Patent classifications
C07D209/24
MAO INHIBITORS AND THEIR CONJUGATES AS THERAPEUTICS FOR THE TREATMENT OF BRAIN CANCER
A pharmaceutical composition and method for treating brain cancer are provided. The method includes administering to a patient in need thereof an effective amount of one or more compounds that include moclobemide, clorgyline, clorgyline's Near-infra-red dye Monoamine Oxidase Inhibitor (NMI), and MHI 148-clorgyline, and their salt thereof. The composition and method are particularly effective in reducing the size of glioblastomas that are temozolomide (TMZ) resistant.
Indole carboxamide derivatives as P2X7 receptor antagonists
The invention relates to indole carboxamide derivatives of formula (I), ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Indole carboxamide derivatives as P2X7 receptor antagonists
The invention relates to indole carboxamide derivatives of formula (I), ##STR00001##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10 and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
ASH1L degraders and methods of treatment therewith
Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.
ASH1L degraders and methods of treatment therewith
Provided herein are small molecules comprising a first domain that binds to ASH1L and a second domain that facilitates ASH1L degradation. In particular, ASH1L-targeting proteolysis targeting chimeras (PROTACs) and methods of use thereof for the treatment of disease (e.g., acute leukemia, solid cancers and other diseases dependent on activity of ASH1L) are provided.
PLATFORM DRUG DELIVERY SYSTEM UTILIZING CRYSTAL ENGINEERING AND THEANINE DISSOLUTION
A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.
PLATFORM DRUG DELIVERY SYSTEM UTILIZING CRYSTAL ENGINEERING AND THEANINE DISSOLUTION
A platform drug delivery system and a method of improving the delivery of low solubility pharmaceuticals utilizing crystal engineering and Theanine dissolution resulting in enhanced bioactivity, dissolution rate, and solid state stability.
ORAI channel inhibitors
The present application in one embodiment provides a compound of Formula (I) ##STR00001## or a pharmaceutically acceptable salt thereof, wherein X.sup.1, X.sub.2, X.sub.3, X.sub.4, X.sup.5, X.sup.6, Y.sup.1, Y.sup.2, Y.sup.3, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.A, R.sup.B, W and Cy.sup.1 are as described herein. Pharmaceutical compositions containing these compounds, and methods of using these compounds for treating cancer, autoimmune diseases, and inflammatory diseases are also provided.
ORAI channel inhibitors
The present application in one embodiment provides a compound of Formula (I) ##STR00001## or a pharmaceutically acceptable salt thereof, wherein X.sup.1, X.sub.2, X.sub.3, X.sub.4, X.sup.5, X.sup.6, Y.sup.1, Y.sup.2, Y.sup.3, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.A, R.sup.B, W and Cy.sup.1 are as described herein. Pharmaceutical compositions containing these compounds, and methods of using these compounds for treating cancer, autoimmune diseases, and inflammatory diseases are also provided.
COMPOUNDS, COMPOSITIONS AND METHODS THEREOF
Among other things, the present disclosure provides compounds, e.g., of formula I or salts thereof. In some embodiments, the present disclosure provides methods for modulating MRGPRX4 activity. In some embodiments, the present disclosure provides methods for preventing or treating conditions, disorders or diseases, e.g., MRGPRX4-associated conditions, disorders or diseases.