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1. 发明申请

WO2006128802A3 3-METHANESULFONYLQUINOLINES AS GABA-B ENHANCERS 审中-公开
标题翻译：作为GABA-B增强剂的3-甲磺酰基胆碱
公开(公告)号：WO2006128802A3
公开(公告)日：2007-04-12
申请号：PCT/EP2006062514
申请日：2006-05-23
申请人： HOFFMANN LA ROCHE , MALHERBE PARICHEHR , MASCIADRI RAFFAELLO , NORCROSS ROGER DAVID , PRINSSEN ERIC
发明人： MALHERBE PARICHEHR , MASCIADRI RAFFAELLO , NORCROSS ROGER DAVID , PRINSSEN ERIC
IPC分类号： C07C225/22 , A61K31/47 , A61K31/4709 , C07D215/36 , C07D215/38 , C07D215/42 , C07D265/22 , C07D401/04
CPC分类号： C07D265/22 , C07D215/36 , C07D215/38 , C07D215/42 , C07D401/04
摘要： The present invention relates to compounds of formula (I) wherein R 1 , R 2 and R 3 are as defined hereinabove which are active at the GABA B receptor and which can be used for the preparation of medicaments useful in the control or prevention of CNS disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3和R 3如上所定义，其在 GABA B 受体，其可用于制备可用于控制或预防CNS障碍的药物。

2. 发明申请

WO2006063709A1 BI- AND TRICYCLIC SUBSTITUTED PHENYL METHANONES AS GLYCINE TRANSPORTER I (GLYT-1) INHIBITORS FOR THE TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译：作为治疗阿尔茨海默病的糖蛋白转运蛋白I（GLYT-1）抑制剂的BI-和三聚取代的苯甲醇
公开(公告)号：WO2006063709A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/012994
申请日：2005-12-05
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： C07D495/04 , C07D513/04 , C07D487/04 , C07D471/04 , A61K31/4985 , A61K31/4365 , A61K31/437 , A61P25/28
CPC分类号： C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The present invention relates to compounds of the general formula (I), wherein formula (II) is A or B or C or D or E or F. R 1 is a non aromatic heterocycle, or is OR' or N(R") 2 ; R' is lower alkyl, lower alkyl substituted by halogen or is -(CH 2 ) ri cycloalkyl; R" is lower alkyl; R 2 is NO 2 , CN or SO 2 R"; R 3 is hydrogen, halogen, lower alkyl, lower alkoxy, or lower alkyl substituted by halogen; R 4 is hydrogen, lower alkyl, phenyl substituted by halogen or CF 3 , or is a five or six membered aromatic heterocycle; R 5 /R 6 are hydrogen, halogen, lower alkyl, lower alkoxy, or are lower alkyl or lower alkoxy, substituted by halogen; R 7 is hydrogen or lower alkyl; n is 0, 1 or 2; and to pharmaceutically active acid addition salts for the treatment of neurological and neuropsychiatric disorders.
摘要翻译：本发明涉及通式（I）的化合物，其中式（II）是A或B或C或D或E或F.R 1是非芳族杂环，或OR '或N（R“）2'; R'是低级烷基，被卤素取代的低级烷基，或是 - （CH 2）n N' ; R“为低级烷基; R 2是NO 2，CN或SO 2 R“; R 3是氢，卤素，低级烷基，低级烷氧基或被卤素取代的低级烷基; R 4是氢，低级烷基，被卤素或CF 3 N取代的苯基，或是五或六元芳族杂环 R 5是氢，卤素，低级烷基，低级烷氧基，或被卤素取代的低级烷基或低级烷氧基; R 7， SUP>是氢或低级烷基; n是0,1或2;以及用于治疗神经和神经精神障碍的药学活性的酸加成盐。

