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1. 发明申请

WO2002048124A3 PIPERAZINE DERIVATIVES 审中-公开
公开(公告)号：WO2002048124A3
公开(公告)日：2002-06-20
申请号：PCT/EP2001/014343
申请日：2001-12-06
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , GEORGE, Ashley, Roger , MANSELL, Howard, Langham , MATTEI, Patrizio , MIZRAHI, Jacques , NETTEKOVEN, Matthias, Heinrich , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , ROEVER, Stephan , SPECKLIN, Jean-Luc , STALDER, Henri , WILKINSON, Kerry
IPC分类号： C07D295/20
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R 1 to 4 4 , A 1 , A 2 m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

2. 发明授权

EP1343775B1 PIPERAZINE DERIVATIVES 有权
标题翻译：哌嗪衍生物
公开(公告)号：EP1343775B1
公开(公告)日：2008-06-04
申请号：EP01990522.3
申请日：2001-12-06
申请人： F. Hoffmann-La Roche AG , VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , GEORGE, Ashley, Roger , MANSELL, Howard, Langham , MATTEI, Patrizio , MIZRAHI, Jacques , NETTEKOVEN, Matthias, Heinrich , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , ROEVER, Stephan , SPECKLIN, Jean-Luc , STALDER, Henri , HARRISON, Kerry
IPC分类号： C07D295/20 , A61K31/495 , A61P3/04 , C07D261/08 , C07D213/30
CPC分类号： C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D413/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R?1 to 44, A1, A2¿ m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.
摘要翻译：本发明涉及式（I）的化学化合物及其药学上可用的盐，溶剂合物和酯，其中R 1至44，A 1，A 2和m具有权利要求1中给出的含义。可以使用它们其为用于治疗或预防中枢神经系统疾病，心血管疾病，胃肠疾病，糖尿病，肥胖症和睡眠呼吸暂停的药物制剂形式。

3. 发明公开

EP1343775A2 PIPERAZINE DERIVATIVES 有权
标题翻译：哌嗪衍生物
公开(公告)号：EP1343775A2
公开(公告)日：2003-09-17
申请号：EP01990522.3
申请日：2001-12-06
申请人： F. HOFFMANN-LA ROCHE AG , VERNALIS RESEARCH LIMITED
发明人： ADAMS, David, Reginald , BENTLEY, Jonathan, Mark , DAVIDSON, James, Edward, Paul , DAWSON, Claire, Elizabeth , GEORGE, Ashley, Roger , MANSELL, Howard, Langham , MATTEI, Patrizio , MIZRAHI, Jacques , NETTEKOVEN, Matthias, Heinrich , PRATT, Robert, Mark , ROFFEY, Jonathan, Richard, Anthony , ROEVER, Stephan , SPECKLIN, Jean-Luc , STALDER, Henri , WILKINSON, Kerry
IPC分类号： C07D295/20 , A61K31/495 , A61P3/04 , C07D261/08 , C07D213/30
CPC分类号： C07D207/325 , C07D213/30 , C07D213/64 , C07D213/643 , C07D261/08 , C07D277/24 , C07D285/14 , C07D295/205 , C07D295/21 , C07D307/12 , C07D307/42 , C07D333/16 , C07D413/04
摘要： The present invention refers to chemical compounds of formula (I) as well as pharmaceutically usable salts, solvates and esters thereof, wherein R?1 to 44, A1, A2¿ m and n have the significance given in claim 1. They can be used in the form of pharmaceutically preparations for the treatment or prevention of disorders of the central nervous system, cardiovascular disorders, gastrointestinal disorders, diabetes, obesity and sleep apnoea.

