RU2005104818A - Азаиндольные ингибиторы киназ - Google Patents
Азаиндольные ингибиторы киназ Download PDFInfo
- Publication number
- RU2005104818A RU2005104818A RU2005104818/04A RU2005104818A RU2005104818A RU 2005104818 A RU2005104818 A RU 2005104818A RU 2005104818/04 A RU2005104818/04 A RU 2005104818/04A RU 2005104818 A RU2005104818 A RU 2005104818A RU 2005104818 A RU2005104818 A RU 2005104818A
- Authority
- RU
- Russia
- Prior art keywords
- substituted
- pyrrolo
- yloxy
- fluoro
- methyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title claims 3
- 150000001875 compounds Chemical class 0.000 claims 15
- 239000001257 hydrogen Substances 0.000 claims 12
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 238000000034 method Methods 0.000 claims 11
- 241000124008 Mammalia Species 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 6
- 229910052760 oxygen Inorganic materials 0.000 claims 6
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 125000000547 substituted alkyl group Chemical group 0.000 claims 5
- 102000009465 Growth Factor Receptors Human genes 0.000 claims 4
- 108010009202 Growth Factor Receptors Proteins 0.000 claims 4
- -1 R 31 Chemical compound 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 239000003937 drug carrier Substances 0.000 claims 4
- 125000000623 heterocyclic group Chemical group 0.000 claims 4
- 230000002401 inhibitory effect Effects 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 230000001093 anti-cancer Effects 0.000 claims 3
- 239000002246 antineoplastic agent Substances 0.000 claims 3
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 229940127089 cytotoxic agent Drugs 0.000 claims 3
- 239000002254 cytotoxic agent Substances 0.000 claims 3
- 231100000599 cytotoxic agent Toxicity 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 239000001301 oxygen Substances 0.000 claims 3
- OMJKVIFSWSQTGQ-UHFFFAOYSA-N 6,7-bis(aziridin-1-yl)quinazoline-5,8-dione Chemical compound C1CN1C=1C(=O)C2=NC=NC=C2C(=O)C=1N1CC1 OMJKVIFSWSQTGQ-UHFFFAOYSA-N 0.000 claims 2
- KDCGOANMDULRCW-UHFFFAOYSA-N 7H-purine Chemical compound N1=CNC2=NC=NC2=C1 KDCGOANMDULRCW-UHFFFAOYSA-N 0.000 claims 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin 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 2
- NWIBSHFKIJFRCO-WUDYKRTCSA-N Mytomycin Chemical compound C1N2C(C(C(C)=C(N)C3=O)=O)=C3[C@@H](COC(N)=O)[C@@]2(OC)[C@@H]2[C@H]1N2 NWIBSHFKIJFRCO-WUDYKRTCSA-N 0.000 claims 2
- 102000001253 Protein Kinase Human genes 0.000 claims 2
- 102000004022 Protein-Tyrosine Kinases Human genes 0.000 claims 2
- 108090000412 Protein-Tyrosine Kinases Proteins 0.000 claims 2
- NKANXQFJJICGDU-QPLCGJKRSA-N Tamoxifen Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN(C)C)=CC=1)/C1=CC=CC=C1 NKANXQFJJICGDU-QPLCGJKRSA-N 0.000 claims 2
- RJURFGZVJUQBHK-UHFFFAOYSA-N actinomycin D Natural products CC1OC(=O)C(C(C)C)N(C)C(=O)CN(C)C(=O)C2CCCN2C(=O)C(C(C)C)NC(=O)C1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)NC4C(=O)NC(C(N5CCCC5C(=O)N(C)CC(=O)N(C)C(C(C)C)C(=O)OC4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-UHFFFAOYSA-N 0.000 claims 2
- 230000001772 anti-angiogenic effect Effects 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- NEHMKBQYUWJMIP-UHFFFAOYSA-N chloromethane Chemical compound ClC NEHMKBQYUWJMIP-UHFFFAOYSA-N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 2
- 108060006633 protein kinase Proteins 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 230000008728 vascular permeability Effects 0.000 claims 2
- NTKPIEALXMYDOX-SECBINFHSA-N (2r)-1-[4-[(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-amine Chemical compound N1=C2NC=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@H](N)C)=C1 NTKPIEALXMYDOX-SECBINFHSA-N 0.000 claims 1
- ACPWZRGLIIWDAZ-SECBINFHSA-N (2r)-1-[4-[(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-ol Chemical compound N1=C2NC=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@H](O)C)=C1 ACPWZRGLIIWDAZ-SECBINFHSA-N 0.000 claims 1
- IEVVBXWLVDGZEQ-SECBINFHSA-N (2r)-1-[4-[(4-fluoro-2-methyl-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-amine Chemical compound N1=C2NC(C)=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@H](N)C)=C1 IEVVBXWLVDGZEQ-SECBINFHSA-N 0.000 claims 1
- SDISWWDGAUTYAI-SNVBAGLBSA-N (2r)-1-[4-[(4-fluoro-2-methyl-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-ol Chemical compound N1=C2NC(C)=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@H](O)C)=C1 SDISWWDGAUTYAI-SNVBAGLBSA-N 0.000 claims 1
- ACPWZRGLIIWDAZ-VIFPVBQESA-N (2s)-1-[4-[(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxypropan-2-ol Chemical compound N1=C2NC=CC2=C(F)C(OC2=NC=NN3C=C(C(=C32)C)OC[C@@H](O)C)=C1 ACPWZRGLIIWDAZ-VIFPVBQESA-N 0.000 claims 1
- LKJPYSCBVHEWIU-KRWDZBQOSA-N (R)-bicalutamide Chemical compound C([C@@](O)(C)C(=O)NC=1C=C(C(C#N)=CC=1)C(F)(F)F)S(=O)(=O)C1=CC=C(F)C=C1 LKJPYSCBVHEWIU-KRWDZBQOSA-N 0.000 claims 1
- LHMXHXQYVFYCCQ-UHFFFAOYSA-N 2-[4-[(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]oxyethanamine Chemical compound N1=C2NC=CC2=C(F)C(OC2=NC=NN3C=C(OCCN)C(=C23)C)=C1 LHMXHXQYVFYCCQ-UHFFFAOYSA-N 0.000 claims 1
- AOJJSUZBOXZQNB-VTZDEGQISA-N 4'-epidoxorubicin 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-VTZDEGQISA-N 0.000 claims 1
- YYOLIACIIOCPPM-UHFFFAOYSA-N 4-[(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)oxy]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-ol Chemical compound N1=C2NC=CC2=C(F)C(OC2=NC=NN3C=C(O)C(=C23)C)=C1 YYOLIACIIOCPPM-UHFFFAOYSA-N 0.000 claims 1
- SGOOQMRIPALTEL-UHFFFAOYSA-N 4-hydroxy-N,1-dimethyl-2-oxo-N-phenyl-3-quinolinecarboxamide Chemical group OC=1C2=CC=CC=C2N(C)C(=O)C=1C(=O)N(C)C1=CC=CC=C1 SGOOQMRIPALTEL-UHFFFAOYSA-N 0.000 claims 1
- OOQXPATWSOGSAV-UHFFFAOYSA-N 6-(5-methyl-1,3,4-oxadiazol-2-yl)-n-(2-methyl-1h-pyrrolo[2,3-b]pyridin-5-yl)-5-propan-2-ylpyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical compound C=1N2N=CN=C(NC=3C=C4C=C(C)NC4=NC=3)C2=C(C(C)C)C=1C1=NN=C(C)O1 OOQXPATWSOGSAV-UHFFFAOYSA-N 0.000 claims 1
- 102000012936 Angiostatins Human genes 0.000 claims 1
- 108010079709 Angiostatins Proteins 0.000 claims 1
- BFYIZQONLCFLEV-DAELLWKTSA-N Aromasine Chemical compound O=C1C=C[C@]2(C)[C@H]3CC[C@](C)(C(CC4)=O)[C@@H]4[C@@H]3CC(=C)C2=C1 BFYIZQONLCFLEV-DAELLWKTSA-N 0.000 claims 1
- 208000023275 Autoimmune disease Diseases 0.000 claims 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- CMSMOCZEIVJLDB-UHFFFAOYSA-N Cyclophosphamide Chemical compound ClCCN(CCCl)P1(=O)NCCCO1 CMSMOCZEIVJLDB-UHFFFAOYSA-N 0.000 claims 1
- UHDGCWIWMRVCDJ-CCXZUQQUSA-N Cytarabine Chemical compound O=C1N=C(N)C=CN1[C@H]1[C@@H](O)[C@H](O)[C@@H](CO)O1 UHDGCWIWMRVCDJ-CCXZUQQUSA-N 0.000 claims 1
- 108010092160 Dactinomycin Proteins 0.000 claims 1
- ZQZFYGIXNQKOAV-OCEACIFDSA-N Droloxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=C(O)C=CC=1)\C1=CC=C(OCCN(C)C)C=C1 ZQZFYGIXNQKOAV-OCEACIFDSA-N 0.000 claims 1
- HTIJFSOGRVMCQR-UHFFFAOYSA-N Epirubicin Natural products COc1cccc2C(=O)c3c(O)c4CC(O)(CC(OC5CC(N)C(=O)C(C)O5)c4c(O)c3C(=O)c12)C(=O)CO HTIJFSOGRVMCQR-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims 1
