Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
February 24, 2020
Date of Patent:
June 29, 2021
Assignee:
ORION CORPORATION
Inventors:
Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Koivikko, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
Abstract: A set of small molecules ER? biomodulators that kill therapy-resistant ER? positive breast, ovarian, and endometrial cancer cells. These small molecules have increased therapeutic potential because of an increased ability to kill therapy-resistant breast cancer cells compared to BHPI and other conventional therapies (endocrine therapies, tamoxifen and fulvestrant/ICI). The new compounds do not only inhibit proliferation of the cancer cells but actually kills them, which prevents reactivation of tumors years later.
Type:
Grant
Filed:
February 26, 2020
Date of Patent:
June 29, 2021
Assignee:
The Board of Trustees of the University of Illinois
Inventors:
David J. Shapiro, Paul J. Hergenrother, Matthew W. Boudreau
Abstract: The present invention is a method of treating or preventing Mycobacterium tuberculosis infection in a subject by administering to the subject an effective amount of oxazolidinone, specifically (N-(((S)-3-(dibenzo[b,e][1,4]dioxin-7-yl)-2-oxooxazolidin-5-yl)methyl)acetamide) or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof.
Type:
Grant
Filed:
February 17, 2017
Date of Patent:
June 22, 2021
Assignees:
The Johns Hopkins University, University of St. Thomas
Abstract: Described herein are liver X receptor (LXR) modulators and methods of utilizing LXR modulators in the treatment of LXR-associated diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
Abstract: In a 1,3-dipolar compound of formula Q-A-B, Q comprises a dipole containing at least and preferably one nitrogen atom, A, which is preferably divalent, is an atom or a group of atoms connecting Q to B, and B comprises an imidazole ring. An unsaturated polymer modified by grafting the 1,3-dipolar compound is also disclosed.
Type:
Grant
Filed:
December 21, 2018
Date of Patent:
June 15, 2021
Assignee:
COMPAGNIE GENERALE DES ETABLISSEMENTS MICHELIN
Abstract: Disclosed is a pyrazole amide compound as represented by general formula I, wherein, R1 is selected from hydrogen, C1-C4 alkyl, C2-C6 alkenyl and C2-C6 alkyl; and R2 and R3 can be the same or different, and are respectively and independently selected from the C1-C6 alkyl. The general formula I compound has an excellent bactericidal activity, and can be used to prevent and control fungal diseases.
Type:
Grant
Filed:
November 24, 2014
Date of Patent:
June 15, 2021
Assignee:
SHENYANG SINOCHEM AGROCHEMICALS R & D CO., LTD.
Inventors:
Liang Lv, Yugang Li, Zhonggang Shan, Shasha Wu, Bin Wang, Jiyong Liu, Peng Liu, Jizhong Zhou, Huibin Yang, Bin Li
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof. Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Type:
Grant
Filed:
March 23, 2018
Date of Patent:
June 15, 2021
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Liangqin Guo, Yongxin Han, Kun Liu, Shuwen He, Joseph Kozlowski, Ravi Nargund, Wensheng Yu, Hongjun Zhang, Qinglin Pu, Derun Li, Abdelghani Achab, Guoqing Li
Abstract: The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
Type:
Grant
Filed:
September 18, 2019
Date of Patent:
June 8, 2021
Assignee:
Firmenich Incorporated
Inventors:
Lyudmyla Chumakova, Andrew Patron, Chad Priest, Donald Karanewsky, Rachel Kimmich, Brant Clayton Boren, Jeffrey Robert Hammaker, Volodymyr Chumakov, Wen Zhao, Alain Noncovich, Jane Ung
Abstract: The present invention relates to compounds of Formula I, a stereoisomer, enantiomer, a pharmaceutically acceptable salt or an amino acid conjugate thereof; wherein variables are as defined herein; and their pharmaceutical compositions, which are useful as modulators of the activity of Farnesoid X receptors (FXR).
