HRP20150024T1 - Derivati pirazolokinolinona, njihovo dobivanje i upotreba u terapiji - Google Patents

Derivati pirazolokinolinona, njihovo dobivanje i upotreba u terapiji Download PDF

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HRP20150024T1
HRP20150024T1 HRP20150024AT HRP20150024T HRP20150024T1 HR P20150024 T1 HRP20150024 T1 HR P20150024T1 HR P20150024A T HRP20150024A T HR P20150024AT HR P20150024 T HRP20150024 T HR P20150024T HR P20150024 T1 HRP20150024 T1 HR P20150024T1
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compound
dihydro
pyrazolo
quinolin
trifluoroethyl
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Alexandre Benazet
Olivier Duclos
Nathalie Guillo
Gilbert Lassalle
Karim Macary
Valérie Viv
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Sanofi
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    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
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Claims (14)

1. Spoj koji odgovara formuli (I): [image] , naznačen time što: R1 predstavlja: • -(C1-C4)alkil • -(C1-C4)halogenalkil R2 predstavlja: • skupinu: [image] • skupinu: [image] • skupinu: -A-X R3 predstavlja: • -H • halogen • -(C1-C6)alkil • cijano skupinu • -CO2H • -CONH2 A predstavlja: • arilnu ili heteroarilnu skupinu X je odsutan ili predstavlja: • halogen • cijano skupinu • oxo skupinu • -(CH2)nOH • -(C1-C6)halogenalkil • -(C1-C6)alkil • -(C1-C6)alkoxy • -(CH2)n-aril • -CHOH-aril • heterocikl • heteroaril • -(C1-C6)alkil-heterocikl • -(C1-C6)alkil-heteroaril • -(C1-C6)alkil-COORa • -(C1-C6)alkil-NRaRb • -heteroaril-(CH2)n-NRaRb • -(CH2)n-NRa-C(O)-Rb • -NRaRb • -NRa-(CH2)n-O-Rb • -NRa-heterocikl • -NRa-aril • -NRa-C(O)-(CH2)n-NRaRb • -NRa-C(O)-aril • -NRaC(O)-(Cl-C6)alkil • -NRa-C(O)-(C1-C6)alkil-aril • -NRa-C(O)-(CH2)n-O-Rb • -NRa-SO2-(CH2)n-aril • -NRa-SO2-(CH2)n-NRaRb • -NRa-SO2-Rb • -NRa-SO2-aril-O-aril • -NRa-SO2-aril-(CH2)n-NRb-C(O)-Rb • -COORa • -CONRaRb • -C(O)-NRa-(CH2)n-O-Rb • -C(O)-NRa-aril-C(O)-NRaRb • -C(O)-NRa-(CH2)n-NRaRb • -C(O)-NRa-(CH2)n-heteroaril • -O-(CH2)n-NRaRb • -O-heterocikl • -CO-heterocikl • -CO-heteroaril • -SO2NRaRb • -SO2-heterocikl Ra i Rb, neovisno, predstavljaju: • -H • -(C1-C6)alkil n predstavlja 0, 1, 2 ili 3 u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
2. Spoj formule (I) u skladu s patentni zahtjev 1, naznačen time što R3 predstavlja H ili halogen, specifičnije klor; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
3. Spoj formule (I) u skladu s either of patentni zahtjevi 1 i 2, naznačen time što R1 predstavlja etil ili trifluoretil; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
4. Spoj formule (I) u skladu s bilo kojim od patentnih zahtjeva 1 do 3, naznačen time što R2 predstavlja skupinu -A-X, gdje A predstavlja arilnu ili heteroarilnu skupinu, a X je odsutan ili predstavlja heterocikl, NRaRb, (C1-C6)alkil, halogen, specifičnije klor ili fluor, cijano skupinu, NRa-SO2-Rb, CO-heterocikl; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
5. Spoj formule (I) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što ga se bira između sljedećih spojeva: – spoj 1: 7-(pirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 2: 7-(2-aminopirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 3: 7-(2-fluorfenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 4: 5-etil-7-pirid-2-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 5: 5-etil-7-(4-fluorfenil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 6: 7-(pirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 7: 5-etil-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 8: 7-(2-dimetilaminofenil)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 9: N-(3-dimetilaminopropil)-4-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzamid; – spoj 10: 5-etil-7-(4-piperazin-1-ilfenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 11: 5-etil-7-[4-(4-metilpiperazin-1-il)fenil]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 12: 7-[2-(morfolin-4-ilkarbonil)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 13: N-(2-dimetilaminoetil)-4-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzamid; – spoj 14: 7-(2-morfolin-4-ilfenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 15: 7-[4-(1-dimetilaminoetil)fenil]-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 16: 7-(2-morfolin-4-ilmetilfenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 17: 5-etil-7-(2-morfolin-4-ilmetilfenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 18: 5-etil-7-[4-(piperazin-1-karbonil)fenil]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 19: 7-[4-(4-metilpiperazin-1-il)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 20: 5-etil-7-(2-piperazin-1-ilpirimidin-5-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 21: 5-etil-7-[4-(4-metilpiperazin-1-karbonil)fenil]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 22: 5-etil-7-[4-(1-pirolidin-1-il-etil)fenil]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 23: 7-(4-dietilaminofenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 24: 7-(4-amino-2-metilfenil)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 25: 7-(4-morfolin-4-ilfenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 26: 5-etil-7-(4-morfolin-4-ilfenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 