e.g. Filippa Pettersson or Cancer Res. 75(6) , 1102-12, (2015) or 10.1002/anie.201600521

4, 4-Disubstituted cyclohexylamine NK 1 receptor antagonists II

…, JL Castro, GG Chicchi, K Dinnell, J Di Salvo…

Index: Cooper, Laura C.; Carlson, Emma J.; Castro, Jose L.; Chicchi, Gary G.; Dinnell, Kevin; Di Salvo, Jerry; Elliott, Jason M.; Hollingworth, Gregory J.; Kurtz, Marc M.; Ridgill, Mark P.; Rycroft, Wayne; Tsao, Kwei-Lan; Swain, Christopher J. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 13 p. 1759 - 1762

Full Text: HTML

Citation Number: 16

Abstract

The mammalian tachykinin Substance P (SP) has been implicated in numerous conditions 1, 2 and 3 including cystitis, depression and cytotoxin-induced emesis. This wide range of therapeutic indications has led to the development of various potent antagonists 3, 4 and 5 of the receptor to which SP preferentially binds, neurokinin-1 (NK 1 ). ... The lead compound 1 and Figure 1 for the cyclohexyl series of NK 1 receptor antagonists was identified during targeted ...

Ethyl N-Boc-piperidine-4-carboxylate Structure

Ethyl N-Boc-pip...

~%

1,1-Dimethylethyl 2-Oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

1,1-Dimethyleth...

1-TERT-BUTYL 4-ETHYL 4-ALLYLPIPERIDINE-1,4-DICARBOXYLATE Structure

1-TERT-BUTYL 4-...

~%

1,1-Dimethylethyl 2-Oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

1,1-Dimethyleth...

1,4-Piperidinedicarboxylic acid, 4-(2-hydroxyethyl)-, 1-(1,1-dimethylethyl) 4-ethyl ester Structure

1,4-Piperidined...

~%

1,1-Dimethylethyl 2-Oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

1,1-Dimethyleth...

Ethyl N-Boc-piperidine-4-carboxylate Structure

Ethyl N-Boc-pip...

~%

2-Oxa-8-azaspiro[4.5]decane Structure

2-Oxa-8-azaspir...

tert-butyl 1-oxo-2-oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

tert-butyl 1-ox...

~%

2-Oxa-8-azaspiro[4.5]decane Structure

2-Oxa-8-azaspir...

tert-butyl 4-(2-hydroxyethyl)-4-(hydroxymethyl)piperidine-1-carboxylate Structure

tert-butyl 4-(2...

~%

2-Oxa-8-azaspiro[4.5]decane Structure

2-Oxa-8-azaspir...

1-TERT-BUTYL 4-ETHYL 4-ALLYLPIPERIDINE-1,4-DICARBOXYLATE Structure

1-TERT-BUTYL 4-...

~%

2-Oxa-8-azaspiro[4.5]decane Structure

2-Oxa-8-azaspir...

1,4-Piperidinedicarboxylic acid, 4-(2-hydroxyethyl)-, 1-(1,1-dimethylethyl) 4-ethyl ester Structure

1,4-Piperidined...

~%

2-Oxa-8-azaspiro[4.5]decane Structure

2-Oxa-8-azaspir...

N-(tert-Butoxycarbonyl)-4-piperidone Structure

N-(tert-Butoxyc...

~%

1-Oxa-8-azaspiro[4.5]decane Structure

1-Oxa-8-azaspir...

1-Piperidinecarboxylic acid, 4-(3-ethoxy-3-oxo-1-propyn-1-yl)-4-hydroxy-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

~%

1-Oxa-8-azaspiro[4.5]decane Structure

1-Oxa-8-azaspir...

tert-butyl 2-oxo-1-oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

tert-butyl 2-ox...

~%

1-Oxa-8-azaspiro[4.5]decane Structure

1-Oxa-8-azaspir...

1-Piperidinecarboxylic acid, 4-hydroxy-4-(3-hydroxypropyl)-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

~%

1-Oxa-8-azaspiro[4.5]decane Structure

1-Oxa-8-azaspir...

1-[(1,1-DIMETHYLETHOXY)CARBONYL]-4-HYDROXY-4-PIPERIDINEPROPANOIC ACID ETHYL ESTER Structure

1-[(1,1-DIMETHY...

~%

1-Oxa-8-azaspiro[4.5]decane Structure

1-Oxa-8-azaspir...

tert-butyl 1-oxo-2-oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

tert-butyl 1-ox...

~%

1,1-Dimethylethyl 2-Oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

1,1-Dimethyleth...

tert-butyl 4-(2-hydroxyethyl)-4-(2-hydroxypropan-2-yl)piperidine-1-carboxylate Structure

tert-butyl 4-(2...

~%

1,1-DIMETHYL-2-OXA-8-AZASPIRO[4.5]DECANE Structure

1,1-DIMETHYL-2-...

1-TERT-BUTYL 4-ETHYL 4-ALLYLPIPERIDINE-1,4-DICARBOXYLATE Structure

1-TERT-BUTYL 4-...

