81 results about "Geldanamycin" patented technology

The invention provides purified 18,21-didehydro-18,21-dideoxo-18,21-dihydroxy-geldanamycin derivatives, pharmaceutically acceptable salts thereof and prodrugs thereof that are potent Hsp90 binding agents that are useful for the treatment and/or the amelioration of symptoms of cancer and other proliferative tissue disorders.

A method for treating multiple myeloma in a subject by administering to the subject 17-allylamino-17-demethoxy-geldanamycin or 17-amino geldanamycin, or a pro drug of either 17-AAG or 17-AG, in combination with a proteasome inhibitor.

A geldanamycin derivative exhibiting significant preliminary in vivo activity, particularly significant oral in vivo activity, and a method of treating or preventing cancer in a host comprising administering a geldanamycin derivative to a host in an amount sufficient to treat or prevent cancer.

A geldanamycin derivate with nucleoside base is prepare by inducing soluble nucleoside by geldanamycin and obtaining the final product. Nucleoside base is connected with geldanamycin on Linker. It can keep or strengthen antiviral activity of geldanamycin and improve solubility and tissue distribution.

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.

The present invention relates to novel geldanamycin derivatives which have antitumor and antiparasitic properties. The geldanamycin derivatives disclosed herein have antitumor properties in humans due to their interaction with human heat shock protein 90 (hsp90). The human parasites Plasmodium falciparum, Trypanosoma Cruzi, and Leishmania donovani are lethally susceptible to exposure to geldanamycin via complexation of geldanamycin with their homologs (Pfhsp90, hsp83, and hsp90, respectively) of the human hsp90. The geldanamycin derivatives disclosed herein also interact with these parasitic hsp90 homologs so as to have antiparasitic properties.

A pharmaceutical formulation comprising (a) 17-allylamino-17-demethoxy-geldanamycin; (b) an ester of d-α-tocopheryl succinate and polyethylene glycol; and (c) a pharmaceutically acceptable, water-miscible organic solvent.

FK506 and geldanamycin promote nerve regeneration by a common mechanism that involves the binding of these compounds to polypeptide components of steroid receptor-complexes other than the steroid hormone binding portion of the complex (FKBP52 and hsp90, respectively). These and other agents cause hsp90 dissociation from steroid receptor complexes or block association of hsp90 with steroid receptor complexes.

A method for treating multiple myeloma in a subject by administering 17-allylamino-17-demethoxy-geldanamycin or 17-amino geldanamycin, or a prodrug of either 17-AAG or 17-AG, to the subject.

The invention discloses a making method of radioactive iodine-17-allylamine-17-normethoxy geldanamycin in the nuclear medical, tumour and medical agent technical domain, which is characterized by the following: marking the product of 17-allylamine-17-normethoxy geldanamycin through iodine for HSP90; modifying the structure of 17-allylamine-17-normethoxy geldanamycin; guiding radioactive nuclear iodine on the end of double-bond; providing the medical acceptable drug or drug composition to treat tumor or cancer.

The invention relates to a kueide mycin which is a novel derivative of geldanamycin. According to the anticancer activity experiment, kueide mycin has in both vitro and vivo antitumor activities. The kueide mycin has the in vitro activity characteristics of inhibiting tumor cell proliferation, inducing the tumor cell apoptosis, reducing related target proteins of Hsp 90 in the tumor cells, as well as inhibiting the tumor cell migration, and has in vivo antitumor activity characteristics of notably reducing poisonousness compared to the geldanamycin. The kueide mycin can obviously inhibit the growth of solid tumor of a nude mouse model of Human breast carcinoma xenografts after being injected in a peritoneal cavity and is expected to be developed into a clinical effective antitumor drug.

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

The invention relates to new application of geldanamycin and a derivative thereof in treating and inhibiting posterior capsular opacification, belonging to the technical field of medicines. Experiments prove that a geldanamycin derivative 17AAG inhibits human lens epithelial cells from proliferating and induces lens epithelial cells to die; in an in vitro rat lens capsular bag cultivation model, 17AAG inhibits residual lens epithelial cells from proliferating, migrating and fiberizing in a lens posterior capsule greatly, induces cells with posterior capsule overgrown to die, and promotes turbid lens posterior capsule to recover transparency; in a rabbit intraocular lens replacement model, 17AAG can inhibit posterior capsular opacification. The geldanamycin and the derivative thereof inhibit posterior capsular opacification by inhibiting HSP90 molecular chaperone activity of lens cells, and have a therapeutical effect on the formed posterior capsular opacification at the same time. 17AAG has new application in treating posterior capsular opacification, and is a candidate medicine that 17AAG has development potential and can prevent and treat posterior capsular opacification.

A method for prophylaxis or treatment of a mammal, particularly human, at risk for a fibrogenic disorder is disclosed. The compositions and methods of the invention are directed both to treatments for existing fibrogenic disorders and prevention thereof. Such disorders include, but are not limited to, connective tissue diseases, such as scleroderma (or systemic sclerosis), polymyositis, systemic lupus erythematosis and rheumatoid arthristis, and other fibrotic disorders, including liver cirrhosis, keloid formation, interstitial nephritis and pulmonary fibrosis. A therapeutic composition according to the invention includes, as a therapeutic agent, an inhibitor of a collagen promoter in a pharmaceutically acceptable inert carrier vehicle, preferably for local, and particularly topical, application. Exemplary inhibitors include those that interfere with heat shock protein 90 (Hsp 90) chaperone function, e.g., the specific inhibitor geldanamycin or other known Hsp90 inhibitors such as macbecin I and II, herbimycin, radcicol and novobiocin.

Geldanamycin compounds having a structure according to formula I

where Q¹, L, L¹, R⁵, R⁶, and R¹¹ are as defined herein, are useful for treating a disease or disorder ameliorated by inhibiting the function of extracellular heat shock protein-90.

Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.

An injection of water-soluble 17-allylamino-17-demethoxy geldanamycin (17-AAG) for treating multiple kinds of cancers is prepared from 17-AAG and polyethanediol for increasing the solubility of 17-AAG in water.