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公开(公告)号：US09682052B2
公开(公告)日：2017-06-20
申请号：US14838842
申请日：2015-08-28
IPC分类号： A01N37/00 , A61K31/21 , A61K31/197 , C07C271/22 , C07D317/40 , C07C231/02 , C07C233/56 , C07C243/30 , C07D319/06 , C07D207/263 , A61K31/24 , A61K31/27 , A61K31/365 , A61K45/06 , C07C243/28 , C07C243/26 , A61K31/167 , A61K31/165 , A61K31/16 , A61K31/166 , A61K31/164
CPC分类号： A61K31/197 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/24 , A61K31/27 , A61K31/365 , A61K45/06 , C07C231/02 , C07C233/56 , C07C243/26 , C07C243/28 , C07C243/30 , C07C271/22 , C07D207/263 , C07D317/40 , C07D319/06
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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公开(公告)号：US09670186B2
公开(公告)日：2017-06-06
申请号：US14812095
申请日：2015-07-29
申请人： Melissa Fleury , Adam D. Hughes
发明人： Melissa Fleury , Adam D. Hughes
IPC分类号： C07D263/38 , C07D405/12 , A61K31/415 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K45/06 , C07D231/14 , C07D231/20 , C07D249/04 , C07D261/18
CPC分类号： C07D405/12 , A61K31/415 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K45/06 , C07D231/14 , C07D231/20 , C07D249/04 , C07D261/18 , C07D263/38
摘要： In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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公开(公告)号：US09499487B2
公开(公告)日：2016-11-22
申请号：US13475076
申请日：2012-05-18
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Jane Schmidt
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Jane Schmidt
IPC分类号： A61K31/565 , A61K31/4418 , C07D261/18 , A61K31/42 , C07D213/81 , C07D237/04 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/10 , C07D249/18 , C07D263/34 , C07D307/68 , C07D333/38 , C07D401/06 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D261/18 , A01N47/16 , A61K31/4196 , A61K31/42 , A61K31/4355 , A61K31/437 , A61K45/06 , A61K47/55 , A61K47/6895 , C07D213/81 , C07D237/04 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/10 , C07D249/18 , C07D263/34 , C07D307/68 , C07D333/38 , C07D401/06 , C07D471/04 , C07D487/04 , C07D498/04 , C09K15/30
摘要： In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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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公开(公告)号：US20160083372A1
公开(公告)日：2016-03-24
申请号：US14812095
申请日：2015-07-29
申请人： Melissa Fleury , Adam D. Hughes
发明人： Melissa Fleury , Adam D. Hughes
IPC分类号： C07D405/12 , C07D249/04 , C07D263/38 , A61K31/421 , A61K45/06 , A61K31/42 , C07D231/20 , A61K31/415 , C07D231/14 , A61K31/4192 , C07D261/18
CPC分类号： C07D405/12 , A61K31/415 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K45/06 , C07D231/14 , C07D231/20 , C07D249/04 , C07D261/18 , C07D263/38
摘要： In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中X，Ra，Rb，R2和R7如说明书中所定义，或其药学上可接受的盐。 这些化合物是具有去甲苯胺抑制活性的化合物的前药。 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：US09120758B2
公开(公告)日：2015-09-01
申请号：US14024974
申请日：2013-09-12
申请人： Cameron Smith , Melissa Fleury , Roland Gendron , Ryan Hudson , Adam D. Hughes
发明人： Cameron Smith , Melissa Fleury , Roland Gendron , Ryan Hudson , Adam D. Hughes
IPC分类号： C07D231/14 , C07D401/06 , C07D261/18 , C07D249/10 , C07D471/04 , C07D257/04 , C07D263/34 , C07C281/02 , C07D231/20 , C07D231/22 , C07D231/40 , C07D237/24 , C07D239/36 , C07D239/54 , C07D249/04 , C07D249/12 , C07D249/18 , C07D263/38 , C07D277/56 , C07D401/04 , C07D403/04 , C07D403/06 , C07D413/04 , C07D239/28 , C07D239/34 , C07D239/52
CPC分类号： C07D471/04 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/5377 , C07C281/02 , C07D231/14 , C07D231/20 , C07D231/22 , C07D231/40 , C07D237/14 , C07D237/24 , C07D239/28 , C07D239/34 , C07D239/36 , C07D239/52 , C07D239/54 , C07D249/04 , C07D249/10 , C07D249/12 , C07D249/18 , C07D257/04 , C07D261/12 , C07D261/18 , C07D263/32 , C07D263/34 , C07D263/38 , C07D277/34 , C07D277/56 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D413/04 , Y02P20/55
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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公开(公告)号：US20150166469A1
公开(公告)日：2015-06-18
申请号：US14516866
申请日：2014-10-17
申请人： Erik Fenster , Melissa Fleury , Adam D. Hughes
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： C07C235/78 , A61K45/06 , C07D207/08 , A61K31/4015 , C07D213/75 , A61K31/44 , C07D261/04 , A61K31/42 , C07D295/32 , A61K31/5375 , C07D205/04 , A61K31/397 , C07D207/14 , A61K31/40 , A61K31/495 , C07D491/107 , A61K31/197
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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7.发明授权Diamide compounds having muscarinic receptor antagonist and β2 adrenergic receptor agonist activity 有权具有毒蕈碱受体拮抗剂和二肾上腺素受体激动剂活性的二酰胺化合物公开(公告)号：US09000173B2
