摘要:
Decapaptides substituted on the N-terminal nitrogen atom by acyl groups are potent antagonists of LHRH and are useful for suppressing the levels of sex hormones in mammals.
摘要:
Decapaptide and undecapaptides substituted on the N-terminal nitrogen atom by acyl groups which include furo-2-yl, isonicotinyl, nicotinyl, 2-, 3-, and 4-quinolinecarbonyl, shikimyl, dihydroshikimyl, and tetrahydrofur-2-oyl are potent antagonists of LHRH and are useful for suppressing the levels of sex hormones in mammals.
摘要:
The present invention provides a process for the preparation of peptides which have or side-chains containing an alkyl- or dialkyl-substituted guanidinyl group or a imidazinylamino or tetrahydropyrimidinylamino group. The process provides higher overall yields of peptide product by permitting the synthesis of the entire peptide chain prior to modification of the side-chain to introduce the groups.
摘要:
The present invention provides a class of decapeptide compounds which are potent antagonists of LHRH activity and which have the structure A.sup.1 -D.sup.2 -E.sup.3 -G.sup.4 -J.sup.5 -L.sup.6 -M.sup.7 -Q.sup.8 -R.sup.9 -T.sup.10. The compounds of the percent invention are characterized by having an .OMEGA.-amino-functionalized side chain on the D-aminoacyl residue at position 6. The .OMEGA.-amino group of this side chain is further derivatized by the attachment of an extending group which likewise has a terminal amino group which is capped by an acyl group.
摘要:
Tetrahydroisoquinoline derivatives of the formula: ##STR1## or a pharmaceutically acceptable salt, ester, or prodrug thereof, having activity as an LHRH antagonist, as well as pharmaceutical compositions containing the same, and methods for their use and preparation.
摘要:
A class of potent LHRH decapeptide antagonists possess N-alkylated aminoacyl residues where the side-chain portion of the residue is a 4-(substimtedamino)phenylalanyl, 4-(substituted-amino)cyclohexylalanyl, or .OMEGA.-(substitutedamino)alkyl group, and additionally the aminoacyl residues at position 5 are N-alkylated on the nitrogen atom of the peptide backbone.
摘要:
Peptides possessing LHRH antagonistic activity, and useful for the controlling the release of LHRH in mammals are decapeptide analogues of LHRH having a lactam group at the N-terminus of the formula ##STR1## where n is 1, 2, or 3 and R.sup.1 is selected from the group consisting of hydrogen, benzyl, 4-chlorobenzyl, 2-methylnaphth-1-yl, 1-methylnaphth-2-yl, and quinolin-3-ylmethyl.
摘要:
Peptide vectors having high KDR binding affinity and processes for making such vectors are provided. The peptide vectors may be conjugated to phospholipids and included in ultrasound contrast agent compositions. Such ultrasound contrast agents are particularly useful in therapeutic and diagnostic methods, such as in imaging KDR-containing tissue and in the evaluation and treatment of angiogenic processes associated with neoplastic conditions. The present invention also provides processes for the large scale production of highly pure dimeric and monomeric peptide phospholipid conjugates as well as precursor materials used to form the conjugates. The present invention further provides processes for the large scale production of highly pure peptide phospholipid conjugates which contain very low levels of TFA.
摘要:
Fibrin-binding peptides having high binding affinity and excellent physical characteristics compared to previously known fibrin-binding peptides are provided. These fibrin-binding peptides may be conjugated to a detectable label or a therapeutic agent and used to detect and facilitate treatment of pathological conditions associated with the presence of fibrin such as thrombic, angiogenic and neoplastic conditions. These peptides may be used in imaging processes such as MRI, ultrasound and nuclear medicine imaging (e.g. PET, scintigraphic imaging, etc.). The peptides may also be used therapeutically. The present invention also provides processes and methods for making and using such peptides and conjugates thereof.
摘要:
Novel methods of treating prostate tumors or of delaying the progression of prostate tumors are also provided, including, methods of treating bone or soft tissue metastases of prostate cancer methods for treating hormone sensitive and hormone refractory prostate cancer, methods for delaying the progression of hormone sensitive prostate cancer, for facilitating combination therapy in patients with hormone sensitive prostate cancer and for decreasing aberrant vascular permeability in patients with hormone sensitive prostate cancer, said methods comprising the step of administering to a subject a dose comprising an amount of radioactively labeled L70, N-[4-[[[[[4,7,10-Tris(carboxymethyl)-1,4,7,10-tetraazacyclododec-1-yl]acetyl]amino]acetyl]amino]benzoyl]-L-glutaminyl-L-tryptophyl-L-alanyl-L-valyl-glycyl-L-histidyl-L-leucyl-L-methioninamide.