Abstract: Provided is an additive for imparting ultraviolet absorbency, or an additive for imparting a high refractive index, which has satisfactory compatibility with a resin serving as a matrix and can maintain high transparency even if added in high concentrations. Also provided is an additive with which the function of imparting both ultraviolet absorbency and a high refractive index can be realized by means of one kind of additive. This additive is represented by the following Formula (I): wherein at least one of R1a to R9a is a monovalent sulfur-containing group represented by the following Formula (i-1) or Formula (i-2): R10amSH??(i-1) R11anSR12a—SpR13a??(i-2) wherein R10a to R12a each represent a divalent hydrocarbon group or the like; and R13a represents a monovalent hydrocarbon group or the like.
Abstract: The disclosure discloses a sulfur-containing polycyclic-hydroxypyridone carboxamide analog against HIV and an application thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analog has a compound represented by the following formula (I) or a stereoisomer thereof or a pharmaceutically acceptable salt thereof. The sulfur-containing polycyclic-hydroxypyridone carboxamide analogs provided by the disclosure have good anti-HIV activity, and in particularly, compound 2, compound 18, compound 34 and compound 66 have strong inhibitory effects on HIV-1 replication in vitro, and the therapeutic index thereof against HIV is hundreds of times greater than that of the existing drugs TDF and Dolutegravir. The development of such the compounds is of great significance for the development of AIDS drugs and will bright good news to AIDS patients.
Abstract: The invention relates to compounds for treating and/or preventing obesity and obesity-related disorders. Particularly, the invention provides chromanone derivatives used as ATF3 inducer and for treating and/or preventing obesity and obesity-related disorders such as heart disease, hypertension, hyperlipidemia and diabetes.
Type:
Grant
Filed:
March 22, 2018
Date of Patent:
June 21, 2022
Assignees:
TAIPEI MEDICAL UNIVERSITY, NATIONAL RESEARCH INSTITUTE OF CHINESE MEDICINE, MINISTRY OF HEALTH AND WELFARE, ACADEMIA SINICA, BUDDHIST TZU CHI MEDICAL FOUNDATION
Inventors:
Heng Lin, Ming-jaw Don, Ching-feng Cheng, Jing-jy Cheng, Wen-shan Li, Hui-chen Ku, Hsiao-fen Li, Hsi-hsien Chen, W J Huang
Abstract: The present invention relates to a method for preparing an intermediate (Formula IV) of sodium elagolix. The intermediate is prepared by the following route. The method has advantages of simple and safe operation, high yield, less environmental pollution, good economic effect and suitability for industrial production, wherein R represents C1-C4 substituted or unsubstituted benzyl or allyl.
Abstract: The present disclosure relates to mTOR inhibitors. Specifically, the embodiments are directed to compounds and compositions inhibiting mTOR, methods of treating diseases mediated by mTOR, and methods of synthesizing these compounds.
Type:
Grant
Filed:
October 28, 2020
Date of Patent:
June 21, 2022
Assignee:
REVOLUTION MEDICINES, INC.
Inventors:
Jennifer Pitzen, G. Leslie Burnett, James Bradley Aggen
Abstract: p-phenylenediamine derivatives as potassium channel regulators and preparation methods and medical applications thereof. A compound represented by general formula A or a pharmaceutically acceptable salt thereof. A preparation method of the compound and a use of the same as a potassium channel opener.
Abstract: A di(hetero)aryl macrocyclic compound having an inhibitory effect on protein kinase activity, preparation and the use thereof. Specifically, disclosed are a di(hetero)aryl macrocyclic compound represented by formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug or an active metabolite thereof, a pharmaceutical composition comprising said compound and the derivative thereof, and methods of using the same, including methods of treating cancers, pain, neurological diseases, autoimmune diseases and inflammation.
Abstract: The present disclosure describes carbamate and urea compounds as novel multikinase inhibitors and methods for preparing them. The pharmaceutical compositions comprising such multikinase inhibitors and methods of using them for treating cancer, infectious diseases, and other disorders associated with kinases are also described.
Type:
Grant
Filed:
December 10, 2018
Date of Patent:
June 14, 2022
Assignee:
ANGEX PHARMACEUTICAL, INC.
Inventors:
Wen-Lian Wu, Zhiqiang Yang, Francis Lee, John Qiang Tan
Abstract: Compositions and methods for inhibits the binding of GTP to oncogenic mutant KRas are disclosed. These compositions may be used in method to treat a subject with cancer. In particular, the compositions may be used to treat cancers involving overactive Ras signaling.
Type:
Grant
Filed:
July 13, 2020
Date of Patent:
June 7, 2022
Assignees:
H. Lee Moffitt Cancer Center and Research Institute, Inc., Torrey Pines Institute for Molecular Studies
Inventors:
Said M. Sebti, Yangmei Li, Richard A. Houghten
Abstract: The invention provides substituted pyrrolo[1,2-a]pyrimidines 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 pyrrolo[1,2-a]pyrimidines compounds described herein include substituted 2,4-dimethyl-N-phenylpyrrolo[1,2-a]pyrimidine-8-carboxamide compounds and variants thereof.
Type:
Grant
Filed:
July 15, 2020
Date of Patent:
June 7, 2022
Assignee:
Bial—R&D Investments, S.A.
Inventors:
Renato T. Skerlj, Peter T. Lansbury, Andrew C. Good, Elyse Marie Josee Bourque, Richard B. Silverman, Dimitri Krainc, Jianbin Zheng
Abstract: Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Grant
Filed:
May 28, 2019
Date of Patent:
June 7, 2022
Assignee:
MERCK SHARP & DOHME CORP.
