340756-75-4

Upstream product

• 300345-77-1 N-[5-((1S)-2-azido-1-hydroxyethyl)-2-hydroxyphenyl]methanesulfonamide 
• 14347-18-3 1-[4-hydroxy-3-[(methylsulfonyl)amino]phenyl]ethanone 
• 508233-89-4 N-(5-chloroacetyl-2-hydroxy-phenyl)-methanesulfonamide 
• 508233-91-8 N-[5-(2-chloro-1-hydroxy-ethyl)-2-hydroxy-phenyl]-methanesulfonamide 
• 170687-82-8 N-{2-(benzyloxy)-5-[(1R)-2-bromo-1-hydroxyethyl]phenyl}methane sulfonamide 
• 686780-64-3 N-[2-(benzyloxy)-5-((1R)-1-hydroxy-2-{[(1S)-2-hydroxy-1-phenylethyl]amino}ethyl)phenyl]methanesulfonamide 
• 662111-56-0 N-[2-hydroxy-5-((1R)-1-hydroxy-2-{[(1S)-2-hydroxy-1-phenylethyl]amino}ethyl)phenyl]methanesulfonamide 
• 100-46-9 benzylamine 
• 246262-39-5 (R)-N-[5-[2-iodo-1-[(triethylsilyl)-oxy]ethyl]-2-(phenylmethoxy)phenyl]methanesulfonamide 
• 340756-77-6 [4-(4-oxopiperidin-1-yl)phenyl]acetic acid 
• 373359-62-7 3-[4-(4-oxopiperidin-1-yl)phenylsulfamoyl]thiophene-2-carboxylic acid methyl ester 
• 79421-41-3 1-[4-(1,4-dioxa-8-azaspiro[4.5]dec-8-yl)phenyl]ethanone 

Downstream Products

• 571146-14-0 1-[4-(4-{[2-hydroxy-2-(4-hydroxy-3-methanesulfonylamino-phenyl)-ethylamino]-methyl}-piperidine-1-sulfonyl)-phenyl]-1H-pyrazole-4-carboxylic acid methyl ester 
• 686350-77-6 N-[5-((1R)-2-{[6-({4-[3-(cyclopentylsulfonyl)phenyl]butyl}oxy)hexyl]amino}-1-hydroxyethyl)-2-hydroxyphenyl]methanesulfonamide 
• 392642-64-7 N-(5-{[4-(4-{2-[((2R)-2-hydroxy-2-{4-hydroxy-3-[(methylsulfonyl)amino]phenyl}-ethyl)amino]ethyl}anilino)piperidin-1-yl]sulfonyl}-4-methyl-1,3-thiazol-2-yl)acetamide 
• 392643-27-5 N-(2-Hydroxy-5-{(1R)-1-hydroxy-2-[2-(4-{1-[4-(piperidine-1-sulfonyl)-phenyl]-piperidin-4-ylamino}-phenyl)-ethylamino]-ethyl}-phenyl)-methanesulfonamide 
• 392689-07-5 N-(5-{(1R)-2-[(1-{4-[3-(2,6-Difluoro-benzyl)-3-isopropyl-ureido]-benzenesulfonyl}-piperidin-4-ylmethyl)-amino]-1-hydroxy-ethyl}-2-hydroxyphenyl)-methane-sulfonamide 
• 392689-10-0 N-[5-[(R)-2-[[[1-[[4-[[[[(2,5-Difluorophenyl)methyl]-methylamino]-carbonyl]amino]-phenyl]sulfonyl]-4-piperidinyl]methyl]amino]-1-hydroxyethyl]-2-hydroxyphenyl]-methanesulfonamide 
• 392689-12-2 [3-Fluoro-4-[[[[[4-[[4-[[[(R)-2-hydroxy-2-[4-hydroxy-3-[(methylsulfonyl)amino]-phenyl]-ethyl]amino]methyl]-1-piperidinyl]sulfonyl]phenyl]amino]carbonyl]-amino]-methyl]phenoxy]acetic acid 

Relevant academic research and scientific papers

MEDICINAL COMPOUNDS

Compounds of formula (I), and salts, solvates, and physiologically functional derivatives thereof, useful for the prophylaxis or treatment of a clinical condition for which a selective β2-adrenoreceptor agonist is indicated, for example asthma

PHENETHANOLAMINE DERIVATIVE FOR THE TREATMENT OF RESPIRATORY DISEASES

The present invention relates to novel compounds of formula (I), to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use in the prophylaxis and treatment of respiratory diseases.

MEDICINAL COMPOUNDS

The present invention relates to novel compounds of formula (I),and salts, solvates and physiologically acceptable derivatives thereof, to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in par

MEDICINAL COMPOUNDS

The present invention concerns compounds of formula (I) and salts, solvates, and physiologically functional derivatives thereof, wherein: R1 is hydrogen or -XSO2NR6R7; R2 and R3 are indepen

Novel substituted 4-aminomethylpiperidines as potent and selective human β3-agonists. Part 2: Arylethanolaminomethylpiperidines

The synthesis and SAR of a series of β3 adrenoreceptor agonists based on a novel template derived from 4-aminomethylpiperidine coupled with a common pharmacophore, arylethylamine, is described. This combination led to the identification of human β3 adrenoreceptor agonists with in vivo activity in a transgenic mouse model.

2-substituted thiazolidinones as beta-3 adrenergic receptor agonists

This invention provides compounds of Formula I having the structure wherein: A, X, Y, Z, R1, R2, R3, R4, R5, and R6are as defined hereinbefore or a pharmaceutically acceptable salt thereof, which are useful in treating or inhibiting metabolic disorders related to insulin resistance or hyperglycemia (typically associated with obesity or glucose intolerance), atherosclerosis, gastrointestinal disorders, neurogenetic inflammation, and frequent urination; and are particularly useful in the treatment or inhibition of type II diabetes.

Novel (4-piperidin-1-yl)-phenyl sulfonamides as potent and selective human β3 agonists

A series of novel (4-piperidin-1-yl)-phenyl sulfonamides was prepared and evaluated for their biological activity on the human β3-adrenergic receptor (AR). Replacement of the 3,4-dihydroxyl group of the catechol moiety with 4-hydroxyl-3-methyl

2,4-Thiazolidinediones as potent and selective human β3 agonists

Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50 = 0.01 μM, IA = 1.19) and selective (more than 110-fold over β1 and β2 agonist activity) β3 agonist. This compound has also been proven to be active and selective in an in vivo mode.

4-Aminopiperidine ureas as potent selective agonists of the human β3-Adrenergic receptor

The preparation and structure-activity relationships (SARs) of potent agonists of the human β3-adrenergic receptor (AR) derived from a 4-aminopiperidine scaffold are described. Examples combine human β3-AR potency with selectivity over human β1-AR and/or human β2-AR agonism. Compound 29s was identified as a potent (EC50 = 1 nM) and selective (greater than 400-fold over β1- with no β2-AR agonism) full β3-AR agonist with in vivo activity in a transgenic mouse model of thermogenesis.