US4595674A
Expired / Lapsed
US
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Homologues of aprotinin with, in place of lysine, other aminoacids in position 15, process for their preparation and their use as medicaments
Assignee: Bayer AG
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Filing: 1985-03-13
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Granted: 1986-06-17
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Expires: 2005-03-13
Abstract
Abstract The invention relates to homologs of aprotinin with, in place of lysine, other amino acid moieties in position 15, methods for their preparation and their use as proteinase inhibitors.
Inventors
- 👤 Harald Tschesche
- 👤 Herbert Wenzel
- 👤 Rainer Schmuck
- 👤 Eugen Schnabel
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-28 03:10
CPC Classifications
C; C07; C07K; C07K1/00; C07K1/12; C07K14/00; C07K14/81; C07K14/8107; C07K14/811; C07K14/8114; C07K14/8117; A; A61; A61K; A61K38/00; Y; Y10; Y10S; Y10S930/00; Y10S930/01; Y10S930/26
Claims Analysis
Total Claims: 22
Claim 1
Independent Claim
45 words
A homolog of aprotitin in which the lysine residue in position 15 in the active centre of the aprotinin inhibitor has been replaced by one of the residues of the aminoacids glycine, L-alanine, L-valine, L-leucine, L-isoleucine, L-methionine, L-arginine, L-α-aminobutyric acid, L-norvaline, L-norleucine, dehydroalanine and L-homoserine.
Claim 2
Dependent Claim
45 words
A homolog of aprotitin in which the lysine residue in position 15 in the active centre of the aprotinin inhibitor has been replaced by one of the residues of the aminoacids glycine, L-alanine, L-valine, L-leucine, L-isoleucine, L-methionine, L-arginine, L-α-aminobutyric acid, L-norvaline, L-norleucine, dehydroalanine and L-homoserine.
Claim 3
Dependent Claim
78 words
A homolog of aprotinin, in which only the lysine residue in position 15 in the active centre of the aprotinin inhibitor has been replaced by one of the residues of the aminoacids glycine, L-alanine, L-isoleucine, L-valine, L-leucine, L-arginine, L-α-aminobutyric acid, L-norvaline, L-norleucine, dehydroalanine and L-homoserine or alkyl esters of these homologs in which all or some of their additional carboxyl groups in the side-chains of the acidic aminoacids and in the terminal position have, where appropriate, been esterified.
Claim 4
Dependent Claim
78 words
A homolog of aprotinin, in which only the lysine residue in position 15 in the active centre of the aprotinin inhibitor has been replaced by one of the residues of the aminoacids glycine, L-alanine, L-isoleucine, L-valine, L-leucine, L-arginine, L-α-aminobutyric acid, L-norvaline, L-norleucine, dehydroalanine and L-homoserine or alkyl esters of these homologs in which all or some of their additional carboxyl groups in the side-chains of the acidic aminoacids and in the terminal position have, where appropriate, been esterified.
Claim 5
Dependent Claim
33 words
A homolog of aprotinin according to claim 1 or 2, in which the lysine residue in position 15 in the active centre of the inhibitor has been replaced by the residue of L-valine.
Claim 6
Dependent Claim
33 words
A homolog of aprotinin according to claim 1 or 2, in which the lysine residue in position 15 in the active centre of the inhibitor has been replaced by the residue of L-leucine.
Claim 7
Dependent Claim
33 words
A homolog of aprotinin according to claim 1 or 2, in which the lysine residue in position 15 in the active centre of the inhibitor has been replaced by the residue of L-norleucine.
Claim 8
Dependent Claim
33 words
A homolog of aprotinin according to claim 1 or 2, in which the lysine residue in position 15 in the active centre of the inhibitor has been replaced by the residue of L-norvaline.
Claim 9
Dependent Claim
34 words
A homolog of aprotinin according to claim 1 or 2, in which the lysine residue in position 15 in the active centre of the inhibitor has been replaced by the resiue of L-α-aminobutyric acid.
Claim 10
Dependent Claim
69 words
A derivative of aprotinin in which the peptide bond between the lysine-15 residue and the alanine-16 residue is open and in which only the carboxyl group on the lysine 15 is free, all other carboxyl groups in the side-chains of the aspartic acid residues (positions 3 and 50) and of the glutamic acid residue (positions 7 and 49) and of the C-terminal alanine (position 58) bearing alkyl ester groups.
Claim 11
Dependent Claim
69 words
A derivative of aprotinin in which the peptide bond between the lysine-15 residue and the alanine-16 residue is open and in which only the carboxyl group on the lysine 15 is free, all other carboxyl groups in the side-chains of the aspartic acid residues (positions 3 and 50) and of the glutamic acid residue (positions 7 and 49) and of the C-terminal alanine (position 58) bearing alkyl ester groups.
Claim 12
Dependent Claim
14 words
A derivative according to claim 8, in which the ester groups are methyl esters.
Claim 13
Dependent Claim
53 words
A derivative of aprotinin having a peptide bond on alanine-16 cleaved, in which the lysine-15 residue is missing, and the carboxyl groups in the side-chains of the aspartate residues--3 and 50--and the glutamate residues--7 and 49--and the C-terminal alanine--58--bear alkyl esters, and only the carboxyl group on the half-cystine residue 14 is non-esterified.
Claim 14
Dependent Claim
53 words
A derivative of aprotinin having a peptide bond on alanine-16 cleaved, in which the lysine-15 residue is missing, and the carboxyl groups in the side-chains of the aspartate residues--3 and 50--and the glutamate residues--7 and 49--and the C-terminal alanine--58--bear alkyl esters, and only the carboxyl group on the half-cystine residue 14 is non-esterified.
Claim 15
Dependent Claim
16 words
A derivative according to claim 10, in which the alkyl ester group is a methyl group.
Claim 16
Dependent Claim
26 words
A pharmaceutical proteinase inhibiting composition containing as an active ingredient a proteinase inhibiting amount of a compound of claim 1 together with an inert pharmaceutical carrier.
Claim 17
Dependent Claim
19 words
A pharmaceutical proteinase inhibiting composition of claim 12 in the form of a sterile or physiologically isotonic aqueous solution.
Claim 18
Dependent Claim
25 words
A proteinase inhibiting medicament in dosage unit form comprising an effective proteinase inhibiting amount of a compound of claim 1 and an inert pharmaceutical carrier.
Claim 19
Dependent Claim
18 words
A proteinase inhibiting medicament of claim 14 in the form of tablets, pills, dragees, capsules, ampoules or suppositories.
Claim 20
Dependent Claim
31 words
A method of providing proteinase inhibition which comprises administering to a warm-blooded animal, an effective proteinase inhibiting amount of a compound of claim 1 in admixture with an inert pharmaceutical carrier.
Claim 21
Dependent Claim
26 words
A method according to claim 16 wherein the active compound is administered in an amount of 0.1 to 20 mg per kg body weight per day.
Claim 22
Dependent Claim
26 words
A method according to claim 16 wherein the active compound is administered in an amount of 1 to 10 mg per kg body weight per day.
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) | 1989-06-16 | 1989-12-16 | 1990-06-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1993-06-16 | 1993-12-16 | 1994-06-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1997-06-16 | 1997-12-16 | 1998-06-17 | $7700.00 | Window Closed / Lapsed |