Patents by Inventor Richard A Partis

Richard A Partis 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: 5144037
    Abstract: Antiviral O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol are disclosed that contain an N-alkyl or N-aroyl radical in which from one to four of the free hydroxyl groups are O-acylated with carboxylic alkanoyl radicals selected from the group consisting of .omega.,.omega.,.omega.-trifluoro alkanoyl having from three to eight carbon atoms, carboxylic cycloalkanoyl groups having from four to eight carbon atoms and carboxylic acyclic alkanoyl groups having from two to ten carbon atoms, wherein the N-aroyl radical is selected from the group consisting of p-decylbenzoyl, 3-(p-chlorophenoxy)propanoyl, 2-(acetyloxy)benzoyl, [1,1'-biphenyl]-4-ylcarbonyl, 2-thiopheneacetyl, trans-3-furanacryloyl, 3-methoxyphenylacetyl and 3-(trifluoromethyl)benzoyl, and wherein the N-alkyl contains from one to fourteen carbon atoms, provided that when N-alkyl contains from one to five carbon atoms the O-acylated groups are .omega.,.omega.,.omega.-trifluoro alkanoyl or carboxylic cycloalkanoyl.
    Type: Grant
    Filed: January 10, 1991
    Date of Patent: September 1, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5082854
    Abstract: The present invention is directed to a method of stimulating superoxide generation using phenolic thioethers which stimulate the generation of superoxide.
    Type: Grant
    Filed: September 7, 1990
    Date of Patent: January 21, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Akira Nakao, Richard A. Partis
  • Patent number: 5071876
    Abstract: The compounds of this invention are anilides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is hydrogen or lower alkyl; and R.sub.4 is phenyl or substituted phenyl. The compounds of the present invention are useful in the treatment of inflammation, allergy and hypersensitivity reactions and other disorders of the immune system.
    Type: Grant
    Filed: July 27, 1990
    Date of Patent: December 10, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5066679
    Abstract: The compounds of the present invention comprise substituted phenolic thioalkylamides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: March 9, 1989
    Date of Patent: November 19, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5064860
    Abstract: The present invention relates to a method of inhibiting superoxide generation which comprises administering to a mammal in need of such treatment an amount of a compound of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; Alk.sup.1 represents straight or branched chain alkylene of 1 to 10 carbon atoms, X represents sulfur or oxygen, Alk.sup.2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and m is 0, 1 or 2; or a pharmaceutically acceptable salt or stereoisomer or geometric isomer thereof, which is effective to inhibit superoxide generation.
    Type: Grant
    Filed: September 7, 1990
    Date of Patent: November 12, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Akira Nakao, Richard A. Partis
  • Patent number: 5030638
    Abstract: A method for providing enhanced antiviral activity with N-alkyl derivatives of 1,5-dideoxy-1,5-imino-D-glucitol is disclosed which comprises selectively increasing the alkyl chain length to at least 5 carbon atoms and up to about 10 carbon atoms to thereby improve the spectrum of enzyme inhibitory activity and the in vivo half life.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: July 9, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller
  • Patent number: 5019597
    Abstract: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: July 30, 1987
    Date of Patent: May 28, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5013864
    Abstract: A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R--OH wherein R is alkyl, substituted alkyl, or cycloalkyl, or cycloalkyl alkyl with a base in an aprotic organic solvent to give an alkoxide followed by removal of the organic solvent and reaction of the alkoxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding alkoxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the alkoxy acetate salt with an acid.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: May 7, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Arthur L. Campbell, Richard A. Mueller, John S. Ng, Richard A. Partis
  • Patent number: 5002967
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers, sulfoxides, and disulfides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metablic pathway are involved.
    Type: Grant
    Filed: July 11, 1989
    Date of Patent: March 26, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5003072
    Abstract: O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aryl derivatives in which from one to four of the free hydroxyl groups are acylated with acyl groups having from one to eight carbon atoms and in which the N-alkyl and N-acyl substituents contain from four to fourteen carbon atoms and the N-aryl substituents contain from seven to fourteen carbon atoms are disclosed, provided that when N-aryl is benzyloxycarbonyl, the O-acyl groups contain four to eight carbon atoms.
