JP2020536067A5 - - Google Patents
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- JP2020536067A5 JP2020536067A5 JP2020517956A JP2020517956A JP2020536067A5 JP 2020536067 A5 JP2020536067 A5 JP 2020536067A5 JP 2020517956 A JP2020517956 A JP 2020517956A JP 2020517956 A JP2020517956 A JP 2020517956A JP 2020536067 A5 JP2020536067 A5 JP 2020536067A5
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- JP
- Japan
- Prior art keywords
- composition
- composition according
- formula
- item
- pharmaceutically acceptable
- Prior art date
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- 239000000203 mixture Substances 0.000 claims description 144
- 150000001875 compounds Chemical class 0.000 claims description 53
- 150000003839 salts Chemical class 0.000 claims description 45
- 208000017442 Retinal disease Diseases 0.000 claims description 43
- 206010038923 Retinopathy Diseases 0.000 claims description 43
- 208000003556 Dry Eye Syndromes Diseases 0.000 claims description 40
- 239000003937 drug carrier Substances 0.000 claims description 35
- 229920000858 Cyclodextrin Polymers 0.000 claims description 24
- AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical group OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 claims description 21
- 239000001116 FEMA 4028 Substances 0.000 claims description 20
- 229960004853 betadex Drugs 0.000 claims description 20
- -1 2-hydroxypropyl Chemical group 0.000 claims description 18
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 claims description 11
- 229920000053 polysorbate 80 Polymers 0.000 claims description 11
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 7
- 229920002675 Polyoxyl Polymers 0.000 claims description 6
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 5
- 229930195725 Mannitol Natural products 0.000 claims description 5
- 239000000594 mannitol Substances 0.000 claims description 5
- 235000010355 mannitol Nutrition 0.000 claims description 5
- 229940113116 polyethylene glycol 1000 Drugs 0.000 claims description 5
- 239000003755 preservative agent Substances 0.000 claims description 5
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 5
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 4
- 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 claims description 3
- 108010036949 Cyclosporine Proteins 0.000 claims description 3
- 239000003242 anti bacterial agent Substances 0.000 claims description 3
- 229940088710 antibiotic agent Drugs 0.000 claims description 3
- 229960001265 ciclosporin Drugs 0.000 claims description 3
- 229930182912 cyclosporin Natural products 0.000 claims description 3
- 239000003889 eye drop Substances 0.000 claims description 3
- 229920001214 Polysorbate 60 Polymers 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 150000005846 sugar alcohols Chemical class 0.000 claims description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 4
- 230000002335 preservative effect Effects 0.000 claims 4
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical compound O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims 3
- 239000013543 active substance Substances 0.000 claims 2
- 229930105110 Cyclosporin A Natural products 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 22
- IXPNQXFRVYWDDI-UHFFFAOYSA-N 1-methyl-2,4-dioxo-1,3-diazinane-5-carboximidamide Chemical compound CN1CC(C(N)=N)C(=O)NC1=O IXPNQXFRVYWDDI-UHFFFAOYSA-N 0.000 description 9
- 239000000661 sodium alginate Substances 0.000 description 9
- 235000010413 sodium alginate Nutrition 0.000 description 9
- 229940005550 sodium alginate Drugs 0.000 description 9
- 239000002105 nanoparticle Substances 0.000 description 7
- 206010012689 Diabetic retinopathy Diseases 0.000 description 6
- 206010015958 Eye pain Diseases 0.000 description 6
- 229920002148 Gellan gum Polymers 0.000 description 6
- 208000002193 Pain Diseases 0.000 description 6
- 239000000216 gellan gum Substances 0.000 description 6
