US4829052A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Serine protease inhibitors
Assignee: Monsanto Co
•
Filing: 1987-05-08
•
Granted: 1989-05-09
•
Expires: 2007-05-08
Abstract
Abstract Synthetic polypeptides are disclosed which exhibit potent serine protease inhibition. Methods and compositions useful for treating conditions caused by unwanted serine protease activity are also disclosed.
Inventors
- 👤 George I. Glover
- 👤 Charles A. McWherter
- 👤 Charles S. Schasteen
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 13:54
CPC Classifications
C; C07; C07K; C07K14/00; C07K14/81; C07K14/8107; C07K14/811; A; A61; A61P; A61P11/00; A61P29/00; A61P7/00; A61P7/02; A61K; A61K38/00
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
36 words
A synthetic serine protease inhibitor having the following sequence: ##STR2## which exhibits inhibitory activity towards elastase in which X is selected from the group consisting of isoleucine, norvaline, valine, norleucine, methionine, leucine, alanine, glycine and phenylalanine.
Claim 2
Dependent Claim
36 words
A synthetic serine protease inhibitor having the following sequence: ##STR2## which exhibits inhibitory activity towards elastase in which X is selected from the group consisting of isoleucine, norvaline, valine, norleucine, methionine, leucine, alanine, glycine and phenylalanine.
Claim 3
Dependent Claim
12 words
A serine protease inhibitor of claim 1 in which X is valine.
Claim 4
Dependent Claim
12 words
A serine protease inhibitor of claim 1 in which X is iosleucine.
Claim 5
Dependent Claim
20 words
A serine protease inhibitor of claim 1 exhibiting inhibitory activity toward elastase and cathepsin G in which X is phenylalanine.
Claim 6
Dependent Claim
20 words
A serine protease inhibitor of claim 1 exhibiting inhibitory activity toward elastase and cathepsin G in which X is methionine.
Claim 7
Dependent Claim
1662 words
A serine protease inhibitor selected from the group consisting of R V C P I I L M K C K K D S D C L A E C V C L E H G Y C G, H E E R V
C P I I L M K C K K D S D C L A E C V C L E H G Y C G, R V C P I I L
M E C K K D S D C L A E C V C L E H G Y C G, R V C P I I L M E C K K
D S D C L A E C I C L E H G Y C G, H E E R V C P I I L M E C K K D S D C
L A E C I C L E H G Y C G, M V C P I I L M K C K H D S D C L L D C V
C L E D I G Y C G, M M C P I I L M K C K H D S D C L P G C V C L E H
I E Y C G, R V C P V I L M K C K K D S D C L A E C V C L E H G Y C G,
H E E R V C P V I L M K C K K D S D C L A E C V C L E H G Y C G, R V
C P V I L M E C K K D S D C L A E C V C L E H G Y C G, R V C P V I L
M E C K K D S D C L A E C I C L E H G Y C G, H E E R V C P V I L M E C K
K D S D C L A E C I C L E H G Y C G, M V C P V I L M K C K H D S D C
L L D C V C L E D I G Y C G, M M C P V I L M K C K H D S D C L P G C
V C L E H I E Y C G, R V C P F I L M K C K K D S D C L A E C V C L E
H G Y C G, H E E R V C P F I L M K C K K D S D C L A E C V C L E H G Y C
G, R V C P F I L M E C K K D S D C L A E C V C L E H G Y C G, R V
C P F I L M E C K K D S D C L A E C I C L E H G Y C G, H E E R V C P F I
L M E C K K D S D C L A E C I C L E H G Y C G, M V C P F I L M K C K
H D S D C L L D C V C L E D I G Y C G, M M C P F I L M K C K H D S D
C L P G C V C L E H I E Y C G, R V C P M I L M K C K K D S D C L A E
C V C L E H G Y C G, H E E R V C P M I L M K C K K D S D C L A E C V C L
E H G Y C G, R V C P M I L M E C K K D S D C L A E C V C L E H G Y C
G, R V C P M I L M E C K K D S D C L A E C I C L E H G Y C G, H E E R
V C P M I L M E C K K D S D C L A E C I C L E H G Y C G, M V C P M I
