Abstract: An ethyl benzylphosphinate derivative represented by the general formula (I) ##STR1## wherein Y represents a hydrogen or fluorine atom, X represents a methylene group or an oxygen atom, and n is 2, 3 or 4.The said compounds can be produced by reacting a compound represented by the following formula (II) ##STR2## wherein Y is as defined above, with a compound represented by the following formula (III) ##STR3## wherein X and n are as defined, and M is an alkali metal atom, in an inert medium. These compounds are useful as a calcium antagonist.
Abstract: A method is provided for preparing phosphinic acid prodrug intermediates which are useful in preparing phosphinic acid angiotensin-converting enzyme inhibitors which method includes the step of coupling a phosphonous acid or its ester of the structure ##STR1## wherein R is H or lower alkyl and R.sup.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl, with an alkylating agent of the structure ##STR2## wherein Hal is Cl, Br or I, n is 0 or 1, R.sup.2 is H or lower alkyl, and Z is H, lower alkyl, --CO.sub.2 R.sup.3 (wherein R.sup.3 is H or lower alkyl), ##STR3## (wherein R.sup.4 is H, lower alkyl, aryl or arylalkyl), --CN, or ##STR4## (wherein R.sup.5 and R.sup.6 may be the same or different and are selected from the group consisting of H, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkylalkyl and at least one of R.sup.5 and R.sup.6 is other than H, or R.sup.5 and R.sup.
Abstract: Methine dyes are disclosed which contain a 2-halo or pseudohalo substituted 1,2,5-oxatellurazole ring fused with an aromatic nucleus, the aromatic nucleus being substituted with a methine linkage terminating in an auxochrome providing a conjugated resonance chromophore. The dyes can be formed by condensing a methine linkage precursor with a compound containing an oxatellurazole ring fused with an aromatic nucleus. The dyes are useful in optical recording elements and in photographic elements.
Abstract: A method is provided for preparing phosphinic acid prodrug intermediates which are useful in preparing phosphinic acid angiotensin-converting enzyme inhibitors which method includes the step of coupling a phosphonous acid or its ester of the structure ##STR1## wherein R is H or lower alkyl and R.sup.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl, with a conjugated compound of the structure ##STR2## wherein R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each is independently H, lower alkyl or aryl, and Z is --CO.sub.2 R.sup.5 (wherein R.sup.5 is H or lower alkyl), ##STR3## (wherein R.sup.6 is H, lower alkyl aryl or arylalkyl), ##STR4## (wherein R.sup.7 and R.sup.8 are the same or different and are selected from the group consisting of H, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkylalkyl and at least one of R.sup.7 and R.sup.8 is other than H, or R.sup.7 and R.sup.
Abstract: Phosphorus containing compounds of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid and A is ##STR2## These compounds possess angiotensin converting enzyme activity and are thus useful as hypertensive agents.
Type:
Grant
Filed:
December 24, 1981
Date of Patent:
November 26, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Donald S. Karanewsky, Edward W. Petrillo, Jr.
Abstract: Angiotensin converted enzyme inhibitor activity if exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is hydrogen, aryl, or heteroaryl; R.sub.2 is hydrogen, amino, alkanoylamino, arylcarbonylamino, or heteroarylcarbonylamino;R.sub.3 is hydrogen, alkyl, or aminoalkyl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, alkyl, halogen, aryl, arylalkyl, hydroxy, alkoxy, alkylthio, aryloxy, arylthio, or cycloalkyl, or R.sub.4 and R.sub.5 taken together are oxo, ethylenedithio or propylenedithio;one of R.sub.6 and R.sub.7 is ##STR2## and the other is hydrogen, alkyl or arylalkyl; R.sub.8 is hydrogen, alkl or aryl;R.sub.9 is hydrogen or alkyl;n is 0 or an integer of 1 to 8;m is 0 or 1; andA is --(CH.sub.2).sub.p --wherein p is 0 or 1, --NH--, or --O--.
Abstract: Diphosphonic acid derivatives of Formula I ##STR1## wherein R is hydrogen, an alkali metal atom, an alkaline earth metal atom, or an alkyl group of 1-4 carbon atoms andA is derived from a carboxylic acid having anti-inflammatory and antiphlogistic activity and containing an aromatic or heteroaromatic group, of Formula IIACOOH (II),are pharmacologically efficacious compounds.
