HRP20201966T1 - Supstituirani triciklični spojevi kao inhibitori fgfr - Google Patents
Supstituirani triciklični spojevi kao inhibitori fgfr Download PDFInfo
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- HRP20201966T1 HRP20201966T1 HRP20201966TT HRP20201966T HRP20201966T1 HR P20201966 T1 HRP20201966 T1 HR P20201966T1 HR P20201966T T HRP20201966T T HR P20201966TT HR P20201966 T HRP20201966 T HR P20201966T HR P20201966 T1 HRP20201966 T1 HR P20201966T1
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- HR
- Croatia
- Prior art keywords
- pyrido
- dimethoxyphenyl
- tetrahydro
- methyl
- pyrrolo
- Prior art date
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- 150000001875 compounds Chemical class 0.000 title claims 20
- 239000003112 inhibitor Substances 0.000 title 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 40
- 125000005843 halogen group Chemical group 0.000 claims 36
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 34
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 33
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims 27
- 125000001424 substituent group Chemical group 0.000 claims 26
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 19
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 claims 18
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 18
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 18
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 17
- 125000000217 alkyl group Chemical group 0.000 claims 16
- 125000006568 (C4-C7) heterocycloalkyl group Chemical group 0.000 claims 15
- 101100310928 Caenorhabditis elegans sra-6 gene Proteins 0.000 claims 11
- 125000006272 (C3-C7) cycloalkyl group Chemical group 0.000 claims 10
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 8
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 7
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 claims 4
- 101100310926 Caenorhabditis elegans sra-3 gene Proteins 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 125000004767 (C1-C4) haloalkoxy group Chemical group 0.000 claims 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims 3
- 125000003282 alkyl amino group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 230000003176 fibrotic effect Effects 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- HHGBASPZCGVBLW-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(2-morpholin-4-ylethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C=1C2=C3N(CC)C(=O)N(C=4C(=C(OC)C=C(OC)C=4F)F)CC3=CN=C2NC=1CCN1CCOCC1 HHGBASPZCGVBLW-UHFFFAOYSA-N 0.000 claims 2
- HCDMJFOHIXMBOV-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C=1C2=C3N(CC)C(=O)N(C=4C(=C(OC)C=C(OC)C=4F)F)CC3=CN=C2NC=1CN1CCOCC1 HCDMJFOHIXMBOV-UHFFFAOYSA-N 0.000 claims 2
- XSNHNDWDZPRWCO-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)=O)=C1F XSNHNDWDZPRWCO-UHFFFAOYSA-N 0.000 claims 2
- SRZAANLPOLQXJY-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-[(4-ethylpiperazin-1-yl)methyl]-1-methyl-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C1CN(CC)CCN1CC1=CC2=C(N(C)C(=O)N(C3)C=4C(=C(OC)C=C(OC)C=4F)F)C3=CN=C2N1 SRZAANLPOLQXJY-UHFFFAOYSA-N 0.000 claims 2
- 101100310920 Caenorhabditis elegans sra-2 gene Proteins 0.000 claims 2
- 102100038417 Cytoplasmic FMR1-interacting protein 1 Human genes 0.000 claims 2
- 101710181791 Cytoplasmic FMR1-interacting protein 1 Proteins 0.000 claims 2
- 206010016654 Fibrosis Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 230000004761 fibrosis Effects 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 2
- KDDUJWRQAZKENT-ZDUSSCGKSA-N (3r)-1-[[3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-8-yl]methyl]pyrrolidine-3-carbonitrile Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CN5C[C@@H](CC5)C#N)NC4=NC=C3C2)=O)=C1F KDDUJWRQAZKENT-ZDUSSCGKSA-N 0.000 claims 1
- KDDUJWRQAZKENT-CYBMUJFWSA-N (3s)-1-[[3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-8-yl]methyl]pyrrolidine-3-carbonitrile Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CN5C[C@H](CC5)C#N)NC4=NC=C3C2)=O)=C1F KDDUJWRQAZKENT-CYBMUJFWSA-N 0.000 claims 1
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 1
- 125000006584 (C3-C10) heterocycloalkyl group Chemical group 0.000 claims 1
- MECCLZYVIQVWGC-UHFFFAOYSA-N 1-[2-[3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-8-yl]ethyl]azetidine-3-carbonitrile Chemical compound C=1C2=C3N(CC)C(=O)N(C=4C(=C(OC)C=C(OC)C=4F)F)CC3=CN=C2NC=1CCN1CC(C#N)C1 MECCLZYVIQVWGC-UHFFFAOYSA-N 0.000 claims 1
- WPLWQIYEJTYRPX-UHFFFAOYSA-N 1-[[3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-8-yl]methyl]azetidine-3-carbonitrile Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CN5CC(C5)C#N)NC4=NC=C3C2)=O)=C1F WPLWQIYEJTYRPX-UHFFFAOYSA-N 0.000 claims 1
