1554015-52-9

Upstream product

• 914654-63-0 (1-tert-butoxycarbonylpiperidine-4-)-carbaldehyde 
• 155535-54-9 1-(4-(hydroxymethyl)piperidin-1-yl)-2,2-dimethylpropan-1-one 
• 6457-49-4 4-piperidinemethanol 
• 3282-30-2 pivaloyl chloride 
• 768290-38-6 ethyl 1-pivaloylpiperidine-4-carboxylate 
• 1126-09-6 4-carbethoxypiperidine 
• 95-03-4 5-chloro-2-methoxyaniline 
• 577-19-5 2-nitrophenyl bromide 
• 1427502-95-1 1-(4-chloro-7-methoxyspiro[indoline-3,4'-piperidine]-1'-yl)-2,2-dimethylpropan-1-one 
• 202823-24-3 (5-chloro-2-methoxyphenyl)hydrazine 

Downstream Products

• 1554015-79-0 4-chloro-1-(2-isothiocyanatophenyl)-7-methoxy-1'-neopentylspiro[indoline-3,4'-piperidine] 
• 1554015-82-5 N-(2-(4-chloro-7-methoxy-1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-3-phenyl-1,2,4-thiadiazol-5-amine 
• 1554015-85-8 (Z)-3-(2-(4-chloro-7-methoxy-1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenylamino)-3-(methylthio)-1-(4-(trifluoromethyl)phenyl)prop-2-en-1-one 
• 1554015-86-9 N-(2-(4-chloro-7-methoxy-1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)phenyl)-5-(4-(trifluoromethyl)phenyl)isoxazol-3-amine 
• 1554015-19-8 4-chloro-1'-neopentyl-1-{2-[(3-phenyl-1,2,4-thiadiazol-5-yl)amino]phenyl}-1,2-dihydrospiro[indole-3,4'-piperidine]-7-ol 
• 1554015-24-5 4-chloro-1'-neopentyl-1-[2-({5-[4-(trifluoromethyl)phenyl]-1,2-oxazol-3-yl}amino)phenyl]-1,2-dihydrospiro[indole-3,4'-piperidine]-7-ol 
• 1554015-56-3 1-(1-(2-aminophenyl)-4-chloro-7-methoxyspiro[indoline-3,4'-piperidine]-1'-yl)-2,2-dimethylpropan-1-one 
• 1554015-57-4 2-(4-chloro-7-methoxy-1'-neopentylspiro[indoline-3,4'-piperidine]-1-yl)aniline 

Relevant academic research and scientific papers

7-HYDROXY-SPIROPIPIPERIDINE INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR

The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of Ρ2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.

Identification of 1-{2-[4-chloro-1′-(2,2-dimethylpropyl)-7-hydroxy-1, 2-dihydrospiro[indole-3,4′-piperidine]-1-yl]phenyl}-3-{5-chloro-[1,3] thiazolo[5,4-b]pyridin-2-yl}urea, a potent, efficacious and orally bioavailable P2Y1 antagonist as an antiplatelet agent

Spiropiperidine indoline-substituted diaryl ureas had been identified as antagonists of the P2Y1 receptor. Enhancements in potency were realized through the introduction of a 7-hydroxyl substitution on the spiropiperidinylindoline chemotype. SAR studies were conducted to improve PK and potency, resulting in the identification of compound 3e, a potent, orally bioavailable P2Y1 antagonist with a suitable PK profile in preclinical species. Compound 3e demonstrated a robust antithrombotic effect in vivo and improved bleeding risk profile compared to the P2Y12 antagonist clopidogrel in rat efficacy/bleeding models.

AMINO-HETEROARYL 7-HYDROXY-SPIROPIPERIDINE INDOLINYL ANTAGONISTS OF P2Y1 RECEPTOR

The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor which may be used as medicaments.