JP2015536948A5 - - Google Patents
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- JP2015536948A5 JP2015536948A5 JP2015540794A JP2015540794A JP2015536948A5 JP 2015536948 A5 JP2015536948 A5 JP 2015536948A5 JP 2015540794 A JP2015540794 A JP 2015540794A JP 2015540794 A JP2015540794 A JP 2015540794A JP 2015536948 A5 JP2015536948 A5 JP 2015536948A5
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- hematological malignancy
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- 239000000203 mixture Substances 0.000 claims 20
- 239000003112 inhibitor Substances 0.000 claims 19
- 230000002401 inhibitory effect Effects 0.000 claims 19
- 206010066476 Haematological malignancy Diseases 0.000 claims 18
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 18
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 239000003795 chemical substances by application Substances 0.000 claims 12
- 239000000090 biomarker Substances 0.000 claims 8
- 108010011536 PTEN Phosphohydrolase Proteins 0.000 claims 7
- 102000014160 PTEN Phosphohydrolase Human genes 0.000 claims 7
- -1 WX-554 Chemical compound 0.000 claims 7
- 102000010400 1-phosphatidylinositol-3-kinase activity proteins Human genes 0.000 claims 6
- 108040005185 1-phosphatidylinositol-3-kinase activity proteins Proteins 0.000 claims 6
- 102100013894 BCL2 Human genes 0.000 claims 6
- 108060000885 BCL2 Proteins 0.000 claims 6
- 102100009639 CXCL13 Human genes 0.000 claims 6
- 101710032192 CXCL13 Proteins 0.000 claims 6
- 102100006844 MMP9 Human genes 0.000 claims 6
- 101700067851 MMP9 Proteins 0.000 claims 6
- 150000001875 compounds Chemical class 0.000 claims 6
- YTKUWDBFDASYHO-UHFFFAOYSA-N Bendamustine Chemical compound ClCCN(CCCl)C1=CC=C2N(C)C(CCCC(O)=O)=NC2=C1 YTKUWDBFDASYHO-UHFFFAOYSA-N 0.000 claims 5
- 108010001645 Rituximab Proteins 0.000 claims 5
- 108090001123 antibodies Proteins 0.000 claims 5
- 102000004965 antibodies Human genes 0.000 claims 5
- 229960002707 bendamustine Drugs 0.000 claims 5
- 229960004641 rituximab Drugs 0.000 claims 5
- 101700041849 EZH2 Proteins 0.000 claims 4
- 102100016041 EZH2 Human genes 0.000 claims 4
- 108010001801 Tumor Necrosis Factor-alpha Proteins 0.000 claims 4
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims 4
- 102100009312 BTK Human genes 0.000 claims 3
- 102100009641 CXCL10 Human genes 0.000 claims 3
- 101710032181 CXCL10 Proteins 0.000 claims 3
- 206010008943 Chronic leukaemia Diseases 0.000 claims 3
- 206010008958 Chronic lymphocytic leukaemia Diseases 0.000 claims 3
- 102000013462 Interleukin-12 Human genes 0.000 claims 3
- 108010065805 Interleukin-12 Proteins 0.000 claims 3
- 239000002177 L01XE27 - Ibrutinib Substances 0.000 claims 3
- 102100019436 PLK1 Human genes 0.000 claims 3
- 101700062434 PLK1 Proteins 0.000 claims 3
- 239000003276 histone deacetylase inhibitor Substances 0.000 claims 3
- XYFPWWZEPKGCCK-GOSISDBHSA-N ibrutinib Chemical compound C1=2C(N)=NC=NC=2N([C@H]2CN(CCC2)C(=O)C=C)N=C1C(C=C1)=CC=C1OC1=CC=CC=C1 XYFPWWZEPKGCCK-GOSISDBHSA-N 0.000 claims 3
- 229960001507 ibrutinib Drugs 0.000 claims 3
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims 3
- MIMNFCVQODTQDP-NDLVEFNKSA-N oblimersen Chemical compound O=C1NC(=O)C(C)=CN1[C@@H]1O[C@H](COP(S)(=O)O[C@@H]2[C@H](O[C@H](C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=C(C(NC(N)=N3)=O)N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C3=NC=NC(N)=C3N=C2)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(N=C(N)C=C2)=O)COP(O)(=S)O[C@@H]2[C@H](O[C@H](C2)N2C(NC(=O)C(C)=C2)=O)CO)[C@@H](O)C1 MIMNFCVQODTQDP-NDLVEFNKSA-N 0.000 claims 3
- LQBVNQSMGBZMKD-UHFFFAOYSA-N 4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide Chemical group C=1C=C(Cl)C=CC=1C=1CC(C)(C)CCC=1CN(CC1)CCN1C(C=C1OC=2C=C3C=CNC3=NC=2)=CC=C1C(=O)NS(=O)(=O)C(C=C1[N+]([O-])=O)=CC=C1NCC1CCOCC1 LQBVNQSMGBZMKD-UHFFFAOYSA-N 0.000 claims 2
- HPLNQCPCUACXLM-PGUFJCEWSA-N 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl]sulfonylbenzamide Chemical compound C([C@@H](CCN(C)C)NC=1C(=CC(=CC=1)S(=O)(=O)NC(=O)C=1C=CC(=CC=1)N1CCN(CC=2C(=CC=CC=2)C=2C=CC(Cl)=CC=2)CC1)[N+]([O-])=O)SC1=CC=CC=C1 HPLNQCPCUACXLM-PGUFJCEWSA-N 0.000 claims 2
- 102100003279 CD38 Human genes 0.000 claims 2
- 101700044948 CD38 Proteins 0.000 claims 2
- 102100005832 CD69 Human genes 0.000 claims 2
- 101700080416 CD69 Proteins 0.000 claims 2
- 108091007936 ERK family Proteins 0.000 claims 2
- GOTYRUGSSMKFNF-UHFFFAOYSA-N Lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 claims 2
- QGZYDVAGYRLSKP-UHFFFAOYSA-N N-[7-(hydroxyamino)-7-oxoheptyl]-2-(N-phenylanilino)pyrimidine-5-carboxamide Chemical compound N1=CC(C(=O)NCCCCCCC(=O)NO)=CN=C1N(C=1C=CC=CC=1)C1=CC=CC=C1 QGZYDVAGYRLSKP-UHFFFAOYSA-N 0.000 claims 2
- JLYAXFNOILIKPP-KXQOOQHDSA-N Navitoclax Chemical compound C([C@@H](NC1=CC=C(C=C1S(=O)(=O)C(F)(F)F)S(=O)(=O)NC(=O)C1=CC=C(C=C1)N1CCN(CC1)CC1=C(CCC(C1)(C)C)C=1C=CC(Cl)=CC=1)CSC=1C=CC=CC=1)CN1CCOCC1 JLYAXFNOILIKPP-KXQOOQHDSA-N 0.000 claims 2
- RFTSSZJZXOSICM-VXLYETTFSA-N Obatoclax Chemical compound COC1=CC(C=2NC3=CC=CC=C3C=2)=N\C1=C\C=1NC(C)=CC=1C RFTSSZJZXOSICM-VXLYETTFSA-N 0.000 claims 2
- 208000009052 Precursor T-Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 2
- 206010042971 T-cell lymphoma Diseases 0.000 claims 2
- 230000004913 activation Effects 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 229960004942 lenalidomide Drugs 0.000 claims 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 claims 2
- 230000035772 mutation Effects 0.000 claims 2
- 229960003347 obinutuzumab Drugs 0.000 claims 2
- 108010045555 obinutuzumab Proteins 0.000 claims 2
- 230000037361 pathway Effects 0.000 claims 2
- 108091007934 protein kinase B family Proteins 0.000 claims 2
- 229960003452 romidepsin Drugs 0.000 claims 2
- OHRURASPPZQGQM-GCCNXGTGSA-N romidepsin Chemical compound O1C(=O)[C@H](C(C)C)NC(=O)C(=C/C)/NC(=O)[C@H]2CSSCC\C=C\[C@@H]1CC(=O)N[C@H](C(C)C)C(=O)N2 OHRURASPPZQGQM-GCCNXGTGSA-N 0.000 claims 2
- 108010091666 romidepsin Proteins 0.000 claims 2
- 229960001183 venetoclax Drugs 0.000 claims 2
- FKSFKBQGSFSOSM-QFIPXVFZSA-N 1-[(2S)-butan-2-yl]-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-methyl-6-(6-piperazin-1-ylpyridin-3-yl)indole-4-carboxamide Chemical compound C1=C2N([C@@H](C)CC)C=C(C)C2=C(C(=O)NCC=2C(NC(C)=CC=2C)=O)C=C1C(C=N1)=CC=C1N1CCNCC1 FKSFKBQGSFSOSM-QFIPXVFZSA-N 0.000 claims 1
