Abstract: Compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl groups containing 1 to 6 carbon atoms; R.sup.3 is a haloalkyl group of the formula C.sub.m Y.sub.(m-1) X.sub.(m+2) wherein X is fluoro, chloro, bromo or iodo and m=1 or 2; Y is hydrogen, fluoro, chloro, bromo or iodo; R.sup.4 is hydrogen, an alkyl group containing 1 to 6 carbon atoms, alkoxy containing 1 to 6 carbon atoms, alkenyl containing 2 to 6 carbon atoms, nitro, hydroxy, alkoxyalkyl containing 2 to 6 carbon atoms, fluoro, bromo, chloro or iodo and n-1, 2, 3 or 4, have fungicidal activity.
Abstract: Compatibility agents were developed for improving the compatibility and stability of mixtures of liquid fertilizers and liquid or wettable powdered pesticides. These compatibility agents contain water, a low alkanol and an alkylaryl polyoxyethylene glycol phosphate ester. The compatibility agent is used at a preferred concentration range of 0.1 to 0.4% of the fertilizer solution. The preferred compatibility agent not only improves the compatibility of liquid fertilizer-pesticide mixtures, but also results in uniform and stable mixtures ensuring accurate pesticide applications. The preferred compatibility agent is a mixture containing about 16% water, about 20% methanol and about 64% of an octylphenol polyoxyethylene glycol phosphate ester.
Abstract: The compounds are amino- or cyano-bearing dihydroquinolines, which have either of the combinations of (a) 2-amino, 3-carboxylic and 4-oxo functions, or (b) 2-oxo, 3-cyano and 4-hydroxy functions, and may be optionally substituted at 1 or 2 of the 5, 6, 7 or 8 positions, eg 1-allyl-2-amino-1,4-dihydro-6,7-dimethoxy-4-oxo-quinoline-3-carboxylic acid ethyl ester, and 1-allyl 3-cyano-1,2-dihydro-4-hydroxy-6,7-dimethoxy-2-oxo-quinoline. The compounds are useful as pharmaceuticals.
Abstract: The compounds of this invention are cephalosporins having various acyl substituents at the 7-position and a substituted tetrazolyl thiomethyl group at the 3-position of the cephem nucleus and intermediates for the preparation thereof. The 7-acylated compounds have antibacterial activity.
Abstract: R.sup.2 is an aliphatic hydrocarbon residue which may be substituted with hydroxy, protected hydroxy or lower alkylthio,R.sup.3 is a heterocyclic group substituted with amino(lower)alkyl, protected amino(lower)alkyl or hydroxy(lower)alkyl, andR.sup.4 is carboxy or functionally modified carboxy, "syn" or "anti" isomer.
Abstract: Naphthalimide derivatives of the general formula ##STR1## where R.sup.1 is hydrogen or C.sub.1 - to C.sub.4 -alkyl,R.sup.2 is nitrile or a radical containing a carbonyl group or an acetalized carbonyl group andR.sup.3 and R.sup.4 are unsubstituted or substituted alkyl.The compounds are excellent optical brighteners, especially for synthetic fibers.
November 17, 1978
Date of Patent:
September 2, 1980
Jochen Karg, Manfred Patsch, Walter Himmele
Abstract: The preparation of vincadifformine and some derivatives thereof for use as a starting material for synthesis of the corresponding vincamine derivatives or for synthesis of bisindole alkaloids having clinically important antitumor properties.
Abstract: Quinoline derivatives, especially those of the formula ##STR1## wherein X represents halogen, nitro or CF.sub.3,Z represents hydrogen, alkyl or aryl,Y represents hydrogen, OH, CN, COR or SO.sub.3 H,R represents alkyl, alkoxy or aryl andn represents an integer from 0 to 4,are obtained in high yields when corresponding aromatic orthodichloromethyl isocyanates are converted by hydrolysis and decarboxylation into the corresponding ortho-aminoaldehydes and these are subjected to a condensation reaction with carbonyl compounds containing an active .alpha.-methylene group.The process products are starting materials for dyestuffs, insecticides and others.
June 30, 1978
Date of Patent:
September 2, 1980
Volker Ehrig, Hans-Samuel Bien, deceased, Erich Klauke, Detlef-Ingo Schutze
Abstract: Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium, or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, lower alkyl, cycloalkyl, cycloalkenyl, cycloalkadienyl, substituted or unsubstituted phenyl, benzyl, phenethyl, thienyl, furyl, or pyridyl, or 2-amino-4-thiazolyl; X is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, ##STR2## R.sub.3 is hydrogen, ##STR3## --O--lower alkyl, or certain substituted or unsubstituted heterothio groups; are disclosed. These compounds possess useful antibacterial activity.
Abstract: Compounds having the following formula: ##STR1## wherein X is a radical selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, methyl and amino.Y is a radical selected from the group consisting of hydrogen and hydroxy, andA is an organic compound residue selected from the group consisting of having the formula: ##STR2## wherein Z is a radical selected from the group consisting hydrogen, acyloxy, carbamoyloxy, (heteroaromatic) thio, pyridinium, quinolinium and picolinium; and salts thereof, are useful as anti-bacterial agents active against Pseudomonas aeruginosa.
Abstract: A series of novel 7-(D-.alpha.-acylaminoarylacetamido)-.DELTA..sup.3 -cephem derivatives have been prepared wherein the acyl moiety contains an epoxy group immediately adjacent to the carbonyl carbon atom. These compounds are useful as antibacterial agents for the treatment of diseases caused by Gram-negative and Gram-positive bacteria. Preferred members include 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]-3-(1-meth yl-1,2,3,4-tetrazol-5-ylthiomethyl)-.DELTA..sup.3 -cephem-4-carboxylic acid and 7-[D-.alpha.-(cis-2-carboxyoxiran-3-carboxamido)phenylacetamido]cephalospo ranic acid. Alternate methods of preparation are provided for these compounds and the principal synthetic route is described in detail.
Abstract: Antibacterial 7.alpha.-methoxy-3-cephem derivatives of the formula: ##STR1## [wherein R.sup.1 is hydrogen, or organic or inorganic acyl;R.sup.2 is alkyl; andCOR.sup.3 is carboxy or protected carboxy],methods of production, and pharmaceutical preparations thereof.
Abstract: Vindesine is prepared by converting 4-desacetyl VLB C-3 carboxhydrazide to the corresponding azide with a nitrite such as n-butyl nitrite in THF and then reacting the thus formed azide with triphenylphosphine to yield an intermediate acyl iminophosphorane, which compound is decomposed with acid to yield vindesine of high purity and in good yield.
Abstract: Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b, which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl, C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together wth the carbon atom to which they are attached form a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c and R.sup.d, which may be the same or different, each represents a hydrogen atom or a substituting group e.g. an alkyl group or substituted alkyl group; or R.sup.c and R.sup.d together with the nitrogen atom to which they are attached form a saturated or unsaturated heterocyclic ring which contains 5-7 ring members and which may contain additional hetero atoms, and may be substituted by lower alkyl; R.sup.e represents hydrogen or C.sub.
November 28, 1977
Date of Patent:
June 17, 1980
Glaxo Operations UK Limited
Michael W. Foxton, Gordon I. Gregory, David M. Rogers
Abstract: Oxazolines having at least one 3,5-dialkyl-4-hydroxypheny l alkanoic acid ester substituent are provided. Such oxazolines are found to be useful an antioxidants in organic substances normally susceptible to oxidative deterioration.