159 results about "Selective antagonist" patented technology

The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula Iwhich are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

The subject invention provides compounds having the structure: wherein R1 is substituted or unsubstituted phenyl or a 5-6 membered heterocyclic or heteroaromatic ring containing from 1 to 5 heteroatoms; R2 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety; R3 is hydrogen, or a substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R2 and R3 are joined to form a heterocyclic ring; wherein the dashed line represents a second bond which may be present or absent, and when present R3 is oxygen; R4 and R5 are each independently substituted or unsubstituted alkyl, —C(O)-alkyl, —C(O)—O-alkyl, alkoxy, cycloalkyl, alkenyl, monocyclic or bicyclic aryl, heteroaryl or heterocyclic moiety, or R4NR5 together form a substituted or unsubstituted monocyclic or bicyclic, heterocyclic or heteroaryl moiety containing from 1 to 6 heteroatoms; R12 is hydrogen, alkyl, halogen or cyano; and n is 0, 1, 2, 3 or 4, or an enantiomer, or a specific tautomer, or a pharmaceutically acceptable salt thereof and a method for treating a disease associated with the A2b adenosine receptor by administering a therapeutically effective amount of the compounds of the invention.

MDM2 and MDM4 proteins prevent apoptosis of cancer cells by negatively regulating the transcription factor p53. Compounds according to Formula Iare selective antagonists of MDM2 and MDM4 proteins, disrupting the p53 / MDM2 and p53 / MDM4 complex. These compounds therefore are candidate therapeutics for treating cancer as well as other cell proliferative disease states.

Selective antagonists of A2B adenosine receptors like those of formula I are provide.The compounds and compositions are useful as pharmaceutical agents.

The present invention provides methods of treating chronic pain in a mammal by administering to the mammal an effective amount of a selective persistent sodium channel antagonist that has at least 20-fold selectivity for persistent sodium current relative to transient sodium current.

The present invention relates to methods for elevating high density lipoprotein (HDL) plasma levels, decreasing the absorption of dietary cholesterol in the intestine, decreasing the plasma level of low density lipoprotein (LDL), and increasing the conversion of cholesterol to bile acids, utilizing LXRβ selective agonists, usually without elevating the plasma levels of triglycerides. Also provided are methods of using such agonists to treat metabolic diseases alone or in combination with other active agents. Also provided are methods for decreasing hyperglycemia and insulin resistance methods for treating type II diabetes, and methods for treating type II diabetes and reducing the cardiovascular complications of type II diabetes, utilizing an LXR agonist. Further provided are methods for treating obesity and methods for treating the complications of obesity including type II diabetes, cardiovascular disease, hyperlipidemia, and hypertension, administering an LXRα-selective antagonist.

The present invention is directed to novel compounds of formula Iand their use as therapeutic compounds.

The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula Iwhich are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xanthines of formula Iwhich are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.

Selective antagonists of A2A adenosine receptors like those of formula I are provided, wherein Y forms a ring.The novel A2A blockers are useful for the treatment of Parkinsons disease and other diseases.

Ophthalmic formulations are provided. The ophthalmic formulations include one or more active agents that act to optimize pupil light reflex while minimizing, or effectively eliminating, any undesired eye redness in response to application thereof. The active agents include, for example, alpha 1 antagonists, such as alpha 1a selective antagonists.

The present invention provides processes for making pyridyl-linked-xanthines of formula VII, from 5,6-diamino-1H-pyrimidine-2,4-diones of formula II and acylating agents of formula VI.The xanthines are expected to be are selective antagonists of A2B adenosine receptors (ARs).

The present invention is directed to novel compounds of formula Iand their use as therapeutic compounds.