- CODBZFJPKJDNDT-UHFFFAOYSA-N 2-[[5-[3-(dimethylamino)propyl]-2-methylpyridin-3-yl]amino]-9-(trifluoromethyl)-5,7-dihydropyrimido[5,4-d][1]benzazepine-6-thione Chemical compound CN(C)CCCC1=CN=C(C)C(NC=2N=C3C4=CC=C(C=C4NC(=S)CC3=CN=2)C(F)(F)F)=C1 CODBZFJPKJDNDT-UHFFFAOYSA-N 0.000 claims 1
- OMKHWTRUYNAGFG-IEBDPFPHSA-N 3-Deazaneplanocin A Chemical compound C1=NC=2C(N)=NC=CC=2N1[C@@H]1C=C(CO)[C@@H](O)[C@H]1O OMKHWTRUYNAGFG-IEBDPFPHSA-N 0.000 claims 1
- RCLQNICOARASSR-SECBINFHSA-N 3-[(2R)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione Chemical compound FC=1C(=O)N(C)C=2N=CN(C[C@@H](O)CO)C(=O)C=2C=1NC1=CC=C(I)C=C1F RCLQNICOARASSR-SECBINFHSA-N 0.000 claims 1
- GWRSATNRNFYMDI-UHFFFAOYSA-N 4-[(9-cyclopentyl-7,7-difluoro-5-methyl-6-oxo-8H-pyrimido[4,5-b][1,4]diazepin-2-yl)amino]-2-fluoro-5-methoxy-N-(1-methylpiperidin-4-yl)benzamide Chemical compound FC=1C=C(NC=2N=C3N(C4CCCC4)CC(F)(F)C(=O)N(C)C3=CN=2)C(OC)=CC=1C(=O)NC1CCN(C)CC1 GWRSATNRNFYMDI-UHFFFAOYSA-N 0.000 claims 1
- VVLHQJDAUIPZFH-UHFFFAOYSA-N 4-[4-[[5-fluoro-4-[3-(prop-2-enoylamino)anilino]pyrimidin-2-yl]amino]phenoxy]-N-methylpyridine-2-carboxamide Chemical compound C1=NC(C(=O)NC)=CC(OC=2C=CC(NC=3N=C(NC=4C=C(NC(=O)C=C)C=CC=4)C(F)=CN=3)=CC=2)=C1 VVLHQJDAUIPZFH-UHFFFAOYSA-N 0.000 claims 1
- JIFCFQDXHMUPGP-UHFFFAOYSA-N 4-tert-butyl-N-[2-methyl-3-[4-methyl-6-[4-(morpholine-4-carbonyl)anilino]-5-oxopyrazin-2-yl]phenyl]benzamide Chemical compound C1=CC=C(C=2N=C(NC=3C=CC(=CC=3)C(=O)N3CCOCC3)C(=O)N(C)C=2)C(C)=C1NC(=O)C1=CC=C(C(C)(C)C)C=C1 JIFCFQDXHMUPGP-UHFFFAOYSA-N 0.000 claims 1
- ZHJGWYRLJUCMRT-QGZVFWFLSA-N 5-[6-[(4-methylpiperazin-1-yl)methyl]benzimidazol-1-yl]-3-[(1R)-1-[2-(trifluoromethyl)phenyl]ethoxy]thiophene-2-carboxamide Chemical compound O([C@H](C)C=1C(=CC=CC=1)C(F)(F)F)C(=C(S1)C(N)=O)C=C1N(C1=C2)C=NC1=CC=C2CN1CCN(C)CC1 ZHJGWYRLJUCMRT-QGZVFWFLSA-N 0.000 claims 1
- ACWZRVQXLIRSDF-UHFFFAOYSA-N 6-(4-bromo-2-fluoroanilino)-7-fluoro-N-(2-hydroxyethoxy)-3-methylbenzimidazole-5-carboxamide Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims 1
- AOJJSUZBOXZQNB-TZSSRYMLSA-N ADRIAMYCIN Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 1
- 102100017507 AKT1S1 Human genes 0.000 claims 1
- 101710031851 AKT1S1 Proteins 0.000 claims 1
- 101710009063 CARD11 Proteins 0.000 claims 1
- 102100002586 CARD11 Human genes 0.000 claims 1
- 102100019449 CD79B Human genes 0.000 claims 1
- 101700045471 CD79B Proteins 0.000 claims 1
- 102100006400 CSF2 Human genes 0.000 claims 1
- BSMCAPRUBJMWDF-KRWDZBQOSA-N Cobimetinib Chemical compound C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F BSMCAPRUBJMWDF-KRWDZBQOSA-N 0.000 claims 1
- 229960002271 Cobimetinib Drugs 0.000 claims 1
- 230000008836 DNA modification Effects 0.000 claims 1
- 229960004679 Doxorubicin Drugs 0.000 claims 1
- 108010017213 Granulocyte-Macrophage Colony-Stimulating Factor Proteins 0.000 claims 1
- 102100015977 IL16 Human genes 0.000 claims 1
- 101700036616 IL16 Proteins 0.000 claims 1
- 102100019517 JAK1 Human genes 0.000 claims 1
- 101700034277 JAK1 Proteins 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 102100004961 MMP12 Human genes 0.000 claims 1
- 108090000028 MMP12 Proteins 0.000 claims 1
- 102100010074 MYD88 Human genes 0.000 claims 1
- 101700079836 MYD88 Proteins 0.000 claims 1
- 206010026798 Mantle cell lymphomas Diseases 0.000 claims 1
- OCKHRKSTDPOHEN-BQYQJAHWSA-N N-(4-methoxyphenyl)sulfonyl-N-[2-[(E)-2-(1-oxidopyridin-1-ium-4-yl)ethenyl]phenyl]acetamide Chemical compound C1=CC(OC)=CC=C1S(=O)(=O)N(C(C)=O)C1=CC=CC=C1\C=C\C1=CC=[N+]([O-])C=C1 OCKHRKSTDPOHEN-BQYQJAHWSA-N 0.000 claims 1
- NSQSAUGJQHDYNO-UHFFFAOYSA-N N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-3-[ethyl(oxan-4-yl)amino]-2-methyl-5-[4-(morpholin-4-ylmethyl)phenyl]benzamide Chemical compound C=1C(C=2C=CC(CN3CCOCC3)=CC=2)=CC(C(=O)NCC=2C(NC(C)=CC=2C)=O)=C(C)C=1N(CC)C1CCOCC1 NSQSAUGJQHDYNO-UHFFFAOYSA-N 0.000 claims 1
- ULNXAWLQFZMIHX-UHFFFAOYSA-N N-[(6-methyl-2-oxo-4-propyl-1H-pyridin-3-yl)methyl]-6-[2-(4-methylpiperazin-1-yl)pyridin-4-yl]-1-propan-2-ylindazole-4-carboxamide Chemical compound C1=C(C)NC(=O)C(CNC(=O)C=2C=3C=NN(C=3C=C(C=2)C=2C=C(N=CC=2)N2CCN(C)CC2)C(C)C)=C1CCC ULNXAWLQFZMIHX-UHFFFAOYSA-N 0.000 claims 1
- RDSACQWTXKSHJT-NSHDSACASA-N N-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims 1
- CDOOFZZILLRUQH-GDLZYMKVSA-N N-[3-[6-[4-[(2R)-1,4-dimethyl-3-oxopiperazin-2-yl]anilino]-4-methyl-5-oxopyrazin-2-yl]-2-methylphenyl]-4,5,6,7-tetrahydro-1-benzothiophene-2-carboxamide Chemical compound CN1CCN(C)C(=O)[C@H]1C(C=C1)=CC=C1NC1=NC(C=2C(=C(NC(=O)C=3SC=4CCCCC=4C=3)C=CC=2)C)=CN(C)C1=O CDOOFZZILLRUQH-GDLZYMKVSA-N 0.000 claims 1
- KXBDTLQSDKGAEB-UHFFFAOYSA-N N-[3-[[5-fluoro-2-[4-(2-methoxyethoxy)anilino]pyrimidin-4-yl]amino]phenyl]prop-2-enamide Chemical compound C1=CC(OCCOC)=CC=C1NC1=NC=C(F)C(NC=2C=C(NC(=O)C=C)C=CC=2)=N1 KXBDTLQSDKGAEB-UHFFFAOYSA-N 0.000 claims 1
- 101710033916 NRAS Proteins 0.000 claims 1
- 102100001119 NRAS Human genes 0.000 claims 1
- 229960002450 Ofatumumab Drugs 0.000 claims 1
- LZMPYSIUWPEIRA-XFXZXTDPSA-N Ofatumumab Chemical compound N1=C2C=3COCCC=3N=CC2=N\C1=C1\NOC=C1 LZMPYSIUWPEIRA-XFXZXTDPSA-N 0.000 claims 1
- 206010025310 Other lymphomas Diseases 0.000 claims 1
- SUDAHWBOROXANE-VIFPVBQESA-N PD 0325901-Cl Chemical compound OC[C@H](O)CONC(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F SUDAHWBOROXANE-VIFPVBQESA-N 0.000 claims 1
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- 101710027440 PIK3CA Proteins 0.000 claims 1
- FWZRWHZDXBDTFK-ZHACJKMWSA-N Panobinostat Chemical compound CC1=NC2=CC=C[CH]C2=C1CCNCC1=CC=C(\C=C\C(=O)NO)C=C1 FWZRWHZDXBDTFK-ZHACJKMWSA-N 0.000 claims 1
- 208000008425 Protein Deficiency Diseases 0.000 claims 1
- 102000001708 Protein Isoforms Human genes 0.000 claims 1
- 108010029485 Protein Isoforms Proteins 0.000 claims 1
- OWBFCJROIKNMGD-BQYQJAHWSA-N Rigosertib Chemical compound COC1=CC(OC)=CC(OC)=C1\C=C\S(=O)(=O)CC1=CC=C(OC)C(NCC(O)=O)=C1 OWBFCJROIKNMGD-BQYQJAHWSA-N 0.000 claims 1
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- 101700038204 TGFA Proteins 0.000 claims 1
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- LIRYPHYGHXZJBZ-UHFFFAOYSA-N Trametinib Chemical compound CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims 1
