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1. 发明申请

US20100094011A1 DIAZONIUM-FREE METHOD TO MAKE AN INDAZOLE INTERMEDIATE IN THE SYNTHESIS OF BICYCLIC 5-(TRIFLUORMETHOXY)-1H-3-INDAZOLECARBOXYLIC ACID AMIDES 有权
标题翻译：在双酚-5-（三氟甲基）-1H-3-异吲哚酸酰胺的合成中制备吲哚中间体的无氮方法
公开(公告)号：US20100094011A1
公开(公告)日：2010-04-15
申请号：US12576259
申请日：2009-10-09
申请人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
发明人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
IPC分类号： C07D221/22 , C07D231/56
CPC分类号： C07D453/02 , C07D231/56
摘要： The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
摘要翻译：本发明提供了制备5-（三氟甲氧基）-1H-3-吲哚羧酸（3）的新方法，其是制备式（I）的双环-5-三氟甲氧基-1H-吲唑-3-羧酸酰胺的有用前体（1）。式（1）的化合物作为烟酸α-7受体的激动剂和部分激动剂是有活性的，并且正在研究用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体（特别是脑）有关的疾病状况，例如治疗阿尔茨海默病和精神分裂症，以及其他精神和神经障碍。本发明的方法可用于按比例制备化合物（3）。

2. 发明授权

US08232412B2 Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides 有权
标题翻译：在双环5-（三氟甲氧基）-1H-3-吲哚羧酸酰胺的合成中制备吲唑中间体的无重氮方法
公开(公告)号：US08232412B2
公开(公告)日：2012-07-31
申请号：US12576259
申请日：2009-10-09
申请人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
发明人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
IPC分类号： C07D231/56 , C07D231/54
CPC分类号： C07D453/02 , C07D231/56
摘要： The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
摘要翻译：本发明提供了制备5-（三氟甲氧基）-1H-3-吲哚羧酸（3）的新方法，其是制备式（I）的双环-5-三氟甲氧基-1H-吲唑-3-羧酸酰胺的有用前体（1）。式（1）的化合物作为烟酸α-7受体的激动剂和部分激动剂是有活性的，并且正在研究用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体（特别是脑）有关的疾病状况，例如治疗阿尔茨海默病和精神分裂症，以及其他精神和神经障碍。本发明的方法可用于按比例制备化合物（3）。

3. 发明申请

US20080312467A1 NOVEL PROCESS FOR THE PREPARATION OF 3-AMINO-PENTAN-1,5-DIOL 失效
标题翻译：制备3-氨基 - 戊烷-1,5-二醇的新方法
公开(公告)号：US20080312467A1
公开(公告)日：2008-12-18
申请号：US12135240
申请日：2008-06-09
申请人： Thomas Cleary , Yaohui Ji , Gary R. Lee , Thimma Rawalpally , Keshab Sarma
发明人： Thomas Cleary , Yaohui Ji , Gary R. Lee , Thimma Rawalpally , Keshab Sarma
IPC分类号： C07C271/16 , C07C271/22 , C07C209/44
CPC分类号： C07C269/04 , C07C213/08 , C07C213/10 , C07C215/10 , C07C227/08 , C07C227/16 , C07C269/06 , C07C271/16 , C07C271/22 , C07C229/24 , C07C229/30
摘要： The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.
摘要翻译：本发明提供了一种制备关键中间体3-氨基 - 戊-1,5-二醇（2）的新方法，其可用于制备6-（2,4-二氟苯氧基）-2- [3- 羟基-1-（2-羟乙基） - 丙基氨基] -8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮（1）可用于治疗类风湿性关节炎的MAP-激酶抑制剂。

4. 发明授权

US07635784B2 Process for the preparation of 3-amino-pentan-1,5-diol 失效
标题翻译： 3-氨基 - 戊-1,5-二醇的制备方法
公开(公告)号：US07635784B2
公开(公告)日：2009-12-22
申请号：US12135240
申请日：2008-06-09
申请人： Thomas Cleary , Yaohui Ji , Gary R. Lee , Thimma Rawalpally , Keshab Sarma
发明人： Thomas Cleary , Yaohui Ji , Gary R. Lee , Thimma Rawalpally , Keshab Sarma
IPC分类号： C07C269/00
CPC分类号： C07C269/04 , C07C213/08 , C07C213/10 , C07C215/10 , C07C227/08 , C07C227/16 , C07C269/06 , C07C271/16 , C07C271/22 , C07C229/24 , C07C229/30
摘要： The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.
摘要翻译：本发明提供一种制备关键中间体3-氨基 - 戊-1,5-二醇（2）的新方法，其可用于制备6-（2,4-二氟苯氧基）-2- [3- 羟基-1-（2-羟乙基） - 丙基氨基] -8-甲基-8H-吡啶并[2,3-d]嘧啶-7-酮（1）可用于治疗类风湿性关节炎的MAP-激酶抑制剂。

