JP2013513596A5 - - Google Patents

Info

Publication number

JP2013513596A5

JP2013513596A5 JP2012542622A JP2012542622A JP2013513596A5 JP 2013513596 A5 JP2013513596 A5 JP 2013513596A5 JP 2012542622 A JP2012542622 A JP 2012542622A JP 2012542622 A JP2012542622 A JP 2012542622A JP 2013513596 A5 JP2013513596 A5 JP 2013513596A5

Authority

JP

Japan

Prior art keywords

alkyl

compound

hck

activity

optionally substituted

Prior art date

2010-12-10

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.)

Pending

Links

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• 150000001875 compounds Chemical class 0.000 claims 24
• 125000000217 alkyl group Chemical group 0.000 claims 18
• 230000000694 effects Effects 0.000 claims 13
• 241000712461 unidentified influenza virus Species 0.000 claims 6
• 230000002401 inhibitory effect Effects 0.000 claims 5
• 150000003839 salts Chemical class 0.000 claims 5
• 239000000126 substance Substances 0.000 claims 5
• 102100027389 Tyrosine-protein kinase HCK Human genes 0.000 claims 4
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 4
• 208000015181 infectious disease Diseases 0.000 claims 4
• 238000000034 method Methods 0.000 claims 4
• 229910052757 nitrogen Inorganic materials 0.000 claims 4
• 229910052760 oxygen Inorganic materials 0.000 claims 4
• 229910052717 sulfur Inorganic materials 0.000 claims 4
• 125000003545 alkoxy group Chemical group 0.000 claims 3
• 229910052799 carbon Inorganic materials 0.000 claims 3
• 125000004663 dialkyl amino group Chemical group 0.000 claims 3
• 239000003814 drug Substances 0.000 claims 3
• 229910052736 halogen Inorganic materials 0.000 claims 3
• 125000005842 heteroatom Chemical group 0.000 claims 3
• 125000000623 heterocyclic group Chemical group 0.000 claims 3
• 239000003112 inhibitor Substances 0.000 claims 3
• 230000002265 prevention Effects 0.000 claims 3
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
• 238000012216 screening Methods 0.000 claims 3
• 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
• 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
• 102000004190 Enzymes Human genes 0.000 claims 2
• 108090000790 Enzymes Proteins 0.000 claims 2
• 102000014150 Interferons Human genes 0.000 claims 2
• 108010050904 Interferons Proteins 0.000 claims 2
• QNRRHYPPQFELSF-CNYIRLTGSA-N Laninamivir Chemical compound OC[C@@H](O)[C@@H](OC)[C@@H]1OC(C(O)=O)=C[C@H](N=C(N)N)[C@H]1NC(C)=O QNRRHYPPQFELSF-CNYIRLTGSA-N 0.000 claims 2
• 108010046934 Proto-Oncogene Proteins c-hck Proteins 0.000 claims 2
• 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 2
• 239000003443 antiviral agent Substances 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 239000013000 chemical inhibitor Substances 0.000 claims 2
• 229940079593 drug Drugs 0.000 claims 2
• 238000002866 fluorescence resonance energy transfer Methods 0.000 claims 2
• 125000005843 halogen group Chemical group 0.000 claims 2
• 150000002367 halogens Chemical group 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 229910052739 hydrogen Inorganic materials 0.000 claims 2
• 229940079322 interferon Drugs 0.000 claims 2
• 229950004244 laninamivir Drugs 0.000 claims 2
• VSZGPKBBMSAYNT-RRFJBIMHSA-N oseltamivir Chemical compound CCOC(=O)C1=C[C@@H](OC(CC)CC)[C@H](NC(C)=O)[C@@H](N)C1 VSZGPKBBMSAYNT-RRFJBIMHSA-N 0.000 claims 2
• 229960003752 oseltamivir Drugs 0.000 claims 2
