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1. 发明申请

WO2004105755A1 BENZOTHIAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES RELATED TO THE ADENOSINE A2A RECEPTOR 审中-公开
标题翻译：苯并噻唑衍生物及其在治疗腺苷A2A受体相关疾病中的应用
公开(公告)号：WO2004105755A1
公开(公告)日：2004-12-09
申请号：PCT/EP2004/005474
申请日：2004-05-21
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： A61K31/428
CPC分类号： C07D277/82
摘要： Compounds of the general formula (I) and pharmaceutically acceptable acid addition salts thereof for the treatment of diseases, related to the A2A receptor.
摘要翻译：通式（I）的化合物及其药学上可接受的酸加成盐用于治疗与A2A受体有关的疾病。

2. 发明申请

WO2004103367A1 BENZOTHIAZOLE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF DISEASES RELATES TO THE ADENOSINE A2A RECEPTOR 审中-公开
标题翻译：苯并噻唑衍生物及其用于治疗与腺苷A2A受体相关的疾病
公开(公告)号：WO2004103367A1
公开(公告)日：2004-12-02
申请号：PCT/EP2004/005179
申请日：2004-05-14
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： A61K31/428
CPC分类号： C07D277/82 , C07D417/04 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of the general formula (I): and to pharmaceutically acceptable acid additions salts thereof. The compounds may be used for the treatment of diseases relates to the A2A receptor.
摘要翻译：本发明涉及通式（I）的化合物及其药学上可接受的酸加成盐。该化合物可用于治疗涉及A2A受体的疾病。

3. 发明申请

WO2004101558A1 2-IMIDAZO-BENZOTHIAZOLES AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译： 2-IMIDAZO-BENZOTHIAZOLES作为腺苷受体配体
公开(公告)号：WO2004101558A1
公开(公告)日：2004-11-25
申请号：PCT/EP2004/004843
申请日：2004-05-06
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, ALexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
发明人： FLOHR, ALexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： C07D417/04
CPC分类号： C07D417/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D491/04
摘要： The invention relates to 2-imidazo-benzothiazoles of general formula (I), wherein R 1 is phenyl or a N and/or O containing heterocycle; R 2 is an imidazol or an annulated imidazol, selected from the group consisting of formulae a), b), c), d) or e); R 3 is hydrogen, phenyl, 2,3-dihydro-benzo [1,4] dioxin-6-yl, benzo [b] thiophen-3-yI, 3-methyl-benzo[b]thiophen-2-yl, thiophen-2-yl,thiophen-3-yl or thiophen-2-yl-methyl, R 4 is hydrogen,-(CH 2 ) n O-lower alkyl or lower alkyl; R 5 is hydrogen, lower alkyl, halogen, morpholinyl, -NR'R", piperidinyl, optionally substituted by hydroxy, or is pyrrolidin- l-yl; R 6 is hydrogen, benzyl or -(CH 2 ) n O-lower alkyl, R 7 is hydrogen, -C(O)O-lower alkyl, -C(O)-C 6 H 4 -halogen, -C(O)-C 6 H 4 -lower alkyl, -C(O)-lower alkyl, -C(O)-cycloalkyl, -C(O)-NR'R", -C(O)-(CH 2 ) n O-lower alkyl, -S(O) 2 -lower alkyl, -(CH 2 ) n O-lower alkyl, -C(O) -pyridin-4-yl, which ring may be substituted by lower alkyl, halogen-lower alkyl or by pyrrol-l-yl-methyl, or is -(CH 2 ) n -C(O)-NR'R"; R’/R’’ are independently from each other hydrogen, lower alkyl or -(CH 2 ) n -tetrahydropyran-4-yl, X is -CH 2 -,-NR’’’-or-O-; R’’’ is hydrogen, -C(O)-lower alkyl, -C(O)O-lower alkyl, -C(O)-C 6 H 4 CH 3 , or benzyl; n is 1or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds are adenosine receptor ligands and therefore suitable for tha treatment of diseases related to this receptor.
摘要翻译：本发明涉及通式（I）的2-咪唑并苯并噻唑，其中R 1是苯基或含N和/或O的杂环; R 2是选自式a），b），c），d）或e）的咪唑或环状咪唑。 R 3是氢，苯基，2,3-二氢 - 苯并[1,4]二氧杂环己烯-6-基，苯并[b]噻吩-3-基，3-甲基 - 苯并[b]噻吩-2-基，噻吩-2-基，噻吩-3-基或噻吩-2-基 - 甲基，R 4是氢， - （CH 2）n O-低级烷基或低级烷基; R 5是氢，低级烷基，卤素，吗啉基，-NR'R“，哌啶基，任选被羟基取代，或是吡咯烷-1-基; R 6是氢，苄基或 - （CH 2）低级烷基，R 7是氢，-C（O）O-低级烷基，-C（O）-C 6 H 4 - 卤素，-C（O）-C 6 H 4 - 低级烷基，-C（O） -C（O） - 环烷基，-C（O）-NR'R“， - C（O） - （CH 2）n O-低级烷基，-S（O）2 - 低级烷基， - （CH 2）烷基，-C（O） - 吡啶-4-基，该环可以被低级烷基，卤素 - 低级烷基或吡咯-1-基甲基取代，或是 - （CH 2）n C（O）-NR' R“; R'/ R”彼此独立地为氢，低级烷基或 - （CH 2）n - 四氢吡喃-4-基，X为-CH 2 - ， - NR“' - 或-O-; R' “是氢，-C（O） - 低级烷基，-C（O）O-低级烷基，-C（O）-C 6 H 4 CH 3或苄基; n是1或2;以及其药学上可接受的酸加成盐。化合物是腺苷受体配体，因此适用于治疗与该受体有关的疾病。

