Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
Type:
Grant
Filed:
June 19, 2018
Date of Patent:
July 5, 2022
Assignee:
MADRIGAL PHARMACEUTICALS, INC.
Inventors:
Neera Jain, Weiwen Ying, Dinesh U. Chimmanamada, Junyi Zhang, Amit Kale
Abstract: The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.
Type:
Grant
Filed:
October 29, 2020
Date of Patent:
July 5, 2022
Assignee:
Enanta Pharmaceuticals, Inc.
Inventors:
Joseph Panarese, Samuel Bartlett, Dexter Davis, Katherine Chong, Yat Sun Or
Abstract: Methods and pharmaceutical compositions containing gaboxadol or a pharmaceutically acceptable salt thereof for treating 1p36 deletion syndrome are provided.
Abstract: The present invention relates to the derivatives of compound of formula (I) and pharmaceutically acceptable salts thereof. The present invention further provides the methods of preparation of compound of formula (I) and use thereof as PRMT5 inhibitors. The compounds are useful as medicaments in the treatment of conditions where PRMT5 inhibition is desired, such as cancer, metabolic disorders, inflammation, autoimmune disease and hemoglobinopathies.
Abstract: An azatricyclic compound (as represented by Formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases are provided. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like.
Type:
Grant
Filed:
February 27, 2018
Date of Patent:
June 21, 2022
Assignee:
Betta Pharmaceuticals Co., Ltd.
Inventors:
Xiaofeng Xu, Jiabing Wang, Lieming Ding, Xiangyong Liu
Abstract: There is provided herein a compound of formula (I) wherein R1, R2, n, X, Q, L, m, R3 and p are as defined herein, which compounds are useful in the treatment of treatment of diseases characterised by impaired signalling of neurotrophins and/or other trophic factors, such as Alzheimer's disease and the like.
Abstract: The present invention belongs to the technical field of pharmaceuticals, and particularly relates to a compound of formula (I), a pharmaceutically acceptable salt thereof, an ester thereof or a stereoisomer of the compound, the salt or the ester, wherein R1, X1, X2, M, Ar, ring A, ring B and L are as defined in the specification. The present invention also relates to: a preparation method for the compound, a pharmaceutically acceptable salt thereof, an ester thereof or a stereoisomer of the compound, the salt or the ester; a pharmaceutical composition and pharmaceutical formulation containing the compound, the pharmaceutically acceptable salt, the ester or the stereoisomer of the compound, the salt or the ester; and a use of the compound, the pharmaceutically acceptable salt, the ester or the stereoisomer of the compound, the salt or the ester in the preparation of a medicament for treating and/or preventing FXR-mediated diseases.
Type:
Grant
Filed:
July 6, 2018
Date of Patent:
June 7, 2022
Assignee:
XUANZHU BIOPHARMACEUTICAL CO., LTD.
Inventors:
Wenkui Ken Fang, Bo Chen, Tingzhong Wang, Jing Cheng
Abstract: Substituted isoindolinones of Formula (I), methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat or ameliorate diseases, disorders, or conditions associated with protein malfunction, such as cancer, are provided.
Type:
Grant
Filed:
June 25, 2020
Date of Patent:
June 7, 2022
Assignee:
BioTheryX, Inc.
Inventors:
Kyle W. H. Chan, Aparajita Hoskote Chourasia, Paul E. Erdman, Leah M. Fung, Imelda Lam, Frank Mercurio, Robert W. Sullivan, Eduardo Torres
Abstract: Provided herein are fluoro-substituted porphyrin compounds, such as those having a structure represented by Formula (I), wherein R1 is a C1-C8 alkyl that is substituted with at least 1 fluorine (e.g., a C1-C8 alkyl substituted with 1-17 fluorine atoms); and X is an anion (e.g. a halogen ion (e.g., chloride, etc.), PF6, tosylate, besylate, and/or mesylate). Also provided herein are methods of making the fluoro-substituted porphyrin compounds, pharmaceutical formulations containing the same, and methods of use thereof.
Type:
Grant
Filed:
September 26, 2018
Date of Patent:
May 31, 2022
Assignee:
Duke University
Inventors:
Ines Batinic-Haberle, Artak Tovmasyan, Ivan Spasojevic
Abstract: Disclosed herein are novel methods of treating pain in a patient in need thereof by providing to the patient a selective dopamine D3 receptor antagonist/partial agonist which when used with an opioid analgesic, can mitigate the development of opioid dependence, by preventing the need for dose escalation while either maintaining the opioid analgesic effect or providing analgesia with a lower dose of the opioid. In addition, the D3 antagonists/partial agonists described herein may be used to augment the effectiveness of current Medication Assisted Treatment regimens (e.g. methadone or buprenorphine) for the treatment of opioid use disorders.
Type:
Grant
Filed:
September 9, 2019
Date of Patent:
May 24, 2022
Assignee:
THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES
Abstract: The present invention relates to imidazo-pyridinyl compounds, or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising such compounds and salts, and to methods of using such compounds, salts and compositions for the treatment of abnormal cell growth, including cancer, in a subject.
Type:
Grant
Filed:
July 13, 2020
Date of Patent:
May 24, 2022
Assignee:
Pfizer Inc.
