Chalcogen Attached Indirectly To The Phosphorus By Acyclic Nonionic Bonding Patents (Class 558/169)
- Nitrogen bonded directly to the phosphorus (Class 558/171)
- The -C(=X)- is part of a -C(=X)X- group, wherein the X's may be the same or diverse chalcogens (Class 558/172)
- Chalcogen, or additional -C(=X), bonded directly to the nitrogen (Class 558/173)
- Two carbons bonded directly to the same chalcogen (e.g., sulfones, carboxylic acid esters, ethers, etc.) (Class 558/174)
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Patent number: 5116992Abstract: The invention relates to glycerol derivatives of general formulae Ia, Ib and Ic ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, A and Y stand for various substituents, to a preparation process of said compounds and to therapeutical compositions containing the same.Type: GrantFiled: December 19, 1990Date of Patent: May 26, 1992Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)Inventors: Pierre Braquet, Colette Broquet, Benedicte Vandamme, Paola Principe-Nicolas
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Patent number: 5099063Abstract: New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.Type: GrantFiled: June 21, 1990Date of Patent: March 24, 1992Assignee: Merck & Co., Inc.Inventors: William H. Parsons, Arthur A. Patchett, William R. Schoen, Masao Taniguchi
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Patent number: 5095009Abstract: The present invention is directed to a new class of 4-(oxoalkyl)phosphono, 4(oxime alkyl)phosphono, or 4-(hydrazine alkyl)phosphono, 2-piperazine carboxylic derivatives that are useful as NMDA antagonistsType: GrantFiled: July 20, 1990Date of Patent: March 10, 1992Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Jeffrey P. Whitten, Bruce M. Baron
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Patent number: 5091527Abstract: The present invention provides phospholipase substrates of the general formula: ##STR1## wherein A is an alkylene or alkenylene radical containing up to 16 carbon atoms, R is a hydrgen atom or an alkyl, alkenyl or acyl radical containing up to 20 carbon atoms or an optionally alkyl-substituted aryl or aralkyl radical containing up to 8 carbon atoms in the alkyl moiety, X is the residue of an aromatic hydroxy or thiol compound and each Y, independently of one another, is an oxygen or sulphur atom and Z is --SO.sub.3.sup..crclbar. or a radical of the general formula: ##STR2## wherein R.sup.1 can be a hydrogen atom or a radical of the general formula --(CH.sub.2).sub.n NR.sub.3.sup.2, in which n is 2, 3 or 4 and R.sup.2 is a hydrogen atom or a methyl radical, or is an inositol or serine (--CH.sub.2 --CH(NH.sub.2)--COOH) or glycerol residue.The present invention also provides a process for the optical determination of phospholipases using these substrates, as well as a reagent containing them.Type: GrantFiled: March 2, 1989Date of Patent: February 25, 1992Assignee: Boehringer Mannheim GmbHInventors: Martina Junius, Ulrich Neumann, Herbert von der Eltz
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Patent number: 5091550Abstract: 5,5-Bis(perfluoroalkylheteromethyl)-2-hydroxy-2-oxo-1,3,2-dioxaphosphorinan es, derived acyclic phosphorus and phosphoric acids obtained by ring-opening, and salts or esters thereof are prepared from heteroatom containing perfluoroalkyl terminated neopentyl glycols of the formula: HO[CH.sub.2 C(CH.sub.2 --X--E.sub.n --R.sub.f).sub.2 CH.sub.2 O]H by cyclization with appropriate phosphorus containing esters or acids, or hydrolysis. These compositions provide improved thermal stability, and useful low surface energy oil and water repellent coatings for textiles, glass, paper, leather and other materials.Another aspect of this invention relates to the use of the phosphite group containing products as polymer stabilizers.Type: GrantFiled: April 20, 1990Date of Patent: February 25, 1992Assignee: Ciba-Geigy CorporationInventors: Robert A. Falk, Kirtland P. Clark
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Phosphoric acid ester, process for preparing the same, and detergent composition containing the same
Patent number: 5071585Abstract: Phosphoric acid esters represented by the following formulae (I) and (IX) as well as processes for preparing them are disclosed. ##STR1## wherein R.sub.1 represents a linear or branched, alkyl or alkenyl group having a C.sub.1-36 carbon atom content, with or without the hydrogen atom(s) being substituted with fluorine atom(s), or a phenyl group with substituted linear or branched alkyl group(s) having a C.sub.1-15 carbon atom content, R.sub.2 represents an alkylene group having a C.sub.2-3 carbon atom content, R.sub.3 and R.sub.4 independently denote a hydrogen atom or an alkyl group having a C.sub.1-3 carbon atom content, R.sub.5 and R.sub.6 independently denote a hydrogen atom, or an alkyl, alkenyl, or phenyl group with or without the hydrogen atom(s) being substituted with group(s) containing hetero atom(s), excepting for a mercapto group, R.sub.7 and R.sub.Type: GrantFiled: October 29, 1990Date of Patent: December 10, 1991Assignee: Kao CorporationInventors: Akira Matsunaga, Junya Wakatsuki, Nobutaka Horinishi, Takashi Imamura, Tomihiro Kurosaki -
