The Chalcogen, X, Is In A -c(=x)- Group, Which Group Is Bonded Directly To The Nitrogen Patents (Class 558/170)
  • Patent number: 5412137
    Abstract: A process for preparing compounds of the formula ##STR1## where X.sub.1 and X.sub.2 are independently O or S, andR.sub.1 is as defined herein,R.sub.2, R.sub.3, and R.sub.4 are each independently straight or branched chain (C.sub.1-4)alkyl,and pharmaceutically acceptable salts, physiological hydrolyzable esters, and pro-drug forms thereof, which are useful as hypoglycemic agents.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: May 2, 1995
    Assignee: Sandoz Ltd.
    Inventors: Mahavir Prashad, Prasad K. Kapa
  • Patent number: 5401845
    Abstract: Compounds of the formula I ##STR1## in which x is 1, 2 or 3, and, if x=1, R.sup.1 is C.sub.1 -C.sub.30 alkyl, C.sub.1 -C.sub.18 alkyl substituted by halogen, --COOR.sup.2, --CN, --NR.sup.3 R.sup.4 or by --CONR.sup.3 R.sup.4, C.sub.2 -C.sub.18 alkyl which is interrupted by --NR.sup.5 --, --O-- or --S--, C.sub.3 -C.sub.18 alkenyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, phenyl which is unsubstituted or substituted by C.sub.1 -C.sub.12 alkyl, halogen, phenyl-C.sub.1 -C.sub.4 alkyl and/or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 is naphthyl, a radical of the formula ##STR2## R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl or phenyl-C.sub.1 -C.sub.4 alkyl, R.sup.6 is hydrogen, methyl, allyl or benzyl, R.sup.7 is hydrogen or --OR.sup.9, R.sup.8 is hydrogen or methyl, R.sup.9 is hydrogen or C.sub.1 -C.sub.30 alkyl, R.sup.10 and R.sup.11, independently of one another, are hydrogen or C.sub.1 -C.sub.
    Type: Grant
    Filed: March 11, 1994
    Date of Patent: March 28, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Rita Pitteloud, Peter Hofmann, Rudolf Maul, Volker Schenk, Eduard Troxler, Horst Zinke
  • Patent number: 5391800
    Abstract: A method of inhibiting tumor cell chemotactic and/or chemoinvasion motility comprising contacting the tumor cell with an inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting phagokinetic activity of tumor cells and neutrophils comprising contacting the cells with a phagokinetic inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives. A method of inhibiting tumor cell metastasis comprising administering to a host in need of treatment a metastasis inhibitory amount of an agent selected from the group consisting of sphingosine-1-phosphate, derivatives of sphingosine-1-phosphate, and mimetics of the sphingosine-1-phosphate or of the derivatives, and pharmaceutically acceptable salts of the agent.
    Type: Grant
    Filed: August 9, 1993
    Date of Patent: February 21, 1995
    Assignee: The Biomembrane Institute
    Inventors: Yasuyuki Igarashi, Fuqiang Ruan, Yoshito Sadahira, Shigeyuki Kawa, Sen-itiroh Hakomori
  • Patent number: 5362899
    Abstract: A stereospecific method of preparing alpha-aminophosphonic acids and derivatives thereof is provided. A protected amino acid is converted to a acyl aroyl or diacyl peroxide which spontaneously rearranges to form an alpha-amino ester. This rearrangement occurs stereospecifically with retention of configuration. The ester is subsequently converted to an appropriate leaving group and displaced with a phosphite yielding a chiral alpha-aminophosphonic acid or derivative.Alpha-aminophosphonic acids are useful for the synthesis of peptide analogs that possess a phosphonate linkage in the place of an amide linkage. This substitution can impart protease resistance in therapeutic peptides thereby increasing the serum half-life.
    Type: Grant
    Filed: September 9, 1993
    Date of Patent: November 8, 1994
    Assignee: Affymax Technologies, N.V.
