstract description 42
- 206010039073 rheumatoid arthritis Diseases 0.000 claims abstract description 40
- 206010061218 Inflammation Diseases 0.000 claims abstract description 31
- 230000004054 inflammatory process Effects 0.000 claims abstract description 31
- 230000002917 arthritic effect Effects 0.000 claims abstract description 25
- 239000000203 mixture Substances 0.000 claims description 86
- 239000003814 drug Substances 0.000 claims description 84
- 230000008685 targeting Effects 0.000 claims description 72
- 239000012216 imaging agent Substances 0.000 claims description 55
- 229920001577 copolymer Polymers 0.000 claims description 51
- 210000001519 tissue Anatomy 0.000 claims description 40
- 229940079593 drug Drugs 0.000 claims description 38
- 229940124597 therapeutic agent Drugs 0.000 claims description 37
- 210000001503 joint Anatomy 0.000 claims description 36
- 125000006850 spacer group Chemical group 0.000 claims description 36
- 239000008194 pharmaceutical composition Substances 0.000 claims description 35
- 238000000034 method Methods 0.000 claims description 34
- 239000003795 chemical substances by application Substances 0.000 claims description 33
- VHSHLMUCYSAUQU-UHFFFAOYSA-N 2-hydroxypropyl methacrylate Chemical compound CC(O)COC(=O)C(C)=C VHSHLMUCYSAUQU-UHFFFAOYSA-N 0.000 claims description 28
- 239000012634 fragment Substances 0.000 claims description 26
- 210000000988 bone and bone Anatomy 0.000 claims description 23
- 239000003862 glucocorticoid Substances 0.000 claims description 20
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 20
- 150000001875 compounds Chemical class 0.000 claims description 19
- 210000000845 cartilage Anatomy 0.000 claims description 18
- 229940021182 non-steroidal anti-inflammatory drug Drugs 0.000 claims description 17
- 230000001225 therapeutic effect Effects 0.000 claims description 17
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 16
- 238000004166 bioassay Methods 0.000 claims description 14
- 238000010171 animal model Methods 0.000 claims description 13
- 230000003110 anti-inflammatory effect Effects 0.000 claims description 13
- 102000004169 proteins and genes Human genes 0.000 claims description 13
- 108090000623 proteins and genes Proteins 0.000 claims description 13
- 238000002360 preparation method Methods 0.000 claims description 11
- 229940037128 systemic glucocorticoids Drugs 0.000 claims description 11
- 229940122361 Bisphosphonate Drugs 0.000 claims description 9
- 150000004663 bisphosphonates Chemical class 0.000 claims description 9
- PCHJSUWPFVWCPO-UHFFFAOYSA-N gold Chemical compound [Au] PCHJSUWPFVWCPO-UHFFFAOYSA-N 0.000 claims description 9
- 229910052737 gold Inorganic materials 0.000 claims description 9
- 239000010931 gold Substances 0.000 claims description 9
- 230000002757 inflammatory effect Effects 0.000 claims description 9
- 229920003169 water-soluble polymer Polymers 0.000 claims description 9
- 239000000126 substance Substances 0.000 claims description 7
- 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 6
- 150000002148 esters Chemical class 0.000 claims description 5
- 239000003112 inhibitor Substances 0.000 claims description 5
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 claims description 4
- 239000002253 acid Substances 0.000 claims description 4
- 238000003556 assay Methods 0.000 claims description 4
- 238000013507 mapping Methods 0.000 claims description 4
- 229960000485 methotrexate Drugs 0.000 claims description 4
- 125000001453 quaternary ammonium group Chemical group 0.000 claims description 4
- 238000002560 therapeutic procedure Methods 0.000 claims description 4
- 230000004044 response Effects 0.000 claims description 3
- 238000012360 testing method Methods 0.000 claims description 3
- 241000282326 Felis catus Species 0.000 claims description 2
- 230000003187 abdominal effect Effects 0.000 claims description 2
- 239000003125 aqueous solvent Substances 0.000 claims description 2
- 210000001165 lymph node Anatomy 0.000 claims description 2
- 239000000041 non-steroidal anti-inflammatory agent Substances 0.000 claims description 2
- 230000009467 reduction Effects 0.000 claims description 2
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical group N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 claims 2
- RYYVLZVUVIJVGH-UHFFFAOYSA-N caffeine Chemical compound CN1C(=O)N(C)C(=O)C2=C1N=CN2C RYYVLZVUVIJVGH-UHFFFAOYSA-N 0.000 claims 2
- 239000000463 material Substances 0.000 claims 2
- 206010003445 Ascites Diseases 0.000 claims 1
- 241000283690 Bos taurus Species 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- LPHGQDQBBGAPDZ-UHFFFAOYSA-N Isocaffeine Natural products CN1C(=O)N(C)C(=O)C2=C1N(C)C=N2 LPHGQDQBBGAPDZ-UHFFFAOYSA-N 0.000 claims 1
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 1
- 150000001412 amines Chemical class 0.000 claims 1
- 229910021529 ammonia Inorganic materials 0.000 claims 1
- 238000000137 annealing Methods 0.000 claims 1
- 239000005557 antagonist Substances 0.000 claims 1
- 230000004888 barrier function Effects 0.000 claims 1
- 244000309464 bull Species 0.000 claims 1
- 229960001948 caffeine Drugs 0.000 claims 1
- VJEONQKOZGKCAK-UHFFFAOYSA-N caffeine Natural products CN1C(=O)N(C)C(=O)C2=C1C=CN2C VJEONQKOZGKCAK-UHFFFAOYSA-N 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 210000003679 cervix uteri Anatomy 0.000 claims 1
- 239000000571 coke Substances 0.000 claims 1
- ALKZAGKDWUSJED-UHFFFAOYSA-N dinuclear copper ion Chemical compound [Cu].[Cu] ALKZAGKDWUSJED-UHFFFAOYSA-N 0.000 claims 1
- 210000000981 epithelium Anatomy 0.000 claims 1
- 239000004744 fabric Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 claims 1
- 230000012447 hatching Effects 0.000 claims 1
- 230000000366 juvenile effect Effects 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 238000005057 refrigeration Methods 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 238000001179 sorption measurement Methods 0.000 claims 1
- 239000004575 stone Substances 0.000 claims 1
- 238000011285 therapeutic regimen Methods 0.000 claims 1
- 102000035160 transmembrane proteins Human genes 0.000 claims 1
- 108091005703 transmembrane proteins Proteins 0.000 claims 1
- 230000002792 vascular Effects 0.000 claims 1
- 229940124549 vasodilator Drugs 0.000 claims 1
- 239000003071 vasodilator agent Substances 0.000 claims 1
- 230000009278 visceral effect Effects 0.000 claims 1
- 241000700159 Rattus Species 0.000 abstract description 78
- 208000009386 Experimental Arthritis Diseases 0.000 abstract description 58
- 239000002872 contrast media Substances 0.000 abstract description 28
- 238000009825 accumulation Methods 0.000 abstract description 17
- 230000014759 maintenance of location Effects 0.000 abstract description 10
- 229920002521 macromolecule Polymers 0.000 abstract description 7
- 230000000451 tissue damage Effects 0.000 abstract description 3
- 231100000827 tissue damage Toxicity 0.000 abstract description 3
- 238000002347 injection Methods 0.000 description 58
- 239000007924 injection Substances 0.000 description 58
- 229940090044 injection Drugs 0.000 description 56
- 238000002595 magnetic resonance imaging Methods 0.000 description 33
- 241001465754 Metazoa Species 0.000 description 25
- 230000000694 effects Effects 0.000 description 23
- 239000000562 conjugate Substances 0.000 description 20
- HZHFFEYYPYZMNU-UHFFFAOYSA-K gadodiamide Chemical compound [Gd+3].CNC(=O)CN(CC([O-])=O)CCN(CC([O-])=O)CCN(CC([O-])=O)CC(=O)NC HZHFFEYYPYZMNU-UHFFFAOYSA-K 0.000 description 17
