Eric J Gordon

US Patent:

51663643, Nov 24, 1992

Filed:

Sep 26, 1991

Appl. No.:

7/765806

Inventors:

Jeffrey O. Saunders - Holland PA
Eric M. Gordon - Pennington NJ

Assignee:

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

International Classification:

C07F 702
C07D30930

US Classification:

549214

Abstract:

Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy- 2-methyl)-substituted-decahydronaphthalene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents. In addition, a method for preparing the above-mevinic acid derivatives is also provided.

US Patent:

41197780, Oct 10, 1978

Filed:

Nov 9, 1977

Appl. No.:

5/850106

Inventors:

Eric M. Gordon - West Trenton NJ

Assignee:

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

International Classification:

C07D50118

US Classification:

544 26

Abstract:

Compounds of the formula ##STR1## R is hydrogen, lower alkyl, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, tri(lower alkyl)silyl, lower alkoxymethyl, 2,2,2-trichloroethyl, ##STR2## Y is halogen or lower alkoxy; R. sub. 1 is lower alkyl, phenyl, or substituted phenyl; and X is hydrogen, lower alkanoyloxy, ##STR3## or certain heterothio groups; R. sub. 4 is hydrogen or lower alkyl; R. sub. 5 is lower alkyl; are disclosed. These compounds, particularly the free acids, possess the useful pharmacological property of inhibiting. beta. -lactamase enzymes as well as being useful as intermediates, particularly where R is a readily cleavable ester, in the preparation of antibacterially active 6. alpha. -methoxy penicillins and 7. alpha. -methoxy cephalosporins.

US Patent:

47228105, Feb 2, 1988

Filed:

Aug 13, 1986

Appl. No.:

6/896318

Inventors:

Norma G. Delaney - Yardley PA
Eric M. Gordon - Pennington NJ
Miguel A. Ondetti - Princeton NJ

Assignee:

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

International Classification:

C08H 300
C08H 902
C07C149273

US Classification:

2604025

Abstract:

Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.

US Patent:

50011480, Mar 19, 1991

Filed:

Jun 7, 1989

Appl. No.:

7/362899

Inventors:

Jeffrey O. Saunders - Holland PA
Eric M. Gordon - Pennington NJ

Assignee:

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

International Classification:

A61K 31365
A61K 31215
C07D30910
C07C 6978

US Classification:

514459

Abstract:

Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R. sup. 1, R. sup. 2 and R. sup. 3 are independently selected from: (1) alkyl, (2) substituted alkyl in which one or more substituents are selected from (a) halogen, (b) hydroxyl, (c) alkoxy, (d) alkoxycarbonyl, (e) acyloxy, (f) cycloalkyl, (g) phenyl, (h) substituted phenyl in which one or more substituents are X or Y, (i) alkyl-S(O). sub. n, (j) cycloalkyl-S(O). sub. n, (k) phenyl-S(O). sub. n, (l) substituted phenyl-S(O). sub. n in which one or more substituents are X or Y, and (m) oxo, (3) alkoxy, (4) alkenyl, (5) cycloalkyl, (6) substituted cycloalkyl in which one or more substituents are selected from (a) alkyl, (b) substituted alkyl in which one or more substituents are selected from (i) halogen, (ii) hydroxy, (iii) alkoxy, (iv) alkoxycarbonyl (v) acyloxy (vi) phenyl (vii) substituted phenyl in which one or more substituents are X and Y, (viii) alkyl-S(O). sub. n, (ix) cycloalkyl-S(O). sub. n, (x) phenyl-S(O). sub.

US Patent:

46365605, Jan 13, 1987

Filed:

Nov 16, 1984

Appl. No.:

6/672044

Inventors:

Jollie D. Godfrey - Trenton NJ
Eric M. Gordon - Pennington NJ
Norma G. Delaney - Princeton NJ

Assignee:

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

International Classification:

C07K 5506
C07K 5508

US Classification:

530331

Abstract:

Analgesic and hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R. sub. 1 and R. sub. 2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl; R. sub. 3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy, or --NY. sub. 1 Y. sub. 2, wherein Y. sub. 1 and Y. sub. 2 are each independently hydrogen, alkyl, aryl, or arylalkyl, or Y. sub. 1 is hydrogen and Y. sub. 2 is substituted alkyl or (heteroaryl)alkyl; A. sub. 1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n. sub. 6 is an integer of 2 to 15; A. sub. 2, A. sub. 3, A. sub. 4 and A. sub.

US Patent:

50990357, Mar 24, 1992

Filed:

Mar 1, 1991

Appl. No.:

7/662597

Inventors:

Jeffrey O. Saunders - Holland PA
Eric M. Gordon - Pennington NJ

Assignee:

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

International Classification:

C07D30930

US Classification:

549292

Abstract:

Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-decahydronapht halene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents. In addition, a method for preparing the above-mevinic acid derivatives is also provided.

US Patent:

41586573, Jun 19, 1979

Filed:

Nov 9, 1977

Appl. No.:

5/849726

Inventors:

Eric M. Gordon - West Trenton NJ

Assignee:

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

International Classification:

C07D27704

US Classification:

2603067C

Abstract:

Compounds of the formula ##STR1## wherein A is ##STR2## R is hydrogen, lower alkyl, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, tri(lower alkyl)silyl, lower alkoxymethyl, 2,2,2-trichloroethyl, ##STR3## or ##STR4## Y is halogen or lower alkoxy; R. sub. 1 is lower alkyl, phenyl, or substituted phenyl; and X is hydrogen, lower alkanoyloxy, ##STR5## or certain heterothio groups; R. sub. 4 is hydrogen or lower alkyl; R. sub. 5 is lower alkyl; are disclosed. These compounds, particularly the free acids, possess the useful pharmacological property of inhibiting. beta. -lactamase enzymes as well as being useful as intermediates, particularly where R is a readily cleavable ester, in the preparation of antibacterially active 6. alpha. -methoxy penicillins and 7. alpha. -methoxy cephalosporins.

US Patent:

41090845, Aug 22, 1978

Filed:

Dec 8, 1976

Appl. No.:

5/748425

Inventors:

Eric M. Gordon - West Trenton NJ

Assignee:

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

International Classification:

C07D50126
C07D50148

US Classification:

544 29

Abstract:

Compounds of the formula ##STR1## wherein A is ##STR2## R is hydrogen, lower alkyl, benzyl, p-methoxybenzyl, p-nitrobenzyl, diphenylmethyl, tri(lower alkyl)silyl, lower alkoxymethyl, 2,2,2-trichloroethyl, ##STR3## Y is halogen or lower alkoxy; R. sub. 1 is lower alkyl, phenyl, or substituted phenyl; and X is hydrogen, lower alkanoyloxy, ##STR4## or certain heterothio groups; R. sub. 4 is hydrogen or lower alkyl; R. sub. 5 is lower alkyl; are disclosed. These compounds, particularly the free acids, possess the useful pharmacological property of inhibiting. beta. -lactamase enzymes as well as being useful as intermediates, particularly where R is a readily cleavable ester, in the preparation of antibacterially active 6. alpha. -methoxy penicillins and 7. alpha. -methoxy cephalosporins.