A compound of formula (I): ##STR00001##
or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.

Compounds and compositions comprising a B-type natriuretic signal peptide fragment agent, and methods of use thereof, are provided for the treatment or prevention of cardiovascular diseases, disorders, and conditions.

An object of the present invention is to provide a process capable of producing a self-assembling peptide derivative that is useful in the fields of regenerative medicine and surgery in large quantities and in an economical and efficient manner. In particular, provided is a production process employing a combination of (i) a step of convergently constructing a sequence with use of a common repeating unit consisting of a specific amino acid sequence and (ii) a step of first isolating the peptide derivative as a disulfuric acid salt, a tetramethanesulfonic acid salt or a tetra(trifluoroacetic acid (TFA) salt), and then subjecting the peptide salt to a salt exchange reaction to yield a tetrahydrochloric acid salt.

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.

Prodrugs of an NMDA antagonist, (S)-1-phenyl-2-(pyridin-2-yl)ethanamine, useful for the treatment of depression (particularly major depressive disorder) or pain; compositions comprising them, and methods of making them.

Compositions of dendrimers conjugated with one or more glutamine antagonist(s) that inhibit glutamine metabolism, preferably in activated microglia, and methods of use thereof for treating, alleviating, and/or preventing one or more neurological, oncological, and/or immune disorders associated with pathogenic or dysregulated glutamine-dependent pathways and/or glutamate transmission, have been developed. Dendrimers conjugated with one or more glutamine antagonists effectively inhibit the activity of glutaminase without any systemic toxicity. Dendrimers conjugated with one or more glutamine antagonists accumulate in activated microglia associated with the injured or diseased cells and tissues.

Provided herein are novel compounds of Formula I, or a pharmaceutically acceptable salt thereof or pharmaceutical compositions comprising the same. Also provided are methods of preparing the compounds of Formula I, or pharmaceutically acceptable salt thereof. Further provided are methods of using the novel compounds of Formula I, or a pharmaceutically acceptable salt thereof, for example, for inhibiting thrombin and/or for the use in the prevention and/or treatment of thrombin-mediated and thrombin-related diseases. ##STR00001##

Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.

The present invention concerns the separation, identification and characterization of active peptide fragments from peptones.

Inhibitors of fibroblast activation protein alpha (FAP) and Prolyl Oligopeptidase (POP) are disclosed, along with their use in various therapies related to conditions, diseases, and disorders involving abnormal cell proliferation such as malignancies and angiogenesis, and in neural disorders such as Alzheimer's disease. Stalk portions of the inhibitor molecules, and substrates of FAP and POP, are also disclosed and may be used, for example, in screening methods for identifying such inhibitors.