C07D295/084

CONJUGATED LIPOMERS AND USES THEREOF

The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as “conjugated lipomers” or “lipomers”) containing one or more groups of the formula (iii):

##STR00001##

wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

Conjugated lipomers and uses thereof

The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

Conjugated lipomers and uses thereof

The present invention provides inventive conjugated polyethyleneimine (PEI) polymers and conjugated aza-macrocycles (collectively referred to herein as conjugated lipomers or lipomers) containing one or more groups of the formula (iii): ##STR00001##
wherein R.sup.3 and R.sup.4 are as defined herein. Also provided are compositions comprising the inventive conjugated lipomers, and methods of preparation and use.

COMPOUND HAVING STAT3 INHIBITORY ACTIVITY AND USE THEREOF
20200354327 · 2020-11-12 ·

The present invention relates to a compound exhibiting STAT3 inhibitory activity, or a pharmaceutically acceptable salt, solvate or hydrate of the same, and pharmaceutical uses of these. The compounds of the present invention efficiently inhibit the abnormal activity of STAT3 associated with various diseases and thus can be usefully utilized for the prevention and treatment of various STAT3-related diseases associated with cancer, autoimmune diseases, inflammatory diseases and the like.

HETEROCYCLIC COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

HETEROCYCLIC COMPOUNDS FOR CANCER IMAGING AND TREATMENT AND METHODS FOR THEIR USE

Compounds having a structure of Formula I:

##STR00001##

or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

BUMETANIDE ANALOGS, COMPOSITIONS AND METHODS OF USE
20240009153 · 2024-01-11 ·

The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup. co-transporter or GABA.sub.A receptor.

BUMETANIDE ANALOGS, COMPOSITIONS AND METHODS OF USE
20240009153 · 2024-01-11 ·

The present invention provides bumetanide analogs and compositions comprising such analogs. The present invention also provides pharmaceutical compositions containing these bumetanide analogs and methods for their use. These analogs are believed useful for the treatment and/or prophylaxis of conditions that involve the Na.sup.+K.sup.+Cl.sup. co-transporter or GABA.sub.A receptor.

AZIRIDINYL AND AMINO DIMERIC NAPHTHOQUINONE COMPOUNDS AND USE FOR ACUTE MYELOID LEUKEMIA

The invention relates to new amino dimeric naphthoquinone compounds with antileukemic activity. Compounds of the invention demonstrated increased aqueous solubility compared to previously available dimeric naphthoquinones and potent nanomolar inhibition of cell survival in AML cells. Preferred compounds contained an aziridine or a secondary amino alcohol pharmacophore.

Sulfide alkyl compounds for HBV treatment

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.