Abstract: The invention relates to a pharmaceutical composition comprising a compound of formula I or a pharmaceutically acceptable salt thereof, and at least one pharmaceutical excipient selected from the group consisting of fillers, binders, disintegrants, glidants and lubricants, wherein the compound according to formula I is represented by:
Type:
Grant
Filed:
October 15, 2020
Date of Patent:
October 10, 2023
Assignee:
Convalife (Shanghai) Co. Limited
Inventors:
Stephen Joseph Shuttleworth, Elisabeth Ann Bone, Franck Alexandre Silva, Alexander Richard Liam Cecil
Abstract: The pyrrolo[3,2-b]quinoline compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Abstract: The 4-arylamino-2-(6-indolylamino)pyrimidine derivative compounds are antibacterial agents having broad spectrum antibacterial activity. The present 4-arylamino-2-(6-indolylamino)pyrimidine compounds have antimicrobial activity against various susceptible and resistant gram-positive and gram-negative bacteria as well as drug resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Abstract: The N-(Pyrido[2,3-b]indol-7-yl)acetamide compounds are antibacterial agents. The emergence of drug-resistant bacteria calls for constant development of new antibacterial agents with the aim of generating medicaments that are potent against drug sensitive and resistant bacteria and are well tolerated. The present compounds are not only new, but have very valuable antimicrobial properties. These compounds showed a broad spectrum of activity against gram-positive and gram-negative bacteria, as well tuberculosis mycobacteria. They also showed potent activity against drug-resistant bacteria, such as MRSA and VRSA. The molecular target of these compounds was identified as DNA Gyrase B. Based on their pharmacological profiles, the present compounds may find important clinical applications for severe infectious diseases and tuberculosis.
Abstract: Disclosed in the present invention are a crystal form of a TrkA inhibitor and a preparation method thereof, and an application thereof in preparation of drugs for treating diseases associated with pain, cancer, inflammation, neurodegenerative diseases, and certain infectious diseases.
Abstract: The invention relates to novel molecules having the general formula (I), and which molecules are useful to treat a disorder or disease characterized by bronchoconstriction, e.g. COPD and asthma inflammation and/or vasoconstriction, e.g. hypertension.
Type:
Grant
Filed:
July 5, 2019
Date of Patent:
June 20, 2023
Assignee:
Arcede Pharma AB
Inventors:
Maria Dalence, Martin Johansson, Viveca Thornqvist Oltner, Jörgen Toftered, David Wensbo
Abstract: The present disclosure provides combination therapy comprising a BET inhibitor and a protein phosphatase 2A (PP2A) activator, a B-cell lymphoma-2 (Bcl-2) inhibitor, a B-cell lymphoma-extra large (Bcl-xl) inhibitor, a casein kinase 2 (CK2) inhibitor, and/or a mediator complex subunit 1 (MED1) for cancer. The combination therapy is expected to be synergistic in treating the cancer, compared to the monotherapy. Methods for identifying a subject having a cancer that is resistant to or at risk of developing resistance to bromodomain and extra terminal (BET) inhibitor therapy are also provided.
Type:
Grant
Filed:
August 10, 2016
Date of Patent:
June 6, 2023
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
Kornelia Polyak, Shaokun Shu, James E. Bradner, Charles Yang Lin
Abstract: The present disclosure provides for treatments of restless legs syndrome (RLS) or one or more symptoms associated with RLS comprising administering leucine, acetyl-leucine or a pharmaceutically acceptable salt thereof.
Abstract: Methods and compounds for use in promoting survival of at least one eukaryotic cell, wherein the compounds are effective as gamma-ketoaldehyde scavengers.
Abstract: The present disclosure provides methods of treating lymphoid malignancies such as B cell malignancies using a BTK inhibitor in the described therapeutic regimens.
Abstract: The present invention relates to compounds of the following general formula (I) or (II) or a pharmaceutically acceptable salt and/or solvate thereof, for use in the prevention and/or the treatment of disorders associated to the inflammation induced by P. acnes, in particular in the prevention and/or the treatment of acne, psoriasis, chronic urticaria, urticaria pigmentosa, cutaneous autoinflammatory diseases, hidradenitis or atopic dermatis.
Type:
Grant
Filed:
July 21, 2020
Date of Patent:
April 4, 2023
Assignees:
Universite de Paris, Assistance Publique—Hopitaux de Paris
Inventors:
Nicolas Dupin, Vincent Calvez, Philippe Grange, Anne-Geneviève Marcelin
Abstract: Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of pemetrexed-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the pemetrexed-based compound is achieved.
Abstract: A pharmaceutical composition, comprising a therapeutically effective amount of an active pharmaceutical ingredient (API) compound represented by the following structural formula at least one acidifying agent; and a vehicle base comprising at least one pharmaceutically acceptable non-aqueous solvent. Values and preferred values of the variables in structural formula (I) are defined herein.
Abstract: The present disclosure is directed to methods for treating Crohn's disease, and in particular, to methods for inducing clinical remission and/or endoscopic improvement of Crohn's disease, using a JAK1 inhibitor. In certain embodiments, the patient is administered an induction dose of the JAK1 inhibitor to induce clinical remission and/or endoscopic improvement of the Crohn's disease, followed by administration of at least one maintenance dose of the JAK1 inhibitor thereafter. In other embodiments, the present disclosure is directed to methods for treating ulcerative colitis using a JAK1 inhibitor.
Type:
Grant
Filed:
April 1, 2022
Date of Patent:
March 21, 2023
Assignee:
AbbVie Inc.
Inventors:
Ana Paula Machado De Lacerda, Jose Jeffrey V. Enejosa, Aileen L. Pangan, Mohamed-Eslam F. Mohamed, Ahmed A. Othman, Ben Klünder, Wen Zhou
Abstract: An emulsifiable concentrate may include: an aminoindane amide having the structure of formula (I); and an amide having the structure of formula (II); wherein R1, R2, R3, R4, R5, R6, R7, R8, R11, R12, R13, and n are as defined herein, as well as to formulations containing the same, and to methods of their preparation and use for treatment and protection of agricultural crops.
Type:
Grant
Filed:
December 13, 2018
Date of Patent:
March 7, 2023
Inventors:
Robbie Moss Haines, Charlie James Flood, Hong Zhang, David Bird, Laibin B. Yan, Frank J. Zawacki, Claudio Dacarro, Elisa Galimberti, Ilenia Mazzali
Abstract: This invention relates to pharmaceutical formulations for topical skin application comprising (R)-3-cyclopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-1H-pyrazol-1-yl]propanenitrile, or a pharmaceutically acceptable salt thereof, and use in the treatment of skin disorders.
Abstract: Provided herein are methods of treating a subject with heart failure, comprising administering to the subject an initial dose of a cardiac sarcomere activator (CSA) for an initial time period, and subsequently administering to the subject a dose of the CSA based on the subject's plasma concentration of the CSA at the end of the initial time period.