JP2022513959A - 大環状化合物及び疾患の処置におけるそれらの使用 - Google Patents
大環状化合物及び疾患の処置におけるそれらの使用 Download PDFInfo
- Publication number
- JP2022513959A JP2022513959A JP2021534681A JP2021534681A JP2022513959A JP 2022513959 A JP2022513959 A JP 2022513959A JP 2021534681 A JP2021534681 A JP 2021534681A JP 2021534681 A JP2021534681 A JP 2021534681A JP 2022513959 A JP2022513959 A JP 2022513959A
- Authority
- JP
- Japan
- Prior art keywords
- dioxide
- thia
- dipyridina
- trifluoromethyl
- diaza
- 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.)
- Pending
Links
- 0 *c(cc1)cc(-c2c(*)ccc(NS3(=O)=O)n2)c1I*c1cccc3n1 Chemical compound *c(cc1)cc(-c2c(*)ccc(NS3(=O)=O)n2)c1I*c1cccc3n1 0.000 description 25
- AAMUWWQPBXHZBM-UHFFFAOYSA-N C=Cc1ccccc1-c1nc(NS(c2cccc(F)n2)(=O)=O)ccc1C(F)(F)F Chemical compound C=Cc1ccccc1-c1nc(NS(c2cccc(F)n2)(=O)=O)ccc1C(F)(F)F AAMUWWQPBXHZBM-UHFFFAOYSA-N 0.000 description 2
- CKVYUPWCSGLAIU-ISSZAVGLSA-N C/C=C\C=C(\CCCCCCCCN(CCCC(O)=O)c1cccc(S(Nc2ccc3c4n2)(=O)=O)n1)/C4=[F]C3(F)F Chemical compound C/C=C\C=C(\CCCCCCCCN(CCCC(O)=O)c1cccc(S(Nc2ccc3c4n2)(=O)=O)n1)/C4=[F]C3(F)F CKVYUPWCSGLAIU-ISSZAVGLSA-N 0.000 description 1
- MHHAMEZBMQNGLE-UHFFFAOYSA-N C/C=S(\c1cccc(N(CCCN(C(C2C3CCCC2)=O)C3=O)CCCCCc2c-3cccc2)n1)/Nc1ccc(C(F)(F)F)c-3n1 Chemical compound C/C=S(\c1cccc(N(CCCN(C(C2C3CCCC2)=O)C3=O)CCCCCc2c-3cccc2)n1)/Nc1ccc(C(F)(F)F)c-3n1 MHHAMEZBMQNGLE-UHFFFAOYSA-N 0.000 description 1
- AYCUADPAPMPRPI-MJUQQIFVSA-N C=C/C=C\C(\N(CCCC(O)=O)CCCCc(cccc1)c1-c(nc(cc1)N2)c1Cl)=N/S2(=O)=O Chemical compound C=C/C=C\C(\N(CCCC(O)=O)CCCCc(cccc1)c1-c(nc(cc1)N2)c1Cl)=N/S2(=O)=O AYCUADPAPMPRPI-MJUQQIFVSA-N 0.000 description 1
- CCNMIJZBOAEHFY-UHFFFAOYSA-N C=CCCCNCC1(CO)COC1 Chemical compound C=CCCCNCC1(CO)COC1 CCNMIJZBOAEHFY-UHFFFAOYSA-N 0.000 description 1
- SHYVACRLDICWHN-UHFFFAOYSA-N C=CCCCNCCCCO Chemical compound C=CCCCNCCCCO SHYVACRLDICWHN-UHFFFAOYSA-N 0.000 description 1
- RATKWZSKGMMWGC-UHFFFAOYSA-N C=CCNCCCCO Chemical compound C=CCNCCCCO RATKWZSKGMMWGC-UHFFFAOYSA-N 0.000 description 1
- AGMMENUPUPNAOS-UHFFFAOYSA-N C=S1(Nc(nc2C34)ccc2[ClH]C3C=CN=C4NCCCCCNc2nc1ccc2)=O Chemical compound C=S1(Nc(nc2C34)ccc2[ClH]C3C=CN=C4NCCCCCNc2nc1ccc2)=O AGMMENUPUPNAOS-UHFFFAOYSA-N 0.000 description 1
- WUVMEAMJDHEVOF-KTKRTIGZSA-N CC(/C=C\CC(N)S(N1)(=O)=O)N(CCCCC(O)=O)CCCCCc(cccc2)c2-c2c(C(F)(F)F)ccc1n2 Chemical compound CC(/C=C\CC(N)S(N1)(=O)=O)N(CCCCC(O)=O)CCCCCc(cccc2)c2-c2c(C(F)(F)F)ccc1n2 WUVMEAMJDHEVOF-KTKRTIGZSA-N 0.000 description 1
- RGXMINDGVIWFNH-UHFFFAOYSA-N CC(C(C1)(C1C1)c2ccccc2CCCCCN(CCCCO)c2cccc3n2)=CC=C1NS3(=O)=O Chemical compound CC(C(C1)(C1C1)c2ccccc2CCCCCN(CCCCO)c2cccc3n2)=CC=C1NS3(=O)=O RGXMINDGVIWFNH-UHFFFAOYSA-N 0.000 description 1
- HJEZRYIJNHAIGY-UHFFFAOYSA-N CC(C)(C)OC(CCCBr)=O Chemical compound CC(C)(C)OC(CCCBr)=O HJEZRYIJNHAIGY-UHFFFAOYSA-N 0.000 description 1
