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: An immobilized lipase is employed in an organic solvent to esterify diol lactone derivatives of HMG-CoA reductase inhibitors to form HMG-CoA reductase inhibitors of formula (I). ##STR1## This process allows for the efficient, one-step production of HMG-CoA reductase inhibitors of structural formula (I).

Abstract: Anti-ulcer agents having a methylsulfinyl bridge between a substituted pyridine moiety and a substituted benzimidazole moiety are prepared by oxidizing the corresponding compounds, having a methylthio bridge, with magnesium monoperoxyphthalate in a suitable solvent. The reaction may be run in an aromatic hydrocarbon solvent, wherein the product may crystallize out of the reaction solution and may be directly isolated by filtration.

Abstract: This invention relates to compounds of formulae I and II ##STR1## which are metabolites of tetrahydrosimvastatin and 5-hydroxy-tetrahydrosimvastatin and which are HMG--CoA reductase inhibitors.

Abstract: A stable blended product comprising a melamine aldehyde, urea aldehyde or melamine-urea aldehyde and colloidal silica is useful as a detackifier for solvent-borne paints and other resinous materials. This product is also useful as a conditioning agent prior to collection of water-borne paints, a treatment for water containing oils or greases, a color-remover in natural waters, and for enhanced removal of suspended solids.

Abstract: The instant invention is directed to a method for enhancing the lowering of plasma cholesterol level in a subject in need thereof which comprises the time-controlled administration of a nontoxic therapeutically effective amount of an HMG-CoA reductase inhibitor to said subject which surprisingly affords an equivalent or improved reduction of plasma cholesterol levels while significantly reducing the amount of HMG-CoA reductase inhibitor circulating in the bloodstream of the subject as compared to the same parameters when the oral administration of a conventional rapid release dosage form is utilized.

Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.

Abstract: This invention relates to compounds of structural formula (I) isolated from an aerobic fermentation of Trichoderma viride MF5628, ATCC 74084: ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents. These compounds are also potent antifungal agents. Additionally, they inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras and are thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).

Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of zaragozic acid A.

Abstract: New cholesterol lowering compounds are formed from the photochemical treatment of the zaragozic acids.

Abstract: This invention is directed to compounds of formula (I) which are novel C3- or C5-acyl sulfonamide, carboxamic acid or tetrazolyl analogs of the Zaragozic acids. These compounds inhibit the enzyme squalene synthase and are useful as cholesterol lowering agents.

Abstract: Cholesterol lowering compounds and compositions are formed from the photochemical treatment of the Zaragozic Acids followed by esterification. These compounds and compositions are active squalene synthetase inhibitors useful in the treatment of hypercholesterolemia.

Abstract: 4-Substituted-1,4-dihydropyridines are prepared by a cycloaddition reaction in which the cyclization is driven to completion, after thermal reaction, by addition of an acid. Felodipine, a vasodilator, is prepared by a cycloaddition reaction of ethyl 3-aminocrotonate with a suitably substituted dichlorobenzylidine under reaction conditions whereby the product crystallizes out of the reaction solution and may be directly isolated by filtration.

Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.

Abstract: Compounds of Structural Formula (I) ##STR1## are produced by directed biosynthesis. These compounds are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer.

Abstract: A pyrroloquinoline compound of the following formula is disclosed: ##STR1## wherein H,C.sub.1-6 alkyl,R.sup.1 is: ##STR2## wherein R is H, C.sub.1-10 alkyl, or C.sub.1-6 alkyloxycarbonyl; R.sup.2 is:H,C.sub.1-6 alkyl, ##STR3## wherein R.sup.5 is C.sub.1-10 alkyl, aryl, or aryl C.sub.1-10 alkyl; R.sup.3 is:(CH.sub.2).sub.n NHR wherein R is H, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxycarbonyl; ##STR4## R.sup.4 is: H,C.sub.1-6 alkyl,C.sub.1-6 alkyloxycarbonyl,RCH.sub.2 --, wherein R is H, C.sub.1-6 alkyl or aryl, or ##STR5## X is O, or NR.sup.6 wherein R.sup.6 is equal to H or C.sub.1-6 alkyl and n is an integer from 1-3.The compounds of the invention exhibit bradykinin antagonist activity as well as activity with .alpha.-adrenergic, histaminergic, and muscarinic receptors.

Abstract: An acyclic tricarboxylic compound has been isolated from a culture of MF5453. The compound and its derivatives are active as squalene synthetase inhibitors and are useful in the treatment of hypercholesterolemia.

Abstract: This invention relates to a fungal microorganism Pseudodiplodia sp. (MF5767) isolated from bark discs of Hibiscus sp. and useful in a fermentation process to form compounds of formula (I): ##STR1## which are squalene synthetase inhibitors and thus useful as cholesterol lowering agents.

Abstract: This invention relates to compounds of structural formula (I): ##STR1## which are squalene synthase inhibitors and thus useful as cholesterol lowering agents and antifungal agents. These compounds are also inhibitors of farnesyl protein transferase and farnesylation of the oncogene protein Ras and thus useful in treating cancer. This invention also relates to a process for obtaining compounds of structural formula (I).

Abstract: Compounds of Structural Formula (I) ##STR1## are produced by chemical modification of directed biosynthesis products. These compounds are squalene synthetase inhibitors and thus useful as cholesterol lowering agents, antifungal agents and cancer treatment agents.