US4285935A
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US
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Dehydropeptide compounds, their production and their medical use
Assignee: Bayer AG
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Filing: 1980-01-23
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Granted: 1981-08-25
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Expires: 2000-01-23
Abstract
Abstract This invention relates to dehydropeptides containing a tryptophan moiety useful as tumour-resolving and/or histolytic medicaments. Also included in the invention are methods for the preparation of said dehydropeptides, compositions containing said dehydropeptides and methods for the use of said dehydropeptides and dehydropeptide compositions.
Inventors
- 👤 Eugen Etschenberg
- 👤 Haireddin Jacobi
- 👤 Wolfgang Opitz
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 08:13
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/06; C07K5/06008; C07K5/06078; A; A61; A61P; A61P43/00; A61P7/00; A61P7/02; A61K; A61K38/00
Claims Analysis
Total Claims: 16
Claim 1
Independent Claim
133 words
A compound which is a dehydropeptide of the formula ##STR6## or a salt thereof, in which R 1 denotes a hydrogen atom, an optionally substituted alkyl, alkenyl, aralkyl, aralkenyl aryl, alkoxy group or a heterocyclic ring, R 2 denotes a phenyl radical which is optionally substituted by alkyl, aryl, alkoxy, hydroxyl, nitro, amino, acylamino or halogen, R 3 and R 4 both denote a hydrogen atom, or together denote an additional bond between the two carbon atoms, R 5 denotes a hydroxyl group or an optionally substituted alkoxy, aralkoxy or amino group and n is 1 or 0, and in which, when R 3 and R 4 both denote a hydrogen atom, the centre of asymmetry C* at the substituent R 3 is in the racemate form, or in the D-form or L-form.
Claim 2
Dependent Claim
133 words
A compound which is a dehydropeptide of the formula ##STR6## or a salt thereof, in which R 1 denotes a hydrogen atom, an optionally substituted alkyl, alkenyl, aralkyl, aralkenyl aryl, alkoxy group or a heterocyclic ring, R 2 denotes a phenyl radical which is optionally substituted by alkyl, aryl, alkoxy, hydroxyl, nitro, amino, acylamino or halogen, R 3 and R 4 both denote a hydrogen atom, or together denote an additional bond between the two carbon atoms, R 5 denotes a hydroxyl group or an optionally substituted alkoxy, aralkoxy or amino group and n is 1 or 0, and in which, when R 3 and R 4 both denote a hydrogen atom, the centre of asymmetry C* at the substituent R 3 is in the racemate form, or in the D-form or L-form.
Claim 3
Dependent Claim
96 words
A compound according to claim 1, in which R 1 denotes a hydrogen atom, an alkyl group with 1 to 4 carbon atoms or a phenyl or benzyl radical, R 2 denotes a phenyl radical which is optionally substituted by alkyl with 1 or 2 carbon atoms or halogen, R 3 and R 4 both denote a hydrogen atom or together represent an additional bond between the two carbon atoms, R 5 denotes a hydroxyl group, an alkoxy group with 1 to 4 carbon atoms, a benzyloxy or amino group and n is 1 or 0.
Claim 4
Dependent Claim
51 words
A compound according to claim 1, in which R 1 denotes a methyl group, R 2 denotes a phenyl radical, R 3 and R 4 both denote a hydrogen atom or together represent an additional bond between the two carbon atoms, R 5 denotes a hydroxyl group and n is 1.
Claim 5
Dependent Claim
28 words
A compound according to claim 3, in which R 3 and R 4 both denote a hydrogen atom, in their racemic form and in their optically active form.
Claim 6
Dependent Claim
28 words
A pharmaceutical composition containing as an active ingredient 1 to 90% of a compound according to claim 1 in admixture with a solid, liquid or liquefied gaseous diluent.
Claim 7
Dependent Claim
17 words
A pharmaceutical composition of claim 5 in the form of a sterile or physiologically isotonic aqueous solution.
Claim 8
Dependent Claim
20 words
A composition according to claim 5 or 6 containing from 5 to 50% by weight of the said active ingredient.
Claim 9
Dependent Claim
18 words
A medicament in dosage unit form comprising a compound according to claim 1 in an inert pharmaceutical carrier.
Claim 10
Dependent Claim
16 words
A medicament of claim 8 in the form of tablets, pills, dragees, capsules, ampoules or suppositories.
Claim 11
Dependent Claim
42 words
A method of treating tissues to provide histolytic effect which comprises administering to warm-blooded animals a histolytically effective amount of an active compound according to claim 1 either alone or in admixture with a diluent or in the form of a medicament.
Claim 12
Dependent Claim
27 words
A method according to claim 10 in which the active compound is administered in an amount of 2 to 40 mg per kg body weight per day.
Claim 13
Dependent Claim
16 words
A method according to claim 10 or 11 in which the active compound is administered parenterally.
Claim 14
Dependent Claim
10 words
A compound according to claim 1 which is N-Acetyl dehydrophenylalanyl-L-tryptophan.
Claim 15
Dependent Claim
10 words
A compound according to claim 1 which is N-Acetyl dehydrophenylalanyl-D-tryptophan.
Claim 16
Dependent Claim
10 words
A compound according to claim 1 which is N-Acetyl dehydrophenylalanyl-dehydrotryptophan.
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) | 1984-08-24 | 1985-02-23 | 1985-08-25 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1988-08-24 | 1989-02-23 | 1989-08-25 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1992-08-24 | 1993-02-23 | 1993-08-25 | $7700.00 | Window Closed / Lapsed |