216 results about "Receptor Inhibition" patented technology

This invention relates to a method for prevention and treatment of Atherosclerosis, Peripheral Vascular Disease, Coronary Artery Disease, and age-related disorders including Osteoporosis, Arthritis, Type II Diabetes, Dementia and Alzheimer's disease in a subject comprising administering to said subject 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, gp130 protein inhibitor/antibody, tyrosine kinases 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 including interleukin-6 inhibitor/antibody, interleukin-6 receptor inhibitor/antibody, gp130 protein inhibitor/antibody, tyrosine kinases 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 inhibition of the signal transduction pathway.

The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y₁ receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y₁ receptor activity.

The present invention provides compounds of Formula (I):

or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

The present invention relates to allergy vaccines and methods of treating and/or preventing asthma, and allergic conditions. The invention is based on the discovery that inhibiting the ligand/receptor interactions involving, e.g., IgE, IL-3, IL-4, IL-5, IL-6, IL-10, IL-13, interferon-alpha, histamine, leukotriene, and their respective receptors, inhibits production of IgE thereby treating or preventing such diseases or conditions. Competitive inhibition of such receptor/ligand interactions is accomplished by immunizing a human or veterinary patient with the interleukin, interferon-alpha, histamine, leukotriene, their receptors, in any combination. Also, the invention relates to inhibiting receptor/ligand interactions involved in IgE production by competitively inhibiting such interactions by administering antibodies to the ligands, receptors, or both, as well as by administering analogs of the receptors (e.g., soluble receptors not associated with a cell).

The present invention relates to allergy vaccines and methods of treating and/or preventing asthma, and allergic conditions. The invention is based on the discovery that inhibiting the ligand/receptor interactions involving, e.g., IgE, IL-3, IL-4, IL-5, IL-6, IL-10, IL-13, interferon-alpha, histamine, leukotriene, and their respective receptors, inhibits production of IgE thereby treating or preventing such diseases or conditions. Competitive inhibition of such receptor/ligand interactions is accomplished by immunizing a human or veterinary patient with the interleukin, interferon-alpha, histamine, leukotriene, their receptors, in any combination. Also, the invention relates to inhibiting receptor/ligand interactions involved in IgE production by competitively inhibiting such interactions by administering antibodies to the ligands, receptors, or both, as well as by administering analogs of the receptors (e.g., soluble receptors not associated with a cell).

The present invention is based upon the surprising discovery that exposure of a non-resistant HIV to a first entry inhibitor, such as an anti-CD4 antibody or a co-receptor inhibitor, which like all current HIV drugs selects for mutations that result in a resistant HIV, surprisingly results in HIV viruses much more susceptible to neutralization by a second entry inhibitor, such as soluble CD4 (sCD4) or an HIV gp41 inhibitor. Therefore, the present invention provides methods and compositions for inhibiting HIV-1 infection in a subject that overcomes the problem of drug resistance.

The invention relates to a 5-HT2A receptor inhibitor, a preparation method and applications thereof, particularly to a compound represented by a general formula (I), and a preparation method thereof,a pharmaceutical composition containing the compound, and uses of the compound as a 5-HT2A receptor inhibitor in preparation of related drugs for prevention and/or treatment of psychogenic diseases and neurodegenerative diseases, wherein each substituent in the formula (I) is defined in the specification. The formula (I) is defined in the specification.

Disclosed is an antithrombotic neurovascular device useful for the treatment of brain aneurysms and/or acute ischemic stroke. The device comprises a mechanical structure, which may be a stent, stent-like structure, or flow diverter, and a drug-eluting coating. This device is designed for local delivery of antiplatelet medication to the site of device implantation in order to improve outcomes for the population of brain aneurysm and/or acute ischemic stroke patients currently being treated with stents, and for use with patients presenting with ruptured aneurysms, in whom systemic dual antiplatelet therapy is contraindicated. The coating comprises an antiplatelet drug, preferably, a GPIIb/IIIa receptor inhibitor, more preferably, abcixmab, and optionally comprises a polymeric binder that functions as a drug modulating polymer. Also disclosed are methods for producing the antithrombotic neurovascular device, and using the device for the treatment of brain aneurysms and/or acute ischemic stroke.

The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

An alternative HER-2/neu product, herstatin, consists of subdomains I and II from the ectodomain of p185HER-2 and a unique 79 amino acid C-terminus encoded by intron 8. Recombinant herstatin added to cells was found to bind to and inhibit p185HER-2. The effects of ectopic expression of herstatin in combination with either p185HER-2 or with its homolog, the EGF receptor, in several cell lines was studied. Cotransfection of herstatin with HER-2 inhibited p185HER-2 levels and caused an approximate 8 fold reduction in p185 tyrosine phosphorylation. Inhibition of p185HER-2 tyrosine phosphorylation corresponded to a dramatic decline in colony formation by cells that coexpressed p185HER-2 and herstatin. Herstatin also interfered with EGF activation of the EGF receptor in cotransfected cells demonstrated by impaired receptor tyrosine phosphorylation, reduced receptor down-regulation, and growth suppression. For both p185HER-2 and the EGF receptor, the extent of inhibition was affected by the expression levels of herstatin relative to the receptor. Herstatin is an autoinhibitor of p185HER-2 and expands its inhibitory activity to another member of the group I family of receptor tyrosine kinases, the EGF receptor.

The present invention provides compounds of Formula (I):

or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein all the variables are as defined herein. These compounds are selective LPA receptor inhibitors.

Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.

In its many embodiments, the present invention provides a novel class of bipiperidinyl compounds as inhibitors of the CCR5 receptors, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with CCR5 using such compounds or pharmaceutical compositions. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

The invention relates to the field of polypeptide purification, especially to a purification method of a polypeptide PDGF receptor inhibitor prepared by a solid-phase synthesis method. According to the method, polypeptide undergoes crude extraction through ion exchange resin, and refining is carried out by high performance liquid chromatography after conversion in the form of salt. Finally, purity reaches more than 95%, and yield reaches 25%. The polypeptide purification method can be used for large-scale preparation of the polypeptide.

The invention relates to Histamine type 4 receptor (H4R) inhibitors for treating tinnitus.

The invention relates to a medicament composition containing sorafenib, hepatocyte growth factor receptor (cMet) inhibitors and epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors and application thereof in preparing medicaments for treating lung cancer, colon cancer, liver cancer, kidney cancer, stomach cancer, encephaloma, sarcoma, pancreatic cancer, ovarian cancer, breast canceror prostatic cancer. The medicament composition has remarkable synergistic effect, improves the curative effect of the medicament, decreases the administration dosage and reduces the occurrence of side effects.

The invention provides a culture system for preparing an endoderm cell line and a method for preparing the endoderm cell line by the culture system. The culture system comprises a composition of a TGF-beta receptor antagonist, an RA receptor activator and a cAMP (cyclic adenosine monophosphate) activating agent, wherein the composition is free from exogenous transcription factors. By the aid of the culture system and the culture method, reprogramming for changing cell fate can be induced, and body cells are reprogrammed into the endoderm cell line.

The invention relates to a pharmaceutical composition containing an insulin-like growth factor-I receptor inhibitor and a histon deacetylase (HDAC) inhibitor and an application thereof in preparing medicines for treating intestinal cancer, liver cancer, lung cancer, kidney cancer, gastric cancer, brain tumor, sarcoma, pancreatic cancer, ovarian cancer, breast cancer or prostate cancer. The pharmaceutical composition of the invention has obvious synergistic effect, thus improving curative effect of medicines, lowering administration dosage and reducing occurrence of side effect.