Rotta Research Laboratorium

Rotta Research Laborarorium S.p.a.

Rolando Chiste

Francesco Makovec

Luigi A Rovati

Walter Peris

Angelo Luigi Rovati

There are described optically active derivatives of (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorophenyl and 3,4-dimethylphenyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.

Optically-active derivatives of (R) 5-pentylamino-5-oxopentanoic acid

There are described optically active derivatives (R) 5-pentylamino-5-oxopentanoic acid and their pharmaceutically acceptable salts, having antagonistic activity towards cholecystokinin, and with the formula: ##STR1## in which R.sub.1 is selected from the groups 2-naphthyl, 3,4-dichlorobenzoyl and 3,4-dimethylbenzoyl and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 carbon atoms, and in which the substituents on the central chiral group (marked with an asterisk in Formula (I)), have the R (rectus) conformation.

New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl. The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

Derivatives of 5-pentylamino-5-oxopentanoic and

New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutanoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl. The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatisis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

N-acylated derivatives of L-tryptophan of general formula (I), ##STR1## in which R is selected from the group consisting of: (a) a phenyl group, mono-substituted or di-substituted in the meta and para positions with halogens, linear or branched alkyl groups containing from 1 to 9 carbon atoms, the cyano group or the trifluoromethyl group, (b) a benzyloxy group, mono-substituted or di-substituted in the meta and para position with substituents selected from those indicated at (a), and (c) a benzydryloxy group. The derivatives are used in therapy, particularly for human pain relief, in the treatment of pathological conditions of the central nervous system and of pathological intestinal conditions.

Pharmaceutical use of derivatives of tryptophan

New original derivatives are described of 5-pentylamino-5-oxopentanoic and 4-pentylamino-4-oxobutasnoic acids having the formula: ##STR1## in which n is 1 or 2, R.sub.1 is selected from the groups 2-naphthyl, 2 (or 3)-quinolinyl, 2 (or 3)-indolyl, 2 (or 3)-benzofuranyl, 2 (or 3)-benzothiophenyl, and R.sub.2 is a pentyl group or an alkoxyalkyl group with 4 or 5 carbon atoms, preferably pentyl, 2-ethoxyethyl, 3-methoxypropyl or 3-ethoxypropyl. The compounds have a powerful antagonistic activity towards cholecystokinin and are particularly useful in the treatment of illnesses of the digestive system, such as colitis, biliary diskinesia, pancreatitis or in the treatment of disorders of the central nervous system imputable to deficiencies in the physiological neuron levels of cholecystokinin or other related bioactive polypeptides.

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Monza, Italy

Rolando Chiste