165528-99-4Relevant academic research and scientific papers
tBuOK-Promoted Cyclization of Imines with Aryl Halides
Li, Ya-Wei,Zheng, Hong-Xing,Yang, Bo,Shan, Xiang-Huan,Qu, Jian-Ping,Kang, Yan-Biao
supporting information, p. 4553 - 4556 (2020/06/08)
A transition-metal-free indole synthesis using radical coupling of 2-halotoluenes and imines via the later-stage C-N bond construction was reported for the first time. It includes an aminyl radical generation by C-H cleaving addition of 2-halotoluenes to imines via the carbanion radical relay and an intramolecular coupling of aryl halides with aminyl radicals. One standard condition can be used for all halides including F, Cl, Br, and I. No extra oxidant or transition metal is required.
Arylaminoaryl-alkyl-substituted imidazolidine-2,4-diones, process for preparing them, medicaments comprising these compounds, and their use
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Page/Page column 70, (2009/09/07)
This invention relates to arylaminoaryl-alkyl-substituted imidazolidone-2,4-diones of formula (I) and also to their physiologically tolerated salts: Wherein R, R′, R1 to R10, A, D, E, G, L and p are as defined herein. The invention also relates to processes for preparing them, pharmaceutical compositions comprising them and their therapeutic use. The compounds are suitable, for example, as anti-obesity drugs and for treating cardiometabolic syndrome.
Benzimidazole derivatives bearing substituted biphenyls as hepatitis C virus NS5B RNA-dependent RNA polymerase inhibitors: Structure-activity relationship studies and identification of a potent and highly selective inhibitor JTK-109
Hirashima, Shintaro,Suzuki, Takayoshi,Ishida, Tomio,Noji, Satoru,Yata, Shinji,Ando, Izuru,Komatsu, Masakazu,Ikeda, Satoru,Hashimoto, Hiromasa
, p. 4721 - 4736 (2007/10/03)
Following the discovery of a new series of benzimidazole derivatives bearing a diarylmethyl group as inhibitors of hepatitis C virus NS5B RNA-dependent RNA polymerase (HCV NS5B RdRp), we extended the structure-activity relationship (SAR) study to analogue
Bicyclic heterocycles useful as serine protease inhibitors
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Page/Page column 31, (2010/02/14)
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or solvate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4, X
Biarylmethyl indolines, indoles and tetrahydroquinolines, useful as serine protease inhibitors
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Page 33, (2010/02/09)
The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt or hydrate form thereof, wherein the variables A, B, L1, L2, X1, X2, X3, X4 an
Bicyclic fibrinogen antagonists
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, (2008/06/13)
This invention relates to compounds of the formulae: wherein A1is O, S, N—R1or CHR1; A4is N—R4or CHR4; R2is a sidechain containing an acid or ester group; R1, R4and R5are substituents such as H, alkyl and aryl alkyl, and R6is a sidechain containing a nitrogen group; and pharmaceutically acceptable salts thereof, which are effective for inhibiting platelet aggregation, pharmaceutical compositions for effecting such activity, and a method for inhibiting platelet aggregation.
Bicyclic fibrinogen antagonists
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, (2008/06/13)
PCT No. PCT/US95/00248 Sec. 371 Date Jul. 3, 1996 Sec. 102(e) Date Jul. 3, 1996 PCT Filed Jan. 9, 1995 PCT Pub. No. WO96/18619 PCT Pub. Date Jul. 13, 1995Certain compounds within formula (I) are inhibitors of platelet aggregation: wherein A1 is NH or CH2;
Structure-activity relationships in 3-oxo-1,4-benzodiazepine-2-acetic acid GPIIb/IIIa antagonists. The 2-benzazepine series
Miller, William H.,Ali, Fadia E.,Bondinell, William E.,Callahan, James F.,Calvo, Raul R.,Eggleston, Drake S.,Haltiwanger, R. Curtis,Huffman, William F.,Hwang, Shing-Mei,Jakas, Dalia R.,Keenan, Richard M.,Koster, Paul F.,Ku, Thomas W.,Kwon, Chet,Newlander, Kenneth A.,Nichols, Andrew J.,Parker, Michael F.,Samanen, James M.,Southall, Linda S.,Takata, Dennis T.,Uzinskas, Irene N.,Valocik, Richard E.,Vasko-Moser, Janice A.,Wong, Angela S.,Yellin, Tobias O.,Yuan, Catherine C. K.
, p. 2481 - 2486 (2007/10/03)
In an investigation of the contribution of N-1 to the binding, antiaggregatory, and oral activity in 3-oxo-1,4-benzodiazepine-2-acetic acid based GPIIb/IIIa antagonists, a series of 2-benzazepine analogs, wherein N-1 of the 1,4-benzodiazepine nucleus has
Synthesis of a 2-benzazepine analog of a potent, nonpeptide GPIIb/IIIa antagonist
Miller, William H.,Newlander, Kenneth A.,Eggleston, Drake S.,Haltiwanger, R. Curtis
, p. 373 - 376 (2007/10/02)
The preparation of the 2-benzazepine derivative 3 as an analog of the potent, nonpeplide GPIIb/IIIa antagonist 2 is reported. The synthetic route employs as key steps a Heck arylation of dimethyl itaconate and a selective cyclization to form the aryl-fuse
