Abstract: The present invention relates to optionally substituted pyrido[2,3-d]pyrimidine-2,4(1H,3H)-diones or optionally substituted pyrido[2,3-d]pyrimidine-2(1H,3H)-ones, i.e., compounds of Formula I: ##STR1## wherein: Y is --CH.sub.2 -- or --C(O)--;R.sup.1 is hydrogen or --(CH.sub.2).sub.n --R.sup.7, wherein:R.sup.7 is aryl or heteroaryl, andn is 1 or 2,provided that when Y is --C(O)--, R.sup.7 is heteroaryl; andR.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are hydrogen, or one is selected from lower alkyl, halo, carboxy, methoxycarbonyl, carbamoyl, methylcarbamoyl, di-methylcarbamoyl, methylcarbonyl, methylthio, methylsulfinyl, methylsulfonyl, hydroxymethyl, amino, trifluoromethyl, cyano or nitro; orR.sup.2, R.sup.3, R.sup.4 and R.sup.5 are independently selected from hydrogen, lower alkyl, nitro, chloro, fluoro, methoxycarbonyl or methylcarbonyl, provided at least one is hydrogen, and R.sup.6 is hydrogen;or a pharmaceutically acceptable ester, ether or salt thereof.

Abstract: A method and device for determining the presence of an analyte in a sample suspected of containing the analyte is disclosed. The method involves contacting a test solution containing the sample, an antibody for the analyte, and a conjugate of the analyte and a label with a contact portion of a strip of bibulous material capable of being traversed by the test solution through capillary action. The strip contains a first receptor capable of binding to said conjugate. The first receptor is non-diffusively bound to a situs on the strip separate from the contact portion of the strip. The strip further contains a second receptor capable of binding the antibody to the analyte between the situs and the contact portion. The second receptor is non-diffusively bound to the strip. At least a portion of the test solution is allowed to traverse the strip by capillary action and thereby contact the situs.

Abstract: Methods and devices for permitting capillary flow of liquid between two or more pieces of bibulous material which, prior to actuation, are in a non-capillary flow relationship. In particular, the device is actuated and a capillary flow relationship is initiated between the two or more pieces of bibulous material in non-capillary flow relationship by utilizing a liquid expandable piece of bibulous material.

Abstract: A method and device for determining the presence of an analyte in a sample suspected of containing the analyte is disclosed. The method involves contacting a test solution containing the sample, an antibody for the analyte, and a conjugate of the analyte and a label with a contact portion of a piece of bibulous material capable of being traversed in at least one direction by the test solution through capillary action. The bibulous material contains a first receptor capable of binding to said conjugate. The first receptor is non-diffusively bound to a situs on the bibulous material separate from the contact portion. The bibulous material further contains a second receptor capable of binding the antibody to the analyte between the situs and the contact portion. The second receptor is non-diffusively bound to the bibulous material. At least a portion of the test solution is allowed to traverse the bibulous material by capillary action and thereby contact the situs.

Abstract: A nucleotide sequence characteristic of Neisseria gonorrhoeae is disclosed. The sequence can be the basis for hybridization type, nucleic acid-based, rapid, in vitro diagnostic assays. The unique nature of the sequence makes it possible to clearly discriminate N. gonorrhoeae from other Neisseria species thus eliminating or substantially reducing the number of false positive readings. A 350 base pair N. gonorrhoeae DNA restriction fragment was cloned after subtractive hybridization to Neisseria meningitidis DNA. In further cloning experiments the sequences adjacent to the original 350 base pair fragment were determined. A portion of this sequence was shown to detect 105 of 106 N. gonorrhoeae strains and no other Neisseria species. In addition to use as detection probes, all or portions of the nucleotide sequence can be used as a ligand for the sandwich capture of N. gonorrhoeae sequences and as primers for in vitro amplification of N. gonorrhoeae sequences.

Abstract: A kit for inactivating interfering binding proteins in a immunoassay for a member of a specific binding pair (sbp). The method comprises including in an assay medium containing a sample suspected of containing an sbp member and an interfering binding protein an effective amount of a water soluble compound having two substituted or unsubstituted phenyl groups linked to a common atom. When the sbp member or its sbp partner has two phenyl groups linked to a common atom, the compound has a number of-groups other than hydrogen attached to the phenyl groups and the atom that differs by at least two from the number of such groups on the sbp member. When the sbp member or its sbp partner has two phenyl groups linked to a common atom and the binding protein is not an antibody, the compound has only one group other than hydrogen attached to a phenyl group or the common atom.

