79601-27-7

Upstream product

• 4385-67-5 3-(3-methylphenyl)pyridine 
• 67-56-1 methanol 
• 201230-82-2 carbon monoxide 
• 1044873-05-3 3-(pyridin-3-yl)benzoyl chloride 
• 4385-77-7 3-(pyridine-3-yl)benzoic acid 
• 1120-90-7 3-iodopyridine 
• 93-58-3 benzoic acid methyl ester 
• 626-55-1 3-Bromopyridine 
• 480425-35-2 methyl 3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzoate 
• 618-91-7 methyl 3-iodo-benzoate 
• 89878-14-8 3-Diethylboranylpyridine 
• 618-89-3 methyl 3-bromobenzoate 
• 1692-25-7 3-pyridylboronic acid 
• 28987-79-3 m-tolylmagnesium bromide 

Downstream Products

• 79412-84-3 1-[3-(3-Amino-phenyl)-piperidin-1-yl]-propan-1-one 
• 79601-28-8 3-(1-Propionylpiperidino-3-yl)-benzoic acid 
• 79412-67-2 3-<3-(methoxycarbonyl)phenyl>-N-propionylpiperidine 
• 79412-82-1 1-[3-(3-Isocyanato-phenyl)-piperidin-1-yl]-propan-1-one 
• 79412-83-2 [3-(1-Propionyl-piperidin-3-yl)-phenyl]-carbamic acid benzyl ester 
• 79412-56-9 3-(3-carbamoylphenyl)-N-n-propylpiperidine hydrochloride 
• 79412-68-3 3-(1-Propyl-piperidin-3-yl)-benzoic acid; hydrochloride 
• 79601-43-7 3-(3-aminophenyl)-N-n-propylpiperidine 
• 79412-81-0 3-<3-hydroxymethyl)phenyl>-N-propylpiperidine 
• 150336-90-6 (+/-)-DS 121 
• 146820-21-5 3-<3-(methoxycarbonyl)phenyl>-N-n-propylpiperidine 
• 900514-76-3 3-(pyridin-3-yl)benzohydrazide 
• 4385-77-7 3-(pyridine-3-yl)benzoic acid 
• 1201769-39-2 C₂₀H₁₈NO₂⁽¹⁺⁾ 

Relevant academic research and scientific papers

N-(1H-IMIDAZOL-2-YL)BENZAMIDE COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AS ACTIVE INGREDIENT

N-(1H-imidazol-2-yl)benzamide compound of formula (I), or a pharmaceutically acceptable salt, a prodrug, a solvate, or a stereoisomer thereof which is a novel compound exhibiting excellent inhibitory activity against IRAK-4, can be used without side effects for efficient prevention and treatment of diseases mediated by IRAK-4 receptors, particularly autoimmune diseases or lymphomas.

Start Selective and Rigidify: The Discovery Path toward a Next Generation of EGFR Tyrosine Kinase Inhibitors

The epidermal growth factor receptor (EGFR), when carrying an activating mutation like del19 or L858R, acts as an oncogenic driver in a subset of lung tumors. While tumor responses to tyrosine kinase inhibitors (TKIs) are accompanied by marked tumor shrinkage, the response is usually not durable. Most patients relapse within two years of therapy often due to acquisition of an additional mutation in EGFR kinase domain that confers resistance to TKIs. Crucially, oncogenic EGFR harboring both resistance mutations, T790M and C797S, can no longer be inhibited by currently approved EGFR TKIs. Here, we describe the discovery of BI-4020, which is a noncovalent, wild-type EGFR sparing, macrocyclic TKI. BI-4020 potently inhibits the above-described EGFR variants and induces tumor regressions in a cross-resistant EGFRdel19 T790M C797S xenograft model. Key was the identification of a highly selective but moderately potent benzimidazole followed by complete rigidification of the molecule through macrocyclization.

The Discovery of Novel Antimalarial Aminoxadiazoles as a Promising Nonendoperoxide Scaffold

Since the appearance of resistance to the current front-line antimalarial treatments, ACTs (artemisinin combination therapies), the discovery of novel chemical entities to treat the disease is recognized as a major global health priority. From the GSK antimalarial set, we identified an aminoxadiazole with an antiparasitic profile comparable with artemisinin (1), with no cross-resistance in a resistant strains panel and a potential new mode of action. A medicinal chemistry program allowed delivery of compounds such as 19 with high solubility in aqueous media, an acceptable toxicological profile, and oral efficacy. Further evaluation of the lead compounds showed that in vivo genotoxic degradants might be generated. The compounds generated during this medicinal chemistry program and others from the GSK collection were used to build a pharmacophore model which could be used in the virtual screening of compound collections and potentially identify new chemotypes that could deliver the same antiparasitic profile.

MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-?B ACTIVITY AND USE THEREOF

A class of novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including obesity, diabetes, inflammatory and immune diseases, and have the

Benzoheterocyclic derivatives

A benzoheterocyclic derivative of the following formula [1]: and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity, vasopressin agonistic activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist, vasopressin agonist or oxytocin antagonist.

THE PYRIDYL CATION AS A REACTIVE INTERMEDIATE IN THE PHOTOREACTION OF IODOPYRIDINES WITH BENZENES

The electrophilic behavior of the reactive entity in the photosubstitution of benzenes with 2-iodopyridine was found to be ascribable to the intermediary 2-pyridyl cation, rather than the electrophilic 2-pyridyl radical.

PHENYL-AZACYCLOALKANES AND USE THEREOF IN TREATMENT OF CENTRAL NERVOUS SYSTEM DISORDERS

Compound of the formula STR1 wherein n is 1 or 2, Y is OH, R 1 COO--, R 2 R 3 NCOO--or R 4 O whereby R 1 is an alkyl group, or a possibly substituted phenyl group, R 2 is an alkyl, phenethyl, or benzyl or phenyl group, R 3 is H or an alkyl group and R 4 i

SUBSTITUTED PHENYL PIPERIDINES

Compounds of the formula wherein n is 1 or 2, Y is OH, R1COO-,R2R3NCOO-or R4O whereby R1 is an alkyl group, or a possibly substituted phenyl group, R2 is an alkyl, phenethyl,benzyl or phenyl group, R3 is H or an alkyl group and R4 is an allyl or benzyl gr

3-Phenylpiperidines. Central Dopamine-Autoreceptor Stimulating Activity

Thirty compounds related to the selective dopamine-autoreceptor agonist 3-(3-hydroxyphenyl)-N-n-propylpiperidine have been synthesized and tested for central dopamine-autoreceptor stimulating activity.The 3-(3-hydroxyphenyl)piperidine moiety seems indispensable for high potency and selectivity.Introduction of an additional hydroxyl group into the 4-position of the aromatic ring gives a compound with dopaminergic activity but lacking selectivity for autoreceptors. 3-(3-Hydroxyphenyl)-N-n-propylpyrrolidine, 3-(3-hydroxy)-N-n-propylperhydroazepine, and 3-(3-hydroxyphenyl)quinuclidine were all inactive.The most potent compounds were the N-isopropyl-, N-n-butyl-, N-n-pentyl-, and N-phenethyl-substituted 3-(3-hydroxyphenyl)piperidine derivatives.None of the compounds investigated seemed to have central noradrenaline- or serotonin-receptor stimulating activity.