27: 5-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)-2-fluor-N-metilbenzamid; – spoj 28: 5-etil-7-(2-fluor-5-metoksifenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 29: 7-[3-klor-4-(morfolin-4-karbonil)fenil]-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 30: 7-[4-(piperazin-1-il)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 31: 5-etil-7-[2-(4-metilpiperazin-1-il)pirimidin-5-il]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 32: 7-(4-dimetilaminofenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 33: 2-klor-4-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzamid; – spoj 34: 5-etil-7-(1H-indazol-5-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 35: N-etil-3-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzamid; – spoj 36: 5-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)-2-fluorbenzamid; – spoj 37: N-(2-dimetilaminoetil)-3-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzamid; – spoj 38: N-[4-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzil]acetamid; – spoj 39: 3-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)-N-(2-metoksietil)benzamid; – spoj 40: 7-(3-hidroksifenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 41: 7-(2-klor-3-fluorpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 42: 7-(2-{5-[(propan-2-ilamino)metil]furan-2-il}fenil)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 43: N-[2-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)fenil]metansulfonamid; – spoj 44: 7-(2-aminofenil)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 45: 5-etil-7-(3-morfolin-4-ilfenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 46: N-[2-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)fenil]acetamid; – spoj 47: 5-etil-7-(2-hidroksifenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 48: 5-etil-7-[4-(morfolin-4-sulfonil)fenil]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 49: 7-(2-hidroksimetil-4-metoksifenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 50: 5-etil-7-(3-pirazol-1-ilfenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 51: 5-etil-7-(1H-indol-5-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 52: 5-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)-thiofene-2-karbonitril; – spoj 53: 7-(3-klor-2-hidroksifenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 54: 5-etil-7-(2-hidroksi-3-metoksifenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 55: metil-3-amino-4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzoat; – spoj 56: 5-etil-7-(4-metil-3,4-dihidro-2H-benzo[1,4]oksazin-7-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 57: 7-(2,5-diklorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 58: 7-(2-klor-5-metoksifenil)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 59: N-(3-dimetilaminopropil)-3-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzamid; – spoj 60: 5-etil-7-(4-fluor-2-hidroksifenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 61: 5-etil-7-(2-fluor-4-metoksifenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 62: 7-(4-aminometilfenil)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 63: 5-etil-7-(2-fluor-3-metoksifenil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 64: 7-(2-dimetilaminometilfenil)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 65: 4-(5-etil-4-okso-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il)benzojeva kiselina; – spoj 66: 7-[6-(piperazin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 67: 5-etil-7-[6-(piperazin-1-il)pirid-3-il]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 68: 7-[2-(4-metilpiperazin-1-il)pirid-4-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 69: 5-etil-7-[2-(4-metilpiperazin-1-il)pirid-4-il]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 70: 7-[2-(piperazin-1-il)pirid-4-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 71: 5-etil-7-(2-piperazin-1-ilpirid-4-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 72: 7-(2-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 73: 5-etil-7-(2-metilpirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 74: 7-(2-klor-6-metilpirid-3-il)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 75: 7-(2-klor-6-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 76: 7-(2-klorpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 77: 7-(2-fluorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 78: 5-etil-7-(2-fluorpirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 79: 7-(6-klor-2-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 80: 7-(2-metoksipirid-3-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 81: 5-etil-7-(2-metoksipirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 82: 7-(6-klor-4-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 83: 7-[6-(morfolin-4-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 84: 7-[6-(3-dimetilaminopropoksi)pirid-3-il]-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 85: 5-etil-7-kinolin-8-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 86: 7-(6-klorpirid-2-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 87: 5-etil-7-kinolin-6-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 88: 7-(6-klorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 89: 