- 108010069236 Goserelin Proteins 0.000 claims 1
- 101001059454 Homo sapiens Serine/threonine-protein kinase MARK2 Proteins 0.000 claims 1
- XDXDZDZNSLXDNA-TZNDIEGXSA-N Idarubicin Chemical compound C1[C@H](N)[C@H](O)[C@H](C)O[C@H]1O[C@@H]1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2C[C@@](O)(C(C)=O)C1 XDXDZDZNSLXDNA-TZNDIEGXSA-N 0.000 claims 1
- XDXDZDZNSLXDNA-UHFFFAOYSA-N Idarubicin Natural products C1C(N)C(O)C(C)OC1OC1C2=C(O)C(C(=O)C3=CC=CC=C3C3=O)=C3C(O)=C2CC(O)(C(C)=O)C1 XDXDZDZNSLXDNA-UHFFFAOYSA-N 0.000 claims 1
- JJKOTMDDZAJTGQ-DQSJHHFOSA-N Idoxifene Chemical compound C=1C=CC=CC=1C(/CC)=C(C=1C=CC(OCCN2CCCC2)=CC=1)/C1=CC=C(I)C=C1 JJKOTMDDZAJTGQ-DQSJHHFOSA-N 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- FBOZXECLQNJBKD-ZDUSSCGKSA-N L-methotrexate Chemical compound C=1N=C2N=C(N)N=C(N)C2=NC=1CN(C)C1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 FBOZXECLQNJBKD-ZDUSSCGKSA-N 0.000 claims 1
- 108010000817 Leuprolide Proteins 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 229940079156 Proteasome inhibitor Drugs 0.000 claims 1
- 102100028904 Serine/threonine-protein kinase MARK2 Human genes 0.000 claims 1
- FOCVUCIESVLUNU-UHFFFAOYSA-N Thiotepa Chemical compound C1CN1P(N1CC1)(=S)N1CC1 FOCVUCIESVLUNU-UHFFFAOYSA-N 0.000 claims 1
- 102000003990 Urokinase-type plasminogen activator Human genes 0.000 claims 1
- 108090000435 Urokinase-type plasminogen activator Proteins 0.000 claims 1
- RJURFGZVJUQBHK-IIXSONLDSA-N actinomycin D Chemical compound C[C@H]1OC(=O)[C@H](C(C)C)N(C)C(=O)CN(C)C(=O)[C@@H]2CCCN2C(=O)[C@@H](C(C)C)NC(=O)[C@H]1NC(=O)C1=C(N)C(=O)C(C)=C2OC(C(C)=CC=C3C(=O)N[C@@H]4C(=O)N[C@@H](C(N5CCC[C@H]5C(=O)N(C)CC(=O)N(C)[C@@H](C(C)C)C(=O)O[C@@H]4C)=O)C(C)C)=C3N=C21 RJURFGZVJUQBHK-IIXSONLDSA-N 0.000 claims 1
- 239000012190 activator Substances 0.000 claims 1
- 150000003838 adenosines Chemical class 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- XCPGHVQEEXUHNC-UHFFFAOYSA-N amsacrine Chemical compound COC1=CC(NS(C)(=O)=O)=CC=C1NC1=C(C=CC=C2)C2=NC2=CC=CC=C12 XCPGHVQEEXUHNC-UHFFFAOYSA-N 0.000 claims 1
- 229960001220 amsacrine Drugs 0.000 claims 1
- 229960002932 anastrozole Drugs 0.000 claims 1
- YBBLVLTVTVSKRW-UHFFFAOYSA-N anastrozole Chemical compound N#CC(C)(C)C1=CC(C(C)(C#N)C)=CC(CN2N=CN=C2)=C1 YBBLVLTVTVSKRW-UHFFFAOYSA-N 0.000 claims 1
- 229940045719 antineoplastic alkylating agent nitrosoureas Drugs 0.000 claims 1
- FZCSTZYAHCUGEM-UHFFFAOYSA-N aspergillomarasmine B Natural products OC(=O)CNC(C(O)=O)CNC(C(O)=O)CC(O)=O FZCSTZYAHCUGEM-UHFFFAOYSA-N 0.000 claims 1
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims 1
- 229960000397 bevacizumab Drugs 0.000 claims 1
- 229960000997 bicalutamide Drugs 0.000 claims 1
- BGECDVWSWDRFSP-UHFFFAOYSA-N borazine Chemical compound B1NBNBN1 BGECDVWSWDRFSP-UHFFFAOYSA-N 0.000 claims 1
- 229960001467 bortezomib Drugs 0.000 claims 1
- GXJABQQUPOEUTA-RDJZCZTQSA-N bortezomib Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)B(O)O)NC(=O)C=1N=CC=NC=1)C1=CC=CC=C1 GXJABQQUPOEUTA-RDJZCZTQSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229960004562 carboplatin Drugs 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 229960004630 chlorambucil Drugs 0.000 claims 1
- JCKYGMPEJWAADB-UHFFFAOYSA-N chlorambucil Chemical compound OC(=O)CCCC1=CC=C(N(CCCl)CCCl)C=C1 JCKYGMPEJWAADB-UHFFFAOYSA-N 0.000 claims 1
- 229910052801 chlorine Inorganic materials 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 229960004397 cyclophosphamide Drugs 0.000 claims 1
- 229960000978 cyproterone acetate Drugs 0.000 claims 1
- UWFYSQMTEOIJJG-FDTZYFLXSA-N cyproterone acetate Chemical compound C1=C(Cl)C2=CC(=O)[C@@H]3C[C@@H]3[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 UWFYSQMTEOIJJG-FDTZYFLXSA-N 0.000 claims 1
- 229960000640 dactinomycin Drugs 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 229950004203 droloxifene Drugs 0.000 claims 1
- XOPYFXBZMVTEJF-PDACKIITSA-N eleutherobin Chemical compound C(/[C@H]1[C@H](C(=CC[C@@H]1C(C)C)C)C[C@@H]([C@@]1(C)O[C@@]2(C=C1)OC)OC(=O)\C=C\C=1N=CN(C)C=1)=C2\CO[C@@H]1OC[C@@H](O)[C@@H](O)[C@@H]1OC(C)=O XOPYFXBZMVTEJF-PDACKIITSA-N 0.000 claims 1
- XOPYFXBZMVTEJF-UHFFFAOYSA-N eleutherobin Natural products C1=CC2(OC)OC1(C)C(OC(=O)C=CC=1N=CN(C)C=1)CC(C(=CCC1C(C)C)C)C1C=C2COC1OCC(O)C(O)C1OC(C)=O XOPYFXBZMVTEJF-UHFFFAOYSA-N 0.000 claims 1
- 229960001904 epirubicin Drugs 0.000 claims 1
- 229930013356 epothilone Natural products 0.000 claims 1
- 150000003883 epothilone derivatives Chemical class 0.000 claims 1
- VJJPUSNTGOMMGY-MRVIYFEKSA-N etoposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@H](C)OC[C@H]4O3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 VJJPUSNTGOMMGY-MRVIYFEKSA-N 0.000 claims 1
- 229960005420 etoposide Drugs 0.000 claims 1
- 229960000255 exemestane Drugs 0.000 claims 1
- 229960004039 finasteride Drugs 0.000 claims 1
- DBEPLOCGEIEOCV-WSBQPABSSA-N finasteride Chemical compound N([C@@H]1CC2)C(=O)C=C[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H](C(=O)NC(C)(C)C)[C@@]2(C)CC1 DBEPLOCGEIEOCV-WSBQPABSSA-N 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 229960002949 fluorouracil Drugs 0.000 claims 1
- 229960002074 flutamide Drugs 0.000 claims 1
- MKXKFYHWDHIYRV-UHFFFAOYSA-N flutamide Chemical compound CC(C)C(=O)NC1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 MKXKFYHWDHIYRV-UHFFFAOYSA-N 0.000 claims 1
- 229960003690 goserelin acetate Drugs 0.000 claims 1
- 239000003102 growth factor Substances 0.000 claims 1
- 229940022353 herceptin Drugs 0.000 claims 1
- 229960000908 idarubicin Drugs 0.000 claims 1
- 229960001101 ifosfamide Drugs 0.000 claims 1
- HOMGKSMUEGBAAB-UHFFFAOYSA-N ifosfamide Chemical compound ClCCNP1(=O)OCCCN1CCCl HOMGKSMUEGBAAB-UHFFFAOYSA-N 0.000 claims 1
- 239000000367 immunologic factor Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 108010044426 integrins Chemical group 0.000 claims 1
- 102000006495 integrins Human genes 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 229960003881 letrozole Drugs 0.000 claims 1
- HPJKCIUCZWXJDR-UHFFFAOYSA-N letrozole Chemical compound C1=CC(C#N)=CC=C1C(N1N=CN=C1)C1=CC=C(C#N)C=C1 HPJKCIUCZWXJDR-UHFFFAOYSA-N 0.000 claims 1
- 229960004961 mechlorethamine Drugs 0.000 claims 1
- HAWPXGHAZFHHAD-UHFFFAOYSA-N mechlorethamine Chemical compound ClCCN(C)CCCl HAWPXGHAZFHHAD-UHFFFAOYSA-N 0.000 claims 1
- 229960004296 megestrol acetate Drugs 0.000 claims 1
- RQZAXGRLVPAYTJ-GQFGMJRRSA-N megestrol acetate Chemical compound C1=C(C)C2=CC(=O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@@](C(C)=O)(OC(=O)C)[C@@]1(C)CC2 RQZAXGRLVPAYTJ-GQFGMJRRSA-N 0.000 claims 1
- 229960001924 melphalan Drugs 0.000 claims 1
- SGDBTWWWUNNDEQ-LBPRGKRZSA-N melphalan Chemical compound OC(=O)[C@@H](N)CC1=CC=C(N(CCCl)CCCl)C=C1 SGDBTWWWUNNDEQ-LBPRGKRZSA-N 0.000 claims 1
- 239000003475 metalloproteinase inhibitor Substances 0.000 claims 1
- 229960000485 methotrexate Drugs 0.000 claims 1
