Abstract: Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.

Abstract: The present invention provides processes which are flexible, cost effective, and commercially viable methods of manufacturing or producing products from 2-hydroxyacetophenone (2-HAP).Of particular interest of the available products are 4-hydroxycoumarin, warfarin-alkali salt, preferably warfarin sodium and warfarin-alkali salt-isopropyl alcohol (2-propanol) complex, more preferably warfarin-sodium-isopropyl alcohol complex.As is known, these compounds are useful as vitamin K dependent anticoagulants in the treatment of humans and animals. In different doses, they are also useful as rodenticide.The inventive process involves contacting 2-HAP, carbonate ester and effective base followed by treatment with an unsaturated ketone and phase transfer catalyst to ultimately yield product.

Abstract: Optically active or racemic compounds represented by the formula ##STR1## where R.sub.1 is C.sub.1 to C.sub.4 straight chain or branched alkyl; R.sub.2 is selected from the group consisting of H, --OR.sub.1, --SR.sub.1, --NH(R.sub.1), --N(R.sub.4)(R.sub.5), aminocarbonyl, halogen, and --CN, where R.sub.4 and R.sub.5 are independently C.sub.1 to C.sub.6 straight chain or branched alkyl, or taken together form a 3- to 7-membered heterocycloalkyl substituent, such heteroatom selected from the group consisting of oxygen, nitrogen and sulfur, optionally including an additional heteroatom which is selected from the group consisting of nitrogen, oxygen, and sulfur; R.sub.3 is cyclopentyl or: ##STR2## where R' and R" are independently H, .dbd.O, --OH, or --NH.sub.2, with the proviso that R' and R" can be taken together form the following structure as R.sub.3 : ##STR3## where R'" is --OH or --NH.sub.2 ; and with the further proviso that when R.sub.3 is cyclopentyl or norbornyl, then R.sub.

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: 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: 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: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

Abstract: Methods of treating chronic arthritis and osteoporosis which utilize both known and novel compounds which would fall under the general formula:(HO)p--A--[--OS(O).sub.2 NR.sup.1 R.sup.2 ].sub.zwherein A encompasses a wide range of values including but not limited to aryl, loweralkyl, cycloalkyl, and carbohydrates including sucrose and fructose; p is equal to the number of unreacted hydroxy groups contained on the molecule and may be zero; z is the number of --OS(O).sub.2 NR.sup.1 R.sup.2 groups and is always at least one; R.sup.1 and R.sup.2 are selected from hydrogen, loweralkyl, carboxy and the like; a novel process for preparing the compounds is provided wherein an appropriate sulfamic acid aryl ester is reacted with a hydroxy substituted A radical which may or may not contain thereon protected carboxyl, amino or hydroxy substituents, in an aprotic solvent containing a tertiary amine base. Pharmaceutical compositions for the treatment of chronic arthritis and osteoporosis are also provided.

Abstract: Disclosed are novel substituted 4-thiazolidinone derivatives having cyclooxygenase and 5-lipoxygenase inhibiting properties and which are topical antiinflammatory agents for inflammed conditions of the skin having the formula: ##STR1## wherein R is hydrogen or loweralkyl; R.sup.1 is loweralkyl or aryl; X is --(CH.sub.2)-aryl, --O--(CH.sub.2).sub.0-3 -aryl, --C(O)(CH.sub.2).sub.0-3 -aryl, --CH(OH)--(CH.sub.2).sub.0-3 -aryl or 3,4 ##STR2## (to form naphthyl ring); aryl is phenyl, substituted phenyl, or 2,3 or 4 pyridyl; W is oxygen; Q is -(alk.sup.1).sub.0-1 --(O).sub.0-1 --(B).sub.0-1 --(alk.sup.2).sub.0-1 --[C(O)Z].sub.0-1 ; B is ##STR3## Z is OR.sup.3 or NR.sup.4 R.sup.5 where R.sup.3 is hydrogen, loweralkyl, or a pharmaceutically acceptable metal cation, R.sup.4 and R.sup.5 are hydrogen or loweralkyl; alk.sup.1 and alk.sup.

Abstract: Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula:(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO.sub.2 NR.sup.1 R.sup.2) wherein R.sup.1 and R.sup.2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O.sub.2)NR.sup.1 R.sup.2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.

Abstract: 3-Aryl-2,1-benzisoxazole compounds having the formula: ##STR1## wherein R.sup.1 and R.sup.2 are hydrogen or methyl;R.sup.3 and R.sup.4 are hydroxyl, loweralkoxy, amino or --OM wherein M is a pharmaceutically acceptable cation;X is hydrogen, halogen, loweralkyl or nitro;Y is selected from hydrogen, halogen, loweralkyl, loweralkoxy, nitro or trifluoromethyl;n and p are zero or one with the proviso that either n or p must be oneare disclosed, having anti-inflammatory activity and novel intermediates in the preparation thereof.