    Inventor: David A. Campbell
  • Patent number: 5362906
    Abstract: The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention, and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: June 18, 1993
    Date of Patent: November 8, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker
  • Patent number: 5348670
    Abstract: Lubricant additives are disclosed which are produced by reacting an alkanolamine, a carboxylic acid and phosphorous acid. The reaction product may also include a boron compound and/or a monofunctional alcohol. The additives are useful in combination with metalworking oils, particularly in extreme pressure applications, to replace currently used chlorinated paraffin additives.
    Type: Grant
    Filed: February 4, 1993
    Date of Patent: September 20, 1994
    Assignee: The Elco Corporation
    Inventors: Randolph A. McDonald, Gerald D. Burt
  • Patent number: 5344930
    Abstract: Compounds of the general formula: ##STR1## are useful as surfactants in the preparation of fluorocarbon emulsions, which can be used as oxygen-carrying blood substitutes, and for many other therapeutic and diagnostic applications. They are further useful in liposomal formulations which are themselves therapeutic agents or provide a vehicle for such agents.
    Type: Grant
    Filed: November 8, 1993
    Date of Patent: September 6, 1994
    Assignee: Alliance Pharmaceutical Corp.
    Inventors: Jean G. Riess, Francois Jeanneaux, Marie-Pierre Krafft, Catherine Santaella, Pierre Vierling
  • Patent number: 5329029
    Abstract: An efficient, technically straightforward and inexpensive process for generating conjugates of phospholipids with biologically important molecules is described.
    Type: Grant
    Filed: November 5, 1992
    Date of Patent: July 12, 1994
    Inventor: Barbara Y. Wan
  • Patent number: 5321153
    Abstract: This invention is selected novel chiral (essentially pure) alpha-amino phosphonates, process for the preparation which is a catalytic asymmetric hydrogenation of olefins and novel intermediates therefor. The alpha-amino phosphonates are useful as antibiotics and/or as intermediates in the preparation of phosphorus-containing analogs of peptides, i.e., phosphonopeptides or pseudopeptides having known uses, such as in antibiotics, antibiotic enhancers, or enzyme inhibitors.
    Type: Grant
    Filed: June 15, 1992
    Date of Patent: June 14, 1994
    Assignee: Monsanto Company
    Inventor: John J. Talley
  • Patent number: 5304549
    Abstract: Compounds of the formula ##STR1## wherein A is the group ##STR2## R.sup.1 is hydrogen, amino, protected amino, acylamino or lower alkyl optionally substituted by aryl, hydroxy, protected hydroxy, amino, protected amino, acylamino, maleimido, succinimido, naphthalimido, 2,3-dihydro-1,3-dioxo-1H-benz[d,e]isoquinol-2-yl, carboxy, protected carboxy, carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, carboxy-lower alkanoylamino, pyrrolidino or morpholino; R.sup.2 is hydrogen or lower alkyl optionally substituted by aryl, amino, protected amino, di(lower alkyl)- amino, guanidino, carboxyl, protected carboxyl, carbamoyl, mono(lower alkyl) carbamoyl, di(lower alkyl)carbamoyl, di(lower alkoxy)phosphinyl, dihydroxyphosphinyl, pyrrolidino, piperidino or morpholino; R.sup.3 is hydrogen or lower alkyl optionally substituted by hydroxy, protected hydroxy, amino or protected amino; R.sup.4 is hydrogen, hydroxy, lower alkoxy or benzyloxy; and R.sup.
    Type: Grant
    Filed: January 21, 1992
    Date of Patent: April 19, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael J. Broadhurst, Paul A. Brown, William H. Johnson, Geoffrey Lawton
  • Patent number: 5300494
    Abstract: The invention relates to a method for topical application of a pharmaceutically or therapeutically active agent through the use of a covalent chitosan derivative or chitosonium polymer. The present invention is particularly well suited for the topical delivery of pharmaceutically active quaternary ammonia compounds of the formula: ##STR1## wherein R is alkyl having between 5 and 11 carbon atoms.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: April 5, 1994
    Assignee: Union Carbide Chemicals & Plastics Technology Corporation
    Inventors: George L. Brode, II, George A. Salensky
  • Patent number: 5298655
    Abstract: The present invention is directed to farnesyl pyrophosphate analogs which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention, and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
    Type: Grant
    Filed: September 27, 1991
    Date of Patent: March 29, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Neville J. Anthony, Ta-Jyh Lee, Robert L. Smith, Gerald E. Stokker
  • Patent number: 5298499
    Abstract: Substituted phosphorothioate derivatives and pharmaceutical compositions thereof as potential antiradiation agents are disclosed.
