601484-33-7

Upstream product

• 403-54-3 m-Fluorobenzonitrile 
• 79-04-9 chloroacetyl chloride 
• 1319746-46-7 (Z)-3-fluoro-N'-hydroxybenzimidamide 
• 844498-76-6 C₉H₈ClFN₂O₂ 
• 54872-79-6 3-fluoro-N-hydroxybenzene-1-carboximidamide 
• 79-11-8 chloroacetic acid 
• 844498-76-6 C₉H₈ClFN₂O₂ 

Downstream Products

• 1201042-14-9 (R)-1-(3-(3-fluoro-phenyl)-[1,2,4]oxadiazol-5-ylmethyl)-3-((S)-2-phenyl-2-piperidin-1-yl-propionyloxy)-1-azonia-bicyclo[2.2.2]octane choride 
• 601484-30-4 (2S)-3-(4-{[3-(3-fluorophenyl)(1,2,4-oxadiazol-5-yl)]methyl}piperazinyl)-1-(2-methylbenzothiazol-5-yloxy)propan-2-ol 

Relevant academic research and scientific papers

1-AZA-BICYCLO [2.2.2] OCTANE DERIVATIVES USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS

The invention provides named compounds of formula (I), pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions and their use in therapy.

SPIRO-OXAZOLIDINONE COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS

Compounds in accord with Formula (I): wherein R1, L, A, B, D, E, m, n, x and y are as defined in the description, processes for the preparation of such compounds and to new intermediates employed in the preparation thereof, pharmaceutical compositions containing such compounds, and the use of such compounds in therapy and for the treatment of diseases mentioned in the specification.

New GABA-modulating 1,2,4-oxadiazole derivatives and their anticonvulsant activity

A series of 3- and 5-aryl-1,2,4-oxadiazole derivatives were prepared and tested for anticonvulsant activity in a variety of models. These 1,2,4-oxadiazoles exhibit considerable activity in both pentylenetetrazole (PTZ) and maximal electroshock seizure (MES) models. Compound 10 was protective in the PTZ model in rats with an oral ED50 of 25.5 mg/kg and in the MES model in rats with an oral ED50 of 14.6 mg/kg. Neurotoxicity (rotarod) was observed with an ED50 of 335 mg/kg. We found several oxadiazoles that acted as selective GABA potentiating compounds with no interaction to the benzodiazepine binding site.

The discovery of a selective, high affinity A2B adenosine receptor antagonist for the potential treatment of asthma

Adenosine has been suggested to play a role in asthma, possibly via activation of A2B adenosine receptors on mast cells and other pulmonary cells. We describe our initial efforts to discover a xanthine based selective A2B AdoR antagonist that resulted in the discovery of CVT-5440, a high affinity A2B AdoR antagonist with good selectivity (A2B AdoR Ki = 50 nM, selectivity A1 > 200: A2A > 200: A3 > 167).

NEW COMPOUNDS

The present invention relates to new compounds of formula I, (I) a process for their preparation and new intermediates prepared therein, pharmaceutical formulations containing said compounds and to the use of said compounds in therapy.

Substituted heterocyclic compounds

Disclosed are novel heterocyclic derivatives, useful for the treatment of various disease states, in particular cardiovascular diseases such as atrial and ventricular arrhythmias, intermittent claudication, Prinzmetal's (variant) angina, stable and unstable angina, exercise induced angina, congestive heart disease, and myocardial infarction. The compounds are also useful in the treatment of diabetes, and for increasing HDL plasma levels in mammals.