194874-12-9Relevant academic research and scientific papers
Aryl tetrahydropyridine inhibitors of farnesyltransferase: Glycine, phenylalanine and histidine derivatives
Gwaltney II, Stephen L.,O'Connor, Stephen J.,Nelson, Lissa T. J.,Sullivan, Gerard M.,Imade, Hovis,Wang, Weibo,Hasvold, Lisa,Li, Qun,Cohen, Jerome,Gu, Wen-Zhen,Tahir, Stephen K.,Bauch, Joy,Marsh, Kennan,Ng, Shi-Chung,Frost, David J.,Zhang, Haiying,Muchmore, Steve,Jakob, Clarissa G.,Stoll, Vincent,Hutchins, Charles,Rosenberg, Saul H.,Sham, Hing L.
, p. 1359 - 1362 (2003)
Inhibitors of farnesyltransferase are effective against a variety of tumors in mouse models of cancer. Clinical trials to evaluate these agents in humans are ongoing. In our effort to develop new farnesyltransferase inhibitors, we have discovered a series of aryl tetrahydropyridines that incorporate substituted glycine, phenylalanine and histidine residues. The design, synthesis, SAR and biological properties of these compounds will be discussed.
PYRANOPYRAZOLE AND PYRAZOLOPYRIDINE IMMUNOMODULATORS FOR TREATMENT OF AUTOIMMUNE DISEASES
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Paragraph 0060; 0061, (2019/06/17)
Pyranoyrazoles and pyrazolopyridines of formula I or formula II are disclosed: (I), (II) These compounds inhibit Coagulation Factor Xlla in the presence of thrombin and other coagulation factors. They are useful to treat autoimmune diseases.
PYRAZOLOPYRIDINE DERIVATIVES FOR THE TREATMENT OF CANCER
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Page/Page column 200, (2017/12/29)
The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders such as cancer, inflammatory disorders and autoimmune diseases.
