Abstract: The invention provides various novel compositions of berberine in combination with pharmacologically active organic acids, and related methods of their use in treating various diseases or disorders. The invention further provides various novel compounds prepared from berberine and pharmacologically active organic acids and prepared from ursodeoxycholic acid and pharmacologically active organic bases, and pharmaceutical compositions thereof, and methods of their preparation and therapeutic use in treating and/or preventing various diseases or disorders.
Abstract: The invention relates to pharmaceutical compositions comprising, compounds of Formula Q: wherein W is —N(H)—, or —N(CH3)—, and Y is —C(?O)— or —O—, in free base or pharmaceutically acceptable salt form, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.
Type:
Grant
Filed:
October 16, 2020
Date of Patent:
June 20, 2023
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
Abstract: The invention provides compounds of Formula (A) that may inhibit ENPP1, and that are accordingly useful for treatment of disorders related to ENPP1. The invention further provides pharmaceutical compositions containing these compounds and methods of using these compounds to treat or prevent disorders related to ENPP1.
Abstract: Crystalline forms of Compound (I): are disclosed. Pharmaceutical compositions comprising the same, methods of inhibiting BTK using the same, and methods for making crystalline forms of Compound (I) are also disclosed.
Type:
Grant
Filed:
January 7, 2021
Date of Patent:
June 6, 2023
Assignee:
Principia Biopharma Inc.
Inventors:
Pasit Phiasivongsa, Jiang Zhu, Kolbot By, Mohammad Reza Masjedizadeh
Abstract: The present invention provides phenyl-2-hydroxy-acetylamino-2-methyl-phenyl compounds, such as compounds of formula I: pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat physiological disorders such as pancreatic cancer.
Type:
Grant
Filed:
April 11, 2018
Date of Patent:
May 23, 2023
Assignee:
ELI LILLY AND COMPANY
Inventors:
Marta Maria Cifuentes-Garcia, Maria Cristina Garcia Paredes
Abstract: Provided are heteroaryl heterocyclic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the variables are as defined in the description. The compounds are Btk inhibitors.
Abstract: The present disclosure provides compounds represented by Formula (I-1): and pharmaceutically acceptable salts thereof, and methods of using the same. The compounds and methods have a range of utilities as therapeutics, diagnostics, and research tools. In particular, the subject compositions and methods are useful for reducing signaling output of oncogenic proteins.
Type:
Grant
Filed:
March 2, 2022
Date of Patent:
May 16, 2023
Assignee:
Kumquat Biosciences Inc.
Inventors:
Baogen Wu, Xiangzhu Wang, Xiaoming Li, Zhiyong Chen, Pingda Ren, Yi Liu
Abstract: Disclosed in the present invention are a crystal form of a [1,2,4]triazolo[1,5-c]pyrimidine compound and a preparation method thereof. Further disclosed is a use of the crystal form in the preparation of a medicament for treating A2A receptor related diseases.
Type:
Grant
Filed:
April 28, 2019
Date of Patent:
May 16, 2023
Assignee:
Medshine Discovery Inc.
Inventors:
Kevin X. Chen, Yanxin Yu, Xinde Chen, Li Zhang, Zhaoguo Chen, Cheng Xie
Abstract: Provided herein, inter alia, are substituted imidazo[1,5-?]pyrazine compounds, compositions and methods for treating or preventing an IRE1?-related disease or disorder. In certain embodiments, the disease or disorder is selected from the group consisting of a neurodegenerative disease, a demyelinating disease, cancer, an eye disease, a fibrotic disease, and diabetes.
Type:
Grant
Filed:
August 31, 2018
Date of Patent:
May 16, 2023
Assignees:
Optikira LLC, The Regents of the University of California
Inventors:
Richard M. Keenan, Bradley J. Backes, Dustin J. Maly, Charles Reynolds, Ben Whittaker, Jamie Knight, Jonathan Mark Sutton, George Hynd, Feroz R. Papa, Scott A. Oakes
Abstract: The invention relates to compounds of formula (I) which are inhibitors of kinase activity, pharmaceutical formulations containing the compounds and their uses in treating and preventing viral infections and disorders caused or exacerbated by the viral infection wherein R1, R2, R3, R4a, R4b, R4c, R5, W, X, Y and Z are defined herein.
