JP2013530179A5 - - Google Patents

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Publication number

JP2013530179A5

JP2013530179A5 JP2013514786A JP2013514786A JP2013530179A5 JP 2013530179 A5 JP2013530179 A5 JP 2013530179A5 JP 2013514786 A JP2013514786 A JP 2013514786A JP 2013514786 A JP2013514786 A JP 2013514786A JP 2013530179 A5 JP2013530179 A5 JP 2013530179A5

Authority

JP

Japan

Prior art keywords

alkyl

nhc

och

compound

integer

Prior art date

2011-06-17

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.)

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• 125000000217 alkyl group Chemical group 0.000 claims 23
• 150000001875 compounds Chemical class 0.000 claims 10
• 239000000203 mixture Substances 0.000 claims 8
• 230000000155 isotopic effect Effects 0.000 claims 7
• 150000003839 salts Chemical class 0.000 claims 6
• 206010061603 Respiratory syncytial virus infection Diseases 0.000 claims 5
• 229910052757 nitrogen Inorganic materials 0.000 claims 5
• 229910052760 oxygen Inorganic materials 0.000 claims 5
• 229910052799 carbon Inorganic materials 0.000 claims 4
• 125000005842 heteroatom Chemical group 0.000 claims 4
• 229910052717 sulfur Inorganic materials 0.000 claims 4
• 125000003545 alkoxy group Chemical group 0.000 claims 3
• 239000003443 antiviral agent Substances 0.000 claims 3
• 229910052736 halogen Inorganic materials 0.000 claims 3
• 125000000623 heterocyclic group Chemical group 0.000 claims 3
• 229910052739 hydrogen Inorganic materials 0.000 claims 3
• 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
• 230000002265 prevention Effects 0.000 claims 3
• 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
• 229920006395 saturated elastomer Polymers 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
• LRFVTYWOQMYALW-UHFFFAOYSA-N 9H-xanthine Chemical class O=C1NC(=O)NC2=C1NC=N2 LRFVTYWOQMYALW-UHFFFAOYSA-N 0.000 claims 2
• 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 2
• 201000003883 Cystic fibrosis Diseases 0.000 claims 2
• 241000725643 Respiratory syncytial virus Species 0.000 claims 2
• 230000000840 anti-viral effect Effects 0.000 claims 2
• 125000003118 aryl group Chemical group 0.000 claims 2
• 208000006673 asthma Diseases 0.000 claims 2
• 125000004429 atom Chemical group 0.000 claims 2
• 229940125388 beta agonist Drugs 0.000 claims 2
• 206010006451 bronchitis Diseases 0.000 claims 2
• 239000003246 corticosteroid Substances 0.000 claims 2
• 238000011257 definitive treatment Methods 0.000 claims 2
• 150000002367 halogens Chemical group 0.000 claims 2
• 125000001072 heteroaryl group Chemical group 0.000 claims 2
• 239000003149 muscarinic antagonist Substances 0.000 claims 2
• 125000001624 naphthyl group Chemical group 0.000 claims 2
• 239000002571 phosphodiesterase inhibitor Substances 0.000 claims 2
• 208000023504 respiratory system disease Diseases 0.000 claims 2
• 229940065721 systemic for obstructive airway disease xanthines Drugs 0.000 claims 2
• ZFXYFBGIUFBOJW-UHFFFAOYSA-N theophylline Chemical compound O=C1N(C)C(=O)N(C)C2=C1NC=N2 ZFXYFBGIUFBOJW-UHFFFAOYSA-N 0.000 claims 2
• XWTYSIMOBUGWOL-UHFFFAOYSA-N (+-)-Terbutaline Chemical group CC(C)(C)NCC(O)C1=CC(O)=CC(O)=C1 XWTYSIMOBUGWOL-UHFFFAOYSA-N 0.000 claims 1
• 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 1
• 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
• MTPVBMVUENFFLL-HXUWFJFHSA-N 1-(2-fluorophenyl)-3-[(3s)-2-oxo-5-phenyl-1,3-dihydro-1,4-benzodiazepin-3-yl]urea Chemical compound FC1=CC=CC=C1NC(=O)N[C@@H]1C(=O)NC2=CC=CC=C2C(C=2C=CC=CC=2)=N1 MTPVBMVUENFFLL-HXUWFJFHSA-N 0.000 claims 1
• MTEZLAATISORQK-UHFFFAOYSA-N 2-methoxyacetamide Chemical compound COCC(N)=O MTEZLAATISORQK-UHFFFAOYSA-N 0.000 claims 1
• 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
• KUVIULQEHSCUHY-XYWKZLDCSA-N Beclometasone Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@]2(Cl)[C@@H]1[C@@H]1C[C@H](C)[C@@](C(=O)COC(=O)CC)(OC(=O)CC)[C@@]1(C)C[C@@H]2O KUVIULQEHSCUHY-XYWKZLDCSA-N 0.000 claims 1
• VOVIALXJUBGFJZ-KWVAZRHASA-N Budesonide Chemical compound C1CC2=CC(=O)C=C[C@]2(C)[C@@H]2[C@@H]1[C@@H]1C[C@H]3OC(CCC)O[C@@]3(C(=O)CO)[C@@]1(C)C[C@@H]2O VOVIALXJUBGFJZ-KWVAZRHASA-N 0.000 claims 1
