Abstract: Bicyclic heterocyclic substituted phenyl oxazolidinone compounds of the formula: wherein Y is a radical of Formulae II or III: in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.

Abstract: A regimen for the administration of tramadol for the treatment of analgesia is described. The regimen involves a slower initial titration rate of tramadol which results in a significantly lower percentage of discontinuations of therapy due to a lower incidence and severity of side effects.

Abstract: The invention is directed to benzoxazinone derivatives useful as peroxisome proliferator activated receptor gamma (PPAR&ggr;) modulators. Pharmaceutical compositions comprising compounds of the present invention and methods of treating conditions such as NIDDM and obesity are also disclosed.

Abstract: This invention relates to a series of arylsubstituted 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 and other disease.

Abstract: This invention is directed to a method for preventing or treating movement disorders comprising administering to a subject in need thereof a therapeutically effective amount of a compound selected from the group consisting of Formula (I) and Formula (II): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1, R2, R3, R4, R5 and R6 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: The invention relates to improved methods of producing aryl dioxoalkanoic acid compounds and derivatives useful as intermediates for diarylpyrrole therapeutic agents by the alcoholysis of benzoylcyclohexanone ketal compounds.

Abstract: The present invention includes compounds of the formula wherein: X is hydrogen or halide; R2 is hydrogen, acyl, or a hydroxy protecting group; R6 is hydrogen, hydroxyl, or —ORa wherein Ra is a substituted or unsubstituted moiety selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; R13 is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of methyl; C3-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heterocyclo, aryl(C1-C10)alkyl, aryl(C2-C10)alkenyl, aryl(C2-C10)alkynyl, heterocyclo(C1-C10)alkyl, heterocyclo(C2-C10)alkenyl, and heterocyclo(C2-C10)alkynyl; and, R is hydrogen or a substituted or unsubstituted moiety wherein the moiety is selected from the group consisting of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, aryl, heteroc

Abstract: A liquid composition for oral administration comprising a pharmaceutically active medicament coated with a taste masking effective amount of a polymer blend of (a) dimethylaminoethyl methacrylate and neutral methacrylic acid ester (MM/MAE) and (b) a cellulose ester, in an aqueous vehicle, wherein the polymer weight ratio of the cellulose ester to the MM/MAE is about 40:60 to about 90:10, preferably about 60:40. The liquid composition utilizes a “reverse enteric coating” which is soluble in the acid pH's of the stomach, generally about 1.0 to 4.0, but relatively insoluble at the non-acidic pH's of the mouth. The coatings provide for rapid release and absorption of the drug, which is generally desirable in the case of liquid dosage forms.

Abstract: This invention provides methods of treating a subject suffering from a leiomyoma which comprise administering to the subject a therapeutically effective amount of an agent, or alternatively a plurality of agents, which inhibit specific metalloproteinases. This invention further provides diagnostic methods of determining whether a tumor in a subject is a leiomyoma. This invention further provides pharmaceutical compositions and kits for practicing the instant methods. Finally, this invention provides a method of determining whether an agent specifically inhibits certain metalloproteinases.

Abstract: A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.

Abstract: The present invention is directed to a series of novel substituted aminoalkylamide derivatives, pharmaceutical compositions containing them and their use in the treatment of reproductive disorders and affective conditions. Further, the compounds of the invention are antagonists of follicle stimulating hormone, a hormone associated with the human reproductive system.

Abstract: The present invention is directed to novel 7-heterocyclyl quinoline and thieno[2,3-b]pyridine derivatives of the general formula (I) or (II) wherein all variables are as herein defined, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions associated with gonadotropin releasing hormone (GnRH). The compounds of the invention are antagonists of GnRH, useful in the treatment of the infertility, prostate cancer, benign prostate hyperplasia (BPH) and as contraceptives.

Abstract: A method for the treatment of an allergic condition, including an an atopic allergic conditions, using substituted pyrazoles.

Abstract: The invention relates to isoxazole and oxadiazole compounds of Formulae I and II, pharmaceutical compositions containing the compounds, and methods for their production and use. These compounds are effective in inhibiting the action of IL-8 and are thus useful as anti-inflammatory agents for a variety of diseases.

Abstract: This invention is directed to aroyl aminoacyl pyrroles pharmaceutically useful as agents and modulators for the treatment of central nervous system disorders and a method for the treatment of central nervous system disorders including, but not limited to, use of the compounds of the present invention as anticonvulsant agents and modulators, antiepileptic agents and modulators, neuroprotective agents and modulators, muscle relaxant agents and modulators and as agents and modulators for the treatment of neuropathic pain.

Abstract: This invention relates to novel dihydropyridine soft drugs of the formula &PHgr;OOR1, where &PHgr; is a dihydropyridine moiety. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibroncho-constriction activity. Use of such soft drug analogs permits the administration of greater doses of the claimed dihydropyridine compounds without intolerable systemic effects. Thus, this invention also provides pharmaceutical compositions, as well as methods, for preventing and treating disorders such as hypersensitivity, allergy, asthma, bronchospasim, dysmenorrhea, esophageal spasm, glaucoma, premature labor, urinary tract disorders, gastrointestinal motility disorders and cardiovascular disorders, while avoiding unwanted systemic effects.

Abstract: This invention provides novel substituted 3-pyridyl-4-arylpyrroles, and pharmaceutical compositions comprising same, useful for treating disorders ameliorated by reducing TNF-&agr; production and/or p38 activity in appropriate cells. This invention also provides therapeutic and prophylactic methods using the instant pharmaceutical compositions.

Abstract: This invention is directed to a method for preventing or treating bipolar disorder comprising administering to a subject in need thereof a therapeutically effective amount of a compound of Formula (I): wherein phenyl is substituted at X with one to five halogen atoms selected from the group consisting of fluorine, chlorine, bromine and iodine; and, R1 and R2 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; wherein C1-C4 alkyl is optionally substituted with phenyl (wherein phenyl is optionally substituted with substituents independently selected from the group consisting of halogen, C1-C4 alkyl, C1-C4 alkoxy, amino, nitro and cyano).

Abstract: This invention relates to a pharmaceutical composition comprising a combination of a tramadol material and an anticonvulsant drug and to the pharmacological use of the composition in treating conditions of pain and neurologic or psychiatric disorders. The composition produces a combination product having improved properties, requiring less of each ingredient and producing a synergistic effect.

Abstract: The present invention provides compounds of the formula: wherein m is 0, 1 or 2; p is 0 or 1; Y is O, S, S(O) or S(O)2 and R1 to R7 are various substituents as selective modulators of the nicotinic acetylcholine receptor useful in the treatment of pain, Alzheimer's disease, memory loss or dementia or loss of motor function.