RU2007121846A - 1,4-замещенные пиразолопиримидины в качестве ингибиторов киназ - Google Patents
1,4-замещенные пиразолопиримидины в качестве ингибиторов киназ Download PDFInfo
- Publication number
- RU2007121846A RU2007121846A RU2007121846/04A RU2007121846A RU2007121846A RU 2007121846 A RU2007121846 A RU 2007121846A RU 2007121846/04 A RU2007121846/04 A RU 2007121846/04A RU 2007121846 A RU2007121846 A RU 2007121846A RU 2007121846 A RU2007121846 A RU 2007121846A
- Authority
- RU
- Russia
- Prior art keywords
- phenyl
- pyrazolo
- pyrimidin
- amine
- alkyl
- Prior art date
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- 229940043355 kinase inhibitor Drugs 0.000 title 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 claims abstract 29
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract 28
- 239000001257 hydrogen Substances 0.000 claims abstract 28
- 150000003839 salts Chemical class 0.000 claims abstract 23
- 150000002431 hydrogen Chemical group 0.000 claims abstract 19
- 102000001253 Protein Kinase Human genes 0.000 claims abstract 18
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims abstract 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract 15
- 229910052736 halogen Inorganic materials 0.000 claims abstract 15
- 150000002367 halogens Chemical class 0.000 claims abstract 15
- 108060006633 protein kinase Proteins 0.000 claims abstract 14
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims abstract 13
- 201000010099 disease Diseases 0.000 claims abstract 12
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims abstract 11
- 125000000547 substituted alkyl group Chemical group 0.000 claims abstract 11
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims abstract 10
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims abstract 10
- 230000002159 abnormal effect Effects 0.000 claims abstract 10
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims abstract 10
- 125000003107 substituted aryl group Chemical group 0.000 claims abstract 10
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims abstract 10
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims abstract 8
- 238000003745 diagnosis Methods 0.000 claims abstract 8
- 230000001225 therapeutic effect Effects 0.000 claims abstract 7
- 102100031983 Ephrin type-B receptor 4 Human genes 0.000 claims abstract 6
- 108700020796 Oncogene Proteins 0.000 claims abstract 6
- 108010058765 Oncogene Protein pp60(v-src) Proteins 0.000 claims abstract 6
- 108091000080 Phosphotransferase Proteins 0.000 claims abstract 6
- 102000001332 SRC Human genes 0.000 claims abstract 6
- 108060006706 SRC Proteins 0.000 claims abstract 6
- 102000020233 phosphotransferase Human genes 0.000 claims abstract 6
- WEVYNIUIFUYDGI-UHFFFAOYSA-N 3-[6-[4-(trifluoromethoxy)anilino]-4-pyrimidinyl]benzamide Chemical class NC(=O)C1=CC=CC(C=2N=CN=C(NC=3C=CC(OC(F)(F)F)=CC=3)C=2)=C1 WEVYNIUIFUYDGI-UHFFFAOYSA-N 0.000 claims abstract 5
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract 5
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract 4
- 230000001939 inductive effect Effects 0.000 claims abstract 4
- 238000006243 chemical reaction Methods 0.000 claims abstract 3
- 208000035475 disorder Diseases 0.000 claims abstract 3
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims abstract 3
- 102000050554 Eph Family Receptors Human genes 0.000 claims abstract 2
- 108091008815 Eph receptors Proteins 0.000 claims abstract 2
- -1 hydroxy, hydroxy Chemical group 0.000 claims 85
- 125000000217 alkyl group Chemical group 0.000 claims 10
- 125000004182 2-chlorophenyl group Chemical group [H]C1=C([H])C(Cl)=C(*)C([H])=C1[H] 0.000 claims 7