- SKCDWNFWRVODIY-UHFFFAOYSA-N CC(C)(C)OC(CCCN(CCCOCc1ccccc1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1nc2ccc1)O Chemical compound CC(C)(C)OC(CCCN(CCCOCc1ccccc1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1nc2ccc1)O SKCDWNFWRVODIY-UHFFFAOYSA-N 0.000 description 1
- GOUBSSDOJOWFHJ-UHFFFAOYSA-N CC(C)(C)OC(N(CCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)CCNc1cccc2n1)=O Chemical compound CC(C)(C)OC(N(CCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)CCNc1cccc2n1)=O GOUBSSDOJOWFHJ-UHFFFAOYSA-N 0.000 description 1
- WSOJNMLCLBHUGQ-UXBLZVDNSA-N CC(C)(C)OC(NCCN(CC/C=C/c(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O Chemical compound CC(C)(C)OC(NCCN(CC/C=C/c(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O WSOJNMLCLBHUGQ-UXBLZVDNSA-N 0.000 description 1
- SQIYKCCSAMGUED-UHFFFAOYSA-N CC(C)(C)OC(NCCN(CCC=C)c1cccc(S(Nc2nc(-c3c(C=C)cccc3)c(C(F)(F)F)cc2)(=O)=O)n1)=O Chemical compound CC(C)(C)OC(NCCN(CCC=C)c1cccc(S(Nc2nc(-c3c(C=C)cccc3)c(C(F)(F)F)cc2)(=O)=O)n1)=O SQIYKCCSAMGUED-UHFFFAOYSA-N 0.000 description 1
- MMAVKAGVPNYFLK-UHFFFAOYSA-N CC(C)(C)OC(NCCN(CCCCc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O Chemical compound CC(C)(C)OC(NCCN(CCCCc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O MMAVKAGVPNYFLK-UHFFFAOYSA-N 0.000 description 1
- QEFUSWNXTZEQCS-UHFFFAOYSA-N CC(C)(C)OC(NCCNCCC=C)=O Chemical compound CC(C)(C)OC(NCCNCCC=C)=O QEFUSWNXTZEQCS-UHFFFAOYSA-N 0.000 description 1
- PBJUJOZVYHCBKB-UHFFFAOYSA-N CC(C)(C)ONCCCOCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS(c2nc(F)ccc2)(=O)=O)n1 Chemical compound CC(C)(C)ONCCCOCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS(c2nc(F)ccc2)(=O)=O)n1 PBJUJOZVYHCBKB-UHFFFAOYSA-N 0.000 description 1
- GEUOTHZIXIEJGC-UHFFFAOYSA-N CC(C)(CN(CCCCCc(ccc(F)c1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)C(O)=O Chemical compound CC(C)(CN(CCCCCc(ccc(F)c1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)C(O)=O GEUOTHZIXIEJGC-UHFFFAOYSA-N 0.000 description 1
- LSLPGSHMMCJHFP-GOTSBHOMSA-N CC1(C)O[C@@H](CO)[C@H](CN(CCCCCc(cccc2)c2-c2c(C(F)(F)F)ccc(NS3(=O)=O)n2)c2cccc3n2)O1 Chemical compound CC1(C)O[C@@H](CO)[C@H](CN(CCCCCc(cccc2)c2-c2c(C(F)(F)F)ccc(NS3(=O)=O)n2)c2cccc3n2)O1 LSLPGSHMMCJHFP-GOTSBHOMSA-N 0.000 description 1
- MPDGYCKNRBOUBA-CLFCUDMKSA-N CCCN(CCC/C=C\C=C(/N)\S(Nc1nc(-c2cc(F)ccc2CC=C)c(C(F)(F)F)cc1)(=O)=O)CCCO Chemical compound CCCN(CCC/C=C\C=C(/N)\S(Nc1nc(-c2cc(F)ccc2CC=C)c(C(F)(F)F)cc1)(=O)=O)CCCO MPDGYCKNRBOUBA-CLFCUDMKSA-N 0.000 description 1
- PZYZOJYKNUEDQS-UHFFFAOYSA-N CCN(CCCCO)c1cccc(S(Nc2nc(-c3c(C=C)cccc3)c(C(F)(F)F)cc2)(=O)=O)n1 Chemical compound CCN(CCCCO)c1cccc(S(Nc2nc(-c3c(C=C)cccc3)c(C(F)(F)F)cc2)(=O)=O)n1 PZYZOJYKNUEDQS-UHFFFAOYSA-N 0.000 description 1
