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公开(公告)号：US20150018371A1
公开(公告)日：2015-01-15
申请号：US14383715
申请日：2013-03-06
发明人： Roger D. Cone , Julien A. Sebag , Jacques Pantel , Savannah Y. Williams , David C. Weaver , Gary A. Sulikowski , Craig W. Lindsley , Padma S. Portonova , Chao Zhang
IPC分类号： A61K31/519 , A61K31/4192 , A61K31/343 , A61K31/427 , A61K31/437 , A61K31/381 , A61K31/495 , A61K31/4355 , A61K31/506 , A61K31/4709 , A61K31/4152 , A61K31/4162 , A61K31/426 , A61K31/517 , A61K31/166 , A61K31/47 , A61K31/436 , A61K31/216 , G01N33/50 , A61K31/4045
CPC分类号： A61K31/519 , A61K31/166 , A61K31/216 , A61K31/343 , A61K31/381 , A61K31/4045 , A61K31/415 , A61K31/4152 , A61K31/4162 , A61K31/4192 , A61K31/426 , A61K31/427 , A61K31/4355 , A61K31/436 , A61K31/437 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/4741 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/517 , C07D209/16 , C07D231/08 , C07D249/06 , C07D277/18 , C07D277/54 , C07D295/12 , C07D307/82 , C07D333/38 , C07D401/12 , C07D403/04 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , G01N33/502 , G01N2333/46 , G01N2500/10
摘要： Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
摘要翻译： 本文描述了黑皮质素受体的正变构调节剂，特别是受体MC3R和MC4R的变构增强子。 还提供了含有正变构调节剂的药物组合物和治疗肥胖症或肥胖相关疾病如2型糖尿病的方法，其包括施用有效量的正变构调节剂。
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公开(公告)号：US20220144794A1
公开(公告)日：2022-05-12
申请号：US17602133
申请日：2020-04-09
IPC分类号： C07D321/00 , A61P31/04
摘要： Provided are 9-dechlorochrysophaentin analog compounds and the synthesis process thereof. The disclosed compound have remarkable antimicrobial activities that are comparable to, or even more potent than, the natural product chrysophaentin A. Also provided are method of inhibiting bacterial growth or treating bacterial infection by administering an effective amount of the disclosed compounds.
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公开(公告)号：US10813355B2
公开(公告)日：2020-10-27
申请号：US16186106
申请日：2018-11-09
发明人： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC分类号： A01N43/653 , A01N43/82 , A01N43/78 , A01N43/90 , A01N25/08 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D513/04
摘要： In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitoes. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US09744171B2
公开(公告)日：2017-08-29
申请号：US14383715
申请日：2013-03-06
发明人： Roger D. Cone , Julien A. Sebag , Jacques Pantel , Savannah Y. Williams , David C. Weaver , Gary A. Sulikowski , Craig W. Lindsley , Padma S. Portonova , Chao Zhang
IPC分类号： A61K31/4965 , A61K31/519 , A61K31/4192 , C07D231/08 , C07D333/38 , C07D401/12 , C07D403/04 , C07D409/12 , C07D417/12 , C07D249/06 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , C07D277/18 , C07D277/54 , C07D209/16 , C07D295/12 , C07D307/82 , A61K31/343 , A61K31/381 , A61K31/415 , A61K31/4162 , A61K31/427 , A61K31/437 , A61K31/4704 , A61K31/4709 , A61K31/4741 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/166 , A61K31/216 , A61K31/4045 , A61K31/4152 , A61K31/426 , A61K31/4355 , A61K31/436 , A61K31/47 , G01N33/50
CPC分类号： A61K31/519 , A61K31/166 , A61K31/216 , A61K31/343 , A61K31/381 , A61K31/4045 , A61K31/415 , A61K31/4152 , A61K31/4162 , A61K31/4192 , A61K31/426 , A61K31/427 , A61K31/4355 , A61K31/436 , A61K31/437 , A61K31/47 , A61K31/4704 , A61K31/4709 , A61K31/4741 , A61K31/495 , A61K31/496 , A61K31/506 , A61K31/517 , C07D209/16 , C07D231/08 , C07D249/06 , C07D277/18 , C07D277/54 , C07D295/12 , C07D307/82 , C07D333/38 , C07D401/12 , C07D403/04 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04 , C07D491/04 , C07D495/04 , G01N33/502 , G01N2333/46 , G01N2500/10
摘要： Positive allosteric modulators of melanocortin receptors, especially allosteric potentiators of the receptors MC3R and MC4R are described herein. Also provided are pharmaceutical compositions containing the positive allosteric modulators and methods of treating obesity or an obesity-related disorder such as type 2 diabetes, comprising administering an effective amount of the positive allosteric modulator.
