US4337244A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Enzyme derivatives for use in the treatment of venous thrombosis
Assignee: Roberts Laboratories Inc
•
Filing: 1980-12-16
•
Granted: 1982-06-29
•
Expires: 2000-12-16
Abstract
Abstract Prophylactic or therapeutic method for the treatment of venous thrombosis by administering preferably intravenously to a human in need thereof a pharmaceutically acceptable carrier and an in vivo fibrinolytic enzyme in which the catalytic site essential for fibrinolytic activity is blocked by a group, such as an acyl group, removable by hydrolysis at a rate such that the pseudo-first order rate constant for hydrolysis is in the range of 10 -6 sec -1 to 10 -3 sec -1 in isotonic aqueous media at pH 7.4 at 37° C.
Inventors
- 👤 Richard A. G. Smith
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 19:08
CPC Classifications
C; C12; C12N; C12N9/00; C12N9/14; C12N9/48; C12N9/50; C12N9/64; C12N9/6421; C12N9/6424; C12N9/6435; A; A61; A61P; A61P7/00; A61P7/02; C07; C07D; C07D307/00; C07D307/02; C07D307/34; C07D307/38; C07D307/54; C07K; C07K14/00; C07K14/195; C07K14/315; C07K14/3153; C12N9/6456; C12N9/6462; C12N9/96; C12Y; C12Y304/00; C12Y304/21; C12Y304/21007; C12Y304/21073; A61K; A61K38/00
Claims Analysis
Total Claims: 14
Claim 1
Independent Claim
83 words
A prophylactic or therapeutic method for the treatment of venous thrombosis which comprises administering to a human in need thereof a pharmaceutically acceptable carrier together with an in vivo fibrinolytic enzyme in which the catalytic site essential for fibrinolytic activity is blocked by a group removable by hydrolysis at a rate such that the pseudo-first order rate constant for hydrolysis is in the range 10 -6 sec -1 to 10 -3 sec -1 in isotonic aqueous media at pH 7.4 at 37° C.
Claim 2
Dependent Claim
83 words
A prophylactic or therapeutic method for the treatment of venous thrombosis which comprises administering to a human in need thereof a pharmaceutically acceptable carrier together with an in vivo fibrinolytic enzyme in which the catalytic site essential for fibrinolytic activity is blocked by a group removable by hydrolysis at a rate such that the pseudo-first order rate constant for hydrolysis is in the range 10 -6 sec -1 to 10 -3 sec -1 in isotonic aqueous media at pH 7.4 at 37° C.
Claim 3
Dependent Claim
14 words
A method according to claim 1, wherein the administration to the human is intravenous.
Claim 4
Dependent Claim
12 words
A method according to claim 1, wherein the enzyme is human plasmin.
Claim 5
Dependent Claim
14 words
A method according to claim 1, wherein the enzyme is streptokinase/human plasminogen activator complex.
Claim 6
Dependent Claim
20 words
A method according to claim 1, wherein the enzyme is a mixture of human plasmin and streptokinase/human plasminogen activator complex.
Claim 7
Dependent Claim
17 words
A method according to claim 1, wherein the blocking group removable by hydrolysis is an acyl group.
Claim 8
Dependent Claim
18 words
A method according to claim 6, wherein the acyl group is benzoyl, substituted benzoyl, acryloyl or substituted acryloyl.
Claim 9
Dependent Claim
47 words
A method according to claim 6, wherein the acyl group is a benzoyl group or a substituted benzoyl group having one or more meta and/or para substituents wherein the sum of the Hammett σ m and σ p values is in the range of +0.1 to -1.1.
Claim 10
Dependent Claim
30 words
A method according to claim 6, wherein the acyl group is benzoyl, optionally substituted with halogen, C 1-6 alkyl, C 1-6 alkoxy, C 1-6 alkanoyloxy, C 1-6 alkanoylamino or p-guanidino.
Claim 11
Dependent Claim
25 words
A method according to claim 6, wherein the acyl group is acryloyl, optionally substituted with C 1-6 alkyl, furyl, phenyl, or C 1-6 alkyl phenyl.
Claim 12
Dependent Claim
14 words
A method according to claim 1, wherein the blocked enzyme is p-anisoyl human plasmin.
Claim 13
Dependent Claim
17 words
A method according to claim 1, wherein the blocked enzyme is p-anisoyl streptokinase human plasminogen activator complex.
Claim 14
Dependent Claim
24 words
A method according to claim 1, wherein the blocked enzyme is a mixture of p-anisoyl human plasmin and p-anisoyl streptokinase human plasminogen activator complex.
References Cited (Backward Citations)
No citation records indexed.
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1985-06-28 | 1985-12-28 | 1986-06-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1989-06-28 | 1989-12-28 | 1990-06-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1993-06-28 | 1993-12-28 | 1994-06-29 | $7700.00 | Window Closed / Lapsed |