- Cation-Cation Pairing by Ni-Ci-H?O Hydrogen Bonds
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The pairing of ions of opposite charge is a fundamental principle in chemistry, and is widely applied in synthesis and catalysis. In contrast, cation-cation association remains an elusive concept, lacking in supporting experimental evidence. While studying the structure and properties of 4-oxopiperidinium salts [OC5H8NH2]X for a series of anions X- of decreasing basicity, we observed a gradual self-association of the cations, concluding in the formation of an isolated dicationic pair. In 4-oxopiperidinium bis(trifluoromethylsulfonyl)amide, the cations are linked by N-H?O=C hydrogen bonds to form chains, flanked by hydrogen bonds to the anions. In the tetra(perfluoro-tert-butoxy)aluminate salt, the anions are fully separated from the cations, and the cations associate pairwise by N-C-H?O=C hydrogen bonds. The compounds represent the first genuine examples of self-association of simple organic cations based merely on hydrogen bonding as evidenced by X-ray structure analysis, and provide a paradigm for an extension of this class of compounds.
- Gamrad, Waltraud,Dreier, Angelika,Goddard, Richard,P?rschke, Klaus-Richard
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- QUINOLINE AND QUINAZOLINE COMPOUNDS AND METHODS OF USE THEREOF
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Compounds and methods for their preparation and use as therapeutic or prophylactic agents, fo example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase- 1 (ENPP1).
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Paragraph 00633-00634
(2020/10/09)
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- Synthesis and antibacterial evaluation of novel oxazolidinone derivatives containing a piperidinyl moiety
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In this article, a series of novel oxazolidinone derivatives containing a piperidinyl moiety was designed and synthesized. Their antibacterial activities were measured against S. aureus, MRSA, MSSA, LREF and VRE by MIC assay. Most of them exhibited potent activity against Gram-positive pathogens comparable to linezolid. Among them, compound 9h exhibited comparable activity with linezolid against human MAO-A for safety evaluation and showed moderate metabolism in human liver microsome. The most promising compound 9h, which showed remarkable antibacterial activity against S. aureus, MRSA, MSSA, LREF and VRE pathogens with MIC value of 0.25–1 μg/mL, was an interesting candidate for further investigation.
- Hou, Yunlei,Dong, Yuhong,Ye, Tianyu,Jiang, Jia,Ding, Liang,Qin, Mingze,Ding, Xiudong,Zhao, Yanfang
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- LSD1 Inhibitors
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The present invention relates to compounds that inhibit LSD1 activity. In particular, the present invention relates to compounds, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions of the present invention.
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Paragraph 0435; 0436
(2017/07/14)
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- PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
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Page/Page column 37
(2014/01/17)
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- Lightening Agents and/or Dyes that Contain Aldehyde(s)
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Agents for dyeing and/or lightening keratin fibers, in particular human hair, containing, relative to the weight thereof, 0.001 to 15 wt. % of at least one aldehyde of the formula (I): wherein X represents —CH(R2)—SO2—Y—R1, —CR3R4R5, or wherein Y represents —CH(CHO)— or —CH2— or a chemical bond, and wherein each of R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 independently represents —H or —CN or —F or —Cl or —Br or —I or —CHO or —NH2 or —NO2 or —CF3 or —CCl3 or —CF2CF3 or —CCl2CCl3 or an optionally substituted (C1-C6) alkyl group or a hydroxyalkyl group or a polyhydroxyalkyl group or an optionally substituted (C1-C6) alkylene group, and wherein the agent contains no oxidation dye precursors of developer and coupler type.
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment of obesity and/or diabetes.
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Page/Page column 39-40
(2009/07/17)
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- THERAPEUTIC COMPOUNDS
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The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAKl, JAK2, JAK3 and/or TYK2) and/or PDKl and are thus useful for the treatment of myeloproliferative disorders or cancer.
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Page/Page column 53
(2009/05/30)
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- SUBSTITUTED SULFONAMIDE DERIVATIVES
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The invention relates to substituted sulfonamide derivatives, processes for the preparation thereof, medicaments containing these compounds and the use of substituted sulfonamide derivatives for the preparation of medicaments.
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Page/Page column 123
(2009/11/29)
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- A new strategy for synthesis of polymeric supports with triazene linkers
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A new strategy based on the use of diethylamine triazenes for stabilization and generation of polymer supported diazonium ions was described. New economical syntheses of four new polymeric supports with 3- and 6-carbon atom spacers and triazene linkers derived from meta- and para-aminophenol were described and compared to the traditional methods. The possible application of the polymer bound triazene masked diazonium salts as supports for immobilization of secondary amines (nortropine and 4-piperidinole and their esterification and oxidation), and as amine scavengers was shown. The new supports with meta-C3-T2 and para-C3-T2 linkers showed higher loadings and typically gave products with good yields and purities.
- Lazny, Ryszard,Nodzewska, Aneta,Klosowski, Piotr
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p. 121 - 130
(2007/10/03)
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- Synthesis of heteroarylpiperazines and heteroarylbipiperidines with a restricted side chain and their affinities for 5-HT1A receptor
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Heteroarylpiperazine and heteroarylbipiperidine derivatives, bearing a 4-piperidine ring instead of an alkylamino side chain to give the semi-rigidity, were prepared and evaluated for their abilities to displace [3H] 8-OH-DPAT binding to the rat hippocampal synaptic membranes. These compounds showed low to moderate affinities for 5-HT1A receptor, with Ki values ranging from 6912 nM to 232 nM. Of these compounds, 8 b and 15 e exhibited the best affinities for 5-HT1A receptor with Ki values of 232 nM and 338 nM, respectively.
- Yoo, Kyung Ho,Choi, Hyun Sik,Kim, Dong Chan,Shin, Kye Jung,Kim, Dong Jin,Song, Yun Seon,Jin, Changbae
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p. 208 - 215
(2007/10/03)
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