- 210000000056 organ Anatomy 0.000 description 17
- 210000000544 articulatio talocruralis Anatomy 0.000 description 15
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 description 14
- 239000003435 antirheumatic agent Substances 0.000 description 14
- -1 chloriquine Substances 0.000 description 13
- 206010028980 Neoplasm Diseases 0.000 description 12
- 230000015572 biosynthetic process Effects 0.000 description 11
- UREBDLICKHMUKA-CXSFZGCWSA-N dexamethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O UREBDLICKHMUKA-CXSFZGCWSA-N 0.000 description 11
- 239000002988 disease modifying antirheumatic drug Substances 0.000 description 11
- 150000003839 salts Chemical class 0.000 description 11
- 238000001727 in vivo Methods 0.000 description 10
- 238000003786 synthesis reaction Methods 0.000 description 10
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 9
- RYGMFSIKBFXOCR-UHFFFAOYSA-N Copper Chemical compound [Cu] RYGMFSIKBFXOCR-UHFFFAOYSA-N 0.000 description 9
- 229960003957 dexamethasone Drugs 0.000 description 9
- 239000000975 dye Substances 0.000 description 9
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 8
- PLCQGRYPOISRTQ-FCJDYXGNSA-L dexamethasone sodium phosphate Chemical compound [Na+].[Na+].C1CC2=CC(=O)C=C[C@]2(C)[C@]2(F)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)COP([O-])([O-])=O)(O)[C@@]1(C)C[C@@H]2O PLCQGRYPOISRTQ-FCJDYXGNSA-L 0.000 description 8
- 238000012377 drug delivery Methods 0.000 description 8
- 230000004962 physiological condition Effects 0.000 description 8
- 102000004171 Cathepsin K Human genes 0.000 description 7
- 108090000625 Cathepsin K Proteins 0.000 description 7
- PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical compound CC[C@@H]1NC(=O)[C@H]([C@H](O)[C@H](C)C\C=C\C)N(C)C(=O)[C@H](C(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](CC(C)C)N(C)C(=O)[C@@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)N(C)C(=O)[C@H](C(C)C)NC(=O)[C@H](CC(C)C)N(C)C(=O)CN(C)C1=O PMATZTZNYRCHOR-CGLBZJNRSA-N 0.000 description 7
- 108010036949 Cyclosporine Proteins 0.000 description 7
- VVNCNSJFMMFHPL-VKHMYHEASA-N D-penicillamine Chemical compound CC(C)(S)[C@@H](N)C(O)=O VVNCNSJFMMFHPL-VKHMYHEASA-N 0.000 description 7
- 239000002616 MRI contrast agent Substances 0.000 description 7
- 210000003423 ankle Anatomy 0.000 description 7
- 229960001265 ciclosporin Drugs 0.000 description 7
- 229930182912 cyclosporin Natural products 0.000 description 7
- 230000006378 damage Effects 0.000 description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 7
- 210000003734 kidney Anatomy 0.000 description 7
- 210000004185 liver Anatomy 0.000 description 7
- 230000035699 permeability Effects 0.000 description 7
- NCEXYHBECQHGNR-UHFFFAOYSA-N sulfasalazine Natural products C1=C(O)C(C(=O)O)=CC(N=NC=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-UHFFFAOYSA-N 0.000 description 7
- 210000001258 synovial membrane Anatomy 0.000 description 7
- 210000005166 vasculature Anatomy 0.000 description 7
- 102000004190 Enzymes Human genes 0.000 description 6
- 108090000790 Enzymes Proteins 0.000 description 6
- 206010015866 Extravasation Diseases 0.000 description 6
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 6
- HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 6
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 6
- 229960002344 dexamethasone sodium phosphate Drugs 0.000 description 6
- 230000036251 extravasation Effects 0.000 description 6
- 210000003127 knee Anatomy 0.000 description 6
- 210000000629 knee joint Anatomy 0.000 description 6
- 239000001301 oxygen Substances 0.000 description 6
- 229910052760 oxygen Inorganic materials 0.000 description 6
- 229960001639 penicillamine Drugs 0.000 description 6
- 239000000243 solution Substances 0.000 description 6
- 210000000952 spleen Anatomy 0.000 description 6
- 210000003932 urinary bladder Anatomy 0.000 description 6
- OZAIFHULBGXAKX-UHFFFAOYSA-N 2-(2-cyanopropan-2-yldiazenyl)-2-methylpropanenitrile Chemical compound N#CC(C)(C)N=NC(C)(C)C#N OZAIFHULBGXAKX-UHFFFAOYSA-N 0.000 description 5
- 102000004506 Blood Proteins Human genes 0.000 description 5
- 108010017384 Blood Proteins Proteins 0.000 description 5
- UETNIIAIRMUTSM-UHFFFAOYSA-N Jacareubin Natural products CC1(C)OC2=CC3Oc4c(O)c(O)ccc4C(=O)C3C(=C2C=C1)O UETNIIAIRMUTSM-UHFFFAOYSA-N 0.000 description 5
- 102000002274 Matrix Metalloproteinases Human genes 0.000 description 5
- 108010000684 Matrix Metalloproteinases Proteins 0.000 description 5
- 241000219061 Rheum Species 0.000 description 5
- 108060008682 Tumor Necrosis Factor Proteins 0.000 description 5
- 239000002671 adjuvant Substances 0.000 description 5
- 229940124347 antiarthritic drug Drugs 0.000 description 5
- 239000002246 antineoplastic agent Substances 0.000 description 5
- 238000012550 audit Methods 0.000 description 5
- 230000008901 benefit Effects 0.000 description 5
- 210000004204 blood vessel Anatomy 0.000 description 5
- 238000002059 diagnostic imaging Methods 0.000 description 5
- 201000010099 disease Diseases 0.000 description 5
- 230000001965 increasing effect Effects 0.000 description 5
- OKPYIWASQZGASP-UHFFFAOYSA-N n-(2-hydroxypropyl)-2-methylprop-2-enamide Chemical compound CC(O)CNC(=O)C(C)=C OKPYIWASQZGASP-UHFFFAOYSA-N 0.000 description 5
- FEMOMIGRRWSMCU-UHFFFAOYSA-N ninhydrin Chemical compound C1=CC=C2C(=O)C(O)(O)C(=O)C2=C1 FEMOMIGRRWSMCU-UHFFFAOYSA-N 0.000 description 5
- 238000011552 rat model Methods 0.000 description 5
- 229960001940 sulfasalazine Drugs 0.000 description 5
- NCEXYHBECQHGNR-QZQOTICOSA-N sulfasalazine Chemical compound C1=C(O)C(C(=O)O)=CC(\N=N\C=2C=CC(=CC=2)S(=O)(=O)NC=2N=CC=CC=2)=C1 NCEXYHBECQHGNR-QZQOTICOSA-N 0.000 description 5
- 102000003390 tumor necrosis factor Human genes 0.000 description 5
- 230000000007 visual effect Effects 0.000 description 5
- WUBBRNOQWQTFEX-UHFFFAOYSA-N 4-aminosalicylic acid Chemical compound NC1=CC=C(C(O)=O)C(O)=C1 WUBBRNOQWQTFEX-UHFFFAOYSA-N 0.000 description 4
- 206010051728 Bone erosion Diseases 0.000 description 4
- COXVTLYNGOIATD-HVMBLDELSA-N CC1=C(C=CC(=C1)C1=CC(C)=C(C=C1)\N=N\C1=C(O)C2=C(N)C(=CC(=C2C=C1)S(O)(=O)=O)S(O)(=O)=O)\N=N\C1=CC=C2C(=CC(=C(N)C2=C1O)S(O)(=O)=O)S(O)(=O)=O Chemical compound CC1=C(C=CC(=C1)C1=CC(C)=C(C=C1)\N=N\C1=C(O)C2=C(N)C(=CC(=C2C=C1)S(O)(=O)=O)S(O)(=O)=O)\N=N\C1=CC=C2C(=CC(=C(N)C2=C1O)S(O)(=O)=O)S(O)(=O)=O COXVTLYNGOIATD-HVMBLDELSA-N 0.000 description 4
- CURLTUGMZLYLDI-UHFFFAOYSA-N Carbon dioxide Chemical compound O=C=O CURLTUGMZLYLDI-UHFFFAOYSA-N 0.000 description 4
- 229910052688 Gadolinium Inorganic materials 0.000 description 4
- 102000007562 Serum Albumin Human genes 0.000 description 4
- 108010071390 Serum Albumin Proteins 0.000 description 4
- 229960004909 aminosalicylic acid Drugs 0.000 description 4
- 238000013459 approach Methods 0.000 description 4
- 230000017531 blood circulation Effects 0.000 description 4
- 201000011510 cancer Diseases 0.000 description 4
- 230000007423 decrease Effects 0.000 description 4
- 229960003699 evans blue Drugs 0.000 description 4
- 210000002683 foot Anatomy 0.000 description 4
- UIWYJDYFSGRHKR-UHFFFAOYSA-N gadolinium atom Chemical compound [Gd] UIWYJDYFSGRHKR-UHFFFAOYSA-N 0.000 description 4
- 238000002354 inductively-coupled plasma atomic emission spectroscopy Methods 0.000 description 4
- 229910052500 inorganic mineral Inorganic materials 0.000 description 4
- 239000002502 liposome Substances 0.000 description 4
- 239000011707 mineral Substances 0.000 description 4