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公开(公告)号：US11856955B2
公开(公告)日：2024-01-02
申请号：US17003327
申请日：2020-08-26
发明人： Laurence J. Zwiebel , Ian M. Romaine , Sam Ochieng , Alex Gregory Waterson , Gary A. Sulikowski
IPC分类号： A01N43/653 , A01N33/06
CPC分类号： A01N43/653 , A01N33/06 , A01N2300/00 , A01N43/653 , A01N25/18 , A01N33/06 , A01N33/06 , A01N25/18
摘要： In one aspect, the invention relates to binary compositions that disrupt ORco-mediated odorant sensing. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in organisms that express ORco receptors such as airborne insects, e.g., mosquitos, and ticks. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US20190308991A1
公开(公告)日：2019-10-10
申请号：US16379100
申请日：2019-04-09
IPC分类号： C07D493/10 , G01N21/64 , G01N33/68
摘要： Provided are novel rhodol-based compounds, the preparation method thereof, and use thereof in Tl+ flux assays. The disclosed compounds may be used as more red-shifted and less pH-sensitive variants of Thallos.
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公开(公告)号：US20190075798A1
公开(公告)日：2019-03-14
申请号：US16186106
申请日：2018-11-09
发明人： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC分类号： A01N43/653 , C07D491/048 , C07D491/056 , A01N25/08 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D513/04 , C07D491/052 , A01N43/82 , A01N43/90 , A01N43/78 , A01N25/34 , A01N27/00 , A01N29/02 , A01N33/18 , A01N33/22 , A01N47/08 , A01N47/14 , A01N57/12 , A01N57/14 , A01N57/16
摘要： In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitoes. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US11519859B2
公开(公告)日：2022-12-06
申请号：US16379100
申请日：2019-04-09
IPC分类号： G01N21/64 , G01N33/68 , C07D493/10 , C09B11/24 , G01N33/84
摘要： Provided are novel rhodol-based compounds, the preparation method thereof, and use thereof in Tl+ flux assays. The fluorescent thallium ion sensor compounds have a rhodol fluorophore attached to an amino dicarboxylic acid metal binding moiety. The compounds are prepared in the “pro-dye” form, with the rhodol oxygen and the carboxylic acids of the metal binding unit masked by protecting groups. The disclosed compounds may be used as more red-shifted and less pH-sensitive variants of Thallos.
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公开(公告)号：US20210219551A1
公开(公告)日：2021-07-22
申请号：US16945369
申请日：2020-07-31
发明人： Laurence Zwiebel , Gregory M. Pask , David C. Rinker , Ian M. Romaine , Gary A. Sulikowski , Paul R. Reid , Alex G. Waterson , Kwangho Kim , Patrick L. Jones , Robert W. Taylor
IPC分类号： A01N43/653 , A01N43/82 , A01N43/78 , A01N43/90 , A01N25/08 , A01N47/16 , A01N47/18 , A01N53/00 , C07D249/12 , C07D401/04 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/14 , C07D471/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D513/04
摘要： In one aspect, the invention relates to chemical modulators of insect olfactory receptors. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in airborne insects such as mosquitos. Methods of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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公开(公告)号：US10791739B2
公开(公告)日：2020-10-06
申请号：US15561427
申请日：2016-03-24
发明人： Laurence J. Zwiebel , Ian M. Romaine , Sam Ochieng , Alex Gregory Waterson , Gary A. Sulikowski
IPC分类号： A01N43/653 , A01N33/06
摘要： In one aspect, the invention relates to binary compositions that disrupt ORco-mediated odorant sensing. In particular, compounds and compositions are provided that can inhibit sensory (e.g., host targeting) functions in organisms that express ORco receptors such as airborne insects, e.g., mosquitoes, and ticks. Method of employing such agents, and articles incorporating the same, are also provided. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
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