65618-98-6Relevant 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; 0257; 0326, (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.
8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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Paragraph 0214; 0217; 0305, (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; 0170; 0171; 0293, (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.
3-(Carboxymethyl)-8-Amino-2-Oxo-1,3-Diaza-Spiro-[4.5]-Decane Derivatives
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Paragraph 0215; 0218; 0314, (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.
3-((HETERO-)ARYL)-ALKYL-8-AMINO-2-OXO-1,3-DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES
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Paragraph 0167; 0172-0173; 0312, (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.
4-Amino-4-arylcyclohexanones and Their Derivatives, a Novel Class of Analgesics. 1. Modification of the Aryl Ring
Lednicer, Daniel,VonVoigtlander, Philip F.,Emmert, D. Edward
, p. 424 - 430 (2007/10/02)
Investigation of central nervous system activity of phenylcyclohexylamines was continued by preparation of "reversed" analogues.Following the unexpected finding of analgesic activity with 1-(dimethylamino)-1-phenylcyclohexylamine, the SAR of the series was investigated.Synthesis starts by double Michael reaction of acrylate on arylacetonitriles.Following cyclization, decarboxylation, ketalization, and saponification, the geminally substituted acid is rearranged to the isocyanate by means of (C6H5O)2PON3.Isocyanates were then converted to the title compounds.Analgesic activity is very sensitive to the nature and position of the substituent on the aromatic ring.The most potent compounds in this series (p-CH3, p-Br) showed 50percent the potency of morphine.Deletion of the ring oxygen abolishes activity.
Analgetic compounds, compositions and process of treatment
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, (2008/06/13)
Novel compounds of the formula: STR1 wherein R1 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, CH2 -alkenyl wherein alkenyl is from 2 to 4 carbon atoms, inclusive, cycloalkyl of from 3 to 6 carbon atoms, inclusive, cycloalkylmethyl of from 3 to 6 carbon atoms, inclusive; R2 is a variable consisting of hydrogen, alkyl of from 1 to 8 carbon atoms, inclusive, with the proviso that R1 and R2 cannot both be hydrogen at the same time; Y is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, halogen, trifluoromethyl, hydroxy, alkanoyloxy from 2 to 5 carbon atoms, inclusive, alkoxy of from 1 to 4 carbon atoms, inclusive, cycloalkyloxy of from 3 to 6 carbon atoms, inclusive, benzyloxy; m is an integer 0, 1, 2; R5 is a variable consisting of hydrogen and alkyl of from 1 to 4 carbon atoms, inclusive; R3 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive; R4 is a variable consisting of alkyl of from 1 to 4 carbon atoms, inclusive, CH2 -alkenyl wherein alkenyl is of from 2 to 4 carbon atoms, inclusive, and arylalkyl wherein alkyl is from 1 to 4 carbon atoms, inclusive, and aryl is STR2 WHEREIN Y' is CF3, halogen, alkyl of 1 to 4 carbon atoms, inclusive, and alkoxy of from 1 to 4 carbon atoms, inclusive; and R3 and R4 when taken together with the nitrogen atom to which they are attached can form saturated heterocycles of from 5 to 7 ring members, a second hetero atom of said ring can be oxygen or nitrogen, e.g., morpholine, piperazine, and said heterocycles can be monosubstituted having a total of up to 9 carbon atoms, with the proviso that when STR3 is pyrrolidinyl, then m = 1, 2, having analgetic activity in humans and animals are prepared in unit dosage forms. The compositions are useful in relieving pain by administering orally, parenterally, and rectally to humans and animals.
