65619-92-3Relevant academic research and scientific papers
3-(Carboxyethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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Paragraph 0254-0255, (2017/08/01)
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.
3-((HETERO-)ARYL)-ALKYL-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES
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Paragraph 0167-0169, (2017/09/02)
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.
3-(Carboxymethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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Paragraph 0215; 0216, (2017/08/01)
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.
8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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Paragraph 0214; 0215, (2017/08/01)
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
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Paragraph 0165; 0166; 0167, (2017/08/07)
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.
SUBSTITUTED AZASPIRO(4.5)DECANE DERIVATIVES
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Page/Page column 56, (2016/02/10)
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 a potent analgesic NOP and opioid receptor agonist: Cebranopadol
Schunk, Stefan,Linz, Klaus,Hinze, Claudia,Frormann, Sven,Oberb?rsch, Stefan,Sundermann, Bernd,Zemolka, Saskia,Englberger, Werner,Germann, Tieno,Christoph, Thomas,K?gel, Babette-Y.,Schr?der, Wolfgang,Harlfinger, Stephanie,Saunders, Derek,Kless, Achim,Schick, Hans,Sonnenschein, Helmut
, p. 857 - 862 (2014/09/29)
In a previous communication, our efforts leading from 1 to the identification of spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amine 2a as analgesic NOP and opioid receptor agonist were disclosed and their favorable in vitro and in vivo pharmacological properties revealed. We herein report our efforts to further optimize lead 2a, toward trans-6′-fluoro-4′, 9′-dihydro-N,N-dimethyl-4-phenyl-spiro[cyclohexane-1,1′(3′H) -pyrano[3,4-b]indol]-4-amine (cebranopadol, 3a), which is currently in clinical development for the treatment of severe chronic nociceptive and neuropathic pain.
Discovery of spiro[cyclohexane-dihydropyrano[3,4-b]indole]-amines as potent NOP and opioid receptor agonists
Schunk, Stefan,Linz, Klaus,Frormann, Sven,Hinze, Claudia,Oberb?rsch, Stefan,Sundermann, Bernd,Zemolka, Saskia,Englberger, Werner,Germann, Tieno,Christoph, Thomas,K?gel, Babette-Y.,Schr?der, Wolfgang,Harlfinger, Stephanie,Saunders, Derek,Kless, Achim,Schick, Hans,Sonnenschein, Helmut
supporting information, p. 851 - 856 (2014/09/17)
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.
Spirocyclic Cyclohexane Compounds
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Page/Page column 10, (2010/03/31)
Spirocyclic cyclohexane compounds corresponding to formula I In which R1, R2, R3 and R5 through R10 and X have defined meanings, a process for their preparation, pharmaceutical compositions containing such compounds, and the use of such spirocyclic cyclohexane compounds in the treatment and/or inhibition of pain and other conditions mediated by the ORL-1 or the ?-opioid receptor.
Substituted Spiroamine Compounds
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Page/Page column 33-34, (2010/05/13)
Substituted spiroamine compounds corresponding to the formula (I) In which m, n, o, p, Q, r, s, t, R1, R2, R3, R4a, R4b, R5a, R5b, R6a, R6b, R7, R8, R9, R10 and R11 have defined meanings; a process for the preparation of such compounds, pharmaceutical compositions containing such compounds and the use of substituted spiroamines for the treatment or inhibition of pain and/or other conditions mediated by the bradykinin 1 receptor.
