JPWO2020181060A5 - - Google Patents
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- JPWO2020181060A5 JPWO2020181060A5 JP2021552571A JP2021552571A JPWO2020181060A5 JP WO2020181060 A5 JPWO2020181060 A5 JP WO2020181060A5 JP 2021552571 A JP2021552571 A JP 2021552571A JP 2021552571 A JP2021552571 A JP 2021552571A JP WO2020181060 A5 JPWO2020181060 A5 JP WO2020181060A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- therapeutic agent
- biodegradable
- composition according
- depot
- 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
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- 239000008194 pharmaceutical composition Substances 0.000 claims 58
- 239000003814 drug Substances 0.000 claims 33
- 229940124597 therapeutic agent Drugs 0.000 claims 33
- 238000000034 method Methods 0.000 claims 17
- 229920002988 biodegradable polymer Polymers 0.000 claims 16
- 239000004621 biodegradable polymer Substances 0.000 claims 16
- 239000011159 matrix material Substances 0.000 claims 16
- 229920000642 polymer Polymers 0.000 claims 13
- 208000027866 inflammatory disease Diseases 0.000 claims 12
- 229920001519 homopolymer Polymers 0.000 claims 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 8
- 208000015122 neurodegenerative disease Diseases 0.000 claims 8
- 229920006149 polyester-amide block copolymer Polymers 0.000 claims 8
- 229920001244 Poly(D,L-lactide) Polymers 0.000 claims 7
- 239000007943 implant Substances 0.000 claims 7
- 229960003957 dexamethasone Drugs 0.000 claims 6
- 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 claims 6
- 108091000080 Phosphotransferase Proteins 0.000 claims 5
- 229920001577 copolymer Polymers 0.000 claims 5
- 239000003246 corticosteroid Substances 0.000 claims 5
- 102000020233 phosphotransferase Human genes 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 125000006755 (C2-C20) alkyl group Chemical group 0.000 claims 4
- 229920003178 (lactide-co-glycolide) polymer Polymers 0.000 claims 4
- -1 3-hydroxy-2,2-bis(hydroxymethyl)propyl Chemical group 0.000 claims 4
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 4
- 208000010837 Diabetic eye disease Diseases 0.000 claims 4
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims 4
- 206010013774 Dry eye Diseases 0.000 claims 4
- 206010061218 Inflammation Diseases 0.000 claims 4
- 208000000208 Wet Macular Degeneration Diseases 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 208000011325 dry age related macular degeneration Diseases 0.000 claims 4
- 230000004054 inflammatory process Effects 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 230000004770 neurodegeneration Effects 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- SMNDYUVBFMFKNZ-UHFFFAOYSA-N 2-furoic acid Chemical compound OC(=O)C1=CC=CO1 SMNDYUVBFMFKNZ-UHFFFAOYSA-N 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 208000010412 Glaucoma Diseases 0.000 claims 2
- 208000031886 HIV Infections Diseases 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- 102000015617 Janus Kinases Human genes 0.000 claims 2
- 108010024121 Janus Kinases Proteins 0.000 claims 2
- 208000022873 Ocular disease Diseases 0.000 claims 2
- 206010030043 Ocular hypertension Diseases 0.000 claims 2
- 206010046851 Uveitis Diseases 0.000 claims 2
- 108091008605 VEGF receptors Proteins 0.000 claims 2
