JP5020073B2 - 第Xa因子阻害剤 - Google Patents
第Xa因子阻害剤 Download PDFInfo
- Publication number
- JP5020073B2 JP5020073B2 JP2007516824A JP2007516824A JP5020073B2 JP 5020073 B2 JP5020073 B2 JP 5020073B2 JP 2007516824 A JP2007516824 A JP 2007516824A JP 2007516824 A JP2007516824 A JP 2007516824A JP 5020073 B2 JP5020073 B2 JP 5020073B2
- Authority
- JP
- Japan
- Prior art keywords
- chloro
- methyl
- thiophene
- phenyl
- ylmethyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Fee Related
Links
- 0 C*[C@](*(*)C(C(N)=CC=***)=*)C(C=C(C*)S)=CC Chemical compound C*[C@](*(*)C(C(N)=CC=***)=*)C(C=C(C*)S)=CC 0.000 description 20
- HHJMMALGFIFWBN-UHFFFAOYSA-N Bc(cc1)ccc1C#N Chemical compound Bc(cc1)ccc1C#N HHJMMALGFIFWBN-UHFFFAOYSA-N 0.000 description 1
- XIPRERXNTBUHLO-UHFFFAOYSA-N C#CCNC(c([s]1)ccc1Cl)=O Chemical compound C#CCNC(c([s]1)ccc1Cl)=O XIPRERXNTBUHLO-UHFFFAOYSA-N 0.000 description 1
- XKHBWGQCTAHWGN-UHFFFAOYSA-N CC(C)C(N(C)CC1=CCCO1)=N Chemical compound CC(C)C(N(C)CC1=CCCO1)=N XKHBWGQCTAHWGN-UHFFFAOYSA-N 0.000 description 1
- DSQBHNQQJSUZGT-UHFFFAOYSA-N CC(C)C(N1CCN(C)CC1)=N Chemical compound CC(C)C(N1CCN(C)CC1)=N DSQBHNQQJSUZGT-UHFFFAOYSA-N 0.000 description 1
- UGRGQCUZCLNATC-UHFFFAOYSA-N CC(C)C(N1CCNCC1)=N Chemical compound CC(C)C(N1CCNCC1)=N UGRGQCUZCLNATC-UHFFFAOYSA-N 0.000 description 1
- XDXRVYYTEDKRPC-UHFFFAOYSA-N CC(C)C(N1CCOCC1)=N Chemical compound CC(C)C(N1CCOCC1)=N XDXRVYYTEDKRPC-UHFFFAOYSA-N 0.000 description 1
- WBDOLBIBGXIARJ-UHFFFAOYSA-N CC(C)N(C=C(C=C1)F)C1=O Chemical compound CC(C)N(C=C(C=C1)F)C1=O WBDOLBIBGXIARJ-UHFFFAOYSA-N 0.000 description 1
- HMTPOXJNEFVQOI-UHFFFAOYSA-N CC(C)N(C=C(C=C1)OC)C1=O Chemical compound CC(C)N(C=C(C=C1)OC)C1=O HMTPOXJNEFVQOI-UHFFFAOYSA-N 0.000 description 1
- GVDQKJQFVPXADH-UHFFFAOYSA-N CC(C)N(CCCC1)C1=O Chemical compound CC(C)N(CCCC1)C1=O GVDQKJQFVPXADH-UHFFFAOYSA-N 0.000 description 1
- WAWBBMSQWUPYOW-UHFFFAOYSA-N CC(C)N(CCNC1)C1=O Chemical compound CC(C)N(CCNC1)C1=O WAWBBMSQWUPYOW-UHFFFAOYSA-N 0.000 description 1
- IIYIYDOKNRRIEQ-UHFFFAOYSA-N CC(C)N(CCOC1)C1=O Chemical compound CC(C)N(CCOC1)C1=O IIYIYDOKNRRIEQ-UHFFFAOYSA-N 0.000 description 1
- HIDDRQKMANCQFT-UHFFFAOYSA-N CC(C)Oc(cc(cc1)C(N2CCCC2)=N)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1 Chemical compound CC(C)Oc(cc(cc1)C(N2CCCC2)=N)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1 HIDDRQKMANCQFT-UHFFFAOYSA-N 0.000 description 1
- IOILKZYWNMYWJY-UHFFFAOYSA-N CC(C)c1ncc[n]1C Chemical compound CC(C)c1ncc[n]1C IOILKZYWNMYWJY-UHFFFAOYSA-N 0.000 description 1
- IXAQCGHSXRCXFF-UHFFFAOYSA-N CC(CNC(c([s]1)ccc1Cl)=O)(C1)ON=C1c(cc1)ccc1OC Chemical compound CC(CNC(c([s]1)ccc1Cl)=O)(C1)ON=C1c(cc1)ccc1OC IXAQCGHSXRCXFF-UHFFFAOYSA-N 0.000 description 1
- LAILHIOPQOSEOS-UHFFFAOYSA-N CC(N1CCCC1)=N Chemical compound CC(N1CCCC1)=N LAILHIOPQOSEOS-UHFFFAOYSA-N 0.000 description 1
- SHPVKLYHXZHYNJ-UHFFFAOYSA-N CC(N1CCCCC1)=N Chemical compound CC(N1CCCCC1)=N SHPVKLYHXZHYNJ-UHFFFAOYSA-N 0.000 description 1
- NANIMOOULVVYEF-UHFFFAOYSA-N CC1(C)SC(C(NCc2c[s]c(-c(cc3)ccc3C(N(C)C)=N)n2)O)=CC1 Chemical compound CC1(C)SC(C(NCc2c[s]c(-c(cc3)ccc3C(N(C)C)=N)n2)O)=CC1 NANIMOOULVVYEF-UHFFFAOYSA-N 0.000 description 1
- FSQDGNHTIYPXDL-UHFFFAOYSA-N CC1(c(cc2)ccc2C#N)SC=C(CN)N1 Chemical compound CC1(c(cc2)ccc2C#N)SC=C(CN)N1 FSQDGNHTIYPXDL-UHFFFAOYSA-N 0.000 description 1
- UFAFUGDWXUBCIN-UHFFFAOYSA-N CC1=CC=CN(c(cc2)ccc2-[n]2nnc(CNC(c([s]3)ccc3Cl)=O)c2)C1=O Chemical compound CC1=CC=CN(c(cc2)ccc2-[n]2nnc(CNC(c([s]3)ccc3Cl)=O)c2)C1=O UFAFUGDWXUBCIN-UHFFFAOYSA-N 0.000 description 1
- RUGSRRKQHCNABK-UHFFFAOYSA-N CCC(C)N(C=CN=C1)C1=O Chemical compound CCC(C)N(C=CN=C1)C1=O RUGSRRKQHCNABK-UHFFFAOYSA-N 0.000 description 1
- RHDIRBFDNPYOFQ-UHFFFAOYSA-N CCCN(C)C(c(cc1)ccc1-c1n[o]c(CN(C)C(c2ccc(C3[IH]C3)[s]2)=O)c1)=N Chemical compound CCCN(C)C(c(cc1)ccc1-c1n[o]c(CN(C)C(c2ccc(C3[IH]C3)[s]2)=O)c1)=N RHDIRBFDNPYOFQ-UHFFFAOYSA-N 0.000 description 1
- FQGMBKNHZFAIOS-UHFFFAOYSA-N CCN(C)C(C(C)C)=N Chemical compound CCN(C)C(C(C)C)=N FQGMBKNHZFAIOS-UHFFFAOYSA-N 0.000 description 1
- JIRLQUVHZUABQD-UHFFFAOYSA-N CCN(CC)CCN(C)C(c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)=O Chemical compound CCN(CC)CCN(C)C(c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)=O JIRLQUVHZUABQD-UHFFFAOYSA-N 0.000 description 1
- GZDFANYPFBRZMK-UHFFFAOYSA-N CCN(CCOCC1)C1=O Chemical compound CCN(CCOCC1)C1=O GZDFANYPFBRZMK-UHFFFAOYSA-N 0.000 description 1