- 238000012544 monitoring process Methods 0.000 description 4
- 230000005298 paramagnetic effect Effects 0.000 description 4
- 210000000457 tarsus Anatomy 0.000 description 4
- 230000008728 vascular permeability Effects 0.000 description 4
- LJRDOKAZOAKLDU-UDXJMMFXSA-N (2s,3s,4r,5r,6r)-5-amino-2-(aminomethyl)-6-[(2r,3s,4r,5s)-5-[(1r,2r,3s,5r,6s)-3,5-diamino-2-[(2s,3r,4r,5s,6r)-3-amino-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-6-hydroxycyclohexyl]oxy-4-hydroxy-2-(hydroxymethyl)oxolan-3-yl]oxyoxane-3,4-diol;sulfuric ac Chemical compound OS(O)(=O)=O.N[C@@H]1[C@@H](O)[C@H](O)[C@H](CN)O[C@@H]1O[C@H]1[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](N)C[C@@H](N)[C@@H]2O)O[C@@H]2[C@@H]([C@@H](O)[C@H](O)[C@@H](CO)O2)N)O[C@@H]1CO LJRDOKAZOAKLDU-UDXJMMFXSA-N 0.000 description 3
- XSVWFLQICKPQAA-UHFFFAOYSA-N 2-[4,10-bis(carboxymethyl)-7-[2-(2,5-dioxopyrrolidin-1-yl)oxy-2-oxoethyl]-1,4,7,10-tetrazacyclododec-1-yl]acetic acid Chemical compound C1CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CCN1CC(=O)ON1C(=O)CCC1=O XSVWFLQICKPQAA-UHFFFAOYSA-N 0.000 description 3
- OZAIFHULBGXAKX-VAWYXSNFSA-N AIBN Substances N#CC(C)(C)\N=N\C(C)(C)C#N OZAIFHULBGXAKX-VAWYXSNFSA-N 0.000 description 3
- IAZDPXIOMUYVGZ-UHFFFAOYSA-N Dimethylsulphoxide Chemical compound CS(C)=O IAZDPXIOMUYVGZ-UHFFFAOYSA-N 0.000 description 3
- 229940119178 Interleukin 1 receptor antagonist Drugs 0.000 description 3
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 description 3
- 239000003708 ampul Substances 0.000 description 3
- 229940041181 antineoplastic drug Drugs 0.000 description 3
- 210000001185 bone marrow Anatomy 0.000 description 3
- 210000004027 cell Anatomy 0.000 description 3
- 208000037976 chronic inflammation Diseases 0.000 description 3
- 230000006020 chronic inflammation Effects 0.000 description 3
- 150000001879 copper Chemical class 0.000 description 3
- 229910052802 copper Inorganic materials 0.000 description 3
- 239000010949 copper Substances 0.000 description 3
- 230000003111 delayed effect Effects 0.000 description 3
- 238000009826 distribution Methods 0.000 description 3
- 230000009977 dual effect Effects 0.000 description 3
- 210000000610 foot bone Anatomy 0.000 description 3
- 230000008595 infiltration Effects 0.000 description 3
- 238000001764 infiltration Methods 0.000 description 3
- 230000005764 inhibitory process Effects 0.000 description 3
- 210000005067 joint tissue Anatomy 0.000 description 3
- 210000003141 lower extremity Anatomy 0.000 description 3
- 238000004519 manufacturing process Methods 0.000 description 3
- 239000011159 matrix material Substances 0.000 description 3
- 230000007246 mechanism Effects 0.000 description 3
- 238000002483 medication Methods 0.000 description 3
- 238000001000 micrograph Methods 0.000 description 3
- 201000008482 osteoarthritis Diseases 0.000 description 3
- 229960003330 pentetic acid Drugs 0.000 description 3
- 230000000144 pharmacologic effect Effects 0.000 description 3
- 239000000047 product Substances 0.000 description 3
- 230000001105 regulatory effect Effects 0.000 description 3
- 238000012552 review Methods 0.000 description 3
- SDKPSXWGRWWLKR-UHFFFAOYSA-M sodium;9,10-dioxoanthracene-1-sulfonate Chemical compound [Na+].O=C1C2=CC=CC=C2C(=O)C2=C1C=CC=C2S(=O)(=O)[O-] SDKPSXWGRWWLKR-UHFFFAOYSA-M 0.000 description 3
- 230000008961 swelling Effects 0.000 description 3
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 description 2
- WHTVZRBIWZFKQO-AWEZNQCLSA-N (S)-chloroquine Chemical compound ClC1=CC=C2C(N[C@@H](C)CCCN(CC)CC)=CC=NC2=C1 WHTVZRBIWZFKQO-AWEZNQCLSA-N 0.000 description 2
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 2
- 102000009027 Albumins Human genes 0.000 description 2
- 108010088751 Albumins Proteins 0.000 description 2
- 201000001320 Atherosclerosis Diseases 0.000 description 2
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 description 2
- 208000011231 Crohn disease Diseases 0.000 description 2
- 229930105110 Cyclosporin A Natural products 0.000 description 2
- 229920002307 Dextran Polymers 0.000 description 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- WSFSSNUMVMOOMR-UHFFFAOYSA-N Formaldehyde Chemical compound O=C WSFSSNUMVMOOMR-UHFFFAOYSA-N 0.000 description 2
- 101001076407 Homo sapiens Interleukin-1 receptor antagonist protein Proteins 0.000 description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 description 2
- 206010020772 Hypertension Diseases 0.000 description 2
- 102000051628 Interleukin-1 receptor antagonist Human genes 0.000 description 2
- 208000012659 Joint disease Diseases 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 2
- NQTADLQHYWFPDB-UHFFFAOYSA-N N-Hydroxysuccinimide Chemical compound ON1C(=O)CCC1=O NQTADLQHYWFPDB-UHFFFAOYSA-N 0.000 description 2
- PAKJLBYJIZAVQG-NSEZLWDYSA-N N[C@H]([C@H]1O)C(O)O[C@H](CO)[C@H]1O.N Chemical group N[C@H]([C@H]1O)C(O)O[C@H](CO)[C@H]1O.N PAKJLBYJIZAVQG-NSEZLWDYSA-N 0.000 description 2
- 238000011887 Necropsy Methods 0.000 description 2
- 201000004681 Psoriasis Diseases 0.000 description 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 description 2
- 208000036982 Spinal cord ischaemia Diseases 0.000 description 2
- 208000006011 Stroke Diseases 0.000 description 2
- 208000009205 Tinnitus Diseases 0.000 description 2
- 230000002159 abnormal effect Effects 0.000 description 2
- 229940009456 adriamycin Drugs 0.000 description 2
- 150000001413 amino acids Chemical class 0.000 description 2
- 238000004458 analytical method Methods 0.000 description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 description 2
- 239000002260 anti-inflammatory agent Substances 0.000 description 2
- 229940124599 anti-inflammatory drug Drugs 0.000 description 2
- 230000000703 anti-shock Effects 0.000 description 2
- 210000001188 articular cartilage Anatomy 0.000 description 2
- 208000006673 asthma Diseases 0.000 description 2
- 230000009286 beneficial effect Effects 0.000 description 2
- 210000004369 blood Anatomy 0.000 description 2
- 239000008280 blood Substances 0.000 description 2
- 239000001045 blue dye Substances 0.000 description 2
- 239000002775 capsule Substances 0.000 description 2
- 239000001569 carbon dioxide Substances 0.000 description 2
- 229910002092 carbon dioxide Inorganic materials 0.000 description 2
- 230000015556 catabolic process Effects 0.000 description 2
- 230000008859 change Effects 0.000 description 2
- 229960003677 chloroquine Drugs 0.000 description 2
- WHTVZRBIWZFKQO-UHFFFAOYSA-N chloroquine Natural products ClC1=CC=C2C(NC(C)CCCN(CC)CC)=CC=NC2=C1 WHTVZRBIWZFKQO-UHFFFAOYSA-N 0.000 description 2
- 238000003776 cleavage reaction Methods 0.000 description 2
- 206010009887 colitis Diseases 0.000 description 2
- 230000021615 conjugation Effects 0.000 description 2
- 229940039231 contrast media Drugs 0.000 description 2
- 238000013270 controlled release Methods 0.000 description 2
- 238000007334 copolymerization reaction Methods 0.000 description 2
- 239000003246 corticosteroid Substances 0.000 description 2
- 238000006731 degradation reaction Methods 0.000 description 2
- 230000001419 dependent effect Effects 0.000 description 2
- 238000013461 design Methods 0.000 description 2
- 238000011161 development Methods 0.000 description 2
- XEYBRNLFEZDVAW-ARSRFYASSA-N dinoprostone Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)CC(=O)[C@@H]1C\C=C/CCCC(O)=O XEYBRNLFEZDVAW-ARSRFYASSA-N 0.000 description 2
- 229960002986 dinoprostone Drugs 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 238000009547 dual-energy X-ray absorptiometry Methods 0.000 description 2
