- Nitroxide derivative of ROCK kinase inhibitor
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The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
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- Impact of Stereo- And Regiochemistry on Energetic Materials
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The synthesis, physical properties, and calculated performances of six stereo- and regioisomeric cyclobutane nitric ester materials are described. While the calculated performances of these isomers, as expected, were similar, their physical properties were found to be extremely different. By alteration of the stereo- and regiochemistry, complete tunability in the form of low- or high-melting solids, stand-alone melt-castable explosives, melt-castable explosive eutectic compounds, and liquid propellant materials was obtained. This demonstrates that theoretical calculations should not be the main factor in driving the design of new materials and that stereo- and regiochemistry matter in the design of compounds of potential relevance to energetic formulators.
- Barton, Lisa M.,Edwards, Jacob T.,Johnson, Eric C.,Bukowski, Eric J.,Sausa, Rosario C.,Byrd, Edward F. C.,Orlicki, Joshua A.,Sabatini, Jesse J.,Baran, Phil S.
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supporting information
p. 12531 - 12535
(2019/08/26)
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- Efficient synthesis of 6-amino-2-thiaspiro[3,3]heptane hydrochloride
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A novel compound 6-amino-2-thiaspiro[3,3]heptane hydrochloride was synthesized in nine steps using 2,2-bis(bromomethyl)-1,3-propanediol as starting material, with an overall yield of 31%.
- Lu, Yan,Wang, Jin,Guo, Jianyu,Tang, Yihong,Zhang, Suxia,Tao, Jianwei,Xiong, Lei,Li, Xiujie,Luo, Jingyi
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- 1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE ML RECEPTOR AND THEIR USE IN MEDICINE
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Compounds of formula I or a salt thereof are provided wherein R4, R5, R6, Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
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- SYNTHESIS OF NEW CARBOCYCLIC ANALOGUES OF OXETANOCIN A AND OXETANOCIN G
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The synthesis of cis-3-amino-1-cyclobutanemethanol has been performed in six steps (59.6percent yield) from cis-1,3-cyclobutanedicarboxylic anhydride.This allowed us to obtain two new carbocyclic analogues of oxetanocin A and oxetanocin G related to 7-deazaadenosine and 7-deazaguanosine.
- Pecquet, Pascal,Huet, Francois,Legraverend, Michel,Bisagni, Emile
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p. 739 - 745
(2007/10/02)
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