Type:
Grant
Filed:
January 27, 1983
Date of Patent:
March 5, 1985
Assignee:
Schering Aktiengesellschaft
Inventors:
Helmut Biere, Clemens Rufer, Irmgard Boettcher
Abstract: Novel carbonates of 6(or 5)-hydroxy-2-benzothiazolesulfonamide are useful for the topical treatment of elevated intraocular pressure. Ophthalmic compositions include drops and inserts.
Abstract: Phosphorous diketonate electron accepting compounds are disclosed for use as sensitizers in electron donating photoconductive compositions. Methine dyes having a phosphorous diketonate component and a method of making same are also disclosed.
Type:
Grant
Filed:
September 20, 1982
Date of Patent:
January 29, 1985
Assignee:
Eastman Kodak Company
Inventors:
Chin H. Chen, Thomas E. Goliber, Jerome H. Perlstein, George A. Reynolds
Abstract: Novel phosphorus esters of amidoximes and methods of preparing same. This invention is also directed to pesticidal compositions comprising an acceptable carrier and a pesticidally effective amount of a compound of this invention, as well as to a method of controlling pests which comprises subjecting the pests to a pesticidally effective amount of a compound of this invention.
Abstract: A phosphonic acid ester of the formula ##STR1## exhibits calcium-antagonistic, coronary vasodilating and hypotensive activities. Pharmaceutical compositions containing the same are useful for the prophylaxis and treatment of circulatory organ diseases such as angina pectoris, hypertension and the like.
Abstract: In a synergistic pesticidal composition comprising (1) a pesticidally active compound and (2) a synergizing agent in amount sufficient to synergize the pesticidal activity of the pesticidally active compound, the improvement which comprises employing as the synergizing agent a 2-(thi)oxo-1,3,2-oxazaphospholane of the formula ##STR1## in which X represents oxygen or sulphur,R represents an optionally substituted alkyl, alkenyl, alkynyl, phenyl, alkoxy, alkenoxy, alkynoxy, alkylthio, aralkoxy, amino, mono- or di-alkylamino, heterocyclic amino, N-alkyl-N-aryl-amino, phenoxy or phenylthio radical,R.sup.1 represents hydrogen, optionally substituted alkyl, aralkyl, alkenyl, alkynyl or dialkylaminoalkyl,R.sup.2 represents hydrogen, alkylthioalkyl, or optionally substituted alkyl or aralkyl, or R.sup.1 and R.sup.2 together represent alkylene,R.sup.3 represents hydrogen or alkyl andR.sup.4 represents hydrogen, alkyl, or phenyl.
Type:
Grant
Filed:
November 3, 1980
Date of Patent:
June 7, 1983
Assignee:
Bayer Aktiengesellschaft
Inventors:
Hellmut Hoffmann, Bernd-Wieland Kruger, Wolfgang Behrenz
Abstract: A benzimidazolyl-2-alkane-phosphonic acid of the formula ##STR1## wherein R.sup.1 and R.sup.2 are identical or different and denote hydrogen, lower alkyl, phenyl, halogen, trifluoromethyl, nitro or lower alkoxy, or together form a fused-on benzene ring,R.sup.3 denotes hydrogen, lower alkyl or phenyl or benzyl which is optionally substituted by lower alkyl or halogen andA denotes a straight-chain or branched, saturated or unsaturated bivalent hydrocarbon radical with 1 to 15 carbon atoms, which can be substituted by phenyl which is optionally substituted by lower alkyl or halogen or by carboxyl or the phosphonic acid group,and its salt with an inorganic or organic base or acid, and a method of preparing the same by contacting an o-arylene diamine of the formula ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 have the meaning given above, with a phosphonocarboxylic acid of the formula ##STR3## wherein Y denotes carboxyl, carbalkoxy, carbophenoxy, cyano, carbamido or carbochloride,R.sup.7 and R.sup.