- 102000009484 Vascular Endothelial Growth Factor Receptors Human genes 0.000 claims 2
- OURRXQUGYQRVML-AREMUKBSSA-N [4-[(2s)-3-amino-1-(isoquinolin-6-ylamino)-1-oxopropan-2-yl]phenyl]methyl 2,4-dimethylbenzoate Chemical group CC1=CC(C)=CC=C1C(=O)OCC1=CC=C([C@@H](CN)C(=O)NC=2C=C3C=CN=CC3=CC=2)C=C1 OURRXQUGYQRVML-AREMUKBSSA-N 0.000 claims 2
- 125000004450 alkenylene group Chemical group 0.000 claims 2
- 229960003005 axitinib Drugs 0.000 claims 2
- RITAVMQDGBJQJZ-FMIVXFBMSA-N axitinib Chemical compound CNC(=O)C1=CC=CC=C1SC1=CC=C(C(\C=C\C=2N=CC=CC=2)=NN2)C2=C1 RITAVMQDGBJQJZ-FMIVXFBMSA-N 0.000 claims 2
- 229940092705 beclomethasone Drugs 0.000 claims 2
- NBMKJKDGKREAPL-DVTGEIKXSA-N beclomethasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)CO)(O)[C@@]1(C)C[C@@H]2O NBMKJKDGKREAPL-DVTGEIKXSA-N 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 210000004087 cornea Anatomy 0.000 claims 2
- 201000007717 corneal ulcer Diseases 0.000 claims 2
- 229960001334 corticosteroids Drugs 0.000 claims 2
- 206010014801 endophthalmitis Diseases 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 239000012634 fragment Substances 0.000 claims 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 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical group CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1CC[C@@H](O)CCC1=CC=CC=C1 GGXICVAJURFBLW-CEYXHVGTSA-N 0.000 claims 2
- 229960001160 latanoprost Drugs 0.000 claims 2
- 229960001664 mometasone Drugs 0.000 claims 2
- QLIIKPVHVRXHRI-CXSFZGCWSA-N mometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@@H](C)[C@@](C(=O)CCl)(O)[C@@]1(C)C[C@@H]2O QLIIKPVHVRXHRI-CXSFZGCWSA-N 0.000 claims 2
- 229950009210 netarsudil Drugs 0.000 claims 2
- 125000006239 protecting group Chemical group 0.000 claims 2
- 108091008598 receptor tyrosine kinases Proteins 0.000 claims 2
- 102000027426 receptor tyrosine kinases Human genes 0.000 claims 2
- 102000000568 rho-Associated Kinases Human genes 0.000 claims 2
- 108010041788 rho-Associated Kinases Proteins 0.000 claims 2
- 229950004432 rofleponide Drugs 0.000 claims 2
- IXTCZMJQGGONPY-XJAYAHQCSA-N rofleponide Chemical compound C1([C@@H](F)C2)=CC(=O)CC[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3O[C@@H](CCC)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O IXTCZMJQGGONPY-XJAYAHQCSA-N 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 229940124676 vascular endothelial growth factor receptor Drugs 0.000 claims 2
- JRRDISHSXWGFRF-UHFFFAOYSA-N 1-[2-(2-ethoxyethoxy)ethoxy]-2-methoxyethane Chemical compound CCOCCOCCOCCOC JRRDISHSXWGFRF-UHFFFAOYSA-N 0.000 claims 1
- SPMVMDHWKHCIDT-UHFFFAOYSA-N 1-[2-chloro-4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-3-(5-methyl-3-isoxazolyl)urea Chemical compound C=12C=C(OC)C(OC)=CC2=NC=CC=1OC(C=C1Cl)=CC=C1NC(=O)NC=1C=C(C)ON=1 SPMVMDHWKHCIDT-UHFFFAOYSA-N 0.000 claims 1
- ZESRJSPZRDMNHY-YFWFAHHUSA-N 11-deoxycorticosterone Chemical compound O=C1CC[C@]2(C)[C@H]3CC[C@](C)([C@H](CC4)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 ZESRJSPZRDMNHY-YFWFAHHUSA-N 0.000 claims 1
- XXJWYDDUDKYVKI-UHFFFAOYSA-N 4-[(4-fluoro-2-methyl-1H-indol-5-yl)oxy]-6-methoxy-7-[3-(1-pyrrolidinyl)propoxy]quinazoline Chemical compound COC1=CC2=C(OC=3C(=C4C=C(C)NC4=CC=3)F)N=CN=C2C=C1OCCCN1CCCC1 XXJWYDDUDKYVKI-UHFFFAOYSA-N 0.000 claims 1
