Abstract: Novel substituted isoquinoline compounds of the formula ##STR1## wherein R is lower alkyl,R.sub.1 is lower alkylene, 1-3 lower alkyleneoxy groups or lower alkylenethio, andX is one or more substitutents selected from the group consisting of hydroxyl, carbalkoxy, carboxy and acyloxy.These novel substituted isoquinolines can be used as dyes, toners or color bodies, and in particular as toners for polyesters.
Type:
Grant
Filed:
April 23, 1987
Date of Patent:
October 4, 1988
Assignee:
Eastman Kodak Company
Inventors:
Wayne P. Pruett, Samuel D. Hilbert, John G. Thompson, Max A. Weaver
Abstract: There is presented compounds of the formula ##STR1## wherein X represents the 1,2,5,6-tetrahydro-2-methyl-5,6-dioxo-as-triazin-3-yl group or its corresponding tautomeric form, the 2,5-dihydro-6-hydroxy-2-methyl-5-oxo-as-triazin-3-yl group, and the readily hydrolyzable esters, readily hydrolyzable ethers and salts of the compounds and hydrates of the compounds of formula I or of their esters, ethers and salts. Also provided is a method of their manufacture and intermediates therefor as well as corresponding pharmaceutical preparations.
Abstract: Esters of pyroglutamic acid having the structure: ##STR1## where R' and R" are the same or different and are each represented by H or the groupingCH.sub.3 [(CH.sub.2).sub.w (CHCH.sub.3).sub.x (CHOH).sub.y (CH.dbd.CH).sub.z ]--wheren is an integer of from 1 to 3w is zero, or an integer of from 1 to 21x is zero, or an integer of from 1 to 4y is zero, or an integer of from 1 to 2z is zero, or an integer of from 1 to 4provided that the total number of carbon atoms in each of said grouping will not exceed 22;and provided also that when the subgrouping (CH.dbd.CH) is present, then the total number of carbon atoms in said grouping will be from 16 to 22. Synthesis, and uses of the said esters in topical compositions are also provided.
Abstract: There are disclosed compounds of the formula ##STR1## where X and Y are independently hydrogen, loweralkyl, loweralkoxy, hydroxy, halogen, trifluoromethyl or nitro; R.sub.1 is hydrogen or loweralkyl; R.sub.2 is hydrogen, loweralkyl, loweralkylcarbonyl or arylcarbonyl; and R.sub.3 is hydrogen, loweralkyl, arylloweralkyl, ##STR2## loweralkylcarbonyl or arylcarbonyl, n being an interger of 1 to 6 inclusive and Z being hydrogen, loweralkyl, loweralkoxy, hydroxy or halogen; which are useful as hypotensive agents.
Abstract: Mitomycin derivatives of the formula: ##STR1## wherein X is ##STR2## [wherein R.sub.3 is alkyl, cycloalkyl or optionally substituted phenyl; and R.sub.4 is alkyl or cycloalkyl]; n is an integer of 2 to 8; one of R.sub.1 and R.sub.2 is a hydrogen atom and the other is a carbamoyloxymethyl group, or alternatively R.sub.1 and R.sub.2 may be combined together to form a methylene group (.dbd.CH.sub.2); and Y and Z independently represent hydrogen or methyl;exhibit anti-bacterial and anti-tumor activities.
Abstract: Process for preparing perylenetetracarbimide mix-crystal pigments in the crystal lattice of the .alpha.-modification of the N,N'-bis-3',5'-dimethylphenylperylenetetracarbimide of the formula (1) comprising essentially symmetrical N,N'-bis-3',5'-dimethylphenylperylenetetracarbimide of the formula (1) and at least one asymmetrically substituted diimide of the formula (2) in which R stands for methyl or ethyl ##STR1## by condensing 1 mole of perylenetetracarboxylic dianhydride with an excess of up to 30 moles of 3,5-dimethylaniline which contains in total 0.5-6 percent by weight of 4-ethoxyaniline, and their use for coloring organic polymers.
Abstract: Compound for use in a method for treatment of the human or animal body by therapy, characterized in that the compound is a carboxy azetidine derivative of the general formula I or a pharmaceutically acceptable salt, ester, amide, alkylamide, hydrazide or alkylhydrazide thereof: ##STR1## in which: X represents one of the groups CH.sub.2, CHR or CR.sub.2.Y represents one of the groups CH.sub.2, CHR, CR.sub.2 or CH.CO.sub.2 H andZ represents one of the groups CH.sub.2, CHR, CR.sub.2 or CH.CO.sub.2 H;the or each R independently represents an alkyl, alkenyl or cycloalkyl group or an aryl or aralkyl group optionally substituted on the aryl nucleus by one or more of the same or different substituents selected from halogen atoms, alkyl groups and alkoxy groups;and one but only one of Y and Z must represent a CH.CO.sub.2 H group.
Abstract: Compound of the formula (I) ##STR1## wherein n is zero or an integer of 1 to 3;R is(a) --NHR.sub.3, wherein R.sub.3 is(a') --CON(NO)R.sub.4, in which R.sub.4 is C.sub.1 -C.sub.4 alkyl either unsubstituted or substituted by halogen; or(b') --CO(CH.sub.2).sub.m --R.sub.5, in which R.sub.5 is halogen, oxiranyl, methyloxiranyl, aziridinyl, a group ##STR2## or a group ##STR3## and m is zero or an integer of 1 to 4; or (b) ##STR4## wherein either R.sub.6 and R.sub.7 are the same and are each oxiranemethyl, aziridinemethyl, or C.sub.2 -C.sub.4 alkyl 2-substituted by halogen or by a group --OSO.sub.2 R.sub.8 wherein R.sub.8 is C.sub.1 -C.sub.4 alkyl or phenyl, or one of R.sub.6 and R.sub.7 is hydrogen and the other is as defined above;each group R.sub.1 is, independently, hydrogen or C.sub.1 -C.sub.4 alkyl;R.sub.2 is a C.sub.1 -C.sub.6 alkyl group terminating with (i) a basic moiety chosen from an amino group, a mono- or di- C.sub.1 -C.sub.
