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1. 发明授权

US07829699B2 Process for the preparation of CGRP antagonist 失效
标题翻译：制备CGRP拮抗剂的方法
公开(公告)号：US07829699B2
公开(公告)日：2010-11-09
申请号：US12226244
申请日：2007-04-06
申请人： Kevin Belyk , Nelo Rivera
发明人： Kevin Belyk , Nelo Rivera
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N-[(3R,6S)-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 (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-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。

2. 发明申请

US20090281306A1 Process for the Preparation of Cgrp Antagonist 失效
标题翻译： Cgrp拮抗剂的制备方法
公开(公告)号：US20090281306A1
公开(公告)日：2009-11-12
申请号：US12226244
申请日：2007-04-06
申请人： Kevin Belyk , Nelo Rivera
发明人： Kevin Belyk , Nelo Rivera
IPC分类号： C07D401/14
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N-[(3R,6S)-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 (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; and an efficient preparation of the potassium salt of N-[(3R,6S)-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。

3. 发明授权

US09056859B2 Inhibitors of the renal outer medullary potassium channel 有权
标题翻译：肾外髓质钾通道抑制剂
公开(公告)号：US09056859B2
公开(公告)日：2015-06-16
申请号：US13881574
申请日：2011-10-24
申请人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
发明人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
IPC分类号： C07D257/04 , C07D405/12 , C07D405/14 , C07D413/12 , C07D413/14 , C07D495/04 , A61K31/496 , C07D311/76 , C07D311/80 , C07D403/10 , C07D307/88 , C07D311/02 , C07D405/06 , C07D471/08 , C07D487/08
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分滞留引起的疾病，包括心血管疾病如高血压和慢性和急性心力衰竭。

4. 发明申请

US20130217680A1 Inhibitors of the Renal Outer Medullary Potassium Channel 有权
标题翻译：肾外侧髓质钾通道抑制剂
公开(公告)号：US20130217680A1
公开(公告)日：2013-08-22
申请号：US13881574
申请日：2011-10-24
申请人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
发明人： Alexander Pasternak , Reynalda K. deJesus , Yuping Zhu , Lihu Yang , Shawn Walsh , Haifeng Tang , Dooseop Kim , Barbara Pio , Aurash Shahripour , Kevin Belyk
IPC分类号： C07D405/12 , C07D405/14 , C07D471/08 , C07D413/14 , C07D487/08 , C07D413/12 , C07D257/04
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。

5. 发明申请

US20100286122A1 CGRP Antagonist Salt 审中-公开
标题翻译： CGRP拮抗剂盐
公开(公告)号：US20100286122A1
公开(公告)日：2010-11-11
申请号：US12086670
申请日：2007-04-06
申请人： Kevin Belyk
发明人： Kevin Belyk
IPC分类号： A61K31/55 , C07D401/14 , A61P25/06
CPC分类号： C07D471/04
摘要： An efficient synthesis for the preparation of N-[(3R,6S)-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 (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride with 1,1′-carbonyldiimidazole (“CDI”) as carbonyl source; an efficient preparation of the potassium salt of N-[(3R,6S)-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 (3R,6S)-3-amino-6-(2,3-difluorophenyl)-1-(2,2,2-trifluoroethyl)azepan-2-one and 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and the potassium salt of N-[(3R,6S)-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。

6. 发明申请

US20060122205A1 Potassium salt of an HIV integrase inhibitor 有权
标题翻译： HIV整合酶抑制剂的钾盐
公开(公告)号：US20060122205A1
公开(公告)日：2006-06-08
申请号：US11293678
申请日：2005-12-02
申请人： Kevin Belyk , Henry Morrison , Philip Jones , Vincenzo Summa , V. Cooper , Amar Mahajan , Daniel Kumke , Hsien-Hsin Tung , Lawrence Wai , Vanessa Pruzinsky , Philip Pye , Remy Angelaud , Danny Mancheno
发明人： Kevin Belyk , Henry Morrison , Philip Jones , Vincenzo Summa , V. Cooper , Amar Mahajan , Daniel Kumke , Hsien-Hsin Tung , Lawrence Wai , Vanessa Pruzinsky , Philip Pye , Remy Angelaud , Danny Mancheno
IPC分类号： A61K31/513 , C07D413/02
CPC分类号： C07D239/557 , C07D313/12 , C07D413/12
摘要： Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.
摘要翻译：公开了化合物A的钾盐及其制备方法，其中化合物A具有下式：化合物A是可用于治疗或预防HIV感染，延迟AIDS发作和用于治疗或预防艾滋病的HIV整合酶抑制剂。

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