- ACAONLVTDDPNGF-UHFFFAOYSA-N 1-[[3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-8-yl]methyl]piperidine-4-carbonitrile Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CN5CCC(CC5)C#N)NC4=NC=C3C2)=O)=C1F ACAONLVTDDPNGF-UHFFFAOYSA-N 0.000 claims 1
- DIKIPHVERHHBCG-UHFFFAOYSA-N 1-cyclobutyl-3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(2-morpholin-4-ylethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3CCC3)C3=C4C=C(CCN5CCOCC5)NC4=NC=C3C2)=O)=C1F DIKIPHVERHHBCG-UHFFFAOYSA-N 0.000 claims 1
- XJUQWQLHDWFCFT-UHFFFAOYSA-N 1-cyclobutyl-3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3CCC3)C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)=O)=C1F XJUQWQLHDWFCFT-UHFFFAOYSA-N 0.000 claims 1
- LQRWEVPWNOBUQE-UHFFFAOYSA-N 1-cyclopropyl-3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3CC3)C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)=O)=C1F LQRWEVPWNOBUQE-UHFFFAOYSA-N 0.000 claims 1
- DRVVQUZCPBPENC-UHFFFAOYSA-N 1-cyclopropyl-3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-[(4-ethylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C1CN(CC)CCN1CC1=CC2=C(N(C3CC3)C(=O)N(C3)C=4C(=C(OC)C=C(OC)C=4F)F)C3=CN=C2N1 DRVVQUZCPBPENC-UHFFFAOYSA-N 0.000 claims 1
- QUWWHRWTHJSCEI-UHFFFAOYSA-N 1-cyclopropyl-3-(2,6-difluoro-3,5-dimethoxyphenyl)-8-[(4-methylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3CC3)C3=C4C=C(CN5CCN(C)CC5)NC4=NC=C3C2)=O)=C1F QUWWHRWTHJSCEI-UHFFFAOYSA-N 0.000 claims 1
- ZBPIUMDBNIVOMG-UHFFFAOYSA-N 11-(2-chloro-3,5-dimethoxyphenyl)-13-methyl-4-(2-methylpyrazol-3-yl)-5,7,11,13-tetrazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraen-12-one Chemical compound COC1=CC(OC)=C(Cl)C(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C=2N(N=CC=2)C)=O)=C1 ZBPIUMDBNIVOMG-UHFFFAOYSA-N 0.000 claims 1
- BIKGROGTYNQBNV-KZTHJERWSA-N 13-[(E)-1-amino-3-methyliminoprop-1-en-2-yl]-11-(2,6-difluoro-3,5-dimethoxyphenyl)-4-(morpholin-4-ylmethyl)-5,7,11,13-tetrazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraen-12-one Chemical compound CN=C/C(=C\N)/N1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCOCC5 BIKGROGTYNQBNV-KZTHJERWSA-N 0.000 claims 1
- DAWIYELMDVVFDN-SSQDOHACSA-N 13-[(E)-1-amino-3-methyliminoprop-1-en-2-yl]-11-(2,6-difluoro-3,5-dimethoxyphenyl)-4-[(4-methylpiperazin-1-yl)methyl]-5,7,11,13-tetrazatricyclo[7.4.0.02,6]trideca-1,3,6,8-tetraen-12-one Chemical compound CN=C/C(=C\N)/N1C2=C3C=C(NC3=NC=C2CN(C1=O)C4=C(C(=CC(=C4F)OC)OC)F)CN5CCN(CC5)C DAWIYELMDVVFDN-SSQDOHACSA-N 0.000 claims 1
- AMFHRMYSKQSYBM-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2,3-difluorophenyl)-8-(2-morpholin-4-ylethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CCN5CCOCC5)NC4=NC=C3C2)C=2C(=C(F)C=CC=2)F)=O)=C1F AMFHRMYSKQSYBM-UHFFFAOYSA-N 0.000 claims 1
- OOCWOZVECYYOIJ-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2,3-difluorophenyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)C=2C(=C(F)C=CC=2)F)=O)=C1F OOCWOZVECYYOIJ-UHFFFAOYSA-N 0.000 claims 1
- NKJGLXZRAVLYHU-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2,3-difluorophenyl)-8-[(4-ethylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C1CN(CC)CCN1CC1=CC2=C(N(C(=O)N(C3)C=4C(=C(OC)C=C(OC)C=4F)F)C=4C(=C(F)C=CC=4)F)C3=CN=C2N1 NKJGLXZRAVLYHU-UHFFFAOYSA-N 0.000 claims 1
- GRGJFXIFXZZZKM-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2,3-difluorophenyl)-8-[(4-methylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCN(C)CC5)NC4=NC=C3C2)C=2C(=C(F)C=CC=2)F)=O)=C1F GRGJFXIFXZZZKM-UHFFFAOYSA-N 0.000 claims 1
- ZSEPMWJPKFKHRN-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2,3-difluorophenyl)-8-[2-(4-ethylpiperazin-1-yl)ethyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C1CN(CC)CCN1CCC1=CC2=C(N(C(=O)N(C3)C=4C(=C(OC)C=C(OC)C=4F)F)C=4C(=C(F)C=CC=4)F)C3=CN=C2N1 ZSEPMWJPKFKHRN-UHFFFAOYSA-N 0.000 claims 1
- OVMWGFGGFCVSPJ-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2,3-difluorophenyl)-8-[2-(4-methylpiperazin-1-yl)ethyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CCN5CCN(C)CC5)NC4=NC=C3C2)C=2C(=C(F)C=CC=2)F)=O)=C1F OVMWGFGGFCVSPJ-UHFFFAOYSA-N 0.000 claims 1
- GUQBAGOIOAKELE-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2-fluoroethyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(CCF)C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)=O)=C1F GUQBAGOIOAKELE-UHFFFAOYSA-N 0.000 claims 1
- QOYIKDLHUZDSKV-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2-fluoroethyl)-8-[(4-methylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(CCF)C3=C4C=C(CN5CCN(C)CC5)NC4=NC=C3C2)=O)=C1F QOYIKDLHUZDSKV-UHFFFAOYSA-N 0.000 claims 1
- ONSPEZYKYYWNNU-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2-fluorophenyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)C=2C(=CC=CC=2)F)=O)=C1F ONSPEZYKYYWNNU-UHFFFAOYSA-N 0.000 claims 1
