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1. 发明授权

US08772510B2 PDE10 modulators 有权
标题翻译： PDE10调制器
公开(公告)号：US08772510B2
公开(公告)日：2014-07-08
申请号：US13598848
申请日：2012-08-30
申请人： Stephan Bachmann , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Markus Rudolph
发明人： Stephan Bachmann , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Markus Rudolph
IPC分类号： C07D249/04 , C07D233/54 , C07D231/10 , C07D207/30
CPC分类号： C07D471/04 , C07D231/14 , C07D233/90 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention relates to compounds of formula (I) wherein R1, R2, R3, R5, W, X, X1, Y, Y1, Z and Z1 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit PDE10A and can be used in the treatment of CNS disorders such as schizophrenia, Alzheimer's disease, and Parkinson's disease.
摘要翻译：本发明涉及式（I）化合物，其中R 1，R 2，R 3，R 5，W，X，X 1，Y，Y 1，Z和Z 1如说明书和权利要求书中所定义，以及生理上可接受的盐其中。这些化合物抑制PDE10A，可用于治疗CNS疾病如精神分裂症，阿尔茨海默病和帕金森病。

2. 发明授权

US08703768B2 Nitrogen containing heteroaryl compounds 有权
标题翻译：含氮杂芳基化合物
公开(公告)号：US08703768B2
公开(公告)日：2014-04-22
申请号：US13151301
申请日：2011-06-02
申请人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Felix Gruber , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento
发明人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Felix Gruber , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento
IPC分类号： C07D239/42 , A01N43/54 , A61K31/5355 , C07D403/14 , A61K31/497 , A61P25/18
CPC分类号： C07D401/14 , C07D403/12 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl compounds of formula (I) wherein A1, A2, R1, R2, R3, R4, R5 and R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used as therapeutics.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基化合物，其中A1，A2，R1，R2，R3，R4，R5和R6如说明书和权利要求书中所定义，以及生理上可接受的盐和的酯。这些化合物抑制PDE10A，可用作治疗剂。

3. 发明授权

US08263584B2 Imidazopyridines 有权
标题翻译：咪唑并吡啶
公开(公告)号：US08263584B2
公开(公告)日：2012-09-11
申请号：US13151310
申请日：2011-06-02
申请人： Daniela Alberati , Ruben Alvarez Sanchez , Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Markus Rudolph
发明人： Daniela Alberati , Ruben Alvarez Sanchez , Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Markus Rudolph
IPC分类号： A61K31/437 , A61K31/5377 , A61K31/4985 , A61K31/553 , A61K31/541 , C07D519/00 , C07D471/04 , A61P25/22 , A61P25/18
CPC分类号： C07D471/04 , A61K31/437 , A61K31/496 , A61K31/5025 , A61K31/5377 , A61K31/553 , C07D487/04
摘要： The invention is concerned with novel imidazopyridine derivatives of formula (I) wherein R1, R2, R3, R4, R5 and A are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit PDE10A and can be used for the treatment of various diseases, including central nervous system disorders such as Alzheimer's disease, Parkinson's disease, and schizophrenia.
摘要翻译：本发明涉及式（I）的新咪唑并吡啶衍生物，其中R 1，R 2，R 3，R 4，R 5和A如说明书和权利要求书中所定义，以及其生理上可接受的盐和酯。这些化合物抑制PDE10A，可用于治疗各种疾病，包括中枢神经系统疾病如阿尔茨海默病，帕金森病和精神分裂症。

4. 发明授权

US07371748B2 Benzothiazole derivatives 有权
标题翻译：苯并噻唑衍生物
公开(公告)号：US07371748B2
公开(公告)日：2008-05-13
申请号：US10847558
申请日：2004-05-17
申请人： Alexander Flohr , Roland Jakob-Roetne , Roger David Norcross , Claus Riemer
发明人： Alexander Flohr , Roland Jakob-Roetne , Roger David Norcross , Claus Riemer
IPC分类号： C07D413/14 , C07D417/02 , A61K31/4436 , A61K31/5377
CPC分类号： C07D417/04 , C07D417/14 , C07D491/10
摘要： This invention relates to compounds of formula I wherein R1 and R2 are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compounds of formula I are adenosine receptor ligands with good affinity to the A2A-receptor and a high selectivity to the A1- and A3 receptors. These compounds are useful, inter alia, in treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.
摘要翻译：本发明涉及其中R 1和R 2 2定义的式I化合物或其药学上可接受的盐。已经发现，式I化合物是对A 2A受体具有良好亲和力的腺苷受体配体，对A 1 - 和 - A _{3个受体。这些化合物尤其可用于治疗阿尔茨海默氏病，抑郁症，帕金森病和ADHD。}