7-(6-klor-5-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 90: 5-etil-7-(3-fluorpirid-4-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 91: 7-(3-klorpirid-4-il)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 92: 5-etil-7-(6-fluor-5-metilpirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 93: 7-(2-etoksipirid-3-il)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 94: 5-etil-7-(5-metoksipirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 95: 7-(6-aminopirid-3-il)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 96: 5-etil-7-pirid-3-il-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 97: 7-(2-klor-6-izopropilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 98: 7-(5-klor-2-metoksipirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 99: 7-(pirid-3-iloksi)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 100: 5-etil-7-(pirid-3-iloksi)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 101: 7-(pirid-3-ilamino)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 102: 5-(2,2-difluoretil)-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 103: 5-ciklopropilmetil-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 104: 5-propil-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 105: 5-(2,2-difluorciklopropilmetil)-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 106: 5-(2-fluoretil)-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 107: 5-izopropil-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 108: 5-ciklopropil-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 109: 8-fluor-7-pirid-2-il-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 110: 7-(2-klorpirid-3-il)-8-metil-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 111: 7-(2-klorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 112: 7-[2-(dimetilamino)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 113: izopropil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzoat; – spoj 114: {2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}amid ciklopropankarboksilne kiseline; – spoj 115: 7-[2-(1-metil-1H-imidazole-2-karbonil)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 116: 7-(4-ciklopentilpirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 117: 7-(4-cikloheksilpirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 118: 7-(2-propilaminometilfenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 119: 2-metoksi-N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}acetamid; – spoj 120: N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}isobutiramid; – spoj 121: N-{4-metil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}propionamid; – spoj 122: N-izopropil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzamid; – spoj 123: 7-[4-metil-2-(piperidin-4-iloksi)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 124: 7-[2-(1,4-diazepan-1-ilmetil)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 125: etil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzoat; – spoj 126: 7-(2-aminofenil)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 127: 7-(2-piperazin-1-ilfenil)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 128: 7-(6-metoksipirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 129: 7-(5-klor-2-fluorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 130: N-{5-metil-3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-2-il}acetamid; – spoj 131: 7-[2-(2-hidroksietil)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 132: 7-(2-amino-5-fluorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 133: 7-[2-(pirolidin-1-sulfonil)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 134: N-izopropil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzensulfonamid; – spoj 135: 7-(2-fluor-5-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 136: N,N-dietil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzensulfonamid; – spoj 137: 7-(6-amino-4-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 138: 7-(6-metoksi-2-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 139: 7-(5-metil-6-[1,2,4]triazol-4-ilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 140: 7-(4-metil-6-[1,2,4]triazol-4-ilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 141: 7-[6-(morfolin-4-karbonil)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 142: 7-(6-amino-2-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 143: 7-(4-etilpirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 144: metil-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}acetat; – spoj 145: 7-(4-metoksipirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 146: 7-(4-propilpirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 147: N-{6-metil-5-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-2-il}propionamid; – spoj 148: 7-(2-oksazol-5-ilfenil)-5-(2,2,2-triftuoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 149: 7-(4-dimetilamino-2-metoksipirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 150: 7-[2-(5-etil-[1,2,4]oksadiazol-3-il)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 151: N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzil}acetamid; – spoj 152: 7-[5-(hidroksifenilmetil)pirid-2-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 153: 6-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karbonitril; – spoj 154: 