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1.发明授权公开(公告)号：US11691958B2
公开(公告)日：2023-07-04
申请号：US17455014
申请日：2021-11-15
发明人： Karl A. Scheidt , Ansoo Lee , Richard C. Betori
IPC分类号： C07D309/30 , C07D409/06 , C07D405/06 , B01J31/18
CPC分类号： C07D309/30 , C07D405/06 , C07D409/06
摘要： Disclosed are enantioselective cross dehydrogenative coupling reactions for synthesizing tetrahydropyran compounds. Novel tetrahydropyran compounds may be synthesized by the disclosed methods as well as tetrahydropyran precursor compounds for synthesizing various naturally occurring compounds. The enantioselective cross dehydrogenative coupling reactions utilize in situ Lewis Acid activation in combination with oxidative formation of an oxocarbenium ion to provide a highly efficient and selective coupling reaction for synthesizing tetrahydropyran compounds.
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2.发明申请公开(公告)号：US20220259171A1
公开(公告)日：2022-08-18
申请号：US17455014
申请日：2021-11-15
发明人： Karl A. Scheidt , Ansoo Lee , Richard C. Betori
IPC分类号： C07D309/30 , C07D409/06 , C07D405/06
摘要： Disclosed are enantioselective cross dehydrogenative coupling reactions for synthesizing tetrahydropyran compounds. Novel tetrahydropyran compounds may be synthesized by the disclosed methods as well as tetrahydropyran precursor compounds for synthesizing various naturally occurring compounds. The enantioselective cross dehydrogenative coupling reactions utilize in situ Lewis Acid activation in combination with oxidative formation of an oxocarbenium ion to provide a highly efficient and selective coupling reaction for synthesizing tetrahydropyran compounds.
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3.发明申请公开(公告)号：US20210214352A1
公开(公告)日：2021-07-15
申请号：US16766217
申请日：2019-10-02
IPC分类号： C07D471/04 , A61P25/36 , A61P25/18 , A61P25/28 , A61P3/04
摘要： Disclosed are novel small molecules, methods of synthesis of the small molecules, and uses of the small molecules for modulating activity of the human serotonin receptor 2C (5-HT2c), preferably selectively. The small molecules have a substituted beta-carboline core structure, which optionally may be saturated at one or more bonds to provide a dihydro-beta-carboline core or a tetrahydro-beta-carboline core. The small molecules may be administered to treat and/or prevent diseases, disorders, and/or conditions associated with human serotonin receptor 2C (5-HT2C) including psychiatric, mental, and/or neurological diseases, disorders, and conditions such as cognitive impairment, addiction, and obsessive compulsive disorder. The disclosed small molecules also may be administered to treat and/or prevent obesity, for example, via appetite suppression.
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4.发明申请公开(公告)号：US20210070725A1
公开(公告)日：2021-03-11
申请号：US16986718
申请日：2020-08-06
发明人： Karl A. Scheidt , Rick C. Betori
IPC分类号： C07D309/32 , C07D405/06
摘要： Disclosed are 3-methylideneoxan-4-one compounds, derivatives thereof, and methods of their synthesis and methods of their use in treating a disease or disorder in a subject in need thereof, such as diseases and disorders that are associated with telomerase activity such as cancer. The disclosed compounds may be formulated in a pharmaceutical composition for treating diseases and disorders that are associated with telomerase activity such as cancer.
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5.发明申请公开(公告)号：US20210024473A1
公开(公告)日：2021-01-28
申请号：US16920566
申请日：2020-07-03
发明人： Karl A. Scheidt , Ansoo Lee
IPC分类号： C07D265/22 , C07D413/04 , C07D215/233 , C07D265/16
摘要： Disclosed are dihydrobenzoxazinone compounds, dihydroquinolone compounds, and methods of their synthesis. The disclosed compounds may be prepared by reacting a benzoxazinedione compound and a ketone compound in the presence of an N-heterocyclic carbine (NHC) catalyst to perform a NHC-catalyzed decarboxylative cycloaddition. The disclosed compounds may be utilized to treat diseases and disorders associated with the biological activity of dihydrobenzoxazinone compounds and dihydroquinolone compounds.
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公开(公告)号：US10654865B2
公开(公告)日：2020-05-19
申请号：US16439638
申请日：2019-06-12
IPC分类号： C07D491/052 , C07D211/02 , C07D211/32 , C07C311/19
摘要： Enantioselective syntheses of cis- and trans-bicyclic dihydropyran compounds, and other intermediates, en route to heteroyohimbine alkaloids.
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公开(公告)号：US20180153853A1
公开(公告)日：2018-06-07
申请号：US15839322
申请日：2017-12-12
发明人： Raymond C. Bergan , Karl A. Scheidt , Li Xu
IPC分类号： A61K31/353 , A61K31/4188 , A61K45/06
CPC分类号： A61K31/353 , A61K31/167 , A61K31/4188 , A61K45/06 , A61K2300/00
摘要： Provided herein are compositions and methods for inhibiting cancer cell motility and/or metastasis. In particular embodiments, KBU2046 (or an analog thereof) and one or more additional therapies (e.g., cancer therapies (e.g., hormone therapies and chemotherapies) are provided to inhibit cancer cell motility, inhibit metastasis, and/or treat cancer (e.g., prostate cancer, lung cancer, breast cancer, colon cancer, etc.).
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公开(公告)号：US09527812B2
公开(公告)日：2016-12-27
申请号：US14701814
申请日：2015-05-01
IPC分类号： C07D209/08 , C07D409/04 , C07D401/04 , C07D209/10 , C07D209/14 , C07D209/12 , C07D209/26
CPC分类号： C07D209/08 , C07D209/10 , C07D209/12 , C07D209/14 , C07D209/26 , C07D401/04 , C07D409/04
摘要： Transition metal-free catalytic methods for access to 2-arylindole compounds.
摘要翻译： 用于进入2-芳基吲哚化合物的无金属过渡催化方法。
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9.发明授权公开(公告)号：US11840514B2
公开(公告)日：2023-12-12
申请号：US17027687
申请日：2020-09-21
发明人： Karl A. Scheidt , Brice Uno
IPC分类号： C07D207/416 , B01J31/18 , C07D405/12 , C07D401/04
CPC分类号： C07D207/416 , B01J31/185 , C07D401/04 , C07D405/12 , B01J2231/348 , B01J2531/23
摘要： Disclosed are complexes and methods of using the complexes as catalysts for addition of amines to unsaturated electrophiles, as well as novel compounds produced by the disclosed complexes and methods. The disclosed methods may utilize the disclosed complexes as catalysts for adding unprotected primary amines and secondary amines to unsaturated electrophiles in an enantioselective manner to produce novel compounds which may include amino substituted succinimide compounds.
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10.发明公开公开(公告)号：US20230265093A1
公开(公告)日：2023-08-24
申请号：US18051300
申请日：2022-10-31
IPC分类号： C07D471/04 , A61P25/36 , A61P25/28 , A61P3/04 , A61P25/18
CPC分类号： C07D471/04 , A61P25/36 , A61P25/28 , A61P3/04 , A61P25/18
摘要： Disclosed are novel small molecules, methods of synthesis of the small molecules, and uses of the small molecules for modulating activity of the human serotonin receptor 2C (5-HT2c), preferably selectively. The small molecules have a substituted beta-carboline core structure, which optionally may be saturated at one or more bonds to provide a dihydro-beta-carboline core or a tetrahydro-beta-carboline core. The small molecules may be administered to treat and/or prevent diseases, disorders, and/or conditions associated with human serotonin receptor 2C (5-HT2c) including psychiatric, mental, and/or neurological diseases, disorders, and conditions such as cognitive impairment, addiction, and obsessive compulsive disorder. The disclosed small molecules also may be administered to treat and/or prevent obesity, for example, via appetite suppression.
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