HRP20220502T1 - Kombinacije koje sadrže derivate 5-fenoksi-3h-pirimidin-4-ona i njihova uporaba za profilaksu ili liječenje infekcije hiv-om - Google Patents

Kombinacije koje sadrže derivate 5-fenoksi-3h-pirimidin-4-ona i njihova uporaba za profilaksu ili liječenje infekcije hiv-om Download PDF

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HRP20220502T1
HRP20220502T1 HRP20220502TT HRP20220502T HRP20220502T1 HR P20220502 T1 HRP20220502 T1 HR P20220502T1 HR P20220502T T HRP20220502T T HR P20220502TT HR P20220502 T HRP20220502 T HR P20220502T HR P20220502 T1 HRP20220502 T1 HR P20220502T1
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alkyl
haloalkyl
independently
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ariq
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Kenneth L. Arrington
Christopher Burgey
Robert Gilfillan
Yongxin Han
Mehul Patel
Chun Sing Li
Yaozong LI
Yunfu Luo
Jiayi Xu
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Merck Sharp & Dohme Corp.
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Claims (15)

1. Kombinacija koja sadrži (i) spoj formule (Ia): [image] ili njegovu farmaceutski prihvatljivu sol i (ii) jedno ili više sredstava protiv HIV-a izabranih od antivirusnih sredstava protiv HIV-a, imunomodulatora i anti-infektivnih sredstava, gdje: M je CH2, CH2CH2, CH2CH2CH2, CH(CH3), C(CH3)2 ili C(O)N(RA); Z je izabran iz grupe koja se sastoji od: piridazina, piridazinona, pirimidina, pirimidinona, pirazina, pirazinona, triazina i triazinona, svaki izborno supstituiran sa jednim ili više supstituenata do maksimalnog broja dozvoljenog valentnošću izabranog od R4 i R5; svaki K1 i K2 su neovisno F, Br, Cl, OCHF2, CF3 ili CN; R2 je izabran iz grupe koja se sastoji od: (1) H, (2) C1-6 alkila, (3) C1-6 haloalkila, (4) C1-6 alkila supstituiranog sa od 1 do 3 supstituenta od kojih je svaki neovisno OH, O-C1-6 alkil, O-C1-6 haloalkil, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB ili N(RA)C(O)C(O)N(RA)RB, (5) O-C1-6 alkila u kojem je alkil izborno supstituiran sa 1 do 3 supstituenta neovisno izabrana od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, ili S(O)2N(RA)RB, (6) O-C1-6 haloalkila, (7) halogena, (8) CN, (9) NO2, (10) N(RA)RB, (11) C(O)N(RA)RB, (12) C(O)RA, (13) C(O)-C1-6 haloalkila, (14) C(O)ORA, (15) OC(O)RA, (16) OC(O)N(RA)RB, (17) SRA, (18) S(O)RA, (19) S(O)2RA, (20) S(O)2N(RA)RB, (21) N(RA)S(O)2RB, (22) N(RA)S(O)2N(RA)RB, (23) N(RA)C(O)RB, (24) N(RA)C(O)N(RA)RB, (25) N(RA)C(O)-C(O)N(RA)RB, (26) N(RA)CO2RB, (27) N(RC)RD, (28) C(O)N(RC)RD, (29) OC(O)N(RC)RD, (30) S(O)2N(RC)RD, (31) N(RA)S(O)2N(RC)RD, (32) N(RA)C(O)N(RC)RD, (33) N(RA)C(O)-C(O)N(RC)RD, (34) CycA, (35) -O-CycA, (36) ArilA, ili (37) HetA; R3 je H, C1-6 alkil, halogen, CN, C1-6 fluoroalkil, OH, O-C1-6 alkil ili O-C1-6 haloalkil; R4 i R5 su svaki neovisno izabrani od: (1) H, (2) C1-6 alkila, C2-6 alkenila ili C2-6 alkinila, svaki izborno supstituiran sa jednim ili više supstituenata do maksimalnog broja dozvoljenog valentnošću izabranog od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, N(RA)C(O)C(O)N(RA)RB, CycB, ArilB i HetB, (3) C1-6 haloalkila izborno dodatno supstituiranog sa jednim ili više supstituenata do maksimalnog