- 102000006747 Transforming growth factor alpha Human genes 0.000 claims 1
- 108010078814 Tumor Suppressor Protein p53 Proteins 0.000 claims 1
- 229960004528 Vincristine Drugs 0.000 claims 1
- WAEXFXRVDQXREF-UHFFFAOYSA-N Vorinostat Chemical compound ONC(=O)CCCCCCC(=O)NC1=CC=CC=C1 WAEXFXRVDQXREF-UHFFFAOYSA-N 0.000 claims 1
- 229960000237 Vorinostat Drugs 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000003247 decreasing Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 229960000435 oblimersen Drugs 0.000 claims 1
- 108010052070 ofatumumab Proteins 0.000 claims 1
- 229960005184 panobinostat Drugs 0.000 claims 1
- 229960005267 tositumomab Drugs 0.000 claims 1
- 229960004066 trametinib Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-XQKSVPLYSA-N vincristine Chemical compound C([N@]1C[C@@H](C[C@]2(C(=O)OC)C=3C(=CC4=C([C@]56[C@H]([C@@]([C@H](OC(C)=O)[C@]7(CC)C=CCN([C@H]67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)C[C@@](C1)(O)CC)CC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-XQKSVPLYSA-N 0.000 claims 1
- LFUYRYYQBCVUSJ-UHFFFAOYSA-N CC(C(N1c2ccccc2)=Cc2cccc(C)c2C1=O)NC1N(C)C=Nc2c1nc[nH]2 Chemical compound CC(C(N1c2ccccc2)=Cc2cccc(C)c2C1=O)NC1N(C)C=Nc2c1nc[nH]2 LFUYRYYQBCVUSJ-UHFFFAOYSA-N 0.000 description 1
Claims (15)
- 対象における血液悪性腫瘍の治療に使用するための、下記の構造を有する化合物、又はその医薬として許容し得る形態を含む医薬組成物であって、
- 対象における血液悪性腫瘍の治療のための医薬品の製造における、下記の構造を有する化合物、又はその医薬として許容し得る形態の使用であって、
bcl-2阻害剤、HDAC阻害剤、MEK阻害剤、EZH2阻害剤、及びPLK-1阻害剤からなる群から選択される第二の活性剤と組合せて使用するように製剤化される、前記使用。 - 前記第二の活性剤が、下記からなる群から選択される、請求項１又は２記載の医薬組成物又は使用：
(i)ベリノスタット、ボリノスタット、パノビノスタット、ACY-1215、及びロミデプシンからなる群から選択されるHDAC阻害剤；
(ii)タメチニブ/GSK1120212、セルメチノブ、ピマセルチブ/AS703026/MSC1935369、XL-518/GDC-0973、ラファメチニブ/BAY869766/RDEA119、PD-0325901、TAK733、MEK162/ARRY438162、RO5126766、WX-554、RO4987655/CH4987655、及びAZD8330からなる群から選択されるMEK阻害剤；
(iii)EPZ-6438、GSK-126、GSK-343、El1、及び3-デアザネプラノシンA(DNNep)からなる群から選択されるEZH2阻害剤；並びに
(iv)ボラセルチブ(BI6727)、BI2536、ZK-チアゾリドン、TAK-960、MLN0905、GSK461364、リゴセルチブ(ON-01910)、及びHMN-214からなる群から選択されるPLK-1阻害剤。 - 前記PI3K阻害剤が、bcl-2阻害剤と組合せて使用するように製剤化されており、該bcl-2阻害剤が、ABT-199、ABT-737、ABT-263、GX15-070（メシル酸オバトクラックス）、又はG3139（オブリメルセン）からなる群から任意に選択される、請求項１〜３のいずれか一項記載の医薬組成物又は使用。
- 前記PI3K阻害剤が、下記からなる群から選択される第二の活性剤と組合せて使用するように製剤化されている、請求項１〜４のいずれか一項記載の医薬組成物又は使用：
(i)抗CD37抗体；
(ii)131I トシツモマブ、90Y イブリツモマブ、111I イブリツモマブ、オビヌツズマブ、及びオファツムマブからなる群から選択される抗CD20抗体；及び
(iii)抗CD52抗体。 - 前記PI3K阻害剤が、抗CD20抗体と組合せて投与され、該抗CD20抗体が、任意にオビヌツズマブである、請求項１〜５のいずれか一項記載の医薬組成物又は使用。
- 前記PI3K阻害剤が、下記からなる群から選択される第二の活性剤と組合せて投与される、請求項１〜６のいずれか一項記載の医薬組成物又は使用：
(i)前記血液悪性腫瘍がiNHLである場合の、リツキシマブ、ベンダムスチン、もしくはレナリドマイド、又はこれらの組合せである第二の活性剤；
(ii)前記血液悪性腫瘍がCLLである場合の、リツキシマブ、ベンダムスチン、もしくはレナリドマイド、又はこれらの組合せである第二の活性剤；
(iii)前記血液悪性腫瘍がDLBCLである場合の、リツキシマブ、ベンダムスチン、R-GDP、もしくはイブルチニブ、又はこれらの組合せである第二の活性剤；
(iv)前記血液悪性腫瘍がDLBCLである場合の、ACY-1215である第二の活性剤；
(v)前記血液悪性腫瘍がT細胞リンパ腫である場合の、リツキシマブ、ベンダムスチン、もしくはロミデプシン、又はこれらの組合せである第二の活性剤；
(vi)前記血液悪性腫瘍がマントル細胞リンパ腫である場合の、リツキシマブ、ベンダムスチン、もしくはイブルチニブ、又はこれらの組合せである第二の活性剤；並びに
(vii)前記血液悪性腫瘍がT-ALLであり、かつ前記対象がPTEN欠損を有する場合の、ドキソルビシン及び/又はビンクリスチンである第二の活性剤。 - 前記対象が、一定の期間にわたってバイオマーカーのレベルの変化をモニタリングされる、請求項１〜７のいずれか一項記載の医薬組成物又は使用。
- 前記バイオマーカーが、CXCL13、CCL4、CCL17、CCL22、TNF-α、もしくはMMP-9、又はこれらの組合せから選択され、該バイオマーカーのレベルが前記一定の期間にわたって減少する場合に、前記対象が、前記治療に対して応答性である、請求項８記載の医薬組成物又は使用。
- 前記対象が、下記の1以上のレベルの変化についてモニタリングされる、請求項１〜９のいずれか一項記載の医薬組成物又は使用：
(i)IGH7、KRAS、NRAS、A20、CD79B、TP53、CARD11、MYD88、EZH2、JAK1/2、PTEN、及びPIK3CAのうちの1つ又は複数の突然変異；
(ii)PTEN発現の低下、PTENのDNA修飾、PTEN欠失、PTEN突然変異、又はこれらの組合せ：
(iii)1以上のPI3Kアイソフォームの発現レベル；及び/又は
(iv)RAS経路の活性化、PI3K経路の活性化、又はその両方。 - (i)前記血液悪性腫瘍がCLL又はSLLであり、前記バイオマーカーが、CCL1、IL-10、CXCL13、CCL3、CCL4、CCL17、CCL22、TNFα、IL-12（p40）、CXCL10、もしくはMMP-9、又はこれらの組合せである；
(ii)前記血液悪性腫瘍がリンパ腫であり、前記バイオマーカーが、CXCL13、CCL17、もしくはMMP-9、又はこれらの組合せである；
(iii)前記血液悪性腫瘍がiNHLであり、前記バイオマーカーが、CCL1、CCL17、CCL22、CXCL13、IL-12（p40）、MMP-12、MMP-9、TNFα、もしくはIL-16、又はこれらの組合せである；
(iv)前記血液悪性腫瘍がMCLであり、前記バイオマーカーが、CCL17、CCL22、CXCL10、CXCL13、もしくはMMP-9、又はこれらの組合せである；
(v)前記血液悪性腫瘍がT細胞リンパ腫であり、前記バイオマーカーが、CCL17、CCL22、CXCL10、CXCL13、MMP-9、GM-CSF、IL-12（p40）、TNF-α、TGF-α、ERK（細胞外シグナル調節キナーゼ）、PRAS40、もしくはpS6、又はこれらの組合せである；
(vi)前記血液悪性腫瘍がCLLであり、前記患者が、CD38陽性、CD69陽性、CD38/CD69二重陽性、Ki67陽性、pAKT陽性、又はKi67/pAKT二重陽性癌細胞を有する；又は
(vii)前記血液悪性腫瘍がT-ALLであり、前記対象がPTEN欠損を有する、
請求項８又は９記載の医薬組成物又は使用。 - 対象における血液悪性腫瘍の治療において、BTK阻害剤と組合せて使用するための、下記の構造を有する化合物、又はその医薬として許容し得る形態を含む医薬組成物：
- 前記BTK阻害剤が、イブルチニブ、GDC-0834、CGI-560、CGI-1746、HM-71224、AVL-292、ONO-4059、CNX-774、又はLFM-A13から選択される、請求項１２記載の医薬組成物。
- 対象における血液悪性腫瘍の治療において、BCL-2阻害剤と組合せて使用するための、下記の構造を有する化合物、又はその医薬として許容し得る形態を含む医薬組成物：
- 前記BCL-2阻害剤が、ABT-199、ABT-737、ABT-263、GX15-070（メシル酸オバトクラックス）、又はG3139（オブリメルセン）から選択される、請求項１４記載の医薬組成物。
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Families Citing this family (96)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JPWO2003040013A1 (ja) * | 2001-11-08 | 2005-02-24 | 三菱電機株式会社 | 巻上機及びエレベータ装置 |
| MX2010007418A (es) | 2008-01-04 | 2010-11-12 | Intellikine Inc | Ciertas entidades quimicas, composiciones y metodos. |
| US8193182B2 (en) | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| BRPI0920209A2 (pt) | 2008-10-15 | 2015-12-22 | Angiochem Inc | conjugados de agonistas de glp-1 e usos dos mesmos |
| WO2011160206A1 (en) | 2010-06-23 | 2011-12-29 | Morin Ryan D | Biomarkers for non-hodgkin lymphomas and uses thereof |
| EP2663309B1 (en) | 2011-01-10 | 2017-03-15 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
| WO2012121953A1 (en) | 2011-03-08 | 2012-09-13 | The Trustees Of Columbia University In The City Of New York | Methods and pharmaceutical compositions for treating lymphoid malignancy |
| WO2012151525A1 (en) | 2011-05-04 | 2012-11-08 | Rhizen Pharmaceuticals Sa | Novel compounds as modulators of protein kinases |
| CN104080786A (zh) * | 2011-11-08 | 2014-10-01 | 因特利凯有限责任公司 | 使用多种药剂的治疗方案 |
| WO2013075084A1 (en) | 2011-11-18 | 2013-05-23 | Constellation Pharmaceuticals | Modulators of methyl modifying enzymes, compositions and uses thereof |
| CA2862289C (en) | 2012-02-10 | 2019-11-26 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| 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 |
| CA2782774A1 (en) * | 2012-07-06 | 2014-01-06 | Pharmascience Inc. | Protein kinase inhibitors |
| TR201812261T4 (tr) * | 2012-11-01 | 2018-11-21 | Infinity Pharmaceuticals Inc | Pi3 ki̇naz i̇zoform modülatörleri̇ i̇le kanser tedavi̇si̇ |
| US9446064B2 (en) | 2013-03-14 | 2016-09-20 | Epizyme, Inc. | Combination therapy for treating cancer |
