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Hydroxamic acid derivatives of mercaptoacyl amino acids

Assignee: ER Squibb and Sons LLC
•
Filing: 1979-12-03
•
Granted: 1981-08-18
•
Expires: 1999-12-03
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Abstract

Abstract Hydroxamic acid derivatives of certain mercaptoacyl amino acids inhibit the conversion of angiotensin I to angiotensin II in mammals and are useful for the treatment of hypertension.

Inventors

  • 👤 Edward W. Petrillo, Jr.
  • 👤 Miguel A. Ondetti

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 02:29
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/10; C07D207/16

Claims Analysis

Total Claims: 20
Claim 1
Independent Claim 125 words
A compound having the formula ##STR9## wherein R 1 is hydrogen, alkyl, aryl, arylalkyl or ##STR10## wherein R 5 is alkyl or aryl; R 2 is hydrogen, alkyl, trifluoromethyl or pentafluoroethyl; R 3 is --CH 2 --, --CH(OH)--, --CH(O-alkyl)--, --CH(O-aryl)--, --CH(S-alkyl), --CH(S-aryl), --C(O-alkyl) 2 , --C(S-alkyl) 2 , ##STR11## --CCl 2 --, --CF 2 --, --CHCl--, or --CHF-- and R 4 is --CH 2 ; or together, R 3 and R 4 are --CH═CH--; and n is 0, 1 or 2; wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR12## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.
Claim 2
Dependent Claim 125 words
A compound having the formula ##STR9## wherein R 1 is hydrogen, alkyl, aryl, arylalkyl or ##STR10## wherein R 5 is alkyl or aryl; R 2 is hydrogen, alkyl, trifluoromethyl or pentafluoroethyl; R 3 is --CH 2 --, --CH(OH)--, --CH(O-alkyl)--, --CH(O-aryl)--, --CH(S-alkyl), --CH(S-aryl), --C(O-alkyl) 2 , --C(S-alkyl) 2 , ##STR11## --CCl 2 --, --CF 2 --, --CHCl--, or --CHF-- and R 4 is --CH 2 ; or together, R 3 and R 4 are --CH═CH--; and n is 0, 1 or 2; wherein the term "aryl" refers to phenyl or phenyl substituted with one, two or three halogen, alkyl, alkoxy, hydroxy, ##STR12## nitro, amino, alkylamino, dialkylamino, trifluoromethyl, cyano or carboxyl groups, and the terms "alkyl" and "alkoxy" refer to groups having 1 to 8 carbon atoms.
Claim 3
Dependent Claim 11 words
A compound in accordance with claim 1 wherein n is 1.
Claim 4
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CH(OH)--.
Claim 5
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CH(O-alkyl)--.
Claim 6
Dependent Claim 14 words
A compound in accordance with claim 4 wherein R 3 is --CH(OCH 3 )--.
Claim 7
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CH(O-aryl)--.
Claim 8
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CH(S-alkyl)--.
Claim 9
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CH(S-aryl)--.
Claim 10
Dependent Claim 14 words
A compound in accordance with claim 2 wherein R 3 is --C(O-alkyl) 2 --.
Claim 11
Dependent Claim 16 words
A compound in accordance with claim 9 wherein R 3 is --C(OCH 3 ) 2 --.
Claim 12
Dependent Claim 14 words
A compound in accordance with claim 2 wherein R 3 is --C(S-alkyl) 2 --.
Claim 13
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is ##STR13##
Claim 14
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is ##STR14##
Claim 15
Dependent Claim 13 words
A compound in accordance with claim 2 wherein R 3 --CCl 2 --.
Claim 16
Dependent Claim 14 words
A compound in accordance with claim 2 wherein R 3 is --CF 2 --.
Claim 17
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CHCl--.
Claim 18
Dependent Claim 12 words
A compound in accordance with claim 2 wherein R 3 is --CHF--.
Claim 19
Dependent Claim 16 words
A compound in accordance with claim 2 wherein R 3 and R 4 are together --CH═CH--.
Claim 20
Dependent Claim 8 words
The compound in accordance with claim 1 (S)-N-hydroxy-1-(3-mercapto-2-methyl-1-oxopropyl)-L-prolinamide.

References Cited (Backward Citations)

US4046889A Cited
US4154840A Cited
US4105776A Cited
BE861454A Cited
GB2014132A Cited
US4129566A Cited
US4154942A Cited
US4154935A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-08-17 1985-02-16 1985-08-18 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-08-17 1989-02-16 1989-08-18 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-08-17 1993-02-16 1993-08-18 $7700.00 Window Closed / Lapsed

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