Azolobenzazine compounds of the formula I and N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof are disclosed, as well as are methods for controlling invertebrate pests using the disclosed compounds. Further disclosed are plant propagation materials, agricultural compositions, and veterinary compositions that include the disclosed compounds.

##STR00001##

Azolobenzazine compounds of the formula I and N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof are disclosed, as well as are methods for controlling invertebrate pests using the disclosed compounds. Further disclosed are plant propagation materials, agricultural compositions, and veterinary compositions that include the disclosed compounds.

##STR00001##

A compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is LY; each L is a direct bond, C.sub.1-C.sub.10 alkylene, C.sub.2-C.sub.10 alkenylene or C.sub.2-C.sub.10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, halogen, fluoro C.sub.1-C.sub.10 alkyl, O—C.sub.1-C.sub.10 alkyl, NH—C.sub.1-C.sub.10 alkyl, S—C.sub.1-C.sub.10 alkyl, O-fluoro C.sub.1-C.sub.10 alkyl, NH-acyl, NH—C(O)—NH—C.sub.1-C.sub.10 alkyl, C(O)—NH—C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.

A compound of formula I: ##STR00001##
or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is LY; each L is a direct bond, C.sub.1-C.sub.10 alkylene, C.sub.2-C.sub.10 alkenylene or C.sub.2-C.sub.10 alkynylene; Y is an optionally substituted fused, bridged or spirocyclic non-aromatic 5-12 membered heterocycle containing up to 4 heteroatoms selected from N or O; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, halogen, fluoro C.sub.1-C.sub.10 alkyl, O—C.sub.1-C.sub.10 alkyl, NH—C.sub.1-C.sub.10 alkyl, S—C.sub.1-C.sub.10 alkyl, O-fluoro C.sub.1-C.sub.10 alkyl, NH-acyl, NH—C(O)—NH—C.sub.1-C.sub.10 alkyl, C(O)—NH—C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are useful as inhibitors of the class IA phosphoinositide 3-kinase enzyme, PI3K-p110δ, and therefore have potential utility in the therapy of cancer, immune and inflammatory diseases.

The present invention relates to novel substituted pyrazoloazepin-4-ones with phosphodiesterase inhibitory activity, as well as to their use as therapeutic agents in the treatment of inflammatory diseases and conditions.

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.

##STR00001##

Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions.

##STR00001##

Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Described herein are compounds of Formula (XVII) that are TYK2 inhibitors, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of Using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of TYK2 activity. ##STR00001##

Disclosed herein are tetrahydropyranoindole compounds and derivatives thereof, as well as their methods of synthesis and use. The disclosed compounds may be synthesized by methods that utilize a cooperative hydrogen bond donor/Brønsted acid system. The disclosed compounds may be useful for treating a disease, disorder, or a symptom thereof in a subject in need thereof, such as pain, swelling, and joint stiffness. The disclosed compounds also may be useful for treating cell proliferative diseases and disorders such as cancer.

Provided are any one novel compound selected from the group consisting of 9-deoxo-36,37-dihydro-prolyl FK506, 9-deoxo-31-O-demethyl-36,37-dihydro-prolyl FK506, 9-deoxo-prolyl FK520, and 9-deoxo-31-O-demethyl-prolyl FK520, and use thereof.