Abstract: The instant invention provides a homologation process for making a zincate homoenolate from a carbon bound enolate zincate, by treating the carbon bound enolate zincate with an alkoxy lithium reagent. The homologation step can be coupled with a homoaldol reaction, as well as with other transmetallation reactions, in a one pot process. The zincate homoenolate is a useful intermediate in the preparation of a variety of different end-products, such as HIV protease inhibitors and renin inhibitors.

Abstract: Controlled delivery of a beneficial agent in a dispersion is provided using (i) a compressed core which contains the beneficial agent, a polymer which forms gelatinous microscopic particles upon hydration, and if desired, an agent to modulate the hydration; and (ii) a water insoluble coating which adheres to and surrounds the core and contains apertures which provide an area for the hydration and release of the dispersion. The release rate of the beneficial agent is a function of the number and size of the apertures in the coating.

Abstract: Fibrinogen receptor antagonists of the general formula:X-A-Y-Z-B Iand which includes, for example, the compounds of formula ##STR1## are useful for inhibiting the binding of fibrinogen to blood platelets, inhibiting the aggregation of blood platelets, treating thrombus formation or embolus formation, and preventing thrombus or embolus formation.

Abstract: Ergostanone derivatives substituted with dissaccharides are cholesterol absorption inhibitors useful in the treatment of hypercholesterolemia and related disorders. These cholesterol absorption inhibitors may be employed alone or in combination with other cholesterol lowering agents.

Abstract: The NER receptor is a novel member of the steroid hormone receptor superfamily and has been prepared by cDNA cloning from a human osteosarcoma SAOS-2/B10 cell library. The complete sequence of human NER complementary DNA (Seq. ID No. 1), expression systems including a COS stable expression system, the expressed protein (SEQ. ID No. 2) and an assay using the COS expression system are disclosed. The assay may be used to identify agents which activate transcription mediated by the NER receptor, and which are useful for potentiating the activity of a modulator of a G-protein coupled receptor wherein the G-protein coupled receptor is a member of the steroid hormone receptor superfamily.

Abstract: A process is described for the removal of a silyl protecting group from the 4-hydroxy group of a tetrahydro-pyran-2-one moiety.

Abstract: A process is disclosed for making a chiral compound of the formula ##STR1## comprising reacting an epoxide compound of the formula ##STR2## and an amide of the formula ##STR3## in the presence of a strong base at a low temperature.

Abstract: Use of the novel receptor NER TOFA (5-(tetradecyloxy)-2-furan-carboxylic acid) to treat Alzheimer's disease.

Abstract: 17.beta.-N-monosubstituted-carbamoyl-4-5.alpha.-androst-1-en-3-ones of the formula ##STR1## wherein R.sup.1 is selected from hydrogen, methyl and ethyl and R.sup.2 is a branched chain alkyl of from 3-12 carbons, and R', R", R'" are hydrogen or methyl are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of androgenic alopecia.

Abstract: 17.beta.-N-monosubstituted-carbamoyl-4-5.alpha.-androst-1-en-3-ones of the formula ##STR1## wherein R.sup.1 is selected from hydrogen, methyl and ethyl and R.sup.2 is a branched chain alkyl of from 3-12 carbons, and R', R", R"' are hydrogen or methyl are active as testosterone 5.alpha.-reductase inhibitors and thus are useful topically for treatment of androgenic alopecia.

Abstract: The instant invention involves a method of treating and/or reversing androgenic alopecia and promoting hair growth, and methods of treating acne vulgaris, seborrhea, and female hirsutism, by administering to a patient in need of such treatment a 5.alpha.-reductase 2 inhibitor, such as finasteride, in a dosage amount under 5 mgs/day.

Abstract: Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Compounds of the formula ##STR1## are inhibitors of 5.alpha.-reductase and are useful alone or in combination with other active agents for the treatment of hyperandrogenic disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.

Abstract: The instant invention involves methods of treating sweat related conditions with compounds that are 5.alpha.-reductase inhibitors. The 5.alpha.-reductase inhibitors may be administered alone or in combination with other active agents to treat conditions such as apocrine gland sweating, hyperhidrosis, and hydradenitis suppurativa.

Abstract: Disclosed herein are compounds of structural formula (I) ##STR1## which are useful as cholesterol lowering agents. These compounds are also useful as inhibitors of squalene synthetase, inhibitors of fungal growth, inhibitors of farnesyl-protein transferase and farnesylation of the oncogene protein Ras. These compounds are also useful in the treatment of cancer.

Abstract: Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Abstract: The novel process of this invention involves the reduction of certain .DELTA.-5 steroidal alkenes to selectively produce either the 5.alpha. or 5.beta. reduction products. Particularly, this invention involves reduction of .DELTA.-5 steroidal alkenes using a rhodium based catalyst in the presence of hydrogen to selectively yield 5.alpha. steroids or alternatively reduction of .DELTA.-5 steroidal alkenes in an ionizing medium with a trialkylsilane to selectively yield 5.beta. steroids.

Abstract: A compound of structural formula ##STR1## having antihypercholesterolemic utility is produced by culturing a Streptomyces sp.