broja dozvoljenog valentnošću izabranog od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, N(RA)C(O)C(O)N(RA)RB, CycB, ArilB i HetB (4) O-C1-6 alkila u kojem je dio alkila izborno supstituiran sa jednim ili više supstituenata do maksimalnog broja dozvoljenog valentnošću izabranog od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, N(RA)C(O)C(O)N(RA)RB, CycB, ArilB i HetB, (5) O-C1-6 haloalkila, izborno dodatno supstituiranog sa jednim ili više supstituenata do maksimalnog broja dozvoljenog valentnošću izabranog od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, N(RA)C(O)C(O)N(RA)RB, CycB, ArilB i HetB, (6) halogena, (7) CN, (8) NO2, (9) N(RA)RB, (10) C(O)N(RA)RB, (11) C(O)RA, (12) C(O)-C1-6 haloalkila, (13) C(O)ORA, (14) OC(O)RA, (15) OC(O)N(RA)RB, (16) SRA, (17) S(O)RA, (18) S(O)2RA, (19) S(O)2N(RA)RB, (20) N(RA)S(O)2RB, (21) N(RA)S(O)2N(RA)RB, (22) N(RA)C(O)RB, (23) N(RA)C(O)N(RA)RB, (24) N(RA)C(O)-C(O)N(RA)RB, (25) N(RA)CO2RB, (26) N(RC)RD, (27) C(O)N(RC)RD, (28) OC(O)N(RC)RD, (29) S(O)2N(RC)RD, (30) N(RA)S(O)2N(RC)RD, (31) N(RA)C(O)N(RC)RD, (32) N(RA)C(O)-C(O)N(RC)RD, (33) OH, (34) CycB, (35) ArilB, (36) HetB, (37) -J-CycB, (38) -J-ArilB, i (39) -J-HetB, ili R4 i R5 na susjednim atomima mogu biti spojeni zajedno sa atomima za koje su vezani tako da formiraju fuzionirani CycC, ArilC ili HetC; CycA, CycB i CycC su neovisno karbociklil koji je C3-8 cikloalkil, C5-8 cikloalkenil ili C7-12 bicikličan, zasićeni ili nezasićeni, nearomatičan sustav prstena u kojem je jedan prsten fuzioniran za ili premošćen sa drugim prstenom; pri čemu je karbociklil izborno supstituiran sa ukupno od 1 do 6 supstituenata, pri čemu: (i) od nula do 6 supstituenata su svaki neovisno: (1) halogen, (2) CN, (3) C1-6 alkil, (4) OH, (5) O-C1-6 alkil, (6) C1-6 haloalkil, (7) O-C1-6 haloalkil, (8) C1-6 alkenil, ili (9) C1-6 alkenil supstituiran sa CN, i (ii) od nula do 2 supstituenta su svaki neovisno: (1) CycQ, (2) AriQ, (3) HetQ, (4) HetR, (5) J-CycQ, (6) J-AriQ, (7) J-HetQ, (8) J-HetR, (9) C1-6 alkil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR, (10) C2-6 alkenil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR, ili (11) C2-6 alkinil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR; ArilA, ArilB i ArilC su neovisno aril koji je izborno supstituiran sa ukupno od 1 do 8 supstituenata, pri čemu: (i) od nula do 8 supstituenata su svaki neovisno: (1) C1-6 alkil, (2) C1-6 haloalkil, koji je izborno supstituiran sa 1 do 3 dodatna supstituenta od kojih je svaki neovisno izabran od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (3) C1-6 alkila supstituiranog sa od 1 do 3 supstituenta od kojih je svaki neovisno izabran od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (4) C2-6 alkenil, (5) C2-6 alkenil supstituiran sa od 1 do 3 supstituenta od kojih je svaki neovisno OH, O-C1-6 alkil, O-C1-6 haloalkil, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (6) C2-6 alkinil, (7) C2-6 alkinil supstituiran sa od 1 do 3 supstituenta od kojih je svaki neovisno OH, O-C1-6 alkil, O-C1-6 haloalkil, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (8) O-C1-6 alkil, (9) O-C1-6 haloalkil, (10) OH, (11) halogen, (12) CN, (13) NO2, (14) N(RA)RB, (15) C(O)N(RA)RB, (16) C(O)RA, (17) C(O)-C1-6 