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The condensation reactions of the tetrachloro mono (1 and 2) and bisferrocenylspirocyclotriphosphazenes (3-5) with 1,4-dioxa-8-azaspiro[4,5] decane (DASD) resulted in the formation of the partly and fully DASD-substituted phosphazenes. The reactions of equal amounts of 1-5 and DASD produced the mono-DASD-substituted ferrocenylphosphazenes (1a-5a), as the major product. When the reactions were carried out with 1 equiv of 1-5 and 2 equiv of DASD, corresponding geminal-phosphazenes (1b-5b) were isolated. Moreover, the reactions of 1 equiv of 1-5 and 3 equiv of DASD gave the tri- (1c-4c) and tetra-substituted (1d-5d) phosphazenes. When the excess DASD was used, the fully-substituted phosphazenes (1d-5d) were obtained. The chirality of 3a was evaluated using chiral HPLC column. The structures of all the phosphazenes were verified by FTIR, MS, 1H, 13C and 31P NMR, and HSQC spectral data. The crystal structures of 4a, 2b, 5b, and 1d were determined by X-ray diffraction techniques. The 10 phosphazene derivatives were screened for antimicrobial activity. Meanwhile, interactions between the compounds and pBR322 plasmid DNA were presented by agarose gel electrophoresis. The compounds 2b, 1d, 2d, and 4d were tested against HeLa cancer cell lines. Among these compounds, 4d had cytotoxic effect on HeLa cell after 24 h treatment.

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In this study, we systematically investigated 39 secondary amines as additives in concentrated EB/NMP solutions for gelation and degradation. We discovered that when both the width (defined as the longest distance between two hydrogens in the plane perpendicular to the NH bond of the amine) and depth (defined as the longest distance between two atoms in a plane perpendicular to the width) of the amines are <4.53 A and their pKa is >7.7, the amines significantly extend the gelation times of 20 mass % EB/NMP solutions for more than 12 h. However, some of these amines also significantly degrade the polymer. Amines with small width and depth and strong basicity, such as azetidine and pyrrolidine, can significantly destroy the EB structures. This was evidenced by order-of-magnitude decreases in doped film conductivity, by significantly changed UV-vis spectra, and by significantly reduced molecular weights of the aged EB solutions as measured by gel permeation chromatography (GPC). However, when both the width and depth of amines are >4.53 A, these amines neither prolong gelation time nor appreciably degrade EB.

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The present invention relates to compounds of the formula I wherein A1, A2, R1, R2, R3, X and n are as defined in the claims, which are valuable pharmaceutically active compounds for the therapy and prophylaxis of diseases, for example of cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body?s production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of diseases which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical preparations which comprise compounds of the formula I

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Facile synthetic approaches to a few novel classes of amidophosphates, omega- aminophosphonates, and bisphosphonates having a 3,5-bis(arylidene) piperid-4-one backbone have been elaborated starting from piperid-4-ones functionalized with phosphorus motives followed by aldol-crotonic condensation with a range of (hetero)aromatic aldehydes or via introduction of the corresponding phosphorus function into the preformed NH-3,5- bis(arylidene)piperid-4-ones. Combination of phosphorus-containing moieties possessing inherent bioactivity and cytotoxic 3,5-bis(arylidene)piperid-4-one moiety resulted in the compounds with high antitumor activity towards human carcinoma cell lines Caov3, A549, Scov3, PC3, KB 3-1, and KB 8-5 (IC 50 in the range of 1-80 muM). Copyright Taylor & Francis Group, LLC.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 177-11-7, molcular formula is C7H13NO2, introducing its new discovery. Safety of 1,4-Dioxa-8-azaspiro[4.5]decane

The present invention relates to use of small organic compounds interacting with the Voltage-Dependent Anion Channel (VDAC) for the treatment of diseases associated with central nervous system (CNS) disorders, including psychotic disorders, mood disorders, neurodegenerative diseases. In particular the present invention relates to the use of substituted piperazine- and piperidine-derivatives and pharmaceutical compositions comprising same for the treatment of psychotic disorders including schizophrenia, mood disorders, and neurodegenerative diseases.

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The invention encompasses a series of pyrimidinone compounds which inhibit HIV integrase and thereby prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses intermediates useful for making the pyrimidone compounds. Additionally, pharmaceutical compositions and methods for treating those infected with HIV are encompassed.

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The elongation condensing enzymes in the bacterial fatty acid biosynthesis pathway represent desirable targets for the design of novel, broad-spectrum antimicrobial agents. A series of substituted benzoxazolinones was identified in this study as a novel class of elongation condensing enzyme (FabB and FabF) inhibitors using a two-step virtual screening approach. Structure activity relationships were developed around the benzoxazolinone scaffold showing that N-substituted benzoxazolinones were most active. The benzoxazolinone scaffold has high chemical tractability making this chemotype suitable for further development of bacterial fatty acid synthesis inhibitors.

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Curative interferon and ribavirin sparing treatments for hepatitis C virus (HCV)-infected patients require a combination of mechanistically orthogonal direct acting antivirals. A shared component of these treatments is usually an HCV NS5A inhibitor. First generation FDA approved treatments, including the component NS5A inhibitors, do not exhibit equivalent efficacy against HCV virus genotypes 1-6. In particular, these first generation NS5A inhibitors tend to select for viral drug resistance. Ombitasvir is a first generation HCV NS5A inhibitor included as a key component of Viekira Pak for the treatment of patients with HCV genotype 1 infection. Since the launch of next generation HCV treatments, functional cure for genotype 1-6 HCV infections has been achieved, as well as shortened treatment duration across a wider spectrum of genotypes. In this paper, we show how we have modified the anchor, linker, and end-cap architecture of our NS5A inhibitor design template to discover a next generation NS5A inhibitor pibrentasvir (ABT-530), which exhibits potent inhibition of the replication of wild-type genotype 1-6 HCV replicons, as well as improved activity against replicon variants demonstrating resistance against first generation NS5A inhibitors.

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The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer’s disease. Precursors for the preparation of the compounds according to the present invention are also provided.

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A convenient protocol for the parallel solution-phase synthesis of a library of thiocarbamates, ureas, carbamates, and amides from carbamoylimidazolium salts has been developed. The crystalline carbamoylimidazolium salts are readily synthesized from secondary amines, CDI and iodomethane, and act as stable carbamoylation reagents. A common set of reaction conditions and a straightforward non-chromatographic liquid-liquid extraction purification protocol were developed for reactions with thiols, amines, phenols, and carboxylic acids, giving the products with high purities and yields. The resultant library incorporates diversity arising from the choice of reaction partners and the functional group linkage generated in the couplings.

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Piperidine – Wikipedia,
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