C07C233/66

PROCESS FOR DEOXYFLUORINATION OF PHENOLS

The present invention refers to a process for transition-metal-assisted .sup.18F-deoxyfluorination of phenols. The transformation benefits from readily available phenols as starting materials, tolerance of moisture and ambient atmosphere, large substrate scope, and translatability to generate doses appropriate for positron emission tomography (PET) imaging.

Heterocyclic Ligands of PAR1 and Methods of Use

The present invention provides novel compounds with increased plasma stability that modulate PAR1 signaling, and methods of using them. The present invention provides methods of using the novel PAR1 modulators for the treatment of a number of disorders, including, inflammation, thrombosis, kidney disease, sepsis, stroke, as well as proliferation-related diseases. Furthermore, the PAR1 modulators of the present invention provide cytoprotection for certain cells and tissues, for example, in coronary blood vessels and tissues after a heart attack.

Heterocyclic Ligands of PAR1 and Methods of Use

The present invention provides novel compounds with increased plasma stability that modulate PAR1 signaling, and methods of using them. The present invention provides methods of using the novel PAR1 modulators for the treatment of a number of disorders, including, inflammation, thrombosis, kidney disease, sepsis, stroke, as well as proliferation-related diseases. Furthermore, the PAR1 modulators of the present invention provide cytoprotection for certain cells and tissues, for example, in coronary blood vessels and tissues after a heart attack.

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPASE

Compounds of general formula IA, IB and IC outlined below, including pharmaceutically acceptable salts, solvates and hydrates thereof. Such compounds and pharmaceutical compositions comprising them may be used in medical conditions involving Ran GTPase.

##STR00001##

COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USE THEREOF AS INHIBITORS OF RAN GTPASE

Compounds of general formula IA, IB and IC outlined below, including pharmaceutically acceptable salts, solvates and hydrates thereof. Such compounds and pharmaceutical compositions comprising them may be used in medical conditions involving Ran GTPase.

##STR00001##

Endoparasite control agent

The present invention is intended to provide a novel parasiticide, antiprotozoal or other endoparasite control agents which are effective for controlling animal endoparasites that have been impossible to control by conventional ones. Provided is an endoparasite control agent comprising, as an active ingredient, a carboxamide derivative represented by the general formula (I): ##STR00001##
or a salt thereof.

Endoparasite control agent

The present invention is intended to provide a novel parasiticide, antiprotozoal or other endoparasite control agents which are effective for controlling animal endoparasites that have been impossible to control by conventional ones. Provided is an endoparasite control agent comprising, as an active ingredient, a carboxamide derivative represented by the general formula (I): ##STR00001##
or a salt thereof.

Inhibitors of human phosphatidylinositol 3-kinase delta

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity. Methods of using PI3K inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K inhibitory compounds to inhibit PI3K-mediated processes in vitro and in vivo.

Inhibitors of human phosphatidylinositol 3-kinase delta

Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K) activity, and methods of treating diseases, such as disorders of immunity and inflammation, in which PI3K plays a role in leukocyte function are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K activity, including compounds that selectively inhibit PI3K activity. Methods of using PI3K inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K inhibitory compounds to inhibit PI3K-mediated processes in vitro and in vivo.

COMPOUNDS AND METHODS FOR INDUCING CHONDROGENESIS

Described herein are compounds and compositions for the amelioration of arthritis or joint injuries by inducing mesenchymal stem cells into chondrocytes.