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公开(公告)号：US08236846B2
公开(公告)日：2012-08-07
申请号：US13191100
申请日：2011-07-26
申请人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A01N43/56 , A61K31/415 , C07D231/00
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and 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，Y，Z，Q，W，X和R5-7如说明书中所定义，及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：US20120165381A1
公开(公告)日：2012-06-28
申请号：US13413076
申请日：2012-03-06
申请人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A61K31/4174 , A61P13/12 , A61P9/00 , C07D233/70 , A61P9/12
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and 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，R2-3，X和R5-7如说明书中所定义，及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：US20110251249A1
公开(公告)日：2011-10-13
申请号：US13165975
申请日：2011-06-22
IPC分类号： A61K31/4184 , A61P9/12 , A61P9/00 , A61K31/4178 , A61K31/4164
CPC分类号： C07D233/68 , C07D233/60 , C07D233/70 , C07D233/84 , C07D233/90 , C07D409/12
摘要： The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and 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：Q，W，Y，Z，r和Ar如说明书中所定义，及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：US07777077B2
公开(公告)日：2010-08-17
申请号：US12012161
申请日：2008-01-31
申请人： Seok-Ki Choi , Paul R. Fatheree , Ryan Hudson , Keith Jendza , Robert M. McKinnell , Vivek Sasikumar
发明人： Seok-Ki Choi , Paul R. Fatheree , Ryan Hudson , Keith Jendza , Robert M. McKinnell , Vivek Sasikumar
IPC分类号： C07C239/00 , C07D257/00
CPC分类号： C07C237/20 , C07C243/32 , C07C319/12 , C07C323/22 , C07C323/41 , C07C323/60 , C07C2601/14 , C07D257/04
摘要： The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及式I化合物：其中Ar，r，R 3，X和R 5-7如说明书中所定义，及其药学上可接受的盐。 式I的化合物具有AT1受体拮抗剂活性和去皮质激素抑制活性。 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：US20090270473A1
公开(公告)日：2009-10-29
申请号：US12431056
申请日：2009-04-28
IPC分类号： A61K31/4184 , C07D233/54 , A61K31/4164 , A61K31/4178 , C07D235/02 , A61P9/00 , A61P9/12
CPC分类号： C07D233/68 , C07D233/60 , C07D233/70 , C07D233/84 , C07D233/90 , C07D409/12
摘要： The invention relates to compounds having the formula: wherein: Q, W, Y, Z, r, and Ar are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and 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：Q，W，Y，Z，r和Ar如说明书中所定义，及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：US20090023228A1
公开(公告)日：2009-01-22
申请号：US12148842
申请日：2008-04-23
申请人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A61K31/4196 , C07D233/64 , A61K31/4164 , G01N33/53 , A61P9/04 , G01N33/566 , C07D249/08
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5.7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and 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，R2-3，X和R5.7如说明书中所定义，及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：US20080176895A1
公开(公告)日：2008-07-24
申请号：US12075669
申请日：2008-03-13
申请人： Daniel Marquess , Paul R. Fatheree , S. Derek Turner , Daniel D. Long , Seok-Ki Choi , Adam A. Goldblum , Daniel Genov
发明人： Daniel Marquess , Paul R. Fatheree , S. Derek Turner , Daniel D. Long , Seok-Ki Choi , Adam A. Goldblum , Daniel Genov
CPC分类号： C07D451/02 , C07D451/04
摘要： The invention provides novel quinolinone-carboxamide 5-HT4 receptor agonist compounds. The invention also provides 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： 本发明提供新颖的喹啉酮 - 甲酰胺5-HT 4受体激动剂化合物。 本发明还提供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受体活性相关的疾病的方法，以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：US20080132491A1
公开(公告)日：2008-06-05
申请号：US12008840
申请日：2008-01-15
申请人： Paul Fatheree , Roland Gendron , Adam A. Goldblum , Daniel D. Long , Daniel Marquess , S.Derek Turner , Seok-Ki Choi
发明人： Paul Fatheree , Roland Gendron , Adam A. Goldblum , Daniel D. Long , Daniel Marquess , S.Derek Turner , Seok-Ki Choi
IPC分类号： A61K31/551 , A61P1/00 , C07D471/08 , A61K31/439 , A61K31/496 , A61K31/5377
CPC分类号： C07D451/04
摘要： The invention provides novel indazole-carboxamide 5-HT4 receptor agonist compounds. The invention also provides 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：US07329752B2
公开(公告)日：2008-02-12
申请号：US11602888
申请日：2006-11-21
IPC分类号： A61K31/439 , A61K31/541 , C07D401/12 , C07D417/14
CPC分类号： C07D451/04
摘要： The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b are defined in the disclosure. The invention also provides 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： 本发明提供新的苯并咪唑酮 - 甲酰胺衍生的氨基甲酸酯5-HT 4受体激动剂式（I）化合物：其中R 1，R 2， 在本公开中限定了R 3，R 4，R 4，a和b。 本发明还提供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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公开(公告)号：US20070117796A1
公开(公告)日：2007-05-24
申请号：US11602888
申请日：2006-11-21
申请人： Daniel Long , Seok-Ki Choi , Paul Fatheree , Adam Goldblum , Daniel Marquess
发明人： Daniel Long , Seok-Ki Choi , Paul Fatheree , Adam Goldblum , Daniel Marquess
IPC分类号： A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/46 , C07D453/02
CPC分类号： C07D451/04
摘要： The invention provides novel benzoimidazolone-carboxamide-derived carbamate 5-HT4 receptor agonist compounds of formula (I): wherein R1, R2, R3, R4, a, and b are defined in the disclosure. The invention also provides 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： 本发明提供新的苯并咪唑酮 - 甲酰胺衍生的氨基甲酸酯5-HT 4受体激动剂式（I）化合物：其中R 1，R 2， 在本公开中限定了R 3，R 4，R 4，a和b。 本发明还提供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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