Patents Represented by Attorney, Agent or Law Firm J. Timothy Keane
  • Patent number: 6458803
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.
    Type: Grant
    Filed: November 23, 2001
    Date of Patent: October 1, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6455519
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N- disubstituted fused-heterocyclo amines.
    Type: Grant
    Filed: November 15, 2001
    Date of Patent: September 24, 2002
    Assignee: G.D. SEarle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6451852
    Abstract: A class of substituted phenylacetonitrile-alkylaminoalkyl-ortho-substituted aryl 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.
    Type: Grant
    Filed: January 22, 2001
    Date of Patent: September 17, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Dean Liang, John P. McKearn, John M. Farah, Jr., Richard A. Mueller
  • Patent number: 6451823
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenoxy-N-phenyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 17, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6451830
    Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 17, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6451833
    Abstract: A class of N-substituted (&agr;-imidazolyl-toluyl)pyrrole compounds described for use in treatment of circulatory disorders.
    Type: Grant
    Filed: November 1, 2000
    Date of Patent: September 17, 2002
    Assignee: Pharmacia Corporation
    Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
  • Patent number: 6448295
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-fused-phenyl-N-benzyl aminoalcohols.
    Type: Grant
    Filed: November 14, 2001
    Date of Patent: September 10, 2002
    Assignee: G.D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6420404
    Abstract: D-4-amino-3-isoxazolidone is described for use to improve implicit memory in patients susceptible to or afflicted with Alzheimer's Disease.
    Type: Grant
    Filed: February 26, 2001
    Date of Patent: July 16, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Robert L. Herting, Barbara L. Schwartz, Stephen I. Deutsch
  • Patent number: 6410524
    Abstract: Combinations of an ACE inhibitor, an aldosterone antagonist, and a loop diuretic are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril, enalapril or lisinopril co-administered with spironolactone. This co-therapy would be particularly useful to reduce the death rate or the number of non-fatal hospitalizations or prevent the progression of congestive heart failure in patients with cardiovascular disease.
    Type: Grant
    Filed: November 5, 1999
    Date of Patent: June 25, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Alfonzo T. Perez, Debra J. Asner, Richard J. LaChapelle, John C. Alexander, Barbara Roniker
  • Patent number: 6403648
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated &bgr;-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R2 is selected from hydrido, methyl, ethyl and phenyl; wherein R3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R5 is methyl; wherein R7 is cyclohexylmethyl; wherein R8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R9 and R10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: January 17, 2001
    Date of Patent: June 11, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Barbara B. Chen
  • Patent number: 6391867
    Abstract: Use of an aldosterone receptor antagonist, spironolactone, is described for treatment of heart failure. This therapy would be particularly useful to treat or retard the development of symptomatic heart failure, while avoiding or reducing aldosterone-antagonist-induced side effects, such as hyperkalemia.
    Type: Grant
    Filed: January 9, 2001
    Date of Patent: May 21, 2002
    Assignee: G.D. Searle & Co.
    Inventors: Todd E. MacLaughlan, Alfonso T. Perez
  • Patent number: 6342624
    Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity.
    Type: Grant
    Filed: January 6, 2000
    Date of Patent: January 29, 2002
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 6291529
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated sulfide/sulfonyl-containing propargyl amino-diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula II: wherein q is two or three; wherein r is zero or two; wherein R2 is selected from hydrido, methyl, ethyl and phenyl; wherein R3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R5 is propargyl or a propargyl containing moiety; wherein R7 is cyclohexylmethyl; wherein R8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R12 and R13 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: June 6, 2000
    Date of Patent: September 18, 2001
    Assignee: G. D. Searle & Co.
    Inventor: Gunnar J. Hanson
  • Patent number: 6281235
    Abstract: Compounds characterized generally as amino acyl amino propargyl diol derivatives are useful as renin inhibitors for the treatment of a renin-mediated disease Compounds of particular interest are those of Formula I wherein A is selected from CO and SO2; wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is a group independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, benzyl, &bgr;,&bgr;&bgr;-trifluoroethyl, t-butyloxycarbonyl and methoxymethylcarbonyl, and wherein the nitrogen atom to which R1 and R9 are attached may be combined with oxygen to form an N-oxide; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, cyclohexylmethyl, phenethyl, imidazolemethyl, pyridylmethyl and 2-pyridylethyl; wherein R5 is selected from hydrido, alkyl, pyrazolealkyl, pyridylalkyl, thiazolylalkyl, imidazolealkyl, thienylalkyl, furanylalkyl, oxazolylalkyl, isoxazolylalkyl, pyrimidinylalkyl, pyridazinylalkyl and pyrazi
    Type: Grant
    Filed: May 24, 1999
    Date of Patent: August 28, 2001
    Assignee: G.D. Searle & Co.
