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公开(公告)号：US08080572B2
公开(公告)日：2011-12-20
申请号：US12949114
申请日：2010-11-18
IPC分类号： A61K31/4164 , A61K31/4196 , C07D233/54 , C07D249/08
CPC分类号： A61K31/4196 , A61K45/06 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D249/10 , C07D401/06 , C07D401/14 , C07D403/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，r，Z，X，R 3和R 5-7如说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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42.发明授权公开(公告)号：US08377964B2
公开(公告)日：2013-02-19
申请号：US12796902
申请日：2010-06-09
申请人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
发明人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
IPC分类号： A61K31/4545
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , G01N33/5058
摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明涉及式（I）的苯并咪唑 - 甲酰胺5-HT 4受体激动剂化合物，其中R 1和X如说明书中所定义，或其药学上可接受的盐或溶剂合物或立体异构体。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗与5-HT 4受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。
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43.发明申请公开(公告)号：US20090209582A1
公开(公告)日：2009-08-20
申请号：US11920817
申请日：2006-05-24
申请人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess , Sean Dalziel , Kirsten M. Phizackerley
发明人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess , Sean Dalziel , Kirsten M. Phizackerley
IPC分类号： A61K31/4545 , C07D401/14 , A61P1/00
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , G01N33/5058
摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds. The invention further relates to crystalline forms of a compound of formula (I).
摘要翻译： 本发明涉及式（I）的苯并咪唑 - 甲酰胺5-HT 4受体激动剂化合物，其中R 1和X如说明书中所定义，或其药学上可接受的盐或溶剂合物或立体异构体。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗与5-HT 4受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。 本发明还涉及式（I）化合物的结晶形式。
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公开(公告)号：US08513432B2
公开(公告)日：2013-08-20
申请号：US13483399
申请日：2012-05-30
IPC分类号： A61K31/4184 , C07D235/08
CPC分类号： C07D235/08 , C07D235/26 , C07D403/10
摘要： The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2′, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中Ar，r，n，X，R2，R2'，R3和R5-7如本说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20120238611A1
公开(公告)日：2012-09-20
申请号：US13483399
申请日：2012-05-30
IPC分类号： A61K31/4184 , A61P7/10 , A61P9/12 , A61P3/10 , A61P3/06 , A61P7/02 , C07D235/08 , A61P29/00
CPC分类号： C07D235/08 , C07D235/26 , C07D403/10
摘要： The invention relates to compounds having the formula: wherein Ar, r, n, X, R2, R2′, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中Ar，r，n，X，R2，R2'，R3和R5-7如本说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20130273568A1
公开(公告)日：2013-10-17
申请号：US13742783
申请日：2013-01-16
申请人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-Ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
发明人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-Ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
IPC分类号： G01N33/50
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , G01N33/5058
摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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公开(公告)号：US08338418B2
公开(公告)日：2012-12-25
申请号：US13298493
申请日：2011-11-17
IPC分类号： A61K31/5377 , A61K31/44 , A61K31/4155 , A61K31/41 , A61K31/415 , A61K31/4245 , C07D413/14 , C07D401/14 , C07D259/00 , C07D271/06 , C07D231/10
CPC分类号： A61K31/4196 , A61K45/06 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D249/10 , C07D401/06 , C07D401/14 , C07D403/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，r，Z，X，R 3和R 5-7如说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20120214849A1
公开(公告)日：2012-08-23
申请号：US13298493
申请日：2011-11-17
IPC分类号： A61K31/4439 , A61K31/4178 , C07D401/06 , A61P9/12 , C07D233/90 , C07D401/14 , A61P29/00 , A61P3/10 , A61K31/4164 , C07D401/10
CPC分类号： A61K31/4196 , A61K45/06 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D249/10 , C07D401/06 , C07D401/14 , C07D403/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，r，Z，X，R 3和R 5-7如说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20110230525A1
公开(公告)日：2011-09-22
申请号：US12949114
申请日：2010-11-18
IPC分类号： A61K31/4439 , A61K31/4164 , A61K31/41 , A61K31/4196 , A61P13/12
CPC分类号： A61K31/4196 , A61K45/06 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D249/10 , C07D401/06 , C07D401/14 , C07D403/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，r，Z，X，R 3和R 5-7如说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 另一方面，本发明涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US07863309B2
公开(公告)日：2011-01-04
申请号：US12507995
申请日：2009-07-23
IPC分类号： A61K31/4164 , A61K31/4196 , C07D233/54 , C07D249/08
CPC分类号： A61K31/4196 , A61K45/06 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D249/10 , C07D401/06 , C07D401/14 , C07D403/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, r, Z, X, R3, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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