Nitrogen Attached To The Acid Group Directly Or Indirectly By Acyclic Nonionic Bonding (e.g., N-hydroxy Ureas, Dihydroxamic Acids, Etc.) Patents (Class 562/623)
Abstract: Novel compounds of formula (I)Ar--(L--Ar').sub.q --(X).sub.k --(Y).sub.p --Q (I)wherein:k, p and q are independently 0 or 1;Ar represents either:(i) naphthyl, tetrahydronaphthyl, pyridyl or(ii) phenyl, optionally substituted,L is selected from --(CH.sub.2).sub.r -- (where r is 1-4), --O--, --CH.sub.2 O--, --CH.sub.2 S--, --OCH.sub.2 --, --CONH--, --NHCO--, --CO-- and --CH.sub.2 NH--, and,Ar' represents phenylene, thienylene or pyridylene optionally substituted,X represents oxygen, sulphur or carbonyl,Y is C.sub.1-10 alkylene or C.sub.1-10 alkenylene;Q represents a non-cyclic moiety selected from groups of formula ##STR1## in which one of m and n is 0 and the other is 1, R.sup.1 and R.sup.2 is selected from hydrogen, C.sub.1-4 alkyl, amino, C.sub.1-4 alkylamino, di-C.sub.1-4 alkylamino, C.sub.5-7 cycloalkylamino, C.sub.5-7 cycloalkyl (C.sub.1-4 alkyl) amino, anilino, N-C.sub.
Type:
Grant
Filed:
March 10, 1987
Date of Patent:
July 30, 1991
Assignee:
Burroughs Wellcome Co.
Inventors:
Geoffrey Kneen, William P. Jackson, Peter J. Islip, Peter J. Wates
Abstract: Compounds having 5- and 12-lipoxygenase inhibitory activity have the structure ##STR1## where A is straight or branched divalent alkylene of from one to four carbon atoms, R.sub.1 is methyl, amino, or alkylamino of from one to six carbon atoms and the substituent group R.sub.2 is C.sub.1 -C.sub.2 alkyl.The group R.sub.3 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, halogen, cyano, and trihalomethyl, and R.sub.4 is one or more substituents selected from hydrogen, alkyl of from one to six carbon atoms, alkoxy of from one to six carbon atoms, thioalkoxy of from one to six carbon atoms, hydroxy, halogen, cyano, and trihalomethyl, with the proviso that when R.sub.1 is amino and A is >CHCH.sub.3, R.sub.3 and R.sub.4 may not both be hydrogen.The group designated M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group.
Type:
Grant
Filed:
November 2, 1989
Date of Patent:
June 25, 1991
Assignee:
Abbott Laboratories
Inventors:
Dee W. Brooks, James B. Summers, James H. Holms
Abstract: An N-methyl-.alpha.-dialkylaminoacetohydroxamic acid represented by formula (I): ##STR1## wherein R.sub.1 and R.sub.2, which may be the same or different, each represents a substituted or unsubstituted methyl group or a substituted or unsubstituted ethyl group.
Abstract: A hydroxamic acid compound represented by the general formula (I) or a salt thereof; ##STR1## wherein R.sup.1 represents a hydrogen atom, or a substituted or unsubstituted alkanoyl group, R.sup.2 represents an unsubstituted alkanoyl, substituted lower alkanoyl or substituted lower alkyl group, and m represents an integer of 3 to 7, which are useful for the prevention and/or treatment of diseases caused by lipoxygenase-mediated metablites.
Abstract: Compounds of the formula ##STR1## wherein A is a group of the formula HN(OH)--CO-- or HCO--N(OH)--; R.sup.1 is a C.sub.2 -C.sub.5 -alkyl; R.sup.2 is the characterizing group of a natural .alpha.-amino acid in which any functional group present may be protected, any amino group present may be acylated and any carboxyl group present may be amidated, with the proviso that R.sup.2 is not hydrogen or methyl; R.sup.3 is hydrogen, amino, hydroxy, mercapto, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.6 -alkylamino, C.sub.1 -C.sub.6 -alkylthio or aryl-(C.sub.1 -C.sub.6 -alkyl), or amino-(C.sub.1 -C.sub.6 -alkyl), hydroxy-(C.sub.1 -C.sub.6 -alkyl), mercapto-(C.sub.1 -C.sub.6 -alkyl) or carboxy-(C.sub.1 -C.sub.6 -alkyl) in which the amino, hydroxy, mercapto or carboxyl group may be protected, the amino group may be acylated or the carboxyl group may be amidated; R.sup.4 is hydrogen or methyl; R.sup.5 is hydrogen or a C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy-C.sub.1 -C.sub.6 -alkyl, di(C.
