277 results about "Discovery and development of mTOR inhibitors" patented technology

The present invention relates, in part, to compositions and methods for enhancement of an immune response by partial mTOR inhibition, e.g., with low, immune enhancing, doses of an mTOR inhibitor, such as RAD001.

The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).

Compounds represented by Formula (I) or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

The invention provides for the use of an mTOR inhibitor in the treatment or inhibition of fibroids.

Compounds represented by Formula (I)or a pharmaceutically acceptable salt thereof, are inhibitors of mTOR and useful in the treatment of cancer.

The present invention provides a method for treating NSCL, pancreatic, colon or breast cancer tumors or tumor metastases in a patient, comprising administering to the patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein the agent is an mTOR inhibitor, with or without additional agents or treatments, such as other anti-cancer drugs or radiation therapy. The present invention also provides a method for treating tumors or tumor metastases in a patient, comprising administering to said patient simultaneously or sequentially a therapeutically effective amount of a combination of an EGFR kinase inhibitor and an agent that sensitizes tumor cells to the effects of EGFR kinase inhibitors, wherein said agent is an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases. The present invention also provides a pharmaceutical composition comprising an EGFR kinase inhibitor and an mTOR inhibitor that binds to and directly inhibits both mTORC1 and mTORC2 kinases, in a pharmaceutically acceptable carrier. A preferred example of an EGFR kinase inhibitor that can be used in practicing the methods of this invention is the compound erlotinib HCl (also known as TARCEVA®).

The invention which belongs to the technical field of medicines concretely relates to dual PI3K and mTOR inhibitor compounds with a general formula represented by formula (I), pharmaceutically acceptable salts thereof, or stereoisomers thereof. In the formula (I), R<1>, R<2>, R<3>, R<4>, R<5>, R<6>, R<7>, X and Y are defined in the specification. The invention also relates to a preparation method of the compounds, medicinal preparations containing the compounds, medicinal compositions containing the compounds, and an application of the compounds in the preparation of medicines for treating and / or preventing proliferative diseases.

Provided herein is a combination therapy comprising a JAK kinase inhibitor and a dual PI3K / mTOR inhibitor, as well as methods of treating various cancers through the use of such a combination therapy.

The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine mammalian target of rapamycin (mTOR) inhibitor which is shown as a general formula (I), pharmaceutically acceptable salts and stereoisomers thereof, and deuterated pyridopyrimidine mammalian mTOR inhibitors, wherein Z<1>, Z<2>, Z<3>, R<1>, R<2>, R<3>, X and W are defined in the specifications. The invention also relates to preparation methods for the compounds, medicinal inhibitors and medicinal compositions which contain the compounds, and the application of the compounds to preparation of medicines for treating and / or preventing post-transplant lymphoproliferative diseases which have response to inhibition of mTOR activity.

The present application demonstrates that HDAC inhibitors can be used in combination with hormonal therapy to treat and prevent estrogen receptor positive breast cancer. HDAC inhibitors can also be combined with IGF-1R inhibitors, mTOR inhibitors, and EGFR inhibitors to treat breast cancer, optionally in combination with hormonal therapy if indicated. Combinations of the compounds, with or without HDAC inhibitors, and with or without hormonal therapy, can also be used. The invention therefore provides methods of treatment and pharmaceutical compositions.

The invention provides the use of a combination of an mTOR inhibitor and capecitabine in the treatment of cancer.

Disclosed is the use of an mTOR inhibitor for treatment of certain eye disorders.

Compounds of formula Iwherein:R1 isand R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.

The present invention relates to compositions containing an mTOR inhibitor, such as rapamycin or a rapamycin derivative, in combination with a PI3 kinase inhibitor and / or a leptin inhibitor, intraluminal devices configured to release such compositions, and methods for the treatment and / or prevention of intimal hyperplasia, vascular stenosis and / or restenosis comprising delivery of such compositions or intraluminal devices to subjects in need thereof. The compositions, intraluminal devices, and methods of the invention are particularly well-suited for the treatment or prevention of vascular stenosis and restenosis in obese and diabetic subjects.