78 results about "PI3 Kinases" patented technology

The present invention provides compositions and methods for the production of differentiated mammalian cells. More particularly, the present invention provides cellular differentiation methods employing culturing the cells on a feeder layer or under feeder-free conditions in cell culture and further contacting the cells with an inhibitor of the PI3-kinase pathway for the generation of differentiated mammalian cells from pluripotent mammalian stem cells. Preferably, the differentiated cell is selected from the group consisting of a mesendodermal cell, a mesodermal cell, and an endodermal cell.

The present invention provides novel compounds that are antagonists of PI3 kinase, PI3 kinase and tryosine kinase, PI3Kinase and mTOR, or PI3Kinase, mTOR and tryosine kinase.

Invented is a method of inhibiting the activity / function of PI3 kinases using quinoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoline derivatives.

An embodiment of the present invention is a method for measuring the post translational states and expression levels of proteins in the PI3K and / or mTor for use in diagnosis, prognosis and drug screening applications.

The invention which belongs to the technical field of medicines concretely relates to tricyclic dual PI3K and mTOR inhibitors 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>, X, A, and B are defined in the specification. The invention also relates to a preparation method of above compounds, a medicinal preparation containing the compounds, and an application of the compounds in the preparation of medicines for treating and / or preventing proliferative diseases responding to the inhibition of the activity of lipase and / or PI3-kinase-related protein kinase, especially the PI3 kinase and / or mTOR.

The invention is directed to certain novel compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.

The invention is directed to to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.

The present invention relates to Imidazolopyrimidine Analogs, methods of making Imidazolopyrimidine Analogs, compositions comprising an Imidazolopyrimidine Analog, and methods for treating or preventing a PI3K-related disorder comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog. The invention also relates to methods for treating or preventing mTOR-related disorders comprising administering to a subject in need thereof an effective amount of an Imidazolopyrimidine Analog.

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.

Invented is a method of inhibiting the activity / function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of P13-kinase activity.

The invention is directed to certain novel compounds directed to compounds of formula (I) and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.

The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I):and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.

Invented is a method of inhibiting the activity / function of PI3 kinases using pyridosulfonamide derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of pyridosulfonamide derivatives.

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Highly effective combinations of a compound of formula A (a PI3Kδ selective inhibitor) and anti-CD20 antibodies are provided herein for the treatment and amelioration of PI3Kδ and / or CD20 mediated diseases and disorders. In particular, the combination can be used to treat cancers and autoimmune diseases. More particularly, the invention provided for a combination of a compound of formula A, or stereoisomers thereof, and ublituximab for the treatment and / or amerioration of hematological malignancies such as leukemia and lymphoma.

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.

Invented is a method of inhibiting the activity / function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.

Invented is a method of inhibiting the activity / function of PI3 kinases using naphthyridine derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of naphthyridine derivatives.

Invented is a method of inhibiting the activity / function of PI3 kinases using quinazoline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinazoline derivatives.

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

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.

There is provided compounds of formula (I), wherein A1, A4, A4a, A5, B1, B1a, B2, B2a, B3, B3a, B4, B4a and R3 have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein or lipid kinase (e.g. a PI3-K and / or mTOR) is desired and / or required, and particularly in the treatment of cancer or a proliferative disease.

Compounds of formula 1 are effective modulators of PI3 kinase: wherein R1 is H, hydroxy, amino, lower alkyl, or trihalomethyl;R2 is amino, lower alkylamino, lower acylamino, arylamino, arylacyl-amino, heteroaryl-amino, heteroaryl-acyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, trihalomethyl, hydroxy, lower alkyl and lower alkoxy, or a substituent of the form —(CH2)n—C(═X)—R8, where n is 014 3 inclusive and X is O or NR9, where R9 is H, lower alkyl, or R1 and R2 together form —CH═N—X— where X is CH, NH, O, or S, and R8 is H, lower alkyl, lower alkoxy, aryl, aralkyl, or —(CH2)mCR10R11R12, where m is 0-3 inclusive, and R10, R11, and R12 are each independently H, lower alkyl, aryl, aralkyl, hydroxy, lower alkoxy, aryloxy, aralkoxy, amino, lower alkyl-amino, arylamino, aralkylamino, heteroaryl amino, or heteroaralkyl amino, where aryl and heteroaryl are substituted with 0-3 substituents selected from the group consisting of halo, hydroxy, and lower alkyl;R3 is H or lower alkyl; andR4, R5, R6, R7 are each independently H, halo, hydroxy, amino, nitro, lower alkyl, or lower alkoxy;and pharmaceutically acceptable salts thereof.

The invention relates to compounds of formula (I) R<1> is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, C1-C4-alkyl- sulfonyl, acryloyl, or methacryloyl; or R<1> is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R<2> and R<3>, independently of each other, are hydrogen or C1-C4-alkyl, or R<2> and R<3> together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and / or mTOR, in particular treating a hyperproliferative disorder.