Abstract: The present disclosure provides methods for treating Alzheimer's disease (AD) comprising administering clomipramine or a pharmaceutically acceptable salt thereof. The administration of clomipramine increases the levels of TAp73 and decreases the levels of proliferating cell nuclear antigen (PCNA) and cleaved caspase-3 in the AD patients. The methods of the present disclosure reduce the neurodegeneration and improve the cognitive and functional decline in AD patients.
Abstract: The present invention provides crystalline solids of 6?-((6-aminopyrimidin-4-yl)amino)-8?-methyl-2?H-spiro[cyclohexane-1,3?-imidazo[1,5-a]pyridine]-1?,5?-dione: The crystalline compounds of the present application are inhibitors of Mnk and finds utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.
Type:
Grant
Filed:
September 24, 2021
Date of Patent:
April 9, 2024
Assignee:
eFFECTOR Therapeutics Inc.
Inventors:
Siegfried H. Reich, Paul A. Sprengeler, Stephen E. Webber, Alan X. Xiang, Justin T. Ernst, Bennett C. Borer, Samuel Sperry, Jo Ann Z. Wilson
Abstract: The present invention provides compounds, e.g., compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are implantable elements (e.g., devices and materials) comprising the same, as well as methods of use thereof, e.g., for treating or preventing a disease, disorder, or condition.
Type:
Grant
Filed:
October 3, 2017
Date of Patent:
April 2, 2024
Assignee:
SIGILON THERAPEUTICS, INC.
Inventors:
Omid Veiseh, Richard Heidebrecht, Paul Kevin Wotton, Matthias Alexander Oberli, Robert James Miller
Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
Type:
Grant
Filed:
August 23, 2021
Date of Patent:
April 2, 2024
Assignee:
Karyopharm Therapeutics Inc.
Inventors:
Erkan Baloglu, Sharon Shacham, Dilara McCauley, Trinayan Kashyap, William Senapedis, Yosef Landesman, Gali Golan, Ori Kalid, Sharon Shechter
Abstract: The application relates to a compound having Formula X: which modulates the activity of HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which HER2 and/or a mutant thereof, and/or EGFR and/or a mutant thereof, plays a role.
Type:
Grant
Filed:
October 20, 2021
Date of Patent:
April 2, 2024
Assignee:
Dana-Farber Cancer Institute, Inc.
Inventors:
John M. Hatcher, Nathanael S. Gray, Jaebong Jang, Dries De Clercq, Pasi Janne, Jamie A. Saxon, Michael Eck, David A. Scott, Alyssa Verano
Abstract: Biotransformation of an aromatase inhibitor, testolactone (1), yielded four metabolites, 7?-hydroxy-3-oxo-13,17-seco-5?-androsta-1-eno-17,13?-lactone (2), 3?,11?-dihydroxy-13,17-seco-5?-androsta-17,13?-lactone (3), 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (4), and 4?,5?-epoxy-3?-hydroxy-13,17-secoandrosta-1-eno-17,13?-lactone (5). Aromatase (estrogen synthase) involves in the synthesis of estrogen, and promotes the growth of breast cancerous cells. It is a key target for the discovery of chemotherapeutic agents against ER+(estrogen-positive) breast-cancers. Metabolites 2 (IC50=8.63±0.402 nM), and 3 (IC50=9.23±1.31 nM) were identified as potent inhibitors against human aromatase enzyme, in comparison to 1 (IC50=0.716±0.031 ?M), and the standard aromatase inhibiting drug, exemestane (IC50=0.232±0.031 ?M). Derivatives 4 (IC50=10.37±0.50 ?M) and 5 (IC50=0.82±0.059 ?M) also showed a good inhibition against aromatase enzyme.
Abstract: Embodiments of the present invention provide a pharmaceutical intervention in the neonatal pig that inhibits and delays development and activation of the HPG axis, growth of the boar testis and inhibits testicular production of testosterone and androstenone, which prevents the development of aggressive behavior in the maturing boars and the presence of boar taint in the meat. The invention comprises treatment with a combination of an androgen and an estrogen in the newborn male piglet using extended drug delivery methods, with a defined duration of no more than 12 weeks, for the purpose of inhibiting the production of testosterone and androstenone and the accumulation of the boar taint-inducing molecules androstenone and skatole in the fat.
Type:
Grant
Filed:
October 3, 2022
Date of Patent:
March 26, 2024
Assignee:
Insigna Inc.
Inventors:
CheMyong Ko, ChanJin Park, Po-Ching Patrick Lin, Rex Allen Hess, Suzanne Rene Broussard, Sherry Qi Zhou
Abstract: The invention provides substituted pyrazolo[1,5-a]pyrimidine and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted pyrazolo[1,5-a]pyrimidine compounds described herein include 5,7-dimethyl-N-phenylpyrazolo[1,5-a]pyrimidine-3-carboxamide compounds and variants thereof.
Type:
Grant
Filed:
July 7, 2021
Date of Patent:
March 19, 2024
Assignee:
Bial—R & D Investments, S.A.
Inventors:
Renato T. Skerlj, Peter T. Lansbury, Andrew C. Good, Elyse Marie Josee Bourque
Abstract: Disclosed are compounds of Formula (I) to (VIII): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate or prodrug thereof, wherein R3 is a tricyclic heteroaryl group substituted with R3a and zero to 2 R3b; and Ri, R2, R3a, R3b, R4, and n are defined herein. Also disclosed are methods of using such compounds as PAR4 inhibitors, and pharmaceutical compositions comprising such compounds. These compounds are useful in inhibiting or preventing platelet aggregation, and are useful for the treatment of a thromboembolic disorder or the primary prophylaxis of a thromboembolic disorder.