Inventors:
Shuwen He, Dane Clausen, Liangqin Guo, Yongxin Han, Xianhai Huang, Alexander Pasternak, Qinglin Pu, Dong Xiao, Li Xiao, Feng Ye, Hongjun Zhang
Abstract: The present invention provides an industrially advantageous method for producing a 3,5-disubstituted triazine compound that is useful as an active pharmaceutical ingredient. More specifically, the present invention provides a production method, whereby it becomes possible to efficiently produce a 3-oxo-5-substituted triazine in water without the need to isolate an intermediate that may have mutagenicity, and it also becomes possible to perform the production without the need to isolate a product in each of multiple steps. Namely, the present invention provides a method for producing a compound represented by formula I or a salt thereof, the method including a step of reacting a compound represented by the following formula IV or a salt thereof with a base in water, and optionally including a step of forming a salt thereof.
Abstract: A compound capable of being used as a tumor inhibitor, a preparation method therefor, and application thereof. The compound has a structure represented by general formula I; a stereoisomer, an enantiomer, a raceme, a cis/trans isomer, a tautomer, and an isotopic variant of the compound are comprised; the compound can be used separately or in combination with other drugs for treating tumors or inflammatory diseases, or for treating other disorders or diseases mediated by the activity of MDM2 and/or MDM4, and shows prominent curative activity.
Abstract: This invention relates to compounds useful as lysyl oxidase (LOX) and lysyl oxidase-like (LOXL) family member (LOXL1, LOXL2, LOXL3, LOXL4) inhibitors. In addition there are contemplated pharmaceutical compositions comprising the compounds and the use of the compounds in the treatment of conditions mediated by LOX and LOXL, for example cancer. In particular a LOX inhibitor such as the present compounds may be for use in the treatment of a cancer associated with EGFR. The present invention also contemplates the identification of biomarkers that predict responsiveness to a LOX inhibitor.
Type:
Grant
Filed:
October 12, 2018
Date of Patent:
May 10, 2022
Assignee:
The Institute of Cancer Research: Royal Cancer Hospital
Inventors:
Richard Marais, Caroline Springer, Dan Niculescu-Duvaz, Natalie Miller, Mohammed Aljarah, Alfonso Zambon, Leo Leung, Deborah Smithen, Michael Brown, Haoran Tang
Abstract: The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: (I), where R1, R2, R3, R4, R4?, R5, R6, X, and n are described herein.
Type:
Grant
Filed:
August 26, 2020
Date of Patent:
May 10, 2022
Assignee:
VALO HEALTH, INC.
Inventors:
David Joseph Guerin, Kenneth W. Bair, Justin A. Caravella, Stephanos Ioannidis, David R. Lancia, Jr., Hongbin Li, Steven Mischke, Pui Yee Ng, David Richard, Shawn E. R. Schiller, Tatiana Shelekhin, Zhongguo Wang
Abstract: The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R1 is hydrogen, halogen, lower alkyl, lower alkoxy or lower alkyl substituted by halogen, and may be the same or different, if two R1 occur; R2 is lower alkyl or a mono- or polydeutered derivative thereof, lower alkyl substituted by halogen or lower alkoxy, lower alkenyl unsubstituted or substituted by halogen, cycloalkyl or CH2-cycloalkyl unsubstituted or substituted by halogen, heterocycloalkyl or CH2-heterocycloalkyl unsubstituted or substituted by lower alkyl; R3 is halogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy substituted by halogen or S(O)2-lower alkyl; n is 1, 2 or 3; if n is >1, then R3 may be the same or different; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or to its corresponding enantiomer and/or an optical isomer and/or stereoisomer thereof.
Type:
Grant
Filed:
November 6, 2017
Date of Patent:
May 3, 2022
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Bjoern Bartels, Stefan Berchtold, Guido Galley, Annick Goergler, Roland Jakob-Roetne, Daniela Krummenacher, Anja Limberg, Werner Neidhart, Hasane Ratni, Michael Reutlinger, Rosa Maria Rodriguez Sarmiento, Christian Schnider
Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those benzodiazepine derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with central nervous system (CNS) disorders. In particular, it relates to the use of a ?5-containing GABAA receptor agonist (e.g.
Type:
Grant
Filed:
September 22, 2020
Date of Patent:
April 26, 2022
Assignee:
AGENEBIO, INC.
Inventors:
Belew Mekonnen, John A. Butera, Jianxing Huang
Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs) and/or desumoylating enzymes. In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase 7 or ubiquitin specific peptidase 7 (USP7). The invention further relates to the use of DUB or desumoylating inhibitors in the treatment of cancer. Described herein are compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1a, R1b, R1c and R1d each independently represent hydrogen, optionally substituted C1-C6 alkyl or R1a and R1b together form an optionally substituted C3-C6 cycloalkyl ring, or R1c and R1d together form an optionally substituted C3-C6 cycloalkyl ring; A is a 5 membered nitrogen-containing aromatic ring and is substituted with at least one optionally substituted 5 to 10 membered monocyclic or bicyclic heteroaryl or aryl ring attached through an optional linker.
Type:
Grant
Filed:
March 17, 2017
Date of Patent:
April 19, 2022
Assignee:
MISSION THERAPEUTICS LIMITED
Inventors:
Alison Jones, Mark Ian Kemp, Martin Lee Stockley, Michael David Woodrow
Abstract: The present invention is relates to an improved process for the preparation of pazopanib or a pharmaceutically acceptable salts thereof. The present invention also relates to novel polymorphic Forms of pazopanib hydrochloride, and its intermediates thereof.