Abstract: Substituted imidazolyl-alkyl-piperazine and diazepine derivatives of Formula A: ##STR1## wherein: R.sup.1 is aryl, lower alkyl, cycloalkyl or hydrogen;R.sup.2 is aryl, lower alkyl or hydrogen;R.sup.3 is lower alkyl, hydroxy, or hydrogen;R.sup.4 is aryl or hydrogen;R.sup.5 is aryl or hydrogen;m is two or three;n is zero, one or two, provided that when R.sup.3 is hydroxy, n is oneor two; andq is zero, one, two, or three;and the pharmaceutically acceptable salts thereof, are calcium channel antagonists useful for treating mammals having a variety of disease states, such as stroke, epilepsy, hypertension, angina, migraine, arrhythmia, thrombosis, embolism and also for treatment of spinal injuries.

Abstract: Compounds of the Formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl of 3 to 8 carbon atoms;R.sup.3 is fluoro lower alkyl; cyano; or nitro;R.sup.4 is ##STR2## R.sup.5 and R.sup.6 are independently hydrogen or lower alkyl; and R.sup.7 is --NR.sup.8 R.sup.9 ; wherein:R.sup.8 is hydrogen; lower alkyl; lower alkoxy; hydroxy; or hydroxy lower alkyl; andR.sup.9 is hydrogen; lower alkyl; hydroxy lower alkyl; --SO.sub.2 R.sup.10 ; --CO.sub.2 R.sup.10 ; --C(O)NR.sup.11 R.sup.12 ; --C(S)NR.sup.11 R.sup.12 ; or --C(O)R.sup.12 ;whereinR.sup.10 is lower alkyl;R.sup.11 is hydrogen or lower alkyl; andR.sup.12 is hydrogen, lower alkyl, or fluoro lower alkyl;with the proviso that R.sup.8 and R.sup.9 cannot both be hydrogen; and the pharmaceutically acceptable salts thereof.

Abstract: Compounds useful as antiviral agents are defined by the following formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen or --C(O)R.sup.7 wherein R.sup.7 is hydrogen, alkyl of one to nineteen carbon atoms, hydroxyalkyl of one to eight carbon atoms, alkoxyalkyl of two to nine carbon atoms, alkenyl of two to nineteen carbon atoms, phenyl, 1-adamantyl or 2-carboxyethyl and the pharmaceutically acceptable alkali metal salts thereof;R.sup.2 is --C(O)R.sup.7 wherein R.sup.7 is as defined above;R.sup.3 is hydrogen, halo, thio, lower alkylthio of one to six carbon atoms, azido, NR.sup.9 R.sup.10 wherein R.sup.9 and R.sup.10 are independently hydrogen or lower alkyl of one to six carbon atoms or --NHC(O)R.sup.8 wherein R.sup.8 is hydrogen, alkyl of one to nineteen carbon atoms or 1-adamantyl; and(a) R.sup.6 is hydrogen, halo, lower alkoxy of one to six carbon atoms, azido, thio, lower alkylthio of one to six carbon atoms, --NR.sup.9 R.sup.10 wherein R.sup.9 and R.

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: This invention relates to a novel process for making an allenic prostanoic acid derivative in the form of a single stereoisomer, or a mixture of stereoisomers, represented by the formula (I): ##STR1## wherein R is lower alkyl, R.sup.1 is a protecting group which can be selectively removed in the presence of R.sup.2, R.sup.2 is an acid-labile, base-stable protecting group, X is --(CH.sub.2).sub.2 --, trans --CH.dbd.CH-- or --C.tbd.C--, Y is --C(R.sup.3)(OR.sup.2)CH.sub.2 --, in which --OR.sup.2 is in the .alpha. or .beta. configuration and R.sup.3 is hydrogen or methyl, Z is alkyl, or phenyl, benzyl or phenoxy each optionally substituted on the phenyl ring, and the wavy lines represent the .alpha. or .beta. configuration with the proviso that when one wavy line is .alpha. the other is .beta..

Abstract: Mycophenolate mofetil is made non-catalytically by refluxing mycophenolic acid with 2-morpholinoethanol in an inert organic solvent capable of azeotropic removal of water.

Abstract: A method for determining the presence of a predetermined minimum detectible amount of one or more analytes in a sample suspected of containing the analyte is disclosed. Each analyte is a member of a specific binding pair ("sbp member") consisting of ligand and its complementary receptor. The method comprises contacting with a test solution containing said sample and predetermined amounts of two or more of a plurality of first sbp members, each respectively analogous to one of said analytes, a contact portion of a piece of bibulous material capable of being traversed in at least one direction by the test solution by capillary migration. The bibulous material contains predetermined amounts of two or more of a plurality of second sbp members, each respectively capable of binding one of the analytes and corresponding first sbp member.

