234 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 invention relates to a combination of treatments, more particularly a combination treatment for HIV-1 infection. The present invention is directed to the use of bryostatin-1 and their natural and synthetic derivatives for AIDS therapy, in particular to the use of bryostatins in combination with other active drugs such as Histone Deacetylases (HDACs) inhibitors and anti-retrovirals, for the treatment of HIV-1 latency. According to the present invention, we provide a combination therapy for the treatment of HIV-1 latency which employs bryostatin-1 (and analogues) and one of the following HDAC inhibitors; valproic acid, butyrate derivatives, hydroxamic acids and benzamides. While HDACi can be used in continuous dosing protocol, bryostatins can be used following a cyclical dosing protocol. Bryostatins can be formulated in pharmaceutical acceptable carriers including nanoparticles, phospholipids nanosomes and / or biodegradable polymer nanospheres. This combination therapy needs to be used in patients treated with antiretroviral therapy (HIV-1 protease inhibitors, HIV-1 reverse transcriptase inhibitors, HIV-1 integrase inhibitors, CCR5 co-receptor inhibitors and fusion inhibitors).

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.

This invention relates to 2-pyridyl substituted imidazoles which are inhibitors of the transforming growth factor-β (TGF-β) type I receptor (ALK5) and / or the activin type I receptor (ALK4), methods for their preparation, and their use in medicine, specifically in the treatment and prevention of a disease state mediated by these receptors.

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.

The present invention provides methods for treating moderate-to-severe or severe atopic dermatitis (AD). The methods of the present invention comprise administering to a subject in need thereof one or more doses of an interleukin-4 receptor (IL-4R) inhibitor such as an anti-IL-4R antibody. In certain embodiments, the methods of the present invention are used to treat severe AD in a patient whose disease is not controlled with systemic therapy (e.g., cyclosporine A) or when such therapy is inadvisable.

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 invention discloses a dihydropyrimidine compound as well as a preparation method and application thereof, belongs to the technical field of medicinal chemistry, and solves the problems of poor effect and large adverse reaction of a P2X3 receptor inhibitor in the prior art. The structure of the dihydropyrimidine compound is as shown in a formula I in the specification. The invention further provides a preparation method of the compound shown in the formula I and application of the compound in preparation of drugs for treating or preventing P2X3 and / or P2X2 / 3 receptor related diseases. The dihydropyrimidine compound provided by the invention has good affinity with P2X3, has a relatively strong antagonistic effect on a P2X3 receptor, and is safe and effective.

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.

The present invention provides methods for treating moderate-to-severe or severe atopic dermatitis (AD). The methods of the present invention comprise administering to a subject in need thereof one or more doses of an interleukin-4 receptor (IL-4R) inhibitor such as an anti-IL-4R antibody. In certain embodiments, the methods of the present invention are used to treat severe AD in a patient whose disease is not controlled with systemic therapy (e.g., cyclosporine A) or when such therapy is inadvisable.

The invention belongs to the technical fields of molecular biology and genetic engineering, and provides an encoding sequence for encoding cDNA of Jatropha curcas farnesyl pyrophosphate synthase. The farnesyl pyrophosphate synthase catalyzes isopentenyl pyrophosphate and dimethylallyl pyrophosphate to carry out continuous condensation reaction to form farnesyl pyrophosphate, is key enzyme for metabolic pathway of Jatropha curcas isoprene, and contributes to reducing the content of phorbol esters and precursor thereof in the Jatropha curcas. Due to the use of the Jatropha curcas protein, substances interacting with the Jatropha curcas protein, or receptors, inhibitors or antagonists, and the like can be screened by various conventional screening methods. The encoding sequence for encoding the cDNA of the Jatropha curcas farnesyl pyrophosphate synthase has great application prospects.

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.

Provided are chemical inducers of pluripotency (CIP) which include glycogen synthase kinase inhibitors, TGF[beta] receptor inhibitors, cyclic AMP agonists and S-adenosylhomocysteine hydrolase (SAH) inhibitors or histone acetylators. A method of inducing pluripotency in a partially or completely differentiated cell by using such chemical inducers of pluripotency is also provided. The method includes: (i) contacting a cell with the CIPs for a sufficient period of time to result in reprogramming the cell into a pluripotent stem cell having ESC-like characteristics (CiPSC). Isolated chemically induced pluripotent stem cells (CiPSCs) and their progeny, produced by inducing differentiation of the CiPSCs, can be used in a number of applications, including but not limited to cell therapy and tissue engineering

The present invention provides methods for treating moderate-to-severe or severe atopic dermatitis (AD). The methods of the present invention comprise administering to a subject in need thereof one or more doses of an interleukin-4 receptor (IL-4R) inhibitor such as an anti-IL-4R antibody.