| EP2970305B1 (en) | 2013-03-15 | 2017-02-22 | Constellation Pharmaceuticals, Inc. | Modulators of methyl modifying enzymes, compositions and uses thereof |
| UY35464A (es) | 2013-03-15 | 2014-10-31 | Araxes Pharma Llc | Inhibidores covalentes de kras g12c. |
| WO2014194254A1 (en) * | 2013-05-30 | 2014-12-04 | Infinity Pharmaceuticals, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| ES2672018T3 (es) | 2013-07-02 | 2018-06-12 | Rhizen Pharmaceuticals S.A. | Inhibidores de proteína cinasa PI3K, particularmente inhibidores delta y/o gamma |
| WO2015011236A1 (en) * | 2013-07-26 | 2015-01-29 | Boehringer Ingelheim International Gmbh | Treatment of myelodysplastic syndrome |
| EP3033334A1 (en) | 2013-08-15 | 2016-06-22 | Constellation Pharmaceuticals, Inc. | Indole derivatives as modulators of methyl modifying enzymes, compositions and uses thereof |
| US9403779B2 (en) * | 2013-10-08 | 2016-08-02 | Acetylon Pharmaceuticals, Inc. | Combinations of histone deacetylase inhibitors and either Her2 inhibitors or PI3K inhibitors |
| JO3805B1 (ar) | 2013-10-10 | 2021-01-31 | Araxes Pharma Llc | مثبطات كراس جي12سي |
| CA2931431A1 (en) * | 2013-12-05 | 2015-06-11 | Acerta Pharma B.V. | Therapeutic combination of a pi3k inhibitor and a btk inhibitor |
| KR102473113B1 (ko) | 2013-12-06 | 2022-12-01 | 에피자임, 인코포레이티드 | 암 치료를 위한 병용 요법 |
| WO2015160986A2 (en) * | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| WO2015160975A2 (en) * | 2014-04-16 | 2015-10-22 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| EP2950097A1 (en) * | 2014-05-28 | 2015-12-02 | Universitätsspital Basel | Podoplanin as a biomarker of the activation of PI3K/mTOR signaling in human tumors |
| KR102497728B1 (ko) * | 2014-06-17 | 2023-02-09 | 에피자임, 인코포레이티드 | 림프종 치료를 위한 ｅｚｈ2 억제제 |
| WO2016004221A1 (en) * | 2014-07-01 | 2016-01-07 | Mayo Foundation For Medical Education And Research | Methods and materials for identifying and treating mammals resistant to proteasome inhibitor treatments |
| CR20160600A (es) | 2014-07-04 | 2017-03-07 | Lupin Ltd | Quinolizione derivados como inhibidores pi3k |
| WO2016022358A1 (en) * | 2014-08-08 | 2016-02-11 | The Regents Of The University Of California | Compositions and methods for reactivating latent viral infections |
| WO2016025656A1 (en) * | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a pi3k inhibitor or dual pi3k/tor inhibitor and related methods |
| WO2016025649A1 (en) * | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a dot1l inhibitor and related methods |
| WO2016025652A1 (en) * | 2014-08-13 | 2016-02-18 | Celgene Avilomics Research, Inc. | Combinations of an erk inhibitor and a bcl-2 pathway modulator and related methods |
| EP4070795A1 (en) | 2014-08-25 | 2022-10-12 | Salk Institute for Biological Studies | Novel ulk1 inhibitors and methods using same |
| WO2016040848A1 (en) | 2014-09-12 | 2016-03-17 | G1 Therapeutics, Inc. | Treatment of rb-negative tumors using topoisomerase inhibitors in combination with cyclin dependent kinase 4/6 inhibitors |
| EP3191098A4 (en) | 2014-09-12 | 2018-04-25 | G1 Therapeutics, Inc. | Combinations and dosing regimes to treat rb-positive tumors |
| ES2826443T3 (es) * | 2014-09-25 | 2021-05-18 | Araxes Pharma Llc | Inhibidores de proteínas mutantes KRAS G12C |
| WO2016090255A1 (en) * | 2014-12-05 | 2016-06-09 | Sriram Balasubramanian | Biological markers for predicting responsiveness to ibrutinib and r-chop combination therapy and methods of using the same |
| CN106146508A (zh) * | 2015-03-19 | 2016-11-23 | 浙江导明医药科技有限公司 | 优化的联合用药及其治疗癌症和自身免疫疾病的用途 |
| AU2016236578B2 (en) * | 2015-03-20 | 2019-04-04 | Crystal Pharmatech Co., Ltd. | Preparation method of crystalline form a of pci-32765 |
| JP2018513853A (ja) | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| CA2982435C (en) | 2015-04-13 | 2020-05-26 | Daiichi Sankyo Company, Limited | Treatment method by combined use of mdm2 inhibitor and btk inhibitor |
| EP3307713A4 (en) | 2015-06-10 | 2019-01-23 | Epizyme, Inc. | EZH2 INHIBITOR FOR THE TREATMENT OF LYMPHOMA |
| JP6823055B2 (ja) | 2015-06-15 | 2021-01-27 | アンジオケム インコーポレーテッド | 軟髄膜癌腫症の治療方法 |
| TWI746449B (zh) * | 2015-07-20 | 2021-11-21 | 美商Ａｉ治療公司 | 使用阿吡莫德治療癌症之方法 |
| CN106366085A (zh) * | 2015-07-25 | 2017-02-01 | 复旦大学 | 异喹啉酮类化合物或其盐及其制备方法和用途 |
| BR112018001960A2 (pt) | 2015-08-03 | 2018-09-18 | Bristol-Myers Squibb Company | compostos heterocíclicos úteis como moduladores de tnf alfa |
| WO2017033113A1 (en) * | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| US10577350B2 (en) | 2015-08-28 | 2020-03-03 | Constellation Pharmaceuticals, Inc. | Crystalline forms of (R)-N-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide |
| WO2017058728A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017058902A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| EP3356359B1 (en) | 2015-09-28 | 2021-10-20 | Araxes Pharma LLC | Inhibitors of kras g12c mutant proteins |
| WO2017058768A1 (en) | 2015-09-28 | 2017-04-06 | Araxes Pharma Llc | Inhibitors of kras g12c mutant proteins |
| WO2017068412A1 (en) | 2015-10-21 | 2017-04-27 | Otsuka Pharmaceutical Co., Ltd. | Benzolactam compounds as protein kinase inhibitors |
| CN108137592B (zh) * | 2015-11-03 | 2021-03-05 | 纽弗姆制药有限公司 | 用于治疗血癌的氘代化合物以及其组合物和方法 |
| WO2017096458A1 (en) * | 2015-12-07 | 2017-06-15 | Ontario Institute For Cancer Research (Oicr) | Immune gene signature predictive of anthracycline benefit |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| CN109562107A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| WO2017223422A1 (en) | 2016-06-24 | 2017-12-28 | Infinity Pharmaceuticals, Inc. | Combination therapies |
| RU2019102647A (ru) | 2016-07-01 | 2020-08-03 | Г1 Терапьютикс, Инк. | Антипролиферационные средства на основе пиримидина |
| WO2018013474A1 (en) * | 2016-07-11 | 2018-01-18 | Hennepin Life Sciences, Llc | Compositions for sexually transmitted diseases |
| US10646488B2 (en) | 2016-07-13 | 2020-05-12 | Araxes Pharma Llc | Conjugates of cereblon binding compounds and G12C mutant KRAS, HRAS or NRAS protein modulating compounds and methods of use thereof |
| WO2018053437A1 (en) * | 2016-09-19 | 2018-03-22 | Mei Pharma, Inc. | Combination therapy |
| US10925880B2 (en) | 2016-09-23 | 2021-02-23 | Bayer Pharma Aktiengesellschaft | Combination of PI3K-inhibitors |
