C07K5/1021

METAL COMPOUND HAVING PHASE TRANSFORMATION AND METHOD OF PREPARING THE SAME
20220041461 · 2022-02-10 · ·

The present invention relates to a metal phase transformation compound and a method for preparing the same.

Therapeutic compositions including frataxin, lactoferrin, and mitochondrial energy generating enzymes, and uses thereof
11141456 · 2021-10-12 · ·

Disclosed herein are methods and compositions for the treatment and/or prevention of diseases or conditions comprising administration of a therapeutic biological molecule, and/or naturally or artificially occurring derivatives, analogues, or pharmaceutically acceptable salts thereof, alone or in combination with one or more active agents (e.g., an aromatic-cationic peptide). The present technology provides compositions related to aromatic-cationic peptides linked to a therapeutic biological molecule and uses of the same. In some embodiments, the aromatic-cationic peptide comprises 2′,6′-dimethyl-Tyr-D-Arg-Phe-Lys-NH.sub.2, Phe-D-Arg-Phe-Lys-NH.sub.2, or D-Arg-2′,6′-Dmt-Lys-Phe-NH.sub.2.

Small Molecule Drug Conjugates

A binding moiety (B) for Carbonic Anhydrase IX (CAIX), the binding moiety comprising:

##STR00001##

The binding moiety is univalent, bivalent, or multivalent. A targeted therapeutic agent may comprise the binding moiety. The invention also includes a method for treating a disease expressing elevated levels of CAIX by administering the targeted therapeutic agent.

SOLUTION PHASE SYNTHESIS OF BETA-TURN PEPTIDOMIMETIC CYCLIC SALTS
20210300966 · 2021-09-30 ·

The present disclosure relates to methods of preparing and crystallizing β-turn cyclic peptidomimetic salts of formula I:

##STR00001##

where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, X, Y and n are as defined in the specification.

The present disclosure provides a more efficient route for preparing a crystalline form of a β-turn cyclic peptidomimetic compounds and salts thereof.

PEPTIDE-COATED CALCIUM PHOSPHATE PARTICLES

The invention features methods and compositions for (i) controlling the amount of peptide bound to calcium phosphate particles; and (ii) for tightly binding peptide to the surface of calcium phosphate particles. The methods and compositions can be useful for preparing implants useful for promoting bone deposition at the site of implantation, and for repairing a variety of orthopedic conditions.

Solution phase synthesis and crystallization of beta-turn peptidomimetic cyclic salts

The present disclosure relates to methods of preparing and crystallizing β-turn cyclic peptidomimetic salts of formula I: ##STR00001##
where R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.10, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of β-turn cyclic peptidomimetic compounds and salts thereof.

Inhibitors of transglutaminases

The invention relates to the compound of general formula (I) as novel inhibitors of transglutaminases, to methods for producing the inventive compounds, to pharmaceutical compositions containing said inventive compounds and to their use for the prophylaxis and treatment of diseases associated with transglutaminases.

PEPTIDOMIMETIC INHIBITORS OF THE PEPTIDYL-PROLYL CIS/TRANS ISOMERASE (PIN1)

Disclosed are compounds which inhibit Pin1 activity, methods of making the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds to treat diseases or disorders characterized or mediated by dysregulated Pin1 activity.

TETRAPEPTIDES, COMPOSITIONS COMPRISING THEM, AND THEIR COSMETIC USE
20230398049 · 2023-12-14 · ·

They have the general Formula X-(Xaa).sub.nLE(Xaa).sub.m-Z wherein Xaa is selected from L, K, E and D, either n=2 and m=0, or n=1 and m=1, at the N-terminal end X being selected from H, —CO—R.sup.1, —SO.sub.2-R.sup.1 or a biotinoyl group, at the C-terminal end Z being selected from OH, OR.sup.1, NH.sub.2, NHR.sup.1 or NR.sup.1R.sup.2, and R.sup.1 and R.sup.2 being selected from an alkyle, aryle, aralkyle, alkylaryl, alkoxy, saccharide and aryloxy, said group having from 1 to 24 carbon atoms. Preferred peptide sequences are X-LKLE-Z and X-ELED-Z. These tetrapeptides stimulate the synthesis of molecules constituting the ECM, in particular collagen 1 and 4, hyaluronic acid and fibronectin, and can be used for a cosmetic treatment, in particular anti-aging, anti-wrinkle and fine lines, to improve the skin mechanical properties, to increase skin density and volume, hydration, and/or to fight against stretch marks, and skin sagging.

Cytotoxic benzodiazepine derivatives

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.