HRP20140641T1 - Kondenzirani imidazoli i sastavi koji ih sadrže za lijeäśenje parazitnih bolesti kao što je primjerice malarija - Google Patents
Kondenzirani imidazoli i sastavi koji ih sadrže za lijeäśenje parazitnih bolesti kao što je primjerice malarija Download PDFInfo
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- HRP20140641T1 HRP20140641T1 HRP20140641AT HRP20140641T HRP20140641T1 HR P20140641 T1 HRP20140641 T1 HR P20140641T1 HR P20140641A T HRP20140641A T HR P20140641AT HR P20140641 T HRP20140641 T HR P20140641T HR P20140641 T1 HRP20140641 T1 HR P20140641T1
- Authority
- HR
- Croatia
- Prior art keywords
- amino
- fluorophenyl
- imidazo
- pyrazin
- methylpropan
- Prior art date
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- 201000004792 malaria Diseases 0.000 title claims 2
- 239000000203 mixture Substances 0.000 title claims 2
- 208000030852 Parasitic disease Diseases 0.000 title 1
- 150000002460 imidazoles Chemical class 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims 18
- 241000224016 Plasmodium Species 0.000 claims 7
- 201000010099 disease Diseases 0.000 claims 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 7
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 239000003795 chemical substances by application Substances 0.000 claims 3
- WGKXETUOZHHSRI-UHFFFAOYSA-N 2-amino-1-[3-(3,4-difluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C(F)=C1 WGKXETUOZHHSRI-UHFFFAOYSA-N 0.000 claims 2
- CLKQZPRZINRQOP-UHFFFAOYSA-N 2-amino-1-[3-(3,4-difluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)C(C)(N)C)CCN2C=1NC1=CC=C(F)C(F)=C1 CLKQZPRZINRQOP-UHFFFAOYSA-N 0.000 claims 2
- KFSKTWYDIHJITF-UHFFFAOYSA-N 2-amino-1-[3-(4-chloroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)CN)CCN2C=1NC1=CC=C(Cl)C=C1 KFSKTWYDIHJITF-UHFFFAOYSA-N 0.000 claims 2
- BUPRVECGWBHCQV-UHFFFAOYSA-N 2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)CN)CCN2C=1NC1=CC=C(F)C=C1 BUPRVECGWBHCQV-UHFFFAOYSA-N 0.000 claims 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 claims 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 2
- LOUPRKONTZGTKE-WZBLMQSHSA-N Quinine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@@H]2[C@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-WZBLMQSHSA-N 0.000 claims 2
- 239000003430 antimalarial agent Substances 0.000 claims 2
- LOUPRKONTZGTKE-UHFFFAOYSA-N cinchonine Natural products C1C(C(C2)C=C)CCN2C1C(O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-UHFFFAOYSA-N 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 239000001257 hydrogen Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- LOUPRKONTZGTKE-LHHVKLHASA-N quinidine Chemical compound C([C@H]([C@H](C1)C=C)C2)C[N@@]1[C@H]2[C@@H](O)C1=CC=NC2=CC=C(OC)C=C21 LOUPRKONTZGTKE-LHHVKLHASA-N 0.000 claims 2
