公开(公告)号：MX2011008360A

公开(公告)日：2011-08-24

申请号：MX2011008360

申请日：2010-02-19

Applicant: HOFFMANN LA ROCHE

Inventor： KUHN BERND ,  PETERS JENS-UWE ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  RUDOLPH MARKUS ,  KOERNER MATTHIAS ,  ALBERATI DANIELA ,  ROGERS-EVANS MARK

IPC: C07D403/14 ,  A61K31/501 ,  A61P25/00 ,  A61P25/18

Abstract: La presente invención trata de los derivados de piridazinona novedosos de la fórmula (I) en donde R', R2, R3 y R4 son como se definiera en la descripción y en las reivindicaciones, así como también sales y ésteres fisiológicamente aceptables de los mismos. Estos compuestos inhiben la PDE10A y se pueden utilizar como medicamentos.

公开(公告)号：MX2011002755A

公开(公告)日：2011-04-07

申请号：MX2011002755

申请日：2009-09-15

Applicant: HOFFMANN LA ROCHE

Inventor： JAESCHKE GEORG ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  STEWARD LUCINDA ,  GOBBI LUCA

IPC: C07D498/04 ,  A61K31/437 ,  A61P25/30

Abstract: La presente invención se refiere a compuestos de la fórmula general (I), que tienen afinidad y selectividad para los receptores de dopamina D3, su manufactura, composiciones farmacéuticas que los contienen y su uso como medicamentos. Los compuestos activos de la presente invención son útiles para el tratamiento terapéutico y/o profiláctico de trastornos cognitivos.

公开(公告)号：AU2009294695A1

公开(公告)日：2010-03-25

申请号：AU2009294695

申请日：2009-09-11

Applicant: HOFFMANN LA ROCHE

Inventor： GOBBI LUCA ,  JAESCHKE GEORG ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  STEWARD LUCINDA

IPC: C07D261/20 ,  A61K31/496 ,  A61P25/00 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D413/12 ,  C07D493/08

Abstract: The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.

公开(公告)号：MY139027A

公开(公告)日：2009-08-28

申请号：MYPI20031959

申请日：2003-05-28

Applicant: HOFFMANN LA ROCHE

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

IPC: A61P3/00 ,  C07C233/05 ,  A61K31/15 ,  A61K31/167 ,  A61K31/216 ,  A61K31/275 ,  A61P3/04 ,  A61P25/00 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P25/34 ,  A61P29/00 ,  A61P43/00 ,  C07C231/02 ,  C07C233/15 ,  C07C233/25 ,  C07C233/33 ,  C07C233/60 ,  C07C235/16 ,  C07C237/04 ,  C07C237/22 ,  C07C243/14 ,  C07C243/28 ,  C07C255/19 ,  C07C255/23 ,  C07C255/25 ,  C07C255/58 ,  C07C259/06 ,  C07C323/41

Abstract: THIS INVENTION RELATES TO N-ACYLAMINO ARYL DERIVATIVES OF THE GENERAL FORMULA WHEREIN R1 IS HALOGEN, HALOGEN-(C1-C6)-ALKYL, CYANO, C1-C6-ALKOXY OR HALOGEN-(C1-C6)-ALKOXY; R21, R22, R23 AND R24 INDEPENDENTLY FROM EACH OTHER ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, (C1-C6)-ALKYL, HALOGEN, HALOGEN-( C1-C6)-ALKYL, HYDROXY, C1-C6-ALKOXY OR -CHO; R3 IS HYDROGEN OR C1-C3-ALKYL; R4, R5 INDEPENDENTLY FROM EACH OTHER ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, C1-C6-ALKYL, C1-C6-ALKOXY OR - COO (C1-C6) ALKYL; OR R4 AND R5 FORM TOGETHER WITH THE C-ATOM TO WHICH THEY ARE ATTACH A C3-C7-CYCLOALKYL RING; R6 IS - CO- NR7R8; - COO (C1-C6)-ALKYL, -CN, -NR2 OR - NHC (O) R; R7 AND R8 INDEPENDENTLY FROM EACH OTHER ARE SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, C1-C6-ALKYL, NH2 OR HYDROXY; R IS HYDROGEN OR C1-C6-ALKYL; N IS 0, 1, 2 OR 3. X IS -CHRO, -OCHR-, -CH2S-, -SCH2-, -CH2CH2-, -CH=CH- OR -C=C-; AND TO PHARMACEUTICALLY ACTIVE ACID ADDITION SALTS THEREOF. IT HAS BEEN FOUND THAT THE COMPOUNDS OF GENERAL FORMULA I ARE SELECTIVE MONOAMINE OXIDASE B INHIBITORS AND THEY ARE THEREFORE USEFUL IN THE TREATMENT OF DISEASES MEDIATED BY MONOAMINE OXIDASE B INHIBITORS, FOR EXAMPLE FOR THE TREATMENT OF ALZHEIMER'S DISEASE OR SENILE DEMENTIA.

公开(公告)号：AU2003267381B2

公开(公告)日：2009-08-27

申请号：AU2003267381

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

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

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

Abstract: The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, e.g. which are mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.

公开(公告)号：NO20091675L

公开(公告)日：2009-05-28

申请号：NO20091675

申请日：2009-04-28

Applicant: HOFFMANN LA ROCHE

Inventor： GOBBI LUCA CLAUDIO ,  ROCHE OLIVIER ,  JAESCHKE GEORG ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  STEWARD LUCINDA

IPC: C07D211/46

Abstract: The present invention relates to ether derivatives according to general formula I, and to their pharmaceutically-acceptable salts, which may be used in treating or preventing cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, or psychoses comprising paranoia and delusions.

公开(公告)号：AU2003293798B8

公开(公告)日：2009-02-12

申请号：AU2003293798

申请日：2003-12-08

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/517 ,  A61P25/28 ,  C07D239/00 ,  C07D239/90

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

公开(公告)号：NO20083584A

公开(公告)日：2008-11-14

申请号：NO20083584

申请日：2008-08-19

Applicant: HOFFMANN LA ROCHE

Inventor： GOBBI LUCA CLAUDIO ,  LUEBBERS THOMAS ,  ROCHE OLIVIER ,  JAESCHKE GEORG ,  SARMIENTO ROSA MARIA RODRIGUEZ ,  STEWARD LUCINDA

IPC: C07D211/30 ,  A61K31/4523 ,  A61P25/00 ,  C07D401/12

CPC classification number: C07D401/06 ,  C07D413/06 ,  C07D417/06

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.