- 230000002708 enhancing effect Effects 0.000 description 2
- 230000003628 erosive effect Effects 0.000 description 2
- 238000002474 experimental method Methods 0.000 description 2
- 210000003414 extremity Anatomy 0.000 description 2
- 239000012530 fluid Substances 0.000 description 2
- 210000002216 heart Anatomy 0.000 description 2
- 210000000548 hind-foot Anatomy 0.000 description 2
- 238000010562 histological examination Methods 0.000 description 2
- 150000007857 hydrazones Chemical class 0.000 description 2
- JYGXADMDTFJGBT-VWUMJDOOSA-N hydrocortisone Chemical compound O=C1CC[C@]2(C)[C@H]3[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 JYGXADMDTFJGBT-VWUMJDOOSA-N 0.000 description 2
- 229910052739 hydrogen Inorganic materials 0.000 description 2
- 239000001257 hydrogen Substances 0.000 description 2
- 206010020718 hyperplasia Diseases 0.000 description 2
- 230000006872 improvement Effects 0.000 description 2
- JYGFTBXVXVMTGB-UHFFFAOYSA-N indolin-2-one Chemical class C1=CC=C2NC(=O)CC2=C1 JYGFTBXVXVMTGB-UHFFFAOYSA-N 0.000 description 2
- 230000006698 induction Effects 0.000 description 2
- 239000003407 interleukin 1 receptor blocking agent Substances 0.000 description 2
- 238000007912 intraperitoneal administration Methods 0.000 description 2
- 208000018937 joint inflammation Diseases 0.000 description 2
- 210000000231 kidney cortex Anatomy 0.000 description 2
- 210000003246 kidney medulla Anatomy 0.000 description 2
- 210000000244 kidney pelvis Anatomy 0.000 description 2
- 238000002372 labelling Methods 0.000 description 2
- 206010025135 lupus erythematosus Diseases 0.000 description 2
- 230000005291 magnetic effect Effects 0.000 description 2
- 230000010534 mechanism of action Effects 0.000 description 2
- 210000001872 metatarsal bone Anatomy 0.000 description 2
- FQPSGWSUVKBHSU-UHFFFAOYSA-N methacrylamide Chemical compound CC(=C)C(N)=O FQPSGWSUVKBHSU-UHFFFAOYSA-N 0.000 description 2
- 201000006417 multiple sclerosis Diseases 0.000 description 2
- 210000005036 nerve Anatomy 0.000 description 2
- 210000002569 neuron Anatomy 0.000 description 2
- 210000002997 osteoclast Anatomy 0.000 description 2
- 239000004033 plastic Substances 0.000 description 2
- 229920003023 plastic Polymers 0.000 description 2
- 229920000728 polyester Polymers 0.000 description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 description 2
- 230000008569 process Effects 0.000 description 2
- 229940002612 prodrug Drugs 0.000 description 2
- 239000000651 prodrug Substances 0.000 description 2
- 230000002035 prolonged effect Effects 0.000 description 2
- XEYBRNLFEZDVAW-UHFFFAOYSA-N prostaglandin E2 Natural products CCCCCC(O)C=CC1C(O)CC(=O)C1CC=CCCCC(O)=O XEYBRNLFEZDVAW-UHFFFAOYSA-N 0.000 description 2
- 238000011555 rabbit model Methods 0.000 description 2
- 238000010526 radical polymerization reaction Methods 0.000 description 2
- 238000012216 screening Methods 0.000 description 2
- 239000011780 sodium chloride Substances 0.000 description 2
- 230000003393 splenic effect Effects 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 238000007920 subcutaneous administration Methods 0.000 description 2
- 238000002636 symptomatic treatment Methods 0.000 description 2
- 208000011580 syndromic disease Diseases 0.000 description 2
- 210000001179 synovial fluid Anatomy 0.000 description 2
- 210000005222 synovial tissue Anatomy 0.000 description 2
- 201000004595 synovitis Diseases 0.000 description 2
- 230000009897 systematic effect Effects 0.000 description 2
- 230000009885 systemic effect Effects 0.000 description 2
- 231100000057 systemic toxicity Toxicity 0.000 description 2
- 210000001137 tarsal bone Anatomy 0.000 description 2
- 210000001550 testis Anatomy 0.000 description 2
- 229940126585 therapeutic drug Drugs 0.000 description 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N thiourea Chemical compound NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 description 2
- 210000002303 tibia Anatomy 0.000 description 2
- 238000011269 treatment regimen Methods 0.000 description 2
- 210000000626 ureter Anatomy 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- NBGAYCYFNGPNPV-UHFFFAOYSA-N 2-aminooxybenzoic acid Chemical compound NOC1=CC=CC=C1C(O)=O NBGAYCYFNGPNPV-UHFFFAOYSA-N 0.000 description 1
- AOYNUTHNTBLRMT-SLPGGIOYSA-N 2-deoxy-2-fluoro-aldehydo-D-glucose Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](F)C=O AOYNUTHNTBLRMT-SLPGGIOYSA-N 0.000 description 1
- UCBKDZNMPMBJAB-UHFFFAOYSA-N 3,4,5-triiodobenzoic acid Chemical compound OC(=O)C1=CC(I)=C(I)C(I)=C1 UCBKDZNMPMBJAB-UHFFFAOYSA-N 0.000 description 1
- DKIDEFUBRARXTE-UHFFFAOYSA-N 3-mercaptopropanoic acid Chemical compound OC(=O)CCS DKIDEFUBRARXTE-UHFFFAOYSA-N 0.000 description 1
- NALREUIWICQLPS-UHFFFAOYSA-N 7-imino-n,n-dimethylphenothiazin-3-amine;hydrochloride Chemical compound [Cl-].C1=C(N)C=C2SC3=CC(=[N+](C)C)C=CC3=NC2=C1 NALREUIWICQLPS-UHFFFAOYSA-N 0.000 description 1
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 description 1
- 206010067484 Adverse reaction Diseases 0.000 description 1
- 208000006386 Bone Resorption Diseases 0.000 description 1
- 208000002177 Cataract Diseases 0.000 description 1
- 229940122156 Cathepsin K inhibitor Drugs 0.000 description 1
- 208000034656 Contusions Diseases 0.000 description 1
- 102000010907 Cyclooxygenase 2 Human genes 0.000 description 1
- 108010037462 Cyclooxygenase 2 Proteins 0.000 description 1
- 206010061818 Disease progression Diseases 0.000 description 1
- ZGTMUACCHSMWAC-UHFFFAOYSA-L EDTA disodium salt (anhydrous) Chemical compound [Na+].[Na+].OC(=O)CN(CC([O-])=O)CCN(CC(O)=O)CC([O-])=O ZGTMUACCHSMWAC-UHFFFAOYSA-L 0.000 description 1
- 241000283073 Equus caballus Species 0.000 description 1
- 241000160765 Erebia ligea Species 0.000 description 1
- 206010021143 Hypoxia Diseases 0.000 description 1
- 102000000589 Interleukin-1 Human genes 0.000 description 1
- 108010002352 Interleukin-1 Proteins 0.000 description 1
- 206010023232 Joint swelling Diseases 0.000 description 1
- YQEZLKZALYSWHR-UHFFFAOYSA-N Ketamine Chemical compound C=1C=CC=C(Cl)C=1C1(NC)CCCCC1=O YQEZLKZALYSWHR-UHFFFAOYSA-N 0.000 description 1
- 238000012307 MRI technique Methods 0.000 description 1
- 241000124008 Mammalia Species 0.000 description 1
- 238000006219 Matteson homologation reaction Methods 0.000 description 1
- 206010061296 Motor dysfunction Diseases 0.000 description 1
- 241001049988 Mycobacterium tuberculosis H37Ra Species 0.000 description 1
- 206010028851 Necrosis Diseases 0.000 description 1
- 241000283973 Oryctolagus cuniculus Species 0.000 description 1
- 208000001132 Osteoporosis Diseases 0.000 description 1
- 229910019142 PO4 Inorganic materials 0.000 description 1
- 239000005662 Paraffin oil Substances 0.000 description 1
- 102000035195 Peptidases Human genes 0.000 description 1
- 108091005804 Peptidases Proteins 0.000 description 1
- 241000009328 Perro Species 0.000 description 1
- 241000042032 Petrocephalus catostoma Species 0.000 description 1
- 102100033076 Prostaglandin E synthase Human genes 0.000 description 1
- 101710096361 Prostaglandin E synthase Proteins 0.000 description 1
- 208000025747 Rheumatic disease Diseases 0.000 description 1
- 229920005654 Sephadex Polymers 0.000 description 1
- 239000012507 Sephadex™ Substances 0.000 description 1
- 235000009233 Stachytarpheta cayennensis Nutrition 0.000 description 1
- 206010043220 Temporomandibular joint syndrome Diseases 0.000 description 1
