Abstract: A compound useful as an A1 adenosine receptor antagonist has the formula: wherein R1 is selected from the group consisting of C1-C8 alkyl; R2 is of the formula:  wherein is an integer ranging from 1 to 8; R5 is H or (CH2)p, wherein p is an integer ranging from 1 to 8 and R6 is H or (CH2)mOH, wherein m is an integer ranging from 1 to 8; R3 is of the formula: —(CH2)qC6H4—R7  wherein q is an integer ranging from 1 to 8; and wherein R7 is selected from the group consisting of H, NH2, (CH2)tOH, wherein t is an integer ranging from 1 to 8; and R9COOH, wherein R9 is an alkyl or alkylidene group having 1 to 8 carbon atoms; and R4 is of the formula:  wherein Rs is selected from the group consisting of H; NH2; (CH2)rOH, wherein s is an integer ranging from 1 to 8; and R10COOH wherein R10 is an alkyl or alkylidene group having 1 to 8 carbon atoms; and r is an integer ranging from 1 to 8.

Abstract: Disclosed herein are methods and associated compositions and medicaments directed generally to the control of cellular and neural activity and for selectively and controllably inducing the in vivo genetic expression of one or more naturally occurring genetically encoded molecules in mammals. More particularly, the present invention selectively activates or derepresses genes encoding for specific naturally occurring molecules such as proteins or neurotrophic factors and induces the endogenous production of such naturally occurring compounds through the administration of carbon monoxide dependent guanylyl cyclase modulating purine derivatives. The methods of the present invention may be used to affect a variety of cellular and neurological functions and activities and to therapeutically or prophylactically treat a wide variety of neurodegenerative, neurological, cellular, and physiological disorders.

Abstract: A corticotropin releasing factor (CRF) antagonist is administered to treat a condition selected from the group consisting of:

Abstract: A skin cream is presented which reduces wrinkles upon topical application to the skin. The main ingredients of the composition include water and a xanthine based compound composition which is mixed together in a first vessel and a glycerin composition heated in a second vessel. The three components of the active ingredient are mixed carefully, making sure that any precipitate produced is remixed into the solution. After heating and mixing the components, the entire composition is cooled with care being taken to push any precipitate back into solution to ensure an even distribution of all of the components. The active ingredient thus produced may be combined with a suitable pharmaceutical vehicle to provide the topical wrinkle reducing moisturizing and protecting composition. The composition is topically applied to the effected area over a period of days or months in order to reduce or entirely eliminate wrinkles and dryness from the skin. The final active ingredient may also be used for other applications.

Abstract: One aspect of the present invention is a method of treating a condition or disease associated with the activity of a multidrug transporter protein comprising administering to a mammal with a condition or disease associated with the activity of a multidrug transporter protein an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. A particularly preferred bifunctional purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide. Methods according to the present invention can be used to treat cancer, a microbial or parasitic infection, HIV, infection, or a condition associated with inflammation such as asthma or rheumatic disease.

Abstract: Novel tricyclic compounds are found to be useful for the treatment or prevention of symptoms or manifestations associated with diseases or disorders affected by cytokine intracellular signaling.

Abstract: Benzimidazole derivatives of Formula I or a pharmaceutically acceptable salt thereof are MCP-1 antagonists and are thus useful in the treatment of inflammation, atherosclerosis, restenosis, and immune disorders such as arthritis and transplant rejection 1

Abstract: The present invention is directed to a method of inducing neurogenesis by administering to a mammal an effective quantity of a compound that induces neurogenesis, where neurogenesis includes proliferation of neural stem and progenitor cells, differentiation of these cells into neurons, and/or survival of these new neurons. In general, the compound comprises three moieties, A, L, and B, covalently linked. A can be a purine, tetrahydroindolone, or pyrimidine; L is a linker, while B is a moiety that promotes absorption of the compound. A particularly preferred compound is N4-[[3-(6-oxo-1,6-dihydropurin-9-yl)-1-oxopropyl] amino] benzoic acid (also known as AIT-082 or leteprinim potassium). Another aspect of the invention is pharmaceutical compositions for inducing neurogenesis.

Abstract: 1

Abstract: The invention features a method of treating rheumatoid arthritis in a mammal comprising administering an agent that inhibits prostaglandin EP4 receptor (EP4) activity. Also featured is a method of identifying agents that selectively inhibit EP4 activity in vivo.

Abstract: A method of treating disease-induced peripheral neuropathy comprises administering to a patient with disease-induced peripheral neuropathy an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The compound can induce peripheral nerve sprouting through the action of a neurotrophic factor such as nerve growth factor (NGF) without the occurrence of hyperalgesia. The peripheral nerve sprouting can be nociceptive nerve sprouting. The disease-induced peripheral neuropathy can be diabetic neuropathy or disease-induced peripheral neuropathy with another basis.

Abstract: A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.