Patent number: 5061806Abstract: New phosphonic acid derivatives are described which display antibacterial activity.Type: GrantFiled: May 24, 1990Date of Patent: October 29, 1991Assignee: Merck & Co., Inc.Inventors: Yoshiharu Morita, Yasuo Hoshide, Haruyuki Chaki, Junko Takashima, Arthur A. Patchett
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Patent number: 5061626Abstract: The invention concerns antigens for the production of antibodies to Platelet Activating Factor (PAF). The antigens are PAF analogues of formula (I) ##STR1## wherein X comprises a high molecular weight group, R.sup.1 is a linking group and R.sup.2 to R.sup.5 are selected from C.sub.1 to C.sub.6 alkyl.Other aspects of the invention include PAF-antibodies produced using said antigens, labelled PAF analogues, intermediates for the preparation of PAF analogues and methods and a kit for the immunoassay of PAF.Type: GrantFiled: November 24, 1987Date of Patent: October 29, 1991Assignee: University of SydneyInventors: Brian A. Baldo, John W. Redmond
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Patent number: 5051413Abstract: The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.Type: GrantFiled: December 18, 1989Date of Patent: September 24, 1991Assignee: Ciba-Geigy CorporationInventors: Christof Angst, Derek E. Brundish, John G. Dingwall, Graham E. Fagg, Hans Allgeier, Guido Bold, Rudolf Duthaler, Roland Heckendorn, Antonio Togni
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Patent number: 5043469Abstract: Process for the introduction of functional or functionalizable substituents para to the amino group in 2-aminophenols and 3-aminophenols. The process proceeds in one step, with substitution occurring selectively at the position para to the amino group. Consequently, the reaction is surprisingly straightforward, with very little or no contamination by isomeric by-products. The process comprises reaction of (a) an aminophenol having an open para position to the amino function, with (b) an unhindered non-enolizable aldehyde, and (c) a thiol or sulfinic acid which acts as a nucleophile. In preferred embodiments, the process is conducted at a temperature of from about 50.degree. C. to about 100.degree. C., and in the presence of a polar solvent. The reaction is promoted by an acid having sufficient acidity to protonate the amino group of the aminophenol. Preferably, the acid promoter is a mineral acid, and it is present in an amount at least substantially equivalent to the amount of aminophenol reactant.Type: GrantFiled: April 13, 1990Date of Patent: August 27, 1991Assignee: Eastman Kodak CompanyInventors: Philip T. S. Lau, Danny R. Thompson
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Patent number: 5034556Abstract: The disclosure is directed to a compound which is a reaction product of at least one phosphonic acid group of an alpha-aminomethylene phosphonic acid containing at least one group corresponding to the formula, ##STR1## with an epoxy group of a compound containing at least one epoxy group. The disclosure is also directed to waterborne coating compositions, organic solvent-borne coating compositions, and powder coating compositions containing the aforesaid reaction product.Type: GrantFiled: April 3, 1989Date of Patent: July 23, 1991Assignee: PPG Industries, Inc.Inventor: Charles F. Kahle, II
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Patent number: 5030733Abstract: Novel hydroxy-, alkoxy- and benzyloxy-substituted phospholipids, a process for the preparation thereof, and methods for treating pain, phospholipase, A.sub.2 mediated inflammation and similar conditions utilizing compounds or compositions thereof are disclosed.Type: GrantFiled: June 15, 1989Date of Patent: July 9, 1991Assignee: Hoechst-Roussel Pharmaceticals IncorporatedInventors: John J. Tegeler, Kirk D. Shoger
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Patent number: 5004826Abstract: The compounds of the formula ##STR1## in which one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, C.sub.1-8 -alkyl, C.sub.3-6 -cycloalkyl, phenyl optionally substituted by halogeno, C.sub. 1-4 -alkyl, C.sub. -4 -alkoxy and/or trifluoromethyl, or C.sub.7-10 -phenylalkyl optionally substituted in the phenyl moiety by halogeno, C.sub.1-4 -alkyl C.sub.1-4 -alkoxy and/or trifluormethyl, and the other two are hydrogen, or salts thereof.These compounds have valuable pharmaceutical properties.Type: GrantFiled: December 1, 1989Date of Patent: April 2, 1991Assignee: Ciba-Geigy CorporationInventors: John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
