Abstract: The present application relates to pharmaceutical formulations and dosage forms of an AXL/MER inhibitor, or a pharmaceutically acceptable salt, solvate, or hydrate thereof, including methods of preparation thereof, which are useful in the treatment of AXL/MER mediated diseases such as cancer.
Abstract: Provided are novel compounds of Formula (I): Formula (I); and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with methyl modifying enzymes. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with methyl modifying enzymes.
Abstract: There is a method of treating or preventing pulmonary arterial hypertension or associated pulmonary arterial hypertension in a patient. The method has the step of systemically administering to the patient a therapeutically effective amount of one or more compounds: (S)-ethyl 8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroethoxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylate or a pharmaceutically acceptable salt thereof, or (S)-8-(2-amino-6-((R)-1-(5-chloro-[1,1?-biphenyl]-2-yl)-2,2,2-trifluoroeth-oxy)pyrimidin-4-yl)-2,8-diazaspiro[4.5]decane-3-carboxylic acid or a pharmaceutically acceptable salt thereof, or a combination of the foregoing. There is also a method of treating or preventing pulmonary arterial hypertension or associated pulmonary arterial hypertension in a patient by systemically administering a therapeutically effective amount of a THP1 inhibitor from about 1 mg/kg/day to about 50 mg/kg/day.
Type:
Grant
Filed:
July 18, 2022
Date of Patent:
February 27, 2024
Assignee:
Altavant Sciences GmbH
Inventors:
Steve Wring, Magdalena Alonso-Galicia, Thomas Pack, Julie Rurka, David Carpenter, Melissa Rhodes
Abstract: Provided are methods for treatment of Fabry disease in patients having HEK assay amenable mutations in ?-galactosidase A. Certain methods comprise administering migalastat or a salt thereof every other day, such as administering about 150 mg of migalastat hydrochloride every other day.
Abstract: The present disclosure related to methods of treating pruritus in a subject by topically administering detomidine, or a pharmaceutically acceptable salt thereof, to the subject.
Type:
Grant
Filed:
November 2, 2021
Date of Patent:
February 20, 2024
Assignee:
CLEXIO BIOSCIENCES LTD.
Inventors:
Yael Rosen, David Dangoor, Richard Fisher
Abstract: Provided is a composition for prevention or treatment of an allergic disease, the composition including an inotodiol compound and a chaga mushroom (Inonotus obliquus) extract including an inotodiol compound as an active ingredient. More particularly, it was found that when an inotodiol compound or a chaga mushroom extract containing an inotodiol compound as one of the active ingredients is administered to a mouse model in which a food allergy was induced, symptoms induced by the allergy were alleviated and cured. Thus, the inotodiol compound or the chaga mushroom extract containing an inotodiol compound as an active ingredient is expected to be useful as a composition for prevention or treatment of an allergic disease.
Type:
Grant
Filed:
May 24, 2018
Date of Patent:
February 13, 2024
Assignee:
CARBOEXPERT INC.
Inventors:
In Kyu Hwang, Young Ho Kim, Thi Minh Nguyet Nguyen, Jong Seong Kang
Abstract: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I), R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAK inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.
Type:
Grant
Filed:
May 6, 2019
Date of Patent:
February 6, 2024
Assignee:
HINOVA PHARMACEUTICALS INC.
Inventors:
Wu Du, Yu Li, Kun Wen, Xinghai Li, Yuanwei Chen
Abstract: The present disclosure relates to: a) crystalline forms of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide; b) pharmaceutical compositions comprising one or more crystalline forms of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide, and, optionally, one or more pharmaceutically acceptable carriers; c) methods of treating a tumor a cancer, or a Rasopathy disorder by administering one or more crystalline forms of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide to a subject in need thereof; and methods of producing essentially pure Form IV of N—((R)-2,3-dihydroxypropoxy)-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-benzamide.
Type:
Grant
Filed:
June 14, 2022
Date of Patent:
January 30, 2024
Assignee:
SPRINGWORKS THERAPEUTICS, INC.
Inventors:
Kristin Patterson, Jiping Liu, Ricky Wayne Couch, Peter Gregory Varlashkin, Mai Li, Yonghong Gan
Abstract: The invention provides compositions, kits, and methods for inducing growth arrest, differentiation, or senescence of cancer cells that express thymine DNA glycosylase, and treating the cancer accordingly. The methods comprise inhibiting expression or biologic activity of thymine DNA glycosylase in cancer cells. Inhibition of thymine DNA glycosylase in cancer cells may induce the cells to revert to a healthy, non-cancerous phenotype and/or may induce the cells to senesce. Cancer cells include melanoma, lung, prostate, pancreatic, ovarian, brain, colon, recto-sigmoid colon, and breast cancer cells.
Type:
Grant
Filed:
June 25, 2021
Date of Patent:
January 30, 2024
Inventors:
Alfonso Bellacosa, Rossella Tricarico, Tim Yen, Vikram Bhattacharjee, Pietro Mancuso, Lionel Larue, Irwin Davidson
Abstract: The present disclosure provides compositions and methods for the treatment of pathogen-induced and/or chemical-induced lung injury, for regenerating lung epithelial cells following lung injury, for treating cancer, and for sensitizing a subject suffering from cancer to a chemotherapeutic agent.