Type:
Grant
Filed:
April 21, 2020
Date of Patent:
June 1, 2021
Assignee:
Novartis AG
Inventors:
Donatella Chianelli, Runyan Li, Valentina Molteni, John Nelson, Jason Thomas Roland, Paul Vincent Rucker, David Charles Tully, Xiaoyang Wang, Liladhar Murlidhar Waykole, Yubo Zhang, Bo Zhou
Abstract: This invention relates to acrystalline form of (10R)-7-amino-12-fluoro-2,10,16-trimethyl-5-oxo-10,15,16,17-tetrahydro-2H-8,4-(metheno)pyrazolo[4,3-h] [2,5,11]benzoxadiazacyclo-tetradecine-3-carbonitrile (lorlatinib) free base (Form 7). This invention also relates to pharmaceutical compositions comprising Form 7, and to methods of using Form 7 and such compositions in the treatment of abnormal cell growth, such as cancer, in a mammal.
Type:
Grant
Filed:
August 8, 2019
Date of Patent:
June 1, 2021
Assignee:
Pfizer Inc.
Inventors:
Klimentina Dimitrova Pencheva, Melissa Jane Birch, Stephen Mark McAllister, Martin Gregory Rowland, Ian Leonard Smales
Abstract: An object of the present invention is to provide a methyllactam ring compound that has an SGLT1 inhibitory activity and is useful for a drug, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof. A compound of Formula [I]: or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.
Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
Abstract: Compounds (citric acid derivatives) represented by formulas (1) and (2) below are novel compounds having an inhibitory effect against liver disorder and can be used as liver disorder inhibitors and food additives (wherein R1 represents a C1 to C3 alkyl group optionally having a carboxyl group or a hydroxyl group, and R2 represents a hydrogen atom, or R1 and R2 optionally form a cyclic structure together to represent a C2 to C3 alkylene chain).
Type:
Grant
Filed:
October 15, 2019
Date of Patent:
May 11, 2021
Assignees:
ADABIO CO., LTD., OTSUKA PHARMACEUTICAL FACTORY, INC.
Abstract: Disclosed herein is a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I). Also disclosed herein are uses of the compounds disclosed herein in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising a compound disclosed herein. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder.
Abstract: Pyrazole compounds substituted with heteroaryl or pharmaceutically acceptable salts thereof that have an SGLT1 inhibitory activity and are useful for a drug, pharmaceutical compositions comprising the same, and pharmaceutical use thereof are disclosed. Specifically, a compound of Formula [X]: wherein R1 is hydrogen or halogen, R2 is C1-6 alkyl or halo-C1-6 alkyl, Ring Het is substituted pyridyl or optionally substituted pyrazinyl, pyrimidinyl, or pyridazinyl, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising it, and pharmaceutical use thereof is provided.
Abstract: The present disclosure relates generally to compounds which bind to the NR1H4 receptor (FXR) and act as agonists of FXR. The disclosure further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
Abstract: The present invention generally relates to 6-amino-2,4-dihydropyrano [2,3-c] pyrazoles as a ubiquitin specific protease 7(USP7) inhibitor useful for the treatment of diseases mediated by malfunction of USP7, such as inflammation, cancer, and immunological disorders. The invention described herein also pertains to pharmaceutical compositions and methods for treating diseases mediated by malfunction of USP7, in mammals using compounds disclosed herein.
Abstract: A compound for inhibiting IDO represented by the following general formula I, wherein a bond represented by a wavy line “” indicates the structure which represents independently a cis-isomer, a trans-isomer, or a mixture of cis- and trans-isomers; R1 and R2 are each independently selected from the group consisting of H, halogen, alkyl, alkoxyl, and haloalkyl; R3 is selected from the group consisting of cyclopentyl, cyclohexyl, piperazinyl, and piperidyl; and the substitution positions of R3 are optionally substituted at 1,2 position, 1,3 position or 1,4 position; m and n are an integer number independently selected from 0 to 5. The compound has a strong inhibiting effect on IDO and can be used to manufacture an IDO inhibitor for the prevention and/or treatment of an IDO-mediated disease with the pathologic features of the tryptophan metabolic pathway.