4. 发明申请

WO2005000842A1 BENZOTHIAZOLE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：苯并噻唑衍生物作为腺苷受体配体
公开(公告)号：WO2005000842A1
公开(公告)日：2005-01-06
申请号：PCT/EP2004/005178
申请日：2004-05-14
申请人： F. HOFFMAN-LA ROCHE AG , FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
发明人： FLOHR, Alexander , JAKOB-ROETNE, Roland , NORCROSS, Roger, David , RIEMER, Claus
IPC分类号： C07D417/14
CPC分类号： C07D417/04 , C07D417/14 , C07D491/10
摘要： The invention relates to compounds of the general formula (I) wherein R 1 is 1,4-dioxepanyl or tetrahydropyran-4-yl; R 2 is -N(R)-(CH 2 ) n ,-5-or 6 membered non aromatic heterocycle, optionally substituted by one or more substituents, selected from the group consisting of lower alkyl or -NR 2 , or is - (CH 2 ) n -5-or 6 membered non aromatic heterocycle, optionally substituted by -(CH 2 ) n -OH, lower alkyl, lower alkoxy, or is -CH 2 ) n -5-or 6 membered aromatic heterocycle, optionally substituted by lower alkyl, lower alkoxy, halogen, halogen-lower alkyl, -CH 2 N(R)(CH 2 ) 2 0CH 3 , -N(R)(CH 2 ) 2 0CH 3 , -CH 2 -morpholinyl or -CH 2 -pyrrolidinyl or is (CH 2 ) n -cycloalkyl, optionally substituted by hydroxy, or is -N(R)-cycloalkyl, optionally substituted by hydroxy or lower alkyl, or is phenyl, optionally substituted by lower alkoxy, halogen, halogen-lower alkyl, lower alkyl, -CH 2 -pyrrolidin-1-yl, -CH 2 -morpholinyl, -CH 2 N(R)(CH 2 ) 2 0CH 3 or -CH 2 -N(R)C(O)-lower alkyl, or is 1,4-dioxa-8-aza-spiro[4,5]decane, or is 2-oxa-5-aza-bicyclo[2.2.1]heptane, or is I-oxa-8-aza-spiro[4,5]decane, or is -N(R)-7-oxa-bicyclo [2.2. 11 hept-2-yl, or is 2-aza-bicyclo[2.2.2]decane; R is hydrogen or lower alkyl; n is 0 or 1; and pharmaceutically acceptable acid addition salts thereof for the treatment of diseases, which relate to the A2A receptor.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是1,4-二氧杂环戊烷基或四氢吡喃-4-基; R 2是-N（R） - （CH 2）n，5-或6-元非芳族杂环，任选地被一个或多个选自低级烷基或-NR 2的取代基取代，或是 - （（CH 2）n -OH，低级烷基，低级烷氧基或-CH 2）n-5-或6元芳族杂环，任选被低级烷基，低级烷氧基，卤素，卤素 - 低级烷基，-CH2N（R）（CH2）20CH3，-N（R）（CH2）20CH3，-CH2-吗啉基或-CH2-吡咯烷基或是（CH2）或被羟基或低级烷基取代的-N（R） - 环烷基，或为任选被低级烷氧基，卤素，卤素 - 低级烷基，低级烷基，-CH 2 - 吡咯烷-1-基，-CH 2 - 吗啉基，-CH 2 N（R）（CH 2）20 CH 3或-CH 2 -N（R）C（O） - 低级烷基，或是1,4-二氧杂-8-氮杂 - 螺[4,5]癸烷或者是2-氧杂-5-氮杂 - 双环[2.2.1]庚烷，或是1-氧杂-8-氮杂 - 螺[4,5]癸烷，或是-N（R）-7-氧杂双环 [2.2。 11庚-2-基，或是2-氮杂 - 双环[2.2.2]癸烷; R是氢或低级烷基; n为0或1; 和其药学上可接受的酸加成盐，用于治疗涉及A2A受体的疾病。