haloalkil, (18) C(O)ORA, (19) OC(O)N(RA)RB, (20) SRA, (21) S(O)RA, (22) S(O)2RA, (23) S(O)2N(RA)RB, (24) N(RA)S(O)2RB, (25) N(RA)S(O)2N(RA)RB, (26) N(RA)C(O)RB, (27) N(RA)C(O)N(RA)RB, (28) N(RA)C(O)-C(O)N(RA)RB, ili (29) N(RA)CO2RB, i (ii) od nula do 2 supstituenta su svaki neovisno: (1) CycQ, (2) AriQ, (3) HetQ, (4) HetR, (5) J-CycQ, (6) J-AriQ, (7) J-HetQ, (8) J-HetR, (9) C1-6 alkil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR, (10) C2-6 alkenil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR, ili (11) C2-6 alkinil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR; HetA, HetB i HetC su neovisno heterociklil ili heteroaril koji je izborno supstituiran sa ukupno od 1 do 8 supstituenata, gdje: (i) od nula do 8 supstituenata su svaki neovisno: (1) C1-6 alkil, (2) C1-6 haloalkil, koji je izborno supstituiran sa 1 do 3 dodatna supstituenta od kojih je svaki neovisno izabran od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (3) C1-6 alkil supstituiran sa od 1 do 3 supstituenta od kojih je svaki neovisno izabran od OH, O-C1-6 alkila, O-C1-6 haloalkila, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (4) C2-6 alkenil, (5) C2-6 alkenil supstituiran sa od 1 do 3 supstituenta od kojih je svaki neovisno OH, O-C1-6 alkil, O-C1-6 haloalkil, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (6) C2-6 alkinil, (7) C2-6 alkinil supstituiran sa od 1 do 3 supstituenta od kojih je svaki neovisno OH, O-C1-6 alkil, O-C1-6 haloalkil, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, S(O)2RA, S(O)2N(RA)RB, N(RA)C(O)RB, N(RA)CO2RB, N(RA)S(O)2RB, N(RA)S(O)2N(RA)RB, OC(O)N(RA)RB, N(RA)C(O)N(RA)RB, ili N(RA)C(O)C(O)N(RA)RB, (8) O-C1-6 alkil, (9) O-C1-6 haloalkil, (10) OH, (11) okso, (12) halogen, (13) CN, (14) NO2, (15) N(RA)RB, (16) C(O)N(RA)RB, (17) C(O)RA, (18) C(O)-C1-6 haloalkil, (19) C(O)ORA, (20) OC(O)N(RA)RB, (21) SRA, (22) S(O)RA, (23) S(O)2RA, (24) S(O)2N(RA)RB, (25) N(RA)S(O)2RB, (26) N(RA)S(O)2N(RA)RB, (27) N(RA)C(O)RB, (28) N(RA)C(O)N(RA)RB, (29) N(RA)C(O)-C(O)N(RA)RB, ili (30) N(RA)CO2Rb, i (ii) od nula do 2 supstituenta su svaki neovisno: (1) CycQ, (2) AriQ, (3) HetQ, (4) HetR, (5) J-CycQ, (6) J-AriQ, (7) J-HetQ, (8) J-HetR, (9) C1-6 alkil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR, (10) C2-6 alkenil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR, ili (11) C2-6 alkinil supstituiran sa CycQ, AriQ, HetQ, HetR, J-CycQ, J-AriQ, J-HetQ, ili J-HetR; svaki CycQ je neovisno C3-8 cikloalkil ili C5-8 cikloalkenil, pri čemu cikloalkil ili cikloalkenil je izborno supstituiran sa od 1 do 4 supstituenta, od kojih je svaki neovisno halogen, C1-6 alkil, OH, O-C1-6 alkil, C1-6 haloalkil ili O-C1-6 haloalkil; svaki AriQ je neovisno fenil ili naftil, gdje je fenil ili naftil izborno supstituiran sa od 1 do 5 supstituenata od kojih je svaki neovisno halogen, CN, NO2, C1-6 alkil, C1-6 haloalkil, OH, O-C1-6 alkil, O-C1-6 haloalkil, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA, SO2RA, SO2N(RA)RB ili SO2N(RA)C(O)RB; svaki HetQ je neovisno heteroaril koji je izborno supstituiran sa od 1 do 4 supstituenta od kojih je svaki neovisno halogen, C1-6 alkil, C1-6 haloalkil, OH, O-C1-6 