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Antihypertensive amides

Assignee: USV Pharmaceutical Corp
•
Filing: 1979-07-13
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Granted: 1981-03-17
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Expires: 1999-07-13
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Abstract

Abstract Compounds of the structure: <IMAGE> wherein R1, R2, R3, R4, R5, and R6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, n is an integer from 0 to 4 inclusive, M is alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, polycycloalkyl, polycyclo-alkyl-alkyl, aryl, aralkyl, heteroaryl, heteroaryl-alkyl, hetero-cycloalkyl, hetero-cycloalkyl-alkyl, alkoxyalkyl, alkylthioalkyl, alkylamino-alkyl, dialkylamino-alkyl, fused aryl-cycloalkyl, fused aryl-cycloalkyl-alkyl, fused heteroaryl-cycloalkyl, or fused heteroaryl-cycloalkyl-alkyl, Y is hydroxy, alkoxy, amino, or substituted amino, aminoalkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, and R7 is hydrogen, alkanoyl, carboxylalkanoyl, hydroxyalkanoyl, amino-alkanoyl, cyano, amidino, carbalkoxy, ZS, or <IMAGE> wherein Z is hydrogen, alkyl, hyroxyalkyl, aminoalkyl or the radical <IMAGE> wherein R1, R2, R3, R4, R5, R6, n, M and Y are as described above; and where Y is hydroxy their non-toxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.

Inventors

  • 👤 John T. Suh
  • 👤 Jerry W. Skiles
  • 👤 Bruce E. Williams
  • 👤 Alfred Schwab

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-04 17:01
CPC Classifications
C; C07; C07D; C07D213/00; C07D213/02; C07D213/04; C07D213/24; C07D213/36; C07D213/40; A; A61; A61P; A61P43/00; A61P9/00; A61P9/12; C07C; C07C327/00; C07D207/00; C07D207/02; C07D207/04; C07D207/08; C07D211/00; C07D211/04; C07D211/06; C07D211/08; C07D211/18; C07D211/26; C07D213/60; C07D213/72; C07D213/75; C07D217/00; C07D217/22; C07D219/00; C07D219/14; C07D235/00; C07D235/02; C07D235/04; C07D235/24; C07D235/30; C07D239/00; C07D239/02; C07D239/24; C07D239/28; C07D239/32; C07D239/42; C07D277/00; C07D277/02; C07D277/20; C07D277/32; C07D277/38; C07D277/44; C07D277/46; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/52; C07D307/56; C07D307/66; C07D307/77; C07D307/78; C07D307/82; C07D309/00; C07D309/02; C07D309/08; C07D309/14; C07D317/00; C07D317/08; C07D317/44; C07D317/46; C07D317/48; C07D317/62; C07D317/66; C07D319/00; C07D319/10; C07D319/14; C07D319/16; C07D319/18; C07D333/00; C07D333/02; C07D333/04; C07D333/06; C07D333/14; C07D333/20; C07D333/26; C07D333/30; C07D333/36; C07D333/46; C07D333/48

