JP2012521997A5 - - Google Patents

Info

Publication number

JP2012521997A5

JP2012521997A5 JP2012502224A JP2012502224A JP2012521997A5 JP 2012521997 A5 JP2012521997 A5 JP 2012521997A5 JP 2012502224 A JP2012502224 A JP 2012502224A JP 2012502224 A JP2012502224 A JP 2012502224A JP 2012521997 A5 JP2012521997 A5 JP 2012521997A5

Authority

JP

Japan

Prior art keywords

compound

weight percent

antihypertensive agent

microspheres

implant

Prior art date

2010-03-25

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.)

Pending

Links

• Espacenet
• Global Dossier
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• 150000001875 compounds Chemical class 0.000 claims 32
• 229940030600 antihypertensive agent Drugs 0.000 claims 13
• 239000002220 antihypertensive agent Substances 0.000 claims 13
• 239000004005 microsphere Substances 0.000 claims 11
• 229920002988 biodegradable polymer Polymers 0.000 claims 10
• 239000004621 biodegradable polymer Substances 0.000 claims 10
• 239000007943 implant Substances 0.000 claims 10
• 229960001160 latanoprost Drugs 0.000 claims 8
• GGXICVAJURFBLW-CEYXHVGTSA-N latanoprost Chemical compound 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 8
• 230000004406 elevated intraocular pressure Effects 0.000 claims 7
• 239000000203 mixture Substances 0.000 claims 7
• 238000013268 sustained release Methods 0.000 claims 6
• 239000012730 sustained-release form Substances 0.000 claims 6
• 230000004410 intraocular pressure Effects 0.000 claims 5
• 150000003839 salts Chemical class 0.000 claims 5
• 229940126062 Compound A Drugs 0.000 claims 4
• NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 4
• 210000002159 anterior chamber Anatomy 0.000 claims 4
• JNGZXGGOCLZBFB-IVCQMTBJSA-N compound E Chemical compound N([C@@H](C)C(=O)N[C@@H]1C(N(C)C2=CC=CC=C2C(C=2C=CC=CC=2)=N1)=O)C(=O)CC1=CC(F)=CC(F)=C1 JNGZXGGOCLZBFB-IVCQMTBJSA-N 0.000 claims 3
• FVIZARNDLVOMSU-UHFFFAOYSA-N ginsenoside K Natural products C1CC(C2(CCC3C(C)(C)C(O)CCC3(C)C2CC2O)C)(C)C2C1C(C)(CCC=C(C)C)OC1OC(CO)C(O)C(O)C1O FVIZARNDLVOMSU-UHFFFAOYSA-N 0.000 claims 3
• ZTQSADJAYQOCDD-UHFFFAOYSA-N ginsenoside-Rd2 Natural products C1CC(C2(CCC3C(C)(C)C(OC4C(C(O)C(O)C(CO)O4)O)CCC3(C)C2CC2O)C)(C)C2C1C(C)(CCC=C(C)C)OC(C(C(O)C1O)O)OC1COC1OCC(O)C(O)C1O ZTQSADJAYQOCDD-UHFFFAOYSA-N 0.000 claims 3
• 238000004519 manufacturing process Methods 0.000 claims 3
• 229920000642 polymer Polymers 0.000 claims 3
• LVTJOONKWUXEFR-FZRMHRINSA-N protoneodioscin Natural products O(C[C@@H](CC[C@]1(O)[C@H](C)[C@@H]2[C@]3(C)[C@H]([C@H]4[C@@H]([C@]5(C)C(=CC4)C[C@@H](O[C@@H]4[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@@H](O)[C@H](O[C@H]6[C@@H](O)[C@@H](O)[C@@H](O)[C@H](C)O6)[C@H](CO)O4)CC5)CC3)C[C@@H]2O1)C)[C@H]1[C@H](O)[C@H](O)[C@H](O)[C@@H](CO)O1 LVTJOONKWUXEFR-FZRMHRINSA-N 0.000 claims 3
• KIUKXJAPPMFGSW-DNGZLQJQSA-N (2S,3S,4S,5R,6R)-6-[(2S,3R,4R,5S,6R)-3-Acetamido-2-[(2S,3S,4R,5R,6R)-6-[(2R,3R,4R,5S,6R)-3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-2-carboxy-4,5-dihydroxyoxan-3-yl]oxy-5-hydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid Chemical compound CC(=O)N[C@H]1[C@H](O)O[C@H](CO)[C@@H](O)[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O[C@H]3[C@@H]([C@@H](O)[C@H](O)[C@H](O3)C(O)=O)O)[C@H](O)[C@@H](CO)O2)NC(C)=O)[C@@H](C(O)=O)O1 KIUKXJAPPMFGSW-DNGZLQJQSA-N 0.000 claims 2
• 229960002470 bimatoprost Drugs 0.000 claims 2
• 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 2
• 150000002148 esters Chemical class 0.000 claims 2
• 229920002674 hyaluronan Polymers 0.000 claims 2
• 229960003160 hyaluronic acid Drugs 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 229920000747 poly(lactic acid) Polymers 0.000 claims 2
• 229940002612 prodrug Drugs 0.000 claims 2
• 239000000651 prodrug Substances 0.000 claims 2
• 229960002368 travoprost Drugs 0.000 claims 2
• MKPLKVHSHYCHOC-AHTXBMBWSA-N travoprost 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(C(F)(F)F)=C1 MKPLKVHSHYCHOC-AHTXBMBWSA-N 0.000 claims 2
• 208000010412 Glaucoma Diseases 0.000 claims 1
• 238000006065 biodegradation reaction Methods 0.000 claims 1
• 238000012377 drug delivery Methods 0.000 claims 1
• 239000011521 glass Substances 0.000 claims 1
• 239000004626 polylactic acid Substances 0.000 claims 1
• 229940117828 polylactic acid-polyglycolic acid copolymer Drugs 0.000 claims 1
• 230000001225 therapeutic effect Effects 0.000 claims 1
• 210000001585 trabecular meshwork Anatomy 0.000 claims 1
• KWSBJDFUFKXKNW-UHFFFAOYSA-N CC(C)OC(COc1cc(NC(c(cc(cc2)-c3cc(F)ccc3)c2F)=O)ccc1)=O Chemical compound CC(C)OC(COc1cc(NC(c(cc(cc2)-c3cc(F)ccc3)c2F)=O)ccc1)=O KWSBJDFUFKXKNW-UHFFFAOYSA-N 0.000 description 1
• WYWNQAGBBPVQMT-KEKNWZKVSA-N CCCCC[C@@H](c(cc1)ccc1N(C(CCCc1ccc(C(OC(C)C)=O)[s]1)C(N1)=O)C1=O)O Chemical compound CCCCC[C@@H](c(cc1)ccc1N(C(CCCc1ccc(C(OC(C)C)=O)[s]1)C(N1)=O)C1=O)O WYWNQAGBBPVQMT-KEKNWZKVSA-N 0.000 description 1