1208075-10-8

Upstream product

• 176225-10-8 4-bromo-2-(trifluoromethyl)benzene-1-sulfonyl chloride 

Downstream Products

• 1252637-46-9 (2S,4R)-4-[4-(2-methylpyridin-4-yl)-2-trifluoromethylbenzenesulfonyl]-1-(1-trifluoromethylcyclopropanecarbonyl)pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1434818-59-3 (2S,4R)-4-[4-(2-methylpyridin-4-yl)-2-trifluoromethylphenylsulfanyl]-1-(1-trifluoromethylcyclopropanecarbonyl)pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1252637-35-6 (2S,4R)-4-[4-(1-methyl-1H-pyrazol-4-yl)-2-trifluoromethyl-benzenesulfonyl]-1-(1-trifluoromethyl-cyclopropanecarbonyl)-pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1434818-70-8 (2S,4R)-4-[4-(1-methyl-1H-pyrazol-4-yl)-2-trifluoromethylphenylsulfanyl]-1-(1-trifluoromethylcyclopropanecarbonyl)pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1252637-66-3 (2S,4R)-1-(1-methylcyclopropanecarbonyl)-4-[4-(2-methylpyridin-4-yl)-2-trifluoromethylbenzenesulfonyl]pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1434818-81-1 (2S,4R)-1-(1-methylcyclopropanecarbonyl)-4-[4-(2-methyl-pyridin-4-yl)-2-trifluoromethylphenylsulfanyl]pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)-amide 
• 1434817-47-6 3-(4-bromo-2-trifluoromethyl-phenylsulfanyl)propionamide 
• 1252637-47-0 (2S,4R)-1-(1-methylcyclopropanecarbonyl)-4-[4-(2-methylpyridin-4-yl)-2-trifluoromethylbenzenesulfonyl]pyrrolidine-2-carboxylic acid (1-cyanocyclopropyl)amide 
• 1434817-59-0 3-[4-(1-methyl-1H-pyrazol-4-yl)-2-trifluoromethylphenylsulfanyl]propionamide 
• 1434817-41-0 3-[4-(2-methylpyridin-4-yl)-2-trifluoromethylphenylsulfanyl]propionamide 

Relevant academic research and scientific papers

1-METHYL-4-[(4-PHENYLPHENYL)SULFONYLMETHYL]CYCLOHEXYANOL AND 1-METHYL-4-[[4-(2-PYRIDYL)PHENYL]SULFONYLMETHYL]CYCLOHEXANOL COMPOUNDS AND THEIR THERAPEUTIC USE

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain substituted 1-methyl-4-[(4-phenylphenyl)sulfonylmethyl]cyclohexanol and 1-methyl-4-[[4-(2-pyridyl)phenyl]sulfonylme

N-ACYL-{4-[(4-ARYL-PHENYL)SULFONYLMETHYL]PIPERIDINE} COMPOUNDS AND THEIR THERAPEUTIC USE

The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain N-acyl-{4-[(4-aryl- phenyl)sulfonylmethyl]piperidine} compounds of the following formula (collectively referred to

CYCLIC COMPOUNDS AND USES THEREOF

The invention generally relates to substituted benzothiophenyl, substituted benzothiazolyl, substituted indolyl and substituted benzoimidazolyl compounds and, more particularly, to a compound represented by Structural Formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of a disease or disorder selected from cancer (e.g., lymphoma, such as mantle cell lymphoma), a neurodegenerative disease, inflammatory diseases or an autoimmune system disease (e.g., a T-Cell mediated autoimmune disesase).

PROCESS FOR THE PREPARATION OF 1-ACYL-4-PHENYLSULFONYLPROLINAMIDE DERIVATIVES AND NEW INTERMEDIATES

A novel process for the preparation of proline derivatives of formula (I) wherein,R1 is selected from C1-7-alkyl or from formula (II) wherein R4 is selected from C1-7-alkyl, halogen-C1-7-alkyl or from phenyl which is optionally substituted by halogen; R2 is selected from halogen or halogen-C1-7-alkyl; and R3 is selected from hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy or from a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, the ring which is optionally substituted by C1-7-alkyl or halogen is described. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.

PROCESS FOR THE PREPARATION OF PROLINE DERIVATIVES

The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein, R1 is C1-7-alkyl or wherein R4 is selected from the group consisting of C1-7-alkyl, halogen-C1-7-alkyl and phenyl optionally substituted by halogen; R2 is halogen or halogen-C1-7-alkyl; and R3 is selected from the group consisting of hydrogen, halogen, halogen-C1-7-alkyl, C1-7-alkoxy, halogen-C1-7-alkoxy and a 5- or 6-membered heterocyclic ring containing one or two nitrogen atoms, said ring being optionally substituted by C1-7-alkyl or halogen. The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.

NOVEL CYCLOPENTANE DERIVATIVES

The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

NOVEL PROLINE DERIVATIVES

The invention relates to a compound of formula (I) wherein A, R1-R6 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.