~%

1,4-Piperidinedicarboxylic acid, 4-(2-hydroxyethyl)-, 1-(1,1-dimethylethyl) 4-ethyl ester Structure

1,4-Piperidined...

Ethyl N-Boc-piperidine-4-carboxylate Structure

Ethyl N-Boc-pip...

~%

1,4-Piperidinedicarboxylic acid, 4-(2-hydroxyethyl)-, 1-(1,1-dimethylethyl) 4-ethyl ester Structure

1,4-Piperidined...

Ethyl N-Boc-piperidine-4-carboxylate Structure

Ethyl N-Boc-pip...

~%

tert-butyl 4-(2-hydroxyethyl)-4-(hydroxymethyl)piperidine-1-carboxylate Structure

tert-butyl 4-(2...

1-TERT-BUTYL 4-ETHYL 4-ALLYLPIPERIDINE-1,4-DICARBOXYLATE Structure

1-TERT-BUTYL 4-...

~%

tert-butyl 4-(2-hydroxyethyl)-4-(hydroxymethyl)piperidine-1-carboxylate Structure

tert-butyl 4-(2...

1,4-Piperidinedicarboxylic acid, 4-(2-hydroxyethyl)-, 1-(1,1-dimethylethyl) 4-ethyl ester Structure

1,4-Piperidined...

~%

tert-butyl 4-(2-hydroxyethyl)-4-(hydroxymethyl)piperidine-1-carboxylate Structure

tert-butyl 4-(2...

tert-butyl 2-oxo-1-oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

tert-butyl 2-ox...

~%

1-Piperidinecarboxylic acid, 4-hydroxy-4-(3-hydroxypropyl)-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

N-(tert-Butoxycarbonyl)-4-piperidone Structure

N-(tert-Butoxyc...

~%

1-Piperidinecarboxylic acid, 4-hydroxy-4-(3-hydroxypropyl)-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

1-Piperidinecarboxylic acid, 4-(3-ethoxy-3-oxo-1-propyn-1-yl)-4-hydroxy-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

~%

1-Piperidinecarboxylic acid, 4-hydroxy-4-(3-hydroxypropyl)-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

1-[(1,1-DIMETHYLETHOXY)CARBONYL]-4-HYDROXY-4-PIPERIDINEPROPANOIC ACID ETHYL ESTER Structure

1-[(1,1-DIMETHY...

~%

1-Piperidinecarboxylic acid, 4-hydroxy-4-(3-hydroxypropyl)-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

N-(tert-Butoxycarbonyl)-4-piperidone Structure

N-(tert-Butoxyc...

Ethyl propiolate Structure

Ethyl propiolate

~%

1-Piperidinecarboxylic acid, 4-(3-ethoxy-3-oxo-1-propyn-1-yl)-4-hydroxy-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

1-Piperidinecarboxylic acid, 4-(3-ethoxy-3-oxo-1-propyn-1-yl)-4-hydroxy-, 1,1-dimethylethyl ester Structure

1-Piperidinecar...

~%

1-[(1,1-DIMETHYLETHOXY)CARBONYL]-4-HYDROXY-4-PIPERIDINEPROPANOIC ACID ETHYL ESTER Structure

1-[(1,1-DIMETHY...

N-(tert-Butoxycarbonyl)-4-piperidone Structure

N-(tert-Butoxyc...

~%

1-[(1,1-DIMETHYLETHOXY)CARBONYL]-4-HYDROXY-4-PIPERIDINEPROPANOIC ACID ETHYL ESTER Structure

1-[(1,1-DIMETHY...

Ethyl propiolate Structure

Ethyl propiolate

~%

1-[(1,1-DIMETHYLETHOXY)CARBONYL]-4-HYDROXY-4-PIPERIDINEPROPANOIC ACID ETHYL ESTER Structure

1-[(1,1-DIMETHY...

tert-butyl 1-oxo-2-oxa-8-azaspiro[4.5]decane-8-carboxylate Structure

tert-butyl 1-ox...

~%

2-OXA-8-AZASPIRO[4.5]DECAN-1-ONE HYDROCHLORIDE Structure

2-OXA-8-AZASPIR...

Ethyl N-Boc-piperidine-4-carboxylate Structure

Ethyl N-Boc-pip...

~%

2-OXA-8-AZASPIRO[4.5]DECAN-1-ONE HYDROCHLORIDE Structure

2-OXA-8-AZASPIR...

1-TERT-BUTYL 4-ETHYL 4-ALLYLPIPERIDINE-1,4-DICARBOXYLATE Structure

1-TERT-BUTYL 4-...

~%

2-OXA-8-AZASPIRO[4.5]DECAN-1-ONE HYDROCHLORIDE Structure

2-OXA-8-AZASPIR...

1,4-Piperidinedicarboxylic acid, 4-(2-hydroxyethyl)-, 1-(1,1-dimethylethyl) 4-ethyl ester Structure

1,4-Piperidined...

~%

2-OXA-8-AZASPIRO[4.5]DECAN-1-ONE HYDROCHLORIDE Structure

2-OXA-8-AZASPIR...