5. 发明申请

WO2004089949A1 7-([1,4]DIOXAN-2-YL)-BENZOTHIAZOLE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译： 7 - （[1,4]二恶烷-2-基） - 苯并噻唑衍生物作为腺苷受体配体
公开(公告)号：WO2004089949A1
公开(公告)日：2004-10-21
申请号：PCT/EP2004/003734
申请日：2004-04-07
申请人： F. HOFFMANN-LA ROCHE AG , FLOHR, Alexander , NORCROSS, Roger, David
发明人： FLOHR, Alexander , NORCROSS, Roger, David
IPC分类号： C07D417/14
CPC分类号： C07D417/14 , C07D417/04 , C07D471/08 , C07D491/10
摘要： The present invention relates to compounds of the general formula wherein R 1 is a dioxan group as described in claim 1 and R 2 is unsubstituted or substituted -(CH 2 ) n -pyridin-2,3 or 4-yl; or is unsubstituted or mono- or di-substituted -(CH 2 ) n -PiPeridine- 1-yl; or is unsubstituted or mono-or di-substituted -(CH 2 ) n -phenyl; or is benzof [1.3] dioxol-5-yl; or -(CH 2 ) n -morpholinyl; or -(CH 2 ) n -tetrahydropyran-4-yl; or -(CH 2 ) n -O-lower alk-yl; or -(CH 2 ) n ,-cycloalkyl; or -(CH 2 ) n -C(0)-NR'R"; or -(CH 2 ) n -2-oxo-pyrrolidin-1-yl; or -(CH 2 ) n NRR"; or -2-oxa-5-aza-icyclo[2.2.1]heptane 5-yl; or -l-oxa-8-aza-spiro[4.5]decane-8-yl; and R'and R" are independently from each other lower alkyl, '(CH 2 ) o -O-lower alkyl, mono- or disubstituted cycloalkyl; and n is 0, 1, 2 or 3; m is 0 or 1; and o is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof It has been found that the compounds of general formula I are adenosine receptor ligands with a good affinity to the A 2A -receptor and a high selectivity to the A 1 - and A 3 receptors.
摘要翻译：本发明涉及通式的化合物，其中R 1是如权利要求1所述的二烷基，R 2是未取代的或取代的 - （CH 2）n - 吡啶-2,3或4-基; 或未取代的或单取代或二取代的 - （CH 2）n - 哌啶-1-基; 或未取代的或单或二取代的 - （CH 2）n - 苯基; 或者是[1,3]二氧杂环戊烯-5-基的苯并[ 或 - （CH 2）n - 吗啉基; 或 - （CH 2）n - 四氢吡喃-4-基; 或 - （CH 2）n -O-低级烷基; 或 - （CH 2）n - - 环烷基; 或 - （CH 2）n -C（O）-NR'R“;或 - （CH 2）n -2-氧代 - 吡咯烷-1-基;或 - （CH 2）n NRR”; 或-2-氧杂-5-氮杂 - 环烯[2.2.1]庚烷-5-基; 或-1-氧杂-8-氮杂 - 螺[4.5]癸烷-8-基; 并且R 1和R 2彼此独立地为低级烷基，（CH 2）o-低级烷基，单或二取代的环烷基; n为0,1,2或3; m为0或1;和o 是1或2;以及其药学上可接受的酸加成盐已经发现，通式I的化合物是对A 2A和A A受体具有高亲和力的腺苷受体配体。

