公开(公告)号：ES2307230T3

公开(公告)日：2008-11-16

申请号：ES05825935

申请日：2005-12-05

Applicant: HOFFMANN LA ROCHE

Inventor： BUETTELMANN BERND ,  KNUST HENNER ,  THOMAS ANDREW WILLIAM

IPC: C07D487/14 ,  A61K31/5517

Abstract: Derivados de imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepina de la fórmula (Ver fórmula) en la que R 1 es hidrógeno, halógeno, alquilo inferior, alquilo inferior sustituido por halógeno, alcoxi inferior, alcoxi inferior sustituido por halógeno, nitro, cicloalquilo, -O(CH2)mO(CH2)mOH o -C*C-R''; R 2 es hidrógeno o metilo; R 3 es alquilo inferior, alquilo inferior sustituido por halógeno, alquenilo inferior, alquenilo inferior sustituido por halógeno, alquinilo inferior, -(CH2)n-cicloalquilo, -(CR''R'''')m-CH3, o es fenilo, sin sustituir o sustituido por halógeno, o es piridinilo o tienilo, sin sustituir o sustituidos por alquilo inferior, o es -(CH2)n-NH-cicloalquilo, (alquenilo inferior)-cicloalquilo, (alquinilo inferior)-(CR''R'''')mOH, o es (alquinilo inferior)-fenilo, en el que el anillo fenilo está sin sustituir o sustituido por halógeno, CF3, alquilo inferior o alcoxi inferior; R'' es hidrógeno o alquilo inferior; R'''' es hidrógeno, hidroxi o alquilo inferior; n es 0, 1 ó 2; m es 1, 2 ó 3; o es 1 ó 2; y sus sales de adición de ácido farmacéuticamente aceptables, en donde "alquilo inferior" y "alcoxilo inferior" denotan grupos que contienen 1-7 átomos de carbono; y en donde "alquenilo inferior" y "alquinilo inferior" denotan grupos que contienen 2-7 átomos de carbono.

公开(公告)号：BRPI0517929A

公开(公告)日：2008-10-21

申请号：BRPI0517929

申请日：2005-10-25

Applicant: HOFFMANN LA ROCHE

Inventor： MASCIADRI RAFFAELLO ,  RATNI HASANE ,  MALHERBE PARICHEHR ,  NORCROSS ROGER DAVID ,  THOMAS ANDREW WILLIAM

IPC: C07D215/18 ,  A61K31/4738 ,  A61P25/22 ,  C07D215/20 ,  C07D215/38 ,  C07D401/04 ,  C07D419/04

Abstract: The present invention relates to compounds of formula I wherein R1 to R6 are as described herein, which compounds are active at the GABAB receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.

公开(公告)号：DE602005008633D1

公开(公告)日：2008-09-11

申请号：DE602005008633

申请日：2005-10-04

Applicant: HOFFMANN LA ROCHE

Inventor： KNUST HENNER ,  STADLER HEINZ ,  THOMAS ANDREW WILLIAM

IPC: A61K31/5517 ,  A61P25/00 ,  A61P25/18 ,  A61P25/22 ,  A61P25/28 ,  A61P43/00

Abstract: The present invention is concerned with a method of treating Alzheimer's disease by administering a therapeutically effective amount of a substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine of formula I wherein R1, R2, and R3 are as defined herein, and their pharmaceutically acceptable acid addition salts. The invention also provides novel compounds of formula I-A and pharmaceutical compositions containing them.

公开(公告)号：AU2003236719B2

公开(公告)日：2008-06-05

申请号：AU2003236719

申请日：2003-06-07

Applicant: HOFFMANN LA ROCHE

Inventor： JOLIDON SYNESE ,  WYLER RENE ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  THOMAS ANDREW WILLIAM

IPC: A61P3/04 ,  A61K31/16 ,  A61K31/165 ,  A61K31/166 ,  A61K31/275 ,  A61K31/277 ,  A61P25/00 ,  A61P25/02 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P43/00 ,  C07B53/00 ,  C07C20060101 ,  C07C1/00 ,  C07C231/02 ,  C07C231/14 ,  C07C231/16 ,  C07C233/65 ,  C07C233/69 ,  C07C233/83 ,  C07C235/48 ,  C07C235/50 ,  C07C237/06 ,  C07C253/30 ,  C07C255/24 ,  C07C255/29 ,  C07C255/44 ,  C07C255/55

Abstract: The invention relates to fluorobenzamide derivatives of the formula wherein R 1 , R 2 , R 3 R 4 , R 5 , R 6 and R 7 are as defined herein. =, The compounds of the invention are selective monoamine oxidase B inhibitors and therefore they are suitable for the treatment of diseases mediated by monoamine oxidase B, such as Alzheimer's disease or senile dementia.

