52 results about "Phosphoinositide Kinase" patented technology

The invention relates generally to methods for inhibiting angiogenesis. More particularly, methods for inhibiting angiogenesis comprise selectively inhibiting phosphoinositide 3-kinase delta (PI3Kδ) activity in endothelial cells. The methods may comprise administration of one or more cytotoxic therapies including but not limited to radiation, chemotherapeutic agents, photodynamic therapies, radiofrequency ablation, anti-angiogenic agents, and combinations thereof.

The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

The invention discloses a phosphoinositide 3-kinase (P13K) inhibitor, a pharmaceutical composition containing the P13K inhibitor, and application of the P13K inhibitor and the pharmaceutical composition. The P13K inhibitor comprises a pyrimidine compound and a stereoisomer/hydrate/pharmaceutically-acceptable salt thereof. The pyrimidine compound has a general formula I of which the structure is shown in the specification. The P13K inhibitor and the pharmaceutical composition containing the same can be used for inhibiting PI3 Ks and treating proliferative diseases on which the PI3 Ks act. According to the invention, high-effectiveness and high-selectivity inhibitors for treating proliferative diseases on which PI3Ks act can be provided.

The invention relates to new triazines (G=Q=U are N), pyrimidines (two out of G, Q and U are N), and pyridopyrimidines (one of G and U together with R2 forms an anullated pyridine ring) of formula (I) carrying a spirocyclic substituent, wherein E¹ is CR⁴ or N; X¹ is CHR⁴, CH₂CH₂, NR⁴, NR4→0, or O; and the other substituents are as defined in the specification. The compounds inhibit phosphoinositide 3-kinase (PI3K), mammalian target of rapamycin (mTOR), DNA-PK and ATM kinase, and may be used as therapeutic agents or diagnostic probes. The invention also relates to methods of using the compounds for treatment of associated pathological conditions.

The invention provides an anti-cancer sustained-release agent co-carrying glucocorticoid and chemotherapeutic drugs and belongs to sustained-release injections. The anti-cancer sustained-release agent comprises sustained-release microspheres and a solvent, wherein, the sustained-release microspheres comprise anti-cancer active components and sustained-release auxiliary materials; and the solvent is a particular solvent containing a suspending agent. The glucocorticoid is selected from prednisolone, methylprednisolone, dexamethasone, betemethasone, triamcinolone acetonide or triamcinolone acetonide; the chemotherapeutic drugs are selected from phosphoinositide 3-kinase inhibitor, pyrimidine analogues and the like; the sustained-release auxiliary materials are biocompatible high-polymers, such as polylactic acid and the copolymers thereof, polyethylene glycol, carboxyl-terminated polylactic acid copolymers, polyfatty acid dimer-sebacic acid copolymers, poly(erucic acid dimer-sebacic acid), poly(fumaric-co-sebacic acid), polifeprosan and the like; and the suspending agent with the viscosity being 100cp to 3,000cp (at the temperature of 20 to 30 DEG C) is selected from sodium carboxymethyl cellulose and the like. The anti-cancer active components and the sustained-release microspheres can further be prepared into sustained-release implants which can effectively inhibit the growth of tumors, alleviate edema and improve the curative effects of radiotherapy and chemotherapy by intra-tumor or peri-tumor injection or placement.

The invention provides a compound of Formula I,

Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.

A slow-release anticancer injection contains the slow-release microspheres and solvent. Said slow-release microsphere contains the active anticancer component chosen from 6 Pt compounds including bicycloplatinum, etc and 3 cytotoxins including phosphoinositide 3-kinase inhibitor, pyrimidine analog or DNA repairase inhibitor, and the slow-release auxiliary.

The present invention is directed to a dual inhibitor of phosphoinositide 3-kinase (PI3K) and histone deacetylase (HDAC), including a core containing a quinazoline moiety or a quinazolin-4(3H)-one moiety, a kinase hinge binding moiety, and a histone deacetylase pharmacophore, a pharmaceutically acceptable salt thereof, a prodrug thereof, or solvate thereof. The present invention is also directed to a histone deacetylase inhibitor, including a core containing a quinazolin-4(3H)-one moiety and a histone deacetylase pharmacophore.

The invention discloses a phosphoinositide 3-kinase EST segment in common wild rice expressed by bacterial blight stress. The nucleotide sequence of the EST segment is disclosed as SEQ ID NO:1. The invention provides the EST segment for the first time, and the EST directly participates in the anti-disease response process of common wild rice and is a gene directly related to bacterial blight resistance. The EST segment provides partial sequence information for separating and cloning the gene full-length cDNA sequence, and provides theoretical references for researching bacterial blight resistance mechanism of the phosphoinositide 3-kinase in common wild rice. The primer designed by using the EST segment can detection the expression condition of the EST segment by bacterial blight stress in common wild rice leaves, thereby obtaining the expression spectrum of the gene after expression by bacterial blight stress in common wild rice, and laying the foundation for recognizing the functions of the gene and deeply researching the bacterial blight resistance mechanism of the gene in common wild rice.

