A substituted trans-cycloheptene according to formula (I); wherein: a) Z and L are each selected from the group consisting of SiR.sup.1.sub.R.sup.2, CH.sub.2, CHOH, and CHR.sup.2; R.sup.1 is phenyl or CH.sub.3; R.sup.2 is phenyl, CH.sub.3, (CH.sub.2).sub.nCN, or (CH.sub.2).sub.nOH, wherein n is an integer from 1 to 5; R.sup.a and R.sup.b are each individually selected from the group consisting of H, OH, and CH.sub.3; and Z and L are not both SiR.sup.1R.sup.2; or b) Z is BocN, L is CH.sub.2, R.sup.a is H, and R.sup.b is H; or c) Z is C=0, L is CH.sub.2, R.sup.a is H, and R.sup.b is H.

##STR00001##

This invention relates to novel compounds of formula (I). The compounds of the invention are hedgehog pathway antagonists. Specifically, the compounds of the invention are useful as Smoothened (SMO) inhibitors. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of the Hedgehog pathway and SMO, for example cancer.

This invention relates to novel compounds of formula (I). The compounds of the invention are hedgehog pathway antagonists. Specifically, the compounds of the invention are useful as Smoothened (SMO) inhibitors. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of the Hedgehog pathway and SMO, for example cancer.

This application discloses compounds according to generic Formula I: (I) wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient. ##STR00001##

The present disclosure provides compounds and methods useful for inhibiting SARM1 and/or treating and/or preventing neurodegenerative disease or axonal degeneration. The provided SARM1 inhibitors may reduce or inhibit binding of NAD+ by SARM1. Alternatively, provided SARM1 inhibitors bind to SARM1 within a pocket comprising one or more catalytic residues (e.g., a catalytic cleft of SARM1).

The present disclosure provides compounds and methods useful for inhibiting SARM1 and/or treating and/or preventing neurodegenerative disease or axonal degeneration. The provided SARM1 inhibitors may reduce or inhibit binding of NAD+ by SARM1. Alternatively, provided SARM1 inhibitors bind to SARM1 within a pocket comprising one or more catalytic residues (e.g., a catalytic cleft of SARM1).

A method for a high yield production of a difluoromethyl-substituted aromatic heterocyclic compound having a partial structure represented by formula (II), which includes reacting an N-oxido aromatic heterocyclic compound having a partial structure represented by formula (I) with tetrafluoroethylene in a solvent selected from an aromatic hydrocarbon solvent, an ester solvent, and an ether solvent. ##STR00001##

A method for a high yield production of a difluoromethyl-substituted aromatic heterocyclic compound having a partial structure represented by formula (II), which includes reacting an N-oxido aromatic heterocyclic compound having a partial structure represented by formula (I) with tetrafluoroethylene in a solvent selected from an aromatic hydrocarbon solvent, an ester solvent, and an ether solvent. ##STR00001##

The present invention relates to the compounds of formula (I), and the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof wherein the variables are defined according to description formula (I). The compounds of formula (I), as well as the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof, are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds. ##STR00001##

The present invention relates to the compounds of formula (I), and the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof wherein the variables are defined according to description formula (I). The compounds of formula (I), as well as the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof, are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds. ##STR00001##