50 results about "Glucocorticoid Receptor Agonists" patented technology

Combination therapy comprising the administration of an 11β-hydroxysteroid dehydrogenase type 1 inhibitor and a glucocorticoid receptor agonist for treating some forms of cancer, diseases and disorders having inflammation as a component, and to minimize the side effects associated with glucorticoid receptor agonist therapy.

The invention involves the treatment, prevention, and reduction of immunoinflammatory disorders involving the combination of an agent that increases the signal activity of a glucocorticoid receptor (e.g., glucocorticoid receptor agonist) and an agent that modulates the signaling activity of one or more signaling pathways selected from the NF-κB pathway, NFAT pathway, AP-1 pathway, and Elk-1 pathway such that proinflammatory cytokine secretion or production, or any other inflammatory response, is reduced. Further, screening methods are provided for identifying candidate compounds and strategies useful for treating, preventing, or reducing such conditions.

A composition for treating or reducing a dry eye condition or an ophthalmological disorder that has an etiology in inflammation comprises a dissociated glucocorticoid receptor agonist (“DIGRA”). The composition can be formulated for topical application, injection, or implantation.

Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure

where Z is CONR¹R² or CH²NR¹R² and where R, R^a, R^b, R^c, R^d, Z, A and B are defined herein.

A composition for treating, controlling, reducing, ameliorating, or alleviating infections and their inflammatory sequelae comprises a dissociated glucocorticoid receptor agonist (“DIGRA”) and an anti-infective agent, such as an antibacterial, antiviral, antifungal, antiprotozoal agent, or a combination thereof. The composition can be formulated for topical application, injection, or implantation.

A composition for treating, controlling, reducing, ameliorating, or preventing allergy comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an anti-allergic medicament and/or an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. The anti-allergic medicament can comprise an antihistamine, a mast-cell stabilizer, a leukotriene inhibitor, an immunomodulator, an anti-IgE agent, or a combination thereof.

A composition for treating, controlling, reducing, or ameliorating inflammatory pain comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. It may be used in a method of managing post-surgical ocular pain such that it has lower risk of eliciting adverse side effects seen with other therapeutic agents.

Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure

where A, B, and R¹-R³ are defined herein.

The present invention is related to glucocorticoid receptor agonists comprised of a compound represented by formula (1) which is 2,2,4-trimethyl-6-phenyl-1,2-dihydroquinoline derivative or a salt thereof and novel pharmacological effects of the glucocorticoid receptor agonists. In the formula (1), R¹ represents formula (2a), (3a), (4a) or (5a); R² represents —(CO)—R8, —(CO)O—R9, or the like; R²—O— is substituted at the 4- or -5-position of benzene ring A; R³ represents a lower alkyl group; R⁴, R⁵, R⁶ or R⁷ represents a halogen atom, a lower alkyl group which may have a substituent, or the like; m, n, p or q represents 0, 1 or the like; R⁸, R⁹ or the like represents a lower alkyl group which may have a substituent, a lower alkenyl group, or the like.

Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure

where R¹–R⁹, X, Y and Z are defined herein.

A composition for treating or controlling an inflammatory anterior-segment disease or condition comprises a dissociated glucocorticoid receptor agonist (“DIGRA”). The composition can optionally include an anti-inflammatory agent, an anti-infective agent, or both. The composition can be formulated for topical application, injection, or implantation in the anterior portion of the eye or a tissue adjacent thereto.

The invention provides a pharmaceutical product comprising, in combination, (1) a named glucocorticosteroid receptor agonist and (2) a beta2 adrenoreceptor agonist, a dual beta 2 adrenoreceptor agonist/M3 receptor antagonist, a muscarinic antagonist, a p38 kinase inhibitor, a neutrophil elastase inhibitor, a phosphodiesterase PDE4 inhibitor, an IKK2 kinase inhibitor or a non-steroidal glucocorticoid receptor agonist, and the use of said product in treating respiratory diseases.

A composition for treating or controlling an ocular disease or condition comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), which disease or condition has an etiology, or results, in inflammation. The composition can optionally include an anti-inflammatory agent, an anti-infective agent, or both. The composition can be formulated for topical application, injection, or implantation in an affected eye to treat or control the ocular inflammatory disease or condition.

Cyclic peptides of formula I are potent and selective agonists of melanocortin-4 receptors, and as such are useful research tool for the determination of the physiological roles of the MC-4 receptor, as well as for the diagnoses, treatment or prevention of disorders or diseases mediated through the MC-4 receptor.

This invention is directed to a method for treating an inflammatory condition, treating haematological and other malignancies, causing immunosuppression, or preventing or treating transplant rejection in man or other animals which comprises administering to a patient a compound that has the structure of Formula (I) or Formula (II) as defined below, or a pharmaceutically acceptable derivative thereof or pro-drug therefor, wherein R═NH₂, NHR¹, NHOR², NHNHR², NHCOR², and R¹═C_(1-4)alkyl, C_(3-6)cycloalkyl, C_n, where n=1-3, R₂=methyl, ethyl, R₃=alkyl, cycloalkyl, substituted alkyl, substituted cycloalkyl, aryl, heteroaryl, substituted aryl, or substituted hetrecoaryl; wherein R⁴, R⁵═C_(1-4)alkyl. Novel compounds according to Formula (III), wherein R⁶ and R⁷ are any of H, CH₃CO, CH₃CH₂CO, CH₃CH₂CH₂CO provided that R⁶ and R⁷ are not both H, or Formula (IV), wherein R⁵ and R⁹ are any of H, CH₃CO, CH₃CH₂CO or CH₃CH₂CH₂CO, having use in such methods, are also described.

The present invention is directed to methods for enhanced retroviral delivery of a nucleic acid to a target cell in vitro, ex vivo or in vivo, which involves increasing infectivity of a retrovirus carrying a transgene of interest to a target cell. In one particular aspect the invention relates to a method for increasing retroviral infectivity of target cells comprising culturing packaging cells transfected with retroviral vector containing a transgene of interest in medium containing a glucocorticoid receptor agonist or analog or derivative thereof present in the medium in an amount effective to increase titer of propagated retrovirus; and subsequently culturing a target cell in medium comprising the propagated retrovirus from a) and a glucocorticoid receptor antagonist or analog or derivative thereof present in the medium in an amount effective to increase target cell sensitivity to infection by the propagated retrovirus.

A composition for treating, reducing, ameliorating, or alleviating a back-of-the-eye condition or disorder that has an etiology in inflammation comprises a dissociated glucocorticoid receptor agonist (“DIGRA”). The compositions also can include other anti-inflamatory agents, anti-angiogenic agents, or combinations thereof. The composition can be formulated for topical application, injection, or implantation. The composition can be administered alone or in combination with another procedure chosen to enhance the outcome of the treatment.

The invention relates to an androstane azotic glucocorticoid receptor stimulant compound and a preparation method thereof. The invention further relates to the pharmaceutical preparations comprising the compound and the therapeutic use of the compound, in particular to inflammatory disease, allergic disease or anaphylactic disease.

A composition for treating, controlling, reducing, or ameliorating inflammatory pain comprises a dissociated glucocorticoid receptor agonist (“DIGRA”), a prodrug thereof, a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable ester thereof. The composition can comprise an additional anti-inflammatory agent and can be formulated for topical application, injection, or implantation. It may be used in a method of managing ocular inflammation and/or pain such that it has lower risk of eliciting increased intraocular pressure seen with glucocorticoids.