- QYGSUOBGONKBPY-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2-hydroxyethyl)-8-(2-morpholin-4-ylethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(CCO)C3=C4C=C(CCN5CCOCC5)NC4=NC=C3C2)=O)=C1F QYGSUOBGONKBPY-UHFFFAOYSA-N 0.000 claims 1
- XAXUVBLETFGUPE-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(2-hydroxyethyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(CCO)C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)=O)=C1F XAXUVBLETFGUPE-UHFFFAOYSA-N 0.000 claims 1
- DYWAPJKBTUFIKX-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(3-fluorophenyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)C=2C=C(F)C=CC=2)=O)=C1F DYWAPJKBTUFIKX-UHFFFAOYSA-N 0.000 claims 1
- RVKHZHIKDOUREE-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(3-fluorophenyl)-8-[(4-methylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCN(C)CC5)NC4=NC=C3C2)C=2C=C(F)C=CC=2)=O)=C1F RVKHZHIKDOUREE-UHFFFAOYSA-N 0.000 claims 1
- SJSQASZJOOONGL-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(4-fluorophenyl)-8-(2-morpholin-4-ylethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CCN5CCOCC5)NC4=NC=C3C2)C=2C=CC(F)=CC=2)=O)=C1F SJSQASZJOOONGL-UHFFFAOYSA-N 0.000 claims 1
- GJYRYVMUQHDRKI-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(4-fluorophenyl)-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCOCC5)NC4=NC=C3C2)C=2C=CC(F)=CC=2)=O)=C1F GJYRYVMUQHDRKI-UHFFFAOYSA-N 0.000 claims 1
- XDLFDPINUQJMSP-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(4-fluorophenyl)-8-[(4-methylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CN5CCN(C)CC5)NC4=NC=C3C2)C=2C=CC(F)=CC=2)=O)=C1F XDLFDPINUQJMSP-UHFFFAOYSA-N 0.000 claims 1
- LQOBRJXLLSUOKJ-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-(4-fluorophenyl)-8-[2-(4-methylpiperazin-1-yl)ethyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C3=C4C=C(CCN5CCN(C)CC5)NC4=NC=C3C2)C=2C=CC(F)=CC=2)=O)=C1F LQOBRJXLLSUOKJ-UHFFFAOYSA-N 0.000 claims 1
- YKEMSBPURCMYKG-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-[(2-methoxypyridin-4-yl)methyl]-8-(morpholin-4-ylmethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C1=NC(OC)=CC(CN2C3=C4C=C(CN5CCOCC5)NC4=NC=C3CN(C2=O)C=2C(=C(OC)C=C(OC)C=2F)F)=C1 YKEMSBPURCMYKG-UHFFFAOYSA-N 0.000 claims 1
- FHVNZZSAUYFVRA-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-(pyridin-3-yloxymethyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C=1C2=C3N(CC)C(=O)N(C=4C(=C(OC)C=C(OC)C=4F)F)CC3=CN=C2NC=1COC1=CC=CN=C1 FHVNZZSAUYFVRA-UHFFFAOYSA-N 0.000 claims 1
- CGXOSAJJYGWHOC-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-[(2-oxopyridin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C=1C2=C3N(CC)C(=O)N(C=4C(=C(OC)C=C(OC)C=4F)F)CC3=CN=C2NC=1CN1C=CC=CC1=O CGXOSAJJYGWHOC-UHFFFAOYSA-N 0.000 claims 1
- HJELNEFMOSOPSO-UHFFFAOYSA-N 3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-ethyl-8-[(4-ethylpiperazin-1-yl)methyl]-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound C1CN(CC)CCN1CC1=CC2=C(N(CC)C(=O)N(C3)C=4C(=C(OC)C=C(OC)C=4F)F)C3=CN=C2N1 HJELNEFMOSOPSO-UHFFFAOYSA-N 0.000 claims 1
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- MOKRHZBXMHAQDR-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-1-methyl-8-(1-methylpiperidin-4-yl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=CC(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C2CCN(C)CC2)=O)=C1 MOKRHZBXMHAQDR-UHFFFAOYSA-N 0.000 claims 1
- MWPGCNXAICIHQE-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-1-methyl-8-(1-methylpyrazol-4-yl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=CC(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C2=CN(C)N=C2)=O)=C1 MWPGCNXAICIHQE-UHFFFAOYSA-N 0.000 claims 1
- KVWDJGIRKNYBJM-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-1-methyl-8-(4-methylpiperazine-1-carbonyl)-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=CC(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C(=O)N2CCN(C)CC2)=O)=C1 KVWDJGIRKNYBJM-UHFFFAOYSA-N 0.000 claims 1
- WNJWXMOGYZAYDF-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-8-(3-hydroxyazetidine-1-carbonyl)-1-methyl-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=CC(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C(=O)N2CC(O)C2)=O)=C1 WNJWXMOGYZAYDF-UHFFFAOYSA-N 0.000 claims 1
- PLAKMBVWBCYBSZ-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-8-(3-hydroxypyrrolidine-1-carbonyl)-1-methyl-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=CC(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C(=O)N2CC(O)CC2)=O)=C1 PLAKMBVWBCYBSZ-UHFFFAOYSA-N 0.000 claims 1
- PMVUEUHJHPDSDQ-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-n,1-dimethyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidine-8-carboxamide Chemical compound C1C2=CN=C3NC(C(=O)NC)=CC3=C2N(C)C(=O)N1C1=CC(OC)=CC(OC)=C1 PMVUEUHJHPDSDQ-UHFFFAOYSA-N 0.000 claims 1
