Patents Examined by Michael B. Hydorn
  • Patent number: 5278308
    Abstract: Compounds of the formula ##STR1## where R.sub.1 and R.sub.2 are independently selected from the group consisting of H, OH, OCH.sub.3, and Halogen or R.sub.1 and R.sub.2 can be taken together to form --O--CH.sub.2 --O--;R.sub.3 and R.sub.4 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, and ##STR2## n is an integer from 0 to 5; X and Y are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen and --R.sub.7 --CH.dbd.CHI;R.sub.5 and R.sub.6 are independently selected from the group consisting of H, OH, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 alkoxy, C.sub.1 -C.sub.10 alkenyloxy, --R.sub.7 --CH.dbd.CHI, --CONR.sub.8 R.sub.9 and ##STR3## X' and Y' are independently selected from the group consisting of H, OH, OCH.sub.3, Halogen, and --R.sub.7 --CH.dbd.CHI;R.sub.7 is selected from the group consisting of a chemical bond and C.sub.1 -C.sub.10 alkyl; andR.sub.8 and R.sub.
    Type: Grant
    Filed: February 28, 1992
    Date of Patent: January 11, 1994
    Assignee: The Trustees of The University of Pennsylvania
    Inventor: Hank F. Kung
  • Patent number: 5278312
    Abstract: Derivatives of benzeneborinic acid corresponding to the formula (1) ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 represent, each independently of the others, either a (C.sub.1 -C.sub.2)alkyl group or an aryl group, the group --CR.sub.1 R.sub.2 R.sub.3 being in position 1 or 2 of the tetrazole ring, preparation thereof, and method of use as synthetic intermediates.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: January 11, 1994
    Assignee: Synthelabo
    Inventors: Isaac Chekroun, Jose Ruiz-Montes, Manuel Bedoya-Zurita, Guy Rossey
  • Patent number: 5278310
    Abstract: Free radical deactivating 4- or 1,4-substituted, 2,2,6,6-tetramethyl piperidines are condensed with UV absorbing cinnamic acids or benzoic acids or benzoazols or benzophenones to produce skin anti-aging compounds and compositions which have both free radical deactivation and UV absorbing properties.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: January 11, 1994
    Assignee: Sigma Prodotti Chimici S.p.A.
    Inventor: Giuseppe Raspanti
  • Patent number: 5276037
    Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --whereinX.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: January 4, 1994
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Robert I. Dowell, Philip N. Edwards, Keith Oldham
  • Patent number: 5276120
    Abstract: A process for the preparation of a 1,5-dideoxyazafuranose or 1,6-dideoxy-azapyranose is disclosed. In such a process, an azido-substituted .alpha.-ketose phosphate having a five- or a six-carbon chain is hydrogenated in the presence of a palladium catalyst. The carbon atom bearing the azido substituent and the carbon atom of the keto group of the .alpha.-ketose phosphate starting material are separated by two or three carbon atoms.
    Type: Grant
    Filed: February 13, 1992
    Date of Patent: January 4, 1994
    Assignee: The Scripps Research Institute
    Inventors: Chi-Huey Wong, Tetsuya Kajimoto, Kun-Chin Liu, Lihren Chen
  • Patent number: 5276169
    Abstract: Novel antimycotic carbonyl- and amino-substituted tetrahydrofurans of the formula ##STR1## in which one of A and B is an oxygen atom and the other -CHR.sup.5,D is O, S or NH, andR.sup.1, R.sup.2, R.sup.3 R.sup.4 and R.sup.5 each independently is hydrogen or an organic radical.
    Type: Grant
    Filed: October 13, 1992
    Date of Patent: January 4, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Franz Kunisch, Joachim Mittendorf, Manfred Plempel
  • Patent number: 5274157
    Abstract: Compounds of the formula Ib ##STR1## in which R.sub.1 and R.sub.2 independently of one another are linear or branched C.sub.1 -C.sub.12 alkyl, cycloalkyl having 5 to 8 ring carbon atoms, phenylalkyl having 1 to 4 C atoms in the alkylene group, the cyclic radicals being unsubstituted or substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 and R.sub.2 independently of one another are --SiR.sub.4 R.sub.5 R.sub.6 in which R.sub.4, R.sub.5 and R.sub.6 independently of one another are C.sub.1 -C.sub.12 alkyl, phenyl, benzyl, or phenyl or benzyl, each of which is substituted by C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkoxy, and R.sub.3 is a bridging member which, together with the radical --OCH--CH.sub.2 --CHO-- to which it is bonded, forms a 6- to 8-membered ring. These compounds are valuable intermediates for the preparation of carbacyclic nucleosides of the natural and unnatural series and of the racemates.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: December 28, 1993
    Assignee: Ciba-Geigy Corporation
    Inventor: Heinz Moser
  • Patent number: 5272128
    Abstract: This invention pertains to phosphosulfonates, having the general formula ##STR1## wherein Y is phenyl, naphthyl, benzyl, a (C.sub.5 -C.sub.8)cycloalkyl, a 5-membered heteroaromatic ring, a 6-membered heteraromatic ring, a fused 5,6-membered heteroaromatic ring, or a fused 6,6-membered heteroaromatic ring; andX is oxygen or sulfur; andR.sup.1 and R.sup.2 are each independently selected from substituted or unsubstituted alkyl, alkoxy, alkylthio, alkenyloxy, alkynyloxy, haloalkoxy, cyanoalkoxy, alkoxyalkoxy, cycloalkyloxy, cycloalkylalkoxy, alkylideneiminooxy, chloro, amino, phenyl or phenoxy; or R.sup.1 and R.sup.2 are both alkoxy, taken together with the phosphorus atom to form a 6-membered oxygen-containing ring; compositions containing these compounds and their use as herbicides.