7-(6-hidroksimetilpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 155: 7-[3-(2-dimetilaminoetoksi)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 156: metil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzoat; – spoj 157: 7-(5-hidroksimetilpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 158: 7-(2-metoksipirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 159: 7-(2-[1,2,4]triazol-1-ilmetilfenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 160: 7-(4-fenilpirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 161: 7-(6-metoksi-4-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 162: 7-(4-izopropilpirimidin-5-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 163: 7-(6-fluorpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 164: metil-6-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksilat; – spoj 165: 7-(5-fluorpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 166: 7-[2-(4-metilpiperazin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 167: 7-(3-aminopirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 168: 7-(2,6-dimetilpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 169: 7-(3-klorpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 170: metil-3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksilat; – spoj 171: 7-(6-metilpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 172: 7-[2-(morfolin-4-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 173: 5-(2,2,2-trifluoretil)-7-(2-trifluormetilpirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 174: 7-(2-ciklopropilaminopirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 175: 5-(2,2,2-trifluoretil)-7-(3-trifluormetilpirid-2-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 176: 3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karbonitril; – spoj 177: 2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-3-karbonitril; – spoj 178: metil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]nikotinat; – spoj 179: 7-(2-propoksipirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 180: 7-(3-hidroksipirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 181: 7-[2-(4-fluorfenilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 182: 7-(2-metilaminofenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 183: 7-(2-etoksipirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 184: 7-(2-izopropoksipirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 185: 7-(5-klor-2-metoksipirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 186: 7-(2-metilpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 187: 7-(4-metilpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 188: 7-(6-morfolin-4-ilpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 189: 7-(4-metilaminofenil)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 190: 5-(2,2,2-trifluoretil)-7-(6-trifluormetilpirid-3-il)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 191: 7-(6-metoksipirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 192: 7-[4-(2H-tetrazol-5-il)fenil]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 193: 7-(3,5-diklorpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 194: 8-klor-7-(pirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 195 8-brom-7-pirid-2-il-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 196: 8-klor-7-(pirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 197: 8-brom-7-(pirid-4-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 198: 8-klor-5-etil-7-pirid-4-il-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 199: 8-klor-7-(2-klorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 200: 8-metil-7-pirid-2-il-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 201: 4-okso-7-pirid-4-il-5-(2,2,2-trifluoretil)-4,5-dihidro-2H,4H-pirazolo[4,3-c]kinolin-8-karbonitril; – spoj 202: 4-okso-7-pirid-4-il-5-(2,2,2-trifluoretil)-4,5-dihidro-2H,4H-pirazolo[4,3-c]kinolin-8-karboksilna kiselina; – spoj 203: 3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksilna kiselina; – spoj 204: 2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzojeva kiselina; – spoj 205: 4-okso-7-(pirid-4-il)-5-(2,2,2-trifluoretil)-4,5-dihidro-2H-pirazolo[4,3-c]kinolin-8-karboksamid; – spoj 206: 7-[2-(morfolin-4-ilkarbonil)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 207: N-[2-(dimetilamino)etil]-N-metil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzamid; – spoj 208: N-(2-dimetilaminoetil)-N-etil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzamid; – spoj 209: 7-{2-[(4-metil-1,4-diazepan-1-il)karbonil]fenil}-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 210: 7-{2-[(4-metilpiperazin-1-il)karbonil]fenil}-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 211: N-(3-karbamoilfenil)-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzamid; – spoj 212: N-(3-dimetilaminopropil)-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]benzamid; – spoj 213: N,N-dimetil-3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksamid; – spoj 214: 2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]-N-[2-(pirid-4-il)etil]benzamid; – spoj 215: N-[2-(dimetilamino)etil]-N-metil-3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksamid; – spoj 216: 7-[2-(1,4-oksazepan-4-ilkarbonil)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 