    Type: Grant
    Filed: July 5, 1991
    Date of Patent: March 29, 1994
    Assignee: Research Triangle Institute
    Inventors: Frank I. Carroll, Philip Abraham
  • Patent number: 5294616
    Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: March 25, 1992
    Date of Patent: March 15, 1994
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Melissa S. Egbertson, Wasyl Halczenko, George D. Hartman, Laura M. Turchi, William L. Laswell
  • Patent number: 5274162
    Abstract: The composition, methods of synthesis, and applications of a new class of tumor selective antineoplastic drugs is described. These novel antineoplastic agents are of the general structure: A-C-B. The agents are designed with two key functionalities: a trigger which toxifies the drug; (A) and a deactivator which detoxifies the drug (B) The trigger is selected such that it is activated by an enzyme which is present in elevated levels in the tumor. The deactivator is selected such that it is actuated by an enzyme ubiquitous to all tissues. The fate of the drug in a given cell is then determined by the ratio of the enzymatic activity that triggers toxication to the enzymatic activity which detoxifies the drug. The partitioning of the drug between toxic metabolite and nontoxic metabolite defines the resulting specificity of cytotoxic effect.
    Type: Grant
    Filed: December 13, 1991
    Date of Patent: December 28, 1993
    Inventor: Arnold Glazier
  • Patent number: 5232915
    Abstract: 9.alpha.-Hydroxy-19,11.beta.-bridged steroids of general formula I ##STR1## are described. The more detailed meaning of A, B, R.sup.1, R.sup.2, G, Z, R.sup.4 --Y and R.sup.4' --Y' follows from the description. The steroids of general formula I have antigestagen and/or antiglucocorticoidal action and can be used for the production of pharmaceutical agents.
    Type: Grant
    Filed: January 14, 1992
    Date of Patent: August 3, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Eckhard Ottow, Gunter Neef, Rudolf Wiechert, Walter Elger, Sybille Beier, Karl-Heinrich Fritzemeier
  • Patent number: 5215976
    Abstract: There is provided longlasting contraceptives against human and animal sperm which contain a synthetic phospholipid spermicide of the formula: ##STR1## wherein: x=1 to 3 or mixtures thereof;x+y=3;z=x;a=0 to 2;B=0.sup.- or OM;A=Anion;M is a cation;R, R.sub.1 and R.sub.2 are the same or different and are alkyl, substituted alkyl, alkyl aryl or alkenyl groups of up to 16 carbon atoms with the proviso that the total carbon atoms in R+R.sub.1 +R.sub.2 is between 10 and 24; or ##STR2## wherein: x is as hereinabove defined;x+y=3;z=x;a=0 to 2;B=O.sup.- or OM;A is on Anion;M is a Cation;R.sub.3 is an amidoamine moiety of the formula: ##STR3## wherein: R.sub.7 is alkyl, alkenyl, alkoxy or hydroxyalkyl of from 5 to 21 carbon atoms each, or aryl or alkaryl of up to 20 carbon atoms;R.sub.6 is hydrogen or alkyl, hydroxyalkyl or alkenyl of up to 6 carbon atoms each or cycloalkyl of up to 6 carbon atoms, polyoxyalkylene of up to 10 carbon atoms;R.sub.4 and R.sub.
    Type: Grant
    Filed: June 19, 1992
    Date of Patent: June 1, 1993
    Assignee: Mona Industries, Inc.
    Inventors: Dennis L. Fost, Joseph A. Komor
  • Patent number: 5208224
    Abstract: Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.