- YNDHSQNRGWJGDR-UHFFFAOYSA-N CCOC(CCCNCCCC=C)=O Chemical compound CCOC(CCCNCCCC=C)=O YNDHSQNRGWJGDR-UHFFFAOYSA-N 0.000 description 1
- OIVIZBSSKKRYJY-UHFFFAOYSA-N CCOC(CNCCCC=C)=O Chemical compound CCOC(CNCCCC=C)=O OIVIZBSSKKRYJY-UHFFFAOYSA-N 0.000 description 1
- PDNUDKMYLHAIAD-UHFFFAOYSA-N COC(CN(CCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O Chemical compound COC(CN(CCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O PDNUDKMYLHAIAD-UHFFFAOYSA-N 0.000 description 1
- SCPJAUGAIUQJSD-UHFFFAOYSA-N COC(CNCCCCC=C)=O Chemical compound COC(CNCCCCC=C)=O SCPJAUGAIUQJSD-UHFFFAOYSA-N 0.000 description 1
- ZZXQHZDYADUJCC-UHFFFAOYSA-N Cc1ccccc1C(N(CCCN(CCCCCc(cccc1)c1-c1nc(NS2)ccc1C(F)(F)F)c1nc2ccc1)C=O)=O Chemical compound Cc1ccccc1C(N(CCCN(CCCCCc(cccc1)c1-c1nc(NS2)ccc1C(F)(F)F)c1nc2ccc1)C=O)=O ZZXQHZDYADUJCC-UHFFFAOYSA-N 0.000 description 1
- PQOZYVTUPKTNRL-UHFFFAOYSA-N Cc1ccnc(Cl)c1-c1nc(NS(c2nc(F)ccc2)(=O)=O)ccc1Cl Chemical compound Cc1ccnc(Cl)c1-c1nc(NS(c2nc(F)ccc2)(=O)=O)ccc1Cl PQOZYVTUPKTNRL-UHFFFAOYSA-N 0.000 description 1
- QVFSHFNZPLWBID-UHFFFAOYSA-N NCCCOCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS(c2nc(F)ccc2)(=O)=O)n1 Chemical compound NCCCOCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS(c2nc(F)ccc2)(=O)=O)n1 QVFSHFNZPLWBID-UHFFFAOYSA-N 0.000 description 1
- LZETXPGGJFQDTP-WTDSWWLTSA-N O=C(c1ccccc11)N(CCCN(CCC/C=C/c(cccc2)c2-c2nc(NS3(=O)=O)ccc2C(F)(F)F)c2nc3ccc2)C1=O Chemical compound O=C(c1ccccc11)N(CCCN(CCC/C=C/c(cccc2)c2-c2nc(NS3(=O)=O)ccc2C(F)(F)F)c2nc3ccc2)C1=O LZETXPGGJFQDTP-WTDSWWLTSA-N 0.000 description 1
- GCVIFZZHJJFJCQ-UHFFFAOYSA-N O=CCCCN(CCCCCc(cccc1)c1-c1nc(NS2OC=O)ccc1C(F)(F)F)c1nc2ccc1 Chemical compound O=CCCCN(CCCCCc(cccc1)c1-c1nc(NS2OC=O)ccc1C(F)(F)F)c1nc2ccc1 GCVIFZZHJJFJCQ-UHFFFAOYSA-N 0.000 description 1
- VVEDQCCYDOSXET-UHFFFAOYSA-N O=S(c1cccc(F)n1)(Nc1nc(-c(cccn2)c2F)c(C(F)(F)F)cc1)=O Chemical compound O=S(c1cccc(F)n1)(Nc1nc(-c(cccn2)c2F)c(C(F)(F)F)cc1)=O VVEDQCCYDOSXET-UHFFFAOYSA-N 0.000 description 1
- MDWAUKXIVBXREA-UHFFFAOYSA-N O=S(c1cccc(NCCCCCNc2ncccc2-2)n1)(Nc1ccc(C(F)(F)F)c-2n1)=O Chemical compound O=S(c1cccc(NCCCCCNc2ncccc2-2)n1)(Nc1ccc(C(F)(F)F)c-2n1)=O MDWAUKXIVBXREA-UHFFFAOYSA-N 0.000 description 1
- XKKUHYBAQQCVHJ-UHFFFAOYSA-N O=S(c1cccc(OCCCCCOc2c-3cccn2)n1)(Nc1ccc(C(F)(F)F)c-3n1)=O Chemical compound O=S(c1cccc(OCCCCCOc2c-3cccn2)n1)(Nc1ccc(C(F)(F)F)c-3n1)=O XKKUHYBAQQCVHJ-UHFFFAOYSA-N 0.000 description 1
- JEYNHGHPXQAVPY-UHFFFAOYSA-N O=S(c1nc(NCCNCCCCc2c-3cccc2)ccc1)(Nc1nc-3c(C(F)(F)F)cc1)=O Chemical compound O=S(c1nc(NCCNCCCCc2c-3cccc2)ccc1)(Nc1nc-3c(C(F)(F)F)cc1)=O JEYNHGHPXQAVPY-UHFFFAOYSA-N 0.000 description 1
- ZTEYXNOHDSCOFX-UHFFFAOYSA-N OC(CCCCCN(CCCCCC1C(c(nc(cc2)NS3(=O)=O)c2Cl)=CC=CC1)c1cccc3n1)=O Chemical compound OC(CCCCCN(CCCCCC1C(c(nc(cc2)NS3(=O)=O)c2Cl)=CC=CC1)c1cccc3n1)=O ZTEYXNOHDSCOFX-UHFFFAOYSA-N 0.000 description 1
