摘要:
The invention provides lapachone analogs and derivatives as well as methods of use thereof. These compounds can be used in pharmaceutical compositions for the treatment or prevention of cell proliferation disorders. These compounds can also be used in the treatment or prevention of cancer or precancerous conditions.
摘要:
The present invention relates to substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted imidazolyl-5,6-dihydrobenzo[n]isoquinoline compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要:
In general, the present invention relates to compounds capable of inhibiting p38, methods for inhibiting p38 in vivo or in vitro, and methods for treating conditions associated with p38 activity or cytokine activity.
摘要:
The present invention relates to quinone prodrug compositions and therapeutic methods using such prodrug compositions. Preferably, the quinone compounds of the invention are napthoquinone compounds such as β-lapachone or β-lapachone analogs. The quinone prodrug compositions of the invention exhibit improved solubility, stability, bioavailability, and pharmacokinetic properties, as well as improved plasma half-life in vivo.
摘要:
The present invention relates to substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof.
摘要:
In general, the present invention relates to compounds capable of inhibiting P38, methods for inhibiting P38 in vivo or in vitro, diagnostics for determining activity in the treatment of P38 and/or cytokine-associated conditions and methods for treating conditions associated with P38 activity or cytokine activity.
摘要:
Disclosed herein are antibacterial compounds that inhibit fabl, a NADH-dependent enoyl [acyl carrier protein] reductase enzyme in the fatty acid biosynthesis pathway. The compounds are represented by structural formulas Ia and Ib: R1 and R2 are independently monocyclic aryl or heteroaryl groups, wherein the groups represented by R1 and R2 are optionally substituted with one or more acyclic substituents; R3 is —H or an optionally substituted C1-C8 aliphatic, C3-C8 cycloaliphatic, aryl, or heteroaryl group. X1 is a bond or a C1-C3 alkylene chain that is optionally substituted with a C1-C4 alkyl or an acidic group. X2 is an aryl, heteroaryl or C3-C8 cycloaliphatic ring, wherein the group represented by X2 is optionally substituted with triazole, tetrazole, and/or one or more acyclic substituents.
摘要:
This invention provides compound of formulae I or II having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined in the specification or a pharmaceutically acceptable salt thereof which are useful for the treatment of the inflammatory component of diseases and are particularly useful in treating atherosclerosis, myocardial infarction, congestive heart failure, inflammatory bowel disease, arthritis, type II diabetes, and autoimmune diseases such as multiple sclerosis and rheumatiod arthritis.
摘要:
The present invention relates to pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds, and methods of preparation of these compounds. The present invention also relates to pharmaceutical compositions comprising pyrroloquinolinyl-pyrrole-2,5-dione compounds and pyrroloquinolinyl-pyrrolidine-2,5-dione compounds. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention.
摘要:
The present invention relates to polymer-modified quinone-containing and carbonyl-containing therapeutic agents, including polymer-modified β-lapachone compounds, and methods of treating cancer by administering the polymer-modified therapeutic agents to a subject. Polymer-modification of therapeutic agents, such as β-lapachone compounds, provides effective transport of polymer-modified therapeutic agents to tumor cells or tumor tissues by exploiting the EPR effect in tumor tissues.