- KSAQXKVBGSGAJE-UHFFFAOYSA-N CCOC(C(CC1)CCN1C(c(cc1)ccc1-c1nc(CNC(c([s]2)ccc2Cl)=O)c[o]1)=N)=O Chemical compound CCOC(C(CC1)CCN1C(c(cc1)ccc1-c1nc(CNC(c([s]2)ccc2Cl)=O)c[o]1)=N)=O KSAQXKVBGSGAJE-UHFFFAOYSA-N 0.000 description 1
- PDWMRERZMIJGFN-UHFFFAOYSA-N CCOc(cc(cc1)C(N2CCCCC2)=N)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1 Chemical compound CCOc(cc(cc1)C(N2CCCCC2)=N)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1 PDWMRERZMIJGFN-UHFFFAOYSA-N 0.000 description 1
- AURNPQSMNMFSIF-UHFFFAOYSA-N CCOc1cc(Nc(cc2)ccc2C2=NOC(CNC(c([s]3)ccc3Cl)=O)C2)ccn1 Chemical compound CCOc1cc(Nc(cc2)ccc2C2=NOC(CNC(c([s]3)ccc3Cl)=O)C2)ccn1 AURNPQSMNMFSIF-UHFFFAOYSA-N 0.000 description 1
- ZZAQLLOCRKOOPM-UHFFFAOYSA-N CCc1c[s]c(-c(cc2)ccc2C#N)n1 Chemical compound CCc1c[s]c(-c(cc2)ccc2C#N)n1 ZZAQLLOCRKOOPM-UHFFFAOYSA-N 0.000 description 1
- YCHGXGYRJQEUFO-UHFFFAOYSA-N CN(C)C(c(cc1)cc(F)c1-[n]1nnc(CNC(c([s]2)ccc2Cl)=O)c1)=N Chemical compound CN(C)C(c(cc1)cc(F)c1-[n]1nnc(CNC(c([s]2)ccc2Cl)=O)c1)=N YCHGXGYRJQEUFO-UHFFFAOYSA-N 0.000 description 1
- ZGCMIWVQZBNZBL-UHFFFAOYSA-N CN(C)C(c(cc1)cc(F)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)=N Chemical compound CN(C)C(c(cc1)cc(F)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)=N ZGCMIWVQZBNZBL-UHFFFAOYSA-N 0.000 description 1
- SHZASYDPJZTPTH-UHFFFAOYSA-N CN(C)C(c(cc1)cc(Oc2ccccc2)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)=N Chemical compound CN(C)C(c(cc1)cc(Oc2ccccc2)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)=N SHZASYDPJZTPTH-UHFFFAOYSA-N 0.000 description 1
- WTPOIIZOZLZWPI-UHFFFAOYSA-N CN(C)C(c(cc1)ccc1-[n]1ncc(CNC(c([s]2)ccc2Cl)=O)c1)=N Chemical compound CN(C)C(c(cc1)ccc1-[n]1ncc(CNC(c([s]2)ccc2Cl)=O)c1)=N WTPOIIZOZLZWPI-UHFFFAOYSA-N 0.000 description 1
- IWHOQWRXSPXNKM-UHFFFAOYSA-N CN(C)C(c1ccc(-c2n[o]c(CNC(c([s]3)ccc3Cl)=O)c2)c(N2CCOCC2)c1)=N Chemical compound CN(C)C(c1ccc(-c2n[o]c(CNC(c([s]3)ccc3Cl)=O)c2)c(N2CCOCC2)c1)=N IWHOQWRXSPXNKM-UHFFFAOYSA-N 0.000 description 1
- JFUIQOJIJDGDNU-UHFFFAOYSA-N CN(C)Cc(c(-c(cc1)ccc1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)c1)ccc1OC Chemical compound CN(C)Cc(c(-c(cc1)ccc1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)c1)ccc1OC JFUIQOJIJDGDNU-UHFFFAOYSA-N 0.000 description 1
- DKJLNUZAUXSRON-UHFFFAOYSA-N CN(C)Cc(c(-c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)c1)ccc1OC Chemical compound CN(C)Cc(c(-c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)c1)ccc1OC DKJLNUZAUXSRON-UHFFFAOYSA-N 0.000 description 1
- CQLLNFQNZRSDEO-UHFFFAOYSA-N CN(C)Cc1cccc(-c2cc(-c3n[o]c(CNC(c([s]4)ccc4Cl)=O)c3)ccc2)c1 Chemical compound CN(C)Cc1cccc(-c2cc(-c3n[o]c(CNC(c([s]4)ccc4Cl)=O)c3)ccc2)c1 CQLLNFQNZRSDEO-UHFFFAOYSA-N 0.000 description 1
- WGGTUZSBHMOLDD-UHFFFAOYSA-N CN(C)c1cc(C(N2CCCC2)=N)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 Chemical compound CN(C)c1cc(C(N2CCCC2)=N)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 WGGTUZSBHMOLDD-UHFFFAOYSA-N 0.000 description 1
- OXLPBZUYGNQHCS-MSUUIHNZSA-N CN(CC1)CCN1c(cc(cc1)N(C=CC=C2)C2=O)c1N(/C=C(/CNC(c([s]1)ccc1Cl)=O)\N)N Chemical compound CN(CC1)CCN1c(cc(cc1)N(C=CC=C2)C2=O)c1N(/C=C(/CNC(c([s]1)ccc1Cl)=O)\N)N OXLPBZUYGNQHCS-MSUUIHNZSA-N 0.000 description 1
- GSOPKPYARNNIAH-UHFFFAOYSA-N CN(CCN1c(cc2)ccc2C2=NOC(CNC(c([s]3)ccc3Cl)=O)C2)C1=O Chemical compound CN(CCN1c(cc2)ccc2C2=NOC(CNC(c([s]3)ccc3Cl)=O)C2)C1=O GSOPKPYARNNIAH-UHFFFAOYSA-N 0.000 description 1
- VCQRNBPKGCVGCX-UHFFFAOYSA-N CN(CCOC)C(c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)=N Chemical compound CN(CCOC)C(c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)=N VCQRNBPKGCVGCX-UHFFFAOYSA-N 0.000 description 1
- ZANHDXOCLSUSLY-UHFFFAOYSA-N CN(CCSC1)C1=O Chemical compound CN(CCSC1)C1=O ZANHDXOCLSUSLY-UHFFFAOYSA-N 0.000 description 1
- YFOIFNZMFMSUNB-UHFFFAOYSA-N CN1C(c(cc2)cc(N3CCOCC3)c2-c2n[o]c(CNC(c([s]3)ccc3Cl)=O)c2)=NCC1 Chemical compound CN1C(c(cc2)cc(N3CCOCC3)c2-c2n[o]c(CNC(c([s]3)ccc3Cl)=O)c2)=NCC1 YFOIFNZMFMSUNB-UHFFFAOYSA-N 0.000 description 1
- JVJFPAIWUYRASS-UHFFFAOYSA-N CN1C(c(cc2)ccc2-c(cc(CNC(c([s]2)ccc2Cl)=O)cc2)c2F)=NCC1 Chemical compound CN1C(c(cc2)ccc2-c(cc(CNC(c([s]2)ccc2Cl)=O)cc2)c2F)=NCC1 JVJFPAIWUYRASS-UHFFFAOYSA-N 0.000 description 1
- SCWJGRIOLJJVQF-UHFFFAOYSA-N CN1C(c2ccc(C3=NOC(CNC(c([s]4)ccc4Cl)=O)C3)c(N3CCCCCC3)c2)=NCC1 Chemical compound CN1C(c2ccc(C3=NOC(CNC(c([s]4)ccc4Cl)=O)C3)c(N3CCCCCC3)c2)=NCC1 SCWJGRIOLJJVQF-UHFFFAOYSA-N 0.000 description 1
