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公开(公告)号：US10544136B2
公开(公告)日：2020-01-28
申请号：US15959935
申请日：2018-04-23
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： C07D413/04 , C07D413/14 , C07D271/06 , C07D471/04 , A61K31/4245 , C07D401/04 , C07D263/32
摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
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公开(公告)号：US20190023700A1
公开(公告)日：2019-01-24
申请号：US15924119
申请日：2018-03-16
发明人： Edward Roberts , Miguel A. Guerrero , Mariangela Urbano , Hugh Rosen , Robert M. Jones , Candace Mae Laxamana , Xianrui Zhao , Eric Douglas Turtle
IPC分类号： C07D413/14 , A61P25/00 , A61P25/06
摘要： Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.
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公开(公告)号：US20240343719A1
公开(公告)日：2024-10-17
申请号：US18542394
申请日：2023-12-15
发明人： Edward Roberts , Miguel A. Guerrero , Mariangela Urbano , Hugh Rosen , Robert M. Jones , Candace Mae Laxamana , Xianrui Zhao , Eric Douglas Turtle
IPC分类号： C07D413/14 , A61P25/00 , A61P25/06
CPC分类号： C07D413/14 , A61P25/00 , A61P25/06
摘要： Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof:
wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.-
公开(公告)号：US20210047310A1
公开(公告)日：2021-02-18
申请号：US16846136
申请日：2020-04-10
发明人： Edward Roberts , Miguel A. Guerrero , Mariangela Urbano , Hugh Rosen , Robert M. Jones , Candace Mae Laxamana , Xianrui Zhao , Eric Douglas Turtle
IPC分类号： C07D413/14 , A61P25/00 , A61P25/06
摘要： Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.
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公开(公告)号：US20190084947A1
公开(公告)日：2019-03-21
申请号：US15959935
申请日：2018-04-23
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： C07D271/06 , C07D413/14 , A61K31/4245 , C07D413/04 , C07D471/04 , C07D263/32 , C07D401/04
摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphinogosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
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公开(公告)号：US20180009770A1
公开(公告)日：2018-01-11
申请号：US15713237
申请日：2017-09-22
发明人： Edward Roberts , Hugh Rosen , Steven Brown , Miguel A. Guerrero , Xuemei Peng , Ramulu Poddutoori
IPC分类号： C07D271/06 , C07D413/14 , C07D413/04 , C07D471/04 , A61K31/4245 , C07D401/04 , C07D263/32
CPC分类号： C07D271/06 , A61K31/4245 , C07D263/32 , C07D401/04 , C07D413/04 , C07D413/14 , C07D471/04
摘要： Compounds that activate a sphingosine-1-phosphate receptor of the subtype 1 are provided. Certain compounds selectively activate the receptor subtype 1 in relation to the sphingosine-1-phosphate receptor subtype 3. Uses and methods of inventive compounds for treatment of malconditions wherein activation, agonism, inhibition or antagonism of the S1P1 is medically indicated are provided.
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7.发明申请公开(公告)号：US20170217963A1
公开(公告)日：2017-08-03
申请号：US15514891
申请日：2015-09-28
IPC分类号： C07D471/04 , C07D213/61 , C07D215/12 , C07D213/38 , C07D413/12 , C07D213/40 , C07D213/80 , C07D405/12 , C07D401/12 , C07D409/12 , C07D239/30 , C07D213/75 , C07D333/20 , C07D241/16 , C07D237/08 , C07D239/26 , C07D213/55 , C07D235/14 , C07D263/32 , C07D217/18 , C07D249/08 , C07D263/58 , C07D241/42 , C07D413/14 , C07D413/04 , C07D271/06 , C07D271/10 , C07C255/63
CPC分类号： C07D471/04 , C07C255/63 , C07D211/16 , C07D213/38 , C07D213/40 , C07D213/55 , C07D213/61 , C07D213/75 , C07D213/78 , C07D213/80 , C07D215/12 , C07D217/18 , C07D235/14 , C07D237/08 , C07D239/26 , C07D239/30 , C07D241/16 , C07D241/42 , C07D249/08 , C07D263/32 , C07D263/58 , C07D271/06 , C07D271/10 , C07D285/12 , C07D309/06 , C07D309/14 , C07D333/20 , C07D401/12 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14 , C09B55/002 , C09B55/005 , C09B55/007
摘要： The invention provides compounds effective as sphingosine-1-phosphate receptor modulators for treatment of cardiopulmonary diseases, such as hypertension (including malignant hypertension), angina, myocardial infarction, cardiac arrhythmias, congestive heart failure, coronary heart disease, atherosclerosis, angina pectoris, dysrhythmias, cardiomyothopy (including hypertropic cardiomyothopy), heart failure, cardiac arrest, bronchitis, asthma, chronic obstructive pulmonary disease, cystic fibrosis, croup, emphysema, pleurisy, pulmonary fibrosis, pneumonia, pulmonary embolus, pulmonary hypertension, mesothelioma, ventricular conduction abnormalities, complete heart block, adult respiratory distress syndrome, sepsis syndrome, idiopathic pulmonary fibrosis, scleroderma, systemic sclerosis, retroperitoneal fibrosis, prevention of keloid formation, or cirrhosis.
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公开(公告)号：US11897873B2
公开(公告)日：2024-02-13
申请号：US17390531
申请日：2021-07-30
发明人： Edward Roberts , Miguel A. Guerrero , Mariangela Urbano , Hugh Rosen , Robert M. Jones , Candace Mae Laxamana , Xianrui Zhao , Eric Douglas Turtle
IPC分类号： C07D413/14 , A61P25/00 , A61P25/06
CPC分类号： C07D413/14 , A61P25/00 , A61P25/06
摘要： Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof:
wherein X, Y, R1, R2, R4, R5, R6, R7, R8 and R11 are as defined herein.-
公开(公告)号：US10676469B2
公开(公告)日：2020-06-09
申请号：US15924119
申请日：2018-03-16
发明人： Edward Roberts , Miguel A. Guerrero , Mariangela Urbano , Hugh Rosen , Robert M. Jones , Candace Mae Laxamana , Xianrui Zhao , Eric Douglas Turtle
IPC分类号： C07D413/14 , A61P25/00 , A61P25/06
摘要： Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.
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公开(公告)号：US09682966B2
公开(公告)日：2017-06-20
申请号：US14421932
申请日：2013-08-16
IPC分类号： A61P25/04 , A61K31/4545 , A61P37/02 , A61K31/435 , A61P25/28 , C07D405/14 , C07D413/14 , C07D401/04 , C07D211/58
CPC分类号： C07D405/14 , C07D211/58 , C07D401/04 , C07D413/14
摘要： The invention provides novel ligands of Kappa (κ) opioid receptors, such as can be used to modulate a Kappa opioid receptor. Methods of synthesis and methods of use are also provided. Compounds of the invention can be used therapeutically in the treatment of dissociative disorders or pain, or to provide neuroprotection, or to induce diuresis, or to modulate the immune system, or for treatment of one or more of an affective disorders comprising depression or stress/anxiety; an addictive disorder; alcoholism, epilepsy; a cognition deficiency; schizophrenia; Alzheimer's disease; or pain.
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