Claims Analysis

Total Claims: 19
Claim 1
Independent Claim 214 words
Compounds of the structure ##STR13## wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are independently hydrogen, lower alkyl, lower alkenyl, lower alkenyl, or phenyl-lower alkyl, wherein the lower alkyl, lower alkenyl and lower alkynyl groups have up to 6 carbon atoms, n is an integer from 0 to 4, M is lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, fused arylcycloalkyl, phenyl, lower alkylphenyl, phenyl-lower alkyl, hydroxyphenyl, methylenedioxyphenyl, bicycloalkyl-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, halophenyl or, lower alkylthiophenyl, wherein the lower alkyl, lower alkenyl and lower alkynyl groups contain up to 6 carbon atoms and the cycloalkyl, cycloalkyl lower alkyl, bicycloalkyl, and fused aryl-cycloalkylkyl groups contain from 3 to 16 carbon atoms, Y is hydroxy, lower alkoxy having 1 to 6 carbon atoms or amino, R 7 is hydrogen, lower alkanoyl, benzoyl, ZS or ##STR14## wherein the lower alkanoyl contains up to 6 carbon atoms Z is hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, or a radical of the formula ##STR15## wherein R 1 , R 2 , R 3 , R 4 , R 6 , n, M and Y are as defined above, and where Y is hydroxy, their non-toxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.
Claim 2
Dependent Claim 214 words
Compounds of the structure ##STR13## wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are independently hydrogen, lower alkyl, lower alkenyl, lower alkenyl, or phenyl-lower alkyl, wherein the lower alkyl, lower alkenyl and lower alkynyl groups have up to 6 carbon atoms, n is an integer from 0 to 4, M is lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, fused arylcycloalkyl, phenyl, lower alkylphenyl, phenyl-lower alkyl, hydroxyphenyl, methylenedioxyphenyl, bicycloalkyl-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, halophenyl or, lower alkylthiophenyl, wherein the lower alkyl, lower alkenyl and lower alkynyl groups contain up to 6 carbon atoms and the cycloalkyl, cycloalkyl lower alkyl, bicycloalkyl, and fused aryl-cycloalkylkyl groups contain from 3 to 16 carbon atoms, Y is hydroxy, lower alkoxy having 1 to 6 carbon atoms or amino, R 7 is hydrogen, lower alkanoyl, benzoyl, ZS or ##STR14## wherein the lower alkanoyl contains up to 6 carbon atoms Z is hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, or a radical of the formula ##STR15## wherein R 1 , R 2 , R 3 , R 4 , R 6 , n, M and Y are as defined above, and where Y is hydroxy, their non-toxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.
Claim 3
Dependent Claim 29 words
A compound according to claim 1 where R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are hydrogen or lower alkyl.
Claim 4
Dependent Claim 10 words
A compound according to claim 2 wherein n is 1.
Claim 5
Dependent Claim 10 words
A compound according to claim 3 wherein Y is hydroxy.
Claim 6
Dependent Claim 29 words
A compound according to claim 4 wherein R 1 , R 3 , R 4 , R 5 and R 6 are hydrogen and R 2 is lower alkyl.
Claim 7
Dependent Claim 11 words
A compound according to claim 5 wherein R 2 is methyl.
Claim 8
Dependent Claim 11 words
A compound according to claim 6 wherein R 7 is hydrogen.
Claim 9
Dependent Claim 12 words
A compound according to claim 6 wherein R 7 is lower alkanoyl.
Claim 10
Dependent Claim 11 words
A compound according to claim 8 wherein R 7 is acetyl.
Claim 11
Dependent Claim 10 words
A compound according to claim 7 wherein M is cyclopropyl.
Claim 12
Dependent Claim 10 words
A compound according to claim 7 wherein M is cyclopentyl.
Claim 13
Dependent Claim 10 words
A compound according to claim 9 wherein M is cyclopentyl.
Claim 14
Dependent Claim 10 words
A compound according to claim 7 wherein M is exo-norbornyl.
Claim 15
Dependent Claim 10 words
A compound according to claim 9 wherein M is exo-norbornyl.
Claim 16
Dependent Claim 10 words
A compound according to claim 7 wherein M is cyclobutyl.
Claim 17
Dependent Claim 10 words
A compound according to claim 7 wherein M is cycloheptyl.
Claim 18
Dependent Claim 23 words
A method of reducing the blood pressure in mammals having hypertension which comprises administering an effective amount of a compound of claim 1.
Claim 19
Dependent Claim 10 words
A compound according to claim 7 wherein M is 2-indanyl.

References Cited (Backward Citations)

US3869492A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-03-16 1984-09-15 1985-03-17 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-03-16 1988-09-15 1989-03-17 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-03-16 1992-09-15 1993-03-17 $7700.00 Window Closed / Lapsed

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