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1. 发明授权

US07229999B2 Pyridine-3-carboxamide derivatives as CB1 inverse agonists 有权
标题翻译：吡啶-3-甲酰胺衍生物作为CB1反向激动剂
公开(公告)号：US07229999B2
公开(公告)日：2007-06-12
申请号：US11397743
申请日：2006-04-04
申请人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst , Stephan Roever , Beat Wirz
发明人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst , Stephan Roever , Beat Wirz
IPC分类号： A61K31/44 , A51N43/54 , C07D213/22 , C07D213/56 , C07D401/00
CPC分类号： C07D213/64 , C07D213/74 , C07D213/82 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of the formula wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译：本发明涉及下式的化合物，其中X和R 1至R 8如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体如肥胖相关的疾病。

2. 发明申请

US20070293509A1 Pyrazinecarboxamide derivatives as CB1 antagonists 失效
标题翻译：吡嗪甲酰胺衍生物作为CB1拮抗剂
公开(公告)号：US20070293509A1
公开(公告)日：2007-12-20
申请号：US11809047
申请日：2007-05-30
申请人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
发明人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
IPC分类号： A61K31/497 , A61K31/4965 , A61P1/00 , A61P3/04 , A61P3/10 , C07D241/10 , C07D419/02
CPC分类号： C07D241/26 , C07D241/24 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译：本发明涉及式I化合物：其中R 1至R 8如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体如肥胖相关的疾病。

3. 发明授权

US07629346B2 Pyrazinecarboxamide derivatives as CB1 antagonists 失效
标题翻译：吡嗪甲酰胺衍生物作为CB1拮抗剂
公开(公告)号：US07629346B2
公开(公告)日：2009-12-08
申请号：US11809047
申请日：2007-05-30
申请人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
发明人： Paul Hebeisen , Hans Iding , Matthias Heinrich Nettekoven , Ulrike Obst Sander , Stephan Roever , Urs Weiss , Beat Wirz
IPC分类号： A61K31/4965 , A61K31/497
CPC分类号： C07D241/26 , C07D241/24 , C07D401/12 , C07D403/12 , C07D405/12
摘要： The present invention relates to compounds of the formula I: wherein R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译：本发明涉及式I化合物：其中R 1至R 8如说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体如肥胖相关的疾病。

4. 发明申请

US20060229326A1 Pyridine-3-carboxamide derivatives as CB1 inverse agonists 有权
标题翻译：吡啶-3-甲酰胺衍生物作为CB1反向激动剂
公开(公告)号：US20060229326A1
公开(公告)日：2006-10-12
申请号：US11397743
申请日：2006-04-04
申请人： Paul Hebeisen , Hans Iding , Matthias Nettekoven , Ulrike Obst , Stephan Roever , Beat Wirz
发明人： Paul Hebeisen , Hans Iding , Matthias Nettekoven , Ulrike Obst , Stephan Roever , Beat Wirz
IPC分类号： A61K31/513 , A61K31/444 , A61K31/4439 , A61K31/4412 , A61K31/44 , C07D403/02 , C07D213/62
CPC分类号： C07D213/64 , C07D213/74 , C07D213/82 , C07D401/12 , C07D413/12 , C07D417/12
摘要： The present invention relates to compounds of the formula wherein X and R1 to R8 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors, such as obesity.
摘要翻译：本发明涉及下式的化合物，其中X和R 1至R 8如在说明书和权利要求书中所定义，及其药学上可接受的盐。该化合物可用于治疗和/或预防与调节CB1受体如肥胖相关的疾病。

5. 发明授权

US07037935B2 4-Pyrrolidino-phenyl-benzyl ether derivatives 失效
标题翻译： 4-吡咯烷基 - 苯基 - 苄基醚衍生物
公开(公告)号：US07037935B2
公开(公告)日：2006-05-02
申请号：US10667088
申请日：2003-09-18
申请人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
发明人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/402 , C07D209/34
CPC分类号： C07D207/273 , C07D207/277
摘要： The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.
摘要翻译：本发明涉及外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途，特别是其由单胺氧化酶B抑制剂介导的，特别是阿尔茨海默氏病或老年痴呆症。