- JJTUDXZGHPGLLC-IMJSIDKUSA-N 4511-42-6 Chemical compound C[C@@H]1OC(=O)[C@H](C)OC1=O JJTUDXZGHPGLLC-IMJSIDKUSA-N 0.000 claims 1
- XBGQGAPUUJJOTA-KWLUMGGGSA-N 4b52439y33 Chemical compound O.C([C@@H]1C2)C3=CC=CC=C3C[C@@]1(C(=O)CO)[C@]1(C)[C@@H]2[C@H](CCC=2[C@@]3(C=CC(=O)C=2)C)[C@]3(F)[C@@H](O)C1 XBGQGAPUUJJOTA-KWLUMGGGSA-N 0.000 claims 1
- 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 1
- VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims 1
- LUKZNWIVRBCLON-GXOBDPJESA-N Ciclesonide Chemical compound C1([C@H]2O[C@@]3([C@H](O2)C[C@@H]2[C@@]3(C[C@H](O)[C@@H]3[C@@]4(C)C=CC(=O)C=C4CC[C@H]32)C)C(=O)COC(=O)C(C)C)CCCCC1 LUKZNWIVRBCLON-GXOBDPJESA-N 0.000 claims 1
- DRSFVGQMPYTGJY-GNSLJVCWSA-N Deprodone propionate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)CC)[C@@]1(C)C[C@@H]2O DRSFVGQMPYTGJY-GNSLJVCWSA-N 0.000 claims 1
- WJOHZNCJWYWUJD-IUGZLZTKSA-N Fluocinonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O WJOHZNCJWYWUJD-IUGZLZTKSA-N 0.000 claims 1
- YCISZOVUHXIOFY-HKXOFBAYSA-N Halopredone acetate Chemical compound C1([C@H](F)C2)=CC(=O)C(Br)=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2CC[C@](OC(C)=O)(C(=O)COC(=O)C)[C@@]2(C)C[C@@H]1O YCISZOVUHXIOFY-HKXOFBAYSA-N 0.000 claims 1
- 229940122245 Janus kinase inhibitor Drugs 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002147 L01XE04 - Sunitinib Substances 0.000 claims 1
- 239000005511 L01XE05 - Sorafenib Substances 0.000 claims 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 1
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims 1
- 239000002144 L01XE18 - Ruxolitinib Substances 0.000 claims 1
- 239000002138 L01XE21 - Regorafenib Substances 0.000 claims 1
- UIARLYUEJFELEN-LROUJFHJSA-N LSM-1231 Chemical compound C12=C3N4C5=CC=CC=C5C3=C3C(=O)NCC3=C2C2=CC=CC=C2N1[C@]1(C)[C@](CO)(O)C[C@H]4O1 UIARLYUEJFELEN-LROUJFHJSA-N 0.000 claims 1
- FQISKWAFAHGMGT-SGJOWKDISA-M Methylprednisolone sodium succinate Chemical compound [Na+].C([C@@]12C)=CC(=O)C=C1[C@@H](C)C[C@@H]1[C@@H]2[C@@H](O)C[C@]2(C)[C@@](O)(C(=O)COC(=O)CCC([O-])=O)CC[C@H]21 FQISKWAFAHGMGT-SGJOWKDISA-M 0.000 claims 1
- FPABVZYYTCHNMK-YNRDDPJXSA-N PGF2alpha isopropyl ester Chemical compound CCCCC[C@H](O)\C=C\[C@H]1[C@H](O)C[C@H](O)[C@@H]1C\C=C/CCCC(=O)OC(C)C FPABVZYYTCHNMK-YNRDDPJXSA-N 0.000 claims 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 239000004012 Tofacitinib Substances 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 229960001686 afatinib Drugs 0.000 claims 1
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims 1
- 229950000971 baricitinib Drugs 0.000 claims 1
- XUZMWHLSFXCVMG-UHFFFAOYSA-N baricitinib Chemical compound C1N(S(=O)(=O)CC)CC1(CC#N)N1N=CC(C=2C=3C=CNC=3N=CN=2)=C1 XUZMWHLSFXCVMG-UHFFFAOYSA-N 0.000 claims 1
- 229960002537 betamethasone Drugs 0.000 claims 1
- UREBDLICKHMUKA-DVTGEIKXSA-N betamethasone 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-DVTGEIKXSA-N 0.000 claims 1
- AQOKCDNYWBIDND-FTOWTWDKSA-N bimatoprost Chemical compound CCNC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)CCC1=CC=CC=C1 AQOKCDNYWBIDND-FTOWTWDKSA-N 0.000 claims 1
- 229960002470 bimatoprost Drugs 0.000 claims 1
- 229960004436 budesonide Drugs 0.000 claims 1
- 229960002412 cediranib Drugs 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 229960003728 ciclesonide Drugs 0.000 claims 1
