140 results about "Phosphatidylinositol" patented technology

This invention relates to a method for prevention and treatment of aging and age-related disorders including atherosclerosis, peripheral vascular disease, coronary artery disease, osteoporosis, type 2 diabetes, dementia and some forms of arthritis and cancer in a subject comprising administering to said subject, separately, sequentially or simultaneously a therapeutically effective dosage of each component or combination of statins, bisphosphonates, cholesterol lowering agents or techniques, interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, interleukin-6 antisense oligonucleotide (ASON), gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, serine / threonine kinases inhibitors / antibodies, mitogen-activated protein (MAP) kinase inhibitors / antibodies, phosphatidylinositol 3-kinase (PI3K) inhibitors / antibodies, Nuclear factor κB (NF-κB) inhibitors / antibodies, IκB kinase (IKK) inhibitors / antibodies, activator protein-1 (AP-1) inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof, administered separately, in sequence or simultaneously. Inhibition of the signal transduction pathway for Interleukin 6 mediated inflammation is key to the prevention and treatment of atherosclerosis, peripheral vascular disease, coronary artery disease, aging and age-related disorders including osteoporosis, type 2 diabetes, dementia and some forms of arthritis and tumors. Inhibition of Interleukin 6 mediated inflammation may be achieved indirectly through regulation of endogenous cholesterol synthesis and isoprenoid depletion or by direct inhibition of the signal transduction pathway utilizing interleukin-6 inhibitor / antibody, interleukin-6 receptor inhibitor / antibody, interleukin-6 antisense oligonucleotide (ASON), gp130 protein inhibitor / antibody, tyrosine kinases inhibitors / antibodies, serine / threonine kinases inhibitors / antibodies, mitogen-activated protein (MAP) kinase inhibitors / antibodies, phosphatidylinositol 3-kinase (PI3K) inhibitors / antibodies, Nuclear factor κB (NF-κB) inhibitors / antibodies, IκB kinase (IKK) inhibitors / antibodies, activator protein-1 (AP-1) inhibitors / antibodies, STAT transcription factors inhibitors / antibodies, altered IL-6, partial peptides of IL-6 or IL-6 receptor, or SOCS (suppressors of cytokine signaling) protein, or a functional fragment thereof. Said method for prevention and treatment of said disorders is based on inhibition of Interleukin-6 inflammation through regulation of cholesterol metabolism, isoprenoid depletion and / or inhibition of the signal transduction pathway.

The present invention relates to hovel fused azolepyrimidine derivatives, processes for preparing them and pharmaceutical preparations containing them. The fused azolepyrimidine derivatives of the present invention exhibit enhanced potency for phosphotidylinositol-3-kinase (PI3K) inhibition, especially for PI3K-γ inhibition and can be used for the prophylaxis and treatment of diseases associated with PI3K and particularly with PI3K-γ activity. More specifically, the azole derivatives of the present invention are useful for treatment and prophylaxis of diseases as follows: inflammatory and immunoregulatory disorders, such as asthma, atopic dermatitis, rhinitis, allergic diseases, chronic obstructive pulmonary disease (COPD), septic shock, joint diseases, autoixnmune pathologies such as rheumatoid arthritis, and Graves' disease, cancer, myocardial contractility disorders, heart failure, thromboembolism, ischemia, and atherosclerosis. The compounds of the present invention are also useful for pulmonary hypertension, renal failure, cardiac hypertrophy, as well as neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease, diabetes and focal ischemia, since the diseases also relate to PI3K activity in a human or animal subject.

Medicinal compositions which are useful as phosphatidylinositol 3-kinase (PI3K) inhibitors and anticancer agents; and novel bicyclic or tricyclic condensed heteroaryl derivatives or salts thereof having favorable effects of inhibiting PI3K and suppressing the proliferation of cancer cells.

This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and / or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

This invention relates to novel sulfone 2I3-dihydroimidazo[1 l2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and / or angiogenesis mediated disorders, as a sole agent or in combination with other active ingredients.

The present invention refers to the renin / prorenin receptor (RER) signal transduction pathway and, in particular, to the role of promyelocytic zinc finger protein (PLZF) and its downstream targets involved in this pathway, e.g. the p85α subunit of phosphatidylinositol-3 kinase (PI3K-p85α). In more detail, the present invention refers to a method for determination of RER activity, e.g. stimulation or inhibition of RER activity, using PLZF activity as a measurement from which RER activity is derived. For the determination of RER activity, use can be made of RER / PLZF protein interaction, PLZF translocation and / or PLZF recruitment. The present invention further refers to a use of said method for identifying RER ligands, e.g. pharmaceutically active agonists or antagonists, as well as for studying undesired side-effects of renin inhibitors.

This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and / or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

The invention relate to a high-density sialic acid modified ibrutinib (IBR) nanocomposite and a preparation method thereof. The sialic acid modified IBR nanocomposites comprises IBR, phospholipid anda sialic acid derivative, wherein the molar ratio of IBR to phospholipid is 1:0.5 to 1:5, and the molar ratio of the sialic acid derivative to phospholipid is 1:19 to 1:1. The phospholipid is one or more of phosphatidylglycerol, phosphatidic acid, phosphatidylserine, phosphatidylinositol and cardiolipin. The nanocomposite can obviously improve the drug dissolution performance, provides an injectable product for reducing the daily dose of drugs, and can be used for clinical critical patients to solve the problem that the patients cannot take drugs orally. Based on the theory of ''immunopharmaceuticals'', the sialic acid is used to modify the composite, accumulation of the preparation in tumor site and the inhibitory effect on tumor microenvironment stromal cells are increased, so that the tumor therapeutic spectrum of IBR is expanded, and the drug efficacy is improved.

The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.