- CFCUWKMKBJTWLW-BKHRDMLASA-N mithramycin Chemical compound O([C@@H]1C[C@@H](O[C@H](C)[C@H]1O)OC=1C=C2C=C3C[C@H]([C@@H](C(=O)C3=C(O)C2=C(O)C=1C)O[C@@H]1O[C@H](C)[C@@H](O)[C@H](O[C@@H]2O[C@H](C)[C@H](O)[C@H](O[C@@H]3O[C@H](C)[C@@H](O)[C@@](C)(O)C3)C2)C1)[C@H](OC)C(=O)[C@@H](O)[C@@H](C)O)[C@H]1C[C@@H](O)[C@H](O)[C@@H](C)O1 CFCUWKMKBJTWLW-BKHRDMLASA-N 0.000 claims 1
- 229960004857 mitomycin Drugs 0.000 claims 1
- DNLFTHMQMOVEOZ-UHFFFAOYSA-N n-(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)-6-(3-methyl-1,2,4-oxadiazol-5-yl)-5-propan-2-ylpyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical compound C=1N2N=CN=C(NC=3C(=C4C=CNC4=NC=3)F)C2=C(C(C)C)C=1C1=NC(C)=NO1 DNLFTHMQMOVEOZ-UHFFFAOYSA-N 0.000 claims 1
- CIANRPXQIFFCFG-UHFFFAOYSA-N n-(4-fluoro-1h-pyrrolo[2,3-b]pyridin-5-yl)-6-(5-methyl-1,3,4-oxadiazol-2-yl)-5-propan-2-ylpyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical compound C=1N2N=CN=C(NC=3C(=C4C=CNC4=NC=3)F)C2=C(C(C)C)C=1C1=NN=C(C)O1 CIANRPXQIFFCFG-UHFFFAOYSA-N 0.000 claims 1
- IXYUGLGTMIXVHB-UHFFFAOYSA-N n-(4-fluoro-2-methyl-1h-pyrrolo[2,3-b]pyridin-5-yl)-6-(5-methyl-1,3,4-oxadiazol-2-yl)-5-propan-2-ylpyrrolo[2,1-f][1,2,4]triazin-4-amine Chemical compound C=1N2N=CN=C(NC=3C(=C4C=C(C)NC4=NC=3)F)C2=C(C(C)C)C=1C1=NN=C(C)O1 IXYUGLGTMIXVHB-UHFFFAOYSA-N 0.000 claims 1
- BLCLNMBMMGCOAS-UHFFFAOYSA-N n-[1-[[1-[[1-[[1-[[1-[[1-[[1-[2-[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amin Chemical compound C1CCC(C(=O)NNC(N)=O)N1C(=O)C(CCCN=C(N)N)NC(=O)C(CC(C)C)NC(=O)C(COC(C)(C)C)NC(=O)C(NC(=O)C(CO)NC(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C(CC=1NC=NC=1)NC(=O)C1NC(=O)CC1)CC1=CC=C(O)C=C1 BLCLNMBMMGCOAS-UHFFFAOYSA-N 0.000 claims 1
- 229960002653 nilutamide Drugs 0.000 claims 1
- XWXYUMMDTVBTOU-UHFFFAOYSA-N nilutamide Chemical compound O=C1C(C)(C)NC(=O)N1C1=CC=C([N+]([O-])=O)C(C(F)(F)F)=C1 XWXYUMMDTVBTOU-UHFFFAOYSA-N 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 229960003171 plicamycin Drugs 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 239000003207 proteasome inhibitor Substances 0.000 claims 1
- 229960004622 raloxifene Drugs 0.000 claims 1
- GZUITABIAKMVPG-UHFFFAOYSA-N raloxifene Chemical compound C1=CC(O)=CC=C1C1=C(C(=O)C=2C=CC(OCCN3CCCCC3)=CC=2)C2=CC=C(O)C=C2S1 GZUITABIAKMVPG-UHFFFAOYSA-N 0.000 claims 1
- 102000005962 receptors Human genes 0.000 claims 1
- 108020003175 receptors Proteins 0.000 claims 1
- 229960003522 roquinimex Drugs 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 230000019491 signal transduction Effects 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 1
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 1
- 229960001603 tamoxifen Drugs 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- NRUKOCRGYNPUPR-QBPJDGROSA-N teniposide Chemical compound COC1=C(O)C(OC)=CC([C@@H]2C3=CC=4OCOC=4C=C3[C@@H](O[C@H]3[C@@H]([C@@H](O)[C@@H]4O[C@@H](OC[C@H]4O3)C=3SC=CC=3)O)[C@@H]3[C@@H]2C(OC3)=O)=C1 NRUKOCRGYNPUPR-QBPJDGROSA-N 0.000 claims 1
- 229960001278 teniposide Drugs 0.000 claims 1
- 229960001196 thiotepa Drugs 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 229960005026 toremifene Drugs 0.000 claims 1
- XFCLJVABOIYOMF-QPLCGJKRSA-N toremifene Chemical compound C1=CC(OCCN(C)C)=CC=C1C(\C=1C=CC=CC=1)=C(\CCCl)C1=CC=CC=C1 XFCLJVABOIYOMF-QPLCGJKRSA-N 0.000 claims 1
- 229940121358 tyrosine kinase inhibitor Drugs 0.000 claims 1
- 239000005483 tyrosine kinase inhibitor Substances 0.000 claims 1
- 229960005356 urokinase 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
- 229960004528 vincristine Drugs 0.000 claims 1
- OGWKCGZFUXNPDA-UHFFFAOYSA-N vincristine Natural products C1C(CC)(O)CC(CC2(C(=O)OC)C=3C(=CC4=C(C56C(C(C(OC(C)=O)C7(CC)C=CCN(C67)CC5)(O)C(=O)OC)N4C=O)C=3)OC)CN1CCC1=C2NC2=CC=CC=C12 OGWKCGZFUXNPDA-UHFFFAOYSA-N 0.000 claims 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/10—Drugs for disorders of the urinary system of the bladder
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P21/00—Drugs for disorders of the muscular or neuromuscular system
- A61P21/04—Drugs for disorders of the muscular or neuromuscular system for myasthenia gravis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
- A61P25/16—Anti-Parkinson drugs
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/10—Antimycotics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/20—Antivirals for DNA viruses
- A61P31/22—Antivirals for DNA viruses for herpes viruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/04—Immunostimulants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/06—Antianaemics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/06—Antiarrhythmics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/08—Vasodilators for multiple indications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Virology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Physical Education & Sports Medicine (AREA)
- Oncology (AREA)
- Diabetes (AREA)
- Epidemiology (AREA)
- Communicable Diseases (AREA)
- Urology & Nephrology (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Rheumatology (AREA)
- Hematology (AREA)
- Dermatology (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US39725602P | 2002-07-19 | 2002-07-19 | |
| US60/397256 | 2002-07-19 | ||
| US44721303P | 2003-02-13 | 2003-02-13 | |
| US60/447213 | 2003-02-13 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| RU2005104818A true RU2005104818A (ru) | 2005-07-20 |
Family
ID=30773005
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005104818/04A RU2005104818A (ru) | 2002-07-19 | 2003-07-18 | Азаиндольные ингибиторы киназ |
| RU2005104422/04A RU2331642C2 (ru) | 2002-07-19 | 2003-07-18 | Новые ингибиторы киназ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| RU2005104422/04A RU2331642C2 (ru) | 2002-07-19 | 2003-07-18 | Новые ингибиторы киназ |
Country Status (32)
| Country | Link |
|---|---|
| US (6) | US6869952B2 (Direct) |
| EP (3) | EP2280012A3 (Direct) |
| JP (2) | JP4361485B2 (Direct) |
| KR (1) | KR100901939B1 (Direct) |
| CN (3) | CN1315833C (Direct) |
| AR (1) | AR040500A1 (Direct) |
| AT (2) | ATE505471T1 (Direct) |
| AU (2) | AU2003254017A1 (Direct) |
| BR (2) | BRPI0312940B1 (Direct) |
| CA (2) | CA2492665A1 (Direct) |
| CO (1) | CO5680407A2 (Direct) |
| CY (1) | CY1112628T1 (Direct) |
| DE (1) | DE60336732D1 (Direct) |
| DK (1) | DK1534290T3 (Direct) |
| ES (1) | ES2377963T3 (Direct) |
| GE (2) | GEP20074124B (Direct) |
| HR (2) | HRP20050058A2 (Direct) |
| IL (3) | IL166129A0 (Direct) |
| IS (2) | IS7646A (Direct) |
| MX (2) | MXPA05000716A (Direct) |
| MY (1) | MY134848A (Direct) |
| NO (2) | NO330132B1 (Direct) |
| NZ (1) | NZ537523A (Direct) |
| PE (1) | PE20040680A1 (Direct) |
| PL (2) | PL216663B1 (Direct) |
| PT (1) | PT1534290E (Direct) |
| RS (2) | RS52325B (Direct) |
| RU (2) | RU2005104818A (Direct) |
| SI (1) | SI1534290T1 (Direct) |
| TW (1) | TWI329112B (Direct) |
| UA (1) | UA82846C2 (Direct) |
| WO (2) | WO2004009784A2 (Direct) |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2404765C2 (ru) * | 2005-08-26 | 2010-11-27 | Антисома Рисерч Лимитед | Комбинации (составы), включающие dmxaa для лечения рака |
