Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives including The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.

Abstract: The invention provides coelenterazine derivatives which are substrates for a non-luminescent enzyme and a pro-substrate for a luminescent enzyme. The invention also provides a method of using the derivatives.

Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives. The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.

Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.

Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.

Abstract: The present invention provides, among other things, imidazo[1,2-?]pyrazine derivatives according for Formula (Ia) or Formula (Ib). The derivatives are useful in any method which other coelenterazines have been used. For example, the derivatives may be used in a bioluminogenic method to detect the presence of certain compounds or molecules.

Abstract: An isolated polynucleotide encoding a modified luciferase polypeptide and novel coelenterazine-based substrates. The OgLuc variant polypeptide has at least 60% amino acid sequence identity to SEQ ID NO: 1 and at least one amino acid substitution at a position corresponding to an amino acid in SEQ ID NO: 1. The OgLuc variant polypeptide has at least one of enhanced luminescence, enhanced signal stability, and enhanced protein stability relative to the corresponding polypeptide of the wild-type Oplophorus luciferase.

Abstract: The invention provides coelenterazine derivatives which are substrates for a non-luminescent enzyme and a pro-substrate for a luminescent enzyme. The invention also provides a method of using the derivatives.

Abstract: The invention relates to dipyrrometheneboron difluoride-substituted nucleotides substituted by a dipyrrometheneboron difluoride label on a phosphate moiety. The nucleotides of the invention are useful in fluorescence assays, including protein binding assays and assays for hydrolase enzymes.

Abstract: Facile syntheses for fluorinated resorcinol and aminophenol derivatives are provided that yield isomer-free products in good yield. These novel methods use generally available precursors and standard laboratory reagents and equipment to reproducibly produce these synthetically useful reagents in relatively large quantities. The resulting fluorinated resorcinols and aniinophenols possess utility in the preparation of fluorinated fluorescein and rhodol dyes.

Abstract: The family of dyes of the invention are fluoresceins and rhodols that are directly substituted on one or more aromatic carbons by fluorine. These fluorine-substituted fluorescent dyes possess greater photostability and have lower sensitivity to pH changes in the physiological range of 6-8 than do non-fluorinated dyes, exhibit less quenching when conjugated to a substance, and possess additional advantages. The dyes of the invention are useful as detectable tracers and for preparing conjugates of organic and inorganic substances.

Abstract: The invention relates to fluorescent dyes that are substituted or unsubstituted derivatives of 1-(isoindolyl)methylene-isoindole that are bound through both isoindole nitrogens to a boron difluoride moiety, forming a fluorescent dibenzopyrrometheneboron difluoride compound ##STR1## that is further substituted by bathochromic substituents that are aryl or heteroaryl moieties further substituted by an additional aryl or heteroaryl, that is itself optionally further substituted by an additional aryl or heteroaryl. These aryl and heteroaryl groups are separated by a covalent bond, or by an ethenyl, butadienyl or hexatrienyl linkage. The dyes of the invention are particularly useful as labels for carriers, particularly polymeric microparticles. The resulting microparticles have a long-wavelength fluorescence emission, and possess utility for tracing flow in biological systems, particularly in tracing blood flow.

Abstract: The invention relates to diaryl antimicrobial compounds of the general formula: ##STR1## where G, E L, J, q, m, X, Ar, W, p, n and A are as described herein, pharmaceutical compositions containing the compounds, methods for their production and their use in treating bacterial infections.

Abstract: A novel process for producing a 1-H-tetrazole-5-thiol of the formula: ##STR1## in which R.sup.1 is hydrogen; lower alkyl; lower alkyl substituted with a carboxylic acid, a carboxylic acid lower alkyl ester, or an hydroxy group; phenyl or phenyl substituted with a halogen, a lower alkyl group, or a lower alkoxy group; benzyl or benzyl substituted with a halogen, a lower alkyl group, or 1-3 alkoxy groups of 1-3 carbon atoms; or trichloroethyl,which process comprises:(a) reacting a sulfinyl or sulfonyl cyanide of the formula:RS(O).sub.n CNin whichn is 1 or 2 andR is alkyl; phenyl or phenyl substituted with a halogen, a lower alkyl group, or a lower alkoxy group; benzyl or benzyl substituted on the phenyl ring with a halogen, a lower alkyl group, or a lower alkoxy group; or an alicyclic group,with an azide of the formula R.sup.1 N.sub.5, in which R.sup.1 is as defined above, to form a 5-sulfinyl or sulfonyl-1-H-tetrazole of the formula: ##STR2## in which n is 1 or 2, andR and R.sup.

