Abstract: Alkynyl pyrrolo [2,3-d] pyrimidines of Formula I are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.

Abstract: Efficient chemical processes for preparing high yields, purities, and different polymorphic forms of 17-allyl amino geldanamycin (17-AAG) and other ansamycins are described and claimed.

Abstract: Zearalanol compounds are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various disorders. Methods of synthesis and use of such compounds are also described and claimed.

Abstract: Alkynyl pyrrolo[2,3-d]pyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders. Methods of synthesis and use of such compounds are also described and claimed.

Abstract: Ansamycins and methods of preparing and using the same are described. At least some of these ansamycins exhibit one or more of improved aqueous formulation ability, chemical stability, and bioavailability. Some of the derivatives described are dimers. These and others described can include one or more solubilizing groups that have expected merit in rendering the overall compounds useful as drugs and prodrugs.

Abstract: The invention relates in general to 7,9-dihydro-purin-8-one and related compounds that show broad utility, e.g., in inhibiting heat shock protein 90 (HSP90) to thereby treat or prevent HSP90-mediated diseases.

Abstract: 2-Aminopurine analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.

Abstract: Pyrrolopyrimidines and related analogs are described and demonstrated to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents used in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Methods of synthesis and use of such compounds are also described and claimed.

Abstract: Novel purine compounds of Formula I. and tautomers, pharmaceutically acceptable salts, and prodrugs thereof, wherein X is S, S(O), or S(O)2; and O is selected from alkyl, cycloalkyl, arylalkyl, aryl, heteroaryl, and heterocyclic, all optionally substituted, are described, as are pharmaceutical compositions comprising the same, complexes comprising the same, e.g., HSP90 complexes, and methods of using the same.

Abstract: Provided are pharmaceutical compositions containing an oil phase and an aqueous phase, the oil phase including an ansamycin and less than 2% w/w oleic acid, wherein the ansamycin is geldanamycin, 17-aminogeldanamycin, 17-allyalamino-17-demethoxy-geldanamycin, compound 563, or compound 237 having the structures below, or a salt of any one of the aforementioned ansamycins

Abstract: Novel purine compounds and tautomers and pharmaceutically acceptable salts thereof are described, as are pharmaceutical compositions comprising the same, complexes comprising the same, e.g., HSP90 complexes, and methods of using the same. Methods of using the novel purine compounds of the invention, and tautomers and pharmaceutically acceptable salts thereof, include their use in inhibiting heat shock protein 90's (HSP90's) to thereby treat or prevent HSP90-dependent diseases, e.g., proliferative disorders such as breast cancer.

Abstract: Pyrazolopyrimidines and related analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.

Abstract: Triazolopyrimidines and related compounds are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.

Abstract: The present invention provides a method of treating an individual having an HSP90 mediated disorder comprising administering to said individual a pharmaceutical composition comprising a pharmaceutically effective amount of a synthetic heterocyclic HSP90 inhibitor, wherein the activity of the HSP90 inhibitor is substantially independent of multi drug resistance. In one embodiment, the activity of the HSP90 inhibitor is substantially independent of P-gp and MRP expression.

Abstract: A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, pharmaceutically acceptable salt or prodrug thereof: wherein: R1 is halogen, —OR1, —SR11 or lower alkyl; R2 is —NHR8; R3 is selected from the group consisting of hydrogen, halogen, —SR8, —OR8, —CN, —C(O)R9, —CO2H, —NO2, —NR8R10, lower alkyl, lower alkenyl, lower alkynyl, lower perhaloalkyl, aryl, heteroaryl, alicyclic and heterocyclic, all optionally substituted, wherein: the aryl, heteroaryl, alicyclic and heterocyclic groups are optionally mono-, bi- or tri-cyclic, R4 is —CHR12—, —C(O), —C(S), —S(O)—, or —SO2—; R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 3 to 5 substituents, the heteroaryl group is substituted with 2 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, the heterocyclic group is substituted with 3 to 5 substituents.

Abstract: 2-Aminopurine analogs are described and demonstrated or predicted to have utility as Heat Shock Protein 90 (HSP90) inhibiting agents in the treatment and prevention of various HSP90 mediated disorders, e.g., proliferative disorders. Method of synthesis and use of such compounds are also described and claimed.

Abstract: The present invention provides compounds represented by Formula I.

Abstract: A compound represented by Formula I, or a polymorph, ester, tautomer, enantiomer, diastereomer, pharmaceutically acceptable salt or prodrug thereof, Wherein R1 is halogen, —OR11, —SR11 or lower alkyl; R2 is —NHR8; R4 is —CHR12—, —C(O)—, —C(S)—, —S(O)— or —S2—; and R5 is aryl, heteroaryl, alicyclic, or heterocyclic, wherein the aryl group is substituted with 4 to 5 substituents, the heteroaryl group is substituted with 3 to 5 substituents, the alicyclic group is substituted with 3 to 5 substituents, and the heterocyclic group is substituted with 3 to 5 substituents.

Abstract: Drug formulations having emulsifying agents and both medium and long chain triglycerides are described. In preferred embodiments, the long chain triglycerides negate or lessen deleterious central nervous system effects that are caused by medium chain triglycerides.

Abstract: Efficient chemical processes for preparing high yields, purities, and different polymorphic forms of 17-allyl amino geldanamycin (17-AAG) and other ansamycins are described and claimed.