- CRRCPYYOOPWAGN-UHFFFAOYSA-N COC(c(cc1)ccc1Nc(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)=O Chemical compound COC(c(cc1)ccc1Nc(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1)=O CRRCPYYOOPWAGN-UHFFFAOYSA-N 0.000 description 1
- WBVHJLGPJGESRR-UHFFFAOYSA-N COc(cc(cc1)C(N2CCCC2)=N)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1 Chemical compound COc(cc(cc1)C(N2CCCC2)=N)c1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1 WBVHJLGPJGESRR-UHFFFAOYSA-N 0.000 description 1
- RFYCCJMETPCEMQ-UHFFFAOYSA-N COc1cc(C(N2CCCC2)=N)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 Chemical compound COc1cc(C(N2CCCC2)=N)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 RFYCCJMETPCEMQ-UHFFFAOYSA-N 0.000 description 1
- HASCDZPGZDNFIJ-UHFFFAOYSA-N COc1ccc(CN2CCCC2)c(-c(cc2)ccc2-c2n[o]c(CNC(c([s]3)ccc3Cl)=O)c2)c1 Chemical compound COc1ccc(CN2CCCC2)c(-c(cc2)ccc2-c2n[o]c(CNC(c([s]3)ccc3Cl)=O)c2)c1 HASCDZPGZDNFIJ-UHFFFAOYSA-N 0.000 description 1
- RVJRDSLTCFMMNI-UHFFFAOYSA-N CSc(cc(cc1)C(N2CCCCC2)=N)c1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 Chemical compound CSc(cc(cc1)C(N2CCCCC2)=N)c1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 RVJRDSLTCFMMNI-UHFFFAOYSA-N 0.000 description 1
- OEYWGDSPHMYUKL-UHFFFAOYSA-N CSc1ccccc1-c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 Chemical compound CSc1ccccc1-c(cc1)ccc1C1=NOC(CNC(c([s]2)ccc2Cl)=O)C1 OEYWGDSPHMYUKL-UHFFFAOYSA-N 0.000 description 1
- JXCWLIAYTJNSCN-LLVKDONJSA-N C[C@H](c1cc(-c(cc2)ccc2C(N(C)C)=N)n[o]1)NC(c([s]1)ccc1Cl)=O Chemical compound C[C@H](c1cc(-c(cc2)ccc2C(N(C)C)=N)n[o]1)NC(c([s]1)ccc1Cl)=O JXCWLIAYTJNSCN-LLVKDONJSA-N 0.000 description 1
- LDNOHDUJNAVWFT-UHFFFAOYSA-N Cc1c[n](-c(cc2)ccc2C#N)nc1 Chemical compound Cc1c[n](-c(cc2)ccc2C#N)nc1 LDNOHDUJNAVWFT-UHFFFAOYSA-N 0.000 description 1
- MOLONWICPKJAPY-UHFFFAOYSA-N Cc1ccc(COCNCc2c[s]c(-c(cc3)ccc3C#N)n2)[s]1 Chemical compound Cc1ccc(COCNCc2c[s]c(-c(cc3)ccc3C#N)n2)[s]1 MOLONWICPKJAPY-UHFFFAOYSA-N 0.000 description 1
- OWVIJGHYHFWKPL-UHFFFAOYSA-N N#Cc(cc1)ccc1-[n]1ncc(CBr)c1 Chemical compound N#Cc(cc1)ccc1-[n]1ncc(CBr)c1 OWVIJGHYHFWKPL-UHFFFAOYSA-N 0.000 description 1
- FBUINNUZIAJOSV-UHFFFAOYSA-N N#Cc(cc1)ccc1-[n]1ncc(CNC(c([s]2)ccc2Cl)=O)c1 Chemical compound N#Cc(cc1)ccc1-[n]1ncc(CNC(c([s]2)ccc2Cl)=O)c1 FBUINNUZIAJOSV-UHFFFAOYSA-N 0.000 description 1
- PIXZNHNAOYXPCQ-SEYXRHQNSA-N N/C(/CNC(c([s]1)ccc1Cl)=O)=C\N(c(cc1)ccc1N(CCOCC1)C1=O)N Chemical compound N/C(/CNC(c([s]1)ccc1Cl)=O)=C\N(c(cc1)ccc1N(CCOCC1)C1=O)N PIXZNHNAOYXPCQ-SEYXRHQNSA-N 0.000 description 1
- DEHNGURMHZRQQW-QXMHVHEDSA-N N/C(/CNC(c([s]1)ccc1Cl)=O)=C\N(c(ccc(N(C=CC=C1)C1=O)c1)c1F)N Chemical compound N/C(/CNC(c([s]1)ccc1Cl)=O)=C\N(c(ccc(N(C=CC=C1)C1=O)c1)c1F)N DEHNGURMHZRQQW-QXMHVHEDSA-N 0.000 description 1
- PANFSRYLUOMFCB-LUAWRHEFSA-N N/C(/CNC(c([s]1)ccc1Cl)=O)=C\N(c(ccc(N(CCOC1)C1=O)c1)c1F)N Chemical compound N/C(/CNC(c([s]1)ccc1Cl)=O)=C\N(c(ccc(N(CCOC1)C1=O)c1)c1F)N PANFSRYLUOMFCB-LUAWRHEFSA-N 0.000 description 1
- WUFYWFMWSQJRGQ-LUAWRHEFSA-N N/C(/CNCc([s]1)ccc1Cl)=C\N(c(ccc(C#N)c1)c1F)N Chemical compound N/C(/CNCc([s]1)ccc1Cl)=C\N(c(ccc(C#N)c1)c1F)N WUFYWFMWSQJRGQ-LUAWRHEFSA-N 0.000 description 1
- AQWIGKAMGKNUES-UHFFFAOYSA-N N=C(c(cc1)ccc1-c1c[s]c(CNC(c([s]2)ccc2Cl)=O)n1)N1CCCC1 Chemical compound N=C(c(cc1)ccc1-c1c[s]c(CNC(c([s]2)ccc2Cl)=O)n1)N1CCCC1 AQWIGKAMGKNUES-UHFFFAOYSA-N 0.000 description 1
- RDOOLACSLCESER-UHFFFAOYSA-N N=C(c(cc1)ccc1-c1c[s]c(CNC(c([s]2)ccc2Cl)=O)n1)N1CCCCC1 Chemical compound N=C(c(cc1)ccc1-c1c[s]c(CNC(c([s]2)ccc2Cl)=O)n1)N1CCCCC1 RDOOLACSLCESER-UHFFFAOYSA-N 0.000 description 1
- NHXSEPLILRRYCH-UHFFFAOYSA-N N=C(c(cc1)ccc1-c1cncc(CNC(c([s]2)ccc2Cl)=O)c1)N1CCCC1 Chemical compound N=C(c(cc1)ccc1-c1cncc(CNC(c([s]2)ccc2Cl)=O)c1)N1CCCC1 NHXSEPLILRRYCH-UHFFFAOYSA-N 0.000 description 1
- SDAJHHWYLHUSOZ-UHFFFAOYSA-N N=C(c(cc1)ccc1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)N1CCCC1 Chemical compound N=C(c(cc1)ccc1-c1n[o]c(CNC(c([s]2)ccc2Cl)=O)c1)N1CCCC1 SDAJHHWYLHUSOZ-UHFFFAOYSA-N 0.000 description 1
- FUKWTMJZHKZKFA-UHFFFAOYSA-N NC(c(cc1)ccc1C#N)=O Chemical compound NC(c(cc1)ccc1C#N)=O FUKWTMJZHKZKFA-UHFFFAOYSA-N 0.000 description 1
- FVLBKOUQOKBIPC-UHFFFAOYSA-N NC(c(cc1)ccc1C#N)=S Chemical compound NC(c(cc1)ccc1C#N)=S FVLBKOUQOKBIPC-UHFFFAOYSA-N 0.000 description 1
- GNZXZEDKLUUUGK-UHFFFAOYSA-N NCc1c[n](-c(cc2)ccc2C#N)nc1 Chemical compound NCc1c[n](-c(cc2)ccc2C#N)nc1 GNZXZEDKLUUUGK-UHFFFAOYSA-N 0.000 description 1