6. 发明申请

WO2006048146A1 QUINOLINE AS ALLOSTERIC ENHANCERS OF THE GABA-B RECEPTORS 审中-公开
标题翻译：喹啉作为GABA-B受体的独立增强剂
公开(公告)号：WO2006048146A1
公开(公告)日：2006-05-11
申请号：PCT/EP2005/011403
申请日：2005-10-25
申请人： F. HOFFMANN-LA ROCHE AG , MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger, David , RATNI, Hasane , THOMAS, Andrew, William
发明人： MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger, David , RATNI, Hasane , THOMAS, Andrew, William
IPC分类号： C07D215/18 , C07D215/20 , C07D491/04 , C07D215/38 , C07D401/04 , A61K31/4738 , A61P25/22
CPC分类号： C07D215/38 , C07D215/18 , C07D215/20 , C07D401/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 to R 6 are as defined as described herein, which compounds are active at the GABA B receptor and can be used for the preparation of medicaments useful in the treatment of CNS disorders comprising anxiety and depression.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 6如本文所述，其化合物在GABA B上具有活性， / SUB>受体，可用于制备用于治疗包括焦虑和抑郁症的中枢神经系统疾病的药物。

7. 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。

8. 发明申请

WO2004063177A1 BENZOXAZOLE DERIVATIVES AND THEIR USE AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：苯并噻唑衍生物及其作为腺苷受体配体的用途
公开(公告)号：WO2004063177A1
公开(公告)日：2004-07-29
申请号：PCT/EP2004/000053
申请日：2004-01-08
申请人： F. HOFFMANN-LA ROCHE AG , NORCROSS, Roger, David
发明人： NORCROSS, Roger, David
IPC分类号： C07D263/58
CPC分类号： C07D263/58 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The invention relates to compounds of formula (I), wherein R is phenyl, unsubstituted or substituted by halogen or -CH 2 N(CH 3 )(CH 2 ) n OCH 3 , or is benzyl, lower alkyl, lower alkoxy, -(CH 2 ) n OCH 3 , or is pyridin 3-or 4-yl, unsubstituted or substituted by lower alkyl, halogen, morpholinyl, -(CH 2 ) n -halogen, -(CH 2 ) n OCH 3 -(CH 2 ) n -morpholin-4-yl, or -(CH 2 ) n pyrrolidin-1-yl; R 1 is phenyl, unsubstituted or substituted by halogen, tetrahydropyran-4-yl, 3,6-dihydro-2 H -pyran-4-yl or morpholin-4-yl; n is independently from each other 1 or 2; and to pharmaceutically acceptable acid addition salts thereof for the treatment of diseases related to the adenosine A 2A -receptor.
摘要翻译：本发明涉及式（I）化合物，其中R是未被取代或被卤素或-CH 2 N（CH 3）（CH 2）n OCH 3或被苄基，低级烷基，低级烷氧基， - （CH 2）n OCH 3或取代的苯基，吡啶3-或4-基，未取代或被低级烷基，卤素，吗啉基， - （CH 2）n - 卤素， - （CH 2）n OCH 3 - （CH 2）n - 吗啉-4-基或 - （CH 2）环丁烷-1-基; R 1是未被取代或被卤素取代的苯基，四氢吡喃-4-基，3,6-二氢-2H-吡喃-4-基或吗啉-4-基; n彼此独立地为1或2; 以及其药学上可接受的酸加成盐，用于治疗与腺苷A2A受体有关的疾病。

9. 发明申请

WO2005028484A1 THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：作为腺苷受体配体的噻唑吡啶衍生物
公开(公告)号：WO2005028484A1
公开(公告)日：2005-03-31
申请号：PCT/EP2004/010179
申请日：2004-09-11
申请人： F. HOFFMANN-LA ROCHE AG , NORCROSS, Roger, David
发明人： NORCROSS, Roger, David
IPC分类号： C07D513/04
CPC分类号： C07D513/04
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is morpholin-4-yl, phenyl or tetrahydropyran-4-yl; R 2 is -(CH 2 ) n -aryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkoxy, lower alkyl, -(CH 2 ) n NR’R", -0 (CH 2 ) n -O -lower alkyl, or -(CH 2 ) n -heterocyclyl, or is heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, -(CH 2 ) n NR'R", -(CH 2 ) n -heterocyclyl, which is optionally substituted by hydroxy or lower alkoxy, or is -(CH 2 ) n -heterocyclyl, optionally substituted by one or more substituents selected from the group consisting of -(CH 2 ) n ,-OH, -(CH 2 ) n -O-lower alkyl or lower alkyl, or is -(CH 2 ) n -cycloalkyl, or is - (CH 2 ) n ,-O -lower alkyl, or is NR'R’’, or is benzo[1,3]dioxole, 2-methyl-l-oxo-2,8-diaza-spiro[4,5] decane, 2-oxa-5-azabicyclo [2.2.1]heptane or I-oxa-8-aza-spiro[4.5]decane; R',R" are independently from each other lower alkyl, - (CH 2 ) n ,-O -lower alkyl or cycloalkyl, optionally substituted by hydroxy; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaernia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure. The most preferred indications in accordance with the present invention are those which include disorders of the central nervous system, for example the treatment or prevention of Alzheimer's disease, certain depressive disorders, drug addiction, neuroprotection and Parkinson's disease as well as ADHD.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是吗啉-4-基，苯基或四氢吡喃-4-基; R 2是未被取代或被一个或多个选自卤素，低级烷氧基，低级烷基， - （CH 2）n NR'R“， - O（CH 3）的取代基取代的 - （CH 2）或（O） - 低级烷基，或 - （CH 2）n - 杂环基，或是未被取代或被一个或多个选自低级烷基，低级烷氧基， - （CH 2）n NR' （CH 2）n - 杂环基，其任选被羟基或低级烷氧基取代，或是 - （CH 2）n - 杂环基，任选被一个或多个选自以下的取代基取代： - （CH 2）n， -OH， - （CH 2）n O-低级烷基或低级烷基，或是 - （CH 2）n - 环烷基，或是 - （CH 2）n，-O-低级烷基或NR'R“ [1,3]二氧杂环戊烯，2-甲基-1-氧代-2,8-二氮杂 - 螺[4,5]癸烷，2-氧杂-5-氮杂双环[2.2.1]庚烷或1-氧杂-8-氮杂 - 螺[4.5]癸烷; R'，R“彼此独立地为低级烷基， - （CH 2）n，-O-低级烷基或环烷基，任选被羟基取代; n为0,1或2;以及其药学上可接受的酸加成盐。基于腺苷系统的调节，诸如阿尔茨海默氏病，帕金森病，亨廷顿病，神经保护，精神分裂症，焦虑症，疼痛，呼吸缺陷，抑郁症，药物成瘾如安非他明，化合物可用于控制或预防疾病，可卡因，阿片样物质，乙醇，尼古丁，大麻素，或抗哮喘，过敏反应，缺氧，异己蝇，癫痫发作和药物滥用。此外，本发明化合物可用作镇静剂，肌肉松弛剂，抗精神病药，抗癫痫药，抗惊厥药和心脏保护剂冠状动脉疾病和心力衰竭等疾病的药剂。根据本发明的最优选的适应症是包括疾病的那些例如中枢神经系统，例如治疗或预防阿尔茨海默病，某些抑郁障碍，药物成瘾，神经保护和帕金森病以及ADHD。

