HRP20191840T1 - Derivati tieno[3,2-d]pirimidina s inhibitornom aktivnosti za protein kinaze - Google Patents

Derivati tieno[3,2-d]pirimidina s inhibitornom aktivnosti za protein kinaze Download PDF

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HRP20191840T1
HRP20191840T1 HRP20191840TT HRP20191840T HRP20191840T1 HR P20191840 T1 HRP20191840 T1 HR P20191840T1 HR P20191840T T HRP20191840T T HR P20191840TT HR P20191840 T HRP20191840 T HR P20191840T HR P20191840 T1 HRP20191840 T1 HR P20191840T1
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amino
pyrimidine
thieno
carboxamide
methylisoquinolin
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In Hwan Bae
Jung Beom Son
Sang Mi Han
Eun Joo Kwak
Ho Seok Kim
Ji Young Song
Eun Young Byun
Seung Ah JUN
Young Gil Ahn
Kwee Hyun Suh
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Hanmi Pharm. Co., Ltd.
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Claims (22)

1. Derivat tieno[3,2-d]pirimidina formule (I): pri čemu, A je C6-10 aril ili 5- do 10-člani heteroaril; W je O, S, S(O), S(O)2, NH, -NHNH- ili 3- do 6- člani heterocikloalkil; X i Y su svaki neovisno CH ili N; Z je hidrogen, C1-3 alkil ili NR3R4, pri čemu navedeni R3 i R4 su svaki neovisno vodik, C1-6 alkil ili -(CH2)q-B, B predstavlja NR5R6, C1-6 alkoksi, C3-6 cikloalkil ili 3- do 6-člani heterocikloalkil; R1 je vodik, halogen, C1-3 alkil ili C1-3 alkoksi, pri čemu je navedeni alkil ili alkoksi nesupstituiran ili supstituiran s jednim ili više atoma halogena; R2 je vodik, halogen, -CF3, -NO2, -OH, -CN, C1-6 alkoksi, C1-6 alkil, C2-4 alkenil, C2-4 alkinil, -NR7R8, -NHSO2R9, -SO2R10, -C(O)R11, -NHC(O)R12, -NHC(O)OR13,-S(O)R14, C3-6 cikloalkil, 5- do 10-člani heterocikloalkil, C6-10 aril, C6-10 ariloksi, 5- do 10-člani heteroaril ili 3- do 6- člani heteroariloksi, pri čemu je navedeni R2 povezan s A pomoću -(CH2)p- ili supstituiran sa C1-4 alkil, C2-4alkinil, C1-4alkilkarbonil ili jedan ili više atoma halogena; R5, R6, R7, R8, R9, R10, R11, R12, R13 i R14 su svaki neovisno vodik, -NH2, C1-6 alkil, C1-6 alkoksi, C3-6 cikloalkil ili 3- do 6-člani heterocikloalkil, navedeni alkil, alkoksi, cikloalkil ili heterocikloalkil su nesupstituirani ili supstituirani s jednim ili više atoma halogena; q je cijeli broj u rasponu od 0 do 3; p je cijeli broj u rasponu od 0 do 3; m je cijeli broj u rasponu od 0 do 5; n je cijeli broj u rasponu od 0 do 2; ili njihova farmaceutski prihvatljiva sol.
2. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 1, pri čemu W je NH ili njegova farmaceutski prihvatljiva sol.
3. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 1, pri čemu Z je NR3R4 ili njegova farmaceutski prihvatljiva sol.
4. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 1, pri čemu X je CH i Y je N ili njegova farmaceutski prihvatljiva sol.
