Abstract: The present invention provides heteroaryl ketone fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.
Type:
Grant
Filed:
September 13, 2019
Date of Patent:
April 13, 2021
Assignee:
Corcept Therapeutics, Inc.
Inventors:
Hazel Hunt, Tony Johnson, Nicholas Ray, Iain Walters
Abstract: The invention relates to an amorphous solid dispersion comprising elagolix sodium and at least one silicon-based inorganic compound and to a process for preparing the same. Furthermore, it relates to a pharmaceutical composition comprising said solid dispersion and one or more additional pharmaceutical acceptable excipient(s), wherein the pharmaceutical composition can be used as a medicament, in particular for the treatment of endometriosis and uterine fibroids.
Abstract: Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.
Type:
Grant
Filed:
March 15, 2018
Date of Patent:
March 30, 2021
Assignee:
TEMPLE UNIVERSITY-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
Inventors:
Benjamin E. Blass, Daniel J. Canney, Kevin M. Blattner
Abstract: Provided are compositions comprising Compound I having the following structure: or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
Abstract: In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be useful as Liver X-? receptor (LXR?) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
Type:
Grant
Filed:
October 9, 2017
Date of Patent:
March 30, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Michael T. Rudd, Zhaoyang Meng, Jenny Wai, David Jonathan Bennett, Edward J. Brnardic, Nigel J. Liverton, Shawn J. Stachel, Yongxin Han, Paul Tempest, Jiuxiang Zhu, Xuewang Xu
Abstract: The present invention relates to a solution for resisting destruction of living plants and a related method. A solution including a buffered amine oxide admixed with at least one material selected from the group consisting of insecticides and fungicides is applied to the living plant and provides a synergistically effective greater resistance to living plant deterioration than any of the individual buffered amine oxide, insecticides and fungicides achieve. A related method is disclosed.
Type:
Grant
Filed:
December 4, 2018
Date of Patent:
March 23, 2021
Assignee:
KOP-COAT, INC.
Inventors:
Ronald W. Clawson, Jr., Hans A. Ward, Kenneth Allen Cutler, Cameron R. Scott
Abstract: The present invention provides novel Compound (1) having tumor vascular remodeling effect and/or anti-CAF (Cancer Associated Fibroblasts) activity, or a pharmaceutically acceptable salt thereof, optionally in a pharmaceutically acceptable and medical uses thereof.
Type:
Grant
Filed:
April 3, 2018
Date of Patent:
March 23, 2021
Assignees:
President and Fellows of Harvard College, Eisai R&D Management Co., Ltd.
Abstract: The present invention includes composition and methods for treating stroke comprising: identifying a subject in need of treatment for a stroke; and providing the subject with a therapeutically effective amount of an Aquaporin-4 inhibitor that blocks a filter portion of an Aquaporin-4 channel region, and identifying modulators of the different aquaporin specific splice variants.
Abstract: The present disclosure provides methods of treating with a BTK inhibitor a blistering disease, in particular pemphigus vulgaris or pemphigus folliaceous in a mammal, use of a BTK inhibitor as a replacement therapy for corticosteroid therapy for diseases treatable with a corticosteroid, such as autoimmune or inflammatory disease and in particular where corticosteroids are used as first or second line therapy, and pharmaceutical formulations comprising the same.
Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
Abstract: Provided are compositions comprising Compound I having the following structure: or a pharmaceutically acceptable salt thereof, and a solubilizing agent; methods of making the same; and methods of using the same.
Type:
Grant
Filed:
July 12, 2019
Date of Patent:
March 9, 2021
Assignee:
Plexxikon Inc.
Inventors:
Prabha N. Ibrahim, Hamid Rezaei, Gary Conard Visor, Tomoari Kamo, Hiroshi Yamakose
Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.
Type:
Grant
Filed:
July 2, 2019
Date of Patent:
March 9, 2021
Assignee:
Neurocrine Biosciences, Inc.
Inventors:
Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Willy Moree, Martin Rowbottom, Warren Wade, Liren Zhao, Richard Lowe, Nicole Smith, Neil Ashweek, Yun-Fei Zhu
Abstract: This invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof. Specifically, the present invention provides a compound represented by formula (1) or a pharmaceutically acceptable salt thereof [Therein, A is O, S, or N—R6; ring G is a 5-membered or 6-membered aromatic ring, etc., including 1-3 heteroatoms selected from O, S and N as constituent atoms; R1 and R2 are each independently a hydrogen atom, a halogen atom, or an optionally-substituted C1-6 alkyl carbonyl group, etc.; R3, R4 and R5 are each independently a hydrogen atom, a halogen atom, or an optionally-substituted C1-6 alkyl carbonyl group, etc.; and R6 is a hydrogen atom or an optionally-substituted C1-6 alkyl group, etc.].
Type:
Grant
Filed:
December 27, 2018
Date of Patent:
March 2, 2021
Assignee:
Sumitomo Dainippon Pharma Oncology, Inc.
Abstract: Disclosed herein are spirocyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.
Type:
Grant
Filed:
October 3, 2017
Date of Patent:
March 2, 2021
Assignee:
Recurium IP Holdings, LLC
Inventors:
Peter Qinhua Huang, Mehmet Kahraman, Kevin Duane Bunker
Abstract: The present invention relates to anhydrous sugar alcohol flakes and a manufacturing method therefor and, more specifically, to a particular form of anhydrous sugar alcohol flakes capable of preventing or mitigating caking occurring during the storage of products, and to a manufacturing method therefor.
Abstract: CRF1 receptor antagonists have the potential to directly inhibit ACTH release in patients with CAH and thereby allow normalization of androgen production while using lower, more physiologic doses of hydrocortisone, and thus reducing treatment-associated side effects.
Abstract: The present invention relates to a 3,4-bipyridyl pyrazole derivative, and a preparation method therefor and a medical application thereof. Specifically, the present invention relates to a new 3,4-bipyridyl pyrazole derivative as shown in formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, a use of the derivative as a therapeutic agent, in particular as a TGF-? inhibitor, and a use of the derivative in the preparation of a drug which treats, prevents or reduces cancer mediated by TGF-? overexpression. The substituents in formula (I) have the same definitions as in the description.
Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
Type:
Grant
Filed:
April 8, 2019
Date of Patent:
January 26, 2021
Assignee:
Board of Regents, The University of Texas System
Inventors:
Kang Le, Michael J. Soth, Gang Liu, Philip Jones, Jason Bryant Cross, Timothy Joseph Mcafoos, Christopher L. Carroll, Richard T. Lewis
Abstract: The present invention provides compounds of Formula (I) wherein all variables are as defined in the specification, and compositions comprising any of such novel compounds. These compounds are APJ agonists which may be used as medicaments.
Type:
Grant
Filed:
June 14, 2017
Date of Patent:
January 12, 2021
Assignee:
Bristol-Myers Squibb Company
Inventors:
Ji Jiang, Heather Finlay, Soong-Hoon Kim, Wei Meng, George O. Tora