3. 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。

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

WO2006072435A1 SULFANYL SUBSTITUTED PHENYL METHANONES AS GLYCINE TRANSPORTER 1 (GLYT-1) INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL AND NEUROPSYCHIATRIC DISORDERS 审中-公开
标题翻译： SULFANYL取代苯甲酸酯作为甘油运输机1（GLYT-1）用于治疗神经病学和神经病学疾病的抑制剂
公开(公告)号：WO2006072435A1
公开(公告)日：2006-07-13
申请号：PCT/EP2005/014081
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： C07D295/18 , C07D213/74 , C07D239/42 , A61K31/506 , A61K31/496 , A61K31/495 , A61P25/28
CPC分类号： C07D213/74 , C07D239/42 , C07D295/192
摘要： The present invention relates to compounds of the general formula (I) wherein R 1 is lower alkyl or lower alkyl substituted by halogen; R 2 is -S(O) 2 -lower alkyl, -S(O) 2 NH-lower alkyl, NO 2 or CN; R 3 is halogen, CN, lower alkyl, lower alkyl substituted by halogen, NO 2 , -C(O)-lower alkyl or S(O) 2 -lower alkyl; X/X 1 are independently from each other CR 4 or N; R 4 is hydrogen or halogen; 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 (G1yT-1) for the treatment of schizophrenia.
摘要翻译：本发明涉及通式（I）的化合物，其中R 1是被卤素取代的低级烷基或低级烷基; R 2是-S（O）2 - 低级烷基，-S（O）2 NH-低级烷基，NO 2 或CN; R 3是卤素，CN，低级烷基，被卤素取代的低级烷基，NO 2 - ， - C（O） - 低级烷基或S（O）2 低级烷基; X / X 1彼此独立地为CR 4或N; R 4是氢或卤素; n为0,1或2; 和其药学上可接受的酸加成盐。已经发现，通式（I）的化合物是用于治疗精神分裂症的甘氨酸转运蛋白1（G1yT-1）的良好抑制剂。

6. 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。

7. 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。

8. 发明申请

WO2007014843A1 2-HYDROXY-PROPIONIC ACID DERIVATIVES AND 3-HYDROXY-BENZOFURAN-2-ONE DERIVATIVES WITH AFFINITY FOR THE GABA-B-RECEPTOR 审中-公开
标题翻译： 2-羟基 - 丙酸衍生物和具有GABA-B受体亲和性的3-羟基 - 苯并呋喃-2-酮衍生物
公开(公告)号：WO2007014843A1
公开(公告)日：2007-02-08
申请号：PCT/EP2006/064347
申请日：2006-07-18
申请人： F. HOFFMANN-LA ROCHE AG , MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger David , PRINSSEN, Eric
发明人： MALHERBE, Parichehr , MASCIADRI, Raffaello , NORCROSS, Roger David , PRINSSEN, Eric
IPC分类号： C07D307/84 , C07D209/34 , C07C235/00 , C07C59/00 , A61K31/343 , A61K31/404 , A61P25/00
CPC分类号： C07D209/38 , C07C59/56 , C07C69/732 , C07D209/34 , C07D307/83 , C07D307/84
摘要： The present invention relates to compounds of formula I, wherein R 1 , R 2 , R 3 , R 4 , R 5 and R 6 are as defined in the specification and claims, which compounds are active on the GABA B receptor and are useful in the control or prevention of CNS illnesses, especially of illnesses and disorders comprising anxiety, depression, epilepsy, schizophrenia, and cognitive disorders.
摘要翻译：本发明涉及式I化合物，其中R 1，R 2，R 3，R 4， R 5和R 6如说明书和权利要求中所定义，该化合物在GABA B受体上具有活性，并且可用于控制或预防CNS疾病，特别是包括焦虑，抑郁，癫痫，精神分裂症和认知障碍的疾病和病症。

9. 发明申请

WO2006079467A1 PHENYL METHANONE DERIVATIVES AND THEIR USE AS GLYCINE TRANSPORTER 1 INHIBITORS 审中-公开
标题翻译：苯甲酮衍生物及其作为甘氨酸运输商1抑制剂
公开(公告)号：WO2006079467A1
公开(公告)日：2006-08-03
申请号：PCT/EP2006/000361
申请日：2006-01-17
申请人： F. HOFMANN-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： C07D471/04 , C07D217/06 , C07D215/14 , C07D491/04 , A61K31/47 , A61K31/472 , A61K31/519
CPC分类号： C07D471/04 , C07D215/14 , C07D217/06 , C07D491/04
摘要： The present invention relates to compounds of general formula IA or IB. The compounds may be used for the treatment of diseases related to the glycine transporter inhibitor.
摘要翻译：本发明涉及通式IA或IB的化合物。该化合物可用于治疗与甘氨酸转运蛋白抑制剂有关的疾病。

10. 发明申请

WO2006063732A1 THIENO-PYRIDINE DERIVATIVES AS GABA-B ALLOSTERIC ENHANCERS 审中-公开
标题翻译：三苯基吡啶衍生物作为GABA-B无菌增强剂
公开(公告)号：WO2006063732A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/013194
申请日：2005-12-09
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： C07D495/04 , A61K31/435 , A61P25/00 , C07D495/14
CPC分类号： C07D495/04 , C07D495/14
摘要： The present invention relates to compounds of formula (I), Wherein R 1 to R 5 are as defined in the specification which compounds are active on the GABA B receptor and can be used for the manufacture of medicaments useful for treating CNS disorders.
摘要翻译：本发明涉及式（I）化合物，其中R 1至R 5如本说明书中所定义，其化合物在GABA B上具有活性， / SUB>

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