alkil, O-C1-6 haloalkil, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SO2RA, N(RA)C(O)N(RA)RB ili N(RA)CO2RB; svaki HetR je neovisno 4- do 7-člani, zasićeni ili nezasićeni, nearomatični heterociklični prsten koji sadrži najmanje jedan atom ugljika i od 1 do 4 heteroatoma neovisno izabrana od N, O i S, gdje je svaki S izborno oksidiran do S(O) ili S(O)2, i gdje je zasićeni ili nezasićeni heterociklični prsten izborno supstituiran sa od 1 do 4 supstituenta od kojih je svaki neovisno halogen, CN, C1-6 alkil, OH, okso, O-C1-6 alkil, C1-6 haloalkil, O-C1-6 haloalkil, C(O)N(RA)RB, C(O)RA, CO2RA, ili SO2RA; svaki J je neovisno: (i) O, (ii) S, (iii) S(O), (iv) S(O)2, (v) O-C1-6 alkilen, (vi) S-C1-6 alkilen, (vii) S(O)-C1-6 alkilen, (viii) S(O)2-C1-6 alkilen, (ix) N(RA), ili (x) N(RA)-C1-6 alkilen; svaki RA, RB, RC i RD su neovisno izabrani od H, C1-6 alkila i C3-6cikloalkila, pri čemu su navedeni C1-6 alkil i C3-6cikloalkil izborno supstituirani sa jednim ili više supstituenata do maksimalnog broja dozvoljenog valentnošću izabranog iz grupe koja se sastoji od: halogena, OH, CN, C1-4alkoksi, C3-6cikloalkila i fenila; ili alternativno svaki par RC i RD zajedno sa dušikom za koji su oba vezani formiraju 4- do 7-člani zasićeni ili mono-nezasićeni prsten koji izborno sadrži heteroatom pored N za koji su RC i RD vezani, pri čemu je dodatni heteroatom izabran od N, O i S; pri čemu je prsten izborno supstituiran sa 1 ili 2 supstituenta od kojih je svaki neovisno C1-6 alkil, C(O)RA, C(O)ORA, C(O)N(RA)RB ili S(O)2RA; i pri čemu je izborni S u prstenu izborno u obliku S(O) ili S(O)2 svaki aril je neovisno (i) fenil, (ii) 9- ili 10-člani biciklični, fuzionirani karbociklični sustav prstena u kojem je najmanje jedan prsten aromatičan, ili (iii) 11- do 14-člani tricikličan, fuzionirani karbocikličan sustav prstena u kojem je najmanje jedan prsten aromatičan; svaki heterociklil je neovisno (i) 4- do 8-člani, zasićeni ili nezasićeni monociklični prsten, (ii) 7- do 12-člani biciklični sustav prstena, ili (iii) 10- do 18-člani tricikličan sustav prstena, gdje je svaki prsten u (ii) ili (iii) neovisan od, fuzioniran sa ili premošćen sa drugim prstenom ili prstenovima i svaki prsten je zasićen ili nezasićen; gdje monocikličan prsten sadrži od 1 do 4 heteroatoma i ravnotežu atoma ugljika; bicikličan sustav prstena ili tricikličan sustav prstena sadrži od 1 do 8 heteroatoma i ravnotežu atoma ugljika, gdje jedan ili više od prstenova sadrže jedan ili više od heteroatoma; gdje su heteroatomi izabrani od N, O i S; i gdje su bilo koji ili više od heteroatoma dušika i sumpora izborno oksidirani, i bilo koji ili više od heteroatoma dušika je izborno kvaterniziran; svaki heteroaril je neovisno (i) 5- ili 6-člani heteroaromatični prsten koji sadrži od 1 do 4 heteroatoma neovisno izabrana od N, O i S, gdje je svaki N izborno u obliku oksida, ili (ii) 9- ili 10-člani heterobicikličan, fuzionirani sustav prstena koji sadrži od 1 do 6 heteroatoma neovisno izabrana od N, O i S, gdje bilo koji ili oba prstena sadrže jedan ili više od heteroatoma, najmanje jedan prsten je aromatičan, svaki N je izborno u obliku oksida i svaki S u prstenu koji nije aromatičan je izborno S(O) ili S(O)2.
