The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1,R2,R3,R4,R5,R6,R7,R8and R9are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', NO2,NH2,NHR', N(R')2,NHC(O)R', CN, halogen, =O, C(=O)H, C(=
The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1,R2,R3,R4,R5,R6,R7,R8and R9are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', NO2,NH2,NHR', N(R')2,NHC(O)R', CN, halogen, =O, C(=O)H, C(=O)R', CO2H, CO2R', C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, 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-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7and R8may be joined into a carbocyclic or heterocyclic ring system; and wherein X1and X2are each independently defined as above for R1-R8,and each further includes specific preferred groups as defined herein.
대표청구항▼
The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1,R2,R3,R4,R5,R6,R7,R8and R9are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', NO2,NH2,NHR', N(R')2,NHC(O)R', CN, halogen, =O, C(=O)H, C(=
The present invention is directed to the synthesis and characterization of compounds having the formula: wherein R1,R2,R3,R4,R5,R6,R7,R8and R9are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO2R', NO2,NH2,NHR', N(R')2,NHC(O)R', CN, halogen, =O, C(=O)H, C(=O)R', CO2H, CO2R', C1-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, 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-C12alkyl, C2-C12alkenyl, C2-C12alkynyl, aryl, aralkyl, and heteroaromatic; wherein each dotted circle represents one, two or three optional double bonds; wherein R7and R8may be joined into a carbocyclic or heterocyclic ring system; and wherein X1and X2are each independently defined as above for R1-R8,and each further includes specific preferred groups as defined herein. n-Peptide Drugs in Acute-Phase Responses" Eur. J. Pharmacol. 271:319-327 (1994). Clancy et al., "Chlorpromazine Modulates Cytokine Expression in the Liver and Lung After Burn Injury and Endotoxemia" J. Trauma, 48:215-222 (2000). Corsini et al., "Induction of Tumor Necrosis Factor-Alpha In Vivo by a Skin Irritant, Tributytin, Through Activation of Transcription Factors: Its Pharmacological Modulation by Anti-Inflammatory Drugs" J. Invest. Dermatol. 108: 892-896 (1997). Cubria et al., "Aromatic Diamidines are Reversible Inhibitors of Porcine Kidney Diamine Oxidase" Biochem. Pharmacol. 45:1355-1357 (1993). Dautzenberg et al., "Pentamidine Aerosol in the Prevention Treatment of Pneumocystosis in AIDS Patients. Comparison of Two Salts and Two Nebulizers" Presse. Med. 20: 1117-1120 (1991). Del Poeta et al., "Structure-In Vitro Activity Relationships of Pentamidine Analogues and Dication-Substituted Bis-Benzimidazoles as New Antifungal Agents" Antimicrob. Agents Chemother. 42:2495-2502 (1998). Fimognari et al., "Flow Cytometric Analysis of Genetic Damage, Effect on Cell Cycle Progression, and Apoptosis by Thiophanate-Methyl in Human Lymphocytes" Environ. Mol. Mutagen. 33:173-176 (1999). Ferroni et al., "N1-Substituted Benzamidines: Synthesis, Antiproteinase Activity and Inhibition of Tumor Cell Growth" Farmaco 46:1311-1321 (1991). Herberich et al., "Synthesis of a Netropsin Conjugate of a Water-Soluble epi-Quinocarcin Analogue: the Importance of Stereochemistry at Nitrogen" Bioorganic & Medicinal Chemistry 8:523-532 (2000). Jansen et al, "Chlorpromazine Down-Regulates Tumor Necrosis Factor-Alpha and Attenuates Experimental Multiple Organ Dysfunction Syndrome in Mice" Crit. Care Med. 26:1244-1250 (1998). Jiang et al., "Transformation of Lupus-Inducing Drugs to Cytotoxic Products by Activated Neutrophils" Science 266:810-813 (1994). Jones, "Successful Cancer Therapy with Promethazine: The Rationale" Med. Hypotheses, 46:25-29 (1996). Kim et al., "Effects of Calmodulin Antagonists and Anesthetics on the Skin Lesions Induced by 2-Chloroethylethyl Sulfide" Eur. J. Pharmacol. 313:107-114 (1996). Kitamura et al., "Inhibition of Constitutive Nitric Oxide Synthase In the Brain by Pentamidine, a Calmodulin Antagonist" Eur. J. Pharmacol. 289:299-304 (1995). Krishan et al., "Synergistic Effects of Prochlorperazine and Dipyridamole on the Cellular Retention and Cytotoxicity of Doxorubicin" Clinical Cancer Research 6:1508-1517 (2000). Kumar et al., "Inhibition of Protein Synthesis by Antagonists of Calmodulin in Ehrlich Ascites Tumor Cells" Eur. J. Biochem. 195:313-319 (1991). Mesa-Valle et al., "In Vitro Action of Platinum (II) and Platinum (IV) Complexes on Trypanosoma cruzi and Leishmania donovani" Arzneimittelforschung 39:838-842 (1989). Mesa-Valle et al., "In Vitro and In Vivo Activity of Two Pt(IV) Salts Against Leishmania donovani" Pharmacology 57:160-72 (1998). Mesa-Valle CM et al., "Action of New Organometallic Complexes Against Leishmania donovani" J. Antimicrob. Chemother. 40:47-57 (1997). Mongiardo et al., "Pentamidine Salts" Lancet 2:108 (1989). Navas et al., "Structural Determinants of Putrescine Uptake Inhibition Produced by Cationic Diamidines in the Model of Trypanosomatid Crithidia Fasciculata" Biol. Chem. 377:833-836 (1996). Nunn et al., "Sequence-Dependent Drug Binding to the Minor Groove of DNA: Crystal Structure of the DNA Dodecamer d(CGCAAATTTGCG)2Complexed with Propamidine" J. Med. Chem. 38:2317-2325 (1995). Ohtsuka et al., "Inhibitory Effect on LPS-Induced Tumor Necrosis Factor in Calves Treated with Chlorpromazine or Pentoxifylline" J. Vet. Med. Sci. 59:1075-1077 (1997). Palmer et al., "Correlation of Activity of Chlorpromazine and Respective Hydroxy, Dimethoxy and Sulphoxide Analogues on Dopamine, Muscarinic, Histamine and Calmodulin Sites of Action" Xenobiotica 18:277-289 (1988). Perez et al., "DNA Binding Properties and Antileukemic (L1210) Activity of Pt-Pentamidine Complex" Chem. Bio
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