The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO
The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are each independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(═O)R′ NHC(═O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7 and R8 may be are joined into a carbocyclic or heterocyclic ring system; and wherein X1 and X2 are each independently defined as above for R1-R8 R1-R6 and R9, and each further includes specific preferred groups as defined herein.
대표청구항▼
What is claimed is: 1. Compounds having the formula: wherein each of the groups X1, X2, R1, R2, R3, R4, R5, R6, R7, R8 and R9 is independently selected from the group consisting of H, OH, OR′, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′
What is claimed is: 1. Compounds having the formula: wherein each of the groups X1, X2, R1, R2, R3, R4, R5, R6, R7, R8 and R9 is independently selected from the group consisting of H, OH, OR′, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′ NHC(═O)R′, CN, halogen, ═O, C(═O)H, C(═O)R′, CO2H, CO2R′, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NH2, NO2, SH, CN, halogen, ═O, C(═O)H, C═O)CH3 C(═O)CH3, CO2H, CO2CH3, C1-C12 alkyl, C2-C12 alkenyl, C2-C12 alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; and wherein R7 and R8 may be are joined into a carbocyclic or heterocyclic ring system. 2. The compounds of claim 1 wherein X1 and X2 are independently selected from the group consisting of: or the formula: wherein Z is selected from the group consisting of: where n=1, 2, 3 . . . 20 wherein each R group is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, nitro, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, substituted or unsubstituted phenyl or substituted or unsubstituted benzyl. 3. Compounds of the formula: wherein each of the groups X1, X2, R1, R2, R3, R4, R5, R6, and R9 is independently selected from the group consisting of H, OH, OR′, SH, SR′, SOR′, SO2R′, NO2, NH2, NHR′, N(R′)2, NHC(O)R′ NHC(═O)R′, CN, halogen, ═O, C1-C6 alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, and substituted or unsubstituted heteroaromatic; wherein each of the R′ groups is independently selected from the group consisting of H, OH, NO2, NH2, SH, CN, halogen, ═O, C(═O)H, C(═O)CH3, CO2H, CO2CH3, C1-C6 alkyl, phenyl, benzyl, and heteroaromatic; and wherein each dotted circle represents one, two or three optional double bonds. 4. The compounds of claim 3, wherein X1 and X2 are each independently selected from the group consisting of: or the formula: wherein Z is selected from the group consisting of: wherein each R group is independently selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alky-laryl alkylaryl. 5. The compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: R1 is H, OH, SH or NH2; R2 is H, OH, OCH3; R3 is H, OH, SH, NH2 or CH3; R4 is H, OH, SH, NH2, OCH3, or halogen; R5 is H or C1-C6 alkyl; R6 is CN, OH, SH, NH2, OR, SR, or O(C═O)R; R9 is C1-C6 alkyl; wherein X1 is selected from the group consisting of: where each R group, which may be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, alyl aryl or alkylaryl. 6. The compound of claim 5, wherein X1 is: 7. The compound of claim 5, wherein X1 is: 8. The compound of claim 5, wherein X1 is: 9. The compound of claim 5, wherein X1 is: 10. The compound of claim 5, wherein X1 is: 11. The compound of claim 5, wherein X1 is: 12. The compound of claim 5, wherein X1 is: 13. The compound of claim 9 5, wherein X1 is: 14. The compound of claim 5, wherein X1 is: 15. The compound of claim 5, wherein X1 is: 16. The compound of claim 5, wherein X1 is: 17. The compound of claim 5, wherein X1 is: 18. The compound of claim 5, wherein X1 is: 19. Pharmaceutical compositions comprising an effective antitumor amount of a compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: R1 is H, OH, SH or NH2; R2 is H, OH, OCH3; R3 is H, OH, SH, NH2 or CH3; R4 is H, OH, SH, NH2, OCH3, or halogen; R5 is H or C1-C6 alkyl; R6 is CN, OH, SH, NH2, OR, SR, or O(CO)R; R9 is C1-C6 alkyl; wherein X1 is selected from the group consisting of: and wherein each R group, which many be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl. 20. The pharmaceutical composition of claim 19, wherein X1 is: 21. The pharmaceutical composition of claim 19, wherein X1 is: 22. The pharmaceutical composition of claim 19, wherein X1 is: 23. The pharmaceutical