6. 发明申请

US20050065204A1 Process for the preparation of enantiopure pyrrolidin-2-one derivatives 失效
标题翻译：制备对映体积吡咯烷-2-酮衍生物的方法
公开(公告)号：US20050065204A1
公开(公告)日：2005-03-24
申请号：US10940155
申请日：2004-09-14
申请人： Hans Iding , Daniela Krummenacher , Beat Wirz , Wolfgang Wostl
发明人： Hans Iding , Daniela Krummenacher , Beat Wirz , Wolfgang Wostl
IPC分类号： C07D207/26 , C07D207/277 , C12P17/10 , C12P41/00 , C12P13/24 , A61K31/4015
CPC分类号： C07D207/26 , C07D207/277 , C12P17/10 , C12P41/005
摘要： The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II wherein R21, R22, R23 and R24 are as defined in the description and claims.
摘要翻译：本发明涉及制备可用于合成有价值的药物活性化合物的对映体纯中间体的方法，例如， MAOB抑制剂和式I和II的新型中间体，其中R 21，R 22，R 23和R 24如说明书和权利要求中所定义。

7. 发明授权

US07642366B2 Phosphine ligands 失效
标题翻译：膦配体
公开(公告)号：US07642366B2
公开(公告)日：2010-01-05
申请号：US11591277
申请日：2006-11-01
申请人： Hans Iding , Ernst Kupfer , Bruno Lohri , Kazimierz Michal Pietrusiewicz , Kurt Puentener , Michelangelo Scalone , Wioleta Swierczynska , Beat Wirz
发明人： Hans Iding , Ernst Kupfer , Bruno Lohri , Kazimierz Michal Pietrusiewicz , Kurt Puentener , Michelangelo Scalone , Wioleta Swierczynska , Beat Wirz
IPC分类号： C07F15/04
CPC分类号： C07F15/006 , C07B53/00 , C07F9/65683 , C07F15/0066
摘要： The invention is concerned with new phosphine ligands of the formula I wherein R1 and R2 are independently of each other alkyl, aryl, cycloalkyl or heteroaryl, said alkyl, aryl, cycloalkyl or heteroaryl may be substituted by alkyl, alkoxy, halogen, hydroxy, amino, mono- or dialkylamino, aryl, —SO2—R7, —SO3−, —CO—NR8R8′, carboxy, alkoxycarbonyl, trialkylsilyl, diarylalkylsilyl, dialkylarylsilyl or triarylsilyl; R3 is alkyl, cycloalkyl, aryl or heteroaryl; R4′ and R4 signify independently of each other hydrogen, alkyl or optionally substituted aryl; or R4′ and R4 together with the C-atom they are attached to form a 3-8-membered carbocyclic ring; dotted line is absent or is present and forms a double bond; R5 and R6 are independently of each other hydrogen, alkyl or aryl; or linked together to form a 3-8-membered carbocyclic ring or an aromatic ring; R7 is alkyl, aryl or NR8R8′; and R8 and R8′ are independently of each other hydrogen, alkyl or aryl; metal complexes with such ligands as well as the use of such metal complexes as catalysts in asymmetric reactions.
摘要翻译：本发明涉及式I的新膦配体，其中R 1和R 2彼此独立地为烷基，芳基，环烷基或杂芳基，所述烷基，芳基，环烷基或杂芳基可以被烷基，烷氧基，卤素，羟基，氨基，一或二烷基氨基，芳基，-SO 2 -R 7，-SO 3 - ，-CO-NR 8 R 8'，羧基，烷氧基羰基，三烷基甲硅烷基，二芳基烷基甲硅烷基，二烷基芳基甲硅烷基或三芳基甲硅烷基; R3是烷基，环烷基，芳基或杂芳基; R4'和R4独立地表示氢，烷基或任选取代的芳基; 或R 4'和R 4与它们所连接的C原子一起形成3-8-元碳环; 虚线不存在或存在并形成双键; R5和R6彼此独立地为氢，烷基或芳基; 或连接在一起形成3-8元碳环或芳环; R7是烷基，芳基或NR8R8'; R8和R8'彼此独立地为氢，烷基或芳基; 与这种配体的金属络合物以及在不对称反应中使用这样的金属络合物作为催化剂。