To provide a therapeutic or prophylactic agent for frequent urination / strong urge to urinate or incontinence associated with overactive bladder, a lower urinary tract disease accompanied by a lower urinary tract pain such as interstitial cystitis and chronic prostatitis or a disease accompanied by a pain, which acts based on excellent trkA receptor-inhibiting activity. [MEANS FOR SOLVING PROBLEMS] Disclosed is a novel azolecarboxamide derivative having an azole ring (e.g., a thiazole or oxazole ring) bound to a benzene, pyridine or pyrimidine ring through a carboxamide. It is confirmed that the azolecarboxamide derivative has a potent trkA receptor-inhibiting activity. It is found that the azolecarboxamide derivative can be used as a very efficient, safe therapeutic or prophylactic agent for a lower urinary tract disease or a disease accompanied by a pain.

The invention relates to compounds having pharmacological activity towards the sigma receptor, and more particularly to 1,2,3-triazole derivatives of formula (I) and to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy and prophylaxis, in particular for the treatment of psychosis or pain.

The present invention provides methods for inhibiting or attenuating tumor growth in a subject by administering an IL-6 antagonist to the subject. In certain embodiments, the methods of the invention are used to inhibit the growth of an anti-VEGF-resistant tumor in a subject. The IL-6 antagonist may be, e.g., an antibody that specifically binds IL-6R. The IL-6 antagonist may be administered in combination with a VEGF antagonist, and / or an EGFR antagonist.

This invention provides a method for treating a subject either during or soon after a seizure, in order to reduce the extent of neuronal damage in the subject resulting from the seizure comprising administering to the subject, either during or soon after the seizure, a therapeutically effective amount of an inhibitor of receptor for advanced glycation endproducts (RAGE), so as to thereby reduce the extent of neuronal damage in the subject. This invention further provides a method for inhibiting neuronal damage which would otherwise result from a seizure in a subject predisposed to having a seizure, comprising administering to the subject a prophylactically effective amount of an inhibitor of receptor for advanced glycation endproducts (RAGE), so as to inhibit neuronal damage which would otherwise result from a seizure in the event the subject were to suffer a seizure.

The invention, belonging to the field of biological pharmacy, relates to an indole benzothiazole derivative and an application of the derivative for preparing inhibitors of 5-HT receptor, especially an application in the field of medicines of nerve system diseases related to the 5-HT receptor. The test of bioactivity shows the indole benzothiazole derivative has inhibiting effect on the 5-HT receptor related to the pathological mechanism of nerve system diseases. The derivative can be used as a medical precursor for synthesizing the inhibitor of the 5-HT receptor, further can be used for preparing medicines for schizophrenia, parkinsonism and other nerve system diseases caused by disfunction of the 5-HT system.

The invention relates to a chiral CB1 (cannabinoid) receptor inhibitor which is showed as a general formula A1 and a general formula A2 and has optical asymetery performance, and slat or solvate which is physiologically acceptable, in particular relates to a diaryl-replaced pyrazole ramification CB1 receptor inhibitor which is showed as the general formula A and the general formula B, has optical asymetery performance and is hypotoxic, and the method also discloses a preparation method and an application used for preparing medicaments for detoxification, weight losing, diabetes mellitus treatment or cardiovascular disease preventing, and all application on medical science related with the CB1 receptor inhibitor.

The present invention provides methods for treating moderate-to-severe or severe atopic dermatitis (AD). The methods of the present invention comprise administering to a subject in need thereof one or more doses of an interleukin-4 receptor (IL-4R) inhibitor such as an anti-IL-4R antibody. In certain embodiments, the methods of the present invention are used to treat severe AD in a patient whose disease is not controlled with systemic therapy (e.g., cyclosporine A) or when such therapy is inadvisable.

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 invention discloses a cultivation system used for generation of a chemically induced pluripotent stem cell, the cultivation system includes a basal culture medium and a composition for promoting chemical reprogramming, wherein the composition for promoting the chemical reprogramming includes a thymine analogue, a cAMP activator, a TGF-[beta] receptor inhibitor, bone morphogenetic protein, a RAreceptor activator, a GSK3 inhibitor, and a basic fibroblast growth factor, and the cultivation system does not comprise serum. In a process of performing the chemical reprogramming of somatic cellsby the method provided by the invention, frequent disc sorting does not require to be performed on cells, compared with an existing cultivation method, operation steps are simplified, cell loss generated in a disc sorting process is reduced, and utilization of the cultivation system provided by the invention does not require usage of the serum, so sequent collection and molecular mechanism analysis of pluripotent stem cells are further simplified, and the system facilitates subsequent establishment of an animal-derived free cultivation system for induced pluripotent stem cells.