公开(公告)号：ZA9706222B

公开(公告)日：1998-01-19

申请号：ZA9706222

申请日：1997-07-14

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 ,  C07D ,  A61K

CPC classification number: A61K31/427 ,  A61K31/426

公开(公告)号：CA2210613A1

公开(公告)日：1998-01-19

申请号：CA2210613

申请日：1997-07-16

Applicant: HOFFMANN LA ROCHE

Inventor： R VER STEPHAN ,  CESURA ANDREA

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 invention is concerned with the use of sulphonamide derivatives of the general formula (see fig. I) wherein R Signifies lower-alkyl, phenyl, benzyl, naphthyl, pyridyl or thienyl, optionally substituted by one or more lower-alkyl, lower-alkoxy, lower-alkyl carbonyl-amino, halogen, cycloalkyl, nitro, amino, methylenedioxy, phenoxy or benzyloxy substituents, and the aromatic rings, can, in turn, be substituted by nitro, halogen or amino, R1-R4 signify hydrogen, halogen, hydroxy, lower-alkyl, nitro, cyano, amino, lower-alkoxy, benzyloxy, trifluoromethyl or phenyl, optionally substituted by one or more lower-alkyl, trifluoromethyl, nitro, amino or hydroxy substituents, and wherein R1 and R2 or R2 and R3 together can form a benzene ring which optionally can be substituted by halogen, trifluromethyl, nitro, lower-alkyl or lower alkoxy, and of their pharmaceutically acceptable salts as kynurenin-3-hydroxylase inhibitors in the control or prevention of neuro-degenerative disorders, neurological disorders resulting from an activation of the immune system, or psychiatric illnesses and, respectively, for the production of corresponding medicaments.

公开(公告)号：PT1501804E

公开(公告)日：2009-10-29

申请号：PT03725018

申请日：2003-04-14

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D217/04 ,  C07D217/24 ,  A61K31/472 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D405/06

公开(公告)号：CA2464042C

公开(公告)日：2009-09-29

申请号：CA2464042

申请日：2004-04-13

Applicant: HOFFMANN LA ROCHE

Inventor： CESURA ANDREA ,  PINARD EMMANUEL

IPC: C07C49/683 ,  C12Q1/02 ,  A61K31/12 ,  A61K31/122 ,  A61K31/277 ,  A61K31/35 ,  A61K31/353 ,  A61P25/28 ,  A61P43/00 ,  C07C49/665 ,  C07C255/47 ,  C07D311/22 ,  C07D311/56 ,  G01N33/567 ,  G01N33/58

Abstract: The present invention provides the use of compounds of general formula I (see formula I) and compounds of general formula II (see formula II) as modulators and affinity labels of the MPTP complex. Furthermore, the present invention provides methods for modulating the activity of the MPTP complex, methods for determining the presence of a component of the MPTP complex, and methods for identifying an active agent that modulates the activity of the MPTP complex, specifically methods for identifying an active agent that modulates the activity of the MPTP complex by interacting with the VDAC1 component. Moreover, novel compounds of general formula I are provided by the present invention.

公开(公告)号：CA2255171C

公开(公告)日：2009-09-29

申请号：CA2255171

申请日：1998-12-03

Applicant: HOFFMANN LA ROCHE

Inventor： WICHMANN JURGEN ,  ADAM GEO ,  ROVER STEPHAN ,  JENCK FRANCOIS ,  CESURA ANDREA ,  GALLEY GUIDO

IPC: C07D235/02 ,  C07D471/10 ,  A61K31/00 ,  A61K31/41 ,  A61K31/435 ,  A61K31/438 ,  A61K31/53 ,  A61K31/535 ,  A61P3/00 ,  A61P3/04 ,  A61P9/00 ,  A61P25/00 ,  A61P25/02 ,  A61P25/04 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P43/00 ,  C07D207/04 ,  C07D233/30

Abstract: The present invention relates to compounds of the general formula (see formula I) wherein R1 is hydrogen, lower alkyl, halogen, lower alkoxy, trifluoromethyl, lower alkyl-phenyl or (C5-7)-cycloalkyl; R2 is hydrogen, lower alkyl, phenyl or lower alkyl-phenyl; R3 is hydrogen, lower alkyl, benzyl, lower alkyl-phenyl, lower alkyl- diphenyl, triazinyl, cyanomethyl, lower alkyl-piperidinyl, lower alkyl-naphthyl, (C5-7)-cycloalkyl, lower alkyl-(C5-7)-cycloalkyl, lower alkyl-pyridinyl, lower alkyl-morpholinyl, lower alkyl- dioxolanyl, lower alkyl-oxazolyl or lower alkyl-2-oxo-oxazolidinyl and wherein the ring systems may be substituted by additional lower alkyl, lower alkoxy, trifluoromethyl or phenyl, or -(CH2)n C(O)O-lower alkyl, -(CH2)n C(O)NH2, -(CH2)n C(O)N(lower alkyl)2, -(CH2)n OH or -(CH2)n C(O)NHCH2C6H5; R4 is hydrogen, lower alkyl or nitrilo; A is a ring system, consisting of (a) (C5-15)-cycloalkyl, which may be in addition to R4 optionally substitute d by lower alkyl, trifluoromethyl, phenyl, (C5-7)-cycloalkyl, spiro-undecan- alkyl or by 2-norbornyl, or is one of the following groups (see formula b) (see formula c) (see formula d) dodecahydro-acenaphthylen-1yl (e), bicyclo[6.2.0]dec-9-yl (f) and bicyclononan-9-yl (g); and wherein R5 and R6 are hydrogen, lower alkyl or taken together and with the carbon atoms to which they are attached form a phenyl ring; R7 is hydrogen or lower alkyl; the dotted line represents an optional bond and n is 1 to 4; and to pharmaceutically acceptable acid addition salts thereof. Compounds of the present invention are agonists and/or antagonists of the Orphanin FQ (OFQ) receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, trauma, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions, acu te and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na+ excretion, arterial blood pressure disorders a nd metabolic disorders such as obesity.

