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1. 发明申请

US20110201647A1 [4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-[7-FLUORO-1-(2-METHOXY-ETHYL)-4-TRIFLUOROMETHOXY-1H-INDOL-3-YL]-METHANONE AS AN INHIBITOR OF MAST CELL TRYPTASE 有权
标题翻译： - 哌啶-1-基] - [7-氟-2-（2-甲氧基 - 乙基）-4-三氟甲基-1H-吲哚-3-基] - [4-（5-氨基乙基-2-氟 - 苯基） - 哌啶-1-基] 甲烷作为细胞培养物的抑制剂
公开(公告)号：US20110201647A1
公开(公告)日：2011-08-18
申请号：US13028745
申请日：2011-02-16
申请人： Yong Mi CHOI-SLEDESKI , Nakyen CHOY , Gregory Bernard POLI , John J. SHAY, JR. , Patrick Wai-Kwok SHUM , Adam W. SLEDESKI
发明人： Yong Mi CHOI-SLEDESKI , Nakyen CHOY , Gregory Bernard POLI , John J. SHAY, JR. , Patrick Wai-Kwok SHUM , Adam W. SLEDESKI
IPC分类号： A61K31/454 , C07D401/06 , A61P29/00 , A61P27/02 , A61P17/02 , A61P17/00 , A61P31/12 , A61P1/00 , A61P35/00 , A61P1/16 , A61P11/06 , A61P11/00
CPC分类号： C07D401/06
摘要： The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及式I的吲哚苄胺化合物，其可用作类胰蛋白酶抑制剂。此外，本发明涉及该化合物用于治疗患有或受制于需要通过抑制类胰蛋白酶而改善的生理条件的患者，其包括向患者施用治疗有效量的化合物以及包含药学有效量的式I化合物和药学上可接受的载体的药物组合物。

2. 发明申请

US20120283445A1 [4-(5-AMINOMETHYL-2-FLUORO-PHENYL)-PIPERIDIN-1-YL]-[7-FLUORO-1-(2-METHOXY-ETHYL)-4-TRIFLUOROMETHOXY-1H-INDOL-3-YL]-METHANONE AS AN INHIBITOR OF MAST CELL TRYPTASE 有权
标题翻译： - 哌啶-1-基] - [7-氟-2-（2-甲氧基 - 乙基）-4-三氟甲基-1H-吲哚-3-基] - [4-（5-氨基乙基-2-氟 - 苯基） - 哌啶-1-基] 甲烷作为细胞培养物的抑制剂
公开(公告)号：US20120283445A1
公开(公告)日：2012-11-08
申请号：US13534580
申请日：2012-06-27
申请人： Yong Mi CHOI-SLEDESKI , Nakyen CHOY , Gregory Bernard POLI , John J. SHAY, JR. , Patrick Wai-Kwok SHUM , Adam W. SLEDESKI
发明人： Yong Mi CHOI-SLEDESKI , Nakyen CHOY , Gregory Bernard POLI , John J. SHAY, JR. , Patrick Wai-Kwok SHUM , Adam W. SLEDESKI
IPC分类号： C07D213/40 , C07D211/26 , C07D213/38
CPC分类号： C07D401/06
摘要： The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及式I的吲哚苄胺化合物，其可用作类胰蛋白酶抑制剂。此外，本发明涉及该化合物用于治疗患有或受制于需要通过抑制类胰蛋白酶而改善的生理条件的患者，其包括向患者施用治疗有效量的化合物以及包含药学有效量的式I化合物和药学上可接受的载体的药物组合物。