Inventors:
Omar Ahmad, Andrew Fensome, Erik Alphie LaChapelle, Ethan Lawrence Fisher, Rayomand J. Unwalla, Jun Xiao, Lei Zhang
Abstract: The present invention relates to inhibitors of Transient Receptor Potential Channel 6 (TRPC6) protein activity. The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising a compound of the invention, a method for manufacturing compounds of the invention and therapeutic uses thereof.
Type:
Grant
Filed:
October 18, 2018
Date of Patent:
May 17, 2022
Assignee:
TEIJIN PHARMA LIMITED
Inventors:
Michael D. Bartberger, Nagasree Chakka, Hua Gao, Angel Guzman-Perez, Daniel B. Horne, Zihao Hua, Madeleine Kieffer, Daniel C. H. Lin, Benjamin Charles Milgram, Jane Panteleev, Laurie Schenkel, John Stellwagen, Matthew Weiss, Ryan D. White, Wei Zhao
Abstract: The present invention relates to the combination of activators of soluble guanylate cyclase (sGC activators) with mineralocorticoid receptor antagonists (MR antagonists) and to the use of the combination for the treatment and/or prophylaxis of cardiac and cardiovascular disorders, of renal and cardiorenal disorders, of pulmonary and cardiopulmonary disorders and also for the treatment and/or prophylaxis of fibrotic disorders.
Abstract: The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates.
Type:
Grant
Filed:
January 22, 2020
Date of Patent:
April 26, 2022
Inventors:
Joel Mercier, Laurent Provins, Celine Vermeiren, Yogesh Anil Sabnis
Abstract: The present invention is directed to a process for continuous production of copper (I) nitrotetrazolate (DBX-1) by reacting aqueous copper salt with aqueous 5-nitrotetrazolate salt in the presence of a reducing agent. All the reactants are introduced into a continuous flow reactor system, which is composed of a temperature controlled tubular reactor and a mixer that allows for radial mixing. An optional stirred tank reactor may also be incorporated into the process to complete the reaction and allow for crystal growth.
Type:
Grant
Filed:
October 17, 2019
Date of Patent:
April 26, 2022
Assignee:
The United States of America as Represented by the Secretary of the Army
Inventors:
Neha Mehta, Jon G. Bragg, Matthew L. Jorgensen, Andrew G. Pearsall, Jerry S. Salan, Daniel W. Ward
Abstract: The present invention relates to a novel thieno[3,2-b]pyridine-5(4H)-one derivative compound, a preparation method thereof, and a use thereof. The novel thieno[3,2-b]pyridine-5(4H)-one derivative compound according to the present invention is synthesized via an aza-[3+3] cyclization addition reaction using BOP, wherein the compound is obtained by synthesizing a 4-arylthiophen-3-amine in which aryl groups such as 4-piperidyl-C6H4, 4-pyrrolidyl-C6H4, 4-MeOC6H4, 3,4,5-(MeO)3C6H4, C6H5, 4-C6H5C6H4, and 4-F3COC6H4 are introduced via a synthesis process by a bromination reaction, a hydrolysis reaction, a decarboxylation reaction, and a Suzuki coupling reaction of methyl 3-aminothiophene carboxylate, and by synthesizing 4-arylthiophen-3-amine and mono-methyl fumarate via a formal aza-[3+3] cyclization addition reaction using BOP and conjugation.
Type:
Grant
Filed:
December 27, 2017
Date of Patent:
April 19, 2022
Inventors:
Jong Seok Lee, Dan Bi Sung, Bo Hyun Mun, Hyi Seung Lee, Yeon Ju Lee, Ji Hoon Lee, Hee Jae Shin, Sol Park
Abstract: Disclosed are compounds of Formula (I) or salts thereof, wherein G, R1, R5, R7, R8, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.
Type:
Grant
Filed:
December 19, 2018
Date of Patent:
April 19, 2022
Assignee:
Bristol-Myers Squibb Company
Inventors:
Alaric J. Dyckman, Dharmpal S. Dodd, Christopher P. Mussari, David R. Tortolani, Tasir Shamsul Haque, Shoshana L. Posy
Abstract: The present invention provides a salt and crystal form of a modified andrographolide compound and a preparation method and pharmaceutical use thereof.
Abstract: The present invention relates to a process for preparing cyclic carbonates of formula Ia or Ib or mixtures thereof (Ia) (Ib) comprising the process step: a) reacting a propargylic alcohol of formula II (II) with carbon dioxide in the presence of at least one transition metal catalyst TMC1, which comprises a transition metal selected from metals of groups 10, 11 and 12 of the periodic table of the elements according to IUPAC and at least one bulky ligand.
Type:
Grant
Filed:
August 14, 2018
Date of Patent:
April 5, 2022
Assignee:
BASF SE
Inventors:
Bilguun Bayarmagnai, Thomas Schaub, Verena Mormul, Peter Rudolf
Abstract: Provided herein are Ir(III) complexes comprising N-heterocyclic carbene ligand, method of synthesis of the Ir(III) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Ir(III) complexes under both dark and light conditions. Also provided is a method of detecting the Ir(III) complex in a biological system. Also provided is a method of making the Ir(III) complex. The Ir(III) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.
Type:
Grant
Filed:
July 31, 2019
Date of Patent:
March 29, 2022
Assignee:
THE UNIVERSITY OF HONG KONG
Inventors:
Chi Ming Che, Tsz Lung Lam, Ka Chung Tong