- 125000004195 4-methylpiperazin-1-yl group Chemical group [H]C([H])([H])N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 241001465754 Metazoa Species 0.000 claims 6
- 150000001412 amines Chemical class 0.000 claims 6
- 125000003261 o-tolyl group Chemical group [H]C1=C([H])C(*)=C(C([H])=C1[H])C([H])([H])[H] 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 5
- 108091005682 Receptor kinases Proteins 0.000 claims 4
- 230000001419 dependent effect Effects 0.000 claims 4
- 125000004484 1-methylpiperidin-4-yl group Chemical group CN1CCC(CC1)* 0.000 claims 3
- 108700020978 Proto-Oncogene Proteins 0.000 claims 3
- 102000052575 Proto-Oncogene Human genes 0.000 claims 3
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000004194 piperazin-1-yl group Chemical group [H]N1C([H])([H])C([H])([H])N(*)C([H])([H])C1([H])[H] 0.000 claims 3
- 125000006701 (C1-C7) alkyl group Chemical group 0.000 claims 2
- 125000004161 1,4-diazepinyl group Chemical group 0.000 claims 2
- NEVKWSNYPQZDQX-UHFFFAOYSA-N 1-(4-methoxyphenyl)-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1=CC(OC)=CC=C1N1C2=NC=NC(NC=3C(=CC=CC=3)C)=C2C=N1 NEVKWSNYPQZDQX-UHFFFAOYSA-N 0.000 claims 2
- 125000004204 2-methoxyphenyl group Chemical group [H]C1=C([H])C(*)=C(OC([H])([H])[H])C([H])=C1[H] 0.000 claims 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 claims 2
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 2
- 125000002785 azepinyl group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000004069 aziridinyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000002576 diazepinyl group Chemical group N1N=C(C=CC=C1)* 0.000 claims 2
- 230000000694 effects Effects 0.000 claims 2
- RWTNPBWLLIMQHL-UHFFFAOYSA-N fexofenadine Chemical compound C1=CC(C(C)(C(O)=O)C)=CC=C1C(O)CCCN1CCC(C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CC1 RWTNPBWLLIMQHL-UHFFFAOYSA-N 0.000 claims 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000001301 oxygen Substances 0.000 claims 2
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 2
- 125000000636 p-nitrophenyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)[N+]([O-])=O 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 2
- 125000004434 sulfur atom Chemical group 0.000 claims 2
- PTAVYJBCZAPEBZ-UHFFFAOYSA-N 1-(3-methoxyphenyl)-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound COC1=CC=CC(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)=C1 PTAVYJBCZAPEBZ-UHFFFAOYSA-N 0.000 claims 1
- LXHHJLJPJDCURN-UHFFFAOYSA-N 1-(4-bromophenyl)-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound CC1=CC=CC=C1NC1=NC=NC2=C1C=NN2C1=CC=C(Br)C=C1 LXHHJLJPJDCURN-UHFFFAOYSA-N 0.000 claims 1
- PLCARNJOQDDPQG-UHFFFAOYSA-N 1-[4-(4-methyl-1,4-diazepan-1-yl)phenyl]-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCCN1C1=CC=C(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 PLCARNJOQDDPQG-UHFFFAOYSA-N 0.000 claims 1
- KYWKYEDMARGTEE-HXUWFJFHSA-N 1-[4-[(3r)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1[C@H](N(C)C)CCN1C1=CC=C(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 KYWKYEDMARGTEE-HXUWFJFHSA-N 0.000 claims 1
- KYWKYEDMARGTEE-FQEVSTJZSA-N 1-[4-[(3s)-3-(dimethylamino)pyrrolidin-1-yl]phenyl]-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1[C@@H](N(C)C)CCN1C1=CC=C(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 KYWKYEDMARGTEE-FQEVSTJZSA-N 0.000 claims 1
- NKNNXEPJAFOPLG-UHFFFAOYSA-N 1-[4-[4-(diethylamino)piperidin-1-yl]phenyl]-n-(2-methylphenyl)-6-phenylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CC(N(CC)CC)CCN1C1=CC=C(N2C3=NC(=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=2C=CC=CC=2)C=C1 NKNNXEPJAFOPLG-UHFFFAOYSA-N 0.000 claims 1