L M K C K H D S D C L L D C V C L E D I G Y C G, M M C P M I L M K C
K H D S D C L P G C V C L E H I E Y C G, R V C P L I L M K C K K D S
D C L A E C V C L E H G Y C G, H E E R V C P L I L M K C K K D S D C L A
E C V C L E H G Y C G, R V C P L I L M E C K K D S D C L A E C V C L
E H G Y C G, R V C P L I L M E C K K D S D C L A E C I C L E H G Y C
G, H E E R V C P L I L M E C K K D S D C L A E C I C L E H G Y C G, M
V C P L I L M K C K H D S D C L L D C V C L E D I G Y C G, M M C P L
I L M K C K H D S D C L P G C V C L E H I E Y C G, R V C P A I L M K
C K K D S D C L A E C V C L E H G Y C G, H E E R V C P A I L M K C K K D
S D C L A E C V C L E H G Y C G, R V C P A I L M E C K K D S D C L A
E C V C L E H G Y C G, R V C P A I L M E C K K D S D C L A E C I C L
E H G Y C G, H E E R V C P A I L M E C K K D S D C L A E C I C L E H G Y
C G, M V C P A I L M K C K H D S D C L L D C V C L E D I G Y C G,
M M C P A I L M K C K H D S D C L P G C V C L E H I E Y C G, R V C P
V I L Nle K C K K D S D C L A E C V C L E H G Y C G, R V C P V S L M
K C K K D S D C L A E C V C L E H G Y C G, R V C P V I L L K C K K D
S D C L A E C V C L E H G T C G, R V C G V I L M K C K K D S D C L A
E C V C L E H G Y C G, R V C Hyp V I L M K C K K D S D C L A E C V C L E H
G Y C G, R V C P V A L M K C K K D S D C L A E C V C L E H G Y C G,
R V C P G I L M K C K K D S D C L A E C V C L E H G Y C G, H E E R V
C P G I L M K C K K D S D C L A E C V C L E H G Y C G, R V C P G I L
M E C K K D S D C L A E C V C L E H G Y C G, R V C P G I L M E C K K
D S D C L A E C I C L E H G Y C G, H E E R V C P G I L M E C K K D S D C
L A E C I C L E H G Y C G, M V C P G I L M K C K H D S D C L L D C V
C L E D I G Y C G, and M M C P G I L M K C K H D S D C L P G C V C L E H I
E Y C G.
Claim 8
Dependent Claim
1662 words
A serine protease inhibitor selected from the group consisting of R V C P I I L M K C K K D S D C L A E C V C L E H G Y C G, H E E R V
C P I I L M K C K K D S D C L A E C V C L E H G Y C G, R V C P I I L
M E C K K D S D C L A E C V C L E H G Y C G, R V C P I I L M E C K K
D S D C L A E C I C L E H G Y C G, H E E R V C P I I L M E C K K D S D C
L A E C I C L E H G Y C G, M V C P I I L M K C K H D S D C L L D C V
C L E D I G Y C G, M M C P I I L M K C K H D S D C L P G C V C L E H
I E Y C G, R V C P V I L M K C K K D S D C L A E C V C L E H G Y C G,
H E E R V C P V I L M K C K K D S D C L A E C V C L E H G Y C G, R V
C P V I L M E C K K D S D C L A E C V C L E H G Y C G, R V C P V I L
M E C K K D S D C L A E C I C L E H G Y C G, H E E R V C P V I L M E C K
K D S D C L A E C I C L E H G Y C G, M V C P V I L M K C K H D S D C
L L D C V C L E D I G Y C G, M M C P V I L M K C K H D S D C L P G C
V C L E H I E Y C G, R V C P F I L M K C K K D S D C L A E C V C L E
H G Y C G, H E E R V C P F I L M K C K K D S D C L A E C V C L E H G Y C
G, R V C P F I L M E C K K D S D C L A E C V C L E H G Y C G, R V
C P F I L M E C K K D S D C L A E C I C L E H G Y C G, H E E R V C P F I
L M E C K K D S D C L A E C I C L E H G Y C G, M V C P F I L M K C K
H D S D C L L D C V C L E D I G Y C G, M M C P F I L M K C K H D S D
C L P G C V C L E H I E Y C G, R V C P M I L M K C K K D S D C L A E
C V C L E H G Y C G, H E E R V C P M I L M K C K K D S D C L A E C V C L
E H G Y C G, R V C P M I L M E C K K D S D C L A E C V C L E H G Y C
G, R V C P M I L M E C K K D S D C L A E C I C L E H G Y C G, H E E R
V C P M I L M E C K K D S D C L A E C I C L E H G Y C G, M V C P M I
L M K C K H D S D C L L D C V C L E D I G Y C G, M M C P M I L M K C
K H D S D C L P G C V C L E H I E Y C G, R V C P L I L M K C K K D S
