公开(公告)号：WO2006000324A2

公开(公告)日：2006-01-05

申请号：PCT/EP2005006398

申请日：2005-06-15

Applicant: HOFFMANN LA ROCHE ,  JOLIDON SYNESE ,  RODRIGUEZ-SARMIENTO ROSA MARIA ,  THOMAS ANDREW WILLIAM ,  WOSTL WOLFGANG ,  WYLER RENE

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

IPC: C07C233/00 ,  A61K31/165 ,  A61K31/277 ,  C07C235/20 ,  C07C255/54

CPC classification number: C07C255/54 ,  C07C235/20

Abstract: The invention relates to compounds of the general formula (I), wherein R 1 , R 2 are independently from each other hydrogen or C l -C 6 -alkyl; R 3 , R 4 are independently from each other hydrogen or C 1 -C 6 -alkyl; R 5 is halogen, CN, (C 1 -C 6 )-alkyl or (C 1 -C 6 )-alkoxy; n, m or o is 0, 1 or 2; as well as to their pharmaceutically acceptable salts. The compounds may be used for the treatment and prevention of Alzheimer's disease or senile dementia.

Abstract translation: 本发明涉及通式（I）的化合物，其中R 1，R 2，2彼此独立地为氢或C 1〜 ç _{6 - 烷基; R 3，R 4，R 4彼此独立地为氢或C 1 -C 6 - 烷基; R 5是卤素，CN，（C 1 -C 6 - ） - 烷基或（C 1 -C 6 - 6 ） - 烷氧基; n，m或o为0,1或2; 以及它们的药学上可接受的盐。 该化合物可用于治疗和预防阿尔茨海默病或老年痴呆。}

公开(公告)号：WO2006077024A3

公开(公告)日：2006-09-08

申请号：PCT/EP2006000125

申请日：2006-01-10

Applicant: HOFFMANN LA ROCHE ,  NETTEKOVEN MATTHIAS HEINRICH ,  PLANCHER JEAN-MARC ,  ROCHE OLIVIER ,  RODRIGUEZ-SARMIENTO ROSA MARIA

Inventor： NETTEKOVEN MATTHIAS HEINRICH ,  PLANCHER JEAN-MARC ,  ROCHE OLIVIER ,  RODRIGUEZ-SARMIENTO ROSA MARIA

IPC: C07D209/40 ,  A61K31/404 ,  A61P3/04

CPC classification number: C07D401/14 ,  C07D401/12

Abstract: The present invention relates to compounds of formula (I) wherein R 1 , R 2 , R 3 , R 4 and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical compositions comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

Abstract translation: 本发明涉及式（I）的化合物，其中R 1，R 2，R 3，R 4， >和m如说明书和权利要求书中所定义，及其药学上可接受的盐以及包含这些化合物的药物组合物及其制备方法。 该化合物可用于治疗和/或预防与H3受体调节相关的疾病。

公开(公告)号：WO2006013049A3

公开(公告)日：2006-06-22

申请号：PCT/EP2005008143

申请日：2005-07-27

Applicant: HOFFMANN LA ROCHE ,  RODRIGUEZ-SARMIENTO ROSA MARIA ,  WOSTL WOLFGANG ,  WYLER RENE

Inventor： RODRIGUEZ-SARMIENTO ROSA MARIA ,  WOSTL WOLFGANG ,  WYLER RENE

IPC: C07D207/27 ,  A61K31/4015 ,  A61K31/4025 ,  A61P25/00 ,  C07D207/277 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

CPC classification number: C07D207/26 ,  C07D207/277 ,  C07D403/04 ,  C07D413/04 ,  C07D417/04

Abstract: The present invention relates to compounds of the general formula (I); wherein R l is halogen; R 2 is -C(O)NH 2 ,-C(NH 2 )=N-OH, -C(O)CH 2 Br, -C(O)N(CH 3 )OCH 3 or-C(O)-lower alkyl, or is a 5-membered heteroaryl group, containing 2 or 3 heteroatoms, selected from the group consisting of N, O or S, optionally substituted by R 3 , wherein R 3 is lower alkyl, -NR'R" or -C(O)R; R is NR'R", lower alkyl, or lower alkoxy; R'/R" are independently hydrogen or lower alkyl; as well as their pharmaceutically acceptable salts for the treatment of diseases, which are mediated by monoamine oxidase B inhibitors, for example Alzheimer's disease and senile dementia.

Abstract translation: 本发明涉及通式（I）的化合物; 其中R 1是卤素; R 2是-C（O）NH 2，-C（NH 2）= N-OH，-C（O）CH 3， 或（C）（O） - 低级烷基，或者是5-（CH 3） 含有2或3个选自N，O或S的杂原子，任选被R 3取代，其中R 3是低级烷基， - NR'R“或-C（O）R; R是NR'R”，低级烷基或低级烷氧基; R'/ R“独立地为氢或低级烷基;以及用于治疗由单胺氧化酶B抑制剂例如阿尔茨海默氏病和老年痴呆介导的疾病的药学上可接受的盐。

公开(公告)号：PL216030B1

公开(公告)日：2014-02-28

申请号：PL37602103

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

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

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

公开(公告)号：SI1542970T1

公开(公告)日：2010-08-31

申请号：SI200331830

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

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

IPC: C07D207/00 ,  A61K31/4015 ,  A61P25/16 ,  A61P25/28 ,  C07D207/26 ,  C07D207/273 ,  C07D207/277 ,  C07D401/00 ,  C07D401/04

公开(公告)号：PL1761480T3

公开(公告)日：2009-07-31

申请号：PL05761873

申请日：2005-06-15

Applicant: HOFFMANN LA ROCHE

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

IPC: C07C235/34 ,  A61K31/165 ,  A61K31/27 ,  A61K31/277 ,  A61P25/28 ,  C07C235/20 ,  C07C255/54 ,  C07C271/12

公开(公告)号：AU2003270213B2

公开(公告)日：2009-02-12

申请号：AU2003270213

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

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

IPC: A61K31/4015 ,  A61P25/16 ,  A61P25/28 ,  C07D207/26 ,  C07D207/273 ,  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：AT412636T

公开(公告)日：2008-11-15

申请号：AT05822659

申请日：2005-12-07

Applicant: HOFFMANN LA ROCHE

Inventor： NETTEKOVEN MATTHIAS ,  ROCHE OLIVIER ,  RODRIGUEZ-SARMIENTO ROSA MARIA

IPC: C07D213/74 ,  A61K31/496 ,  A61P3/04 ,  C07D213/75 ,  C07D213/76

Abstract: The present invention relates to compounds of formula I wherein R1, R2, X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

公开(公告)号：BRPI0517032A

公开(公告)日：2008-09-30

申请号：BRPI0517032

申请日：2005-12-07

Applicant: HOFFMANN LA ROCHE

Inventor： NETTEKOVEN MATHIAS HEINRICH ,  ROCHE OLIVIER ,  RODRIGUEZ-SARMIENTO ROSA MARIA

IPC: C07D213/74 ,  A61K31/496 ,  A61P3/04 ,  C07D213/75 ,  C07D213/76

Abstract: The present invention relates to compounds of formula I wherein R1, R2, X, Y, Z and m are as defined in the description and claims, and pharmaceutically acceptable salts thereof as well as to pharmaceutical composition comprising these compounds and to methods for their preparation. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

公开(公告)号：AU2003273901B2

公开(公告)日：2008-07-10

申请号：AU2003273901

申请日：2003-09-18

Applicant: HOFFMANN LA ROCHE

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

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.