- UKXUTOVCEUPHGM-UHFFFAOYSA-N 1-[4-[4-(diethylamino)piperidin-1-yl]phenyl]-n-(2-methylphenyl)-6-pyridin-4-ylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CC(N(CC)CC)CCN1C1=CC=C(N2C3=NC(=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=2C=CN=CC=2)C=C1 UKXUTOVCEUPHGM-UHFFFAOYSA-N 0.000 claims 1
- STTLIMCCZAVEAI-UHFFFAOYSA-N 1-[4-[4-(diethylamino)piperidin-1-yl]phenyl]-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CC(N(CC)CC)CCN1C1=CC=C(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 STTLIMCCZAVEAI-UHFFFAOYSA-N 0.000 claims 1
- XVUXZMNJKZLDKD-UHFFFAOYSA-N 1-[4-[4-(dipropylamino)piperidin-1-yl]phenyl]-n-(2-methylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CC(N(CCC)CCC)CCN1C1=CC=C(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 XVUXZMNJKZLDKD-UHFFFAOYSA-N 0.000 claims 1
- 125000006276 2-bromophenyl group Chemical group [H]C1=C([H])C(Br)=C(*)C([H])=C1[H] 0.000 claims 1
- 125000004172 4-methoxyphenyl group Chemical group [H]C1=C([H])C(OC([H])([H])[H])=C([H])C([H])=C1* 0.000 claims 1
- SWJUELRUGYLLPX-UHFFFAOYSA-N 6-[3-(dimethylamino)propyl]-n-(2-methylphenyl)-1-phenylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C=12C=NN(C=3C=CC=CC=3)C2=NC(CCCN(C)C)=NC=1NC1=CC=CC=C1C SWJUELRUGYLLPX-UHFFFAOYSA-N 0.000 claims 1
- LRSPQPJJXJVMGW-UHFFFAOYSA-N 6-methyl-n-(2-methylphenyl)-1-[3-(4-methylpiperazin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1=CC=CC(N2C3=NC(C)=NC(NC=4C(=CC=CC=4)C)=C3C=N2)=C1 LRSPQPJJXJVMGW-UHFFFAOYSA-N 0.000 claims 1
- CMNDCBIFZSELPL-UHFFFAOYSA-N 6-methyl-n-(2-methylphenyl)-1-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1=CC=C(N2C3=NC(C)=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 CMNDCBIFZSELPL-UHFFFAOYSA-N 0.000 claims 1
- NGDTXTYEHLAOFU-UHFFFAOYSA-N 6-methyl-n-(2-methylphenyl)-1-phenylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound CC1=CC=CC=C1NC1=NC(C)=NC2=C1C=NN2C1=CC=CC=C1 NGDTXTYEHLAOFU-UHFFFAOYSA-N 0.000 claims 1
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000005036 alkoxyphenyl group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 1
- 229910052794 bromium Inorganic materials 0.000 claims 1
- 125000001589 carboacyl group Chemical group 0.000 claims 1
- OGEBRHQLRGFBNV-RZDIXWSQSA-N chembl2036808 Chemical compound C12=NC(NCCCC)=NC=C2C(C=2C=CC(F)=CC=2)=NN1C[C@H]1CC[C@H](N)CC1 OGEBRHQLRGFBNV-RZDIXWSQSA-N 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000004029 hydroxymethyl group Chemical group [H]OC([H])([H])* 0.000 claims 1
- 125000002632 imidazolidinyl group Chemical group 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 230000003993 interaction Effects 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 125000002757 morpholinyl group Chemical group 0.000 claims 1
- HSQBWCUIAJYDBO-UHFFFAOYSA-N n',n'-dimethyl-n-[4-[4-(2-methylanilino)pyrazolo[3,4-d]pyrimidin-1-yl]phenyl]ethane-1,2-diamine Chemical compound C1=CC(NCCN(C)C)=CC=C1N1C2=NC=NC(NC=3C(=CC=CC=3)C)=C2C=N1 HSQBWCUIAJYDBO-UHFFFAOYSA-N 0.000 claims 1
- FQVNMBJNKVLSMU-UHFFFAOYSA-N n-(2-methylphenyl)-1-(4-morpholin-4-ylphenyl)pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound CC1=CC=CC=C1NC1=NC=NC2=C1C=NN2C1=CC=C(N2CCOCC2)C=C1 FQVNMBJNKVLSMU-UHFFFAOYSA-N 0.000 claims 1
- VLHYAENDGCNZES-UHFFFAOYSA-N n-(2-methylphenyl)-1-[3-(4-methylpiperazin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1=CC=CC(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)=C1 VLHYAENDGCNZES-UHFFFAOYSA-N 0.000 claims 1
- QCTWASNVDUUTSQ-UHFFFAOYSA-N n-(2-methylphenyl)-1-[3-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1CCN(C=2C=C(C=CC=2)N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)CC1 QCTWASNVDUUTSQ-UHFFFAOYSA-N 0.000 claims 1
