AU2015259173B2 - Hsp70 modulators and methods for making and using the same - Google Patents
Hsp70 modulators and methods for making and using the same Download PDFInfo
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- AU2015259173B2 AU2015259173B2 AU2015259173A AU2015259173A AU2015259173B2 AU 2015259173 B2 AU2015259173 B2 AU 2015259173B2 AU 2015259173 A AU2015259173 A AU 2015259173A AU 2015259173 A AU2015259173 A AU 2015259173A AU 2015259173 B2 AU2015259173 B2 AU 2015259173B2
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- 0 CN1CC(*)C1 Chemical compound CN1CC(*)C1 0.000 description 14
- ZZZRXGKTICQJAP-UHFFFAOYSA-N C#CCN(CC1)CCN1c(nc1OCc2cccc(Cl)c2)ncc1Sc(cc1C(F)(F)F)ccc1C#N Chemical compound C#CCN(CC1)CCN1c(nc1OCc2cccc(Cl)c2)ncc1Sc(cc1C(F)(F)F)ccc1C#N ZZZRXGKTICQJAP-UHFFFAOYSA-N 0.000 description 1
- CUVQEZIRSILQRS-UHFFFAOYSA-N C#CCN(CC1)CCN1c(nc1OCc2cccc(Cl)c2)ncc1Sc1ccc(C(N)=O)c(C(F)(F)F)c1 Chemical compound C#CCN(CC1)CCN1c(nc1OCc2cccc(Cl)c2)ncc1Sc1ccc(C(N)=O)c(C(F)(F)F)c1 CUVQEZIRSILQRS-UHFFFAOYSA-N 0.000 description 1
- AJFZGQPNNLDIQM-LNKIKWGQSA-N C/C(/COc1nc(N2CCNCC2)ncc1Sc(cc1)cnc1N)=C\C=C Chemical compound C/C(/COc1nc(N2CCNCC2)ncc1Sc(cc1)cnc1N)=C\C=C AJFZGQPNNLDIQM-LNKIKWGQSA-N 0.000 description 1
- PTYHVJFDGLJOFU-UHFFFAOYSA-N CC(C)(C1)N(C)CCN1c(nc1OCc2cccc(C)c2)ncc1Sc(cc1)ccc1C#N Chemical compound CC(C)(C1)N(C)CCN1c(nc1OCc2cccc(C)c2)ncc1Sc(cc1)ccc1C#N PTYHVJFDGLJOFU-UHFFFAOYSA-N 0.000 description 1
- PDLCCNYKIIUWHA-UHFFFAOYSA-N CC(C)c(cc1)ccc1C(C)=O Chemical compound CC(C)c(cc1)ccc1C(C)=O PDLCCNYKIIUWHA-UHFFFAOYSA-N 0.000 description 1
- MLXDAOFCUKUYQP-UHFFFAOYSA-N CC(C)c1ccc(C(N)=O)c(F)c1 Chemical compound CC(C)c1ccc(C(N)=O)c(F)c1 MLXDAOFCUKUYQP-UHFFFAOYSA-N 0.000 description 1
- YVRXGIACHNLZCV-GOSISDBHSA-N CC(c(cc1)ccc1Sc1cnc(N(CC2)C[C@@H]2NC)nc1OCc1cc(N)ncc1)=O Chemical compound CC(c(cc1)ccc1Sc1cnc(N(CC2)C[C@@H]2NC)nc1OCc1cc(N)ncc1)=O YVRXGIACHNLZCV-GOSISDBHSA-N 0.000 description 1
- CDRHURWXGOLMEI-JXMROGBWSA-N CCOC(/C=C/c(cc1)ccc1C(OCC)=O)=O Chemical compound CCOC(/C=C/c(cc1)ccc1C(OCC)=O)=O CDRHURWXGOLMEI-JXMROGBWSA-N 0.000 description 1
- XFJORYJXGYFUCY-UHFFFAOYSA-N CCOC(C(Cc(cc1)ccc1C(OCC)=O)C=O)=O Chemical compound CCOC(C(Cc(cc1)ccc1C(OCC)=O)C=O)=O XFJORYJXGYFUCY-UHFFFAOYSA-N 0.000 description 1
- OYMFFRUCMOQDON-UHFFFAOYSA-N CCOC(CCc(cc1)ccc1C(OCC)=O)=O Chemical compound CCOC(CCc(cc1)ccc1C(OCC)=O)=O OYMFFRUCMOQDON-UHFFFAOYSA-N 0.000 description 1
- SWQFPRDHVYGYBA-UHFFFAOYSA-N CCOC(COc(cc1)ccc1C#N)=C Chemical compound CCOC(COc(cc1)ccc1C#N)=C SWQFPRDHVYGYBA-UHFFFAOYSA-N 0.000 description 1