    Type: Grant
    Filed: March 13, 1991
    Date of Patent: May 4, 1993
    Assignee: Warner-Lambert Company
    Inventors: Gary L. Bolton, Janak K. Padia, Bharat K. Trivedi
  • Patent number: 5194654
    Abstract: Compounds are disclosed for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and human immunodeficiency virus (HIV) by means of lipid derivatives of antiviral agents. The compounds consist of lipid derivatives of phosphonoacids having antiviral activity which are linked, commonly through the phosphate group of the phosphonoacid, to one of a selected group of lipids.The lipophilic nature of these compounds provides advantages over the use of the phosphonoacids alone. It also makes it possible to incorporate them into the lamellar structure of liposomes when combined with similar molecules. In the form of liposomes, these antiviral molecules are preferentially taken up by macrophages and monocytes, cells which have been found to harbor the target human immunodeficiency virus (HIV).
    Type: Grant
    Filed: November 22, 1989
    Date of Patent: March 16, 1993
    Assignee: Vical, Inc.
    Inventors: Karl Y. Hostetler, Raj Kumar
  • Patent number: 5179085
    Abstract: N-substituted .alpha.-amino acids and derivatives thereof are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in selectively blocking the N-methyl-D-aspartate (NMDA) excitatory amino acid receptors in mammals and also are useful in treating cerebrovascular disorders such as cerebral ischemia or cerebral infarction resulting from thromboembolic or hemorrhagic stroke, cerebral vasospasm, hypoglycemia, cardiac arrest, status epilepticus and cerebral trauma as well as for treating schizophrenia, epilepsy, neurodegenerative disorders, Alzheimer's disease or Huntington's disease and also additionally useful as anesthetics in surgical procedures where a finite risk of cerebrovascular damage exists.
    Type: Grant
    Filed: April 22, 1991
    Date of Patent: January 12, 1993
    Assignee: Warner-Lambert Company
    Inventors: Christopher F. Bigge, Graham Johnson
  • Patent number: 5171678
    Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6; R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.
    Type: Grant
    Filed: April 17, 1990
    Date of Patent: December 15, 1992
    Assignee: Centre National de la Recherche Scientifique
    Inventors: Jean-Paul Behr, Jean-Philippe Loeffler
  • Patent number: 5155100
    Abstract: The invention relates to the N-phosphonomethyl-biaryl substituted dipeptide derivatives of formula I ##STR1## wherein A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; R.sub.2 represents hydrogen, hydroxy, lower alkyl, aryl-lower alkyl, C.sub.5 -C.sub.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: October 13, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Mark D. Erion, Stephane De Lombaert
  • Patent number: 5155099
    Abstract: Compounds of formula I ##STR1## in which R denotes a straight-chain or branched, saturated or unsaturated aliphatic hydrocarbon radical having 6-30 C atoms wich may optionally be substituted by halogen or the radicals OR.sub.1, SR.sub.1 or NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 in each case denote a hydrogen atom or an alkyl or acyl radical having 1-6 C atoms which have excellent virustatic and cytostatic action.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: October 13, 1992
    Assignee: Hafslund Nycomed Pharma Aktiengesellschaft
    Inventors: Hans Brachwitz, Reinhild Schonfeld, Peter Langen, Friedrich Paltauf, Albin Hermetter
  • Patent number: 5151521
    Abstract: New phosphonic acid derivatives are described which display antibacterial activity.
    Type: Grant
    Filed: June 12, 1991
    Date of Patent: September 29, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Yoshiharu Morita, Haruyuki Chaki, Yasuo Hoshide, Junko Takashima, Arthur A. Patchett
  • Patent number: 5147868
    Abstract: Novel chemical compounds are provided which selectively inhibit the metabolism of dipeptidase (E.C.3.4.13.11) and therefore are useful in combination with antibacterial products. These chemical compounds are z-2-acylamino-3-monosubstituted propenoates.
    Type: Grant
    Filed: February 19, 1992
    Date of Patent: September 15, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Donald W. Graham, Edward F. Rogers, Frederick M. Kahan
  • Patent number: 5144045
    Abstract: Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: September 1, 1992
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Robert E. Schaub, Kenneth E. Green, Philip R. Hamann
  • Patent number: 5116992
    Abstract: 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: Grant
    Filed: December 19, 1990
    Date of Patent: May 26, 1992
    Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques (S.C.R.A.S.)