- XEEQGYMUWCZPDN-DOMZBBRYSA-N (-)-(11S,2'R)-erythro-mefloquine Chemical compound C([C@@H]1[C@@H](O)C=2C3=CC=CC(=C3N=C(C=2)C(F)(F)F)C(F)(F)F)CCCN1 XEEQGYMUWCZPDN-DOMZBBRYSA-N 0.000 claims 1
- TVERBZNSBJEOHL-GFCCVEGCSA-N (2r)-2-amino-1-[3-(4-chloro-3-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]propan-1-one Chemical compound C1N(C(=O)[C@H](N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(Cl)C(F)=C1 TVERBZNSBJEOHL-GFCCVEGCSA-N 0.000 claims 1
- PLPBUDLQQFEQLJ-ZDUSSCGKSA-N (2s)-2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]propan-1-one Chemical compound C1N(C(=O)[C@@H](N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C=C1 PLPBUDLQQFEQLJ-ZDUSSCGKSA-N 0.000 claims 1
- WHTVZRBIWZFKQO-AWEZNQCLSA-N (S)-chloroquine Chemical compound ClC1=CC=C2C(N[C@@H](C)CCCN(CC)CC)=CC=NC2=C1 WHTVZRBIWZFKQO-AWEZNQCLSA-N 0.000 claims 1
- CBQREQZBYMQOQS-GFCCVEGCSA-N 2-amino-1-[(8r)-3-(4-chloro-3-fluoroanilino)-2-(4-fluorophenyl)-8-methyl-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound NCC(=O)N([C@@H](C1=NC=2C=3C=CC(F)=CC=3)C)CCN1C=2NC1=CC=C(Cl)C(F)=C1 CBQREQZBYMQOQS-GFCCVEGCSA-N 0.000 claims 1
- CBQREQZBYMQOQS-LBPRGKRZSA-N 2-amino-1-[(8s)-3-(4-chloro-3-fluoroanilino)-2-(4-fluorophenyl)-8-methyl-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound NCC(=O)N([C@H](C1=NC=2C=3C=CC(F)=CC=3)C)CCN1C=2NC1=CC=C(Cl)C(F)=C1 CBQREQZBYMQOQS-LBPRGKRZSA-N 0.000 claims 1
- BYLGMXUNERRZLL-UHFFFAOYSA-N 2-amino-1-[3-(2,4-difluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C=C1F BYLGMXUNERRZLL-UHFFFAOYSA-N 0.000 claims 1
- OINKJECGQPNTCV-UHFFFAOYSA-N 2-amino-1-[3-(2,4-difluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C1N(C(=O)CN)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C=C1F OINKJECGQPNTCV-UHFFFAOYSA-N 0.000 claims 1
- FZPNGLXOHOHAOL-UHFFFAOYSA-N 2-amino-1-[3-(3,4-dichloroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(Cl)C(Cl)=C1 FZPNGLXOHOHAOL-UHFFFAOYSA-N 0.000 claims 1
- XFVQXPQCEKHCOO-UHFFFAOYSA-N 2-amino-1-[3-(3,4-dichloroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)C(C)(N)C)CCN2C=1NC1=CC=C(Cl)C(Cl)=C1 XFVQXPQCEKHCOO-UHFFFAOYSA-N 0.000 claims 1
- HTGFLXKWKVKCNV-UHFFFAOYSA-N 2-amino-1-[3-(3,4-difluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C1N(C(=O)CN)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C(F)=C1 HTGFLXKWKVKCNV-UHFFFAOYSA-N 0.000 claims 1
- HXGAEYRFHZWDBV-UHFFFAOYSA-N 2-amino-1-[3-(3,5-dichloroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC(Cl)=CC(Cl)=C1 HXGAEYRFHZWDBV-UHFFFAOYSA-N 0.000 claims 1
- ZWBBISWLYYRQMK-UHFFFAOYSA-N 2-amino-1-[3-(3,5-difluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC(F)=CC(F)=C1 ZWBBISWLYYRQMK-UHFFFAOYSA-N 0.000 claims 1
- DOPAIQZTNAFKJZ-UHFFFAOYSA-N 2-amino-1-[3-(3,5-difluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C1N(C(=O)CN)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC(F)=CC(F)=C1 DOPAIQZTNAFKJZ-UHFFFAOYSA-N 0.000 claims 1