| CN110036010A (zh) | 2016-09-29 | 2019-07-19 | 亚瑞克西斯制药公司 | Kras g12c突变蛋白的抑制剂 |
| US10899767B2 (en) | 2016-10-05 | 2021-01-26 | Hangzhou Solipharma Co., Ltd. | Crystal form of ACP-196, preparation method therefor and pharmaceutical composition thereof |
| CN109843870A (zh) | 2016-10-19 | 2019-06-04 | 星座制药公司 | Ezh2抑制剂的合成 |
| JP2020502062A (ja) | 2016-11-17 | 2020-01-23 | ザ ユニバーシティ オブ ノース カロライナ アット チャペル ヒル | アルキルピロロピリミジン類似体、及びその製造方法と使用方法 |
| NZ754944A (en) | 2016-12-07 | 2023-02-24 | Beigene Ltd | Imidazo [1,5-a] pyrazine derivatives as pi3kdelta inhibitors |
| GB201706327D0 (en) | 2017-04-20 | 2017-06-07 | Otsuka Pharma Co Ltd | A pharmaceutical compound |
| JP2020521741A (ja) | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| US20230201212A1 (en) * | 2017-06-13 | 2023-06-29 | Epizyme, Inc. | Inhibitors of ezh2 and methods of use thereof |
| BR112019027967A2 (pt) | 2017-06-29 | 2020-07-14 | G1 Therapeutics, Inc. | forma b cristalina isolada, composição farmacêutica, método para o tratamento de um distúrbio, método de um composto ou composição, e, processo para produzir forma b cristalina. |
| GB201710851D0 (en) * | 2017-07-06 | 2017-08-23 | Galápagos Nv | Novel compounds and pharmaceutical compositions thereof for the treatment of fibrosis |
| JP2020529418A (ja) | 2017-07-31 | 2020-10-08 | ザ トラスティーズ オブ コロンビア ユニバーシティ イン ザ シティ オブ ニューヨークＴｈｅ Ｔｒｕｓｔｅｅｓ Ｏｆ Ｃｏｌｕｍｂｉａ Ｕｎｉｖｅｒｓｉｔｙ Ｉｎ Ｔｈｅ Ｃｉｔｙ Ｏｆ Ｎｅｗ Ｙｏｒｋ | Ｔ細胞急性リンパ芽球性白血病を治療するための化合物、組成及び方法 |
| FI3679042T3 (fi) * | 2017-09-08 | 2023-05-15 | Beigene Ltd | IMIDATSO[1,5-A]PYRATSIINIJOHDANNAISIA PI3Kdelta-ESTÄJINÄ |
| US11597933B2 (en) | 2017-11-29 | 2023-03-07 | The Trustees Of Columbia University In The City Of New York | Combination therapy of lymphoma |
| CN109942556A (zh) * | 2017-12-21 | 2019-06-28 | 上海青煜医药科技有限公司 | 嘧啶酮化合物及其应用 |
| WO2019139399A1 (ko) * | 2018-01-12 | 2019-07-18 | 보령제약 주식회사 | Pi3 키나아제 억제제 및 세포독성 항암제를 포함하는 암의 예방 또는 치료용 약학적 조성물 |
| WO2019183003A1 (en) * | 2018-03-18 | 2019-09-26 | The University Of North Carolina At Chapel Hill | Methods and assays for endometrial diseases |
| JP2021519337A (ja) | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Ｉｋａｒｏｓの分解のためのセレブロン結合剤 |
| US20210148894A1 (en) * | 2018-04-13 | 2021-05-20 | Bionomics Limited | Method of monitoring response to a treatment |
| CN108743947B (zh) * | 2018-07-04 | 2020-12-15 | 复旦大学附属肿瘤医院 | 一种治疗b细胞淋巴瘤的药物组合物 |
| US10579964B1 (en) * | 2018-08-21 | 2020-03-03 | Intelligrated Headquarters, Llc | Method, apparatus and system for goods replenishment |
| EP3846800A4 (en) | 2018-09-04 | 2022-08-24 | C4 Therapeutics, Inc. | COMPOUNDS FOR THE DEGRADATION OF BRD9 OR MTH1 |
| EP3897631A4 (en) | 2018-12-20 | 2022-11-23 | C4 Therapeutics, Inc. | TARGETED PROTEIN DEGRADATION |
| KR20200129704A (ko) * | 2019-05-09 | 2020-11-18 | 보령제약 주식회사 | Pi3k 저해제의 결정다형 및 이의 제조방법 |
| CA3160091A1 (en) | 2019-11-05 | 2021-05-14 | Abbvie Inc. | Dosing regimens for use in treating myelofibrosis and mpn-related disorders with navitoclax |
| CN110975919B (zh) * | 2019-12-25 | 2021-06-01 | 福州大学 | 一种氮掺杂碳量子点原位生长脱硝抗硫催化剂及其制备方法 |
| CN111402523A (zh) * | 2020-03-24 | 2020-07-10 | 宋钰堃 | 一种基于面部影像识别的医疗报警系统及方法 |
| WO2022019920A1 (en) * | 2020-07-24 | 2022-01-27 | Verastem, Inc. | Treatment of cancers using pi3 kinase isoform modulators |
| CN114432490B (zh) * | 2021-11-10 | 2023-01-06 | 北京大学口腔医学院 | 3d打印材料及其制备方法和应用 |
| WO2023239821A2 (en) * | 2022-06-07 | 2023-12-14 | Lantern Pharma Inc. | Treating cancers with combinations of acylfulvenes with ibrutinib or bortezomib |
| CN114788830B (zh) * | 2022-06-08 | 2024-01-23 | 东阳市人民医院 | 一种能够抑制弓形虫增殖的小分子抑制剂的应用 |
Family Cites Families (167)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3536809A (en) | 1969-02-17 | 1970-10-27 | Alza Corp | Medication method |
| US3598123A (en) | 1969-04-01 | 1971-08-10 | Alza Corp | Bandage for administering drugs |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US3916899A (en) | 1973-04-25 | 1975-11-04 | Alza Corp | Osmotic dispensing device with maximum and minimum sizes for the passageway |
| US4008719A (en) | 1976-02-02 | 1977-02-22 | Alza Corporation | Osmotic system having laminar arrangement for programming delivery of active agent |
| US4270537A (en) | 1979-11-19 | 1981-06-02 | Romaine Richard A | Automatic hypodermic syringe |
| KR890002631B1 (ko) | 1984-10-04 | 1989-07-21 | 몬산토 캄파니 | 생물학적으로 활성인 소마토트로핀을 지속적으로 유리하는 조성물 |
| IE58110B1 (en) | 1984-10-30 | 1993-07-14 | Elan Corp Plc | Controlled release powder and process for its preparation |
| US4596556A (en) | 1985-03-25 | 1986-06-24 | Bioject, Inc. | Hypodermic injection apparatus |
| US5023252A (en) | 1985-12-04 | 1991-06-11 | Conrex Pharmaceutical Corporation | Transdermal and trans-membrane delivery of drugs |
| CA1283827C (en) | 1986-12-18 | 1991-05-07 | Giorgio Cirelli | Appliance for injection of liquid formulations |
| GB8704027D0 (en) | 1987-02-20 | 1987-03-25 | Owen Mumford Ltd | Syringe needle combination |
| US5001139A (en) | 1987-06-12 | 1991-03-19 | American Cyanamid Company | Enchancers for the transdermal flux of nivadipine |
| US4992445A (en) | 1987-06-12 | 1991-02-12 | American Cyanamid Co. | Transdermal delivery of pharmaceuticals |
| US4790824A (en) | 1987-06-19 | 1988-12-13 | Bioject, Inc. | Non-invasive hypodermic injection device |
| US4941880A (en) | 1987-06-19 | 1990-07-17 | Bioject, Inc. | Pre-filled ampule and non-invasive hypodermic injection device assembly |
| US4940460A (en) | 1987-06-19 | 1990-07-10 | Bioject, Inc. | Patient-fillable and non-invasive hypodermic injection device assembly |
| US5339163A (en) | 1988-03-16 | 1994-08-16 | Canon Kabushiki Kaisha | Automatic exposure control device using plural image plane detection areas |
| US5073543A (en) | 1988-07-21 | 1991-12-17 | G. D. Searle & Co. | Controlled release formulations of trophic factors in ganglioside-lipsome vehicle |
| FR2638359A1 (fr) | 1988-11-03 | 1990-05-04 | Tino Dalto | Guide de seringue avec reglage de la profondeur de penetration de l'aiguille dans la peau |
| GB8827305D0 (en) | 1988-11-23 | 1988-12-29 | British Bio Technology | Compounds |
| IT1229203B (it) | 1989-03-22 | 1991-07-25 | Bioresearch Spa | Impiego di acido 5 metiltetraidrofolico, di acido 5 formiltetraidrofolico e dei loro sali farmaceuticamente accettabili per la preparazione di composizioni farmaceutiche in forma a rilascio controllato attive nella terapia dei disturbi mentali organici e composizioni farmaceutiche relative. |
