Abstract: This invention concerns compounds having the Z-configuration of formula: ##STR1## or salts thereof, wherein R represents an optionally substituted aryl or heteroaryl radical, R.sup.1, R.sup.2 and R.sup.3 each independently represent hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, (C.sub.1 -C.sub.6 alkoxy)carbonyl, carboxy, hydroxy (C.sub.1 -C.sub.6)alkyl, halogen, halo(C.sub.1 -C.sub.6)alkyl, carboxy(C.sub.1 -C.sub.6)alkyl, optionally substituted aryl or heteroaryl or optionally substituted aralkyl or heteroarylalkyl; n represents O, 1 or 2; R.sup.4 and R.sup.5 each independently represent hydrogen or a substituent selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl or R.sup.4 and R.sup.5 are geminal C.sub.1 -C.sub.6 alkyl substituents and R.sup.6 is hydrogen or C.sub.1 -C.sub.6 alkyl which possess antiinflammatory activity.

Abstract: The invention provides a method of attenuating lung capillary leak in a mammal by administering an effective amount of an antifolate, methotrexate.

Abstract: The disclosure describes an improved process for producing optically active compounds of Formula II or III, which compounds are useful as intermediates for preparing compounds active as inhibitors of retroviral protease enzymes: ##STR1## wherein R.sub.1, R.sub.50 and Z are described in the specification. The improved process includes either synthesis of diastereomeric iodolactones which are separated prior to conversion to compounds of Formula II or III or synthesis of an epoxide which is converted directly to compounds of Formula II and III.

Abstract: This invention relates to a technique for treating a mammal with rapamycin which comprises removal of blood from the patient, treatment of the formed blood elements with rapamycin which binds rapidly and reversibly with erythrocytes, and returning the treated blood cells to the circulatory system of the patient for the treatment of any of the diseases, syndromes, conditions, or immune responses which respond to treatment with rapamycin. Alternatively, blood to be treated with rapamycin can be obtained from a hematologically compatible donor mammal.

Abstract: This invention relates to a technique for treating a mammal with rapamycin which comprises removal of blood from the patient, treatment of the formed blood elements with rapamycin which binds rapidly and reversibly with erythrocytes, and returning the treated blood cells to the circulatory system of the patient for the treatment of any of the diseases, syndromes, conditions, or immune responses which respond to treatment with rapamycin. Alternatively, blood to be treated with rapamycin can be obtained from a hematologically compatible donor mammal.

Abstract: This invention relates to compounds useful as anxiolytic agents having the formula: ##STR1## where A is ##STR2## wherein X is O or S;R.sup.1 is selected from H, --CN, --OR.sup.3, --NO.sub.2, --NR.sup.3 R.sup.4, --NR.sup.3 COR.sup.4, --NR.sup.3 COOR.sup.4, --COR.sup.3, --COOR.sup.3, --CONR.sup.3 R.sup.4, --SR.sup.3, --SOR.sup.3, --SO.sub.2 R.sup.3, --SO.sub.2 NR.sup.3 R.sup.4, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, -perhalo-C.sub.1 -C.sub.6 -alkyl, F, Cl, Br, and I;R.sup.2 is selected from H, --COR.sup.3, --COOR.sup.3, --CONR.sup.3 R.sup.4, --CONHR.sup.3, --COCHR.sup.3 R.sup.4, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 alkenyl, and C.sub.2 -C.sub.6 -alkynyl;R.sup.3 and R.sup.4 are independently selected from C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 alkynyl, benzyl, or phenyl which may be optionally substituted by one to three groups selected from F, Cl, Br, I, --NO.sub.2, --CN, and --C.sub.1 -C.sub.6 alkoxy; or R.sup.3 and R.sup.

