112372-06-2Relevant articles and documents
FACTOR XIIA INHIBITORS
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Paragraph 00284; 00286, (2019/10/19)
This invention relates to compoundsof formula (I)and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.
Orally bioavailable highly potent HIV protease inhibitors against PI-resistant virus
Lu, Zhijian,Bohn, Joann,Rano, Tom,Rutkowski, Carrie A.,Simcoe, Amy L.,Olsen, David B.,Schleif, William A.,Carella, Anthony,Gabryelski, Lori,Jin, Lixia,Lin, Jiunn H.,Emini, Emilio,Chapman, Kevin,Tata, James R.
, p. 5311 - 5314 (2007/10/03)
Efforts directed to identifying potent HIV protease inhibitors (PI) have yielded a class of compounds that are not only very active against wild-type (NL4-3) HIV virus but also very potent against a panel of PI-resistant viral isolates. Chemistry and biol
Quinuclidines-substituted-multi-cyclic-heteroaryls for the treatment of disease
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, (2008/06/13)
The invention provides compounds of Formula I: 1where in W is 2These compounds may be in the form of pharmaceutical salts or compositions, racemic mixtures, or pure enantiomers thereof. The compounds of Formula I are useful to treat diseases or conditions in which α7 is known to be involved.
Synthesis and Evaluation of 2-Pyridinone Derivatives as HIV-1-Specific Reverse Transcriptase Inhibitors. 2. Analogues of 3-Aminopyridin-2(1H)-one
Saari, Walfred S.,Wai, John S.,Fisher, Thorsten E.,Thomas, Craig M.,Hoffman, Jacob M.,et al.
, p. 3792 - 3802 (2007/10/02)
A series of nonnulceoside 3-aminopyridin-2(1H)-one derivatives was synthesized and evaluated for HIV-1 RT inhibitory properties.Several analogs proved to be potent and highly selective antagonists with in vitro IC50 values as low as 19 nM in the enzyme assay using rC*dG as template*primer.Two compounds from this series, 3-amino>-5-ethyl-6-methylpyridin-2(1H)-one (34, L-697,639) and the corresponding 4,7-dichloro analogue (37, L-697,661) inhibited the spread of HIV-1 IIIb infection by 95percent in MT4 cell culture at concentrations of 25-50 nM and were selected for clinical trials as antiviral agents.
Furopyridines. VII. Preparation and Hydrolysis of 2-Cyano and 3-Cyano Derivatives of Furo-, Furo-, and Furopyridine
Morita, Hiroyuki,Shiotani, Shunsaku
, p. 373 - 376 (2007/10/02)
This paper describes the preparation and hydrolysis of 2-cyano and 3-cyano derivatives of furo-, furo-, and furopyridine.Treatment of furopyridines 1a, 1b and 1c with n-butyllithium in hexane-tetrahydrofuran at -70 deg C and subsequent addition of N,N-dimethylformamide yielded 2-formyl derivatives 2a, 2b and 2c.Dehydration of the oximes 4a, 4b and 4c of 2a, 2b and 2c gave 2-cyano compounds 5a, 5b and 5c, which were hydrolyzed to give 2-carboxylic acids, 6a, 6b and 6c, respectively.Reaction of 3-bromo compounds 7a, 7b and 7c with copper(I) cyanide in N,N-dimethylformamide afforded 3-cyano derivatives 8a, 8b and 8c.Alkaline hydrolysis of 8a, 8b and 8c gave compounds formed by fission of the 1-2 bond of furopyridines 9a, 9b and 9c, while acidic hydrolysis gave the corresponding carboxamides, 10a, 10b and 10c.