Patents by Inventor Richard H. Mueller

Richard H. Mueller has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5237095
    Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: August 17, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
  • Patent number: 5237096
    Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: August 17, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
  • Patent number: 5233086
    Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylene-cyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: August 3, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
  • Patent number: 5218142
    Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta.,3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobut yl]-1,9-dihydro-6H-purin-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
    Type: Grant
    Filed: October 16, 1992
    Date of Patent: June 8, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
  • Patent number: 5210262
    Abstract: A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal=Cl,Br,I) with an alkoxide of the structure ##STR2## wherein M is an alkali metal and R.sup.2c is lower alkyl. The resulting phosphonic acid ester is an intermediate in preparing a squalene synthetase inhibitor which is used for inhibiting cholesterol biosynthesis.
    Type: Grant
    Filed: September 14, 1992
    Date of Patent: May 11, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Richard H. Mueller
  • Patent number: 5194604
    Abstract: Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: March 16, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Christopher M. Cimarusti, Janak Singh, Richard H. Mueller
  • Patent number: 5185463
    Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-pur in-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
    Type: Grant
    Filed: October 2, 1991
    Date of Patent: February 9, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
  • Patent number: 5177239
    Abstract: A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal.dbd.Cl,Br,I) with an alkoxide of the structure ##STR2## wherein M is an alkali metal and R.sup.2c is lower alkyl. The resulting phosphonic acid ester is an intermediate in preparing a squalene synthetase inhibitor which is used for inhibiting cholesterol biosynthesis.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: January 5, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Richard H. Mueller
  • Patent number: 5106977
    Abstract: Novel intermediates for preparing 2-oxo-1-[[(substituted sulfonyl)-amino]carbonyl]azetidines are disclosed. These intermediates have the formula ##STR1## wherein Prot is as defined herein.
    Type: Grant
    Filed: September 27, 1990
    Date of Patent: April 21, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller
  • Patent number: 5039795
    Abstract: An improved process for preparation of compounds of the formula ##STR1## as disclosed. These compounds are useful as intermediates in the preparation of boronic acid adducts of technetium 99m dioxime complexes of the formula.sup.99m Tc X(Y).sub.3 Zwhich are useful as imaging agents.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: August 13, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Richard H. Mueller
  • Patent number: 4980465
    Abstract: An improved process for making compounds having the formula ##STR1## includes subjecting an intermediate of the formula ##STR2## to hydrogenolysis in the presence of a ketonic solvent so as to simultaneously remove both Z-protecting groups from compound II while selectively reprotecting the --A.sub.1 --NH.sub.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: December 25, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Robert Zahler
  • Patent number: 4973747
    Abstract: A process has now been discovered by which an intermediate in preparation of antibiotics ##STR1## may be directly derived from the substrate ##STR2## by treatment with aqueous solutions of MHCO.sub.3 and MOH, wherein: R.sup.1, R.sup.2 and R.sup.3 are each independently alkyl, alkenyl, alkynyl, substituted alkyl, substituted alkenyl, substituted alkynyl, aryl, or substituted aryl;M is alkali metal (such as Na, Li, or K); andX is halogen.
    Type: Grant
    Filed: August 15, 1989
    Date of Patent: November 27, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Richard H. Mueller
  • Patent number: 4937355
    Abstract: A process is provided for preparing (trans)-4-phenyl-DL-proline derivatives, which are useful in preparing certain angiotensin converting enzyme inhibitors, which process involves reacting an ester of the structure ##STR1## wherein X is a leaving group such as tosylate, R.sup.3 is lower alkyl, R is cyclohexyl, phenyl or substituted phenyl, and R.sup.1a is a protecting group, with a potassium amide base such as potassium hexamethyldisilazide under reduced temperatures to form the trans-4-substituted proline ester derivative of the structure ##STR2## then hydrolyzing the proline ester to the acid of the structure ##STR3## and removing the R.sup.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: June 26, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Kloss, David Kronenthal, Christopher M. Cimarusti, Richard H. Mueller
  • Patent number: 4912231
    Abstract: A process is provided for preparing (trans)-4-phenyl-L-proline derivatives with excellent stereospecificity, which are useful in preparing certain ACE inhibitors, which process involves reacting a proline derivative of the structure ##STR1## whereing R is a nitrogen protecting group, R.sub.1 is H, aryl, arylalkyl or lower alkyl, and X is a leaving group such as fluorine, an alkyl sulfonate, arylsulfonate or cycloalkyl sulfonate is reacted with an aromatic nucleophile, such as benzene, in the presence of a Lewis acid such as AlCl.sub.
    Type: Grant
    Filed: June 17, 1988
    Date of Patent: March 27, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David Kronenthal, Paula L. Kuester, Richard H. Mueller
  • Patent number: 4889930
    Abstract: An improved process for making compounds having the formula ##STR1## includes subjecting an intermediate of the formula ##STR2## to hydrogenolysis in the presence of a ketonic solvent so as to simultaneously remove both Z-protecting groups from compound II while selectively reprotecting the --A.sub.1 --NH.sub.2 end of that molecule.
    Type: Grant
    Filed: December 21, 1987
    Date of Patent: December 26, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Richard H. Mueller, Robert Zahler
  • Patent number: 4633017
    Abstract: Processes for preparing the useful intermediates having the formula ##STR1## are disclosed herein, utilizing novel chemical compounds having the formula ##STR2##
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: December 30, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard H. Mueller, Jakob-Matthias Drossard, Peter H. Ermann
  • Patent number: 4581170
    Abstract: Processes for preparing the useful intermediates having the formula ##STR1## are disclosed herein, utilizing novel chemical compounds having the formula ##STR2##
    Type: Grant
    Filed: August 3, 1984
    Date of Patent: April 8, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard H. Mueller, Jakob-Matthias Drossard, Peter H. Ermann
  • Patent number: 4421686
    Abstract: Compounds having the formula ##STR1## can be prepared by reacting a compound having the formula ##STR2## with a Grignard reagent having the formulaR.sub.3 -Mg-X.sub.1 ,wherein R.sub.1 is phenylacetyl or phenoxyacetyl;R.sub.2 is a not readily enolyzable alkyl group, aryl or norbornyl;R.sub.3 is alkyl, alken-1-yl, alkyn-1-yl, 2-phenylethenyl, 2-phenylethynyl, aryl or arylalkyl;X.sub.1 is bromine or chlorine.(3R-cis)-3-Acylamino-4-norbornylsulfonyl-2-azetidinones are novel compounds that form an integral part of this invention.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: December 20, 1983
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard H. Mueller, Christopher M. Cimarusti, Thomas P. Kissick