There is provided a composition for improving memory, learning ability, and cognitive ability and a method of enhancing a brain or cognitive function by administering the composition to a subject in need thereof. It has been confirmed that a peptide having a C-terminal region ended to GAG had an effect of improving the memory. In order for the peptide to have the effect, it has been confirmed that the peptide should be a peptide of which the length consists of at least 4 amino acids. Further, it has been confirmed that a peptide of which the length of the peptide having the C-terminal region ended to GAG consists of 5 to 9 amino acids has the same effect. As a result, the peptide of the present invention can be used as the composition for improving memory, learning ability, and cognitive ability, and the method of enhancing a brain or cognitive function.

Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.

A pharmaceutical composition comprising a synthetic neuromodulatory peptide is described. The invention discloses neuromodulatory peptides as defined in the claims and methods of using such molecules for therapeutic application. The neuromodulatory peptides included in the composition have been found to be effective in treatment of depression and other mood disorders, including anxiety.

The present disclosure relates to the biopharmaceutical field, in particular, Exatecan derivatives, linker-payloads, and conjugates and thereof antibody-drug conjugates, and the corresponding preparing process and use thereof.

Provided is at least one peptide of formula (I) and its use, where formula (I) is as follows: X-(Xaa.sub.1).sub.n-Pro*-(Xaa.sub.2).sub.m-Y (I). In formula (I), n=0 and m=1. At the N terminal end of the peptide, X is selected from H, —CO—R.sub.1 and —SO.sub.2—R.sub.1. At the C terminal end of the peptide, Y is selected from OH, OR.sub.1, NH.sub.2, NHR.sub.1 or NR.sub.1R.sub.2, R.sub.1 and R.sub.2 being independently selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy and aryloxy group, that can be linear, branched, cyclic, poly-cyclic, non-saturated, hydroxylated, carbonylated, phosphorylated and/or sulphured, with the possibility to have in said group skeleton a O, S and/or N heteroatom. Pro* corresponds to a Proline, an analogue or derivative thereof.

A linker molecule for targeting molecule-drug conjugate, has the structure of formula (I): A1p-D1q-Y-Lk-W-A2q-D2p (I). A conjugate has the structure of formula (III): A-((compound of formula (1))-PL .sub.t) .sub.z (III). The conjugate can be used in the manufacture of a medicament for treating a disease.

A method for producing a compound represented by formula (C) wherein R.sup.1 represents an amino group protected with a protecting group, the method comprising a step of subjecting a compound represented by formula (B) wherein R.sup.1 represents the same meaning as above, to intramolecular cyclization to convert the compound into the compound represented by formula (C). ##STR00001##

Doxorubicin derivatives for targeted activation by Legumain, its preparation method and use. The doxorubicin derivatives are obtained by condensation between the amino group of compound A and the carboxyl group of compound B and have the following structure: ##STR00001##
compounds A and B have the following structures, respectively: ##STR00002##
wherein R.sub.3 in compound B is Leu or absent; R.sub.4 is any one amino acid selected from the group consisting of Ala and Thr; R.sub.5 is any one amino acid selected from the group consisting of Ala, Thr and Asn; R.sub.6 is ##STR00003##
wherein n=1-20; or ##STR00004##
wherein R.sub.7 is substituted or unsubstituted, linear or branched, saturated or unsaturated C1-C20 fatty hydrocarbon, or substituted or unsubstituted C6-C20 aromatic hydrocarbon. The doxorubicin derivatives of the present invention are specifically tumor-targeted and have a long in vivo metabolic half-life, as compared with doxorubicin. They exhibit an efficient and safe anti-tumor effect and could be used to prepare an anti-tumor drug.

The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.

Novel peptoid oligomers are disclosed that have a formula represented by the following formula Ia or Ib: ##STR00001##
The peptoid oligomers are prepared as modulators of androgen receptor (AR), and may be prepared as pharmaceutical compositions and used for the prevention or treatment of a variety of conditions in mammals, including humans, associated with unwanted or aberrant AR activity. The present peptoid oligomers are particularly valuable for the treatment of subjects with cancer.