EA024171B1 - Ингибиторы вируса гепатита с - Google Patents

Info

Publication number

EA024171B1

EA024171B1 EA201390190A EA201390190A EA024171B1 EA 024171 B1 EA024171 B1 EA 024171B1 EA 201390190 A EA201390190 A EA 201390190A EA 201390190 A EA201390190 A EA 201390190A EA 024171 B1 EA024171 B1 EA 024171B1

Authority

EA

Eurasian Patent Office

Prior art keywords

mmol

sar

mixture

hcv

stage

Prior art date

2010-08-12

Links

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• 241000711549 Hepacivirus C Species 0.000 title claims abstract description 87
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• 238000000034 method Methods 0.000 claims abstract description 50
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• 229910052757 nitrogen Inorganic materials 0.000 claims description 53
• 230000000840 anti-viral effect Effects 0.000 claims description 51
• 125000000217 alkyl group Chemical group 0.000 claims description 42
• 102000014150 Interferons Human genes 0.000 claims description 32
• 108010050904 Interferons Proteins 0.000 claims description 32
• 229940079322 interferon Drugs 0.000 claims description 31
• 108090000623 proteins and genes Proteins 0.000 claims description 18
• IWUCXVSUMQZMFG-AFCXAGJDSA-N Ribavirin Chemical compound N1=C(C(=O)N)N=CN1[C@H]1[C@H](O)[C@H](O)[C@@H](CO)O1 IWUCXVSUMQZMFG-AFCXAGJDSA-N 0.000 claims description 17
• 102000004169 proteins and genes Human genes 0.000 claims description 17
• 229960000329 ribavirin Drugs 0.000 claims description 16
• HZCAHMRRMINHDJ-DBRKOABJSA-N ribavirin Natural products O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1N=CN=C1 HZCAHMRRMINHDJ-DBRKOABJSA-N 0.000 claims description 16
• 108010047761 Interferon-alpha Proteins 0.000 claims description 14
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• 229910052799 carbon Inorganic materials 0.000 claims description 11
• 125000004435 hydrogen atom Chemical group [H]* 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
• 210000002845 virion Anatomy 0.000 claims description 9
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• JRGLVBAMCARXFL-UHFFFAOYSA-N [1-[2-[5-[4-[4-[2-[1-[2-(methoxycarbonylamino)-3-methylbutanoyl]pyrrolidin-2-yl]-1H-imidazol-5-yl]phenyl]naphthalen-1-yl]-1H-imidazol-2-yl]pyrrolidin-1-yl]-3-methyl-1-oxobutan-2-yl]carbamic acid Chemical compound COC(=O)NC(C(C)C)C(=O)N1CCCC1C1=NC=C(C=2C=CC(=CC=2)C=2C3=CC=CC=C3C(C=3NC(=NC=3)C3N(CCC3)C(=O)C(NC(O)=O)C(C)C)=CC=2)N1 JRGLVBAMCARXFL-UHFFFAOYSA-N 0.000 claims description 4
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• 125000000623 heterocyclic group Chemical group 0.000 description 25
• 125000001424 substituent group Chemical group 0.000 description 25
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• RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 description 24
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• 238000000132 electrospray ionisation Methods 0.000 description 22
• 239000000706 filtrate Substances 0.000 description 22
• 239000011734 sodium Substances 0.000 description 22
• 238000003756 stirring Methods 0.000 description 22
• DTQVDTLACAAQTR-UHFFFAOYSA-N trifluoroacetic acid Substances OC(=O)C(F)(F)F DTQVDTLACAAQTR-UHFFFAOYSA-N 0.000 description 21
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• 239000005909 Kieselgur Substances 0.000 description 18
• HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 description 18
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