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Patent number: 4992429Abstract: Disclosed are novel substituted cyclohexenyl phosphinylhydroxybutyrates as 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula: ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: August 24, 1989Date of Patent: February 12, 1991Assignee: Rhone-Poulenc Rorer Pharmaceuticals Inc.Inventors: John W. Ullrich, Kent W. Neuenschwander, John R. Regan
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Phosphoric acid ester, process for preparing the same, and detergent composition containing the same
Patent number: 4985412Abstract: Phosphoric acid esters represented by the following formulae (I) and (IX) as well as processes for preparing them are disclosed. ##STR1## wherein R.sub.1 represents a linear or branched, alkyl or alkenyl group having a C.sub.1-36 carbon atom content, with or without the hydrogen atom(s) being substituted with fluorine atom(s), or a phenyl group with substituted linear or branched alkyl group(s) having a C.sub.1-15 carbon atom content, R.sub.2 represents an alkylene group having a C.sub.2-3 carbon atom content, R.sub.3 and R.sub.4 independently denote a hydrogen atom or an alkyl group having a C.sub.1-3 carbon atom content, R.sub.5 and R.sub.6 independently denote a hydrogen atom, or an alkyl, alkenyl, or phenyl group with or without the hydrogen atom(s) being substituted with group(s) containing hetero atom(s), excepting for a mercapto group, R.sub.7 and R.sub.Type: GrantFiled: October 21, 1988Date of Patent: January 15, 1991Assignee: Kao CorporationInventors: Akira Matsunaga, Junya Wakatsuki, Nobutaka Horinishi, Takashi Imamura, Tomihiro Kurosaki -
Patent number: 4981989Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from one or more of: (a) C.sub.1 -C.sub.24 branched or straight chain alkyl; (b) C.sub.1 -C.sub.24 branched or straight chain alkoxy; (c) ##STR2## wherein n and m are integers from 0 to 25 and the sum of n and m is less than or equal to 25; phenyl; substituted phenyl wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from the group consisting of: ##STR3## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.Type: GrantFiled: November 8, 1989Date of Patent: January 1, 1991Assignee: American Cyanamid CompanyInventors: Allan Wissner, Phaik E. Sum, Robert E. Schaub
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Patent number: 4965391Abstract: Novel radioiodinated analogues of naturally occurring phospholipid ethers are tumor-specific to enable selective visualization of neoplastic lesions by gamma-camera scintigraphy. The novel compounds enable a physician to differentiate neoplastic lesions from non-neoplastic lesions in a manner not heretofore available.Type: GrantFiled: October 23, 1987Date of Patent: October 23, 1990Assignee: The University of MichiganInventors: Raymond E. Counsell, Karen L. Meyer, Susan W. Schwendner
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Patent number: 4962097Abstract: Dipeptide mimics which contain phosphorus and their pharmaceutical use and preparation are disclosed. The compounds have dehydropeptidase (DHP) enzyme inhibitor activity.Type: GrantFiled: August 17, 1989Date of Patent: October 9, 1990Assignee: Merck & Co., Inc.Inventors: William H. Parsons, William R. Schoen, ARthur A. Patchett
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Patent number: 4950776Abstract: Pharmaceutical compositions active on cerebral metabolism and on neuronal transmission containing as the active principle glycerophosphoryl-O-serine.Type: GrantFiled: October 8, 1987Date of Patent: August 21, 1990Assignee: S. Team S.R.L. Corso Lodi, 47Inventors: Carlo Scolastico, Camillo M. Palazzi
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Patent number: 4931575Abstract: Enantiomerically pure glycerol derivatives, e.g. S-1,2-O-isopropylidene, S-1,2-O-benzylidene, and R-1,2-O-dibenzyl glycerol, have been prepared from 1,2R-O-protected erythritols in high yields. The latter compounds are easily obtained from erythorbic acid and are useful building blocks in the synthesis of a host of optically active compounds having biological activity.Type: GrantFiled: March 13, 1987Date of Patent: June 5, 1990Assignee: The Board of Governors for Higher Education, State of Rhode Island and Providence PlantationsInventor: Elie Abushanab
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Patent number: 4921991Abstract: Phosphonic diesters, capable of being employed as intermediates for making herbicides, having the formula ##STR1## in which R denotes a hydrogenolyzable group; preferably an arylalkyl group,R.sup.1 denotes a hydrolyzable group,R.sup.2 denotes a hydrogen atom or hydrolyzable group such as those defined for R.sup.1.Preparation of the compounds of the formula (I) from phosphites, formaldehyde and N-substituted glycine esters.Type: GrantFiled: December 31, 1986Date of Patent: May 1, 1990Inventor: Guy Lacroix
