Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention relates to certain pyrazole derivatives of Formula (I): that are p-38 MAP kinase inhibitors, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.

Abstract: A trellis wire support apparatus and a trellis system and method for use in vineyards and the like. The trellis wire support comprises a body having at least one a fold configured to releasibly engage a corresponding slot in a support element, and at least one clip or hook configured to releasibly engage a trellis wire. The trellis systems comprise at least one support element having a slot therein, and at least one trellis wire support comprising at least one clip configured to releasibly engage a trellis wire and a fold configured to releasibly engage the slot in the support element. The trellis system may additionally comprise a cross arm, with the support element configured to couple to the cross arm. The cross arm may include parallel ridges extending along its length, and the support element may have notches adjacent each end thereof that are configured to engage the ridges on the cross arm.

Abstract: The invention provides compounds of the formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein m, p, q, r, A, E, X, Y, R1, R4, R5, R6, R7, R8, R9 and are as defined herein. The invention also provides methods for preparing, compositions comprising, and methods for using compounds of formula I.

Abstract: This invention relates to compounds which are generally IP receptor antagonists and which are represented by Formula I: wherein G1 is selected from the group consisting of a, b1 and b2, and A and G2 are as defined in the specification; or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: This invention relates to compounds which are generally EP4 receptor agonists and which are represented by Formula I: wherein A is a —CH2—CH2—, or —CH?CH—; B is absent, an aryl, or heteroaryl group; R1 is alkyl, alkenyl, alkynyl, cycloalkylalkyl, heterocyclylalkyl, aryl, arylalkyl or heteroaryl, when B is aryl or heteroaryl and R3, R4, R5 and R6 are not simultaneously hydrogen, or R1 is heterocyclylalkyl, aryl, or heteroaryl when B is absent and R3, R4, R5 and R6 are simultaneously hydrogen; and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: Compounds of the formula: or pharmaceutically acceptable salts or prodrugs thereof, where each of n and p independently is 2 or 3, Y is —SO2— or —SO2—N(R10)—, Z1 is CH or N, and R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are as defined herein. The compounds have selective 5-HT6 affinity and are useful in the treatment of certain CNS disorders. Also provided are compositions comprising, methods for using, and methods for preparing Compounds of Formula I.

Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein X is —S(O)n— or —C(O)—, A is C1-6alkyl, aryl, heteroaryl, hydroxyalkyl, or —(CH2)p—NRaRb, and the other substituents are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: This invention relates to 8-aza prostanoid analogs which are generally EP4 receptor agonists and are represented by Formula I: wherein Q, B, X, J, Z, A and R1-R6 are as defined, their synthesis and use for treatment of osteoporosis and increasing bone density.

Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula (I): wherein Ar, R1, R2, R3 or R4 are as defined in the specification, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein R3 is SO2—Ar, Ar is aryl or heteroaryl; and R1, R2, R4 and R5 are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: This invention relates to certain sulfonamide derivatives that are inhibitors of procollagen C-proteinase, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.

Abstract: This invention relates to compounds which have generally 5-HT6 receptor affinity and which are represented by Formula I: wherein one of R5, R6 or R7 is a group of general Formula B, wherein W is a —CH— group or a nitrogen atom, and the other substituents are as defined herein; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention provides a compound of the formula: a pharmaceutically acceptable salt or a prodrug thereof, where R1, R2, R3, R4, R5, R6, and n are as defined herein. The present invention also provides compositions comprising, methods for using, and methods for preparing Compound of Formula I.

Abstract: Compounds of the formula (I) wherein m, n, R1, R2, R3, R4, R5 and R6 are as described herein, together with methods for making the compounds and using the compounds for treatment of diseases or conditions mediated by Cathepsin K.

Abstract: Compounds of the Formula: where R1-R6 are those defined herein and methods for producing the same. Also provided are pharmaceutical compositions comprising a Compound of Formula I and methods for their use as therapeutic agents.

Abstract: The present invention relates to compound of formula (I) wherein R1, R2, R3, R4, R5 and n are as defined in the description and claims and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are useful for the treatment of diseases which are associated with cysteine proteases such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Abstract: A method for identifying compounds that can be useful for producing analgesia is disclosed. In particular, the method involves providing preparation of a cell, that expresses an alpha1B adrenergic receptor, combining a test compound with the cell preparation, measuring the effect of the test compound on the alpha1B receptor activity, and evaluating the compound thus identified for analgesic activity.

Abstract: The present invention provides compounds of the Formula I and II: wherein R1, R3, W, Z, X1, X2, Ar1, R8 and R9 are as defined herein, and methods and intermediates for their preparation and uses thereof.