- RLMBRRQWBTWGMB-UHFFFAOYSA-N Nc(ccc(C#N)c1)c1F Chemical compound Nc(ccc(C#N)c1)c1F RLMBRRQWBTWGMB-UHFFFAOYSA-N 0.000 description 1
- ZVMSJANFBJSXAK-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1-c1cc(Cl)ccc1CN1CCCC1 Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1-c1cc(Cl)ccc1CN1CCCC1 ZVMSJANFBJSXAK-UHFFFAOYSA-N 0.000 description 1
- HEOVMDLNTHSBBY-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1N(C=C(C=C1)F)C1=O Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1N(C=C(C=C1)F)C1=O HEOVMDLNTHSBBY-UHFFFAOYSA-N 0.000 description 1
- WSNNTBZHQXZQKM-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc(c(Cl)cnc1)c1Cl Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc(c(Cl)cnc1)c1Cl WSNNTBZHQXZQKM-UHFFFAOYSA-N 0.000 description 1
- WLBNKKXWYGQSBV-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc(cc1)ccc1F Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc(cc1)ccc1F WLBNKKXWYGQSBV-UHFFFAOYSA-N 0.000 description 1
- AUMAMPZKKXJRJQ-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc1cc2cccnc2cc1 Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc1cc2cccnc2cc1 AUMAMPZKKXJRJQ-UHFFFAOYSA-N 0.000 description 1
- VMDXZEFVYNRDHC-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc1ccncc1 Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c(cc1)ccc1Nc1ccncc1 VMDXZEFVYNRDHC-UHFFFAOYSA-N 0.000 description 1
- VKZKQZYWFNXOJZ-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c1cc(-c2ccncc2)ccc1 Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c1cc(-c2ccncc2)ccc1 VKZKQZYWFNXOJZ-UHFFFAOYSA-N 0.000 description 1
- YICNCQJXJJOVPZ-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c1cccc(Br)c1 Chemical compound O=C(c([s]1)ccc1Cl)NCC(C1)ON=C1c1cccc(Br)c1 YICNCQJXJJOVPZ-UHFFFAOYSA-N 0.000 description 1
- VZNQRZSEUMYTBP-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)ccc2N(C=C(C=C2)Cl)C2=O)nn1 Chemical compound O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)ccc2N(C=C(C=C2)Cl)C2=O)nn1 VZNQRZSEUMYTBP-UHFFFAOYSA-N 0.000 description 1
- FCFIIPNBPWAMJT-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)cnc2N2CCCCC2)nn1 Chemical compound O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)cnc2N2CCCCC2)nn1 FCFIIPNBPWAMJT-UHFFFAOYSA-N 0.000 description 1
- RUMDUZGTRCEVML-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)cnc2N2CCNCC2)nn1 Chemical compound O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)cnc2N2CCNCC2)nn1 RUMDUZGTRCEVML-UHFFFAOYSA-N 0.000 description 1
- NFAYBIHYYPDCTC-UHFFFAOYSA-N O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)cnc2N2CCNCCC2)nn1 Chemical compound O=C(c([s]1)ccc1Cl)NCc1c[n](-c(cc2)cnc2N2CCNCCC2)nn1 NFAYBIHYYPDCTC-UHFFFAOYSA-N 0.000 description 1
- NFOPXWPHVWHMJE-UHFFFAOYSA-N Oc(cc(cc1)N(C=CC=C2)C2=O)c1-[n]1nnc(CNC(c([s]2)ccc2Cl)=O)c1 Chemical compound Oc(cc(cc1)N(C=CC=C2)C2=O)c1-[n]1nnc(CNC(c([s]2)ccc2Cl)=O)c1 NFOPXWPHVWHMJE-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- 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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
-
- 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
-
- 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
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- A61P9/10—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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
- C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
- C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
- C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
- C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Cardiology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Compounds Containing Sulfur Atoms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US58089904P | 2004-06-18 | 2004-06-18 | |
| US60/580,899 | 2004-06-18 | ||
| PCT/US2005/021817 WO2006002099A2 (en) | 2004-06-18 | 2005-06-20 | Factor xa inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2008503497A JP2008503497A (ja) | 2008-02-07 |
| JP2008503497A5 JP2008503497A5 (enExample) | 2008-06-19 |
| JP5020073B2 true JP5020073B2 (ja) | 2012-09-05 |
Family
ID=35782278
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007516824A Expired - Fee Related JP5020073B2 (ja) | 2004-06-18 | 2005-06-20 | 第Xa因子阻害剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (3) | US7521470B2 (enExample) |
| EP (1) | EP1893572B1 (enExample) |
| JP (1) | JP5020073B2 (enExample) |
| KR (1) | KR101195801B1 (enExample) |
| CN (1) | CN1968922A (enExample) |
| AU (1) | AU2005257999B2 (enExample) |
