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21. 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。

22. 发明授权

US08008503B2 Methyl-benzimidazole derivatives 失效
标题翻译：甲基 - 苯并咪唑衍生物
公开(公告)号：US08008503B2
公开(公告)日：2011-08-30
申请号：US12862823
申请日：2010-08-25
申请人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Rainer E Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
发明人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Rainer E Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
IPC分类号： A61K31/4184 , C07D235/06
CPC分类号： C07D235/06 , C07D405/12 , C07D409/12
摘要： The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型取代的苯并咪唑衍生物，其中R 1至R 10如说明书和权利要求书中所定义，以及其生理学上可接受的盐和酯。这些化合物可以用作药物。

23. 发明申请

US20100331371A1 METHYL-BENZIMIDAZOLE DERIVATIVES 失效
标题翻译：甲基苯并咪唑衍生物
公开(公告)号：US20100331371A1
公开(公告)日：2010-12-30
申请号：US12862823
申请日：2010-08-25
申请人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
发明人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
IPC分类号： A61K31/4439 , C07D235/04 , A61K31/4184 , C07D401/02 , A61P3/10 , A61P3/06
CPC分类号： C07D235/06 , C07D405/12 , C07D409/12
摘要： The invention is concerned with novel substituted benzimidazole derivatives of formula (I) wherein R1 to R10 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型取代的苯并咪唑衍生物，其中R 1至R 10如说明书和权利要求书中所定义，以及其生理学上可接受的盐和酯。这些化合物可以用作药物。

24. 发明申请

US20090163552A1 CARBOXYL- OR HYDROXYL-SUBSTITUTED BENZIMIDAZOLE DERIVATIVES 有权
标题翻译：羧甲基或羟基取代的苯并咪唑衍生物
公开(公告)号：US20090163552A1
公开(公告)日：2009-06-25
申请号：US12331461
申请日：2008-12-10
申请人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
发明人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor , Minmin Yang
IPC分类号： A61K31/4184 , C07D401/12 , C07D401/14 , A61P9/00 , A61P25/28 , A61P35/00 , C07D235/16 , A61K31/4439
CPC分类号： C07D401/04 , C07D235/12 , C07D401/12 , C07D401/14
摘要： This invention relates to novel carboxyl- or hydroxyl-substituted benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to FXR and can be used as medicaments.
摘要翻译：本发明涉及式（I）的新型羧基或羟基取代的苯并咪唑衍生物，其中R 1至R 6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。这些化合物与FXR结合，可用作药物。

25. 发明授权

US07384945B2 Indole or benzimidazole derivatives as CB1 inverse agonists 失效
标题翻译：吲哚或苯并咪唑衍生物作为CB1反向激动剂
公开(公告)号：US07384945B2
公开(公告)日：2008-06-10
申请号：US11257885
申请日：2005-10-25
申请人： Konrad Bleicher , Matthias Heinrich Nettekoven , Philippe Pflieger , Stephan Roever
发明人： Konrad Bleicher , Matthias Heinrich Nettekoven , Philippe Pflieger , Stephan Roever
IPC分类号： A61K31/497 , A61K31/40 , A01N43/38 , C07D401/00 , C07D211/78 , C07D211/90 , C07D213/81 , C07D209/42 , C07D403/00
CPC分类号： C07D235/12 , C07D209/12 , C07D401/06
摘要： Provided are compounds of the formula I: and pharmaceutically acceptable salts thereof, processes for making said compounds and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising said compound and pharmaceutically acceptable salts thereof, and methods of using said compounds. 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：提供式I化合物及其药学上可接受的盐，制备所述化合物及其药学上可接受的盐的方法，包含所述化合物的药物组合物及其药学上可接受的盐以及使用所述化合物的方法。该化合物可用于治疗和/或预防与调节CB1受体相关的疾病。

26. 发明申请

US20050143373A1 Benzodioxole derivatives 失效
标题翻译：苯并二恶醇衍生物
公开(公告)号：US20050143373A1
公开(公告)日：2005-06-30
申请号：US11062973
申请日：2005-02-22
申请人： Alexander Alanine , Konrad Bleicher , Wolfgang Guba , Wolfgang Haap , Dagmar Kube , Thomas Luebbers , Jean-Marc Plancher , Olivier Roche , Mark Rogers-Evans , Gisbert Schneider , Jochen Zuegge
发明人： Alexander Alanine , Konrad Bleicher , Wolfgang Guba , Wolfgang Haap , Dagmar Kube , Thomas Luebbers , Jean-Marc Plancher , Olivier Roche , Mark Rogers-Evans , Gisbert Schneider , Jochen Zuegge
IPC分类号： A61K31/36 , C07D317/46 , C07D317/54 , C07D317/62 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10 , A61K31/551 , A61K31/4025 , A61K31/452 , A61K31/496 , A61K31/5377 , C07D47/02
CPC分类号： C07D317/46 , C07D317/72 , C07D405/06 , C07D405/12 , C07D405/14 , C07D407/12 , C07D417/06 , C07D451/06 , C07D491/10
摘要： The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.
摘要翻译：本发明涉及通式的化合物及其药学上可接受的盐。该化合物可用于通过选择性调节CB1受体来治疗和/或预防诸如肥胖症的疾病。