- OZBWJBDRFXFHDU-UHFFFAOYSA-N OC(CCCCN(CCCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O Chemical compound OC(CCCCN(CCCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O OZBWJBDRFXFHDU-UHFFFAOYSA-N 0.000 description 1
- SHMWYLMPWLOFNO-UHFFFAOYSA-N OC(CCCN(CCCCCc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O Chemical compound OC(CCCN(CCCCCc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O SHMWYLMPWLOFNO-UHFFFAOYSA-N 0.000 description 1
- KSJHHPZTDAUPNN-UHFFFAOYSA-N OC(CCCN(CCCOCc1ccccc1-c1c(C(F)(F)F)ccc(NS2)n1)c1cccc2n1)=O Chemical compound OC(CCCN(CCCOCc1ccccc1-c1c(C(F)(F)F)ccc(NS2)n1)c1cccc2n1)=O KSJHHPZTDAUPNN-UHFFFAOYSA-N 0.000 description 1
- VFHLNVTYZYCZEN-UHFFFAOYSA-N OC(CCN(CCCCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O Chemical compound OC(CCN(CCCCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O VFHLNVTYZYCZEN-UHFFFAOYSA-N 0.000 description 1
- JZJSFHOIDKXCQT-UHFFFAOYSA-N OC(CCN(CCCCCc(c(-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1)ccc1F)c1cccc2n1)=O Chemical compound OC(CCN(CCCCCc(c(-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1)ccc1F)c1cccc2n1)=O JZJSFHOIDKXCQT-UHFFFAOYSA-N 0.000 description 1
- GQZWHXIYPNNGGG-UHFFFAOYSA-N OC(CN(CCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O Chemical compound OC(CN(CCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)=O GQZWHXIYPNNGGG-UHFFFAOYSA-N 0.000 description 1
- GMVQPLFPROXPQJ-UHFFFAOYSA-N OC(CN(CCCCOc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O Chemical compound OC(CN(CCCCOc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1)=O GMVQPLFPROXPQJ-UHFFFAOYSA-N 0.000 description 1
- GTTKGSDAHVOHSD-UHFFFAOYSA-N OCC1(CN(CCCCCc2ccccc2-c2c(C(F)(F)F)ccc(NS3(=O)=O)n2)c2cccc3n2)CC1 Chemical compound OCC1(CN(CCCCCc2ccccc2-c2c(C(F)(F)F)ccc(NS3(=O)=O)n2)c2cccc3n2)CC1 GTTKGSDAHVOHSD-UHFFFAOYSA-N 0.000 description 1
- GUVYPXTZRDDFOY-XNWCZRBMSA-N OCCCCN(CCC/C=C/c(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1 Chemical compound OCCCCN(CCC/C=C/c(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1 GUVYPXTZRDDFOY-XNWCZRBMSA-N 0.000 description 1
- XBFLGVKYRZIAMW-UHFFFAOYSA-N OCCCCN(CCCCCCc(ccc(F)c1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 Chemical compound OCCCCN(CCCCCCc(ccc(F)c1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 XBFLGVKYRZIAMW-UHFFFAOYSA-N 0.000 description 1
- PQMUXJRERFMSMC-UHFFFAOYSA-N OCCCCN(CCCCCc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1 Chemical compound OCCCCN(CCCCCc(cccc1)c1-c1nc(NS2(=O)=O)ccc1C(F)(F)F)c1nc2ccc1 PQMUXJRERFMSMC-UHFFFAOYSA-N 0.000 description 1