Abstract: A novel process for producing a 1-H-tetrazole-5-thiol of the formula ##STR1## in which R.sup.1 is hydrogen; lower alkyl; lower alkyl substituted with a carboxylic acid, a carboxylic acid lower alkyl ester, or an hydroxy group; phenyl or phenyl substituted with a halogen, a lower alkyl group, or a lower alkoxy group; benzyl or benzyl substituted with a halogen, a lower alkyl group, or 1-3 alkoxy groups of 1-3 carbon atoms; or trichloroethyl,which process comprises:(a) reacting a sulfinyl or sulfonyl cyanide of the formula:RS(O).sub.n CNin whichn is 1 or 2 andR is alkyl; phenyl or phenyl substituted with a halogen, a lower alkyl group, or a lower alkoxy group; benzyl or benzyl substituted on the phenyl ring with a halogen, a lower alkyl group, or a lower alkoxy group; or an alicyclic group, with an azide of the formula R.sup.1 N.sub.3, in which R.sup.1 is as defined above, to form a 5-sulfinyl or sulfonyl-1-H-tetrazole of the formula: ##STR2## in which n is 1 or 2, andR and R.sup.

Abstract: 2,6-Diaminobenzonitriles, useful in the production of N-(2-cyano-3-substituted or unsubstituted amino-phenyl)oxamate and N-(2-cyano-3-substituted or unsubstituted amino-phenyl)tetrazole-5-carboxamide antiallergy and antisecretory agents, are prepared by sequential displacement of the fluoro substituents from 2,6-difluorobenzonitrile with the appropriately substituted amine.

Abstract: The compounds of the formula ##STR1## in which R is hydrogen, halogen, alkyl, alkoxy, hydroxyl, nitro or cyano; andR.sup.2 is .dbd.O, .dbd.S, H.sub.2, --SCH.sub.3, or an amino group; with the proviso that when R is chloro in 8-position, R.sup.2 must be other than oxygen or sulfur; or a pharmaceutically acceptable salt thereof.

Abstract: The compound of formula: ##STR1## where R.sub.1 and R.sub.2 are hydrogen or alkyl;R is ##STR2## R.sub.3 and R.sub.4 are hydrogen, alkyl or alkylene; R.sub.5 and R.sub.6 are hydrogen, alkyl or alkylene;m is 1 to 6 and n is 2 to 6; and,R.sub.7 is hydrogen or alkyl;or a pharmaceutically acceptable salt thereof, are H.sub.2 -receptor antagonists useful in the treatment of peptic ulcer disease.

Abstract: The compounds ##STR1## wherein each X is, independently, --O-- or --NR.sub.5, in which R.sub.5 is hydrogen or alkyl; R is alkyl, R.sub.1 is hydrogen or alkyl, R.sub.2 is hydrogen, hydroxy, amino, alkylamino, dialkylamino or alkanoylamino and when m or n is O, R.sub.2 is hydroxymethyl, aminomethyl, alkylaminomethyl, dialkylaminomethyl or alkanoylaminomethyl; R.sub.3 is hydrogen, --CN, --CONH.sub.2 or --CO.sub.2 M in which M is hydrogen, alkyl or ##STR2## in which p is an integer from 2 to 6 and R.sub.6 and R.sub.7 are, independently, hydrogen or alkyl; R.sub.4 is --NH.sub.2, --NHCOR.sub.8 in which R.sub.8 is alkyl, --NHCOCO.sub.2 Z or --NHCOCH.sub.2 CH.sub.2 CO.sub.2 Z in which Z is hydrogen or alkyl; m and n are 0, 1, 2, 3 or 4 such that when n is from 1 to 4, m is 0 or 1 and when m is from 1 to 4, n is 0 or 1; or pharmaceutically acceptable salts thereof are leucotriene antagonists useful as antiallergy agents.

Abstract: Compounds of the formula ##STR1## wherein A is a moiety of the formula ##STR2## in which R.sub.1 and R.sub.2 may be hydrogen, lower alkyl, lower alkoxy, halogen or thioalkyl; andZ is O or S;R is an amine selected from the group ##STR3## wherein R.sub.3 and R.sub.4 may be hydrogen, lower alkyl, cycloloweralkyl or R.sub.3 and R.sub.4 taken together form an N-containing heterocycle of 2-7 carbon atoms;a=b=c=1-5; andpharmaceutically acceptable salts thereof have H.sub.2 --antagonist activity.The compounds can be used in the treatment of ulcers.