- VGQWAZLAYNRZEE-UHFFFAOYSA-N CCc1cc(COc2nc(N3CCN(C)CC3)ncc2Sc(cc2C(F)(F)F)ccc2C#N)ccc1 Chemical compound CCc1cc(COc2nc(N3CCN(C)CC3)ncc2Sc(cc2C(F)(F)F)ccc2C#N)ccc1 VGQWAZLAYNRZEE-UHFFFAOYSA-N 0.000 description 1
- IZRMJQMKVULXCP-UHFFFAOYSA-N CN(C)C(CC1)CN1c(nc1O)ncc1Sc(cc1)cnc1N Chemical compound CN(C)C(CC1)CN1c(nc1O)ncc1Sc(cc1)cnc1N IZRMJQMKVULXCP-UHFFFAOYSA-N 0.000 description 1
- PEXJKRSJDMUVBX-UHFFFAOYSA-N CN(C)C(CC1)CN1c(nc1OCc2cc(Cl)ccc2)ncc1Sc(cc1)cnc1N Chemical compound CN(C)C(CC1)CN1c(nc1OCc2cc(Cl)ccc2)ncc1Sc(cc1)cnc1N PEXJKRSJDMUVBX-UHFFFAOYSA-N 0.000 description 1
- BTWSFOJQRYVLCR-UHFFFAOYSA-N CN(CC1)CCN1c(nc1)nc(OCc2cccc(C#N)c2)c1Sc(cc1)ccc1C#N Chemical compound CN(CC1)CCN1c(nc1)nc(OCc2cccc(C#N)c2)c1Sc(cc1)ccc1C#N BTWSFOJQRYVLCR-UHFFFAOYSA-N 0.000 description 1
- DSIBSFXNFQSBLJ-UHFFFAOYSA-N CN(CC1)CCN1c(nc1)nc(OCc2ccccc2)c1Oc(cc1)ccc1C#N Chemical compound CN(CC1)CCN1c(nc1)nc(OCc2ccccc2)c1Oc(cc1)ccc1C#N DSIBSFXNFQSBLJ-UHFFFAOYSA-N 0.000 description 1
- YVUVIRQUINTZNL-UHFFFAOYSA-N CN(CC1)CCN1c(nc1)nc(OCc2ccccc2)c1Oc(cc1)ccc1C(N)=O Chemical compound CN(CC1)CCN1c(nc1)nc(OCc2ccccc2)c1Oc(cc1)ccc1C(N)=O YVUVIRQUINTZNL-UHFFFAOYSA-N 0.000 description 1
- SSMTZPQOKGRABN-UHFFFAOYSA-N CN(CC1)CCN1c(nc1OCc2ccccc2)ncc1Sc(cc1)ccc1C(OC)=O Chemical compound CN(CC1)CCN1c(nc1OCc2ccccc2)ncc1Sc(cc1)ccc1C(OC)=O SSMTZPQOKGRABN-UHFFFAOYSA-N 0.000 description 1
- AKFQWZHTEPWQMD-UHFFFAOYSA-N CN(CC1)CCN1c(nc1OCc2ccccc2)ncc1Sc1c(N)nccc1 Chemical compound CN(CC1)CCN1c(nc1OCc2ccccc2)ncc1Sc1c(N)nccc1 AKFQWZHTEPWQMD-UHFFFAOYSA-N 0.000 description 1
- FXLWNYKQWJQEDG-UHFFFAOYSA-N CN(CC1)CCN1c1nc(OCc(cc2)ccc2C#N)c(Cc(cc2)ccc2C(N)=O)cn1 Chemical compound CN(CC1)CCN1c1nc(OCc(cc2)ccc2C#N)c(Cc(cc2)ccc2C(N)=O)cn1 FXLWNYKQWJQEDG-UHFFFAOYSA-N 0.000 description 1
- PSRSDJWVGVWFBW-UHFFFAOYSA-N CN(CC1)CCN1c1nc(OCc2ccccc2)c(Cc(cc2)ccc2C(N)=O)cn1 Chemical compound CN(CC1)CCN1c1nc(OCc2ccccc2)c(Cc(cc2)ccc2C(N)=O)cn1 PSRSDJWVGVWFBW-UHFFFAOYSA-N 0.000 description 1
- SXXIZVPDUPGXGG-UHFFFAOYSA-N CN(CCN(C1)c(nc2OCc3cccc(OC)c3)ncc2Sc(cc2)ccc2C(N)=O)C1=O Chemical compound CN(CCN(C1)c(nc2OCc3cccc(OC)c3)ncc2Sc(cc2)ccc2C(N)=O)C1=O SXXIZVPDUPGXGG-UHFFFAOYSA-N 0.000 description 1
- CDZMIJFSAZPYEZ-VOTSOKGWSA-N COC(/C=C/c(cc1)ccc1C#N)=O Chemical compound COC(/C=C/c(cc1)ccc1C#N)=O CDZMIJFSAZPYEZ-VOTSOKGWSA-N 0.000 description 1
- BDKBJHDTWPUYOW-UHFFFAOYSA-N COc(cc(COc1nc(Cl)ncc1Sc(cc1)cc(Cl)c1C#N)cc1)c1F Chemical compound COc(cc(COc1nc(Cl)ncc1Sc(cc1)cc(Cl)c1C#N)cc1)c1F BDKBJHDTWPUYOW-UHFFFAOYSA-N 0.000 description 1