5. 发明申请

US20080108809A1 BENZOTHIAZOLE DERIVATIVES WITH ACTIVITY AS ADENOSINE RECEPTOR LIGANDS 审中-公开
标题翻译：具有作为腺苷受体配体的活性的苯并噻唑衍生物
公开(公告)号：US20080108809A1
公开(公告)日：2008-05-08
申请号：US11930799
申请日：2007-10-31
申请人： Alexander Alanine , Alexander Flohr , Aubry Miller , Roger Norcross , Claus Riemer
发明人： Alexander Alanine , Alexander Flohr , Aubry Miller , Roger Norcross , Claus Riemer
IPC分类号： C07D277/82 , C07D417/00
CPC分类号： C07D417/04 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/5375 , A61K31/541 , A61K31/5513 , C07D277/82 , C07D417/12 , C07D417/14
摘要： The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
摘要翻译：本发明涉及取代的苯并噻唑衍生物及其药学上可接受的盐，其可用于治疗与腺苷受体有关的疾病。

6. 发明授权

US07166587B2 Carbamic acid alkyl ester derivatives 有权
标题翻译：氨基甲酸烷基酯衍生物
公开(公告)号：US07166587B2
公开(公告)日：2007-01-23
申请号：US10951229
申请日：2004-09-27
申请人： Alexander Flohr , Guido Galley , Roland Jakob-Roetne , Eric Argirios Kitas , Jens-Uwe Peters , Wolfgang Wostl
发明人： Alexander Flohr , Guido Galley , Roland Jakob-Roetne , Eric Argirios Kitas , Jens-Uwe Peters , Wolfgang Wostl
IPC分类号： C07D243/18 , C07D243/12 , A61K31/55 , A61K31/5513 , A61P25/28
CPC分类号： C07D409/12 , C07D223/16 , C07D223/18 , C07D243/12 , C07D243/24
摘要： The present invention provides compounds of the general formula wherein R4 is one of the following groups and R1, R2, R3, R7, R8, and R9 are as defined in the specification and pharmaceutically acceptable salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are useful for the treatment of Alzheimer's disease.
摘要翻译：本发明提供以下通式的化合物，其中R 4为下列基团之一，R 1，R 2，R 2， 3，R 7，R 8和R 9如本说明书和药学上可接受的盐，光学纯对映异构体，外消旋物或非对映体混合物。该化合物可用于治疗阿尔茨海默病。

7. 发明授权

US07019001B2 Substituted benzothiazole amide derivatives 失效
标题翻译：取代的苯并噻唑酰胺衍生物
公开(公告)号：US07019001B2
公开(公告)日：2006-03-28
申请号：US10691770
申请日：2003-10-23
申请人： Alexander Flohr , Roland Jakob-Roetne , Roger David Norcross , Claus Riemer
发明人： Alexander Flohr , Roland Jakob-Roetne , Roger David Norcross , Claus Riemer
IPC分类号： A61K31/5377 , C07D413/02
CPC分类号： A61K31/428 , A61K31/5377 , C07D277/82 , C07D417/12 , C07D451/06 , C07D453/06 , C07D471/10 , C07D487/10 , C07D491/08
摘要： A compound of formula I and a method of treatment of diseases, related to modulation of the adenosine A2 receptor system comprising administering a compound of formula to a person in need of such treatment.
摘要翻译：式I的化合物和与腺苷A 2受体系统的调节相关的疾病的治疗方法，包括向需要这种治疗的人施用配方的化合物。