| BR (1) | BRPI0512273A (enExample) |
| CA (1) | CA2565437A1 (enExample) |
| IL (1) | IL178807A0 (enExample) |
| MX (1) | MXPA06013960A (enExample) |
| NZ (1) | NZ552187A (enExample) |
| WO (1) | WO2006002099A2 (enExample) |
| ZA (1) | ZA200610138B (enExample) |
Families Citing this family (58)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2254385T3 (es) | 2000-02-29 | 2006-06-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| CN1968922A (zh) | 2004-06-18 | 2007-05-23 | 米伦纽姆医药公司 | 因子xa抑制剂 |
| US7696352B2 (en) * | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| AU2006244072B2 (en) | 2005-05-10 | 2012-09-20 | Intermune, Inc. | Pyridone derivatives for modulating stress-activated protein kinase system |
| WO2007007588A1 (ja) * | 2005-07-08 | 2007-01-18 | Ono Pharmaceutical Co., Ltd. | 平面性を有する環状基を母核とする化合物 |
| EP1998612A4 (en) | 2006-01-25 | 2010-11-24 | Synta Pharmaceuticals Corp | SUBSTITUTED BIARYL COMPOUNDS FOR USE AGAINST INFLAMMATION AND IMMUNE DISORDERS |
| CA2641766A1 (en) | 2006-02-15 | 2007-08-23 | Abbott Laboratories | Novel acetyl-coa carboxylase (acc) inhibitors and their use in diabetes, obesity and metabolic syndrome |
| JP5369257B2 (ja) * | 2006-02-15 | 2013-12-18 | アッヴィ・インコーポレイテッド | 新規なアセチル−CoAカルボキシラーゼ(ACC)阻害薬およびそれらの糖尿病、肥満および代謝症候群での使用 |
| US20090186810A1 (en) * | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| NZ572418A (en) * | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| DE102006025314A1 (de) * | 2006-05-31 | 2007-12-06 | Bayer Healthcare Ag | Arylsubstituierte Heterozyklen und ihre Verwendung |
| DE102006039589A1 (de) * | 2006-08-24 | 2008-03-06 | Bayer Healthcare Ag | Aminoacyl-Prodrugs II |
| US20080242694A1 (en) * | 2006-09-18 | 2008-10-02 | D Sidocky Neil R | Amino-substituted heterocycles, compositions thereof, and methods of treatment therewith |
| AU2007308197A1 (en) * | 2006-10-25 | 2008-05-02 | F. Hoffmann-La Roche Ag | Novel heteroaryl carboxamides |
| US8524907B2 (en) | 2006-11-02 | 2013-09-03 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing pharmaceutical salts of a factor Xa inhibitor |
| US20080293704A1 (en) * | 2007-01-05 | 2008-11-27 | Millennium Pharmaceuticals, Inc. | FACTOR Xa INHIBITORS |
| JP5469595B2 (ja) | 2007-04-13 | 2014-04-16 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | 第Xa因子阻害薬として作用する化合物との併用抗凝固療法 |
| NZ599556A (en) * | 2007-05-02 | 2013-10-25 | Portola Pharm Inc | Combination therapy with a compound acting as a platelet adp receptor inhibitor |
| EP2520561B1 (en) | 2007-06-08 | 2016-02-10 | MannKind Corporation | IRE-1A Inhibitors |
| DE102007028407A1 (de) * | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| DE102007028406A1 (de) | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| DE102007028319A1 (de) * | 2007-06-20 | 2008-12-24 | Bayer Healthcare Ag | Substituierte Oxazolidinone und ihre Verwendung |
| US8168678B2 (en) | 2008-02-01 | 2012-05-01 | Panmira Pharmaceuticals, Inc. | N,N-disubstituted aminoalkylbiphenyl antagonists of prostaglandin D2 receptors |
| AR071069A1 (es) * | 2008-03-26 | 2010-05-26 | Takeda Pharmaceutical | Derivados sustituidos de pirazol y su uso para la prevencion o el tratamiento de cancer |
| CA2721452A1 (en) * | 2008-04-16 | 2009-10-22 | Biolipox Ab | Bis-aryl compounds for use as medicaments |
| EP2296653B1 (en) | 2008-06-03 | 2016-01-27 | Intermune, Inc. | Compounds and methods for treating inflammatory and fibrotic disorders |
| GB2463788B (en) | 2008-09-29 | 2010-12-15 | Amira Pharmaceuticals Inc | Heteroaryl antagonists of prostaglandin D2 receptors |
| WO2010039977A2 (en) | 2008-10-01 | 2010-04-08 | Amira Pharmaceuticals, Inc. | Heteroaryl antagonists of prostaglandin d2 receptors |
| US8524748B2 (en) | 2008-10-08 | 2013-09-03 | Panmira Pharmaceuticals, Llc | Heteroalkyl biphenyl antagonists of prostaglandin D2 receptors |
| MX2012001542A (es) | 2009-08-05 | 2012-06-19 | Panmira Pharmaceuticals Llc | Antagonista dp2 y usos del mismo. |
| US8742120B2 (en) | 2009-12-17 | 2014-06-03 | Millennium Pharmaceuticals, Inc. | Methods of preparing factor xa inhibitors and salts thereof |
| CN102762550B (zh) * | 2009-12-17 | 2015-04-01 | 米伦纽姆医药公司 | Xa因子抑制剂的盐和结晶形式 |
| CA2784904C (en) | 2009-12-17 | 2017-10-10 | Millennium Pharmaceuticals, Inc. | Methods of synthesizing factor xa inhibitors |
| DE102010028362A1 (de) | 2010-04-29 | 2011-11-03 | Bayer Schering Pharma Aktiengesellschaft | Herstellverfahren |