composition of claim 19, wherein X1 is: 24. The pharmaceutical composition of claim 19, wherein X1 is: 25. The pharmaceutical composition of claim 19, wherein X1 is: 26. The pharmaceutical composition of claim 19, wherein X1 is: 27. The pharmaceutical composition of claim 19, wherein X1 is: 28. The pharmaceutical composition of claim 19, wherein X1 is: 29. The pharmaceutical composition of claim 19, wherein X1 is: 30. The pharmaceutical composition of claim 19, wherein X1 is: 31. The pharmaceutical composition of claim 19, wherein X1 is: 32. The pharmaceutical composition of claim 19, wherein X1 is: 33. A method of treating tumors selected from the group consisting of lung cancer, colon cancer and prostate cancer in mammals comprising administering to a mammal in need of such treatment, an effective antitumor amount of a compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: R1 is H, OH, SH or NH2; R2 is H, OH, OCH3; R3 is H, OH, SH, NH2 or CH3; R4 is H, OH, SH, NH2, OCH3, or halogen; R5 is H or C1-C6 alkyl; R6 is CN, OH, SH, NH2, OR, SR, or O(CO)R; R9 is C1-C6 alkyl, wherein X1 is selected from the group consisting of: and wherein each R group, which may be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl. 34. The method of treatment of claim 33, wherein X1 is: 35. The method of treatment of claim 33, wherein X1 is: 36. The method of treatment of claim 33, wherein X1 is: 37. The method of treatment of claim 33, wherein X1 is: 38. The method of treatment of claim 33, wherein X1 is: 39. The method of treatment of claim 33, wherein X1 is: 40. The method of treatment of claim 33, wherein X1 is: 41. The method of treatment of claim 33, wherein X1 is: 42. The method of treatment of claim 33, wherein X1 is: 43. The method of treatment of claim 33, wherein X1 is: 44. The method of treatment of claim 33, wherein X1 is: 45. The method of treatment of claim 33, wherein X1 is: 46. The method of treatment of claim 33, wherein X1 is: 47. The compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: R1 is H, OH, SH or NH2; R2 is H, OH, OCH3; R3 is H, OH, SH, NH2 or CH3; R4 is H, OH, SH, NH2, OCH3, or halogen; R5 is H or C1-C6 alkyl; R6 is CN, OH, SH, NH2, OR, SR, or O(C═O)R; R9 is C1-C6 alkyl; wherein X1 is selected from the group consisting of: where each R group, which may be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl. 48. Pharmaceutical compositions comprising an effective antitumor amount of a compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: R1 is H, OH, SH or NH2; R2 is H, OH, OCH3; R3 is H, OH, SH, NH2 or CH3; R4 is H, OH, SH, NH2, OCH3, or halogen; R5 is H or C1-C6 alkyl; R6 is CN, OH, SH, NH2, OR, SR, or O(C═O)R; R9 is C1-C6 alkyl; wherein X1 is selected from the group consisting of: and wherein each R group, which many be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl. 49. A method of treating tumors selected from the group consisting of lung cancer, colon cancer and prostate cancer in mammals comprising administering to a mammal in need of such treatment, an effective antitumor amount of a compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: R1 is H, OH, SH or NH2; R2 is H, OH, OCH3; R3 is H, OH, SH, NH2 or CH3; R4 is H, OH, SH, NH2, OCH3, or halogen; R5 is H or C1-C6 alkyl; R6 is CN, OH, SH, NH2, OR, SR, or O(C═O)R; R9 is C1-C6 alkyl; wherein X1 is selected from the group consisting of: and wherein each R group, which may be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl. 50. Pharmaceutical compositions comprising an effective antitumor amount of a compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: X1 is selected from the group consisting of: and wherein each R group, which many be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl. 51. A method of treating tumors selected from the group consisting of lung cancer, colon cancer and prostate cancer in mammals comprising administering to a mammal in need of such treatment, an effective antitumor amount of a compound of the formula: and pharmaceutically acceptable salts and derivatives thereof, wherein: X1 is selected from the group consisting of: and wherein each R group, which may be the same or be different, is selected from the group consisting of H, OH, SH, NH2, NO2, halogen, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-acyl, aryl or alkylaryl.
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