Abstract: The present invention relates to indazolo-tetrahydropyrimidine-carboxamide derivatives, compositions and medicaments containing the same, as well as processes for the preparation and use of such compounds, compositions and medicaments. Such indazolo-tetrahydropyrimidine-carboxamide derivatives are useful in the treatment of diseases associated with inappropriate ROCK-1 kinase.

Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: The present invention relates to the design of libraries, such as combinatorial libraries, which may be used in the discovery of novel potentially useful compounds. The invention operates on a population of libraries that is refined iteratively. The refinement involves the following steps: calculating the relative dominance of the libraries in the population; selecting libraries for modification according to dominance; modifying the selected libraries using genetic operators; and inserting the modified libraries back in the population. The refinement steps are repeated until adequate convergence is deemed to have occurred or for a specified number of iterations. The Pareto optimal set of libraries in the final population is output for further processing such as storage or manufacture.

Abstract: The present invention relates to a pharmaceutical formation which comprises an aqueous suspension of particulate (2S)-3-[4-({[4-aminocarbonyl)-1-piperidinyl]carbonyl}oxy)phenyl]-2-[((2S)-4-methyl-2-{[2-(2-methylphenoxy)acetyl]amino}pentanoyl)amino]propanoic acid or a salt or solvate thereof. Methods and uses of the formulation in the treatment of allergic rhinitis are also described, as are containers containing said formulation.

Abstract: The present invention relates to a pharmaceutical aerosol formulation comprising a hydrofluoroalkane (HFA) propellant having suspended therein particulate (2S)-3-[4-({[4-(aminocarbonyl)-1-piperidinyl]carbonyl}oxy)phenyl]-2-[((2S)-4-methyl-2-{[2-(2-methylphenoxy)acetyl]amino}pentanoyl)amino] propanoic acid or a salt or solvate thereof. Methods and uses of the formulation in the treatment of respiratory disorders are also described, as are canisters and metered dose inhalers containing said formulation.

Abstract: The present invention relates to a dry powder pharmaceutical formulation suitable for inhalation therapy comprising particulate (2S)-3-[4-({[4-(aminocarbonyl)-1-piperidinyl]carbonyl}oxy)phenyl]-2-[((2S)-4-methyl-2-{[2-(2-methylphenoxy)acetyl]amino}pentanoyl)amino] propanoic acid or a salt or solvate thereof and one or more suitable excipients. Methods and uses of the formulation in the treatment of inflammatory diseases are also described, as are medicament packs and inhalation devices containing said formulation.