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
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| US20120101114A1 (en) | 2007-03-28 | 2012-04-26 | Pharmacyclics, Inc. | Inhibitors of bruton's tyrosine kinase |
| WO2009046448A1 (en) | 2007-10-04 | 2009-04-09 | Intellikine, Inc. | Chemical entities and therapeutic uses thereof |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| DK2240451T3 (da) | 2008-01-04 | 2017-11-20 | Intellikine Llc | Isoquinolinonderivater substitueret med en purin, der er anvendelig som pi3k-inhibitorer |
| EP2252293B1 (en) | 2008-03-14 | 2018-06-27 | Intellikine, LLC | Kinase inhibitors and methods of use |
| WO2009114874A2 (en) | 2008-03-14 | 2009-09-17 | Intellikine, Inc. | Benzothiazole kinase inhibitors and methods of use |
| US20110224223A1 (en) | 2008-07-08 | 2011-09-15 | The Regents Of The University Of California, A California Corporation | MTOR Modulators and Uses Thereof |
| US9096611B2 (en) | 2008-07-08 | 2015-08-04 | Intellikine Llc | Kinase inhibitors and methods of use |
| EP3311818A3 (en) | 2008-07-16 | 2018-07-18 | Pharmacyclics, LLC | Inhibitors of bruton's tyrosine kinase for the treatment of solid tumors |
| US20100015141A1 (en) * | 2008-07-21 | 2010-01-21 | 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 |
| WO2010036380A1 (en) | 2008-09-26 | 2010-04-01 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| US8697709B2 (en) * | 2008-10-16 | 2014-04-15 | 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 |
| MY152972A (en) * | 2009-07-10 | 2014-12-15 | Taiho Pharmaceutical Co Ltd | Azabicyclo compound and salt thereof |
| KR101721280B1 (ko) | 2009-08-17 | 2017-03-29 | 인텔리카인, 엘엘씨 | 헤테로사이클릭 화합물 및 이의 용도 |
| WO2011047384A2 (en) | 2009-10-16 | 2011-04-21 | The Regents Of The University Of California | Methods of inhibiting ire1 |
| EP2571357B1 (en) | 2010-05-21 | 2016-07-06 | Infinity Pharmaceuticals, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| EA031737B1 (ru) | 2010-06-03 | 2019-02-28 | Фармасайкликс, Инк. | Применение ингибиторов тирозинкиназы брутона (btk) для лечения лейкоза и лимфомы |
| AU2011305525B2 (en) | 2010-09-22 | 2016-08-18 | Arena Pharmaceuticals, Inc. | Modulators of the GPR119 receptor and the treatment of disorders related thereto |
| WO2012064973A2 (en) | 2010-11-10 | 2012-05-18 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| JP2013542966A (ja) * | 2010-11-19 | 2013-11-28 | エフ．ホフマン−ラ ロシュ アーゲー | ピラゾロピリジンならびにｔｙｋ２阻害剤としてのピラゾロピリジン及びそれらの使用 |
| DK2663309T3 (en) | 2011-01-10 | 2017-06-19 | Infinity Pharmaceuticals Inc | METHODS FOR PRODUCING ISOQUINOLINONES AND SOLID FORMS OF ISOQUINOLINONES |
| EP2678018A4 (en) | 2011-02-23 | 2015-09-30 | Intellikine Llc | COMBINATION OF CHINESE HEMMER AND USES THEREOF |
| EP2731612A4 (en) | 2011-07-13 | 2015-04-08 | Pharmacyclics Inc | BRUTON TYROSINE KINASE HEMMER |
| KR20140063605A (ko) | 2011-07-19 | 2014-05-27 | 인피니티 파마슈티칼스, 인코포레이티드 | 헤테로사이클릭 화합물 및 그의 용도 |
| US8969363B2 (en) | 2011-07-19 | 2015-03-03 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| AR091790A1 (es) | 2011-08-29 | 2015-03-04 | Infinity Pharmaceuticals Inc | Derivados de isoquinolin-1-ona y sus usos |
| MX370814B (es) | 2011-09-02 | 2020-01-08 | Univ California | Pirazolo[3,4-d]pirimidinas sustituidas y usos de las mismas. |
| EA025881B1 (ru) | 2011-09-30 | 2017-02-28 | Онкодизайн С.А. | Макроциклические ингибиторы flt3-киназы |
| 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 |
| US9296753B2 (en) | 2012-06-04 | 2016-03-29 | Pharmacyclics Llc | Crystalline forms of a Bruton's tyrosine kinase inhibitor |
| 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 |
| EP3550031A1 (en) | 2012-07-24 | 2019-10-09 | Pharmacyclics, LLC | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| AU2013323426A1 (en) | 2012-09-26 | 2015-04-23 | The Regents Of The University Of California | Modulation of ire1 |
