公开(公告)号：US12215127B2

公开(公告)日：2025-02-04

申请号：US17231432

申请日：2021-04-15

Applicant: CORNELL UNIVERSITY

Inventor： Pamela Chang ,  Bibudha Parasar ,  Lin Han

IPC: C07J43/00 ,  G01N33/68

Abstract: A composition having the following structure: wherein: R1 is OH, ester group, ether group, amine, thiol, thioether, halide, or a group containing an alkynyl or azido functionality; R2 is H, OH, ester group, ether group, amine, thiol, thioether, halide, or a group containing an alkynyl or azido functionality; R3 is a group containing a reactive functionality capable of covalent binding to a thiol or amine; and R4 is H, OH, ester group, ether group, amine, thiol, thioether, halide, or a group containing an alkynyl or azido functionality; wherein one of R1, R2 and R4 is a group containing an alkynyl or azido functionality. Also disclosed is a method for profiling changes in BSH enzyme activity by attaching active BSH enzymes in a sample to the probe shown above, attaching a tag to the probe, and detecting the active BSH enzymes to obtain an activity profile.

公开(公告)号：US20250026781A1

公开(公告)日：2025-01-23

申请号：US18709256

申请日：2022-11-10

Applicant: Emory University

Inventor： Dennis Liotta ,  Russell Fritzemeier ,  Alet van der Westhuyzen ,  Luke E. Hodson ,  Gouthami Pashikanti

IPC: C07J41/00 ,  A61K31/57 ,  A61K31/58 ,  C07J43/00

Abstract: Prodrugs of neurosteroid analogs are disclosed. Pharmaceutical formulations containing the prodrugs are also disclosed. Additionally, methods of treating a condition, disorder, or disease using the prodrugs or their pharmaceutical formulations are disclosed. Exemplary conditions, disorders, and diseases relevant to this disclosure include stroke, subarachnoid hemorrhage, cerebral ischemia, cerebral vasospasm, hypoxia, CNS injury, concussion, traumatic brain injury, depression, postpartum depression, epilepsy, seizure disorder, essential tremor, fragile X syndrome, and neurodegenerative disease.

公开(公告)号：US12139508B2

公开(公告)日：2024-11-12

申请号：US16969133

申请日：2019-01-31

Applicant: JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD. ,  SHANGHAI HANSOH BIOMEDICAL CO., LTD.

Inventor： Yidong Su ,  Haining Deng ,  Xiaopo Chen ,  Rudi Bao ,  Fujun Zhang

IPC: C07J43/00 ,  C07J1/00 ,  C07J7/00 ,  C07J9/00 ,  C07J41/00

Abstract: Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound of formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator the of GABAA receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.

公开(公告)号：US12122804B2

公开(公告)日：2024-10-22

申请号：US17426951

申请日：2019-01-31

Applicant: SHENZHEN RENTAI PHARMATECH LTD.

Inventor： Guobin Ren ,  Weijie Ji ,  Dongxu Yi ,  Jiajun Huang

IPC: C07J7/00 ,  C07J43/00

CPC classification number: C07J7/009 ,  C07B2200/13 ,  C07J43/003

Abstract: A crystal form X of 3α-hydroxy-3β-methyl-21-(4-cyano-1H-pyrazol-1′-yl)-19-nor-5β-pregnan-20-one, a preparation method of said crystal form and an application thereof in preparing a drug for treatment of central nervous system disease.

公开(公告)号：US20240343755A1

公开(公告)日：2024-10-17

申请号：US18557899

申请日：2022-04-29

Applicant: ALCON INC.

Inventor： Mitchell A. deLong ,  Jill M. Sturdivant ,  Cynthia L. Lichorowic

IPC: C07J43/00 ,  A61K31/573 ,  A61K31/58 ,  A61K47/55 ,  A61P27/02 ,  C07J5/00 ,  C07J71/00

CPC classification number: C07J43/003 ,  A61K31/573 ,  A61K31/58 ,  A61K47/55 ,  A61P27/02 ,  C07J5/0053 ,  C07J5/0076 ,  C07J71/0031

Abstract: Provided herein are compounds and pharmaceutical compositions useful in modulating kinase activity, and related diseases. These compounds are conjugates of glucocorticoids with rho-kinase inhibitors. Also provided herein are methods of treating an eye disease or disorder in a subject. Also provided herein are methods of reducing intraocular pressure in a subject. Also provided herein are methods of modulating kinase activity in a cell. Also provided herein are methods of making the compounds provided herein, and compounds useful for the preparation of the compounds provided herein.

