CA2583494C - 3-ether and 3-thioether substituted cyclosporin derivatives for the treatment and prevention of hepatitis c infection - Google Patents

Info

Publication number

CA2583494C

CA2583494C CA2583494A CA2583494A CA2583494C CA 2583494 C CA2583494 C CA 2583494C CA 2583494 A CA2583494 A CA 2583494A CA 2583494 A CA2583494 A CA 2583494A CA 2583494 C CA2583494 C CA 2583494C

Authority

CA

Canada

Prior art keywords

carbon atoms

cyclosporin

branched

straight

same

Prior art date

2004-10-01

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.)

Expired - Fee Related

Links

• Espacenet
• Global Dossier
• CIPO
• Discuss

• PMATZTZNYRCHOR-CGLBZJNRSA-N Cyclosporin A Chemical class 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 title claims abstract description 133
• 238000011282 treatment Methods 0.000 title claims abstract description 34
• 208000010710 hepatitis C virus infection Diseases 0.000 title claims description 28
• RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 title description 26
• 208000005176 Hepatitis C Diseases 0.000 title description 21
• 230000002265 prevention Effects 0.000 title description 16
• 150000001875 compounds Chemical class 0.000 claims description 178
• 229960001265 ciclosporin Drugs 0.000 claims description 116
• 239000000203 mixture Substances 0.000 claims description 106
• 108010036949 Cyclosporine Proteins 0.000 claims description 100
• 229930182912 cyclosporin Natural products 0.000 claims description 96
• 229930105110 Cyclosporin A Natural products 0.000 claims description 92
• -1 hydroxy, amino Chemical group 0.000 claims description 83
• 150000003839 salts Chemical class 0.000 claims description 79
• 125000004432 carbon atom Chemical group C* 0.000 claims description 72
• 239000002552 dosage form Substances 0.000 claims description 51
• 125000000217 alkyl group Chemical group 0.000 claims description 50
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 30
• 239000003814 drug Substances 0.000 claims description 29
• 108010050904 Interferons Proteins 0.000 claims description 27
• 102000014150 Interferons Human genes 0.000 claims description 27
• 229940079322 interferon Drugs 0.000 claims description 27
• 229910052736 halogen Inorganic materials 0.000 claims description 26
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 24
• 229910052757 nitrogen Inorganic materials 0.000 claims description 24
• 229910052760 oxygen Inorganic materials 0.000 claims description 24
• 239000001301 oxygen Substances 0.000 claims description 24
• 150000002367 halogens Chemical class 0.000 claims description 23
• NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 20
• 239000001257 hydrogen Substances 0.000 claims description 19
• 229910052739 hydrogen Inorganic materials 0.000 claims description 19
• 229910052717 sulfur Inorganic materials 0.000 claims description 19
• 239000011593 sulfur Substances 0.000 claims description 19
• 125000004453 alkoxycarbonyl group Chemical group 0.000 claims description 18
• 125000004663 dialkyl amino group Chemical group 0.000 claims description 15
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 14
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 14
• 125000000753 cycloalkyl group Chemical group 0.000 claims description 13
• 125000003342 alkenyl group Chemical group 0.000 claims description 12
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims description 12
• 125000006413 ring segment Chemical group 0.000 claims description 12
• 125000000304 alkynyl group Chemical group 0.000 claims description 11
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims description 11
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 11
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• 125000000623 heterocyclic group Chemical group 0.000 claims description 10
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• 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 7
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• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 7
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• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 5
• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 5
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
• 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims description 2
• 125000004705 ethylthio group Chemical group C(C)S* 0.000 claims description 2
• 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims description 2
• 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
• MZVQCMJNVPIDEA-UHFFFAOYSA-N [CH2]CN(CC)CC Chemical group [CH2]CN(CC)CC MZVQCMJNVPIDEA-UHFFFAOYSA-N 0.000 claims 1
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• HEDRZPFGACZZDS-MICDWDOJSA-N Trichloro(2H)methane Chemical compound [2H]C(Cl)(Cl)Cl HEDRZPFGACZZDS-MICDWDOJSA-N 0.000 description 10
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