公开(公告)号：US11312733B2

公开(公告)日：2022-04-26

申请号：US17074717

申请日：2020-10-20

Applicant: California Institute of Technology

Inventor： Anton Toutov ,  Kerry Betz ,  Alexey Fedorov ,  Brian M. Stoltz ,  Wenbo Liu ,  Robert H. Grubbs

IPC: C07F7/08 ,  C07D209/12

Abstract: The present disclosure describes methods for silylating aromatic derivatives, comprising the use of hydrosilanes and potassium hydroxide.

公开(公告)号：US20220119377A1

公开(公告)日：2022-04-21

申请号：US17566919

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).

公开(公告)号：US20220106325A1

公开(公告)日：2022-04-07

申请号：US17263453

申请日：2019-07-26

Applicant: California Institute of Technology ,  The Regents Of The University Of California ,  1200 Pharma LLC

Inventor： Brendan M. O'Boyle ,  Justin A. Hilf ,  Scott C. Virgil ,  Alexander W. Sun ,  Brian M. Stoltz ,  Dylan Conklin ,  Martina S. McDermott ,  Neil A. O'Brien ,  Michael J. Palazzolo ,  Dennis Slamon ,  Michael D. Bartberger

IPC: C07D491/107 ,  C07D413/14 ,  C07D498/10 ,  C07D401/14 ,  C07D495/10 ,  A61P35/00

Abstract: The present disclosure provides compounds and compositions that are CDK inhibitors selective for CDK4 and/or CDK6, and methods of use thereof.

公开(公告)号：US20220002294A1

公开(公告)日：2022-01-06

申请号：US17294225

申请日：2019-11-15

Applicant: California Institute of Technology ,  1200 Pharma LLC ,  The Regents of the University of California

Inventor： Corey M. Reeves ,  Brandan M. O'Boyle ,  Justin A. Hilf ,  Dylan Conklin ,  Martina S. McDermott ,  Neil A. O'Brien ,  Michael J. Palazzolo ,  Dennis Slamon ,  Steven J. Wittenberger ,  Oliver C. Loson ,  Michael D. Bartberger ,  Brian M. Stoltz

IPC: C07D471/04 ,  C07D519/00

Abstract: The present disclosure provides compounds and compositions that are inhibitors of ERK1, ERK2, or both, and methods of use thereof.

公开(公告)号：US20210323983A1

公开(公告)日：2021-10-21

申请号：US17332394

申请日：2021-05-27

Applicant: California Institute Of Technology

Inventor： Anton Toutov ,  Wenbo Liu ,  David P. Schuman ,  Brian M. Stoltz ,  Robert H. Grubbs

IPC: C07F7/08 ,  C07F7/18

Abstract: The present disclosure is directed to methods of silylating organic substrates containing C—H or O—H bonds. In some embodiments, the methods use compositions that are derived from the preconditioning of mixtures of hydrosilanes or organodisilanes with bases, including metal hydroxide, metal alkoxide, metal silanoates, potassium amides, and/or graphitic potassium bases.

公开(公告)号：US20210155592A1

公开(公告)日：2021-05-27

申请号：US17164204

申请日：2021-02-01

Applicant: California Institute of Technology

Inventor： Brian M. Stoltz ,  Scott C. Virgil ,  David E. White ,  Taiga Yurino ,  Yiyang Liu ,  Douglas C. Behenna ,  Douglas Duquette ,  Christian Eidamshaus

IPC: C07D211/78 ,  C07D265/32 ,  C07D211/60 ,  C07D207/16 ,  C07D223/10 ,  C07D309/04 ,  C07D223/04 ,  C07D241/04 ,  C07D241/08 ,  C07D241/52 ,  C07D207/06 ,  C07D265/30 ,  C07D207/08 ,  C07D207/10 ,  C07D207/26 ,  C07D207/263 ,  C07D207/27 ,  C07D207/46 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/38 ,  C07D211/76 ,  C07D211/88 ,  C07D211/94 ,  C07D211/96 ,  C07D309/30 ,  C07D207/267 ,  C07D207/273 ,  C07D207/277 ,  C07D211/90

Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.

公开(公告)号：US10745354B2

公开(公告)日：2020-08-18

申请号：US16511138

申请日：2019-07-15

Applicant: California Institute of Technology

Inventor： Brian M. Stoltz ,  Aurapat Ngamnithiporn ,  Carina I. Jette ,  Shoshana Bachman ,  Scott C. Virgil ,  Sebastian Lackner

IPC: C07C69/75 ,  C07D211/86 ,  C07D407/06 ,  C07D409/06 ,  C07D309/30 ,  C07D211/76 ,  B01J31/24 ,  C07D309/32 ,  C07B37/04

Abstract: The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic α-quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation.

公开(公告)号：US20200157102A1

公开(公告)日：2020-05-21

申请号：US16692518

申请日：2019-11-22

Applicant: California Institute of Technology

Inventor： Brian M. Stoltz ,  Eric R. Welin ,  Scott C. Virgil ,  Pamela Tadross ,  Gerit M. Pototschnig ,  Aurapat (Fa) Ngamnithiporn ,  Kenji Negoro ,  Guillaume Lapointe ,  Max Klatte ,  Christopher Haley ,  Christian Gruenanger ,  Emil Glibstrup ,  Christopher Gilmore ,  Kevin McCormack Allan

IPC: C07D471/18 ,  C07D401/04 ,  A61P35/00

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.

公开(公告)号：US10343996B2

公开(公告)日：2019-07-09

申请号：US16049434

申请日：2018-07-30

Applicant: California Institute of Technology

Inventor： Brian M. Stoltz ,  Scott C. Virgil ,  David E. White ,  Taiga Yurino ,  Yiyang Liu ,  Douglas C. Behenna ,  Douglas Duquette ,  Christian Eidamshaus

IPC: C07D211/78 ,  C07D211/16 ,  C07D211/18 ,  C07D211/22 ,  C07D211/34 ,  C07D211/38 ,  C07D211/60 ,  C07D211/76 ,  C07D211/88 ,  C07D211/90 ,  C07D211/94 ,  C07D211/96 ,  C07D207/06 ,  C07D207/08 ,  C07D207/10 ,  C07D207/16 ,  C07D207/26 ,  C07D207/263 ,  C07D207/267 ,  C07D207/27 ,  C07D207/273 ,  C07D207/277 ,  C07D207/46 ,  C07D223/04 ,  C07D223/10 ,  C07D241/04 ,  C07D241/08 ,  C07D265/30 ,  C07D265/32 ,  C07D309/04 ,  C07D309/30 ,  C07D241/52

Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.

公开(公告)号：US10336678B2

公开(公告)日：2019-07-02

申请号：US15977638

申请日：2018-05-11

Applicant: California Institute of Technology

Inventor： Samantha E. Shockley ,  John C. Hethcox ,  Brian M. Stoltz

IPC: C07C51/08 ,  C07C57/03 ,  C07C67/22 ,  C07C69/52 ,  C07C233/09 ,  B01J31/12 ,  B01J31/18 ,  C07C231/18 ,  C07C201/12 ,  C07C253/30 ,  C07C67/00

Abstract: The present disclosure provides methods for enantioselective synthesis of acyclic α-quaternary carboxylic acid derivatives via iridium-catalyzed allylic alkylation.