Abstract: The compounds of the invention have the following general formula (I) ##STR1## wherein each of the groups R, R.sub.1 and R.sub.2, which may be the same or different, represents a hydrogen atom, a C.sub.1 -C.sub.6 alkoxy or C.sub.1 -C.sub.6 alkyl group, and R.sub.3 represents a straight or branched chain, saturated or unsaturated, C.sub.1 -C.sub.8 aliphatic hydrocarbon group. The compounds are useful as antilipolytic agents.
Type:
Grant
Filed:
December 5, 1986
Date of Patent:
August 23, 1988
Assignee:
Farmitalia Carlo Erba, S.p.A.
Inventors:
Paolo Cozzi, Antonio Pillan, Leone Bertone, Pier P. Lovisolo
Abstract: The compounds of the following formula are histamine H.sub.1 -receptor antagonists: ##STR1## where R.sup.3 and R.sup.4 are, independently, hydrogen, halo, alkoxy of 1 to 3 carbon atoms or alkyl of 1 to 3 carbon atoms; R.sup.2 is hydrogen or halo;n is one of the integers 0, 1 or 2;p is one of the integers 0 or 1;Y is --N.dbd. or --CH.dbd., with the proviso that when Y is --N.dbd., p is zero, and when Y is --CH.dbd., p is one; andone of X.sub.1 and X.sub.2 is nitrogen and the other is --CH.dbd.; or a pharmaceutically acceptable salt thereof.
Abstract: Saturated nitrogen-containing five-membered and six-membered heterocycles are aromatized by dehydrogenation in the gas phase in the presence of a supported palladium catalyst containing an alkaline earth metal halide, at from 150.degree. to 350.degree. C. and under from 0.1 to 10 bar.
Abstract: A cephem derivative represented by the general formula ##STR1## wherein R.sup.1 represents hydrogen or methyl, R.sup.2 represents carboxyl or esterified carboxyl, and n represents 0 or 1, or a pharmaceutically acceptable salt thereof; intermediates for the cephem derivative or salt thereof; processes for producing these compounds; and a pharmaceutical composition and method for preventing or treating bacterial infectious diseases, wherein the cephem derivative or the salt thereof is used.
Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, alkyl(C.sub.1 -C.sub.3), vinyl, acetyloxy or ##STR2## wherein R.sub.3 is hydrogen or alkyl(C.sub.1 -C.sub.6); R.sub.2 is hydrogen or diphenylmethyl and A is R.sub.4 --C, where R.sub.4 is acetyl or benzoyl, are useful as intermediates in the preparation of biologically active cephalosporin derivatives.
Abstract: The invention relates to a novel water soluble aminobenzoic acid in a complexed state which is derived from the reaction between a poly(N-vinyl-2-pyrrolidone)-halogen complex and an aminobenzoic acid and to the process for the preparation of said multicomplex.
Abstract: Disclosed herein are the derivatives of substituted cephalosporanic acid represented by the formula (I): ##STR1## wherein R.sup.1 represents a 4-pyridylthiomethyl group, an alpha-aminobenzyl group, a cyanomethyl group or a 1-tetrazolylmethyl group; R.sup.2 represents a hydrogen atom, an acetoxy group or a (5-methyl-1,3,4-thiadiazol-2-yl)thio group; R.sup.3 represents a hydrogen atom, a hydroxyl group, a carbamoyl group, an alkyl group having 1 to 4 carbon atoms or --(CONH).sub.m (CH.sub.2).sub.n --COOH wherein m is 0 or 1, n is 0, 1 or 2 and the carboxyl group may have been converted to a salt or an ester thereof; p is 0, 1 or 2 and X represents carbon atom or nitrogen atom, and antibiotics comprising the derivatives of substituted cephalosporanic acid represented by the formula (I).
Abstract: The present invention relates to phenylalkylamino-ketone derivatives, namely the phenyl-(3-hexamethyleneiminopropyl)-ketone and its addition salts, by way of new industrial products.These new products are useful in therapy as vasodilating agents.
Type:
Grant
Filed:
July 8, 1986
Date of Patent:
July 19, 1988
Assignee:
Societe Anonyme Dite: Laboratoire L. Lafon
Abstract: Disclosed are the compounds of the formula ##STR1## wherein n represents the integer 1,2,3 or 4; R.sub.1 represents hydrogen, lower alkyl, halogen, trifluoromethyl, hydroxy or lower alkoxy; R.sub.2 represents hydrogen or lower alkyl; R.sub.3 represents hydrogen, lower alkyl or halogen; R.sub.4 represents amino, lower alkylamino, di-lower alkylamino, morpholino, N-lower alkyl or N-aryl piperazino, pyrrolidino, piperidino or substituted piperidino selected from ##STR2## in which R.sub.5 represents hydrogen, halogen or lower alkyl; and pharmaceutically acceptable salts thereof; which are useful in mammals as calmodulin antagonists for the treatments of gastrointestinal disorders.
Abstract: A compound of the formula: ##STR1## wherein R is 2-methylpropyl, 2,2-dimethylpropyl, 1-ethylpropyl, 1-methylbutyl, 2-methylbutyl, 3-methylbutyl, n-pentyl, an alkyl group of 6 or 7 carbon atoms, or an alkenyl group of 2 to 7 carbon atoms, or a pharmaceutically acceptable salt thereof and processes for preparing the same are provided. The compound can orally be applied as antibiotics having improved absorbability.