Described herein are substituted indazoles comprising formula (II) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (II) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. ##STR00001##

Described herein are substituted indazoles comprising formula (II) that may selectively bind to Hsp90, methods of using the compounds, and kits including the compounds. Formula (II) may link to detection moieties such as fluorophores that may allow for selective detection of Hsp90 in a sample. ##STR00001##

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.

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.

The present invention relates to compounds of formula (I), ##STR00001## wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

The present invention relates to compounds of formula (I), ##STR00001## wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

The present invention relates to compounds of formula (I),

##STR00001## wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

The present invention relates to compounds of formula (I),

##STR00001## wherein R.sup.1, R.sup.2 and R.sup.3 are as described herein, and their prodrugs or pharmaceutically acceptable salt, enantiomer or diastereomer thereof, and compositions including the compounds and methods of using the compounds.

The present invention relates to certain purines of the following formulae, which act as topoisomerase II catalytic inhibitors: wherein: J is independently: H or NR.sup.N1R.sup.N2; X is independently: O, or S; Q is independently: a covalent bond, C.sub.1-7alkylene, C.sub.2-7alkenylene, C.sub.2-7alkynylene, C.sub.3-7cycloalkylene, C.sub.3-7cycloalkenylene, or C.sub.3-7cycloalkynylene; T is independently: a group A.sup.1 or a group A.sup.2; A.sup.1 is independently: C.sub.6-14carboaryl, C.sub.4-14heteroaryl, C.sub.3-12carbocyclic, or C.sub.3-12heterocyclic; and is independently unsubstituted or substituted; A.sup.2 is independently: H, CN, OH, or O(CO)C.sub.1-7alkyl; R is independently H or a nitrogen ring substituent: R.sup.8 is independently H or a ring substituent; either: each of R.sup.N1 and R.sup.N2 is independently H or a nitrogen substituent; or: R.sup.N1 and R.sup.N2 taken together with the nitrogen atom to which they are attached form a ring having from 3 to 7 ring atoms; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are also useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin.

##STR00001##

The present invention relates to certain purines of the following formulae, which act as topoisomerase II catalytic inhibitors: wherein: J is independently: H or NR.sup.N1R.sup.N2; X is independently: O, or S; Q is independently: a covalent bond, C.sub.1-7alkylene, C.sub.2-7alkenylene, C.sub.2-7alkynylene, C.sub.3-7cycloalkylene, C.sub.3-7cycloalkenylene, or C.sub.3-7cycloalkynylene; T is independently: a group A.sup.1 or a group A.sup.2; A.sup.1 is independently: C.sub.6-14carboaryl, C.sub.4-14heteroaryl, C.sub.3-12carbocyclic, or C.sub.3-12heterocyclic; and is independently unsubstituted or substituted; A.sup.2 is independently: H, CN, OH, or O(CO)C.sub.1-7alkyl; R is independently H or a nitrogen ring substituent: R.sup.8 is independently H or a ring substituent; either: each of R.sup.N1 and R.sup.N2 is independently H or a nitrogen substituent; or: R.sup.N1 and R.sup.N2 taken together with the nitrogen atom to which they are attached form a ring having from 3 to 7 ring atoms; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, N-oxides, chemically protected forms, and prodrugs thereof. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are also useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin.

##STR00001##