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US 4,064,236 AGranted
Peptide carbazates and pharmaceutical composition
AssigneeMerck & Co., Inc.
InventorsConrad P. Dorn, Shu S. Yang
Life of this patent
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Abstract
Certain novel peptide carbazates, their preparation, pharmaceutical compositions and novel methods of treating pancreatitis.
Claims4
A compound of the formula:
- ##STR5## wherein B is C.sub.1-5 alkanoyl, t-butoxycarbonyl or carbobenzyloxy,
- P.sub.4 is alanyl or prolyl,
- P.sub.3 is alanyl,
- P.sub.2 is prolyl or leucyl,
- R.sub.1 is C.sub.1-5 alkyl,
- R.sub.2 is methyl, benzyl or 4-aminobutyl, and
- R.sub.3 is hydroxy, C.sub.1-5 Alkoxy, amino, N-C.sub.1-5 alkylamino, N,N-di-(C.sub.1-5 alkyl)amino, N-benzylamino, N-phenylamino, hydrazino, methylhydrazino, ethylhydrazino, phenylhydrazino, benzylhydrazino, benzyloxy, or p-iodobenzyloxy or ##STR6## wherein R.sub.4 is methyl or benzyl, and
- R.sub.5 is hydroxy, C.sub.1-5 alkoxy, amino, N-C.sub.1-5 alkylamino, N,N-di-(C.sub.1-5 alkyl)amino, N-benzylamino, N-phenylamino, hydrazino, benzyloxy, or p-iodobenzyloxy and
- Z is -NH- or --0--.
6 more elements
The compound of claim 3 wherein P.sub.4 is alanyl. 5. The compound of
- claim 3 wherein P.sub.4 is prolyl. 6. Acetylprolylalanylprolyl-2-azaalanyl-di-lacthydrazide according to
- claim 5. 7. Acetylprolylalanylprolyl-2-azaalanyl-di-lactamide according to
- claim 5. 8. Acetylalanylalanylprolyl-2-azaalanyl-di-lactamide according to
- 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.sub.1-5 alkanoyl, t-butoxycarbonyl or carbobenzyloxy,
- P.sub.4 is alanyl or prolyl,
- P.sub.3 is alanyl,
- P.sub.2 is prolyl or leucyl,
- R.sub.1 is C.sub.1-5 alkyl,
- R.sub.2 is methyl, benzyl or 4-aminobutyl, and
- R.sub.3 is hydroxy, C.sub.1-5 alkoxy, amino, N-C.sub.1-5 alkylamino, N-benzylamino, N-phenylamino, hydrazino, methylhydrazino, ethylhydrazino, phenylhydrazino, benzylhydrazino, benzyloxy, or ##STR8## wherein R.sub.4 is methyl or benzyl, and
- R.sub.5 is hydroxy, C.sub.1-5 alkoxy, amino, N-C.sub.1-5 alkylamino, N-benzylamino, N-phenylamino, hydrazino, benzyloxy, or p-iodobenzyloxy and
- Z is --NH--or --0--.
10 more elements
Dependencies are inferred from the claim text.