Abstract: Compounds of formula (I), and their pharmaceutically acceptable derivatives, wherein R.sup.1 and R.sup.2 are optional substituents and independently represent C.sub.1-6 alkyl, C.sub.2-6 alkenyl [optionally substituted by CO.sub.2 H or CO.sub.2 (C.sub.1-6 alkyl)], C.sub.2-6 alkynyl, halogen, C.sub.1-3 perfluoroalkyl, (CH.sub.2).sub.m Ar.sup.1, (CH.sub.2).sub.m Het.sup.1, (CH.sub.2).sub.m CONR.sup.7 R.sup.8, (CH.sub.2).sub.m CO.sub.2 R.sup.8, O(CH.sub.2).sub.q CO.sub.2 R.sup.8, (CH.sub.2).sub.m COR.sup.8, (CH.sub.2).sub.m OR.sup.8, O(CH.sub.2).sub.p OR.sup.8, (CH.sub.2).sub.m NR.sup.7 R.sup.8, CO.sub.2 (CH.sub.2).sub.q NR.sup.7 R.sup.8, (CH.sub.2).sub.m CN, S(O).sub.n R.sup.8, SO.sub.2 NR.sup.7 R.sup.8, CONH(CH.sub.2).sub.m Ar.sup.1 or CONH(CH.sub.2).sub.m Het.sup.1 ; R.sup.3 represents H, C.sub.1-6, alkyl, (CH.sub.2).sub.p NR.sup.9 R.sup.10, SO.sub.2 R.sup.10, SO.sub.2 NR.sup.9 R.sup.10, (CH.sub.2).sub.m COR.sup.10, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, (CH.sub.2).sub.m CONR.sup.9 R.sup.10, (CH.sub.2).sub.

Abstract: The invention relates to compounds of the formula (I) ##STR1## and pharmaceutically acceptable salts thereof, wherein Ar, Z and Het are as defined herein. The compounds of formula (I) possess activity as antifungal agents. The invention also relates to pharmaceutical compositions containing said compounds of formula (I) and to methods of treating fungal infections by administering said compounds of formula (I).

Abstract: A method of and apparatus for spectrophotometrically analyzing a tablet by NIR transmission measurements includes a tablet holder 1 having a recess 5 within which a tablet 20 is located. A probe 40 is applied to the tablet 20 to direct an NIR beam 45 to and through the tablet for sensing at a detector 32 from which measurements characteristics of the tablet are analyzed. The recess 5 accommodates the tablet 20 as a close, possibly complementary fit. The tablet is clamped in the recess 5 by a spring loaded rod 8 to ensure that the tablet is located and retained at a predetermined position in the recess 5 relative to an aperture 7 through which the transmitted beam is directed to the detector 32. Preferably the tablet 20 is subjected to clamping forces applied by two spring loaded clamping rods disposed substantially perpendicularly relative to each other in the tablet holder.

Abstract: A process of purifying a (6-chloro-2-carbazolyl)methyl-malonic acid di(C.sub.1 -C.sub.6 alkyl) ester of Formula (I): ##STR1## wherein R.sub.a and R.sub.b must be the same and are selected from the group consisting of C.sub.1 -C.sub.6 alkyl; comprises phase separating one or more impurities from said carbazole ester at least once wherein the solvent used to carry out said phase separation is acetic acid. In a preferred embodiment said acetic acid is glacial acetic acid which is maintained at a temperature of from about 30.degree. to about 110.degree.0 C. and said carbazole ester is obtained in a purity of at least 99.90% by weight, so that the amount of impurities present therein is 0.10% or less by weight. In a more preferred embodiment of said process, said temperature is from about 50.degree. to about 70.degree. C., and said phase separation is carried out only once.

Abstract: The invention relates to processes and intermediates for preparing compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R, R.sup.1, R.sup.2, and R.sup.3 are as defined herein. The above compounds of formula (I) are selective inhibitors of phosphodiesterase type IV and the production of tumor necrosis factor, and therefore may be used in the treatment of various inflammatory disorders such as asthma, joint inflammation, and other conditions or diseases.

Abstract: The invention relates to the trihydrate of the mesylate salt of (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propano l, pharmaceutical compositions containing said compound and methods of treating disorders of the central nervous system by administering said compound.

Abstract: The present invention relates to certain compounds of the formula (I), ##STR1## which are useful in the synthesis of certain .beta.-adrenergic receptor agonists. The invention also relates to a process for synthesizing the compounds of formula (I) and to compounds of the formula (II), ##STR2## wherein R.sup.1, R.sup.2 and R.sup.4 are defined herein, which are useful in the synthesis of the compounds of formula (I). The invention also relates to a process for synthesizing a compound of formula (II). The invention further relates to processes for synthesizing compounds of formula (Z*), ##STR3## R.sup.1, R.sup.2 and Y.sup.2* are defined herein.

