Abstract: This invention relates to 2- or 3-(substituted aminoalkoxyphenyl)quinazolin-4-ones which are partial estrogen agonists and are useful in treating osteoporosis, prostatic hypertrophy, breast cancer and endometrial cancer.

Abstract: This invention relates to compounds of Formula I ##STR1## wherein: R.sup.1 and R.sup.2 are independently selected from hydrogen, straight-chain and branched alkyl group having up to 10 carbon atoms or --(CH.sub.2).sub.m Ar where Ar is phenyl, naphthyl or thienyl, each optionally substituted by one or two substituents selected independently from C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxide and trifluoromethyl;or NR.sup.1 R.sup.2 is 1, 2, 3, 4-tetrahydroquinolin-1-yl or 1, 2, 3, 4-tetrahydroisoquinoline-2-yl;m is 1-5;n is 1 or 2;Y is hydrogen, C.sub.1 -C.sub.6 alkyl, and C.sub.1 -C.sub.6 alkoxy;or the pharmaceutically acceptable salts thereof, which are dopamine D.sub.2 agonists and therefore useful in the treatment of psychoses and Parkinson's disease.

Abstract: This invention relates to a process of recovering a neutral macrolide antibiotic, especially a tricyclic macrolide such as rapamycin from concentrates of fermentation broth extracts or mother liquors whereby acidic and/or basic components formed in the fermentation process are removed by utilizing aqueous base or acid extraction procedures from a water-immiscible solution of said concentrate and non-polar components are separated from the neutral macrolide by selective solubility.

Abstract: The earliest lesion of atherosclerosis is development of the fatty streak lesions which contain lipid-laden macrophages and lipid-laden smooth muscle cells. Macrophages do not take up native low density lipoprotein (LDL) but do take up modified, i.e., acetylated LDL or oxidized LDL via acetyl-LDL or "scavenger" receptors to form the foam cells of atherosclerotic plaque. Arterial smooth muscle cells generate superoxide and oxidize LDL in the presence of micromolar concentrations of Cu.sup.+2 or Fe.sup.+2. The way LDL can be modified by endothelial cells can be mimicked in vitro by incubation of the lipoprotein in the presence of CuCl.sub.2. The compounds of this invention inhibit copper mediated oxidation of LDL in vitro and are thus useful in the prophylaxis and treatment of clinical conditions for which inhibition of the oxidative modification of lipids is indicated, for example, atherosclerosis. The compounds of this invention are represented by the formula 1 below ##STR1## wherein: R.sup.1 is hydrogen, C.

Abstract: The compounds of this invention which have the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl;R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ;X is --CH.sub.2 -- or --OCH.sub.2 --;n is 1 or 2;or a pharmaceutically acceptable salt thereof,are useful in treating or inhibiting the long-term complications of diabetes such as diabetic retinopathy, nephropathy and neuropathy through the inhibition of the enzyme aldose reductase. Aldose reductase inhibitors have been shown to prevent the biochemical, functional and morphological changes induced by hyperglycemia.

Abstract: This invention relates to compounds which have oral antihyperglycemic activity of the formula: ##STR1## wherein: R.sup.1 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, thienyl, furyl, pyridyl, ##STR2## R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; X os O or S;n is 0, 1, or 2;A is ##STR3## Y is O or S;Z is N or CH when Y is O and Z is CH when Y is S;or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to 4-phenoxy (and 4-substituted phenoxy)5-hydroxy-2(5H)-furanones of the formula: ##STR1## where Z is ##STR2## where R is H, halogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, trifluoromethyl, or ##STR3## and X is H, C.sub.1 -C.sub.8 alkyl, --O--C.sub.1 -C.sub.8 alkyl, or halogen;a process for their preparation, their use in the treatment of osteoporosis, and pharmaceutical compositions thereof.

Abstract: This invention relates esterified polysulfated cyclodextrins, their use in treating diseases and conditions which are characterized by excessive smooth muscle cell (SMC) proliferation such as restenosis and a pharmaceutical composition thereof. The compounds useful in this invention are represented by Formula I: ##STR1## where: M is a pharmaceutically acceptable cation;R is selected from the group consisting of C.sub.1 -C.sub.12 lower alkyl, C.sub.3 -C.sub.12 cycloalkyl, and aryl optionally substituted with 1-3 substituents independently selected from halogen, C.sub.1 -C.sub.12 lower alkyl or C.sub.1 -C.sub.12 alkoxy; andn is an integer from 6-8, representing .alpha.-cyclodextrin (n=6), .beta.-cyclodextrin (n=7), and .gamma.-cyclodextrin (n=8).

