公开(公告)号：US20230018615A1

公开(公告)日：2023-01-19

申请号：US17818873

申请日：2022-08-10

Applicant: Trustees of Dartmouth College

Inventor： Glenn C. Micalizio

IPC: C07J11/00 ,  A61P35/00 ,  C07J75/00 ,  C07J15/00

Abstract: Methods for producing enantiodefined polycyclic compounds, particularly tetracyclic compounds, are provided. More particularly, synthetic methods for producing biologically active enantiodefined steroidal compositions of both natural (“nat-”) and unnatural (“ent-”) absolute stereochemistry are provided. An exemplary method for manufacturing a tetracyclic compound comprises a step of forming a hydrindane intermediate through coupling of a suitably functionalized enyne with a suitably functionalized alkyne and subsequently performing an intramolecular ring-closing reaction to form the tetracyclic compound. Steroidal compounds obtained by this method and methods of using such steroidal compounds in human and/or animal therapeutics and medicines are also provided.

公开(公告)号：US11530237B2

公开(公告)日：2022-12-20

申请号：US16748117

申请日：2020-01-21

Applicant: Sage Therapeutics, Inc.

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

IPC: C07J43/00 ,  C07J1/00 ,  C07J7/00 ,  A61K31/58 ,  A61K31/575 ,  A61P23/00 ,  A61P25/00 ,  A61P25/06 ,  A61P25/08 ,  A61P25/14 ,  A61P25/18 ,  A61P25/20 ,  A61K45/06 ,  C07J9/00 ,  C07J3/00 ,  C07J5/00 ,  C07J11/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J51/00 ,  C07J71/00

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein , A, R1, R2, R3a, R4a, R4b, R5, R7a, and R7b 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：US20210101927A1

公开(公告)日：2021-04-08

申请号：US17025475

申请日：2020-09-18

Applicant: Intercept Pharmaceuticals, Inc.

Inventor： Roberto Pellicciari ,  Antimo Gioiello

IPC: C07J11/00 ,  A61K47/54

Abstract: The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.

公开(公告)号：US10323059B2

公开(公告)日：2019-06-18

申请号：US15698151

申请日：2017-09-07

Applicant: Sage Therapeutics, Inc.

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

IPC: C07J41/00 ,  A61K45/06 ,  A61K31/56 ,  A61K31/565 ,  A61K31/567 ,  C07J1/00 ,  C07J5/00 ,  C07J11/00 ,  C07J21/00 ,  C07J31/00 ,  C07J51/00 ,  C07J71/00

Abstract: Described herein are neuroactive steroids of the Formula (I): or a pharmaceutically acceptable salt thereof; wherein R1a and R1b 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：US20190092807A1

公开(公告)日：2019-03-28

申请号：US16081835

申请日：2017-03-02

Applicant: BIONICE, S.L.U

Inventor： Celso Miguel SANDOVAL RODRÍGUEZ ,  Ignacio HERRÁIZ SIERRA ,  lvano MESSINA ,  Jesús Miguel IGLESIAS RETUERTO

IPC: C07J11/00

Abstract: The invention relates to a process for the preparation of 11-methylene steroids through selective olefination of the ketone at position 11. The resulting products are useful intermediates in the preparation of several pharmaceutically active agents, such as Etonogestrel and Desogestrel.

公开(公告)号：US20190002493A1

公开(公告)日：2019-01-03

申请号：US16124122

申请日：2018-09-06

Applicant: Intercept Pharmaceuticals, Inc.

Inventor： Roberto Pellicciari ,  Antimo Gioiello

IPC: C07J11/00 ,  A61K47/54 ,  C07J31/00 ,  C07J9/00

Abstract: The present application provides Compound 1: or a pharmaceutically acceptable salt or amino acid conjugate thereof. The present invention relates to an FXR activator and to methods of making and using said compound.

公开(公告)号：US10053485B2

公开(公告)日：2018-08-21

申请号：US15077099

申请日：2016-03-22

Applicant: Evestra, Inc.