Abstract: A method of treating a glycosylation-defective protein associated disease or disorder in a subject, the method includes administering to the subject a therapeutically effective amount of a Sarco/ER ATPase (SERCA) inhibitor.
Type:
Grant
Filed:
September 7, 2021
Date of Patent:
January 9, 2024
Assignee:
CASE WESTERN RESERVE UNIVERSITY
Inventors:
Alagramam N. Kumar, Suhasini Gopal Ramanujam
Abstract: Described herein are compounds having the following structure: formula (I) or a stereoisomer, pharmaceutically acceptable salt, oxide, or solvate thereof. Also disclosed are compositions containing the compounds, methods of inhibiting activity of DYRK1 A in a cell, methods of increasing cell proliferation in a population of pancreatic beta cells, methods of treating a subject for a condition associated with insufficient insulin secretion, and methods of treating a subject for a neurological disorder.
Type:
Grant
Filed:
March 20, 2019
Date of Patent:
January 9, 2024
Assignee:
ICAHN SCHOOL OF MEDICINE AT MOUNT SINAI
Inventors:
Kunal Kumar, Peng Wang, Roberto Sanchez, Adolfo Garcia Ocaña, Andrew Stewart, Robert Devita
Abstract: The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIi): wherein: R2?H or Me; R3?H or Me; R4=Alkyl; R5?O-Alkyl; and Alkyl=aliphatic C1-C4 alkyl. The present disclosure further provides methods of making compounds of general formula (VIIIi), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIi), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIi) to the subject.
Type:
Grant
Filed:
July 25, 2023
Date of Patent:
January 9, 2024
Assignee:
PTC Innovations, LLC
Inventors:
Pendleton Wickersham, Stephen Bendel, Todd Mathis, Christian Warren
Abstract: The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIk): wherein: R2?H or Me; R3?H or Me; R4=Alkyl; R5?O-Alkyl; and Alkyl=aliphatic C1-C4 alkyl. The present disclosure further provides methods of making compounds of general formula (VIIIk), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIk), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIk) to the subject.
Type:
Grant
Filed:
July 25, 2023
Date of Patent:
January 9, 2024
Assignee:
PTC Innovations, LLC
Inventors:
Pendleton Wickersham, Stephen Bendel, Todd Mathis, Christian Warren
Abstract: The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (XIII): wherein: R8=NH2, NH(Me), N(Me)2, The present disclosure further provides methods of making compounds of general formula (XIII), compositions comprising a therapeutically effective amount of a compound of general formula (XIII), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (XIII) to the subject.
Type:
Grant
Filed:
July 26, 2023
Date of Patent:
January 9, 2024
Assignee:
PTC Innovations, LLC
Inventors:
Pendleton Wickersham, Stephen Bendel, Todd Mathis, Christian Warren
Abstract: Provided herein are compounds, crystalline forms, and pharmaceutical compositions of Compound 1 and/or Compound 2. Also provided are methods of treating a disease or disorder such as a cancer or infectious disease that comprises administering to a subject in need thereof one or more of the compounds or compositions of the present disclosure.
Abstract: Described herein are compounds of Formula I: wherein R1-R6 are as described herein, for use in the treatment of a coronavirus infection; a method of inhibiting a coronavirus 3CL protease, by contacting the 3CL protease with a compound of Formula I; as well as methods pharmaceutical composition comprising a compound of Formula I and at least one phospholipid, wherein a weight ratio of the phospholipid(s) to the compound in the composition is in a range of from 10:1 to 1:10. Further described herein is a method of treating a coronavirus infection in a subject in need thereof, by administering to the subject at least one compound that exhibits at least two of: inhibition of an activity of a 3CL protease of the coronavirus; inhibition of inflammation in the subject; and inhibition of autophagy in the subject.
Abstract: The present disclosure provides for methods of treating a patient with a CYP3A4 substrate drug, wherein the patient is treated with posaconazole. In some embodiments, the patient stops posaconazole treatment, waits for at least 3 days, and then is treated with the CYP3A4 substrate drug as soon as it is safe to do so. In some embodiments, treatment with the CYP3A4 substrate drug is delayed for about 3-42 days after stopping posaconazole. In some embodiments, the patient is treated with a reduced dose of the CYP3A4 substrate drug for about 3-42 days.
Type:
Grant
Filed:
March 8, 2023
Date of Patent:
January 2, 2024
Assignee:
BOW RIVER LLC
Inventors:
Sundar Srinivasan, Christina Chow Wallen
Abstract: The present disclosure provides compounds useful as anesthetics, such as topical anesthetics, of general formula (VIIIg): wherein: R2=H or Me; R3=H or Me; R4=Alkyl; R5=O-Alkyl; and Alkyl=aliphatic C1-C4 alkyl. The present disclosure further provides methods of making compounds of general formula (VIIIg), compositions comprising a therapeutically effective amount of a compound of general formula (VIIIg), and methods of treating or preventing pain in a subject by administering (e.g., topically applying) compositions comprising an effective amount of a compound of general formula (VIIIg) to the subject.
Type:
Grant
Filed:
July 25, 2023
Date of Patent:
December 19, 2023
Assignee:
PTC Innovations, LLC
Inventors:
Pendleton Wickersham, Stephen Bendel, Todd Mathis, Christian Warren