Abstract: This invention relates to novel 2-[4-(5-substituted-1,2,4-oxadiazol-3-ylmethoxy)benzyl]-1,2,5-oxadiazolidi ne-3,5-diones which have demonstrated antihyperglycemic activity in diabetic (ob/ob and db/db) mice, genetic animal models of non-insulin dependent diabetes mellitus (NIDDM or Type II diabetes). These compounds are represented by Formula I below: ##STR1## wherein R.sup.1 is C.sub.6 -C.sub.10 aryl, optionally substituted by one to three substituents independently selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.3 trifluoroalkyl or C.sub.1 -C.sub.3 trifluoroalkoxy; andR.sup.2 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.6 alkyl, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.3 trifluoroalkyl, and C.sub.1 -C.sub.3 trifluoroalkoxy,or a pharmaceutically acceptable salt thereof.

Abstract: A derivative of rapamycin of general formula (1) and (2) ##STR1## wherein ##STR2## R.sup.2 =hydrogen, or lower alkyl having 1 to 6 carbon atoms; ##STR3## wherein X=hydrogen, lower alkyl having 1 to 6 carbon atoms, --CF.sub.3, --NO.sub.2, --OR.sup.2, NR.sup.2, SR.sup.2, or halogen;R.sup.4 =lower alkyl, alkenyl or alkynyl having 1 to 6 carbon atoms or an aromatic or heterocyclic moiety selected from the group consisting of phenyl, naphthyl, thiophenyl and quinolinyl;Y.sup.- =halide, methanesulfonate, toluene sulfonate or maleate: andZ=oxygen or OH and H.which by virtue of its immunosuppressive activity is useful in treating transplantation rejection, host versus graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: Antiinfluenza A activity was found in compounds of the formula: ##STR1## wherein: X is 2-phenylethyl, 2-furanylmethyl, or ##STR2## where one of R.sup.1 and R.sup.2 is H and the other is phenylamino; Z is --SCH.sub.3 when X is ##STR3## when X is 2-phenylethyl or 2-furanylmethyl; or a pharmaceutically acceptable salt thereof.

Abstract: The invention concerns compounds of formula (I) ##STR1## where R.sup.1 is alkyl, haloalkyl, alkenyl, or alkynyl containing 1 to 6 carbon atoms; or an aromatic moiety selected from phenyl, naphthyl and 4-(phenylaza) phenyl wherein said aromatic group is optionally substituted by one or more substituents selected from C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.6) thioalkyl, halo, cyano, nitro, trifuluoromethyl, trifluoromethoxy or R.sup.1 is a heteroaromatic group of 5 to 10 ring atoms containing oxygen, nitrogen and/or sulfur as heteroatom(s) wherein said heteroaromatic group is optionally substituted by one or more substituents selected form C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, hydroxy, amino, mono- or di-(C.sub.1 -C.sub.6)alkylamino, carboxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, C.sub.2 -C.sub.7 alkanoyl, (C.sub.1 -C.sub.

Abstract: A derivative of rapamycin of general formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are selected from the group consisting of hydrogen, acyl, sulfonyl or alkyl or a pharmaceutically acceptable salt thereof, which is by virtue of its immunosuppressive activity is useful in treating transplantation rejection host vs. graft disease, autoimmune diseases, and diseases of inflammation.

Abstract: The invention relates to a method of treating alcoholism, sleep disorders or behavioral symptoms of Alzheimer's disease which comprises administration of bridged 2-(4-arylpiperazin-1-ylalkyl)-hexahydroisoindol-1,3-dione derivatives to a warm-blooded animal in need thereof.

Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarboxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.

Abstract: Derivatives of 2-amino-1-phenylethanol were prepared from substituted amines and benzoin, stilbene oxide or styrene oxide to give compounds of Formula: ##STR1## where R is H or (un)substituted phenyl and C is a linking group or terminal group. The compounds of this invention can inhibit ulceration in in-vivo studies in rats.

Abstract: Inhibition of the enzymes cholesterol ester hydrolase (CEH) and/or acyl coenzyme A: cholesterol acyltransferase (ACAT) results in inhibition of absorption of cholesterol and thus lowers serum cholesterol levels. Compounds of the formula below: ##STR1## where R.sup.1 is selected from alkyl, alkenyl, cycloalkyl, cycloalkylalkyl or arylalkyl and R.sup.2 is hydrogen or alkyl or --NR.sup.1 R.sup.2 is morpholine, thiomorpholine or 4-substituted or unsubstituted piperidine and R.sup.3, R.sup.4, R.sup.5, R.sup.6 are hydrogen, alkyl, alkoxy, halogen, nitro, cyano, perhaloalkyl, alkanoyloxy, alkoxycarbonyl or hydroxycarbonyl have been shown to inhibit the enzymes CEH and/or ACAT in in vitro tests to inhibit absorption of radio-labeled cholesterol in rats.

Abstract: Reduction of the C-33 ketone of rapamycin gives the C-33 hydroxy analog of Formula I. ##STR1## The reduction product prevents cleavage of the C-31/C-32 bond due to base degradation. The Formula I compounds exhibit immunosupressant, antifungal, and antiinflammatory activities.