- 239000007983 Tris buffer Substances 0.000 description 1
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 description 1
- 210000001015 abdomen Anatomy 0.000 description 1
- 230000002378 acidificating effect Effects 0.000 description 1
- 230000009471 action Effects 0.000 description 1
- 239000000443 aerosol Substances 0.000 description 1
- 150000001345 alkine derivatives Chemical class 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 230000002152 alkylating effect Effects 0.000 description 1
- 125000003277 amino group Chemical group 0.000 description 1
- 210000003484 anatomy Anatomy 0.000 description 1
- 230000033115 angiogenesis Effects 0.000 description 1
- 229940124346 antiarthritic agent Drugs 0.000 description 1
- 239000003443 antiviral agent Substances 0.000 description 1
- 210000000702 aorta abdominal Anatomy 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 230000001174 ascending effect Effects 0.000 description 1
- WXNRAKRZUCLRBP-UHFFFAOYSA-N avridine Chemical compound CCCCCCCCCCCCCCCCCCN(CCCN(CCO)CCO)CCCCCCCCCCCCCCCCCC WXNRAKRZUCLRBP-UHFFFAOYSA-N 0.000 description 1
- 229910052788 barium Inorganic materials 0.000 description 1
- DSAJWYNOEDNPEQ-UHFFFAOYSA-N barium atom Chemical compound [Ba] DSAJWYNOEDNPEQ-UHFFFAOYSA-N 0.000 description 1
- 230000004071 biological effect Effects 0.000 description 1
- 229960002685 biotin Drugs 0.000 description 1
- 235000020958 biotin Nutrition 0.000 description 1
- 239000011616 biotin Substances 0.000 description 1
- 230000000740 bleeding effect Effects 0.000 description 1
- 239000001055 blue pigment Substances 0.000 description 1
- 230000004097 bone metabolism Effects 0.000 description 1
- 230000024279 bone resorption Effects 0.000 description 1
- 239000000969 carrier Substances 0.000 description 1
- 239000013522 chelant Substances 0.000 description 1
- 239000003153 chemical reaction reagent Substances 0.000 description 1
- 239000013626 chemical specie Substances 0.000 description 1
- 238000002512 chemotherapy Methods 0.000 description 1
- 230000010405 clearance mechanism Effects 0.000 description 1
- 210000005257 cortical tissue Anatomy 0.000 description 1
- 229960001334 corticosteroids Drugs 0.000 description 1
- 229940111134 coxibs Drugs 0.000 description 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 description 1
- 230000008021 deposition Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 229950000812 dexamethasone palmitate Drugs 0.000 description 1
- 206010012601 diabetes mellitus Diseases 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 230000005750 disease progression Effects 0.000 description 1
- 239000000890 drug combination Substances 0.000 description 1
- 238000007876 drug discovery Methods 0.000 description 1
- 230000000857 drug effect Effects 0.000 description 1
- 230000004064 dysfunction Effects 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 230000003511 endothelial effect Effects 0.000 description 1
- 210000000918 epididymis Anatomy 0.000 description 1
- 201000010063 epididymitis Diseases 0.000 description 1
- 210000003237 epithelioid cell Anatomy 0.000 description 1
- 210000003608 fece Anatomy 0.000 description 1
- 239000012467 final product Substances 0.000 description 1
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 description 1
- MHMNJMPURVTYEJ-UHFFFAOYSA-N fluorescein-5-isothiocyanate Chemical compound O1C(=O)C2=CC(N=C=S)=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 MHMNJMPURVTYEJ-UHFFFAOYSA-N 0.000 description 1
- 235000013305 food Nutrition 0.000 description 1
- 229960005063 gadodiamide Drugs 0.000 description 1
- 230000002496 gastric effect Effects 0.000 description 1
- 239000003193 general anesthetic agent Substances 0.000 description 1
- 210000004392 genitalia Anatomy 0.000 description 1
- 239000004220 glutamic acid Substances 0.000 description 1
- 244000144993 groups of animals Species 0.000 description 1
- 230000002440 hepatic effect Effects 0.000 description 1
- 238000013427 histology analysis Methods 0.000 description 1
- 229960000890 hydrocortisone Drugs 0.000 description 1
- 230000002209 hydrophobic effect Effects 0.000 description 1
- 230000007954 hypoxia Effects 0.000 description 1
- 238000010191 image analysis Methods 0.000 description 1
- 230000002163 immunogen Effects 0.000 description 1
- 229960003444 immunosuppressant agent Drugs 0.000 description 1
- 239000003018 immunosuppressive agent Substances 0.000 description 1
- 238000010348 incorporation Methods 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 210000004969 inflammatory cell Anatomy 0.000 description 1
- 230000006749 inflammatory damage Effects 0.000 description 1
- 230000028709 inflammatory response Effects 0.000 description 1
- 239000007972 injectable composition Substances 0.000 description 1
- 210000000936 intestine Anatomy 0.000 description 1
- 239000011630 iodine Substances 0.000 description 1
- 229910052740 iodine Inorganic materials 0.000 description 1
- 230000001788 irregular Effects 0.000 description 1
- 210000004731 jugular vein Anatomy 0.000 description 1
- 229960003299 ketamine Drugs 0.000 description 1
- 210000002414 leg Anatomy 0.000 description 1
- 230000003902 lesion Effects 0.000 description 1
- 238000011694 lewis rat Methods 0.000 description 1
- 150000002632 lipids Chemical class 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- 238000004811 liquid chromatography Methods 0.000 description 1
- 244000144972 livestock Species 0.000 description 1
- 230000004807 localization Effects 0.000 description 1
- 210000004072 lung Anatomy 0.000 description 1
- 210000004324 lymphatic system Anatomy 0.000 description 1
- 210000004698 lymphocyte Anatomy 0.000 description 1
- 238000011271 lymphoscintigraphy Methods 0.000 description 1
- 230000002080 lysosomotropic effect Effects 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 229960001924 melphalan Drugs 0.000 description 1
- 210000004379 membrane Anatomy 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000003228 microsomal effect Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- XHIRWEVPYCTARV-UHFFFAOYSA-N n-(3-aminopropyl)-2-methylprop-2-enamide;hydrochloride Chemical compound Cl.CC(=C)C(=O)NCCCN XHIRWEVPYCTARV-UHFFFAOYSA-N 0.000 description 1
- DBALITJIRDFXKL-UHFFFAOYSA-N n-[2-[(2-hydrazinyl-2-oxoethyl)amino]-2-oxoethyl]-2-methylprop-2-enamide Chemical compound CC(=C)C(=O)NCC(=O)NCC(=O)NN DBALITJIRDFXKL-UHFFFAOYSA-N 0.000 description 1
- 230000017074 necrotic cell death Effects 0.000 description 1
- 210000000440 neutrophil Anatomy 0.000 description 1
- 239000002674 ointment Substances 0.000 description 1
- 230000004768 organ dysfunction Effects 0.000 description 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 230000008506 pathogenesis Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 230000006320 pegylation Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- 210000003200 peritoneal cavity Anatomy 0.000 description 1
- 210000004303 peritoneum Anatomy 0.000 description 1
- 206010034674 peritonitis Diseases 0.000 description 1
- RGCLLPNLLBQHPF-HJWRWDBZSA-N phosphamidon Chemical compound CCN(CC)C(=O)C(\Cl)=C(/C)OP(=O)(OC)OC RGCLLPNLLBQHPF-HJWRWDBZSA-N 0.000 description 1
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 description 1
- 239000010452 phosphate Substances 0.000 description 1
- 239000006187 pill Substances 0.000 description 1
- 210000004180 plasmocyte Anatomy 0.000 description 1
- 229920001562 poly(N-(2-hydroxypropyl)methacrylamide) Polymers 0.000 description 1