217: N-metil-3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksamid; – spoj 218: 2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]-N-(pirid-3-ilmetil)benzamid; – spoj 219: N-etil-2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]-N-(pirid-4-ilmetil)benzamid; – spoj 220: 3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksamid; – spoj 221: N-[2-(dimetilamino)etil]-N-etil-3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karboksamid; – spoj 222: 7-[2-((2S,6R)-2,6-dimetilmorfolin-4-karbonil)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 223: N-{3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-2-il}acetamid; – spoj 224: 3-dimetilamino-N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-2H,4H-pirazolo[4,3-c]kinolin-7-il]fenil}propionamid; – spoj 225: 4-(dimetilamino)-N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}butanamid; – spoj 226: N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}acetamid; – spoj 227: N-{3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-2-il}ciklopropankarboksamid; – spoj 228: 2-metoksi-N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}-2-fenilacetamid; – spoj 229: N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}-2-fenilpropionamid; – spoj 230: 2-(3-klorfenil)-N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}acetamid; – spoj 231: 2-(2,4-diklorfenil)-N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}acetamid; – spoj 232: N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-2H-pirazolo[4,3-c]kinolin-7-il]fenil}metansulfonamid; – spoj 233: 2-(dimetilamino)-N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}etansulfonamid; – spoj 234: N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}-1-fenilmetansulfonamid; – spoj 235: 3-klor-N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]fenil}benzensulfonamid; – spoj 236: N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}metansulfonamid; – spoj 237: N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}-1-fenilmetansulfonamid; – spoj 238: 3-klor-N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}benzensulfonamid; – spoj 239: N-(4-metoksi-3-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-ilsulfamoil}benzil)acetamid; – spoj 240: N-{4-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-3-il}-2-fenoksibenzensulfonamid; – spoj 241: N-metil-N-{3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-2-il}acetamid; – spoj 242: N-metil-N-{3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]pirid-2-il}ciklopropankarboksamid; – spoj 243: 7-[2-(metilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 244: 7-[2-(1,4-diazepan-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 245: 7-(3,4,5,6-tetrahidro-2H-[1,2′]bipiridinil-3′-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 246: 7-[2-(3-hidroksipirolidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 247: 7-[2-(3,4-dihidroksipirolidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 248: 7-[2-(dimetilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 249: 7-{2-[etil(metil)amino]pirid-3-il}-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 250: 7-{2-[(2-hidroksietil)(metil)amino]pirid-3-il}-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 251: 7-[2-(pirolidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 252: 7-[2-(1,4-oksazepan-4-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 253: 7-[2-(3-oksopiperazin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 254: 7-[2-(azetidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 255: 7-{2-[(2-metoksietil)metilamino]pirid-3-il}-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 256: 7-[2-(4-acetilpiperazin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 257: 7-[2-(dietilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 258: 7-[2-(ciklobutilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 259: 7-[2-(2,6-dimetilmorfolin-4-il)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 260: 7-[2-(4-ciklopropilpiperazin-1-il)pirid-4-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 261: 7-(2-cikloheksilaminopirid-3-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 262: 7-[2-(izopropilmetilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 263: 7-(2-ciklopentilaminopirid-3-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 264: 7-(6-pirolidin-1-ilpirid-2-il)-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 265: 7-[6-(2,6-dimetilmorfolin-4-il)pirid-2-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 266: 7-{2-[cikloheksil(metil)amino]pirid-3-il}-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 267: 7-[2-(4-ciklopropilpiperazin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 268: 7-[3-(4-ciklopropilpiperazin-1-il)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 269: 7-[2-(4-acetil-1,4-diazepan-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 270: 7-[2-(4-metil-1,4-diazepan-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 271: 7-[2-(4-ciklopropil-[1,4]diazepan-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 272: 7-[2-(3-fluorpirolidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-2,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 273: 7-[2-(4-fluorpiperidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 274: 7-(2-hidroksipirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 275: 7-(1-oksipirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 276: 7-(1-oksipirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