| CN116813526A (zh) * | 2023-05-22 | 2023-09-29 | 四川省医学科学院·四川省人民医院 | 异吲哚啉酮类化合物、其制备方法及其应用 |
Families Citing this family (217)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP4579351B2 (ja) * | 1996-12-03 | 2010-11-10 | スローン−ケッタリング インスティトュート フォア キャンサー リサーチ | エポチロンの合成とその中間体及びその類似物並びにその使用 |
| EP0881669B1 (en) * | 1997-05-30 | 2005-12-14 | STMicroelectronics S.r.l. | Manufacturing process of a germanium implanted heterojunction bipolar transistor |
| US20020058286A1 (en) * | 1999-02-24 | 2002-05-16 | Danishefsky Samuel J. | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6982265B1 (en) * | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| US6867300B2 (en) | 2000-11-17 | 2005-03-15 | Bristol-Myers Squibb Company | Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors |
| US6670357B2 (en) * | 2000-11-17 | 2003-12-30 | Bristol-Myers Squibb Company | Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors |
| TW200300350A (en) * | 2001-11-14 | 2003-06-01 | Bristol Myers Squibb Co | C-5 modified indazolylpyrrolotriazines |
| ATE418546T1 (de) | 2002-04-23 | 2009-01-15 | Bristol Myers Squibb Co | Als kinase inhibitoren geeignete arylketonpyrrolotriazin-verbindungen |
| WO2003090912A1 (en) | 2002-04-23 | 2003-11-06 | Bristol-Myers Squibb Company | Pyrrolo-triazine aniline compounds useful as kinase inhibitors |
| TW200401638A (en) * | 2002-06-20 | 2004-02-01 | Bristol Myers Squibb Co | Heterocyclic inhibitors of kinases |
| TWI329112B (en) * | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| NZ538522A (en) * | 2002-08-23 | 2008-03-28 | Sloan Kettering Inst Cancer | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| TW200420565A (en) | 2002-12-13 | 2004-10-16 | Bristol Myers Squibb Co | C-6 modified indazolylpyrrolotriazines |
| PL378121A1 (pl) | 2003-02-05 | 2006-03-06 | Bristol-Myers Squibb Company | Sposób wytwarzania pirolotriazynowych inhibitorów kinazy |
| BRPI0412885A (pt) | 2003-07-18 | 2006-10-03 | Amgen Inc | polipeptìdios, agentes de ligação especìficos, moléculas de ácido nucleico e linhas de células isoladas, células hospedeiras, composições e anticorpo ou domìnio de ligação de antìgeno e métodos de tratamento de cáncer e de tumor sólido num paciente, de detecção do nìvel do fator de crescimento hepatócito (hgf) numa amostra, de obtenção de anticorpo e de inibição da ligação de hgf a met e de diminuição ou prevenção da ligação de qualquer um dos agentes de ligação especìficos ao fator de crescimento hepatócito (hgf) |
| US7102001B2 (en) | 2003-12-12 | 2006-09-05 | Bristol-Myers Squibb Company | Process for preparing pyrrolotriazine |
| US20060014741A1 (en) * | 2003-12-12 | 2006-01-19 | Dimarco John D | Synthetic process, and crystalline forms of a pyrrolotriazine compound |
| US7064203B2 (en) | 2003-12-29 | 2006-06-20 | Bristol Myers Squibb Company | Di-substituted pyrrolotriazine compounds |
| MY145634A (en) | 2003-12-29 | 2012-03-15 | Bristol Myers Squibb Co | Pyrrolotriazine compounds as kinase inhibitors |
| US7459562B2 (en) * | 2004-04-23 | 2008-12-02 | Bristol-Myers Squibb Company | Monocyclic heterocycles as kinase inhibitors |
| TW200538453A (en) * | 2004-04-26 | 2005-12-01 | Bristol Myers Squibb Co | Bicyclic heterocycles as kinase inhibitors |
| US7102002B2 (en) * | 2004-06-16 | 2006-09-05 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US7498342B2 (en) | 2004-06-17 | 2009-03-03 | Plexxikon, Inc. | Compounds modulating c-kit activity |
| US7439246B2 (en) * | 2004-06-28 | 2008-10-21 | Bristol-Myers Squibb Company | Fused heterocyclic kinase inhibitors |
| US7432373B2 (en) * | 2004-06-28 | 2008-10-07 | Bristol-Meyers Squibb Company | Processes and intermediates useful for preparing fused heterocyclic kinase inhibitors |
| US20050288290A1 (en) * | 2004-06-28 | 2005-12-29 | Borzilleri Robert M | Fused heterocyclic kinase inhibitors |
| CN101005843A (zh) * | 2004-06-28 | 2007-07-25 | 布里斯托尔-迈尔斯·斯奎布公司 | 吡咯并三嗪激酶抑制剂 |
| US7253167B2 (en) * | 2004-06-30 | 2007-08-07 | Bristol-Myers Squibb Company | Tricyclic-heteroaryl compounds useful as kinase inhibitors |
| TW200600513A (en) * | 2004-06-30 | 2006-01-01 | Bristol Myers Squibb Co | A method for preparing pyrrolotriazine compounds |
| US7102003B2 (en) * | 2004-07-01 | 2006-09-05 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds |
| SE0401790D0 (sv) * | 2004-07-07 | 2004-07-07 | Forskarpatent I Syd Ab | Tamoxifen response in pre- and postmenopausal breast cancer patients |
| US7504521B2 (en) | 2004-08-05 | 2009-03-17 | Bristol-Myers Squibb Co. | Methods for the preparation of pyrrolotriazine compounds |
| PE20060421A1 (es) | 2004-08-12 | 2006-06-01 | Bristol Myers Squibb Co | Procedimiento para preparar un compuesto de pirrolotriazina anilina como inhibidores de cinasa |
| US7151176B2 (en) * | 2004-10-21 | 2006-12-19 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds |
| MX2007006230A (es) | 2004-11-30 | 2007-07-25 | Amgen Inc | Quinolinas y analogos de quinazolinas y su uso como medicamentos para tratar cancer. |
| DE102004060659A1 (de) | 2004-12-15 | 2006-07-06 | Lanxess Deutschland Gmbh | Neue substituierte 1H-Pyrrolo[2,3-b]pyridine und deren Herstellung |
| US7534882B2 (en) | 2005-04-06 | 2009-05-19 | Bristol-Myers Squibb Company | Method for preparing pyrrolotriazine compounds via in situ amination of pyrroles |
| US20060257400A1 (en) * | 2005-05-13 | 2006-11-16 | Bristol-Myers Squibb Company | Combination therapy |
| EP1885723A2 (en) | 2005-05-17 | 2008-02-13 | Plexxikon, Inc. | Pyrrolo[2,3-b]pyridine derivatives as protein kinase inhibitors |
| US7393667B2 (en) | 2005-05-31 | 2008-07-01 | Bristol-Myers Squibb Company | Stereoselective reduction process for the preparation of pyrrolotriazine compounds |
| US20060288309A1 (en) * | 2005-06-16 | 2006-12-21 | Cross Charles W Jr | Displaying available menu choices in a multimodal browser |
| WO2007002325A1 (en) | 2005-06-22 | 2007-01-04 | Plexxikon, Inc. | Pyrrolo[2,3-b] pyridine derivatives as protein kinase inhibitors |
| US7405213B2 (en) * | 2005-07-01 | 2008-07-29 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith |
| US7442700B2 (en) * | 2005-07-01 | 2008-10-28 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith |
| US7402582B2 (en) * | 2005-07-01 | 2008-07-22 | Bristol-Myers Squibb Company | Pyrrolotriazine compounds useful as kinase inhibitors and methods of treating kinase-associated conditions therewith |
| JP4994379B2 (ja) | 2005-09-01 | 2012-08-08 | ブリストル−マイヤーズ スクイブ カンパニー | 血管内皮成長因子受容体−2モジュレーターに対する感受性を決定するためのバイオマーカーおよび方法 |
| JP2009511440A (ja) * | 2005-09-27 | 2009-03-19 | ブリストル−マイヤーズ スクイブ カンパニー | [(1R),2S]−2−アミノプロピオン酸2−[4−(4−フルオロ−2−メチル−1H−インドール−5−イルオキシ)−5−メチルピロロ[2,1−f][1,2,4]トリアジン−6−イルオキシ]−1−メチルエチルエステルの結晶形 |
| US7547782B2 (en) * | 2005-09-30 | 2009-06-16 | Bristol-Myers Squibb Company | Met kinase inhibitors |
