Abstract: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5?-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Abstract: The present invention discloses the identification of the novel inhibitors of IMPDH (inosine-5?-monophosphate dehydrogenase). The compounds and pharmaceutical compositions disclosed herein are useful in treating or preventing IMPDH associated disorders, such as transplant rejection and autoimmune diseases.

Abstract: Quinazoline and pyrido[2,3-d]pyrimidine phosphodiesterase 7 (PDE 7) inhibitors of the following formula wherein R1, R2, L, Y1, Y2, Y3 and Z are as described herein, are provided which are useful in treating T-cell mediated diseases.

Abstract: The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest.

Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where Z is CONR1R2 or CH2NR1R2 and where R, Ra, Rb, Rc, Rd, Z, A and B are defined herein.

Abstract: Multiple samples are prepared in slurry form and deposited through a funnel plate by a multiprobe liquid handler into an array of inserts situated in openings in a housing. Each insert has a recess that extends through the insert body and a filter disc situated in the recess to support the sample. The filter is held in place by an annular part which defines a channel providing access to the filter through the lower portion of the recess. A pressure differential is created across each of the filters by attaching a vacuum manifold to the bottom of the housing to simultaneously remove the liquid from each of the samples, leaving the samples in powder form. The housing is then placed in the X-ray diffractometer for sequential analysis of each of the samples, while the samples are situated in the inserts.

Abstract: A process for the production of tertiary amines by reductive amination of carbonyl compounds with secondary amines in the presence of a water scavenger, preferably trifluoroacetic acid anhydride, is disclosed. This process has applications in the preparation of imidazole-containing benzodiazepines, which are inhibitors of farnesyl protein transferase.

Abstract: Compounds of the formula wherein X1 is C(O), —S(O)—, or —S(O)2—; X2 is CR3 or N; X3 is —NH—, —O—, or —S—; X4 is CR4 or N; X5 is CR5 or N; and X6 is CR6 or N are useful as inhibitors of IMPDH enzyme. Thus, these compounds can be used as therapeutic agents for IMPDH-associated disorders.

Abstract: Compounds having the formula (I), and pharmaceutically acceptable salts thereof, are useful for modulating mitochondrial F1F0 ATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.

Abstract: Provided are processes and synthetic intermediates useful for the preparation of azaindole piperazine diamide derivatives of the formula These azaindole piperazine diamide derivatives, among other things, are useful as therapeutic agents for the treatment of HIV and AIDS.

Abstract: Indanes, benzopyrans and analogues thereof are potassium channel inhibitors and blockers of IKur and have the structure: where A, B, D, Q, X1, R, R1, X2 and R2 are as defined herein. These compounds are useful as antiarrhythmic agents. In addition, a method is provided for preventing cardiac arrhythmia employing the above compounds.

Abstract: Biologically active crystalline solvates of paclitaxel are precipitated using polar, aprotic, organic solvents. A pharmaceutical composition is also disclosed, as well as the preparation of the novel solvates and their uses as anti-tumor agents.

Abstract: Purine phosphodiesterase 7 (PDE 7) inhibitors of the following formulas wherein R1, Z, Y and J are described herein, and analogs thereof are provided which are useful in treated T-cell mediated diseases. R2 is defined by the following (a) heteroaryl, or heterocyclo, either of which may be optionally substituted with one to three groups T1, T2, T3; (b) aryl substituted with one to three groups T1, T2, T3 provided that at least one of T1, T2, T3 is other than H; or (c) aryl fused to a heteroaryl or heterocyclo ring wherein the combined ring system may be optionally substituted with one to three groups T1, T2, T3.

Abstract: Novel benzothiazoles and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic disorders.

Abstract: The present invention is directed to novel stereoselective processes for the preparation of (S)-1-arylethanols by the reduction of the corresponding keto group containing compounds by microorganisms. (S)-1-arylethanols are useful as intermediates in the synthesis of compounds that are inhibitors of &ggr;-secretase useful in the treatment of Alzheimer's disease.

Abstract: A system and method for measuring ventricular function in an isolated, perfused heart using an intraventricular balloon connected to a plumbing circuit containing a fluid, the plumbing circuit including (a) a valve for selectively opening the plumbing circuit to (i) atmospheric pressure or (ii) a pressure control circuit of a pressure control apparatus or (b) a pressure control apparatus which can be selectively connected to the plumbing circuit, including the steps of establishing a base pressure by (1) opening the valve to atmospheric pressure or the pressure control circuit or (2) operating the pressure control apparatus, after equalization of the pressure within the intraventricular balloon with the base pressure, closing the valve or stopping operation of the pressure control apparatus, following the closing of the valve, measuring ventricular function as a function of a titrated infusion of fluid into the plumbing circuit and intraventricular balloon, performing an intervention, and repeating at least t

Abstract: Compounds having the formula (I), —NR11R12; G is a novel side chain selected from C2-6alkenyl, A3-aryl, —OR18, heteroaryl, A1-cyano, A2—OR17, A1—C(═O)R18, A1—CO2R18, A1—C(═O)NR18R19, A1—OC(═O)R18, A1—NR18C(═O)R19, A1—OC(═O)NR18R19, A1—NR18CO2R19, A1—NR18SO2R17, A1—SO2R17, A1—NR20C(═O)NR18R19, and A1—SR18; or when y is 0 or when W is not NHR22, G may be A1-heterocyclo, wherein A1 is a bond, C1-6alkylene or C2-alkenylene, A2 is C1-6alkylene or C2-6alkenylene, and A3 is C2-6alkenylene; W is selected from —NR21R22, —OR23, —NR21C(═O)R24, —NR21CO2R24, amidino, guanidino, or a heteroaryl, heterocyclo or C3-7cycloalkyl as defined in the specification, and X and R1 through R24 are as defined in the specification, are effective as modulators of melanocortin-receptors, particularly MC-1R and MC-4R.

Abstract: Compounds having the formula (I): and pharmaceutically-acceptable salts thereof, are useful for treating inflammatory or immune diseases, in which A is a four to seven membered heterocyclic or carbocyclic saturated ring; L and K are O or S; M is N or CH; Y is N or CH; Z is hydrogen, alkyl or substituted alkyl; and R1-R4 are as defined in the specification.

Abstract: The invention relates to a prokaryotic cell system for monitoring protease activity. The invention also includes assays for identifying protease inhibitors and protease modulators, determining the amino acid sequence of a protease cleavage site for a known protease, identifying and cloning a protease whose cleavage site is known, and rapidly identifying a form of a protease exhibiting increased activity relative to a control protease.

Abstract: The modified sFv molecules of the present invention stimulate adhesion between cells thereby enhancing the immune response against disease. These molecules generally comprise an antigen binding site of an antibody and at least a portion of a transmembrane domain of a cell surface receptor.