146137-79-3Relevant academic research and scientific papers
Synthesis of 5-cyanoindazole and 1-methyl and 1-aryl-5-cyanoindazoles
Halley, Frank,Sava, Xavier
, p. 1199 - 1207 (1997)
5-Cyanoindazoles are conveniently prepared in two to three steps from commercially available 5-bromo-2-fluorobenzaldehyde.
Selective Metalation and Functionalization of Fluorinated Nitriles Using 2,2,6,6-Tetramethylpiperidyl Bases
Dos Santos, Thiago,Orenha, Henrique P.,Murie, Valter E.,Vessecchi, Ricardo,Clososki, Giuliano C.
supporting information, p. 7396 - 7400 (2021/10/01)
We have accomplished regioselective deprotometalation of aromatic and heteroaromatic nitriles via (TMP)2Zn·2MgCl2·2LiCl and TMPMgCl·LiCl (TMP = 2,2,6,6-tetramethylpiperidyl) with the exploration of new and scarcely investigated metalation positions. Regio
A 3 - ethyl -4 - fluoro phenyl nitrile of preparation method (by machine translation)
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Paragraph 0008; 0009, (2019/01/08)
The invention discloses a 3 - ethyl - 4 - fluoro phenyl nitrile of preparation method, the method to the fluoro phenyl nitrile as the starting material, through the hydroformylation, Wittig reaction, obtaining the catalytic hydrogenation. (by machine tran
CATECHOL DIETHERS AS POTENT ANTI-HIV AGENTS
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Page/Page column 63, (2013/04/25)
The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or sec
Computationally-guided optimization of a docking hit to yield catechol diethers as potent anti-HIV agents
Bollini, Mariela,Domaoal, Robert A.,Thakur, Vinay V.,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Anderson, Karen S.,Jorgensen, William L.
supporting information; experimental part, p. 8582 - 8591 (2012/02/02)
A 5-μM docking hit has been optimized to an extraordinarily potent (55 pM) non-nucleoside inhibitor of HIV reverse transcriptase. Use of free energy perturbation (FEP) calculations to predict relative free energies of binding aided the optimizations by identifying optimal substitution patterns for phenyl rings and a linker. The most potent resultant catechol diethers feature terminal uracil and cyanovinylphenyl groups. A halogen bond with Pro95 likely contributes to the extreme potency of compound 42. In addition, several examples are provided illustrating failures of attempted grafting of a substructure from a very active compound onto a seemingly related scaffold to improve its activity. (Figure presented)
HETERO COMPOUND
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Page/Page column 30-31, (2009/01/24)
[Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 a
Indazole compounds, compositions thereof and methods of treatment therewith
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, (2008/06/13)
This invention is generally directed to the use of Indazole Compounds for treating or preventing diseases associated with protein kinases, including tyrosine kinases, such as proliferative diseases, inflammatory diseases, abnormal angiogenesis and diseases related thereto, atherosclerosis, macular degeneration, diabetes, obesity, pain and others. The methods comprise the administration to a patient in need thereof of an effective amount of an indazole compound that inhibits, modulates or regulates tyrosine kinase signal transduction. Novel indazole compounds or pharmaceutically acceptable salt thereof are presented herein.
Methods for treating an inflammatory condition or inhibiting JNK
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, (2008/06/13)
This invention is generally directed to Indazole Derivatives having the following structure: 1 or pharmaceutically acceptable salt thereof, wherein R1, R2 and A are as defined herein. Such compounds have utility in the treatment of a wide range of diseases and disorders that are responsive to JNK inhibition, such as an inflammatory disease or disorder. Thus, methods of treating such diseases and disorders are also disclosed, as are pharmaceutical compositions containing one or more compounds of the above compounds.
Thrombin inhibitors
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, (2008/06/13)
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is NY or O; c is CY2or N; d is CY3or N; e is CY4or N; f is CY5or N; g is CY6or N; Y4, Y5, and Y6are independently hydrogen, C1-4alkyl, or halogen; Y1and Y2are independently hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, NH2, OH or C1-4alkoxy, and Y3is hydrogen, C1-4alkyl, C3-7cycloalkyl, halogen, —CN, NH2, OH or C1-4alkoxy; A is and W, W1, R1, R3, R4, R5, X and Z are defined in the specification.
Design, synthesis and structure-activity relationships of benzoxazinone-based factor Xa inhibitors
Huang, Wenrong,Zhang, Penglie,Zuckett, Jingmei F.,Wang, Lingyan,Woolfrey, John,Song, Yonghong,Jia, Zhaozhong J.,Clizbe, Lane A.,Su, Ting,Tran, Katherine,Huang, Brian,Wong, Paul,Sinha, Uma,Park, Gary,Reed, Andrea,Malinowski, John,Hollenbach, Stanley J.,Scarborough, Robert M.,Zhu, Bing-Yan
, p. 561 - 566 (2007/10/03)
A series of benzoxazinone derivatives was designed and synthesized as factor Xa inhibitors. We demonstrated that the naphthyl moiety in the aniline-based compounds 1 and 2 can be replaced with benzene-fused heterobicycles and biaryls to give factor Xa inh