| US7514435B2 (en) * | 2005-11-18 | 2009-04-07 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP1957485B1 (en) | 2005-12-02 | 2013-02-13 | Bayer HealthCare, LLC | Substituted 4-amino-pyrrolotriazine derivatives useful for treating hyper-proliferative disorders and diseases associated with angiogenesis |
| PE20070855A1 (es) | 2005-12-02 | 2007-10-14 | Bayer Pharmaceuticals Corp | Derivados de 4-amino-pirrolotriazina sustituida como inhibidores de quinasas |
| US20080108664A1 (en) | 2005-12-23 | 2008-05-08 | Liu Belle B | Solid-state form of AMG 706 and pharmaceutical compositions thereof |
| AR059066A1 (es) | 2006-01-27 | 2008-03-12 | Amgen Inc | Combinaciones del inhibidor de la angiopoyetina -2 (ang2) y el inhibidor del factor de crecimiento endotelial vascular (vegf) |
| JP2009526050A (ja) | 2006-02-10 | 2009-07-16 | アムジエン・インコーポレーテツド | Amg706の水和物形態 |
| US8063208B2 (en) | 2006-02-16 | 2011-11-22 | Bristol-Myers Squibb Company | Crystalline forms of (3R,4R)-4-amino-1-[[4-[(3-methoxyphenyl)amino]pyrrolo[2,1-f][1,2,4]triazin-5-yl]methyl]piperidin-3-ol |
| JP2009535295A (ja) | 2006-03-07 | 2009-10-01 | ブリストル−マイヤーズ スクイブ カンパニー | キナーゼ阻害剤として有用なピロロトリアジンアニリンプロドラッグ化合物 |
| KR101423789B1 (ko) * | 2006-04-21 | 2014-07-30 | 브리스톨-마이어스 스큅 컴퍼니 | [(1R), 2S]-2-아미노프로피온산 2-[4-(4-플루오로-2-메틸-1H-인돌-5-일옥시)-5-메틸피롤로[2,1-f][1,2,4]트리아진-6-일옥시]-1-메틸에틸 에스테르의 제조 방법 |
| ATE537450T1 (de) | 2006-06-30 | 2011-12-15 | Schering Corp | Igfbp2-biomarker |
| AU2007269163B2 (en) * | 2006-07-07 | 2011-07-28 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| PE20121506A1 (es) | 2006-07-14 | 2012-11-26 | Amgen Inc | Compuestos triazolopiridinas como inhibidores de c-met |
| US8217177B2 (en) | 2006-07-14 | 2012-07-10 | Amgen Inc. | Fused heterocyclic derivatives and methods of use |
| US7531539B2 (en) * | 2006-08-09 | 2009-05-12 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| EP2049542B1 (en) * | 2006-08-09 | 2012-09-19 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| US7851623B2 (en) * | 2006-11-02 | 2010-12-14 | Astrazeneca Ab | Chemical process |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| WO2008079291A2 (en) | 2006-12-20 | 2008-07-03 | Amgen Inc. | Substituted heterocycles and methods of use |
| US7872018B2 (en) | 2006-12-21 | 2011-01-18 | Plexxikon, Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2008079909A1 (en) * | 2006-12-21 | 2008-07-03 | Plexxikon, Inc. | Pyrrolo [2,3-b] pyridines as kinase modulators |
| PE20081581A1 (es) | 2006-12-21 | 2008-11-12 | Plexxikon Inc | COMPUESTOS PIRROLO[2,3-b]PIRIDINAS COMO MODULADORES DE QUINASA |
| CN101627027B (zh) * | 2007-01-05 | 2013-06-19 | 百时美施贵宝公司 | 氨基吡唑激酶抑制剂 |
| EP2118069B1 (en) | 2007-01-09 | 2014-01-01 | Amgen Inc. | Bis-aryl amide derivatives useful for the treatment of cancer |
| US7820421B2 (en) | 2007-02-08 | 2010-10-26 | Codexis, Inc. | Ketoreductases and uses thereof |
| US8314087B2 (en) | 2007-02-16 | 2012-11-20 | Amgen Inc. | Nitrogen-containing heterocyclyl ketones and methods of use |
| WO2008127526A2 (en) * | 2007-03-12 | 2008-10-23 | Bristol-Myers Squibb Company | Biomarkers and methods for determining sensitivity to vascular endothelial growth factor receptor-2 modulators |
| KR20090128474A (ko) | 2007-04-13 | 2009-12-15 | 브리스톨-마이어스 스큅 컴퍼니 | 혈관 내피 성장인자 수용체-2 조절제에 대한 감수성을 판정하기 위한 방법 및 바이오마커 |
| EP2134716A1 (en) * | 2007-04-18 | 2009-12-23 | Bristol-Myers Squibb Company | Pyrrolotriazine kinase inhibitors |
| TW200902019A (en) * | 2007-04-26 | 2009-01-16 | Ono Pharmaceutical Co | Dicyclic heterocyclic compound |
| SG183036A1 (en) | 2007-07-17 | 2012-08-30 | Plexxikon Inc | Compounds and methods for kinase modulation, and indications therefor |
| EA023555B1 (ru) | 2007-08-21 | 2016-06-30 | Амген Инк. | АНТИГЕНСВЯЗЫВАЮЩИЕ БЕЛКИ, СВЯЗЫВАЮЩИЕ c-fms ЧЕЛОВЕКА |
| MX2010004327A (es) | 2007-10-22 | 2010-05-13 | Schering Corp | Anticuerpos anti-vegf completamente humanos y metodos de uso. |
| US20110086850A1 (en) * | 2008-04-11 | 2011-04-14 | Board Of Regents, The University Of Texas System | Radiosensitization of tumors with indazolpyrrolotriazines for radiotherapy |
| AR071717A1 (es) | 2008-05-13 | 2010-07-07 | Array Biopharma Inc | Pirrolo[2,3-b]piridinas inhibidoras de quinasas chk1 y chk2,composiciones farmaceuticas que las contienen,proceso para prepararlas y uso de las mismas en el tratamiento y prevencion del cancer. |
| WO2010071885A1 (en) | 2008-12-19 | 2010-06-24 | Cephalon, Inc. | Pyrrolotriazines as alk and jak2 inhibitors |
| WO2010099139A2 (en) | 2009-02-25 | 2010-09-02 | Osi Pharmaceuticals, Inc. | Combination anti-cancer therapy |
| WO2010099138A2 (en) | 2009-02-27 | 2010-09-02 | Osi Pharmaceuticals, Inc. | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| US8642834B2 (en) | 2009-02-27 | 2014-02-04 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| US8465912B2 (en) | 2009-02-27 | 2013-06-18 | OSI Pharmaceuticals, LLC | Methods for the identification of agents that inhibit mesenchymal-like tumor cells or their formation |
| AU2010232670B2 (en) | 2009-04-03 | 2015-07-09 | F. Hoffmann-La Roche Ag | Propane- I-sulfonic acid {3- [5- (4 -chloro-phenyl) -1H-pyrrolo [2, 3-b] pyridine-3-carbonyl] -2, 4-difluoro-pheny l } -amide compositions and uses thereof |
| US8329724B2 (en) | 2009-08-03 | 2012-12-11 | Hoffmann-La Roche Inc. | Process for the manufacture of pharmaceutically active compounds |
| JP2013506687A (ja) | 2009-09-30 | 2013-02-28 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | オートファジー促進遺伝子産物の変調によりオートファジーを変調する方法 |
| US8778893B2 (en) * | 2009-10-05 | 2014-07-15 | Bristol-Myers Squibb Company | (R)-1-(4-(4-fluoro-2-methyl-1H-indol-5-yloxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yloxy)propan-2-ol metabolites |
| ES2633317T3 (es) | 2009-11-06 | 2017-09-20 | Plexxikon, Inc. | Compuestos y métodos para la modulación de quinasas, e indicaciones para ello |
| EP2512476A1 (en) | 2009-12-18 | 2012-10-24 | Novartis AG | Method for treating haematological cancers |
| EP2937345B1 (en) | 2009-12-29 | 2018-03-21 | Dana-Farber Cancer Institute, Inc. | Type ii raf kinase inhibitors |
| EP2531507A1 (en) * | 2010-02-03 | 2012-12-12 | Bristol-Myers Squibb Company | Crystalline forms of (s)-1-(4-(5-cyclopropyl-1h-pyrazol-3- ylamino)pyrrolo [1,2-f][1,2,4]triazin-2-yl)-n-(6-fluoropyridin- 3-yl)-2-methylpyrrolidine-2-carboxamide |
| JP5093527B2 (ja) * | 2010-02-10 | 2012-12-12 | 日本電気株式会社 | 複合光導波路、波長可変フィルタ、波長可変レーザ、および光集積回路 |
| WO2011161217A2 (en) | 2010-06-23 | 2011-12-29 | Palacký University in Olomouc | Targeting of vegfr2 |
| US20130178517A1 (en) * | 2010-07-09 | 2013-07-11 | Richard L. Atkinson | Methods And Compositions For Treatment Of Lipogenic Virus Related Conditions |
| US8338771B2 (en) * | 2010-11-05 | 2012-12-25 | Green Plus Co., Ltd. | Apparatus for tracking and condensing sunlight of sliding type |
| CN103517710B (zh) | 2011-02-07 | 2017-05-31 | 普莱希科公司 | 用于激酶调节的化合物 |
| TWI558702B (zh) | 2011-02-21 | 2016-11-21 | 普雷辛肯公司 | 醫藥活性物質的固態形式 |
| ES2620521T3 (es) | 2011-03-23 | 2017-06-28 | Amgen Inc. | Inhibidores duales tricíclicos condensados de CDK 4/6 y FLT3 |