    Inventors: Pierre Braquet, Colette Broquet, Benedicte Vandamme, Paola Principe-Nicolas
  • Patent number: 5091550
    Abstract: 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: Grant
    Filed: April 20, 1990
    Date of Patent: February 25, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert A. Falk, Kirtland P. Clark
  • Patent number: 5073547
    Abstract: A monophosphorylated L-dopa ester of formula ##STR1## (wherein the asterisk, R, R.sub.1, R.sub.2 and R.sub.3 have the meanings shown in the description),salts thereof with pharmaceutically acceptable acids or bases, a process for the preparation thereof and a pharmaceutical composition containing said compound or a salt thereof are described.The compound of formula I and the salts thereof are useful in the treatment of Parkinson's disease, renal failure, heart failure and hypertension.
    Type: Grant
    Filed: April 20, 1990
    Date of Patent: December 17, 1991
    Assignee: Simes Societa Italiana Medicinali e Sintetici S.p.A.
    Inventors: Cesare Casagrande, Francesco Santangelo
  • Patent number: 5061806
    Abstract: New phosphonic acid derivatives are described which display antibacterial activity.
    Type: Grant
    Filed: May 24, 1990
    Date of Patent: October 29, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Yoshiharu Morita, Yasuo Hoshide, Haruyuki Chaki, Junko Takashima, Arthur A. Patchett
  • Patent number: 5051413
    Abstract: 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: Grant
    Filed: December 18, 1989
    Date of Patent: September 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Christof Angst, Derek E. Brundish, John G. Dingwall, Graham E. Fagg, Hans Allgeier, Guido Bold, Rudolf Duthaler, Roland Heckendorn, Antonio Togni
  • Patent number: 5006651
    Abstract: The invention relates compounds of the formula ##STR1## wherein R.sup.1 -R.sup.5 and X have the significance given in the description, and their pharmaceutically acceptable salts. The compounds of formula I inhibit the enzyme collagenase and can be used in the form of medicaments for the control or prevention of degenerative joint diseases such as rheumatoid arthritis and osteoarthritis.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: April 9, 1991
    Assignee: Hoffman-La Roche Inc.
    Inventors: Michael J. Broadhurst, Balraj K. Handa, William H. Johnson, Geoffrey Lawton, Peter J. Machin
  • Patent number: 5004826
    Abstract: 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: Grant
    Filed: December 1, 1989
    Date of Patent: April 2, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
  • Patent number: 5001250
    Abstract: Crude N,N-dialkylcarbamoylmethylphosphonates and phosphine oxide extractants, and particularly crude dihexyl N,N-diethylcarbamoylmethylphosphonate and octylphenyl N,N-diisobutylcarbamoyl phosphine oxide, are purified by distilling the crude materials in a thin film evaporator. Preferably, the crude dihexyl N,N-diethylcarbamoylmethylphosphonate is reacted with concentrated hydrochloric acid and subsequently reacted with aqueous sodium hydroxide prior to distillation in the thin film evaporator to hydrolyze impurities contained in the crude product. The purified extractants are useful for extracting actinides and lanthanides from liquid waste streams.
    Type: Grant
    Filed: May 30, 1989
    Date of Patent: March 19, 1991
    Assignee: Occidental Chemical Corporation
    Inventor: Mohan S. Saran
  • Patent number: 4985591
    Abstract: Preparation of a semi-crystalline catalyst for curing coating compositions wherein an isocyanate-sulfonate or -phosphonate is made by a Michael addition followed by chain extension with an isocyanate.
    Type: Grant
    Filed: August 15, 1988
    Date of Patent: January 15, 1991
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Jozef T. Huybrechts, Werner Zimmt
  • Patent number: 4983750
    Abstract: Phosphobetaines of the general formula ##STR1## are disclosed in which R.sup.1 is an alkyl group with 1 to 20 carbon atoms, optionally substituted with OH groups, or the ##STR2## group, in which R.sup.6 is a divalent alkylene group with 1 to 10 carbon atoms, optionally substituted with OH group,R.sup.2 is a divalent hydrocarbon group with 2 to 10 carbon atoms, the chain of which may be interrupted by one or more nitrogen atoms,R.sup.1, R.sup.5 are the same or different and represent alkyl or benzyl groups andR.sup.4 is an alkyl group with 1 to 4 carbon atoms.Also disclosed is the synthesis of these compounds and their use as surface active substances, preferably for the treatment of polar surfaces in the industrial area.
