C07K5/0215

NOVEL RADIOMETAL-BINDING COMPOUNDS FOR DIAGNOSIS OR TREATMENT OF PROSTATE SPECIFIC MEMBRANE ANTIGEN-EXPRESSING CANCER

This application relates to compounds of Formula (I-a) or Formula (I-b), or is salts or solvates thereof. R.sup.1 is (CH.sub.2).sub.5CH.sub.3 or comprises 2-4 fused benzene rings. R.sup.2 is I, Br, F, Cl, H, OH, OCH.sub.3, NH.sub.2, NO.sub.2 or CH.sub.3. R.sup.3 is a peptide-bonded glycine, aspartate or glutamate or is glutamate peptide bonded through C.sub.delta. L is CH.sub.2NH, (CH.sub.2).sub.2NH, (CH.sub.2).sub.3NH, or (CH.sub.2).sub.4NH. R.sup.4 is a radiometal chelator optionally bound by a radiometal. Variable n is 1-3. The compounds may be useful for imaging prostate specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

Cyclic peptidomimetics, compositions containing them and their use in the treatment of diseases associated with angiogenesis

The present invention relates to novel cyclic peptidomimetics, pharmaceutical compositions containing them and their use in the treatment of diseases associated with angiogenesis especially tumors and chronic inflammation in psoriasis, diabetes, degenerative diseases of the eye (ARMD), nephropathy and neuropathy.

Methods and compositions for modulating transport of a drug
10786542 · 2020-09-29 ·

Methods and pharmaceutical compositions for inhibiting or decreasing transport of a drug by a transporter of multidrug resistance-associated protein comprising a compound of Formula (V): ##STR00001##
wherein R.sub.1 and R.sub.2 are small peptides or modified peptides, are provided. The methods and compositions are useful in enhancing efficacy of drugs such as anti-inflammatory agents, neurological agents, thyroid agents, ocular agents, cancer chemotherapeutics, antibiotics, antimicrobials, antivirals and protease inhibitors to treat human immunodeficiency virus.

Cholecystokinin 2 receptor targeted NIR imaging and use thereof

Compounds are described herein where CCK2R targeting ligands are attached to an imaging agent through a linker. The compounds can be used in the detection, diagnosis, imaging and treatment of cancer.

Crystal of reduced glutathione and method for producing same

The present invention provides a crystal of reduced glutathione having excellent powder properties and a method for producing the same. The present invention relates to a crystal of reduced glutathione, wherein the average crystal thickness is 10 m or more.

Prodrugs of NRF2 activating compounds and uses thereof

Aspects of the present disclosure include prodrugs of compounds that activate Nrf2. Such prodrugs find use in the treatment of autoimmune and inflammatory diseases and disorders, such as for example psoriasis and multiple sclerosis. Embodiments of the present disclosure also relate to pharmaceutical compositions that include these prodrugs, methods of using these prodrugs in the treatment of various diseases and disorders, processes for preparing these prodrugs and intermediates useful in these processes.

BRANCHED PEPTIDES FOR ENZYMATIC ASSEMBLY AND MITOCHONDRIA DRUG DELIVERY
20200281854 · 2020-09-10 ·

The present invention relates to a branched peptide that includes a first peptide chain and a second peptide chain having its C-terminal amino acid covalently linked to a sidechain of an amino acid residue of the first peptide chain, wherein the first peptide chain includes a plurality of aromatic amino acids and, optionally, an aromatic group linked to an amino terminus of the first peptide chain; and the second peptide chain includes a plurality of hydrophilic amino acids and an enzyme cleavage site. Pharmaceutical compositions containing the branched peptide and one or more therapeutic agents in an aqueous medium are disclosed, where the branched peptides form micelle structures in the aqueous medium. Methods of using the pharmaceutical composition to deliver therapeutic agents, and for treating various disease conditions are also described.

INHIBITION OF OXIDATIVE STRESS, GLYCATION, AND PROTEIN CROSSLINKING
20200247846 · 2020-08-06 ·

Compositions for the treatment and prevention of symptoms and disease conditions associated with oxidative and carbonyl stress, including advanced glycation end products (AGEs), and to methods using the compositions. In particular, the invention relates to compositions useful in the treatment of diabetic retinopathy and nephropathy, to compositions useful in the treatment of other retinal disorders including macular degeneration and cataracts.

DISULFIDE BOND CONTAINING COMPOUNDS AND USES THEREOF
20200207810 · 2020-07-02 ·

There is provided a range of novel disulfide bond containing compounds. These disulfide bond containing compounds can be used in a variety of applications such as solid phase peptide synthesis, solid phase organic synthesis, formation of dendrimers, formation of macromolecules and formation cyclic peptides; and as a component of a delivery vehicle with a bioactive molecule.

Dual-Enzyme Responsive Peptides
20200199177 · 2020-06-25 ·

An enzyme-responsive peptide and a method off using such enzyme-responsive peptide are disclosed. An enzyme-responsive peptide, the peptide comprising an amino acid having an -amino group, an -carboxylic acid group and a -amine group, wherein the -amine group is covalently bonded with a first group and the -carboxylic acid is covalently bonded with a second group.