- OEWQJOOCEFSQNX-UHFFFAOYSA-N 2-amino-1-[3-(3-chloro-4-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C(Cl)=C1 OEWQJOOCEFSQNX-UHFFFAOYSA-N 0.000 claims 1
- RFFOACDYUIXWJH-UHFFFAOYSA-N 2-amino-1-[3-(3-chloro-4-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C1N(C(=O)CN)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C(Cl)=C1 RFFOACDYUIXWJH-UHFFFAOYSA-N 0.000 claims 1
- FQQJZBAWMHAKTM-UHFFFAOYSA-N 2-amino-1-[3-(3-chloro-4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)C(C)(N)C)CCN2C=1NC1=CC=C(F)C(Cl)=C1 FQQJZBAWMHAKTM-UHFFFAOYSA-N 0.000 claims 1
- AFCWGRQVJGNQCT-UHFFFAOYSA-N 2-amino-1-[3-(3-chloroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)CN)CCN2C=1NC1=CC=CC(Cl)=C1 AFCWGRQVJGNQCT-UHFFFAOYSA-N 0.000 claims 1
- PULYEEPXSDNHJP-UHFFFAOYSA-N 2-amino-1-[3-(3-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=CC(F)=C1 PULYEEPXSDNHJP-UHFFFAOYSA-N 0.000 claims 1
- XXIFVIBMAGHSIC-UHFFFAOYSA-N 2-amino-1-[3-(4-chloro-3-fluoroanilino)-2-(3-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=C(F)C=CC=1)=C2NC1=CC=C(Cl)C(F)=C1 XXIFVIBMAGHSIC-UHFFFAOYSA-N 0.000 claims 1
- AZLJHDZRFZEAKN-UHFFFAOYSA-N 2-amino-1-[3-(4-chloro-3-fluoroanilino)-2-(3-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C1N(C(=O)CN)CCN2C1=NC(C=1C=C(F)C=CC=1)=C2NC1=CC=C(Cl)C(F)=C1 AZLJHDZRFZEAKN-UHFFFAOYSA-N 0.000 claims 1
- MZDVIWLUBFQDCL-UHFFFAOYSA-N 2-amino-1-[3-(4-chloro-3-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(Cl)C(F)=C1 MZDVIWLUBFQDCL-UHFFFAOYSA-N 0.000 claims 1
- NFEGRCPLFOJJLU-UHFFFAOYSA-N 2-amino-1-[3-(4-chloro-3-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C1N(C(=O)CN)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(Cl)C(F)=C1 NFEGRCPLFOJJLU-UHFFFAOYSA-N 0.000 claims 1
- ODIPVGBXMIJZCX-UHFFFAOYSA-N 2-amino-1-[3-(4-chloro-3-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]ethanone Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)CN)CCN2C=1NC1=CC=C(Cl)C(F)=C1 ODIPVGBXMIJZCX-UHFFFAOYSA-N 0.000 claims 1
- MTXUAKHFUYWWHV-UHFFFAOYSA-N 2-amino-1-[3-(4-chloroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(Cl)C=C1 MTXUAKHFUYWWHV-UHFFFAOYSA-N 0.000 claims 1
- WSOUZNRRIWRLDV-UHFFFAOYSA-N 2-amino-1-[3-(4-chloroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)C(C)(N)C)CCN2C=1NC1=CC=C(Cl)C=C1 WSOUZNRRIWRLDV-UHFFFAOYSA-N 0.000 claims 1
- LIEJEBYFAZUZHM-UHFFFAOYSA-N 2-amino-1-[3-(4-fluoroanilino)-2-(2-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C(=CC=CC=1)F)=C2NC1=CC=C(F)C=C1 LIEJEBYFAZUZHM-UHFFFAOYSA-N 0.000 claims 1
- XKAZULVCCJWYHL-UHFFFAOYSA-N 2-amino-1-[3-(4-fluoroanilino)-2-(3-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=C(F)C=CC=1)=C2NC1=CC=C(F)C=C1 XKAZULVCCJWYHL-UHFFFAOYSA-N 0.000 claims 1