Type:
Grant
Filed:
January 6, 2021
Date of Patent:
March 19, 2024
Assignee:
Bristol-Myers Squibb Company
Inventors:
Xiaojun Zhang, Eldon Scott Priestley, Oz Scott Halpern, Wen Jiang, Samuel Kaye Reznik, Jeremy M. Richter
Abstract: A compound of Formula (I), or a pharmaceutically acceptable salt thereof, is provided that has been shown to be useful for treating a PRC2-mediated disease or disorder: wherein R1, R2, R3, R4, R5, and n are as defined herein.
Type:
Grant
Filed:
October 19, 2021
Date of Patent:
March 19, 2024
Assignee:
NOVARTIS AG
Inventors:
Ho Man Chan, Xiang-Ju Justin Gu, Ying Huang, Ling Li, Yuan Mi, Wei Qi, Martin Sendzik, Yongfeng Sun, Long Wang, Zhengtian Yu, Hailong Zhang, Ji Yue (Jeff) Zhang, Man Zhang, Qiong Zhang, Kehao Zhao
Abstract: Compounds and compositions are disclosed in which a NAMPT Drug Unit is conjugated to a targeting Ligand Unit through quaternization by a Linker Unit from which a NAMPT inhibitor compound or derivative thereof is released at the targeted site of action. Methods for treating diseases characterized by the targeted abnormal cells, such as those of cancer or an autoimmune disease, using the compounds and compositions of the invention are also disclosed.
Type:
Grant
Filed:
April 27, 2018
Date of Patent:
March 19, 2024
Assignee:
Seagen Inc.
Inventors:
Christopher Scott Neumann, Kathleen Olivas, Robert Lyon, Kung-Pern Wang
Abstract: Disclosed herein are kinase inhibitory compounds, such as a receptor-interacting protein-1 (RIP1) kinase inhibitor compounds, as well as pharmaceutical compositions and combinations comprising such inhibitory compounds. The disclosed compounds, pharmaceutical compositions, and/or combinations may be used to inhibit a RIP1 kinase in vivo or ex vivo, and also may treat or prevent a kinase-associated disease or condition, particularly a RIP1-associated disease or condition.
Abstract: Provided herein are compounds of Formula (I) and Formula (II) and stereoisomers, tautomers, and pharmaceutically acceptable salts or solvates thereof. Also provided are pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition by using the compounds and pharmaceutical compositions.
Type:
Grant
Filed:
March 1, 2022
Date of Patent:
March 5, 2024
Assignee:
RECURSION PHARMACEUTICALS, INC.
Inventors:
Michael James Genin, Joseph Carpenter, Carl Brooks
Abstract: The present application provides tricyclic heteroaryl compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer.
Abstract: The present invention relates to a method for preventing transmission of influenza, wherein said method comprises administering an effective amount of a compound to a patient having an influenza virus infection, herein referred to as “index patient”, wherein the compound has one of the formulae (I) and (II), or its pharmaceutically acceptable salt. The compound to be used in the present invention reduces infectivity of the influenza virus of the index patient, and therefore, reduces the risk of the index patient to trigger an influenza epidemic or an influenza pandemic as compared to a control patient.
Type:
Grant
Filed:
December 23, 2021
Date of Patent:
February 27, 2024
Assignees:
Shionogi & Co., Ltd.
Inventors:
Takeshi Noshi, Takahiro Noda, Ryu Yoshida, Takao Shishido, Kaoru Baba, Aeron C. Hurt, Leo Yi Yang Lee, Steffen Wildum, Klaus Kuhlbusch, Barry Clinch, Jan Michal Nebesky, Annabelle Lemenuel, Wendy S. Barclay, Jean-Eric Charoin, Yoshinori Ando
Abstract: This application relates to chemical compounds which may act as inhibitors of, or which may otherwise modulate the activity of, PCSK9, or a pharmaceutically acceptable salt, solvate, prodrug or polymorph thereof, and to compositions and formulations comprising such compounds, and methods of using and making such compounds. Compounds include compounds of Formula (I): wherein A, D and Q are described herein.
Type:
Grant
Filed:
June 30, 2021
Date of Patent:
February 13, 2024
Assignee:
CARDIO THERAPEUTICS PTY LTD
Inventors:
Herbert Treutlein, Jun Zeng, Ian Dixon, Ian James, James T. Palmer
Abstract: Novel compounds having D3 receptor antagonistic activity are provided. A compound represented by formula (I): wherein ring A is a heterocycle, X1 is each independently CR4aR4b, X2 is each independently CR4cR4d, Y1 and Y2 are each independently a carbon atom or a nitrogen atom, L is —N(R6)—C(?O)— or the like, W is cyclyl or the like, R2 and R3 are each independently substituted or unsubstituted alkyl or the like, R1a, R1b, R4a to R4d, and R6 are each independently hydrogen atoms or the like, p is 1 or 2, q is an integer of 1 to 3, n is an integer of 1 to 4, s is an integer of 0 to 4, or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
April 21, 2022
Date of Patent:
February 13, 2024
Assignee:
SHIONOGI & CO., LTD.
Inventors:
Hiroyuki Tobinaga, Koji Masuda, Masanao Inagaki, Manami Masuda