2743-05-7

Upstream product

• 2743-06-8 2-[(4-bromobenzyl)-(2-hydroxy-ethyl)-amino]-ethanol 

Downstream Products

• 287201-87-0 1-(4-bromobenzyl)-4-(4-prop-2-ynyloxybenzenesulfonyl)piperidine-4-carboxylic acid ethyl ester 
• 287201-54-1 1-(4-bromobenzyl)-4-(4-but-2-ynyloxybenzenesulfonyl)piperidine-4-carboxylic acid ethyl ester 
• 287201-63-2 1-(4-bromobenzyl)-4-(4-pent-2-ynyloxybenzenesulfonyl)piperidine-4-carboxylic acid ethyl ester 
• 287201-67-6 1-(4-bromobenzyl)-4-(4-oct-2-ynyloxybenzenesulfonyl)piperidine-4-carboxylic acid ethyl ester 
• 212770-76-8 1-(4-bromo-benzyl)-4-(4-methoxy-benzenesulfonyl)-piperidine-4-carboxylic acid ethyl ester 
• 287201-92-7 1-(4-bromobenzyl)-4-[4-(4-morpholin-4-ylbut-2-ynyloxy)benzenesulfonyl]piperidine-4-carboxylic acid ethyl ester 
• 287201-91-6 1-(4-bromobenzyl)-4-[4-(4-morpholin-4-ylbut-2-ynyloxy)benzenesulfonyl]piperidine-4-carboxylic acid 
• 287201-53-0 1-(4-bromobenzyl)-4-(4-but-2-ynyloxybenzenesulfonyl)piperidine-4-carboxylic acid 
• 287201-88-1 1-(4-bromobenzyl)-4-(4-prop-2-ynyloxybenzenesulfonyl)piperidine-4-carboxylic acid 

Relevant academic research and scientific papers

ALKYNYL CONTAINING HYDROXAMIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE AS MATRIX METALLOPROTEINASE (MMP) INHIBITORS / TNF-ALPHA CONVERTING ENZYME (TACE) INHIBITORS

Compounds of the formula:useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.

N-HYDROXY-2-(ALKYL, ARYL, OR HETEROARYL SULFANYL, SULFINYL OR SULFONYL)-3-SUBSTITUTED ALKYL, ARYL OR HETEROARYLAMIDES AS MATRIX METALLOPROTEINASE INHIBITORS

Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF- alpha converting enzymes (TACE), a pro-inflammatory cytokine, catalyze the formation of TNF- alpha from membrane-bound TNF- alpha precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF- alpha converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection. The compounds of this invention are represented by formula (I), where R, R, R and R are described herein.

N-hydroxy-2-(Alkyl,Aryl or Heteroaryl sulfanyl, sulfinyl or sulfonyl) 3-substituted alkyl, aryl or heteroarylamides as matrix metalloproteinase inhibitors

Matrix metalloproteinases (MMps) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-α converting enzyme (TACE), a pro-inflammatory cytokine, catalyzes the formation of TNF-α from membrane bound TNF-α precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states. The present invention provides low molecular weight, non-peptide inhibitors of matrix metalloproteinases (MMPs) and TNF-α converting enzyme (TACE) for the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection. The compounds of this invention are represented by the formula where R1, R2, R3and R4are described herein.