Abstract: This invention relates to compounds which inhibit lipoxygenase in the metabolism of arachidonic acid and thus inhibits formation of leukotrienes which are implicated in inflammatory processes and bronchoconstriction and inhibits the oxidation of LDL which is implicated in formation of atherosclerotic plaque.The compounds useful in this invention are represented by the formula: ##STR1## wherein: R.sup.2 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl; Y of O or S;R.sup.5 is hydrogen or methylR.sup.6 is --NH.sub.2, --CH.sub.3 or --OCH.sub.3 ;and R.sup.1 is ##STR2## wherein R.sup.7, R.sup.8 and R.sup.10 are independently halogen, trifluoromethyl, alkyl, alkoxy, methanesulfonyl or trifluoromethanesulfonyl; R.sup.9 is hydrogen or methyl; and Z is O or S,or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to novel compounds which have demonstrated oral antihyperglycemic activity in diabetic ob/ob and db/db mice, animal models on non-insulin dependent diabetes mellitus (NIDDM ot Type II diabetes). These compounds have 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## where R.sup.10 is hydrogen, C.sub.1 -C.sub.6 alkyl, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.6 alkyoxy, trifluoroalkyl or trifluoroalkoxy;R.sup.2 is hydrogen or C.sub.1 -C.sub.6 alkyl;X is O or S;n is 0, 1, or 2;A is ##STR3## where R.sup.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, halogen, C.sub.1 -C.sub.6 alkoxy, trifluoroalkyl or trifluoroalkoxy;B is ##STR4## where R.sup.4 is hydrogen, C.sub.1 -C.sub.6 alkyl, allyl, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 aryl-(CH.sub.2).sub.1-6 --, fluorine, chlorine, bromine, iodine, trimethylsilyl or C.sub.3 -C.sub.8 cycloalkyl;R.sup.5 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.6 -C.sub.10 aryl, or C.

Abstract: Compounds which inhibit the enzyme cholesterol ester hydrolase (CEH) thus inhibit the formation of esterified cholesterol. Esterified cholesterol is absorbed through the intestine and inhibition of the enzyme therefore results in inhibition of cholesterol absorption. The compounds of this invention inhibit cholesterol ester hydrolase and have the formula: ##STR1## wherein Z is --Ar.sup.1, --Ar.sup.1 --Ar.sup.2, --Ar.sup.1 --O--Ar.sup.2, --Ar.sup.1 --S--Ar.sup.2, ##STR2## --Ar.sup.1 --(CH.sub.2).sub.1-20 --Ar.sup.2, --Ar.sup.1 --(CH.sub.2).sub.1-20 --O--Ar.sup.2, --Ar.sup.1 --O--(CH.sub.2).sub.1-20 --Ar.sup.2, --Ar.sup.1 --(CR.sup.6 .dbd.CR.sup.6).sub.1-3 --Ar.sup.2 or --Ar.sup.1 --NR.sup.7 --Ar.sup.2 ; andA is a hydrocarbon linking group which may be interrupted by a heteroatom or a cycloalkyl, aryl, heterocycloalkyl, or an azacycloalkyl group;and R.sup.4 and R.sup.5 are independently alkyl, alkenyl, acyl, alkoxycarbonyl or H or R.sup.4 and R.sup.

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

Abstract: This invention relates to novel compounds which have demonstrated oral antihyperglycemic activity in diabetic ob/ob and db/db mice, animal models on non-insulin dependent diabetes mellitus (NIDDM ot Type II diabetes). These compounds have the formula: ##STR1## wherein: X os O or S;n is 0, 1, or 2; ##STR2## A is ##STR3## B is 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 compounds having 5-lipoxygenase inhibiting properties and inhibition of oxidative modification of low density lipoprotein which have the formula: ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, or C.sub.1 -C.sub.6 trifluoroalkoxy;R.sub.2 is hydrogen or methyl;R.sup.4 is hydrogen, methyl or hydroxy;R.sup.5 is hydrogen, --NH.sub.2, C.sub.1 -C.sub.6 alkyl, aryl, aralkyl, or --N.dbd.C(CH.sub.3).sub.2 ;X and Y are independently O or S; and n is 0 or 1; or a pharmaceutically acceptable salt thereof. Compounds which inhibit 5-lipoxygenase are useful in the treatment of diseases mediated by leukotrienes such as inflammation or bronchoconstriction. Compounds which inhibit oxidative metabolism of low density lipoprotein are useful in the inhibition of atherosclerotic plaque formation.

Abstract: The present invention relates to novel cyclobut-3-ene-1,2-dione-3-yl substituted benzopyrans, indanes and tetrahydronaphthalenones having smooth muscle relaxant activity, pharmaceutical compositions containing them, and to their use in the treatment of diseases and disorders involving excessive smooth muscle contractions in the cardiovascular system, urinary tract, pulmonary system, or gastrointestinal tract.The compounds of this invention are represented by Formula (I): ##STR1## wherein: the substituents are as defined herein.

