Patents Represented by Attorney Paul D. Matukaitis

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  • .alpha.-aminoacyl .beta.-aminoacyl aminodiols as anti-hypertensive agents
    Patent number: 4931429
    Abstract: Compounds characterized generally as .alpha.-aminoacyl .beta.-aminoactyl aminodiols are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: October 1, 1987
    Date of Patent: June 5, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Use of 8-azapurin-6-one derivatives for control of hypertension
    Patent number: 4923874
    Abstract: A class of 8-azapurin-6-one derivatives is described for use in control of hypertension. A compound of particular interest is 8-aza-2-(2-n-propoxyphenyl)purin-6-one.
    Type: Grant
    Filed: July 21, 1988
    Date of Patent: May 8, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Ellen G. McMahon, Robert E. Manning
  • Leukotriene LTD.sub.4 and LTB.sub.4 antagonists
    Patent number: 4923891
    Abstract: This invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:X, Y, and Z are each independently O or S with S optionally oxidized to S=O;Alk is straight or branched chain alkylene or hydroxyalkylene containing 1-6 carbon atoms;R.sub.1 is hydrogen or lower alkyl;n is 0 to 5;R.sub.2 is hydrogen, lower alkyl, cycloalkyl, --(CH.sub.2).sub.n --CO.sub.2 R.sub.1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; andAr is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl.This invention is in the field of pharmaceutical agents which act as leukotriene D.sub.4 (LTD.sub.4) antagonists and includes embodiments which act as leukotriene B.sub.4 (LTD.sub.4) antagonists.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: May 8, 1990
    Assignee: G. D. Searle & Co.
    Inventors: James R. Deason, Michael A. Stealey, Richard M. Weier
  • Phenyl glycines for use in reducing neurotoxic injury
    Patent number: 4918064
    Abstract: A class of phenyl glycine compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phenyl glycine compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.
    Type: Grant
    Filed: October 21, 1987
    Date of Patent: April 17, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Alex A. Cordi, Michael L. Vazquez
  • Structure and properties of modified interferons
    Patent number: 4914033
    Abstract: A composition of matter comprising a polypeptide of the formula:A-R.sub.1 -B-R.sub.2-22 -CwhereinA is the amino acid sequence 1-16 of human beta interferon;R.sub.1 is cysteine, serine or alanine;B is the amino acid sequence 18-31 of human beta interferon;R.sub.2-22 are naturally occurring amino acids;C is the amino acid sequence 53-166 of human beta interferon.
    Type: Grant
    Filed: May 18, 1988
    Date of Patent: April 3, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Leslie D. Bell, Paul G. Boseley, Alan G. Porter
  • D-cycloserine and its prodrugs as cognitive enhancers
    Patent number: 4904681
    Abstract: The compound D-4-amino-3-isoxazolidone, its pharmaceutically-acceptable salts and its prodrug compounds are described as having cognitive-enhancing activity.
    Type: Grant
    Filed: December 1, 1987
    Date of Patent: February 27, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Alex A. Cordi, Gail E. Handelmann, Joseph B. Monahan
  • Aminoalkylaminocarbonyl aminodiol amino acid derivatives as antihypertensive agents
    Patent number: 4902706
    Abstract: Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: February 20, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Poly(aminoalkyl)aminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents
    Patent number: 4900745
    Abstract: Non-peptidyl compounds characterized generally as poly(aminoalkyl)aminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: February 13, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Ethereal N-terminal aminodiol amino acid derivatives as anti-hypertensive agents
    Patent number: 4900746
    Abstract: Non-peptidyl compounds characterized generally as ethereal N-terminal aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: July 1, 1988
    Date of Patent: February 13, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Substituted glutaric acid lactones in the treatment of hyperlipidemia
    Patent number: 4895973
    Abstract: Compounds of formula I ##STR1## are described which are useful to inhibit the formation of serum cholesterol by virtue of their ability to inhibit .beta.-hydroxy-.beta.-methylglutaryl-CoA(HMG CoA), the rate-controlling substance in the synthesis of serum cholesterol.
    Type: Grant
    Filed: December 21, 1988
    Date of Patent: January 23, 1990
    Assignee: G. D. Searle & Company
    Inventors: John S. Baran, Thomas J. Lindberg, Harman S. Lowrie
  • Use of substituted dihydrobenzopyrans for allergy and inflammation
    Patent number: 4888356
    Abstract: The invention relates to compounds of the formula: ##STR1## which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies and inflammatory conditions.
    Type: Grant
    Filed: June 14, 1988
    Date of Patent: December 19, 1989
    Assignee: G. D. Searle and Company
    Inventors: Masateru Miyano, Robert L. Shone, Daniel D. Sohn
  • Biarylalkylimidazole derivatives as anti-depressants
    Patent number: 4882343
    Abstract: Certain 4(5)-(biarylethyl)imidazole derivatives are selectiv3 .alpha..sub.2 -adrenergic receptor blockers and are useful as anti-depressant agents.
