77253-85-1

Upstream product

• 22428-87-1 4,4-ethylenedioxycyclohexan-1-ol 
• 65619-92-3 8-(dimethylamino)-1,4-dioxaspiro-[4.5]-decane-8-carbonitrile 
• 100-58-3 phenylmagnesium bromide 
• 100-59-4 phenylmagnesium chloride 
• 591-51-5 phenyllithium 
• 1071066-97-1 N-(1,4-dioxaspiro-[4,5]-decan-8-yliden)-methanamine 
• 79741-33-6 methyl-(8-phenyl-1,4-dioxaspiro[4.5]dec-8-yl)amine 
• 50-00-0 formaldehyd 
• 65619-18-3 4-methylamino-4-phenylcyclohexanone, ethylene ketal hydrochloride 
• 4746-97-8 cyclohexanedione monoethylene ketal 
• 65619-17-2 4-isocyanato-4-phenylcyclohexanone, ethylene ketal 
• 51509-99-0 8-Phenyl-1,4-dioxaspiro<4.5>decan-8-carbonsaeure 

Downstream Products

• 65619-20-7 4-dimethylamino-4-phenylcyclohexanone 

Relevant academic research and scientific papers

4,5-DIHYDRO-1H-THIENO[2,3-G]INDAZOLYL DERIVATIVES HAVING MULTIMODAL ACTIVITY AGAINST PAIN

wherein the meanings for the various substituents are as disclosed in the description, having dual pharmacological activity towards both the α2δ subunit, in particular the α2δ-1 subunit, of the voltage-gated calcium channel and the μ-opioid receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.

3-(Carboxyethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives

The invention relates to 3-(carboxyethyl)-8-amino-2-oxo-1,3-diazaspiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives

The invention relates to 8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

3-((HETERO-)ARYL)-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES

The invention relates to 3-((hetero-)aryl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

3-(Carboxymethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives

The invention relates to 3-(carboxymethyl)-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

3-((HETERO-)ARYL)-ALKYL-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES

The invention relates to 3-((hetero-)aryl)-alkyl-8-amino-2-oxo-1,3-diaza-spiro-[4.5]-decane derivatives, their preparation and their use in medicine, particularly in the treatment of pain.

SUBSTITUTED AZASPIRO(4.5)DECANE DERIVATIVES

The invention relates to substituted spirocyclic cyclohexane derivatives which have an affinity for the μ opioid receptor and/or the ORL1 receptor, processes for the preparation thereof, medicaments containing these compounds and the use of these compounds for the preparation of medicaments.

Discovery of spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as potent NOP and opioid receptor agonists

We report the discovery of spiro[cyclohexane-pyrano[3,4-b]indole]-amines, as functional nociceptin/orphanin FQ peptide (NOP) and opioid receptor agonists with strong efficacy in preclinical models of acute and neuropathic pain. Utilizing 4-(dimethylamino)-4-phenylcyclo-hexanone 1 and tryptophol in an oxa-Pictet-Spengler reaction led to the formation of spiroether 2, representing a novel NOP and opioid peptide receptor agonistic chemotype. This finding initially stems from the systematic derivatization of 1, which resulted in alcohols 3-5, ethers 6 and 7, amines 8-10, 22-24, and 26-28, amides 11 and 25, and urea 12, many with low nanomolar binding affinities at the NOP and mu opioid peptide (MOP) receptors.

Method for Synthesizing Substituted Aminocyclohexanone Compounds

A method of synthesizing a substituted aminocyclohexanone compound comprising reacting a compound of formula (II) with an organolithium compound to form a compound of formula (III)

METHOD FOR SYNTHESISING SUBSTITUTED AMINOCYCLOHEXANONE DERIVATIVES

The present invention relates to a method for synthesising substituted aminocyclohexanone derivatives, comprising the following step (b) reaction of a compound of general formula (II) with an organolithium compound to form a compound of general formula (III).