    Type: Grant
    Filed: April 1, 1992
    Date of Patent: December 21, 1993
    Assignee: Rohm and Haas Company
    Inventors: Robert E. Rosen, Damian G. Weaver, Jane W. Cornille, Lori A. Spangler
  • Patent number: 5272173
    Abstract: The invention concerns an aryl derivative of the formula I, ##STR1## wherein Ar.sup.1 is optionally substituted phenyl, naphthyl or a heterocyclic moiety, and X.sup.1 is oxy, thio, sulphinyl, sulphonyl, difluoromethylene, imino, (1-4C)alkylimino or optionally substituted (1-4C)alkylene, or X.sup.1 is a group of the formula--X.sup.4 --CR.sub.2 -- or --CR.sub.2 --X.sup.4 --wherein X.sup.4 is oxy, thio, sulphinyl, sulphonyl or carbonyl and each R is hydrogen, methyl or ethyl;each of Ar.sup.2 and Ar.sup.3 is optionally substituted phenylene;X.sup.2 is oxy, thio, sulphinyl or sulphonyl;R.sup.1 is (1-4C)alkyl; andR.sup.2 and R.sup.3 together form a group of the formula --A.sup.1 --X.sup.3 --A.sup.2 -- which together with the carbon atom to which A.sup.1 and A.sup.2 are attached define a ring having 5 to 7 ring atoms, wherein each of A.sup.1 and A.sup.2 is (1-3C)alkylene and X.sup.
    Type: Grant
    Filed: April 14, 1993
    Date of Patent: December 21, 1993
    Assignees: Imperial Chemical Industries PLC, Ici Pharma
    Inventors: Robert I. Dowell, Philip N. Edwards, Keith Oldham
  • Patent number: 5266700
    Abstract: Process employing bipyridyls as inks, of the general formula ##STR1## in which R, R' are, for example, alkyl and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are, for example hydrogen or alkyl radicals, or R.sup.1 and R.sup.2 or R.sup.2 and R.sup.3, and/or R.sup.4 and R.sup.5 or R.sup.5 and R.sup.6 together with the pyridine ring form in isoquinoline or quinoline ring system.
    Type: Grant
    Filed: December 31, 1991
    Date of Patent: November 30, 1993
    Assignee: Riedel-De-Haen
    Inventors: Heinz Langhals, Christoph Naumann
  • Patent number: 5262564
    Abstract: The subject invention provides for novel anti-tumor and anti-retroviral compounds. More specifically, the invention relates to the sulfinic acid adducts of therapeutic C-nitroso compounds. The formation of the adducts increases the stability and more solubility of the C-nitroso compounds. These compounds include the L-cysteinesulfinic acid adducts of 6-nitroso-1,2-benzopyrone and 3-nitrosobenzamide. The invention also provides for compositions containing one or more of the compounds, and for methods of treating retroviral infections, cancer, infectious virus concentration with the subject compounds and compositions.
    Type: Grant
    Filed: October 30, 1992
    Date of Patent: November 16, 1993
    Assignee: Octamer, Inc.
    Inventors: Ernest Kun, Jerome Mendeleyev
  • Patent number: 5262571
    Abstract: A process of synthesizing enantiomerically pure compounds defined by Formula V, ##STR1## which are useful as chiral auxiliaries is disclosed. The process comprises, first, combining a base of Formula Y.sup.- Z.sup.+ (Formula I), wherein Y.sup.- is an organic anion and Z.sup.+ is an inorganic cation, with a compound of Formula II, ##STR2## wherein R.sub.1 is a C.sub.1 -C.sub.4 alkyl group and R.sub.2 is the same as R.sub.1, or wherein R.sub.1 and R.sub.2 together form cyclopentane or cyclohexane, and wherein R.sub.3 is a substituted or unsubstituted aryl group, to form a compound defined by Formula III, ##STR3## then: (b) reacting the compound of Formula III with a cyclic epoxide defined by Formula IV, ##STR4## wherein n is 1, 2, or 3, to form a racemic mixture of a compound defined by Formula V.
    Type: Grant
    Filed: March 20, 1992
    Date of Patent: November 16, 1993
    Assignee: North Carolina State University
    Inventors: Daniel L. Comins, James M. Salvador
  • Patent number: 5260485
    Abstract: Alkylphosphines are made by a reaction of gaseous phosphine and the corresponding gaseous olefin in contact with at least one non-oxidizing acid catalyst. Products produced thereby are alkylphosphines which contain substantially no metallic or oxygenating impurities. The process is a continuous process and employs a mineral acid catalyst either in solid form or as a liquid supported on a solid, inert material.