    Inventors: Gunnar J. Hanson, J. Timothy Keane
  • Patent number: 6265439
    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.
    Type: Grant
    Filed: April 3, 2000
    Date of Patent: July 24, 2001
    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: 6174923
    Abstract: Compounds characterized generally as ethynyl alanine amino diol derivatives are useful to treat disorders mediated by plasma renin activity.
    Type: Grant
    Filed: January 28, 1999
    Date of Patent: January 16, 2001
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • Patent number: 6114381
    Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a .beta.-phenyl-.alpha.-aminopropionic acid N phenyl amide compound as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula ##STR1## wherein each of R.sup.1 and R.sup.5 is independently selected from hydrido, fluoro, chloro, bromo, methyl and ethyl; wherein R.sup.3 is selected from hydroxy, methoxy, ethoxy, methoxycarbonyloxy, ethoxycarbonyloxy, (2-methylpropoxy)carbonyloxy and (2-propenyloxy) carbonyloxy; wherein each of R.sup.6, R.sup.7 and R.sup.8 is hydrido; wherein each of R.sup.9 and R.sup.10 is independently selected from hydrido, methyl and ethyl; wherein R.sup.
    Type: Grant
    Filed: October 13, 1998
    Date of Patent: September 5, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Barnett S. Pitzele, Nizal S. Chandrakumar, Michael Clare
  • Patent number: 6084093
    Abstract: The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: ##STR1## wherein R, R', R.sub.1, R'.sub.1, R.sub.2, R'.sub.2, R.sub.3, R'.sub.3, R.sub.4, R'.sub.4, R.sub.5, R'.sub.5, R.sub.6, R'.sub.6, R.sub.7, R'.sub.7, R.sub.8, R'.sub.8, R.sub.9, and R'.sub.9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: July 4, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Dennis P. Riley, Randy H. Weiss, William L. Neuman, Anil S. Modak, Patrick J. Lennon, Karl W. Aston
  • Patent number: 6008368
    Abstract: Pharmaceutical compositions comprising a compound selected from a class of N-substituted (.alpha.-imidazolyl-toluyl)pyrrole compounds are described for use in treatment of circulatory disorders. Compositions of particular interest comprise angiotensin II antagonist compounds of the formula ##STR1## wherein m is one; wherein R.sup.0 is selected from CH.sub.2 OH, CO.sub.2 H, CHO, CO.sub.2 CH.sub.3, CO.sub.2 C.sub.2 H.sub.5, CH.sub.2 OCH.sub.3, CH.sub.2 OCHOCH.sub.3 and CH.sub.2 --CO.sub.2 C.sub.2 H.sub.5 ; wherein R.sup.1 is selected from Cl, CF.sub.3, CHO, n-butyl, cyano, CO.sub.2 CH.sub.3 and CO.sub.2 CH.sub.2 CH.sub.3 ; wherein R.sup.2 is selected from methyl, ethyl, n-propyl, isopropyl, n-butyl, sec-butyl, isobutyl, tert-butyl, n-pentyl, isopentyl, neopentyl, phenyl, benzyl, phenethyl, cyclohexyl, cyclohexylmethyl, cyclohexylethyl, propylthio, butylthio and hydroxyalkyl; wherein each of R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.9 and R.sup.10 is hydrido; wherein each of R.sup.5 and R.sup.
    Type: Grant
    Filed: November 24, 1997
    Date of Patent: December 28, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joe T. Collins, Robert E. Manning
  • Patent number: 5968984
    Abstract: Compounds characterized generally as alkylaminoalkyl-terminated .beta.-alanineamide amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of the formula ##STR1## wherein n is two or three; wherein x is a number selected from zero, one and two; wherein R.sup.2 is selected from hydrido, methyl, ethyl and phenyl; wherein R.sup.3 is selected from hydrido, cyclohexylmethyl, benzyl, fluorobenzyl, chlorobenzyl, napthylmethyl, fluoronaphthylmethyl and chloronaphthylmethyl; wherein R.sup.5 is methyl; wherein R.sup.7 is cyclohexylmethyl; wherein R.sup.8 is selected from n-propyl, isobutyl, cyclopropyl, cyclopropylmethyl, allyl and vinyl; and wherein each of R.sup.9 and R.sup.10 is a group independently selected from methyl, ethyl and isopropyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 14, 1997
    Date of Patent: October 19, 1999
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran, Barbara B. Chen