74733-30-5Relevant academic research and scientific papers
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
A Dual Modulator of Farnesoid X Receptor and Soluble Epoxide Hydrolase to Counter Nonalcoholic Steatohepatitis
Schmidt, Jurema,Rotter, Marco,Weiser, Tim,Wittmann, Sandra,Weizel, Lilia,Kaiser, Astrid,Heering, Jan,Goebel, Tamara,Angioni, Carlo,Wurglics, Mario,Paulke, Alexander,Geisslinger, Gerd,Kahnt, Astrid,Steinhilber, Dieter,Proschak, Ewgenij,Merk, Daniel
supporting information, p. 7703 - 7724 (2017/10/06)
Nonalcoholic steatohepatitis arising from Western diet and lifestyle is characterized by accumulation of fat in liver causing inflammation and fibrosis. It evolves as serious health burden with alarming incidence, but there is no satisfying pharmacological therapy to date. Considering the disease's multifactorial nature, modulation of multiple targets might provide superior therapeutic efficacy. In particular, farnesoid X receptor (FXR) activation that revealed antisteatotic and antifibrotic effects in clinical trials combined with inhibition of soluble epoxide hydrolase (sEH) as anti-inflammatory strategy promises synergies. To exploit this dual concept, we developed agents exerting partial FXR agonism and sEH inhibitory activity. Merging known pharmacophores and systematic exploration of the structure-activity relationship on both targets produced dual modulators with low nanomolar potency. Extensive in vitro characterization confirmed high dual efficacy in cellular context combined with low toxicity, and pilot in vivo data revealed favorable pharmacokinetics as well as engagement on both targets in vivo.
HETEROCYCLIC AMIDE DERIVATIVE AND MEDICINE CONTAINING SAME
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Paragraph 0309, (2015/10/28)
Compound represented by formula (I): wherein each symbol is as defined herein, exhibit TRPA1 antagonist activity, and are useful for the prophylaxis or treatment of diseases involving TRPA1 antagonist and TRPA1.
Mild Benzylic Monobromination of Methyl Toluates in Aqueous CTAB
Reddy, Kancharla Rajendar,Rajanna, Kamatala C.,Venkateswarlu, Marri,Saiprakash
, p. 2485 - 2487 (2015/07/27)
A strategy has been developed for the regioselective monobromination of methyl toluates by using tert-butylhydrogen peroxide and potassium bromide (TBHP/KBr) in a cetyltrimethylammonium bromide (CTAB) micellar medium. Ultrasonic and microwave-assisted protocols recorded increased rates and product yields under mild reaction conditions, coupled with a straightforward isolation procedure.
Histone Deacetylase Inhibitors
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Paragraph 0468, (2013/12/04)
This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
HISTONE DEACETYLASE INHIBITORS
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Page/Page column 97-98, (2012/09/21)
This invention relates to generally inhibiting histone deacetylase (HDAC) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
Heterobiaryl human immunodeficiency virus entry inhibitors
Lu, Rong-Jian,Tucker, John A.,Pickens, Jason,Ma, You-An,Zinevitch, Tatiana,Kirichenko, Olga,Konoplev, Vitalii,Kuznetsova, Svetlana,Sviridov, Sergey,Brahmachary, Enugurthi,Khasanov, Alisher,Mikel, Charles,Yang, Yang,Liu, Changhui,Wang, Jian,Freel, Stephanie,Fisher, Shelly,Sullivan, Alana,Zhou, Jiying,Stanfield-Oakley, Sherry,Baker, Brian,Sailstad, Jeff,Greenberg, Michael,Bolognesi, Dani,Bray, Brian,Koszalka, Barney,Jeffs, Peter,Jeffries, Cynthia,Chucholowski, Alexander,Sexton, Connie
supporting information; experimental part, p. 4481 - 4487 (2010/03/01)
Previously disclosed HIV (human immunodeficiency virus) attachment inhibitors, exemplified by BMS 806 (formally BMS378806, 1), are characterized by a substituted indole or azaindole ring linked to a benzoylpiperazine via a ketoamide or sulfonamide group. In the present report, we describe the discovery of a novel series of potent HIV entry inhibitors in which the indole or azaindole ring of previous inhibitors is replaced by a heterobiaryl group. Several of these analogues exhibited IC50 values of less than 5 nM in a pseudotyped antiviral assay, and compound 13k was demonstrated to exhibit potency and selectivity similar to those of 1 against a panel of clinical viral isolates. Moreover, current structure-activity relationship studies of these novel biaryl gp120 inhibitors revealed that around the biaryl, a fine crevice might exist in the gp120 binding site. Taken in sum, these data reveal a hitherto unsuspected flexibility in the structure-activity relationships for these inhibitors and suggest new avenues for exploration and gp120 inhibitor design. 2009 American Chemical Society.
SMALL MOLECULE BRADYKININ B1 RECEPTOR ANTAGONISTS
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Page/Page column 97-98, (2009/04/25)
Disclosed are compounds of formula (I) which are bradykinin B1 receptor (B1R) antagonists. These compounds are useful to treat diseases or relieve adverse symptoms associated with inflammation and pain. The invention encompasses novel compounds and acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases involving inflammation and pain.
Non-nucleoside reverse transcriptase inhibitors
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Page/Page column 39; 40, (2008/12/06)
The present invention provides for compounds useful for treating an HIV infection, or preventing an HIV infection, or treating AIDS or ARC. The compounds of the invention are of formula I wherein R1, R2, R3, R4, R5a, R5b, R6a, R6b and X are as herein defined. Also disclosed in the present invention are methods of treating an HIV infection with compounds defined herein and pharmaceutical compositions containing said compounds.
Optimization of sulfonamide derivatives as highly selective EP1 receptor antagonists
Naganawa, Atsushi,Matsui, Toshiaki,Ima, Masaki,Yoshida, Koji,Tsuruta, Hiroshi,Yamamoto, Shingo,Yamamoto, Hiroshi,Okada, Hiroki,Maruyama, Takayuki,Nakai, Hisao,Kondo, Kigen,Toda, Masaaki
, p. 7774 - 7789 (2007/10/03)
A series of 4-[(2-{isobutyl[(5-methyl-2-furyl)sulfonyl]amino}phenoxy)methyl]benzoic acids and 4-({2-[isobutyl(1,3-thiazol-2-ylsulfonyl)amino]phenoxy}methyl)benzoic acids were synthesized and evaluated for their EP receptor affinities and EP1 receptor anta
