Abstract: The present invention relates to .DELTA..sup.16 unsaturated steroids which are useful as steroid C.sub.17-20 lyase inhibitors.

Abstract: This invention relates to acylated enol derivatives of .alpha.-ketoesters and .alpha.-ketoamides. The compounds of this invention are either prodrugs of known elastase inhibitors or are elastase inhibitors in their own right and are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema.

Abstract: A method of attenuating a cognitive deficit in a patient in need thereof comprising administering to the patient a xanthine derivative.

Abstract: The present invention is a process of converting a hydroxy aromatic into a 2-hydroxy-N-arylacetamide, comprising:(1) treating a reaction mixture comprising a salt of a hydroxy aromatic with an alkylating agent; and(2) treating the reaction mixture with a Smiles solvent system and raising the temperature of the reaction mixture.

Abstract: Xanthine derivatives having general structure (I) including the (R) and (S) enantiomers and racemic mixtures thereof, and the pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently (C.sub.1 -C.sub.4)lower alkyl or (C.sub.2 -C.sub.4)lower alkenyl, Z is (II) or (III) or (IV) wherein R.sub.3 is hydrogen, (C.sub.1 -C.sub.3)lower alkyl, nitro, amino, hydroxy, fluoro, bromo or chloro, R.sub.4 is (C.sub.1 -C.sub.4)lower alkyl and n is 1 or 2 which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.

Abstract: The present invention relates to achiral polyurea oligomers, their uses and formulations as anti-HIV pharmaceuticals and to a process for the preparation of narrow mono- and polydispersed oligomers as an emodiment of the invention. The achiral oligomers are derived from repeating units of the monomer 4,4'-diamino-biphenyl-3,3'-disulfonic acid and are water soluble, have a rigid backbone, possess ordered anionic spacing and have a number average molecular weight of <20,000. The process relates to the synthesis of narrow poly- and mono-dipersed oligomers comprising the steps of: 1) restricting the crude olydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture to a narrow polydispersed anionic oligomer mixture; and/or 2) isolating the monodispersed anionic oligomer; and 3) optionally converting the narrow poly- or mono-dispersed anionic oligomer salt from Step 1 or 2 to a desired pharmaceutically-acceptable salt, especially a solim or potassium salt.

Abstract: This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.

Abstract: This invention relates to acylated enol derivatives of known elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases, including cystic fibrosis and emphysema or as prodrugs of compounds which are useful in the treatment of said diseases.

Abstract: This invention relates to oxazolidine inhibitors of calpain and/or cathepsin B and to compositions containing them. As inhibitors of calpain and/or cathepsin B, the compounds are useful in the treatment of patients afflicted with acute or chronic neurodegenerative disorders.

Abstract: The present invention relates to .DELTA..sup.16 unsaturated C.sub.17 heterocyclic steroids which are useful as steroid C.sub.17-20 lyase inhibitors.

Abstract: The present invention relates to compounds of formula 1, ##STR1## including all of its stereoisomers, compositions, and processes for preparation of the same. The compounds of the present invention are also useful in their pharmacological activities as they directly act as inhibitors of prolyl endopeptidase and thereby provide a methods for memory enhancement, preventing or slowing the affects of amnesia or memory deficits.

Abstract: Novel compounds which are chemically linked inhibitors of the proteases Elastase and Cathepsin G prevent connective tissue degradation associated with neutrophil induced inflammatory disease.

Abstract: The present invention is directed to a method of using a certain compounds which are 2,19-methyleneoxy or 2,19 methylenethio bridged steroids, and related steroidal compounds as inhibitors of the enzyme steroid aromarase, 19-hydroxylase and as treatment for various estrogen dependent/mediated disorders including hormonal dependent breast cancer.

Abstract: This invention relates to novel morpholinourea and related derivatives of pentafluoroethyl peptides which are orally active elastase inhibitors. These compounds are useful in the treatment of various inflammatory diseases and emphysema.

Abstract: The invention provides the compounds 1,2-dideoxy-2-(hydroxymethyl)-1-(methylamino)-myo-inositol hydrochloride, 1,2-dideoxy-2-(hydroxymethyl)-1-(methylamino)-scyllo-inositol, 1,6-dideoxy-6-(hydroxymethyl)-1-(methylamino)-myo-inositol.

Abstract: The compound (R)-2-[(phenylisopropyl)amino]adenosine whose structure is given below: ##STR1## (R)-2-[(phenylisopropyl)amino]adenosine is about two orders of magnitude greater in its selectivity between the A-1 and A-2 adenosine receptors than its diastereoisomer. This compound is useful for lowering blood pressure.

Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.

Abstract: Substituted (1.alpha., 2.beta., 3.alpha. or .beta.,4.alpha.,5.alpha. or .beta.)-2,3,4-trihydroxy-5-(hydroxymethyl)cyclopentylamines are inhibitors of alphamannosidase and alpha-fucosidase and are useful immunostimulants, antiviral and antimetastatic agents.

Abstract: Sulfonic acid stilbenes are disclosed which block the infection of cells by HSV, HIV and CMV.

Abstract: Adenosine analogues which act selectively at adenosine receptors and which act in general as adenosine antagonists are disclosed. From in vitro studies it is known that specific physiological effects can be distinguished as a result of this selectivity and that adenosine receptor activity in vitro correlates with adenosine receptor activity in vivo.Pharmaceutical preparations of the subject compounds can be prepared on the basis of the selective binding activity of the compounds disclosed herein which will enhance certain physiological effects while minimizing others, such as decreasing blood pressure without decreasing heart rate.