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US4404206A Expired / Lapsed US ⏱️ 0.0 years remaining

Substituted iminoacid derivatives, process for preparing them and their use as enzyme inhibitors

Assignee: Institut Servier de Medecine Translationnelle SARL
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Filing: 1980-12-03
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Granted: 1983-09-13
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Expires: 2000-12-03
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Abstract

Abstract Bicyclic imino acids, particularly 2-carboxylic acid derivatives of azabicycloalkanes and process for preparing them. These compounds have therapeutical activity and may be used as medicines, particularly as cardiovascular and antihypertensive drugs in human or veterinary medicine.

Inventors

  • 👤 Michel Vincent
  • 👤 Georges Remond
  • 👤 Michel Laubie

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-10-23 18:58
CPC Classifications
C; C07; C07D; C07D471/00; C07D471/02; C07D471/04; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/42; C07D209/44; C07D217/00; C07D217/22; C07D217/26; C07D495/00; C07D495/02; C07D495/04; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06017; C07K5/06026

Claims Analysis

Total Claims: 10
Claim 1
Independent Claim 109 words
A compound selected from the group consisting of bicyclic iminoacids of the formula I ##STR6## wherein A, m, and n are selected to provide a perhydroquinoline or perhydroisoquinoline ring system, q represents 0 or the number 1 or 2, R is hydrogen, methyl, or benzyl, R 1 is hydrogen or lower-alkyl of no more than 5 carbon atoms, R 2 is hydroxyl or lower-alkoxy of no more than 5 carbon atoms, and Z is carboxyl, cyano, hydroxyl, sulfhydryl, or amino, in racemic or optically-active form, and pharmaceutically-acceptable addition salts thereof, when R 2 is hydroxy with a mineral or organic base and, when Z is amino, with an acid.
Claim 2
Dependent Claim 109 words
A compound selected from the group consisting of bicyclic iminoacids of the formula I ##STR6## wherein A, m, and n are selected to provide a perhydroquinoline or perhydroisoquinoline ring system, q represents 0 or the number 1 or 2, R is hydrogen, methyl, or benzyl, R 1 is hydrogen or lower-alkyl of no more than 5 carbon atoms, R 2 is hydroxyl or lower-alkoxy of no more than 5 carbon atoms, and Z is carboxyl, cyano, hydroxyl, sulfhydryl, or amino, in racemic or optically-active form, and pharmaceutically-acceptable addition salts thereof, when R 2 is hydroxy with a mineral or organic base and, when Z is amino, with an acid.
Claim 3
Dependent Claim 2 words
2-[3-Mercapto-2-(RS)-methylpropionyl]-cis-perhydroisoquinoline-3-carboxylic acid.
Claim 4
Dependent Claim 2 words
2-[3-Mercapto-2-(RS)-methylpropionyl]-cis-perhydroisoquinoline-3-carboxylic acid.
Claim 5
Dependent Claim 1 words
1-(3-mercapto-2-(RS)-methylpropionyl)-2-(RS)-carboxyperhydroquinoline.
Claim 6
Dependent Claim 1 words
1-(3-mercapto-2-(RS)-methylpropionyl)-2-(RS)-carboxyperhydroquinoline.
Claim 7
Dependent Claim 33 words
Pharmaceutical composition, useful for treatment of high blood pressure and cardiac failure, containing as active ingredient a compound of claim 1 in admixture or conjunction with an inert, non-toxic, therapeutically-compatible carrier or vehicle.
Claim 8
Dependent Claim 20 words
A pharmaceutical composition as claimed in claim 4 in which the carrier is adapted for oral, parenteral, or rectal administration.
Claim 9
Dependent Claim 20 words
A pharmaceutical composition as claimed in claim 4 containing the active principle at the dose of 25 to 250 mg.
Claim 10
Dependent Claim 39 words
A method of treating high blood pressure and cardiac failure in a subject, which consists in administering to said subject an effective amount of a compound of claim 1 or a salt thereof together with a therapeutically suitable carrier.

References Cited (Backward Citations)

GB975835A Cited
DE2435169A1 Cited
GB1524481A Cited
US4261895A Cited
EP0012845A1 Cited
US4256751A Cited
FR2448533B1 Cited
US4294832A Cited
US4303583A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1986-09-12 1987-03-14 1987-09-13 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1990-09-12 1991-03-14 1991-09-13 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1994-09-12 1995-03-14 1995-09-13 $7700.00 Window Closed / Lapsed

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