200214-48-8

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 89951-56-4 4-chloro-5-hydroxymethyl aniline 
• 80866-80-4 2-chloro-5-nitrobenzyl alcohol 
• 89-54-3 2-chloro-5-aminobenzoic acid 
• 543-27-1 isobutyl chloroformate 
• 6361-21-3 2-chloro-5-nitrobenzaldehyde 
• 64401-55-4 5-amino-2-chloro-benzoic acid ethyl ester 

Downstream Products

• 1228658-06-7 tert-butyl (4-chloro-3-formylphenyl)carbamate 
• 1569737-95-6 tert-butyl N-[4-chloro-3-[(cyclopentylsulfanyl)methyl]phenyl]carbamate 
• 1569737-05-8 N-{4-chloro-3-[(cyclopentylsulfanyl)methyl]phenyl}thiophene-2-carboximidamide 
• 1341693-01-3 4-chloro-3-[(cyclopentylsulfanyl)methyl]aniline 
• 1251929-41-5 tert-butyl N-[3-(bromomethyl)-4-chlorophenyl]carbamate 
• 934477-05-1 C₂₂H₃₀ClN₃O₇S 
• 934477-04-0 2-(5-tert-butoxycarbonylamino-2-chloro-phenyl)-acrylic acid ethyl ester 
• 200214-52-4 ethyl (2-chloro-5-(Boc-amino)phenyl)acetate 
• 200214-50-2 (2-chloro-5-(Boc-amino)phenyl)acetonitrile 
• 409082-02-6 ethyl 2-(5-amino-2-chlorophenyl)acetate 
• 200214-49-9 2-chloro-5-(Boc-amino)benzyl mesylate 

Relevant academic research and scientific papers

New hits as antagonists of GPR103 identified by HTS

Preclinical data indicate that GPR103 receptor and its endogenous neuropeptides QRFP26 and QRFP43 are involved in appetite regulation. A high throughput screening (HTS) for small molecule GPR103 antagonists was performed with the clinical goal to target weight management by modulation of appetite. A high hit rate from the HTS and initial low confirmation with respect to functional versus affinity data challenged us to revise the established screening cascade. To secure high quality data while increasing throughput, the binding assay was optimized on quality to run at single concentration. This strategy enabled evaluation of a larger fraction of chemical clusters and singletons delivering 17 new compound classes for GPR103 antagonism. Representative compounds from three clusters are presented. One of the identified clusters was further investigated, and an initial structure-activity relationship study is reported. The most potent compound identified had a pIC50 of 7.9 with an improved ligand lipophilic efficiency.

BENZOTHIOPHENE SULFONAMIDES AND OTHER COMPOUNDS THAT INTERACT WITH GLUCOKINASE REGULATORY PROTEIN

The present invention relates to benzothiophene sulfonamides and other compounds that interact with glucokinase regulatory protein. In addition, the present invention relates to methods of treating type 2 diabetes, and other diseases and/or conditions where glucokinase regulatory protein is involved using the compounds, or pharmaceutically acceptable salts thereof, and pharmaceutical compositions that contain the compounds, or pharmaceutically acceptable salts thereof.

(PYRAZOL-3-YL)-1,3,4-THIADIAZOL-2-AMINE AND (PYRAZOL-3-YL)-1,3,4-THIAZOL-2-AMINE COMPOUNDS

A compound of Formula (I) wherein: either X is N and Y is CR5 or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and Me; R2 is selected from H, OH, OMe and Me; each R3 is independently selected from C1-3alkyl, F, Cl, Br, CF3 and NH2; R4 is selected from Me, CF3, NO2 and CHF2; R5 is selected from H, Me and CHF2; R6 is selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.

3-Mercaptopropionic acids as efficacious inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa)

A novel series of cyclic potent, selective, small molecule, thiol-based inhibitors of activated thrombin activatable fibrinolysis inhibitor (TAFIa) and the crystal structures of TAFIa inhibitors bound to porcine pancreatic carboxypeptidase B are described. Three series of cyclic arginine and lysine mimetic inhibitors vary significantly in their selectivity against other human basic carboxypeptidases, carboxypeptidase N and carboxypeptidase B. (-)2a displays TAFIa IC50 = 3 nM and 600-fold selectivity against CPN. Inhibition of TAFIa with (rac)2a resulted in dose dependent acceleration of human plasma clot lysis in vitro and was efficacious as an adjunct to tPA in an in vivo rabbit jugular vein thrombolysis model.

AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS

There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.