http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-112233-A1

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filingDate 2017-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_91a896e898b07e8760ff7635d36a5a01
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publicationDate 2019-10-09-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber AR-112233-A1
titleOfInvention CYCLIC AMINES OF 6 MEMBERS OR LACTAMS SUBSTITUTED WITH UREA AND PHENYL AS MODULATORS OF RPF2
abstract This compound acts as a modulator of FPR2 and can be used in the treatment and / or prevention of disorders that are at least partially mediated by FPR2. Claim 1: A compound according to the general formula (1) characterized in that: X² represents N (L-R⁴) and X¹, X³ and X⁴ represent CH₂; or X² represents N (L-R⁴) and X³ represents C (O) and X¹ and X⁴ represent CH₂; or X⁴ represents N (L-R⁴) and X³ represents CH₂ or C (O) and X¹ and X² represent CH₂; and n represents 0, 1 or 2; R¹ represents 5- or 6-membered phenyl or heteroaryl; R² represents H, F, Cl, Br, CN, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, CHF₂, CH₂F, CF₃, OH, OCHF₂, OCH₂F, OCF₃, O-C₁₋₆ alkyl, S-C₁₋₆ alkyl, S (O) -C₁₋₆alkyl, S (O) ₂-C₁₋₆ alkyl, O-C₃₋₆ cycloalkyl, S-C₃₋₆ cycloalkyl, S (O) -C₃₋₆ cycloalkyl, S (O) ₂ -C₃₋₆ cycloalkyl, NH₂, N (H) (C₁₋₆ alkyl), N (C₁₋₆ alkyl) ₂, N (H) (C₃₋₆ cycloalkyl), N (C₁₋₆ alkyl) (C₃₋ cycloalkyl *), NC (O) (C₁₋₆ alkyl), NC (O) (C₃₋₆ cycloalkyl), NC (O) (3-6 membered heterocycloalkyl); R³ represents F, Cl, Br, CHF₂, CH₂F, CF₃, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, O-C₁₋₆ alkyl, OCHF₂, OCH₂F, OCF₃, S (O) -C₁₋₆ alkyl, S (O ) -C₃₋₆ cycloalkyl, S (O) ₂-C₁₋₆ alkyl, S (O) ₂-C₃₋₆ cycloalkyl; L represents bond, C₁₋₆ alkylene, C₍O₎, S₍O₎₂, C₍CH₃) ₂; and R⁴ represents H, C₁₋₆ alkyl, C₃₋₆ cycloalkyl, 3-6 membered heterocycloalkyl, aryl, 5- or 6-membered heteroaryl, C (O) NH₂, C (O) N (H) (C₁₋₆ alkyl) , C (O) N (C₁₋₆ alkyl) ₂, C (O) N (H) (C₃₋₆ cycloalkyl), C (O) N (H) (3-6 membered heterocycloalkyl), C (O) N (H) (aryl), C (O) N (H) (5- or 6-membered heteroaryl), C (O) N (C₁₋₆ alkyl) (C₃₋₆ cycloalkyl), C (O) N (alkyl C₁₋₆) (3-6 membered heterocycloalkyl), C (O) N (C₁₋₆ alkyl) (aryl), C (O) N (C₁₋₆ alkyl) (5- or 6-membered heteroaryl), C ( O) N (C₃₋₆ cycloalkyl) (C₃₋₆ cycloalkyl), C (O) N (C₃₋₆ cycloalkyl) (3- to 6-membered heterocycloalkyl), C (O) N (C₃₋₆ cycloalkyl) (aryl) , C (O) N (C₃₋₆ cycloalkyl) (5- or 6-membered heteroaryl), C (O) O- (C₁₋₆ alkyl), C (O) O- (C₃₋₆ cycloalkyl), C (O ) O- (3-6 membered heterocycloalkyl), C (O) O- (aryl), C (O) O- (5- or 6-membered heteroaryl), S (O) -C₁₋₆alkyl, S (O ) ₂-C₁₋₆ alkyl, S (O) -C₃₋₆ cycloalkyl, S (O) ₂-C₃₋₆ cycloalkyl, C₁₋₆-OH alkylene, C₁₋₆-O-C₁₋₆ alkylene, C₁ alkylene ₋₆-cycloalkyl C₃₋₆, 3-6 membered C₁₋₆ alkylene-heterocycloalkyl, C₁₋₆ alkylene-aryl, 5- or 6-membered C₁₋₆ alkylene-heteroaryl; wherein C₁₋₆ alkyl in each case independently of one another is linear or branched, saturated or unsaturated; wherein C₁₋₆ alkylene is linear and saturated or unsaturated; wherein C₁₋₆ alkyl, C₁₋₆ alkylene, C₃₋₆ cycloalkyl and 3- to 6-membered heterocycloalkyl in each case independently