8. 发明授权

US07122562B2 4-pyrrolidino-phenyl-benzyl ether derivatives 失效
标题翻译： 4-吡咯烷基 - 苯基 - 苄基醚衍生物
公开(公告)号：US07122562B2
公开(公告)日：2006-10-17
申请号：US11325747
申请日：2006-01-05
申请人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
发明人： Hans Iding , Synese Jolidon , Daniela Krummenacher , Rosa Maria Rodriguez-Sarmiento , Andrew William Thomas , Beat Wirz , Wolfgang Wostl , Rene Wyler
IPC分类号： A61K31/4439 , C07D401/04
CPC分类号： C07D207/273 , C07D207/277
摘要： The invention relates to racemic or enantiomerically pure 4-pyrrolidino derivatives, processes for their preparation, pharmaceutical compositions comprising said derivatives, and their use in the prevention and treatment of illness, in particular which is mediated by monoamine oxidase B inhibitors, in particular Alzheimer's disease or senile dementia.
摘要翻译：本发明涉及外消旋或对映体纯的4-吡咯烷子基衍生物，其制备方法，包含所述衍生物的药物组合物及其在预防和治疗疾病中的用途，特别是其由单胺氧化酶B抑制剂介导的，特别是阿尔茨海默氏病或老年痴呆症。

9. 发明授权

US07011960B2 Substituted 2-amino-3-(2-amino-phenylsulfanyl)-propionic acids 有权
标题翻译：取代的2-氨基-3-（2-氨基 - 苯硫基） - 丙酸
公开(公告)号：US07011960B2
公开(公告)日：2006-03-14
申请号：US10252971
申请日：2002-09-23
申请人： Konrad Bleicher , Scott Borthwick , Hans Iding , Mark Rogers-Evans , Stefan Schmid , Han Min Tong , Beat Wirz
发明人： Konrad Bleicher , Scott Borthwick , Hans Iding , Mark Rogers-Evans , Stefan Schmid , Han Min Tong , Beat Wirz
IPC分类号： C12P13/04 , A61K38/17 , A01N43/10 , C07D291/06 , C07C323/02
CPC分类号： C12P13/04 , C07C323/59 , C07C323/63 , C07D285/36 , C12P11/00 , C12P41/005
摘要： The present invention relates to a new process for the preparation compounds of formula I wherein R1, R2, R3 and n are as described in the description which process comprises reacting compounds of formula II wherein R1, R2, R3, n and R4 are as described in the description, with a protease in an aqueous system containing an organic co-solvent. The compound of formula I are useful for the preparation of 1,5-benzothiazepines which are useful as enzyme inhibitors, such as protease, interleukin-1β-converting enzyme, elastase or angiotensin converting enzyme, GPCR antagonists (cholecystokinin, angiotensin II receptor).
摘要翻译：本发明涉及制备式I化合物的新方法，其中R 1，R 2，R 3和n如上所述在描述中，该方法包括使式II化合物其中R 1，R 2，R 3，R 3，R 4和R 4， / SUP>如描述中所述，在含有有机共溶剂的水性体系中具有蛋白酶。式I化合物可用于制备可用作酶抑制剂的1,5-苯并硫氮杂，如蛋白酶，白细胞介素-1β转换酶，弹性蛋白酶或血管紧张素转换酶，GPCR拮抗剂（缩胆囊素，血管紧张素II受体）。

10. 发明申请

US20110054174A1 PROCESS FOR THE PREPARATION OF A GLUCOKINASE ACTIVATOR COMPOUND 审中-公开
标题翻译：制备GLUCOKINASE激活剂化合物的方法
公开(公告)号：US20110054174A1
公开(公告)日：2011-03-03
申请号：US12859795
申请日：2010-08-20
申请人： Stephan Bachmann , Alec Fettes , Hans Iding , Beat Wirz , Ulrich Zutter
发明人： Stephan Bachmann , Alec Fettes , Hans Iding , Beat Wirz , Ulrich Zutter
IPC分类号： C07D241/20 , C07C233/01 , C12P17/12
CPC分类号： C07D241/20 , C07C259/06
摘要： The present invention relates to a process for the preparation of a compound of formula I, wherein R1 is C1-6-alkyl and R2 is hydrogen or halogen.(R)-2-phenyl propionic acid derivatives of formula I are key intermediates in the synthesis of 5-substituted-pyrazine or pyridine glucokinase activators of the formula Xa, which have the potential to be useful for the treatment and/or prophylaxis of type II diabetes.
摘要翻译：本发明涉及制备式I化合物的方法，其中R 1为C 1-6 - 烷基且R 2为氢或卤素。式I的（R）-2-苯基丙酸衍生物是合成式Xa的5-取代 - 吡嗪或吡啶葡萄糖激酶活化剂的关键中间体，其具有可用于治疗和/或预防类型 II型糖尿病

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