| KR102229478B1 (ko) | 2012-11-01 | 2021-03-18 | 인피니티 파마슈티칼스, 인코포레이티드 | Pi3 키나아제 동형단백질 조절인자를 사용하는 암의 치료 |
| BR112015011171A2 (pt) | 2012-11-15 | 2017-07-11 | Pharmacyclics Inc | compostos de pirrolopirimidina como inibidores da quinase |
| 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 |
| CA2907726A1 (en) | 2013-03-22 | 2014-09-25 | Millennium Pharmaceuticals, Inc. | Combination of catalytic mtorc1/2 inhibitors and selective inhibitors of aurora a kinase |
| EP3027192A4 (en) | 2013-08-02 | 2017-03-22 | 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 |
| PL3052485T3 (pl) | 2013-10-04 | 2022-02-28 | Infinity Pharmaceuticals, Inc. | Związki heterocykliczne i ich zastosowania |
| US9751888B2 (en) | 2013-10-04 | 2017-09-05 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds and uses thereof |
| CA2943075C (en) | 2014-03-19 | 2023-02-28 | Infinity Pharmaceuticals, Inc. | Heterocyclic compounds for use in the treatment of pi3k-gamma mediated disorders |
| EP3119910A4 (en) | 2014-03-20 | 2018-02-21 | Pharmacyclics LLC | Phospholipase c gamma 2 and resistance associated mutations |
| US20150320755A1 (en) | 2014-04-16 | 2015-11-12 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| EP3174539A4 (en) | 2014-08-01 | 2017-12-13 | Pharmacyclics, LLC | Inhibitors of bruton's tyrosine kinase |
| AU2015300798A1 (en) | 2014-08-07 | 2017-02-02 | 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 |
| CN116850181A (zh) | 2015-01-06 | 2023-10-10 | 艾尼纳制药公司 | 治疗与s1p1受体有关的病症的方法 |
| IL315294A (en) | 2015-03-03 | 2024-10-01 | Pharmacyclics Llc | Pharmaceutical formulations of bruton's tyrosine kinase inhibitor |
| AU2016284162A1 (en) | 2015-06-22 | 2018-02-01 | 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(Compound1) for use in SIP1 receptor-associated disorders |
| NZ740616A (en) | 2015-09-14 | 2023-05-26 | Infinity Pharmaceuticals Inc | Solid forms of isoquinolinone derivatives, process of making, compositions comprising, and methods of using the same |
| WO2017161116A1 (en) | 2016-03-17 | 2017-09-21 | 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 |
| IL263680B2 (en) | 2016-06-24 | 2025-10-01 | Infinity Pharmaceuticals Inc | PI3K inhibitors for use in combination with a second therapeutic agent for the treatment, management or prevention of cancer |
| AU2018220521A1 (en) | 2017-02-16 | 2019-09-05 | Arena Pharmaceuticals, Inc. | Compounds and methods for treatment of primary biliary cholangitis |
| WO2019232403A1 (en) | 2018-06-01 | 2019-12-05 | Cornell University | Combination therapy for pi3k-associated disease or disorder |
| WO2019236757A1 (en) | 2018-06-06 | 2019-12-12 | Arena Pharmaceuticals, Inc. | Methods of treating conditions related to the s1p1 receptor |
| 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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- 2005-11-10 WO PCT/EP2005/012045 patent/WO2006050946A1/en not_active Ceased
- 2005-11-10 KR KR1020077010778A patent/KR20070084191A/ko not_active Withdrawn
- 2005-11-10 CA CA002585660A patent/CA2585660A1/en not_active Abandoned
- 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 |
|---|---|
| GT200500325A (es) | 2006-05-22 |
| US20080096868A1 (en) | 2008-04-24 |
| WO2006050946A1 (en) | 2006-05-18 |
| EP1812441A1 (en) | 2007-08-01 |
| CA2585660A1 (en) | 2006-05-18 |
| JP2008519790A (ja) | 2008-06-12 |
| AR051485A1 (es) | 2007-01-17 |
| CN101098873A (zh) | 2008-01-02 |
| MX2007005644A (es) | 2007-06-05 |
| AU2005303965A1 (en) | 2006-05-18 |
| GB0425035D0 (en) | 2004-12-15 |
| BRPI0517803A (pt) | 2008-10-21 |
| TW200621783A (en) | 2006-07-01 |
| KR20070084191A (ko) | 2007-08-24 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20100520 |