- ZEFFPNIKFAPKNB-UHFFFAOYSA-N OCCCCN(CCCCc(cccc1)c1-c(nc(cc1)NS2(=O)=O)c1Cl)c1nc2ccc1 Chemical compound OCCCCN(CCCCc(cccc1)c1-c(nc(cc1)NS2(=O)=O)c1Cl)c1nc2ccc1 ZEFFPNIKFAPKNB-UHFFFAOYSA-N 0.000 description 1
- PWINRDJHKCJUHZ-UHFFFAOYSA-N OCCCN(CCCCCCCc1ccccc1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 Chemical compound OCCCN(CCCCCCCc1ccccc1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 PWINRDJHKCJUHZ-UHFFFAOYSA-N 0.000 description 1
- OFJJEEHLFYNLBR-UHFFFAOYSA-N OCCCN(CCCCCCc(ccc(F)c1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 Chemical compound OCCCN(CCCCCCc(ccc(F)c1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 OFJJEEHLFYNLBR-UHFFFAOYSA-N 0.000 description 1
- MCERMXMSQMRPOV-UHFFFAOYSA-N OCCCN(CCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 Chemical compound OCCCN(CCCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1 MCERMXMSQMRPOV-UHFFFAOYSA-N 0.000 description 1
- FYUOZOQVDXBZGX-GOTSBHOMSA-N O[C@@H](CN(CCN(CCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)C1)[C@H]1O Chemical compound O[C@@H](CN(CCN(CCCCCc(cccc1)c1-c1c(C(F)(F)F)ccc(NS2(=O)=O)n1)c1cccc2n1)C1)[C@H]1O FYUOZOQVDXBZGX-GOTSBHOMSA-N 0.000 description 1
- YUFHEWITJCJOBY-UHFFFAOYSA-N [O]#[S]1(NC(CC=C2C(F)(F)F)N=C2c2ccccc2CC/C=[O]/CCN(CC2CC2)c2cccc1n2)#[O] Chemical compound [O]#[S]1(NC(CC=C2C(F)(F)F)N=C2c2ccccc2CC/C=[O]/CCN(CC2CC2)c2cccc1n2)#[O] YUFHEWITJCJOBY-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D419/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms
- C07D419/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen, oxygen, and sulfur 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/439—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom the ring forming part of a bridged ring system, e.g. quinuclidine
-
- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
-
- 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
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
-
- 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
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D513/18—Bridged systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
- C07D515/18—Bridged systems
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pulmonology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862783270P | 2018-12-21 | 2018-12-21 | |
| US62/783,270 | 2018-12-21 | ||
| PCT/IB2019/061054 WO2020128925A1 (en) | 2018-12-21 | 2019-12-18 | Macrocyclic compounds and their use in the treatment of disease |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2022513959A true JP2022513959A (ja) | 2022-02-09 |
| JP2022513959A5 JP2022513959A5 (https=) | 2022-11-07 |
Family
ID=69165443
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021534681A Pending JP2022513959A (ja) | 2018-12-21 | 2019-12-18 | 大環状化合物及び疾患の処置におけるそれらの使用 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20220071971A1 (https=) |
