公开(公告)号：US12139475B2

公开(公告)日：2024-11-12

申请号：US17816614

申请日：2022-08-01

Applicant: CHEMOCENTRYX, INC.

Inventor： Xi Chen ,  Dean R. Dragoli ,  Pingchen Fan ,  Manmohan Reddy Leleti ,  Rebecca M. Lui ,  Viengkham Malathong ,  Jay P. Powers ,  Rajinder Singh ,  Hiroko Tanaka ,  Ju Yang ,  Chao Yu ,  Penglie Zhang

IPC: C07D405/04 ,  A61P1/00 ,  A61P11/00 ,  A61P17/00 ,  A61P19/00 ,  A61P35/00 ,  C07D209/34 ,  C07D401/04 ,  C07D405/14

Abstract: Oxindole compounds useful for the treatment of CCR(9) mediated conditions or diseases are provided.

公开(公告)号：US20240360091A1

公开(公告)日：2024-10-31

申请号：US18688300

申请日：2022-09-02

Applicant: Emory University ,  Neurop, Inc.

Inventor： Dennis Liotta ,  Stephen Traynelis ,  Lawrence Wilson ,  Yesim Altas Tahirovic ,  David Menaldino ,  Scott Myers ,  Kamalesh Poornachary

IPC: C07D295/135 ,  A61K31/495 ,  A61K31/496 ,  C07D209/34 ,  C07D215/22 ,  C07D295/096

CPC classification number: C07D295/135 ,  A61K31/495 ,  A61K31/496 ,  C07D209/34 ,  C07D215/22 ,  C07D295/096

Abstract: Compounds that selectively inhibit GluN2B-containing N-methyl-D-aspartic acid receptors (NMDARs) are disclosed. In some cases, the compounds selectively target GluN2B over GluN2A, GluN2C, and/or GluN2D. Generally, the compounds possess an enhanced potency to GluN2B at a pH that is more acidic compared to the physiological pH. Pharmaceutical formulations containing one or more of the compounds are also disclosed. Additionally, methods of treating a condition, disorder or disease using the compounds or their pharmaceutical formulations thereof are disclosed. Exemplary conditions, disorders, and diseases relevant to this disclosure include stroke, subarachnoid hemorrhage, cerebral ischemia, cerebral vasospasm, hypoxia, acute CNS injury, spinal cord injury, traumatic brain injury, coronary artery bypass graft, persistent or chronic cough, substance abuse disorder, opiate withdrawal, opiate tolerance, bipolar disorder, suicidal ideation, pain, fibromyalgia, depression, postpartum depression, resting tremor, dementia, epilepsy, seizure disorder, movement disorder, and neurodegenerative disease.

公开(公告)号：US20240351994A1

公开(公告)日：2024-10-24

申请号：US17999400

申请日：2021-05-20

Applicant: Kaerus Bioscience Limited

Inventor： Roman FLECK ,  John PROUDFOOT

IPC: C07D401/04 ,  C07D209/34 ,  C07D401/14 ,  C07D403/10 ,  C07D471/04 ,  C07D491/107 ,  C07D498/04

CPC classification number: C07D401/04 ,  C07D209/34 ,  C07D401/14 ,  C07D403/10 ,  C07D471/04 ,  C07D491/107 ,  C07D498/04

Abstract: The present invention relates to the compounds of formula (I) and pharmaceutical compositions containing these compounds. The compounds provided herein can act as maxi-K potassium channel openers, which makes them suitable for use in therapy, particularly in the treatment or prevention of fragile X associated disorders, such as fragile X syndrome.

公开(公告)号：US20240350458A1

公开(公告)日：2024-10-24

申请号：US18580822

申请日：2022-07-21

Applicant: Simona Rapposelli ,  Eugenio Gaudio ,  Fabrizio Dal Piaz

Inventor： Simona Rapposelli ,  Eugenio Gaudio ,  Fabrizio Dal Piaz

IPC: A61K31/4178 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61P5/00 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

CPC classification number: A61K31/4178 ,  A61K31/404 ,  A61K31/4155 ,  A61K31/4439 ,  A61P5/00 ,  C07D209/34 ,  C07D401/06 ,  C07D403/06 ,  C07D409/06

Abstract: The invention relates to a 2-oxoindole compound of Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are, independently from each other, hydrogen, 1H-imidazolyl, thienyl and 1-methyl-1H-imidazolyl, 2-methyl-1H-imidazolyl, 2-aminopyridinyl, 1H-pyrazolyl, with the proviso that one of R1 and R2 is hydrogen; or R1 and R2 together form 9H-fluorene R3 is hydrogen, (C1-C3)alkyl, halogen or NO2; for use as a 14-3-3 protein modulator of a tumor selected from the group consisting of a lymphoma, chronic lymphocytic leukaemia (CLL), Ewing sarcoma, colon cancer, melanoma and anaplastic thyroid cancer (ATC). The invention relates also new 2-oxoindole compound of Formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240150368A1

公开(公告)日：2024-05-09

申请号：US18456831

申请日：2023-08-28

Applicant: Deciphera Pharmaceuticals, LLC

Inventor： Justin T. Proto ,  Andrew Michael Harned ,  Kristen Stoltz ,  Timothy Caldwell ,  Lakshminarayana Vogeti ,  Yu Mi Ahn ,  Bertrand Le Bourdonnec ,  Daniel L. Flynn

IPC: C07D487/10 ,  A61K45/06 ,  C07D209/34 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

CPC classification number: C07D487/10 ,  A61K45/06 ,  C07D209/34 ,  C07D401/14 ,  C07D403/12 ,  C07D405/14 ,  C07D413/12 ,  C07D487/04 ,  C07D487/08 ,  C07D491/107

Abstract: Described herein are compounds that are inhibitors of autophagy and their use in the treatment of disorders such as cancers.