| AR083431A1 (es) | 2010-06-28 | 2013-02-27 | Bayer Cropscience Ag | Compuestos heterociclicos como pesticidas |
| AR082804A1 (es) | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Formas cristalinas de un inhibidor del factor xa |
| AR082803A1 (es) | 2010-09-01 | 2013-01-09 | Portola Pharm Inc | Metodos y formulaciones para el tratamiento de la trombosis con betrixaban y un inhibidor de la glicoproteina p |
| CN102219753B (zh) * | 2011-04-21 | 2012-10-31 | 山东大学 | 一种三氮唑类化合物及其制备方法与应用 |
| US20150224091A1 (en) | 2011-08-31 | 2015-08-13 | Portola Pharmaceuticals, Inc. | Prevention and treatment of thrombosis in medically ill patients |
| MX2015000830A (es) * | 2012-07-18 | 2015-10-26 | Sunshine Lake Pharma Co Ltd | Derivados heterociclicos nitrogenosos y su aplicacion en farmacos. |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| US8987461B2 (en) | 2012-12-06 | 2015-03-24 | Quanticel Pharmaceuticals, Inc. | Histone demethylase inhibitors |
| CN110452216B (zh) | 2014-04-02 | 2022-08-26 | 英特穆恩公司 | 抗纤维化吡啶酮类 |
| WO2015172196A1 (en) * | 2014-05-13 | 2015-11-19 | Monash University | Heterocyclic compounds and use of same |
| CN104045634A (zh) * | 2014-06-06 | 2014-09-17 | 浙江工业大学 | 含二氟甲基吡唑甲酰胺类化合物及其制备方法和用途 |
| TW201706265A (zh) | 2015-03-09 | 2017-02-16 | 必治妥美雅史谷比公司 | 做為Rho激酶(ROCK)抑制劑之內醯胺 |
| EP3078378B1 (en) | 2015-04-08 | 2020-06-24 | Vaiomer | Use of factor xa inhibitors for regulating glycemia |
| PE20180506A1 (es) | 2015-06-03 | 2018-03-09 | Bristol Myers Squibb Co | Agonistas de receptor de apelina (apj) de 4-hidroxi-3-(heteroaril) piridin-2-ona como para uso en el tratamiento de trastornos cardiovasculares |
| AR109304A1 (es) | 2016-08-10 | 2018-11-21 | Sumitomo Chemical Co | Compuesto de oxadiazol y su uso |
| WO2019036024A1 (en) | 2017-08-17 | 2019-02-21 | Bristol-Myers Squibb Company | 2- (1,1'-BIPHENYL) -1H-BENZO [D] IMIDAZOLE DERIVATIVES AND RELATED COMPOUNDS AS AGONISTS OF APELIN AND APJ FOR THE TREATMENT OF CARDIOVASCULAR DISEASES |
| AR119774A1 (es) * | 2019-08-19 | 2022-01-12 | Pi Industries Ltd | Compuestos de oxadiazol que contienen un anillo heteroaromático de 5 miembros para controlar o prevenir hongos fitopatogénicos |
| BR112022010735A2 (pt) | 2019-12-20 | 2022-08-23 | Bayer Ag | Tiofeno carboxamidas substituídos, ácidos tiofeno carboxílicos e derivados dos mesmos |
| BR112022010333A2 (pt) | 2019-12-20 | 2022-08-16 | Bayer Ag | Tieniloxazolonas e análogos |
| AU2021241530A1 (en) * | 2020-03-23 | 2022-10-20 | Praxis Precision Medicines, Inc. | KCNT1 inhibitors and methods of use |
| WO2021207031A1 (en) * | 2020-04-05 | 2021-10-14 | Coagulo Medical Technologies, Inc. | Methods of treating and preventing coronavirus infections using inhibitors of coagulation factor xa |
| AU2022405116A1 (en) | 2021-12-09 | 2024-07-11 | Deciphera Pharmaceuticals, Llc | Raf kinase inhibitors and methods of use thereof |
| EP4393919A1 (en) * | 2022-12-27 | 2024-07-03 | Exscientia Al Limited | Lsd1 modulators |
| US20240336608A1 (en) * | 2023-03-29 | 2024-10-10 | Merck Sharp & Dohme Llc | Il4i1 inhibitors and methods of use |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4588587A (en) | 1983-03-01 | 1986-05-13 | Pennsylvania Hospital | Method of treatment to inhibit metastasis |
| ATE177752T1 (de) | 1992-12-15 | 1999-04-15 | Corvas Int Inc | Neue inhibitoren von faktor xa |
| DE69529770T2 (de) | 1994-12-02 | 2003-12-24 | Yamanouchi Pharmaceutical Co., Ltd. | Neues amidinonaphthylderivat oder dessen salz |
| US5849759A (en) | 1995-12-08 | 1998-12-15 | Berlex Laboratories, Inc. | Naphthyl-substituted benzimidazole derivatives as anti-coagulants |
| IL130286A0 (en) | 1996-12-23 | 2000-06-01 | Du Pont Pharm Co | Nitrogen containing heteroaromatics as factor Xa inhibitors |
| US6514977B1 (en) | 1997-05-22 | 2003-02-04 | G.D. Searle & Company | Substituted pyrazoles as p38 kinase inhibitors |
| KR20010023364A (ko) | 1997-08-27 | 2001-03-26 | 간자와 무츠와 | 3-아미디노아닐린 유도체, 활성화 혈액응고 제 x 인자저해제 및 그것의 제조중간체 |
| GB9725244D0 (en) | 1997-11-29 | 1998-01-28 | Zeneca Ltd | Chemical compounds |
| JP2000178243A (ja) * | 1998-12-14 | 2000-06-27 | Teijin Ltd | ビフェニルアミジン誘導体 |
| US6844367B1 (en) | 1999-09-17 | 2005-01-18 | Millennium Pharmaceuticals, Inc. | Benzamides and related inhibitors of factor Xa |
| WO2001021160A2 (en) | 1999-09-23 | 2001-03-29 | Axxima Pharmaceuticals Aktiengesellschaft | Carboxymide and aniline derivatives as selective inhibitors of pathogens |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| ES2254385T3 (es) | 2000-02-29 | 2006-06-16 | Millennium Pharmaceuticals, Inc. | Benzamidas e inhibidores relacionados del factor xa. |