Inventor： Hareesh Nair ,  Bindu Santhamma ,  Klaus Nickisch

IPC: C07J1/00 ,  C07J11/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J21/00 ,  C07J51/00 ,  C07J71/00

CPC classification number: C07J1/0096 ,  C07J11/00 ,  C07J21/006 ,  C07J31/006 ,  C07J41/0083 ,  C07J43/003 ,  C07J51/00 ,  C07J71/001

Abstract: Described herein are new anti-cancer compounds and methods of using such compounds, acting through a new mechanism of action by simultaneous inhibition of leukemia inhibitory factor (LIF) and MDM2.

公开(公告)号：US10040816B2

公开(公告)日：2018-08-07

申请号：US15012471

申请日：2016-02-01

Applicant: INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE) ,  UNIVERSITE DE BORDEAUX

Inventor： Pier Vincenzo Piazza ,  Monique Vallee ,  Giovanni Marsicano ,  Francois-Xavier Felpin ,  Luigi Bellocchio ,  Daniela Cota ,  Jean-Michel Revest ,  Sergio Vitiello ,  Umberto Spampinato ,  Rafael Maldonado

IPC: C07J7/00 ,  C07J31/00 ,  C07J41/00 ,  C07J5/00 ,  C07J11/00 ,  C07J13/00 ,  A61K31/57

Abstract: The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases.

公开(公告)号：US20170265510A1

公开(公告)日：2017-09-21

申请号：US15610958

申请日：2017-06-01

Applicant: BASF SE

Inventor： THOMAS SUBKOWSKI ,  Claus Bollschweiler ,  Jens Wittenberg ,  Wolfgang Siegel ,  Ralf Pelzer

IPC: A23L27/20 ,  A23L27/00 ,  A61K8/35 ,  A61K8/49 ,  A61K8/55 ,  A61Q19/00 ,  C07C49/665 ,  C07C49/675 ,  C07D209/48 ,  C07D311/78 ,  C07D311/94 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D471/04 ,  C07D491/20 ,  C07D493/10 ,  C07D495/10 ,  C07D495/20 ,  C07F9/572 ,  C07J33/00 ,  C07J63/00 ,  C07J73/00 ,  C07J11/00

CPC classification number: A23L27/2056 ,  A23L27/88 ,  A61K8/35 ,  A61K8/49 ,  A61K8/492 ,  A61K8/4926 ,  A61K8/498 ,  A61K8/4986 ,  A61K8/55 ,  A61K2800/244 ,  A61Q19/00 ,  C07C49/665 ,  C07C49/675 ,  C07C2603/26 ,  C07D209/48 ,  C07D311/78 ,  C07D311/94 ,  C07D339/06 ,  C07D339/08 ,  C07D405/06 ,  C07D471/04 ,  C07D491/20 ,  C07D493/10 ,  C07D495/10 ,  C07D495/20 ,  C07F9/5728 ,  C07J11/00 ,  C07J33/007 ,  C07J63/008 ,  C07J73/003

Abstract: The invention relates to new types of modulators of the cold menthol receptor TRPM8, to methods of modulating the TRPM8 receptor using these modulators; and in particular the use of the modulators for inducing a sensation of coldness; and also the articles and compositions produced using these modulators.

公开(公告)号：US20170190731A1

公开(公告)日：2017-07-06

申请号：US15314771

申请日：2015-05-28

Applicant: BAR PHARMACEUTICALS S.R.L.

Inventor： Angela Zampella ,  Stefano Fiorucci

IPC: C07J31/00 ,  C07J11/00 ,  C07J9/00

CPC classification number: C07J31/006 ,  C07J9/00 ,  C07J9/005 ,  C07J11/00 ,  C07J41/0094

Abstract: The present invention relates to compounds having cholane scaffolds of formula (I), said compounds for use in the treatment and/or prevention of FXR and TGR5/GPBAR1 mediated diseases.