The present invention relates to trioxacarcin compounds of the formula: (I) or pharmaceutically acceptable forms thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined herein. The present invention also provides processes for preparing such compounds and intermediates thereto; pharma
The present invention relates to trioxacarcin compounds of the formula: (I) or pharmaceutically acceptable forms thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8, and R9 are as defined herein. The present invention also provides processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; and methods of use and treatment.
대표청구항▼
1. A compound of the Formula (I): or a pharmaceutically acceptable form thereof; wherein: R1 is hydrogen or ═O;each instance of R2 and R3 is hydrogen;R4 is hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubst
1. A compound of the Formula (I): or a pharmaceutically acceptable form thereof; wherein: R1 is hydrogen or ═O;each instance of R2 and R3 is hydrogen;R4 is hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; —ORD1; —C(═O)RD2; —CO2RD2; —CN; —SCN; —SRD1; —SORD1; —SO2RD2; —NO2; —N3; —N(RD2)2; —NRD2C(═O)RD2; —NRD2C(═O)N(RD2)2; —OC(═O)ORD1; —OC(═O)RD2; —OC(═O)N(RD2)2; —NRD2C(═O)ORD1; or —C(RD2)3; wherein each occurrence of RD1 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; and wherein each occurrence of RD2 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; substituted hydroxyl; substituted thiol; amino; or substituted amino; or two RD2 groups are optionally joined to form a heterocyclyl or heteroaryl ring;R5 is hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; —ORE1; —C(═O)RE2; —CO2RE1; —CN; —SCN; —SRE1; —SORE1; —SO2RE2; —NO2; —N3; —N(RE2)2; —NRE2C(═O)RE2; —NRE2C(═O)N(RE2)2; —OC(═O)ORE1; —OC(═O)RE2; —OC(═O)N(RE2)2; —NRE2C(═O)ORE1; or —C(RE2)3; wherein each occurrence of RE1 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; and wherein each occurrence of RE2 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; substituted hydroxyl; substituted thiol); amino; or substituted amino; or two RE2 groups are optionally joined to form a heterocyclyl or heteroaryl ring;R6 is hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; —ORF1; —C(═O)RF2; —CO2RF1; —CN; —SCN; —SRF1; —SORF1; —SO2RF2; —NO2; —N3; —N(RF2)2; —NRF2C(═O)RF2; —NRF2C(═O)N(RF2)2; —OC(═O)ORF1; —OC(═O)RF2; —OC(═O)N(RF2)2; —NRF2C(═O)ORF1; or —C(RF2)3; wherein each occurrence of RF1 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; and wherein each occurrence of RF2 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; substituted hydroxyl; substituted thiol; amino; or substituted amino; or two RF2 groups are optionally joined to form a heterocyclyl or heteroaryl ring;R7 is hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; —ORG1; —C(═O)RG2; —-CO2RG1; —CN; —SCN; —SRG1; —SORG1; —SO2RG2; —NO2; —N3; —N(RG)2; —NRG2C(═O)RG2; —NRG2C(═O)N(RG2)2; —OC(═O)ORG1; —OC(═O)RG2; —OC(═O)N(RG2)2; —NRG2C(═O)ORG1; or —C(RG2)3; wherein in each occurrence of RG1 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; and wherein each occurrence of RG2 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; substituted hydroxyl; substituted thiol; amino; or substituted amino; or two RG2 groups are optionally joined to form a heterocyclyl or heteroaryl ring;R8 is —ORH1, wherein each occurrence of RH1 is independently hydrogen, carbohydrate, an oxygen-protecting group, cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; or acyl;R9 is hydrogen; halogen; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; substituted or unsubstituted aryl; substituted or unsubstituted heteroaryl; —ORI1; —C(═O)RI2; —CO2RI1; —CN; —SCN; —SRI1; —SORI1; —SO2RI2; —NO2; —N3; —N(RI2)2; —NRI2C(═O)RI2; —NRI2C(═O)N(RI2)2; —OC(═O)ORI1; —OC(═O)RI2; —OC(═O)N(RI2)2; —NRI2C(═O)ORI1; or —C(RI2)3; wherein each occurrence of RI1 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; each occurrence of RI2 is independently hydrogen; carbohydrate; a protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl; substituted hydroxyl; substituted thiol; amino; or substituted amino); or two RI2 groups are optionally joined to form a heterocyclyl or heteroaryl ring;or R4 and R7 are optionally be taken together with the intervening carbon atoms to form an optionally substituted cyclic moiety;or R6 and R7 are optionally be taken together with the intervening carbon atoms to form an optionally substituted cyclic moiety. 2. The compound of claim 1, wherein the compound is of the formula: or a pharmaceutically acceptable form thereof. 3. The compound of claim 2, wherein the compound is of formula: or a pharmaceutically acceptable form thereof. 4. The compound of claim 1, wherein the compound is of the formula: or a pharmaceutically acceptable form thereof. 5. The compound of claim 1, wherein R1 is hydrogen. 6. The compound of claim 1, wherein R4 is —ORD1. 7. The compound of claim 1, wherein R5 is —ORE1. 8. The compound of claim 1, wherein R6 is C1-6 alkyl. 9. The compound of claim 1, wherein R7 is hydrogen. 10. The compound of claim 1, wherein R8 is —ORH1. 11. The compound of claim 10, wherein RH1 is hydrogen, a carbohydrate, or C1-6 alkyl. 12. The compound of claim 11, wherein the carbohydrate is: wherein Ra and Rb are independently selected from the group consisting of hydrogen; carbohydrate; an oxygen protecting group; cyclic or acyclic, substituted or unsubstituted, branched or unbranched aliphatic; cyclic or acyclic, substituted or unsubstituted, branched or unbranched heteroaliphatic; acyl; substituted or unsubstituted aryl; or substituted or unsubstituted heteroaryl. 13. The compound of claim 1, wherein R9 is —CH(ORI3)2; and each occurrence of RI3 is independently hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, or a carbohydrate. 14. The compound of claim 1, wherein R1 is ═O. 15. The compound of claim 6, wherein RD1 is C1-6alkyl. 16. The compound of claim 7, wherein RE1 is hydrogen. 17. The compound of claim 13, wherein R9 is —CH(OCH3)2. 18. The compound of claim 1, wherein the compound is: or a pharmaceutically acceptable form thereof. 19. A pharmaceutical composition comprising a compound of claim 1 or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. 20. A method of treating a disease, disorder or condition selected from the group consisting of proliferative diseases, diabetic retinopathy, inflammatory diseases, autoimmune diseases, and infectious diseases, comprising administering to a subject an effective amount of a compound of claim 1 or pharmaceutically acceptable form thereof.
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