ZA200504440B - Pyrrolopyrimidine derivatives - Google Patents
Pyrrolopyrimidine derivatives Download PDFInfo
- Publication number
- ZA200504440B ZA200504440B ZA200504440A ZA200504440A ZA200504440B ZA 200504440 B ZA200504440 B ZA 200504440B ZA 200504440 A ZA200504440 A ZA 200504440A ZA 200504440 A ZA200504440 A ZA 200504440A ZA 200504440 B ZA200504440 B ZA 200504440B
- Authority
- ZA
- South Africa
- Prior art keywords
- phenyl
- isopropyl
- carbonyl
- amino
- pyrrolo
- Prior art date
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- 150000004944 pyrrolopyrimidines Chemical class 0.000 title description 5
- 125000000217 alkyl group Chemical group 0.000 claims description 121
- 150000001875 compounds Chemical class 0.000 claims description 78
- 125000003118 aryl group Chemical group 0.000 claims description 55
- 125000005843 halogen group Chemical group 0.000 claims description 51
- 125000000623 heterocyclic group Chemical group 0.000 claims description 45
- 239000004202 carbamide Substances 0.000 claims description 37
- 229910052799 carbon Inorganic materials 0.000 claims description 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 29
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 28
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 28
- 125000001072 heteroaryl group Chemical group 0.000 claims description 27
- 125000001424 substituent group Chemical group 0.000 claims description 19
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 16
- 125000003545 alkoxy group Chemical group 0.000 claims description 13
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 125000002252 acyl group Chemical group 0.000 claims description 11
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims description 11
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims description 9
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims description 9
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 239000003112 inhibitor Substances 0.000 claims description 7
- -1 dimethyl-phenyl Chemical group 0.000 claims description 6
- 241000124008 Mammalia Species 0.000 claims description 5
- 230000002159 abnormal effect Effects 0.000 claims description 5
- 239000003102 growth factor Substances 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 239000000651 prodrug Substances 0.000 claims description 5
- 229940002612 prodrug Drugs 0.000 claims description 5
- 150000003839 salts Chemical class 0.000 claims description 5
- 230000003463 hyperproliferative effect Effects 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 125000003342 alkenyl group Chemical group 0.000 claims description 3
- 125000000304 alkynyl group Chemical group 0.000 claims description 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 3
- 150000001602 bicycloalkyls Chemical group 0.000 claims description 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims description 3
- 238000004519 manufacturing process Methods 0.000 claims description 3
- 229910052760 oxygen Inorganic materials 0.000 claims description 3
- 239000001301 oxygen Substances 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 230000008569 process Effects 0.000 claims description 3
- 102000004190 Enzymes Human genes 0.000 claims description 2
- 108090000790 Enzymes Proteins 0.000 claims description 2
- 239000002253 acid Substances 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 230000004044 response Effects 0.000 claims description 2
- 230000010261 cell growth Effects 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- ANHIVJBWMLUKHH-UHFFFAOYSA-N (3-aminophenyl)-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidin-5-yl)methanone Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C1=CC=CC(N)=C1 ANHIVJBWMLUKHH-UHFFFAOYSA-N 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- FZAKKMJTXLAJEQ-UHFFFAOYSA-N (2,3-dimethylphenyl)urea Chemical compound CC1=CC=CC(NC(N)=O)=C1C FZAKKMJTXLAJEQ-UHFFFAOYSA-N 0.000 claims 1
- FTJBMYITMFAUCP-UHFFFAOYSA-N (3,5-dichlorophenyl)urea Chemical compound NC(=O)NC1=CC(Cl)=CC(Cl)=C1 FTJBMYITMFAUCP-UHFFFAOYSA-N 0.000 claims 1
- PPCUBWWPGYHEJE-UHFFFAOYSA-N (3-chlorophenyl)urea Chemical compound NC(=O)NC1=CC=CC(Cl)=C1 PPCUBWWPGYHEJE-UHFFFAOYSA-N 0.000 claims 1
- CDHGVGXTWWQIHH-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)-2-methylphenyl]-3-(2-chlorophenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1C)=CC=CC=1NC(=O)NC1=CC=CC=C1Cl CDHGVGXTWWQIHH-UHFFFAOYSA-N 0.000 claims 1
- UKJZUGUHHIRELO-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)-2-methylphenyl]-3-(3,5-difluorophenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1C)=CC=CC=1NC(=O)NC1=CC(F)=CC(F)=C1 UKJZUGUHHIRELO-UHFFFAOYSA-N 0.000 claims 1
- DYIXYQYNXNHZCI-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(2,6-difluorophenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1)=CC=CC=1NC(=O)NC1=C(F)C=CC=C1F DYIXYQYNXNHZCI-UHFFFAOYSA-N 0.000 claims 1
- NBBUFLANDGOPCL-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(2-chloro-5-methylphenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1)=CC=CC=1NC(=O)NC1=CC(C)=CC=C1Cl NBBUFLANDGOPCL-UHFFFAOYSA-N 0.000 claims 1
- RQMZRLYFCRPRFD-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(2-methoxyphenyl)urea Chemical compound COC1=CC=CC=C1NC(=O)NC1=CC=CC(C(=O)C=2C3=C(N)N=CN=C3N(C(C)C)C=2)=C1 RQMZRLYFCRPRFD-UHFFFAOYSA-N 0.000 claims 1
- JYCUGYRJLXPLAT-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(3,4-difluorophenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1)=CC=CC=1NC(=O)NC1=CC=C(F)C(F)=C1 JYCUGYRJLXPLAT-UHFFFAOYSA-N 0.000 claims 1
- LVKYWGHBTMCTGO-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(3-fluorophenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1)=CC=CC=1NC(=O)NC1=CC=CC(F)=C1 LVKYWGHBTMCTGO-UHFFFAOYSA-N 0.000 claims 1
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- ADPWOQHEGMITGH-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(4-chloro-2-methylphenyl)urea Chemical compound C12=C(N)N=CN=C2N(C(C)C)C=C1C(=O)C(C=1)=CC=CC=1NC(=O)NC1=CC=C(Cl)C=C1C ADPWOQHEGMITGH-UHFFFAOYSA-N 0.000 claims 1
- QRWBSACLFSVZEF-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(4-ethoxyphenyl)urea Chemical compound C1=CC(OCC)=CC=C1NC(=O)NC1=CC=CC(C(=O)C=2C3=C(N)N=CN=C3N(C(C)C)C=2)=C1 QRWBSACLFSVZEF-UHFFFAOYSA-N 0.000 claims 1
- ZZQWAEVPQHAGBK-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(4-ethylphenyl)urea Chemical compound C1=CC(CC)=CC=C1NC(=O)NC1=CC=CC(C(=O)C=2C3=C(N)N=CN=C3N(C(C)C)C=2)=C1 ZZQWAEVPQHAGBK-UHFFFAOYSA-N 0.000 claims 1
- SRFZAYPTSGQICB-UHFFFAOYSA-N 1-[3-(4-amino-7-propan-2-ylpyrrolo[2,3-d]pyrimidine-5-carbonyl)phenyl]-3-(4-methoxy-2-methylphenyl)urea Chemical compound CC1=CC(OC)=CC=C1NC(=O)NC1=CC=CC(C(=O)C=2C3=C(N)N=CN=C3N(C(C)C)C=2)=C1 SRFZAYPTSGQICB-UHFFFAOYSA-N 0.000 claims 1
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Landscapes
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