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Patent number: 4921992Abstract: Amide compounds useful as additives in lubricating fluids as extreme pressure/antiwear agents are produced on a manufacturing scale. The amides are produced by simultaneously adding together and reacting a phosphorus-containing acid and aqueous acrylamide. Substantially equal molar amounts of the phosphorus-containing acid and the aqueous acrylamide are added together with sufficient cooling to maintain the reaction at a temperature below 50.degree. C. After isolation, the reaction product obtained is preferably further reacted with a coupling agent, preferably paraformaldehyde.Type: GrantFiled: December 16, 1988Date of Patent: May 1, 1990Assignee: The Lubrizol CorporationInventors: Paul E. Adams, Darryl W. Kinzer
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Patent number: 4916249Abstract: The invention relates to novel glycero-3(2)phospho-L-serine derivatives of the general formula ##STR1## in which A represents unsubstituted or substituted (C5-C30) alkoxy, or unsubstituted or substituted (C5-C30) alkenoxy, whereby a double bond of the alkenoxy residue does not originate at the C atom bound to oxygen, or halogen, or a group of the general formula--O--(CH.sub.2).sub.n --CF.sub.3 II,wherein n is 0 or an integer 1, 2 or 3, one of the two residues B and C, which is identical to or different from A, has one of the definitions given for A or represents hydrogen, and the respective other residue represents the phosphatidyl-Lserine group of the formula ##STR2## with the proviso that at least one residue A, B or C represents (C5-C30) alkoxy or (C5-C30) alkenoxy; and the pharmaceutically acceptable salts of compounds of general formula I with bases, a process for the preparation thereof, pharmaceutical preparations containing the said compounds, and their use in drugs with cytostatic activity.Type: GrantFiled: July 7, 1989Date of Patent: April 10, 1990Inventors: Hans Brachwitz, Peter Langen, Christine Lehmann, Eckart Matthes, Jurgen Schildt, Iduna Fichtner, Albin Hermetter, Friedrich Paltauf
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Patent number: 4914210Abstract: Oligonucleotide functionalizing reagents are disclosed which are useful in introducing sulfhydryl, amino and additional hydroxyl groups into oligonucleotides. The reagents are substantially linear in structure, at one end provided with a phosphoramidite moiety, at an opposing end provided with a sulfhydryl, amino or hydroxyl moiety, the two ends linked through a hydrophilic spacer chain. Methods of using and synthesizing the novel reagents are disclosed as well.Type: GrantFiled: October 2, 1987Date of Patent: April 3, 1990Assignee: Cetus CorporationInventors: Corey Levenson, Chu-An Chang, Fred T. Oakes
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Patent number: 4900731Abstract: Antihypertensive phosphate derivatives are described having the following formula: ##STR1## wherein n is an integer 1 or 2; m is an integer 1 or 2, and the sum of n and m must be 3; X is selected from the group consisting of C.sub.1 -C.sub.24 branched or straight chain alkoxy and substituted phenoxy wherein the substituents are selected from one or more of the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, phenyl and substituted phenyl; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino, Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR).sub.p --, where p is an integer from 2 to 12 and the moiety --(CHR).sub.Type: GrantFiled: September 15, 1987Date of Patent: February 13, 1990Assignee: American Cyanamid CompanyInventors: Allan Wissner, Robert E. Schaub
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Patent number: 4898944Abstract: Precursors for the preparation of fiber-reactive triphendioxazine dyestuffs correspond to the general formulas: ##STR1## in which Y' is a vinyl, a beta-hydroxyethyl or an ethyl group which contains in the beta-position a substituent which can be eliminated by an alkali;T is an optionally substituted alkyl (e.g.Type: GrantFiled: October 27, 1988Date of Patent: February 6, 1990Assignee: Hoechst AktiengesellschaftInventors: Gunther Schwaiger, Hartmut Springer, Walter Helmling
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Patent number: 4897382Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.Type: GrantFiled: June 21, 1988Date of Patent: January 30, 1990Assignee: Fidia S.p.A.Inventors: Francesco della Valle, Aurelio Romeo
