588679-10-1

Upstream product

• 105-39-5 chloroacetic acid ethyl ester 
• 3964-56-5 4-bromo-2-chlorophenol 
• 105-36-2 ethyl bromoacetate 

Downstream Products

• 689300-67-2 (2-chloro-4-furan-2-yl-phenoxy)-acetic acid ethyl ester 
• 497081-40-0 2-(4'-bromo-2'-chlorophenoxy)-N-(4'-sulfamoylphenyl)acetamide 
• 587841-73-4 2-(4-Bromo-2-chlorophenoxy)-N-[[[4-[[(4,6-dimethyl-2-pyrimidinyl)amino]sulfonyl]phenyl]amino]thioxomethyl]acetamide 
• 1449004-69-6 2-(4-bromo-2-chlorophenoxy)-N-(3-(N-(N-carbobenzoxy-L-leucyl)-sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-68-5 2-(4-bromo-2-chlorophenoxy)-N-(3-(N-(N-carbobenzoxy-L-phenylalanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-67-4 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-Lisoleucyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-66-3 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-tert-butoxycarbonyl-Lleucyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-65-2 N-(4-(N-(N-carbobenzoxy-(L-leucyl))-sulfamoyl)phenylcarbamothioyl)-2-(4-bromo-2-chlorophenoxy)acetamide 
• 1449004-64-1 N-(4-(N-(L-leucyl)sulfamoyl)-phenylcarbamothioyl)-2-(4-bromo-2-chlorophenoxy) acetamide 
• 1449004-38-9 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-Ltryptophanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-37-8 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-L-3-(4-nitrophenyl)alanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-36-7 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-Lphenylalanyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-35-6 2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-tert-butoxycarbonyl-L-(2-phenyl)glycyl)sulfamoyl)phenylcarbamothioyl)acetamide 
• 1449004-34-5 (S)-2-(4-bromo-2-chlorophenoxy)-N-(4-(N-(N-carbobenzoxy-2-(4-acetoxyphenyl)glycyl)sulfamoyl)phenylcarbamothioyl)acetamide 

Relevant academic research and scientific papers

Discovery, synthesis and biological characterization of a series of: N -(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1 H -pyrazol-5-yl)acetamide ethers as novel GIRK1/2 potassium channel activators

The present study describes the discovery and characterization of a series of N-(1-(1,1-dioxidotetrahydrothiophen-3-yl)-3-methyl-1H-pyrazol-5-yl)acetamide ethers as G protein-gated inwardly-rectifying potassium (GIRK) channel activators. From our previous lead optimization efforts, we have identified a new ether-based scaffold and paired this with a novel sulfone-based head group to identify a potent and selective GIRK1/2 activator. In addition, we evaluated the compounds in tier 1 DMPK assays and have identified compounds that display nanomolar potency as GIRK1/2 activators with improved metabolic stability over the prototypical urea-based compounds. This journal is

Design and synthesis of α-phenoxy-N-sulfonylphenyl acetamides as Trypanosoma brucei Leucyl-tRNA synthetase inhibitors

Human African trypanosomiasis (HAT), caused by the parasitic protozoa Trypanosoma brucei, is one of the fatal diseases in tropical areas and current medicines are insufficient. Thus, development of new drugs for HAT is urgently needed. Leucyl-tRNA synthetase (LeuRS), a recently clinically validated antimicrobial target, is an attractive target for development of antitrypanosomal drugs. In this work, we report a series of α-phenoxy-N-sulfonylphenyl acetamides as T. brucei LeuRS inhibitors. The most potent compound 28g showed an IC50 of 0.70 μM which was 250-fold more potent than the starting hit compound 1. The structure-activity relationship was also discussed. These acetamides provided a new scaffold and lead compounds for the further development of clinically useful antitrypanosomal agents.

