Patent classifications
C07D475/08
NOVEL IMMUNE SYSTEM MODULATORS
The present invention relates to a compound of Formula I:
##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
Prodrug using nitroimidazole
Provided is a prodrug of 2-nitro-1-imidazolepropionic acid and a therapeutically active organic compound having on the molecule an amino group, a cyclic amino group or a hydroxyl group, particularly a prodrug in which the therapeutically active organic compound is selected from among antitumor agents. The prodrug cleaves specifically under hypoxic conditions in vivo to exhibit the inherent therapeutic activity.
Prodrug using nitroimidazole
Provided is a prodrug of 2-nitro-1-imidazolepropionic acid and a therapeutically active organic compound having on the molecule an amino group, a cyclic amino group or a hydroxyl group, particularly a prodrug in which the therapeutically active organic compound is selected from among antitumor agents. The prodrug cleaves specifically under hypoxic conditions in vivo to exhibit the inherent therapeutic activity.
Immune system modulators
The present invention relates to a compound of Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
Immune system modulators
The present invention relates to a compound of Formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same; and a method for treating or preventing autoimmunity disease using the same.
MODIFIED CYTOTOXINS AND THEIR THERAPEUTIC USE
The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.
MODIFIED CYTOTOXINS AND THEIR THERAPEUTIC USE
The present disclosure generally provides compounds useful for treating cancer. In some aspects, the disclosure provides small-molecule cytotoxins that are chemically modified to include one or more moieties that include hydrophobic portions. In some embodiments, the disclosure provides small-molecule cytotoxins that are chemically modified with fatty acid-containing moieties. In some aspects, the disclosure provides compositions, such as pharmaceutical compositions, that include such modified small-molecule cytotoxins and a protein. In some embodiments, the protein is albumin or an albumin mimetic. Further, the disclosure provides various uses of these compounds and compositions.
MODULATORS OF TOLL-LIKE RECEPTORS
Provided are modulators of TLRs of Formula II:
##STR00001##
pharmaceutically acceptable salts thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.
ALPHA POLYGLUTAMATED METHOTREXATE AND USES THEREOF
The disclosure relates generally to alpha polyglutamated methotrexate, formulations containing liposomes filled with alpha polyglutamated methotrexate, methods of making the alpha polyglutamated methotrexate and liposome containing formulations, and methods of using polyglutamated alpha polyglutamated methotrexate and liposome containing formulations to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., an autoimmune disease such as rheumatoid arthritis).
Gamma polyglutamated pemetrexed and uses thereof
The disclosure relates generally to gamma polyglutamated pemetrexed compositions, including delivery vehicles such as liposomes containing the gamma polyglutamated pemetrexed, and methods of making and using the gamma polyglutamated pemetrexed compositions to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., inflammation and autoimmune diseases such as rheumatoid arthritis).