5. Derivat tieno[3,2-d]pirimidina, koji je izabran iz skupine koja se sastoji od: 1) 4-amino-N-(1-((4-klorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7- karboksamid; 2) 4-amino-N-(6-metil-1-((3-(trifluorometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7- karboksamid; 3) N-(1-((4-klorofenil)amino)-6-metilizokvinolin-5-il)-4-(ciklopropilamino)tieno[3,2-d]pirimidin-7-karboksamid; 4) 4-(ciklopropilamino)-N-(6-metil-1-((3-(trifluorometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 5) 4-amino-N-(6-metil-1-((3-(4-metil-1H-imidazol-1-il)-5-(trifluorometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 6) 4-(ciklopropilamino)-N-(6-metil-1-((3-(4-metil-1H-imidazol-1-il)-5-(trifluorometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 7) 4-amino-N-(1-((4-((4-etilpiperazin-1-il)metil)-3-(trifluorometil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 8) 4-(ciklopropilamino)-N-(1-((4-((4-etilpiperazin-1-il)metil)-3-(trifluorometil)phenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 9) N-(1-((4-((4-etilpiperazin-1-il)metil)-3-(trifluorometil)fenil)amino)-6-metilizokvinolin-5-il)-4-(metilamino)tieno[3,2-d]pirimidin-7-karboksamid; 10) 4-amino-N-(1-((4-(4-etilpiperazin-1-il)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 11) 4-amino-N-(1-((4-((4-etilpiperazin-1-il)metil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 12) 4-amino-N-(6-metil-1-((3-(trifluorometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 13) 4-amino-N-(1-((4-kloro-3-(trifluorometil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 14) 4-amino-N-(1-((2-metoksi-5-(trifluorometil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 15) 4-amino-N-(6-metil-1-((4-(trifluorometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 16) 4-amino-N-(1-((4-metoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 17) 4-amino-N-(6-metil-1-(p-tolilamino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 18) 4-amino-N-(1-((4-izopropilfenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 19) 4-amino-N-(1-((5-(t-butil)izoksazol-3-il)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 20) 4-amino-N-(1-((4-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 21) 4-amino-N-(6-metil-1-(tiazol-2-ilamino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 22) 4-amino-N-(1-((4-cijanofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 23) 4-amino-N-(6-metil-1-(kvinolin-5-ilamino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 24) 4-amino-N-(1-((4-etoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 25) 4-amino-N-(6-metil-1-((4-fenoksifenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 26) 4-amino-N-(1-((4-hidroksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 27) 4-amino-N-(1-((4-izopropoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 28) 4-amino-N-(1-((4-(dimetilamino)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 30) 4-amino-N-(1-((3,4-dimetoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 31) 4-amino-N-(1-((3-fluoro-4-metoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 32) 4-amino-N-(6-metil-1-((3,4,5-trimetoksifenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 36) 4-amino-N-(4-((4-klorofenil)amino)-7-metilkvinazolin-8-il)tieno[3,2-d]pirimidin-7-karboksamid; 37) 4-(ciklopropilamino)-N-(1-((4-metoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 38) 4-amino-N-(1-((3-klorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 39) 4-amino-N-(1-((3-bromofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 40) 4-amino-N-(1-((2,4-diklorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 41) 4-amino-N-(1-((3,4-diklorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 42) 4-amino-N-(1-((3,5-diklorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 43) 4-amino-N-(6-metil-1-((3,4,5-triklorofenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 44) 4-amino-N-(1-((4-kloro-3-metoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 45) 4-amino-N-(1-benzilamino-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 46) 4-amino-N-(6-metil-1-fenoksizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 47) 4-amino-N-(6-metil-1-((4-morfolinofenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 48) N-(1-((4-(1H-pirol-1-il)fenil)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid; 49) 4-amino-N-(6-metil-1-(pirimidin-4-ilamino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 50) 4-amino-N-(1-((4-(difluorometoksi)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 51) 4-amino-N-(6-metil-1-((4-(trifluorometoksi)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 52) 4-amino-N-(1-((4-klorofenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 53) 4-amino-N-(5-((4-klorofenil)amino)naftalen-1-il)tieno[3,2-d]pirimidin-7-karboksamid; 54) 4-amino-N-(1-((4-etinilfenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 57) 4-amino-N-(1-((4-(fluorometoksi)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 58) N-(1-(4-klorofenilamino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 59) 4-amino-N-(1-((4-kloro-3-((dimetilamino)metil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 60) 4-amino-N-(1-((4-kloro-3-(pirolidin-1-ilmetil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 61) 4-amino-N-(1-((4-kloro-3-((dietilamino)metil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 63) 4-amino-N-(1-((4-kloro-3-(piperidin-1-ilmetil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 64) 