← Back to Patent Explorer
US4880827A Expired / Lapsed US ⏱️ 0.0 years remaining

Pyrrolidine derivatives having inhibitory action for proline specific endopepidase

Assignee: Sumitomo Pharma Co Ltd
•
Filing: 1987-03-13
•
Granted: 1989-11-14
•
Expires: 2007-03-13
📄 Original PDF 🌐 Google Patents 🔄 Sync Now

Abstract

Abstract Pyrrolidine derivatives having inhibitory action for proline-specific endopeptidase which are useful for anti-amnestic agent. The disclosed pyrrolidine derivatives as well as their acid addition salts can be administered orally or parenterally in the form of conventional pharmaceutical preparations. For instance, they can be administered orally in the form of conventional solid pharmaceutical preparations such as tablets, capsules, syrups and suspensions. Alternatively, they can be administered parenterally by injection in the form of conventional liquid pharmaceutical preparations such as solutions, emulsions, suspensions, etc. Also, they may be directly applied to rectum in the form of suppository. Further, the preparations may contain physiologically acceptable carriers, excipients, activators, binding agents, stabilizers, etc. In the case of injections, physiologically acceptable buffers, solubilizing agents or isotonic agents may be incorporated therein. Methods of production are also disclosed.

Inventors

  • 👤 Katsumi Tamoto
  • 👤 Renzo Ohuchi
  • 👤 Keiichi Ono

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-09 15:19
CPC Classifications
C; C07; C07D; C07D207/00; C07D207/02; C07D207/04; C07D207/08

Claims Analysis

Total Claims: 9
Claim 1
Independent Claim 122 words
A compound of the formula: ##STR60## wherein R 1 is ##STR61## R 3 , R 4 and R 5 are each independently hydrogen, hydroxy, halogen, C 1-4 alkyl, C 1-4 alkoxy, phenyl unsubstituted or substituted with at least one substituent selected from the group of consisting of halogen, C 1-4 alkyl and C 1-4 alkoxy, ##STR62## wherein R 17 is C 1-4 alkyl; R 18 and R 19 are each independently C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; R 9 is hydrogen, C 1-4 alkyl or phenyl; R 10 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy or halogen; m is an integer of 0 to 3 and R 11 is hydrogen, C 1-4 alkyl, phenyl or ##STR63##
Claim 2
Dependent Claim 122 words
A compound of the formula: ##STR60## wherein R 1 is ##STR61## R 3 , R 4 and R 5 are each independently hydrogen, hydroxy, halogen, C 1-4 alkyl, C 1-4 alkoxy, phenyl unsubstituted or substituted with at least one substituent selected from the group of consisting of halogen, C 1-4 alkyl and C 1-4 alkoxy, ##STR62## wherein R 17 is C 1-4 alkyl; R 18 and R 19 are each independently C 1-4 alkyl; R 6 is hydrogen or C 1-4 alkyl; R 9 is hydrogen, C 1-4 alkyl or phenyl; R 10 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy or halogen; m is an integer of 0 to 3 and R 11 is hydrogen, C 1-4 alkyl, phenyl or ##STR63##
Claim 3
Dependent Claim 56 words
The compound according to claim 1, wherein R 3 , R 4 and R 5 are each independently hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy, halogen or phenyl; R 10 is hydrogen, halogen, C 1 -C 4 alkyl or C 1 -C 4 alkoxy; R 11 is C 1 -C 4 alkyl.
Claim 4
Dependent Claim 31 words
The compound according to claim 2, wherein R 1 is ##STR64## R 3 , R 4 and R 5 are each independently hydrogen, C 1-4 alkyl, C 1-4 alkoxy or halogen.
Claim 5
Dependent Claim 13 words
The compound according to claim 3, wherein R 1 R 1 is ##STR65##
Claim 6
Dependent Claim 37 words
The compound according to claim 1, wherein R 1 is ##STR66## wherein R 3 , R 4 , and R 5 are each independently hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy or halogen.
Claim 7
Dependent Claim 37 words
The compound according to claim 1, wherein R 1 is ##STR67## wherein R 3 , R 4 , and R 5 are each independently hydrogen, C 1 -C 4 alkyl, C 1 -C 4 alkoxy or halogen.
Claim 8
Dependent Claim 39 words
A method of treating a patient suffering from dementia comprising administering at least one dose to said patient of the compound according to claim 1, at a daily dosage of between 1 mg and 1000 mg/kg of body weight.
Claim 9
Dependent Claim 25 words
A therapeutic composition for the treatment of dementia comprising an anti-amnestic effective amount of a compound according to claim 1 and a therapeutically acceptable carrier.

References Cited (Backward Citations)

EP0010347A1 Cited
JPS60172929A Cited
EP0154353A2 Cited
EP0172458A2 Cited
JPS61183297A Cited
EP0201742A2 Cited
EP0201741A2 Cited
EP0201743A2 Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1992-11-13 1993-05-15 1993-11-14 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1996-11-13 1997-05-15 1997-11-14 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 2000-11-13 2001-05-15 2001-11-14 $7700.00 Window Closed / Lapsed

Assigned Categories & Tags

No categories assigned to this patent yet.

Assign Category Tag