- 229960004299 clocortolone Drugs 0.000 claims 1
- YMTMADLUXIRMGX-RFPWEZLHSA-N clocortolone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(Cl)[C@@H]2[C@@H]2C[C@@H](C)[C@H](C(=O)CO)[C@@]2(C)C[C@@H]1O YMTMADLUXIRMGX-RFPWEZLHSA-N 0.000 claims 1
- 230000002354 daily effect Effects 0.000 claims 1
- ZESRJSPZRDMNHY-UHFFFAOYSA-N de-oxy corticosterone Natural products O=C1CCC2(C)C3CCC(C)(C(CC4)C(=O)CO)C4C3CCC2=C1 ZESRJSPZRDMNHY-UHFFFAOYSA-N 0.000 claims 1
- 229960001145 deflazacort Drugs 0.000 claims 1
- FBHSPRKOSMHSIF-GRMWVWQJSA-N deflazacort Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(C)=N[C@@]3(C(=O)COC(=O)C)[C@@]1(C)C[C@@H]2O FBHSPRKOSMHSIF-GRMWVWQJSA-N 0.000 claims 1
- 229960003662 desonide Drugs 0.000 claims 1
- WBGKWQHBNHJJPZ-LECWWXJVSA-N desonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O WBGKWQHBNHJJPZ-LECWWXJVSA-N 0.000 claims 1
- 229960003654 desoxycortone Drugs 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- 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 1
- 229950006990 etiprednol dicloacetate Drugs 0.000 claims 1
- QAIOVDNCIZSSSF-RFAJLIJZSA-N etiprednol dicloacetate Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@](OC(=O)C(Cl)Cl)(C(=O)OCC)[C@@]1(C)C[C@@H]2O QAIOVDNCIZSSSF-RFAJLIJZSA-N 0.000 claims 1
- 230000003203 everyday effect Effects 0.000 claims 1
- 229960002011 fludrocortisone Drugs 0.000 claims 1
- AAXVEMMRQDVLJB-BULBTXNYSA-N fludrocortisone Chemical compound O=C1CC[C@]2(C)[C@@]3(F)[C@@H](O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 AAXVEMMRQDVLJB-BULBTXNYSA-N 0.000 claims 1
- 229960000676 flunisolide Drugs 0.000 claims 1
- 229960001347 fluocinolone acetonide Drugs 0.000 claims 1
- FEBLZLNTKCEFIT-VSXGLTOVSA-N fluocinolone acetonide Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@H]3OC(C)(C)O[C@@]3(C(=O)CO)[C@@]2(C)C[C@@H]1O FEBLZLNTKCEFIT-VSXGLTOVSA-N 0.000 claims 1
- 229960000785 fluocinonide Drugs 0.000 claims 1
- WWSWYXNVCBLWNZ-QIZQQNKQSA-N fluprostenol Chemical compound C([C@H](O)\C=C\[C@@H]1[C@H]([C@@H](O)C[C@H]1O)C\C=C/CCCC(O)=O)OC1=CC=CC(C(F)(F)F)=C1 WWSWYXNVCBLWNZ-QIZQQNKQSA-N 0.000 claims 1
- 229950009951 fluprostenol Drugs 0.000 claims 1
- 229960002714 fluticasone Drugs 0.000 claims 1
- MGNNYOODZCAHBA-GQKYHHCASA-N fluticasone Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(O)[C@@]2(C)C[C@@H]1O MGNNYOODZCAHBA-GQKYHHCASA-N 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical group C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 229960002475 halometasone Drugs 0.000 claims 1
- GGXMRPUKBWXVHE-MIHLVHIWSA-N halometasone Chemical compound C1([C@@H](F)C2)=CC(=O)C(Cl)=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)CO)(O)[C@@]2(C)C[C@@H]1O GGXMRPUKBWXVHE-MIHLVHIWSA-N 0.000 claims 1
- 229950004611 halopredone acetate Drugs 0.000 claims 1
- MNWFXJYAOYHMED-UHFFFAOYSA-N heptanoic acid Chemical compound CCCCCCC(O)=O MNWFXJYAOYHMED-UHFFFAOYSA-N 0.000 claims 1
- 229960000890 hydrocortisone Drugs 0.000 claims 1
- 238000002347 injection Methods 0.000 claims 1
- 239000007924 injection Substances 0.000 claims 1
- 229960004891 lapatinib Drugs 0.000 claims 1
- 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 1
- 229950001845 lestaurtinib Drugs 0.000 claims 1