4-amino-N-(1-((4-kloro-3-(morfolinometil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 65) 4-amino-N-(1-((4-kloro-3-((4-metilpiperazin-1-il)metil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 66) 4-amino-N-(1-((4-kloro-3-((diizopropilamino)metil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 67) 4-amino-N-(6-metil-1-((3-(metilsulfonamido)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 68) tert-butil 4-(5-((5-(4-aminotieno[3,2-d]pirimidin-7-karboksamido)-6-metilizokvinolin-1-il)amino)-2-klorobenzil)piperazin-1-karboksilat; 69) 4-amino-N-(1-((4-kloro-3-(piperazin-1-ilmetil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 70) 4-amino-N-(1-((3-kloro-4-metoksifenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 73) 4-amino-N-(1-((4-kloro-2-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 74) 4-amino-N-(1-((4-bromo-2-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 75) 4-amino-N-(1-((4-metoksibenzil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 76) 4-amino-N-(1-((4-klorobenzil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 77) 4-amino-N-(1-(2-(4-klorofenil)hidrazinil)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 78) 4-amino-N-(1-((3-((dimetilamino)metil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 79) 4-amino-N-(6-metil-1-((4-okso-4H-kromen-6-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 80) N-(1-((3-acetilfenil)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid; 82) 4-amino-N-(6-metil-1-((3-(trifluorometoksi)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 83) N-(1-((4-acetilfenil)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid; 84) 4-amino-N-(6-metil-1-((4-(metilsulfonamido)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 85) 4-amino-N-(6-metil-1-((3-(metilsulfonil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 86) 4-amino-N-(1-((4-kloro-3-(metoksimetil)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 87) 4-amino-N-(1-((4-metoksi-3-(metilsulfonamido)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 88) 4-amino-N-(1-((4-kloro-3-(metilsulfonamido)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 89) 4-amino-N-(1-((6-kloropiridin-3-il)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 90) 4-amino-N-(1-((2-kloropiridin-4-il)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidine-7-karboksamid; 91) 4-amino-N-(6-metil(4-(metilsulfonamidometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 92) 4-amino-N-(6-metil-1-((3-(metilsulfonamidometil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 93) 4-amino-N-(1-((4-kloro-3-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 94) 4-amino-N-(1-((3-bromo-4-klorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 96) N-(1-((3-acetamidofenil)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid; 97) 4-amino-N-(6-metil-1-((1-metil-1H-indazol-6-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 98) 4-amino-N-(6-metil-1-((4-(metilsulfinil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 99) 4-amino-N-(6-metil-1-((2-metil-1,3-dioksoizoindolin-5-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 100) 4-amino-N-(1-((6-metoksipiridin-3-il)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 101) 4-amino-N-(6-metil-1-((3-(2,2,2-trifluoroacetil)fenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 102) 4-amino-N-(6-metil-1-((4-propionilfenil)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 103) 4-amino-N-(1-((4-heksanoilfenil)amino)-6-metilizokvinolin-il)tieno[3,2-d]pirimidin-7-karboksamid; 104) N-(1-((1-acetil-1H-indazol-6-il)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid; 105) 4-amino-N-(1-((3-kloro-4-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 107) 4-amino-N-(6-metil-1-((2-metil-2H-indazol-6-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 108) metil 4-((5-(4-aminotieno[3,2-d]pirimidin-7-karboksamido)-6-metilizokvinolin-1-il)amino)benzoat; 109) 4-amino-N-(6-metil-1-((1-metil-1H-indazol-5-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 110) 4-amino-N-(6-metil-1-((2-metil-2H-indazol-5-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 111) 4-amino-N-(6-metil-1-((6-metilpiridin-3-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 112) 4-amino-N-(6-metil-1-((1-metil-1H-indol-6-il)amino)izokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 113) tert-butil 6-((5-(4-aminotieno[3,2-d]pirimidin-7-karboksamido)-6-metilizokvinolin-1-il)amino)-1H-indazol-1-karboksilat; 114) N-(1-((1H-indazol-6-il)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid hidroklorid; 115) 4-amino-N-(1-((5-kloro-2-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 116) 4-amino-N-(1-((3-kloro-2-fluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 117) 4-amino-N-(1-((3-fluoro-4-(4-metilpiperazin-1-il)fenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 118) 4-amino-N-(1-((3-kloro-1-metil-1H-indazol-6-il)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 119) 4-amino-N-(6-metil-1-((4-(prop-2-in-1-iloksi)fenil)amino)izokvmolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 120) 4-amino-N-(1-((2-metoksi-4-morfolinofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 121) 4-amino-N-(1-(benzo[d]tiazol-6-ilamino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; 122) N-(1-((1H-indazol-5-il)amino)-6-metilizokvinolin-5-il)-4-aminotieno[3,2-d]pirimidin-7-karboksamid; i 123) 4-amino-N-(1-((3-kloro-2,4-difluorofenil)amino)-6-metilizokvinolin-5-il)tieno[3,2-d]pirimidin-7-karboksamid; ili njegova farmaceutski prihvatljiva sol.
6. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
7. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
8. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
9. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
10. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
11. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
12. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
13. Derivat tieno[3,2-d]pirimidina u skladu s patentnim zahtjevom 5, sljedeće strukture: ili njegova farmaceutski prihvatljiva sol.
14. Farmaceutski pripravak koji sadrži spoj u skladu s bilo kojim od patentnih zahtjeva 1 do 13, kao aktivni sastojak.
15. Spoj ili pripravak u skladu s bilo kojim od prethodnih patentnih zahtjeva za uporabu u prevenciji ili liječenju bolesti uzrokovane nenormalnom aktivacijom protein kinaze.
16. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevom 15, pri čemu je navedena protein kinaza izabrana iz skupine koja se sastoji od: ALK, AMPK, Aurora A, Aurora B, Aurora C, Axl, Blk, Bmx, BTK, CaMK, CDK2/cyclinE, CDK5/p25, CHK1, CK2, c-RAF, DDR1, DDR2, DMPK, EGFR1, Her2, Her4, EphAl, EphB1, FAK, FGFR2, FGFR3, FGFR4, Flt-1, Flt-3, Flt-4, Fms (CSF-1), Fyn, GSK3beta, HIPK1, IKKbeta, IGFR-1R, IR, Itk, JAK2, JAK3, KDR, Kit, Lck, Lyn, MAPK1, MAPKAP-K2, MEK1, Met, MKK6, MLCK, NEK2, p70S6K, PAK2, PDGFR alfa, PDGFR beta, PDK1, Pim-1, PKA, PKBalfa, PKCalfa, Plkl, Ret, ROCK-I, Rskl, SAPK2a, SGK, Src, Syk, Tie-2, Tec, Trk i ZAP-70.
17. Spoj ili pripravak za uporabu u skladu s patentnim zahtjevom 15, pri čemu je navedena bolest izabrana iz skupine koja se sastoji od: karcinoma želuca, karcinoma pluća, karcinoma jetre, kolorektalnog karcinoma, karcinoma tankog crijeva, karcinoma gušterače, karcinoma mozga, raka kostiju, melanoma, raka dojke, sklerozirajuće adenoze, raka maternice, raka grlića maternice, karcinoma glave i vrata, karcinoma jednjaka, karcinoma štitnjače, paratiroidnog karcinoma, karcinoma bubrega, sarkoma, karcinoma prostate, karcinoma uretre, karcinoma mokraćnog mjehura, karcinoma krvi, limfoma, fibroadenoma, upale, dijabetesa, pretilosti, psorijaze, reumatoidnog artritisa, hemangioma, akutne ili kronične bolesti bubrega, koronarne restenoze, autoimunih bolesti, astme, neurodegenerativnih bolesti, akutne infekcije ili očnih bolesti uzrokovanih angiogenezom.
18. Farmaceutski pripravak u skladu s patentnim zahtjevom 14, pri čemu farmaceutski pripravak nadalje sadrži aktivnu tvar izabranu iz skupine koja se sastoji od inhibitora transdukcije staničnog signala, inhibitora mitoze, alkilirajućih sredstava, antimetabolita, antibiotika, inhibitora faktora rasta, inhibitora staničnog ciklusa, inhibitora topoizomeraze, modifikatora biološke reakcije, antihormonalnih sredstava, antiandrogena, inhibitora stanične diferencijacije / proliferacije / preživljavanja, inhibitora apoptoze, inhibitora upale i inhibitora P-glikoproteina.
19. Farmaceutska formulacija koja sadrži farmaceutski pripravak u skladu s patentnim zahtjevom 14.
20. Farmaceutska formulacija u skladu s patentnim zahtjevom 19, pri čemu je navedena formulacija formulacija za oralnu primjenu.
21. Farmaceutska formulacija u skladu s patentnim zahtjevom 19, pri čemu je navedena formulacija u obliku tablete, pilule, praška, kapsule, sirupa, emulzije ili mikroemulzije.
22. Farmaceutska formulacija u skladu s patentnim zahtjevom 19, koja se koristi u kombinaciji ili je razvijena u kombiniranu formulaciju s aktivnom tvari izabranom iz skupine koja se sastoji od inhibitora transdukcije staničnog signala, inhibitora mitoze, alkilirajućih sredstava, antimetabolita, antibiotika, inhibitora faktora rasta, inhibitora staničnog ciklusa, inhibitora topoizomeraze, modifikatora biološke reakcije, antihormonalnih sredstava, antiandrogena, inhibitora stanične diferencijacije / proliferacije / preživljavanja, inhibitora apoptoze, inhibitora upale i inhibitora P-glikoproteina.
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