Abstract: A process for resolving 1-azabicyclo[2.2.2]octan-3-amine, (2-diphenylmethyl)-N-[[2-methoxy-5-(1-methylethyl)phenyl]methyl] in which 1-azabicyclo[2.2.2]octan-3-amine, (2-diphenylmethyl)-N-[[2-methoxy-5-(1-methylethyl)phenyl]methyl] is reacted with 1R-(-)-10-camphorsulfonic acid in a solvent capable of dissolving both the foregoing reactants and selectively dissolving the camphorsulfonic acid salt of the corresponding (2R, 3R) enantiomer relative to the (2S, 3S) enantiomer.

Abstract: The enantioselective borane reduction of prochiral ketones to optically pure alcohols is effectively achieved by performing the reduction in the presence of catalytic amounts of the new and valuable oxazaborolidine compounds of formulae (I) and (II). The compounds of formulae (I) and (II) may be isolated and purified prior to use in the reduction reactions or the compounds of formulae (I) and (II) may be generated in situ.

Abstract: A compound of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.9 and R.sup.10 are as defined above The compound of formula I and the pharmaceutically acceptable salts thereof are useful in inhibiting phosphodiesterase (PDE) type IV and the production of tumor necrosis factor (TNF) and in the treatment of asthma, arthritis, bronchitis, chronic obstructive airways disease, psoriasis, allergic rhinitis, dermatitis and other inflammatory diseases characterized by phosphodiesterase (PDE) Type IV activity as well as AIDS, sepsis, septic shock and other diseases, such as cachexia, involving the production of TNF.

Abstract: A compound of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.17, R.sup.18 and R.sup.1 are as defined below. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.

Abstract: The present invention relates to the use of certain .beta.-adrenergic agonists to reduce a wasting condition in a mammal (e.g., human).

Abstract: A parenteral formulation for 25-cyclohexyl-avermectin Bl, compound (I), which is effective against both internal and external parasites, is well tolerated by animals on both subcutaneous and intramuscular administration and is compatible with conventional injection equipment. ##STR1## The solution comprises compound (I), in a solvent consisting of from 50 to 95% by volume of sesame oil with the remainder ethyl oleate.

Abstract: This invention provides a process for producing a macrocyclic lactone compound, which comprises cultivating Actinoplanes sp. FERM BP-3832, in the presence of L-proline, L-hydroxyproline or L-nipecotic acid, and then isolating a macrocyclic lactone compound from the fermentation broth. The compounds produced by this process include a compound of formula (I). The present invention also relates to a pharmaceutical composition comprising the same, which is useful as immunosuppressive, antimycotic, antitumor agent or the like.

Abstract: A process for preparing the compound of formula (1) is disclosed. ##STR1## The starting materials are an N-triazolylmethyl-6-aminoisoquinoline and a 4-biphenyl-2-carboxylic acid derivative.

Abstract: Substituted tetralins, chromans and related compounds which, by inhibiting 5-lipoxygenase enzyme and/or blocking leukotriene receptors, are useful in the prevention or treatment of asthma, arthritis, psoriasis, ulcers, myocardial infarction and related disease states in mammals, pharmaceutical compositions thereof, a method of treatment therewith, and to intermediates useful in the synthesis thereof.

Abstract: This invention relates to certain 5-acyl-2-oxo-indole-3-carboxamides useful as inhibitors of glycogen phosphorylase, methods of treating glycogen phosphorylase dependent diseases or conditions with such compounds and pharmaceutical compositions comprising such compounds. This invention also relates to pharmaceutical compositions comprising those 5-acyl-2-oxo-indole-3-carboxamides in combination with antidiabetes agents and methods of treating glycogen phosphorylase dependent diseases or conditions with such compositions.

Abstract: The fumarate salt of (R)-5-(methylaminosulphonylmethyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-in dole, useful in the treatment of migraine.

Abstract: Compounds of the formula ##STR1## wherein A, B, D, E, and F are each independently nitrogen or carbon; R.sub.1 is hydrogen, C.sub.1 to C.sub.6 alkyl, --(CH.sub.2).sub.n R.sub.7, or C.sub.1 to C.sub.3 alkyl-aryl; R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are each independently hydrogen, C.sub.1 to C.sub.6 alkyl, aryl, C.sub.1 to C.sub.3 alkyl-aryl, halogen, cyano, nitro, --(CH.sub.2).sub.m NR.sub.8 R.sub.9, --(CH.sub.2).sub.m OR.sub.9, --SR.sub.9, --SO.sub.2 NR.sub.8 R.sub.9, --(CH.sub.2).sub.m NR.sub.8 SO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.8 CO.sub.2 R.sub.9, --(CH.sub.2).sub.m NR.sub.8 COR.sub.9, --(CH.sub.2).sub.m CONR.sub.7 R.sub.9, or --(CH.sub.2).sub.m CO.sub.2 R.sub.9 ; R.sub.2 and R.sub.3, R.sub.3 and R.sub.4, R.sub.4 and R.sub.5, and R.sub.5 and R.sub.

Abstract: A compound of the formula ##STR1## wherein n, X, R.sup.3, R.sup.4 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, restenosis, periodontal disease, epidermolysis bullosa, scleritis and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF.