Abstract: Novel pyrido[4?,3?:4,5]pyrrolo[3,2-c][2,7]naphthyridin-10-one compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrido[4?,3?:4,5]pyrrolo[3,2-c][2,7]naphthyridin-10-one compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.
Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts or solvates thereof, wherein all the variables are as defined herein. These compounds are antagonists to ?V-containing integrins. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating a disease, disorder, or condition associated with dysregulation of ?v-containing integrins, such as pathological fibrosis, transplant rejection, cancer, osteoporosis, and inflammatory disorders, by using the compounds and pharmaceutical compositions.
Type:
Grant
Filed:
February 24, 2021
Date of Patent:
January 30, 2024
Assignee:
Bristol-Myers Squibb Company
Inventors:
Guohua Zhao, Pratik Devasthale, Xiang-Yang Ye, Kumaravel Selvakumar, Suresh Dhanusu, Palanikumar Balasubramanian, Leatte R. Guernon, Rita Civiello, Xiaojun Han, Michael Frederick Parker, Swanee E. Jacutin-Porte
Abstract: The present teachings relate generally to conjugates and methods for imaging a tumor microenvironment in a patient, and to conjugates and methods for treating LHRH-R expressing cancer in a patient. The present teachings relate generally to method of making conjugates comprising an LHRH-R antagonist.
Abstract: Described herein are spiropiperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described spiropiperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described spiropiperidine compounds and synthetic intermediates that are useful in those syntheses.
Type:
Grant
Filed:
May 25, 2021
Date of Patent:
January 23, 2024
Assignee:
89BIO LTD
Inventors:
Robert L Hudkins, David B. Whitman, Craig A. Zificsak, Allison L. Zulli, Melody McWherter
Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds. Also described herein are methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.
Type:
Grant
Filed:
February 15, 2021
Date of Patent:
January 23, 2024
Assignee:
89BIO LTD
Inventors:
Nadine C. Becknell, Reddeppa Reddy Dandu, Bruce D. Dorsey, Dimitar B. Gotchev, Robert L. Hudkins, Linda Weinberg, Craig A. Zificsak
Abstract: The invention concerns compounds of Formula (I): or pharmaceutically acceptable salts thereof, wherein R1, R2, X, Ring A, Ring B and Ring C have any of the meanings hereinbefore defined in the description; process for their preparation; pharmaceutical compositions containing them and their use in treating MCT4 mediated diseases.
Abstract: The invention provides methods of delaying or preventing NF1-related malignancies or tumors using mebendazole. The administration of mebendazole results in decreased Ras activation in NF1-related tumor cells. Invention methods include the use of a cyclooxygenase-2 inhibitor such as celecoxib in combination with mebendazole. The methods include methods of treatment and methods of prevention or delaying of neurofibromatosis type 1-related malignancies or tumors.
Abstract: The methods include treating atypical teratoid/rhabdoid tumor by administration of HydroxyUreaMethyl Acylfulvene. Some embodiments relate to treatment of atypical teratoid/rhabdoid tumor by administration of HydroxyUreaMethyl Acylfulvene to a population or subject expressing SMARCB1.
Abstract: The present disclosure relates to a method for treating certain types of tumors or cancers, such as plexiform neurofibromas (PN), plexiform neurofibromas associated with neurofibromatosis type 1 (NF1-PN), by orally administering an effective amount of mirdametinib to the patient, where an amount of mirdametinib is administered on the first day of treatment to provide (i) an AUC0-tau less than 400 ng·h/mL, (ii) a Cmax no more than 40 ng/mL, or (iii) both.
Type:
Grant
Filed:
March 20, 2023
Date of Patent:
December 12, 2023
Assignee:
SPRINGWORKS THERAPEUTICS, INC.
Inventors:
Uchenna H Iloeje, Abraham J Langseth, Todd Shearer
Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.
Abstract: Methods of treating or suppressing mitochondrial diseases, such as Friedreich's ataxia (FRDA), Leber's Hereditary Optic Neuropathy (LHON), mitochondrial myopathy, encephalopathy, lactacidosis, and stroke (MELAS), Kearns-Sayre Syndrome (KSS), are disclosed, as well as compounds useful in the methods of the invention, such as 4-(p-quinolyl)-2-hydroxybutanamide derivatives. Methods and compounds useful in treating other disorders such as amyotrophic lateral sclerosis (ALS), Huntington's disease, Parkinson's disease, and pervasive developmental disorders such as autism are also disclosed. Energy biomarkers useful in assessing the metabolic state of a subject and the efficacy of treatment are also disclosed. Methods of modulating, normalizing, or enhancing energy biomarkers, as well as compounds useful for such methods, are also disclosed.
Type:
Grant
Filed:
February 22, 2021
Date of Patent:
December 12, 2023
Assignee:
PTC Therapeutics, Inc.
Inventors:
Orion D. Jankowski, Kieron E. Wesson, Paul Mollard, William D. Shrader
Abstract: Disclosed are compounds of Formula (I), methods of using the compounds for inhibiting ALK2 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with ALK2 activity such as cancer.
Type:
Grant
Filed:
June 10, 2021
Date of Patent:
December 12, 2023
Assignee:
Incyte Corporation
Inventors:
Jun Pan, Yu Bai, Liangxing Wu, Wenqing Yao
Abstract: The present disclosure relates to Alkynylphenylbenzamide compounds and the applications thereof. The said Alkynylphenylbenzamide compounds have the structure shown in Formula (I). The compounds can be used as protein kinase inhibitors, which can effectively inhibit the activity of TRK protein kinase and the proliferation, migration and invasion of various tumor cells. At the same time, it has the characteristics of good pharmacokinetics and low toxicity.
Type:
Grant
Filed:
September 20, 2022
Date of Patent:
December 5, 2023
Assignee:
SHENZHEN NEWDEL BIOTECH CO., LTD.
Inventors:
Xiaoyun Lu, Zhang Zhang, Ke Ding, Shuang Xiang, Jie Wang, Zhengchao Tu, Zhimin Zhang, Xia Tang, Zuqin Wang, Xun He, Feng Jin, Shuihua Zhang, Zhenwei Li
Abstract: The present invention provides compounds of formula (I) wherein A, R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
Type:
Grant
Filed:
November 16, 2020
Date of Patent:
November 28, 2023
Assignees:
Hoffmann-La Roche Inc., PTC Therapeutics, Inc.
Inventors:
Hasane Ratni, Luke Green, Marla L. Weetall, Nikolai A. Naryshkin
Abstract: The present disclosure relates to methods of treating gastrointestinal stromal tumors to a subject in need thereof, comprising administering to the subject a therapeutically effective amount of ripretinib or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
December 30, 2022
Date of Patent:
November 14, 2023
Assignee:
Deciphera Pharmaceuticals, LLC
Inventors:
Rodrigo Ruiz Soto, Oliver Rosen, Jama Pitman
Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
Type:
Grant
Filed:
September 17, 2020
Date of Patent:
November 14, 2023
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
John Patrick Maxwell, Paul S. Charifson, Qing Tang, Steven M. Ronkin, Katrina Lee Jackson, Albert Charles Pierce, David J. Lauffer, Pan Li, Simon Giroux, Jinwang Xu, Kevin Michael Cottrell, Mark A. Morris, Nathan D. Waal, John J. Court, Wenxin Gu, Hongbo Deng
Abstract: The present disclosure relates to a method for treating certain types of tumors or cancers, such as plexiform neurofibromas (PN), plexiform neurofibromas associated with neurofibromatosis type 1 (NF1-PN), by orally administering an effective amount of mirdametinib to the patient, where an amount of mirdametinib is administered on the first day of treatment to provide (i) an AUC0-tau less than 400 ng·h/mL, (ii) a Cmax no more than 40 ng/mL, or (iii) both.
Type:
Grant
Filed:
March 16, 2023
Date of Patent:
November 7, 2023
Assignee:
SPRINGWORKS THERAPEUTICS, INC.
Inventors:
Uchenna H Iloeje, Abraham J Langseth, Todd Shearer
Abstract: Disclosed are methods and compositions for the treatment of facioscapulohumeral muscular dystrophy. In some cases, the methods and compositions involve the use of kinase inhibitors include Src, Syk, Abl, Tie, Flt, ErbB, Trk, PRKDC, and Yes families to repress DUX4 expression in muscle cells. Further disclosed are methods and cell based assays for screening compounds for the treatment of facioscapulohumeral muscular dystrophy.
Type:
Grant
Filed:
July 14, 2021
Date of Patent:
November 7, 2023
Assignee:
Sonic Master Limited
Inventors:
Amanda Rickard, Uli Schmidt, Alexander Kiselyov