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61. 发明授权

US08183380B2 2-aminoquinolines 失效
标题翻译： 2-氨基喹啉
公开(公告)号：US08183380B2
公开(公告)日：2012-05-22
申请号：US12393058
申请日：2009-02-26
申请人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： C07D215/38
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D451/14
摘要： The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
摘要翻译：本发明涉及式I的2-氨基喹啉衍生物，其中R 1，R 2，R 3，R 4，R 5，R 6，A和n如说明书和权利要求书中所定义，它们的用途为5-HT5A受体拮抗剂，和含有它们的药物组合物。

62. 发明申请

US20100075959A1 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：US20100075959A1
公开(公告)日：2010-03-25
申请号：US12628243
申请日：2009-12-01
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： A61K31/5377 , A61K31/425 , A61P25/16 , A61P25/00
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 derivatives 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。

63. 发明申请

US20090227628A1 2-AMINOQUINOLINES 失效
标题翻译： 2-氨基喹啉
公开(公告)号：US20090227628A1
公开(公告)日：2009-09-10
申请号：US12394083
申请日：2009-02-27
申请人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
发明人： Sabine Kolczewski , Claus Riemer , Olivier Roche , Lucinda Steward , Juergen Wichmann , Thomas Woltering
IPC分类号： A61K31/4709 , C07D215/38 , A61K31/47 , A61P25/24 , A61P25/22 , A61P25/00
CPC分类号： C07D215/38 , C07D405/12
摘要： The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
摘要翻译：本发明涉及式I的2-氨基喹啉衍生物，其中Z，R 1和Ar 1如本文所定义，含有它们的药物组合物，其制备方法。这些化合物是5-HT5A受体拮抗剂，可用于预防和/或治疗抑郁症，焦虑障碍，精神分裂症，恐慌症，广场恐怖症，社交恐惧症，强迫症，创伤后应激障碍，疼痛，记忆障碍，痴呆饮食行为障碍，性功能障碍，睡眠障碍，药物滥用，运动障碍如帕金森病，精神病或胃肠疾病。

64. 发明授权

US07317007B2 Benzothiazole derivatives with activity as adenosine receptor ligands 有权
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：US07317007B2
公开(公告)日：2008-01-08
申请号：US11219577
申请日：2005-09-02
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： A61K31/535 , C07D413/00
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。

65. 发明申请

US20070021475A1 Substituted triazole derivatives 失效
标题翻译：取代的三唑衍生物
公开(公告)号：US20070021475A1
公开(公告)日：2007-01-25
申请号：US11488837
申请日：2006-07-18
申请人： Luca Gobbi , Marius Hoener , Claus Riemer , Will Spooren
发明人： Luca Gobbi , Marius Hoener , Claus Riemer , Will Spooren
IPC分类号： A61K31/4192 , C07D249/16 , C07D407/02
CPC分类号： C07D249/04 , C07D403/12
摘要： The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in the specification and to pharmaceutically suitable acid addition salts thereof. The invention includes all sterioisomeric forms, including individual diastereoisomers and enantiomers of the compound of formula (I) as well as racemic and non-racemic mixtures thereof. It has been found that the present compounds are selective allosteric positive modulators of the human NK-3 receptor for the treatment of anxiety, depression, bipolar disorders, Parkinson's disease, schizophrenia and pain.
摘要翻译：本发明涉及式（I）的化合物，其中R 1，R 2和R 3 3如说明书中所定义，并且与药学上其合适的酸加成盐。本发明包括所有的异构异构体形式，包括式（I）化合物的单独非对映异构体和对映异构体，以及其外消旋和非外消旋混合物。已经发现，本发明化合物是用于治疗焦虑，抑郁，双相情感障碍，帕金森病，精神分裂症和疼痛的人NK-3受体的选择性变构的阳性调节剂。

66. 发明授权

US07122545B2 Imidazo-benzothiazoles 失效
标题翻译：咪唑 - 苯并噻唑
公开(公告)号：US07122545B2
公开(公告)日：2006-10-17
申请号：US10843241
申请日：2004-05-11
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 , A61K31/55 , A61K31/428 , C07D413/02 , C07D487/04 , 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 wherein R1, R2, R3, R4, R5, R6, R7, R′, R″, X, R′″ and n are defined herein, or a pharmaceutically acceptable salt thereof. It has been found that the compound of formula I are adenosine receptor ligands with good affinity to the A1 and A3 receptors. These compounds have useful pharmaceutical activities.
摘要翻译：本发明涉及以下通式的2-咪唑并苯并噻唑：其中R 1，R 2，R 3，R 4， R 5，R“，R”，X“，R”'和n被定义，R“，R”，R“，R” 或其药学上可接受的盐。已经发现，式I化合物是对Aβ1和3 N 3受体具有良好亲和力的腺苷受体配体。这些化合物具有有用的药物活性。