3. 发明授权

US08217178B2 [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-[7-flouro-1-(2-methoxy-ethyl)-4-trifluorom as an inhibitor of mast cell tryptase 有权
标题翻译： [4-（5-氨基甲基-2-氟 - 苯基） - 哌啶-1-基] - [7-氟-1-（2-甲氧基 - 乙基）-4-三氟甲磺隆作为肥大细胞类胰蛋白酶抑制剂
公开(公告)号：US08217178B2
公开(公告)日：2012-07-10
申请号：US13028745
申请日：2011-02-16
申请人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory Bernard Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
发明人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory Bernard Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
IPC分类号： C07D401/00 , A61K31/445
CPC分类号： C07D401/06
摘要： The present invention is directed to an indole benzylamine compound of formula I: useful as an inhibitor of tryptase. In addition, the present invention is directed to the use of the compound for treating a patient suffering from, or subject to, a physiological condition in need of amelioration by inhibition of tryptase, comprising administering to the patient of a therapeutically effective amount of the compound, and to a pharmaceutical composition comprising a pharmaceutically effective amount of the compound of formula I, and a pharmaceutically acceptable carrier.
摘要翻译：本发明涉及式I的吲哚苄胺化合物，其可用作类胰蛋白酶抑制剂。此外，本发明涉及该化合物用于治疗患有或受制于需要通过抑制类胰蛋白酶而改善的生理条件的患者，其包括向患者施用治疗有效量的化合物以及包含药学有效量的式I化合物和药学上可接受的载体的药物组合物。

4. 发明授权

US08497379B2 Method and intermediates for the preparation of 2,2,2-trifluoro-N-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride 有权
标题翻译：用于制备2,2,2-三氟-N-（4-氟-3-吡啶-4-基 - 苄基） - 乙酰胺盐酸盐的方法和中间体
公开(公告)号：US08497379B2
公开(公告)日：2013-07-30
申请号：US13534580
申请日：2012-06-27
申请人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory B. Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
发明人： Yong Mi Choi-Sledeski , Nakyen Choy , Gregory B. Poli , John J. Shay, Jr. , Patrick Wai-Kwok Shum , Adam W. Sledeski
IPC分类号： A61K31/44 , C07D401/00
CPC分类号： C07D401/06
摘要： The present invention is directed to a method for the preparation of 2,2,2-trifluoro-n-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride of the formula: and reaction intermediates used in the method.
摘要翻译：本发明涉及制备下式的2,2,2-三氟正（4-氟-3-吡啶-4-基 - 苄基） - 乙酰胺盐酸盐的方法：和方法。

5. 发明申请

US20120184745A1 SYNTHESIS OF (4-FLUORO-3-PIPERIDIN-4-YL-BENZYL)-CARBAMIC ACID TERT-BUTYL ESTER AND INTERMEDIATES THEREOF 有权
标题翻译：（4-氟-3-哌啶-4-基 - 苯甲酰基） - 氨基丁酸叔丁酯的合成及其中间体
公开(公告)号：US20120184745A1
公开(公告)日：2012-07-19
申请号：US13426721
申请日：2012-03-22
申请人： Nakyen CHOY , John J. SHAY, JR. , Adam W. SLEDESKI
发明人： Nakyen CHOY , John J. SHAY, JR. , Adam W. SLEDESKI
IPC分类号： C07D211/02 , C07D213/55 , C07F5/02
CPC分类号： C07D211/18 , C07D213/16 , C07F5/025
摘要： The present invention is an improved method for the preparation of 4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).
摘要翻译：本发明是制备式I化合物的4-氟-3-哌啶-4-基 - 苄基） - 氨基甲酸叔丁酯的改进方法。本发明涉及一种合成化合物的方法的式I化合物包括形成5 - （（叔丁氧基羰基）氨基甲基）-2-氟苯硼酸（化合物11），化合物11在Suzuki偶联条件下反应，得到（4-氟-2-吡啶-4-基 - 苄基） - 氨基甲酸叔丁酯，并在氢化条件下对上述产物进行选择性氢化，得到化合物I.本发明还涉及中间体5 - （（叔丁氧基羰基）氨基 - 甲基）-2-氟苯硼（化合物11）和（4-氟-2-吡啶-4-基 - 苄基） - 氨基甲酸叔丁酯（化合物13）。

