Abstract: The present invention provides crystalline forms, solvates and hydrates of 4-amino-2-butoxy-8-(3-(pyrrolidin-1-ylmethyl)benzyl)-7,8-dihydropteridin-6(5H)-one, and methods of making.
Type:
Grant
Filed:
June 21, 2021
Date of Patent:
October 3, 2023
Assignee:
GILEAD SCIENCES, INC.
Inventors:
Krista Marie Diaz, Patricia Andres, Valeriya N. Smolenskaya
Abstract: Disclosed are crystalline forms of sepiapterin free base selected from polymorphs A, B, C, D, E, F, and G, and combinations thereof, as well as crystalline polymorphs of salts of sepiapterin. Also disclosed are pharmaceutical compositions containing one or more such polymorphs and methods for preparing such polymorphs. Sepiapterin is useful in the treatment of a number diseases associated with low cellular levels of BH4, for example, phenylketonuria.
Abstract: Nuclear transport modulators are disclosed. The compounds can inhibit nuclear transporters such as the exportin-1 transporter. The compounds and pharmaceutical compositions comprising the compounds can be used to treat neurological diseases and cancer.
Type:
Grant
Filed:
December 4, 2020
Date of Patent:
September 26, 2023
Assignee:
XWPHARMA LTD.
Inventors:
Jia-Ning Xiang, Zude Qi, Xianbo Liu, Dezheng Ning
Abstract: Compositions of ?-aminoisobutyric acid (BAIBA), and methods of using the same to achieve a physiological objective, are provided. Compositions of BAIBA having enantiomeric purity, in which a selected proportion of the BAIBA is L-?-aminoisobutyric acid (L-BAIBA) and/or a selected proportion of the BAIBA is D-?-aminoisobutyric acid (D-BAIBA), are also provided.
Abstract: Disclosed herein are mono- and di-substituted tetrazines and methods of their preparation and converting an oxetanyl ester to a thio-substituted tetrazine, which is then converted to a mono-substituted tetrazine, a di-substituted tetrazine, or a vinylether disubstituted tetrazine.
Type:
Grant
Filed:
October 1, 2021
Date of Patent:
September 26, 2023
Assignee:
UNIVERSITY OF DELAWARE
Inventors:
Joseph M. Fox, William Lambert, Yinzhi Fang, Christopher William am Ende, Subham Mahapatra, Yixin Xie, Chuanqi Wang
Abstract: Heterocyclic compounds of Formula (I) and pharmaceutically acceptable salt thereof are disclosed. The use of such heterocyclic compounds and pharmaceutically acceptable salt thereof for the treatment of cancers, and more particularly cancers sensitive to mitochondrial activity inhibition and increased reactive oxygen species (ROS) levels, is also disclosed.
Type:
Grant
Filed:
November 2, 2018
Date of Patent:
September 19, 2023
Assignee:
UNIVERSITÉ DE MONTRÉAL
Inventors:
Yves Gareau, Stéphane Gingras, Yves Chantigny, Gaoqiang Yang, Guy Sauvageau, Irène Baccelli, Anne Marinier
Abstract: Provided herein is a synthesis for omecamtiv mecarbil dihydrochloride hydrate and various intermediates.
Type:
Grant
Filed:
May 19, 2021
Date of Patent:
September 12, 2023
Assignee:
AMGEN INC.
Inventors:
Sebastien Caille, Kyle Quasdorf, Philipp C. Roosen, Xianqing Shi, Andrew Cosbie, Fang Wang, Zufan Wu, Archana Neergunda, Bin Peter Quan, Lianxiu Guan
Abstract: The invention relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): wherein L1, A, X1, X2, Y1, Y2, Y3, Y4, R1, R2, and R3 are described herein.
