Abstract: The present invention relates to compounds of general formula (I) wherein the variables X, R1, n, p and q are defined as in claim 1, which have valuable pharmacological properties, in particular bind to ghrelin O-acyl transferase (GOAT) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular obesity.
Type:
Grant
Filed:
January 28, 2019
Date of Patent:
May 3, 2022
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Thomas Trieselmann, Cedrickx Godbout, Viktor Vintonyak
Abstract: Disclosed are a series of pyrimidine sulfamide compounds and applications thereof in preparing a drug for a disease related to an ETA receptor antagonist. In particular, disclosed is a derived compound represented by formula (I) or a tautomer or pharmaceutically acceptable composition thereof.
Type:
Grant
Filed:
November 19, 2018
Date of Patent:
May 3, 2022
Assignee:
Shijiazhuang Sagacity New Drug Development Co., Ltd.
Abstract: Disclosed are methods of alleviating or preventing one or more symptoms associated with fragile X syndrome in an individual in need thereof via administration of a therapeutically effective amount of a GABA(A) alpha 2 and/or 3 partial agonist. The one or more symptoms may include impaired functional communication, anxiety, inattention, hyperactivity, sensory reactivity, autonomic nervous system dysregulation, aberrant eye gaze, self-injury, aggression, seizures, EEG abnormalities, including but not limited to, abnormal spectral analysis, event related potentials which may include auditory and visual responses, abnormalities in cortical responses as evoked by transcranial magnetic stimulation including resting and active motor thresholds and abnormal responses in measures of cortical inhibition and excitation, aberrant impaired cognitive function, compromised daily living skills, or a combination thereof.
Abstract: Disclosed are methods of preparing everninomicin analogs by genetic alteration of Micromonospora carbonacea. Everninomicin analogs prepared by these methods and methods of using these analogs to treat infections are also disclose.
Type:
Grant
Filed:
June 26, 2020
Date of Patent:
April 26, 2022
Assignee:
VANDERBILT UNIVERSITY
Inventors:
Brian O. Bachmann, Emilianne M. Limbrick, Kasia Derewacz
Abstract: The present invention provides, inter alia, compounds having the structures of formulas described herein; pharmaceutically acceptable salts, solvates, hydrates, tautomers, and isotopic forms thereof; and compositions (e.g., pharmaceutical compositions and kits) containing one or more of the foregoing. Also provided are methods of administering and uses involving the compounds and/or pharmaceutical compositions for treating or preventing disease. The disease can be a proliferative disease, such as a cancer (e.g., a blood cancer (e.g., a leukemia or lymphoma), a brain cancer, a breast cancer, melanoma, multiple myeloma, or an ovarian cancer) a benign neoplasm, pathologic angiogenesis, or a fibrotic disease.
Type:
Grant
Filed:
January 16, 2019
Date of Patent:
April 26, 2022
Assignee:
Syros Pharmaceuticals, Inc.
Inventors:
Jason J. Marineau, Claudio Edmundo Chuaqui, Stephane Ciblat, Anzhelika Kabro, Henri Piras, Kenneth Matthew Whitmore, Kate-Lyn Lund
Abstract: A method of treating or preventing adverse outcomes associated with tissue plasminogen activator (tPA) administration, cerebral edema-related side effects, cerebral edema associated with radiation therapy, or migraine headaches by administering an effective amount of a SUR1-TRPM4 channel inhibitor, such as glyburide, and optionally the co-administration of a second therapeutically active agent, to a subject in need thereof. Adverse outcomes associated with tPA include cerebral hemorrhage, cerebral edema, physical impairment or death. The administration of the SUR1-TRPM4 channel inhibitors occurs prior to the radiation therapy, during the radiation therapy, after the radiation therapy, or combinations thereof. The SUR1-TRPM4 channel inhibitor is administered prior to surgical excision of a brain tumor, CAR-T therapy, or administration of flutarabine. Alternatively, or in addition, the SUR1-TRPM4 channel inhibitor is administered prior the onset of the cerebral edema-related side effects.
Abstract: The invention provides compounds of the formula (I): (I) wherein A1, A2, R2, R4, B1, B2, X, X1, n, a and b are as defined are defined in the specification, to pharmaceutical compositions comprising the compounds and the compounds for use as medicaments. The compounds potentiate AMPA receptor function and are expected to be useful in the treatment of central nervous system disorders, for example in the treatment of depressive disorders, mood disorders and cognitive dysfunction associated with neuropsychiatric disorders such as schizophrenia.
Type:
Grant
Filed:
March 1, 2019
Date of Patent:
April 12, 2022
Assignee:
University College Cardiff Consultants Limited
Inventors:
Simon Ward, Paul Beswick, Lewis Pennicott, Tristan Reuillon, Irina Chuckowree, Carolina Villalonga-Barber, Roderick Alan Porter
Abstract: The present disclosure provides compounds, compositions and methods useful for the treatment of neurodegenerative diseases, in particular synucleinopathies.
Type:
Grant
Filed:
May 14, 2021
Date of Patent:
April 5, 2022
Assignee:
APRINOIA THERAPEUTICS LIMITED
Inventors:
Ming-Kuei Jang, Paul Tempest, Yih-Shyan Lin
Abstract: The present invention relates to crystalline forms of ethyl 2-[[3-[[3-chloro-5-fluoro-6-[3-methyl-2,6-dioxo-4-(trifluoromethyl)pyrimidin-1-yl]-2-pyridyl]oxy]-2-pyridyl]oxy]acetate, herein after also referred to as “compound of formula (I)”. The invention also relates to a process for the production of these crystalline forms, formulations for plant protection and herbicidal compositions which contain one of these crystalline forms.
