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    DERIVATI AMINO-TRIAZOLOPIRIDINA
    5.
    发明专利
    DERIVATI AMINO-TRIAZOLOPIRIDINA 未知

    公开(公告)号：YU13502A

    公开(公告)日：2004-11-25

    申请号：YUP13502

    申请日：2000-08-28

    Applicant: HOFFMANN LA ROCHE

    Inventor： HUBER TROTTMANN GERDA ,  HUNKELER WALTER ,  JAKOB-ROETNE ROLAND ,  KILPATRICK GAVIN JOHN ,  NETTEKOVEN MATTHIAS HEINRICH ,  RIEMER CLAUS

    IPC: C07D213/73 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/635 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/08 ,  A61P43/00 ,  C07D409/04 ,  C07D471/04 ,  C07D519/00

    Abstract: Pronalazak se odnosi na jedinjenja formule I, naznacena time sto R1 perdstavlja 5-to ili 6-toclanu heteroarilnu grupu, koja sadrzi 1 do 3 heteroatoma, izabrana izmedju N, O ili S, i cije su grupe opciono supstituisane jednim ili sa dva supstituenta, koji su nizi alkil, -(CH2)nOH, halogen ili nizi alkoksi, i naznacena time sto heteroarilne grupe mogu biti opciono vezane za pirazolski prsten preko nekog alkilena ili alkenil grupe ili je to fenil, opciono supstituisan jednim ili sa dva supstituenta, koji su nizi alkil, hidroksi-nizi alkil, halogen, hidroksi ili nizi alkoksi ili je -O(CH2)nfenil, benzofuril, indolil ili benzotiofenil ili je -S-nizi alkil; R2 i R4 su nezavisno jedan od drugog, vodonik, cijano ili -S(O)2-fenil; R3 je vodonik, halogen ili 5-to ili 6-toclana heteroarilna grupa, koja sadrzi 1 do 3 heteroatoma, izabrana izmedju N, O ili S i gde su grupe opciono supstituisane jednim ili sa dva supstituenta, koji su nizi alkil, -(CH2)n-aril, hldroksi, halogen, nizi alkoksi, morfolinil, amino, nizi alkilamino ili -C(O)NR'2, naznaceno time sto je R* nizi alkil ili vodonik ili je fenil, opciono supstituisan jednim ili sa dva supstituenta koji su halogen, nizi alkoksi, amino, di-nizi alkil amino, CF3, -OCF3, -NHC(O)nizi alkil cijano, -C(O)-nizi alkil, -C(O)O-nizi alkil, -S-nizi alkil, -S(O)2NH-fenil, -S(O)2metilpiperazinil; ili je NR'R", naznacen time sto su R' i R", nezavisno jedan od drugog, vodonik, -(CH2)nfenil, koji je opciono supstituisan halogenom ili nizom alkoksi grupom, -CH(nizi alkil)-fenil, indan-1-il, 1,2,3,4-tetrahidro-naftalen ili cikloalkil; ili je O-fenil, ciji je fenilni prsten opciono supstituisan halogenom, nizom alkil ili nizom alkoksi grupom, -O-tetraidronaftalenil ili -O-CH2-6-metil-piridin-2-il; ili je -benzol[1,3]dioksolil, -1H-indol-5-il, naftil, benzofuran-2-il, 1,3,4,9-tetrahidro-b-karbolin-2-il, piperidin-1-il, pirolidin-1-il, piperazin-4-il-metil ili morfolinil; R5 je -NR2, pri cemu R moze ili ne mora biti vodonik, nizi alkil, fenil, benzil, -CO-nizi alkil, -CO-nizi alkoksi, -nizi alkenil, -CO(CH2)n-fenil ili -COO(CH2)n-fenil, naznacen time sto je fenilni prsten opciono supstituisan sa CF3 nizom alkoksi, halogen ili nizom alkil grupom, -CO(CH2)3-NHCO-nizi alkoksi, -(CH2)n-fenil, naznacen time, sto je fenilni prsten opciono supstituisan nizom alkoksi, CF3 ili halogenom ili je 4,5-dihidro-1H-imidazol-2-il-benzojeva kiselina, 1,4,5,6-tetrahidro-pirimidin-2-il-benzojeva kiselina ili 4,5,6,7-tetrahidro-1H-[1,3]diazepin-2-il-benzojeva kiselina; n je 0-4, i njihove farmaceutski prihvatljive soli.

