928628-29-9

Upstream product

• 928628-24-4 tert-butyl [2-(2-chlorophenyl)ethyl]{3-[(2-{[(2R)-2-hydroxy-2-(4-hydroxy-2-oxo-2,3-dihydro-1,3-benzothiazol-7-yl)ethyl]amino}ethyl)thio]propyl}carbamate 
• 13078-80-3 2-(2-chlorophenyl)ethanamine 
• 662111-33-3 7-acetyl-4-hydroxy-1,3-benzothiazol-2(3H)-one 
• 928628-25-5 tert-butyl allyl[2-(2-chlorophenyl)ethyl]carbamate 
• 928628-27-7 tert-butyl [2-(2-chlorophenyl)ethyl]{3-[(2-hydroxyethyl)thio]propyl}carbamate 
• 928628-28-8 tert-butyl [2-(2-chlorophenyl)ethyl]{3-[(2-oxoethyl)thio]propyl}carbamate 
• 1179336-08-3 7-(2-chloroacetyl)-4-hydroxy-3H-benzothiazol-2-one 
• 1179336-09-4 7-(2-azido-acetyl)-4-hydroxy-3H-benzothiazol-2-one 
• 928628-26-6 tert-butyl (2-chlorophenethyl)carbamate 
• 22568-07-6 1-chloro-2-[(E)-2-nitrovinyl]benzene 
• 89-98-5 2-chloro-benzaldehyde 
• 1053240-12-2 [(3-{[2-(2-chlorophenyl)ethyl]amino}-3-oxopropyl)thio]acetic acid 
• 1053240-13-3 2-[(3-{[2-(2-chlorophenyl)ethyl] amino}propyl)thio]ethanol 
• 1053240-11-1 N-[2-(2-chlorophenyl)ethyl]acrylamide 

Downstream Products

• 1053239-67-0 7-[(1R)-2-({2-[(3-{[2-(2-chlorophenyl)ethyl]amino}propyl)thio]ethyl}-amino)-1-hydroxyethyl]-4-hydroxy-1,3-benzothiazol-2(3H)-one monofumarate 
• 1053239-66-9 7-[(1R)-2-({2-[(3-{[2-(2-chlorophenyl)ethyl]amino}propyl)thio]ethyl}amino)-1-hydroxyethyl]-4-hydroxy-1,3-benzothiazol-2(3H)-one monoxinafoate 

Relevant academic research and scientific papers

Design-driven LO: The discovery of new ultra long acting dibasic β2-adrenoceptor agonists

Starting with the molecular scaffold of the DA2/β 2 dual agonist sibenadet (Viozan), a number of molecular changes were incorporated, which were designed to increase the potency and selectivity of the target molecule, and improve its

COMBINATIONS OF BETA-2-ADRENOCEPTOR AGONISTIC BENZOTHIAZOLONE

The invention provides a pharmaceutical product, kit or composition comprising a first active ingredient which is 7-[(1R)-2-({2-[(3-{[2-(2-Chlorophenyl)ethyl]amino}propyl)-thio]ethyl}amino)-1-hydroxyethyl]-4-hydroxy-1,3-benzothiazol-2(3H)-one or a salt thereof, and a second active ingredient selected from: a non-steroidal Glucocorticoid Receptor (GR Receptor) Agonist; an antioxidant; a CCR1 antagonist; a chemokine antagonist (not CCR1); a corticosteroid; a CRTh2 antagonist; a DP1 antagonist; an Histone Deacetylase Inducer; an IKK2 inhibitor; a COX inhibitor; a lipoxygenase inhibitor; a leukotriene receptor antagonist; an MPO inhibitor; a muscarinic antagonist which is Aclidinium bromide, Glycopyrrolate, Oxitropium bromide, Pirenzepine, telenzepine or Tiotropium bromide; a p38 inhibitor; a PDE inhibitor; a PPAR gamma agonist; a protease inhibitor; a Statin; a thromboxane antagonist; a vasodilator; or, an ENAC blocker (Epithelial Sodium-channel blocker); and its use in the treatment of respiratory disease

SALTS OF A SELECTIVE BETA-2 ANDRENOCEPTOR AGONIST

A pharmaceutically acceptable salt of 7-[(1R)-2-({2-[(3-{[2-(2-Chlorophenyl)ethyl]amino}propyl)thio]ethyl}amino)-1-hydroxyethyl]-4-hydroxy-1,3-benzothiazol-2(3H)-one provided it is not the ditrifluoroacetate, dihydrobromide or di-acetate salt; and the use of such a compound as a medicament (for example in the treatment of respiratory diseases (such as asthma or COPD).

7-(2-AMINO-1-HYDROXY-ETHYL)-4-HYDROXYBENZOTHIAZOL-2(3H)-ONE-DERIVATIVES AS β2 ADRENOCEPTOR AGONISTS

The present invention provides compounds of formula (I) wherein the variables are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.