44 results about "Competitive antagonist" patented technology

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

This invention provides novel substituted tricyclic pyridyl carboxamides which act as oxytocin receptor competitive antagonists, as well as methods of their manufacture, pharmaceutical compositions and methods of their use in treatment, inhibition, suppression or prevention of preterm labor, dysmenorrhea, endometritis, suppression of labor at term prior to caesarean delivery, and to facilitate antinatal transport to a medical facility. These compounds are also useful in enhancing fertility rates, enhancing survival rates and synchronizing estrus in farm animals; and may be useful in the prevention and treatment of disfunctions of the oxytocin system in the central nervous system including obsessive compulsive disorder (OCD) and neuropsychiatric disorders.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.

Methods for treating diseases in humans and vertebrate animals are provided using competitive antagonists of cellular metabolites combined with a protective agent for protecting host cells from toxic effects of the drugs. Also provided are kits comprising competitive antagonists and suitable protective agents. In addition, screening methods for identifying competitive antagonists, protective agents and potentiating agents, for use according to the methods of the invention, are provided.

Drug compositions combining antagonists with agonists to prevent desensitization of cellular receptors. An agonist is a substance or drug that produces a maximal or nearly maximal response, whereas an antagonist is a substance or molecule that produces no response, but can block the action of the agonist/drug. A partial agonist produces a moderate response and can also block the response of the receptor to the agonist/drug. The instant invention solves the problem of determining the optimal concentration of an antagonist or inhibitor which is necessary to prevent desensitization, without causing unnecessary and unwanted inhibition, by providing a formulative method detailing how a competitive antagonist of the receptor should be combined with an agonist in a specific proportion to maximize and maintain receptor response throughout drug therapy/administration. Use of the "optimal ratio method" to determine a specific agonist/antagonist composition to prevent .beta..sup.2 receptor desensitization is experimentally verified and validated.

Provided is a method of treating conditions and disorders for which full mGluR5 antagonists are potentially effective, such as, e.g., anxiety, epilepsy, schizophrenia and other psychotic disorders, Parkinson's disease, addictive disorders, and the like in a subject in need of such treatment, comprising administration to such subject of a therapeutically effective amount of a partial, non-competitive mGluR5 antagonist compound of the invention. Specific examples of partial MgluR5 antagonists provided include those compounds having the formula:

wherein: Z is, independently N or —CH—, provided that one, and only one Z is N; R is halogen (e.g., Br, F and the like), alkyl (e.g., methyl), alkenyl (e.g., CH═CH2, aryl (e.g., phenyl), heterocyclic (e.g., thiophenyl).

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

Optimal ratios of pharmaceutical compositions of beta-1 and beta-2 agonists with their respective antagonists. Safer, more cost-effective drugs for heart and lung therapies are made by combining specific antagonists with their agonists to prevent desensitization of cellular receptors, reducing some of the unwanted side-effects of the agonist drugs alone. Determining the optimal concentration of an antagonist or inhibitor, which is necessary to prevent desensitization, without causing unnecessary and unwanted inhibition, creates a new class of pharmaceuticals. To derive an optimum ratio for a specific composition, a formulative method is provided to detail how competitive antagonists of the receptor should be combined with agonists, in specific proportions, to maximize and maintain receptor response throughout drug administration. The "optimal ratio" methodology used to determine a specific agonist/antagonist composition, to prevent beta-1 or beta-2 receptor desensitization, is experimentally verified and validated for specific compositions. Alteration of a specific ratio is practiced to account for the pharmacokinetic/dynamic differences between animals and humans and within human populations.