公开(公告)号：AU2001283955B2

公开(公告)日：2006-05-18

申请号：AU2001283955

申请日：2001-07-24

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LIMITED

Inventor： MATTEI PATRIZIO ,  MULLER MARC ,  BENTLEY JONATHAN MARK ,  ROEVER STEPHAN ,  TAYLOR SVEN ,  HEBEISEN PAUL ,  RICHTER HANS

IPC: C07D487/04 ,  A61K31/337 ,  A61K31/4985 ,  A61K45/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32

Abstract: The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I): as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.

公开(公告)号：DE60203481T2

公开(公告)日：2006-02-16

申请号：DE60203481

申请日：2002-01-28

Applicant: HOFFMANN LA ROCHE

Inventor： KOLCZEWSKI SABINE ,  ROEVER STEPHAN ,  SCHNIDER PATRICK

IPC: A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D211/14 ,  C07D211/16 ,  C07D211/18 ,  C07D211/26 ,  C07D211/58 ,  C07D295/12 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12

Abstract: The invention relates to compounds of the formulawherein R is optionally substituted phenyl, morpholinyl, piperazinyl, pyrrolidinyl, piperidinyl or is thiomorpholinyl, 1-oxo-thiomorpholinyl or 1,1-dioxothiomorpholinyl. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable in the control or treatment of diseases, related to this receptor.

公开(公告)号：AU2004299198A1

公开(公告)日：2005-06-30

申请号：AU2004299198

申请日：2004-11-29

Applicant: HOFFMANN LA ROCHE

Inventor： ROEVER STEPHAN ,  NETTEKOVEN MATTHIAS HEINRICH

IPC: C07D417/06 ,  C07D277/56 ,  C07D417/12

Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 and R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof, for use as therapeutically active substances. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, including obesity.

公开(公告)号：AT292128T

公开(公告)日：2005-04-15

申请号：AT02710043

申请日：2002-01-28

Applicant: HOFFMANN LA ROCHE

Inventor： KOLCZEWSKI SABINE ,  ROEVER STEPHAN ,  SCHNIDER PATRICK

IPC: A61K31/451 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61P1/04 ,  A61P1/08 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P11/08 ,  A61P17/02 ,  A61P19/02 ,  A61P25/00 ,  A61P25/02 ,  A61P25/06 ,  A61P25/16 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D211/14 ,  C07D211/16 ,  C07D211/18 ,  C07D211/26 ,  C07D211/58 ,  C07D295/12 ,  C07D295/135 ,  C07D401/04 ,  C07D401/12 ,  C07D413/12

Abstract: The invention relates to compounds of the formulawherein R is optionally substituted phenyl, morpholinyl, piperazinyl, pyrrolidinyl, piperidinyl or is thiomorpholinyl, 1-oxo-thiomorpholinyl or 1,1-dioxothiomorpholinyl. These compounds have a good affinity to the NK-1 receptor and they are therefore suitable in the control or treatment of diseases, related to this receptor.

公开(公告)号：BR0307291A

公开(公告)日：2004-12-07

申请号：BR0307291

申请日：2003-01-17

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： ADAMS DAVID REGINALD ,  BENTLEY JONATHAN MARK ,  BLENCH TOBY JONATHAN ,  HEBEISEN PAUL ,  MONCK NATHANIEL JULIUS THOMAS ,  RICHTER HANS ,  ROEVER STEPHAN ,  ROFFEY JONATHAN RICHARD ANTHON ,  TAYLOR SVEN

IPC: C07D305/12 ,  A61K31/365 ,  A61K31/495 ,  A61K31/498 ,  A61K31/4985 ,  A61K45/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/12 ,  A61P9/00 ,  A61P15/10 ,  A61P17/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/16 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P43/00 ,  C07D20060101 ,  C07D471/04 ,  C07D471/14 ,  C07D487/14

Abstract: The present invention relates to compounds of formula (I) as well as pharmaceutically acceptable salts, solvates and esters thereof. These compounds can be used to prepare pharmaceutical compositions for the treatment or prevention of disorders of the central nervous system, damage to the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

公开(公告)号：ZA200306613B

公开(公告)日：2004-11-25

申请号：ZA200306613

申请日：2003-08-25

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： HEBEISEN PAUL ,  MULLER MARC ,  ROEVER STEPHAN ,  MATTEI PATRIZIO ,  RICHTER HANS ,  TAYLOR SVEN

IPC: A61K31/337 ,  A61K31/4985 ,  A61P3/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/02 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  A61P29/00 ,  A61P43/00 ,  C07D487/04 ,  C07D ,  A61K ,  A61P

Abstract: The present invention provides piperazine derivatives in accordance with formula (I)as well as salts, hydrates and esters thereof. The substituent designations are as provided in the specification. The compounds of the present invention can be used in the treatment of type II diabetes or obesity.