- YCSPLANNUDMEGK-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-(4-methylpiperazin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1=CC=C(N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=C1 YCSPLANNUDMEGK-UHFFFAOYSA-N 0.000 claims 1
- ZRLPORAOJNMUPC-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-(4-morpholin-4-ylpiperidin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound CC1=CC=CC=C1NC1=NC=NC2=C1C=NN2C1=CC=C(N2CCC(CC2)N2CCOCC2)C=C1 ZRLPORAOJNMUPC-UHFFFAOYSA-N 0.000 claims 1
- QJGVSTGBTDCYJI-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-(4-pyrrolidin-1-ylpiperidin-1-yl)phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound CC1=CC=CC=C1NC1=NC=NC2=C1C=NN2C1=CC=C(N2CCC(CC2)N2CCCC2)C=C1 QJGVSTGBTDCYJI-UHFFFAOYSA-N 0.000 claims 1
- KARVNYNAFUTERX-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-[4-(1-methylpiperidin-4-yl)piperazin-1-yl]phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCC1N1CCN(C=2C=CC(=CC=2)N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)CC1 KARVNYNAFUTERX-UHFFFAOYSA-N 0.000 claims 1
- NEQZZPYVLJQROE-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-6-phenylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1CCN(C=2C=CC(=CC=2)N2C3=NC(=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=2C=CC=CC=2)CC1 NEQZZPYVLJQROE-UHFFFAOYSA-N 0.000 claims 1
- RLYARYDCULMKSD-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-6-pyridin-2-ylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1CCN(C=2C=CC(=CC=2)N2C3=NC(=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=2N=CC=CC=2)CC1 RLYARYDCULMKSD-UHFFFAOYSA-N 0.000 claims 1
- GVLORRVCMXALGM-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1CCN(C=2C=CC(=CC=2)N2C3=NC(=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=2C=NC=CC=2)CC1 GVLORRVCMXALGM-UHFFFAOYSA-N 0.000 claims 1
- ZSTLFNOOIQTRNB-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]-6-pyridin-4-ylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1CCN(C=2C=CC(=CC=2)N2C3=NC(=NC(NC=4C(=CC=CC=4)C)=C3C=N2)C=2C=CN=CC=2)CC1 ZSTLFNOOIQTRNB-UHFFFAOYSA-N 0.000 claims 1
- YSUBOPZXMFDLMU-UHFFFAOYSA-N n-(2-methylphenyl)-1-[4-[4-(4-methylpiperazin-1-yl)piperidin-1-yl]phenyl]pyrazolo[3,4-d]pyrimidin-4-amine Chemical compound C1CN(C)CCN1C1CCN(C=2C=CC(=CC=2)N2C3=NC=NC(NC=4C(=CC=CC=4)C)=C3C=N2)CC1 YSUBOPZXMFDLMU-UHFFFAOYSA-N 0.000 claims 1
- MKNHNEOFLFOENW-UHFFFAOYSA-N n-(2-methylphenyl)-1-phenylpyrazolo[3,4-d]pyrimidin-4-amine Chemical compound CC1=CC=CC=C1NC1=NC=NC2=C1C=NN2C1=CC=CC=C1 MKNHNEOFLFOENW-UHFFFAOYSA-N 0.000 claims 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 claims 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 1
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 1
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 1
- 125000005505 thiomorpholino group Chemical group 0.000 claims 1
- 125000004568 thiomorpholinyl group Chemical group 0.000 claims 1
- 108020003175 receptors Proteins 0.000 abstract 1
- 102000005962 receptors Human genes 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- 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
- A61P11/06—Antiasthmatics
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Landscapes
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- Life Sciences & Earth Sciences (AREA)
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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| GB0425035A GB0425035D0 (en) | 2004-11-12 | 2004-11-12 | Organic compounds |
| GB0425035.3 | 2004-11-12 | ||
| PCT/EP2005/012045 WO2006050946A1 (en) | 2004-11-12 | 2005-11-10 | 1,4 substituted pyrazolopyrimidines as kinase inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2007121846A true RU2007121846A (ru) | 2008-12-20 |