| DE10027151A1 (de) | 2000-05-31 | 2001-12-06 | Bayer Ag | Herbizide Mittel auf Basis von substituierten Carbonsäureamiden |
| AU2001273040A1 (en) | 2000-06-27 | 2002-01-08 | Du Pont Pharmaceuticals Company | Factor xa inhibitors |
| EP1217000A1 (en) * | 2000-12-23 | 2002-06-26 | Aventis Pharma Deutschland GmbH | Inhibitors of factor Xa and factor VIIa |
| DE10105989A1 (de) * | 2001-02-09 | 2002-08-14 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| US7312235B2 (en) | 2001-03-30 | 2007-12-25 | Millennium Pharmaceuticals, Inc. | Benzamide inhibitors of factor Xa |
| DE10129725A1 (de) | 2001-06-20 | 2003-01-02 | Bayer Ag | Kombinationstherapie substituierter Oxazolidinone |
| ES2180456B1 (es) | 2001-07-20 | 2004-05-01 | Laboratorios S.A.L.V.A.T., S.A. | Isoxazoles sustituidos y su utilizacion como antibioticos. |
| US6914058B2 (en) | 2002-01-18 | 2005-07-05 | Dr. Reddy's Laboratories, Limited | Antibacterial compounds: process for their preparation and pharmaceutical compositions containing them |
| WO2003074501A1 (en) * | 2002-03-07 | 2003-09-12 | Sds Biotech K.K. | Substituted isoxazole alkylamine derivative and agri- and horticultural fungicide |
| JP3090812U (ja) | 2002-06-18 | 2002-12-26 | アルプス電気株式会社 | 高周波モジュール |
| EP1616862A4 (en) * | 2003-04-18 | 2008-07-16 | Ono Pharmaceutical Co | HETEROCYCLIC NITROGEN COMPOUND AND USE THEREOF |
| WO2004101531A1 (en) | 2003-04-29 | 2004-11-25 | Dr. Reddy's Laboratories Ltd. | Antiinfective 1,2,3-triazole derivatives, process for their preparation and pharmaceutical compositions containing them |
| DE10322469A1 (de) * | 2003-05-19 | 2004-12-16 | Bayer Healthcare Ag | Heterocyclische Verbindungen |
| WO2004106329A2 (en) | 2003-06-03 | 2004-12-09 | Dr. Reddy's Laboratories Ltd. | Novel antiinfective compounds and their pharmaceutical compositions |
| US7199149B2 (en) | 2003-10-01 | 2007-04-03 | Bristol Myers Squibb Company | Monocyclic and bicyclic lactams as factor Xa inhibitors |
| US7022695B2 (en) | 2003-10-09 | 2006-04-04 | Millennium Pharmaceuticals, Inc. | Thioether-substituted benzamides as inhibitors of Factor Xa |
| WO2005035528A2 (en) | 2003-10-14 | 2005-04-21 | Dr. Reddy's Laboratories Ltd. | Triazole derivatives as antibacterial agents |
| WO2005082892A2 (en) | 2004-02-17 | 2005-09-09 | Dr. Reddy's Laboratories Ltd. | Triazole compounds as antibacterial agents and pharmaceutical compositions containing them |
| CN1968922A (zh) | 2004-06-18 | 2007-05-23 | 米伦纽姆医药公司 | 因子xa抑制剂 |
| US7696352B2 (en) | 2004-06-18 | 2010-04-13 | Millennium Pharmaceuticals, Inc. | Factor Xa inhibitors |
| JP2008528691A (ja) | 2005-02-02 | 2008-07-31 | ビテ ファーマシューティカルズ, インコーポレイテッド | レニン阻害剤としての1−アシルアミノ−2−ヒドロキシ−3−アミノ−ω−アリールアルカン |
| WO2007007588A1 (ja) | 2005-07-08 | 2007-01-18 | Ono Pharmaceutical Co., Ltd. | 平面性を有する環状基を母核とする化合物 |
| AR057976A1 (es) | 2005-08-29 | 2008-01-09 | Boehringer Ingelheim Int | Biarilos sustituidos y su uso como medicamentos. |
| JP2007060967A (ja) | 2005-08-30 | 2007-03-15 | Tokyo Institute Of Technology | 遺伝子多型の検出方法および薬物のスクリーニング方法 |
| EA017402B1 (ru) | 2005-11-03 | 2012-12-28 | Портола Фармасьютикалз, Инк. | [4-(6-галоген-7-замещенные-2,4-диоксо-1,4-дигидро-2н-хиназолин-3-ил)фенил]-5-хлортиофен-2-илсульфонилмочевины, их формы, способы получения соединений, фармацевтические композиции, содержащие эти соединения, и их применение |
| ATE549317T1 (de) | 2005-11-08 | 2012-03-15 | Millennium Pharm Inc | Pharmazeutische salze und polymorphe aus n-(5- chloro-2-pyridinyl)-2-ää4- ä(dimethylamino)iminomethylübenzoylüaminoü-5- methoxy-benzamid, einem faktor-xa-hemmer |
| US20090186810A1 (en) | 2006-03-27 | 2009-07-23 | Portola Pharmaceuticals, Inc. | Potassium channel modulators and platelet procoagulant activity |
| NZ572418A (en) | 2006-05-05 | 2011-08-26 | Millennium Pharm Inc | Factor xa inhibitors |
| DE102006025314A1 (de) | 2006-05-31 | 2007-12-06 | Bayer Healthcare Ag | Arylsubstituierte Heterozyklen und ihre Verwendung |
| US20080051578A1 (en) | 2006-08-24 | 2008-02-28 | Georg Dahmann | Substituted biaryls, process for their manufacture and use thereof as medicaments |
| ES2409090T3 (es) | 2006-12-08 | 2013-06-24 | Millennium Pharmaceuticals, Inc. | Formulaciones de dosis unitaria y métodos para el tratamiento de trombosis con un inhibidor oral del factor Xa |
