73017-76-2

Upstream product

• 3637-61-4 1-amino-cyclopentanemethanol 
• 124-63-0 methanesulfonyl chloride 
• 162167-97-7 tert-butyl 3-(aminomethyl)piperidine-1-carboxylate 

Downstream Products

• 847063-78-9 methyl 3-(4-cyclopentylmethyloxyphenyl)Propionate 
• 243861-74-7 2-cyclopentylmethyl-4-ethoxycarbonyl-6-(4-methoxyphenyl)-2H-pyridazin-3-one 
• 455256-35-6 (azidomethyl)cyclopentane 
• 4492-51-7 1-cyclopentanemethyl-N-methylamine 
• 1215077-02-3 (3-bromophenyl)(cyclopentylmethyl)sulfane 
• 280583-54-2 1-(2-chloro-4-(cyclopentylmethyloxy)benzyl)-6-(ethoxycarbonyl)-2-methylbenzimidazole> 

Relevant academic research and scientific papers

On the mechanism of the dyotropic expansion of hydrindanes into decalins

A combined computational/experimental approach has revealed key mechanistic aspects in a recently reported dyotropic expansion of hydrindanes into decalins. While computer simulations had already anticipated the need for acid catalysis for making this reaction feasible under the mild conditions used in the laboratory, this work places the dyotropic step not into the reaction flask but at a later step, during the work up instead. With this information in hand the reaction has been optimized by exploring the performance of different activating agents and shown to be versatile, particularly in steroid related chemistry due to the two scaffolds that this reaction connects. Finally, the scope of the reaction has been significantly broadened by showing that this protocol can also operate in the absence of the fused six-member ring.

Design, synthesis and biological evaluation of pyrazolo[3,4-d]pyrimidine-based protein kinase D inhibitors

The multiple roles of protein kinase D (PKD) in various cancer hallmarks have been repeatedly reported. Therefore, the search for novel PKD inhibitors and their evaluation as antitumor agents has gained considerable attention. In this work, novel pyrazolo[3,4-d]pyrimidine based pan-PKD inhibitors with structural variety at position 1 were synthesized and evaluated for biological activity. Starting from 3-IN-PP1, a known PKD inhibitor with IC50 values in the range of 94–108 nM, compound 17m was identified with an improved biochemical inhibitory activity against PKD (IC50 = 17–35 nM). Subsequent cellular assays demonstrated that 3-IN-PP1 and 17m inhibited PKD-dependent cortactin phosphorylation. Furthermore, 3-IN-PP1 displayed potent anti-proliferative activity against PANC-1 cells. Finally, a screening against different cancer cell lines demonstrated that 3-IN-PP1 is a potent and versatile antitumoral agent.

Phenyl-substituted dihydronaphthyridine compound and application thereof (by machine translation)

The invention relates to a phenyl-substituted dihydronaphthyridine compound and application thereof, and further relates to a pharmaceutical composition containing the compound. The compounds or pharmaceutical compositions of the present invention may be used as a mineralocorticoid receptor antagonist. (by machine translation)

Conformational Aspects in the Design of Inhibitors for Serine Hydroxymethyltransferase (SHMT): Biphenyl, Aryl Sulfonamide, and Aryl Sulfone Motifs

Malaria remains a major threat to mankind due to the perpetual emergence of resistance against marketed drugs. Twenty-one pyrazolopyran-based inhibitors bearing terminal biphenyl, aryl sulfonamide, or aryl sulfone motifs were synthesized and tested towards serine hydroxymethyltransferase (SHMT), a key enzyme of the folate cycle. The best ligands inhibited Plasmodium falciparum (Pf) and Arabidopsis thaliana (At) SHMT in target, as well as PfNF54 strains in cell-based assays in the low nanomolar range (18–56 nm). Seven co-crystal structures with P. vivax (Pv) SHMT were solved at 2.2–2.6 ? resolution. We observed an unprecedented influence of the torsion angle of ortho-substituted biphenyl moieties on cell-based efficacy. The peculiar lipophilic character of the sulfonyl moiety was highlighted in the complexes with aryl sulfonamide analogues, which bind in their preferred staggered orientation. The results are discussed within the context of conformational preferences in the ligands.

SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF

Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.

QUINOLINE DERIVATIVES AS RENIN INHIBITORS

A compound of formula (I), formula (I) or pharmaceutically acceptable salt thereof, as renin inhibitor, process of preparation thereof, and to the use of the compounds in the preparation of pharmaceutical compositions for the therapeutic treatment of card

4, 6-DISUBSTITUTED 2-AMINO-PYRIMIDINES AS HISTAMINE H4 RECEPTOR MODULATORS

The present invention relates to substituted heterocyclic compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides or quaternary ammonium salts thereof wherein constituent members are provided hereinwith, as well as their compositions and methods of use, which are histamine H4 receptor inhibitors/antagonists useful in the treatment of histamine H4 receptor-associated conditions or diseases or disorders including, for example, inflammatory diseases or disorders, pruritus, and pain.

Imine derivatives as new potent and selective CB2 cannabinoid receptor agonists with an analgesic action

In this study, a novel series of CB2 receptor agonist imine derivatives, 1-6, was synthesized and evaluated for activity against the CB2 receptor. In a previous paper we reported the synthesis and SARs of thiazole derivative 1, a pot

Heteroaromatic Glucokinase Activators

The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, of Formula (I) wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; p

OXAZOLE COMPOUND AND PHARMACEUTICAL COMPOSITION

ABSTRACT The present invention provides a oxazole compound represented by Formula (1), or a salt thereof: wherein R1 is an aryl group which may have one or more substituents; R2 is an aryl group or a nitrogen atom-containing heterocyclic group each of which may have one or more substituents; and W is a divalent group represented by -Y1-A1- or -Y2-C(=O)- wherein Y1 is a group such as -C(=O)-, A1 is a group such as a lower alkylene group, and Y2 is a group such as a piperazinediyl group. The oxazole compound has a specific inhibitory action against phosphodiesterase 4.