2985-50-4Relevant academic research and scientific papers
Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors
Yamashita, Dennis S.,Marquis, Robert W.,Xie, Ren,Nidamarthy, Sirishkumar D.,Oh, Hye-Ja,Jeong, Jae U.,Erhard, Karl F.,Ward, Keith W.,Roethke, Theresa J.,Smith, Brian R.,Cheng,Geng, Xiaoliu,Lin, Fan,Offen, Priscilla H.,Wang, Bing,Nevins, Neysa,Head, Martha S.,Haltiwanger, R. Curtis,Sarjeant, Amy A. Narducci,Liable-Sands, Louise M.,Zhao, Baoguang,Smith, Ward W.,Janson, Cheryl A.,Gao, Enoch,Tomaszek, Thaddeus,McQueney, Michael,James, Ian E.,Gress, Catherine J.,Zembryki, Denise L.,Lark, Michael W.,Veber, Daniel F.
, p. 1597 - 1612 (2006)
The syntheses, in vitro characterizations, and rat and monkey in vivo pharmacokinetic profiles of a series of 5-, 6-, and 7-methyl-substituted azepanone-based cathepsin K inhibitors are described. Depending on the particular regiochemical substitution and
Bisheterocycle substituted oxa-spiro derivative, and preparation method and medical application thereof
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Paragraph 0224-0226, (2020/09/23)
The invention relates to a bisheterocyclic substituted oxa-spiro derivative, and a preparation method and medical application thereof. Specifically, the invention discloses compounds of formula (I) and formula (II) or pharmaceutically acceptable salts, stereoisomers or solvates thereof, and a preparation method and application thereof. Each group in the formulas is as defined in the specificationand claims in detail.
Base-catalysed intramolecular hydroamination of vinyl sulfiies
Quinet, Coralie,Sampoux, Laetitia,Marko, Istvan E.
supporting information; experimental part, p. 1806 - 1811 (2009/09/06)
Small amounts of n-butyllithium catalyse the highly efficient hydroamination of a large variety of vinyl sulfides. This novel methodology offers an easy access to a wide range of nitrogen heterocycles, including simple pyrrolidines and piperidines, as well as more complex bicyclic compounds. Subsequent transformations of the sulfur group led to the formation of functionalised alkaloid-like substructures. Wiley-VCH Verlag GmbH & Co. KGaA.
Protease inhibitors
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, (2008/06/13)
The present invention provides C1-6alkyl-4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease; and parasitic diseases, including malaria, by administering to a patient in need thereof one or more compounds of the present invention.
P(RNCH2CH2)3N: Efficient 1,4-addition catalysts
Kisanga, Philip B.,Ilankumaran, Palanichamy,Fetterly, Brandon M.,Verkade, John G.
, p. 3555 - 3560 (2007/10/03)
The 1,4-addition of primary alcohols, higher nitroalkanes, and a Schiff's base of an α-amino ester to α,β-unsaturated substrates produces the corresponding products in moderate to excellent yields when carried out at -63 to 70°C in the presence of catalytic amounts of the nonionic strong bases P(RNCH2CH2)3N (R = Me, i-Pr, i-Bu) in isobutyronitrile. Diastereoselectivity for the anti form of the product is high in the case of the Schiff's base in the absence of lithium ion. These catalysts are easily removed from the product by either column filtration through silica gel or via aqueous workup.
