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Carbocyclic side chain containing metalloprotease inhibitors
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A kind of technology of heterocycle and cycloalkyl, applied in the field of metalloprotease inhibitors containing carbocyclic side chain
Inactive Publication Date: 2003-05-14
THE PROCTER & GAMBLE COMPANY
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Summary
Abstract
Description
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Application Information
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Problems solved by technology
Although various MP inhibitors have been prepared, there remains a need for potent inhibitors of matrix metalloproteinases for the treatment of such diseases associated with metalloprotease activity
Method used
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[0177] VII Example - Preparation of Compounds
[0178] The following abbreviations are used in this document:
[0186] The R groups used to describe the compound examples are independent of the individual R groups used to describe the various moieties of formula (I). That is, for example, R used to describe formula (I) in the Summary of the Invention section and the Detailed Description section II 1 , R 2 and R 3 Not denoted with the R in this section VII 1 , R 2 and R 3 same.
Embodiment 1-23
[0188] The following substructures and tables show the structures of compounds prepared according to the methods described in Examples 1-23. In these compounds, according to formula (I), A is cyclohexane, R 1 is -OH, n=0.
Embodiment 1
[0190] Preparation of N-{[4'-methoxy-(1,1'-biphenyl)-4-yl]-sulfonylamino}-(4-hydroxycyclohex-1-yl)-acetic acid
[0191] a. (R)-(4-Hydroxycyclohex-1-yl)-aminoacetic acid: starting D-4-hydroxyphenylglycine (glycene) (10 g, 59.8 mmol) in 10 mL 50% NaOH and 25 g Raney nickel Placed in 180mL of water in the presence of The mixture was pressurized at about 100 psi of hydrogen at 80° C. for 3 days, filtered through celite, and concentrated to about half the original volume.
[0192] b. (R)-N-{[4'-methoxy-(1,1'-biphenyl)-4-yl]-sulfonyl}-amino-(4-hydroxyl-cyclohex-1-yl )-methyl acetate: Dilute the crude amino acid 1a solution with 100 mL of dioxane and 10 mL of triethylamine, and wash with [4′-methoxy-(1,1′-biphenyl)-4-yl]-sulfonylchloride ( 18.6g, 65.8mmol) treatment. The resulting solution was stirred for 12 hours, then concentrated to about half its original volume and acidified with concentrated hydrochloric acid. The resulting white precipitate was washed with water and dried...
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Abstract
The present invention discloses compounds which are inhibitors of metalloproteases which are effective in the treatment of conditions characterized by excess activity of these enzymes. Specifically, the compound has the structure of formula (I), wherein R 1 , R 2 , n, A, E, E', L, L', G and Z have the meanings described in the specification and claims. Optical isomers, diastereomers and enantiomers of the compound of formula (I) and pharmaceutically acceptable salts thereof, and biohydrolyzable amides, esters and imides thereof are also disclosed. The invention also describes pharmaceutical compositions containing these compounds, and methods of treating diseases associated with metalloproteases using the compounds or pharmaceutical compositions.
Description
[0001] cross reference [0002] This application claims priority under Title 35 of USC 119(e) to Provisional Application Serial No. 60 / 191,059 filed March 21,2000. technical field [0003] The present invention relates to compounds useful in the treatment of diseases associated with the activity of metalloproteases, especially zinc-containing metalloproteases. The present invention also relates to a pharmaceutical composition comprising the compound, and a method for treating metalloprotease-related diseases with the compound or the pharmaceutical composition. Background of the invention [0004] There are many structurally related metalloproteases that destroy structural proteins. These metalloproteases normally act on the intercellular matrix, so they are involved in the destruction and remodeling of tissues. These proteins are called metalloproteases or MPs. [0005] Several different families of MPs classified by sequence homology have been disclosed in the art. Thes...
Claims
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