189753-93-3

Upstream product

• 676560-15-9 Ethyl (cis/trans)-4-<(tert-butyldimethylsilyl)oxy>cyclohexanecarboxylate 
• 3618-04-0 4-hydroxycyclohexyl carboxylic acid ethyl ester 
• 18162-48-6 tert-butyldimethylsilyl chloride 
• 126781-91-7 methyl 4-{[tert-butyl(dimethyl)silyl]oxy}cyclohexanecarboxylate 
• 69739-34-0 t-butyldimethylsiyl triflate 
• 3618-03-9 methyl 4-hydroxycyclohexanecarboxylate 

Downstream Products

• 126781-92-8 4-[tert-butyldimethylsilyl]oxycyclohexanecarboxaldehyde 
• 1464802-73-0 C₃₀H₅₀N₂O₄Si 
• 1456900-77-8 (3R,6S)-5-ethoxy-6-isopropyl-1-(4-methoxybenzyl)-3-((4-oxocyclohexyl)methyl)-1,6-dihydropyrazin-2(3H)-one 
• 1464802-74-1 C₃₅H₅₂N₂O₅Si 

Relevant academic research and scientific papers

Bcl-2 INHIBITORS

Disclosed herein is a compound of Formula (I) for inhibiting Bcl-2 and treating disease associated with undesirable bcl-2 activity (Bcl-2 related diseases), a method of using the compounds disclosed herein for treating dysregulated apoptotic diseases including cancers and treating autoimmune disease, and a pharmaceutical composition comprising the same.

Substituted Oxopyridine Derivatives and Use Thereof in the Treatment of Cardiovascular Disorders

The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

SUBSTITUTED OXOPYRIDINE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF CARDIOVASCULAR DISORDERS

The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.

The synthesis and biological testing of bacilysin analogues

A series of compounds based on the structure of bacilysin were synthesised and tested for antibacterial activity. The key steps in the syntheses are the coupling of an iodide to a diketopiperazine (DKP) and mono-lactim ether scaffold, respectively. The diastereoselectivity of the coupling reactions was dependant on the scaffold, with selectivity for DKP of about 4:1 and mono-lactim ether exceeding 98:2. Subsequent elaboration of the compounds to give open chain dipeptides and DKPs that mimic the structure of bacilysin but substitute the epoxy ketone for a saturated or unsaturated ketone is described. Overall yield from coupling to final product was between 5 and 21 %, with the yield of the saturated products notably higher. The open chain dipeptides demonstrated moderate antibacterial and antifungal activity.

Discovery of small molecule Mer kinase inhibitors for the treatment of pediatric acute lymphoblastic leukemia

Ectopic Mer expression promotes pro-survival signaling and contributes to leukemogenesis and chemoresistance in childhood acute lymphoblastic leukemia (ALL). Consequently, Mer kinase inhibitors may promote leukemic cell death and further act as chemosensitizers increasing efficacy and reducing toxicities of current ALL regimens. We have applied a structure-based design approach to discover novel small molecule Mer kinase inhibitors. Several pyrazolopyrimidine derivatives effectively inhibit Mer kinase activity at subnanomolar concentrations. Furthermore, the lead compound shows a promising selectivity profile against a panel of 72 kinases and has excellent pharmacokinetic properties. We also describe the crystal structure of the complex between the lead compound and Mer, opening new opportunities for further optimization and new template design.

CYCLICALLY SUBSTITUTED 3,5-DICYANO-2-THIOPYRIDINES AND USE THEREOF

The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.

Heterocyclic antiviral compounds

This invention relates to piperidine derivatives of formula I wherein R1, R2, R3 and R4 are as defined herein useful in the treatment of a variety of disorders, including those in which the modulation of CCR5 re

NOVEL COMPOUNDS

Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.

Enantioselective total synthesis of the antifungal natural products chorotetaine, bacilysin, and anticapsin and of related compounds: Revision of the relative configuration

Enantioselective and diastereoselective syntheses of the title antifungal natural products and some of their diastereoisomers are described. Key steps include the diastereoselective 1,6-addition of bislactim ether 14 and a stereoselective deprotonation of