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Patent number: 4897385Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from the group consisting of a phenyl radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen, and a naphthalene radical substituted at any position with a C.sub.1 -C.sub.20 branched or straight chain alkoxy or benzyloxy and optionally substituted at any other positions with one or more groups consisting of C.sub.1 -C.sub.15 branched or straight chain alkyl, C.sub.1 -C.sub.15 branched or straight chain alkoxy and halogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.Type: GrantFiled: September 15, 1987Date of Patent: January 30, 1990Assignee: American Cyanamid CompanyInventors: Allan Wissner, Phaik-Eng Sum
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Patent number: 4888328Abstract: Novel alkoxycarbonylalkylalkylphospholipids and alkylaminocarbonylalkylphospholipids of the formula ##STR1## wherein A.sup.1 is a bivalent radical of the formula --C.sub.m H.sub.2m --wherein m is an integer having a value from 0 to 20, inclusive; A.sup.2 is a bivalent radical of the formula --C.sub.p H.sub.2p --wherein p is an integer having a value from 2 to 6, inclusive; X is a bivalent radial of the formula --O--or --N(R)--wherein R is selected from the group consisting of hydrogen, alkyl radicals having up to 6 carbon atoms, inclusive and phenyl radicals of the formula: ##STR2## where Z and a are as difined in the specification; Y is ##STR3## wherein R.sup.1 is an anlkyl radicals having up to 6 carbon atoms, inclusive and R.sup.2 and R.sup.3 are independently alkyl radicals having up to 6 carbon atoms, inclusive, or taken together with R.sup.1 and the nitrogen atom to which they are attached form a group of the formula ##STR4## wherein r is 0 or 1, and W is oxygen, CH.sub.2, sulfur or N(R.sup.Type: GrantFiled: March 10, 1988Date of Patent: December 19, 1989Assignee: Hoeschst-Roussel IncorporatedInventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
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Patent number: 4827011Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is a C.sub.1 -C.sub.24 branched or straight chain alkyl group; R is selected from the group consisting of hydrogen and C.sub.1 -C.sub.4 alkyl, with the proviso that at least one R group is not hydrogen; T is selected from the group consisting of hydrogen and ##STR2## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.4 branched or straight chain alkoxy and C.sub.1 -C.sub.4 branched or straight chain alkylamino; Q is a bivalent radical selected from the group consisting of --(CH.sub.2).sub.p -- and --(CHR.sup.1).sub.p --, wherein p is an integer from 2 to 12 and the moiety --(CHR.sup.1).sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.10 alkyl groups or phenyl groups; Z is selected from the group consisting of ##STR3## wherein R.sub.Type: GrantFiled: December 10, 1984Date of Patent: May 2, 1989Assignee: American Cyanamid CompanyInventors: Allan Wissner, Robert E. Schaub
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Patent number: 4824978Abstract: The diacylesters, particularly bis(pyridyl-3-carboxilate) of glycerylphosphorylcholine, both optically active L(alpha) or racemic D,L(alpha) and their complexes having general formula: ##STR1## wherein: Y represents ##STR2## M represents Ca, Mg, Al, Zn X represents a halogen, particularly chlorine, n=2,3 ed m=0,1 are anti-dislipemic and cerebroactive agents.Their preparation takes place through acylation with an anhydride of a complex of glycerylphosphorylcholine with calcium or zinc chloride.Type: GrantFiled: July 7, 1987Date of Patent: April 25, 1989Assignee: Neopharmed SpaInventors: Carlo Scolastico, Giovanni Tronconi
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Patent number: 4824603Abstract: Amphoteric and zwitter-ionic phosphate surfactants corresponding to the following formula ##STR1## (a) in which R.sup.1 is a C.sub.6 -C.sub.22 alkyl group, a group R.sup.4 (OC.sub.n H.sub.2n).sub.x --, where n=2 to 4, x=1 to 6, and R.sup.4 is a C.sub.6 -C.sub.22 alkyl group, or a group R.sup.5 --CONH(CH.sub.2).sub.m, where R.sup.5 is a C.sub.5 -C.sub.21 group and m=2 to 4; R.sup.2 is hydrogen; and R.sup.3 is a C.sub.1 -C.sub.4 alkyl group or a group --(C.sub.n H.sub.2n O).sub.x --H or --(C.sub.n H.sub.2n O).sub.x --PO.sub.3 H.sub.2, where n=2 to 4 and x=1 to 6, or(b) in which R.sup.1 is a C.sub.1 -C.sub.4 alkyl group or a C.sub.2 -C.sub.4 2-hydroxyalkyl group; R.sup.2 is a C.sub.6 -C.sub.22 alkyl group; and R.sup.3 is as defined above.to mixtures thereof with correspondingly substituted phosphate surfactants corresponding to formula (I), in which the --PO.sub.3 H.sub.2 group or groups are replaced by hydrogen; and to neutral and basic salts of the foregoing.Type: GrantFiled: October 28, 1987Date of Patent: April 25, 1989Assignee: Henkel Kommanditgesellschaft auf AktienInventors: Hinrich Moller, Ulrich Zeidler
