TW200813094A - Compounds and compositions as channel activating protease inhibitors - Google Patents

Info

Publication number

TW200813094A

TW200813094A TW096118422A TW96118422A TW200813094A TW 200813094 A TW200813094 A TW 200813094A TW 096118422 A TW096118422 A TW 096118422A TW 96118422 A TW96118422 A TW 96118422A TW 200813094 A TW200813094 A TW 200813094A

Authority

TW

Taiwan

Prior art keywords

compound

reference compound

doc

etoac

group

Prior art date

2006-05-23

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• 150000001875 compounds Chemical class 0.000 title claims abstract description 297
• 230000003213 activating effect Effects 0.000 title claims abstract description 22
• 239000000203 mixture Substances 0.000 title claims description 62
• 239000000137 peptide hydrolase inhibitor Substances 0.000 title description 15
• 229940042399 direct acting antivirals protease inhibitors Drugs 0.000 title description 8
• 238000000034 method Methods 0.000 claims abstract description 117
• 108091005804 Peptidases Proteins 0.000 claims abstract description 48
• 102000035195 Peptidases Human genes 0.000 claims abstract description 47
• 239000004365 Protease Substances 0.000 claims abstract description 47
• 101000798702 Homo sapiens Transmembrane protease serine 4 Proteins 0.000 claims abstract description 22
• 102100032471 Transmembrane protease serine 4 Human genes 0.000 claims abstract description 22
• 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 13
• 102100037942 Suppressor of tumorigenicity 14 protein Human genes 0.000 claims abstract description 11
• 101000897856 Homo sapiens Adenylyl cyclase-associated protein 2 Proteins 0.000 claims abstract description 8
• 101000836079 Homo sapiens Serpin B8 Proteins 0.000 claims abstract description 8
• 101000836075 Homo sapiens Serpin B9 Proteins 0.000 claims abstract description 8
• 101000661807 Homo sapiens Suppressor of tumorigenicity 14 protein Proteins 0.000 claims abstract description 8
• 101000798707 Homo sapiens Transmembrane protease serine 13 Proteins 0.000 claims abstract description 8
• 102100033174 Neutrophil elastase Human genes 0.000 claims abstract description 8
• 102100032467 Transmembrane protease serine 13 Human genes 0.000 claims abstract description 8
• 102000004142 Trypsin Human genes 0.000 claims abstract description 8
• 108090000631 Trypsin Proteins 0.000 claims abstract description 8
• 239000012588 trypsin Substances 0.000 claims abstract description 8
• 102100022046 Brain-specific serine protease 4 Human genes 0.000 claims abstract description 7
• 101000896891 Homo sapiens Brain-specific serine protease 4 Proteins 0.000 claims abstract description 7
• 101000598054 Homo sapiens Transmembrane protease serine 11B Proteins 0.000 claims abstract description 7
• 101000798700 Homo sapiens Transmembrane protease serine 3 Proteins 0.000 claims abstract description 7
• 108010028275 Leukocyte Elastase Proteins 0.000 claims abstract description 7
• 102100037023 Transmembrane protease serine 11B Human genes 0.000 claims abstract description 7
• 108010059081 Cathepsin A Proteins 0.000 claims abstract description 6
• 102000005572 Cathepsin A Human genes 0.000 claims abstract description 6
• 101000637855 Homo sapiens Transmembrane protease serine 11E Proteins 0.000 claims abstract description 6
• 101000638154 Homo sapiens Transmembrane protease serine 2 Proteins 0.000 claims abstract description 6
• 102100032001 Transmembrane protease serine 11E Human genes 0.000 claims abstract description 6
• 102100031989 Transmembrane protease serine 2 Human genes 0.000 claims abstract description 6
• 101100069392 Mus musculus Gzma gene Proteins 0.000 claims abstract description 5
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• QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 3
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• 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 2
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• 125000003039 tetrahydroisoquinolinyl group Chemical group C1(NCCC2=CC=CC=C12)* 0.000 claims description 2
• MWPLVEDNUUSJAV-UHFFFAOYSA-N anthracene Chemical compound C1=CC=CC2=CC3=CC=CC=C3C=C21 MWPLVEDNUUSJAV-UHFFFAOYSA-N 0.000 claims 4
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• 125000003259 prostaglandin group Chemical group 0.000 claims 2
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• 125000005959 diazepanyl group Chemical group 0.000 claims 1
• PCHPORCSPXIHLZ-UHFFFAOYSA-N diphenhydramine hydrochloride Chemical compound [Cl-].C=1C=CC=CC=1C(OCC[NH+](C)C)C1=CC=CC=C1 PCHPORCSPXIHLZ-UHFFFAOYSA-N 0.000 claims 1
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