5. 发明授权

US08354536B2 Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides 有权
标题翻译：在双环5-（三氟甲氧基）-1H-3-吲哚羧酸酰胺的合成中制备吲唑中间体的无重氮方法
公开(公告)号：US08354536B2
公开(公告)日：2013-01-15
申请号：US13528894
申请日：2012-06-21
申请人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
发明人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
IPC分类号： C07D453/02 , C07D241/38
CPC分类号： C07D453/02 , C07D231/56
摘要： The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
摘要翻译：本发明提供了制备5-（三氟甲氧基）-1H-3-吲哚羧酸（3）的新方法，其是制备式（I）的双环-5-三氟甲氧基-1H-吲唑-3-羧酸酰胺的有用前体（1）。式（1）的化合物作为烟酸α-7受体的激动剂和部分激动剂是有活性的，并且正在研究用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体（特别是脑）有关的疾病状况，例如治疗阿尔茨海默病和精神分裂症，以及其他精神和神经障碍。本发明的方法可用于按比例制备化合物（3）。

6. 发明申请

US20120259120A1 DIAZONIUM-FREE METHOD TO MAKE AN INDAZOLE INTERMEDIATE IN THE SYNTHESIS OF BICYCLIC 5-(TRIFLUORMETHOXY)-1H-3-INDAZOLECARBOXYLIC ACID AMIDES 有权
标题翻译：在双酚-5-（三氟甲基）-1H-3-异吲哚酸酰胺的合成中制备吲哚中间体的无氮方法
公开(公告)号：US20120259120A1
公开(公告)日：2012-10-11
申请号：US13528894
申请日：2012-06-21
申请人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
发明人： Thomas Cleary , Yaohui Ji , Thimma Rawalpally
IPC分类号： C07D231/56 , C07D453/02
CPC分类号： C07D453/02 , C07D231/56
摘要： The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic α-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.
摘要翻译：本发明提供了制备5-（三氟甲氧基）-1H-3-吲哚羧酸（3）的新方法，其是制备式（I）的双环-5-三氟甲氧基-1H-吲唑-3-羧酸酰胺的有用前体（1）。式（1）的化合物作为烟酸α-7受体的激动剂和部分激动剂是有活性的，并且正在研究用于治疗与缺陷或功能异常的烟碱乙酰胆碱受体（特别是脑）有关的疾病状况，例如治疗阿尔茨海默病和精神分裂症，以及其他精神和神经障碍。本发明的方法可用于按比例制备化合物（3）。

7. 发明授权

US08063076B2 Solid forms of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine 有权
标题翻译：固体形式的2-氯-4- [1-（4-氟 - 苯基）-2,5-二甲基-1H-咪唑-4-基乙炔基] - 吡啶
公开(公告)号：US08063076B2
公开(公告)日：2011-11-22
申请号：US11957515
申请日：2007-12-17
申请人： Thomas Cleary , Alexander Glomme , Olaf Grassmann , Shan-Ming Kuang , Roland Meier , Doreen Miller , Regina Moog , Franziska E. Rohrer , Jason Yang
发明人： Thomas Cleary , Alexander Glomme , Olaf Grassmann , Shan-Ming Kuang , Roland Meier , Doreen Miller , Regina Moog , Franziska E. Rohrer , Jason Yang
IPC分类号： A61K31/4439 , C07D401/06
CPC分类号： C07D401/06
摘要： The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.
摘要翻译：本发明涉及单硫酸盐，单硫酸盐的结晶形式A和B，单硫酸盐的无定形形式，半硫酸盐和结晶形式A的半硫酸盐化合物2-氯-4- [1-（4-氟 - 苯基）-2,5-二甲基-1H-咪唑-4-基乙炔基] - 吡啶。