| PH30995A (en) | 1989-07-07 | 1997-12-23 | Novartis Inc | Sustained release formulations of water soluble peptides. |
| US5120548A (en) | 1989-11-07 | 1992-06-09 | Merck & Co., Inc. | Swelling modulated polymeric drug delivery device |
| US5312335A (en) | 1989-11-09 | 1994-05-17 | Bioject Inc. | Needleless hypodermic injection device |
| US5064413A (en) | 1989-11-09 | 1991-11-12 | Bioject, Inc. | Needleless hypodermic injection device |
| US5733566A (en) | 1990-05-15 | 1998-03-31 | Alkermes Controlled Therapeutics Inc. Ii | Controlled release of antiparasitic agents in animals |
| US5190521A (en) | 1990-08-22 | 1993-03-02 | Tecnol Medical Products, Inc. | Apparatus and method for raising a skin wheal and anesthetizing skin |
| US5527288A (en) | 1990-12-13 | 1996-06-18 | Elan Medical Technologies Limited | Intradermal drug delivery device and method for intradermal delivery of drugs |
| GB9118204D0 (en) | 1991-08-23 | 1991-10-09 | Weston Terence E | Needle-less injector |
| SE9102652D0 (sv) | 1991-09-13 | 1991-09-13 | Kabi Pharmacia Ab | Injection needle arrangement |
| US5580578A (en) | 1992-01-27 | 1996-12-03 | Euro-Celtique, S.A. | Controlled release formulations coated with aqueous dispersions of acrylic polymers |
| US5328483A (en) | 1992-02-27 | 1994-07-12 | Jacoby Richard M | Intradermal injection device with medication and needle guard |
| WO1993018186A1 (en) | 1992-03-04 | 1993-09-16 | The Regents Of The University Of California | Comparative genomic hybridization (cgh) |
| US5383851A (en) | 1992-07-24 | 1995-01-24 | Bioject Inc. | Needleless hypodermic injection device |
| US5569189A (en) | 1992-09-28 | 1996-10-29 | Equidyne Systems, Inc. | hypodermic jet injector |
| US5334144A (en) | 1992-10-30 | 1994-08-02 | Becton, Dickinson And Company | Single use disposable needleless injector |
| TW333456B (en) | 1992-12-07 | 1998-06-11 | Takeda Pharm Ind Co Ltd | A pharmaceutical composition of sustained-release preparation the invention relates to a pharmaceutical composition of sustained-release preparation which comprises a physiologically active peptide. |
| US5455258A (en) | 1993-01-06 | 1995-10-03 | Ciba-Geigy Corporation | Arylsulfonamido-substituted hydroxamic acids |
| US5591767A (en) | 1993-01-25 | 1997-01-07 | Pharmetrix Corporation | Liquid reservoir transdermal patch for the administration of ketorolac |
| US6087324A (en) | 1993-06-24 | 2000-07-11 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
| WO1995024176A1 (en) | 1994-03-07 | 1995-09-14 | Bioject, Inc. | Ampule filling device |
| US5466220A (en) | 1994-03-08 | 1995-11-14 | Bioject, Inc. | Drug vial mixing and transfer device |
| IT1270594B (it) | 1994-07-07 | 1997-05-07 | Recordati Chem Pharm | Composizione farmaceutica a rilascio controllato di moguisteina in sospensione liquida |
| US5599302A (en) | 1995-01-09 | 1997-02-04 | Medi-Ject Corporation | Medical injection system and method, gas spring thereof and launching device using gas spring |
| US5863949A (en) | 1995-03-08 | 1999-01-26 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| WO1996033172A1 (en) | 1995-04-20 | 1996-10-24 | Pfizer Inc. | Arylsulfonyl hydroxamic acid derivatives as mmp and tnf inhibitors |
| US5730723A (en) | 1995-10-10 | 1998-03-24 | Visionary Medical Products Corporation, Inc. | Gas pressured needle-less injection device and method |
| AU6242096A (en) | 1995-06-27 | 1997-01-30 | Takeda Chemical Industries Ltd. | Method of producing sustained-release preparation |
| TW448055B (en) | 1995-09-04 | 2001-08-01 | Takeda Chemical Industries Ltd | Method of production of sustained-release preparation |
| JP2909418B2 (ja) | 1995-09-18 | 1999-06-23 | 株式会社資生堂 | 薬物の遅延放出型マイクロスフイア |
| ES2183905T3 (es) | 1995-12-20 | 2003-04-01 | Hoffmann La Roche | Inhibidores de metaloproteasa de matriz. |
| US5893397A (en) | 1996-01-12 | 1999-04-13 | Bioject Inc. | Medication vial/syringe liquid-transfer apparatus |
| US5980945A (en) | 1996-01-16 | 1999-11-09 | Societe De Conseils De Recherches Et D'applications Scientifique S.A. | Sustained release drug formulations |
| GB9607549D0 (en) | 1996-04-11 | 1996-06-12 | Weston Medical Ltd | Spring-powered dispensing device |
| US6264970B1 (en) | 1996-06-26 | 2001-07-24 | Takeda Chemical Industries, Ltd. | Sustained-release preparation |
| ATE217315T1 (de) | 1996-07-18 | 2002-05-15 | Pfizer | Matrix metalloprotease-inhibitoren auf basis von phosphinsäuren |
| US6153609A (en) | 1996-08-23 | 2000-11-28 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| US6419961B1 (en) | 1996-08-29 | 2002-07-16 | Takeda Chemical Industries, Ltd. | Sustained release microcapsules of a bioactive substance and a biodegradable polymer |
| CA2217134A1 (en) | 1996-10-09 | 1998-04-09 | Sumitomo Pharmaceuticals Co., Ltd. | Sustained release formulation |
| ATE272394T1 (de) | 1996-10-31 | 2004-08-15 | Takeda Chemical Industries Ltd | Zubereitung mit verzögerter freisetzung |
| DE69719367T2 (de) | 1996-12-20 | 2003-10-16 | Takeda Chemical Industries Ltd | Verfahren zur herstellung einer zusammensetzung mit verzoegerter abgabe |
| CA2277100C (en) | 1997-01-06 | 2005-11-22 | Pfizer Inc. | Cyclic sulfone derivatives |
| US5891474A (en) | 1997-01-29 | 1999-04-06 | Poli Industria Chimica, S.P.A. | Time-specific controlled release dosage formulations and method of preparing same |
| US6303636B1 (en) | 1997-02-03 | 2001-10-16 | Pfizer Inc | Arylsulfonylamino hydroxamic acid derivatives |
| AU5493598A (en) | 1997-02-07 | 1998-08-26 | Pfizer Inc. | N-hydroxy-beta-sulfonyl-propionamide derivatives and their use as inhibitors of matrix metalloproteinases |
| CN1247531A (zh) | 1997-02-11 | 2000-03-15 | 辉瑞大药厂 | 芳基磺酰基异羟肟酸衍生物 |
| US5993412A (en) | 1997-05-19 | 1999-11-30 | Bioject, Inc. | Injection apparatus |
| GB9725782D0 (en) | 1997-12-05 | 1998-02-04 | Pfizer Ltd | Therapeutic agents |
| IT1298087B1 (it) | 1998-01-08 | 1999-12-20 | Fiderm S R L | Dispositivo per il controllo della profondita' di penetrazione di un ago, in particolare applicabile ad una siringa per iniezioni |
| GB9801690D0 (en) | 1998-01-27 | 1998-03-25 | Pfizer Ltd | Therapeutic agents |
