127918-34-7

Upstream product

• 61830-23-7 ethyl 5‐bromo‐1,3‐thiazole‐4‐carboxylate 
• 1423-26-3 (meta-(trifluoromethyl)phenyl)boronic acid 
• 127918-60-9 O-methyl 3-(α,α,α-trifluoromethyl)thiobenzoate 

Downstream Products

• 1038509-15-7 5-(3-trifluoromethylphenyl)-1,3-thiazole-4-carboxylic acid 
• 1047673-68-6 1-azabicyclo[2.2.2]oct-4-yl {5-[3-(trifluoromethyl)phenyl]-1,3-thiazol-4-yl}carbamate hydrochloride 

Relevant academic research and scientific papers

Novel quinuclidinyl heteroarylcarbamate derivatives as muscarinic receptor antagonists

Herein, we describe the synthesis and pharmacological profiles of novel quinuclidinyl heteroarylcarbamate derivatives. Among them, the quinuclidin-4-yl thiazolylcarbamate derivative ASP9133 was identified as a promising long-acting muscarinic antagonist (LAMA) showing more selective inhibition of bronchoconstriction against salivation and more rapid onset of action in a rat model than tiotropium bromide.

AZA-BRIDGED-RING COMPOUND

[PROBLEMS] Provided is a compound which has an antagonistic action on a muscarinic M3 receptor and is useful as an active ingredient of a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like. [MEANS FOR SOLVING PROBLEMS] The present inventors have made studies on a compound having an antagonistic action on the binding of a muscarinic M3 receptor, and they have found that an aza-bridged-ring compound or a salt thereof has an antagonistic action on the binding of a muscarinic M3 receptor, thereby completing the present invention. The aza-bridged-ring compound of the present invention has an antagonistic action on the binding of a muscarinic M3 receptor, and can be used as a prophylactic and/or therapeutic agent for an inflammatory disease such as a chronic obstructive pulmonary disease (COPD), asthma and the like.

COMPOUNDS FOR TREATING AND PREVENTING COGNITIVE DISEASES AND DEPRESSION AND METHODS OF MAKING SAME

Ethylenediamine monoamides of the formula R--CO--NH--CH2 --CH2 --NH2. wherein R is one of groups in which R1 is phenyl monohalophenyl, monolower-alkylphenyl, monolower-alkoxypheynl, monotrifluoromethylphenyl, monocyanophenyl or monoaryl-lower-alkoxyphenyl, dihalophenyl, furyl, thienyl or monohalothienyl, R2 is hydrogen, halogen or amino, R3, R5 and R7 each are phenyl, monohalophenyl, dihalophenyl, thienyl, furyl or monohalofuryl, R4 and R6 each are hydrogen or amino and R8 is hydrogen or lower-alkyl, as well as their pharmaceutically usable acid addition salts are disclosed. The compounds have monoamine oxidase inhibiting properties with low toxicity and are useful for the treatment of depressive states and cognitive disorders