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Patent number: 4820632Abstract: The present invention is concerned with the use of aniline derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkyl or aryl radical, R.sub.2 is a hydrogen atom or a lower alkyl radical which can be substituted by hydroxyl, amino, carboxyl, lower alkoxycarbonyl, lower alkanoylamido, aryl lower alkyl or aryl or by a group of the structure: ##STR2## in which R.sub.5 and R.sub.6 have the meanings given hereinafter, R.sub.3 is a hydrogen or halogen atom or a carboxyl group, R.sub.4 and R'.sub.4, which can be the same or different, are hydrogen or halogen atoms, carboxyl groups or lower alkoxy radicals or lower alkyl radicals which are preferably in the m-position and R.sub.1 and R.sub.4 or R.sub.2 and R.sub.4 or R.sub.4 and R'.sub.4, when the two substituents are ortho to one another, can together form a saturated or unsaturated hydrocarbon chain containing 2 to 6 carbon atoms which can be substituted by hydroxyl or oxo groups, R.sub.Type: GrantFiled: September 10, 1985Date of Patent: April 11, 1989Assignee: Boehringer Mannheim GmbHInventors: Gunter Frey, Gerd Zimmermann
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Patent number: 4795578Abstract: A process and composition are provided for the froth flotation beneficiation of iron minerals from iron ores containing silicate and phosphate minerals, comprising as collectors a combination of a primary amine and a nitrogen compound containing an anionic group selected from methylene carboxylic acid, ethylene phosphoric acid and methylene phosphonic acid.Type: GrantFiled: December 21, 1987Date of Patent: January 3, 1989Assignee: Berol Kemi ABInventors: Martin Hellsten, Marie Ernstsson, Bo Idstrom
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Patent number: 4788182Abstract: Described are phosphatidyl compounds of the formula I ##STR1## in which R.sup.1 represents C.sub.3-14 -alkanoyl, benzoyl, the acyl radical of an .alpha.-aminocarboxylic acid that is other than glycine, L-alanine and derivatives thereof having a substituted amino group, and of which the .alpha.-amino group may be substituted by lower alkanoyl, lower alkoxycarbonyl or by benzyloxycarbonyl, or the acyl radical of a .beta.-aminocarboxylic acid or an .alpha.- or .beta.-hydroxycarboxylic acid,T represents a group NH that is unsubstituted or is substituted by lower alkyl, or oxygen,Y represents dimethylene that is unsubstituted or is substituted by free, etherified or amidated carboxy,W represents hydrogen, andZ represents a 1,2-dihydroxyethyl, 2-hydroxyethyl or hydroxymethyl group, in which at least one of the hydroxy groups is esterified by an aliphatic C.sub.8-30 -carboxylic acid or is etherified by an aliphaticC.sub.Type: GrantFiled: October 23, 1987Date of Patent: November 29, 1988Assignee: Ciba-Geigy CorporationInventors: Gerhard Baschang, Bruno Fechtig, Albert Hartmann, Bohumir Lukas, Oskar Wacker
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Patent number: 4786728Abstract: Triphendioxazine compounds with properties of fiber-reactive dyestuffs corresponding to the general formula ##STR1## in which T is an optionally substituted alkyl group with 1 to 6 carbon atoms, excluding a radical of the group Y defined below, it also being possible for the alkyl group to be interrupted by hetero atoms, or is an optionally substituted aryl group,B is an oxygen or sulfur atom or an amino group,W is a divalent, optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic-carbocyclic radical or a benzotriazole radical combined with one of these radicals, it being possible for the aliphatic radicals to be interrupted by hetero groups and/or for aliphatic and aryl radicals to be bonded to one another by a hetero group,R is hydrogen, alkyl with 1 to 6 carbon atoms, alkoxy with 1 to 5 carbon atoms, halogen, carboxy or sulfo,X.sup.Type: GrantFiled: September 18, 1986Date of Patent: November 22, 1988Assignee: Hoechst AktiengesellschaftInventors: Gunther Schwaiger, Hartmut Springer, Walter Helmling
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Patent number: 4778912Abstract: Phospholipid derivatives of the formula: ##STR1## wherein R.sup.1 is a higher alkyl, acylmethyl or alkylcarbamoyl group which may be substituted by cycloalkyl; R.sup.2 is a lower alkyl which may be substituted by carboxy, formyl or lower acyl, a carbamoyl or thiocarbamoyl group which is substituted by lower alkyl, or an acetoacetyl group; R.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or lower alkyl, or ##STR2## represents a cyclic ammonio group; and n represents an integer of 8 to 14, and salts thereof have antitumor activity.Type: GrantFiled: November 21, 1986Date of Patent: October 18, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Normura, Tetsuya Okutani