- 229960004584 methylprednisolone Drugs 0.000 claims 1
- 229950005486 naflocort Drugs 0.000 claims 1
- 229950008835 neratinib Drugs 0.000 claims 1
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims 1
- 229940094443 oxytocics prostaglandins Drugs 0.000 claims 1
- 229960005205 prednisolone Drugs 0.000 claims 1
- OIGNJSKKLXVSLS-VWUMJDOOSA-N prednisolone Chemical compound O=C1C=C[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 OIGNJSKKLXVSLS-VWUMJDOOSA-N 0.000 claims 1
- 229960004618 prednisone Drugs 0.000 claims 1
- XOFYZVNMUHMLCC-ZPOLXVRWSA-N prednisone Chemical compound O=C1C=C[C@]2(C)[C@H]3C(=O)C[C@](C)([C@@](CC4)(O)C(=O)CO)[C@@H]4[C@@H]3CCC2=C1 XOFYZVNMUHMLCC-ZPOLXVRWSA-N 0.000 claims 1
- OCNSAYQJDKJOLH-AHTXBMBWSA-N propan-2-yl (z)-7-[(1r,2r,3r,5s)-2-[(e,3r)-4-(3-chlorophenoxy)-3-hydroxybut-1-enyl]-3,5-dihydroxycyclopentyl]hept-5-enoate Chemical compound CC(C)OC(=O)CCC\C=C/C[C@H]1[C@@H](O)C[C@@H](O)[C@@H]1\C=C\[C@@H](O)COC1=CC=CC(Cl)=C1 OCNSAYQJDKJOLH-AHTXBMBWSA-N 0.000 claims 1
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| CA3166738A1 (en) | 2020-02-06 | 2021-08-12 | Charles D. Blizzard | Travoprost compositions and methods for treating ocular diseases |
| CA3171563A1 (en) | 2020-03-25 | 2021-09-30 | Charles D. Blizzard | Ocular implant containing a tyrosine kinase inhibitor |
| WO2021207486A1 (en) * | 2020-04-08 | 2021-10-14 | Aerie Pharmaceuticals, Inc. | Treatments |
| IL307997A (en) | 2021-04-30 | 2023-12-01 | Perfuse Therapeutics Inc | Pharmaceutical compositions and intravitreal drug delivery systems for the treatment of ocular diseases |
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| TW202448436A (zh) | 2023-04-11 | 2024-12-16 | 美商視爾普斯眼科公司 | 含有酪胺酸激酶抑制劑之眼部植入物 |
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| WO2025169089A1 (en) | 2024-02-05 | 2025-08-14 | Sun Pharmaceutical Industries Limited | Ophthalmic compositions of tyrosine kinase inhibitors and their uses |
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| JP6330815B2 (ja) * | 2012-10-02 | 2018-05-30 | ディーエスエム アイピー アセッツ ビー．ブイ． | タンパク質および生分解性ポリエステルアミドを含む薬物送達組成物 |
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| KR20160100992A (ko) * | 2013-12-06 | 2016-08-24 | 엔비시아 테라퓨틱스 인코포레이티드 | 눈의 병태의 치료를 위한 전방내 이식물 |
| CA2933900A1 (en) * | 2013-12-20 | 2015-06-25 | Georgia Tech Research Corporation | Formulations and methods for targeted ocular delivery of therapeutic agents |
| JP7026507B2 (ja) * | 2014-09-06 | 2022-02-28 | インテグラル バイオシステムズ エルエルシー | 眼において薬物徐放を達成する方法及び生体適合性組成物 |
| WO2016097297A1 (en) | 2014-12-18 | 2016-06-23 | Dsm Ip Assets B.V. | Drug delivery system for delivery of acid sensitive drugs |
| CN115337254A (zh) * | 2015-07-23 | 2022-11-15 | 爱瑞制药公司 | 用于治疗眼病的玻璃体内药物递送系统 |
| WO2017120600A1 (en) * | 2016-01-08 | 2017-07-13 | Clearside Biomedical, Inc. | Compositions and methods of treating wet age-related macular degeneration |
| US20180117148A1 (en) * | 2016-10-28 | 2018-05-03 | Andrew J. Holman | Compounds, pharmaceutical compositions and methods of treatments of immune related diseases and disorders |
| WO2018161035A1 (en) * | 2017-03-03 | 2018-09-07 | Macregen, Inc. | Treatment of age-related macular degeneration and other eye diseases with one or more therapeutic agents |
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