Azaindoline compounds as granzyme B inhibitors, compositions that include the compounds, and methods for using the compounds. Methods for treating cutaneous scleroderma, epidermolysis bullosa, radiation dermatitis, alopecia areata, and discoid lupus erythematosus are provided.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability.

##STR00001##

Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

The present invention relates to compounds of formula (I)

##STR00001## wherein X.sup.1 to X.sup.8 and R.sup.1 to R.sup.8 are as described herein, as well as pharmaceutically acceptable salts thereof for the use in the treatment or prevention of infections and resulting diseases caused by Pseudomonas aeruginosa.

The present disclosure provides a compound targeting prostate specific membrane antigen (PSMA), wherein the compound has the following structure shown in Formula (I); R.sub.1 is a compound structure targeting prostate specific membrane antigen; L.sub.1 is (X).sub.n(CH.sub.2).sub.m(Y).sub.q, X and Y are independently selected from lysine, glutamic acid or a derivative structure containing lysine and glutamic acid, n is an integer from 0 to 12, m is an integer from 0 to 60, q is an integer from 0 to 12, and each CH.sub.2 may be individually substituted with O, NH(CO), or (CO)NH; L.sub.2 is (CH.sub.2).sub.p, p is an integer from 0 to 30, and each CH.sub.2 may be individually substituted with O, NH(CO), or (CO)NH; and R.sub.2 is a nuclide chelating group. The present disclosure also provides a radiolabeled complex based on the structure of the compound. The compound and the radiolabeled complex have appropriate blood circulation time, high uptake in tumors and long retention time, and are suitable for nuclide therapy and imaging of tumors with high expression of PSMA.

##STR00001##

The present disclosure provides human tumor necrosis factor alpha antibody glucocorticoid receptor agonist conjugates and methods of using the conjugates for the treatment of autoimmune and inflammatory diseases.

Peptides, peptidomimetics and small molecules, collectively referred to as decoy peptides, are provided, which interfere with binding to a TIR domain of a toll-like receptor 4 (TLR4), and inhibit a TLR4-induced signaling pathway. These decoy peptides may be useful for treating diseases associated with induction of TLR4 signaling pathway such as a disease or disorder secondary to a cardiovascular disease, sepsis or an inflammatory disease.

Charged or pro-charged cross-linking moieties and conjugates of cell binding agents and drugs comprising the charged or pro-charged cross-linking moieties and method of making the same.

The invention relates to a method for inhibiting an ADAM protease, comprising inhibiting binding to an integrin-binding loop of a disintegrin domain in the ADAM protease. Also provided are cyclic peptides which inhibit binding to an integrin-binding loop of an ADAM protease, as well as associated pharmaceutical compositions, uses and methods of treatment.

Provided are compounds of Formula I: ##STR00001## and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of virus infections, particularly hepatitis C infections.

Certain embodiments are directed to compositions and methods of inhibiting a pathogenic bacterial infection involving ADAM10, specifically a method for treating pore-forming toxin-inducted pathology caused by exposure to staphylococcus in a subject, comprising administering an effective amount of a ADAM10 inhibitor to a patient. The methods include treating pneumonia or inhibiting disruption to epithelial barrier in a subject, having or at risk of developing staphylococcal infection.