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Patent number: 4775758Abstract: Novel phospholipids, inclusive of salts thereof, of the formula ##STR1## wherein R.sup.1 and R.sup.2 are independently an aliphatic hydrocarbon residue containing 1 to 20 carbon atoms, with the numbers of the carbon atoms for both totalling 8 to 30, andR.sup.3, R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 alkyl, or ##STR2## represents a cyclic ammonio group, exhibit inhibitory activity against multiplication or tumor cells and antifungal activity.Type: GrantFiled: October 28, 1986Date of Patent: October 4, 1988Assignee: Takeda Chemical Industries, Ltd.Inventors: Shoshichi Nojima, Hiroaki Nomura, Susumu Tsushima
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Patent number: 4774350Abstract: Novel phosphoric esters represented by the following general formula (I) ##STR1## wherein R.sub.1 represents a linear or branched alkyl or alkenyl group having 1 to 36 carbon atoms, or a phenyl group substituted with a linear or branched alkyl group having 1 to 15 carbon atoms, R.sub.2 represents an alkylene group having 2 to 3 carbon atoms, R.sub.3, R.sub.4 and R.sub.5 individually represent a hydrogen atom or a linear or branched alkyl group having 1 to 36 carbon atoms providing that any one of R.sub.3, R.sub.4 and R.sub.5 has 5 or more carbon atoms, and n is a number from 0 to 30 are obtained by reacting phosphoric esters of the following formula ##STR2## with amines at a high purity and in a high yield. The phosphoric esters (I) are excellent in the surface tension and foaming property, and give extremely low stimulus to the skin, so that they can be utilized in detergent compositions, cosmetic compositions, emulsifiers, dispersants, anti-static agents and the like.Type: GrantFiled: August 13, 1986Date of Patent: September 27, 1988Assignee: Kao CorporationInventors: Junya Wakatsuki, Tohru Katoh, Tomihiro Kurosaki
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Patent number: 4762942Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein X is selected from one or more of: (a) C.sub.1 -C.sub.24 branched or straight chain alkyl; (b) C.sub.1 -C.sub.24 branched or straight chain alkoxy; (c) ##STR2## wherein n and m are integers from 0 to 25 and the sum of n and m is less than or equal to 25; phenyl; substituted phenyl wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, C.sub.1 -C.sub.20 branched or straight chain alkoxy, halogen, trifluoromethyl, phenyl, and substituted phenyl, phenoxy; and substituted phenoxy, wherein the substituents are selected from the group consisting of C.sub.1 -C.sub.20 branched or straight chain alkyl, halogen, trifluoromethyl, phenyl and substituted phenyl; Q is selected from the group consisting of: ##STR3## wherein R.sub.1 is selected from the group consisting of hydrogen, C.sub.1 -C.sub.4 branched or straight chain alkyl, C.sub.1 -C.sub.Type: GrantFiled: December 10, 1984Date of Patent: August 9, 1988Assignee: American Cyanamid Co.Inventors: Allan Wissner, Phaik E. Sum, Robert E. Schaub
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Patent number: 4755614Abstract: Preparation of intermediates for herbicides of formula ##STR1## by the reaction of organic phosphites with benzoxazines of formulaBzx--CH.sub.2 --CO--Y (II)in whichBzx denotes the radical of formula: ##STR2## X is a usual substituent of phenols n is an integer from 0 to 4R.sup.1 and R.sup.2 are H or such that OR.sup.1 and OR.sup.2 are hydrolyzableY is --OM or --NR.sup.3 R.sup.4M is H or is such that COOM is a salt or an esterR.sup.3 and R.sup.4 are H or a hydrocarbon radical, and one of them can be R.sup.5 --SO.sub.2 --, andR.sup.5 is a hydrocarbon radical, substiuted if appropriate. Products obtained by the process and their use as herbicides.Type: GrantFiled: March 20, 1986Date of Patent: July 5, 1988Assignee: Rhone-Poulenc AgrochimieInventor: Jean-Pierre Corbet
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Patent number: 4751320Abstract: A novel phosphoric ester represented by the following formula (I): ##STR1## is produced by halogenating the hydroxyl group of a monoalkyl phosphoric acid, reacting the halogenated product with N-benzoyloxycarbonyl serine ester and then removing protecting groups for the carboxyl group and amino group.According to the present production process, the phosphoric ester can be obtained inexpensively at a high yield and high purity. Further, the phosphoric ester has a structure similar to that of the phospholipid and has nitrogen-containing polar groups such as amino group in one molecule, so that it has excellent emulsification ability and moisture keeping function. It is thus useful as emulsifiers, humectants and the like.Type: GrantFiled: October 31, 1986Date of Patent: June 14, 1988Assignee: Kao CorporationInventors: Mitsuharu Masuda, Tomihiro Kurosaki
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Patent number: 4749805Abstract: Compounds related to phospholipids and a method for their preparations.Type: GrantFiled: February 11, 1987Date of Patent: June 7, 1988Assignee: Max-Planck-Gesellschaft Zur Foerderung der Wissenschaften e.V.Inventor: Hansjorg Eibl
