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US4713369A
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Oligopeptidylargininol derivatives and their homologs, a process for their preparation, their use and agents containing them
Assignee: Siemens Healthcare Diagnostics GmbH Germany
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Filing: 1986-02-14
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Granted: 1987-12-15
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Expires: 2006-02-14
Abstract
Abstract The invention relates to new peptidylargininol derivatives and their homologs of the general formula X-D-Phe-Pro-A-Y.(HB)n, X being a hydrogen atom or a known protective group customary in peptide chemistry, D-Phe being D-phenylalanine, Pro being L-proline, A being a omega -guanidiano- beta -aminoalkanol residue of the formula -NHCH (CH2)mNHC(NH)NH2CH2O, with m being 2 to 5, preferably an argininol residue or a homoargininol residue, Y being a hydrogen atom or an ester-forming group, B being an acid residue, and n being 0, 1 or 2, and to a process for the preparation of these compounds, to pharmaceutical agents containing these compounds, and to the use of these agents as thrombin inhibitors.
Inventors
- 👤 Werner Stuber
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 20:04
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06078; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 11
Claim 1
Independent Claim
150 words
An oligopeptidylargininol derivative and its homologs of the formula X-D-Phe-Pro-A-Y.(HB).sub.n being a hydrogen atom or a known protective group customary in peptide chemistry, D-Phe being D-phenylalanine, Pro being L-proline, A being an argininol residue or homologs of argininol of the general formula --NHCH [(CH 2 ) m NHC(NH)NH 2 ]CH 2 --O-- m being 2 to 5; Y being a hydrogen atom, a radical of the following structure: Y=--OC--R, with R=H, an aliphatic radical having up to 4 carbon atoms, or ##STR4## R' being H, CH 3 , OCH 3 or NO 2 , and n being 0, 1 or 2, or a radical of the following structure: Y=--SO 2 --R with R=OH, an aromatic or araliphatic radical of the structure ##STR5## R' being H, CH 3 or OCH 3 , and n being 0, 1 or 2, B being an acid residue, and n being 0, 1 or 2.
Claim 2
Dependent Claim
150 words
An oligopeptidylargininol derivative and its homologs of the formula X-D-Phe-Pro-A-Y.(HB).sub.n being a hydrogen atom or a known protective group customary in peptide chemistry, D-Phe being D-phenylalanine, Pro being L-proline, A being an argininol residue or homologs of argininol of the general formula --NHCH [(CH 2 ) m NHC(NH)NH 2 ]CH 2 --O-- m being 2 to 5; Y being a hydrogen atom, a radical of the following structure: Y=--OC--R, with R=H, an aliphatic radical having up to 4 carbon atoms, or ##STR4## R' being H, CH 3 , OCH 3 or NO 2 , and n being 0, 1 or 2, or a radical of the following structure: Y=--SO 2 --R with R=OH, an aromatic or araliphatic radical of the structure ##STR5## R' being H, CH 3 or OCH 3 , and n being 0, 1 or 2, B being an acid residue, and n being 0, 1 or 2.
Claim 3
Dependent Claim
13 words
A compound as claimed in claim 1 wherein m is 3 or 4.
Claim 4
Dependent Claim
15 words
A compound as claimed in claim 1, wherein A is an L-argininol or L-homoargininol residue.
Claim 5
Dependent Claim
6 words
D-phenylalanyl-L-prolyl-L-arininol and its physiologically tolerated salts.
Claim 6
Dependent Claim
6 words
D-phenylalanyl-L-prolyl-L-arininol and its physiologically tolerated salts.
Claim 7
Dependent Claim
35 words
A pharmaceutical agent which contains a pharmaceutically effective amount for inhibition of thrombin or as an anticoaqulent of a substance as claimed in claim 1, or its physiologically tolerated salt, and a physiologically acceptable vehicle.
Claim 8
Dependent Claim
24 words
A pharmaceutical agent containing a pharmaceutically effective amount for inhibition of thrombin or as an anticoagulant of D-phenylalanyl-L-prolyl-L- arginol or its physiologically tolerated salts.
Claim 9
Dependent Claim
24 words
A pharmaceutical agent containing a pharmaceutically effective amount for inhibition of thrombin or as an anticoagulant of D-phenylalanyl-L-prolyl-L- arginol or its physiologically tolerated salts.
Claim 10
Dependent Claim
38 words
A method for the treatment of a mammal in need of inhibitory action on thrombin which comprises administering to said mammal a pharmaceutically effective amount of a compound as claimed in claim 1 to inhibit formation of thrombin.
Claim 11
Dependent Claim
34 words
A method for the treatment of a mammal in need of an anticoagulent which comprises administering to said mammal a pharmaceutically effective amount of a compound as claimed in claim 1 to inhibit coagulation.
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) | 1990-12-14 | 1991-06-15 | 1991-12-15 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1994-12-14 | 1995-06-15 | 1995-12-15 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1998-12-14 | 1999-06-15 | 1999-12-15 | $7700.00 | Window Closed / Lapsed |