Family
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Family Applications (1)
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|---|---|---|---|
| RU2007121846/04A RU2007121846A (ru) | 2004-11-12 | 2005-11-10 | 1,4-замещенные пиразолопиримидины в качестве ингибиторов киназ |
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| EP (1) | EP1812441A1 (https=) |
| JP (1) | JP2008519790A (https=) |
| KR (1) | KR20070084191A (https=) |
| CN (1) | CN101098873A (https=) |
| AR (1) | AR051485A1 (https=) |
| AU (1) | AU2005303965A1 (https=) |
| BR (1) | BRPI0517803A (https=) |
| CA (1) | CA2585660A1 (https=) |
| GB (1) | GB0425035D0 (https=) |
| GT (1) | GT200500325A (https=) |
| MX (1) | MX2007005644A (https=) |
| RU (1) | RU2007121846A (https=) |
| TW (1) | TW200621783A (https=) |
| WO (1) | WO2006050946A1 (https=) |
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| MXPA05007485A (es) | 2003-01-14 | 2006-01-30 | Arena Pharm Inc | Derivados de arilo y heteroarilo 1,2,3-trisubstituidos como moduladores del metabolismo y la profilaxis y tratamiento de trastornos relacionados con ello tales como diabetes e hiperglicemia. |
| US9512125B2 (en) | 2004-11-19 | 2016-12-06 | The Regents Of The University Of California | Substituted pyrazolo[3.4-D] pyrimidines as anti-inflammatory agents |
| KR20070118068A (ko) * | 2004-11-23 | 2007-12-13 | 레디 유에스 테라퓨틱스 인코포레이티드 | 신규의 이원 헤테로고리 화합물, 그 제조방법 및 이들을포함하는 조성물 |
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| WO2007114926A2 (en) | 2006-04-04 | 2007-10-11 | The Regents Of The University Of California | Kinase antagonists |
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| BRPI0622054B8 (pt) * | 2006-09-22 | 2021-05-25 | Oxford Amherst Llc | composto e composição farmacêutica |
| TW200840581A (en) * | 2007-02-28 | 2008-10-16 | Astrazeneca Ab | Novel pyrimidine derivatives |
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| GB2467670B (en) | 2007-10-04 | 2012-08-01 | Intellikine Inc | Chemical entities and therapeutic uses thereof |
| EP3613743B1 (en) | 2008-01-04 | 2022-03-16 | Intellikine, LLC | Processes for the preparation of 1h-pyrazolo[3,4-d]pyrimidin-4-amine derivatives |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| US8993580B2 (en) | 2008-03-14 | 2015-03-31 | Intellikine Llc | Benzothiazole kinase inhibitors and methods of use |
| US8637542B2 (en) | 2008-03-14 | 2014-01-28 | Intellikine, Inc. | Kinase inhibitors and methods of use |
| JP5788316B2 (ja) | 2008-07-08 | 2015-09-30 | インテリカイン， エルエルシー | キナーゼインヒビターおよび使用方法 |
| US20110224223A1 (en) | 2008-07-08 | 2011-09-15 | The Regents Of The University Of California, A California Corporation | MTOR Modulators and Uses Thereof |
| ES2660418T3 (es) | 2008-07-16 | 2018-03-22 | Pharmacyclics Llc | Inhibidores de la tirosina quinasa de Bruton para el tratamiento de tumores sólidos |
| WO2010011620A1 (en) * | 2008-07-21 | 2010-01-28 | Wyeth | 4-phenoxy-6-aryl-1h-pyrazolo[3,4-d]pyrimidine and n-aryl-6-aryl-1h-pyrazolo[3,4-d]pyrimidin-4-amine compounds, their use as mtor kinase and pi3 kinase inhibitors, and their syntheses |
| US8703778B2 (en) | 2008-09-26 | 2014-04-22 | Intellikine Llc | Heterocyclic kinase inhibitors |
| WO2010045542A2 (en) * | 2008-10-16 | 2010-04-22 | The Regents Of The University Of California | Fused ring heteroaryl kinase inhibitors |
| US8476431B2 (en) | 2008-11-03 | 2013-07-02 | Itellikine LLC | Benzoxazole kinase inhibitors and methods of use |
| EP2427195B1 (en) | 2009-05-07 | 2019-05-01 | Intellikine, LLC | Heterocyclic compounds and uses thereof |