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Patent number: 4742051Abstract: Compounds are described having the formula ##STR1## wherein R.sup.1 is an alkyl or alkenyl group having from about 11 to about 23 carbon atoms;R.sup.2 is hydrogen or an alkyl or alkenyl group having from about 1 to about 11 carbon atoms;R.sup.3 is NR.sub.4 R.sub.5 or NR.sub.4 R.sub.5 R.sub.6.sup.+ An.sup.-wherein R.sub.4, R.sub.5 and R.sub.6 are independently hydrogen or lower alkyl having from 1 to 3 carbon atoms and An is an anion; andY represents the hydrogens of a methylene group or the oxygen of a carbonyl group.These compounds are useful as vasodilators and antihypertensive agents.Type: GrantFiled: July 17, 1981Date of Patent: May 3, 1988Assignee: University of Tennessee Research CorporationInventors: Ernest E. Muirhead, Byron E. Leach, deceased, Lawrence W. Byers
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Patent number: 4735649Abstract: Novel hydroxyalkylesters of N-phosphonomethylglycine have been identified which prove to be effective gametocides.Type: GrantFiled: September 25, 1985Date of Patent: April 5, 1988Assignee: Monsanto CompanyInventors: Om P. Dhingra, John E. Franz, Geoffrey Keyes, Dale F. Loussaert, Cynthia S. Mamer
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Patent number: 4734225Abstract: The mannite derivatives have the formula (1) wherein R' and R.sup.2, idenal or different, represent when they are identical a straight or branched alkyl, alkenyl or alkynyl group containing from 5 to 24 atoms of carbon which may be substituted by a cycloalkyl residue having from 3 to 6 atoms of carbon, an aryl, benzyloxy, allyloxy, mesyloxy residue and/or halogen atoms and when R' and R.sup.2 are different, they represent a straight or branched alkyl group with 1 to 24 atoms or carbon, which may be substituted by a cycloalkyl residue having from 3 to 6 atoms of carbon, an aryl, benzyloxy, allyloxy, mesyloxy residue and/or halogen atoms, with the possibility for R' of being also a trityl group. From said mannite derivatives, it is possible to obtain in a simple way and with good yields the phospholipids in the form of their optical stereo isomers.Type: GrantFiled: March 5, 1984Date of Patent: March 29, 1988Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.Inventor: Hansjorg Eibl
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Patent number: 4725588Abstract: The composition of this invention is 1-O-alkyl-2-acetoyl-sn-glycero-3-phosphocholine, having the ionic structural formula; ##STR1## wherein R is saturated alkyl having 9-21 carbon atoms, or salts or hydrates of the composition. Preferably R has 13-19 carbon atoms and most preferably R has 15 carbon atoms. The composition of this invention is useful for reducing hypertension in warm-blooded animals, including humans, when administered either orally or by injection or innoculation, e.g., intravenous injection. The composition can be prepared from naturally occurring lipids or synthetically from commercially available material.Type: GrantFiled: February 9, 1981Date of Patent: February 16, 1988Assignee: The United States of America as represented by the United States Department of EnergyInventors: Fred L. Snyder, Merle L. Blank, Ernest E. Muirhead, Byron E. Leach, deceased, Lawrence W. Byers
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Patent number: 4723029Abstract: This invention relates to organic acid-substituted guanidine compounds. Also disclosed are methods for preparing the compounds, compositions containing them, and methods for their use as anthelmintics.Type: GrantFiled: September 23, 1983Date of Patent: February 2, 1988Assignee: Schering CorporationInventors: Dhiru B. Vashi, Jeffrey N. Clark, Neil A. Lindo
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Patent number: 4717512Abstract: Preparation of chemically defined pure enantiomeric 1,2-diacyl-sn-glycero-3-phosphocholines and 1,2-diacyl-sn-glycero-3-phosphoethanolamines which are substituted in positions 1 and 2 of the glycerol, by acylation of triphenylmethyl derivatives of sn-glycero-3-phosphocholine and sn-glycero-3-phosphoethanolamine.Type: GrantFiled: July 29, 1986Date of Patent: January 5, 1988Assignee: Chemie Linz AktiengesellschaftInventors: Friedrich Paltauf, Albin Hermetter
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Patent number: 4715994Abstract: New 3-(1-aminoalkylphosphinyl)-(2-substituted)propionic acids are described which display antibacterial activity and potentiate carbapenem antibiotics.Type: GrantFiled: November 5, 1986Date of Patent: December 29, 1987Assignee: Merck & Co., Inc.Inventors: William H. Parsons, William R. Schoen, Arthur A. Patchett, Masao Taniguchi