The present invention discloses an oxime ether compound with novel structure. The structure is shown in general formula I. The definition of each substituent in the formula is provided in the description. ##STR00001## The compound of general formula I has excellent microbicidal 1 activity, and has good control effects on plant bacterial diseases and fungal diseases. The present invention comprises an application of the compound of the general formula I as a microbicide in agriculture and other fields.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

The present invention relates to novel sulfur derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.

Disclosed are novel compounds of Formula I that are cGAS antagonists, methods of preparation of the compounds, pharmaceutical compositions comprising the compounds, and their use in medical therapy.

Compounds of the formula II: ##STR00001## wherein R.sup.1 and R.sup.2 are independently H, F or CH.sub.3; or R.sup.1 forms an ethynyl bond and R.sup.2 is H or C.sub.3-C.sub.6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF.sub.3, OMe or halo; R.sup.3 is C.sub.1-C.sub.3 alkyl or C.sub.3-C.sub.6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R.sup.3 is C.sub.3-C.sub.6 cycloalkyl it may alternatively be gem subsituted with fluoro; R.sup.4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A.sub.1 is CH or N, A.sub.2 is CR.sup.6R7 or NR.sup.6, provided at least one of A.sub.1 and A.sub.2 comprises N; R.sup.6 is H, C.sub.1-C.sub.4 alkyl, C.sub.1-C.sub.4 haloalkyl, C.sub.1-C.sub.3 alkyl-O-C.sub.1-C.sub.3 alkyl, or when A.sub.2 is C, R.sup.6 can also be C.sub.1-C.sub.4 alkoxy or F; R.sup.7 is H, C.sub.1-C.sub.4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

Compounds of the formula II: ##STR00001## wherein R.sup.1 and R.sup.2 are independently H, F or CH.sub.3; or R.sup.1 forms an ethynyl bond and R.sup.2 is H or C.sub.3-C.sub.6 cycloalkyl which is optionally substituted with one or two substituents independently selected from methyl, CF.sub.3, OMe or halo; R.sup.3 is C.sub.1-C.sub.3 alkyl or C.sub.3-C.sub.6 cycloalkyl, either of which is optionally substituted with one or two methyl and/or a fluoro, trifluoromethyl or methoxy, when R.sup.3 is C.sub.3-C.sub.6 cycloalkyl it may alternatively be gem subsituted with fluoro; R.sup.4 is methyl or fluoro; m is 0, 1 or 2; E is a bond, or thiazolyl, optionally substituted with methyl or fluoro; A.sub.1 is CH or N, A.sub.2 is CR.sup.6R7 or NR.sup.6, provided at least one of A.sub.1 and A.sub.2 comprises N; R.sup.6 is H, C.sub.1-C.sub.4 alkyl, C.sub.1-C.sub.4 haloalkyl, C.sub.1-C.sub.3 alkyl-O-C.sub.1-C.sub.3 alkyl, or when A.sub.2 is C, R.sup.6 can also be C.sub.1-C.sub.4 alkoxy or F; R.sup.7 is H, C.sub.1-C.sub.4 alkyl or F or a pharmaceutically acceptable salt, N-oxide or hydrate thereof, have utility in the treatment of disorders characterized by inappropriate expression or activation of cathepsin K, such as osteoporosis, osteoarthritis, rheumatoid arthritis or bone metastases.

The present invention relates to a process for the preparation 2-chloro-1-(2-chlorothiazol-5-yl)ethanone.

Compounds of formula (I):
A-B-D-E
or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is monocyclic and bicyclic heteroaryl; B is alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl, or alkylene; D is aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine, or sulfamoyl; and E is aryl, heteroaryl, cycloalkyl, or heterocyclyl. These compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).

Compounds of formula (I):
A-B-D-E
or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is monocyclic and bicyclic heteroaryl; B is alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl, or alkylene; D is aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine, or sulfamoyl; and E is aryl, heteroaryl, cycloalkyl, or heterocyclyl. These compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5).

The present inventors have shown that specific benzene sulfonamide thiazole compounds (I) have the ability to induce an early endoplasmic reticulum stress. These compounds also lead to cancerous cells growth inhibition and death.

##STR00001##