3936-54-7Relevant academic research and scientific papers
EIF4E INHIBITORS AND USES THEREOF
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Paragraph 00337; 00364, (2021/09/11)
The present invention provides compounds inhibiting elF4E activity and compositions and methods of using thereof.
Lipase-catalyzed aza-michael reaction on acrylate derivatives
Steunenberg, Peter,Sijm, Maarten,Zuilhof, Han,Sanders, Johan P. M.,Scott, Elinor L.,Franssen, Maurice C. R.
, p. 3802 - 3813 (2013/06/05)
A methodology has been developed for an efficient and selective lipase-catalyzed aza-Michael reaction of various amines (primary and secondary) with a series of acrylates and alkylacrylates. Reaction parameters were tuned, and under the optimal conditions it was found that Pseudomonas stutzeri lipase and Chromobacterium viscosum lipase showed the highest selectivity for the aza-Michael addition to substituted alkyl acrylates. For the first time also, some CLEAs were examined that showed a comparable or higher selectivity and yield than the free enzymes and other formulations.
Promiscuous behavior of Rhizomucor miehei lipase in the synthesis of N-substituted β-amino esters
Monsalve, Leandro N.,Gillanders, Florencia,Baldessari, Alicia
experimental part, p. 1164 - 1170 (2012/04/10)
A mild and efficient procedure for the aza-Michael addition of amines to acrylates by using lipases as catalysts is reported. Various lipases, mono- and bifunctional amines, alkyl acrylates, and reaction parameters were studied. Under the optimal conditio
Synthesis of a polyunsaturated amino ketone isolated from a Guangxi sponge of the genus Haliclona
Vik, Anders,Hansen, Trond Vidar
supporting information; experimental part, p. 1060 - 1061 (2011/03/22)
The first synthesis of (all-Z)-1-[(2-phenylethyl)amino]-octadeca-6,9,12,15- tetraen-3-one has been achieved in nine steps and in 13% overall yield using eicosapentaenoic acid as the starting material.
Aurora kinase A inhibitors: Identification, SAR exploration and molecular modeling of 6,7-dihydro-4H-pyrazolo-[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione scaffold
Coumar, Mohane Selvaraj,Wu, Jian-Sung,Leou, Jiun-Shyang,Tan, Uan-Kang,Chang, Chung-Yu,Chang, Teng-Yuan,Lin, Wen-Hsing,Hsu, John T.-A.,Chao, Yu-Sheng,Wu, Su-Ying,Hsieh, Hsing-Pang
, p. 1623 - 1627 (2008/12/21)
Tricyclic 6,7-dihydro-4H-pyrazolo[1,5-a]pyrrolo[3,4-d]pyrimidine-5,8-dione was identified as a novel scaffold for Aurora kinase A inhibition through virtual screening. SAR exploration coupled with molecular modeling of 8a reveals the minimum pharmacophore requirements for Aurora kinase A inhibition.
Samarium(III) triflate catalyzed conjugate addition of amines to electron-deficient alkenes
Yadav,Ramesh Reddy,Gopal Rao,Narsaiah,Subba Reddy
, p. 3447 - 3450 (2008/09/19)
Amines undergo smooth nucleophilic addition to α,β-unsaturated compounds in the presence of a catalytic amount of samarium(III) triflate at ambient temperature to produce the corresponding β-amino compounds in excellent yields. This method is simple, convenient, and works efficiently under mild conditions. Georg Thieme Verlag Stuttgart.
Cadmium chloride (CdCl2): An efficient catalyst for conjugate addition of amines to electron-poor alkenes
Vijender, Medamoni,Kishore,Satyanarayana
, p. 591 - 594 (2007/10/03)
Electron-deficient olefins undergo rapid Aza-Michael reaction with a wide range of amines catalyzed by cadmium chloride at room temperature. Copyright Taylor & Francis Group, LLC.
4-Aminopiperidine derivatives
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Page/Page column 15, (2010/11/08)
The present invention relates to compounds of the formula (I) wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP-IV, such as diabetes, non-insulin dependent diabetes mellitus and/or impaired glucose tolerance, obesity, and/or metabolic syndrome or β-cell protection.
14C-Labeling of the New Antiasthmatic Flezelastine
Engel, J.,Bork, A.,Fleischhauer, I.,Kutscher, B.,Lieflaender, M.
, p. 207 - 210 (2007/10/02)
Flezelastine is a new phthalazinone derivative with antiasthmatic/antiallergic activity.For pharmacokinetic studies 14C-labeled flezelastine was synthesized starting with -phthalic anhydride.In a convergent synthesis 1.5 g of double 14C-labeled f
Cholecystokinin Peptidomimetics as Selective CCK-B Antagonists: Design, Synthesis, and in Vitro and in Vivo Biochemical Properties
Blommaert, Armand G.S.,Weng Jian-Hui,Dorville, Agnes,McCort, Isabelle,Ducos, Bertrand,et al.
, p. 2868 - 2877 (2007/10/02)
Antagonists of cholecystokinin-B (CCK-B) receptors have been shown to alleviate CCK4-induced panic attacks in humans and to potentiate opioid effects in animals.The clinical use of these compounds is critically dependent on their ability to cross the blood-brain barrier.In order to improve this property, new, peptoid-derived CCK-B antagonists, endowed with high affinity, selectivity, and increased lipophilicity have been developed.The affinity and selectivity of these compounds have been cheracterized in vitro and in vivo using guinea pig, rat, and mouse.Most of these compounds proved to be selective for the CCK-B receptor, the most potent analog, N--D-α-methyltryptophanyl>-N-i value of 6.1 nM for guinea pig cortex membranes in vitro and a good selectivity ratio (Ki CCK-A/Ki CCK-B = 174).Furthermore, the in vivo affinity of 26A for mouse brain CCK-B receptors, following intracerebroventricular injection at different concentrations, was found to be 10 nmol.Using competition experiments with the specific CCK-B ligand pBC 264, compound 26A was shown to cross the blood-brain barrier (0.2percent) after intraperitoneal administration in mice.This compound is therefore an interesting pharmacological tool to further elucidate the physicopathological role of endogenous CCK.
