Patent classifications
C07K5/08
Cyclic peptides as protein targeting agents
Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I): ##STR00001##
including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R.sup.1, L.sup.1, L.sup.2, G, M, Y.sup.1Y.sup.2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.
Cyclic peptides as protein targeting agents
Peptides having activity as protein binding agents are disclosed. The peptides have the following structure (I): ##STR00001##
including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R, R.sup.1, L.sup.1, L.sup.2, G, M, Y.sup.1Y.sup.2 and SEQ are as defined herein. Methods associated with preparation and use of such peptides, as well as pharmaceutical compositions comprising such peptides, are also disclosed.
Immunoproteasome inhibitor
Methods and pharmaceutical compositions for treating malaria and immune related disorders are provided. The pharmaceutical compositions include an effective amount a carmaphycin B analog that inhibits immunoproteasome activity in a subject.
INHIBITORS FOR PROLIFERATING CELL NUCLEAR ANTIGEN AND USES
The present invention relates to series of compounds as an inhibitor targeting Proliferating Cell Nuclear Antigen (PCNA). Pharmaceutical compositions of those compounds and methods of using them in the treatment of cancer are within the scope of this disclosure.
INHIBITORS FOR PROLIFERATING CELL NUCLEAR ANTIGEN AND USES
The present invention relates to series of compounds as an inhibitor targeting Proliferating Cell Nuclear Antigen (PCNA). Pharmaceutical compositions of those compounds and methods of using them in the treatment of cancer are within the scope of this disclosure.
Hemiasterlin Derivative Having Cysteine Residue
A compound represented by formula (1):
##STR00001##
wherein b represents an integer of 1 to 5; X represents —NH— or —CO—; Z represents a group represented, for example, by formula (Z-1); R.sup.1 represents a hydrogen atom or (AB).sub.m; AB represents a particular amino acid residue, and when there is a plurality of ABs, each AB may be the same as or different from each other and ABs are bonded to each other via an amide bond; m represents an integer of 1 to 9; R.sup.2 represents a hydroxy group or (AC).sub.g; AC represents a particular amino acid residue, and when there is a plurality of ACs, each AC may be the same as or different from each other and ACs are bonded to each other via an amide bond; and g represents an integer of 1 to 9,
or a salt thereof.
Hemiasterlin Derivative Having Cysteine Residue
A compound represented by formula (1):
##STR00001##
wherein b represents an integer of 1 to 5; X represents —NH— or —CO—; Z represents a group represented, for example, by formula (Z-1); R.sup.1 represents a hydrogen atom or (AB).sub.m; AB represents a particular amino acid residue, and when there is a plurality of ABs, each AB may be the same as or different from each other and ABs are bonded to each other via an amide bond; m represents an integer of 1 to 9; R.sup.2 represents a hydroxy group or (AC).sub.g; AC represents a particular amino acid residue, and when there is a plurality of ACs, each AC may be the same as or different from each other and ACs are bonded to each other via an amide bond; and g represents an integer of 1 to 9,
or a salt thereof.
PSMA binding ligand-linker conjugates and methods for using
Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
PSMA binding ligand-linker conjugates and methods for using
Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.
PEPTIDE AND METHOD FOR MANUFACTURING SAME
A peptide having a fluoroalkyl group as its side chain and a method for producing, which comprises condensing a compound represented by the formula (6-2) or (6-4), where means that an asymmetric carbon atom has an absolute configuration of S or R, Rf is a C.sub.1-30 alkyl group which is substituted with at least two fluorine atoms, and which may further be substituted with a halogen atom other than a fluorine atom (when the C.sub.1-30 alkyl group is a C.sub.2-30 alkyl group, it may have 1 to 5 etheric oxygen atoms between carbon atoms), and R.sup.2 is a protecting group for the amino group, with a fluorinated amino acid having its carboxy group protected, an amino acid having its carboxy group protected, a fluorinated peptide having its C-terminal protected, or a peptide having its C-terminal protected.