| US6613358B2 (en) | 1998-03-18 | 2003-09-02 | Theodore W. Randolph | Sustained-release composition including amorphous polymer |
| US6432970B2 (en) | 1998-04-09 | 2002-08-13 | Johns Hopkins University School Of Medicine | Inhibitors of hedgehog signaling pathways, compositions and uses related thereto |
| PA8469401A1 (es) | 1998-04-10 | 2000-05-24 | Pfizer Prod Inc | Derivados biciclicos del acido hidroxamico |
| PA8469501A1 (es) | 1998-04-10 | 2000-09-29 | Pfizer Prod Inc | Hidroxamidas del acido (4-arilsulfonilamino)-tetrahidropiran-4-carboxilico |
| KR19990085365A (ko) | 1998-05-16 | 1999-12-06 | 허영섭 | 지속적으로 약물 조절방출이 가능한 생분해성 고분자 미립구 및그 제조방법 |
| US6927024B2 (en) | 1998-11-30 | 2005-08-09 | Genentech, Inc. | PCR assay |
| US6248363B1 (en) | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| AU780846B2 (en) | 1999-09-16 | 2005-04-21 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
| US20070021493A1 (en) | 1999-09-16 | 2007-01-25 | Curis, Inc. | Mediators of hedgehog signaling pathways, compositions and uses related thereto |
| WO2001027135A2 (en) | 1999-10-13 | 2001-04-19 | Johns Hopkins University School Of Medicine | Regulators of the hedgehog pathway, compositions and uses related thereto |
| ATE324876T1 (de) | 1999-10-14 | 2006-06-15 | Curis Inc | VERMITTLER VON ßHEDGEHOGß ÜBERMITTELNDEN BAHNEN, DAZUGEHÖRIGE ZUSAMMENETZUNGEN UND VERWENDUNGEN |
| AU3074001A (en) | 1999-12-09 | 2001-06-18 | Advanced Research And Technology Institute, Inc. | Fluorescent in situ rt-pcr |
| IL133809A0 (en) | 1999-12-30 | 2001-04-30 | Yeda Res & Dev | Steroidal alkaloids and pharmaceutical compositions comprising them |
| ES2250377T5 (es) | 2000-03-30 | 2010-04-06 | Curis, Inc. | Moleculas organicas pequeñas reguladoras de la proliferacion celular. |
| CA2439402A1 (en) | 2001-03-02 | 2002-09-12 | University Of Pittsburgh Of The Commonwealth System Of Higher Education | Pcr method |
| EA007339B1 (ru) | 2001-07-27 | 2006-08-25 | Кьюэрис, Инк. | Медиаторы путей передачи сигналов генами hedgehog, содержащие их композиции и способы применения указанных веществ |
| ES2367422T3 (es) | 2001-10-09 | 2011-11-03 | Amgen Inc. | Derivados de imidazol como agentes antiinflamatorios. |
| US20030113828A1 (en) | 2001-11-09 | 2003-06-19 | Ginsberg Mark H. | Compositions and methods for modulating Syk function |
| US20030158195A1 (en) | 2001-12-21 | 2003-08-21 | Cywin Charles L. | 1,6 naphthyridines useful as inhibitors of SYK kinase |
| CA2483311A1 (en) | 2002-04-22 | 2003-10-30 | Philip A. Beachy | Modulators of hedgehog signaling pathways, compositions and uses related thereto |
| WO2004020599A2 (en) | 2002-08-29 | 2004-03-11 | Curis, Inc. | Hedgehog antagonists, methods and uses related thereto |
| US7199119B2 (en) | 2002-10-31 | 2007-04-03 | Amgen Inc. | Antiinflammation agents |
| FR2850022B1 (fr) | 2003-01-22 | 2006-09-08 | Centre Nat Rech Scient | Nouvelle utilisation de la mifepristone et de ses derives comme modulateurs de la voie de signalisation des proteines hedgehog et ses applications |
| JP2007524397A (ja) | 2003-07-03 | 2007-08-30 | ザ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・ペンシルベニア | Ｓｙｋキナーゼ発現の阻害 |
| WO2005013800A2 (en) | 2003-07-15 | 2005-02-17 | The Johns Hopkins University | Elevated hedgehog pathway activity in digestive system tumors, and methods of treating digestive system tumors having elevated hedgehog pathway activity |
| WO2005016348A1 (en) | 2003-08-14 | 2005-02-24 | Icos Corporation | Method of inhibiting immune responses stimulated by an endogenous factor |
| GB0321710D0 (en) | 2003-09-16 | 2003-10-15 | Novartis Ag | Organic compounds |
| US8067608B2 (en) | 2003-09-29 | 2011-11-29 | The Johns Hopkins University | Hedgehog pathway antagonists |
| WO2005032343A2 (en) | 2003-10-01 | 2005-04-14 | The Johns Hopkins University | Hedgehog signaling in prostate regeneration neoplasia and metastasis |
| WO2005042700A2 (en) | 2003-10-20 | 2005-05-12 | The Johns Hopkins University | Use of hedgehog pathway inhibitors in small-cell lung cancer |
| US20050267059A1 (en) | 2003-11-14 | 2005-12-01 | Diana Beardsley | Syk-targeted nucleic acid interference |
| US7122799B2 (en) | 2003-12-18 | 2006-10-17 | Palo Alto Research Center Incorporated | LED or laser enabled real-time PCR system and spectrophotometer |
| US8057815B2 (en) | 2004-04-19 | 2011-11-15 | Portola Pharmaceuticals, Inc. | Methods of treatment with Syk inhibitors |
| ES2389955T3 (es) | 2004-04-30 | 2012-11-05 | Genentech, Inc. | Inhibidores de quinoxalina de la vía de señalización hedgehog |
| LT2612862T (lt) | 2004-05-13 | 2017-01-25 | Icos Corporation | Chinazolinonai kaip žmogaus fosfatidilinozitol-3-kinazės delta inhibitoriai |
| EP1817308B1 (en) | 2004-08-27 | 2014-10-08 | Infinity Pharmaceuticals, Inc. | Cyclopamine analogues and methods of use thereof |
| EA017262B1 (ru) | 2004-09-02 | 2012-11-30 | Дженентек, Инк. | Соединения 2-(2-галоген-4-аминофенил)пиридиновых ингибиторов передачи сигналов белком hedgehog (варианты), способ их получения, композиция и способы лечения рака и ингибирований ангиогенеза и сигнального пути hedgehog в клетках на их основе |
| CA2583812A1 (en) | 2004-10-28 | 2006-05-11 | Irm Llc | Compounds and compositions as hedgehog pathway modulators |
| WO2006093247A1 (ja) | 2005-02-28 | 2006-09-08 | Japan Tobacco Inc. | Ｓｙｋ阻害活性を有する新規なアミノピリジン化合物 |
| AR053272A1 (es) * | 2005-05-11 | 2007-04-25 | Hoffmann La Roche | Determinacion de responsivos a la quimioterapia |
| WO2007054623A2 (en) | 2005-11-11 | 2007-05-18 | Licentia Oy | Mammalian hedgehog signaling inhiabitors |
| EP1957461B1 (en) | 2005-11-14 | 2016-11-02 | Genentech, Inc. | Bisamide inhibitors of hedgehog signaling |
| EP1998777A1 (en) | 2006-03-20 | 2008-12-10 | F. Hoffmann-La Roche AG | Methods of inhibiting btk and syk protein kinases |
| CN101420949A (zh) | 2006-04-14 | 2009-04-29 | 诺瓦提斯公司 | 联芳基甲酰胺类在治疗Hedgehog通路相关病症中的用途 |
| UA93548C2 (uk) | 2006-05-05 | 2011-02-25 | Айерем Елелсі | Сполуки та композиції як модулятори хеджхогівського сигнального шляху |
| ES2542344T3 (es) | 2006-05-09 | 2015-08-04 | Novaremed Ltd. | Uso de inhibidores de tirosina cinasa Syk para el tratamiento de trastornos proliferativos celulares |
| KR101435692B1 (ko) * | 2006-08-08 | 2014-09-01 | 추가이 세이야쿠 가부시키가이샤 | Ｐｉ3ｋ 저해제로서의 피리미딘 유도체 및 그의 용도 |
