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US4735965A Expired / Lapsed US ⏱️ 0.0 years remaining

7-oxo-PGI2 -ephedrine salts and their pharmaceutical compositions and methods

Assignee: Chinoin Private Co Ltd
•
Filing: 1986-05-28
•
Granted: 1988-04-05
•
Expires: 2006-05-28
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Abstract

Abstract The invention relates to new 7-oxo-PGI 2 -ephedrine salt analogues of the Formula I ##STR1## wherein A stands for --(CH 2 ) 2 --, cis or trans --CH═CH-- or --C.tbd.C--; R 1 is lower alkyl or hydrogen; B represents a chemical bond, --CH 2 -- or --CR 2 R 3 ; R 2 stands for lower alkyl or hydrogen; R 3 represents lower alkyl or hydrogen; X is a chemical bond, --O-- or --CH 2 --; R 4 stands for C 1-6 alkyl, C 4-7 cycloalkyl, C 1-6 fluoroalkyl, C 2-6 alkenyl, C 2-6 alkynyl, phenyl, substituted phenyl or heteroaryl. The salts of the Formula I show the same pharmacological profile as the sodium salt of PGI 2 , they inhibit blood aggregation and the secretion of gastric acid, are useful in the prevention of anginal attacks. Accordingly the salts of the present invention are useful in the prevention of peripheral vascular diseases, in improving circulation of extremities, in relieving the seriousness of cardiac infarction and also in the treatment and prevention of gastrointestinal ulcer and acute or chronical liver injury.

Inventors

  • 👤 Gabor Kovacs
  • 👤 Geza Galambos
  • 👤 Istvan Tomoskozi
  • 👤 Karoly Kanai
  • 👤 Peter Gyory
  • 👤 Peter Kormoczy
  • 👤 Istvan Stadler
  • 👤 Laszlo Szekeres
  • 👤 Gyula Papp
  • 👤 Eva Udvary
  • 👤 Pal Hadhazy
  • 👤 Jeno Marton
  • 👤 Gyorgy Dorman

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-06 10:49
CPC Classifications
C; C07; C07H; C07H1/00; C07D; C07D307/00; C07D307/77; C07D307/93; C07D307/935; C07D307/937; A; A61; A61P; A61P1/00; A61P1/04; A61P1/16; A61P35/00; A61P43/00; A61P7/00; A61P7/02; A61P9/00; A61P9/08; A61P9/10; A61P9/12

Claims Analysis

Total Claims: 12
Claim 1
Independent Claim 92 words
An 7-oxo-PGI 2 ephedrine salt of the Formula I, ##STR4## wherein A stands for --(CH 2 ) 2 --, cis or trans --CH═CH-- or --C.tbd.C--; R 1 is lower alkyl or hydrogen; B represents a chemical bond, --CH 2 -- or CR 2 R 3 ; R 2 stands for lower alkyl or hydrogen; R 3 represents lower alkyl or hydrogen; X is a chemical bond, --O-- or --CH 2 --; R 4 stands for C 1-6 alkyl, C 4-7 cycloalkyl, C 1-6 fluoroalkyl, C 2-6 alkenyl, C 2-6 alkynyl or phenyl.
Claim 2
Dependent Claim 92 words
An 7-oxo-PGI 2 ephedrine salt of the Formula I, ##STR4## wherein A stands for --(CH 2 ) 2 --, cis or trans --CH═CH-- or --C.tbd.C--; R 1 is lower alkyl or hydrogen; B represents a chemical bond, --CH 2 -- or CR 2 R 3 ; R 2 stands for lower alkyl or hydrogen; R 3 represents lower alkyl or hydrogen; X is a chemical bond, --O-- or --CH 2 --; R 4 stands for C 1-6 alkyl, C 4-7 cycloalkyl, C 1-6 fluoroalkyl, C 2-6 alkenyl, C 2-6 alkynyl or phenyl.
Claim 3
Dependent Claim 9 words
7-oxo-PGI 2 -(-)-ephedrine salt as defined in claim 1.
Claim 4
Dependent Claim 9 words
7-oxo-16,17,18,19,20-pentanor-15-cyclopentyl-PGI 2 -(-)-ephedrine salt as defined in claim 1.
Claim 5
Dependent Claim 9 words
7-oxo-PGI 2 -(-)-ephedrine salt as defined in claim 1.
Claim 6
Dependent Claim 9 words
7-oxo-16,17,18,19,20-pentanor-15-cyclopentyl-PGI 2 -(+)-ephedrine salt as defined in claim 1.
Claim 7
Dependent Claim 4 words
7-oxo-PGI 2 -(±)-ephedrine salt.
Claim 8
Dependent Claim 4 words
7-oxo-PGI 2 -(±)-ephedrine salt.
Claim 9
Dependent Claim 4 words
7-oxo-16,17,18,19,20-pentanor-15-cyclopentyl-PGI 2 -(±)-ephedrine salt.
Claim 10
Dependent Claim 4 words
7-oxo-16,17,18,19,20-pentanor-15-cyclopentyl-PGI 2 -(±)-ephedrine salt.
Claim 11
Dependent Claim 25 words
A pharmaceutical composition for PGI 2 type therapy consisting essentially of a compound of claim 1 in admixture with suitable inert pharmaceutical carriers and/or excipients.
Claim 12
Dependent Claim 26 words
A method of treating a subject responsive to PGI 2 type therapy which comprises administering an effective amount of a compound as defined in claim 1.

References Cited (Backward Citations)

US4330553A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1991-04-05 1991-10-05 1992-04-05 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1995-04-05 1995-10-05 1996-04-05 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1999-04-05 1999-10-05 2000-04-05 $7700.00 Window Closed / Lapsed

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