• XRQDFNLINLXZLB-CKIKVBCHSA-N peramivir Chemical compound CCC(CC)[C@H](NC(C)=O)[C@@H]1[C@H](O)[C@@H](C(O)=O)C[C@H]1NC(N)=N XRQDFNLINLXZLB-CKIKVBCHSA-N 0.000 claims 2
• 229960001084 peramivir Drugs 0.000 claims 2
• 230000026731 phosphorylation Effects 0.000 claims 2
• 238000006366 phosphorylation reaction Methods 0.000 claims 2
• 108090000765 processed proteins & peptides Proteins 0.000 claims 2
• 229960000329 ribavirin Drugs 0.000 claims 2
• 229920006395 saturated elastomer Polymers 0.000 claims 2
• 239000012453 solvate Substances 0.000 claims 2
• 230000009385 viral infection Effects 0.000 claims 2
• 229960001028 zanamivir Drugs 0.000 claims 2
• ARAIBEBZBOPLMB-UFGQHTETSA-N zanamivir Chemical compound CC(=O)N[C@@H]1[C@@H](N=C(N)N)C=C(C(O)=O)O[C@H]1[C@H](O)[C@H](O)CO ARAIBEBZBOPLMB-UFGQHTETSA-N 0.000 claims 2
• 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 1
• 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
• MTEZLAATISORQK-UHFFFAOYSA-N 2-methoxyacetamide Chemical compound COCC(N)=O MTEZLAATISORQK-UHFFFAOYSA-N 0.000 claims 1
• -1 4- (4- (3- (3-tert-butyl-1-p-tolyl-1H-pyrazol-5-yl) ureido) naphthalen-1-yloxy) pyridin-2-yl Chemical group 0.000 claims 1
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
• 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
• 208000017667 Chronic Disease Diseases 0.000 claims 1
• 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
• MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
• 206010019280 Heart failures Diseases 0.000 claims 1
• 108091030071 RNAI Proteins 0.000 claims 1
• 208000001647 Renal Insufficiency Diseases 0.000 claims 1
• 125000002947 alkylene group Chemical group 0.000 claims 1
• 125000004429 atom Chemical group 0.000 claims 1
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
• 210000004027 cell Anatomy 0.000 claims 1
• 239000003795 chemical substances by application Substances 0.000 claims 1
• 238000002512 chemotherapy Methods 0.000 claims 1
• 230000002860 competitive effect Effects 0.000 claims 1
• 206010012601 diabetes mellitus Diseases 0.000 claims 1
• WJJMNDUMQPNECX-UHFFFAOYSA-N dipicolinic acid Chemical compound OC(=O)C1=CC=CC(C(O)=O)=N1 WJJMNDUMQPNECX-UHFFFAOYSA-N 0.000 claims 1
• 230000009368 gene silencing by RNA Effects 0.000 claims 1
• 125000004404 heteroalkyl group Chemical group 0.000 claims 1
• 238000000338 in vitro Methods 0.000 claims 1
• 230000005764 inhibitory process Effects 0.000 claims 1
• 201000006370 kidney failure Diseases 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• AVUUHIYJPTWYNX-UHFFFAOYSA-N n-[4-[4-[[5-tert-butyl-2-(4-methylphenyl)pyrazol-3-yl]carbamoylamino]naphthalen-1-yl]oxypyridin-2-yl]-2-methoxyacetamide Chemical compound C1=NC(NC(=O)COC)=CC(OC=2C3=CC=CC=C3C(NC(=O)NC=3N(N=C(C=3)C(C)(C)C)C=3C=CC(C)=CC=3)=CC=2)=C1 AVUUHIYJPTWYNX-UHFFFAOYSA-N 0.000 claims 1
• 125000001624 naphthyl group Chemical group 0.000 claims 1
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
• 230000036963 noncompetitive effect Effects 0.000 claims 1
• 125000004043 oxo group Chemical group O=* 0.000 claims 1
• 239000001301 oxygen Substances 0.000 claims 1
• 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
• 230000002685 pulmonary effect Effects 0.000 claims 1
• 125000001424 substituent group Chemical group 0.000 claims 1
• 125000004434 sulfur atom Chemical group 0.000 claims 1
• 230000009885 systemic effect Effects 0.000 claims 1