公开(公告)号：US20230365488A1

公开(公告)日：2023-11-16

申请号：US18248232

申请日：2021-10-08

Applicant: The Research Foundation for The State University of New York

Inventor： Iwao Ojima ,  Martin Kaczocha ,  Monaf Awwa ,  Antonella Pepe

IPC: C07C69/757 ,  C07C255/55 ,  C07D317/54 ,  C07D209/34 ,  C07D319/18 ,  C07D215/227 ,  C07D239/26 ,  A61P35/04 ,  A61K31/337 ,  A61K31/277 ,  A61K31/36 ,  A61K31/216 ,  A61K31/404 ,  A61K31/357 ,  A61K31/4704 ,  A61K31/505

CPC classification number: C07C69/757 ,  C07C255/55 ,  C07D317/54 ,  C07D209/34 ,  C07D319/18 ,  C07D215/227 ,  C07D239/26 ,  A61P35/04 ,  A61K31/337 ,  A61K31/277 ,  A61K31/36 ,  A61K31/216 ,  A61K31/404 ,  A61K31/357 ,  A61K31/4704 ,  A61K31/505 ,  C07C2601/04 ,  C07C2603/18 ,  C07C2602/08

Abstract: The present invention provides a compound, and method of selectively inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, said compound having the structure:

公开(公告)号：US11787767B2

公开(公告)日：2023-10-17

申请号：US17231834

申请日：2021-04-15

Applicant: Escient Pharmaceuticals, Inc.

Inventor： Marcos Sainz ,  Adam Yeager ,  Brandon Selfridge ,  Esther Martinborough ,  Marcus Boehm ,  Liming Huang

IPC: C07D215/227 ,  C07D209/34 ,  C07D209/46 ,  C07D217/24 ,  C07D413/12

CPC classification number: C07D215/227 ,  C07D209/34 ,  C07D209/46 ,  C07D217/24 ,  C07D413/12

Abstract: Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4 dependent condition more specifically, by contacting the MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having the structure of Formula (I):




or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein m, n, p, t, A, B, Z, R1, R2 and R3 are as defined herein. Pharmaceutical compositions containing such compounds, as well as to compounds themselves, are also provided.

公开(公告)号：US20230212120A1

公开(公告)日：2023-07-06

申请号：US17928075

申请日：2021-05-27

Applicant: The Regents of the University of Michigan ,  Purdue Research Foundation

Inventor： John J.G. Tesmer ,  Rachel Rowlands ,  Andrew White

IPC: C07D209/34 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14

CPC classification number: C07D209/34 ,  C07D403/06 ,  C07D405/12 ,  C07D405/14

Abstract: This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having an indolinone structure which function as inhibitors of GRK5, and their use as therapeutics for the treatment of heart conditions and cancer.

公开(公告)号：US11623009B2

公开(公告)日：2023-04-11

申请号：US16927773

申请日：2020-07-13

Applicant: Purdue Research Foundation ,  University of Utah

Inventor： Stewart Andrew Low ,  Philip S. Low ,  Christopher Galliford ,  Jindrich Kopecek ,  Jiyan Yang

IPC: A61K47/42 ,  A61L27/22 ,  A61K9/107 ,  A61K31/404 ,  C07D403/04 ,  C07D209/34 ,  C07D487/00 ,  A61L27/54 ,  C07K7/06 ,  C07K7/08 ,  A61P19/00 ,  A61M5/00

Abstract: Aspects of the present disclosure generally relate to compounds for targeting and healing bone fractures. Some of these compounds include a negatively charged oligopeptide comprising an acidic oligopeptide, a linker, which may be hydrolyzable or may be a substrate for the protease cathepsin K, and at least one molecule that promotes bone healing. In some compounds the molecule that promotes bone healing is an anabolic compound that inhibits GSK3β, in some compounds the molecule that promotes the healing of bone fracture is a pro-inflammatory agent such as PGE1. Other embodiments include methods of treating a bone fracture comprising administering a therapeutic amount of any one of the compounds disclosed herein.

公开(公告)号：US20230093124A1

公开(公告)日：2023-03-23

申请号：US17947287

申请日：2022-09-19

Applicant: Apotex Inc.

Inventor： Fabio E. S. Souza ,  Alexander J. Stirk ,  Avedis Karadeolian ,  Fatemeh Mohammadpourmir ,  Allan W. Rey

IPC: C07D209/34

Abstract: Provided are novel salts of nintedanib and crystalline forms thereof. Specific salts of nintedanib provided by the present invention include glutarate, hippurate, levulinate, acesulfamate, diacesulfamate, and saccharinate. Also provided are pharmaceutical compositions including the nintedanib salts and crystalline forms thereof, and the use of these salts in the treatment or prevention of fibrotic diseases selected from the group including idiopathic pulmonary fibrosis, chronic fibrosing interstitial lung disease with a progressive phenotype, and systemic sclerosis-associated interstitial lung disease.