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Thiopropionamides, and the pharmaceutical compositions

Assignee: Science Union et Cie
•
Filing: 1978-09-25
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Granted: 1981-08-11
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Expires: 1998-09-25
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Abstract

Abstract This invention relates to omega-mercaptopropionylamides, the nitrogen atom of which is included as a ring atom of a cyclic amino acid. The application also discloses a process for producing said compounds which comprises reacting an omega-mercaptopropionic acid, or a functional derivative thereof, with a cyclic amino acid. This invention further relates to pharmaceutical compositions incorporating such an omega-mercaptopropionylamide as active ingredient together with a pharmaceutically-acceptable carrier or vehicle, and a method of employing said compounds. They find a use in human therapy, namely, as antihypertensive agents.

Inventors

  • 👤 Charles Malen
  • 👤 Pierre Roger
  • 👤 Michel Laubie

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 17:57
CPC Classifications
C; C07; C07D; C07D277/00; C07D277/02; C07D277/04; C07D277/06; A; A61; A61P; A61P9/00; A61P9/12; C07D279/00; C07D279/10; C07D279/12

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 84 words
A compound of the formula ##STR19## where R is hydrogen, loweralkyl, loweralkanoyl, phenylloweralkyl or phenyl, where each of such phenyl rings may be substituted with one to three substituents selected from the group consisting of halogen, trifluoromethyl, lower alkyloxy, vinyl, lower alkylenedioxy, hydroxy and lower alkyl; R 2 is hydrogen, loweralkyl or lower cycloalkyl; Z is sulfur, sulfoxide or sulfonyl; R 3 is hydrogen or loweralkyl; m is 1; n is 1; p is 0, 1, or 2; and X is an amino group.
Claim 2
Dependent Claim 84 words
A compound of the formula ##STR19## where R is hydrogen, loweralkyl, loweralkanoyl, phenylloweralkyl or phenyl, where each of such phenyl rings may be substituted with one to three substituents selected from the group consisting of halogen, trifluoromethyl, lower alkyloxy, vinyl, lower alkylenedioxy, hydroxy and lower alkyl; R 2 is hydrogen, loweralkyl or lower cycloalkyl; Z is sulfur, sulfoxide or sulfonyl; R 3 is hydrogen or loweralkyl; m is 1; n is 1; p is 0, 1, or 2; and X is an amino group.
Claim 3
Dependent Claim 18 words
The salts of the compounds of formula I according to claim 1 with an organic or inorganic base.
Claim 4
Dependent Claim 14 words
The diastereisomers and the optically active isomers of a compound according to claim 1.
Claim 5
Dependent Claim 13 words
A compound according to claim 1 which is N-(3 mercapto 2-methyl propionyl) thiazolidinyl-4-carboxamide.
Claim 6
Dependent Claim 33 words
The pharmaceutical compositions which includes as active ingredient (s) at least one compound of claim 1 or a base-addition salt thereof in admixture or conjunction with an inert non-toxic pharmaceutically-acceptable carrier or vehicle.
Claim 7
Dependent Claim 26 words
A pharmaceutical composition according to claim 5 in which the amount of a compound of claim 1 ranges from 10 to 100 mg per unit dosage.
Claim 8
Dependent Claim 49 words
A method for treating hypertension in hypertensive patients suffering from an excessive blood content of Angiotensin II which consists in administering to said patients a small but effective amount of a compound of claim 1 or a salt thereof to curb the conversion of Angiotensin I into Angiotensin II.
Claim 9
Dependent Claim 32 words
The method of claim 7 wherein the small but effective amount of a compound of claim 1 or a salt thereof ranges from 20 to 100 mg a day in the man.

References Cited (Backward Citations)

FR2285876B1 Cited
FR2315271B1 Cited
US4192878A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1984-08-10 1985-02-09 1985-08-11 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1988-08-10 1989-02-09 1989-08-11 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1992-08-10 1993-02-09 1993-08-11 $7700.00 Window Closed / Lapsed

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