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- RXJYRABGWBCEHE-UHFFFAOYSA-N COc1cccc(COc(nc(N2CCN(Cc3ccc[o]3)CC2)nc2)c2Sc(cc2)ccc2C#N)c1 Chemical compound COc1cccc(COc(nc(N2CCN(Cc3ccc[o]3)CC2)nc2)c2Sc(cc2)ccc2C#N)c1 RXJYRABGWBCEHE-UHFFFAOYSA-N 0.000 description 1
- NANNLPAAJYQWGH-UHFFFAOYSA-N COc1cccc(COc2nc(N3CCN(CCCCC#C)CC3)ncc2Sc(cc2)ccc2C#N)c1 Chemical compound COc1cccc(COc2nc(N3CCN(CCCCC#C)CC3)ncc2Sc(cc2)ccc2C#N)c1 NANNLPAAJYQWGH-UHFFFAOYSA-N 0.000 description 1
- GVWAZHUWEBCHPP-UHFFFAOYSA-N CS(c1nc(OCc(cc2)ccc2C#N)c(Cc(cc2)ccc2C(N)=O)cn1)(=O)=O Chemical compound CS(c1nc(OCc(cc2)ccc2C#N)c(Cc(cc2)ccc2C(N)=O)cn1)(=O)=O GVWAZHUWEBCHPP-UHFFFAOYSA-N 0.000 description 1
- HZJSJLQIGHULCL-UHFFFAOYSA-N CSc1nc(OCc(cc2)ccc2C#N)c(Cc(cc2)ccc2C(N)=O)cn1 Chemical compound CSc1nc(OCc(cc2)ccc2C#N)c(Cc(cc2)ccc2C(N)=O)cn1 HZJSJLQIGHULCL-UHFFFAOYSA-N 0.000 description 1
- ODDTVVQPZZQIEE-ZWKOTPCHSA-N C[C@@H](C1)N(C)C[C@@H](C)N1c(nc1OCc2ccccc2)ncc1Sc(cc1)ccc1C(N)=O Chemical compound C[C@@H](C1)N(C)C[C@@H](C)N1c(nc1OCc2ccccc2)ncc1Sc(cc1)ccc1C(N)=O ODDTVVQPZZQIEE-ZWKOTPCHSA-N 0.000 description 1
- XIBBOOKVCXHOAY-KRWDZBQOSA-N C[C@@H](c(cc1)ccc1F)Oc(nc(N1CCN(C)CC1)nc1)c1Sc(cc1)ccc1C#N Chemical compound C[C@@H](c(cc1)ccc1F)Oc(nc(N1CCN(C)CC1)nc1)c1Sc(cc1)ccc1C#N XIBBOOKVCXHOAY-KRWDZBQOSA-N 0.000 description 1
- SGVKTXOXEGGKFR-GOSISDBHSA-N C[C@H](c(cc1)ccc1F)Oc(nc(N1CCN(C)CC1)nc1)c1Sc(cc1)ccc1C(C)=O Chemical compound C[C@H](c(cc1)ccc1F)Oc(nc(N1CCN(C)CC1)nc1)c1Sc(cc1)ccc1C(C)=O SGVKTXOXEGGKFR-GOSISDBHSA-N 0.000 description 1
- HHAOOPAUMXSHBT-UHFFFAOYSA-N Cc(c(F)c(COc1nc(N2CCN(C)CC2)ncc1Sc(cc1)cnc1N)cc1)c1F Chemical compound Cc(c(F)c(COc1nc(N2CCN(C)CC2)ncc1Sc(cc1)cnc1N)cc1)c1F HHAOOPAUMXSHBT-UHFFFAOYSA-N 0.000 description 1
- QRSLVUJNTJQHBA-UHFFFAOYSA-N Cc(cc(COc1nc(N2CCN(C)CC2)ncc1Sc(cc1)cnc1N)cc1)c1F Chemical compound Cc(cc(COc1nc(N2CCN(C)CC2)ncc1Sc(cc1)cnc1N)cc1)c1F QRSLVUJNTJQHBA-UHFFFAOYSA-N 0.000 description 1
- WVSCEBGQKRABBE-UHFFFAOYSA-N Cc(nc(N1CCN(C)CC1)nc1)c1I Chemical compound Cc(nc(N1CCN(C)CC1)nc1)c1I WVSCEBGQKRABBE-UHFFFAOYSA-N 0.000 description 1
- WFDLWULWLAJJAV-UHFFFAOYSA-N Cc1cc(COc2nc(N(CCN3C)CC3=O)ncc2Sc(cc2)ccc2C#N)ccc1 Chemical compound Cc1cc(COc2nc(N(CCN3C)CC3=O)ncc2Sc(cc2)ccc2C#N)ccc1 WFDLWULWLAJJAV-UHFFFAOYSA-N 0.000 description 1
- RESHKAHTSWIWOO-UHFFFAOYSA-N Cc1cc(COc2nc(N3CCN(C)CC3)ncc2Sc2ccc(N)nc2)cc(C(F)(F)F)c1 Chemical compound Cc1cc(COc2nc(N3CCN(C)CC3)ncc2Sc2ccc(N)nc2)cc(C(F)(F)F)c1 RESHKAHTSWIWOO-UHFFFAOYSA-N 0.000 description 1
- CPRZFVYISWTZLT-UHFFFAOYSA-N Cc1ccc(C(N)=O)c(C(F)(F)F)c1 Chemical compound Cc1ccc(C(N)=O)c(C(F)(F)F)c1 CPRZFVYISWTZLT-UHFFFAOYSA-N 0.000 description 1