6. Spoj formule (I) u skladu s bilo kojim od prethodnih patentnih zahtjeva, naznačen time što ga se bira između sljedećih spojeva: – spoj 1: 7-(pirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 2: 7-(2-aminopirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 6: 7-(pirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 19: 7-[4-(4-metilpiperazin-1-il)fenil]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 67: 5-etil-7-[6-(piperazin-1-il)pirid-3-il]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 68: 7-[2-(4-metilpiperazin-1-il)pirid-4-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 69: 5-etil-7-[2-(4-metilpiperazin-1-il)pirid-4-il]-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 72: 7-(2-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 74: 7-(2-klor-6-metilpirid-3-il)-5-etil-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 75: 7-(2-klor-6-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 76: 7-(2-klorpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 77: 7-(2-fluorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 79: 7-(6-klor-2-metilpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 83: 7-[6-(morfolin-4-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 88: 7-(6-klorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 111: 7-(2-klorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 168: 7-(2,6-dimetilpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 169: 7-(3-klorpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 171: 7-(6-metilpirid-2-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 172: 7-[2-(morfolin-4-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 176: 3-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-1H-pirazolo[4,3-c]kinolin-7-il]piridin-2-karbonitril; – spoj 186: 7-(2-metilpirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 196: 8-klor-7-(pirid-4-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 199: 8-klor-7-(2-klorpirid-3-il)-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 209: 7-{2-[(4-metil-1,4-diazepan-1-il)karbonil]fenil}-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 232: N-{2-[4-okso-5-(2,2,2-trifluoretil)-4,5-dihidro-2H-pirazolo[4,3-c]kinolin-7-il]fenil}metansulfonamid; – spoj 248: 7-[2-(dimetilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 251: 7-[2-(pirolidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 257: 7-[2-(dietilamino)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; – spoj 273: 7-[2-(4-fluorpiperidin-1-il)pirid-3-il]-5-(2,2,2-trifluoretil)-1,5-dihidro-4H-pirazolo[4,3-c]kinolin-4-on; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
7. Spoj formule (V): [image] , naznačen time što R3 je definiran kao u patentnom zahtjevu 1, a Hal predstavlja atom halogena; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
8. Spoj formule (VI): [image] , naznačen time što R3 je definiran kao u patentnom zahtjevu 1, Hal predstavlja atom halogena, a PG predstavlja zaštitnu skupinu; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
9. Spoj formule (VII): [image] , naznačen time što su R1 i R3 definirani kao u patentnom zahtjevu 1, Hal predstavlja atom halogena, a PG predstavlja zaštitnu skupinu; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
10. Spoj formule (VIII): [image] , naznačen time što su R1, R2 i R3 definirani kao u patentnom zahtjevu 1, a PG predstavlja zaštitnu skupinu; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
11. Spoj formule (IX): [image] , naznačen time što je R2 definiran kao u patentnom zahtjevu 1, R3 predstavlja -H, halogen, -(C1-C6)alkil, cijano skupinu ili -CONH2, a PG predstavlja zaštitnu skupinu; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
12. Spoj formule (XIV): [image] , naznačen time što su R1 i R3 definirani kao u patentnom zahtjevu 1, a Hal predstavlja atom halogena; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
13. Spoj formule (XIX): [image] , naznačen time što su R1 i R3 definirani kao u patentnom zahtjevu 1, a R predstavlja atom vodika ili su obje skupine R atomi ugljika vezani zajedno i izborno supstituirani s jednom ili više (C1-C4)alkilnih skupina; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
14. Spoj formule (XX): [image] , naznačen time što su R1 i R3 definirani kao u patentnom zahtjevu 1, R predstavlja atom vodika ili su obje skupine R atomi ugljika vezani zajedno i izborno supstituirani s jednom ili više (C1-C4)alkilnih skupina, a PG predstavlja zaštitnu skupinu; u obliku baze ili adicijske soli s kiselinom, te također u obliku hidrata.
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UY34350A (es) 2013-04-30
AR088000A1 (es) 2014-04-30
ES2605152T3 (es) 2017-03-13
MX2014003675A (es) 2014-08-21
AU2012314620A1 (en) 2014-03-27
KR20140082743A (ko) 2014-07-02
SG11201400403SA (en) 2014-08-28
RU2621037C2 (ru) 2017-05-31
TWI527815B (zh) 2016-04-01
CA2847921A1 (en) 2013-04-04
SI2573073T1 (sl) 2015-02-27
EP2760841B1 (en) 2016-08-24
PT2573073E (pt) 2015-02-05
TW201313719A (zh) 2013-04-01
CN103958479B (zh) 2017-06-13
EP2760841A1 (en) 2014-08-06

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