Abstract: In one embodiment, the present invention discloses a method and pharmaceutical composition for lowering serum cholesterol in a patient. The method comprises administering to the patient a pharmaceutical composition comprising a therapeutically effective cholesterol lowering amount of an imidazole.

Abstract: The present invention relates to identification of a novel, de novo priming activity of hepatitis C virus replicase. This activity can be used to screen for anti-HCV replicase compounds, or to characterize the biological relevance of lead compounds that have already been identified.

Abstract: Amide derivatives of 1,4 di-substituted piperidine compounds of the formula or a pharmaceutically acceptable salt, ester or solvate thereof, wherein Q and Q1 are each —CH═, or one of Q and Q1 is —CH═ and the other is —N═; X is —CH2— or Y and Z are —C(R5)═, or one of Y and Z is —C(R5)═ and the other is —N═; R1 is 1 to 3 substituents selected from H, halogen and alkoxy; R2 and R5 are 1 to 3 substituents selected from H, halogen, alkyl and alkoxy; and R3 and R4 are H or (C1-C6)alkyl are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed.

Abstract: Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) wherein R, R1, R2, R3, R4, R21, R27, R28, X, Y, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.

Abstract: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase.

Abstract: The present invention provides methods for isolating adjunct isoforms of proteins and converting them to the desired protein. In preferred embodiments, the present invention contemplates the use of acid solutions or zinc solutions to cleave a chemical group from a desired protein. In further preferred embodiments, the present invention contemplates the oxidation of reduced sulfhydryl groups with cleavage of chemical groups to form a functional desired protein.

Abstract: Nucleic acids encoding various lymphocyte cell proteins from mammalian, including primate, reagents related thereto, including specific antibodies, and purified proteins are described. Methods of using said reagents and related diagnostic kits are also provided.

Abstract: Interleukin-10 for producing a population of cells which are capable of inhibiting or suppressing reactions to alloantigens, for example in graft-versus-host disease or tissue rejection, is described. Interleukin-10 for reducing responses in mixed lymphocyte response (MLR) is also described. Exogenous or induced endogenous IL-10 may be used for the inhibition or suppression of the reactions to alloantigens.

Abstract: The invention relates to compounds of the formula wherein R1, R2, R3, R4, R5, R6, R7, R8, Y, A, B, X, a, b, c, d, v, and w are as described herein. The compounds of formula (1.0) are useful for inhibiting tumor growth.

Abstract: 5′-Amino acid esters of ribavirin represented by formula I: wherein R is CH3CH(NH2)—CO—, CH3CH2(CH3)CHCH(NH2)—CO—or H2N(CH2)4CH(NH2)—CO—; preferably R is or a pharmaceutically acceptable salt thereof, e.g., trifluoroacetate, tosylate, mesylate, and chloride, pharmaceutical compositions containing them as well as methods of treating patients having susceptible viral infections, e.g., chronic hepatitis C infections by administering a therapeutically effective amount of a ribavirin derivative, alone or in combination with a therapeutically effective amount of interferon-alpha are disclosed.

Abstract: Purified genes encoding intracellular regulatory molecules from a human, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding these molecules are provided. Methods of using said reagents and diagnostic kits are also provided.

Abstract: CTLA-8 antigen from a mammal, reagents related thereto including purified proteins, specific antibodies, and nucleic acids encoding said antigen. Methods of using said reagents and diagnostic kits are also provided.

Abstract: Disclosed is a process for preparing a compound having the formula: wherein R1 is selected from the group consisting of: alkyl, alkenyl, alkynyl, aryl, aralkyl, cycloalkyl, and cycloalkylalkyl, R1 being optionally substituted by substituents selected from halo, —OH, alkyl, alkoxy, or —CF3, said process comprising the following steps: (a) reacting a ketone having the formula with a carbanion having the formula wherein R1 is as defined above, and R2 and R3 are independently selected from the group consisting of —ORA and —RA, wherein RA is alkyl, phenyl, substituted phenyl, cycloalkyl, substituted cycloalkyl, cycloalkylalkyl, or substituted cycloalkylalkyl; (b) treating the reaction mixture from step (a) with a protonating agent; and (c) thermally decomposing the product of 16, to form the compound of formula (I). The compounds made by this process have antihistaminic activity, e.g., loratadine.

Abstract: Methods of treating and/or preventing sleep disorders in a human afflicted with upper airway passage allergic inflammation and/or congestion associated with allergic rhinitis, including seasonal allergic rhinitis or perennial allergic rhinitis, by administering a therapeutically effective amount of desloratadine, alone or in combination with other active such as a decongestant, e.g., pseudoephedrine are disclosed.

Abstract: Intermediates having the formula wherein BI is —CH2OH or —CH2ORP, and RP is an alcohol protecting group; a is 1, 2, or 3; TI is —OH or QI is phenyl, naphthyl ohr heteroaryl having 1-3 substituents; Ra and Rc are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl cycloalkyl, aryl, or —OH; or Ra and Rc together with the C—N—C chain to which they are bound, form a 5-7 membered ring; Rb and Rd are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl, cycloalkyl, aryl, or —OH; and D is a directing group capable of directing lithiation alpha to a nitrogen atom of a nitrogen compound having D as a substituent bound to the nitrogen atom when the nitrogen compound is reacted with s-butyl lithium, are disclosed

Abstract: The present invention provides human ras converting endoprotease (RCE), the encoding nucleic acids, recombinant vectors, transformed host cells and methods of making human RCE. More particularly, the invention provides methods of using human RCE in screening systems to identify inhibitors of human RCE useful for the treatment of various medical conditions. This invention further relates to inhibitors of human RCE.

Abstract: The present invention is directed towards a pharmaceutical composition useful for the treatment of allergic rhinitis, asthma and related disorders. In one embodiment, the composition comprises, in combination, a therapeutically effective amount of at least one neurokinin antagonist, and a therapeutically effective amount of at least one 5-lipoxygenase inhibitor.

Abstract: A short practical commercial process for the efficient enantioselective synthesis of the non-steroidal antiestrogen of formula I or XIV or a pharmaceutically acceptable salt thereof.

Abstract: Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused Spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nocicepti

Abstract: The invention provides methods for purifying a virus from impurities in an aqueous medium.