6. 发明申请

US20100174088A1 PROCESS FOR THE PREPARATION OF BENZIMIDAZOL THIENYLAMINE COMPOUNDS AND DERIVATIVES THEREOF USEFUL AS SODIUM/PROTON EXCHANGER TYPE 3 INHIBITORS 审中-公开
标题翻译：制备苯并咪唑类三苯胺化合物的方法及其作为钠/原子交换剂类型3抑制剂有用的衍生物
公开(公告)号：US20100174088A1
公开(公告)日：2010-07-08
申请号：US12637096
申请日：2009-12-14
申请人： Timothy Allen Ayers , Nakyen Choy , Harpal S. Gill , Andrea Hillegass , John J. Shay, JR. , Volker Derdau
发明人： Timothy Allen Ayers , Nakyen Choy , Harpal S. Gill , Andrea Hillegass , John J. Shay, JR. , Volker Derdau
IPC分类号： C07D409/12 , C07D235/04 , C07D333/04
CPC分类号： C07D409/12 , C07D333/36
摘要： The present invention is an improved process for the preparation of a sodium/proton exchange inhibitor of sub-type 3 (NHE-3) useful in the treatment of sleep apnea and other related respiratory disorders. The improved synthesis of the NHE-3 inhibitor, more specifically a benzimidazol thienylamine, utilizes novel reagents and chemical intermediates and thereby results in an improved yield and purity of the final product with less reaction or synthetic steps required
摘要翻译：本发明是用于制备用于治疗睡眠呼吸暂停和其它相关呼吸障碍的亚型3型（NHE-3）的钠/质子交换抑制剂的改进方法。 NHE-3抑制剂，更特别是苯并咪唑噻吩胺的改进合成利用新型试剂和化学中间体，从而导致最终产物的产率和纯度提高，反应或合成步骤少

7. 发明授权

US08633321B2 Synthesis of (4-fluoro-3-piperidin-4-yl-benzyl)-carbamic acid tert-butyl ester and intermediates thereof 有权
标题翻译：（4-氟-3-哌啶-4-基 - 苄基） - 氨基甲酸叔丁酯的合成及其中间体
公开(公告)号：US08633321B2
公开(公告)日：2014-01-21
申请号：US13426721
申请日：2012-03-22
申请人： Nakyen Choy , John J. Shay, Jr. , Adam W. Sledeski
发明人： Nakyen Choy , John J. Shay, Jr. , Adam W. Sledeski
IPC分类号： C07D211/02
CPC分类号： C07D211/18 , C07D213/16 , C07F5/025
摘要： The present invention is an improved method for the preparation of (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester, compound of formula I. The invention is directed to a method of synthesis for the compound of formula I in three steps, comprising formation of 5-((tert-butoxycarbonyl)aminomethyl)-2-fluorobenzeneboronic acid (compound 11), reaction of compound 11 under Suzuki coupling conditions to yield (4-fluoro-2-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester and selective hydrogenation of the aforementioned product under hydrogenation conditions yields compound I. The invention is also directed to the intermediates 5-((tert-butoxycarbonyl)amino-methyl)-2-fluorobenzeneboronic acid (compound 11), and (4-fluoro-3-pyridin-4-yl-benzyl)-carbamic acid tert-butyl ester (compound 13).
摘要翻译：本发明是制备（4-氟-3-吡啶-4-基 - 苄基） - 氨基甲酸叔丁酯，式I化合物的改进方法。本发明涉及一种合成方法包括形成5 - （（叔丁氧基羰基）氨基甲基）-2-氟苯硼酸（化合物11），化合物11在Suzuki偶联条件下的反应，得到（4-氟-2-吡啶-2-基）苄基） - 氨基甲酸叔丁酯，并在氢化条件下对上述产物进行选择性氢化，得到化合物I.本发明还涉及中间体5 - （（叔丁氧基羰基）氨基 - 甲基）-2- 氟化硼酸（化合物11）和（4-氟-3-吡啶-4-基 - 苄基） - 氨基甲酸叔丁酯（化合物13）。

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