67. 发明申请

US20050026906A1 Benzothiazole derivatives with actitvity as adenosine receptor ligands 审中-公开
标题翻译：具有活性的苯并噻唑衍生物作为腺苷受体配体
公开(公告)号：US20050026906A1
公开(公告)日：2005-02-03
申请号：US10930361
申请日：2004-08-30
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： 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 , A61K31/55 , C07D417/02
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 derivatives 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。

68. 发明授权

US06713499B2 7-Amino-benzothiazole derivatives 失效
标题翻译： 7-氨基 - 苯并噻唑衍生物
公开(公告)号：US06713499B2
公开(公告)日：2004-03-30
申请号：US10307702
申请日：2002-12-02
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： A61K31428
CPC分类号： C07D277/82 , C07D417/12 , C07D417/14 , C07D491/08
摘要： The present invention relates to compounds of the formula wherein R1, R2 and R3 are as described herewithin. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases, related to this receptor.
摘要翻译：本发明涉及式（Ⅳ）化合物，其中R 1，R 2和R 3如本文所述。已发现式I化合物是腺苷受体配体。具体地说，本发明化合物对A2A受体具有良好的亲和性，因此可用于治疗与该受体有关的疾病。

69. 发明授权

US5998665A Use of sulfonamides 失效
公开(公告)号：US5998665A
公开(公告)日：1999-12-07
申请号：US089706
申请日：1998-06-03
申请人： Michael Bos , Claus Riemer , Andrew Sleight
发明人： Michael Bos , Claus Riemer , Andrew Sleight
IPC分类号： A61K31/63 , A61K31/18 , A61K31/325 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/44 , A61K31/505 , A61P25/00 , C07C311/21 , C07C311/38 , C07C311/44 , C07D209/08 , C07D213/76 , C07D239/48 , C07D239/50 , C07D239/69 , C07D403/04
CPC分类号： C07D213/76 , C07C311/21 , C07C311/44 , C07D209/08 , C07D239/48 , C07D239/50 , C07D239/69 , C07D403/04
摘要： The present invention is concerned with compounds of formula I ##STR1## wherein Z, R.sup.1 and R.sup.2 are as defined herein, as well as their pharmaceutically acceptable salts as therapeutically active substances against central nervous system disorders and for the production of corresponding medicaments.

70. 发明授权

US5698565A Use of phenoxy-pyridine derivatives 失效
标题翻译：使用苯氧基 - 吡啶衍生物
公开(公告)号：US5698565A
公开(公告)日：1997-12-16
申请号：US639386
申请日：1996-04-29
申请人： Thierry Godel , Deborah Hartman , Claus Riemer
发明人： Thierry Godel , Deborah Hartman , Claus Riemer
IPC分类号： C07D211/70 , A61K31/44 , A61K31/4418
CPC分类号： A61K31/4418
摘要： A method of treating or preventing illnesses caused by a disorder of the dopamine system. The method comprises administering to a host requiring such treatment or prevention an effective amount of a pharmaceutical composition comprising a compound of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, halogen, lower-alkoxy or nitro; R.sub.2 is hydrogen, lower alkyl or trifluoromethyl; and R.sup.3 is hydrogen, lower alkyl, trifluoromethyl, benzyl, hydroxy-lower-alkyl, lower alkoxy, lower-alkyl-carbonyl-amino, carbonyl-lower-alkyl, benzyl, di-lower-alkyl-amino-carbonyl, carbonylamino or amino-carbonyl-amino; or R.sup.2 and R.sup.3 together optionally are a fused benzene ring and R.sup.4 is hydrogen or halogen, or a pharmaceutically acceptable salt of a compound of formula I, and a pharmaceutically inert carrier material.
摘要翻译：治疗或预防由多巴胺系统紊乱引起的疾病的方法。该方法包括向需要这种治疗或预防的宿主施用有效量的药物组合物，其包含下式化合物其中R 1是氢，低级烷基，卤素，低级烷氧基或硝基; R2是氢，低级烷基或三氟甲基; 低级烷基 - 氨基 - 羰基，羰基氨基或氨基，其中R 3为氢，低级烷基，三氟甲基，苄基，羟基 - 低级 - 烷基，低级烷氧基，低级 - - 羰基 - 氨基; 或R 2和R 3一起任选为稠合苯环，R 4为氢或卤素，或式I化合物的药学上可接受的盐和药学上惰性的载体材料。

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