JP2017533228A5 - - Google Patents

Info

Publication number

JP2017533228A5

JP2017533228A5 JP2017523822A JP2017523822A JP2017533228A5 JP 2017533228 A5 JP2017533228 A5 JP 2017533228A5 JP 2017523822 A JP2017523822 A JP 2017523822A JP 2017523822 A JP2017523822 A JP 2017523822A JP 2017533228 A5 JP2017533228 A5 JP 2017533228A5

Authority

JP

Japan

Prior art keywords

substituted

unsubstituted

group

composition

composition according

Prior art date

2015-11-02

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

Links

• Espacenet
• Global Dossier
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• 239000000203 mixture Substances 0.000 claims 14
• 125000000217 alkyl group Chemical group 0.000 claims 6
• -1 carbohydrate compound Chemical class 0.000 claims 6
• 125000002009 alkene group Chemical group 0.000 claims 4
• 125000001033 ether group Chemical group 0.000 claims 4
• 229910052739 hydrogen Inorganic materials 0.000 claims 4
• 239000001257 hydrogen Substances 0.000 claims 4
• 229940079593 drug Drugs 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• 229930105110 Cyclosporin A Natural products 0.000 claims 2
• 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 2
• 108010036949 Cyclosporine Proteins 0.000 claims 2
• 208000003556 Dry Eye Syndromes Diseases 0.000 claims 2
• 206010013774 Dry eye Diseases 0.000 claims 2
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
• 125000003368 amide group Chemical group 0.000 claims 2
• 125000003277 amino group Chemical group 0.000 claims 2
• 206010069664 atopic keratoconjunctivitis Diseases 0.000 claims 2
• 229960001265 ciclosporin Drugs 0.000 claims 2
• 150000002431 hydrogen Chemical class 0.000 claims 2
• 125000001165 hydrophobic group Chemical group 0.000 claims 2
• 229960003444 immunosuppressant agent Drugs 0.000 claims 2
• 230000001861 immunosuppressant effect Effects 0.000 claims 2
• 239000003018 immunosuppressive agent Substances 0.000 claims 2
• 239000003120 macrolide antibiotic agent Substances 0.000 claims 2
• 239000008194 pharmaceutical composition Substances 0.000 claims 2
• 229920000642 polymer Polymers 0.000 claims 2
• 125000000547 substituted alkyl group Chemical group 0.000 claims 2
• BXCRLBBIZJSWNS-UHFFFAOYSA-N 2-hydroxyethyl hexadecanoate Chemical compound CCCCCCCCCCCCCCCC(=O)OCCO BXCRLBBIZJSWNS-UHFFFAOYSA-N 0.000 claims 1
• 229920001661 Chitosan Polymers 0.000 claims 1
• 206010010804 Contact lens intolerance Diseases 0.000 claims 1
• 201000004624 Dermatitis Diseases 0.000 claims 1
• HKVAMNSJSFKALM-GKUWKFKPSA-N Everolimus Chemical compound C1C[C@@H](OCCO)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 HKVAMNSJSFKALM-GKUWKFKPSA-N 0.000 claims 1
• 208000022873 Ocular disease Diseases 0.000 claims 1
• 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
• QJJXYPPXXYFBGM-LFZNUXCKSA-N Tacrolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1\C=C(/C)[C@@H]1[C@H](C)[C@@H](O)CC(=O)[C@H](CC=C)/C=C(C)/C[C@H](C)C[C@H](OC)[C@H]([C@H](C[C@H]2C)OC)O[C@@]2(O)C(=O)C(=O)N2CCCC[C@H]2C(=O)O1 QJJXYPPXXYFBGM-LFZNUXCKSA-N 0.000 claims 1
• 208000010668 atopic eczema Diseases 0.000 claims 1
• 229960005167 everolimus Drugs 0.000 claims 1
• 206010023332 keratitis Diseases 0.000 claims 1
• 201000010666 keratoconjunctivitis Diseases 0.000 claims 1
• 150000002632 lipids Chemical class 0.000 claims 1
• 230000026792 palmitoylation Effects 0.000 claims 1
• 239000002245 particle Substances 0.000 claims 1
• 239000000546 pharmaceutical excipient Substances 0.000 claims 1
• 125000001453 quaternary ammonium group Chemical group 0.000 claims 1
• 238000005956 quaternization reaction Methods 0.000 claims 1
• ZAHRKKWIAAJSAO-UHFFFAOYSA-N rapamycin Natural products COCC(O)C(=C/C(C)C(=O)CC(OC(=O)C1CCCCN1C(=O)C(=O)C2(O)OC(CC(OC)C(=CC=CC=CC(C)CC(C)C(=O)C)C)CCC2C)C(C)CC3CCC(O)C(C3)OC)C ZAHRKKWIAAJSAO-UHFFFAOYSA-N 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 238000001338 self-assembly Methods 0.000 claims 1
• QFJCIRLUMZQUOT-HPLJOQBZSA-N sirolimus Chemical compound C1C[C@@H](O)[C@H](OC)C[C@@H]1C[C@@H](C)[C@H]1OC(=O)[C@@H]2CCCCN2C(=O)C(=O)[C@](O)(O2)[C@H](C)CC[C@H]2C[C@H](OC)/C(C)=C/C=C/C=C/[C@@H](C)C[C@@H](C)C(=O)[C@H](OC)[C@H](O)/C(C)=C/[C@@H](C)C(=O)C1 QFJCIRLUMZQUOT-HPLJOQBZSA-N 0.000 claims 1
• 229960002930 sirolimus Drugs 0.000 claims 1
• 238000001356 surgical procedure Methods 0.000 claims 1
• QJJXYPPXXYFBGM-SHYZHZOCSA-N tacrolimus Natural products CO[C@H]1C[C@H](CC[C@@H]1O)C=C(C)[C@H]2OC(=O)[C@H]3CCCCN3C(=O)C(=O)[C@@]4(O)O[C@@H]([C@H](C[C@H]4C)OC)[C@@H](C[C@H](C)CC(=C[C@@H](CC=C)C(=O)C[C@H](O)[C@H]2C)C)OC QJJXYPPXXYFBGM-SHYZHZOCSA-N 0.000 claims 1
• 229960001967 tacrolimus Drugs 0.000 claims 1
• 230000000699 topical effect Effects 0.000 claims 1
• 238000002054 transplantation Methods 0.000 claims 1