| EP (1) | EP3898621A1 (https=) |
| JP (1) | JP2022513959A (https=) |
| KR (1) | KR20210107046A (https=) |
| CN (1) | CN113227087A (https=) |
| AU (1) | AU2019404934B2 (https=) |
| BR (1) | BR112021011643A2 (https=) |
| CA (1) | CA3119656A1 (https=) |
| MX (1) | MX2021007592A (https=) |
| WO (1) | WO2020128925A1 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2019222758B2 (en) | 2018-02-15 | 2022-07-07 | Vertex Pharmaceuticals Incorporated | Macrocycles as modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions thereof, their use in the treatment of cystic fibrosis, and process for making them |
| TWI848092B (zh) | 2019-04-03 | 2024-07-11 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白調節劑 |
| CA3150162A1 (en) | 2019-08-14 | 2021-02-18 | Vertex Pharmaceuticals Incorporated | Crystalline forms of cftr modulators |
| TWI899097B (zh) | 2019-08-14 | 2025-10-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
| TWI867024B (zh) | 2019-08-14 | 2024-12-21 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
| WO2022194399A1 (en) | 2020-07-13 | 2022-09-22 | Idorsia Pharmaceuticals Ltd | Macrocycles as cftr modulators |
| CR20230120A (es) * | 2020-08-07 | 2023-09-01 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quística |
| IL300413A (en) | 2020-08-13 | 2023-04-01 | Vertex Pharma | Crystal forms of CFTR modulators |
| EP4225762A1 (en) | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225765A2 (en) * | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| EP4225447A1 (en) * | 2020-10-07 | 2023-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
| MX2023004074A (es) * | 2020-10-07 | 2023-07-05 | Vertex Pharma | Moduladores del regulador de la conductancia transmembrana de la fibrosis quistica. |
| AU2021397294A1 (en) | 2020-12-10 | 2023-07-06 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
| EP4308575A1 (en) * | 2021-03-16 | 2024-01-24 | Idorsia Pharmaceuticals Ltd | Macrocycles as cftr modulators |
| TWI904194B (zh) * | 2021-07-12 | 2025-11-11 | 瑞士商愛杜西亞製藥有限公司 | 作為cftr調節劑之巨環 |
| IL315715A (en) * | 2022-04-06 | 2024-11-01 | Vertex Pharma | Modulators of cystic fibrosis transmembrane conductance regulation |
| TW202421102A (zh) | 2022-09-15 | 2024-06-01 | 瑞士商愛杜西亞製藥有限公司 | 巨環cftr調節劑與cftr校正子及/或cftr增效劑之組合 |
| CA3267791A1 (en) | 2022-09-15 | 2024-03-21 | Idorsia Pharmaceuticals Ltd | CRYSTALLINE FORM OF (3S,7S,10R,13R)-13-BENZYL-20-FLUORO-7-ISOBUTYL-N-(2-(3-METHOXY-1,2,4-OXADIAZOL-5-YL)ETHYL)-6,9-DIMETHYL-1,5,8,11-TETRAOXO-10-(2,2,2-TRIFLUOROETHYL)-1,2,3,4,5,6,7,8,9,10,11,12,13,14-TETRADECAHYDRO-[1]OXA[4,7,10,14]TETRAAZACYCLOHEPTADECINO [16,17-F]QUINOLINE-3-CARBOXAMIDE |
| KR20250084132A (ko) | 2022-09-15 | 2025-06-10 | 이도르시아 파마슈티컬스 리미티드 | 마크로시클릭 cftr 조절제 |
