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    61.
    发明专利
    未知

    公开(公告)号：NO992873L

    公开(公告)日：1999-12-13

    申请号：NO992873

    申请日：1999-06-11

    Applicant: HOFFMANN LA ROCHE

    Inventor： ADAM GEO ,  CESURA ANDREA ,  JENCK FRANCOIS ,  KOLCZEWSKI SABINE ,  ROEVER STEPHAN ,  WICHMANN JUERGEN

    IPC: C07D401/00 ,  A61K31/00 ,  A61K31/438 ,  A61P3/04 ,  A61P9/10 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D471/10 ,  A61K31/395

    Abstract: The invention relates to compounds of the general formula wherein R is C6-12-cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicycloÄ3.3.1Ünon-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicycloÄ6.2.0Üdec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl; R is =O or hydrogen, R is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, -CH2OR or -CH2N(R )2; R is hydrogen or -CH2OR ; R is hydrogen or lower alkyl; A &cir& is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are agonists and/or antagonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    DIAZA-SPIRO[3,5]NANONE DERIVATIVES
    62.
    发明专利
    DIAZA-SPIRO[3,5]NANONE DERIVATIVES 未知

    公开(公告)号：HU9901911D0

    公开(公告)日：1999-08-30

    申请号：HU9901911

    申请日：1999-06-09

    Applicant: HOFFMANN LA ROCHE

    Inventor： ADAM GEO ,  CESURA ANDREA ,  JENCK FRANCOIS ,  KOLCZEWSKI SABINE ,  ROEVER STEPHAN ,  WICHMANN JUERGEN

    IPC: C07D401/00 ,  A61K31/00 ,  A61K31/438 ,  A61P3/04 ,  A61P9/10 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D471/10

    Abstract: The invention relates to compounds of the general formula wherein R is C6-12-cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicycloÄ3.3.1Ünon-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicycloÄ6.2.0Üdec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl; R is =O or hydrogen, R is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, -CH2OR or -CH2N(R )2; R is hydrogen or -CH2OR ; R is hydrogen or lower alkyl; A &cir& is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are agonists and/or antagonists of the orphamin FQ (OFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    N-(4-ARYL-THIAZOL-2-YL) SULPHONAMIDE DERIVATIVES AND MEDICAMENTS THEREOF
    66.
    发明专利
    N-(4-ARYL-THIAZOL-2-YL) SULPHONAMIDE DERIVATIVES AND MEDICAMENTS THEREOF 未知

    公开(公告)号：NZ328331A

    公开(公告)日：1999-05-28

    申请号：NZ32833197

    申请日：1997-07-14

    Applicant: HOFFMANN LA ROCHE

    Inventor： CESURA ANDREA ,  ROVER STEPHAN

    IPC: C07D277/20 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61P9/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P31/00 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D277/00 ,  C07D277/02 ,  C07D277/22 ,  C07D277/50 ,  C07D277/52 ,  C07D417/12

    Abstract: The use of compounds of formula (I) and their salts is claimed as kynurenine-3-hydroxylase inhibitors for treatment of neurodegenerative disorders, neurological disorders caused by activation of the immune system and psychiatric disorders. R = lower alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower alkyl, lower alkoxy, lower alkylcarbonylamino, halo, cycloalkyl, NO2, NH2, methylenedioxy, phenoxy or benzyloxy groups; the aromatic rings may themselves be substituted by NO2, halo or NH2; R1 - R4 = H, halo, OH, lower alkyl, NO2, CN, NH2, lower alkoxy, benzyloxy, CF3 or phenyl, optionally substituted by one or more lower alkyl, CF3, NO2, NH2 or OH groups; or R1+R2 or R2+R3 = a benzene ring, optionally substituted by halo, CF3, NO2, lower alkyl or lower alkoxy. Also claimed are new compounds of formula (IA) - (IE). (N.B. compounds (IA) are described as being compounds of formula (I) but the aryl group is attached the 5- not the 4-position.) R5 = H or lower alkoxy; R6 = H, lower alkyl, lower alkoxy, cycloalkyl or benzyl; n = 0 or 1; or R5+R6 = methylenedioxy. provided that R5 and R6 cannot both be H. R7 - R9 = H, halo, lower alkoxy or 4-NO2-phenoxy, provided that at least one of R7 - R9 = halo. R10 = NH2 or NHCOR12; R12 = lower alkyl; R11 = H, OH, NO2, CN, NH2, CF3, benzyloxy or phenyl, optionally substituted by one or more lower alkyl, CF3, NO2, NH2 or OH groups; or R11+R3 = a phenyl ring.