公开(公告)号：US20240317729A1

公开(公告)日：2024-09-26

申请号：US18667078

申请日：2024-05-17

Applicant: YALE UNIVERSITY ,  GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  CAMBRIDGE ENTERPRISE LIMITED

Inventor： CRAIG M. CREWS ,  DENNIS BUCKLEY ,  ALESSIO CIULLI ,  WILLIAM L. JORGENSEN ,  PETER C. GAREISS ,  INGE VAN MOLLE ,  JEFFREY GUSTAFSON ,  HYUN-SEOP TAE ,  JULIEN MICHEL ,  DENTON WADE HOYER ,  ANKE G. ROTH ,  JOHN DAVID HARLING ,  IAN EDWARD DAVID SMITH ,  AFJAL HUSSAIN MIAH ,  SEBASTIEN ANDRE CAMPOS ,  JOELLE LE

IPC: C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/54 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/00 ,  C12N9/00

CPC classification number: C07D413/14 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  A61K38/05 ,  A61K38/06 ,  A61K45/06 ,  A61K47/545 ,  A61K47/55 ,  A61K47/64 ,  C07D207/16 ,  C07D207/26 ,  C07D401/06 ,  C07D401/10 ,  C07D403/06 ,  C07D405/06 ,  C07D405/12 ,  C07D413/06 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07J43/003 ,  C12N9/93

Abstract: The present invention relates to bifunctional compounds, which find utility as modulators of targeted ubiquitination, especially inhibitors of a variety of polypeptides and other proteins which are degraded and/or otherwise inhibited by bifunctional compounds according to the present invention. In particular, the present invention is directed to compounds, which contain on one end a VHL ligand which binds to the ubiquitin ligase and on the other end a moiety which binds a target protein such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of that protein. The present invention exhibits a broad range of pharmacological activities associated with compounds according to the present invention, consistent with the degradation/inhibition of targeted polypeptides.

公开(公告)号：US20240309043A1

公开(公告)日：2024-09-19

申请号：US18640607

申请日：2024-04-19

Applicant: Organon R&D Finland Ltd.

Inventor： Leena HIRVELÄ ,  Marjo HAKOLA ,  Tero LINNANEN ,  Pasi KOSKIMIES ,  Camilla STJERNSCHANTZ

IPC: C07J43/00 ,  A61K31/565 ,  A61K31/58 ,  A61K45/06 ,  C07J41/00

CPC classification number: C07J43/003 ,  A61K31/565 ,  A61K31/58 ,  A61K45/06 ,  C07J41/0005 ,  C07J41/0016 ,  C07J41/0044

Abstract: The invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof




wherein R1 to R4 are as defined in the claims. The invention further relates to their use as inhibitors of 17β-HSD1 and in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17β-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration. The present invention also relates to the preparation of the aforementioned compounds and to pharmaceutical compositions comprising as an active ingredient(s) one or more of the aforementioned compounds or pharmaceutically acceptable salts thereof.

公开(公告)号：US20240308969A1

公开(公告)日：2024-09-19

申请号：US18438460

申请日：2024-02-10

Applicant: Board of Regents, The University of Texas System

Inventor： Michael P. Doyle ,  Luca De Angelis ,  Soumen Biswas ,  Gildardo Rivera

IPC: C07D239/28 ,  C07D211/90 ,  C07D401/04 ,  C07D403/04 ,  C07D487/04 ,  C07J43/00

CPC classification number: C07D239/28 ,  C07D211/90 ,  C07D401/04 ,  C07D403/04 ,  C07D487/04 ,  C07J43/003

Abstract: Embodiments are directed to practical strategies for inverse electron demand Diels-Alder (IEDDA) reactions with 1,2,3-triazine 1-oxides. These bench stable N-oxides undergo unprecedented nucleophilic addition with dienophile to form polysubstituted heteroarenes in high yield. Rapid at room temperature, these catalyst free reactions offer a diversity of structural modifications for heterocyclic syntheses.

公开(公告)号：US20240270784A1

公开(公告)日：2024-08-15

申请号：US18535256

申请日：2023-12-11

Applicant: Sage Therapeutics, Inc.

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

IPC: C07J9/00 ,  A61K31/57 ,  C07J17/00 ,  C07J43/00

CPC classification number: C07J9/00 ,  A61K31/57 ,  C07J17/00 ,  C07J43/003

Abstract: Compounds are provided according to Formula (I), and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein A, R1, and R5 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

公开(公告)号：US20240218011A1

公开(公告)日：2024-07-04

申请号：US18356148

申请日：2023-07-20

Applicant: FireFly Bio, Inc.

Inventor： Sean Wesley Smith ,  Scott Allan Mitchell ,  Jack Chang Hung Lee

IPC: C07J43/00 ,  A61K31/58 ,  A61K47/64 ,  C07J9/00 ,  C07J17/00 ,  C07J33/00

CPC classification number: C07J43/003 ,  A61K31/58 ,  A61K47/6425 ,  C07J9/00 ,  C07J17/00 ,  C07J33/002

Abstract: The present disclosure describes glucocorticoid agonist compounds, their conjugates with binding proteins, pharmaceutical compositions thereof, as well as methods and uses for treating diseases or conditions, such as autoimmune or inflammatory conditions.