公开(公告)日：2015-04-07
申请号：US14327853
申请日：2014-07-10
申请人： Adam D. Hughes , Yan Chen , John R. Jacobsen , Eric L. Stangeland , Rose Yen
发明人： Adam D. Hughes , Yan Chen , John R. Jacobsen , Eric L. Stangeland , Rose Yen
IPC分类号： C07D401/12 , A61K45/06 , A61K31/444 , A61K31/4709 , A61K31/56
CPC分类号： C07D401/12 , A61K31/444 , A61K31/4709 , A61K31/56 , A61K45/06
摘要： This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and β2 adrenergic receptor agonist activities. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compounds as bronchodilating agents to treat pulmonary disorders.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐。 这些化合物具有毒蕈碱受体拮抗剂和二肾上腺素能受体激动剂活性。 本发明还涉及包含这些化合物的药物组合物，用于制备这些化合物的方法和中间体，以及使用这些化合物作为支气管扩张剂来治疗肺部疾病的方法。
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8.发明申请DIAMIDE COMPOUNDS HAVING MUSCARINIC RECEPTOR ANTAGONIST AND BETA2 ADRENERGIC RECEPTOR AGONIST ACTIVITY 审中-公开具有肌钙蛋白受体拮抗剂和BETA2 ADRENERGIC受体激动剂的DIAMIDE化合物公开(公告)号：US20140323733A1
公开(公告)日：2014-10-30
申请号：US14327853
申请日：2014-07-10
申请人： Adam D. Hughes , Yan Chen , John R. Jacobsen , Eric L. Stangeland , Rose Yen
发明人： Adam D. Hughes , Yan Chen , John R. Jacobsen , Eric L. Stangeland , Rose Yen
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , A61K31/444 , A61K31/4709 , A61K31/56 , A61K45/06
摘要： This invention relates to a compound of formula I: or a pharmaceutically acceptable salt thereof. Such compounds possess both muscarinic receptor antagonist and β2 adrenergic receptor agonist activities. The invention also relates to pharmaceutical compositions comprising such compounds, processes and intermediates for preparing such compounds, and methods of using such compounds as bronchodilating agents to treat pulmonary disorders.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐。 这些化合物具有毒蕈碱受体拮抗剂和二肾上腺素能受体激动剂活性。 本发明还涉及包含这些化合物的药物组合物，用于制备这些化合物的方法和中间体，以及使用这些化合物作为支气管扩张剂来治疗肺部疾病的方法。
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公开(公告)号：US08853427B2
公开(公告)日：2014-10-07
申请号：US13908619
申请日：2013-06-03
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes
IPC分类号： C07C229/34 , C07C271/22 , C07D231/14 , C07D231/18 , C07D233/70 , C07D235/08 , C07D237/14 , C07D239/34 , C07D249/04 , C07D249/10 , C07D249/12 , C07D249/18 , C07D261/12 , C07D263/18 , C07D309/40 , C07D401/04 , C07D405/12 , C07D471/04 , C07D319/06
CPC分类号： A61K31/675 , A61K31/351 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/50 , A61K31/505 , A61K31/5377 , A61K45/06 , C07B2200/07 , C07C229/34 , C07C271/22 , C07D231/14 , C07D231/18 , C07D231/20 , C07D233/70 , C07D233/90 , C07D235/08 , C07D237/14 , C07D239/34 , C07D239/36 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/18 , C07D261/12 , C07D263/18 , C07D295/10 , C07D309/32 , C07D309/40 , C07D319/06 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/6518
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes 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R 1 -R 6，a，b，Z和X如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 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：US20140256702A1
公开(公告)日：2014-09-11
申请号：US14196624
申请日：2014-03-04
申请人： Erik Fenster , Melissa Fleury , Adam D. Hughes
发明人： Erik Fenster , Melissa Fleury , Adam D. Hughes
IPC分类号： A61K31/5375 , A61K31/197 , C07D207/09 , A61K31/40 , C07D213/56 , C07D491/107 , C07D261/04 , A61K31/42 , C07D295/32 , C07D205/04 , A61K31/397 , C07D207/14 , C07C235/34 , A61K31/44
CPC分类号： C07C243/38 , A61K31/192 , A61K31/197 , A61K31/341 , A61K31/397 , A61K31/40 , A61K31/4015 , A61K31/42 , A61K31/44 , A61K31/4406 , A61K31/4409 , A61K31/495 , A61K31/5375 , A61K45/06 , C07C233/56 , C07C235/12 , C07C235/20 , C07C235/34 , C07C235/74 , C07C235/78 , C07C235/80 , C07C243/24 , C07C243/32 , C07C259/04 , C07C2601/08 , C07C2601/16 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/14 , C07D207/16 , C07D211/22 , C07D211/38 , C07D211/42 , C07D211/46 , C07D211/48 , C07D211/60 , C07D211/62 , C07D213/56 , C07D213/61 , C07D213/65 , C07D213/75 , C07D213/86 , C07D213/87 , C07D233/06 , C07D239/36 , C07D261/02 , C07D261/04 , C07D265/30 , C07D295/32 , C07D307/68 , C07D309/08 , C07D401/04 , C07D405/06 , C07D491/107 , C07D493/10
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R5 and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes 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R1-R5和X如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 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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