- YJLVPLFYKJDHSM-UHFFFAOYSA-N Cc1ccc(C(N)=O)c(I)c1 Chemical compound Cc1ccc(C(N)=O)c(I)c1 YJLVPLFYKJDHSM-UHFFFAOYSA-N 0.000 description 1
- OKPRELYNHXXTAO-UHFFFAOYSA-N Cc1cccc(COc2nc(N(CC3)CC3N(C)C)ncc2Sc(cc2)cnc2N)c1 Chemical compound Cc1cccc(COc2nc(N(CC3)CC3N(C)C)ncc2Sc(cc2)cnc2N)c1 OKPRELYNHXXTAO-UHFFFAOYSA-N 0.000 description 1
- GAYKIMSNWVDJEF-HXUWFJFHSA-N Cc1cccc(COc2nc(N(CC3)C[C@@H]3N(C)C)ncc2Sc(cc2)ccc2C(N)=O)c1 Chemical compound Cc1cccc(COc2nc(N(CC3)C[C@@H]3N(C)C)ncc2Sc(cc2)ccc2C(N)=O)c1 GAYKIMSNWVDJEF-HXUWFJFHSA-N 0.000 description 1
- XIKKYMICMUQGNW-UHFFFAOYSA-N Cc1cccc(COc2nc(N3C(C4)CN(C)C4C3)ncc2Sc(cc2)ccc2C(N)=O)c1 Chemical compound Cc1cccc(COc2nc(N3C(C4)CN(C)C4C3)ncc2Sc(cc2)ccc2C(N)=O)c1 XIKKYMICMUQGNW-UHFFFAOYSA-N 0.000 description 1
- UBVAORPHTYRTIS-UHFFFAOYSA-N Cc1cccc(COc2nc(N3CCN(C)CC3)ncc2Oc(cc2)ccc2C(N)=O)c1 Chemical compound Cc1cccc(COc2nc(N3CCN(C)CC3)ncc2Oc(cc2)ccc2C(N)=O)c1 UBVAORPHTYRTIS-UHFFFAOYSA-N 0.000 description 1
- BDCSCRTWMCCXMZ-UHFFFAOYSA-N Cc1cccc(COc2nc(N3CCN(C)CC3)ncc2Sc(cc2)ccc2C#N)c1 Chemical compound Cc1cccc(COc2nc(N3CCN(C)CC3)ncc2Sc(cc2)ccc2C#N)c1 BDCSCRTWMCCXMZ-UHFFFAOYSA-N 0.000 description 1
- PHBXIXYFTNXSIP-UHFFFAOYSA-N Cc1nccc(COc2nc(N3CCN(C)CC3)ncc2Sc(cc2)ccc2C(N)=O)c1 Chemical compound Cc1nccc(COc2nc(N3CCN(C)CC3)ncc2Sc(cc2)ccc2C(N)=O)c1 PHBXIXYFTNXSIP-UHFFFAOYSA-N 0.000 description 1
- SXWACHMYOAKSGA-UHFFFAOYSA-N N#Cc(c(Cl)c1)ccc1Sc(cnc(O)n1)c1O Chemical compound N#Cc(c(Cl)c1)ccc1Sc(cnc(O)n1)c1O SXWACHMYOAKSGA-UHFFFAOYSA-N 0.000 description 1
- CVNOWLNNPYYEOH-UHFFFAOYSA-N N#Cc(cc1)ccc1O Chemical compound N#Cc(cc1)ccc1O CVNOWLNNPYYEOH-UHFFFAOYSA-N 0.000 description 1
- HHAYQKIKZWUXSH-UHFFFAOYSA-N N#Cc(cc1)ccc1Oc(c(O)n1)cnc1S Chemical compound N#Cc(cc1)ccc1Oc(c(O)n1)cnc1S HHAYQKIKZWUXSH-UHFFFAOYSA-N 0.000 description 1
- ZHNRASVSIGGJMR-UHFFFAOYSA-N N#Cc(cc1)ccc1Sc1cnc(N2CCOCC2)nc1OCc1ccccc1 Chemical compound N#Cc(cc1)ccc1Sc1cnc(N2CCOCC2)nc1OCc1ccccc1 ZHNRASVSIGGJMR-UHFFFAOYSA-N 0.000 description 1
- IPRWIMRMQSUCIG-UHFFFAOYSA-N N#Cc(ccc(Sc(cnc(Cl)n1)c1Cl)c1)c1Cl Chemical compound N#Cc(ccc(Sc(cnc(Cl)n1)c1Cl)c1)c1Cl IPRWIMRMQSUCIG-UHFFFAOYSA-N 0.000 description 1
- WZWIQYMTQZCSKI-UHFFFAOYSA-N N#Cc1ccc(C=O)cc1 Chemical compound N#Cc1ccc(C=O)cc1 WZWIQYMTQZCSKI-UHFFFAOYSA-N 0.000 description 1
- CEIVMXMPBABKGI-ZZXKWVIFSA-N NC(c1ccc(/C=C/C(O)=O)cc1)=O Chemical compound NC(c1ccc(/C=C/C(O)=O)cc1)=O CEIVMXMPBABKGI-ZZXKWVIFSA-N 0.000 description 1
- YKZDVMZFKHGNFO-UHFFFAOYSA-N O=Cc1cccc(Sc(cnc(N2CCNCC2)n2)c2OCc2ccccc2)c1 Chemical compound O=Cc1cccc(Sc(cnc(N2CCNCC2)n2)c2OCc2ccccc2)c1 YKZDVMZFKHGNFO-UHFFFAOYSA-N 0.000 description 1
