公开(公告)号：US12180248B2

公开(公告)日：2024-12-31

申请号：US18169964

申请日：2023-02-16

Applicant: Sage Therapeutics, Inc.

Inventor： Gabriel Martinez Botella ,  Francesco G. Salituro ,  Albert Jean Robichaud ,  Boyd L. Harrison

IPC: C07J75/00 ,  A61K9/00 ,  A61K31/58 ,  A61P25/00 ,  C07D231/14 ,  C07D249/04 ,  C07D249/18 ,  C07D295/033 ,  C07J9/00 ,  C07J13/00 ,  C07J43/00

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein, R1, R2a, R2b, R3 and A are as defined herein. Such compounds are envisioned, in certain embodiments, to behave as GABA modulators. The present invention also provides pharmaceutical compositions comprising a compound of the present invention and methods of use and treatment, e.g., such for inducing sedation and/or anesthesia.

公开(公告)号：US11472833B2

公开(公告)日：2022-10-18

申请号：US17256777

申请日：2019-07-03

Applicant: Drawbridge Pharmaceuticals Pty Ltd

Inventor： Ian Edmonds ,  Edward J. Hessler

IPC: C07J75/00 ,  B01J23/46 ,  C07J7/00 ,  B01J23/44

Abstract: Neuroactive steroid anaesthetic agents, methods for their preparation and compositions comprising the same are disclosed. Also provided are scaled up and/or GMP methods for preparing neuroactive steroids, such as alfaxalone, alfadolone and alfadolone acetate.

公开(公告)号：US20210188898A1

公开(公告)日：2021-06-24

申请号：US17191281

申请日：2021-03-03

Applicant: Trustees of Dartmouth College

Inventor： Glenn C. Micalizio

IPC: C07J75/00 ,  C07J1/00

Abstract: The present disclosure relates to stereodefined polycyclic (e.g., tetracyclic) compounds that contain quaternary centers at one or multiple ring fusions, synthetic methods for preparing such compounds, and methods of using such compounds to treat a disease, such as a brain tumor and, particularly, a glioma.

公开(公告)号：US11008363B2

公开(公告)日：2021-05-18

申请号：US16856374

申请日：2020-04-23

Applicant: ALLERGAN SALES, LLC

Inventor： Achampeta Rathan Prasad ,  Roy A. Swaringen, Jr. ,  John Gregory Reid ,  Robert M. Moriarty ,  Akhila Kumar Sahoo

IPC: C07J9/00 ,  C07J75/00 ,  C07J1/00 ,  C07J13/00

Abstract: Synthetic methods for preparing deoxycholic acid and intermediates thereof are provided.

公开(公告)号：US10800730B2

公开(公告)日：2020-10-13

申请号：US16136830

申请日：2018-09-20

Applicant: The Board of Trustees of the University of Illinois

Inventor： Paul J. Hergenrother ,  Robert W. Huigens, III ,  Karen C. Morrison ,  Robert W. Hicklin, II ,  Timothy A. Flood, Jr.

IPC: C07C69/757 ,  C07J21/00 ,  C07J69/00 ,  C07J71/00 ,  C07J73/00 ,  C07J75/00 ,  C07D401/14 ,  C07D311/94 ,  C07D313/06 ,  C07D223/14 ,  C07D401/04 ,  C07D471/04 ,  C07D471/08 ,  C07D493/08 ,  C07D513/04 ,  C07D519/00 ,  C07C59/205 ,  C07C62/32 ,  C07C62/38 ,  C07D303/10 ,  C07B37/06 ,  C07B37/08 ,  C07D307/93 ,  C07D313/08 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06

Abstract: The invention provides a novel, general, and facile strategy for the creation of small molecules with high structural and stereochemical complexity. Aspects of the methods include ring system distortion reactions that are systematically applied to rapidly convert readily available natural products to structurally complex compounds with diverse molecular architectures. Through evaluation of chemical properties including fraction of sp3 carbons, ClogP, and the number of stereogenic centers, these compounds are shown to be significantly more complex and diverse than those in standard screening collections. This approach is demonstrated with natural products (gibberellic acid, adrenosterone, and quinine) from three different structural classes, and methods are described for the application of this strategy to any suitable natural product.

