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公开(公告)号：US20250099443A1
公开(公告)日：2025-03-27
申请号：US18884373
申请日：2024-09-13
Applicant: California Institute of Technology
Inventor： Hao Yu , Zachary P. Sercel , Samir P. Rezgui , Jonathan Farhi , Brian M. Stoltz , Scott C. Virgil
IPC: A61K31/4375 , A61K31/437 , A61P35/00 , C07D471/06 , C07D519/00
Abstract: Disclosed herein are analogs and derivatives of aleutianamine and methods of making the same. Also disclosed herein are methods of treating pancreatic cancer comprising administration of aleutianamine or its analogs.
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公开(公告)号：US20220213081A1
公开(公告)日：2022-07-07
申请号：US17566915
申请日：2021-12-31
Applicant: California Institute of Technology
Inventor： Brian M. Stoltz , Alexander W. Sun , Stephan N. Hess , Carina I. Jette , Irina Geibel , Shoshana Bachman , Masaki Hayashi , Hideki Shimizu , Jeremy B. Morgan , Shunya Sakurai , Zachary P. Sercel
IPC: C07D413/14 , C07D207/26 , C07D243/08 , C07D239/06 , C07D507/00 , C07D241/08
Abstract: Described here are transition metal-catalyzed enantioselective arylation and vinylation reactions of α-substituted lactams, such as γ-lactams. The use of various electrophiles and ligands are described, and result in the construction of α-quaternary centers in good yields (up to 91% yield) and high enantioselectivities (up to 97% ee).
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3.发明申请公开(公告)号：US20200157020A1
公开(公告)日：2020-05-21
申请号：US16579382
申请日：2019-09-23
Applicant: California Institute of Technology
Inventor： Brian M. Stoltz , Yoshitaka Numajiri , Beau P. Pritchett , Koji Chiyoda
IPC: C07B53/00 , C07D209/88 , C07D265/32 , C07D211/76 , C07D211/74 , C07C271/18 , C07C311/16 , C07C271/50 , C07C233/76
Abstract: This invention provides enantioenriched Mannich adducts with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
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公开(公告)号：US10526334B2
公开(公告)日：2020-01-07
申请号：US16038968
申请日：2018-07-18
Applicant: California Institute of Technology
Inventor： Brian M. Stoltz , Eric R. Welin , Scott C. Virgil , Pamela Tadross , Gerit Maria Pototschnig , Aurapat (Fa) Ngamnithiporn , Kenji Negoro , Guillaume Lapointe , Max Klatte , Christopher Haley , Christian Gruenanger , Emil Glibstrup , Christopher Gilmore , Kevin McCormack Allan
IPC: C07D471/18 , A61P35/00 , C07D401/04
Abstract: (−)-Jorumycin, ecteinascidin 743, saframycin A and related compounds, methods of preparing the same, formulations comprising the compounds, and methods of treating proliferative diseases with the same are provided.
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公开(公告)号：US10106479B2
公开(公告)日：2018-10-23
申请号：US15081157
申请日：2016-03-25
Applicant: California Institute of Technology
Inventor： Brian M. Stoltz , Alexander N. Marziale , Robert A. Craig , Douglas Duquette , Kelly E. Kim , Marc Liniger , Yoshitaka Numajiri
IPC: C07D211/94 , C07C45/65 , C07D223/10 , C07D317/72 , B01J31/04
Abstract: This invention provides efficient and scalable enantioselective methods that yield 2-alkyl-2-allylcycloalkyanone compounds with quaternary stereogenic centers. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II) or (III): with a palladium (II) catalyst under alkylation conditions.
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Patent Agency Ranking
公开(公告)号：US09764995B2
公开(公告)日：2017-09-19
申请号：US15375747
申请日：2016-12-12
Applicant: CALIFORNIA INSTITUTE OF TECHNOLOGY
Inventor： Anton Toutov , Wenbo Liu , Brian M. Stoltz , Robert H. Grubbs , Kerry Betz , David P. Schuman
CPC classification number: C07B47/00 , C07D209/12 , C07F5/04 , C07F7/0827
Abstract: The present invention describes chemical systems and methods for silylating heteroaromatic organic substrates using at least alkoxide base, preferably a potassium alkoxide base and at least one organodisilane and (b) at least one alkoxide base. Both methods and compositions for affecting these transformations are disclosed.
