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Heterocyclic beta-Enamino Esters, 42. Reaction of Heterocyclic beta-Enamino Nitriles with O-Methyllactim Ethers. Dimroth Rearrangement to Novel Heterocondensed Pyrimidophanes

Depending on the ring size of the O-methyllactim ethers employed (4a – f) the heterocyclic beta-enamino nitriles 1 – 3 afford either the linear heterocondensed pyrimidines 5a – d, 6a – f or via Dimroth rearrangement the pyrimidophanes 8 – 13.

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Pyrroline – Wikipedia,
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Synthesis and Reactivity of Polyamines: Part 3 – 2,5-Bis-omega-aminoalkylpyrazines and Piperazines

The nitroenamines (1) and (3) on catalytic reduction under acid conditions give rise to the pyrazines (2) and (4) respectively.The pyrazines (2) can be further hydrogenated to the piperazines (10) which show structural similarity to the naturally occuring polyamine, spermine (11).

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Structure-activity relationship studies and biological characterization of human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase inhibitors

The structure-activity relationship (SAR) study of two chemotypes identified as inhibitors of the human NAD+-dependent 15-hydroxyprostaglandin dehydrogenase (HPGD, 15-PGDH) was conducted. Top compounds from both series displayed potent inhibition (IC50 <50 nM), demonstrate excellent selectivity towards HPGD and potently induce PGE 2 production in A549 lung cancer and LNCaP prostate cancer cells. I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 5264-35-7, help many people in the next few years.Application In Synthesis of 5-Methoxy-3,4-dihydro-2H-pyrrole

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COMPOUNDS FOR THE PREVENTION AND TREATMENT OF MEDICAL DISORDERS AND USES THEREOF

Aspects of the invention relate to compounds, pharmaceutical compositions, methods for the manufacturing of compounds and methods for treatment of various disorders mediated at least in part by one or more galectins.

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Synthesis of [1,2-A]-fused tricyclic dihydroquinolines by palladiumcatalyzed intramolecular C-N cross-coupling of polarized heterocyclic enamines

A simple methodology for [1,2-A]-fused tricyclic dihydroquinolines is established. The key ste of the methodology is an intramolecular Buchwald-Hartwig amination reaction of suitabl halogenated (both bromo and chloro) cyclic enaminoketones, enaminoesters and enaminonitrile with various ring size (from five-to seven-membered). Optimal reaction conditions (palladiu source, base, ligand) depend on the ring size of the starting enamine, giving 65-98% yield of th tricyclic product. A treatment of the products with perchloric acid gives respective quinoliniu perchlorates.

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Nonaromatic amidine derivatives as acylation catalysts

(Chemical Equation Presented) Catalytic activity of nonaromatic bicyclic amidines and bicyclic isothioureas in acylation reactions was found to be remarkably dependent on the sizes of both rings. DBN and especially its thia-analogue (THTP) have been identified as highly active acylation catalysts.

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WDR5-MLL1 INHIBITORS AND MODULATORS

Benzamides and picolinamides that are meta-substituted with imino-, guanidino-, or heterocycle-containing groups disrupt the WDR5-MLL1 protein-protein interaction, and have use in pharmaceutical compositions and in treating proliferative disorders and conditions in a subject, such as cancer.

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2-(Iminoethylidene)-pyrrolidines and tautomeric 2-(aminoethenyl)-1-pyrrolines

The present invention provides new imino compounds having the formula I STR1 wherein R1 represents an aliphatic or cycloaliphatic hydrocarbon radical, unsubstituted or substituted phenyl, or phenyl-lower alkyl or diphenyl-lower alkyl, which radicals are unsubstituted or substituted in the phenyl ring(s), R2 represents unsubstituted or substituted phenyl, unsubstituted or substituted monocyclic heteroaryl or lower alkyl, R3 represents hydrogen, lower alkyl, a carbonyl group linked with R2 to form a five-membered ring, or the group R6 –CO wherein R6 represents lower alkyl or unsubstituted or substituted phenyl, R4 represents, if present, hydrogen or lower alkyl which is independent or is linked with R1 to form a five- to seven-membered ring which can contain as ring members two aromatic ring carbon atoms of an unsubstituted or substituted phenyl or phenyl-lower-alkyl radical R1, and as a six- or seven-membered ring also epoxy or lower alkylimino which is separated by two, or at least two, carbon atoms from the nitrogen atom given in the formula I, R5 represents, if present, hydrogen or lower alkyl, A represents a straight- or branched-chain lower alkylene having 2 to (5-n1 -n2) chain members, Z represents epoxy, epithio, imino or lower alkylimino, and M1 and m2 represent 0 or 1 and together always represent 1, N1 represents 1 or, if Z represents imino or lower alkylimino and n2 represents 1, can also represent 0, N2 represents 0 or 1, And wherein two additional bonds, either corresponding to the dashed lines or corresponding to the dotted lines, are present, with m1 representing 0 in the former case and m2 representing 0 in the latter case, and the acid addition salts, in particular the pharmaceutically acceptable acid addition salts thereof. These new substances possess valuable pharmacological properties, particularly hypoglycaemic activity.

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Pyrroline – Wikipedia,
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MEK INHIBITOR SALTS AND SOLVATES THEREOF

The present invention relates to sodium salt forms of 7-(4-Bromo-2-fluoro- phenylamino)-6-methyl-5-oxo-1,3,5- tetrahydro-indolizine-8-carboxylic acid (2- hydroxyethoxy)-amide and 7-(4-Bromo-2-fluoro-phenylamino)-5-oxo- 1,2,3,5-tetrahydro- indolizine-8-carboxylic acid cyclopropylmethoxy-amide and their corresponding solvates and polymorphs, which are useful in the treatment of a disease, disorder or syndrome associated with MEK inhibition, such as cancer, in mammals

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Pyrroline – Wikipedia,
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Synthesis and mild retro Diels-Alder decomposition of 1,4-methanopyrrolo-, 1,4-methanopyrido- and 1,4-methanoazepino<2,1-b>quinazolinones

From norbornane- and norbornene-fused azetidinones 1a and 1b, 1,4-methanopyrrolo-, 1,4-methanopyrido- and 1,4-methanoazepino<2,1-b>quinazolinones 6a,b-9a,b were prepared by ring enlargement.Norbornene derivatives 6b-9b underwent retrodiene decomposition to give pyrrolo-, pyrido- and azepino<1,2-a>pyrimidinones 10-13, respectively.

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Pyrroline – Wikipedia,
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