HRP20161260T1 - Derivati (r)-arilkilamina i farmaceutski pripravci koji ih sadrže - Google Patents

Derivati (r)-arilkilamina i farmaceutski pripravci koji ih sadrže Download PDF

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HRP20161260T1
HRP20161260T1 HRP20161260TT HRP20161260T HRP20161260T1 HR P20161260 T1 HRP20161260 T1 HR P20161260T1 HR P20161260T T HRP20161260T T HR P20161260TT HR P20161260 T HRP20161260 T HR P20161260T HR P20161260 T1 HRP20161260 T1 HR P20161260T1
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ethyl
phenyl
benzoylphenyl
amino
methyl
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HRP20161260TT
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Marcello Allegretti
Alessio Moriconi
Andrea Aramini
Maria Candida Cesta
Andrea Beccari
Riccardo Bertini
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Dompé Farmaceutici S.P.A.
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Publication of HRP20161260T1 publication Critical patent/HRP20161260T1/hr

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    • C07D213/04Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
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    • C07D295/145Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/15Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with the ring nitrogen atoms and the carbon atoms with three bonds to hetero atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
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Claims (7)

1. (R)-Arilalkilamino derivati formule (I): [image] u kojoj R je - 2-tiazolil, nesupstituiran ili supstituiran sa grupom izabranom od metila ili trifluorometila; - CORa, SO2Ra gdje Ra je izabran od: - C1-C5-alkil, C3-C5-cikloalkil; - fenil, 2-piridil, 2-furil, 2-tiofenil grupa; - grupe formule II, [image] gdje X predstavlja: linearni ili razgranati C1-C6 alkilen, R2 i R3 zajedno sa N atomom za koji su vezani, formiraju 4-6 –člani heterociklični prsten koji sadrži dušik formule (III) [image] gdje Y predstavlja CH2, i p predstavlja cijeli broj od 0 do 2; R1 je metil; Ar je izabran od: 3’ -benzoilfenila, 3’ -(4-kloro-benzoil)-fenila, 3 ’ -(4-metil-benzoil)-fenila, 4’-trifluorometansulfoniloksi-fenila, 4’-benzensulfoniloksi-fenila, 3’-(furan-2-karbonil)-fenila.
2. Spoj izabran od: 4-{(1R)-1-[(fenilsulfonil)amino]etil}fenil trifluorometansulfonata N-[(1R)-1-(3-benzoilfenil)etil]benzensulfonamida 4-{(1R)-1-[(piridin-3-ilsulfonil)amino]etil}feniltrifluorometansulfonata N-[(1R)-1-(3-benzoilfenil)etil]metansulfonamida N-{(1R)-1-[3-(2-furoil)fenil]etil}tiofen-2-sulfonamida N-{(1R)-1-[3-(2-furoil)fenil]etil}metansulfonamida 4-{(1R)-1-[(tien-2-ilsulfonil)amino]etil}fenil trifluorometansulfonata N-[(1R)-1-(3-benzoilfenil)etil]tiofen-2-sulfonamida N-[(1R)-1-(3-benzoilfenil)etil]-3-pirolidin-1-ilpropan-1-sulfonamida metil 5-({[(1R)-1-(3-benzoilfenil)etil]amino}sulfonil)-2-furoata 5-({[(1R)-1-(3-benzoilfenil)etil]amino}sulfonil)-2-furoinske kiseline 4-{(1R)-2-metil-1-[(metilsulfonil)amino]propil}feniltrifluorometansulfonata N-((1R)-1-{4-[1-metil-1-(fenilsulfonil)etil]fenil}etil)metansulfonamida 4-[(1R)-1-(izobutirilamino)etil]feniltrifluorometansulfonata 4-{[(1R)-1-(piridin-3-ilkarbonil)amino]etil]}feniltrifluorometansulfonata N-[(1R)-1-(3-benzoilfenil)etil]benzamida N-[(1R)-1-(3-benzoilfenil)etil]-2-furamida N-[(1R)-1-(3-benzoilfenil)etil]ciklobutankarboksamida N-[(1R)-1-(4-trifluorometansulfoniloksi)feniletil]-4-piperidin-1-ilbutanamida 4-{(1R)-1-[(4-pirolidin-1-ilbutanoil)amino]etil]}fenil trifluorometansulfonata 3-{(1R)-1-[4-(4-trifluorometil-1,3-tiazol-2-il)amino]etil}fenil) (fenil)metanona.
3. Spojevi prema patentnom zahtjevu 1 ili 2, za uporabu kao lijekovi.
4. Spojevi prema patentnom zahtjevu 1 ili 2, za uporabu kao lijek za liječenje bolesti koje uključuju kemotaksiju humanih PMN induciranu sa C5a.
5. Spojevi za uporabu prema patentnom zahtjevu 4 naznačeni time što navedene bolesti su: sepsa, psorijaza, bulozni pemfigoid, reumatoidni artritis, ulcerozni kolitis, akutni respiratorni distres sindrom, idiopatska fibroza, cistična fibroza, kronična opstruktivna bolest pluća, glomerulonefritis i u prevenciji i liječenju povrede uzrokovane ishemijom i reperfuzijom.
6. Postupak za pripremu spojeva formule (I) [image] gdje R je CORa ili SO2Ra i Ra je kao što je definiran u patentnom zahtjevu 1, koji sadrži reakciju između (R)-arilalkilamina formule (IV) [image] gdje Ar i R1 su kao što su definirani u patentnom zahtjevu 1, sa odgovarajućim acil ili sulfonil kloridima.
7. Farmaceutski pripravci koji sadrže spoj prema patentnom zahtjevu 1 ili 2 u smjesi sa njihovim pogodnim nosačem.
HRP20161260TT 2005-11-24 2016-10-03 Derivati (r)-arilkilamina i farmaceutski pripravci koji ih sadrže HRP20161260T1 (hr)

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EP05111257 2005-11-24
PCT/EP2006/068867 WO2007060215A2 (en) 2005-11-24 2006-11-24 (r)-arylkylamino derivatives and pharmaceutical compositions containing them
EP06819736.7A EP1951663B1 (en) 2005-11-24 2006-11-24 (r)-arylkylamino derivatives and pharmaceutical compositions containing them

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CA (1) CA2629935C (hr)
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