Type:
Grant
Filed:
April 11, 1989
Date of Patent:
February 26, 1991
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Balraj K. Handa, William H. Johnson, Peter J. Machin
Abstract: Disclosed is a synthesis of desferrioxamine B and analogs and homologs thereof beginning with the generation of the O-protected N-(4-cyanobutyl)hydroxylamine which is acylated at the O-benzylhydroxylamine nitrogen with either succinic or acetic anhydride. The resulting half-acid amide or amide respectively, is subjected to a series of high yield condensations and reductions which provide desferrioxamine B in 45% overall yield. Finally, a desamino analog of desferrioxamine is prepared in order to demonstrate the synthetic utility of the scheme as applied to desferrioxamine derivatives.
Abstract: A compound having the formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein A is an amino acid identifying group; B is a hydrogen atom, an alkyl group having 1-5, inclusive, carbon atoms, or an aralkyl group having 6-12, inclusive, carbon atoms; carbon atom 2 is of the R configuration; and carbon atom 3 is of the R configuration.
Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective inhibitors of cyclooxygenase and 5-lipoxygenase.
Type:
Grant
Filed:
May 26, 1989
Date of Patent:
January 1, 1991
Assignee:
Warner-Lambert Co.
Inventors:
Thomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
Abstract: Ligand compounds useful as extractants of certain metals from solutions. Effective also as promoters of the growth of microorganisms.A process for the preparation of such hexadentate ligands and methods of selective extraction of transition and related metal ions from admixtures with other metals.
Type:
Grant
Filed:
October 11, 1988
Date of Patent:
October 30, 1990
Assignee:
Yeda Research and Development Co., Ltd.
Inventors:
Abraham Shanzer, Jacqueline Libman, Shneior Lifson
Abstract: Described is a novel process for the introduction of an organic acyl radical selectively at the nitrogen atom of the amino group of desferrioxamine B or of a partially O-acylated derivative thereof. It comprises treating a derivative of desferrioxamine B, in which the amino nitrogen and the hydroxy oxygen of at least one of the hydroxamic acid groupings carries an organic silyl group, with an organic acylating agent and then removing the silyl groups present. The novel N- and O-silylated starting materials can be manufactured, preferably in situ, by reacting an appropriate derivative of desferrioxamine B that has at least one hydroxy group and the amino group in free form, with an organic silicon halide.
Abstract: Dihydroxamic acids derived from succinyl compounds are used in conjunction with monohydroxamic acids to extract gallium, e.g. N,N'-dimethyl n-decylsuccino dihydroxamic acid and a monohydroxamic acid in an organic solvent extracts gallium in the presence of other metals from gallium bearing aqueous solutions.
Type:
Grant
Filed:
July 6, 1989
Date of Patent:
July 3, 1990
Assignee:
Monsanto Company
Inventors:
James P. Coleman, Charles R. Graham, Bruce F. Monzyk
Abstract: The present invention relates to a novel family of chemical compounds possessing a pharmacological activity, in particular a collagenase-inhibiting activity, a process for the production of these compounds and pharmaceutical compositions in which they are present.According to the invention, these compounds correspond to the general formula: ##STR1## in which: W represents an amino acid residue selected from the group comprising valine, lysine, norleucine and methionine, andZ represents an amino radical or an alkylamino radical of which the alkyl part, which contains 1 or 2 carbon atoms, is substituted by a phenyl or trifluorophenyl radical,and also include their diastereoisomers and their addition salts with pharmaceutically acceptable acids.The invention is applicable especially in the pharmaceutical industry.
Abstract: Compounds of the formula: ##STR1## where R.sub.1 is amino or methyl; R.sub.2 is C.sub.1 -C.sub.2 alkyl; R.sub.3 is one or more substituents selected from hydrogen, halogen or trihalomethyl; R.sub.4 is one or more substituents selected from hydrogen, halogen, trihalomethyl, C.sub.1 to C.sub.4 alkoxy or C.sub.1 to C.sub.4 alkyl; and M is hydrogen, a pharmaceutically acceptable cation, aroyl, or C.sub.1 to C.sub.6 alkoyl are inhibitors of 5- and/or 12-lipoxygenase enzymes.
Abstract: Arylmethylenesulfonamidoacetamide and thioacetamide derivatives and arylmethylenesulfonamidoester intermediates therefor. The compounds are useful as selective herbicides especially with respect to the prevention and elimination of barnyardgrass in grass crops, especially in rice crops.