| WO2012149014A1 (en) | 2011-04-25 | 2012-11-01 | OSI Pharmaceuticals, LLC | Use of emt gene signatures in cancer drug discovery, diagnostics, and treatment |
| US8921533B2 (en) | 2011-07-25 | 2014-12-30 | Chromatin Technologies | Glycosylated valproic acid analogs and uses thereof |
| US9745288B2 (en) | 2011-08-16 | 2017-08-29 | Indiana University Research And Technology Corporation | Compounds and methods for treating cancer by inhibiting the urokinase receptor |
| JP6106685B2 (ja) | 2011-11-17 | 2017-04-05 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | C−jun−n−末端キナーゼ(jnk)の阻害剤 |
| AR090263A1 (es) | 2012-03-08 | 2014-10-29 | Hoffmann La Roche | Terapia combinada de anticuerpos contra el csf-1r humano y las utilizaciones de la misma |
| WO2013152252A1 (en) | 2012-04-06 | 2013-10-10 | OSI Pharmaceuticals, LLC | Combination anti-cancer therapy |
| US9724352B2 (en) | 2012-05-31 | 2017-08-08 | Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences | Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof |
| CN103450204B (zh) | 2012-05-31 | 2016-08-17 | 中国科学院上海药物研究所 | 吡咯[2,1-f][1,2,4]并三嗪类化合物,其制备方法及用途 |
| US9150570B2 (en) | 2012-05-31 | 2015-10-06 | Plexxikon Inc. | Synthesis of heterocyclic compounds |
| CN102675323B (zh) * | 2012-06-01 | 2014-04-09 | 南京药石药物研发有限公司 | 吡咯并[2,1-f][1,2,4]三嗪衍生物及其抗肿瘤用途 |
| EP2890696A1 (en) | 2012-08-29 | 2015-07-08 | Amgen, Inc. | Quinazolinone compounds and derivatives thereof |
| CN103664957A (zh) * | 2012-09-25 | 2014-03-26 | 杨子娇 | 一类治疗房角狭窄的化合物及其用途 |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| WO2014063061A1 (en) | 2012-10-19 | 2014-04-24 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged small molecules as inducers of protein degradation |
| US10000483B2 (en) | 2012-10-19 | 2018-06-19 | Dana-Farber Cancer Institute, Inc. | Bone marrow on X chromosome kinase (BMX) inhibitors and uses thereof |
| FR3000494B1 (fr) * | 2012-12-28 | 2015-08-21 | Oribase Pharma | Nouveaux derives d'azaindoles en tant qu'inhibiteurs de proteines kinases |
| US9050345B2 (en) | 2013-03-11 | 2015-06-09 | Bristol-Myers Squibb Company | Pyrrolotriazines as potassium ion channel inhibitors |
| ES2638317T3 (es) | 2013-04-04 | 2017-10-19 | Janssen Pharmaceutica Nv | Nuevos derivados de N-(2,3-dihidro-1H-pirrolo[2,3-b]piridin-5-il)-4-quinazolinamina y N-(2,3-dihidro-1H-indol-5-il)-4-quinazolinamina como inhibidores de PERK |
| EP3059225A4 (en) * | 2013-10-17 | 2017-09-06 | Shionogi & Co., Ltd. | Novel alkylene derivative |
| CN105849099B (zh) | 2013-10-18 | 2020-01-17 | 达纳-法伯癌症研究所股份有限公司 | 周期蛋白依赖性激酶7(cdk7)的多环抑制剂 |
| ES2676734T3 (es) | 2013-10-18 | 2018-07-24 | Syros Pharmaceuticals, Inc. | Compuestos heteroatómicos útiles para el tratamiento de enfermedades proliferativas |
| CN104725381B (zh) * | 2013-12-19 | 2018-04-10 | 南京圣和药业股份有限公司 | 生长因子受体抑制剂及其应用 |
| WO2015164604A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Hydrophobically tagged janus kinase inhibitors and uses thereof |
| WO2015164614A1 (en) | 2014-04-23 | 2015-10-29 | Dana-Farber Cancer Institute, Inc. | Janus kinase inhibitors and uses thereof |
| US9388239B2 (en) | 2014-05-01 | 2016-07-12 | Consejo Nacional De Investigation Cientifica | Anti-human VEGF antibodies with unusually strong binding affinity to human VEGF-A and cross reactivity to human VEGF-B |
| AU2015371251B2 (en) | 2014-12-23 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| HK1247955A1 (zh) | 2015-01-08 | 2018-10-05 | 小利兰.斯坦福大学托管委员会 | 提供骨、骨髓及软骨的诱导的因子和细胞 |
| JP6861166B2 (ja) | 2015-03-27 | 2021-04-21 | ダナ−ファーバー キャンサー インスティテュート, インコーポレイテッド | サイクリン依存性キナーゼの阻害剤 |
| CA2986441A1 (en) | 2015-06-12 | 2016-12-15 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| CA2996978A1 (en) | 2015-09-09 | 2017-03-16 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| JP6896715B2 (ja) | 2015-09-30 | 2021-06-30 | マックス−プランク−ゲゼルシャフト ツール フェルデルング デル ヴィッセンシャフテン エーファウ −ジェネラルフェルヴァルトゥング | セピアプテリン還元酵素としてのヘテロアリール誘導体 |
| KR20180118719A (ko) | 2016-03-04 | 2018-10-31 | 다이호야쿠힌고교 가부시키가이샤 | 악성 종양 치료용 제제 및 조성물 |
| US11883404B2 (en) | 2016-03-04 | 2024-01-30 | Taiho Pharmaceuticals Co., Ltd. | Preparation and composition for treatment of malignant tumors |
| CA3021185C (en) * | 2016-04-28 | 2024-06-04 | Takeda Pharmaceutical Company Limited | Fused heterocyclic compound |
| EP3554506B1 (en) | 2016-12-16 | 2021-04-28 | Cystic Fibrosis Foundation | Bycyclic heteroaryl derivatives as cftr potentiators |
| SG11201906223TA (en) | 2016-12-22 | 2019-08-27 | Amgen Inc | Benzisothiazole, isothiazolo[3,4-b]pyridine, quinazoline, phthalazine, pyrido[2,3-d]pyridazine and pyrido[2,3-d]pyrimidine derivatives as kras g12c inhibitors for treating lung, pancreatic or colorectal cancer |
| CN110139865B (zh) * | 2016-12-29 | 2022-02-18 | 石药集团中奇制药技术(石家庄)有限公司 | Fgfr抑制剂 |
| JOP20190272A1 (ar) | 2017-05-22 | 2019-11-21 | Amgen Inc | مثبطات kras g12c وطرق لاستخدامها |
| UY37870A (es) | 2017-09-08 | 2019-03-29 | Amgen Inc | Inhibidores de kras g12c y métodos para utilizarlos campo de la invención |
| BR112020018697A2 (pt) | 2018-03-19 | 2020-12-29 | Taiho Pharmaceutical Co., Ltd. | Composição farmacêutica incluindo alquilsulfato de sódio |
| CA3099118A1 (en) | 2018-05-04 | 2019-11-07 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| MA52501A (fr) | 2018-05-04 | 2021-03-10 | Amgen Inc | Inhibiteurs de kras g12c et leurs procédés d'utilisation |
| MX2020011907A (es) | 2018-05-10 | 2021-01-29 | Amgen Inc | Inhibidores de kras g12c para el tratamiento de cancer. |
| AU2019278998B2 (en) | 2018-06-01 | 2023-11-09 | Amgen Inc. | KRAS G12C inhibitors and methods of using the same |
| JP7357644B2 (ja) | 2018-06-11 | 2023-10-06 | アムジエン・インコーポレーテツド | がんを処置するためのkras g12c阻害剤 |
| AU2019336588B2 (en) | 2018-06-12 | 2022-07-28 | Amgen Inc. | KRAS G12C inhibitors encompassing a piperazine ring and use thereof in the treatment of cancer |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| JP7516029B2 (ja) | 2018-11-16 | 2024-07-16 | アムジエン・インコーポレーテツド | Kras g12c阻害剤化合物の重要な中間体の改良合成法 |
| JP7377679B2 (ja) | 2018-11-19 | 2023-11-10 | アムジエン・インコーポレーテツド | がん治療のためのkrasg12c阻害剤及び1種以上の薬学的に活性な追加の薬剤を含む併用療法 |
| WO2020106640A1 (en) | 2018-11-19 | 2020-05-28 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| US12441736B2 (en) | 2018-12-20 | 2025-10-14 | Amgen Inc. | KIF18A inhibitors |
| ES2996960T3 (en) | 2018-12-20 | 2025-02-13 | Amgen Inc | Heteroaryl amides useful as kif18a inhibitors |
| JOP20210154B1 (ar) | 2018-12-20 | 2023-09-17 | Amgen Inc | مثبطات kif18a |
| EP3897855B1 (en) | 2018-12-20 | 2023-06-07 | Amgen Inc. | Kif18a inhibitors |
| SG11202106635WA (en) | 2018-12-21 | 2021-07-29 | Daiichi Sankyo Co Ltd | Combination of antibody-drug conjugate and kinase inhibitor |
| AU2019413694B2 (en) | 2018-12-28 | 2025-03-20 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 and uses thereof |
| US20230148450A9 (en) | 2019-03-01 | 2023-05-11 | Revolution Medicines, Inc. | Bicyclic heteroaryl compounds and uses thereof |