    6.
    发明专利
    未知

    公开(公告)号：NO20021077D0

    公开(公告)日：2002-03-05

    申请号：NO20021077

    申请日：2002-03-05

    Applicant: HOFFMANN LA ROCHE

    Inventor： TROTTMANN GERDA HUBER ,  HUNKELER WALTER ,  JAKOB-ROETNE ROLAND ,  KILPATRICK GAVIN JOHN ,  NETTEKOVEN MATTHIAS HEINRICH ,  RIEMER CLAUS

    IPC: C07D213/73 ,  A61K31/437 ,  A61K31/4418 ,  A61K31/444 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  A61K31/635 ,  A61P9/10 ,  A61P11/06 ,  A61P11/16 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P37/08 ,  A61P43/00 ,  C07D409/04 ,  C07D471/04 ,  C07D519/00 ,  C07D

    Abstract: The invention relates to compounds of formulawhereinR1 is a 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)nOH, halogen or lower alkoxy, and wherein the heteroaryl groups may be optionally linked to the pyrazole ring via an alkylene or alkenyl group, or isphenyl, optionally substituted by one or two substituents being lower alkyl, hydroxy-lower alkyl, halogen, hydroxy or lower alkoxy or is-O(CH2)n,phenyl, benzofuryl, indolyl or benzothiophenyl, or is-S-lower alkyl;R2 and R4 are independently from each other hydrogen, cyano or -S(O)2-phenyl;R3 is hydrogen, halogen or isa 5 or 6 membered heteroaryl group, containing 1 to 3 heteroatoms, selected from N, O or S, and which groups are optionally substituted by one or two substituents, which are lower alkyl, -(CH2)n-aryl, hydroxy, halogen, lower alkoxy, morpholinyl, amino, lower alkylamino or -C(O)NR'2, and wherein R' is lower alkyl or hydrogen, or isphenyl, optionally substituted by one or two substituents being halogen, lower alkyl, lower alkoxy, amino, di-lower alkyl amino, CF3, -OCF3, -NHC(O)lower alkyl, cyano, -C(O)-lower alkyl, -C(O)O-lower alkyl, -S-lower alkyl, -S(O)2NH-phenyl, -S(O)2-methylpiperazinyl; or is-NR'R'', wherein R' and R'' are independently from each other hydrogen, -(CH2)nphenyl, which phenyl ring is optionally substituted by halogen or lower alkoxy, -CH(lower alkyl)-phenyl, indan-1-yl, 1,2,3,4-tetrahydro-naphthalen, or cycloalkyl; or is-O-phenyl, which phenyl ring is optionally substituted by halogen, lower alkyl or lower alkoxy, -O-tetrahydronaphthalenyl or -O-CH2-6-methyl-pyridin-2-yl; or is-benzo[1,3]dioxolyl, -1H-indol-5-yl, naphthyl, benzofuran-2-yl, 1,3,4,9-tetrahydro-b-carbolin-2-yl, piperidin-1-yl, pyrrolidin-1-yl, piperazin-4-yl-methyl or morpholinyl;R5 is -NR2, wherein R may be the same or different and is hydrogen, lower alkyl, phenyl, benzyl, -CO-lower alkyl, -CO-lower alkoxy, -lower alkenyl, -CO(CH2)n-phenyl or -COO(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by CF3, lower alkoxy, halogen or lower alkyl, -CO(CH2)3-NHCO-lower alkoxy, -(CH2)n-phenyl, wherein the phenyl ring is optionally substituted by lower alkoxy, CF3 or halogen, or is 4,5-dihydro-1H-imidazol-2-yl-benzoic acid, 1,4,5,6-tetrahydro-pyrimidin-2-yl-benzoic acid or 4,5,6,7-tetrahydro-1H-[1,3]diazepin-2-yl-benzoic acid;n is 0-4and their pharmaceutically acceptable salts

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