Type:
Grant
Filed:
November 8, 2018
Date of Patent:
April 5, 2022
Assignee:
BASF SE
Inventors:
Martin Viertelhaus, Rolf Hellmann, Dennis Koulelis, Tobias Seiser
Abstract: This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.
Abstract: The present disclosure provides methods for preparing (R)-2-((2-amino-7-fluoropyrido[3,2-d]pyrimidin-4-yl)amino)-2-methylhexan-1-ol or a salt thereof and related key intermediates.
Type:
Grant
Filed:
June 25, 2020
Date of Patent:
March 29, 2022
Assignee:
Gilead Sciences, Inc.
Inventors:
Andrea Ambrosi, Florence J. Bachrach, Pavel R. Badalov, Stephen P. Lathrop, Jeffrey E. Merit, Beau P. Pritchett, Christopher S. Regens, Tiago Vieira, Adam B. Weinstein, Todd A. Wenderski, Zehua Zheng
Abstract: A method for treating inflammation and/or autoimmune diseases comprises administering to a subject in need thereof, a composition comprising a CDK8 inhibitor. In another aspect, a method for increasing IL-10 production comprises administering to a subject in need thereof a CDK8 inhibitor. In another aspect, a method for enhancing Treg cell differentiation, comprising administering a composition comprising a CDK8 inhibitor. In certain example embodiments, the subject suffers from an inflammatory bowel disease. In certain other example embodiments, the subject requires immunosuppression to prevent rejection following a transplantation procedure.
Type:
Grant
Filed:
August 3, 2017
Date of Patent:
March 29, 2022
Assignees:
The Broad Institute, Inc., The General Hospital Corporation, Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College
Inventors:
Thomas Sundberg, Alykhan Shamji, Ramnik Xavier, Liv Johannessen, Nathanael Gray, Bernard Khor, Jose Perez
Abstract: The invention relates to a compound of formula (I): Formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein A is heteraryl selected from 1H-benzimidazolyl and imidazo[1,2-a]pyridine, and R1, R2, R3, R4 and R5 are as defined herein, as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5) and its isoenzyme glutaminyl-peptide cyclotransferase-like protein (QPCTL). QC and QPCTL catalyze the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.
Abstract: The present disclosure relates generally to methods for treating neurodegenerative diseases, including their progressive forms. In particular, the present disclosure pertains to methods of treating or preventing neurodegenerative diseases, including their progressive forms and their associated symptoms by administering a combination of ibudilast (3-isobutyryl-2-isopropylpyrazolo[1,5-a]pyridine) and riluzole, or pharmaceutically acceptable salts of one or both thereof.
Abstract: The present invention relates to a method of dewatering post fermentation fluids in a starch to ethanol process. More particularly the invention relates to use of a nuclease enzyme for separation of whole stillage into an insoluble fraction and a supernatant fraction. In a specific embodiment the present invention relates to a method of dewatering whole stillage comprising the steps of: i) subjecting whole stillage to one or more nuclease enzymes; ii) separating the material into an insoluble fraction and a supernatant fraction.
Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1a, R1b, R1c, R1d, R2a, R2b, R3, R3a, R4, R6, R7, R8, A, Z, X1 and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
Type:
Grant
Filed:
May 14, 2020
Date of Patent:
March 8, 2022
Assignee:
ChemoCentryx, Inc.
Inventors:
Pingchen Fan, Christopher Lange, Venkat Reddy Mali, Darren J. McMurtrie, Viengkham Malathong, Sreenivas Punna, Rajinder Singh, Ju Yang, Yibin Zeng, Penglie Zhang
Abstract: The problem of the present invention is to provide a useful prodrug compound of a naphthofuran compound. The present invention relates to a compound represented by the formula (IA): [wherein each symbol is as described in the DESCRIPTION] or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to pyrrolidine sulfonamide analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.
Inventors:
Edward J. Brnardic, Carl A. Brooks, Brian Griffin Lawhorn, Peng Li, Jay M. Matthews, John Jeffrey McAtee, Joseph E. Pero, Matthew Robert Sender, Lamont Roscoe Terrell, David J. Behm
Abstract: Described herein are methods and compositions for the use of treating and/or preventing vaginal bacterial infection and promoting healthy vaginal flora. Aspects of the invention relate to administering to a subject in need thereof a composition comprising a bacterial mixture of L. crispatus, L. gasseri, and L. jensenii.
Type:
Grant
Filed:
July 11, 2017
Date of Patent:
March 1, 2022
Assignee:
THE BRIGHAM AND WOMEN'S HOSPITAL, INC.
Inventors:
Raina Fichorova, Andrew Onderdonk, Hidemi Yamamoto, Mary Delaney, Andrea Dubois
Abstract: Pharmaceuticals for treating patient with excessive lactate production and related acidemia are disclosed. Pharmaceuticals include glutamate, aspartate, BCAA, pyruvate, malate, oxaloacetate, ?-ketoglutarate, AST, ALT, PLP, MDH and GPDH, Lodoxamite and Oxamate. The mechanism is that invented pharmaceuticals inhibit LDH and enhance malate/aspartate shuttle activity.