    Type: Grant
    Filed: October 12, 1989
    Date of Patent: March 26, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 4981853
    Abstract: The compounds of this invention are heterocyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N-R.sub.4, O and CH.sub.2 ; m is 2 or 3; n is 2 or 3 when X is O or N-R.sup.4, and n is 1 to 3 when X is CH.sub.2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: November 14, 1989
    Date of Patent: January 1, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 4973602
    Abstract: Novel N-aryl derivatives of 1,4-dideoxy-1,4-imino-L-arabinitol and their acylated derivatives are disclosed. These compounds have useful antiviral activity.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: November 27, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Francis J. Koszyk, Richard A. Partis, Richard A. Mueller
  • Patent number: 4959364
    Abstract: The compounds of this invention are heterocyclic amides represented by the formula: ##STR1## wherein: R.sub.1 R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; y is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, carboxyl or carboxyloweralkyl; X is selected from the group consisting of N--R.sub.4, O and CH.sub.2 ; m is 2 or 3; n is 2 or 3 when X is O or N--R.sup.4, and n is 1 to 3 when x is CH.sub.2 ; p is 0 to 2; and the pharmaceutically acceptable salts thereof. The compounds are anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: September 25, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 4952724
    Abstract: A process for producing aryloxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R-OH wherein R is aryl or substituted aryl with a base in an aprotic organic solvent to give an aryloxide followed by removal of the organic solvent and reaction of the aryloxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding aryloxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the aryloxyacetate salt with an acid.
    Type: Grant
    Filed: December 8, 1989
    Date of Patent: August 28, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Arthur L. Campbell, Richard A. Mueller, John S. Ng, Richard A, Partis
  • Patent number: 4937357
    Abstract: N-alkyl, N-hydroxylalkyl and N-alkanoyl derivatives of 1,4-dideoxy-1,4-imino-L-arabinitol are disclosed in which the alkyl group has from 4 to about 9 carbon atoms, the hydroxyalkyl group has from 2 to about 5 carbon atoms and the alkanoyl group has from 3 to about 12 carbon atoms. These compounds are useful intermediates for the preparation of acylated derivatives thereof which have antiviral activity.
    Type: Grant
    Filed: September 26, 1989
    Date of Patent: June 26, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Francis J. Koszyk, Richard A. Partis, Richard A. Mueller
  • Patent number: 4876268
    Abstract: Acylated derivatives of 1,4-dideoxy-1,4-imino-L-arabinitol and their N-alkyl and N-hydroxyalkyl derivatives in which all the free hydroxyl groups are acylated with acyl groups having from one to six carbon atoms and in which the N-alkyl substituents in the N-alkyl and N-hydroxyalkyl derivatives contain from one to fourteen carbon atoms are disclosed.
    Type: Grant
    Filed: November 3, 1988
    Date of Patent: October 24, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Francis J. Koszyk, Richard A. Partis, Richard A. Mueller
  • Patent number: 4847305
    Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: July 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 4835190
    Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: June 5, 1987
    Date of Patent: May 30, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 4835189
    Abstract: The compounds of the present invention comprise substituted phenolic thioalkylamides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: June 5, 1987
    Date of Patent: May 30, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 4803294
    Abstract: This invention relates to novel intermediate compounds which are useful for producing the halogenated protease inhibitors that are the subject matter of U.S. Pat. No. 4,469,885. In particular, the invention relates to novel methods and intermediates for making said protease inhibitors, the intermediate compounds being of the formula: ##STR1## wherein R.sub.1 is: (a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) H;wherein R.sub.6 is:(a) straight or branched chain higher alkyl having 13-25 carbon atoms; or(b) straight or branched chain higher alkenyl having 13-25 carbon atoms;wherein R.sub.5 is:(a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) benzyl;wherein R.sub.7 is:(a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) H;wherein R.sub.2 is:(a) --Cl, --Br, or --I; or(b) --CF.sub.3.
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: February 7, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis