Abstract: The disclosed hexenoic acid side-chain derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil, including immune, inflammatory, tumor, proliferative, viral or psoriatic disorders.

Abstract: 5-HT.sub.3 receptor antagonist compounds of Formula I: ##STR1## in which X and Y are independently selected from hydrogen, halogen, hydroxy, lower alkoxy, lower alkyl, nitro, amino, aminocarbonyl, (lower alkyl)amino, di(lower alkyl)amino and (lower alkanoyl)amino;R.sup.1 is hydrogen, lower alkyl, phenyl or halogen;R.sup.

Abstract: This invention pertains to methods to detect a compound in the presence of a homolog that is immunologically related to the analyte. The invention is particularly suited for the detection of homocysteine in the presence of cysteine. The methods of this invention involve chemically modifying both the analyte and the homolog to increase their immunogenicity and facilitate antibody recognition. More importantly, this modification is done to make these compounds immunologically distinct. Antibodies to the immunologically distinct compounds are then prepared. An assay protocol comprises chemically modifying the analyte and homolog and then immunochemically detecting the modified analyte by means of the aforementioned antibodies.

Abstract: The disclosed derivatives of 8-phenylcyclopentenoquinolines and 8-phenylcyclohexenoquinolines are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft, rejection agents, anti-graft-vs-host disease agents, anti-allergic agents, bronchodilation agents, anti-autoimmune agents, and analgetic agents.

Abstract: Mycophenolate mofetil, mycophenolic acid, and ranolazine can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil, mycophenolic acid, or ranolazine liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.

Abstract: A controlled release pharmaceutical composition comprising a physiologically active agent dispersed in preformed porous polymeric microparticles is provided. The active agent concentration may be up to about 10% by weight to achieve controlled release. Each of the porous microparticles has a plurality of preformed pores into which active agent is loaded and from which the active agent is subsequently released to the environment of use. The compositions are capable of delivering physiologically effective amounts of active agent for at least about thirty days, which delivery may be reversibly controlled by exposure to ultrasound.

Abstract: A method is disclosed for conducting an assay for an analyte. The method comprises causing a specific binding pair member in a first aqueous medium to become bound to a first bibulous member by contacting a portion of the first bibulous member with the medium. The first bibulous member is in liquid receiving relationship with an absorbent member. The contacting is carried out under conditions wherein the first medium traverses the first bibulous member and at least a portion of the absorbent member by capillary action. The method further comprises causing the first bibulous member to come into liquid receiving relationship with a second bibulous member. A reagent in a second aqueous medium is absorbed by and preferably becomes non-diffusively bound to the second bibulous member in relation to the presence of analyte in the first medium.

Abstract: The present invention relates to a process for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such process.

Abstract: The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula I, ##STR1## wherein: R.sub.1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; andR.sub.2 is aryl; or a pharmaceutically acceptable salt or N-oxide thereof are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft rejection agents, anti-graft-vs-host disease agents, anti-allergic agents (e.g., asthma, rhinitis and atopic dermatitis), bronchodilation agents, anti-autoimmune agents or analgetic agents.

Abstract: An apparatus for maintaining a biological sample on a support is disclosed. The apparatus comprises a hollow chamber with internal and external surfaces and a first and second end. The first end is open and is adapted for attachment to a first closure member. The second end is either closed or open. If open, the second end is adapted for attachment to a second closure member. The apparatus provides for maintaining the support in contact with a liquid medium at all times regardless of the orientation of the apparatus. In a preferred embodiment, the apparatus provides for maintaining the original orientation of a non-integral support regardless of the orientation of the apparatus. The apparatus is useful for isolating and culturing microorganisms.

Abstract: A compound of the formula ##STR1## wherein: R.sup.1 is independently selected from hydrogen, lower-alkyl, cycloalkyl, cycloalkyl lower-alkyl, lower-alkoxy, formyl, (lower-alkyl)-hydroxylmethyl, aryl, benzyl, arylmethyl, pyridylmethyl,where aryl, benzyl, arylmethyl and pyridylmethyl are unsubstituted or independently mono, di or tri substituted with hydrogen, hydroxy, thiol, amino, halo, nitro, lower-alkylthio, lower-alkoxy, mono-lower-alkylamino, di-lower-alkylamino, hydroxycarbonyl, lower-alkoxycarbonyl, hydroxysulfonyl, lower-alkoxysulfonyl, lower-alkylsulfonyl, lower-alkylsulfinyl, trifluoromethyl, cyano, tetrazoyl, carbamoyl, lower-alkylcarbamoyl, and di-lower-alkylcarbamoyl; andR.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as set forth in the specification.