Abstract: This invention relates to novel 4-(3,4-dioxocyclobuten-1-yl)chromenes and dihydronaphthalenones and 3-(3,4-dioxocyclobuten-1-yl)indenes and salts thereof having smooth muscle relaxing activity, to their use in the treatment of hypertension as well as for treatment of peripheral vascular disease, congestive heart failure, disorders involving excessive smooth muscle contraction of the urinary tract such as incontinence or of the gastrointestinal tract such as irritable bowel syndrome, asthma, and hair loss and to pharmaceutical compositions containing an invention compound. The present invention discloses compounds represented by the formula (I): ##STR1## wherein: R.sub.1 and R.sub.2, independent from each other, are selected from the following: C.sub.1-6 perfluoroalkoxy, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxyl, C.sub.1-6 alkoxycarbonyl, nitro, cyano, halogen, C.sub.1-6 alkylsulfonamido, C.sub.1-6 perfluoroalkylsulfonamido, amino, C.sub.1-6 acylamino, C.sub.

Abstract: This invention relates to a technique for treating a mammal with rapamycin which comprises removal of blood from the patient, treatment of the formed blood elements with rapamycin which binds rapidly and reversibly with erythrocytes, and returning the treated blood cells to the circulatory system of the patient for the treatment of any of the diseases, syndromes, conditions, or immune responses which respond to treatment with rapamycin. Alternatively, blood to be treated with rapamycin can be obtained from a hematologically compatible donor mammal.

Abstract: This invention relates to novel compounds having antihyperglycemic properties of the formula: ##STR1## where A is ##STR2## wherein:n is 1 or 2;R.sup.1 and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkoxy, trifluoromethoxy, halogen or trifluoromethyl;R.sup.2 is hydrogen or methyl; andX is oxygen or sulfur or a pharmaceutically acceptable salt thereof.

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## or ##STR4## when X is 2-phenylethyl or 2-furanylmethyl; or a pharmaceutically acceptable salt thereof.

Abstract: This invention relates to compounds compounds useful in treating diseases mediated by one or more leukotrienes or oxidative modification of low density lipoprotein such as inflammation, bronchoconstriction or atherosclerosis. The compounds of this invention have the formula: ##STR1## wherein R.sup.1 and R.sup.3 are independently hydrogen, fluorine, chlorine, bromine, iodine, C.sub.1 -C.sub.6 alkyl, trifluoromethyl, C.sub.1 -C.sub.6 alkoxy, or C.sub.1 -C.sub.6 trifluoroalkoxy; R.sup.2 and R.sup.4 are hydrogen or methyl independently;R.sup.5 is hydrogen, methyl or hydroxy;X and Z are independently oxygen or sulfur;andY is --CH.sub.2 --, --CH(CH.sub.3)--, or --CH.dbd.CHCH(CH.sub.3)--.

Abstract: The invention relates to a process improvement for making [R-(R*,R*)]-5-[2-[5-(3-chlorophenyl)-2-oxo-3-oxazolidinyl]propyl]-1,3-benz odioxole-2,2-dicarboxylic acid dimethyl ester an intermediate used in the synthesis of beta-3 agonist, [R-(R*,R*)]-5-[2-[5-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-1,3-benz odioxole-2,2-dicarboxylic acid disodium salt.

Abstract: This invention relates to compounds having 5-lipoxygenase inhibiting properties and inhibition of oxidative modification of low density lipoprotein which have the formula: ##STR1## wherein: R.sup.1 and R.sup.3 are independently hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, or C.sub.1 -C.sub.6 trifluoroalkoxy;R.sub.2 is hydrogen or methyl;R.sup.4 is hydrogen, methyl or hydroxy;R.sup.5 is hydrogen, --NH.sub.2, C.sub.1 -C.sub.6 alkyl, aryl, aralkyl, or --N.dbd.C(CH.sub.3).sub.2 ;X and Y are independently O or S;and n is 0 or 1; or a pharmaceutically acceptable salt thereof.Compounds which inhibit 5-lipoxygenase are useful in the treatment of diseases mediated by leukotrienes such as inflammation or bronchoconstriction. Compounds which inhibit oxidative metabolism of low density lipoprotein are useful in the inhibition of atherosclerotic plaque formation.