62 results about "Temsirolimus" patented technology

The present invention relates to a therapeutic method for the treatment of cancer that comprises the use of a combination of inotuzumab ozogamicin (CMC-544) and temsirolimus. The enhanced antitumor of the combination therapy is particularly useful for patient population that are recalcitrant to inotuzumab ozogamicin or temsirolimus therapy, relapse after treatment with inotuzumab ozogamicin or temsirolimus or where enhanced antitumor effect reduces toxicities associated with treatment using inotuzumab ozogamicin or temsirolimus.

A combination of temsirolimus and trastuzumab in the treatment of cancer is provided. A combination of temsirolimus and HKI-272 is provided. A combination of a trastuzumab and a HKI-272 is also provided. Regimens and kits for treatment of metastatic breast cancer, containing trastuzumab, temsirolimus and / or HKI-272, optionally in combination with other anti-neoplastic agents, or immune modulators are described.

A combination of temsirolimus and trastuzumab in the treatment of cancer is provided. A combination of temsirolimus and HKI-272 is provided. A combination of a trastuzumab and a HKI-272 is also provided. Regimens and kits for treatment of metastatic breast cancer, containing trastuzumab, temsirolimus and / or HKI-272, optionally in combination with other anti-neoplastic agents, or immune modulators are described.

The invention features methods for treatment of a patient in need thereof with the administration of mammalian target of rapamycin (mTOR) inhibitors such as sirolimus, temsirolimus, everolimus or rapamycin analogs including AP23573, especially to a cancer patient for 4 or 5 consecutive days per week. The mTOR inhibitor therapy can be used for a wide range of cancers including prostrate, pancreas, ovary, lung, breast, bladder, colon, brain, head and neck, endometrium, leukemia, lymphoma and sarcoma.

Described herein are methods for distributing a combination of a cell division inhibitor (e.g., temsirolimus or paclitaxel) and dexamethasone to a tissue surrounding a blood vessel for treating vascular diseases. Also disclosed are injectable compositions of a cell division inhibitor (e.g., temsirolimus or paclitaxel) and dexamethasone for delivery into the tissue surrounding a blood vessel for treating vascular diseases.

Methods for treating cancer (e.g., breast cancer, lung cancer, pancreatic cancer, primitive neuroectodermal tumors, lung cancer, ovarian cancer, endometrial cancer, pharyngeal cancer, esophageal cancer, and sarcoma) in a subject (such as an human patient) in need thereof by administering eribulin (e.g., eribulin mesylate, i.e., E7389, Halaven) in combination with one or more mammalian target of rapamycin (mTOR) inhibitors (e.g., everolimus, ridaforolimus, and temsirolimus), and kits therefor are provided.

The present invention provides two synthetic routes for the preparation of Temsirolimus (compound 1b and analog of Temsirolimus 1a). The first route includes the synthesis of CCI-779 by directly reacting rapamycin (4b) or Prolyl-rapamycin (4a) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base, followed by deprotection to give CCI-779 or Proline CCI-779. The second route includes a process involving a reaction of rapamycin-OH-31-sily ether (4d) or Prolyl-rapamycin-OH-31-sily ether (4c) with substituent-2,2-bis(methoxy) propionic acid anhydride(11) in the presence of an organic base and followed by subsequent hydrolysis step to obtain the desired CCI-779 or Proline CCI-779.Compound 11, as described in this invention, is stable at room temperature, cost effective and ease of processing.

The invention discloses application of a mTOR signal path inhibitor to preparation of a medicament for preventing or treating extragenetic hearing impairment. The mTOR signal path inhibitor is selected from at least one of sirolimus, sirolimus analogue and second-generation mTOR signal path inhibitor; the sirolimus analogue is selected from at least one of everolimus, temsirolimus and Deforolimus;the second-generation mTOR signal path inhibitor is selected from at least one of PI3K / mTOR double inhibitor, selective mTORC1 / 2 inhibitor and ATP competitive mTOR kinase inhibitor. As found by the inventor of the application, the mTOR signal path inhibitor can effectively relieve damage to inner ear hair cells and spiral ganglion cells caused by non-genetic factors such as ototoxic drug, remarkably improve the impaired listening ability, and effectively prevent and treat extragenetic hearing impairment.

The present invention relates to a prophylactic or therapeutic agent for fibrodysplasia ossificans progressiva comprising as an active ingredient, at least one compound selected from the group consisting of rapamycin, temsirolimus, everolimus, ridaforolimus, TAFA93, umirolimus, olcorolimus, zotarolimus, and pharmaceutically acceptable salts thereof.

The invention discloses a method for separating and purifying temsirolimus. The method comprises the following steps: (1) synthesis of a crude product; and (2) separation and purification. The specific separation and purification method has the advantages of great improvement of the purity and the yield of temsirolimus, reduction of the cost, and broad market application prospect.

The present invention relates to combinations of aplidine with another anticancer drug selected from sorafenib, temsirolimus, and sunitinib, and the use of these combinations in the treatment of cancer.

The invention belongs to the field of preparation of medicines, and particularly relates to a stable temsirolimus albumin nano-composition as well as a lyophilized preparation, a preparation method and application thereof. By adopting the temsirolimus albumin nano-composition disclosed by the invention, the technical defect that organic solvents such as chloroform / dichloromethane are not dissolvedwith water are required to use in the prior art is overcome. The temsirolimus albumin nano-composition is characterized in that temsirolimus or a derivative of the temsirolimus is dissolved by adopting an organic solvent mutually dissolved with the water, albumin is dispersed by adopting water-based medium, and temsirolimus is mixed with the albumin to prepare nano-suspension liquid, so that thenano-composition of which pH is 6.0 to 7.5 and the average particle size is not greater than 200nm is obtained. The nano-composition has nano-particles with excellent stability, so that the stabilityand the security of the medicine are improved; meanwhile, when the lyophilized preparation is prepared by adopting the nano-composition, even if a lyophilization protector and a protein stabilizationagent are not needed, the qualified lyophilized preparation also can be prepared. After the lyophilized preparation is prepared, zeta electrical potential of the lyophilized preparation after dispersion of the water-based medium is -2 to -40mv.

A method for preparing temsirolimus, the method including: using a substituted aromatic aldehyde to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using sulfuric acid to remove a protecting group from the intermediate III to yield temsirolimus.