Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.
Type:
Grant
Filed:
April 2, 2004
Date of Patent:
January 2, 2007
Assignee:
G.D. Searle, LLC
Inventors:
Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
Abstract: A therapeutic method is described for treating cardiofibrosis or cardiac hypertrophy using a combination therapy comprising a therapeutically-effective amount of an angiotensin II receptor antagonist and a therapeutically-effective amount of expoxymexrenone.
Type:
Grant
Filed:
February 21, 2003
Date of Patent:
January 10, 2006
Assignee:
G.D Searle & Co.
Inventors:
James J. Egan, Ellen G. McMahon, Gillian M. Olins, Joseph R. Schuh
Abstract: The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.
Type:
Grant
Filed:
November 6, 2002
Date of Patent:
March 8, 2005
Assignee:
G. D. Searle & Co.
Inventors:
Shilpa S. Thosar, Rajeev D. Gokhale, Dwain S. Tolbert
Abstract: Methods of using eplerenone, an angiotensin converting enzyme inhibitor and optionally a diuretic are described for treatment of heart failure and hypertension.
Type:
Grant
Filed:
February 15, 2002
Date of Patent:
June 8, 2004
Assignee:
Pharmacia Corporation
Inventors:
Alfonzo T. Perez, Debra J. Asner, Richard J. LaChapelle, John C. Alexander, Barbara Roniker
Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful as renin inhibitors for the treatment of hypertension.
Abstract: A class of amino-isoxazolidone compounds is described for use to improve lexical priming in patients susceptible to or afflicted with Alzheimer's Disease. Preferred compounds of this class are D-cycloserine and its prodrugs.
Type:
Grant
Filed:
May 23, 2002
Date of Patent:
December 2, 2003
Assignee:
Pharmacia Corporation
Inventors:
Robert L. Herting, Barbara L. Schwartz, Stephen I. Deutsch
Abstract: Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula:
wherein R1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C.
Type:
Grant
Filed:
March 26, 1999
Date of Patent:
October 14, 2003
Assignee:
G. D Searle & Co
Inventors:
James A. Sikorski, Devadas Balekudru, Daniel P. Getman, David L. Brown, Srinivasan Nagarajan, Mark E. Zupec, Jeffrey I. Gordon
Abstract: Non-peptidic compounds characterized by containing a segment condensed from pipecolic acid, aspartic acid, proline and threonine, or derivatives thereof, are useful to treat autoimmune diseases and inflammatory conditions.
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
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
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
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.
Abstract: Compounds characterized generally as propargyl glycine amino propargyl diol derivatives are useful for treatment of a disorder mediated by inhibiting plasma renin activity.