| TWI460177B (zh) * | 2009-07-10 | 2014-11-11 | Taiho Pharmaceutical Co Ltd | An azabicyclo compound or a salt thereof |
| PE20121148A1 (es) | 2009-08-17 | 2012-09-07 | Intellikine Llc | Compuestos heterociclicos y usos de los mismos |
| US8980899B2 (en) | 2009-10-16 | 2015-03-17 | The Regents Of The University Of California | Methods of inhibiting Ire1 |
| CA2799579A1 (en) | 2010-05-21 | 2011-11-24 | Intellikine, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| CN107898791A (zh) | 2010-06-03 | 2018-04-13 | 药品循环有限责任公司 | 布鲁顿酪氨酸激酶(btk)抑制剂的应用 |
| PH12013500547A1 (en) | 2010-09-22 | 2013-06-10 | Arena Pharm Inc | Modulators of the gpr119 receptor and the treatment of disorders related thereto |
| JP2013545749A (ja) | 2010-11-10 | 2013-12-26 | インフィニティー ファーマシューティカルズ， インコーポレイテッド | 複素環化合物及びその使用 |
| MX2013005445A (es) * | 2010-11-19 | 2013-07-29 | Hoffmann La Roche | Pirazolopiridinas y el uso de pirazolopiridinas como inhibidores de tirosina cinasa 2 (tyk2). |
| TWI674262B (zh) | 2011-01-10 | 2019-10-11 | 美商英菲尼提製藥股份有限公司 | 製備異喹啉酮之方法及異喹啉酮之固體形式 |
| US9295673B2 (en) | 2011-02-23 | 2016-03-29 | Intellikine Llc | Combination of mTOR inhibitors and P13-kinase inhibitors, and uses thereof |
| US9138436B2 (en) | 2011-07-13 | 2015-09-22 | Pharmacyclics Llc | Inhibitors of Bruton's tyrosine kinase |
| MX2014000648A (es) | 2011-07-19 | 2014-09-25 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y sus usos. |
| WO2013012915A1 (en) | 2011-07-19 | 2013-01-24 | Infinity Pharmaceuticals Inc. | Heterocyclic compounds and uses thereof |
| KR20140075693A (ko) | 2011-08-29 | 2014-06-19 | 인피니티 파마슈티칼스, 인코포레이티드 | 헤테로사이클릭 화합물 및 그의 용도 |
| MX370814B (es) | 2011-09-02 | 2020-01-08 | Univ California | Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas. |
| CA2849999A1 (en) | 2011-09-30 | 2013-04-04 | Oncodesign S.A. | Macrocyclic flt3 kinase inhibitors |
| US8377946B1 (en) | 2011-12-30 | 2013-02-19 | Pharmacyclics, Inc. | Pyrazolo[3,4-d]pyrimidine and pyrrolo[2,3-d]pyrimidine compounds as kinase inhibitors |
| US8940742B2 (en) | 2012-04-10 | 2015-01-27 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| JO3754B1 (ar) | 2012-06-04 | 2021-01-31 | Pharmacyclics Llc | أشكال كريستالين لمثبط أنزيم كيناز تيروسين بروتون |
| US8828998B2 (en) | 2012-06-25 | 2014-09-09 | Infinity Pharmaceuticals, Inc. | Treatment of lupus, fibrotic conditions, and inflammatory myopathies and other disorders using PI3 kinase inhibitors |
| CN104704129A (zh) | 2012-07-24 | 2015-06-10 | 药品循环公司 | 与对布鲁顿酪氨酸激酶(btk)抑制剂的抗性相关的突变 |
| MX2015003874A (es) | 2012-09-26 | 2015-12-16 | Univ California | Modulacion de ire1. |
| EP2914296B2 (en) | 2012-11-01 | 2021-09-29 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| EA201590855A1 (ru) | 2012-11-15 | 2015-11-30 | Фармасайкликс, Инк. | Соединения пирролопиримидина как ингибиторы киназ |
| US9481667B2 (en) | 2013-03-15 | 2016-11-01 | Infinity Pharmaceuticals, Inc. | Salts and solid forms of isoquinolinones and composition comprising and methods of using the same |
| WO2014153509A1 (en) | 2013-03-22 | 2014-09-25 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc 1/2 inhibitors and selective inhibitors of aurora a kinase |
| CA2919996A1 (en) | 2013-08-02 | 2015-02-05 | Pharmacyclics Llc | Methods for the treatment of solid tumors |
| US9415050B2 (en) | 2013-08-12 | 2016-08-16 | Pharmacyclics Llc | Methods for the treatment of HER2 amplified cancer |
| CA2925124A1 (en) | 2013-09-30 | 2015-04-02 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| MX2021012208A (es) | 2013-10-04 | 2023-01-19 | Infinity Pharmaceuticals Inc | Compuestos heterocíclicos y usos de los mismos. |
