Patent classifications
C07D211/06
PYRIMIDINE COMPOUNDS AS JAK KINASE INHIBITORS
The invention provides compounds of formula (I):
##STR00001##
wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
Piperidine derivatives as HDAC1/2 inhibitors
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.
Thyromimetics
Compounds are provided having the structure of Formula (I): ##STR00001##
or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X.sup.1, X.sup.2, Q, R.sup.1, R.sup.2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
Phenoxyethyl cyclic amine derivatives and their activity as EP4 receptor modulators
The present invention provides a compound of the Formula (I): wherein X, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as defined herein, or a pharmaceutically acceptable salt thereof. ##STR00001##
Phenoxyethyl cyclic amine derivatives and their activity as EP4 receptor modulators
The present invention provides a compound of the Formula (I): wherein X, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as defined herein, or a pharmaceutically acceptable salt thereof. ##STR00001##
Substituted 4-phenylpiperidines, their preparation and use
The present invention provides a compound having the structure: ##STR00001## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are each independently H, halogen, CF.sub.3 or C.sub.1-C.sub.4 alkyl, wherein two or more of R.sub.1, R.sub.2, R.sub.3, R.sub.4, or R.sub.5 are other than H; R.sub.6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is H, R.sub.2 is CF.sub.3, R.sub.3 is H, R.sub.4 is CF.sub.3, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is H, R.sub.3 is H, R.sub.4 is F, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is H, R.sub.3 is F, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is CF.sub.3, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, or R.sub.1 is Cl, R.sub.2 is F, R.sub.3 is H, R.sub.4 is H, and R.sub.5 is H, then B is other than ##STR00002##
or a pharmaceutically acceptable salt thereof.
Processes and intermediates in the preparation of C5aR antagonists
Intermediates and methods are provided for the preparation of selected C5aR antagonist compounds.
ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE
The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose.
ORGANIC REACTIONS CARRIED OUT IN AQUEOUS SOLUTION IN THE PRESENCE OF A HYDROXYALKYL(ALKYL)CELLULOSE OR AN ALKYLCELLULOSE
The present invention relates to a method of carrying out an organic reaction in aqueous solution in the presence of a hydroxyalkyl(alkyl)cellulose or an alkylcellulose.
Substituted thioureas as heat shock protein 70 inhibitors
The invention provides a compound of Formula I, an isomer, a pharmaceutically acceptable salt, or a solvate thereof, and use thereof in manufacture of a medicament for preventing and/or treating a drug-resistant tumor or disease or disorder caused by a drug-resistant bacterium, or use thereof in manufacture of a medicament for preventing and/or treating a tumor, a neurodegenerative disease, an allogeneic graft rejection, or an infection-associated disease or disorder; preferably, the tumor, neurodegenerative disease, allogeneic graft rejection, or infection-associated disease or disorder is a disease or disorder caused by Heat shock protein 70 (Hsp70). The compounds of the invention, which are a class of Hsp70 inhibitors having a novel structure and a high activity, solve the problem concerning drug resistance of tumors, enhance the effect of treating tumors, and provide a new medical strategy for treatment of tumors in clinic. ##STR00001##