    N-(4-aryl-thiazol-2-yl)-sulphonamide derivatives and their use
    69.
    发明专利
    N-(4-aryl-thiazol-2-yl)-sulphonamide derivatives and their use 未知

    公开(公告)号：AU2875297A

    公开(公告)日：1998-01-29

    申请号：AU2875297

    申请日：1997-07-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： CESURA ANDREA ,  ROVER STEPHAN

    IPC: C07D277/20 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61P9/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P31/00 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D277/00 ,  C07D277/02 ,  C07D277/22 ,  C07D277/50 ,  C07D277/52 ,  C07D417/12

    Abstract: The use of compounds of formula (I) and their salts is claimed as kynurenine-3-hydroxylase inhibitors for treatment of neurodegenerative disorders, neurological disorders caused by activation of the immune system and psychiatric disorders. R = lower alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower alkyl, lower alkoxy, lower alkylcarbonylamino, halo, cycloalkyl, NO2, NH2, methylenedioxy, phenoxy or benzyloxy groups; the aromatic rings may themselves be substituted by NO2, halo or NH2; R1 - R4 = H, halo, OH, lower alkyl, NO2, CN, NH2, lower alkoxy, benzyloxy, CF3 or phenyl, optionally substituted by one or more lower alkyl, CF3, NO2, NH2 or OH groups; or R1+R2 or R2+R3 = a benzene ring, optionally substituted by halo, CF3, NO2, lower alkyl or lower alkoxy. Also claimed are new compounds of formula (IA) - (IE). (N.B. compounds (IA) are described as being compounds of formula (I) but the aryl group is attached the 5- not the 4-position.) R5 = H or lower alkoxy; R6 = H, lower alkyl, lower alkoxy, cycloalkyl or benzyl; n = 0 or 1; or R5+R6 = methylenedioxy. provided that R5 and R6 cannot both be H. R7 - R9 = H, halo, lower alkoxy or 4-NO2-phenoxy, provided that at least one of R7 - R9 = halo. R10 = NH2 or NHCOR12; R12 = lower alkyl; R11 = H, OH, NO2, CN, NH2, CF3, benzyloxy or phenyl, optionally substituted by one or more lower alkyl, CF3, NO2, NH2 or OH groups; or R11+R3 = a phenyl ring.

    70.
    发明专利
    未知

    公开(公告)号：NO973338L

    公开(公告)日：1998-01-20

    申请号：NO973338

    申请日：1997-07-18

    Applicant: HOFFMANN LA ROCHE

    Inventor： CESURA ANDREA ,  ROEVER STEPHAN

    IPC: C07D277/20 ,  A61K31/00 ,  A61K31/425 ,  A61K31/426 ,  A61K31/427 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4439 ,  A61P9/00 ,  A61P25/00 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/28 ,  A61P31/00 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D277/00 ,  C07D277/02 ,  C07D277/22 ,  C07D277/50 ,  C07D277/52 ,  C07D417/12

    Abstract: The use of compounds of formula (I) and their salts is claimed as kynurenine-3-hydroxylase inhibitors for treatment of neurodegenerative disorders, neurological disorders caused by activation of the immune system and psychiatric disorders. R = lower alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower alkyl, lower alkoxy, lower alkylcarbonylamino, halo, cycloalkyl, NO2, NH2, methylenedioxy, phenoxy or benzyloxy groups; the aromatic rings may themselves be substituted by NO2, halo or NH2; R1 - R4 = H, halo, OH, lower alkyl, NO2, CN, NH2, lower alkoxy, benzyloxy, CF3 or phenyl, optionally substituted by one or more lower alkyl, CF3, NO2, NH2 or OH groups; or R1+R2 or R2+R3 = a benzene ring, optionally substituted by halo, CF3, NO2, lower alkyl or lower alkoxy. Also claimed are new compounds of formula (IA) - (IE). (N.B. compounds (IA) are described as being compounds of formula (I) but the aryl group is attached the 5- not the 4-position.) R5 = H or lower alkoxy; R6 = H, lower alkyl, lower alkoxy, cycloalkyl or benzyl; n = 0 or 1; or R5+R6 = methylenedioxy. provided that R5 and R6 cannot both be H. R7 - R9 = H, halo, lower alkoxy or 4-NO2-phenoxy, provided that at least one of R7 - R9 = halo. R10 = NH2 or NHCOR12; R12 = lower alkyl; R11 = H, OH, NO2, CN, NH2, CF3, benzyloxy or phenyl, optionally substituted by one or more lower alkyl, CF3, NO2, NH2 or OH groups; or R11+R3 = a phenyl ring.

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