JP2013522229A5 - - Google Patents

Info

Publication number

JP2013522229A5

JP2013522229A5 JP2012557258A JP2012557258A JP2013522229A5 JP 2013522229 A5 JP2013522229 A5 JP 2013522229A5 JP 2012557258 A JP2012557258 A JP 2012557258A JP 2012557258 A JP2012557258 A JP 2012557258A JP 2013522229 A5 JP2013522229 A5 JP 2013522229A5

Authority

JP

Japan

Prior art keywords

composition

acyl

aryl

hydrogen

pharmaceutical composition

Prior art date

2011-03-10

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

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• 239000000203 mixture Substances 0.000 claims 21
• 239000008194 pharmaceutical composition Substances 0.000 claims 8
• 229910052739 hydrogen Inorganic materials 0.000 claims 7
• 125000002252 acyl group Chemical group 0.000 claims 6
• 125000003118 aryl group Chemical group 0.000 claims 6
• 239000001257 hydrogen Substances 0.000 claims 6
• IXXFZUPTQVDPPK-ZAWHAJPISA-N (1r,2r,4r,6r,7r,8r,10s,13r,14s)-17-[4-[4-(3-aminophenyl)triazol-1-yl]butyl]-7-[(2s,3r,4s,6r)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-13-ethyl-10-fluoro-6-methoxy-2,4,6,8,10,14-hexamethyl-12,15-dioxa-17-azabicyclo[12.3.0]heptadecane-3,9,11,16-tet Chemical compound O([C@@H]1[C@@H](C)C(=O)[C@](C)(F)C(=O)O[C@@H]([C@]2(OC(=O)N(CCCCN3N=NC(=C3)C=3C=C(N)C=CC=3)[C@@H]2[C@@H](C)C(=O)[C@H](C)C[C@@]1(C)OC)C)CC)[C@@H]1O[C@H](C)C[C@H](N(C)C)[C@H]1O IXXFZUPTQVDPPK-ZAWHAJPISA-N 0.000 claims 5
• 239000002535 acidifier Substances 0.000 claims 5
• 125000003545 alkoxy group Chemical group 0.000 claims 5
• 125000000217 alkyl group Chemical group 0.000 claims 5
• 125000004356 hydroxy functional group Chemical group O* 0.000 claims 5
• 125000002877 alkyl aryl group Chemical group 0.000 claims 4
• 125000003710 aryl alkyl group Chemical group 0.000 claims 4
• 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 claims 4
• 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 4
• 125000004404 heteroalkyl group Chemical group 0.000 claims 4
• 125000001072 heteroaryl group Chemical group 0.000 claims 4
• 150000002431 hydrogen Chemical class 0.000 claims 4
• 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
• 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 3
• FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 claims 3
• DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 3
• 229930195725 Mannitol Natural products 0.000 claims 3
• 239000004067 bulking agent Substances 0.000 claims 3
• 229910052799 carbon Inorganic materials 0.000 claims 3
• KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims 3
• 238000010790 dilution Methods 0.000 claims 3
• 239000012895 dilution Substances 0.000 claims 3
• 239000000594 mannitol Substances 0.000 claims 3
• 235000010355 mannitol Nutrition 0.000 claims 3
• 238000007911 parenteral administration Methods 0.000 claims 3
• 239000000546 pharmaceutical excipient Substances 0.000 claims 3
• CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims 2
• 208000035143 Bacterial infection Diseases 0.000 claims 2
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 2
• 239000004471 Glycine Substances 0.000 claims 2
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
• 206010037075 Protozoal infections Diseases 0.000 claims 2
• CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 claims 2
• 229930006000 Sucrose Natural products 0.000 claims 2
• 208000022362 bacterial infectious disease Diseases 0.000 claims 2
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 2
• 150000001875 compounds Chemical class 0.000 claims 2
• 229910052731 fluorine Inorganic materials 0.000 claims 2
• 239000005720 sucrose Substances 0.000 claims 2
• LJGHYPLBDBRCRZ-UHFFFAOYSA-N 3-(3-aminophenyl)sulfonylaniline Chemical group NC1=CC=CC(S(=O)(=O)C=2C=C(N)C=CC=2)=C1 LJGHYPLBDBRCRZ-UHFFFAOYSA-N 0.000 claims 1
• FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 claims 1
• 125000004423 acyloxy group Chemical group 0.000 claims 1
• 230000003113 alkalizing effect Effects 0.000 claims 1
• 125000004450 alkenylene group Chemical group 0.000 claims 1
• 125000005001 aminoaryl group Chemical group 0.000 claims 1
• 230000000844 anti-bacterial effect Effects 0.000 claims 1
• 239000003963 antioxidant agent Substances 0.000 claims 1
• 230000003078 antioxidant effect Effects 0.000 claims 1
• 235000006708 antioxidants Nutrition 0.000 claims 1
• 229960005070 ascorbic acid Drugs 0.000 claims 1
• 235000010323 ascorbic acid Nutrition 0.000 claims 1
• 239000011668 ascorbic acid Substances 0.000 claims 1
• 239000002738 chelating agent Substances 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 235000015165 citric acid Nutrition 0.000 claims 1
• PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• -1 dimethylaminoalkyl Chemical group 0.000 claims 1
• 150000002016 disaccharides Chemical class 0.000 claims 1
• 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
• 208000035475 disorder Diseases 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000011737 fluorine Substances 0.000 claims 1
• 125000001153 fluoro group Chemical group F* 0.000 claims 1
• 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 1
• 125000005842 heteroatom Chemical group 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 150000002772 monosaccharides Chemical class 0.000 claims 1
• 229910052760 oxygen Inorganic materials 0.000 claims 1
• 150000003839 salts Chemical class 0.000 claims 1
• 229910052717 sulfur Inorganic materials 0.000 claims 1
• 239000011975 tartaric acid Substances 0.000 claims 1
• 235000002906 tartaric acid Nutrition 0.000 claims 1