| CN115498160B (zh) * | 2022-09-29 | 2025-09-30 | 郑州大学 | 一种锂-有机硫电池正极材料及其制备方法和应用 |
| WO2025186214A1 (en) | 2024-03-05 | 2025-09-12 | Idorsia Pharmaceuticals Ltd | Macrocyclic cftr modulators |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015138934A1 (en) * | 2014-03-13 | 2015-09-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US20160002265A1 (en) * | 2013-03-15 | 2016-01-07 | Biogen Ma Inc. | Macrocyclic compounds as irak4 inhibitors for the treatment of inflammatory diseases |
| US20170101395A1 (en) * | 2015-10-07 | 2017-04-13 | NuBridge BioSciences | Pyrimidine derivatives as cftr modulators |
| WO2018042316A1 (en) * | 2016-08-29 | 2018-03-08 | Novartis Ag | N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease |
| WO2018148204A1 (en) * | 2017-02-07 | 2018-08-16 | Biogen Ma Inc. | Ask1 inhibiting agents |
| JP2021513967A (ja) * | 2018-02-15 | 2021-06-03 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 嚢胞性線維症膜コンダクタンス制御因子のモジュレーターとしての大環状分子、それらの医薬組成物、嚢胞性線維症の治療におけるそれらの使用、及びそれらの製造方法 |
-
2019
- 2019-12-18 CA CA3119656A patent/CA3119656A1/en active Pending
- 2019-12-18 EP EP19836572.8A patent/EP3898621A1/en not_active Withdrawn
- 2019-12-18 BR BR112021011643-5A patent/BR112021011643A2/pt not_active IP Right Cessation
- 2019-12-18 JP JP2021534681A patent/JP2022513959A/ja active Pending
- 2019-12-18 CN CN201980083703.6A patent/CN113227087A/zh active Pending
- 2019-12-18 US US17/415,335 patent/US20220071971A1/en not_active Abandoned
- 2019-12-18 AU AU2019404934A patent/AU2019404934B2/en not_active Ceased
- 2019-12-18 MX MX2021007592A patent/MX2021007592A/es unknown
- 2019-12-18 WO PCT/IB2019/061054 patent/WO2020128925A1/en not_active Ceased
- 2019-12-18 KR KR1020217022294A patent/KR20210107046A/ko not_active Ceased
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20160002265A1 (en) * | 2013-03-15 | 2016-01-07 | Biogen Ma Inc. | Macrocyclic compounds as irak4 inhibitors for the treatment of inflammatory diseases |
| WO2015138934A1 (en) * | 2014-03-13 | 2015-09-17 | Proteostasis Therapeutics, Inc. | Compounds, compositions, and methods for increasing cftr activity |
| US20170101395A1 (en) * | 2015-10-07 | 2017-04-13 | NuBridge BioSciences | Pyrimidine derivatives as cftr modulators |
| WO2018042316A1 (en) * | 2016-08-29 | 2018-03-08 | Novartis Ag | N-(pyridin-2-yl)pyridine-sulfonamide derivatives and their use in the treatment of disease |
| WO2018148204A1 (en) * | 2017-02-07 | 2018-08-16 | Biogen Ma Inc. | Ask1 inhibiting agents |
| JP2021513967A (ja) * | 2018-02-15 | 2021-06-03 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | 嚢胞性線維症膜コンダクタンス制御因子のモジュレーターとしての大環状分子、それらの医薬組成物、嚢胞性線維症の治療におけるそれらの使用、及びそれらの製造方法 |
Non-Patent Citations (1)
| Title |
|---|