- MOZDYHQDSMTOKE-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-n,n,1-trimethyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidine-8-carboxamide Chemical compound COC1=CC(OC)=CC(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C(=O)N(C)C)=O)=C1 MOZDYHQDSMTOKE-UHFFFAOYSA-N 0.000 claims 1
- ACHCZMUUOAJFTJ-UHFFFAOYSA-N 3-[4-[[3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-8-yl]methyl]piperazin-1-yl]propanenitrile Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CN5CCN(CCC#N)CC5)NC4=NC=C3C2)=O)=C1F ACHCZMUUOAJFTJ-UHFFFAOYSA-N 0.000 claims 1
- WSUFMQVSUICTRP-UHFFFAOYSA-N 8-[3-(4-cyclopropylpiperazin-1-yl)propyl]-3-(2,6-difluoro-3,5-dimethoxyphenyl)-1-methyl-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidin-2-one Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(CCCN5CCN(CC5)C5CC5)NC4=NC=C3C2)=O)=C1F WSUFMQVSUICTRP-UHFFFAOYSA-N 0.000 claims 1
- HMJDFBIIQCJVKS-UHFFFAOYSA-N CCN1CCN(CC2=CC3=C(N2)N=CC2=C3N(CC3=CC(F)=CC=C3)C(=O)N(C2)C2=C(F)C(OC)=CC(OC)=C2F)CC1 Chemical compound CCN1CCN(CC2=CC3=C(N2)N=CC2=C3N(CC3=CC(F)=CC=C3)C(=O)N(C2)C2=C(F)C(OC)=CC(OC)=C2F)CC1 HMJDFBIIQCJVKS-UHFFFAOYSA-N 0.000 claims 1
- 101100150279 Caenorhabditis elegans srb-6 gene Proteins 0.000 claims 1
- 206010018364 Glomerulonephritis Diseases 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 208000019425 cirrhosis of liver Diseases 0.000 claims 1
- 125000000753 cycloalkyl group Chemical group 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- GCOPCGYUSUOBLO-UHFFFAOYSA-N n-cyclopropyl-3-(2-fluoro-3,5-dimethoxyphenyl)-1-methyl-2-oxo-4,7-dihydropyrrolo[4,5]pyrido[1,2-d]pyrimidine-8-carboxamide Chemical compound COC1=CC(OC)=C(F)C(N2C(N(C)C3=C4C=C(NC4=NC=C3C2)C(=O)NC2CC2)=O)=C1 GCOPCGYUSUOBLO-UHFFFAOYSA-N 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- 230000009885 systemic effect Effects 0.000 claims 1
- 230000029663 wound healing Effects 0.000 claims 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/14—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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/535—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P11/00—Drugs for disorders of the respiratory system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
- C07D471/20—Spiro-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/22—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed systems contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D495/14—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
Claims (18)
1. Spoj za upotrebu u liječenju fibrozne bolesti, spoj ima formulu II:
[image]
ili njegova farmaceutski prihvatljiva sol, gdje:
W je NR9;
X je CR15 ili N;
R1 je H, NRARB, halo, i C1-3 alkil;
R2 i R3 je svaki nezavisno izabran između H, CN, C(O)NRcRd, i C1-7 alkil, gdje spomenuti C1-7 alkil je opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih između halo, ORa, CN, NRcRd, i C(O)NRcRd;
ili R2 i R3 zajedno s ugljikovim atomom za koji su vezani formiraju 3-7 člani cikloalkil prsten ili 4-7 člani heterocikloalkil prsten, svaki opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih između halo, C1-6 alkil, C1-6 haloalkil, CN, ORa, SRa, C(O)Rb, C(O)NRcRd, C(O)ORa, OC(O)Rb, OC(O)NRcRd, NRcRd, NRcC(O)Rb, i NRcC(O)ORa;
R4, R5, R6, R7, i R8 je svaki nezavisno izabran između H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, CN, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, C(=NRe1)Rb1, C(=NRe1)NRc1Rd1, NRc1C(=NRe1)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1; gdje spomenuti C1-6 alkil, C2-6 alkenil, C2- 6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, i 4-10 člani heterocikloalkil je svaki opcionalno supstituirani sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih između halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, C(=NRe1)NRc1Rd1, NRc1C(=NRe1)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)ORa1, NRc1C(O)NRc1Rd1, NRc1S(O)Rb1, NRc1S(O)2Rb1, NRc1S(O)2NRc1Rd1, S(O)Rb1, S(O)NRc1Rd1, S(O)2Rb1, i S(O)2NRc1Rd1;
R9 je H, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, ili (4-10 člani heterocikloalkil)-C1-4 alkil, gde spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, i (4-10 člani heterocikloalkil)-C1-4 alkil su svaki opcionalno supstituirani sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih od R9a;
svaki R9a je nezavisno izabran od Cy1, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2 , Rc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, i S(O)2NRc2Rd2, gdje spomenuti C1-6 alkil, C2-6 alkenil, i C2-6 alkinil su svaki opcionalno supstituirani sa 1, 2, ili 3 supstituenta nezavisno izabranih od Cy1, halo, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, C(=NRe2)NRc2Rd2, NRc2C(=NRe2)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)ORa2, NRc2C(O)NRc2Rd2, NRc2S(O)Rb2, NRc2S(O)2Rb2, NRc2S(O)2NRc2Rd2, S(O)Rb2, S(O)NRc2Rd2, S(O)2Rb2, i S(O)2NRc2Rd2;