公开(公告)号：AU2003205677B2

公开(公告)日：2008-04-24

申请号：AU2003205677

申请日：2003-01-27

Applicant: HOFFMANN LA ROCHE

Inventor： THOMAS ANDREW WILLIAM ,  CESURA ANDREA ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  WYLER RENE

IPC: C07D213/82 ,  A61K31/44 ,  A61K31/455 ,  A61P3/04 ,  A61P25/00 ,  A61P25/02 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/32 ,  A61P25/34 ,  A61P43/00 ,  C07D213/81

Abstract: Disclosed are pyridine amido derivatives of the formulawherein X, Y, and R to R are as defined herein. These compounds are selective MAO-B inhibitors and are useful in treating diseases such as, for example, Alzheimer's and senile dementia. Also disclosed are pharmaceutical compositions containing such compounds and a method of preparing such compounds.

公开(公告)号：MY133332A

公开(公告)日：2007-11-30

申请号：MYPI20033558

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

Inventor： IDING HANS ,  JOLIDON SYNESE ,  KRUMMENACHER DANIELA ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  THOMAS ANDREW WILLIAM ,  WIRZ BEAT ,  WOSTL WOLFGANG ,  WYLER RENE

IPC: A61K31/40 ,  C07D207/26 ,  A61K31/4015 ,  A61K31/44 ,  A61P25/16 ,  A61P25/28 ,  C07D207/273 ,  C07D207/277 ,  C07D401/04 ,  C07D401/06

Abstract: RACEMIC OR ENANTIOMERICALLY PURE 4-PYRROLIDINO DERIVATIVES, PROCESSES FOR THEIR PEREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING SAID DERIVATIVES, AND THEIR USE IN THE PREVENTION AND TREATMENT OF A DISEASE WHICH IS MEDIATED BY A MONOAMINE OXIDASE B INHIBITOR, IN PARTICULAR ALZHEIMER'S DISEASE AND SENILE DEMENTIA.

公开(公告)号：JO2385B1

公开(公告)日：2007-06-17

申请号：JOP20030170

申请日：2003-12-11

Applicant: HOFFMANN LA ROCHE

Inventor： PINARD EMMANUEL ,  THOMAS ANDREW WILLIAM ,  ROSA MARIA RODRIGUEZ

Abstract: This invention relates to 3H- quinazoline -4- one derivative as defined in the specification and claims, to a process fro their preparation, to pharmaceutical compositions comprising them and to their use as selective monoamine oxidase B inhibitors.

公开(公告)号：NZ538049A

公开(公告)日：2007-05-31

申请号：NZ53804903

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

Inventor： JOLIDON SYNESE ,  THOMAS ANDREW WILLIAM ,  WOSTL WOLFGANG ,  WYLER RENE ,  RODRIGUEZ-SARMIENTO ROSA MARIA

IPC: A61K31/4015 ,  A61P25/16 ,  A61P25/28 ,  C07D207/26 ,  C07D207/273 ,  C07D207/277 ,  C07D401/04

Abstract: Disclosed are compounds of formula I and processes of preparing them wherein: X-Y is -CH2-CH2-, -CH=CH- or -CH2O-; R1, R1.1 and R1.2 independently from each other are selected from the group consisting of H, halogen, cyano, alkyl, halogen-alkyl, alkoxy or halogen-alkoxy; R21, R22 and R23 independently from each other are selected from the group consisting of H and halogen; R24 is H, halogen or methyl; R3 is H; R4 is -CONHR5, -CH or -NHR6; R5 is H or alkyl; and R6 is -CO-H, -CO-alkyl, -CO-halogen-alkyl, -CO-O-alkyl, -CO-NH2 or -SO2-alkyl. Compounds of the type disclosed are monoamine oxidase B (MOAB) inhibitors useful in the treatment of diseases such as Alzheimer's disease and senile dementia.

公开(公告)号：NO20071967L

公开(公告)日：2007-05-14

申请号：NO20071967

申请日：2007-04-17

Applicant: HOFFMANN LA ROCHE

Inventor： THOMAS ANDREW WILLIAM ,  KNUST HENNER

IPC: C07D487/14 ,  A61P25/00

Abstract: The present invention is concerned with substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1 is hydrogen, halogen, lower alkyl, lower alkynyl, cycloalkyl, heterocycloalkyl, benzyl, cyano, lower alkoxy, OCF3, -NHR, -NHC(O)R or -NHSO2R; R2 is lower alkyl substituted by halogen; R3 is hydrogen, methyl or aryl; R is lower alkyl, cycloalkyl or aryl; and pharmaceutically acceptable acid addition salts thereof.

公开(公告)号：NO20072046L

公开(公告)日：2007-04-26

申请号：NO20072046

申请日：2007-04-20

Applicant: HOFFMANN LA ROCHE

Inventor： THOMAS ANDREW WILLIAM ,  KNUST HENNER

IPC: C07D487/14 ,  A61P25/00

Abstract: The invention relates to halogen substituted imidazo[1,5-a][1,2,4]triazolo[1,5-d][1,4]benzodiazepine derivatives of formula I wherein R1, R2, R3, R4 and n are as defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The compounds can be used as a cognitive enhancer or for the treatment of cognitive disorders, anxiety, Alzheimer's disease and schizophrenia.