34099-69-9Relevant academic research and scientific papers
Pyrazolobenzodiazepines: Part I. Synthesis and SAR of a potent class of kinase inhibitors
Liu, Jin-Jun,Daniewski, Irena,Ding, Qingjie,Higgins, Brian,Ju, Grace,Kolinsky, Kenneth,Konzelmann, Fred,Lukacs, Christine,Pizzolato, Giacomo,Rossman, Pamela,Swain, Amy,Thakkar, Kshitij,Wei, Chung-Chen,Miklowski, Dorota,Yang, Hong,Yin, Xuefeng,Wovkulich, Peter M.
scheme or table, p. 5984 - 5987 (2010/10/21)
A novel series of pyrazolobenzodiazepines 3 has been identified as potent inhibitors of cyclin-dependent kinase 2 (CDK2). Their synthesis and structure-activity relationships (SAR) are described. Representative compounds from this class reversibly inhibit CDK2 activity in vitro, and block cell cycle progression in human tumor cell lines. Further exploration has revealed that this class of compounds inhibits several kinases that play critical roles in cancer cell growth and division as well as tumor angiogenesis. Together, these properties suggest a compelling basis for their use as antitumor agents.
Reactions of 1,4-benzodiazepinic N-nitrosoamidines with tosylmethyl isocyanide: A novel synthesis of midazolam
Del Pozo, Carlos,Macias, Alberto,Alonso, Eduardo,Gonzalez, Javier
, p. 2697 - 2703 (2007/10/03)
Reaction of 1,4-benzodiazepinic N-nitrosoamidines, used as synthetic equivalents of imidoyl chlorides, with the monoanion of tosylmethyl isocyanide is described. The process gives entry to 3-(4-tosyl)imidazo[1,5-a][1,4] benzodiazepines, compounds which have not been described yet in the literature. These systems can be derivatized to the corresponding trisubstituted 1,4-benzodiazepines by alkylation or acylation of the imidazole ring. These new heterocyclic derivatives are potentially useful in the field of medicinal chemistry. In addition, midazolam 3, the anesthetic properties of which are well established, can be easily prepared in one step by desulfonylation of compound 7a.
Therapeutic agent for osteoporosis and diazepine compound
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, (2008/06/13)
A therapeutic agent for osteoporosis, comprising an azepine compound of the formula STR1 wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof as an active ingredient, a method for treating osteoporosis comprising administering said compound and a use of said compound for the production of a therapeutic agent for osteoporosis. The compounds of the formula (I) have superior bone resorption-inhibitory activity and act to reduce the increased amount of calcium in blood serum, which is caused by bone resorption. Accordingly, these compounds are usable as pharmaceutical agents to effectively inhibit bone resorption, to prevent decrease of bone mass and to prevent or suppress the increase of calcium amount in blood serum which is caused by the progress of bone resorption, with regard to Paget's disease, hypercalcemia, osteoporosis and so on in which the progress of bone resorption is considered to be deeply associated with the symptom, and to the symptoms of progressing bone resorption (development into osteoporosis) along with inflammatory joint diseases such as rheumatoid arthritis.
Reaction of Phosphorus Pentasulfide with Organolithiums. An In Situ Reagent for the Preparation of Thiolactams
Goel, O. P.,Krolls, U.
, p. 162 - 164 (2007/10/02)
Phosphorus pentasulfide reacts under mild conditions with four equivalents of n-butyllithium, methyllithium or phenyllithium giving solutions in tetrahydrofuran.The new reagents in situ convert lactams to thiolactams and show significant selectivity in the type of reactive lactams.
