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1. 发明申请

WO2012058134A1 INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL 审中-公开
标题翻译：肾脏外部药物通道的抑制剂
公开(公告)号：WO2012058134A1
公开(公告)日：2012-05-03
申请号：PCT/US2011/057421
申请日：2011-10-24
申请人： MERCK SHARP & DOHME CORP. , PASTERNAK, Alexander , DEJESUS, Reynalda, K. , ZHU, Yuping , YANG, Lihu , WALSH, Shawn , PIO, Barbara , SHAHRIPOUR, Aurash , TANG, Haifeng , BELYK, Kevin , KIM, Dooseop
发明人： PASTERNAK, Alexander , DEJESUS, Reynalda, K. , ZHU, Yuping , YANG, Lihu , WALSH, Shawn , PIO, Barbara , SHAHRIPOUR, Aurash , TANG, Haifeng , BELYK, Kevin , KIM, Dooseop
IPC分类号： A61K31/496
CPC分类号： C07D405/12 , A61K31/496 , C07D257/04 , C07D307/88 , C07D311/02 , C07D311/76 , C07D311/80 , C07D403/10 , C07D405/06 , C07D405/14 , C07D413/12 , C07D413/14 , C07D471/08 , C07D487/08 , C07D495/04
摘要： This invention relates to compounds having structural Formula (I); and pharmaceutically acceptable salts thereof which are inhibitors of the Renal Outer Medullary Potassium (ROMK) channel (Kir 1.1). The compounds of Formula I are useful as diuretics and natriuretics and therefore are useful for the therapy and prophylaxis of disorders resulting from excessive salt and water retention, including cardiovascular diseases such as hypertension and chronic and acute heart failure.
摘要翻译：本发明涉及具有结构式（I）的化合物; 和它们的药学上可接受的盐，它们是肾外
膜髓质（ROMK）通道（Kir1.1）的抑制剂。式I的化合物可用作利尿剂和利尿钠，因此可用于治疗和预防由过度的盐和水保持引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

2. 发明申请

WO2016196932A1 PROCESS FOR PREPARING SUBSTITUTED TETRACYCLIC HETEROCYCLE COMPOUNDS 审中-公开
标题翻译：制备取代的四环杂环化合物的方法
公开(公告)号：WO2016196932A1
公开(公告)日：2016-12-08
申请号：PCT/US2016/035717
申请日：2016-06-03
申请人： MERCK SHARP & DOHME CORP. , YIN, Jingjun , ITOH, Tetsuji , YIN, Jianguo , XIANG, Bangping , CAMPOS, Kevin, R. , KALININ, Alexei , LIU, Zhuqing , CHRISTENSEN, Melodie Deniz , BELYK, Kevin , VARSOLONA, Richard, J. , BRUNSKILL, Andrew
发明人： YIN, Jingjun , ITOH, Tetsuji , YIN, Jianguo , XIANG, Bangping , CAMPOS, Kevin, R. , KALININ, Alexei , LIU, Zhuqing , CHRISTENSEN, Melodie Deniz , BELYK, Kevin , VARSOLONA, Richard, J. , BRUNSKILL, Andrew
IPC分类号： A61K31/404 , A61K31/407 , A61P31/14 , C07D498/04
CPC分类号： C07D498/04 , B01J31/04 , C07D403/04 , C07F5/025
摘要： The present invention is directed to processes for preparing Substituted Tetracyclic Heterocycle Compounds of formula (I): (I) which may be useful as HCV NS5A inhibitors. The present invention is also directed to compounds that may be useful as synthetic intermediates and catalysts in the processes of the invention.
摘要翻译：本发明涉及制备式（I）的取代的四环杂环化合物的方法：（I），其可用作HCV NS5A抑制剂。本发明还涉及在本发明方法中可用作合成中间体和催化剂的化合物。

3. 发明申请

WO2007120591A1 PROCESS FOR THE PREPARATION OF CGRP ANTAGONIST 审中-公开
标题翻译：制备CGRP拮抗剂的方法
公开(公告)号：WO2007120591A1
公开(公告)日：2007-10-25
申请号：PCT/US2007/008702
申请日：2007-04-06
申请人： MERCK & CO., INC. , BELYK, Kevin , RIVERA, Nelo
发明人： BELYK, Kevin , RIVERA, Nelo
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N -[(3 R ,6 S )-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine -1-carboxamide, by coupling (3 R ,6 S )-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1 H -imidazo[4,5-b]pyridine dihydrochloride with 1,1'-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3 R, 6 S )-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine -1-carboxamide.
摘要翻译：制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] -4- （3R，6S）-3-氨基-6-（2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺，（2,2-二氟苯基）-1-（2,2,2-三氟乙基）氮杂环庚烷-2-酮和2-氧代-1-（4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b] 吡啶二盐酸盐与1,1'-羰基二咪唑（“CDI”）作为羰基源; 并且有效制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] - 4-（2-氧代-2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺。

4. 发明申请

WO2007120592A1 CGRP ANTAGONIST SALT 审中-公开
公开(公告)号：WO2007120592A1
公开(公告)日：2007-10-25
申请号：PCT/US2007/008703
申请日：2007-04-06
申请人： MERCK & CO., INC. , BELYK, Kevin
发明人： BELYK, Kevin
IPC分类号： A61K31/55 , C07D401/14
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N -[(3 R ,6 S )-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine -1-carboxamide, by coupling (3 R, 6 S )-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1 H -imidazo[4,5-b]pyridine dihydrochloride with 1,1'-carbonyldiimidazole ("CDI") as carbonyl source; an efficient preparation of the potassium salt of N -[(3 R ,6 S )-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine -1-carboxamide; efficient syntheses for the preparation of intermediates (3 R ,6 S )-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1 H -imidazo[4,5-b]pyridine dihydrochloride, and the potassium salt of N -[(3 R ,6 S )-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine -1-carboxamide including the potassium salt ethanolate and potassium salt hydrate.
摘要翻译：制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] -4- （3R，6S）-3-氨基-6-（2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺，（2,2-二氟苯基）-1-（2,2,2-三氟乙基）氮杂环庚烷-2-酮和2-氧代-1-（4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b] 吡啶二盐酸盐与1,1'-羰基二咪唑（“CDI”）作为羰基源; 有效制备N - [（3R，6S）-6-（2,3-二氟苯基）-2-氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] -4 - （2-氧代-2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺; 制备中间体（3R，6S）-3-氨基-6-（2,3-二氟苯基）-1-（2,2,2-三氟乙基）氮杂环庚烷-2-酮和2-氧代-1- （4-哌啶基）-2,3-二氢-1H-咪唑并[4,5-b]吡啶二盐酸盐和N - [（3R，6S）-6-（2,3-二氟苯基）-2 氧代-1-（2,2,2-三氟乙基）氮杂环庚烷-3-基] -4-（2-氧代-2,3-二氢-1H-咪唑并[4,5-b]吡啶-1-基）哌啶-1-甲酰胺，包括钾盐乙醇化物和钾盐水合物。

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