Type:
Grant
Filed:
January 15, 2019
Date of Patent:
May 16, 2023
Assignee:
GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
Inventors:
Nicholas Paul Barton, Sophie Marie Bertrand, Kenneth David Down, Matthew Gray
Abstract: This invention is in the area of cell cycle inhibiting compounds for the treatment of disorders involving abnormal cellular proliferation, and include selective CDK2 inhibitors for medical therapy and their pharmaceutically acceptable salts and compositions.
Abstract: Provided are compounds of formula (I): or cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Additionally provided are cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof. Also provided are therapeutic and/or cosmetic methods using the cosmeceutical and/or pharmaceutical compositions comprising the compounds of formula (I), or the cosmeceutically acceptable or pharmaceutically acceptable salts thereof, for modulating cyclic adenosine monophosphate response element binding (CREB)-binding protein (CBP)/?-catenin mediated signaling in treating skin related diseases, conditions, or disorders mediated by aberrant CBP/?-catenin signaling and cosmetic methods for treating skin conditions mediated by aberrant CBP/?-catenin signaling.
Abstract: Disclosed is a novel class of MDM2-p53 inhibitor compounds having an imidaxopyrolone structure, and specifically disclosed are compounds represented by formulas (I-1) and (I-2) and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
March 12, 2019
Date of Patent:
May 2, 2023
Assignees:
LUOXIN PHARMACEUTICAL (SHANGHAI) CO., LTD., SHANDONG LUOXIN PHARMACEUTICAL GROUP STOCK CO., LTD., MEDSHINE DISCOVERY INC.
Inventors:
Kevin X Chen, Xiaobing Yan, Jianglei Huang, Yuekun Nie, Guoping Hu, Jian Li, Shuhui Chen, Jiaqiang Dong, Tie-Lin Wang
Abstract: The compound of formula (II) is an advantageous intermediate for improving the process of synthesizing the linker-drug vc-seco-DUBA, as well as for the overall process for preparing an antibody-drug conjugate comprising the vc-seco-DUBA linker-drug. The methods of making the compound of formula (II) can include recovery of the compound as a solid, such as via crystallization, in high yields and purity.
Abstract: The present invention provides a compound of Formula I: wherein R is or a pharmaceutically acceptable salt thereof, useful for treating psoriasis, systemic lupus erythematosus, or type 1 diabetes.
Type:
Grant
Filed:
February 5, 2021
Date of Patent:
April 25, 2023
Assignee:
Eli Lilly and Company
Inventors:
Thomas John Bleisch, Zhaogen Chen, Theodore Curtis Jessop
Abstract: Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
Abstract: The present disclosure relates to substituted pyrrollo[3,4-D]imidazoles as JAK inhibitor compounds and uses thereof. Specifically, the present disclosure discloses a compound represented by formula (I), optical isomer thereof, geometric isomer thereof, a tautomer thereof or a mixture of various isomers, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a metabolite thereof. The present disclosure also relates to the application of the compounds in the treatment of JAK-related diseases or disorders.
Abstract: A novel antibody-pyrrolodiazepine derivative and a novel antibody-pyrrolodiazepine derivative conjugate using the same, comprising substituted benzo[e]pyrrolo[1,2-a][1,4]diazepines represented by the [Formula 24], [Formula 25], [Formula 26], and/or [Formula 27].
Abstract: The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein.
Type:
Grant
Filed:
November 28, 2017
Date of Patent:
April 18, 2023
Assignee:
PRAXIS PRECISION MEDICINES, INC.
Inventors:
Kiran Reddy, Gabriel Martinez Botella, Andrew Mark Griffin, Brian Edward Marron
Abstract: The present disclosure provides compounds of formula (I) or (II) or a pharmaceutically acceptable salt or stereoisomer thereof, wherein Rx-R8 are defined herein. Also provided are compositions comprising a compound described herein and a pharmaceutically effective excipient, methods of stabilizing microtubules in a patient comprising administering to the patient a microtubule-stabilizing amount of a compound described herein, methods of treating cancer in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein, and methods of treating a neurodegenerative disease in a patient comprising administering to the patient a therapeutically effective amount of a compound described herein.
Type:
Grant
Filed:
February 28, 2019
Date of Patent:
April 11, 2023
Assignees:
The Trustees of the University of Pennsylvania, The Regents of the University of California
Inventors:
Kurt R. Brunden, Virginia M. Y. Lee, John Q. Trojanowski, Carlo Ballatore, Killian Oukoloff, Amos B. Smith, III