Abstract: The preferred embodiments generally relate to methods and compositions that affect the GTP-binding activity of members of the Rho family GTPases, preferably Rac (Rac1, Rac2 and/or Rac3), such compositions include compounds that modulate the GTP/GDP exchange activity, along with uses for the compounds including screening for compounds which recognize Rac GTPase, and methods of treating pathological conditions associated or related to a Rho family GTPase, including Rac. The preferred embodiments also relate to methods of using such compounds, or derivatives thereof, e.g., in therapeutics, diagnostics, and as research tools.

Abstract: Compounds of Formula II wherein R1, A, R2, R3, R4, R5, R8, n, m and q are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositions containing and methods for using the same.

Abstract: The present invention relates to the use of nucleoside derivatives of formula I wherein B signifies a 9-purinyl residue B1 of formula or a 1-pyrimidyl residue B2 of formula wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof; for the treatment of diseases mediated by the Hepatitis C Virus (HCV), for the preparation of a medicament for such treatment and to pharmaceutical compositions containing such compounds.

Abstract: The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of general formula (1): wherein X?C?O, C—S—CH3, C—S, —C—NHOH, Z—C or N, Y— with the adjacent ring, a phenyl or thienyl group, the ring(s) of said derivatives being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, —COM, —COOM, or —CH2COOM groups (where M=H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups) nitroso, or cyano, R5?H, or C1 to C5 alkyl and R12?H, or —C—CO2—(CH3)3 and the phy

Abstract: Formulations for minimizing damage to at least one of cells, organs and systems within the body of a subject afflicted with Diabetes Mellitus. The invention additionally encompasses methods for minimizing said damage which comprise administering to subjects in need thereof a therapeutic amount of a formulation(s) according to the invention.

Abstract: An object of the present invention is to provide a cyclic amine compound which has a potent inhibitory effect on the binding of ?2C-adrenoceptor and is useful in preventing and treating disorders attributable to ?2C-adrenoceptor. The above-described object is solved by the following cyclic amine compound, etc., wherein X is O, S, SO, SO2 or NR2, etc.; R1 is a hydrogen atom, a cyano group, a carboxyl group, a C2-C13 alkoxycarbonyl group, a carbamoyl group, etc.; Ar1 and Ar2 are the same or different and each represent an aryl or heteroaryl group which may be substituted by 1 to 3 substituents and so on; ring B is a benzene ring may be substituted by 1 to 3 substituents and so on; n is an integer from 1 to 10; and p and q are the same or different and each represent an integer of 1 or 2.

Abstract: A method is provided for first line treatment of type 2 diabetes employing a combination of metformin and glyburide. A method for treating diabetes in drug naive human patients is also provided employing the above formulation to reduce insulin resistance and/or post-prandial glucose excursion and/or hemoglobin 1Ac, and/or increase post-prandial insulin, thereby treating the diabetes.

Abstract: Compounds of formula (I) are potent and selective 5-HT2A antagonists, useful in treatment of a variety of adverse conditions of the CNS.

Abstract: This invention generally relates to derivatives of substituted azabicyclo hexanes. The compounds of this invention can function as muscarinic receptor antagonists, and can be used for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to a process for the preparation of the compounds of the present invention, pharmaceutical compositions containing the compounds of the present invention and the methods of treating the diseases mediated through muscarinic receptors.

Abstract: It is an object of the present invention to provide an external preparation having enhanced transdermal penetration of a mast cell degranulation inhibitor. It is also an object of the present invention to provide a method for improving the photostability of a preparation containing a mast cell degranulation inhibitor. The present invention provides an external preparation containing a mast cell degranulation inhibitor and a topical anesthetic. Further, the method for enhancing the photostability of a preparation containing a mast cell degranulation inhibitor according to the present invention includes adding a topical anesthetic thereto.

Abstract: Disclosed are compounds of formula (I): wherein R1 and R4 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases, cardiovascular disease and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

Abstract: The present invention relates to 4,5-dihydropyrrolo[3,2-c]pyridin-4-one compounds of formula IA and processes for preparing such compounds, their use in the treatment of obesity, psychiatric and neurological disorders, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with alkene piperidine derivatives that possess unique antiviral activity. More particularly, the present disclosure relates to compounds useful for the treatment of HIV and AIDS.

Abstract: The present invention provides an MMP-inhibitory composition comprising chalcone or its derivatives. They inhibit the MMPs in collagenase subfamily as well as those in gelatinase subfamily. The MMP inhibitory activity of chalcone derivatives was similar to or greater than that of parent compound, chalcone. Chalcone or its derivatives of the present invention inhibit activity of matrix metalloproteinase, so that it can be applied to treat and prevent diseases related to matrix metalloproteinase.

Abstract: The use of angelicin and its structural analogues for the preparation of a medicament for the therapeutic treatment of beta-thalassaemia is described. A structural analogue which is particularly preferred for this purpose is bergapten.

Abstract: A compound of the formula wherein R1, R2 and R3 are as defined above, which are inhibitors of the enzyme protein tyrosine kinases such as Janus Kinase 3 and as such are useful therapy as immunosuppressive agents for organ transplants, lupus, multiple sclerosis, rheumatoid arthritis, psoriasis, Type 1 diabetes and complications from diabetes, cancer, asthma, atopic dermatitis, autoimmune thyroid disorders, ulcerative colitis, Crohn's disease, Alzheimer's disease, Leukemia and other autoimmune diseases.

Abstract: A treatment protocol by which a renal stone patient is administered a chelating agent, generally once a day and preferably by mouth, during a treatment phase and is later administered the same chelating agent once a week, during a “maintenance” phase. The chelating agent is most preferably ethylene diamine tetraacetic acid (EDTA) and may be provided in a dosage form having an enteric coating and at least one external cathode and at least one external anode to create a galvanic current upon contact of the dosage form with the patient's intestinal contents.

Abstract: Provided is a method of treating hypertension, which comprises administering an effective amount of a compound represented by the following formula (1) or (2): wherein, R1 and R2 are the same or different and each independently represents hydrogen, alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkoxyalkyl, aryl, alkylaryl, aralkyl, or acyl, R3 represents hydroxyl, ester bond residue, or amide bond residue, R4 represents ester bond residue or amide bond residue, or a pharmaceutically acceptable salt thereof (except ferulic acid).

Abstract: The present invention provides an antiallergic agent comprising, as an active ingredient, at least one of a tomato extract, tomato pericarp, naringenin chalcone or its derivatives, tricaffeoylquinic acid or its derivatives and dicaffeoylsuccinylquinic acid or its derivatives; a histamine-release inhibitor or a leukotriene-release inhibitor; and a medicament, food, drink or cosmetic comprising the antiallergic agent, the histamine-release inhibitor or the leukotriene-release inhibitor mentioned above; and a method for producing an antiallergic agent comprising extracting raw material tomato with a solvent.

Abstract: An antidiabetic pharmaceutical formulation is provided, especially adapted for treating Type II diabetes, which includes a combination of metformin and glipizide in a manner to control moisture in the formulation so that the glipizide does not hydrolyze, yet the metformin is compressible, if necessary. A method for treating diabetes is also provided employing the above formulation.