| US20080293704A1 (en) * | 2007-01-05 | 2008-11-27 | Millennium Pharmaceuticals, Inc. | FACTOR Xa INHIBITORS |
| JP5469595B2 (ja) | 2007-04-13 | 2014-04-16 | ミレニアム ファーマシューティカルズ, インコーポレイテッド | 第Xa因子阻害薬として作用する化合物との併用抗凝固療法 |
| NZ599556A (en) | 2007-05-02 | 2013-10-25 | Portola Pharm Inc | Combination therapy with a compound acting as a platelet adp receptor inhibitor |
-
2005
- 2005-06-20 CN CNA2005800190908A patent/CN1968922A/zh active Pending
- 2005-06-20 JP JP2007516824A patent/JP5020073B2/ja not_active Expired - Fee Related
- 2005-06-20 US US11/158,274 patent/US7521470B2/en not_active Expired - Fee Related
- 2005-06-20 BR BRPI0512273-2A patent/BRPI0512273A/pt not_active Application Discontinuation
- 2005-06-20 CA CA002565437A patent/CA2565437A1/en not_active Abandoned
- 2005-06-20 NZ NZ552187A patent/NZ552187A/en not_active IP Right Cessation
- 2005-06-20 EP EP05762149.2A patent/EP1893572B1/en not_active Expired - Lifetime
- 2005-06-20 KR KR1020077001313A patent/KR101195801B1/ko not_active Expired - Fee Related
- 2005-06-20 WO PCT/US2005/021817 patent/WO2006002099A2/en not_active Ceased
- 2005-06-20 AU AU2005257999A patent/AU2005257999B2/en not_active Ceased
- 2005-06-20 MX MXPA06013960A patent/MXPA06013960A/es active IP Right Grant
-
2006
- 2006-10-23 IL IL178807A patent/IL178807A0/en unknown
- 2006-12-04 ZA ZA200610138A patent/ZA200610138B/en unknown
-
2009
- 2009-01-05 US US12/348,879 patent/US8153670B2/en not_active Expired - Fee Related
-
2011
- 2011-08-19 US US13/213,927 patent/US8377974B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| KR20070027714A (ko) | 2007-03-09 |
| WO2006002099A2 (en) | 2006-01-05 |
| AU2005257999B2 (en) | 2011-12-08 |
| MXPA06013960A (es) | 2007-03-15 |
| JP2008503497A (ja) | 2008-02-07 |
| US8153670B2 (en) | 2012-04-10 |
| EP1893572A2 (en) | 2008-03-05 |
| CA2565437A1 (en) | 2006-01-05 |
| US20060100193A1 (en) | 2006-05-11 |
| AU2005257999A1 (en) | 2006-01-05 |
| IL178807A0 (en) | 2007-03-08 |
| NZ552187A (en) | 2010-08-27 |
| US20090298806A1 (en) | 2009-12-03 |
| US8377974B2 (en) | 2013-02-19 |
| KR101195801B1 (ko) | 2012-11-05 |
| US20120178733A1 (en) | 2012-07-12 |
| EP1893572B1 (en) | 2016-12-14 |
| BRPI0512273A (pt) | 2008-02-19 |
| US7521470B2 (en) | 2009-04-21 |
| EP1893572A4 (en) | 2010-09-08 |
| ZA200610138B (en) | 2007-12-27 |
| CN1968922A (zh) | 2007-05-23 |
| WO2006002099A3 (en) | 2006-05-04 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP5020073B2 (ja) | 第Xa因子阻害剤 | |
| AU2007247928B2 (en) | Factor XA inhibitors | |
| US7696352B2 (en) | Factor Xa inhibitors | |
| US20080293704A1 (en) | FACTOR Xa INHIBITORS | |
| US7678913B2 (en) | Ureas as factor Xa inhibitors | |
| US7612089B2 (en) | Tetrahydroisoquinolines as factor Xa inhibitors |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20080430 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20080430 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20110309 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20110406 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20110630 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20110707 |
|
| A601 | Written request for extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A601 Effective date: 20110805 |
|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20110809 |
|
| A602 | Written permission of extension of time |
Free format text: JAPANESE INTERMEDIATE CODE: A602 Effective date: 20110812 |
|
| TRDD | Decision of grant or rejection written | ||
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 Effective date: 20120516 |
|
| A01 | Written decision to grant a patent or to grant a registration (utility model) |
Free format text: JAPANESE INTERMEDIATE CODE: A01 |
|
| A61 | First payment of annual fees (during grant procedure) |
Free format text: JAPANESE INTERMEDIATE CODE: A61 Effective date: 20120612 |
|
| R150 | Certificate of patent or registration of utility model |
Ref document number: 5020073 Country of ref document: JP Free format text: JAPANESE INTERMEDIATE CODE: R150 Free format text: JAPANESE INTERMEDIATE CODE: R150 |
|
| FPAY | Renewal fee payment (event date is renewal date of database) |
Free format text: PAYMENT UNTIL: 20150622 Year of fee payment: 3 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| R250 | Receipt of annual fees |
Free format text: JAPANESE INTERMEDIATE CODE: R250 |
|
| LAPS | Cancellation because of no payment of annual fees |