Abstract: This invention relates to pharmaceutical compositions and methods for treating a vision disorder, improving vision, treating memory impairment, or enhancing memory performance using heterocyclic thioesters and ketones.

Abstract: Cyclic oxyguanidine pyrazinone compounds are described, including compounds of the Formula I: 1

Abstract: A condensed thiophene compound of the formula (I) 1

Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.

Abstract: This invention relates to compositions comprising thalidomide and another anti-cancer drug which can be used in the treatment or prevention of cancer. Preferred anti-cancer drugs are topoisomerase inhibitors. A particular composition comprises thalidomide, or a pharmaceutically acceptable salt, solvate, or clathrate thereof, and irinotecan. The invention also relates to methods of treating or preventing cancer which comprise the administration of a thalidomide and another anti-cancer drug to a patient in need of such treatment or prevention. The invention further relates to methods of reducing or avoiding adverse side effects associated with the administration of chemotherapy or radiation therapy which comprise the administration of thalidomide to a patient in need of such reduction or avoidance.

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 composition having antibacterial activity is disclosed. More particularly, a mixture of an oxazolidinone compound, sulbactam, and ampicillin active agents, demonstrating activity against resistant strains of bacteria is disclosed. Methods for using an oxazolidinone compound, sulbactam, and ampicillin to treat a bacterial infection are also described.

Abstract: Cyclic oxyguanidine compounds, including compounds of Formulae I and II: 1

Abstract: Novel pharmaceutical formulations for treating a cellular proliferative disease are provided comprising: a therapeutically effective amount of a Golgi apparatus disturbing agent; a biocompatible carrier; and a solvent. In preferred formulations, the Golgi apparatus disturbing agent is brefeldin A (BFA) and the biocompatible carrier is a polymer such as chitin or chitosan. Methods of treating cellular proliferative diseases using the pharmaceutical formulations are also described.

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: This invention provides novel compounds and methods and compositions using them in the treatment of central nervous system disorders, including depression and anxiety, the compounds having the formula: wherein Ar is an aryl group of 4 to 10 carbon atoms or a heteraryl group of 4 to 10 carbon atoms; R1 and R2 are independently selected from hydrogen, straight chain alkyl of 1 to 12 carbon atoms, branched alkyls of 3 to 10 carbon atoms or cycloalkyl of 3 to 10 carbon atoms; R3 is H, straight chain, branched or cyclic alkyl, halogen, alkoxy, haloalkyl, OH, nitro, nitrile, amino, CN, carboxy, alkoxycarbonyl, alkylcarbonyl, aminocarbonyl and alkylaminocarbonyl; or a pharmaceutically acceptable salt thereof.

Abstract: Disclosed are methods and kits for treating lymphoproliferative diseases in a host including (co)administering to the host pentostatin, at least one alkylating agent and at least one methylated xanthine.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formulas 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: A method for treating neoplasms is disclosed, particularly using the &bgr;-isozyme selective PKC inhibitor, (S)-3,4-[N, N′-1,1′-((2″-ethoxy)-3′″(O)-4′″-(N,N-dimethylamino)-butane)-bis-(3,3′-indolyl)]-1(H)-pyrrole-2,5-dione or one of its salts, such PKC inhibitors enhance the clinical efficacy of oncolytic agents and radiation therapy.

Abstract: The present invention provides compounds of the general formula: as well as methods and pharmaceutical compositions utilizing these compounds for the inducement of temporary delay of urination or the treatment of disorders which may be remedied or alleviated by vasopressin agonist activity, including diabetes insipidus, nocturnal enuresis, nocturia, urinary incontinence, bleeding and coagulation disorders.

Abstract: A biphenyl derivative represented by the following general formula (1) and a pharmaceutically acceptable salt thereof: [In the formula (1), A represents a single bond, —CH2—, —CO—, —CS— or —SO2—; B represents a single bond or —CH2—; R1 represents a hydrogen atom, —OH, —NR11R12 (wherein R11 and R12 each independently represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms), —OCOCH3, or a halogen atom; R2 represents a hydrogen atom or R1 and R2 form a group ═O together; R3 represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; provided that in the formula, the absolute configuration of the position a may be either R or S]. The compound of the present invention has considerably high safety and efficacy and is useful as, in particular, a vasopressin receptor antagonist.

Abstract: 4-Aryl-1-(indanmethyl, dihydrobenzofuramethyl or dihydrobenzothiophenemethyl) piperidine, -tetrahydropyridine or -piperazine compounds of general formula (I) wherein one of X and Y is CH2, and the other one is CH2, O or S; Z is N, C, CH or COH; Ar is an optionally substituted aryl group; R1 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, aryl, arylalkyl, acyl, thioacyl, alkylsulfonyl, trifluoromethylsulfonyl, arylsulfonyl, a group R9VCO— where V is O or S and R9 is alkyl or aryl, or a group R10R11NCO— or R10R11NCS— wherein R10 and R11 are hydrogen, alkyl or aryl, or R10 and R11 are linked to form a ring; R2 is hydrogen, alkyl, cycloalkyl or cycloalkylalkyl; or R1 and R2 are linked to form a ring; R3-R5 are hydrogen, halogen, alkyl, alkylcarbonyl, phenylcarbonyl, alkoxy, alkylthio, hydroxy, alkylsulfonyl, cyano, trifluoromethyl, cycloalkyl, cycloalkylalkyl or nitro; R6 and R7 are hydrogen or alkyl or they are linked to constitute a 3-7-membered ring; R8 is hydrogen or alkyl

Abstract: The invention provides a method for treating or preventing ocular neovascularization. The method administers an effective amount of a staurosporine derivative to treat or prevent retinal or choroidal neovascularization. In each case, the effect on the pathologic blood vessels is dramatic and profound with complete or near-complete inhibition, but there is no identifiable toxic effect on mature retinal vessels.

Abstract: When administered locally, tricyclic, second generation and third generation antidepressants, such as amitriptyline and desipramine, have been shown to produce analgesia in a subject having a site of local discomfort. The analgesic effect of such antidepressants, when administered locally is equal to that achieved by systemic administration and lasts longer. The invention provides compositions containing tricyclic, second generation, and third generation antidepressants for local administration, such as those formulated for topical application, or for injection in slow release delivery vehicles, and methods for their use for producing local analgesia.