JP2008514732A5 - - Google Patents

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Publication number

JP2008514732A5

JP2008514732A5 JP2007534872A JP2007534872A JP2008514732A5 JP 2008514732 A5 JP2008514732 A5 JP 2008514732A5 JP 2007534872 A JP2007534872 A JP 2007534872A JP 2007534872 A JP2007534872 A JP 2007534872A JP 2008514732 A5 JP2008514732 A5 JP 2008514732A5

Authority

JP

Japan

Prior art keywords

carbon atoms

cyclosporine

different

same

group

Prior art date

2005-09-30

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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• -1 hydroxy, amino Chemical group 0.000 claims 36
• 125000004432 carbon atom Chemical group C* 0.000 claims 35
• 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 claims 32
• 108010036949 Cyclosporine Proteins 0.000 claims 25
• 229960001265 ciclosporin Drugs 0.000 claims 25
• 229930182912 cyclosporin Natural products 0.000 claims 25
• 125000000217 alkyl group Chemical group 0.000 claims 19
• 229910052736 halogen Inorganic materials 0.000 claims 18
• 150000002367 halogens Chemical class 0.000 claims 18
• 239000008194 pharmaceutical composition Substances 0.000 claims 17
• 150000003839 salts Chemical class 0.000 claims 14
• IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 12
• 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 12
• QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 12
• 125000004663 dialkyl amino group Chemical group 0.000 claims 12
• 229910052760 oxygen Inorganic materials 0.000 claims 12
• 239000001301 oxygen Substances 0.000 claims 12
• 229910052757 nitrogen Inorganic materials 0.000 claims 11
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 9
• NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 9
• 229910052739 hydrogen Inorganic materials 0.000 claims 9
• 239000001257 hydrogen Substances 0.000 claims 9
• 229910052717 sulfur Inorganic materials 0.000 claims 9
• 239000011593 sulfur Substances 0.000 claims 9
• 125000000753 cycloalkyl group Chemical group 0.000 claims 7
• 125000003342 alkenyl group Chemical group 0.000 claims 6
• 125000000304 alkynyl group Chemical group 0.000 claims 6
• 125000005842 heteroatom Chemical group 0.000 claims 6
• 125000000623 heterocyclic group Chemical group 0.000 claims 6
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
• 125000006413 ring segment Chemical group 0.000 claims 6
• 229920006395 saturated elastomer Polymers 0.000 claims 6
• 125000001301 ethoxy group Chemical group [H]C([H])([H])C([H])([H])O* 0.000 claims 5
• 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 5
• 208000010710 hepatitis C virus infection Diseases 0.000 claims 5
• 230000002265 prevention Effects 0.000 claims 5
• ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 4
• 125000004066 1-hydroxyethyl group Chemical group [H]OC([H])([*])C([H])([H])[H] 0.000 claims 3
• 125000003545 alkoxy group Chemical group 0.000 claims 3
• 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
• 150000001875 compounds Chemical class 0.000 claims 3
• 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
• 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 3
• 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
• QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
• VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims 2
• KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 2
• AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
• 229910019142 PO4 Inorganic materials 0.000 claims 2
• XBDQKXXYIPTUBI-UHFFFAOYSA-M Propionate Chemical compound CCC([O-])=O XBDQKXXYIPTUBI-UHFFFAOYSA-M 0.000 claims 2
• 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 2
• 125000003253 isopropoxy group Chemical group [H]C([H])([H])C([H])(O*)C([H])([H])[H] 0.000 claims 2
• 238000004519 manufacturing process Methods 0.000 claims 2
• 239000010452 phosphate Substances 0.000 claims 2
• 125000002467 phosphate group Chemical group [H]OP(=O)(O[H])O[*] 0.000 claims 2
• 239000012453 solvate Substances 0.000 claims 2
• 125000000022 2-aminoethyl group Chemical group [H]C([*])([H])C([H])([H])N([H])[H] 0.000 claims 1
• 125000003858 2-ethylbutoxy group Chemical group [H]C([H])([H])C([H])([H])C([H])(C([H])([H])O*)C([H])([H])C([H])([H])[H] 0.000 claims 1
• 125000001137 3-hydroxypropoxy group Chemical group [H]OC([H])([H])C([H])([H])C([H])([H])O* 0.000 claims 1
• JGSIAOZAXBWRFO-UHFFFAOYSA-N 3-methylsulfanyl-1-phenyl-4,5-dihydrobenzo[g]indazole Chemical compound C1CC2=CC=CC=C2C2=C1C(SC)=NN2C1=CC=CC=C1 JGSIAOZAXBWRFO-UHFFFAOYSA-N 0.000 claims 1
• 102000014150 Interferons Human genes 0.000 claims 1
• 108010050904 Interferons Proteins 0.000 claims 1
• ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
• MZVQCMJNVPIDEA-UHFFFAOYSA-N [CH2]CN(CC)CC Chemical group [CH2]CN(CC)CC MZVQCMJNVPIDEA-UHFFFAOYSA-N 0.000 claims 1
• 125000003282 alkyl amino group Chemical group 0.000 claims 1
• 125000002474 dimethylaminoethoxy group Chemical group [H]C([H])([H])N(C([H])([H])[H])C([H])([H])C([H])([H])O* 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 239000003937 drug carrier Substances 0.000 claims 1
• 125000004705 ethylthio group Chemical group C(C)S* 0.000 claims 1
• 229940079322 interferon Drugs 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 1
• 239000000203 mixture Substances 0.000 claims 1
• 125000002572 propoxy group Chemical group [*]OC([H])([H])C(C([H])([H])[H])([H])[H] 0.000 claims 1
• 229940126585 therapeutic drug Drugs 0.000 claims 1