Abstract: The present invention relates to the use of quinolone carboxylic acid formulations in the treatment of ocular and periocular infections. The present invention also relates to sustained release compositions comprising specific quinolone carboxylic acid compounds. The invention also relates to quinolone carboxylic acid compositions and methods of preparing the same.

Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: wherein R3, R4, R5, W, and A are as set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. The compounds of the invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, thrombin, plasmin and factor Xa. Certain of the compounds exhibit antithrombotic activity via direct, selective inhibition of thrombin. Compositions for inhibiting loss of blood platelets, inhibiting formation of blood platelet aggregates, inhibiting formation of fibrin, inhibiting thrombus formation, and inhibiting embolus formation are described.

Abstract: Compounds of formula I wherein W is optionally substituted alkylene; Y is N or CRa; Ra is hydrogen, halogen or alkyl; R1n represents hydrogen or 1 to 4 substituents; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is optionally substituted alkyl, cycloalkyl, aryl or hetaryl; A is N—OR4, CH—OR4, CH—SR4 or CHR5; R4 is alkyl or haloalkyl; R5 is halogen, alkyl or haloalkyl; methods and intermediates for their preparation. The compounds and compositions comprising them are useful for combating animal pests and harmful fungi.

Abstract: The present invention is substituted amines of formula (X) 1

Abstract: Novel hydroxamic acid compounds are disclosed. These hydroxamates inhibit peptide deformylase (PDF), an enzyme present in prokaryotes and are therefore useful as antimicrobials and antibiotics. Methods of synthesis and of use of the compounds are also disclosed.

Abstract: The invention relates to new hydroxyindoles of the Formula, 1

Abstract: The invention relates to dihydropyrimidines of the general formula and to the use of dihydropyrimidines as medicaments for the treatment and prophylaxis of hepatitis B. The invention further relates to a process for the preparation of medicaments comprising the corresponding dihydropyrimidines.

Abstract: The invention provides the use in combating fungi of compounds of general formula (I) wherein R1 is hydrogen, hydroxy, acyl, acyloxy, optionally substituted amino, Ra, Ra3Si, RaS or RaO, where Ra is optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted cycloalkyl, optionally substituted cycloalkenyl, optionally substituted aryl or optionally substituted heterocyclyl; R2 has the same meaning as Ra or can be hydrogen; Z is oxygen or sulfur, M is a thiophene ring, and R3 and R4, which may be the same or different, have the same meaning as Ra or can be optionally substituted amino, hydrogen, halogen, cyano, nitro or a group ORc or S(O)mRc, where Rc has the same meaning as Ra or is hydrogen or acyl and m is 0, 1 or 2; or R3 and R4 together with the atoms to which they are attached form an optionally substituted carbocyclic or heterocyclic ring; together with tautomers of compounds where R1 is hydrogen.

Abstract: There is provided a pharmaceutical composition suitable for topical administration to an eye, the composition comprising as active agent at least one oxazolidinone antibacterial drug, for example linezolid, in a concentration effective for treatment and/or prophylaxis of a gram-positive bacterial infection of an eye, and at least one ophthalmically acceptable excipient ingredient that reduces a rate of removal of the composition from the eye by lacrimation such that the composition has an effective residence time in the eye of about 2 to about 24 hours. The composition is, for example, an in situ gellable solution, suspension or solution/suspension.

Abstract: The present invention relates to cyclized amide derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: Pyrimidone compounds of formula (I): 1

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian factor Xa are disclosed. The compounds are useful in vitro or in vivo for preventing or treating coagulation disorders.

Abstract: The present invention relates to a class of compounds represented by the Formula I 1

Abstract: This invention relates a to a series of heterocyclic substituted piperazines of Formula I pharmaceutical compositions containing them and intermediates used in their manufacture. The compounds of the invention selectively inhibit binding to the &agr;-1a adrenergic receptor, a receptor which has been implicated in benign prostatic hyperplasia. As such the compounds are potentially useful in the treatment of this disease.

Abstract: This invention relates to urea compounds that are muscarinic receptor antagonists and agonists, pharmaceutical compositions comprising such compounds, and methods of preparing these compounds.

Abstract: The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.

Abstract: Disclosed are methods of treating rheumatoid arthritis by coadministering synergistic effective amounts of pentostatin and methotrexate to a host in need thereof, and kits and compositions that include pentostatin and methotrexate.

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

Abstract: A method of promoting neuronal survival and helping prevent neuronal death administers (di-substituted-phenyl) pyrimidinyl imidazole derivative compounds represented by 1

Abstract: The present invention is substituted amines of formula (XV) 1

Abstract: The present invention is directed to substituted 1,4-thiazepine and analogs thereof, represented by the general Formula I: 1

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present application relates to novel acylated 4-amino-pyridine derivatives in which R1, R2, R3, R4, A, X1, X2, m and n are as defined in the description, to process for their separation and to their use for controlling animal pests and as fungicides.

Abstract: One aspect of the present invention relates to novel heterocyclic compounds comprising urea functionality. A second aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as ligands for various cellular receptors, including opioid receptors, other G-protein-coupled receptors and ion channels. An additional aspect of the present invention relates to the use of the novel heterocyclic compounds comprising urea functionality as analgesics.

Abstract: The present invention provides a compound of formula I 1

Abstract: The present invention relates to a novel pyrimidinone compounds and the pharmaceutical acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, thereby, being useful in treating cardiovascular disease caused by binding angiotensin II to its receptor.

Abstract: Compounds of the formula (I): where X1, A, Ar1, X and R are as defined in the specification, and pharmaceutically-acceptable salts thereof, are new, and are useful as tachykinin inhibitors which act at the NK1, NK2 and NK3 receptors or a combination of two or more thereof.