Abstract: This invention relates to a compound of the formula: or a pharmaceutically acceptable salt thereof, wherein A and R1 are each an optionally substituted 5 to 6-membered heteroaryl, wherein the heteroaryl is optionally fused to a carbocyclic ring or 5 to 6-heteroaryl; R2 is (C1-C4)alkyl optionally substituted with halo, amino or an alkyl amino; R3 and R4 are each hydrogen, halo, (C1-C4)alkyl optionally substituted with halo and the like; and X1 to X4 are each hydrogen, halo, hydroxy, (C1-C4)alkyl optionally substituted with halo and the like. These compounds have COX-2 inhibiting activity and thus useful for treating or preventing inflammation or other COX-2 related diseases.

Abstract: A process for preparing a 1,4-dihydropyridine compound comprising contacting an enamine compound and a compound having a structure of in the presence of a base; and treating the reaction mixture thus obtained in the presence of an acid or a combination of acids under mild reaction conditions. A resulting 1,4-dihydropyridine compound is useful as an anti-inflammatory agent or the like.

Abstract: A compound of the formula or the pharmaceutically acceptable salt thereof; wherein a, b, c, d, e, j, R1, R2, R3, and R4 are as defined herein and are useful to treat inflammation and other immune disorders.

Abstract: This invention relates to certain indole-2-carboxamides of formula (I) and the pharmaceutically acceptable salts and prodrugs thereof, wherein R6 is carboxy, (C1-C8)alkoxycarbonyl, C(O)NR8R9 or C(O)R12, useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds.

Abstract: This application is directed to compounds useful as inhibitors at PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, or 2; n is 1 or 2; W1 is —O—; or —S(═O)t—, where t is 0, 1, or 2; Y is —C(R1a); Q1 is phenyl or substituted phenyl; Q2 is biphenyl or substituted biphenyl; and the remaining variables are defined as set forth in the specification. This application is also directed to pharmaceutical compositions comprising those compounds and to methods of treating diseases regulated by the activation and degranulation of eosinophils, in particular asthma, chronic bronchitis and chronic obstructive pulmonary disease.

Abstract: Compounds of formula I, wherein R1 represents C1-4 alkoxy optionally substituted by one or more fluorine atoms; R2 represents an aryl group or a heteroaryl group, optionally substituted by C1-4 alkyl or SO2NH2; R3 represents a 4-, 5-, 6-, or 7-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring being optionally fused to a benzene ring or a 5- or 6-membered heterocyclic ring containing at least one heteroatom selected from N, O and S, the ring system as a whole being optionally substituted; X represents CH or N; and L is absent, or represents a cyclic group of formula Ia,  or represents a chain of formula Ib,  and pharmaceutically acceptable salts thereof, are useful in the treatment of a variety of disorders including benign prostatic hyperplasia.

Abstract: Compounds of the formula are neuropeptide Y antagonists and are effective in treating feeding disorders, cardiovascular diseases and other physiological disorders related to an excess of neuropeptide Y.

Abstract: The invention relates to crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate salts having the formula shown below: 1

Abstract: A compound of the formula 1

Abstract: This invention relates to methods of treating or preventing type 2 diabetes, diabetic neuropathy, diabetic cardiomyopathy, cataracts, diabetic retinopathy, foot ulcers, diabetic microangiopathy, diabetic macroangiopathy, diabetic ischemia reperfusion injury, diabetic cardiac ischemia reperfusion injury and/or insulin resistance syndrome (IRS) in mammals, particularly in humans, by administering a sodium-hydrogen exchanger type 1 (NHE-1) inhibitor or a pharmaceutical composition containing such an inhibitor. This invention also relates to combinations comprising NHE-1 inhibitors and a second pharmaceutical agent, said combinations being useful in treating type 2 diabetes, IRS, diabetic neuropathy, diabetic cardiomyopathy, cataracts, diabetic retinopathy, foot ulcers, diabetic ischemia reperfusion injury, diabetic cardiac ischemia reperfusion injury, diabetic microangiopathy and/or diabetic macroangiopathy.

Abstract: Treating or preventing inflammatory processes and diseases in dogs associated with the activity of inducible cyclo-oxygenase-2 (COX-2), while at the same time reducing or eliminating undesirable side effects associated with simultaneous inhibition of the activity of constitutive cyclo-oxygenase-1 (COX-1) by selectively inhibiting COX-2 activity with reference to COX-1 activity, wherein the selectivity ratio or COX-2:COX-1 activity inhibition is at least 3:1 based on ex vivo inhibition levels measured in whole blood; the inhibitor is a member selected from the group of anti-inflammatory compounds consisting essentially of salicylic acid derivatives, p-aminophenol derivatives, indole and indene acetic acids, heteroaryl acetic acids, arylpropionic acids, anthranilic acids, enolic acids, and alkanones; the inhibitor in particular is comprised of (+)(S)-enantiomer of 6-chloro-&agr;-methyl-9H-carbazole-2-acetic acid.

Abstract: This invention relates to a novel improved three-item screener which is a valid and reliable screening instrument for migraine headaches. Its ease of use and operating characteristics suggest that it could significantly improve migraine recognition in primary care.

Abstract: The present invention provides methods of determining the proper dosage of Compound 122 (and other drugs that are metabolized by cytochrome P450 2D6) to be given to a patient. Also provided are methods of determining the metabolizer status of persons, devices for performing the invention methods, and antibodies for use in these devices and methods.

Abstract: The present invention provides &bgr;3-adrenergic receptor agonists of structural Formula (I) as well as pharmaceutical formulations thereof and methods for treating &bgr;3-adrenergic receptor-mediated diseases, conditions, or disorders using such compounds.

Abstract: The present invention is directed to a process for the preparation of the mesylate trihydrate of the (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol compound having the formula (I): The present invention is also further comprises a process for enantiomeric resolution and isolation of the (D)-(−)-tartrate salt of the compound of the formula (I).

Abstract: The invention relates to crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate salts having the formula shown below: and to pharmaceutical compositions containing the above compound, methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above compound, and to methods of preparing the crystal forms of the above compound and related compounds.

Abstract: The invention described herein relates to a process for the preparation of (7-(3-carboxyphenyl)-4-chloroisoquinolin-1-yl)guanidine (I), intermediates thereto and new forms and formulations thereof, including the zwitterion monohydrate of (I), suitable for pharmaceutical use.

Abstract: The invention relates to processes for preparing compounds of formula 1: as well as intermediates useful in such processes, wherein R1-R4 are as defined herein. The compounds of formula 1 are useful in the treatment or alleviation of inflammation and other inflammation associated disorders.

Abstract: This invention provides a compound of the formula: 1

Abstract: This invention relates to a series of substituted aromatic ethers of the formula I 1