| WO2015051241A1 (en) | 2013-10-04 | 2015-04-09 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| NZ724368A (en) | 2014-03-19 | 2023-07-28 | Infinity Pharmaceuticals Inc | Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders |
| WO2015143400A1 (en) | 2014-03-20 | 2015-09-24 | Pharmacyclics, Inc. | Phospholipase c gamma 2 and resistance associated mutations |
| WO2015160975A2 (en) | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| AU2015296215A1 (en) | 2014-08-01 | 2017-03-23 | Pharmacyclics Llc | Inhibitors of bruton's tyrosine kinase |
| SG11201700849XA (en) | 2014-08-07 | 2017-03-30 | Pharmacyclics Llc | Novel formulations of a bruton's tyrosine kinase inhibitor |
| WO2016054491A1 (en) | 2014-10-03 | 2016-04-07 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| MX386419B (es) | 2015-01-06 | 2025-03-18 | Arena Pharm Inc | Metodos de condiciones de tratamiento relacionadas con el receptor s1p1. |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| EP3939965A1 (en) | 2015-06-22 | 2022-01-19 | Arena Pharmaceuticals, Inc. | Crystalline l-arginine salt of (r)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid for use in sipi receptor-associated disorders |
| EP4585268A3 (en) | 2015-09-14 | 2025-10-15 | Twelve Therapeutics, Inc. | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| US10759806B2 (en) | 2016-03-17 | 2020-09-01 | Infinity Pharmaceuticals, Inc. | Isotopologues of isoquinolinone and quinazolinone compounds and uses thereof as PI3K kinase inhibitors |
| WO2017214269A1 (en) | 2016-06-08 | 2017-12-14 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| RU2754507C2 (ru) | 2016-06-24 | 2021-09-02 | Инфинити Фармасьютикалз, Инк. | Комбинированная терапия |
| MA47504A (fr) | 2017-02-16 | 2019-12-25 | Arena Pharm Inc | Composés et méthodes de traitement de l'angiocholite biliaire primitive |
| CN113194752A (zh) | 2018-06-01 | 2021-07-30 | 康奈尔大学 | Pi3k相关疾病或病症的组合疗法 |
| ES2987794T3 (es) | 2018-06-06 | 2024-11-18 | Arena Pharm Inc | Procedimientos de tratamiento de afecciones relacionadas con el receptor S1P1 |
| CN110734437B (zh) * | 2018-07-19 | 2022-04-08 | 南京烁慧医药科技有限公司 | 吡唑并嘧啶化合物和药物组合物及其应用 |
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| WO2004009597A2 (en) * | 2002-07-23 | 2004-01-29 | Smithkline Beecham Corporation | Pyrazolopyrimidines as protein kinase inhibitors |
| JP2007210887A (ja) * | 2004-06-21 | 2007-08-23 | Astellas Pharma Inc | 縮合二環性ピリミジン誘導体 |
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- 2005-11-10 US US11/718,730 patent/US20080096868A1/en not_active Abandoned
- 2005-11-10 MX MX2007005644A patent/MX2007005644A/es not_active Application Discontinuation
- 2005-11-10 CA CA002585660A patent/CA2585660A1/en not_active Abandoned
- 2005-11-10 AU AU2005303965A patent/AU2005303965A1/en not_active Abandoned
- 2005-11-10 EP EP05819276A patent/EP1812441A1/en not_active Withdrawn
- 2005-11-10 CN CNA2005800464109A patent/CN101098873A/zh active Pending
- 2005-11-11 TW TW094139701A patent/TW200621783A/zh unknown
- 2005-11-11 AR ARP050104725A patent/AR051485A1/es not_active Application Discontinuation
Also Published As
| Publication number | Publication date |
|---|---|
| US20080096868A1 (en) | 2008-04-24 |
| KR20070084191A (ko) | 2007-08-24 |
| AR051485A1 (es) | 2007-01-17 |
| EP1812441A1 (en) | 2007-08-01 |
| GB0425035D0 (en) | 2004-12-15 |
| WO2006050946A1 (en) | 2006-05-18 |
| GT200500325A (es) | 2006-05-22 |
| BRPI0517803A (pt) | 2008-10-21 |
| AU2005303965A1 (en) | 2006-05-18 |
| MX2007005644A (es) | 2007-06-05 |
| TW200621783A (en) | 2006-07-01 |
| CN101098873A (zh) | 2008-01-02 |
| CA2585660A1 (en) | 2006-05-18 |
| JP2008519790A (ja) | 2008-06-12 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20100520 |