R10 je izabran između halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3; gdje spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, i 4-10 člani heterocikloalkil su svaki opcionalno supstituirani sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih od R10a;
R15 je svaki nezavisno izabran između H, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, C(=NRe3)Rb3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, id S(O)2NRc3Rd3; gdje spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, i 4-10 člani heterocikloalkil je svaki opcionalno supstituiran sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih između R10a;
svaki R10a je nezavisno izabran između Cy2, halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3, gdje spomenuti C1-6 alkil, C2-6 alkenil, i C2-6 alkinil je svaki opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih između Cy2, halo, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, C(=NRe3)NRc3Rd3, NRc3C(=NRe3)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)ORa3, NRc3C(O)NRc3Rd3, NRc3S(O)Rb3, NRc3S(O)2Rb3, NRc3S(O)2NRc3Rd3, S(O)Rb3, S(O)NRc3Rd3, S(O)2Rb3, i S(O)2NRc3Rd3;
RA i RB je svaki nezavisno izabran između H, C1-4 alkil, C1-4 haloalkil, C2-4 alkenil, C2-4 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, ili (4-10 člani heterocikloalkil)-C1-4 alkil, gdje spomenuti C1-4 alkil, C2-4 alkenil, C2-4 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, i (4-10 člani heterocikloalkil)-C1-4 alkil je opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih između OH, CN, amino, halo, C1-4 alkil, C1-4 alkoksi, C1-4 alkiltio, C1-4 alkilamino, di(C1-4 alkil)amino, C1-4 haloalkil, i C1-4 haloalkoksi;
svaki Cy1 ili Cy2 je nezavisno izabran između C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, od kojih je svaki opcionalno supstituiran sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih između halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 3-10 člani heterocikloalkil, CN, NO2, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, C(=NRe5)Rb5, C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5S(O)Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, i S(O)2NRc5Rd5; gdje spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, i 4-10 člani heterocikloalkil je svaki opcionalno supstituiran sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih između halo, C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C1-6 haloalkil, CN, NO2, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, C(=NRe5)NRc5Rd5, NRc5C(=NRe5)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)ORa5, NRc5C(O)NRc5Rd5, NRc5S(O)Rb5, NRc5S(O)2Rb5, NRc5S(O)2NRc5Rd5, S(O)Rb5, S(O)NRc5Rd5, S(O)2Rb5, i S(O)2NRc5Rd5;
svaki Ra, Rb, Rc, Rd, Ra1, Rb1, Rc1, Rd1, Ra2, Rb2, Rc2, Rd2, Ra3, Rb3, Rc3, Rd3, Ra5, Rb5, Rc5, i Rd5 je nezavisno izabran između H, C1-6 alkil, C1-4 haloalkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)- C1-4 alkil, ili (4-10 člani heterocikloalkil)-C1-4 alkil, gdje spomenuti C1-6 alkil, C2-6 alkenil, C2-6 alkinil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, i (4-10 člani heterocikloalkil)-C1-4 alkil je opcionalno supstituiran sa 1, 2, 3, 4, ili 5 supstituenata nezavisno izabranih između C1-4 alkil, C1-4 haloalkil, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6;
ili bilo koji Rc i Rd zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu opcionalno supstituiranu sa 1, 2, ili 3 supstituenata nezavisno izabranih između C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, 5-6 člani heteroaril, C1-6 haloalkil, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6, gdje spomenuti C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, i 5-6 člani heteroaril su opcionalno supstituirani sa 1, 2, ili 3 supstituenata nezavisno izabranih između halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6;
ili bilo koji od Rc1 i Rd1 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu opcionalno supstituiranu sa 1, 2, ili 3 supstituenata nezavisno izabranih između C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, 5-6 člani heteroaril, C1-6 haloalkil, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6, gdje spomenuti C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, i 5-6 člani heteroaril su opcionalno supstituirani sa 1, 2, ili 3 supstituenata nezavisno izabranih između halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6; ili ili bilo koji Rc2 i Rd2 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu opcionalno supstituiranu sa 1, 2, ili 3 supstituenata nezavisno izabranih od C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, i 5-6 člani heteroaril, C1-6 haloalkil, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O) 2NRc6Rd6, i S(O)2NRc6Rd6, gdje spomenuti C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, i 5-6 člani heteroaril su opcionalno supstituirani sa 1, 2, ili 3 supstituenata nezavisno izabranih od halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6;