    Type: Grant
    Filed: June 26, 1989
    Date of Patent: January 8, 1991
    Assignee: Th. Goldschmidt AG
    Inventors: Joachim Giersberg, Hans-Joachim Kollmeier
  • Patent number: 4963539
    Abstract: Compounds of the formula ##STR1## wherein Y is O or NH and X is ##STR2## will inhibit the action of neutral endopeptidase. As a result, such compounds produce diuresis, natriuresis, and lower blood pressure as well as being useful in the treatment of congestive heart failure, relieving pain, and diarrhea when administered to a mammalian host.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: October 16, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Norma G. Delaney
  • Patent number: 4960920
    Abstract: .alpha.-Aminoalkylphosphonic and .alpha.-aminoalkylphosphinic acids of the formula I ##STR1## where n=1 or 0,R.sub.1 =H, CH.sub.3 or CH.sub.2 --C.sub.6 H.sub.5R.sub.2 =H (for n=1) and also=alkyl or phenyl (for n=0)are prepared by Hofmann deradation from compounds of the formula II ##STR2## wherein n and R.sub.1 have the same meaning as in formula I,R.sub.3 =alkyl (for n=1), alkyl or phenyl (for n=0), andM.sup.p+ =p-valent cation,with subsequent working up in the known manner.Some of the compounds I are biologically active, and some are intermediates for the preparation of biologically active compounds.
    Type: Grant
    Filed: May 2, 1989
    Date of Patent: October 2, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventor: Gunter Bartels
  • Patent number: 4948918
    Abstract: A process for the production of .alpha.-aminoalkylphosphonic acids or salts thereof of the formula A ##STR1## wherein R.sup.1 represents hydrogen, alkyl having from 1 to 4 carbon atoms or CH.sub.2 --C.sub.6 H.sub.5 and X hydrogen or a metal cation, which comprises reacting a compound of the formula B ##STR2## in which R.sup.1 has the same meaning as in formula A and Mp.sym. represents hydrogen or a p-valent metal cation, with a hypohalite of a p-valent metal cation, and isolating the metal salt produced or acidifying the reaction mixture obtained to produce the .alpha.-aminoalkyl-phosphonic acid.
    Type: Grant
    Filed: June 29, 1989
    Date of Patent: August 14, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Hans-Jerg Kleiner, Gunter Bartels
  • Patent number: 4939127
    Abstract: Antihypertensive phosphate derivatives having the following formula are described: ##STR1## wherein W is selected from the group consisting of methyl and phenyl optionally substituted with C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy and phenyl; r, n, m and a are integers such that the expression r+(n+1)m+a is also an integer and has a value of 3 to 20; r is greater than or equal to 2; n is greater than or equal to 2; m is greater than or equal to zero and a is greater than or equal to zero; 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 --(CH.sub.2).sub.p -- and --(CHR).sub.p --, wherein p is an integer 2-12 and the moiety --(CHR.sub.p -- represents an alkylene chain which is substituted by one or more C.sub.1 -C.sub.
    Type: Grant
    Filed: September 15, 1987
    Date of Patent: July 3, 1990
    Assignee: American Cyanamid Company
    Inventor: Allan Wissner
  • Patent number: 4919830
    Abstract: Dihydrocarbyl dithiocarbamate-derived organic phosphates have been found to be effective antioxidant/antiwear multifunctional additives for various lubricant media.