- 229920003229 poly(methyl methacrylate) Polymers 0.000 description 1
- 229920002187 poly[N-2-(hydroxypropyl) methacrylamide] polymer Polymers 0.000 description 1
- 239000000580 polymer-drug conjugate Substances 0.000 description 1
- 239000004926 polymethyl methacrylate Substances 0.000 description 1
- 238000002600 positron emission tomography Methods 0.000 description 1
- 238000001556 precipitation Methods 0.000 description 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 150000003180 prostaglandins Chemical class 0.000 description 1
- 235000019833 protease Nutrition 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 230000005855 radiation Effects 0.000 description 1
- 230000009257 reactivity Effects 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000007115 recruitment Effects 0.000 description 1
- 210000005084 renal tissue Anatomy 0.000 description 1
- 238000001226 reprecipitation Methods 0.000 description 1
- 230000000552 rheumatic effect Effects 0.000 description 1
- RZJQGNCSTQAWON-UHFFFAOYSA-N rofecoxib Chemical compound C1=CC(S(=O)(=O)C)=CC=C1C1=C(C=2C=CC=CC=2)C(=O)OC1 RZJQGNCSTQAWON-UHFFFAOYSA-N 0.000 description 1
- 230000007017 scission Effects 0.000 description 1
- 210000004706 scrotum Anatomy 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 238000001542 size-exclusion chromatography Methods 0.000 description 1
- 150000003384 small molecules Chemical class 0.000 description 1
- 210000004872 soft tissue Anatomy 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000010186 staining Methods 0.000 description 1
- 238000003756 stirring Methods 0.000 description 1
- 230000001629 suppression Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 239000006188 syrup Substances 0.000 description 1
- 235000020357 syrup Nutrition 0.000 description 1
- 210000004341 tarsal joint Anatomy 0.000 description 1
- 230000002381 testicular Effects 0.000 description 1
- 231100000886 tinnitus Toxicity 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000759 toxicological effect Toxicity 0.000 description 1
- 238000012546 transfer Methods 0.000 description 1
- 210000000689 upper leg Anatomy 0.000 description 1
- 210000001635 urinary tract Anatomy 0.000 description 1
- 210000003462 vein Anatomy 0.000 description 1
- 210000001631 vena cava inferior Anatomy 0.000 description 1
- 229940087652 vioxx Drugs 0.000 description 1
- 238000012800 visualization Methods 0.000 description 1
- 230000004584 weight gain Effects 0.000 description 1
- 235000019786 weight gain Nutrition 0.000 description 1
- BPICBUSOMSTKRF-UHFFFAOYSA-N xylazine Chemical compound CC1=CC=CC(C)=C1NC1=NCCCS1 BPICBUSOMSTKRF-UHFFFAOYSA-N 0.000 description 1
- 229960001600 xylazine Drugs 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/001—Preparation for luminescence or biological staining
- A61K49/0013—Luminescence
- A61K49/0017—Fluorescence in vivo
- A61K49/005—Fluorescence in vivo characterised by the carrier molecule carrying the fluorescent agent
- A61K49/0054—Macromolecular compounds, i.e. oligomers, polymers, dendrimers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
- A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
- A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
- A61K47/58—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. poly[meth]acrylate, polyacrylamide, polystyrene, polyvinylpyrrolidone, polyvinylalcohol or polystyrene sulfonic acid resin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/001—Preparation for luminescence or biological staining
- A61K49/0013—Luminescence
- A61K49/0017—Fluorescence in vivo
- A61K49/0019—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules
- A61K49/0021—Fluorescence in vivo characterised by the fluorescent group, e.g. oligomeric, polymeric or dendritic molecules the fluorescent group being a small organic molecule
- A61K49/0041—Xanthene dyes, used in vivo, e.g. administered to a mice, e.g. rhodamines, rose Bengal
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K49/00—Preparations for testing in vivo
- A61K49/06—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations
- A61K49/08—Nuclear magnetic resonance [NMR] contrast preparations; Magnetic resonance imaging [MRI] contrast preparations characterised by the carrier
- A61K49/10—Organic compounds
- A61K49/12—Macromolecular compounds
- A61K49/126—Linear polymers, e.g. dextran, inulin, PEG
- A61K49/128—Linear polymers, e.g. dextran, inulin, PEG comprising multiple complex or complex-forming groups, being either part of the linear polymeric backbone or being pending groups covalently linked to the linear polymeric backbone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Radiology & Medical Imaging (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Magnetic Resonance Imaging Apparatus (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Claims (8)
- MiMROMOLÄttÄJS ABMOLÓ RSWDSZÉROÍ AKFÉJtlSZ Ét MÁS ÖTOMA&ÁSOS HTEGSÉÖÍK NKMMtNVAlí V LEKÉPEZÉSÉRE, KIÉRTÉKELÍSÍBE ÉS KEZELÉSÉRE Szahmiáiml IgénypóPink Î*. Gyógyászati készítmény atkalmaMv eépból egy gyulladásos ifôfôgség feetésére, Al uz a kővetkezőket tatalmazzá; egy vizoklhato (WM^-kogeiimM és egy gyulladásgátló terápiás szer egy hatásos mennyiségét, amely a evezet: vlzotdhátó HPMA4opolimerhez kötődik, ahol a vizofdhatú HPMA-kepoilmer a gyülladásgatló terápiás Szerhez egy távtartó csoport (angolul: „spacer") révé» kötődik, amely tartalmaz egy hidrazom kötést. 3* Oyógyász&l! készítmény alkalmazás céljából'! M- l, Igénypont szerint, amely továbbá tanahnaz egy célzó molekulárist (angolul: „targeting moiety"), amely a vizoklható Hk'ki.A-k'opoHmeríiez kötődik.
- 3, Gyógyászati készítmény alkalmazás céljából: m. 1. vagy 2, igénypontok szarmk aboi a gyulladásos betegség magában foglalja a réumaiőid artritiszt, 4 Gyógyászati készítmény alkalmazás céljából m 1~3. igénypontok bármelyike szerínk amely továbbá tartalmaz egy biológiai vizsgálati jelöManyagot: (éltükéi) (angolul: „hioassay label''), amely a vizoidbato ÍÍPMA4mpölimerhez kötődik, & Gyógyászati készítmény alkalmazás cédából: ax l- tgÉtypímt szerint, áheí a gyuliadásigMó terápiái? szer egy gltikokortikotd, ó» Gyógyászati készítmény alkaltnazás céljából a 2, igénypont: szeting aboi a célzó: molekuiarész a készítményt a csotpra vagy porcra irányítja, ?, Gyógyászati készítmény alkalmazás céljából a 2. igénypont vagy a 6. igénypont szerint, almi a célzó molekularész a kivetkezőkből álló csoportból van választva: biszfoszfonátok, kyaterner ammótbum-esoporlok, pepiidéit, ölígo-Asp, oligtM'lu, amino-szaieilsav, antitestek és azok ikigmensei vagy származékai, & Gyógyászati készítmény alkalmazás cilából a 2. vagy 64, igénypont szerint, aboi a kötés (kapcsolat) a célzó molekularész és a vizoldható polimer között hasítható, #, Gyógyászati készítmény alkalmazás céijábói a 2, vagy 6-7, igénypont szerint, ahol a kötés (kapcsolat) a célzó molekularész: és a vlzoMbaió polimer között nem basitbató. 