Abstract: Some embodiments of the disclosure provide new uses of trans-1,3-dilinolein as medicaments and food. In an embodiment, an application of trans-1,3-dilinolein in the preparation of stomachic tonic and an application thereof include the preparation of medicaments for treating gastric cancer. Cell experiments show that trans-1,3-dilinolein promotes the proliferation of human gastric mucosal epithelial cell line GES-1 under normal oxygen and hypoxic conditions and it has concentration-dependent killing effect on human gastric cancer cell line HGC-27 and killing effect on hypoxic gastric cancer cells. At a concentration of 300 ?m and more, trans-1,3-dilinolein kills gastric cancer cells significantly and the killing effect becomes more significant under hypoxic conditions.
Abstract: The present invention relates to the field of anti-cancer compounds. More particularly, the invention relates to a family of benzothiazolyl urea or thiorurea compound useful as such agents. The present invention also relates to methods for treating cancers using these compounds.
Abstract: Disclosed are modified T-cells so that the modified T-cells are capable of penetrating the fugetactic wall generated by tumors, including solid mass tumors, as well as imparting tumor specific targeting for these modified T-cells.
Abstract: The present application provides tricyclic heterocyclic compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.
Type:
Grant
Filed:
March 2, 2021
Date of Patent:
August 1, 2023
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Neil Lajkiewicz, Yingda Ye, Zhenwu Li, Wenqing Yao
Abstract: The present invention relates to phenyl derivatives of formula (I) wherein (R1)n, R3, R4a, R4b, R5a, R5b and Ar1 are as described in the description and their use in the treatment of cancer by modulating an immune response comprising a reactivation of the immune system in the tumor. The invention further relates to novel benzofurane and benzothiophene derivatives of formula (III) and their use as pharmaceuticals, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as modulators of the prostaglandin 2 receptors EP2 and/or EP4.
Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein: R1, R2, R3, R4, R5, and m are defined herein. Also disclosed are methods of using such compounds to inhibit the activity of one or both of diacylglycerol kinase alpha (DGK?) and diacylglycerol kinase zeta (DGK?), and pharmaceutical compositions comprising such compounds. These compounds are useful in the treatment of viral infections and proliferative disorders, such as cancer.
Type:
Grant
Filed:
February 1, 2021
Date of Patent:
August 1, 2023
Assignee:
Bristol-Myers Squibb Company
Inventors:
Upender Velaparthi, Louis S. Chupak, Chetan Padmakar Darne, Min Ding, Robert G. Gentles, Yazhong Huang, Manjunatha Narayana Rao Kamble, Scott W. Martin, Raju Mannoori, Ivar M. McDonald, Richard E. Olson, Hasibur Rahaman, Prasada Rao Jalagam, Saumya Roy, Gopikishan Tonukunuru, Sivasudar Velaiah, Jayakumar Sankara Warrier, Xiaofan Zheng, John S. Tokarski, Bireshwar Dasgupta, Kotha Rathnakar Reddy, Thiruvenkadam Raja
Abstract: The present disclosure provides bifunctional compounds comprising a target protein binding moiety and a E3 ubiquitin ligase binding moiety, and associated methods of use.
Type:
Grant
Filed:
June 9, 2021
Date of Patent:
July 18, 2023
Assignee:
Prelude Therapeutics Incorporated
Inventors:
Hong Lin, Philip Pitis, Liang Lu, Andrew Paul Combs
Abstract: Disclosed is a compound containing a specific structure having an azomethine part, the compound being reversibly fluidized and non-fluidized by being irradiated with light.
Abstract: Pharmaceutical compositions of the invention comprise kinase inhibitors having a disease-modifying action in the treatment of diseases associated with BCR-ABL activity that include cancer, including chronic myeloid leukemia, acute lymphoblastic leukemia, acute myeloid leukemia, chronic lymphocytic leukemia, multiple myeloma, lymphomas, and metastatic carcinoma.
Type:
Grant
Filed:
March 18, 2019
Date of Patent:
July 11, 2023
Assignee:
ALLCRON PHARMA INC.
Inventors:
Ayyappan Rajasekaran, Jon Swanson, Peter Kane, Julia Foster