4. 发明申请

WO2006045478A1 NEW INDOLE OR BENZIMIDAZOLE DERIVATIVES 审中-公开
标题翻译：新的吲哚或苯并咪唑衍生物
公开(公告)号：WO2006045478A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/011176
申请日：2005-10-18
申请人： F. HOFFMANN-LA ROCHE AG , BLEICHER, Konrad , NETTEKOVEN, Matthias, Heinrich , PFLIEGER, Philippe , ROEVER, Stephan
发明人： BLEICHER, Konrad , NETTEKOVEN, Matthias, Heinrich , PFLIEGER, Philippe , ROEVER, Stephan
IPC分类号： C07D235/12 , C07D401/06 , C07D209/12 , A61K31/4184 , A61P3/04
CPC分类号： C07D235/12 , C07D209/12 , C07D401/06
摘要： The present invention relates to compounds of the formula (I), wherein R 1 to R 7 , X and Y 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 CB1 receptors.
摘要翻译：本发明涉及式（I）的化合物，其中R 1至R 7，X和Y如说明书和权利要求书中所定义，以及药学上可接受的盐它们。该化合物可用于治疗和/或预防与调节CB1受体相关的疾病。

5. 发明申请

WO2005014563A1 PIPERAZINE WITH OR-SUBSTITUTED PHENYL GROUP AND THEIR USE AS GLYT1 INHIBITORS 审中-公开
标题翻译：具有或取代的苯基的哌嗪及其作为GLYT1抑制剂的用途
公开(公告)号：WO2005014563A1
公开(公告)日：2005-02-17
申请号：PCT/EP2004/008633
申请日：2004-08-02
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NETTEKOVEN, Matthias, Heinrich , NORCROSS, Roger, David , PINARD, Emmanuel , STALDER, Henri
IPC分类号： C07D295/192
CPC分类号： C07D239/42 , C07D213/85 , C07D241/20 , C07D251/42 , C07D257/04 , C07D263/32 , C07D271/06 , C07D295/192 , C07D309/12
摘要： The invention relates to compounds of formula (I) wherein the substituents are described in claim 1. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
摘要翻译：本发明涉及式（I）化合物，其中取代基描述于权利要求1中。该化合物可用于治疗基于甘氨酸摄取抑制剂的疾病，例如精神病，疼痛，记忆和学习中的神经变性功能障碍，精神分裂症，痴呆症和认知过程受损的其他疾病，如注意力缺陷障碍或阿尔茨海默病。

6. 发明申请

WO2003030904A1 8-AMINO-[1,2,4]TRIAZOLO[1,5-A]PYRIDINE-6-CARBOXYLIC ACID AMIDE 审中-公开
标题翻译： 8-氨基 - [1,2,4]三唑[1,5-A]吡啶-6-羧酸酰胺
公开(公告)号：WO2003030904A1
公开(公告)日：2003-04-17
申请号：PCT/EP2002/011152
申请日：2002-10-04
申请人： F. HOFFMANN-LA ROCHE AG
发明人： NETTEKOVEN, Matthias, Heinrich , SCHMITT, Sébastien
IPC分类号： A61K31/435
CPC分类号： C07D471/04 , A61K31/437
摘要： The invention relates to compounds of formula (I), wherein R 1 is -NR'R", wherein R' and R" are independently from each other lower alkyl, -(CH 2 ) n -C(O)NR a R b , -(CH 2 ) n -heteroaryl, -(CH 2 ) n -aryl, -(CH 2 ) n -CN, -(CH 2 ) n -O-lower alkyl or -(CH 2 ) n -cycloalkyl, or R'and R" form together with the N-atom a five or six-membered none aromatic ring, which may contain one additional O or S heteroatom, and whose rings may be unsubstituted or substituted by one or two substituents, selected from the group consisting of lower alkyl, -C(O)NR a R b or -(CH 2 ) n -O-lower alkyl and R a R b are independently from each other hydrogen or lower alkyl; R 2 is aryl or heteroaryl, unsubstituted or substituted ba lower alkyl or halogen; n is 0, 1, 2 or 3; and to their pharmaceutically acceptable salts. The compounds may be used in the treatment of diseases, associated with the adenosime A2 receptor.
摘要翻译：本发明涉及式（I）化合物，其中R 1为-NR'R“，其中R'和R”彼此独立地为低级烷基， - （CH 2）n C（O）NR a R （CH 2）n - 杂芳基， - （CH 2）n - 芳基， - （CH 2）n -CN， - （CH 2）n O-低级烷基或 - （CH 2） “与N-原子一起形成五元或六元非芳环，其可以含有一个另外的O或S杂原子，并且其环可以是未取代的或被一个或两个选自下列的取代基所取代：低级烷基，-C（O）NR a R b或 - （CH 2）n O-低级烷基和R a R b彼此独立地为氢或低级烷基; R 2为芳基或杂芳基，未取代或取代的低级烷基或卤素; n为0,1,2或3;及其药学上可接受的盐。该化合物可用于治疗与腺苷A2受体相关的疾病。