Abstract: Mycophenolate mofetil and mycophenolic acid can be conveniently manufactured into high dose oral formulations by the hot melt filling of a supercooled mycophenolate mofetil or mycophenolic acid liquid into a pharmaceutical dosage form. High dose oral pharmaceutical formulations and manufacturing methods therefor are disclosed.

Abstract: Methods are disclosed for conducting assays. One such method comprises providing in combination a first bibulous member zone ("first zone") and a liquid medium containing a component. The first zone has non-diffusively bound thereto a reagent interreactive with the component. Conditions are selected wherein the liquid medium and at least a portion of the component contained therein traverse all of the first zone and migrate by capillary migration into a second bibulous member zone ("second zone"). The second zone is of a different composition than the first zone and is incapable of specifically binding the component except when an analyte is to be detected and the method further includes causing a reagent to become bound to the first bibulous member zone in relation to the amount of analyte present.

Abstract: A D-arabinitol dehydrogenase enzyme is disclosed. The enzyme is capable of catalyzing the oxidation of D-arabinitol and substantially incapable of catalyzing the oxidation of D-mannitol and is substantially free of other enzymes capable of oxidizing D-mannitol. Also disclosed are methods for determining D-arabinitol. In one embodiment the method comprises the steps of providing in combination (1) a medium suspected of containing D-arabinitol and (2) a D-arabinitol dehydrogenase enzyme and examining the medium for the product of the oxidation of the D-arabinitol. The enzyme utilized is capable of catalyzing the oxidation of D-arabinitol and substantially incapable of catalyzing the oxidation of D-mannitol. Kits for conducting the present method are also disclosed. The D-arabinitol dehydrogenase in purified form has all of the characteristics of a D-arabinitol dehydrogenase which is obtainable from Candida tropicalis ATCC 750 or Candida shehatae.

Abstract: Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine;X and X' are H, OH or F, provided that at least one is H;Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H;Y' and Z together form a cyclic phosphate ester, provided that Y is H; orZ is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, andwhen X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine;and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.

Abstract: Compounds of the Formula: ##STR1## wherein: R.sup.1-7 are as defined in the specification. The compounds and salts exhibit useful pharmacological properties, including potassium channel activating properties and 5-lipoxygenase inhibiting properties, and in particular are useful as smooth muscle relaxants and bronchodilators.

Abstract: Methods and compositions are disclosed for determining a peroxidatively active substance (PAS). The methods comprise the step of detecting a fluorescent signal produced upon cleavage of a compound of the formula F-L-Q, wherein F is a fluorescer capable of producing the signal, Q is a quencher capable of quenching the signal when linked to F, and L is a bond, or a linking group having a bond, wherein the bond is capable of being cleaved by a reaction of the PAS with a substrate of the PAS and a hydrogen donor wherein the cleavage of the bond substantially reduces the quenching. The methods have application in a wide variety of systems including assays and improved assays for analytes. Also disclosed are kits for conducting the methods and improvements in accordance with the present invention.

Abstract: This invention relates to oligonucleotides having at least one nucleotide that is substituted at the 4' position of the sugar moiety with a substituent other than hydrogen. These oligonucleotides are useful in hybridization assays and as therapeutic agents.

Abstract: The present invention relates to processes for preparing 1-butyl-2-[2'-(2H-tetrazol-5-yl)biphenyl-4-ylmethyl]-1H-indole-3-carboxyli c acid and to intermediates useful in such processes. The present invention also relates to a process for deprotecting compounds containing a protected 2H-tetrazolyl group, which process comprises reacting a the protected compound with a Lewis acid in the presence of a thiol.

Abstract: The disclosed 6-substituted derivatives of mycophenolic acid are therapeutic agents advantageous in the treatment of disease states indicated for mycophenolic acid and/or mycophenolate mofetil.