- NIFJWDNQUGBNEW-UHFFFAOYSA-N 2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5h-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C1N(C(=O)C(C)(N)C)CCN2C1=NC(C=1C=CC(F)=CC=1)=C2NC1=CC=C(F)C=C1 NIFJWDNQUGBNEW-UHFFFAOYSA-N 0.000 claims 1
- IDXDHJWTWYCAHI-UHFFFAOYSA-N 2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one Chemical compound C=1C=C(F)C=CC=1C=1N=C2C(C)(C)N(C(=O)C(C)(N)C)CCN2C=1NC1=CC=C(F)C=C1 IDXDHJWTWYCAHI-UHFFFAOYSA-N 0.000 claims 1
- -1 3-chloro-4-fluorophenyl Chemical group 0.000 claims 1
- 125000004180 3-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C(F)=C1[H] 0.000 claims 1
- LUBUTTBEBGYNJN-UHFFFAOYSA-N 4-amino-n-(5,6-dimethoxypyrimidin-4-yl)benzenesulfonamide;5-(4-chlorophenyl)-6-ethylpyrimidine-2,4-diamine Chemical compound CCC1=NC(N)=NC(N)=C1C1=CC=C(Cl)C=C1.COC1=NC=NC(NS(=O)(=O)C=2C=CC(N)=CC=2)=C1OC LUBUTTBEBGYNJN-UHFFFAOYSA-N 0.000 claims 1
- OVCDSSHSILBFBN-UHFFFAOYSA-N Amodiaquine Chemical compound C1=C(O)C(CN(CC)CC)=CC(NC=2C3=CC=C(Cl)C=C3N=CC=2)=C1 OVCDSSHSILBFBN-UHFFFAOYSA-N 0.000 claims 1
- 235000001258 Cinchona calisaya Nutrition 0.000 claims 1
- FOHHNHSLJDZUGQ-VWLOTQADSA-N Halofantrine Chemical compound FC(F)(F)C1=CC=C2C([C@@H](O)CCN(CCCC)CCCC)=CC3=C(Cl)C=C(Cl)C=C3C2=C1 FOHHNHSLJDZUGQ-VWLOTQADSA-N 0.000 claims 1
- 229960001444 amodiaquine Drugs 0.000 claims 1
- 229940121363 anti-inflammatory agent Drugs 0.000 claims 1
- 239000002260 anti-inflammatory agent Substances 0.000 claims 1
- 229960000981 artemether Drugs 0.000 claims 1
- 229960004191 artemisinin Drugs 0.000 claims 1
- BLUAFEHZUWYNDE-NNWCWBAJSA-N artemisinin Chemical compound C([C@](OO1)(C)O2)C[C@H]3[C@H](C)CC[C@@H]4[C@@]31[C@@H]2OC(=O)[C@@H]4C BLUAFEHZUWYNDE-NNWCWBAJSA-N 0.000 claims 1
- 229930101531 artemisinin Natural products 0.000 claims 1
- 229960004991 artesunate Drugs 0.000 claims 1
- FIHJKUPKCHIPAT-AHIGJZGOSA-N artesunate Chemical compound C([C@](OO1)(C)O2)C[C@H]3[C@H](C)CC[C@@H]4[C@@]31[C@@H]2O[C@@H](OC(=O)CCC(O)=O)[C@@H]4C FIHJKUPKCHIPAT-AHIGJZGOSA-N 0.000 claims 1
- KUCQYCKVKVOKAY-CTYIDZIISA-N atovaquone Chemical compound C1([C@H]2CC[C@@H](CC2)C2=C(C(C3=CC=CC=C3C2=O)=O)O)=CC=C(Cl)C=C1 KUCQYCKVKVOKAY-CTYIDZIISA-N 0.000 claims 1
- 229960003159 atovaquone Drugs 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 229960003677 chloroquine Drugs 0.000 claims 1
- WHTVZRBIWZFKQO-UHFFFAOYSA-N chloroquine Natural products ClC1=CC=C2C(NC(C)CCCN(CC)CC)=CC=NC2=C1 WHTVZRBIWZFKQO-UHFFFAOYSA-N 0.000 claims 1
- ISZNZKHCRKXXAU-UHFFFAOYSA-N chlorproguanil Chemical compound CC(C)\N=C(/N)N=C(N)NC1=CC=C(Cl)C(Cl)=C1 ISZNZKHCRKXXAU-UHFFFAOYSA-N 0.000 claims 1
- 229950000764 chlorproguanil Drugs 0.000 claims 1
- 229960000860 dapsone Drugs 0.000 claims 1
- SXYIRMFQILZOAM-HVNFFKDJSA-N dihydroartemisinin methyl ether Chemical compound C1C[C@H]2[C@H](C)CC[C@H]3[C@@H](C)[C@@H](OC)O[C@H]4[C@]32OO[C@@]1(C)O4 SXYIRMFQILZOAM-HVNFFKDJSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 229960003242 halofantrine Drugs 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- DYLGFOYVTXJFJP-MYYYXRDXSA-N lumefantrine Chemical compound C12=CC(Cl)=CC=C2C=2C(C(O)CN(CCCC)CCCC)=CC(Cl)=CC=2\C1=C/C1=CC=C(Cl)C=C1 DYLGFOYVTXJFJP-MYYYXRDXSA-N 0.000 claims 1
- 229960004985 lumefantrine Drugs 0.000 claims 1
- 229960001962 mefloquine Drugs 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 229960005179 primaquine Drugs 0.000 claims 1
- INDBQLZJXZLFIT-UHFFFAOYSA-N primaquine Chemical compound N1=CC=CC2=CC(OC)=CC(NC(C)CCCN)=C21 INDBQLZJXZLFIT-UHFFFAOYSA-N 0.000 claims 1
- SSOLNOMRVKKSON-UHFFFAOYSA-N proguanil Chemical compound CC(C)\N=C(/N)N=C(N)NC1=CC=C(Cl)C=C1 SSOLNOMRVKKSON-UHFFFAOYSA-N 0.000 claims 1
- 229960005385 proguanil Drugs 0.000 claims 1
- DJUFPMUQJKWIJB-UHFFFAOYSA-N pyronaridine Chemical compound C12=NC(OC)=CC=C2N=C2C=C(Cl)C=CC2=C1NC(C=C(CN1CCCC1)C=1O)=CC=1CN1CCCC1 DJUFPMUQJKWIJB-UHFFFAOYSA-N 0.000 claims 1
- 229950011262 pyronaridine Drugs 0.000 claims 1
- 229960001404 quinidine Drugs 0.000 claims 1
- 229960000948 quinine Drugs 0.000 claims 1
- 229940124530 sulfonamide Drugs 0.000 claims 1
- 150000003456 sulfonamides Chemical class 0.000 claims 1
- IEDVJHCEMCRBQM-UHFFFAOYSA-N trimethoprim Chemical compound COC1=C(OC)C(OC)=CC(CC=2C(=NC(N)=NC=2)N)=C1 IEDVJHCEMCRBQM-UHFFFAOYSA-N 0.000 claims 1
- 229960001082 trimethoprim Drugs 0.000 claims 1
Classifications
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines containing further heterocyclic rings
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- A—HUMAN NECESSITIES
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- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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Claims (12)
1. Spoj, naznačen time, da ima formulu Id:
[image]
u kojoj:
R1 je -NH2;
R2 i R3 su neovisno odabrani između vodika i metila;
R4 i R5 su neovisno odabrani između vodika i metila;
R6 je fenil supstituiran s fluoro; i
R8 je fenil supstituiran s 1 do 2 radikala neovisno odabrana između kloro i fluoro;
ili njegova farmaceutski prihvatljiva sol.
2. Spoj prema zahtjevu 1, naznačen time, da spoj je 2-amino-1-(2-(4-fluorofenil)-3-(4-fluorofenilamino)-8,8-dimetil-5,6-dihidroimidazo[1,2-a]pirazin-7(8H)-il)etanon, koji ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
3. Spoj prema zahtjevu 1, naznačen time, da spoj je 2-amino-1-(3-(3,4-difluorofenilamino)-2-(4-fluorofenil)-5,6-dihidroimidazo[1,2-a]pirazin-7(8H)-il)-2-metilpropan-1-on, koji ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
4. Spoj prema zahtjevu 1, naznačen time, da spoj je 2-amino-1-(3-(4-klorofenilamino)-2-(4-fluorofenil)-8,8-dimetil-5,6-dihidroimidazo [1,2-a]pirazin-7(8H)-il)etanon, koji ima formulu:
[image]
ili njegova farmaceutski prihvatljiva sol.
