This review is an attempt to illustrate the diversity of peptides reported for a potential or an established use in cancer therapy. With 612 references, this work aims at covering the patents and publications up to year 2000 with many inroads in years 2001-2002. The peptides are classed according to four categories of effective (or plausible) biological mechanisms of action: receptor-interacting compounds; inhibitors of protein-protein interaction; enzymes inhibitors; nucleic acid-interacting compounds. The fifth group is made of the peptides for which no mechanism of action has been found yet. Incidentally this work provides an overview of many of the modern targets of anticancer research.

Peptides with anticancer use or potential.

Non-peptidyl compounds characterized generally as poly(aminoalkyl)aminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension.

Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents

A method of treatment of anxiety disorders which comprises administering to a host in need thereof an effective amount of a compound of formula (I):

Pyridine derivatives and their use in the treatment of psychotic disorders

Peptide compounds of the formula (I') ##STR1## in which R 1 is acyl, R 2 is lower alkyl, cyclo(lower)alkyl(lower)alkyl or optionally substituted heterocyclic(lower)alkyl, R 3 is optionally substituted heterocyclic(lower)alkyl or optionally substituted ar(lower)alkyl, R 4 is lower alkyl, amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl or optionally substituted heterocyclic(lower)alkyl, R 5 is carboxy, protected carboxy, carboxy(lower)alkyl or protected carboxy(lower)alkyl, R 6 is hydrogen, lower alkyl, C 6-10 ar(lower)alkyl amino(lower)alkyl, protected amino(lower)alkyl, carboxy(lower)alkyl, protected carboxy(lower)alkyl, or heterocyclic(lower)alkyl, R 7 is hydrogen or lower alkyl, and A is --O--, --NH--, lower alkylimino or lower alkylene, or a pharmaceutically acceptable salt thereof are disclosed. The compounds can be used to treat and prevent endothelin mediated diseases such as hypertension. The preparation of such peptides is also disclosed.

Peptide compound and its preparation

Compounds characterized generally as piperidinyl-terminated alkylamino ethynyl alanine amino diol derivatives are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are those of Formula I ##STR1## wherein A is selected from CO and SO 2 ; wherein x is selected from oxygen atom and methylene; wherein B is selected from a piperidinyl group, an isoindolyl group and an azabicyclononyl group; wherein R 1 is selected from hydrido, methyl, ethyl, isopropyl and n-propyl; wherein R 2 is phenylmethyl; wherein each of R 3 and R 5 is hydrido; wherein R 4 is selected from ##STR2## wherein V is selected from hydrido and methyl; wherein R 6 is cyclohexylmethyl; wherein R 7 is selected from isobutyl, cyclopropyl and cyclopropylmethyl; wherein q is a number selected from zero through three, inclusive; and wherein n is a number selected from zero through three, inclusive; or a pharmaceutically-acceptable salt thereof.

Piperidinyl-terminated alkylamino ethynyl alanine amino diol compounds for treatment of hypertension

A compound of the formula :
 wherein R 1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl,hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula :
 in which R 5 is hydrogen or acyl and
 R 6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and R 2 is hydrogen or lower alkyl; or R 1 and R 2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower)alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl; R 3 is hydrogen or lower alkyl; and R 4 is lower alkyl; and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.

New amino acid derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same

A compound of the formula: ##STR1## wherein R 1 is lower alkyl optionally substituted with a substituent selected from the group consisting of acyl, hydroxy, lower alkoxy, aryl, lower alkylthio and a group of the formula: ##STR2## in which R 5 is hydrogen or acyl and R 6 is hydrogen or lower alkyl; aryl; or amino optionally substituted with substituent(s) selected from the group consisting of lower alkyl and acyl; and R 2 is hydrogen or lower alkyl; or R 1 and R 2 are taken together with the attached nitrogen atom to form a heterocyclic group optionally substituted with substituent(s) selected from the group consisting of lower alkyl, hydroxy(lower )alkyl, lower alkoxy(lower)alkyl, acyl(lower)alkyl, oxo and acyl; R 3 is hydrogen or lower alkyl; and R 4 is lower alkyl; and its pharmaceutically acceptable salt, processes for the preparation thereof and pharmaceutical composition comprising the same.

New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same

This invention relates to new amino acid derivatives and pharmaceutically acceptable salts thereof, wherein the amino acid derivatives are useful in the treatment and/or prevention of hypertension, heart failure, renal diseases or glaucoma.

Amino acid derivatives, a process for the preparation thereof and pharmaceutical composition comprising the same

The invention relates to novel intermediate compounds for preparation of novel amino acid derivatives having renin inhibiting activity.

Hiroshi Marusawa

Papers

New amino acid derivatives, processes for the preparation thereof and pharmaceutical composition comprising the same

New Histidyl amino acid derivatives, and pharmaceutical composition comprising the same

Amino acid derivatives, a process for the preparation thereof and pharmaceutical composition comprising the same

Intermediate for preparation of amino acid derivatives

Prising the same