Disclosed herein are compounds of Formula (I), methods of synthesizing compounds of Formula (I), and methods of using compounds of Formula (I) as an analgesic.

Disclosed herein are compounds of Formula (I), methods of synthesizing compounds of Formula (I), and methods of using compounds of Formula (I) as an analgesic.

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 compounds of formulae: ##STR00001##
and pharmaceutically acceptable salts thereof, wherein the variables, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.11, R.sub.12, R.sub.13, R.sub.14, R.sub.15, R.sub.16, R.sub.17, n, and m are defined herein. These compounds are useful for treating Gram-negative bacteria infections. Also disclosed are methods of making these compounds.

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-OC.sub.1-C.sub.3 alkyl, or when A.sub.2 is C, R.sup.6 can also be C.sub.1-C.sub.4alkoxy 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-OC.sub.1-C.sub.3 alkyl, or when A.sub.2 is C, R.sup.6 can also be C.sub.1-C.sub.4alkoxy 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.

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.

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.