- 235000010492 gellan gum Nutrition 0.000 description 6
- 230000036407 pain Effects 0.000 description 6
- 229920002565 Polyethylene Glycol 400 Polymers 0.000 description 5
- 239000000839 emulsion Substances 0.000 description 5
- 238000009472 formulation Methods 0.000 description 5
- JLFNLZLINWHATN-UHFFFAOYSA-N pentaethylene glycol Chemical compound OCCOCCOCCOCCOCCO JLFNLZLINWHATN-UHFFFAOYSA-N 0.000 description 5
- 0 CC1=C(CC(OCCCCOP(*)(*)=O)=O)C2=CC(F)=CC[C@]2C1=Cc(cc1)ccc1S(C)=O Chemical compound CC1=C(CC(OCCCCOP(*)(*)=O)=O)C2=CC(F)=CC[C@]2C1=Cc(cc1)ccc1S(C)=O 0.000 description 4
- 206010046851 Uveitis Diseases 0.000 description 4
- 239000012190 activator Substances 0.000 description 4
- KGBXLFKZBHKPEV-UHFFFAOYSA-N boric acid Chemical compound OB(O)O KGBXLFKZBHKPEV-UHFFFAOYSA-N 0.000 description 4
- 239000004327 boric acid Substances 0.000 description 4
- 229920001223 polyethylene glycol Polymers 0.000 description 4
- ODLHGICHYURWBS-LKONHMLTSA-N trappsol cyclo Chemical compound CC(O)COC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](COCC(C)O)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)COCC(O)C)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1COCC(C)O ODLHGICHYURWBS-LKONHMLTSA-N 0.000 description 4
- 206010002091 Anaesthesia Diseases 0.000 description 3
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 3
- 206010038926 Retinopathy hypertensive Diseases 0.000 description 3
- 102000005789 Vascular Endothelial Growth Factors Human genes 0.000 description 3
- 108010019530 Vascular Endothelial Growth Factors Proteins 0.000 description 3
- 206010064930 age-related macular degeneration Diseases 0.000 description 3
- 230000037005 anaesthesia Effects 0.000 description 3
- 201000001948 hypertensive retinopathy Diseases 0.000 description 3
- 208000002780 macular degeneration Diseases 0.000 description 3
- 208000004644 retinal vein occlusion Diseases 0.000 description 3
- 206010006784 Burning sensation Diseases 0.000 description 2
- 206010038933 Retinopathy of prematurity Diseases 0.000 description 2
- 230000000202 analgesic effect Effects 0.000 description 2
- 238000002844 melting Methods 0.000 description 2
- 230000008018 melting Effects 0.000 description 2
- 229920000136 polysorbate Polymers 0.000 description 2
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 description 2
- 229920002134 Carboxymethyl cellulose Polymers 0.000 description 1
- 206010013774 Dry eye Diseases 0.000 description 1
- 150000007513 acids Chemical class 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 239000001768 carboxy methyl cellulose Substances 0.000 description 1
- 235000010948 carboxy methyl cellulose Nutrition 0.000 description 1
- 239000008112 carboxymethyl-cellulose Substances 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- 229940012356 eye drops Drugs 0.000 description 1
- 239000007924 injection Substances 0.000 description 1
- 238000002347 injection Methods 0.000 description 1
- 229920001427 mPEG Polymers 0.000 description 1
- 239000002480 mineral oil Substances 0.000 description 1
- 235000010446 mineral oil Nutrition 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229920000747 poly(lactic acid) Polymers 0.000 description 1
- 229940065514 poly(lactide) Drugs 0.000 description 1
- 229920000570 polyether Polymers 0.000 description 1
- 230000002028 premature Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762564595P | 2017-09-28 | 2017-09-28 | |
| US62/564,595 | 2017-09-28 | ||
| US201862649273P | 2018-03-28 | 2018-03-28 | |
| US62/649,273 | 2018-03-28 | ||
| PCT/US2018/053451 WO2019067919A1 (en) | 2017-09-28 | 2018-09-28 | COMPOSITIONS AND METHODS FOR TREATING OPHTHALMIC DISORDERS |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020536067A JP2020536067A (ja) | 2020-12-10 |
| JP2020536067A5 true JP2020536067A5 (enExample) | 2021-10-21 |
Family
ID=65903306
