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 |
| EP3884929B1 (en) | 2020-03-25 | 2023-06-14 | Ocular Therapeutix, Inc. | Ocular implant containing a tyrosine kinase inhibitor |
| WO2021207486A1 (en) * | 2020-04-08 | 2021-10-14 | Aerie Pharmaceuticals, Inc. | Treatments |
| CA3218251A1 (en) | 2021-04-30 | 2022-11-03 | Perfuse Therapeutics, Inc. | Pharmaceutical compositions and intravitreal drug delivery systems for the treatment of ocular diseases |
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| CN120897764A (zh) | 2023-04-11 | 2025-11-04 | 视尔普斯眼科公司 | 包含阿西替尼多晶型物iv的眼部植入物 |
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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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| US20150037422A1 (en) * | 2012-02-22 | 2015-02-05 | Trustees Of Tufts College | Compositions and methods for ocular delivery of a therapeutic agent |
| CA2881729C (en) | 2012-10-02 | 2021-05-04 | Dsm Ip Assets B.V. | Drug delivery composition comprising proteins and biodegradable polyesteramides |
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| CN109602691A (zh) * | 2013-02-15 | 2019-04-12 | 阿勒根公司 | 持续药物递送植入物 |
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| WO2015095772A2 (en) * | 2013-12-20 | 2015-06-25 | Emory University | Formulations and methods for targeted ocular delivery of therapeutic agents |
| CN109481447A (zh) * | 2014-09-06 | 2019-03-19 | 整体生物系统有限责任公司 | 用于在眼中实现持续药物释放的方法和生物相容性组合物 |
| EP3233067B1 (en) * | 2014-12-18 | 2019-11-06 | DSM IP Assets B.V. | Drug delivery system for delivery of acid sensitive drugs |
| EP3324944A4 (en) | 2015-07-23 | 2019-04-03 | Aerie Pharmaceuticals, Inc. | INTRAVITREAL AGGREGATION SYSTEMS FOR THE TREATMENT OF EYE DISEASE |
| WO2017120600A1 (en) | 2016-01-08 | 2017-07-13 | Clearside Biomedical, Inc. | Compositions and methods of treating wet age-related macular degeneration |
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| 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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