7. 发明申请

WO2007131907A3 1H-INDOL-5-YL-PIPERAZIN-1-YL-METHANONE DERIVATIVES 审中-公开
公开(公告)号：WO2007131907A3
公开(公告)日：2007-11-22
申请号：PCT/EP2007/054415
申请日：2007-05-08
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias, Heinrich , ROCHE, Olivier
发明人： NETTEKOVEN, Matthias, Heinrich , ROCHE, Olivier
IPC分类号： C07D209/40 , A61P3/04 , A61K31/404
摘要： The present invention relates to compounds of formula (1) wherein R 1 to R 4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.

8. 发明申请

WO2006058649A1 3-SUBSTITUTED PYRIDINE DERIVATIVES AS H3 ANTAGONISTS 审中-公开
标题翻译： 3-取代的吡啶衍生物作为H3拮抗剂
公开(公告)号：WO2006058649A1
公开(公告)日：2006-06-08
申请号：PCT/EP2005/012556
申请日：2005-11-24
申请人： F. HOFFMANN-LA ROCHE AG , NETTEKOVEN, Matthias, Heinrich , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa, Maria
发明人： NETTEKOVEN, Matthias, Heinrich , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa, Maria
IPC分类号： C07D213/82 , C07D213/83 , A61K31/496 , A61P1/00
CPC分类号： C07D213/74 , C07D213/82 , C07D213/83
摘要： The present invention relates to compounds of formula (I), wherein R 1 , R 2 and A 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.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2和A如说明书和权利要求书中所定义，及其药学上可接受的盐关于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受体的调节相关的疾病。

9. 发明申请

WO2006045416A1 QUINOLINE DERIVATIVES 审中-公开
标题翻译：喹啉衍生物
公开(公告)号：WO2006045416A1
公开(公告)日：2006-05-04
申请号：PCT/EP2005/010814
申请日：2005-10-07
申请人： F. HOFFMANN-LA ROCHE AG , GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , RAAB, Susanne , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
发明人： GATTI McARTHUR, Silvia , HERTEL, Cornelia , NETTEKOVEN, Matthias, Heinrich , RAAB, Susanne , RICHTER, Hans , ROCHE, Olivier , RODRIGUEZ-SARMIENTO, Rosa Maria , SCHULER, Franz
IPC分类号： C07D401/06 , C07D215/20 , A61K31/47
CPC分类号： C07D401/14 , C07D215/48 , C07D401/12 , C07D405/14 , C07D417/12
摘要： The present invention relates to compounds of formula (I) wherein R', R 2 and A 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.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2和A如说明书和权利要求中所定义，及其药学上可接受的盐以及包含这些化合物和给他们准备的方法。该化合物可用于治疗和/或预防与H3受体调节相关的疾病。

10. 发明申请

WO2003066055A1 QUINOLINE DERIVATIVES AS NPY ANTAGONISTS 审中-公开
标题翻译：喹啉衍生物作为NPY拮抗剂
公开(公告)号：WO2003066055A1
公开(公告)日：2003-08-14
申请号：PCT/EP2003/000777
申请日：2003-01-27
申请人： F. HOFFMANN-LA ROCHE AG
发明人： MATTEI, Patrizio , MUELLER, Werner , NEIDHART, Werner , NETTEKOVEN, Matthias, Heinrich , PFLIEGER, Philippe
IPC分类号： A61K31/4709
CPC分类号： C07D401/04 , C07D215/42 , C07D215/46 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12
摘要： Compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R 1 , R 2 , R 3 , R 4 and A have the significance given in claim 1, can be used in the form of pharmaceutical preparations for the treatment or prevention of arthritis, cardiovascular diseases, diabetes, renal failure, eating disorders and obesity.
摘要翻译：式（I）化合物及其药学上可接受的盐和酯，其中R 1，R 2，R 3，R 4和A具有权利要求1中给出的含义，可以以用于治疗或预防关节炎的药物制剂的形式使用，心血管疾病，糖尿病，肾衰竭，饮食失调和肥胖。

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