8. 发明申请

US20120165526A1 Useful Pharmaceutical Salts of 7- [(3R, 4R) - 3 - Hydroxy -4 - Hydroxymethyl - Pyrrolidin -1- Ylmethyl] -3, 5-Dihydro-Pyrrolo [3, 2-D] Pyrimidin -4-One 有权
标题翻译： 7 - [（3R，4R）-3-羟基-4-羟甲基 - 吡咯烷-1-基甲基] -3,5-二氢 - 吡咯并[3,2-D]嘧啶-4-酮的有用药物盐
公开(公告)号：US20120165526A1
公开(公告)日：2012-06-28
申请号：US13258497
申请日：2010-03-24
申请人： Gary Bartley , Thomas Cleary , John Lang
发明人： Gary Bartley , Thomas Cleary , John Lang
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present disclosure provides novel hemi- and mono-salts of 7-[(3R,4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2-d]pyrimidin-4-one (Compound 1) with various organic and inorganic acids. In one embodiment, the organic acid is a C4 organic diacids. The present disclosure further provides novel methods for preparing these salts. The novel monohydrates hemisalts of the C4 organic diacids are isostructural and can be prepared with different properties. Multiple acids can be used simultaneously and the proportion of acids can be varied offering the opportunity to select hemi-salts of compound 1 with desired properties.
摘要翻译：本公开提供了7 - [（3R，4R）-3-羟基-4-羟甲基 - 吡咯烷-1-基甲基] -3,5-二氢 - 吡咯并[3,2-d]的新型半 - 和单 - 盐，嘧啶-4-酮（化合物1）与各种有机和无机酸反应。在一个实施方案中，有机酸是C4有机二酸。本公开进一步提供了制备这些盐的新方法。 C4有机二酸的新型一水合物半盐是同构的，可以用不同的性质制备。可以同时使用多种酸，并且可以改变酸的比例，这提供了选择具有所需性质的化合物1的半盐的机会。

9. 发明申请

US20080312288A1 SOLID FORMS OF 2-CHLORO-4-[1-(4-FLUORO-PHENYL)-2,5-DIMETHYL-1H-IMIDAZOL-4-YLETHYNYL]-PYRIDINE 有权
标题翻译： 2-氯-4- [1-（4-氟 - 苯基）-2,5-二甲基-1H-咪唑-4-基]乙基] - 吡啶的固体形式
公开(公告)号：US20080312288A1
公开(公告)日：2008-12-18
申请号：US11957515
申请日：2007-12-17
申请人： Thomas Cleary , Alexander Glomme , Olaf Grassmann , Shan-Ming Kuang , Roland Meier , Doreen Miller , Regina Moog , Franziska E. Rohrer , Jason Yang
发明人： Thomas Cleary , Alexander Glomme , Olaf Grassmann , Shan-Ming Kuang , Roland Meier , Doreen Miller , Regina Moog , Franziska E. Rohrer , Jason Yang
IPC分类号： A61K31/4439 , C07D401/04 , A61P43/00
CPC分类号： C07D401/06
摘要： The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.
摘要翻译：本发明涉及单硫酸盐，单硫酸盐的结晶形式A和B，单硫酸盐的无定形形式，半硫酸盐和结晶形式A的半硫酸盐化合物2-氯-4- [1-（4-氟 - 苯基）-2,5-二甲基-1H-咪唑-4-基乙炔基] - 吡啶。

10. 发明申请

US20050073172A1 SLIDER WINDOW ASSEMBLY 失效
标题翻译：滑动窗户装配
公开(公告)号：US20050073172A1
公开(公告)日：2005-04-07
申请号：US10678700
申请日：2003-10-03
申请人： Rick Weinert , Thomas Cleary , Paul Kolokowski , Michael Lesle
发明人： Rick Weinert , Thomas Cleary , Paul Kolokowski , Michael Lesle
IPC分类号： B60J1/18 , B60J1/00
CPC分类号： B60J1/1853
摘要： A slider window assembly for an automotive vehicle comprises a fixed glass panel adapted to be installed in a window frame defined by a body panel. The fixed glass panel is bonded to the window frame by an adhesive bead and defines an opening. A sliding window opens and closes the opening and includes an edge that is received in a guide rail that is adhesively bonded to the fixed glass panel. The guide rail defines a channel for the edge of the sliding window and also includes an extension that is bonded to the window frame by the adhesive bead. In this manner, the guide rail continues to support the sliding window in the event that the fixed glass panel is unable to provide the primary support function.
摘要翻译：用于机动车辆的滑动窗组件包括适于安装在由车身面板限定的窗框中的固定玻璃面板。固定的玻璃面板通过粘合剂珠粘合到窗框上并且限定开口。滑动窗口打开和关闭开口，并且包括容纳在导轨中的边缘，该导轨粘合到固定玻璃面板上。导轨限定了用于滑动窗口边缘的通道，并且还包括通过粘合剂珠结合到窗框的延伸部。以这种方式，在固定玻璃面板不能提供主要支撑功能的情况下，导轨继续支撑滑动窗口。

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