27. 发明授权

US06462198B1 Carbamic acid derivatives 失效
公开(公告)号：US06462198B1
公开(公告)日：2002-10-08
申请号：US09545622
申请日：2000-04-10
申请人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
发明人： Konrad Bleicher , Vincent Mutel , Eric Vieira , Jürgen Wichmann , Thomas Johannes Woltering
IPC分类号： C07D41312
CPC分类号： C07D213/30 , C07C233/91 , C07C271/64 , C07C333/10 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D213/61 , C07D263/48 , C07D271/07 , C07D271/113 , C07D295/088 , C07D311/84 , C07D333/16 , C07D335/14 , C07D413/12
摘要： The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulas wherein R4 and R5 signifies hydrogen, lower alkyl, lower alkoxy, cyclohexyl, lower alkyl-cyclohexyl or trifluoromethyl, with the proviso that at least one of R4 or R5 has to be hydrogen; as well as to their pharmaceutically acceptable salts. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.

28. 发明授权

US08143422B2 Benzimidazole derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US08143422B2
公开(公告)日：2012-03-27
申请号：US12577765
申请日：2009-10-13
申请人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor
发明人： Gregory Martin Benson , Konrad Bleicher , Song Feng , Uwe Grether , Bernd Kuhn , Rainer E. Martin , Jean-Marc Plancher , Hans Richter , Sven Taylor
IPC分类号： A61K31/4184 , A61K31/4439 , C07D235/06 , C07D403/12
CPC分类号： C07D235/18
摘要： The invention is concerned with novel benzimidazole derivatives of formula (I) wherein R1 to R6 are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds can be used as medicaments.
摘要翻译：本发明涉及式（I）的新的苯并咪唑衍生物，其中R 1至R 6如在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。这些化合物可用作药物。

29. 发明授权

US08008505B2 Indazole or 4,5,6,7-tetrahydro-indazole derivatives 有权
标题翻译：吲唑或4,5,6,7-四氢 - 吲唑衍生物
公开(公告)号：US08008505B2
公开(公告)日：2011-08-30
申请号：US12563193
申请日：2009-09-21
申请人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Bernd Kuhn , Hans Richter , Sven Taylor
发明人： Gregory Martin Benson , Konrad Bleicher , Uwe Grether , Bernd Kuhn , Hans Richter , Sven Taylor
IPC分类号： C07D487/00 , C07D403/06 , C07D401/06 , A61K31/415 , A61K31/44
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12
摘要： This invention relates to novel indazole or 4,5,6,7-tetrahydro-indazole derivatives of formula I wherein R1 to R8 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are FXR modulators and can be used as medicaments.
摘要翻译：本发明涉及式I的新的吲唑或4,5,6,7-四氢 - 吲唑衍生物，其中R 1至R 8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。这些化合物是FXR调节剂，可用作药物。

30. 发明申请

US20110183979A1 NITROGEN-CONTAINING HETEROARYL DERIVATIVES 有权
标题翻译：含氮含量衍生物
公开(公告)号：US20110183979A1
公开(公告)日：2011-07-28
申请号：US13005572
申请日：2011-01-13
申请人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Eric Vieira
发明人： Konrad Bleicher , Alexander Flohr , Katrin Groebke Zbinden , Matthias Koerner , Bernd Kuhn , Jens-Uwe Peters , Rosa Maria Rodriguez-Sarmiento , Eric Vieira
IPC分类号： A61K31/506 , C07D401/14 , C07D413/14 , A61K31/5377 , A61K31/497 , A61P25/18 , A61P25/22 , A61P25/00 , A61P25/16 , A61P25/28 , A61P25/24 , A61P7/00 , A61P35/00 , A61P3/10
CPC分类号： C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The invention is concerned with novel nitrogen-containing heteroaryl derivatives of formula (I) wherein R1, R2, R3, R4, R5, A1, A2, and Y 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 medicaments.
摘要翻译：本发明涉及式（I）的新型含氮杂芳基衍生物，其中R1，R2，R3，R4，R5，A1，A2和Y如说明书和权利要求书中所定义，以及生理上可接受的盐及其酯。这些化合物抑制PDE10A，并可用作药物。

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