Patent classifications
C07K5/0215
Macrocyclic compounds as proteasome inhibitors
The compounds of the present invention are represented by the following compounds having Formula I and Formula (I): ##STR00001##
where the substituents R.sup.1, R.sup.2, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R, R, X, Y, and Z are as defined herein and ##STR00002##
where the substituents R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R, R, X, Y, and Z are as defined herein. These compounds are used in the treatment of bacterial infections, parasite infections, fungal infections, cancer, immunologic disorders, autoimmune disorders, neurodegenerative diseases and disorders, inflammatory disorders, or muscular dystrophy or for providing immunosuppression for transplanted organs or tissues.
Compositions comprising chemerin analogs and methods of use
The present disclosure relates to peptide compositions and methods for treating an inflammatory condition such as ocular inflammation, retinal inflammation, dry eye, uveitis, allergic conjunctivitis, and inflammation resulting from nerve injury or nerve degeneration. The peptide compositions disclosed herein can also be used for treating pain such as neuropathic pain, ocular pain, chronic pain, pain resulting from chemotherapy or radiation, pain resulting from nerve injury or nerve degeneration, and pain resulting from an inflammatory condition, dysesthesia, or allodynia.
PSMA imaging agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
1,2,4-oxadiazole compounds as inhibitors of CD47 signalling pathways
The present invention relates to compounds of formula (I), compositions, methods and uses involving the said formula (I) that inhibit CD47 signaling pathway. The present invention also relates to methods of making such compounds and their uses for the treatment of diseases or disorders mediated by CD47.
PSMA imaging agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
NRP-1 binding inhibitory peptides and uses thereof
A number of anti-angiogenic strategies connected with the VEGF signalling pathway are used in current clinical treatment or trial phase, but they either cause adverse effects or are not specific. Various strategies were aimed at identifying peptides inhibiting the VEGF-A.sub.165/NRP-1 interaction. A well-known antiangiogenic peptide is the heptapeptide termed A7R having the amino acid sequence ATWLPPR, for which various derivatives have been synthesized, which include peptides having the general sequence Lys(hArg)-AA.sup.2-AA.sup.3-Arg. However, the ability of the known peptides to inhibit the VEGF-A.sub.165/NRP-1 interaction was too low for their use as candidate drugs for inhibiting angiogenesis in subjects in need thereof. The present inventors have now conceived a family of novel peptide-like compounds having a nanomolar affinity for NRP-1, which are thus endowed with a powerful capacity to inhibit the VEGF-A.sub.165/NRP-1 interaction. These novel peptide-like compounds may be relevantly used as antiangiogenic compounds, especially in subjects affected with cancer.