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020517956A Pending JP2020536067A (ja) | 2017-09-28 | 2018-09-28 | 眼の状態を処置するための組成物および方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20200246359A1 (enExample) |
| EP (1) | EP3687524A4 (enExample) |
| JP (1) | JP2020536067A (enExample) |
| KR (1) | KR102675246B1 (enExample) |
| CN (1) | CN111629720A (enExample) |
| AU (1) | AU2018339096A1 (enExample) |
| CA (1) | CA3077033A1 (enExample) |
| WO (1) | WO2019067919A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11510931B2 (en) | 2016-09-28 | 2022-11-29 | Medicon Pharmaceuticals, Inc. | Compositions and methods for treating ophthalmic conditions |
| US10744153B1 (en) * | 2019-07-01 | 2020-08-18 | Cloudbreak Therapeutics Llc | Compositions and methods for treating meibomian gland dysfunction |
| CN113144207A (zh) * | 2021-02-07 | 2021-07-23 | 山西利普达医药科技有限公司 | 一种包括聚季铵盐-1的组合物及其应用 |
| JP2024520463A (ja) | 2021-05-24 | 2024-05-24 | メディコン ファーマシューティカルズ,インコーポレイテッド | 化学療法誘発性末梢神経障害に関連する疼痛の処置 |
| EP4272826A3 (en) | 2021-05-24 | 2024-01-17 | Medicon Pharmaceuticals, Inc. | Treating pain associated with diabetic peripheral neuropathy |
| DE102021212692A1 (de) * | 2021-11-11 | 2023-05-11 | Ursapharm Arzneimittel Gmbh | Selbstemulgierende öl-in wasser-mikro- oder nanoemulsion so-wie emulgierende zusammensetzung |
| KR102640323B1 (ko) * | 2021-11-30 | 2024-02-27 | 대우제약 주식회사 | 사이클로스포린의 안정한 나노 현탁액 |
| MD4522143T2 (ro) | 2022-11-23 | 2025-11-30 | Medicon Pharmaceuticals Inc | Tratamentul durerii asociate cu sensibilizare centrală |
| CN115813853B (zh) * | 2022-12-18 | 2024-07-12 | 山东济坤生物制药有限公司 | 一种立他司特滴眼液及其制备方法 |
| WO2025111079A1 (en) | 2023-11-21 | 2025-05-30 | Medicon Pharmaceuticals, Inc. | Isomers of phosphosulindac |
| WO2025122455A1 (en) * | 2023-12-04 | 2025-06-12 | Invirsa, Inc. | Methods for the use of 5'-adenosine diphosphate ribose (adpr) for vegf modulation |
| CN118340721A (zh) * | 2024-04-24 | 2024-07-16 | 现代中医药海河实验室 | 三七总皂苷眼用凝胶制剂及其制备方法和用途 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1129400A (zh) * | 1994-05-06 | 1996-08-21 | 阿尔康实验室公司 | 维生素e生育酚衍生物在眼科组合物中的应用 |
| JPH08175985A (ja) * | 1994-12-26 | 1996-07-09 | Lion Corp | 点眼剤 |
| JP4748289B2 (ja) * | 2000-06-23 | 2011-08-17 | ライオン株式会社 | 点眼剤、眼科用組成物及び吸着抑制方法 |
| JP2004359679A (ja) * | 2003-05-15 | 2004-12-24 | Taisho Pharmaceut Co Ltd | 点眼剤組成物 |
| US20070299124A1 (en) * | 2006-01-25 | 2007-12-27 | Ousler George W Iii | Formulations and methods for treating dry eye |
| WO2008153746A1 (en) * | 2007-05-24 | 2008-12-18 | Aciex Therapeutics, Inc. | Formulations and methods for treating dry eye |
| EP2180788B1 (en) * | 2007-08-10 | 2016-12-21 | Basil Rigas | Anti-inflammatory compounds and uses thereof |
| US20120295979A1 (en) * | 2011-05-03 | 2012-11-22 | Florida Atlantic University | Use of sulindac for protecting retinal pigment epithelial cells against oxidative stress |
| WO2013130625A1 (en) * | 2012-02-27 | 2013-09-06 | Basil Rigas | Phospho-ester derivatives and uses thereof |
| WO2014160702A1 (en) * | 2013-03-25 | 2014-10-02 | Chs Pharma, Inc. | Retinopathy treatment |
| US11510931B2 (en) * | 2016-09-28 | 2022-11-29 | Medicon Pharmaceuticals, Inc. | Compositions and methods for treating ophthalmic conditions |
-
2018
- 2018-09-28 JP JP2020517956A patent/JP2020536067A/ja active Pending
- 2018-09-28 KR KR1020207012350A patent/KR102675246B1/ko active Active
- 2018-09-28 CA CA3077033A patent/CA3077033A1/en active Pending
- 2018-09-28 US US16/651,846 patent/US20200246359A1/en not_active Abandoned
- 2018-09-28 EP EP18860304.7A patent/EP3687524A4/en not_active Withdrawn
- 2018-09-28 AU AU2018339096A patent/AU2018339096A1/en not_active Abandoned
- 2018-09-28 CN CN201880077118.0A patent/CN111629720A/zh active Pending
- 2018-09-28 WO PCT/US2018/053451 patent/WO2019067919A1/en not_active Ceased
-
2021
- 2021-12-22 US US17/559,578 patent/US20220233556A1/en not_active Abandoned
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