公开(公告)号：CA2310458C

公开(公告)日：2008-11-04

申请号：CA2310458

申请日：1998-12-03

Applicant: HOFFMANN LA ROCHE

Inventor： WICHMANN JURGEN ,  CESURA ANDREA ,  GALLEY GUIDO ,  ROVER STEPHAN ,  JENCK FRANCOIS ,  ADAM GEO

IPC: C07D491/107 ,  A61K31/435 ,  A61K31/438 ,  A61K31/439 ,  A61P25/00 ,  A61P25/04 ,  A61P25/08 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D221/20 ,  C07D451/04 ,  C07D471/10 ,  C07D491/10 ,  C07D491/20 ,  C07D498/10 ,  C07D498/20

Abstract: The present invention relates to compounds of formula (I-1) wherein X is -O- or -CH2-; Y is -C(O)-, -(CH2)n- or -N(CH3)-; n is 1 or 2 or X and Y taken together are -CH-CH-; Z is -NH-, -CH2-, -O- or -CH-; A1 is a group (a) or (b); B is -(CH2)m-; m is 0, 1 or 2; R1 and R2 are each independently hydrogen or lower alkyl; R3 is hydrogen or halogen; R4 is hydrogen or hydroxy and the dotted line is an optional -CH2-CH2-group and to pharmaceutically acceptable acid addition salts thereof. The compounds of the present invention are antagonists of the OFQ receptor. Consequently they will be useful in the treatment of memory and attention deficits, psychiatric, neurological and physiological disorders, especially, but not limited to, amelioration of symptoms of anxiety and stress disorders, depression, memory loss due to Alzheimer's disease or other dementias, epilepsy and convulsions , acute and/or chronic pain conditions, symptoms of addictive drug withdrawal, control of water balance, Na+ excretion and arterial blood pressure disorders and metabolic disorders such as obesity.

公开(公告)号：MY133527A

公开(公告)日：2007-11-30

申请号：MYPI20031578

申请日：2003-04-25

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D217/04 ,  C07D217/22 ,  A61K31/44 ,  A61K31/47 ,  A61K31/472 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D217/02 ,  C07D217/24 ,  C07D401/00 ,  C07D405/06

Abstract: THIS INVENTION RELATES TO ISOQUINOLINO DERIVATIVES OF THE GENERAL FORMULA WHEREIN Y IS >C=O OR -CH2-, Z IS >C=O OR -CH2-, AND R1, R2 AND M ARE AS DEFINED IN THE SPECIFICATION, AS WELL AS THEIR PHARMACEUTICALLY ACCEPTABLE SALTS. THE INVENTION FURTHER RELATES TO MEDICAMENTS CONTAINING THESE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AS WELL AS THEIR USE FOR PREPARATION OF MEDICAMENTS FOR THE TREATMENT OR PREVENTION OF DISEASES IN WHICH MAO-B INHIBITORS MIGHT BE BENEFICIAL.

公开(公告)号：NZ535885A

公开(公告)日：2007-05-31

申请号：NZ53588503

申请日：2003-04-14

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D217/04 ,  A61K31/472 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00 ,  C07D217/24 ,  C07D405/06

Abstract: Isoquinoline derivatives of formula (I) wherein: Y and Z are independently >C=O or -CH2-; R1 is H or a group of formula -CR3R4R5 wherein R3, R4 and R5 are as described in the specification; and each R2 is independently selected from halogen, halogen-alkyl, cyano, alkoxy or halogen-alkoxy. Compounds of the type disclosed are monoamine oxidase B inhibitors (MAOB) useful in the treatment and prevention of Alzheimer's disease and senile dementia.

公开(公告)号：DK1037892T3

公开(公告)日：2005-02-07

申请号：DK98965753

申请日：1998-12-03

Applicant: HOFFMANN LA ROCHE

Inventor： ADAM GEO ,  GALLEY GUIDO ,  JENCK FRANCOIS ,  WICHMANN JUERGEN ,  CESURA ANDREA ,  ROEVER STEPHAN

IPC: C07D491/107

公开(公告)号：AR038342A1

公开(公告)日：2005-01-12

申请号：ARP030100319

申请日：2003-02-03

Applicant: HOFFMANN LA ROCHE

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

IPC: 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 ,  C07D213/82

Abstract: La presente se refiere a derivados piridin-amido de la fórmula general (1). También se refiere a medicamentos que contienen estos compuestos, a un procedimiento para la preparación de los mismos, así como también al empleo de los mismos para preparar medicamentos que se utilizan en el tratamiento o prevención de enfermedades en las cuales los inhibidores de la MAO-B pueden ser beneficios y mal de Alzheimer ó demencia senil. Reivindicación 1: Compuestos de la fórmula general (1), donde: uno de X ó Y es -N= y el otro es -CR7=; R1 es hidrógeno o alquilo C1-6; R2 es hidrógeno o alquilo C1-6; R3 es hidrógeno o alquilo C1-6, R4 es halógeno-alquilo C1-6 ó arilo no sustituido o arilo sustituido por uno ó más sustituyentes seleccionados entre el grupo que comprende alquilo C1-6, halógeno, halógeno-alquilo C1-6, alcoxi C1-6 y ciano; R5 es hidrógeno o alquilo C1-6; R6 es hidrógeno o alquilo C1-6; R7 es hidrógeno o alquilo C1-6; así como también las sales farmacéuticamente aceptables de los mimos.