135545-01-6

Upstream product

• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 41153-30-4 Boc-Phe(p-F) 
• 543-27-1 isobutyl chloroformate 
• 1117-97-1 N,0-dimethylhydroxylamine 

Downstream Products

• 135544-90-0 (S)-tert-butyl (1-(4-fluorophenyl)-3-oxopropan-2-yl)carbamate 
• 149267-74-3 (S)-tert-butyl (1-(4-fluorophenyl)-3-hydroxypropan-2-yl)carbamate 
• 135544-92-2 (5S,3E)-5-t-butoxycarbonylamino-6-(4-fluorophenyl)-1-trimethylsilylhex-3-en-1-yne 
• 135545-02-7 (5S,3Z)-5-t-butoxycarbonylamino-6-(4-fluorophenyl)-1-trimethylhex-3-en-1-yne 
• 135544-94-4 (5S,3E)-5-t-butoxycarbonylamino-6-(4-fluorophenyl)hex-3-enoic acid 
• 949897-97-6 5-[1,2]Dithiolan-3-yl-pentanoic acid {(S)-1-[(S)-2-ethylcarbamoyl-1-(4-fluoro-benzyl)-2-hydroxy-ethylcarbamoyl]-2-methyl-propyl}-amide 
• 949897-56-7 (S)-2-Amino-N-[(S)-2-ethylcarbamoyl-1-(4-fluoro-benzyl)-2-hydroxy-ethyl]-3-methyl-butyramide 

Relevant academic research and scientific papers

CALPAIN MODULATORS AND THERAPEUTIC USES THEREOF

Disclosed herein are small molecule calpain modulator compositions, pharmaceutical compositions, the use and preparation thereof.

Design and synthesis of fused tetrahydroisoquinoline-iminoimidazolines

In the aim of identifying new privileged structures, we describe the 5-steps synthesis of cyclic guanidine compounds "tetrahydroisoquinoline-iminoimidazolinesg" derived from tetrahydroisoquinoline-hydantoin core. In order to evaluate this new minimal structure and the impact of replacing a carbonyle by a guanidine moiety, their affinity towards adenosine receptor A2A was evaluated and compared to those of tetrahydroisoquinoline-hydantoin compounds.

Novel cell-penetrating α-keto-amide calpain inhibitors as potential treatment for muscular dystrophy

Dipeptide-derived α-keto-amide compounds with potent calpain inhibitory activity have been identified. These reversible covalent inhibitors have IC50 values down to 25 nM and exhibit greatly improved activity in muscle cells compared to the reference compound MDL28170. Several novel calpain inhibitors have shown positive effects on histological parameters in an animal model of Duchenne muscular dystrophy demonstrating their potential as a treatment option for this fatal disease.

Piperizinones as modulators of chemokine receptor activity

The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF BRADYKININ ANALOGUES WITH Ψ(E,CH=CH) AND Ψ(CH2-NH) ISOSTERIC PEPTIDE BOND REPLACEMENTS

The synthesis of bradykinin analogues is described in which the Gly4-Phe5, Phe5-Ser6 or the Pro7-Phe8 peptide bond has been replaced by a trans carbon-carbon double bond or by a "reduced" peptide bond.Some of the analogues display high potency and prolonged activity in the rat blood pressure test, indicating increased metabolic stability.A clear selectivity is obtained towards the myotropic effect in the guinea pig ileum.