bilo koji od Rc3 i Rd3 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu opcionalno supstituiranu sa 1, 2, ili 3 supstituenata nezavisno izabranih između C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, 5-6 člani heteroaril, C1-6 haloalkil, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6, gdje spomenuti C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, i 5-6 člani heteroaril su opcionalno supstituirani sa 1, 2, ili 3 supstituenata nezavisno izabranih između halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6;
ili bilo koji od Rc5 i Rd5 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu opcionalno susptituisanu sa 1, 2, ili 3 supstituenata nezavisno izabranih između C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, 5-6 člani heteroaril, C1-6 haloalkil, halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6, gdje spomenuti C1-6 alkil, C3-7 cikloalkil, 4-7 člani heterocikloalkil, C6-10 aril, i 5-6 člani heteroaril su opcionalno supstituirani sa 1, 2, ili 3 supstituenata nezavisno izabranih između halo, CN, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(=NRe6)NRc6Rd6, NRc6C(=NRe6)NRc6Rd6, S(O)Rb6, S(O)NRc6Rd6, S(O)2Rb6, NRc6S(O)2Rb6, NRc6S(O)2NRc6Rd6, i S(O)2NRc6Rd6; svaki Re1, Re2,Re3, i Re5 je nezavisno izabran između H, C1-4 alkil, CN, ORa6, SRb6, S(O)2Rb6, C(O)Rb6, S(O)2NRc6Rd6, i C(O)NRc6Rd6;
svaki Ra6, Rb6, Rc6, i Rd6 je nezavisno izabran između H, C1-4 alkil, C1-4 haloalkil, C2-4 alkenil, i C2-4 alkinil, gdje spomenuti C1-4 alkil, C2-4 alkenil, i C2-4 alkinil, je opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih između OH, CN, amino, halo, C1-4 alkil, C1-4 alkoksi, C1-4 alkiltio, C1-4 alkilamino, di(C1-4 alkil)amino, C1-4 haloalkil, i C1-4 haloalkoksi;
ili bilo koji od Rc6 i Rd6 zajedno sa N atomom za koji su vezani formiraju 4-, 5-, 6-, ili 7-članu heterocikloalkil grupu opcionalno supstituiranu sa 1, 2, ili 3 supstituenata nezavisno izabranih između OH, CN, amino, halo, C1-6 alkil, C1-4 alkoksi, C1-4 alkilthio, C1-4 alkilamino, di(C1-4 alkil)amino, C1-4 haloalkil, i C1-4 haloalkoksi; i svaki Re6 je nezavisno izabran između H, C1-4 alkil, i CN.
2. Spoj za upotrebu prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, gdje:-
a) R9 je H, C1-6 alkil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, ili (4-10 člani heterocikloalkil)-C1-4 alkil, gdje spomenuti C1-6 alkil, C6-10 aril, C3-10 cikloalkil, 5-10 člani heteroaril, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, C3-10 cikloalkil-C1-4 alkil, (5-10 člani heteroaril)-C1-4 alkil, i (4-10 člani heterocikloalkil)-C1-4 alkil su svaki opcionalno supstituirani sa R9a; ili
b) R9 je H, C1-6 alkil, C3-10 cikloalkil, 4-10 člani heterocikloalkil, C6-10 aril-C1-4 alkil, ili C3-10 cikloalkil-C1- 4 alkil; ili
c) R9 je C1-6 alkil: ili
d) R9 je metil.
3. Spoj za upotrebu prema zahtjevu 1 ili 2, ili njegova farmaceutski prihvatljiva sol, gdje svaki od R1, R2, i R3 je H.
4. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 3, ili njegova farmaceutski prihvatljiva sol, gdje:-
a) R4, R5, R6, R7, i R8je svaki nezavisno izabran između H, halo,C1-6 alkil, C1-6 haloalkil, CN, i ORa1; ili
b) R4, R5, R6, R7, i R8 je svaki nezavisno izabran između H, halo i metoksi; ili
c) R5 i R7 su oba metoksi i R4, R6, i R8 je svaki nezavisno izabran između H i halo; ili
d) R4 je halo, R5 je metoksi, R6 je H, R7 je metoksi, i R8 je halo.
5. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 4, ili njegova farmaceutska sol, gdje:-
a) X je CR15; ili
b) X je CH.
6. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 5, ili njegova farmaceutski prihvatljiva sol, gdje R15 je H ili 5-10 člani heteroaril opcionalno supstituiran sa C1-6 alkil.
7. Spoj za upotrebu prema bilo kojem od zahtjeva 1 do 6, ili njegova farmaceutski prihvatljiva sol gdje R10 je C1-6 alkil opcionalno supstituiran sa 4-7 članim heterocikloalkilom gdje spomenuti 4-7 člani heterocikloalkil je izabran između morfolinil, piperazinil, piperidinil, pirolidinil, tetrahidrofuranil, i azetidinil, i gdje spomenuti 4-7 člani heterocikloalkil je opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih od halo, C1-6 alkil, C1-6 haloalkil, CN, ORa5, C(0)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, NRc5Rd5, i NRc5C(O)Rb5.
8. Spoj za upotrebu prema zahtjevu 1, ili njegova farmaceutski prihvatljiva sol, koji ima formulu IIa:
[image]
9. Spoj za upotrebu prema zahtjevu 8, ili njegova prihvatljiva sol, gdje R4 je halo, R5 je metoksi, R6 je H, R7 je metoksi, i R8 je halo.
