Abstract: This invention relates to a series of substituted aromatic ethers of the formula I wherein ring A and X and Y are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: Polynucleotide and polypeptide sequences are described. The polypeptide sequences comprise one or more of: (a) a polypeptide having the deduced amino acid sequence translated from the polynucleotide sequence in SEQ ID NO: 1 and variants, fragments, homologues, analogues and derivatives thereof; (b) a polypeptide of SEQ ID NO: 2 and variants, fragments, homologues, analogues and derivatives thereof; or (c) a polypeptide encoded by the cDNA of NCIMB 41066 and variants, fragments, homologues, analogues and derivatives thereof.

Abstract: An improved device for equilibrium dialysis procedures utilizing a dialysis membrane inserted in a gap in and separating all of any number of test wells contained in the dialysis block into at least a donating and receiving side which can be accessed and manipulated at any time during testing from the top of the device is described. The device may be constructed from a series of nine blocks of virgin teflon, cut and made flat to achieve certain dimensions ideal for making the device compatible with standard 96-well format laboratory equipment and conducive to robotic automation. The bars are placed side-by-side and connected by a pair of alignment pins along which the bars can slide on a horizontal plane relative to one another, individually or collectively, to aid in assembly, usage and cleaning. The bars are further held together during usage by a clamping mechanism to prevent any leakage of the sample being tested.

Abstract: The invention relates to a method of preparing compounds of the formula 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: The invention relates to compounds of the formula and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein R1, R2, R3, R4, R5, R17, Rf, A, X, and Y are as defined herein. The invention also relates to pharmaceutical compositions containing the compounds of formulas 1, methods of using the compounds of formula 1 in the treatment of infections and methods of preparing the compounds of formula 1.

Abstract: The present invention relates to compositions and methods of achieving a therapeutic effect including, the treatment or prevention of Syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.

Abstract: The present invention provides methods and kits for treating osteoarthritis using an estrogen agonist/antagonist.

Abstract: The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.

Abstract: Compound of general formula I: wherein R1, R2, R3, R4, X, Y and R5 have the meanings given herein which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.

Abstract: The invention provides methods for inhibiting oxidative degradation of pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient which methods comprise adding an oxidation-inhibiting amount of a ferrous ion source, preferably in the form of a pharmaceutical excipient, to the formulation. The invention further provides pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient and an oxidation-inhibiting amount of a ferrous iron source, preferably in the form of a pharmaceutical excipient. The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.

Abstract: Conventional spray-drying methods are improved by incorporation of a pressure nozzle and a diffuser plate to improve the flow of drying gas and a drying chamber extension to increase drying time, such improvements leading to the formation of homogeneous solid dispersions of drugs in concentration-enhancing polymers.

Abstract: The invention provides methods of protecting solid-state proteins from the effects of ionizing radiation which comprise combining the protein with a radiation-protecting amount of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde; radiation-protecting amounts of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde, and 6-hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid; or radiation-protecting amounts of a methoxysalicylaldehyde derivative, preferably 3-methoxysalicylaldehyde and isopropanol, prior to exposing the protein to ionizing radiation.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.

Abstract: The present invention is directed to a novel strain of feline immunodeficiency virus, designated herein as FIV-141, and to attenuated forms of the virus produced by mutating specific regions of the viral genome. The virus and mutated forms of the virus may be used to induce the production of antibodies to FIV-141, and in vaccines designed to protect cats from FIV.

Abstract: The present invention relates to a process for preparing pyridazinone aldose reductase inhibitors which are useful in the prevention and/or treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. The invention also relates to novel intermediates useful in preparing those aldose reductase inihibitors.

Abstract: There is provided a compound of formula I: wherein X represents O or NR5 R4 represents H, halo, cyano, nitro, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13, NR16Y(O)R17, N[Y(O)R17]2, SOR18, SO2R19, C(O)AZ, lower alkyl, lower alkenyl, lower alkynyl, Het, alkylHet, aryl, alkylaryl (which latter seven groups are all optionally substituted with one or more substituents selected from halo, cyano, nitro, lower alkyl, halo(loweralkyl), OR6, OC(O)R7, C(O)R8, C(O)OR9, C(O)NR10R11, NR12R13 and SO2NR14R15) which are useful in the curative and prophylactic treatment of a medical condition for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g., cGMP PDE5) is desired.

Abstract: The invention is a compound of Formula (I): wherein R is —OH, R1 is —OH, R2 is —H, n is 2 or 3 and X is sulfur, or a pharmaceutically acceptable salt of a compound having Formula (1), or a pharmaceutical composition comprising a compound having Formula (1) or a pharmaceutically acceptable salt thereof, or methods of treating bone loss, breast cancer or prostate cancer comprising administering an effective amount of the compound having Formula (I) or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to nicotinamide derivatives and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The nicotinamide derivatives according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions as well as for wounds healing.

Abstract: This invention relates to methods, pharmaceutical compositions and kits useful in promoting bone formation and/or preventing bone loss and lowering blood cholesterol. The compositions are comprised of an estrogen agonist/antagonist as a first active component and a statin as a second active component and a pharmaceutically acceptable vehicle, carrier or diluent. The compositions and methods of treatment are effective while substantially reducing the concomitant liability of adverse effects associated with estrogen administration.

Abstract: A compound selected from those of formula (I): wherein R1a, R1b, R2, R3, are as defined in the description, and optionally, its optical isomers, N-oxide, and addition salts thereof with a pharmaceutically-acceptable acid or base, and medicinal products containing the same are useful as specific inhibitors of phosphosdiesterase-7 (PDE-7).