| PUAY-WAH PHUAN ET AL.: "Synergy-Based Small-Molecule Screen Using a Human Lung Epithelial Cell Line Yields ΔF508-CFTR Corre", MOLECULAR PHARMACOLOGY, vol. 86(1), JPN6023044825, 2014, pages 42 - 51, ISSN: 0005191038 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2019404934A1 (en) | 2021-06-03 |
| CN113227087A (zh) | 2021-08-06 |
| BR112021011643A2 (pt) | 2021-09-08 |
| EP3898621A1 (en) | 2021-10-27 |
| WO2020128925A1 (en) | 2020-06-25 |
| KR20210107046A (ko) | 2021-08-31 |
| US20220071971A1 (en) | 2022-03-10 |
| CA3119656A1 (en) | 2020-06-25 |
| AU2019404934B2 (en) | 2022-04-21 |
| MX2021007592A (es) | 2021-08-11 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2022513959A (ja) | 大環状化合物及び疾患の処置におけるそれらの使用 | |
| JP2022513959A5 (https=) | ||
| JP7035055B2 (ja) | N-(ピリジン-2-イル)ピリジン-スルホンアミド誘導体および疾患の処置におけるそれらの使用 | |
| US12583824B2 (en) | 6-membered heteroarylaminosulfonamides for treating diseases and conditions mediated by deficient CFTR activity | |
| TWI703154B (zh) | 作為鈉通道調節劑之吡啶酮醯胺之前藥 | |
| KR20220092920A (ko) | 헬리오스의 소분자 분해제 및 사용 방법 | |
| EP3150592B1 (en) | Alk kinase inhibitor, and preparation method and use thereof | |
| CN109790166A (zh) | 咪唑并吡啶化合物用于治疗癌症 | |
| CN105085482B (zh) | 取代的哌嗪化合物及其使用方法和用途 | |
| JP2022519301A (ja) | N-(ピリジン-2-イル)ピリジン-スルホンアミド誘導体及び疾患の処置におけるそれらの使用 | |
| TW200930703A (en) | Quinolone derivative | |
| AU2017201916B2 (en) | Salts, co-crystals, and polymorphs of an anxiolytic compound | |
| US20230143552A1 (en) | Dopamine d2 receptor ligands | |
| JP2022514253A (ja) | N-(ピリジン-2-イルスルホニル)シクロプロパンカルボキサミド誘導体及びcftr媒介疾患の処置におけるその使用 | |
| JP7508620B2 (ja) | ジヒドロクロメン誘導体 | |
| ES2837018T3 (es) | Ligandos del receptor D3 de dopamina de 6,7,8,9-tetrahidro-5H-pirido[2,3-d]azepina | |
| JP2018109011A (ja) | 抗不安化合物の結晶形態 | |
| US20230159439A1 (en) | Arylamides and methods of use thereof | |
| US20250177382A1 (en) | Nek7 inhibitors | |
| RU2804139C2 (ru) | Макроциклические соединения и их применение в лечении заболевания | |
| TW202304906A (zh) | 高活性hpk1激酶抑制劑 | |
| TW202410897A (zh) | 聯芳醚脲化合物 | |
| CN106065018A (zh) | 取代的吲哚化合物及其使用方法和用途 | |
| WO2025067417A1 (zh) | 并内酰胺环类化合物及其用途 | |
| TW202540096A (zh) | 靶向降解雄激素受體的雙功能嵌合體的雜環化合物及其用途 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| A524 | Written submission of copy of amendment under article 19 pct |
Free format text: JAPANESE INTERMEDIATE CODE: A524 Effective date: 20221027 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20221027 |
|
| A977 | Report on retrieval |
Free format text: JAPANESE INTERMEDIATE CODE: A971007 Effective date: 20231012 |
|
| A131 | Notification of reasons for refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A131 Effective date: 20231107 |
|
| A02 | Decision of refusal |
Free format text: JAPANESE INTERMEDIATE CODE: A02 Effective date: 20240604 |