C07D255/02

TARGETING STAT SUMOYLATION TO ENHANCE IMMUNE RESPONSES

The present disclosure generally relates to compositions and methods for ex vivo expansion of immune cells isolated from a subject, wherein gene expression can be modulated to enhance immune cell activity in the resulting expanded immune cell culture. Modulation of gene expression in an expanded immune cell culture allows for an immune cell therapy contains genetically chemically modified immune cells suitable for the adoptive cell transfer into a subject in need thereof.

Macrocycles, cobalt and iron complexes of same, and methods of making and using same

Provided are macrocyclic compounds and iron or cobalt coordinated macrocyclic compounds. The compounds can be used as MRI contrast agents. Certain compounds are redox active and can be used to assess the biological redox status of a sample.

Macrocycles, cobalt and iron complexes of same, and methods of making and using same

Provided are macrocyclic compounds and iron or cobalt coordinated macrocyclic compounds. The compounds can be used as MRI contrast agents. Certain compounds are redox active and can be used to assess the biological redox status of a sample.

Nrf2 Activating Compounds and Uses Thereof
20210078969 · 2021-03-18 ·

Aspects of the present disclosure include compounds that activate Nrf2. Such compounds 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 compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Nrf2 Activating Compounds and Uses Thereof
20210078969 · 2021-03-18 ·

Aspects of the present disclosure include compounds that activate Nrf2. Such compounds 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 compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS
20210078974 · 2021-03-18 ·

Provided herein are triazacyclododecansulfonamide (TCD)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.

##STR00001##

TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS
20210078974 · 2021-03-18 ·

Provided herein are triazacyclododecansulfonamide (TCD)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.

##STR00001##

Dimerization strategies and compounds for molecular imaging and/or radioimmunotherapy

The present invention provides a multivalent compound for targeted molecular imaging and/or targeted drug delivery, wherein two components or targeting molecules each interacts with one or more biomarkers on a cell. The present invention further provides a multifunctional chelator to combine the targeting molecules. The present invention also provides an in vitro high-throughput screening assay to determine the length of the spacer molecules. The present invention also relates to compounds/probes, kits and methods for use in targeted molecular imaging and/or targeted drug delivery.

Dimerization strategies and compounds for molecular imaging and/or radioimmunotherapy

The present invention provides a multivalent compound for targeted molecular imaging and/or targeted drug delivery, wherein two components or targeting molecules each interacts with one or more biomarkers on a cell. The present invention further provides a multifunctional chelator to combine the targeting molecules. The present invention also provides an in vitro high-throughput screening assay to determine the length of the spacer molecules. The present invention also relates to compounds/probes, kits and methods for use in targeted molecular imaging and/or targeted drug delivery.

METHOD FOR MANUFACTURING NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF AND MANUFACTURING INTERMEDIATE OF NOVEL NITROGEN-CONTAINING COMPOUND OR SALT THEREOF

A compound represented by Formula [3] or a salt thereof and a method of making the same,

##STR00001## in the formula, L.sup.3 represents a group represented by Formula [2c]

##STR00002##

wherein R.sup.3c, R.sup.4c, R.sup.5c, and R.sup.6c are the same as or different from each other and represent a hydrogen atom or a C.sub.1-6 alkyl group; p.sup.3 represents an integer of 1 to 3; q.sup.3 represents an integer of 0 to 3; and r.sup.3 represents an integer of 1 to 6; A.sup.1 represents any one of the groups represented by Formulae [4] to [9],

##STR00003## wherein * represents a binding position; and R.sup.7 represents a carboxyl-protecting group; and m represents an integer of 1 to 3.