公开(公告)号：ZA200305007B

公开(公告)日：2004-09-27

申请号：ZA200305007

申请日：2003-06-26

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： BENTLEY JONATHAN MARK ,  HEBEISEN PAUL ,  LIGHTOWLER SEAN ,  MIZRAHI JACQUES ,  PLANCHER JEAN-MARC ,  ROEVER STEPHAN ,  VICKERS STEVEN PAUL ,  BICKERDIKE MICHAEL JOHN ,  KENNETT GUY ANTHONY ,  MATTEI PATRIZIO ,  MORLEY TIMOTHY JAMES ,  RICHTER HANS ,  TAYLOR SVEN

IPC: A61K20060101 ,  A61P20060101 ,  C07D20060101 ,  C07D ,  A61K ,  A61P

公开(公告)号：CA2511859A1

公开(公告)日：2004-07-22

申请号：CA2511859

申请日：2003-12-22

Applicant: HOFFMANN LA ROCHE

Inventor： NEIDHART WERNER ,  ROEVER STEPHAN ,  PFLIEGER PHILIPPE ,  MUELLER WERNER ,  NARQUIZIAN ROBERT ,  MARTY HANS PETER ,  MAYWEG ALEXANDER

IPC: A61K31/40 ,  A61P3/04 ,  C07D207/34 ,  C07D233/90 ,  C07D401/04 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D521/00

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3 , R4, R5, R6, m and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment . and/or prophylaxis of diseases which are associated with the modulation of CB 1 receptors.

公开(公告)号：ZA200300525B

公开(公告)日：2004-04-20

申请号：ZA200300525

申请日：2003-01-20

Applicant: HOFFMANN LA ROCHE ,  VERNALIS RES LTD

Inventor： BENTLY JONATHAN MARK ,  MULLER MARC ,  ROEVER STEPHAN ,  TAYLOR SVEN ,  HEBEISEN PAUL ,  RICHTER HANS ,  MATTEI PATRIZIO

IPC: A61K31/337 ,  A61K31/4985 ,  A61K45/00 ,  A61P1/00 ,  A61P3/04 ,  A61P3/10 ,  A61P7/02 ,  A61P9/00 ,  A61P11/00 ,  A61P13/00 ,  A61P15/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/18 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  A61P25/32 ,  C07D487/04 ,  C07D ,  A61K ,  A61P

Abstract: The present invention is directed to 1,2,3,4,10,10a-hexahydropyrazino [1,2-a]indole derivatives of formula (I): as well as pharmaceutically acceptable salts, hydrates and esters thereof, wherein the substituents have the meanings provided in the specification. Compounds of the present invention may be used in the treatment or prevention of obesity or Type II diabetes.

公开(公告)号：ZA200209488B

公开(公告)日：2004-02-23

申请号：ZA200209488

申请日：2002-11-21

Applicant: HOFFMANN LA ROCHE

Inventor： GALLEY GUIDO ,  GOERGLER ANNICK ,  KOLCZEWSKI SABINE ,  TORSTEN GODEL THIERRY HOFFMANN ,  ROEVER STEPHAN

IPC: A61K31/437 ,  A61K31/445 ,  A61P1/04 ,  A61P9/00 ,  A61P11/00 ,  A61P11/06 ,  A61P25/06 ,  A61P25/28 ,  A61P25/36 ,  A61P27/02 ,  A61P27/16 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D471/10 ,  C07D ,  A61K

Abstract: The invention relates to compounds of the formulaas described herein and pharmaceutically acceptable acid addition salts thereof. The described compounds have a good affinity to the NK1 receptor.