14 Gyógyászati készítmény alkalmazás céljából m L igénypont szerint, ahol a terápiás szer a kővetkezőkből átló csoportból van választva: proteinek, jmpikiek> MSAID-ok, DMARD-ok, glifcokortikoidok, méiöírekáh sznllaszalazin, kforokin (angolnir „ebloriquíne"), arany, aranysö, réz, rézsö, penieiilamln, iD-penloiilamm, oikleszporln, és: azok keverékek í í. Gyógyászati készítmény alkalmazás céljából az L igénypont szerint egy vizes: oldószerben van bigltószerekben, alkalmazás céljából egy vizes készítménynek az adsgolásám egy alapyttak, amelyről fcltlteiezbctó, hogy reomstoid artritisztö! szenvedi és ahol lehetővé van téve a gyógyászati készítmény akkumulációja egy artridszes ízületben vagy a gyógyászati keszítmÉty céizott irányítása arra, ami áltat javítva van az ámktsz kezdése, WL Gyógyászati készítmény alkalmazás céljából a !L igénypont szerint, ahol az továbbá magában foglalja a terápiás szer egy ntellékltatásának a csökkentését olyan szövetekben, amelyek mások, mint az artniiszes ízület. Ük Gyógyászati készítmény alkalmazás céljából a Π, igénypont szerint, ahol a terápiás szer a következőkből álló csoportból van választva: KvAID-cA, DMARD-ok, eikioozigenázG inhibitor, egy glükoko'okmö. ogs tantor nokx<\ *s faktor blokkok* és eg> míerkvk·n~t receptor antagoniste, |4 Készítmény egy gyulladásos betegség leképezésére és kiértékelésére* amely a \{o ebre,'okot tartalmaz m egy vizokiható N'-ti-hidroxi'pi'opübtnetakril-amid (HPM As-ko poll mert és egy gyógyászati képalkotó szer egy hatásos mennyiségek amely a nevezett vizoldhaió ΗΡΜΛ-kopolitnethez kötődik, és ahol a nevezett vlzoklható ΗΡΜΑ-kopolinter továbbá tartalmaz egy gyulladásgátlő terápiás szén, amely a nevezett vfetsldható HPMA'kopolimerhez kötődik, ahol a viz oldható RPMA-kopoiimer a gyuíiadásgátió terápiás szerhez egy távtartó csoport (angolul: „spacer’*) révén kötődik, amely tartalmaz egy hnlrazon-köíést. Hi* Készítmény a 14. igénypont szerint, ahol a gyógyászati képalkotó szer a kővetkezők közűi legalább az egyikből álló csoportból van választva: egy MRl-hez alkalmazott, PBT-hez alkalmazott. CT-hez alkalmazón és y-szemtigráíiához alkalmazott szer. ii« Készítmény a 14. igénypont szerint, an v\ tana' n, * em *.elzo tulokul t ev?t (angolok „targeting moiety b. amely a vízoldható RPMA-kopolitnerhez kötődik, 41,: Készítmény a 14, igénypont szerint, ahol a gyulladásos betegség magában: iögiálja az artritlszt. II, Készítmény a 14-17. igénypontok bármelyike szerint, amely továbbá tartalmaz egy biológiai vizsgálati jelölöanyagot icímkét; (angolul: „bioassay label”), amely a vi zoldható ki PMA-kopolimcrhcz kötődik. tf, Készítmény a 14-18. igényptmíőferbáanólytke-iz^Bti,, «pplf áovábbé íÉJ^tóápi égy távtartó csoportot a képalkotó szer is a vizoldható HPMA-kopollmér között, ahol & távtartó csoport hasítható,
- 20, Készítmény a 14-18. igénypontok bármelyike szerint, amely továbbá tartalmaz egy tas tartó csopos tot a képalkotó w'r ca a \ molühotó lil'AIAAopohme? között, ahol a távtartó csoport nem hasítható,
- 24, Készítmény a 14, igénypont szerint Ahol a célzó mpleknlaréaz a kesafiritényí egy specifikus szövetre irányítja.22, KvOmmcm a 31 tguwpn ,t ^enrt ahol a ecl/o molekulares/ a ke*,, mneuy* a , v-nim vagy porcra irányítja, II, Készítmény a 21 igénypont szerint, ahol a célzó molekulares?, a kővetkezőkből álló csoportból van választva: biszfosz fonótok, kvatemer ammóni um -csoportok, oeptidek, oltgo-Aap, oligo-Giu, amifio-szaíicifsav. antlfesiek és azok íragmerisei vagy származékai.24, Készítmény a 14. igénypont szerint, ahol a terápiás szer a kővetkezőkből álló csoportból vmt választva: proteinek, peptidek, NSAID-ok, glükokoríikoidok, metotrexát, szolfasn Amin, UrnoK t lángolni: .mhlo;ugnne”), arany, sranyső, réz, rézsó. pcnidllamin, D-pemcillamin, ctkloszporin, és azok keverékei. Ili Eljárás égy gyulladásos hetepég leképezésém, ahol az eljárás magában foglalja a kővetkezőket: egy gyulladásos betegségtől szenvedő páciens vagy állati model esetében aleképezés elvégzése MRI-, PET-, CT- vagy y-szcintigráfiás berendezéssel, mielőtt a nevezett páciensnek vagy állati modellnek adagolva volt a 14. igénypont szerinti készítmény, és a leképezés elvégzése, miután a nevezett páciensnek vagy állati modellnek adagoh a voit a 14 igen) pont szerinti készemen). !& Eljárás a 25. igénypont szerűit, amely továbbá msgáMft. igl#, sf löiÄi# vizsgálat lefolytatását. Eljárás a 25, vagy 26. igénypont szerint, amely továbbá magában foglalja azh hogy a ti oldlnno 11PM \ koooln 'c u <o an -¾ m ina strt t -Λ spí.v> ss szövőn·©, 2S< Eljárás a 27. igénypont szerint, ahol a vegyüld célzott irányítása a csontra vagy pőrém irányit!. M, Eljárás a 27. vagy 28. igénypont szerint, ahol a vegyüietnek a célzott irányítása egy specifikus szövetre magában foglalja egy célzó molekularész (angolul: „targeting moiety’') alkalmazását, amely a következőkből álló csoportból van választva: biszíoszfonátok, kvatemer ammónUmvc söpörtök, pepíidek, oíigo-Asp, oligo-G'lu, amin.#* szalküsav, antitestek és azok fragro.ensei vagy származékát. 3& Eljárás a 27-26. igénypontok bármelyike szerint, amely továbbá megába« foglalja egy kötés hasítását a célzó molekularész és a vizolükuó IfEMA-kopolinter között ü|. Eljárás a 2?, igénypont szerint, ahol egy gyulladásos betegségtől szenvedő páctem vagy állati modell esetében a leképezés elvégzése, ami a vegyüld által varr javítva,,magában foglalja egy ariritiszes ízület leképezését
- 32, Eljárás a 25. igénypont szerint, ahol a gyógyászatt képalkotó szer a következője közöl legalább az egyikből álló csoportból ram választva: egy MRl -hez alkalmazott. FfTE-hez alkalmazok, CT-bez alkalmazóit, y-szctntigráüához alkalmazott szer, és azok kombinációt. II, Gyógyászati készítmény alkalmazás céljából az 1. igénypont szerint, ahol a terápiás széf tartalmaz több különböző tempi a \ vett,
- 34, Gyógyászati készítmény alkalmazás céljából a 2., 6. vagy 7. igénypont©!, szérinf, alto! a célzó molekularész. tartalmaz több különböző célzó moiekularészt. 3§, Gyógyászat! készítmény alkalmazás céljából a 34, igénypont szeriM> ahol a több különböző célzó mokkuiarész által több szövet vast megcélozva, 3& Gyógyászat! készítmény alkalmazás céljából a 4. igénypont szerint, ahol a biológiai vizsgálati jdölöanyag (címke) tartalmaz több különböző biológiái vizsgálati jelölöauyagot: (cimkéíj.
- 37, Gyógyászati készítmény alkalmazás céljából az I igénypont szerint, ahol a távtartó csoport tartalma/. több kémiailag különböző távtartó csoportot.
- 38, Készítmény a 14. igénypont szerint, ahol a képalkotó szer tarialrnaztöbb különböző képalkotó szert, 11*. Eljárás a 32. igénypont szerint, ahol a képalkotó szer tartalmaz legalább kát; képalkotó szert, ahol a két képalkotó szer közül mindegyik egy különböző képalkotó módszerben van alkalmazva, 4lk Készítmény, amely tartalmaz egy vizoldhaiö N-CS-hidmxi-pfopilj^dÄrtl^mld. kopoUmers, amely kötődik egy célzó molektdareszhez (angolul: „targeting tboiety") és egy gíűkokortiköidhoz egy pH-érzékeny hidrazon-kötésen keresztül. 41« Készítmény a 40. igény-pont szerint, ahol a gltikokorííkok! a dexarnetazon. 4% Készítmény a 40. igénypont szerint, ahol a célzó molekularész a hklrazin. 43« Gyógyászati készítmény alkalmazás céljából a 2, igénypont szerint, ahol a célzó molekularész a hsdrazin.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US55804704P | 2004-03-31 | 2004-03-31 |
Publications (1)
Publication Number | Publication Date |
---|---|
HUE034923T2 true HUE034923T2 (hu) | 2018-03-28 |
Family
ID=35124812
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HUE05732710A HUE034923T2 (hu) | 2004-03-31 | 2005-03-30 | Makromolekuláris adagoló rendszerek artritisz és más gyulladásos betegségek nem-invazív leképezésére, kiértékelésére és kezelésére |
Country Status (9)
Country | Link |
---|---|
US (2) | US10092662B2 (hu) |
EP (2) | EP3269394A1 (hu) |
CA (1) | CA2557448C (hu) |
DK (1) | DK1737428T3 (hu) |
ES (1) | ES2641570T3 (hu) |
HU (1) | HUE034923T2 (hu) |
PL (1) | PL1737428T3 (hu) |
PT (1) | PT1737428T (hu) |
WO (1) | WO2005097073A1 (hu) |