10. Spoj za upotrebu prema zahtjevu 8 ili 9, ili njegova farmaceutski prihvatljiva sol, gdje R9 je C1- 6alkil.
11. Spoj za upotrebu prema bilo kojem od zahtjeva 8 do 10, ili njegova farmaceutski prihvatljiva sol, gdje R10 je C1-6 alkil opcionalno supstituiran sa 4-7 članim heterocikloalkilom gdje spomenuti 4-7 člani heterocikloalkil je izabran između morfolinil, piperazinil, piperidinil, pirolidinil, tetrahidrofuranil, i azetidnil, i gdje spomenuti 4-7 člani heterocikloalkil je opcionalno supstituiran sa 1, 2, ili 3 supstituenata nezavisno izabranih od halo, C1-6 alkil, C1-6 haloalkil, CN, ORa5, C(0)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, NRc5Rd5, i NRc5C(O)Rb5.
12. Spoj za upotrebu prema zahtjevu 1, izabran između
(a) 3-(3,5-Dimetoksifenil)-1-metil-8-(1-metil-1H-pirazol-4-il)-1,3,4,7-tetrahidro-2H-pirolo[3',2':5,6] pirido[4,3-d]pirimidin-2-ona;
3-(3,5-Dimetoksifenil)-N,1-dimetil-2-okso-2,3,4,7-tetrahidro-1H-pirolo[3',2':5,6]pirido[4,3- d]pirimidin-8-karboksamida;
3-(2-Kloro-3,5-dimetoksifenil)-1-metil-8-(1-metil-1H-pirazol-4-il)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2-Kloro-3,5-dimetoksifenil)-8-[1-(2-hidroksietil)-1H-pirazol-4-il]-1-metil-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2-Kloro-3,5-dimetoksifenil)-1-metil-8-(1-metil-1H-pirazol-5-il)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2-Kloro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-karbonitrila;
3-(3,5-Dimetoksifenil)-1-metil-8-(1-metil-1,2,3,6-tetrahidropiridin-4-il)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(3,5-Dimetoksifenil)-1-metil-8-(1-metilpiperidin-4-il)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(3,5-Dimetoksifenil)-N,N,1-trimetil-2-okso-2,3,4,7-tetrahidro-1H-pirolo[3',2':5,6]pirido[4,3- d]pirimidin-8-karboksamida;
3-(3,5-Dimetoksifenil)-8-[(3-hidroksiazetidin-1-il)karbonil]-1-metil-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(3,5-Dimetoksifenil)-8-[(3-hidroksipirolidin-1-il)karbonil]-1-metil-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(3,5-Dimetoksifenil)-1-metil-8-[(4-metilpiperazin-1-il)karbonil]-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2-Kloro-3,5-dimetoksifenil)-N,1-dimetil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-karboksamida;
3-(2-kloro-3,5-dimetoksifenil)-N,N,1-trimetil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-karboksamida;
3-(2-Kloro-3,5-dimetoksifenil)-8-[(3-hidroksiazetidin-1-il)karbonil]-1-metil-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2-Kloro-3,5-dimetoksifenil)-1-metil-8-[(4-metilpiperazin-1-il)karbonil]-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
N-Ciklopropil-3-(2-fluoro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-karboksamida;
3-(2-Fluoro-3,5-dimetoksifenil)-8-[(3-hidroksipiperidin-1-il)karbonil]-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2-Fluoro-3,5-dimetoksifenil)-N,N,1-trimetil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-karboksamida;
3-(2,6-Difluoro-3,5-dimetoksifenil)-N,N,1-trimetil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-karboksamida;
ili farmaceutski prihvatljiva sol bilo kojega od gore spomenutih ; ili
b) izabrano od:
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-(tetrahidro-2H-piran-4-il)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-[(4-metilpiperazin-1-il)karbonil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-(morfolin-4-ilkarbonil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4,4-difluoropiperidin-1-il)karbonil]-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
ili farmaceutski prihvatljiva sol bilo kojega od gore spomenutih ; ili
c) izabrano od:
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-etilpiperazin-1-il)metil]-1-metil-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[2-(4-etilpiperazin-1-il)etil]-1-metil-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[3-(4-etilpiperazin-1-il)propil]-1-metil-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(1-etilpiperidin-4-il)metil]-1-metil-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-hidroksipiperidin-1-il)metil]-1-metil-1,3,4,7- tetrahidro-2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4,4-difluoropiperidin-1-il)metil]-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(3,3-difluoropiperidin-1-il)metil]-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-(2-morfolin-4-iletil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
8-[3-(4-ciklopropilpiperazin-1-il)propil]-3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-etilpiperazin-1-il)karbonil]-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-{[(3R,5S)-3,5-dimetilpiperazin-1-il]karbonil}-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
Ili farmaceutski prihvatljiva sol bilo kog od gore spomenutih ; ili
d) izabrano od:
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-[(4-etilpiperazin-1-il)metil]-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-{[4-(2-hidroksietil)piperazin-1-il]metil}-1-metil-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(4-{[3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-il]metil}piperazin-1-il)propannitrila;
1-{[3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-il]metil}piperidin-4-karbonitrila;