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公开(公告)号：US09556206B2
公开(公告)日：2017-01-31
申请号：US14841964
申请日：2015-09-01
Applicant: CALIFORNIA INSTITUTE OF TECHNOLOGY
Inventor： Anton Toutov , Kerry Betz , Brian M. Stoltz , Wenbo Liu , Robert H. Grubbs
CPC classification number: C07F7/0827 , C07F17/02 , C07J1/0096 , C07J7/0005 , C07J51/00 , C07J75/00
Abstract: The present invention is directed to a mild, efficient, and general direct C(sp)-H bond silylation. Various embodiments includes methods, each method comprising or consisting essentially of contacting at least one organic substrate comprising a terminal alkynyl C—H bond, with a mixture of at least one organosilane and an alkali metal hydroxide, under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.
Abstract translation: 本发明涉及温和，有效和通用的直接C（sp）-H键甲硅烷基化。 各种实施方案包括方法，每种方法包括或基本上包括使至少一种包含末端炔基C-H键的有机底物与至少一种有机硅烷和碱金属氢氧化物的混合物在足以形成甲硅烷基化的末端炔基的条件下 部分。 所述方法在基本上不存在过渡金属化合物的情况下是可操作的。 还公开了与这些方法相关联的系统。
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8.发明授权Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof 有权手性烯胺酮的合成及其衍生物及其生物活性研究公开(公告)号：US09518034B2
公开(公告)日：2016-12-13
申请号：US14514001
申请日：2014-10-14
Applicant: California Institute of Technology
Inventor： Brian M. Stoltz , Dennis A. Dougherty , Douglas Duquette , Noah Duffy
IPC: C07D295/116 , C07D209/88
CPC classification number: C07D295/116 , C07D209/88
Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
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9.发明授权Synthetic transtaganolide and basiliolide products, derivatives thereof, and synthesis methods thereof 有权合成的转铁蛋白和巴利内酯产物及其衍生物及其合成方法公开(公告)号：US08912347B2
公开(公告)日：2014-12-16
申请号：US13929425
申请日：2013-06-27
Applicant: California Institute of Technology
Inventor： Hosea Nelson , Kei Murakami , Scott C. Virgil , Brian M. Stoltz , Jonathan R. Gordon
IPC: C07D313/06 , C07D311/78 , C07D493/16 , C07D493/08 , C07D493/18
CPC classification number: C07D311/00 , C07D493/08 , C07D493/16 , C07D493/18
Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.
Abstract translation: 提供由式I表示的化合物，其包括合成的经斯曲肽内酯和巴利内酯产物。 还提供了这些化合物的衍生物和合成方法。
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10.发明申请SYNTHETIC TRANSTAGANOLIDE AND BASILIOLIDE PRODUCTS, DERIVATIVES THEREOF, AND SYNTHESIS METHODS THEREOF 有权合成三羟甲基氨丙菊酯和赖氨酸产品，其衍生物及其合成方法公开(公告)号：US20140005416A1
公开(公告)日：2014-01-02
申请号：US13929425
申请日：2013-06-27
Applicant: California Institute of Technology
Inventor： Hosea Nelson , Kei Murakami , Scott C. Virgil , Brian M. Stoltz , Jonathan R. Gordon
IPC: C07D493/16 , C07D493/08
CPC classification number: C07D311/00 , C07D493/08 , C07D493/16 , C07D493/18
Abstract: Compounds represented by Formula I are provided that include synthetic transtaganolide and basiliolide products. Derivatives of these compounds and methods of synthesis are also provided.
Abstract translation: 提供由式I表示的化合物，其包括合成的经斯曲肽内酯和巴利内酯产物。 还提供了这些化合物的衍生物和合成方法。
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