Abstract: Novel syn isomers of 7-amino-thiazolyl-acetamido-3-acetoxymethyl-cephalosporanic acid derivatives of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of --CN, --CONH.sub.2 and --COOR.sub.1 ', R.sub.1 ' is selected from the group consisting of alkyl of 1 to 3 carbon atoms, hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, A is selected from the group consisting of hydrogen, alkali metal, alkaline earth metal, ammonium, magnesium and a non-toxic, pharmaceutically acceptable organic amine, R' and R" are individually selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms with the ##STR2## group in the syn position with the proviso that when R.sub.1 is --COOR.sub.1 ' and R.sub.1 ' is hydrogen, A is hydrogen and when R.sub.1 is --COOR.sub.1 ' and R.sub.
Abstract: Guanidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. These derivatives have the formula: ##STR1## in which X is oxygen or sulphur;Y is nitrogen or a CH radical;n is 1, 2, 3 or 4;m is 0 or 1;R.sup.1 is, for example, hydrogen or alkyl of 1-6 carbons; andR.sup.2 is, for example, ##STR2## and are characterized by the guanidino and cycloalkyl substituents which are attached directly to the heterocyclic ring.
Abstract: Compounds of the following formula have herbicidal activity: ##STR1## wherein X and Y are hydrogen or halo; R.sup.2 and R.sup.3 are alkyl or are joined to form --CH.sub.2 --.sub.n, n=2 through 7; R is hydrogen, haloacetyl, alkyl, alkoxyalkyl or N-alkylcarbamoyl and R.sup.1 is alkyl, alkenyl, alkynyl, cycloalkyl, polycycloalkyl, alkoxy-alkyl, cyanoalkyl or cyanoalkenyl; with the proviso that when R and R.sup.1 are both alkyl, each contains at least 3 carbon atoms.
Abstract: The invention relates to aminothiazolacetamido-3-cephem-4-carboxylic acid compounds of the formula ##STR1## in which the index n represents an integer of 1 to 4,X represents oxygen, sulphur, an --NH-- group or the direct bond,Y represents oxygen or sulphur,A represents methylene or methylene substituted by amino, hydroxy, carboxyl, sulpho, oxo, or the group .dbd.N--O--R.sup.o in which R.sup.o represents hydrogen or optionally substituted lower alkyl,R.sub.1 represents hydrogen, lower alkyl, an esterified or etherified hydroxy or mercapto group, halogen, formyl or a group of the formula --CH.sub.2 --R.sub.2 in which R.sub.2 represents an esterified or etherified hydroxy or mercapto group or a quaternary ammonium group, andR.sub.3 represents hydrogen or methoxy,in which functional groups are optionally present in protected form,salts of such compounds with acidic and/or basic groups, processes for the manufacture of these compounds, pharmaceutical agents containing such substances and their therapeutic use.
Abstract: 2-amino thiazoline derivative having Formula I: ##STR1## wherein: R represents --R.sub.1 or --CO--R.sub.2, wherein R.sub.1 represents benzyl monosubstituted in the ortho position by lower alkoxy or in the ortho, meta or para position by lower alkyl, trifluoromethyl or halogen, or R.sub.1 represents cycloalkylmethyl; and R.sub.2 represents cycloalkyl, naphthyl, styryl or substituted phenyl; and R.sub.3, R.sub.4, R.sub.5 and R.sub.6, each independently represent hydrogen or lower alkyl.The said 2-amino thiazoline is useful as a medicine in the preparation of pharmaceutical compositions.
Type:
Grant
Filed:
June 6, 1979
Date of Patent:
November 17, 1981
Assignee:
Institut Merieux
Inventors:
Andre L. Boucherle, Marie-Pierre D. Viallet
Abstract: Novel guanidinothiazole compounds of the general formula ##STR1## wherein R represents a hydrogen atom or a lower alkyl group, R.sub.1 represents an amino group, a lower alkyl group, a halogeno lower alkyl group, a substituted- or unsubstituted-aryl group, a mono- or di-lower alkylamino group, an arylamino group or an aralkylamino group, R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group or a lower alkynyl group, Y represents a sulfur atom or a methylene group, m and n, each represents an integer of 1-3, and the pharmacologically acceptable acid addition salts thereof, they are useful as gastric acid secretion inhibitors.
Abstract: By varying the acidity, solvent polarity, and temperature of the reaction of thiosemicarbazide with ethyl 4-chloroacetoacetate, ethyl 2-amino-6H-1,3,4-thiadiazine-5-acetate hydrochloride, ethyl 2-hydrazinothiazole-4-acetate, and ethyl 2-imino-3-aminothiazoline-4-acetate hydrochloride may be prepared selectively. Further derivatives may be prepared by benzoylation and nitrosation. These compounds have demonstrated utilities as herbicides.
Abstract: An organic compound of the general formula ##STR1## where R.sup.1 and R.sup.2 are cyano, formyl, substituted or unsubstituted alkanoyl or aroyl, a carboxylic acid ester group, substituted or unsubstituted carbamoyl or sulfamoyl, alkylsulfonyl, arylsulfonyl or alkylsulfinyl, orR.sup.1 and R.sup.2 together may be a cyclic radical,R.sup.2 may also be alkyl, aryl or hetaryl,R.sup.3 is hydrogen, substituted or unsubstituted alkyl, aryl or hetaryl,X is CH, CR.sup.5 or N,R.sup.4 is a radical of the formula ##STR2## R.sup.5 to R.sup.10 are substituents conventionally present in dyes. The compounds may be used as dyes for synthetic and natural fibers and give very fast dyeings.
Abstract: A class of amides disclosed to be useful as selective pre-emergent and post-emergent herbicides are those having the general structural formula ##STR1## in which R.sup.1 is hydrogen or methyl, R.sup.2 is ethyl, isopropyl, cyclopropyl, tert.butyl, methylamino, dimethylamino, ethylamino or methoxymethylamino, R.sup.3 is phenyl, 4-chlorophenyl, 3,4-dichlorophenyl, 4-methylphenyl or 4-methoxyphenyl, R.sup.4 is hydrogen or C.sub.1 to C.sub.3 lower alkyl, and R.sup.5 is hydrogen or methyl, with the further stipulation that either, but not both R.sup.4 and R.sup.5 may be hydrogen.
Abstract: Urea derivatives of the formula ##STR1## (wherein Ar represents a residue of 5- or 6-membered heteroaromatic ring; R represents a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group; R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group; and R.sup.2 represents a C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or C.sub.1 -C.sub.6 alkoxy group) are produced by reacting an amine of the formulaAr--NH--R(wherein Ar and R have the significance given above) with a carbamoyl halogenide of the formula ##STR2## (wherein X represents a halogen atom, and R.sup.1 and R.sup.2 have the significance given above) in the presence of a Lewis acid in an inert solvent.
Abstract: The invention relates to heterocyclic ester compounds which have been found to be effective ultraviolet stabilizers. The invention also relates to ultraviolet degradable organic compositions containing an amount of a heterocyclic ester composition to prevent such degradation. These stabilizers are effective in the presence of other additives commonly employed in polymeric compositions including, for example, pigments, colorants, fillers, reinforcing agents and the like. These ultravoilet stabilizers may be incorporated into the organic compositions such as polymers by adding to the polymer melt or dissolved in the polymer dope, coated on the exterior of the shaped or molded article, film or extruded fiber.
Type:
Grant
Filed:
January 9, 1978
Date of Patent:
February 27, 1979
Assignee:
Eastman Kodak Company
Inventors:
Gether Irick, Jr., James C. Ownby, Richard H. S. Wang