Abstract: There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

Abstract: This invention relates to 2,3(1H,4H)-quinoxalinedione derivatives which are selective antagonists of N-methyl-D-aspartate receptors. More particularly, this invention relates to 5-triazolyl-2,3(1H,4H)-quinoxalinedione derivatives and to the preparation of, compositions containing, and the uses of, such derivatives. It also relates to a method for treating acute neurodegeneration disorders and chronic neurological disorders.

Abstract: A compound of the formula wherein R1, R2 R3, R4 R5, R6, R7, R8, R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer.

Abstract: This invention relates to immunogenic compositions capable of potentiality growth hormone activity, comprising an immunologically effective amount of a composite peptide comprising at least two non-contiguous somatotropin epitope amino acid sequences, wherein said composite peptide is substantially free of receptor binding domain sequences; and an immunologically acceptable excipient. The invention further relates to methods of using an immunogenic composition of the invention to potentiate the action of growth hormone in pigs.

Abstract: Known bisamidine compounds are newly discovered to possess DNA methyltransferase inhibiting properties, making them useful for preparing pharmaceutical compositions useful as antiproliferative agents for treating a neoplastic or a non-neoplastic disease characterized by abnormally rapid proliferation of tissue involved in said disease; wherein said bisamidines comprise a compound of Formula (5.0.0): and a pharmaceutically acceptable salt thereof, wherein: —X is —C(R34)—; or —N—; —R23, R24, R28 and R29 are each independently —H; or —CH2— where R23 and R24 and R28 and R29 are taken together with the nitrogen atoms to which they are attached, to form an imidazolinyl group; and —R34 is —H; or —CH3. A preferred species of Formula (5.0.0) is the following: 2-(4-Carbamimidoyl-phenyl)-1H-indole-6-carboxamidine.

Abstract: Optically pure thiazolidinedione alcohols and ethers, and synthetic intermediates for preparing said alcohols and ethers. These compounds have utility as hypoglycemic and hypocholesterolemic agents.

Abstract: The invention provides a substituted benzylaminopiperidine compounds that are useful in the treatment of gastrointestinal disorders; central nervous system (CNS) disorders; inflammatory disease; emesis; urinary incontinence; pain; migraine; sunburn; diseases, disorders and adverse conditions caused by Heliobacter pylori; or angiogenesis, especially CNS disorders in a mammalian subject, especially in humans.

Abstract: The invention relates to a method of preparing compounds of the formula 1 and to pharmaceutically acceptable salts thereof. The compounds of formula 1 are antibacterial agents that may be used to treat various bacterial and protozoa infections. The invention also relates to pharmaceutical compositions containing the compounds of formula 1 and to methods of treating bacterial protozoa infections by administering the compounds of formula 1. The invention also relates to methods of preparing the compounds of formula 1 and to intermediates useful in such preparation.

Abstract: A method and device for the automated large scale preparation for testing of drug-drug interactions, particularly with determination of IC50 and Ki, as a screening tool enhancement for determining viability of large numbers of compounds as drug candidates. Small samples of specific probe substrates and new compound inhibitors are automatically dispensed en masse into multi-welled reaction plates which are prefilled with thawed human microsomes, buffer and cofactor. The reaction plates are incubated and the reaction products are tested within degradation time limits, for initial biological determinations of relevant interaction effects of the compounds.

Abstract: The present invention provides compounds of formula (I): and pharmaceutically acceptable salts and solvates thereof, together with processes for the preparation of, compositions containing, uses of and intermediates used in the preparation of such compounds that have A2a receptor agonist activity.

Abstract: The present invention provides novel compounds of the Formula and prodrugs thereof, geometric and optical isomers thereof, and pharmaceutically acceptable salts of such compounds, prodrugs and isomers, wherein R1-R8 and W are as described herein. Pharmaceutical compositions containing such compounds, prodrugs, isomers or pharmaceutically acceptable salts thereof, and methods, pharmaceutical compositions and kits for treating obesity, hyperlipidemia, glaucoma, cardiac arrhythmia, skin disorders, thyroid disease, hypothyroidism and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, hypercholesteremia, depression and osteoporosis are also provided.

Abstract: The invention concerns a method of preparing an 8-cyclopentyl-6-ethyl-3-[substituted]-5,8-dihydro-4H-1,2,3a,7,8-pentaaza-as-indacene compound of the formula: and pharmaceutically acceptable salt forms thereof, where R1 is hydrogen; alkyl; alkoxy; alkoxyalkyl; alkenyl; cycloalkyl; cycloalkylalkyl; a saturated or unsaturated heterocyclic-(CH2)n—group; or a group of the formula —(Y)b—(Z)c-phenyl-(R5)a; comprising: (a) subjecting a solventless reaction mixture of &ggr;-caprolactone and p-methoxybenzylamine to heating whereby there is produced an amide compound N-protected by p-methoxybenzyl; (b) reducing said amide compound whereby there is produced an amino alcohol compound N-protected by p-methoxybenzyl; (c) acylating said aminoalcohol compound with ethyl oxalyl chloride whereby there is produced an oxalamic acid ethyl ester compound N-protected by p-methoxybenzyl; (d) oxidizing said oxalamic acid ethyl ester compound whereby there is produced an oxalamide ketone co

Abstract: The present invention relates to novel atropisomers of 2,3-disubstituted-(5,6)-heteroarylfused-pyrimidin-4-ones, pharmaceutical compositions containing such compounds the use of such compounds to treat neurodegenerative, psychotropic, and drug and alcohol induced central and peripheral nervous system disorders.

Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (−)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.

Abstract: Pharmaceutical combination compositions including certain estrogen agonists/antagonists and prostaglandins or prostaglandin agonists/antagonists. The compositions are useful for the treatment of bone disorders including osteoporosis.

Abstract: This invention relates to novel nucleic acid sequences encoding three novel human phosphodiesterase (hPDE IV) isozymes. It also relates to polypeptides encoded by such sequences. This invention also relates to an assay method for detecting the presence of such novel isozymes in human cells, and to a method of identifying compounds or other substances that inhibit or modify the activity of such isozymes.

Abstract: A compound of the formula wherein m, R1, R2, R3, R4, R5 and X are as defined, useful in treating or preventing migraine, depression and other disorders for which a 5-HT1 agonist or antagonist is indicated.

Abstract: A method of treating hyperproliferation diseases in mammals in need of such treatment which method includes administering to said mammal a therapeutically effective amount of a compound of the formula: or a pharmaceutically acceptable salt, hydrate or prodrug thereof, wherein R1, R2, R3, R4, W, X, Y, Z and t are as defined herein.

Abstract: This invention relates to a process for converting 2,4-dichloropyridines into 2-aryloxy-4-chloropyridines, comprising reacting a compound of formula (I), wherein R1 is (C1-C4)alkyl; R2 is methyl or ethyl; and R3, R4 and R5 are selected, independently, from (C1-C4)alkyl and (C1-C4)alkoxy; or a pharmaceutically acceptable salt thereof; comprising reacting a compound of formula (II), wherein R1 and R2 are defined as above, with a compound of formula (III), wherein R3, R4 and R5 are defined as above, in the presence of a base that is capable of deprotonating the compound of formula (III), optionally in the presence of an organometallic halide or oxide and a suitable solvent, and then optionally converting the resulting compound of formula (I) into a pharmaceutically acceptable salt of such compound.

Abstract: A process for preparing 2-phenyl-3-aminopyridine, and substituted phenyl derivatives and salts thereof.