Type:
Grant
Filed:
December 10, 1979
Date of Patent:
July 14, 1981
Assignee:
Bayer Aktiengesellschaft
Inventors:
Artur Botta, Heinz-Joachim Rother, Gunther Teichmann
Abstract: Metal salts of hydrocarbyl oxazoline phosphorodithioic acids are novel compounds effective for reducing friction and wear when added to a lubricant.
Type:
Grant
Filed:
October 11, 1979
Date of Patent:
March 17, 1981
Assignee:
Mobil Oil Corporation
Inventors:
Robert M. Gemmill, Jr., Andrew G. Horodysky
Abstract: Phosphosulfurized hydrocarbyl oxazoline reacted with nitrogen-containing compounds and certain olefins are novel compounds effective for reducing friction and wear when added to a lubricant.
Type:
Grant
Filed:
November 20, 1979
Date of Patent:
March 10, 1981
Assignee:
Mobil Oil Corporation
Inventors:
Andrew G. Horodysky, Robert M. Gemmill, Jr.
Abstract: Metal salts of phosphosulfurized hydrocarbyl oxazoline phosphorodithioic acids are novel compounds effective for reducing friction and wear when added to a lubricant.
Type:
Grant
Filed:
November 20, 1979
Date of Patent:
March 3, 1981
Assignee:
Mobil Oil Corporation
Inventors:
Andrew G. Horodysky, Robert M. Gemmill, Jr.
Abstract: Metal salts of hydrocarbyl oxazoline phosphorodithioic acids are novel compounds effective for reducing friction and wear when added to a lubricant.
Type:
Grant
Filed:
October 1, 1979
Date of Patent:
March 3, 1981
Assignee:
Mobil Oil Corporation
Inventors:
Robert M. Gemmill, Jr., Andrew G. Horodysky
Abstract: A phosphonic acid ester of the formula: ##STR1## and R is a lower alkyl, exhibits a calcium-antagonistic activity. Pharmaceutical compositions containing the same are useful in prophylaxis and treatment of ischemic heart diseases such as angina pectoris, myocardial, infarction, etc. and hypertension.
Abstract: There are provided complexes of metal salts prepared by (1) reacting a benzotriazole with a monoepoxide to form a hydroxyalkylbenzotriazole, (2) reacting the hydroxyalkylbenzotriazole with an alkenylsuccinic anhydride to form a monoester, and (3) converting the monoester to the salt of a metal which can form Werner complexes and complexing with a ligand containing amine, hydroxyl, oxazoline, or imidazoline groups to form a chelate. These chelates impart detergent and antiwear properties to lubricants.
Abstract: Mono- and di-thiophosphate esters having an isoxazolinone system attached at its 2-position through an optionally alkyl- or phenyl-substituted methylene or ethylene group to the sulphur or to one of the sulphur atoms are useful as insecticides and/or acaricides.
Abstract: The invention relates to bis-benzotriazole compounds which have been found to be effective ultraviolet stabilizers. The invention also relates to ultraviolet degradable organic compositions containing a stabilizing amount of the bis-benzotriazole compounds to prevent such degradation. These stabilizing compounds 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 ultraviolet stabilizers may also be incorporated into the organic compositions in the polymer melt or dissolved in the polymer dope, coated on the exterior of the molded article, film or extruded fiber.
Type:
Grant
Filed:
February 3, 1978
Date of Patent:
February 5, 1980
Assignee:
Eastman Kodak Company
Inventors:
Gether Irick, Jr., Charles A. Kelly, James C. Martin
Abstract: The invention relates to polychromophoric dibenzoxazole compounds which have been found to be effective ultraviolet stabilizers. The invention also relates to ultraviolet degradable organic compositions containing a stabilizing amount of the polychromophoric dibenzoxazole 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 ultraviolet stabilizers may also be incorporated into the organic compositions in the polymer melt or dissolved in the polymer dope, coated on the exterior of the molded article, film or extruded fiber.
Abstract: This invention relates to new di-triazolylstyrene derivatives, useful as optical brighteners for organic polymeric materials, especially when applied to or incorporated in synthetic fibres.
Abstract: Novel benzoxazole compounds of the formula ##STR1## wherein R.sub.1, R.sub.2 and A are certain substituents, a process for their manufacture as well as their use as optical brighteners are disclosed.