    Type: Grant
    Filed: March 9, 1992
    Date of Patent: November 9, 1993
    Assignee: American Cyanamid Company
    Inventors: C. Joseph Calbick, Mark A. Kuck, Donald H. Valentine
  • Patent number: 5256800
    Abstract: There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Furthermore, a method for preparing an optically active compound comprises reacting a racemic 1,3-dioxin-4-one with vinylacetate in the presence of lipase to resolve the racemic compound into optically active compound represented by the formula (3) ##STR1## and an optically active compound represented by the formula (4) ##STR2## which is an antipode of the compound represented by the formula (3).
    Type: Grant
    Filed: February 18, 1992
    Date of Patent: October 26, 1993
    Assignee: Chisso Corporation
    Inventors: Chikara Kaneko, Masayuki Sato
  • Patent number: 5256801
    Abstract: A process for the preparation of a compound of formula (I) ##STR1## comprising contacting a mixture containing at least one taxane compound having an ester linkage at the C-13 position with at least one borohydride reducing salt in a reaction solvent in the presence of a Lewis acid.
    Type: Grant
    Filed: December 4, 1992
    Date of Patent: October 26, 1993
    Assignee: NaPro BioTherapeutics, Inc.
    Inventors: David R. Carver, Timothy R. Prout, Hernita A. Ewald, Donia L. Henderson
  • Patent number: 5252749
    Abstract: The compounds of the invention having the formula: ##STR1## in which: A, which is a ring condensed with cyclopentane, represents a substituted or unsubstituted thiophene ring, Q represents an alkylene chain, R.sub.1 and R.sub.2 each represent H or an alkyl, or they form, with the nitrogen atom to which they are linked, a saturated nitrogenous heterocyclic ring containing 5 to 7 atoms, R.sub.3 and R.sub.4 each represent H, alkyl, cycloalkyl, trifluoromethyl or an optionally substituted phenyl, thienyl or furyl group or R.sub.3 and R.sub.4 together form a (C.sub.5 -C.sub.8) cycloalkyl, as well as their addition salts with an acid and their quaternary ammonium derivatives.They can be used as medicines.
    Type: Grant
    Filed: September 23, 1992
    Date of Patent: October 12, 1993
    Assignee: Elf Sanofi
    Inventors: Alain Badorc, Jean Courregelongue, Daniel Ducros, Daniel Frehel, Antonina Giudice, Claudine Serradeil-Legal
  • Patent number: 5248781
    Abstract: Substituted anilino-nicotinic acid derivatives are readily prepared from the condensation of two intermediates, 2-alkyl-3-perfluoroalkyl-anilines and alkyl 2-chloronicotinates. The 2-alkyl-3-perfluoroalkyl-aniline intermediate can be prepared via a novel three step synthesis. 3-Perfluoroalkyl-anilines are reacted with an amine directing protecting group reagent to protect the amine. The protected amine is then alkylated, and finally, the directing group is removed to form the 2-alkyl-3-perfluoroalkyl-aniline intermediate. The 2-alkyl-3-perfluoroalkyl-aniline intermediate is condensed with the alkyl 2-chloronicotinate to form the anilino-nicotinic acid derivative.
    Type: Grant
    Filed: September 21, 1992
    Date of Patent: September 28, 1993
    Assignee: The Trustees of Princeton University
    Inventor: Alexander McKillop
  • Patent number: 5248812
    Abstract: When 2-naphthylamine-1,5-disulphonic acid is precipitated from the as-sulphonated reaction mixtures by dilution, a purer product is obtained, with a low level of adherent sulphuric acid, if the precipitation by dilution of the reaction mixture is carried out under precisely defined conditions.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: September 28, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Horst Behre, Heinz-Ulrich Blank, Holger Heidenreich, Fritz Pohl, Paul Uhrhan
  • Patent number: 5248825
    Abstract: This invention relates to 1-phenyl-3-phenyl-2-propyne-1-ones, the use of these compounds as calcium uptake inhibitors in leukocytes and thrombocytes, and pharmaceutical compositions containing these compounds as active ingredients, and the process of their preparation.
    Type: Grant
    Filed: June 1, 1992
    Date of Patent: September 28, 1993
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Robert J. Dinerstein, Jeffrey S. Sabol, Keith A. Diekema
  • Patent number: 5245035
    Abstract: The invention concerns novel boron compounds of the formula IV, in which Q, Y.sup.1, G.sup.1 and G.sup.2 have the various meanings defined herein, and their acid and base addition salts. The said compounds are useful in the manufacture of certain quinoline, pyridine and imidazole derivatives which have angiotensin II inhibitory activity. The invention also provides novel processes for the production of the quinoline, pyridine and imidazole derivatives.
    Type: Grant
    Filed: January 17, 1992
    Date of Patent: September 14, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Andrew P. Thomas, David M. G. Martin, Stanley A. Lee, Lyn Powell