- KSNXJLQDQOIRIP-UHFFFAOYSA-N Oc1nc(O)ncc1I Chemical compound Oc1nc(O)ncc1I KSNXJLQDQOIRIP-UHFFFAOYSA-N 0.000 description 1
- IIRVUYFJHBICFO-UHFFFAOYSA-N [O-][N+](c(cc1)ncc1Sc(cnc(N1CCCC1)n1)c1O)=O Chemical compound [O-][N+](c(cc1)ncc1Sc(cnc(N1CCCC1)n1)c1O)=O IIRVUYFJHBICFO-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic 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
- A61K31/535—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
- A61P35/00—Antineoplastic agents
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- 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
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- 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
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
- C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
- C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
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- Chemical & Material Sciences (AREA)
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- Health & Medical Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Hematology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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| US9567318B2 (en) | 2009-08-17 | 2017-02-14 | Memorial Sloan-Kettering Cancer Center | Substituted pyrimidine compounds and uses thereof |
| AU2015259173B2 (en) * | 2014-05-13 | 2019-09-05 | Memorial Sloan Kettering Cancer Center | Hsp70 modulators and methods for making and using the same |
| TW201722422A (zh) | 2015-10-05 | 2017-07-01 | 美國紀念斯隆-凱特琳癌症中心 | 用於治療癌症之合理組合療法 |
| AU2019239658A1 (en) * | 2018-03-21 | 2020-11-12 | Suzhou Puhe BioPharma Co., Ltd. | SHP2 inhibitors and uses thereof |
| WO2020045334A1 (ja) | 2018-08-27 | 2020-03-05 | 大日本住友製薬株式会社 | 光学活性なアザビシクロ環誘導体 |
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| US3248393A (en) | 1960-06-23 | 1966-04-26 | Burroughs Wellcome Co | 1, 3-diazaphenothiazines and method |
| GB990857A (en) | 1961-10-13 | 1965-05-05 | Wellcome Found | 1,3-diazaphenothiazines |
| US4039543A (en) | 1974-12-24 | 1977-08-02 | Hoffmann-La Roche Inc. | Benzylpyrimidines |
| CH605828A5 (enExample) | 1974-12-24 | 1978-10-13 | Hoffmann La Roche | |
| US4096264A (en) | 1975-12-09 | 1978-06-20 | Merck & Co., Inc. | Certain substituted imidazo [1,2-a] pyridines |
| DE3311703A1 (de) | 1983-03-30 | 1984-10-04 | Bayer Ag, 5090 Leverkusen | Harnstoffderivate |
| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| DE69212850T2 (de) | 1991-01-15 | 1997-03-06 | Alcon Lab Inc | Verwendung von Karrageenan in topischen ophthalmologischen Zusammensetzungen |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| CZ101496A3 (en) | 1993-10-12 | 1996-11-13 | Du Pont Merck Pharma | N-alkyl-n-aryl-pyrimidinamines and derivatives thereof |
| DE4423098A1 (de) | 1994-07-01 | 1996-01-04 | Hoechst Ag | Verwendung von Pyrimidingruppen enthaltenden konjugierten Verbindungen als Elektrolumineszenzmaterialien |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| JPH09236070A (ja) | 1996-02-29 | 1997-09-09 | Denso Corp | スタータ |
| US5707930A (en) | 1996-09-16 | 1998-01-13 | Zeneca Limited | 4-cycloalkyl-5-substituted pyrimidine compounds useful as crop protection agents |
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| HU229403B1 (en) | 2000-12-18 | 2013-12-30 | Actelion Pharmaceuticals Ltd | Novel sulfamides and their use as endothelin receptor antagonists |
| US6423720B1 (en) | 2001-02-01 | 2002-07-23 | Duquesne University Of The Holy Ghost | Pyrimidine compounds and methods for making and using the same |
| US7501429B2 (en) | 2001-04-11 | 2009-03-10 | Queen's University At Kingston | Pyrimidine compounds as anti-ictogenic and/or anti-epileptogenic agents |
| DE60222804T2 (de) | 2001-12-21 | 2008-07-03 | Vernalis (Cambridge) Ltd., Abington | 3-(2,4)dihydroxyphenyl-4-phenylpyrazole und deren medizinische verwendung |
| IL166241A0 (en) | 2002-07-29 | 2006-01-15 | Rigel Pharmaceuticals Inc | Method of treating or preventing autoimmune diseases with 2,4-pyrimidinedinediamine compounds |
| MXPA05008619A (es) | 2003-02-13 | 2005-11-04 | Banyu Pharma Co Ltd | Derivados novedosos de 2-piridincarboxamida. |
| WO2005021552A1 (en) | 2003-08-29 | 2005-03-10 | Vernalis (Cambridge) Ltd | Pyrimidothiophene compounds |
| US20050070712A1 (en) | 2003-09-26 | 2005-03-31 | Christi Kosogof | Pyrimidine derivatives as ghrelin receptor modulators |
| PL1725540T3 (pl) | 2004-03-05 | 2013-02-28 | Hoffmann La Roche | Diaminopirymidyny jako antagoniści p2x3 i p2x2/3 |
| EP1745033A4 (en) | 2004-05-08 | 2009-08-26 | Neurogen Corp | 2-ARYLPYRIMIDINES DISUBSTITUTED IN 4,5 |
| MX2007011500A (es) | 2005-03-16 | 2007-11-21 | Targegen Inc | Compuestos pirimidina y metodos de uso. |
| CN101300235B (zh) * | 2005-09-01 | 2011-12-07 | 弗·哈夫曼-拉罗切有限公司 | 作为p2x3和p2x2/3调节剂的二氨基嘧啶类化合物 |
| WO2007131034A1 (en) | 2006-05-03 | 2007-11-15 | The Regents Of The University Of Michigan | Pyrimidone derivatives which are modulators of heat shock protein (hsp) 70 |
| JP2008081492A (ja) | 2006-08-31 | 2008-04-10 | Banyu Pharmaceut Co Ltd | オーロラa選択的阻害作用を有する新規アミノピリジン誘導体 |
