US5064814A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Anti-thrombotic peptide and pseudopeptide derivatives
Assignee: Aventis Pharmaceuticals Inc
•
Filing: 1990-04-05
•
Granted: 1991-11-12
•
Expires: 2010-04-05
Abstract
Abstract Disclosed are novel peptide and pseudopeptide derivatives and phrmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.
Inventors
- 👤 Scott I. Klein
- 👤 Bruce F. Molino
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-02 06:17
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/02; C07K5/0205; C07K5/0202; A; A61; A61K; A61K38/00
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
81 words
A compound of the formula ##STR9## wherein: X is H, amidino or ##STR10## where R 1 is C 1-10 alkyl, aryl or aralkyl; Y is OR 2 , ##STR11## or a naturally occurring L-amino acid, bonded to the carbon atom at the α-amino position; R 2 and R 3 are independently: H, C 1-10 alkyl, aryl, aralkyl or allyl; m is 0 or 1; n is 4; and p is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
81 words
A compound of the formula ##STR9## wherein: X is H, amidino or ##STR10## where R 1 is C 1-10 alkyl, aryl or aralkyl; Y is OR 2 , ##STR11## or a naturally occurring L-amino acid, bonded to the carbon atom at the α-amino position; R 2 and R 3 are independently: H, C 1-10 alkyl, aryl, aralkyl or allyl; m is 0 or 1; n is 4; and p is 0, 1, 2 or 3; or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
40 words
A compound of claim 1 wherein aid naturally occurring L-amino acid is selected from the group consisting of: Val, Ser, Phe, Gly, Leu, Ile, Ala, Tyr, Trp, Thr, Pro, Arg, Asn, Asp, Cys, Glu, His, Lys, Met, Asp and Gln.
Claim 4
Dependent Claim
32 words
A pharmaceutical composition for the prophylaxis or inhibition of abnormal thrombus formation in a mammal comprising a pharmaceutically acceptable carrier and a pharmaceutically effective antithrombotic amount of a compound of claim 1.
Claim 5
Dependent Claim
1 words
N-[2(S)-1-(piperidin-4-yl-carbonyl)azetidin-2-yl-carbonyl]-L-aspartyl-L-valine.
Claim 6
Dependent Claim
1 words
N-[2(S)-1-(piperidin-4-yl-carbonyl)azetidin-2-yl-carbonyl]-L-aspartyl-L-valine.
Claim 7
Dependent Claim
1 words
N-[2(S)-10(1-amidinopiperidin-4-yl-carbonyl)azetidin-2-yl-carbonyl]-L-aspartyl-L-valine.
Claim 8
Dependent Claim
1 words
N-[2(S)-10(1-amidinopiperidin-4-yl-carbonyl)azetidin-2-yl-carbonyl]-L-aspartyl-L-valine.
Claim 9
Dependent Claim
1 words
N-[2(S)-1-(piperidin-3-yl-carbonyl)azetidin-2-yl-carbonyl]-L-aspartyl-L-valine.
Claim 10
Dependent Claim
1 words
N-[2(S)-1-(piperidin-3-yl-carbonyl)azetidin-2-yl-carbonyl]-L-aspartyl-L-valine.
Claim 11
Dependent Claim
1 words
N-[1-(1-amidinopiperidin-3-yl-carbonyl)azetidin-2-yl-carbonyl]-2-aspartyl-L-valine.
Claim 12
Dependent Claim
1 words
N-[1-(1-amidinopiperidin-3-yl-carbonyl)azetidin-2-yl-carbonyl]-2-aspartyl-L-valine.
References Cited (Backward Citations)
US3821188A
Cited
GB2091270A
Cited
US4683291A
Cited
US4683291B1
Cited
EP0255206A2
Cited
EP0317278A2
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1994-11-11 | 1995-05-13 | 1995-11-12 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1998-11-11 | 1999-05-13 | 1999-11-12 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2002-11-11 | 2003-05-13 | 2003-11-12 | $7700.00 | Window Closed / Lapsed |