| JP2010502716A (ja) | 2006-09-07 | 2010-01-28 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | インターロイキン１受容体関連キナーゼの調節物質 |
| CN101616931B (zh) | 2006-10-31 | 2013-08-21 | 美国政府卫生与公共服务部 | Smoothened多肽及使用方法 |
| EP2103619A4 (en) | 2006-12-14 | 2011-11-23 | Daiichi Sankyo Co Ltd | IMIDAZOTHIAZOLDERIVATE |
| TWI433674B (zh) | 2006-12-28 | 2014-04-11 | Infinity Discovery Inc | 環杷明（ｃｙｃｌｏｐａｍｉｎｅ）類似物類 |
| JP2010520310A (ja) | 2007-03-07 | 2010-06-10 | インフィニティ・ディスカバリー・インコーポレイテッド | シクロパミンラクタム類似体及びその使用方法 |
| BRPI0808663A2 (pt) | 2007-03-07 | 2014-08-26 | Infinity Discovery Inc | Análogos de cicloamina heterocíclicos e métodos de uso dos mesmos |
| EP2527330A1 (en) | 2007-03-14 | 2012-11-28 | Exelixis, Inc. | Inhibitors of the hedgehog pathway |
| CN101657430B (zh) | 2007-03-15 | 2013-05-01 | 诺瓦提斯公司 | 有机化合物及其用途 |
| US20090054517A1 (en) | 2007-04-20 | 2009-02-26 | Lubahn Dennis B | Phytoestrogens As Regulators Of Hedgehog Signaling And Methods Of Their Use In Cancer Treatment |
| US20090012031A1 (en) | 2007-07-03 | 2009-01-08 | The Regents Of The University Of Michigan | EZH2 Cancer Markers |
| AU2008335880B2 (en) | 2007-12-13 | 2014-03-13 | Siena Biotech S.P.A. | Hedgehog pathway antagonists and therapeutic applications thereof |
| US8193182B2 (en) * | 2008-01-04 | 2012-06-05 | Intellikine, Inc. | Substituted isoquinolin-1(2H)-ones, and methods of use thereof |
| MX2010007418A (es) | 2008-01-04 | 2010-11-12 | Intellikine Inc | Ciertas entidades quimicas, composiciones y metodos. |
| EP2228350A4 (en) | 2008-01-10 | 2010-12-29 | Asahi Glass Co Ltd | GLASS, COATING MATERIAL FOR LIGHT-EMITTING DEVICE, AND LIGHT-EMITTING DEVICE |
| WO2009089598A2 (en) | 2008-01-18 | 2009-07-23 | Katholieke Universiteit Leuven | Msmb-gene methylation based diagnosis, staging and prognosis of prostate cancer |
| US8637542B2 (en) | 2008-03-14 | 2014-01-28 | Intellikine, Inc. | Kinase inhibitors and methods of use |
| FR2929851B1 (fr) | 2008-04-09 | 2012-11-30 | Centre Nat Rech Scient | Molecules inhibant une voie metabolique impliquant la proteine tyrosine kinase syk et procede d'identification de ces molecules |
| AU2009244897B2 (en) | 2008-04-16 | 2014-11-13 | Alexion Pharmaceuticals, Inc. | 2, 6-diamino- pyrimidin- 5-yl-carboxamides as syk or JAK kinases inhibitors |
| NZ590258A (en) | 2008-07-08 | 2013-10-25 | Intellikine Llc | Kinase inhibitors and methods of use |
| WO2010036380A1 (en) | 2008-09-26 | 2010-04-01 | Intellikine, Inc. | Heterocyclic kinase inhibitors |
| WO2010051550A1 (en) | 2008-10-31 | 2010-05-06 | University Of Rochester | Methods of diagnosing and treating fibrosis |
| PT2355828T (pt) * | 2008-11-13 | 2018-07-02 | Gilead Calistoga Llc | Terapias para malignidades hematológicas |
| US8450321B2 (en) | 2008-12-08 | 2013-05-28 | Gilead Connecticut, Inc. | 6-(1H-indazol-6-yl)-N-[4-(morpholin-4-yl)phenyl]imidazo-[1,2-A]pyrazin-8-amine, or a pharmaceutically acceptable salt thereof, as a SYK inhibitor |
| AU2009325133B2 (en) | 2008-12-08 | 2016-02-04 | Gilead Connecticut, Inc. | Imidazopyrazine Syk inhibitors |
| US8470835B2 (en) | 2009-01-13 | 2013-06-25 | Glaxo Group Limited | Pyrimidinecarboxamide derivatives as inhibitors of Syk kinase |
| CA2751563A1 (en) | 2009-02-04 | 2010-08-12 | Jelena Mann | Methods of inhibiting fibrogenesis and treating fibrotic disease |
| TWI476195B (zh) * | 2009-05-26 | 2015-03-11 | Abbvie Bahamas Ltd | 用於治療癌症及免疫及自體免疫疾病之細胞凋亡誘發劑 |
| SG175708A1 (en) | 2009-05-27 | 2011-12-29 | Genentech Inc | Bicyclic pyrimidine pi3k inhibitor compounds selective for p110 delta, and methods of use |
| US8158625B2 (en) | 2009-05-27 | 2012-04-17 | Genentech, Inc. | Bicyclic indole-pyrimidine PI3K inhibitor compounds selective for P110 delta, and methods of use |
| ES2632220T3 (es) | 2009-06-15 | 2017-09-11 | Rigel Pharmaceuticals, Inc. | Inhibidores de moléculas pequeñas de tirosina cinasa del bazo (SYK) |
| TW201105669A (en) | 2009-07-30 | 2011-02-16 | Irm Llc | Compounds and compositions as Syk kinase inhibitors |
| CN102574847A (zh) | 2009-07-30 | 2012-07-11 | Irm责任有限公司 | 作为syk激酶抑制剂的化合物和组合物 |
| KR20120081164A (ko) | 2009-09-29 | 2012-07-18 | 엑스커버리 홀딩 컴퍼니 엘엘씨 | Ｐｉ3ｋ(델타) 선택적 억제제 |
| EP2512246B1 (en) | 2009-12-17 | 2015-09-30 | Merck Sharp & Dohme Corp. | Aminopyrimidines as syk inhibitors |
| AU2010331927B2 (en) | 2009-12-17 | 2013-10-10 | Merck Canada Inc. | Aminopyrimidines as Syk inhibitors |
| MY159257A (en) | 2009-12-23 | 2016-12-30 | Takeda Pharmaceuticals Co | Fused heteroaromatic pyrrolidinones as syk inhibitors |
| WO2011103016A2 (en) | 2010-02-19 | 2011-08-25 | The Regents Of The University Of Michigan | Compositions and methods for inhibiting ezh2 |
| GB201007203D0 (en) | 2010-04-29 | 2010-06-16 | Glaxo Group Ltd | Novel compounds |
| WO2011146882A1 (en) * | 2010-05-21 | 2011-11-24 | Intellikine, Inc. | Chemical compounds, compositions and methods for kinase modulation |
| JP2013528228A (ja) * | 2010-06-11 | 2013-07-08 | ギリアード カリストガ エルエルシー | キナゾリノン化合物による選択した患者における血液系障害を処置する方法 |
| US20130195843A1 (en) | 2010-06-23 | 2013-08-01 | British Columbia Cancer Agency Branch | Biomarkers for Non-Hodgkin Lymphomas and Uses Thereof |
| US9175331B2 (en) | 2010-09-10 | 2015-11-03 | Epizyme, Inc. | Inhibitors of human EZH2, and methods of use thereof |
| KR102511807B1 (ko) | 2010-09-10 | 2023-03-20 | 에피자임, 인코포레이티드 | 인간 ｅｚｈ2의 억제제 및 이의 사용 방법 |
| US8846928B2 (en) | 2010-11-01 | 2014-09-30 | Portola Pharmaceuticals, Inc. | Benzamides and nicotinamides as Syk modulators |
| EP2637669A4 (en) * | 2010-11-10 | 2014-04-02 | Infinity Pharmaceuticals Inc | Heterocyclic compounds and their use |
| EP2663309B1 (en) * | 2011-01-10 | 2017-03-15 | Infinity Pharmaceuticals, Inc. | Processes for preparing isoquinolinones and solid forms of isoquinolinones |
| WO2012121953A1 (en) * | 2011-03-08 | 2012-09-13 | The Trustees Of Columbia University In The City Of New York | Methods and pharmaceutical compositions for treating lymphoid malignancy |
| EP2704571B1 (en) | 2011-05-04 | 2020-04-22 | Merck Sharp & Dohme Corp. | Amino-pyridine-containing spleen tyrosine kinase (syk) inhibitors |
| TR201812261T4 (tr) * | 2012-11-01 | 2018-11-21 | Infinity Pharmaceuticals Inc | Pi3 ki̇naz i̇zoform modülatörleri̇ i̇le kanser tedavi̇si̇ |
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