52194-65-7Relevant academic research and scientific papers
NAPHTHYRIDINES AS INHIBITORS OF HPK1
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Paragraph 0914; 0915, (2018/10/21)
Naphthyridine compounds and their use as inhibitors of HPK1 are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibiting HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the naphthyridine compounds.
Synthesis of 2,3-dihydro-1H-pyrrolo[1,2-a]benzimidazoles via the cyclopropyliminium rearrangement of substituted 2-cyclopropylbenzimidazoles
Salikov, Rinat F.,Platonov, Dmitry N.,Frumkin, Aleksandr E.,Lipilin, Dmitry L.,Tomilov, Yury V.
, p. 3495 - 3505 (2013/04/23)
2-Cyclopropylbenzimidazole derivatives with various substituents in the small ring undergo cyclopropyliminium rearrangement into 2,3- dihydropyrrolobenzimidazoles substituted at positions 1, 2 or 3. The substrates containing a functional group in position 1 of the cyclopropane ring form products substituted at position 3. Substituents at position 2 in most cases lead to the formation of a mixture of isomers. The reaction can be directed to yield one of the isomers predominantly by varying the solvent polarity.
CANNABINOID-2-RECEPTOR AGONISTS
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Paragraph 00328, (2013/04/10)
The present invention relates to cannabinnoid-2-receptor (CB2R) agonist compounds. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them and to their use as therapeutic agents for the treatment and/or prevention of diseases or conditions in which CB2R stimulation is beneficial (especially inflammatory conditions).
2-ALKYLBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS
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Page/Page column 10, (2008/12/08)
Compounds of formulae I and II: are disclosed as 5-HT3 inhibitors. Those compounds are useful in treating CINV, IBS-D and other diseases and conditions.
SUBSTITUTED CARBOXAMIDES
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Page/Page column 14-15, (2008/12/08)
This application relates to a substituted carboxamide compound of formula I, or a pharmaceutically acceptable salt thereof, as defined herein, a pharmaceutical composition thereof, and its use in treating pain.
Analogs of isovaleramide, a pharmaceutical composition including the same, and a method of treating central nervous system conditions or diseases
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Page/Page column 8, (2010/02/15)
An isovaleramide analog having at least one of an increased potency, an increased half-life, and an increased stability compared to isovaleramide. The isovaleramide analog is a cyclic analog or a noncyclic analog. The isovaleramide analog is formulated into a pharmaceutical composition. A method of treating a central nervous system condition or disease is also disclosed. The method comprises administering an isovaleramide analog to a patient suffering from the central nervous system condition or disease.
Synthesis of chiral β-methyl tryptamine-derived GnRH antagonists
Simeone, Joseph P.,Bugianesi, Robert L.,Ponpipom, Mitree M.,Goulet, Mark T.,Levorse, Mark S.,Desai, Ranjit C.
, p. 6459 - 6461 (2007/10/03)
The stereospecific formation of 2-aryl-β-methyl tryptamine derivatives 15 and 16 from chiral 4-chloro-1-(3,5-dimethylphenyl)-3-methylbutanones is described. These intermediates were further manipulated into the GnRH antagonists 1b and 1c in five steps.
Synthesis and spectral properties of cyclopropyl-substituted phosphaalkenes
Kostitsyn, A. B.,Ruzek, H.,Heydt, H.,Regitz, M.,Nefedov, O. M.
, p. 635 - 640 (2007/10/02)
Cyclopropanecarboxylic acid chlorides 5a-d react with tris(trimethylsilyl)phosphane 6 in benzene at -2 deg C to form cyclopropylcarbonyl-bis(trimethylsilyl)phosphanes 7.These products undergo silylic rearrangement at 25 deg C to yield phosphoalkenes 8.Compounds 8a,b,d are formed as mixtures of Z- and E-isomers where the latter predominante.In the case of 8c, the Z-isomer is formed exclusively. - Key words: phosphaalkenes, cyclopropyl-substituted, E/Z-isomerism.
Generation and Reactions of Lithiated tert-Butyl and 2,6-Di(tert-butyl)-4-methylphenyl Cyclopropanecarboxylates
Haener, Robert,Maetzke, Thomas,Seebach, Dieter
, p. 1655 - 1665 (2007/10/02)
tert-Butyl and 2,6-di(tert-butyl)-4-methylphenyl (BHT) cyclopropanecarboxylates (4, 6, 24, 25) are lithiated with LiN(i-Pr)2 and t-BuLi, respectively.Reactions with alkyl halides, aldehydes, acyl chlorides, and heteroelectrophiles give α-substituted BHT esters which can be cleaved (t-BuOK/H2O/THF) to the corresponding carboxylic acids or reduced (LiAlH4/THF) to the cyclopropanemethanols.