• JGLMVXWAHNTPRF-CMDGGOBGSA-N CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O Chemical compound CCN1N=C(C)C=C1C(=O)NC1=NC2=CC(=CC(OC)=C2N1C\C=C\CN1C(NC(=O)C2=CC(C)=NN2CC)=NC2=CC(=CC(OCCCN3CCOCC3)=C12)C(N)=O)C(N)=O JGLMVXWAHNTPRF-CMDGGOBGSA-N 0.000 claims 1
• OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
• MYMOFIZGZYHOMD-UHFFFAOYSA-N Dioxygen Chemical compound O=O MYMOFIZGZYHOMD-UHFFFAOYSA-N 0.000 claims 1
• UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
• 229940099471 Phosphodiesterase inhibitor Drugs 0.000 claims 1
• 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 1
• GIIZNNXWQWCKIB-UHFFFAOYSA-N Serevent Chemical compound C1=C(O)C(CO)=CC(C(O)CNCCCCCCOCCCCC=2C=CC=CC=2)=C1 GIIZNNXWQWCKIB-UHFFFAOYSA-N 0.000 claims 1
• 239000004480 active ingredient Substances 0.000 claims 1
• NDAUXUAQIAJITI-UHFFFAOYSA-N albuterol Chemical compound CC(C)(C)NCC(O)C1=CC=C(O)C(CO)=C1 NDAUXUAQIAJITI-UHFFFAOYSA-N 0.000 claims 1
• 125000002947 alkylene group Chemical group 0.000 claims 1
• 230000001548 androgenic effect Effects 0.000 claims 1
• 229950000210 beclometasone dipropionate Drugs 0.000 claims 1
• -1 beta agonists Substances 0.000 claims 1
• 229960004436 budesonide Drugs 0.000 claims 1
• 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 1
• 229940082638 cardiac stimulant phosphodiesterase inhibitors Drugs 0.000 claims 1
• 239000000969 carrier Substances 0.000 claims 1
• 229960001334 corticosteroids Drugs 0.000 claims 1
• 230000006735 deficit Effects 0.000 claims 1
• 239000003085 diluting agent Substances 0.000 claims 1
• 239000003814 drug Substances 0.000 claims 1
• 230000005713 exacerbation Effects 0.000 claims 1
• 229960001469 fluticasone furoate Drugs 0.000 claims 1
• XTULMSXFIHGYFS-VLSRWLAYSA-N fluticasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(F)[C@@]4(C)C=CC(=O)C=C4[C@@H](F)C[C@H]3[C@@H]2C[C@H]1C)C(=O)SCF)C(=O)C1=CC=CO1 XTULMSXFIHGYFS-VLSRWLAYSA-N 0.000 claims 1
• 229960000289 fluticasone propionate Drugs 0.000 claims 1
• WMWTYOKRWGGJOA-CENSZEJFSA-N fluticasone propionate Chemical compound C1([C@@H](F)C2)=CC(=O)C=C[C@]1(C)[C@]1(F)[C@@H]2[C@@H]2C[C@@H](C)[C@@](C(=O)SCF)(OC(=O)CC)[C@@]2(C)C[C@@H]1O WMWTYOKRWGGJOA-CENSZEJFSA-N 0.000 claims 1
• 229960002848 formoterol Drugs 0.000 claims 1
• BPZSYCZIITTYBL-UHFFFAOYSA-N formoterol Chemical compound C1=CC(OC)=CC=C1CC(C)NCC(O)C1=CC=C(O)C(NC=O)=C1 BPZSYCZIITTYBL-UHFFFAOYSA-N 0.000 claims 1
• 125000005843 halogen group Chemical group 0.000 claims 1
• 125000004404 heteroalkyl group Chemical group 0.000 claims 1
• 239000001257 hydrogen Substances 0.000 claims 1
• 208000015181 infectious disease Diseases 0.000 claims 1
• 238000004519 manufacturing process Methods 0.000 claims 1
• 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
• WOFMFGQZHJDGCX-ZULDAHANSA-N mometasone furoate Chemical compound O([C@]1([C@@]2(C)C[C@H](O)[C@]3(Cl)[C@@]4(C)C=CC(=O)C=C4CC[C@H]3[C@@H]2C[C@H]1C)C(=O)CCl)C(=O)C1=CC=CO1 WOFMFGQZHJDGCX-ZULDAHANSA-N 0.000 claims 1
• 239000000178 monomer Substances 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
• 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
• 125000004043 oxo group Chemical group O=* 0.000 claims 1
• 239000001301 oxygen Substances 0.000 claims 1
• 239000008194 pharmaceutical composition 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
• 230000000241 respiratory effect Effects 0.000 claims 1
• 229960000329 ribavirin Drugs 0.000 claims 1
• 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 1
• 229960002586 roflumilast Drugs 0.000 claims 1
• MNDBXUUTURYVHR-UHFFFAOYSA-N roflumilast Chemical group FC(F)OC1=CC=C(C(=O)NC=2C(=CN=CC=2Cl)Cl)C=C1OCC1CC1 MNDBXUUTURYVHR-UHFFFAOYSA-N 0.000 claims 1
• 229960002052 salbutamol Drugs 0.000 claims 1
• 229960004017 salmeterol Drugs 0.000 claims 1
• 125000001424 substituent group Chemical group 0.000 claims 1
• 125000004434 sulfur atom Chemical group 0.000 claims 1
• 238000003419 tautomerization reaction Methods 0.000 claims 1
• 229960000195 terbutaline Drugs 0.000 claims 1
• 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
• 229960000278 theophylline Drugs 0.000 claims 1