    Type: Grant
    Filed: August 28, 1987
    Date of Patent: November 21, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Alex A. Cordi, Hugo J. Gorissen
  • Substituted dipeptide amides #3
    Patent number: 4880829
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: November 14, 1989
    Assignee: G. D. Searle and Company
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton
  • Fused polypeptides and methods for their detection
    Patent number: 4880911
    Abstract: Fused-Polypeptides comprising a polypeptide product and a covalently bonded charged amino acid polymer are disclosed. Methods of detecting the presence of the charged amino acid polymer are used to quantitate the presence of the fused-polypeptides either in crude or purified solutions. The charged amino acid polymer is hydrolyzed using an exopeptidase which leaves the polypeptide product. Examples using polyarginine and carboxypeptidase B to produce urogastrone and gamma interferon are included.
    Type: Grant
    Filed: May 9, 1985
    Date of Patent: November 14, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Stephen J. Brewer, Helmut M. Sassenfeld
  • Non-peptidyl beta-succinamidoacyl aminodiols as anti-hypertensive agents
    Patent number: 4877785
    Abstract: Non-peptidyl compounds characterized generally as .beta.-succinamidoacyl aminodios are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: October 1, 1987
    Date of Patent: October 31, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Antagonists of leukotriene D.sub.4
    Patent number: 4870098
    Abstract: This invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:Alk is alkylene or hydroxyalkylene containing 1-6 carbon atoms;Ar is 5,6,7,8-tetrahydro-1-naphthalenyl or phenyl optionally substituted with one or more substituents selected from lower alkyl containing 1 to 6 carbon atoms, hydroxy, lower alkoxy containing 1 to 6 carbon atoms, or lower alkanoyl containing 1 to 6 carbon atoms;R is hydrogen and lower alkyl containing 1 to 6 carbon atoms;X, Y, and Z are each independently O or S with S optionally oxidized to S.dbd.O;m is an integer from 0 to 3;n is an integer from 0 to 5.The compounds are useful as anti-allergy agents and anti-inflammatory agents.
    Type: Grant
    Filed: January 17, 1989
    Date of Patent: September 26, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Michael A. Stealey, Richard M. Weier
  • Diol metabolites of 7-phenyl-1,2,4-triazolo[2,3-c]pyrimidines-5-amines
    Patent number: 4866063
    Abstract: 1-(5-Amino-7-phenyl-[1,2,4] triazolo [1,5,c]pyrimidin-8-yl)-1, 2-ethan diol, a novel glycol of a triazolopyrimidine diuretic which is a metabolite and which exhibits fewer cardiotoxic side effects than the parent compound, but with no decrease in diuretic activity. The invention further provides for compositions incorporating the metabolite, and methods of its use as well as pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 22, 1988
    Date of Patent: September 12, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Earl G. Burton, Christopher P. Chengelis, Gerald M. Walsh
  • Tetraenyl prostaglandins
    Patent number: 4863961
    Abstract: This invention encompasses prostaglandins of the formula ##STR1## wherein R represents hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.1 represents hydrogen, vinyl, or lower alkyl having 1 to 4 carbon atoms and the wavy line represents R or S stereochemistry; R.sub.2, R.sub.3, and R.sub.4 are hydrogen or lower alkyl having 1 to 4 carbon atoms or R.sub.2 and R.sub.3 together with carbon Y form a cycloalkenyl having 4 to 6 carbon atoms or R.sub.3 and R.sub.4 together with carbons X and Y form a cycloalkenyl having 4 to 6 carbons. Compounds of this invention have potent gastric antisecretory and cytoprotective properties with unexpectedly lower diarrheogenic side effects.
    Type: Grant
    Filed: July 28, 1988
    Date of Patent: September 5, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Alan F. Gasiecki
  • Methods and compositions for inhibiting lipoxygenase
    Patent number: 4857558
    Abstract: This invention encompasses a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are same or different members of the group consisting of 1,1-dimethyl ethyl, halo, phenyl and substituted phenyl; Alk is straight or branched chain lower alkylene; R.sub.4 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; or a cycloalkyl group of from 3 to 8 carbon atoms. The formulation of this invention are useful as anti-inflammatory and anti-allergy agents.
    Type: Grant
    Filed: May 20, 1988
    Date of Patent: August 15, 1989
    Assignee: G. D. Searle & Co.
    Inventor: Richard A. Mueller
  • Furyl, phenylene, and thienyl leukotriene B.sub.4 analogues
    Patent number: 4855324
    Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, or --CH.dbd.CH--;wherein Z is OR.sup.1 or --NR.sup.4 R.sup.5 ;wherein R.sup.1 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;wherein R.sup.2 is H, --CH.sub.3 or --C.sub.2 H.sub.5 ;wherein R.sup.3 is OH, H or .dbd.O;wherein R.sup.4 and R.sup.5 may independently be hydrogen, or lower alkyl having 1-6 carbon atoms, or R.sup.4 and R.sup.5 may act together with N to form a cyclic amide of the formula: ##STR2## wherein n is an integer from 4-5; and m is an integer from 0-4. More particularly, this invention relates to compounds of the above formula which have utility as LTB.sub.4 antagonists.
    Type: Grant
    Filed: February 18, 1988
    Date of Patent: August 8, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Stella S. Yu