公开(公告)号：US10597602B2

公开(公告)日：2020-03-24

申请号：US16073437

申请日：2017-01-26

Applicant: Stora Enso OYJ

Inventor： Jari Kavakka

IPC: C11B3/00 ,  B01D11/04 ,  C11B3/12 ,  D21C11/00 ,  C07J9/00 ,  B01D3/14 ,  C07J75/00

Abstract: The present invention relates to extraction of phytosterols from alkaline tall oil soap which is obtained from the Kraft process black liquor by skimming. In the method according to the present invention, phytosterols are extracted using dibromomethane, bromoform, tetrabromomethane or a combination thereof.

公开(公告)号：US10202413B2

公开(公告)日：2019-02-12

申请号：US14767235

申请日：2014-02-14

Applicant: Washington University

Inventor： Douglas Covey

IPC: A61K31/56 ,  A61K31/566 ,  A61K31/568 ,  A61K31/5685 ,  C07J1/00 ,  C07J21/00 ,  C07J15/00 ,  C07J41/00 ,  C07C35/42 ,  C07J13/00 ,  C07J31/00 ,  C07J51/00 ,  C07J61/00 ,  C07J63/00 ,  C07J71/00 ,  C07J75/00 ,  C07C43/307

Abstract: The present disclosure is generally directed to neuroactive enantiomeric 15-, 16- and 17-substituted steroids with additional optional substituents at carbons 3, 4, 6, 7, 10 and 13, and pharmaceutically acceptable salts thereof, for use as, for example, modulators for GABA type-A receptors. The present disclosure is further directed to pharmaceutical compositions comprising such compounds.

公开(公告)号：US20190010420A1

公开(公告)日：2019-01-10

申请号：US16073437

申请日：2017-01-26

Applicant: Stora Enso OYJ

Inventor： Jari Kavakka

IPC: C11B3/00 ,  C11B3/12 ,  C07J75/00 ,  B01D3/14 ,  B01D11/04

CPC classification number: C11B3/006 ,  B01D3/143 ,  B01D11/0492 ,  B01D2257/2062 ,  C07J9/00 ,  C07J75/00 ,  C11B3/12 ,  D21C11/00

Abstract: The present invention relates to extraction of phytosterols from alkaline tall oil soap which is obtained from the Kraft process black liquor by skimming. In the method according to the present invention, phytosterols are extracted using dibromomethane, bromoform, tetrabromomethane or a combination thereof.

公开(公告)号：US10072030B2

公开(公告)日：2018-09-11

申请号：US15375716

申请日：2016-12-12

Applicant: CALIFORNIA INSTITUTE OF TECHNOLOGY

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

IPC: C07F7/08 ,  C07J1/00 ,  C07J51/00 ,  C07F17/02 ,  C07J7/00 ,  C07J75/00

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, alkali metal alkoxide, or alkali metal hydride under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the presence or substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.

公开(公告)号：US20170088563A1

公开(公告)日：2017-03-30

申请号：US15375716

申请日：2016-12-12

Applicant: CALIFORNIA INSTITUTE OF TECHNOLOGY

Inventor： ANTON TOUTOV ,  KERRY BETZ ,  BRIAN M. STOLTZ ,  WENBO LIU ,  ROBERT H. GRUBBS

IPC: C07F7/08 ,  C07J75/00 ,  C07J7/00 ,  C07F17/02

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, alkali metal alkoxide, or alkali metal hydride under conditions sufficient to form a silylated terminal alkynyl moiety. The methods are operable in the presence or substantially absence of transition-metal compounds. The systems associated with these methods are also disclosed.