http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-090106-A2

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filingDate 2013-02-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_295b54755f5bf505d2f4fab6f9fd5377
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publicationDate 2014-10-22-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-090106-A2
titleOfInvention DERIVATIVES OF 4-AMINOCICLOHEXANO REPLACED
abstract Compounds, which have an affinity with the opioid receptor m and with the ORL-1 receptor, to a procedure for obtaining them, to medications containing these compounds and to the use of these compounds for the manufacture of medicaments. Claim 1: Compound characterized in that it has the general formula (1) wherein, Y¹, Y¹, Y², Y², Y³, Y³, Y⁴ and Y⁴ represent -H; Q represents -aryl or -heteroaryl; R¹ and R², independently of each other, represent -H or -CH₃; with the proviso that R¹ and R² do not mean both at the same time -H; R³ represents -aliphatic C₁₋₈, -cycloaliphatic C₃₋₁₂, -aryl, -heteroaryl, -aliphatic C₁₋₈ -cycloaliphatic C₃₋₁₂, -aliphatic C₁₋₈-aryl, -aliphatic C₁₋₈-heteroaryl, -cycloaliphatic C₃ ₋₈-aliphatic C₁₋₈, -cycloaliphatic C₃₋₈-aryl or -cycloaliphatic C₃₋₈-heteroaryl, n represents 0; X represents -NRA-; RA represents -H or -R⁰; where R⁰ represents -aliphatic C₁₋₈, -cycloaliphatic C₃₋₁₂, -aryl, -heteroaryl, -aliphatic C₁₋₈-cycloaliphatic C₃₋₁₂, -aliphatic C₁₋₈-aryl, -aliphatic C₁₋₈-heteroaryl, - C₃₋₈-aliphatic C₁₋₈ cycloaliphatic, C₃₋₈-arylcycloaliphatic or C₃₋₈-heteroaryl-cycloaliphatic; RB represents -C (= O) R⁰; wherein R⁰ represents -aliphatic C₁₋₈-aryl or -aliphatic C₁₋₈-heteroaryl; wherein, aliphatic is in each case a branched or unbranched, saturated or mono- or polyunsaturated aliphatic hydrocarbon moiety, unsubstituted or substituted one or more times; Cycloaliphatic is in each case an alicyclic, mono- or polycyclic, saturated or mono- or polyunsaturated hydrocarbon moiety, unsubstituted or substituted once or several times, whose number of carbon atoms in the ring is preferably in the indicated range (i.e. , cycloaliphatic C₃₋₈ ⁱₙᵈⁱᶜₐ ᶜₒₙ ₚʳₑᶠₑʳₑₙᶜⁱₐ ₃, ₄, ₅, ₆, ₇ ú ₈ áₜₒₘₒₛ ᵈₑ ᶜₐʳᵇₒₙₒ ₑₙ ₑₗ ₐₙⁱₗₗₒ₎; ₑₙ ᵈₒₙᵈₑ, ₑₙ ₗₒ ʳₑᶠₑʳₑₙₜₑ ₐ ₐₗⁱᶠáₜⁱᶜₒ ʸ ᶜⁱᶜₗₒₐₗⁱᶠáₜⁱᶜₒ, ₚₒʳ ₛᵘₛₜⁱₜᵘⁱᵈₒ ₛᵘₛₜⁱₜᵘⁱᵈₒ ₒ ᵛₐʳⁱₐₛ ᵛₑᶜₑₛ ₛₑ ₑₙₜⁱₑₙᵈₑ ᵘₙₐ ₛᵘₛₜⁱₜᵘᶜⁱóₙ úₙⁱᶜₐ ₒ ₘúₗₜⁱₚₗₑ ᵈₑ ᵘₙₒ ₒ ᵛₐʳⁱₒₛ áₜₒₘₒₛ ᵈₑ ₕⁱᵈʳóᵍₑₙₒ, ₚₒʳ ₑʲ. ₗₐ ₛᵘₛₜⁱₜᵘᶜⁱóₙ ᵘₙₐ ᵛₑᶻ, ᵈ ₒₛ ᵛₑᶜₑₛ, ₜʳₑₛ ᵛₑᶜₑₛ ₒ ₜₒₜₐₗ ₚₒʳ ₛᵘₛₜⁱₜᵘʸₑₙₜₑₛ ₑₗₑᵍⁱᵈₒₛ ᶜₒₙ ⁱₙᵈₑₚₑₙᵈₑₙᶜⁱₐ ₑₙₜʳₑ ₛí ᵈₑₗ ᵍʳᵘₚₒ ᶠₒʳₘₐᵈₒ ₚₒʳ ₋F, ₋Cₗ, ₋Bʳ, ₋I, ₋CN, ₋NO₂, -CHO, = O, -R⁰, -C (= O ) R⁰, -C (= O) H, -C (= O) OH, -C (= O) OR⁰, -C (= O) NH₂, -C (= O) NHR⁰, -C (= O) N (R⁰) ₂, -OH, -OR⁰, -OC (= O) H, -OC (= O) R⁰, -OC (= O) OR⁰, -OC (= O) NHR⁰, -OC (= O) N (R⁰) ₂, -SH, -SR⁰, -SO₃H, -S (= O) ₁₋₂-R⁰, -S (= O) ₁₋₂NH₂, -NH₂, -NHR⁰, -N (R⁰) ₂, - N⁺ (R⁰) ₃, -N⁺ (R⁰) ₂O⁻, -NHC (= O) R⁰, -NHC (= O) OR⁰, -NHC (= O) NH₂, -NHC (= O) -NHR⁰, - NH-C (= O) N (R⁰) ₂, -Si (R⁰) ₃ and -PO (OR⁰) ₂; where R⁰ represents -aliphatic C₁₋₈, -cycloaliphatic C₃₋₁₂, -aryl, -heteroaryl, -aliphatic C₁₋₈-cycloaliphatic C₃₋₁₂, -aliphatic C₁₋₈-aryl, -aliphatic C₁₋₈-heteroaryl, - C₃₋₈-aliphatic C₁₋₈ cycloaliphatic, C₃₋₈-arylcycloaliphatic or C₃₋₈-heteroaryl-cycloaliphatic; aryl means, in each case independently, a carbocyclic ring system having at least one aromatic ring, but without heteroatoms in this ring, wherein said aryl moieties may eventually be fused to other saturated, (partially) unsaturated ring systems or aromatic, and each aryl moiety may be present unsubstituted or substituted once or several times, wherein the aryl substituents may be the same or different and may occupy any possible position of the aryl; heteroaryl means a cyclic aromatic moiety of 5, 6 or 7 links, containing 1, 2, 3, 4 or 5 heteroatoms, wherein the heteroatoms can be the same or different and chosen from nitrogen, oxygen or sulfur, and the heterocycle can be unsubstituted or substituted once or several times; wherein in the case of heterocycle substitution, the substituents will be the same or different and may occupy any desired and possible position of the heteroaryl, and where the heterocycle may also be part of a bi- or polycyclic system; wherein, with respect to aryl and heteroaryl, by substituted once or several times a single or multiple substitution of one or more hydrogen atoms of the ring system is understood by substituents chosen from the group consisting of -F, -Cl, -Br , -I, -CN, -NO₂, -CHO, = O, -R⁰, -C (= O) R⁰, -C (= O) H, -C (= O) OH, -C (= O) OR⁰ , -C (= O) NH₂, -C (= O) NHR⁰, -C (= O) -N (R⁰) ₂, -OH, -O (CH₂) ₁₋₂O-, -OR⁰, -OC (= O) H, -OC (= O) R⁰, -OC (= O) OR⁰, -OC (= O) NHR⁰, -OC (= O) N (R⁰) ₂, -SH, -SR⁰, -SO₃H, - S (= O) ₁₋₂-R⁰, -S (= O) ₁₋₂NH₂, -NH₂, -NHR⁰, -N (R⁰) ₂, -N⁺ (R⁰) ₃, -N⁺ (R⁰) ₂O⁻ , -NH-C (= O) R⁰, -NHC (= O) OR⁰, -NH-C (= O) NH₂, -NHC (= O) NHR⁰, -NHC (= O) N (R⁰) ₂, - Yes (R⁰) ₃ or -PO (OR⁰) ₂; wherein any of the N atoms eventually existing in the ring may be oxidized in each case; where R⁰ represents -aliphatic C₁₋₈, -cycloaliphatic C₃₋₁₂, -aryl, -heteroaryl, -aliphatic C₁₋₈-cycloaliphatic C₃₋₁₂, -aliphatic C₁₋₈-aryl, -aliphatic C₁₋₈-heteroaryl, - C₃₋₈-aliphatic C₁₋₈ cycloaliphatic, C₃₋₈-arylcycloaliphatic or C₃₋₈-heteroaryl cycloaliphatic; in the form of an individual stereoisomer or a mixture, the free compounds and / or their physiologically compatible salts.
priorityDate 2013-02-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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