Eric A Gordon

US Patent:

51069920, Apr 21, 1992

Filed:

Apr 30, 1990

Appl. No.:

7/516867

Inventors:

David R. Magnin - Plainsboro NJ
Eric M. Gordon - Pennington NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07D27704
C07D41906

US Classification:

548200

Abstract:

3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R. sup. 6 is an alkali metal, lower alkyl or H; R. sup. 1 and R. sup. 2 are the same or different and are H, lower alkyl or aryl; X is S, O, ##STR3## or a single bond; R. sup. 7 is lower alkyl; R. sup. 3 is lower alkyl or aryl; R. sup. 4 and R. sup. 5 are the same or different and are H or lower alkyl; and --- represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents. In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.

US Patent:

52760219, Jan 4, 1994

Filed:

Dec 19, 1991

Appl. No.:

7/810099

Inventors:

Donald S. Karanewsky - East Windsor NJ
Michael C. Badia - Lawrenceville NJ
Scott A. Biller - Ewing NJ
Eric M. Gordon - Pennington NJ
Michael J. Sofia - Lawrenceville NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07F 902
C07C 6973
A61K 3166

US Classification:

514120

Abstract:

Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## wherein R is OH, or salts thereof or lower alkoxy; R. sup. x is H or alkyl; X is --CH. sub. 2 --, --CH. sub. 2 --CH. sub. 2 --, --CH. dbd. CH--, --C. tbd. C--, --CH. sub. 2 CH. sub. 2 CH. sub. 2 -- or --CH. sub. 2 O-- (where O is linked to Z); Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds.

US Patent:

50177168, May 21, 1991

Filed:

Dec 1, 1989

Appl. No.:

7/444336

Inventors:

Donald S. Karanewsky - East Windsor NJ
Scott A. Biller - Ewing NJ
Eric M. Gordon - Pennington NJ

Assignee:

E.R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07F 708

US Classification:

556405

Abstract:

Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, lower alkoxy or lower alkyl; R. sup. x is H or alkyl; X is --O-- or --NH--; n is 1 or 2 Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds. New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

US Patent:

50913786, Feb 25, 1992

Filed:

Apr 18, 1988

Appl. No.:

7/182710

Inventors:

Donald S. Karanewsky - East Windsor NJ
Michael C. Badia - Lawrenceville NJ
Scott A. Biller - Ewing NJ
Eric M. Gordon - Pennington NJ
Michael J. Sofia - Lawrenceville NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

C07F 96503
C07F 96506
C07F 9572
C07F 96553

US Classification:

514 80

Abstract:

Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesteroleumic agents are provided which have the structure ##STR1## wherein R is OH, or salts thereof or lower alkoxy; R. sup. x is H or alkyl; X is --CH. sub. 2 --, --CH. sub. 2 --CH. sub. 2 --, --CH. dbd. CH--, --C. tbd. C--, --CH. sub. 2 CH. sub. 2 CH. sub. 2 -- or --CH. sub. 2 O-- (where O is linked to Z); Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds. New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.

US Patent:

49702211, Nov 13, 1990

Filed:

Jul 28, 1989

Appl. No.:

7/386162

Inventors:

David R. Magnin - Plainsboro NJ
Eric M. Gordon - Pennington NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

G07D27706
G07D41706
A61K 31425

US Classification:

514365

Abstract:

3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R. sup. 6 is an alkali metal, lower alkyl or H; R. sup. 1 and R. sup. 2 are the same or different and are H, lower alkyl or aryl; X is S, O, ##STR3## or a single bond; R. sup. 7 is lower alkyl; R. sup. 3 is lower alkyl or aryl; R. sup. 4 and R. sup. 5 are the same or different and are H or lower alkyl; and represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents. In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.

US Patent:

49046462, Feb 27, 1990

Filed:

Apr 18, 1988

Appl. No.:

7/182696

Inventors:

Donald S. Karanewsky - East Windsor NJ
Scott A. Biller - Ewing NJ
Eric M. Gordon - Pennington NJ

Assignee:

E. R. Squibb & Sons, Inc. - Princeton NJ

International Classification:

A61K 3166
C07F 930
C07F 932

US Classification:

514120

Abstract:

Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, lower alkoxy or lower alkyl; R. sup. x is H or alkyl; X is --O-- or --NH--; n is 1 or 2 Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds. New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.