1256546-72-1Relevant academic research and scientific papers
CHEMICAL COMPOUNDS
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Paragraph 0266-0268, (2021/04/02)
The present disclosure describes novel compounds, or their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their medical uses. The compounds of the disclosure have activity as Janus kinase (JAK) inhibitors and are useful in the treatment or control of inflammation, auto-immune diseases, cancer, and other disorders and indications where modulation of JAK would be desirable. Also described herein are methods of treating inflammation, auto-immune diseases, cancer, and other conditions susceptible to inhibition of JAK by administering a compound herein described.
ETHANEDIAMINE-HETEROCYCLE DERIVATIVES AS INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASES
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Paragraph 0793, (2019/09/15)
The present invention relates to ethanediamine-heterocycle compounds that are able to act as inhibitors of PRMTs (protein arginine methyltransferases) for treating cancer and other diseases mediated by PRMTs.
Identification of potent, selective and orally bioavailable phenyl ((R)-3-phenylpyrrolidin-3-yl)sulfone analogues as RORγt inverse agonists
Lu, Zhonghui,Duan, James J.-W.,Xiao, Haiyun,Neels,Wu, Dauh-Rurng,Weigelt, Carolyn A.,Sack, John S.,Khan,Ruzanov, Max,An, Yongmi,Yarde, Melissa,Karmakar, Ananta,Vishwakrishnan, Sureshbabu,Baratam, Venkata,Shankarappa, Harisha,Vanteru, Sridhar,Babu, Venkatesh,Basha, Mushkin,Kumar Gupta, Arun,Kumaravel, Selvakumar,Mathur, Arvind,Zhao, Qihong,Salter-Cid, Luisa M.,Carter, Percy H.,Murali Dhar
, p. 2265 - 2269 (2019/07/03)
An X-ray crystal structure of one of our previously discovered RORγt inverse agonists bound to the RORγt ligand binding domain revealed that the cyclohexane carboxylic acid group of compound 2 plays a significant role in RORγt binding, forming four hydrog
Solid dispersions containing an apoptosis-inducing agent
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Page/Page column 265, (2019/03/15)
A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.
B-LACTAMASE INHIBITOR AND APPLICATION THEREOF
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Paragraph 0156; 0157, (2018/03/07)
The present invention relates to a compound of Formula (I)-(IV) useful as β-lactamase inhibitor, a pharmaceutically acceptable salt, ester, solvate or stereoisomer thereof, wherein R1, R2, M and ring A have definitions as those in the specification. The present invention further relates to methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and uses of these compounds. For example, the compounds of the present invention can be used as β-lactamase inhibitors, for treatment and/or prophylaxis of diseases caused by bacterial infections, solving drug-resistance problems caused by β-lactamases, especially bacterial drug-resistant diseases caused by type B metallo-β-lactamases.
CONDENSED RING HETEROCYCLIC COMPOUND
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Paragraph 0364, (2015/06/17)
The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. [wherein, R1 represents optionally substituted lower alkyl and the like, R2 represents optionally substituted lower alkyl and the like, R3 represents the formula (II): (wherein, n represents 0 or 1, R3a represents a hydrogen atom and the like, R3b represents a hydrogen atom and the like, and R3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W1 represents a nitrogen atom and the like, W2 represents a nitrogen atom and the like]
Oxabicyclooctane-linked novel bacterial topoisomerase inhibitors as broad spectrum antibacterial agents
Singh, Sheo B.,Kaelin, David E.,Wu, Jin,Miesel, Lynn,Tan, Christopher M.,Meinke, Peter T.,Olsen, David,Lagrutta, Armando,Bradley, Prudence,Lu, Jun,Patel, Sangita,Rickert, Keith W.,Smith, Robert F.,Soisson, Stephen,Wei, Changqing,Fukuda, Hideyuki,Kishii, Ryuta,Takei, Masaya,Fukuda, Yasumichi
supporting information, p. 609 - 614 (2014/06/09)
Bacterial resistance is eroding the clinical utility of existing antibiotics necessitating the discovery of new agents. Bacterial type II topoisomerase is a clinically validated, highly effective, and proven drug target. This target is amenable to inhibit
ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF
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Paragraph 00333, (2014/10/04)
Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
PYRAZOLE CARBOXAMIDE COMPOUNDS, COMPOSITIONS AND METHODS OF USE
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Page/Page column 95, (2014/03/21)
Provided herein are compounds of formula (AA): N N H HN O N N R R 6 A (R a ) p, (AA) stereoisomers or a pharmaceutically acceptable salt thereof, wherein A, R a, p, R and R 6 are defined herein, compositions including the compounds and methods of manufacturing and using the compounds for the treatment of diseases.
NEW BICYCLIC THIOPHENYLAMIDE COMPOUNDS
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Page/Page column 137, (2014/01/09)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and use thereof as fatty-acid binding protein (FABP) 4/5 inhibitors in the treatment of e.g. type 2 diabetes, atherosclerosis or cancer.
