Abstract: Compounds of the formula I are suitable for preparing pharmaceuticals for the prophylaxis and therapy of disorders in whose course an increased activity of NF?B is involved.

Abstract: The present invention relates to indole derivatives or benzimidazole derivatives, to processes for preparing such compounds, to pharmaceutical compositions comprising such compounds, and methods for the prophylaxis and therapy of a disease associated with an increased activity of I?B kinase comprising administering such compounds.

Abstract: The use of NIPAM polymers to prevent or reduce the formation of protein deposits on the surfaces of medical devices is described. The invention is particularly directed to reduction of the adsorption of proteins on surfaces of contact lenses and other medical prosthetics.

Abstract: This invention relates to nitrogenous (tetrahydropyridyl)(alkyl)heterocycles, to pharmaceutical compositions comprising them, to processes for preparing them and to the method of use thereof in the treatment of pain and diseases related to immune and inflammatory disorders.

Abstract: The present invention is directed to the compound of formula I which is useful for inhibiting the activity of Factor Xa. The present invention is also directed to compositions containing said compounds, processes for their preparation, their use, such as for inhibiting the formation of thrombin or for therapeutically or prophylactically treating a patient suffering from, or subject to, or associated with a disease state associated with a cardiovascular disorder.

Abstract: The present invention relates to acylated arylcycloalkylamines, to pharmaceutical compositions comprising such compounds, to methods for the stimulation of the expression of endothelial NO synthase, and methods of treatment comprising administering such compounds.

Abstract: The present invention is directed C2-disubstituted indan-1-ones of the Formula I, physiologically acceptable salts, and physiologically functional derivatives thereof, and pharmaceutical compositions comprising such compounds, salts and derivatives, which are useful for reducing weight, for the prophylaxis or treatment of obesity, and for the prophylaxis or treatment of type II diabetes in mammals. The invention is directed also to methods for reducing weight and such treatments and prophylaxis. The invention is directed also to processes for the preparation of such compounds.

Abstract: The present invention relates to compounds of general formula (I), wherein R1-R4 have the meanings given in the specification, A is CH2, CHOH or CH—(C1-C3-alkyl), B and C are independently CH2 or CH—(C1-C3-alkyl), and R5 is an aryl or heteroaryl group optionally substituted by the substituents listed in the specification.

Abstract: The present invention relates to certain novel 1-carboxymethyl-2-oxo-azepan derivatives of the formula useful as inhibitors of matrix metalloproteinases (MMPs). The compounds of formula (1) are especially useful as selective inhibitors of MMP-12. Pharmaceutical compositions containing said compounds as well as methods of treating various disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

Abstract: The invention is related to compounds of formula I to pharmaceutical compositions comprising such compounds, to processes for the preparation of such compounds, and to methods of prevention and treatment of disorders, the progression of which involve an enhanced activity of matrix metalloproteinase 13, by administering to a patient in need thereof, a pharmaceutically effective amount of such compounds.

Abstract: The present invention provides a method of inhibiting matrix metallo-proteinases (MMPs) in a patient in need thereof comprising administering to the patient an effective matrix metalloproteinase inhibiting amount of the N-carboxymethyl substituted benzolactams of formula (1): wherein A is —OH or —NRR′. Such inhibitors are useful in treating neoplasms, atherosclorosis, and chronic inflammatory diseases. The present invention also provides novel N-carboxymethyl substituted benzolactams of formula (1a): wherein A is —NRR′.

Abstract: The present invention provides novel 3-substituted pyrrolidines of the formula useful in as inhibitors of matrix metallo-proteinases (MMPs). Pharmaceutical compositions containing said compounds as well as methods of treating disease states responding to inhibition of matrix metalloproteinase are also claimed herein.

Abstract: The present invention relates to novel 4-(1H-benzimidazol-2-yl)[1,4]diazepane derivatives of formula (1): and stereoisomers thereof, and pharmaceutically acceptable salts thereof which are useful as histamine receptor antagonists and tachykinin receptor antagonist. Such antagonists are useful in the treatment of allergic rhinitis, including seasonal rhinitis and sinusitis; inflammatory bowel diseases, including Crohn's disease and ulcerative colitis; asthma; bronchitis; and emesis.

Abstract: A process for preparing the compound (11&bgr;,16&bgr;)-21-(3-CARBOXY-1-OXOPROPOXY)-11-HYDROXY-2′-METHYL-5′H-PREGNA-1,4-DIENO(17,16-D) OXAZOLE-3,20-DIONE which comprises reacting the compound (11&bgr;,16&bgr;)-11,21-DIHYDROXY-2′-METHYL-5′H-PREGNA-1, 4-DIENO(17,16-D)OXAZOLE-3,20-DIONE with succinic anhydride in a (C1-C4) alkyl ester of a (C1-C4) carboxylic acid as solvent, in the presence of a basic catalyst.

Abstract: The present invention provides novel mercaptoacetylamido dipeptide carboxylic acids of the formula which are MMP inhibitors useful for the treatment of smoking-induced emphysema.

Abstract: The present application relates to novel aminomalonamides of the formula and pharmaceutical composition thereof which are useful for inhibiting matrix metalloproteinases.