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公开(公告)号：US20230322774A1
公开(公告)日：2023-10-12
申请号：US18181138
申请日：2023-03-09
发明人： Daniel D. Long , Cameron Smith , Corbin Thompson
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： The invention provides compounds of formula (I):
where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat respiratory diseases.-
![8-AZABICYCLO[3.2.1]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS](/abs-image/US/2021/01/28/US20210024515A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210024515A1
公开(公告)日：2021-01-28
申请号：US16922414
申请日：2020-07-07
发明人： Daniel D. Long , John R. Jacobsen , Lan Jiang
IPC分类号： C07D451/02 , A61K31/46 , A61K31/485 , A61K45/06 , A61K31/439
摘要： The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
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3.发明申请公开(公告)号：US20190389895A1
公开(公告)日：2019-12-26
申请号：US16555222
申请日：2019-08-29
摘要： The invention provides compounds which are prodrugs of a JAK inhibitor agent for the targeted delivery of the JAK inhibitor to the gastrointestinal tract of a mammal. The invention also provides pharmaceutical compositions comprising the compounds, methods of using the compounds to treat gastrointestinal inflammatory diseases, and processes and intermediates useful for preparing the compounds.
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公开(公告)号：US10472366B2
公开(公告)日：2019-11-12
申请号：US15914189
申请日：2018-03-07
发明人： Daniel D. Long , Donna A.A. Wilton , Mandy M. Loo
摘要： The invention relates to glucuronide prodrug compounds of the Janus kinase (JAK) inhibitor tofacitinib having formula I: where A1 and R1 are as defined. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds to treat gastrointestinal inflammatory diseases; and processes and intermediates for preparing such compounds.
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公开(公告)号：US20180193338A1
公开(公告)日：2018-07-12
申请号：US15806730
申请日：2017-11-08
IPC分类号： A61K31/505 , C07D249/14 , C07D239/42 , C07D213/56 , C07D249/04 , C07C229/08 , A61K31/4192 , A61K45/06 , C07D231/14 , A61K31/415 , C07C271/22 , C07D263/34 , A61K31/421 , C07D271/07 , A61K31/4245 , C07D213/81 , A61K31/44 , C07D239/28 , C07D249/10 , A61K31/4196 , C07D307/24 , C07D405/12 , C07D207/16 , C07D403/12 , C07D261/10
CPC分类号： A61K31/505 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/421 , A61K31/4245 , A61K31/44 , A61K45/06 , C07C229/08 , C07C271/22 , C07D207/16 , C07D213/56 , C07D213/81 , C07D231/14 , C07D239/28 , C07D239/42 , C07D249/04 , C07D249/10 , C07D249/14 , C07D261/10 , C07D263/34 , C07D271/07 , C07D307/24 , C07D403/12 , C07D405/12
摘要： In one aspect, the invention relates to compounds having the formula I: where R1, R2a, R2b, and R3-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 these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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公开(公告)号：US20180118696A1
公开(公告)日：2018-05-03
申请号：US15696713
申请日：2017-09-06
IPC分类号： C07D249/04 , C07D249/10 , C07D231/14 , C07D261/18 , C07D263/34 , C07D263/38 , C07D271/07 , C07D239/28 , C07D231/20 , C07D275/03 , C07D471/04 , C07D403/12 , C07D213/81
CPC分类号： C07D249/04 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/437 , A61K31/44 , A61K31/4985 , A61K31/505 , A61K45/06 , A61P9/04 , A61P9/12 , A61P13/12 , C07C229/34 , C07C271/22 , C07D213/81 , C07D231/14 , C07D231/18 , C07D231/20 , C07D233/70 , C07D233/90 , C07D235/08 , C07D237/14 , C07D239/28 , C07D239/34 , C07D249/10 , C07D249/12 , C07D249/18 , C07D261/12 , C07D261/18 , C07D263/18 , C07D263/34 , C07D263/38 , C07D271/07 , C07D275/03 , C07D295/10 , C07D309/40 , C07D319/06 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D471/04
摘要： In one aspect, the invention relates to compounds having the formula I: where R1-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 these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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![4-[2-(2-FLUOROPHENOXYMETHYL)PHENYL]PIPERIDINE COMPOUNDS](/abs-image/US/2018/02/22/US20180050024A1/abs.jpg.150x150.jpg)
公开(公告)号：US20180050024A1
公开(公告)日：2018-02-22
申请号：US15591419
申请日：2017-05-10
IPC分类号： A61K31/4465 , C07D211/22 , C07D211/32
CPC分类号： A61K31/4465 , C07D211/22 , C07D211/32
摘要： The invention relates to compounds of formula I: where a, R1, and R3-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. The invention also 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：US09873692B2
公开(公告)日：2018-01-23
申请号：US15459315
申请日：2017-03-15
发明人： Daniel Marquess , Paul R. Fatheree , S. Derek Turner , Daniel D. Long , Seok-Ki Choi , Adam A. Goldblum
IPC分类号： C07D215/00 , C07D451/04 , C07D451/02
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.
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![8-AZABICYCLO[3.2.1]OCTANE COMPOUNDS AS MU OPIOID RECEPTOR ANTAGONISTS](/abs-image/US/2017/12/07/US20170349578A1/abs.jpg.150x150.jpg)
公开(公告)号：US20170349578A1
公开(公告)日：2017-12-07
申请号：US15496269
申请日：2017-04-25
发明人： Daniel D. Long , John R. Jacobsen , Lan Jiang
IPC分类号： C07D451/02 , A61K31/485 , A61K31/46 , A61K45/06 , A61K31/439
CPC分类号： C07D451/02 , A61K31/439 , A61K31/46 , A61K31/485 , A61K45/06
摘要： The invention provides novel 8-azabicyclo[3.2.1]octane compounds of formula (I): wherein R1, R2, R3, A, and G are defined in the specification, or a pharmaceutically-acceptable salt or solvate thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.
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公开(公告)号：US09783507B2
公开(公告)日：2017-10-10
申请号：US15419217
申请日：2017-01-30
IPC分类号： C07D295/24 , C07D205/04 , C07D267/02 , C07D317/10 , C07D249/04 , C07D249/10 , C07D231/14 , C07D261/18 , C07D263/34 , C07D263/38 , C07D271/07 , C07D213/81 , C07D239/28 , C07D231/20 , C07D275/03 , C07D471/04 , C07D403/12
CPC分类号： C07D249/04 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/4245 , A61K31/425 , A61K31/437 , A61K31/44 , A61K31/4985 , A61K31/505 , A61K45/06 , A61P9/04 , A61P9/12 , A61P13/12 , C07C229/34 , C07C271/22 , C07D213/81 , C07D231/14 , C07D231/18 , C07D231/20 , C07D233/70 , C07D233/90 , C07D235/08 , C07D237/14 , C07D239/28 , C07D239/34 , C07D249/10 , C07D249/12 , C07D249/18 , C07D261/12 , C07D261/18 , C07D263/18 , C07D263/34 , C07D263/38 , C07D271/07 , C07D275/03 , C07D295/10 , C07D309/40 , C07D319/06 , C07D401/04 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D471/04
摘要： In one aspect, the invention relates to compounds having the formula I: where R1-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 these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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