866930-93-0

Upstream product

• 68837-59-2 4-bromo-2-methylbenzoic acid 
• 17100-58-2 4-bromo-2-methylbenzyl alcohol 
• 24078-15-7 4-bromo-1-(chloromethyl)-2-methylbenzene 
• 215800-05-8 2-(4-bromo-2-methylphenyl)acetonitrile 
• 116632-39-4 2-methyl-4-bromoiodobenzene 
• 853796-39-1 2-(4-bromo-2-methyl-phenyl)acetic acid 
• 943741-00-2 4-bromo-2-methyl-1-vinylbenzene 
• 866930-92-9 (4-bromo-2-methyl-phenyl)-acetic acid tert-butyl ester 

Downstream Products

• 943741-36-4 (S)-ethyl 3-(benzyloxycarbonylamino)-3-(3-((4-bromo-2-methylphenethoxy)carbonylamino)phenyl)propanoate 
• 916516-95-5 4-bromo-1-(2-iodo-ethyl)-2-methyl-benzene 
• 943741-05-7 4-(2-(3-cyanophenylcarbamoyloxy)ethyl)-3-methylphenylboronic acid 

Relevant academic research and scientific papers

Atropisomer Control in Macrocyclic Factor VIIa Inhibitors

Incorporation of a methyl group onto a macrocyclic FVIIa inhibitor improves potency 10-fold but is accompanied by atropisomerism due to restricted bond rotation in the macrocyclic structure, as demonstrated by NMR studies. We designed a conformational constraint favoring the desired atropisomer in which this methyl group interacts with the S2 pocket of FVIIa. A macrocyclic inhibitor incorporating this constraint was prepared and demonstrated by NMR to reside predominantly in the desired conformation. This modification improved potency 180-fold relative to the unsubstituted, racemic macrocycle and improved selectivity. An X-ray crystal structure of a closely related analogue in the FVIIa active site was obtained and matches the NMR and modeled conformations, confirming that this conformational constraint does indeed direct the methyl group into the S2 pocket as designed. The resulting rationally designed, conformationally stable template enables further optimization of these macrocyclic inhibitors.

C-LINKED HYDROXAMIC ACID DERIVATIVES USEFUL AS ANTIBACTERIAL AGENTS

The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.

MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS

The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.

Alkyne compounds with MCH antagonistic activity and medicaments comprising these compounds

Alkyne compounds having MCH-receptor antagonistic activity, which are useful for preparing pharmaceutical compositions for the treatment of metabolic disorders and/or eating disorders, particularly obesity and diabetes.

NOVEL ALKYNE COMPOUNDS WITH AN MCH-ANTAGONISTIC ACTION AND MEDICAMENTS COMPRISING SAID COMPOUNDS

The invention relates to individual alkyne compounds with an antagonistic action against the MCH-receptor. Said compounds are suitable for producing medicaments for the treatment of metabolic disorders and/or eating disorders, in particular adiposity and diabetes.