Patent classifications
A61K31/529
MACROCYCLIC COMPOUNDS AS ROS1 KINASE INHIBITORS
Methods for inhibiting a ROS1 kinase with compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, and Z are as defined herein. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).
MACROCYCLIC COMPOUNDS AS ROS1 KINASE INHIBITORS
Methods for inhibiting a ROS1 kinase with compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, and Z are as defined herein. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).
MACROCYCLIC COMPOUNDS AS ROS1 KINASE INHIBITORS
Methods for inhibiting a ROS1 kinase with compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, and Z are as defined herein. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).
MACROCYCLIC COMPOUNDS AS ROS1 KINASE INHIBITORS
Methods for inhibiting a ROS1 kinase with compounds of Formula I:
##STR00001##
and pharmaceutically acceptable salts thereof, wherein ring A, ring B, W, m, D, R.sup.2, R.sup.2a, R.sup.3, R.sup.3a, and Z are as defined herein. The compounds and methods provided herein are useful in the treatment of cancer (e.g., ROS1-associated cancers as defined herein).
Polymorphic form of TG02
The present disclosure provides crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, pharmaceutical compositions comprising crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, and methods of treating cancer and other diseases in a patient with crystalline polymorphic forms of TG02 free base and TG02 acid addition salts.
Polymorphic form of TG02
The present disclosure provides crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, pharmaceutical compositions comprising crystalline polymorphic forms of TG02 free base and TG02 acid addition salts, and methods of treating cancer and other diseases in a patient with crystalline polymorphic forms of TG02 free base and TG02 acid addition salts.
Inhibitors of glucose transporters (GLUTs)
The present invention relates to 2,6-methanobenzo[g][1]oxacin-4-one compounds and their analog compounds and pharmaceutically acceptable salts thereof as selective inhibitor of glucose transporters 1 and 3 (GLUTs 1 and 3), to methods of preparing said compounds, and to the use thereof as pharmaceutically active agents, especially for the prophylaxis and/or treatment of metabolic diseases, immunological diseases, autoimmune diseases, inflammation, graft versus host disease, cancer, and metastasis thereof. Furthermore, the present invention is directed to pharmaceutical composition comprising at least one of 2,6-methanobenzo[g][1]oxacin-4-one compounds and their analog compounds.
P2X7 modulators
The present invention is directed to compounds of Formula (I), which includes enantiomer and diasteromers thereof: ##STR00001## The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
METHODS OF TREATING TRANSPLANT REJECTION
The present invention provides the use of protein kinase inhibitors, in particular JAK2 inhibitors of formula (I), as set forth in the specification, in the treatment of solid organ transplant rejection and graft versus host disease (GvHD). Also provided are combination therapies for the treatment of solid organ transplant rejection and graft versus host disease.
METHODS OF TREATING TRANSPLANT REJECTION
The present invention provides the use of protein kinase inhibitors, in particular JAK2 inhibitors of formula (I), as set forth in the specification, in the treatment of solid organ transplant rejection and graft versus host disease (GvHD). Also provided are combination therapies for the treatment of solid organ transplant rejection and graft versus host disease.