D C L A E C V C L E H G Y C G, H E E R V C P L I L M K C K K D S D C L A
E C V C L E H G Y C G, R V C P L I L M E C K K D S D C L A E C V C L
E H G Y C G, R V C P L I L M E C K K D S D C L A E C I C L E H G Y C
G, H E E R V C P L I L M E C K K D S D C L A E C I C L E H G Y C G, M
V C P L I L M K C K H D S D C L L D C V C L E D I G Y C G, M M C P L
I L M K C K H D S D C L P G C V C L E H I E Y C G, R V C P A I L M K
C K K D S D C L A E C V C L E H G Y C G, H E E R V C P A I L M K C K K D
S D C L A E C V C L E H G Y C G, R V C P A I L M E C K K D S D C L A
E C V C L E H G Y C G, R V C P A I L M E C K K D S D C L A E C I C L
E H G Y C G, H E E R V C P A I L M E C K K D S D C L A E C I C L E H G Y
C G, M V C P A I L M K C K H D S D C L L D C V C L E D I G Y C G,
M M C P A I L M K C K H D S D C L P G C V C L E H I E Y C G, R V C P
V I L Nle K C K K D S D C L A E C V C L E H G Y C G, R V C P V S L M
K C K K D S D C L A E C V C L E H G Y C G, R V C P V I L L K C K K D
S D C L A E C V C L E H G T C G, R V C G V I L M K C K K D S D C L A
E C V C L E H G Y C G, R V C Hyp V I L M K C K K D S D C L A E C V C L E H
G Y C G, R V C P V A L M K C K K D S D C L A E C V C L E H G Y C G,
R V C P G I L M K C K K D S D C L A E C V C L E H G Y C G, H E E R V
C P G I L M K C K K D S D C L A E C V C L E H G Y C G, R V C P G I L
M E C K K D S D C L A E C V C L E H G Y C G, R V C P G I L M E C K K
D S D C L A E C I C L E H G Y C G, H E E R V C P G I L M E C K K D S D C
L A E C I C L E H G Y C G, M V C P G I L M K C K H D S D C L L D C V
C L E D I G Y C G, and M M C P G I L M K C K H D S D C L P G C V C L E H I
E Y C G.
Claim 9
Dependent Claim
37 words
A pharmaceutical composition for inhibiting a target serine protease containing an effective amount of an inhibitor of claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.
Claim 10
Dependent Claim
10 words
The composition of claim 7 in which X is valine.
Claim 11
Dependent Claim
10 words
The composition of claim 7 in which X is isoleucine.
Claim 12
Dependent Claim
10 words
The composition of claim 7 in which X is phenylalanine.
Claim 13
Dependent Claim
10 words
The composition of claim 7 in which X is methionine.
Claim 14
Dependent Claim
32 words
A method for treating an individual having a physiological condition caused by unwanted serine protease activity which comprises administering to the individual a therapeutically effective amount of an inhibitor of claim 1.
Claim 15
Dependent Claim
10 words
The method of claim 12 in which X is valine.
Claim 16
Dependent Claim
9 words
The method claim 12 in which X is isoleucine.
Claim 17
Dependent Claim
9 words
The method of claim 12 in which is phenylalanine.
Claim 18
Dependent Claim
10 words
The method of claim 12 in which X is methionine.
Claim 19
Dependent Claim
30 words
A pharmaceutical composition for inhibiting a target serine protease containing an effecting amount of an inhibitor of claim 6 or a pharmaceutically acceptable salt thereof and a pharmaceutically carrier therefor.
Claim 20
Dependent Claim
32 words
A method for treating an individual having a physiological condition caused by unwanted serin protease activity which comprises administering to the individual a therapeutically effective amount of an ihibitor of claim 6.
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) | 1992-05-08 | 1992-11-07 | 1993-05-09 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1996-05-08 | 1996-11-07 | 1997-05-09 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2000-05-08 | 2000-11-07 | 2001-05-09 | $7700.00 | Window Closed / Lapsed |