Families Citing this family (18)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HUE034923T2 (hu) | 2004-03-31 | 2018-03-28 | Univ Utah Res Found | Makromolekuláris adagoló rendszerek artritisz és más gyulladásos betegségek nem-invazív leképezésére, kiértékelésére és kezelésére |
EP1647283A1 (en) * | 2004-10-12 | 2006-04-19 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Polymeric contrast agent |
EP1902734A1 (en) * | 2006-09-25 | 2008-03-26 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | uPAR selective contrast agent for magnetic resonance imaging |
CN101265331B (zh) * | 2007-03-12 | 2010-10-13 | 中国科学院化学研究所 | Peg改性phpma材料及其制备方法 |
DE102007041625A1 (de) * | 2007-09-03 | 2009-03-05 | Sinn, Hannsjörg, Dr. | Neue Gelatine-Wirkstoff-Konjugate |
US20120189543A1 (en) * | 2009-09-09 | 2012-07-26 | Dong Wang | Compositions and Methods for Detecting and Treating Implant Loosening and Osteolysis |
US20110158901A1 (en) * | 2009-12-29 | 2011-06-30 | Swadeshmukul Santra | Chitosan-based nanoparticles and methods for making and using the same |
WO2011097563A1 (en) | 2010-02-08 | 2011-08-11 | Board Of Regents Of The University Of Nebraska | Biomineral and metal binding liposomes, their synthesis, and methods of use thereof |
US8906649B2 (en) | 2010-09-27 | 2014-12-09 | Janssen Biotech, Inc. | Antibodies binding human collagen II |
JP6126991B2 (ja) | 2010-09-27 | 2017-05-10 | ヤンセン バイオテツク,インコーポレーテツド | ヒトii型コラーゲンに結合する抗体 |
WO2012061695A1 (en) | 2010-11-04 | 2012-05-10 | Board Of Regents Of The University Of Nebraska | Compositions and methods for the treatment of traumatic brain injury |
PL2854769T3 (pl) | 2012-07-05 | 2023-08-07 | Taiwan Liposome Company, Ltd. | Sposoby leczenia zapalenia stawów |
EP3696185A1 (en) | 2015-11-12 | 2020-08-19 | Board of Regents of the University of Nebraska | Polyethylene glycol-conjugated glucocorticoid prodrugs and compositions and methods thereof |
US10905783B2 (en) | 2015-11-27 | 2021-02-02 | Michal RIVLIN | Glucosamine and derivatives thereof in imaging |
CN105797174B (zh) * | 2016-01-22 | 2019-01-11 | 复旦大学附属肿瘤医院 | 一种基于纳米氧化石墨烯的磁共振成像造影剂及其制备方法 |
EP3860660A4 (en) * | 2018-10-05 | 2023-01-25 | Texas Heart Institute | IMAGING AGENTS AND METHODS OF USE |
CN113415908B (zh) * | 2021-05-19 | 2022-04-29 | 河北津宏化工有限公司 | 一种改性水解聚马来酸酐水处理剂及其制备方法 |
CN116076438B (zh) * | 2023-03-21 | 2024-01-30 | 湖南中医药大学 | 类风湿关节炎合并间质性肺病动物模型及其构建方法和应用 |
Family Cites Families (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US4034040A (en) | 1971-05-24 | 1977-07-05 | Pfizer Inc. | Xylene-diamines as antiviral agents |
US6217911B1 (en) * | 1995-05-22 | 2001-04-17 | The United States Of America As Represented By The Secretary Of The Army | sustained release non-steroidal, anti-inflammatory and lidocaine PLGA microspheres |
GB8500209D0 (en) * | 1985-01-04 | 1985-02-13 | Ceskoslovenska Akademie Ved | Synthetic polymeric drugs |
DK110188D0 (da) * | 1988-03-02 | 1988-03-02 | Claus Selch Larsen | High molecular weight prodrug derivatives of antiinflammatory drugs |
US5356633A (en) * | 1989-10-20 | 1994-10-18 | Liposome Technology, Inc. | Method of treatment of inflamed tissues |
US5258453A (en) * | 1992-01-21 | 1993-11-02 | University Of Utah | Drug delivery system for the simultaneous delivery of drugs activatable by enzymes and light |
AU770344B2 (en) | 1998-08-31 | 2004-02-19 | Julian L. Ambrus | Method for removal of HIV and other viruses from blood |
US6436386B1 (en) * | 2000-11-14 | 2002-08-20 | Shearwater Corporation | Hydroxyapatite-targeting poly (ethylene glycol) and related polymers |
US20040043030A1 (en) * | 2001-07-31 | 2004-03-04 | Immunomedics, Inc. | Polymeric delivery systems |
PL374431A1 (en) * | 2002-07-01 | 2005-10-17 | Savient Pharmaceuticals, Inc. | Compositions and methods for therapeutic treatment |
AU2002953073A0 (en) | 2002-11-21 | 2003-01-16 | Access Pharmaceuticals Australia Pty Limited | Amplification of biotin-mediated targeting |
HUE034923T2 (hu) | 2004-03-31 | 2018-03-28 | Univ Utah Res Found | Makromolekuláris adagoló rendszerek artritisz és más gyulladásos betegségek nem-invazív leképezésére, kiértékelésére és kezelésére |
-
2005
- 2005-03-30 HU HUE05732710A patent/HUE034923T2/hu unknown
- 2005-03-30 EP EP17188335.8A patent/EP3269394A1/en not_active Withdrawn
- 2005-03-30 PT PT57327108T patent/PT1737428T/pt unknown
- 2005-03-30 EP EP05732710.8A patent/EP1737428B1/en not_active Not-in-force
- 2005-03-30 WO PCT/US2005/010801 patent/WO2005097073A1/en active Application Filing
- 2005-03-30 ES ES05732710.8T patent/ES2641570T3/es active Active
- 2005-03-30 DK DK05732710.8T patent/DK1737428T3/en active
- 2005-03-30 PL PL05732710T patent/PL1737428T3/pl unknown
- 2005-03-30 CA CA2557448A patent/CA2557448C/en not_active Expired - Fee Related
- 2005-03-30 US US10/591,258 patent/US10092662B2/en active Active
-
2018
- 2018-01-19 US US15/875,015 patent/US10172962B2/en active Active
Also Published As
Publication number | Publication date |
---|---|
EP1737428A1 (en) | 2007-01-03 |
US10092662B2 (en) | 2018-10-09 |
EP3269394A1 (en) | 2018-01-17 |
ES2641570T3 (es) | 2017-11-10 |
WO2005097073A1 (en) | 2005-10-20 |
CA2557448A1 (en) | 2005-10-20 |
US10172962B2 (en) | 2019-01-08 |
PL1737428T3 (pl) | 2018-03-30 |
PT1737428T (pt) | 2017-10-02 |
US20080159959A1 (en) | 2008-07-03 |
CA2557448C (en) | 2015-06-23 |
WO2005097073A8 (en) | 2005-12-08 |
US20180207296A1 (en) | 2018-07-26 |
EP1737428A4 (en) | 2010-12-22 |
EP1737428B1 (en) | 2017-08-30 |
DK1737428T3 (en) | 2017-10-09 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
US10172962B2 (en) | Macromolecular delivery systems for non-invasive imaging, evaluation and treatment of arthritis and other inflammatory diseases | |
Lu | Molecular imaging of HPMA copolymers: visualizing drug delivery in cell, mouse and man | |
Wang et al. | The arthrotropism of macromolecules in adjuvant-induced arthritis rat model: a preliminary study | |
US20090311182A1 (en) | Macromolecular Delivery Systems for Non-Invasive Imaging, Evaluation and Treatment of Arthritis and Other Inflammatory Diseases | |
DE69332952T2 (de) | Diagnostische und therapeutische Einheiten enthaltende biokompatible Polymere | |
AU2018204504A1 (en) | Conjugates for treating diseases caused by PSMA expressing cells | |
JP2011153159A (ja) | 放出システムとしてのポリアセタール薬物抱合体 | |
WO2012158960A2 (en) | Melanocortin 1 receptor ligands and methods of use | |
Bogdanov Jr et al. | Protected graft copolymer (PGC) in imaging and therapy: a platform for the delivery of covalently and non-covalently bound drugs | |
US20230364244A1 (en) | Dendrimer compositions and methods for drug delivery to injured kidney | |
KR20100120971A (ko) | 가돌리늄 착물, 그 제조방법, 및 그것을 포함하는 mri 조영제 | |
Gelb et al. | Poly (trehalose methacrylate) as an Excipient for Insulin Stabilization: Mechanism and Safety | |
CN112675311A (zh) | 18/19f标记的psma靶向诊疗一体化小分子药物偶联物、制备方法及其应用 | |
EP1753466A2 (en) | Copolymers comprising positively and negatively charged aminoacids conjugated to chelants | |
KR101016214B1 (ko) | 근적외선 형광체가 결합된 담즙산-글라이콜키토산 복합체나노입자를 포함하는 류마티스 관절염 진단용 조영제 | |
US20230338554A1 (en) | Galactosylated dendrimers for targeted intracellular delivery to hepatocytes | |
CN117122695A (zh) | 一种靶向活化cd44分子的透明质酸功能化偶联物及制备方法和应用 | |
Dalkaraa et al. | Disulfide cross-linked fab-aggregates: Preparation and biodistribution | |
JP2022535463A (ja) | 放射性同位体をキレート化し、psma受容体を標的とする特異的分子で修飾された表面を有するポリマーナノ粒子を調製するプロセスおよびその使用 | |
Guley | Serum Albumin as a Carrier of Immunostimulatory Oligodeoxynucleotides for Cancer Therapy | |
Liu | POLYMER MODIFICATION OF FULLERENE FOR PHOTODYNAMIC TUMOR THERAPY AND TUMOR IMAGING |