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 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.

The present invention relates to compounds and compositions for use in enhancing flavor and/or saltiness of a food product. Particularly, the present invention relates to compounds of the general formula I) and compositions comprising them.

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Compounds and compositions are disclosed in which a NAMPT Drug Unit is linked to a targeting Ligand Unit through a Unit from which a NAMPT inhibitor compound or derivative thereof is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as cancer or an autoimmune disease, using the compounds and compositions of the invention are also disclosed.

The disclosure relates to pharmaceutical compositions, to methods of preparing such compositions, and to methods for using such compositions for treating or preventing a disease or condition associated with arginase activity.

Isoform-selective lysine deacetylase inhibitors are described. Inhibitors of the lysine deacetylase enzyme are useful as antitumor drugs and for treating addiction, asthma, cardio-vascular disease, immunosuppression, neurodegenerative diseases, sepsis, sickle-cell disease, uveal melanoma and termination of viral latency, particularly HIV-1 latency.

The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. 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. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

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.

The present invention relates to the use of dipeptidyl ketoamide compounds for preventing accumulation of triglycerides in adipose tissue or for reducing the amount of triglycerides in adipose tissue in a subject in need thereof and to novel dipeptidyl ketoamide compounds.

Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.