5. Spoj prema zahtjevu 1, naznačen time, da je odabran od sljedećih:
2-amino-1-[2-(4-fluorofenil)-3-[(4-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]-2-metil-propan-1-on;
2-amino-1-[2-(4-fluorofenil)-3-[(4-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]etan-1-on;
2-amino-1-[2-(2-fluorofenil)-3-[(4-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]-2-metil-propan-1-on;
(2S)-2-amino-1-[2-(4-fluorofenil)-3-[(4-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]propan-1-on;
2-amino-1-{3-[(3,4-difluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3,4-difluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-[2-(4-fluorofenil)-3-[(3-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]-2-metil-propan-1-on;
2-amino-1-[2-(4-fluorofenil)-3-[(3-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]etan-1-on;
2-amino-1-{3-[(4-klorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metil-propan-1-on;
2-amino-1-{3-[(4-klorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-{3-[(3,5-difluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3,5-difluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-[2-(3-fluorofenil)-3-[(4-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]-2-metil-propan-1-on;
2-amino-1-{3-[(4-kloro-3-fluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-{3-[(3-kloro-4-fluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-{3-[(2,4-difluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(2,4-difluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-{3-[(4-kloro-3-fluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(4-kloro-3-fluorofenil)amino]-2-(3-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-{3-[(4-kloro-3-fluorofenil)amino]-2-(3-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3,4-diklorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-[2-(4-fluorofenil)-3-[(4-fluorofenil)amino]-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]etan-1-on;
2-amino-1-{3-[(4-klorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-{3-[(4-kloro-3-fluorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
2-amino-1-[2-(4-fluorofenil)-3-[(4-fluorofenil)amino]-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]-2-metilpropan-1-on;
2-amino-1-{3-[(4-klorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3,4-difluorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3-kloro-4-fluorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3,4-diklorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-[(8R)-3-[(4-kloro-3-fluorofenil)amino]-2-(4-fluorofenil)-8-metil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]etan-1-on;
2-amino-1-[(8S)-3-[(4-kloro-3-fluorofenil)amino]-2-(4-fluorofenil)-8-metil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]etan-1-on;
2-amino-1-[2-(3-fluorofenil)-3-[(4-fluorofenil)amino]-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il]etan-1-on;
(2R)-2-amino-1-{3-[(4-kloro-3-fluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}propan-1-on;
2-amino-1-(3-((3,4-difluorofenil)amino)-2-(4-fluorophenil)-8,8-dimetil-5,6-dihidroimidazo[1,2-a]pirazin-7(8H)-il)-2-metilpropan-1-on;
2-amino-1-(3-((3-kloro-4-fluorofenil)amino)-2-(4-fluorofenil)-8,8-dimetil-5,6-dihidroimidazo[1,2-a]pirazin-7(8H)-il)-2-metilpropan-1-on;
2-amino-1-{3-[(3-kloro-4-fluorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on;
2-amino-1-{3-[(3,5-diklorofenil)amino]-2-(4-fluorofenil)-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}-2-metilpropan-1-on; i
2-amino-1-{3-[(3-klorofenil)amino]-2-(4-fluorofenil)-8,8-dimetil-5H,6H,7H,8H-imidazo[1,2-a]pirazin-7-il}etan-1-on;
ili njegova farmaceutski prihvatljiva sol.
6. Sastav, naznačen time, da obuhvaća spoj prema bilo kojem zahtjevu od 1 do 5 te farmaceutski prihvatljiv nosač.
7. Spoj prema bilo kojem zahtjevu od 1 do 5, naznačen time, da se upotrebljava u liječenju bolesti koja se odnosi na plazmodij, pri čemu je taj spoj po želji u kombinaciji s drugim sredstvom.
8. Uporaba spoja prema bilo kojem zahtjevu od 1 do 5, naznačen time, da je za proizvodnju lijeka za liječenje bolesti koja je povezana s plazmodijem, pri čemu je taj spoj po želji u kombinaciji s drugim sredstvom.
9. Spoj za uporabu u liječenju bolesti koja se odnosi na plazmodij prema zahtjevu 7, ili uporaba prema zahtjevu 8, naznačen(a) time, da bolest koja je povezana s plazmodijem je malarija.