10. 发明申请

WO2006072436A1 [4-(HETEROARYL) PIPERAZIN-1-YL]-(2,5-SUBSTITUTED -PHENYL)METHANONE DERIVATIVES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译：作为用于治疗神经病学和神经病学疾病的甘氨酸运输1（GLYT-1）抑制剂的[4-（异丁基）哌嗪-1-基] - （2,5-取代的苯基）甲酮衍生物
公开(公告)号：WO2006072436A1
公开(公告)日：2006-07-13
申请号：PCT/EP2005/014082
申请日：2005-12-28
申请人： F. HOFFMANN-LA ROCHE AG , JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
发明人： JOLIDON, Synese , NARQUIZIAN, Robert , NORCROSS, Roger, David , PINARD, Emmanuel
IPC分类号： A61K31/427 , A61K31/433 , A61P25/28 , C07D277/42 , C07D277/56 , C07D417/12 , C07D285/12 , C07D285/08
CPC分类号： C07D285/08 , C07D277/42 , C07D277/56 , C07D285/135 , C07D417/12
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is-OR 1’ ,-SR 1’ or is a heterocycloalkyl group; R 1’ is lower alkyl, lower alkyl substituted by halogen or is -(CH 2 ) n -cycloalkyl; R 2 is-S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; X 1 is CR 3 or N; X 2 is CR 3’ or N; R 3 /R 3’ are independently from each other hydrogen, halogen, lower alkyl, CN, NO 2 ,-S(O) 2 -phenyl, -S(O) 2 -lower alkyl, -S(O) 2 -pyridin-2, 3 or 4-yl, phenyl, optionnally substituted by one or two substituents selected from the group consisting of NO 2 or halogen, or is lower alkyl substituted by halogen or is -C(O)-lower alkyl; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. It has been found that the compounds of general formula (I) are good inhibitors of the glycine transporter 1 (GlyT-1). They may be used in the treatment of schizophrenia.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是 - 或 - 1'， - SR 1'或其是杂环烷基 R 1是低级烷基，被卤素取代的低级烷基或是 - （CH 2 CH 2）n - 环烷基; R 2是-S（O）2 - 低级烷基，-S（O）2 NH-低级烷基，NO 2 或CN; X 1是CR 3或N; X 2是CR 3或N; R 3和R 3彼此独立地为氢，卤素，低级烷基，CN，NO 2，-S（O） -S（O）2 - 低级烷基，-S（O）2 - 吡啶基-2,3或4-基 - ，苯基，其选自一个或两个选自NO 2或卤素的取代基，或被卤素取代的低级烷基或-C（O） - 低级烷基; n为0,1或2; 及其药学上可接受的酸加成盐。已经发现通式（I）的化合物是甘氨酸转运蛋白1（GlyT-1）的良好抑制剂。它们可用于治疗精神分裂症。

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