Abstract:
In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
Abstract:
Provided are immediate or prolonged administration of certain salts of KATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving KATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
Abstract:
The invention relates to a composition comprising taurolidine and/or the hydrolysis products thereof and also a biodegradable (co)polymer or inorganic matrix for use as an implant for treating local infections of the skeleton and soft tissue. A lozenge and a spray solution or gargling solution likewise comprises taurolidine and/or the hydrolysis products thereof and is used in the treatment of throat inflammations, sore throats with difficulty in swallowing, inflammations of the mouth and throat area and laryngitis. A method for producing taurolidine is also disclosed.
Abstract:
The present invention relates to arylcarbonyl and heteroarylcarbonyl anthranilate compounds that may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment disorders.
Abstract:
The present invention relates to novel compounds that act as chemical uncouplers. Compounds of the invention are useful, inter alia, in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.
Abstract:
Provided are immediate or prolonged administration of certain salts of K ATP channel openers such as diazoxide to a subject to achieve novel pharmacodynamic, pharmacokinetic, therapeutic, physiological, metabolic and compositional outcomes in the treatment of diseases or conditions involving K ATP channels. Also provided are pharmaceutical formulations, methods of administration and dosing of the salts that achieve these outcomes and reduce the incidence of adverse effects in treated individuals. Further provided are method of co-administering the salts with other drugs to treat diseases of humans and animals.
Abstract:
Compounds having the formula (I) are hepatitis C (HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting hepatitis C (HCV) polymerase, processes for making the compounds, and synthetic intermediates employed in the processes.
Abstract:
The invention provides novel compounds represented by general formula (I) wherein the bond represented by the broken line may be a single, double bond or absent; and if the bond is absent, then the nitrogen is substituted with a hydrogen and R ; X represents SO2 or C=O of CH2; Y represents -CH(R )-, -N(R )- or -N(R )-CH2-, O; and the meaning of R , R , R , R , R , R , and R are as defined in the application. The compounds are useful as positive modulators of the AMPA-receptor.
Abstract:
1,2,4-Benzothiadiazine derivatives represented by formula (I) wherein D, R , R , R , R , R , R , R , R , R are defined in the description, compositions thereof and methods for preparing the compounds are described. The compounds are useful in the treatment of diseases of the central nervous system, the cardiovascular system, the pulmonary system, the gastrointestinal system and the endocrinological system.
Abstract:
A benzothiadiazine derivative represented by general formula (I), a hydrate and acid addition salt thereof, and a remedy for peptic ulcer containing said derivative, said hydrate or said salt as an active ingredient. In formula (I) X represents methylene or a lower alkyl-substituted nitrogen atom; Y and Z represent each methylene or carbonyl; A represents phenylene which may be substituted by methoxycarbonyl; B represents lower alkylene or lower alkenylene; R1 represents hydrogen, acetoxyacetyl, cyclohexylmethyl, or benzyl wherein the benzene ring may be substituted by lower alkoxy, halogen, nitro, lower alkyl, methylenedioxy or hydroxyl; R2 represents lower alkyl or phenyl; and R3 represents hydrogen, halogen or lower alkoxy, provided that the case where X, Y and Z represent each methylene, A represents unsubstituted phenylene, B represents lower alkylene, and R1 represents hydrogen is excluded.