US4064236A
Expired / Lapsed
US
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Peptide carbazates and pharmaceutical composition
Assignee: Merck and Co Inc
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Filing: 1975-12-23
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Granted: 1977-12-20
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Expires: 1995-12-23
Abstract
Abstract Certain novel peptide carbazates, their preparation, pharmaceutical compositions and novel methods of treating pancreatitis.
Inventors
- 👤 Conrad P. Dorn
- 👤 Shu S. Yang
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 10:33
CPC Classifications
C; C07; C07K; C07K5/00; C07K5/04; C07K5/08; C07K5/0821; C07K5/0823; A; A61; A61P; A61P29/00; C07K5/0802; C07K5/0804; C07K5/0806; A61K; A61K38/00
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
105 words
A compound of the formula: ##STR5## wherein B is C 1-5 alkanoyl, t-butoxycarbonyl or carbobenzyloxy, P 4 is alanyl or prolyl, P 3 is alanyl, P 2 is prolyl or leucyl, R 1 is C 1-5 alkyl, R 2 is methyl, benzyl or 4-aminobutyl, and R 3 is hydroxy, C 1-5 Alkoxy, amino, N-C 1-5 alkylamino, N,N-di-(C 1-5 alkyl)amino, N-benzylamino, N-phenylamino, hydrazino, methylhydrazino, ethylhydrazino, phenylhydrazino, benzylhydrazino, benzyloxy, or p-iodobenzyloxy or ##STR6## wherein R 4 is methyl or benzyl, and R 5 is hydroxy, C 1-5 alkoxy, amino, N-C 1-5 alkylamino, N,N-di-(C 1-5 alkyl)amino, N-benzylamino, N-phenylamino, hydrazino, benzyloxy, or p-iodobenzyloxy and Z is -NH- or --0--.
Claim 2
Dependent Claim
105 words
A compound of the formula: ##STR5## wherein B is C 1-5 alkanoyl, t-butoxycarbonyl or carbobenzyloxy, P 4 is alanyl or prolyl, P 3 is alanyl, P 2 is prolyl or leucyl, R 1 is C 1-5 alkyl, R 2 is methyl, benzyl or 4-aminobutyl, and R 3 is hydroxy, C 1-5 Alkoxy, amino, N-C 1-5 alkylamino, N,N-di-(C 1-5 alkyl)amino, N-benzylamino, N-phenylamino, hydrazino, methylhydrazino, ethylhydrazino, phenylhydrazino, benzylhydrazino, benzyloxy, or p-iodobenzyloxy or ##STR6## wherein R 4 is methyl or benzyl, and R 5 is hydroxy, C 1-5 alkoxy, amino, N-C 1-5 alkylamino, N,N-di-(C 1-5 alkyl)amino, N-benzylamino, N-phenylamino, hydrazino, benzyloxy, or p-iodobenzyloxy and Z is -NH- or --0--.
Claim 3
Dependent Claim
40 words
The compound of claim 1 wherein B is C 1-5 alkanoyl, R 1 is methyl or isopropyl, R 2 is methyl or benzyl, and R 3 is C 1-5 alkoxy, benzyloxy, p-iodobenzyloxy, amino, hydrazino, N-phenylamino, N-benzylamino or C 1-5 -alkylamino.
Claim 4
Dependent Claim
33 words
The compound of claim 2 wherein B is acetyl, P 2 is prolyl, R 1 is methyl, R 2 is methyl, and R 3 is benzyloxy, p-iodobenylzoxy, amino, hydrazino, N-phenylamino, N-benzylamino or N-methylamino.
Claim 5
Dependent Claim
14 words
The compound of claim 3 wherein P 4 is alanyl. 5. The compound of
Claim 6
Dependent Claim
11 words
claim 3 wherein P 4 is prolyl. 6. Acetylprolylalanylprolyl-2-azaalanyl-di-lacthydrazide according to
Claim 7
Dependent Claim
6 words
claim 5. 7. Acetylprolylalanylprolyl-2-azaalanyl-di-lactamide according to
Claim 8
Dependent Claim
6 words
claim 5. 8. Acetylalanylalanylprolyl-2-azaalanyl-di-lactamide according to
Claim 9
Dependent Claim
114 words
claim 5. 9. A pharmaceutical composition comprising a non-toxic pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of the formula: ##STR7## wherein B is C 1-5 alkanoyl, t-butoxycarbonyl or carbobenzyloxy, P 4 is alanyl or prolyl, P 3 is alanyl, P 2 is prolyl or leucyl, R 1 is C 1-5 alkyl, R 2 is methyl, benzyl or 4-aminobutyl, and R 3 is hydroxy, C 1-5 alkoxy, amino, N-C 1-5 alkylamino, N-benzylamino, N-phenylamino, hydrazino, methylhydrazino, ethylhydrazino, phenylhydrazino, benzylhydrazino, benzyloxy, or ##STR8## wherein R 4 is methyl or benzyl, and R 5 is hydroxy, C 1-5 alkoxy, amino, N-C 1-5 alkylamino, N-benzylamino, N-phenylamino, hydrazino, benzyloxy, or p-iodobenzyloxy and Z is --NH--or --0--.
References Cited (Backward Citations)
US3888840A
Cited
US3904593A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1980-12-19 | 1981-06-20 | 1981-12-20 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1984-12-19 | 1985-06-20 | 1985-12-20 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1988-12-19 | 1989-06-20 | 1989-12-20 | $7700.00 | Window Closed / Lapsed |