of each other are unsubstituted or are mono- or polysubstituted with one or more substituents selected from F, Cl , CN, C₁₋₆ alkyl, CF₃, CF₂H, CFH₂, CF₂Cl, CFCl₂, C (O) -C₁₋₆ alkyl, C₍O₎₋OH, C₍O₎₋O₋ₐₗqᵘⁱₗₒ C₁₋₆, C₍O ₎₋NH₂, C (O) -N (H) (C₁₋₆ alkyl), C (O) -N (C₁₋₆ alkyl) ₂, OH, = O, OCF₃, OCF₂H, OCFH₂, OCF₂Cl, OCFCl₂, O -C₁₋₆ alkyl, OC (O) -C₁₋₆ alkyl, OC (O) -O-C₁₋₆ alkyl, O- (CO) -N (H) (C₁₋₆ alkyl), OC (O) - N (C₁₋₆ alkyl) ₂, OS (O) ₂-NH₂, OS (O) ₂-N (H) (C₁₋₆ alkyl), OS (O) ₂-N (C₁₋₆ alkyl) ₂, NH₂ , N (H) (C₁₋₆ alkyl), N (C₁₋₆ alkyl) ₂, N (H) -C (O) -C₁₋₆ alkyl, N (H) -C (O) -O-C₁ alkyl ₋₆, N (H) -C (O) -NH₂, N (H) -C (O) -N (H) (C₁₋₆ alkyl), N (H) -C (O) -N (C₁ alkyl ₋₆) ₂, N (C₁₋₆ alkyl) -C (O) -C₁₋₆ alkyl, N (C₁₋₆ alkyl) -C (O) -O-C₁₋₆ alkyl, N (C₁₋₆ alkyl) -C (O) -NH₂, N (C₁₋₆ alkyl) -C (O) -N (H) (C₁₋₆ alkyl), N (C₁₋₆ alkyl) -C (O) -N (C₁₋ alkyl ₆) ₂, N (H) -S (O) ₂OH, N (H) -S (O) ₂-alk C₁₋₆-yl, N (H) -S (O) ₂-O-C₁₋₆-alkyl, N (H) -S (O) ₂-NH₂, N (H) -S (O) ₂-N (H ) (C₁₋₆ alkyl), N (H) -S (O) ₂N (C₁₋₆ alkyl) ₂, N (C₁₋₆ alkyl) -S (O) ₂-OH, N (C₁₋₆ alkyl) - S (O) ₂-C₁₋₆ alkyl, N (C₁₋₆ alkyl) -S (O) ₂-O-C₁₋₆ alkyl, N (C₁₋₆ alkyl) -S (O) ₂-NH₂, N ( C₁₋₆ alkyl -S (O) ₂ -N (H) (C₁₋₆ alkyl), N (C₁₋₆ alkyl) -S (O) ₂ -N (C₁₋₆ alkyl) ₂, SCF₃, SCF₂H, SCFH₂, S-C₁₋₆ alkyl, S (O) -C₁₋₆ alkyl, S (O) ₂-C₁₋₆ alkyl, S (O) ₂-OH, S (O) ₂-O-C₁₋₆ alkyl , S (O) ₂-NH₂, S (O) ₂-N (H) (C₁₋₆ alkyl), S (O) ₂-N (C₁₋₆ alkyl) ₂, C₃₋₆ cycloalkyl, 3-6 heterocycloalkyl members, phenyl, 5- or 6-membered heteroaryl, O-C₃₋₆ cycloalkyl, O- (3-6-membered heterocycloalkyl), O-phenyl, O- (5- or 6-membered heteroaryl), C (O) -cycloalkyl C₃₋₆, C₍O₎₋₍ₕₑₜₑʳₒᶜⁱᶜₗₒₐₗqᵘⁱₗₒ ᵈₑ ₃ ₐ ₆ ₘⁱₑₘᵇʳₒₛ₎, C₍O₎₋ᶠₑₙⁱₗₒ, C₍O₎₋₍ₕₑₜₑʳₒₐʳⁱₗₒ ᵈₑ ₅ or ₆ ₘⁱₑₘᵇʳₒₛ₎, S₍O₎₂- (C₃₋₆ cycloalkyl ), S (O) ₂- (3- to 6-membered heterocycloalkyl), S (O) ₂-phenyl or S (O) ₂- (5- or 6-membered heteroaryl); wherein aryl, phenyl and 5 or 6 membered heteroaryl in each case independently of each other are unsubstituted or mono- or disubstituted with one or two substituents selected from F, Cl, Br, CN, C₁₋₆ alkyl, CF₃ , CF₂H, CFH₂, C₁₋₄-CF₃ alkylene, C₁₋₄-CF₂H alkylene, C₁₋₄-CFH₂ alkylene, C (O) -C₁₋₆ alkyl, C₍O₎₋OH, C₍O₎₋O₋ ₐₗqᵘⁱₗₒ C₁₋₆, C₍O₎₋N₍H₎₍OH₎, C₍O₎₋NH₂, C (O) -N (H) (C₁₋₆ alkyl), C (O) -N (C₁ alkyl ₋₆) ₂, OH, OCF₃, OCF₂H, OCFH₂, OCF₂Cl, OCFCl₂, O-C₁₋₆ alkyl, O-C₃₋₆ cycloalkyl, O- (3- to 6-membered heterocycloalkyl), O-phenyl, O- (heteroaryl 5 or 6-membered), NH₂, N (H) (C₁₋₆ alkyl), N (C₁₋₆ alkyl) ₂, N (H) -C (O) -Cal alkyl, N (C₁₋₆ alkyl ) -C (O) -C₁₋₆ alkyl, N (H) -C (O) -NH₂, N (H) -C (O) -N (H) (C₁₋₆ alkyl), N (H) - C (O) -N (C₁₋₆ alkyl) ₂, N (C₁₋₆ alkyl) -C (O) -N (H) (C₁₋₆ alkyl), N (C₁₋₆ alkyl) -C (O) -N (C₁₋₆ alkyl) ₂, N (H) -S (O) ₂-C₁₋₆ alkyl, SCF₃, S-C₁₋₆ alkyl, S (O) -C₁₋₆ alkyl, S (O) ₂ -C₁₋₆alkyl, S (O) ₂-NH₂, S (O) ₂-N (H) (C₁₋₆ alkyl), S (O) N-N (C₁₋₆ alkyl) ₂, cycloalkyl C₃₋₆, C₁₋₄ alkylene-C₃₋₆ cycloalkyl, 3 to 6 membered heterocycloalkyl, C₁₋₄ alkylene- (3 to 6 membered heterocycloalkyl), 5 or 6 membered phenyl or heteroaryl; in the form of the free compound or one of its physiologically acceptable salts.
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