2. Kombinacija prema patentnom zahtjevu 1, naznačena time što spoj formule (Ia) je izabrano od: [image] i [image] ili njegove farmaceutski prihvatljive soli.
3. Kombinacija prema patentnom zahtjevu 2, naznačena time što spoj formule (Ia) je: [image] ili njegova farmaceutski prihvatljiva sol.
4. Kombinacija prema patentnom zahtjevu 2, naznačena time što spoj formule (Ia) je: [image] ili njegova farmaceutski prihvatljiva sol.
5. Kombinacija prema patentnom zahtjevu 2, naznačena time što spoj formule (Ia) je: [image] ili njegova farmaceutski prihvatljiva sol.
6. Kombinacija prema patentnom zahtjevu 2, naznačena time što spoj formule (Ia) je: [image] ili njegova farmaceutski prihvatljiva sol.
7. Kombinacija prema patentnom zahtjevu 2, naznačena time što spoj formule (Ia) je: [image] ili njegova farmaceutski prihvatljiva sol.
8. Kombinacija prema bilo kojem od patentnih zahtjeva 1-7, naznačena time što jedno ili više sredstava protiv HIV-a je antivirusno sredstvo izabrano od inhibitora HIV proteaze, nukleozidnih inhibitora HIV reverzne transkriptaze, nenukleozidnih inhibitora HIV reverzne transkriptaze, inhibitora HIV integraze, inhibitora fuzije HIV-a i inhibitora ulaska HIV-a.
9. Kombinacija prema bilo kojem od patentnih zahtjeva 1-7, naznačena time što su jedan ili više sredstava protiv HIV-a izabrani od: abakavir, abakavir +lamivudin, abakavir + lamivudin + zidovudin, amprenavir, atazanavir, zidovudin, kapravirin darunavir, zalcitabin, didanozin, gastrorezistentno obložen didanozin, delavirdin, efavirenc, efavirenc + emtricitabin + tenofovir disoproksil fumarat, 4’-etinil-2-fluoro-2’-deoksiadenozin emtricitabin, emtricitabin + tenofovir disoproksil fumarat, emvirin, enfuvirtid, etravirin, fosamprenavir kalcij, indinavir, lamivudin, lamivudin + zidovudin, lopinavir lopinavir + ritonavir, maravirok, nelfinavir, nevirapin, PPL-100 raltegravir, ritonavir, sakvinavir, stavudin, tenofovir disoproksil fumarat, tenofovirheksadeciloksipropil tipranavir, abakavir sulfat, delavirdin mezilat, indinavir sulfat, atazanavir sulfat, nelfinavir mezilat i sakvinavir mezilat
10. Kombinacija prema patentnom zahtjevu 9, naznačena time što jedno ili više anti-HIV sredstava je 4'-etinil-2-fluoro-2'-deoksiadenozin.
11. Farmaceutska kompozicija koja sadrži kombinaciju prema bilo kojem od patentnih zahtjeva 1-10 i farmaceutski prihvatljiv nosač.
12. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10, za uporabu u inhibiciji HIV reverzne transkriptaze kod subjekta.
13. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10, za uporabu u profilaksi infekcije HIV-om ili profilaksi SIDA-e kod subjekta.
14. Kombinacija prema bilo kojem od patentnih zahtjeva 1-10, za uporabu u liječenju infekcije HIV-om, liječenju SIDA-e, ili odlaganju početka SIDA-e kod subjekta.
15. Kombinacija za uporabu prema bilo kojem od patentnih zahtjeva 12-14, naznačena time što subjekt je čovjek.
HRP20220502TT 2012-10-08 2013-10-07 Kombinacije koje sadrže derivate 5-fenoksi-3h-pirimidin-4-ona i njihova uporaba za profilaksu ili liječenje infekcije hiv-om HRP20220502T1 (hr)

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