| WO2020180770A1 (en) | 2019-03-01 | 2020-09-10 | Revolution Medicines, Inc. | Bicyclic heterocyclyl compounds and uses thereof |
| EP4306529B1 (en) * | 2019-05-13 | 2026-01-21 | Relay Therapeutics, Inc. | Fgfr inhibitors and methods of use thereof |
| EP3738593A1 (en) | 2019-05-14 | 2020-11-18 | Amgen, Inc | Dosing of kras inhibitor for treatment of cancers |
| CR20210665A (es) | 2019-05-21 | 2022-01-25 | Amgen Inc | Formas en estado sólido |
| CN114302880B (zh) | 2019-08-02 | 2025-07-15 | 美国安进公司 | Kif18a抑制剂 |
| CN114391012B (zh) | 2019-08-02 | 2025-10-31 | 美国安进公司 | 作为kif18a抑制剂的吡啶衍生物 |
| WO2021026099A1 (en) | 2019-08-02 | 2021-02-11 | Amgen Inc. | Kif18a inhibitors |
| US20220281843A1 (en) | 2019-08-02 | 2022-09-08 | Amgen Inc. | Kif18a inhibitors |
| EP4684786A2 (en) | 2019-10-24 | 2026-01-28 | Amgen Inc. | Pyridopyrimidine derivatives useful as kras g12c and kras g12d inhibitors in the treatment of cancer |
| US11739074B2 (en) | 2019-11-04 | 2023-08-29 | Revolution Medicines, Inc. | Ras inhibitors |
| CN120988055A (zh) | 2019-11-04 | 2025-11-21 | 锐新医药公司 | Ras抑制剂 |
| CA3160142A1 (en) | 2019-11-04 | 2021-05-14 | Revolution Medicines, Inc. | Ras inhibitors |
| JP7812056B2 (ja) | 2019-11-08 | 2026-02-09 | レヴォリューション・メディスンズ,インコーポレイテッド | 二環式ヘテロアリール化合物及びその使用 |
| WO2021094209A1 (en) | 2019-11-12 | 2021-05-20 | Bayer Aktiengesellschaft | Substituted pyrrolo triazine carboxamide derivatives as prostaglandin ep3 receptor antagonists |
| TWI882037B (zh) | 2019-11-14 | 2025-05-01 | 美商安進公司 | Kras g12c抑制劑化合物之改善的合成 |
| AU2020383535A1 (en) | 2019-11-14 | 2022-05-05 | Amgen Inc. | Improved synthesis of KRAS G12C inhibitor compound |
| BR112022009563A2 (pt) * | 2019-11-18 | 2022-08-02 | Jumbo Drug Bank Co Ltd | Compostos de pirrolotriazina atuando como inibidor de mnk |
| CN114980976A (zh) | 2019-11-27 | 2022-08-30 | 锐新医药公司 | 共价ras抑制剂及其用途 |
| BR112022010086A2 (pt) | 2020-01-07 | 2022-09-06 | Revolution Medicines Inc | Dosagem do inibidor de shp2 e métodos de tratamento de câncer |
| TW202214253A (zh) | 2020-06-18 | 2022-04-16 | 美商銳新醫藥公司 | 延遲、預防及治療對ras抑制劑之後天抗性之方法 |
| AU2021344830A1 (en) | 2020-09-03 | 2023-04-06 | Revolution Medicines, Inc. | Use of SOS1 inhibitors to treat malignancies with SHP2 mutations |
| MX2023003060A (es) | 2020-09-15 | 2023-04-05 | Revolution Medicines Inc | Derivados indolicos como inhibidores de ras en el tratamiento del cancer. |
| EP4267250A1 (en) | 2020-12-22 | 2023-11-01 | Qilu Regor Therapeutics Inc. | Sos1 inhibitors and uses thereof |
| WO2022235866A1 (en) | 2021-05-05 | 2022-11-10 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| IL308193A (en) | 2021-05-05 | 2024-01-01 | Revolution Medicines Inc | RAS inhibitors |
| TW202309053A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ras抑制劑 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| EP4430047A1 (en) | 2021-11-08 | 2024-09-18 | Progentos Therapeutics, Inc. | Platelet-derived growth factor receptor (pdgfr) alpha inhibitors and uses thereof |
| US20250282782A1 (en) | 2021-12-17 | 2025-09-11 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| EP4227307A1 (en) | 2022-02-11 | 2023-08-16 | Genzyme Corporation | Pyrazolopyrazine compounds as shp2 inhibitors |
| EP4490146B1 (en) | 2022-03-07 | 2026-02-18 | Amgen Inc. | A process for preparing 4-methyl-2-propan-2-yl-pyridine-3-carbonitrile |
| CN119136806A (zh) | 2022-03-08 | 2024-12-13 | 锐新医药公司 | 用于治疗免疫难治性肺癌的方法 |
| AU2023249795A1 (en) | 2022-04-08 | 2024-10-17 | Shy Therapeutics, Llc | Compounds that interact with ras superfamily proteins for treatment of cancers, inflammatory diseases, rasopathies, and fibrotic disease |
| EP4531927A1 (en) | 2022-05-24 | 2025-04-09 | Daiichi Sankyo Company, Limited | Dosage regimen of an anti-cdh6 antibody-drug conjugate |
| JP2025521232A (ja) | 2022-06-10 | 2025-07-08 | レボリューション メディシンズ インコーポレイテッド | 大環状ras阻害剤 |
| GEAP202516749A (en) | 2022-10-14 | 2025-07-25 | Black Diamond Therapeutics Inc | Methods of treating cancers using isoquinoline or 6-aza-quinoline derivatives |
| WO2024112656A1 (en) * | 2022-11-21 | 2024-05-30 | The Board Of Trustees Of The Leland Stanford Junior University | Use of a tyrosine kinase inhibitor for the treatment of hereditary hemorrhagic telangiectasia and pulmonary arterial hypertension |
| EP4687905A1 (en) | 2023-03-30 | 2026-02-11 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| WO2024211663A1 (en) | 2023-04-07 | 2024-10-10 | Revolution Medicines, Inc. | Condensed macrocyclic compounds as ras inhibitors |
| EP4688790A1 (en) | 2023-04-07 | 2026-02-11 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| KR20250169290A (ko) | 2023-04-14 | 2025-12-02 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형, 이를 함유하는 조성물 및 이의 사용 방법 |
| KR20250172857A (ko) | 2023-04-14 | 2025-12-09 | 레볼루션 메디슨즈, 인크. | Ras 억제제의 결정형 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080653A1 (en) * | 2023-10-10 | 2025-04-17 | Shy Therapeutics, Llc | Pyrrolo[2,1-f][1,2,4]triazine compounds acting against cancers, inflammatory diseases, and fibrotic disease via interaction with ras superfamily proteins |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025137507A1 (en) | 2023-12-22 | 2025-06-26 | Regor Pharmaceuticals, Inc. | Sos1 inhibitors and uses thereof |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IL107041A (en) * | 1992-09-25 | 2000-02-17 | Lilly Co Eli | Process for preparing omega(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo-6-¬2,3-d¾pyrimidin-5-YL)alkarylcarboxylic acids and N-(omega-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo¬2,3-d¾pyrimidin-5-YL)alk-aroyl-4-glutamic acids |
| US6191131B1 (en) * | 1997-07-23 | 2001-02-20 | Dupont Pharmaceuticals Company | Azolo triazines and pyrimidines |
| US6982265B1 (en) * | 1999-05-21 | 2006-01-03 | Bristol Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| EP1183033B1 (en) * | 1999-05-21 | 2006-03-01 | Bristol-Myers Squibb Company | Pyrrolotriazine inhibitors of kinases |
| JP4623483B2 (ja) * | 1999-08-23 | 2011-02-02 | 塩野義製薬株式会社 | sPLA2阻害作用を有するピロロトリアジン誘導体 |
| GB0017256D0 (en) * | 2000-07-13 | 2000-08-30 | Merck Sharp & Dohme | Therapeutic agents |
| JP2004505965A (ja) * | 2000-08-09 | 2004-02-26 | アストラゼネカ アクチボラグ | 化合物 |
| US6670357B2 (en) | 2000-11-17 | 2003-12-30 | Bristol-Myers Squibb Company | Methods of treating p38 kinase-associated conditions and pyrrolotriazine compounds useful as kinase inhibitors |
| US6867300B2 (en) * | 2000-11-17 | 2005-03-15 | Bristol-Myers Squibb Company | Methods for the preparation of pyrrolotriazine compounds useful as kinase inhibitors |
| GEP20063915B (en) * | 2000-11-17 | 2006-09-11 | Bristol Myers Squibb Co | PYRROLOTRIAZINE COMPOUNDS USEFUL AS KINASE INHIBITORS AND USE THEREOF FOR TREATING p38 KINASE-ASSOCIATED CONDITIONS |
| TW200300350A (en) * | 2001-11-14 | 2003-06-01 | Bristol Myers Squibb Co | C-5 modified indazolylpyrrolotriazines |
| WO2003090912A1 (en) * | 2002-04-23 | 2003-11-06 | Bristol-Myers Squibb Company | Pyrrolo-triazine aniline compounds useful as kinase inhibitors |