Abstract: There is disclosed a process for the extraction of volatile solvents entrained in a polymer-based pharmaceutical composition designed for sustained release of drug over an extended period of time prepared in microcapsule form wherein the composition comprises at least one hormonally active water-soluble polypeptide in an effective amount greater than a conventional single dose and a biocompatible, bioerodable encapsulating polymer, which process comprises the steps of contacting the composition to a stream of dense gas, that is, pressurized gas and then removing the dense gas, and volatile solvents contained therein, extracted from the pharmaceutical composition.

Abstract: The invention provides a process for preparing single enantiomers of compounds represented by the formula: ##STR1## and chiral acid addition salts thereof; wherein: X and Y are independently hydrogen; lower alkyl; lower alkoxy; or halo; or X and Y taken together is methylenedioxy or ethylene-1,2-dioxy;which includes reduction of a compound represented by the formula: ##STR2## to give a mixture of stereoisomers represented by the formula: ##STR3## wherein each wavy line independently represents a bond in either the .alpha. or .beta. position;followed by dissolving the mixture of stereoisomers and a chiral resolving acid in a suitable solvent and allowing the solution to crystallize, giving a salt of the desired enantiomer.

Abstract: Compounds of the formula ##STR1## wherein: m is an integer of 1-6;n is an integer of 1 or 2;X and Y are independently hydrogen; hydroxy; lower alkyl; lower alkoxy; or halo; or X and Y when adjacent and taken together are methylenedioxy or ethylene-1,2-dioxy;R is ##STR2## wherein: R.sup.1 and R.sup.2 are independently hydrogen or lower alkyl, or when taken together with the carbon to which they are attached are cycloalkyl;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, hydroxy, trifluoromethyl or halo; and ##STR3## and pharmaceutically acceptable acid addition salts thereof. The compounds and salts exhibit useful pharmacological properties, including selective .alpha..sub.2 -adrenoceptor antagonist properties and 5-HT.sub.1A receptor partial agonist properties, and are particularly useful for the treatment of sexual dysfunction, depression and anxiety.

Abstract: Intermediates and methods for producing intermediates for use in preparing 9-(1,3-dihydroxy-2-propoxymethyl)-guanine and esters and ethers thereof.

Abstract: Receptors are disclosed that are antibodies that exhibit a binding affinity for an immune complex of a monoepitopic antigen and an antibody for such antigen that is substantially greater than the binding affinity for the monoepitopic antigen or the antibody for the monoepitopic antigen apart from the immune complex. In one embodiment the receptors are antibodies prepared against an affinity-labeled complex of an antigen and an antibody for the antigen. Normally, the monoepitopic antigen has a molecular weight less than 1500 and is an organic compound. The antibodies of the present invention find use in a method for determining a monoepitopic antigen in a sample suspected of containing such antigen. The method comprises forming an immune sandwich complex comprising the monoepitopic antigen or an analog thereof, a first monoclonal antibody that binds to the monoepitopic antigen, and a second monoclonal antibody that is an antibody of the present invention and detecting the immune sandwich complex.

Abstract: In a process for the solid phase synthesis of a polypeptide containing at least one serine residue, the improvement comprising temporarily protecting the side chain of the serine residue with a protecting group which is removed immediately following the addition of the serine to the peptide chain.

Abstract: Compound of the Formula (I), (II), or (III): ##STR1## wherein: R.sup.1 is lower alkyl or 2"-(1H-tetrazol-5-yl)biphenyl-4'-ylmethyl;R.sup.2 is lower alkyl when R.sup.1 is 2"-(1H-tetrazol-5-yl)biphenyl-4'-ylmethyl; or R.sup.2 is 2"-(1H-tetrazol-5-yl)biphenyl-4'-ylmethyl when R.sup.1 is lower alkyl;R.sup.3 is hydrogen or lower alkyl;X is hydrogen, lower alkyl, halogen, --C(O)CF.sub.3, --CO.sub.2 R.sup.4, or --C(O)NR.sup.5 R.sup.6 ;Y is hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen, or --CO.sub.2 R.sup.4 ;Z is hydrogen, lower alkyl, lower alkoxy, or halogen; with the proviso that Y and Z cannot be attached to the nitrogen atom in Formula (II); whereinR.sup.4 is hydrogen or lower alkyl;R.sup.5 is hydrogen or lower alkyl;R.sup.6 is hydrogen or lower alkyl; orR.sup.5 and R.sup.6 taken together with the nitrogen to which they are attached represent a heterocycle;and pharmaceutically acceptable salts thereof, exhibit useful pharmacological properties, and are particularly useful as angiotensin II antagonists.