(3S)-1-{[3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-il]metil}pirolidin-3-karbonitrila;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-{[(1-metilpiperidin-4-il)amino]metil}-1,3,4,7- tetrahidro-2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-{[(3S)-tetrahidrofuran-3-ilamino]metil}-1,3,4,7- tetrahidro-2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-{[(3R)-tetrahidrofuran-3-ilamino]metil}-1,3,4,7- tetrahidro-2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-(1H-imidazol-1-ilmetil)-1-metil-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-(1H-pirazol-1-ilmetil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-[(1-metil-1H-pirazol-4-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[2-(3-fluoroazetidin-1-il)etil]-1-metil-1,3,4,7-tetrahidro- 2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[2-(3-metoksiazetidin-1-il)etil]-1-metil-1,3,4,7- tetrahidro-2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2-hidroksietil)-8-(2-morfolin-4-iletil)-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2-fluorofenil)-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-etilpiperazin-1-il)metil]-1-(2-fluorofenil)-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-ciklobutil-3-(2,6-difluoro-3,5-dimetoksifenil)-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-ciklobutil-3-(2,6-difluoro-3,5-dimetoksifenil)-8-(2-morfolin-4-iletil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-(morfolin-4-ilmetil)-1-propil-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-(2-morfolin-4-iletil)-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-ciklopropil-3-(2,6-difluoro-3,5-dimetoksifenil)-8-(morfolin-4-ilmetil)-1,3,4, 7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-ciklopropil-3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-ciklopropil-3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-etilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(4-fluorofenil)-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro- 2Hpirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(4-fluorofenil)-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(4-fluorofenil)-8-[(4-etilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2,3-difluorofenil)-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2,3-difluorofenil)-8-[(4-etilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-(morfolin-4-ilmetil)-1-piridin-4-il-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-metilpiperazin-1-il)metil]-1-piridin-4-il-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-[(2-metoksipiridin-4-il)metil]-8-(morfolin-4-ilmetil)-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(1-metil-1H-pirazol-4-il)-8-(morfolin-4-ilmetil)-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-metilpiperazin-1-il)metil]-1-(1-metil-1H-pirazol-4-il)-1,3,4,7 tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-etilpiperazin-1-il)metil]-1-(1-metil-1H-pirazol-4-il)-1,3,4,7 tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-{[3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H-
pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-il]metil}azetidin-3-karbonitrila;
(3R)-1-{[3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-2-okso-2,3,4,7-tetrahidro-1H-
pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-il]metil}pirolidin-3-karbonitrila;
3-(2,6-difluoro-3,5-dimetoksifenil)-8-[2-(3-fluoroazetidin-1-il)etil]-1-(2-hidroksietil)-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2,3-difluorofenil)-8-(morfolin-4-ilmetil)-1,3,4,7- tetrahidro2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(3-fluorofenil)-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(3-fluorofenil)-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(3-fluorofenil)-8-[(4-etilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-[(2-oksopiridin-1(2H)-il)metil]-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-[(piridin-3-iloksi)metil]-1,3,4,7-tetrahidro-2H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2-hidroksietil)-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2,3-difluorofenil)-8-(2-morfolin-4-iletil)-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2,3-difluorofenil)-8-[2-(4-metilpiperazin-1-il)etil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2,3-difluorofenil)-8-[2-(4-etilpiperazin-1-il)etil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(4-fluorofenil)-8-(2-morfolin-4-iletil)-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(4-fluorofenil)-8-[2-(4-metilpiperazin-1-il)etil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
1-{2-[3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-2-okso-2,3,4,7-tetrahidro-1H- pirolo[3',2':5,6]pirido[4,3-d]pirimidin-8-il]etil}azetidin-3-karbonitrila;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-[2-(3-fluoroazetidin-1-il)etil]-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2-fluoroetil)-8-(morfolin-4-ilmetil)-1,3,4,7-tetrahidro- 2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
i 3-(2,6-difluoro-3,5-dimetoksifenil)-1-(2-fluoroetil)-8-[(4-metilpiperazin-1-il)metil]-1,3,4,7- tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-ona;
ili farmaceutski prihvatljiva sol bilo kojega od gore spomenutih.
13. Spoj za upotrebu prema zahtjevu 1 koje je 3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-(morfolin-4- ilmetil)-1,3,4,7-tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-on, ili njegova farmaceutski prihvatljiva sol.
14. Spoj za upotrebu prema zahtjevu 1 koje je 3-(2,6-difluoro-3,5-dimetoksifenil)-8-[(4-etilpiperazin- 1-il)metil]-1-metil-1,3,4,7-tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-on, ili njegova farmaceutski prihvatljiva sol.
15. Spoj za upotrebu prema zahtjevu 1 koje je 3-(2,6-difluoro-3,5-dimetoksifenil)-1-metil-8-(morfolin- 4-ilmetil)-1,3,4,7-tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-on, ili njegova farmaceutski prihvatljiva sol.
16. Spoj za upotrebu prema zahtjevu 1 koje je 3-(2,6-difluoro-3,5-dimetoksifenil)-1-etil-8-(2-morfolin- 4-iletil)-1,3,4,7-tetrahidro-2H-pirolo[3',2':5,6]pirido[4,3-d]pirimidin-2-on, ili njegova farmaceutski prihvatljiva sol.
17. Spoj za upotrebu prema bilo kojem od zahtjeva 1-16, gdje je simptom bolesti ili poremećaj spomenute fibrozne bolesti u vezi sa fibrozom.
18. Spoj za upotrebu prema bilo kojem od zahtjeva 1-16, gdje spomenuta fibrotička bolest je izabrana između ciroze jetre, glomerulonefritisa, plućne fibroze, sistemske fibroze, reumatoidnog artritisa i zarastanja rana.
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