N-acylic aminoacid derivatives, method for the production thereof, pharmacological composition and the use in the form anti-allergic, anti-inflammatory and hypolipidemic agents

A pharmaceutical composition comprising an N-acyl derivative of an amino acid of formula I

• wherein n is 2 or 3;
• and
• R1 represents
• or a pharmaceutically acceptable salt thereof
• with proviso that the N-acyl derivative of formula I is not succinyl-L-tryptophane, succinyl-D-tryptophane and succinyl-D,L-tryptophane and a dipotassium salt thereof, Nα-succinyl-L-tryptophane methyl ester, Nα-glutaryl-L-histidine methyl ester, Nα-glutaryl-L-tryptophane methyl ester, Nα-succinyl-L-histidine, Nα-glutaryl-D-triptophane methyl ester, Nα-glutaryl-L-triptophane, Nα-glutaryl-L-histidine, or Nα-glutaryl-L-histidine ethyl ester,
• and a pharmaceutically acceptable additive, wherein the N-acyl derivative or pharmaceutically acceptable salt thereof is present in the composition in an amount effective to possess anti-allergic, anti-anaphylactic, or anti-inflammatory activity.

A medicament comprising an N-acyl derivative of an amino acid of formula I

• wherein n is 2 or 3;
• and
• R1 represents
• or a pharmaceutically acceptable salt thereof
• with proviso that the N-acyl derivative of formula I is not succinyl-L-tryptophane, succinyl-D-tryptophane and succinyl-D,L-tryptophane and a dipotassium salt thereof, Nα-succinyl-L-tryptophane methyl ester, Nα-glutaryl-L-histidine methyl ester, Nα-glutaryl-L-tryptophane methyl ester, Nα-succinyl-L-histidine, Nα-glutaryl-D-triptophane methyl ester, Nα-glutaryl-L-triptophane, Nα-glutaryl-L-histidine, or Nα-glutaryl-L-histidine ethyl ester,
• wherein the N-acyl derivative or pharmaceutically acceptable salt thereof is present in the medicament in an amount effective to possess anti-allergic, anti-anaphylactic, anti-inflammatory activity.

A pharmaceutical composition comprising an N-acyl derivative of an amino acid of formula I

• wherein n is 2 or 3;
• and
• R1 represents
• or a pharmaceutically acceptable salt thereof
• with proviso that the N-acyl derivative of Formula I is not succinyl-L-tryptophane, succinyl-D-tryptophane and succinyl-D,L-tryptophane and a dipotassium salt thereof, Nα-succinyl-L-tryptophane methyl ester, Nα-glutaryl-L-histidine methyl ester, Nα-glutaryl-L-tryptophane methyl ester, Nα-succinyl-L-histidine, Nα-glutaryl-D-triptophane methyl ester, Nα-glutaryl-L-triptophane, Nα-glutaryl-L-histidine, or Nα-glutaryl-L-histidine methyl ester
• and a pharmaceutically acceptable additive wherein the N-acyl derivative or pharmaceutically acceptable salt thereof is present in the composition in an amount effective for lowering antigen-dependent histamine secretion, basophil degranulation and controlling the level of eosinophils, neutrophils and lymphocytes.

A pharmaceutical composition comprising an effective amount of the compound of general formula I

• wherein n is 2 or 3;
• and
• R1 represents
• or a pharmaceutically acceptable salt thereof,
• with proviso that the compound of general formula I is not succinyl-L-tryptophane, succinyl-D-tryptophane and succinyl-D, L-tryptophane and a dipotassium salt thereof, Nα-succinyl-L-tryptophane methyl ester, Nα-glutaryl-L-histidine methyl ester, Nα-glutaryl-L-tryptophane methyl ester, Nα-succinyl-L-histidine, Nα-glutaryl-D-triptophane methyl ester, Nα-glutaryl-L-triptophane, Nα-glutaryl-L-histidine, or Nα-glutaryl-L-histidine ethyl ester,
• and a pharmaceutically acceptable additive, wherein the compound is present in the composition in an amount effective for treating an indication selected from the group consisting of allergic rhinitis, pollinoses, seasonal rhinitis, -year-round rhinitis, allergic pneumonitis, atopic dermatitis, urticaria, allergic (including anaphylactic) reactions to insect stings, allergic reactions to medicaments, cold allergy, and allergic conjunctivitis.

A pharmaceutical composition comprising an N-acyl derivative of an amino acid of general formula I

• wherein n is 2 or 3;
• and
• R1 represents
• or a pharmaceutically acceptable salt thereof,
• with proviso that the N-acyl derivative is not succinyl-L-tryptophane, succinyl-D-tryptophane and succinyl-D,L-tryptophane and a dipotassium salt thereof, Nα-succinyl-L-tryptophane methyl ester, Nα-glutaryl-L-histidine methyl ester, Nα-glutaryl-L-tryptophane methyl ester, Nα-succinyl-L-histidine, Nα-glutaryl-D-triptophane methyl ester, Nα-glutaryl-L-triptophane, Nα-glutaryl-L-histidine ethyl ester, and pharmaceutically acceptable additives, wherein the N-acyl derivative or pharmaceutically acceptable salt thereof is present in the composition in an amount effective to possess hypolipidemic activity.

A medicament comprising an N-acyl derivative of an amino acid of general formula I

• wherein n is 2 or 3;
• and
• R1 represents
• or a pharmaceutically acceptable salt thereof,
• with proviso that the compound of general formula I is not succinyl-L-tryptophane, succinyl-D-tryptophane and succinyl-D,L-tryptophane and a dipotassium salt thereof, Nα-succinyl-L-tryptophane methyl ester, Nα-glutaryl-L-histidine methyl ester, Nα-glutaryl-L-tryptophane methyl ester, Nα-succinyl-L-histidine, Nα-glutaryl-D-triptophane methyl ester, Nα-glutaryl-L-triptophane, Nα-glutaryl-L-histidine ethyl ester, wherein the N-acyl derivative or pharmaceutically acceptable salt thereof is present in the medicament in an amount effective to possess hypolipidemic activity.