The invention provides a grape polyphosphoinositide kinase gene VvIPK2 with a sequence of SEQ ID NO:1 in a sequence table and also provides grape polyphosphoinositide kinase with an amino acid sequence of SEQ ID NO:2. In the invention, the polyphosphoinositide kinase gene VvIPK2 of a test tube seedling of a wine grape rootstock variety 'F-242' is cloned, and tests prove that grape blades VvIPK2 participate in a grape cold resisting process and the gene VvIPK2 is transferred to arabidopsis, therefore, the invention provides a theoretical basis for improving the grape resistance by using a transgenic technology. According to the invention, H2O2 is proved to be positioned on the upstream of the VvIPK2 to play a role; and the grape polyphosphoinositide kinase gene VvIPK2 has important guiding significance in researching influence of two signal elements on gene expression with cold regulation, change of transcriptome and change of protein level by means of molecular biology, information biology and proteomics, and deeply researching a plant-influenced low-temperature forced signal transduction mechanism.

A anti-cancer slow-release agent co-loaded with glucocorticosteroid and chemotherapy medicament is a slow-release injection agent composed of slow-release microsphere and solvent, wherein, the slow-release microsphere comprises anti-cancer effective ingredient and slow-release auxiliary materials, the solvent is the special solvent containing suspending agent. The glucocorticosteroid is selected from prednisolone, methylprednisolone, dexamethasone, betamethasone, omcilon or triamcinoloneAcetonide, the chemotherapy medicament is selected from phosphoinositide 3-kinase restrainer and pyrimidine analogue or the like; the slow-release auxiliary materials are polylactic acid and copolymer thereof, polyethyleneglycol, polylactide-COOH copolymer, 2-aliphatic acid, sebacic acid polyester, poly(erucic acid dimmer-sebacic acid), poly(fumaric acid-sebacic acid), polyphenyl and polylactic acid or the like biocompatibility high molecules; the suspending agent viscosity is 100cp-3000cp (20 DEG C-30DEG C) and the suspending agent is selected from sodium carboxymethyl cellulose. The anti-cancer effective compositin and the slow-release microsphere can be made into a slow-release implantation agent, by intra-tumor injection or tumor circumference injection or arrangement, the tumor growth can be effectively inhibited, the edema can be alleviated, and the curative effects of the chemotherapy and the radiation therapy can be reinforced.

Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation. The compounds are useful in treating PI 3-kinase-dependent conditions including cardiovascular diseases such as coronary artery occlusion, stroke, acute coronary syndrome, acute myocardial infarction, vascular restenosis, atherosclerosis, and unstable angina; respiratory diseases such as asthma, chronic obstructive pulmonary diseases (COPD), and bronchitis; inflammatory disorders, neoplasms including cancers such as glioma, prostate cancer, small cell lung cancer, and breast cancer, and diseases linked to disordered white blood cell function, such as autoimmune and inflammatory diseases.

Therapeutic combinations of a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the γ- and δ-isoforms and selective for both γ- and δ-isoforms (PI3K-γ,δ, PI3K-γ, and PI3K-δ, a Janus kinase-2 (JAK-2) inhibitor, a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor, and/or a Bruton's tyrosine kinase (BTK) inhibitor are described. In certain embodiments, the invention includes therapeutic combinations of a cyclin-dependent kinase-4/6 (CDK4/6) inhibitor and a BTK inhibitor, a PI3K-δ inhibitor and a BTK inhibitor, a JAK-2 and a BTK inhibitor, and a JAK-2, PI3K-δ, and BTK inhibitor.

The invention belongs to the field of pharmaceutical chemistry and relates to a novel phosphoinositide 3-kinase inhibitor, a preparation method and an application thereof. Specifically, the present invention provides a compound having the structure of formula I, which can be used as an efficient PI3K inhibitor and has various pharmacological activities such as tumor resistance, resistance to neurodegenerative diseases (such as Alzheimer's disease), inflammatory resistance, etc.

The invention provides an application of a PPP3CC gene or an expression product thereof in treatment of Kawasaki disease, and specifically, relates to an application of the protein phosphatase 3,catalytic subunit,gamma isozyme (PPP3CC) gene, a protein or an accelerator thereof in preparation of a pharmaceutical composition for (i) increasing the expression quantity and/or activity of 1,4,5-trisphosphate3-kinase C (ITPKC) and/or (ii) for treating Kawasaki disease. The gene is beneficial for understanding a pathogenesis and path of Kawasaki disease, and developing drugs for treating Kawasaki disease.