Cdc42 Inhibitor and Uses Thereof

Compounds which inhibit the small G protein Rho GTPase cell division cycle protein Cdc42 are provided. Morphological analyses of filopodia, western blots of Ccd42 phosphorylation, and effects on cellular wound healing and on growth cone formation all demo

Discovery of N-(4-sulfamoylphenyl)thioureas as Trypanosoma brucei leucyl-tRNA synthetase inhibitors

Human African trypanosomiasis (HAT) is one of the most neglected diseases in the tropic regions, which is fatal if not treated in time. There is an urgent need for new therapeutics, especially those in new chemical classes. Leucyl-tRNA synthetase (LeuRS) has been paid much attention as a recently clinically validated antimicrobial target. Our group has previously reported T. brucei LeuRS (TbLeuRS) inhibitors, including benzoxaboroles targeting the editing site and pyrrolinones targeting the synthetic site. Here we report the discovery of N-(4-sulfamoylphenyl)thioureas as a new class of TbLeuRS inhibitors. The R1 and R2 groups, reminiscent of the leucyl and adenyl regions of aa-AMP and aa-AMS, were optimized to result in a significant 13-fold increase of inhibitory activity (compound 19, IC 50 = 13.7 μM). Aided by ligand-protein docking, the 1,3-substitution at the central phenyl ring was predicted and proved to give significantly improved activity (59, IC50 = 1.1 μM). This work provided a new scaffold for the exploration of novel inhibitors against TbLeuRS, which may become potential therapeutics for the treatment of HAT.

COMPOUNDS THAT INHIBIT HIF-1 ACTIVITY, THE METHOD FOR PREPARATION THEREOF AND THE PHARMACEUTICAL COMPOSITION CONTAINING THEM AS AN EFFECTIVE COMPONENT

Disclosed herein are an HIF-1 inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient. The HIF-1 inhibitor shows anticancer activity thanks to the inhibition activity against HIF-1, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer; stomach cancer and breast cancer. Also, the compound having inhibition activity against HIF-1 is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HIF-1-mediated VEGF expression.

COMPOUNDS TEAT INHIBIT HBF-I ACTIVITY, THE METHOD FOR PREPARATION THEREOF AND THE PHARMACEUTICAL COMPOSITION CONTAINING THEM AS AN EFFECTIVE COMPONENT

Disclosed herein are an HIF-I inhibitor, a method for the preparation thereof, and a pharmaceutical composition comprising the same as an active ingredient The BDDF-I inhibitor shows anticancer activity thanks to the inhibition activity against HIF-I, a transcription factor which plays an important role in the growth and metastasis of cancer, but not to general cytotoxicity. Thus, the HIF-inhibitor and a pharmaceutically acceptable salt thereof can be used as a therapeutic for various cancers such as liver cancer, stomach cancer and breast cancer. Also, the compound having inhibition activity against HDDF-I is useful in the treatment of diabetic retinopathy and arthritis, which are aggravated by HEF-l-mediated VEGF expression.

AMINO ALCOHOL DERIVATIVE, MEDICINAL COMPOSITION CONTAINING THE SAME, AND USE OF THESE

The present invention provides compounds represented by general formula (I): a prodrug thereof, or pharmaceutical acceptable salts thereof, wherein R1 is hydrogen or lower alkyl; each of R2 and R3 is independently hydrogen or lower alkyl; each of R4, R5 and R6 is independently hydrogen, halogen, lower alkyl or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogen, lower alkyl, lower alkoxy, etc; R9 is -COR10, -A1-COR10, -O-A2-COR10, etc; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, -OCH2-, etc, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

AMINO ALCOHOL DERIVATIVES, PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME, AND USE THEREOF

The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen or lower alkyl; R3 R4, R5 and R6 are each hydrogen, halogen, lower alkyl or lower alkoxy; R7 and R8 are each hydrogen, halogen, lower alkyl, halo-lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, a hydroxyl group, lower acyl, carboxy or the like; R9 is -C(O)-R10, -A1-C(O)-R10, -O-A2-C(O)-R10 or a tetrazol-5-yl group, which exhibit potent and selective β3-adrenoceptor stimulating activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.

NOVEL AMIDE COMPOUNDS WITH MCH ANTAGONISTIC EFFECT AND MEDICAMENTS COMPRISING SAID COMPOUNDS

The invention relates to amide compounds of general formula (I), in which the groups and residues A, B, b, W, X, Y, Z, R1, R2 and R3 have the meanings given in claim 1. The invention further relates to medicaments comprising at least one of said amides. Said medicaments are suitable for the treatment of metabolic disorders and/or eating disorders, in particular, obesity, bulimia, anorexia, hyperphagia, and diabetes as a result of the MCH receptor antagonism.