    Type: Grant
    Filed: December 30, 1988
    Date of Patent: April 24, 1990
    Assignee: Mobil Oil Corporation
    Inventors: Liehpao O. Farng, Andrew G. Horodysky
  • Patent number: 4897166
    Abstract: Acidic liquids, such as galvanic electrolyte solutions for metal electroplating, contain a surfactant and a foam inhibiting agent which is a perfluoroalkyl-containing ester of phosphoric acid.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: January 30, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Detlef Melzer, Erhardt Tabel, Hans-Peter Biermann
  • Patent number: 4897382
    Abstract: 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: Grant
    Filed: June 21, 1988
    Date of Patent: January 30, 1990
    Assignee: Fidia S.p.A.
    Inventors: Francesco della Valle, Aurelio Romeo
  • Patent number: 4894082
    Abstract: Herbicidal compounds of the formula: ##STR1## in which R.sup.1 denotes an optionally substituted hydrocarbon radical, R denotes the hydrogen atom or has one of the meanings given for R.sup.1, R.sup.2 and R.sup.3 denote the hydrogen atom or are such that OR.sup.2 and OR.sup.3 are hydrolyzable groups; R.sup.4 denotes a hydrogen atom or a hydrogenolyzable group, and the agriculturally acceptable salts of these compounds.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: January 16, 1990
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Guy Borrod, Guy Lacroix
  • Patent number: 4888328
    Abstract: 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: Grant
    Filed: March 10, 1988
    Date of Patent: December 19, 1989
    Assignee: Hoeschst-Roussel Incorporated
    Inventors: Nicholas J. Hrib, Kirk D. Shoger, John J. Tegeler
  • Patent number: 4853476
    Abstract: Novel phosphorous containing compounds and compositions containing said compounds inhibit the actions of enkephalinases in mammals. Methods for preparing said compounds and compositions and methods for their use to elicit analgesia and treat mental disorders are described.Useful intermediates for preparing the compounds are also described.
    Type: Grant
    Filed: September 24, 1987
    Date of Patent: August 1, 1989
    Assignee: Schering Corporation
    Inventors: Konstaninos S. Petrakis, Joel G. Berger, Elijah H. Gold
  • Patent number: 4838923
    Abstract: An organo-phosphorus compound represented by the following formula (I) ##STR1## wherein X and Y are identical or different and each represents a hydrogen atom, a halogen atom, CF.sub.3 or an alkyl group having not more than 5 carbon atoms; Z represents CH or N; R.sup.1, R.sup.2 l and R.sup.3 l are identical or different and each represents a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms; and n is zero or 1. The compound is useful, as a herbicide, for eradicating weeds, especially narrow-leaved weeds.
    Type: Grant
    Filed: March 17, 1987
    Date of Patent: June 13, 1989
    Assignee: Teijin Limited
    Inventors: Shizuo Azuma, Toshiyuki Hiramatsu, Koji Nakagawa, Yataro Ichikawa
  • Patent number: 4820632
    Abstract: 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: Grant
    Filed: September 10, 1985
    Date of Patent: April 11, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Gunter Frey, Gerd Zimmermann
  • Patent number: 4795578
    Abstract: 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: Grant
    Filed: December 21, 1987
    Date of Patent: January 3, 1989
    Assignee: Berol Kemi AB
    Inventors: Martin Hellsten, Marie Ernstsson, Bo Idstrom
  • Patent number: 4794197
    Abstract: All-cis-1,3,5-Triamino-2,4,6-trihydroxycyclohexane derivatives corresponding to the general formula I ##STR1## wherein the symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are identical or different and represent hydrogen atoms, alkyl groups or --CO-alkyl groups wherein the alkyl in the alkyl or --CO-alkyl group has 1 to 18 carbon atoms and the alkyl and --CO-alkyl groups may contain, independently of one another, one or more identical or different functional groups, and at least one of the groups R.sub.1 to R.sub.6 is one of the above mentioned unsubstituted or substituted alkyl groups or --CO-alkyl groups, and their salts with pharmacologically conventionally used inorganic or organic acids and their quaternary ammonium salts, processes for their preparation and their use, and pharmaceutical preparations containing these compounds.
    Type: Grant
    Filed: January 31, 1986
    Date of Patent: December 27, 1988
    Inventors: Walter Schneider, Isidor Erni, Hans K. Hegetschweiler