8. 发明申请

US20060019950A1 Benzathiazol-acetamides 失效
标题翻译：苯并噻唑 - 乙酰胺
公开(公告)号：US20060019950A1
公开(公告)日：2006-01-26
申请号：US11181573
申请日：2005-07-14
申请人： Alexander Flohr , Claus Riemer
发明人： Alexander Flohr , Claus Riemer
IPC分类号： A61K31/5377 , C07D417/04
CPC分类号： C07D491/08 , C07D277/82
摘要： The present invention relates to compounds of the general formula wherein R1 is cycloalkyl, substituted by OR or is 2-(7-oxa-bicyclo[2.2.1]hept-1-yl)-ethyl; R is hydrogen, lower alkyl or C(O)-lower alkyl; X is —CHR′—; and R′ is hydrogen or lower alkyl; and pharmaceutically acceptable acid addition salts, optically pure enantiomeres, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, ADHD, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or for the treatment of asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse, or for use as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for coronary artery disease and heart failure.
摘要翻译：本发明涉及以下通式的化合物：其中R 1是被OR取代的环烷基或是2-（7-氧杂双环[2.2.1]庚-1-基） - 乙基; R为氢，低级烷基或C（O） - 低级烷基; X是-CHR'-; 和R'是氢或低级烷基; 和药学上可接受的酸加成盐，光学纯对映体，外消旋体或非对映异构体混合物，用于治疗阿尔茨海默病，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，ADHD，药物成瘾如苯丙胺，可卡因，阿片样物质，乙醇，尼古丁，大麻素，或用于治疗哮喘，过敏反应，缺氧，局部缺血，癫痫发作和物质滥用，或用作镇静剂，肌肉松弛剂，抗精神病药，抗癫痫药，抗惊厥药和冠状动脉卡介保护剂疾病和心力衰竭。

9. 发明申请

US20060019949A1 Benzothiazole derivatives 有权
标题翻译：苯并噻唑衍生物
公开(公告)号：US20060019949A1
公开(公告)日：2006-01-26
申请号：US11183503
申请日：2005-07-18
申请人： Alexander Flohr , Claus Riemer
发明人： Alexander Flohr , Claus Riemer
IPC分类号： A61K31/5377 , C07D413/14
CPC分类号： C07D417/12
摘要： The present invention relates to compounds of formulae IA and IB wherein R1 and R2 are each independently lower alkyl or —(CH2)m—O-lower alkyl, or together with the N atom to which they are attached form a heterocyclic ring; R3 is hydrogen or lower alkyl; R4 is lower alkyl; hetaryl is 3H-imidazole-2,4-diyl or 1H-pyrazole-1,4-diyl; n is 1 or 2; and m is 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used for the treatment of Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, ADHD, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or for the treatment of asthma, allergic responses, hypoxia, ischaemia, seizure and substance abuse, or for use as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for coronary artery disease and heart failure.
摘要翻译：本发明涉及式IA和IB的化合物，其中R 1和R 2各自独立地为低级烷基或 - （CH 2 CH 2）或者与它们所连接的N原子一起形成杂环; R 3是氢或低级烷基; R 4是低级烷基; 杂芳基是3H-咪唑-2,4-二基或1H-吡唑-1,4-二基; n为1或2; m为1或2; 及其药学上可接受的酸加成盐。这些化合物可用于治疗阿尔茨海默氏病，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，ADHD，药物成瘾如苯丙胺，可卡因，阿片样物质，乙醇，尼古丁，大麻素，或用于治疗哮喘，过敏反应，缺氧，局部缺血，癫痫发作和药物滥用，或用作镇静剂，肌肉松弛剂，抗精神病药，抗癫痫剂，抗惊厥药和心脏保护剂用于冠状动脉疾病和心力衰竭。

10. 发明授权

US06963000B2 Benzothiazole derivatives with activity as adenosine receptor ligands 失效
标题翻译：具有活性作为腺苷受体配体的苯并噻唑衍生物
公开(公告)号：US06963000B2
公开(公告)日：2005-11-08
申请号：US10322272
申请日：2002-12-18
申请人： Alexander Alanine , Alexander Flohr , Aubry Kern Miller , Roger David Norcross , Claus Riemer
发明人： Alexander Alanine , Alexander Flohr , Aubry Kern Miller , Roger David Norcross , Claus Riemer
IPC分类号： A61K31/422 , A61K31/423 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/455 , A61K31/4725 , A61K31/496 , A61K31/5375 , A61K31/5377 , A61K31/541 , A61K31/551 , A61K31/5513 , A61P11/06 , A61P21/02 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/28 , C07D277/82 , C07D417/04 , C07D417/12 , C07D417/14 , C07D277/04
CPC分类号： C07D417/04 , A61K31/427 , A61K31/428 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/5375 , A61K31/541 , A61K31/5513 , C07D277/82 , C07D417/12 , C07D417/14
摘要： The present invention relates to substituted benzothiazole derivitives and to their pharmaceutically acceptable salts useful for the treatment of diseases related to the adenosine receptor.
摘要翻译：本发明涉及取代的苯并噻唑衍生物及其药学上可接受的盐，其可用于治疗与腺苷受体有关的疾病。

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