| US20080124407A1 (en) | 2006-10-10 | 2008-05-29 | University Of Washington | Inhibiting cyp3a4 induction |
| ME00811B (me) | 2006-12-08 | 2012-03-20 | Novartis Ag | JEDINJENJA l KOMPOZICIJE KAO INHIBITORI PROTEIN KINAZE |
| WO2008092199A1 (en) | 2007-01-31 | 2008-08-07 | Cytopia Research Pty Ltd | Thiopyrimidine-based compounds and uses thereof |
| TW200911240A (en) | 2007-06-11 | 2009-03-16 | Kyowa Hakko Kogyo Kk | Anti-tumor agent |
| US8754094B2 (en) | 2007-08-15 | 2014-06-17 | The Research Foundation Of State University Of New York | Methods for heat shock protein dependent cancer treatment |
| US9259399B2 (en) | 2007-11-07 | 2016-02-16 | Cornell University | Targeting CDK4 and CDK6 in cancer therapy |
| PE20091236A1 (es) | 2007-11-22 | 2009-09-16 | Astrazeneca Ab | Derivados de pirimidina como immunomoduladores de tlr7 |
| CN102573486A (zh) | 2009-06-08 | 2012-07-11 | 加利福尼亚资本权益有限责任公司 | 三嗪衍生物及其治疗应用 |
| EP2922843A4 (en) * | 2012-11-13 | 2016-06-01 | Sloan Kettering Inst Cancer | INDOL COMPOUNDS AND USE THEREOF AS ANTIMICROBIAL AGENTS |
| AU2015259173B2 (en) * | 2014-05-13 | 2019-09-05 | Memorial Sloan Kettering Cancer Center | Hsp70 modulators and methods for making and using the same |
| JP6878316B2 (ja) * | 2015-06-19 | 2021-05-26 | ノバルティス アーゲー | Shp2の活性を阻害するための化合物および組成物 |
| ES2922080T3 (es) * | 2015-09-18 | 2022-09-07 | St Jude Childrens Res Hospital | Métodos y composiciones de inhibición de la interacción de DCN1-UBC12 |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| WO2011022440A2 (en) * | 2009-08-17 | 2011-02-24 | Memorial Sloan-Kettering Cancer Center | Heat shock protein binding compounds, compositions, and methods for making and using same |
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| US20170233352A1 (en) | 2017-08-17 |
| US9878987B2 (en) | 2018-01-30 |
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| US20190241526A1 (en) | 2019-08-08 |
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| BR112016026470A8 (pt) | 2021-07-20 |
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| MX375924B (es) | 2025-03-07 |
| EP3143013A1 (en) | 2017-03-22 |
| KR102461419B1 (ko) | 2022-11-02 |
| CN107074806A (zh) | 2017-08-18 |
| IL248792A0 (en) | 2017-01-31 |
| AU2015259173A1 (en) | 2016-12-08 |
| US20180170883A1 (en) | 2018-06-21 |
| TW201601725A (zh) | 2016-01-16 |
| JP2017515857A (ja) | 2017-06-15 |
| BR112016026470A2 (pt) | 2017-08-15 |
| JP6607870B2 (ja) | 2019-11-20 |
| CN107074806B (zh) | 2021-04-23 |
| IL248792B (en) | 2020-01-30 |
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