10. Spoj za uporabu u liječenju bolesti koja se odnosi na plazmodij prema zahtjevu 7, ili uporaba prema zahtjevu 8, naznačen(a) time, da je drugo sredstvo odabrano između inhibitora kinaze, lijeka protiv malarije i protuupalnog sredstva.
11. Spoj za uporabu u liječenju bolesti koja se odnosi na plazmodij prema zahtjevu 7, ili uporaba prema zahtjevu 10, naznačen(a) time, da je lijek protiv malarije odabran između sljedećih: proguanil, klorproguanil, trimetoprim, klorokin, meflokin, lumefantrin, atovakon, pirimetamin-sulfadoksin, pirimetamin-dapson, halofantrin, kinin, kinidin, amodiakin, amopirokin, sulfonamidi, artemisinin, arteflen, artemeter, artesunat, primakuine i pironaridin.
12. Spoj za uporabu u liječenju bolesti koja se odnosi na plazmodij prema zahtjevu 7, ili uporaba prema zahtjevu 11, naznačen(a) time, da se prilikom liječenja, spoj daje prije, istovremeno ili nakon drugog sredstva.
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US22443309P | 2009-07-09 | 2009-07-09 | |
PCT/US2010/041626 WO2011006143A2 (en) | 2009-07-09 | 2010-07-09 | Compounds and compositions for the treatment of parasitic diseases |
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PE (1) | PE20130399A1 (hr) |
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EP2920169A1 (en) * | 2012-11-14 | 2015-09-23 | F. Hoffmann-La Roche AG | Imidazopyridine derivatives |
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CN105189506A (zh) * | 2012-11-19 | 2015-12-23 | 诺华股份有限公司 | 用于治疗寄生虫疾病的化合物和组合物 |
PL2925757T3 (pl) * | 2012-11-19 | 2018-06-29 | Novartis Ag | Związki i kompozycje do leczenia chorób pasożytniczych |
CN103126782B (zh) * | 2013-02-26 | 2016-06-29 | 内蒙古农牧业科学院 | 一种寄生病的治疗方法 |
WO2015095477A1 (en) * | 2013-12-19 | 2015-06-25 | Irm Llc | [1,2,4]triazolo[1,5-a]pyrimidine derivatives as protozoan proteasome inhibitors for the treatment of parasitic diseases such as leishmaniasis |
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US10660334B2 (en) * | 2016-08-15 | 2020-05-26 | Bayer Cropscience Aktiengesellschaft | Fused bicyclic heterocycle derivatives as pesticides |
AU2018260414A1 (en) * | 2017-04-24 | 2019-10-17 | Novartis Ag | Therapeutic regimen of 2-amino-l-(2-(4-fluorophenyl)-3-(4-fluorophenylamino)-8,8-dimethyl-5,6-dihydroimidazo[1,2-a]pyrazin-7(8H)-yl)ethanone and combinations thereof |
KR102664604B1 (ko) | 2017-07-14 | 2024-05-14 | 에프. 호프만-라 로슈 아게 | 이환형 케톤 화합물 및 이의 사용 방법 |
WO2022049548A1 (en) | 2020-09-04 | 2022-03-10 | Novartis Ag | Kaf156 combinations and methods for the treatment of malaria |
WO2023168107A2 (en) * | 2022-03-04 | 2023-09-07 | University Of Central Florida Research Foundation, Inc. | Compounds and compositions for anitmalarial therapeutic and prophylactic use |
CN114569711B (zh) * | 2022-03-24 | 2024-04-19 | 安徽医科大学 | 一种预防弓形虫病的ME49Δcdpk3减毒活疫苗及其制备方法和应用 |
WO2024006974A2 (en) * | 2022-07-01 | 2024-01-04 | The Scripps Research Institute | Antimalarial compounds |
WO2024006971A2 (en) * | 2022-07-01 | 2024-01-04 | The Scripps Research Institute | Antimalarial compounds |
WO2024006970A2 (en) * | 2022-07-01 | 2024-01-04 | The Scripps Research Institute | Antimalarial compounds |
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