| ATE418546T1 (de) * | 2002-04-23 | 2009-01-15 | Bristol Myers Squibb Co | Als kinase inhibitoren geeignete arylketonpyrrolotriazin-verbindungen |
| TW200400034A (en) * | 2002-05-20 | 2004-01-01 | Bristol Myers Squibb Co | Pyrazolo-pyrimidine aniline compounds useful as kinase inhibitors |
| TW200407143A (en) * | 2002-05-21 | 2004-05-16 | Bristol Myers Squibb Co | Pyrrolotriazinone compounds and their use to treat diseases |
| US6933386B2 (en) | 2002-07-19 | 2005-08-23 | Bristol Myers Squibb Company | Process for preparing certain pyrrolotriazine compounds |
| TWI329112B (en) * | 2002-07-19 | 2010-08-21 | Bristol Myers Squibb Co | Novel inhibitors of kinases |
| EP1543009A4 (en) | 2002-08-02 | 2007-08-08 | Bristol Myers Squibb Co | Pyrrolotriazine KINASE INHIBITORS |
| TW200420565A (en) | 2002-12-13 | 2004-10-16 | Bristol Myers Squibb Co | C-6 modified indazolylpyrrolotriazines |
| PL378121A1 (pl) | 2003-02-05 | 2006-03-06 | Bristol-Myers Squibb Company | Sposób wytwarzania pirolotriazynowych inhibitorów kinazy |
-
2003
- 2003-07-14 TW TW092119165A patent/TWI329112B/zh not_active IP Right Cessation
- 2003-07-17 MY MYPI20032690A patent/MY134848A/en unknown
- 2003-07-18 UA UAA200501515A patent/UA82846C2/uk unknown
- 2003-07-18 EP EP10180960A patent/EP2280012A3/en not_active Withdrawn
- 2003-07-18 AU AU2003254017A patent/AU2003254017A1/en not_active Abandoned
- 2003-07-18 US US10/623,171 patent/US6869952B2/en not_active Expired - Lifetime
- 2003-07-18 CN CNB038218208A patent/CN1315833C/zh not_active Expired - Fee Related
- 2003-07-18 CN CN2010101428920A patent/CN101880283B/zh not_active Expired - Lifetime
- 2003-07-18 HR HR20050058A patent/HRP20050058A2/hr not_active Application Discontinuation
- 2003-07-18 AU AU2003254088A patent/AU2003254088B2/en not_active Expired
- 2003-07-18 MX MXPA05000716A patent/MXPA05000716A/es unknown
- 2003-07-18 WO PCT/US2003/022826 patent/WO2004009784A2/en not_active Ceased
- 2003-07-18 EP EP03765881A patent/EP1534290B1/en not_active Expired - Lifetime
- 2003-07-18 HR HRP20050059A patent/HRP20050059B8/hr not_active IP Right Cessation
- 2003-07-18 SI SI200332120T patent/SI1534290T1/sl unknown
- 2003-07-18 MX MXPA05000715A patent/MXPA05000715A/es active IP Right Grant
- 2003-07-18 EP EP03765754A patent/EP1539763B1/en not_active Expired - Lifetime
- 2003-07-18 PL PL375389A patent/PL216663B1/pl unknown
- 2003-07-18 GE GEAP8644A patent/GEP20074124B/en unknown
- 2003-07-18 BR BRPI0312940-3A patent/BRPI0312940B1/pt active IP Right Grant
- 2003-07-18 PT PT03765881T patent/PT1534290E/pt unknown
- 2003-07-18 RS YU20050042A patent/RS52325B/sr unknown
- 2003-07-18 JP JP2004523256A patent/JP4361485B2/ja not_active Expired - Lifetime
- 2003-07-18 AT AT03765754T patent/ATE505471T1/de not_active IP Right Cessation
- 2003-07-18 DK DK03765881.2T patent/DK1534290T3/da active
- 2003-07-18 DE DE60336732T patent/DE60336732D1/de not_active Expired - Lifetime
- 2003-07-18 AR AR20030102587A patent/AR040500A1/es active IP Right Grant
- 2003-07-18 GE GEAP8643A patent/GEP20074213B/en unknown
- 2003-07-18 CN CN038219158A patent/CN1681508B/zh not_active Expired - Lifetime
- 2003-07-18 ES ES03765881T patent/ES2377963T3/es not_active Expired - Lifetime
- 2003-07-18 RS YUP-2005/0041A patent/RS20050041A/sr unknown
- 2003-07-18 RU RU2005104818/04A patent/RU2005104818A/ru not_active Application Discontinuation
- 2003-07-18 US US10/622,593 patent/US6969717B2/en not_active Expired - Lifetime
- 2003-07-18 CA CA002492665A patent/CA2492665A1/en not_active Abandoned
- 2003-07-18 IL IL16612903A patent/IL166129A0/xx active IP Right Grant
- 2003-07-18 CA CA002492804A patent/CA2492804C/en not_active Expired - Lifetime
- 2003-07-18 WO PCT/US2003/022554 patent/WO2004009601A1/en not_active Ceased
- 2003-07-18 JP JP2004523591A patent/JP4381978B2/ja not_active Expired - Fee Related
- 2003-07-18 NZ NZ537523A patent/NZ537523A/en not_active IP Right Cessation
- 2003-07-18 BR BRPI0312801-6A patent/BR0312801A/pt unknown
- 2003-07-18 KR KR1020087022726A patent/KR100901939B1/ko not_active Expired - Lifetime
- 2003-07-18 PL PL03375352A patent/PL375352A1/xx not_active Application Discontinuation
- 2003-07-18 AT AT03765881T patent/ATE537843T1/de active
- 2003-07-18 RU RU2005104422/04A patent/RU2331642C2/ru active
- 2003-07-21 PE PE2003000721A patent/PE20040680A1/es not_active Application Discontinuation
-
2005
- 2005-01-03 IL IL166129A patent/IL166129A/en unknown
- 2005-01-06 NO NO20050072A patent/NO330132B1/no not_active IP Right Cessation
- 2005-01-11 IL IL16623205A patent/IL166232A0/xx unknown
- 2005-01-12 IS IS7646A patent/IS7646A/is unknown
- 2005-01-12 IS IS7647A patent/IS2880B/is unknown
- 2005-01-13 US US11/035,248 patent/US7265113B2/en not_active Expired - Lifetime
- 2005-01-19 CO CO05003967A patent/CO5680407A2/es active IP Right Grant
- 2005-01-25 NO NO20050417A patent/NO20050417L/no not_active Application Discontinuation
- 2005-08-29 US US11/214,267 patent/US20060058304A1/en not_active Abandoned
-
2007
- 2007-08-02 US US11/832,976 patent/US7521450B2/en not_active Expired - Lifetime
-
2009
- 2009-03-06 US US12/399,429 patent/US7820814B2/en not_active Expired - Lifetime
-
2012
- 2012-03-14 CY CY20121100271T patent/CY1112628T1/el unknown
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2404765C2 (ru) * | 2005-08-26 | 2010-11-27 | Антисома Рисерч Лимитед | Комбинации (составы), включающие dmxaa для лечения рака |
| CN116813526A (zh) * | 2023-05-22 | 2023-09-29 | 四川省医学科学院·四川省人民医院 | 异吲哚啉酮类化合物、其制备方法及其应用 |
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| RU2005104818A (ru) | Азаиндольные ингибиторы киназ | |
| JP7206314B2 (ja) | Jak及びpi3k阻害剤併用によるb細胞悪性腫瘍の処置 | |
| KR102014326B1 (ko) | 벤즈옥사제핀 옥사졸리디논 화합물 및 사용 방법 | |
| US9951065B2 (en) | Benzimidazole and imadazopyridine carboximidamide compounds | |
| CA2520898C (en) | Non-cross-linking pyrrolo(2,1-c)(1,4)benzodiazepines as potential antitumour agents and process thereof | |
| AU2004312413C1 (en) | Pyrrolotriazine compounds as kinase inhibitors | |
| WO2022187528A1 (en) | Quinazoline amine derivatives as kras inhibitors | |
| JP2007538092A5 (Direct) | ||
| WO2018024602A1 (en) | 2,7-diazaspiro[4.4]nonanes | |
| CA2974853A1 (en) | 4h-pyrrolo[3,2-c]pyridin-4-one derivatives | |
| JP2006504624A5 (Direct) | ||
| RU2014126750A (ru) | Ингибиторы тирозинкиназы брутона | |
| CA3115068A1 (en) | Method for preparing and delivering bisantrene formulations | |
| JP2006512366A5 (Direct) | ||
| RU98117245A (ru) | 2-(арилфенил)аминоимидазолиновые производные | |
| EP1799689A1 (en) | Furazano `3, 4-b ! pyrazynes and their use as anti-tumor agents | |
| US10836747B2 (en) | Ethane-sulfonate salt of quinoline derivative | |
| WO2025233865A1 (en) | Enpp1 inhibitors | |
| CN121399105A (zh) | 杂芳族dhodh抑制剂 | |
| JP2026021472A (ja) | Jak及びpi3k阻害剤併用によるb細胞悪性腫瘍の処置 | |
| KR20250096877A (ko) | 치환된 헤테로고리 화합물 유도체 및 그의 약학적 용도 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA92 | Acknowledgement of application withdrawn (lack of supplementary materials submitted) |
Effective date: 20061013 |