1044271-29-5

Upstream product

• 17159-79-4 ethyl 4-oxocyclohexane-1-carboxylate 
• 62-53-3 aniline 
• 171361-65-2 1-oxaspiro[2.5]octane-6-carboxylic acid ethyl ester 

Downstream Products

• 1044574-42-6 ethyl 4-hydroxy-4-({phenyl[(phenyloxy)carbonyl]amino}methyl)cyclohexanecarboxylate 
• 1044269-64-8 ethyl (cis)-2-oxo-3-phenyl-1-oxa-3-azaspiro[4.5]decane-8-carboxylate 
• 1044269-87-5 ethyl (trans)-2-oxo-3-phenyl-1-oxa-3-azaspiro[4.5]decane-8-carboxylate 
• 1073560-12-9 N-(5-amino-2-chloro-4-pyrimidinyl)-2-oxo-3-phenyl-1-oxa-3-azaspiro[4.5]decane-8-carboxamide 
• 1073560-13-0 N-(4-amino-2-chloro-5-pyrimidinyl)-2-oxo-3-phenyl-1-oxa-3-azaspiro[4.5]decane-8-carboxamide 

Relevant academic research and scientific papers

Discovery and structure-activity relationship of a novel spirocarbamate series of NPY Y5 antagonists

A novel series of trans-8-aminomethyl-1-oxa-3-azaspiro[4.5]decan-2-one derivatives was identified with potent NPY Y5 antagonist activity. Optimization of the original lead furnished compounds 23p and 23u, which combine sub-nanomolar Y5 activity with metabolic stability, oral bioavailability, brain penetration and strong preclinical profile for development. Both compounds significantly inhibited the food intake induced by a Y5 selective agonist with minimal effective doses of 3 mg/kg po.

BENZIMIDAZOLES WITH A HETERO SPIRO-DECANE RESIDUE AS NPY-Y5 ANTAGONISTS

The present invention relates to compounds of formula (I), or a pharmaceutically acceptable salts, solvates, stereoisomers thereof, formula (I), R1 may be C1-C4 alkyl, aryl or heteroaryl, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; R2 may be halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano, nitro; or aryl, heteroaryl or heterocycle, which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1-C4 haloalkyl, C1-C4 haloalkoxy, cyano; or R2 may correspond to -0-R3; R3 is a 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen X is carbon or oxygen; Z is carbon or nitrogen; G is a fused 6-membered aromatic carbocyclic ring which may contain 1 or 2 nitrogen; m may be 0 or an integer ranging from 1 to 4; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY- Y5 receptor antagonists.

I-OXA-3-AZASPIRO (4.5) DECAN-2-ONE AND 1-OXA-3, 8-DIAZASPIRO (4.5) DECAN-2-ONE DERIVATIVES FOR THE TREATMENT OF EATING DISORDERS

The present invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt or solvate thereof, formula (I) wherein R is an aryl or heteroaryl; which may be substituted by one or more: halogen, C1 -C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; W is -CZ1 or nitrogen; Z1 is hydrogen, C1 -C4 alkyl; A is a 5 membered heteroaryl, pyrazine, pyrimidine, or quinoline or quinazoline which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; B is hydrogen or a 5-10 membered aryl or heteroaryl which may be substituted by one or more: halogen, C1-C4 alkyl, C1-C4 alkoxy, C1 -C4 haloalkyl, C1 -C4 haloalkoxy, cyano; being A and B linked via any atom; provided that when W is -CZ1, compounds of formula (I) have a trans stereochemistry; processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, as NPY Y5 receptor antagonists and as agents for the treatment and/or prophylaxis of eating disorders such as a binge eating disorder.