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: 5476859
    Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives 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.-trifluoroalkanoyl 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 groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
    Type: Grant
    Filed: January 20, 1995
    Date of Patent: December 19, 1995
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5451604
    Abstract: A class of halogenated phenylacetonitrile alkylaminoalkylphenyl compounds having immunosuppressive properties is described. Compounds of this class would be useful in reducing recipient rejection of transplanted organs and for treatment of autoimmune or inflammatory diseases. Compounds of particular interest are of the formula ##STR1## wherein m is a number selected from three to five, inclusive; wherein n one or two; wherein R.sup.1 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, tert-butyl, iso-butyl, n-pentyl, isopentyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cyclopropylmethyl, cyclobutylmethyl, cyclopentylmethyl, cyclohexylmethyl, benzyl and phenethyl; wherein each of R.sup.3 through R.sup.
    Type: Grant
    Filed: July 26, 1993
    Date of Patent: September 19, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Thomas E. Barta, John P. McKearn, Susan A. Gregory, Richard A. Partis, Francis J. Koszyk
  • Patent number: 5411970
    Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives 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.-trifluoroalkanoyl 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 groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
    Type: Grant
    Filed: December 21, 1993
    Date of Patent: May 2, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5393764
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5342838
    Abstract: The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene; or ##STR3## wherein Y is CH, N, O, or S; R.sup.6 is hydrogen, alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or a heterocyclic amine; and R.sup.7 is hydrogen or alkyl. The compounds inhibit 5-lipoxygenase and are useful in the treatment of inflammation and allergic conditions.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: August 30, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5334616
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula(I) and the radicals are defined in the claims: ##STR1## The compounds of the present invention are useful in the treatment of local and systemic inflammation and allergy reactions.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: August 2, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5326907
    Abstract: The present invention relates to compounds of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, halogen, or phenyl; Alk.sup.1 represents straight or branched chain alkylene of 2 to 10 carbon atoms which can optionally be substituted by hydroxy, provided that said hydroxy is not attached to a carbon which is adjacent to sulfur or oxygen, X represents sulfur or oxygen, and Alk.sup.2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts thereof. These compounds are specific 5-lipoxygenase inhibitors and are useful as anti-inflammatory and anti-allergy agents and in the treatment of conditions mediated by 5-lipoxygenase.
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: July 5, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller
  • Patent number: 5310745
    Abstract: A method of inhibiting lentivirus is disclosed which comprises mammalian host susceptible to said lentivirus with a virally inhibitory effective amount of an O-acylated derivative of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aroyl derivatives 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.-trifluoroalkanoyl 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 groups contain from 7 to 14 carbon atoms, the N-acyl groups contain from 4 to 8 carbon atoms and the N-alkyl groups contain from 1 to 14 carbon atoms.
    Type: Grant
    Filed: August 13, 1992
    Date of Patent: May 10, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5298514
    Abstract: The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene.
    Type: Grant
    Filed: September 10, 1992
    Date of Patent: March 29, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5280047
    Abstract: The present invention relates to methods of using and pharmaceutical compositions containing compounds of Formula I: ##STR1## wherein R.sup.1 is hydrogen, --COR.sup.4 wherein R.sup.4 is C.sub.1 -C.sub.4 alkyl, or --COOR.sup.5 wherein R.sup.5 is C.sub.1 -C.sub.4 alkyl; R.sup.2 is C.sub.1 -C.sub.4 alkyl, phenyl, or --OR.sup.6 wherein R.sup.6 is C.sub.1 -C.sub.4 alkyl; and R.sup.3 is C.sub.6 -C.sub.8 alkyl, halogen, or NO.sub.2 ; with the proviso that when R.sup.1 is hydrogen, R.sup.2 is C.sub.1 -C.sub.4 alkyl; and a pharmaceutically acceptable carrier. Compounds of Formula I and pharmaceutical compositions containing them are inhibitors of 5-lipoxygenase and are useful in the treatment of conditions mediated by leukotrienes such as inflammation, allergy, hypersensitivity reactions, and proliferative skin diseases such as psoriasis.
    Type: Grant
    Filed: April 2, 1993
    Date of Patent: January 18, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5272178
    Abstract: The present invention relates to compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, phenyl, or hydrogen; R.sup.3 represents hydrogen or alkyl; X represents O, S or (CH.sub.2).sub.m wherein m is 1 or 2; A represents O or S(O).sub.n wherein n is 0, 1, or 2; p is an integer from 0 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl; or NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl, and R.sup.6 is hydrogen, alkyl, heterocyclealkyl, substituted heterocyclealkyl, cycloalkyl, substituted cycloalkyl, phenyl, substituted phenyl, phenylalkyl, or substituted phenylalkyl, or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl; and the pharmaceutically acceptable salts thereof. The compounds are inhibitors or stimulators of superoxide generation.
    Type: Grant
    Filed: April 8, 1993
    Date of Patent: December 21, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5250567
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.
    Type: Grant
    Filed: June 24, 1992
    Date of Patent: October 5, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5244899
    Abstract: The compounds of this invention are 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 azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: July 29, 1992
    Date of Patent: September 14, 1993
    Assignee: G. D. Searle and Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5225444
    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: August 27, 1991
    Date of Patent: July 6, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5221746
    Abstract: 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: July 27, 1992
    Date of Patent: June 22, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
  • Patent number: 5198435
    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 than 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: March 14, 1991
    Date of Patent: March 30, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5189038
    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: July 2, 1991
    Date of Patent: February 23, 1993
    Assignee: G. D. Searle and Co.
    Inventors: Richard A. Mueller, Akira Nakao, Richard A. Partis
  • Patent number: 5157053
    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, aszabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino, The compounds are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: October 20, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis, James R. Deason
  • Patent number: 5147893
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula (I): ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; or (CH.sub.2).sub.t COOR.sup.7 wherein t is an integer from 1 to 4 and R.sup.7 is hydrogen or alkyl of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts and stereoisomers or geometric isomers thereof.
    Type: Grant
    Filed: May 9, 1991
    Date of Patent: September 15, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5145992
    Abstract: A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 can be hydrogen, alkyl, alkoxy, halo, phenyl, substituted phenyl, or hydroxy; A can be S, O or --CH.sub.2 --; and Alk is straight or branched chain alkylene, with a base in an aprotic solvent, then reacting the resulting alkoxide with a monohaloacetic acid ester to give an alkoxyacetate followed by reaction of the alkoxyacetate with a hydrogen halide, organic acid or Lewis acid in nitromethane to give the corresponding .alpha.-alkoxyacetic acid which then may be recovered or may optionally be converted to the corresponding salt by contracting the .alpha.-alkoxyacetic acid with a base.
    Type: Grant
    Filed: May 6, 1991
    Date of Patent: September 8, 1992
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis