摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
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.
摘要:
N-Protected-tetrazole-5-carboxylic acid derivatives of the formula: ##STR1## in which R is --OM, halo or lower alkoxy wherein M is hydrogen, an alkali metal or an alkaline earth metal; andR.sub.1 is phenyl, 4-methoxyphenyl, 2,4-dimethoxyphenyl or 2,4,6-trimethoxyphenyl,are produced by addition of R.sub.1 --CH.sub.2 --N.sub.3 to a lower alkyl cyanoformate followed by saponification, optional acidification, and conversion to the carbonyl halide. The N-protected tetrazole-5-carbonylhalides are intermediates for the production of anti-allergic agents.
摘要:
The 2-cyano-3-or 4-(substituted amino)oxanilic acid derivatives of the formula: ##STR1## in which the group ##STR2## appears in the designated 3- or 4- position and R is -H; an alkali metal; .sup.+ NH.sub.4 ; alkyl of 1 to 6 carbon atoms, inclusive; aralkyl of 7 or 8 carbon atoms; or cycloalkyl of 5 or 6 carbon atoms;R.sup.1 is --H or alkyl of 1 to 9 carbon atoms;R.sup.2 is --H, alkyl of 1 to 9 carbon atoms or cycloalkyl of 3 to 6 carbon atoms;R.sup.1 and R.sup.2, together, with the nitrogen atom to which they are attached, are aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-lower alkyl-piperazinyl, morpholino or thiomorpholino; and pharmaceutically acceptable acid addition salts thereof are anti-allergic agents.
摘要:
Anti-allergic agents of N-aromatic 1H-(or 2H) tetrazole-5-carboxamide derivation present the following formulae: ##STR1## in which R.sup.1 is --CN or --CONH.sub.2 ;R.sup.2 is hydrogen, lower alkyl, lower alkoxy, halo, polyhalo(lower)alkyl, lower alkyl carbonyl or carb(lower)alkoxy;X is --CH.sub.2 --, ##STR2## where R.sup.3 is lower alkyl and R.sup.4 is hydrogen or lower alkyl;Or a pharmaceutically acceptable salt thereof.
摘要:
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. The derivatives are of Formula II:
摘要:
The present invention provides, among other things, imidazo[1,2-α]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.