- SPIROCYCLOPROPYLAMINE DERIVATIVES USEFUL AS INHIBITORS OF HISTONE DEMETHYLASES KDM1A
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The present invention relates to provided spirocyclopropylamine compounds, endowed with a potent KDM1A (LSD1) inhibitory activity, wherein X, R, and R1 are as defined in the specification, pharmaceutical compositions containing such compounds a
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Page/Page column 27
(2017/07/14)
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- Diels-Alder reaction of fused pyran-2-ones with ethyl vinyl ether
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Ethyl vinyl ether was found to be an appropriate synthetic equivalent of acetylene for a set of Diels-Alder reactions with fused pyran-2-ones that yield fused carbocyclic systems. Transformations were conducted under microwave irradiation with DABCO (as a catalyst for the elimination of ethanol) and with n-butanol as the additive. A single-crystal X-ray diffraction structure is presented for N-(5,6,7,8-tetrahydro-6-methyl-8-oxonaphthalen-2-yl)benzamide. Springer-Verlag 2012.
- Juranovic, Amadej,Kranjc, Kristof,Polanc, Slovenko,Perdih, Franc,Kocevar, Marijan
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experimental part
p. 771 - 777
(2012/08/27)
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- Pyrazinyl-substituted naphthalene derivatives
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Compounds of the formula where R1 is of the formulae R2 is —R4, —O—R4, —O—S (O)2—R4, —NR4R5, R4—(CH2)b—NH(C═X)—(CH2)—, R4—(CH2)b—O(C═O)NH—(CH2)c—(C═O)NH—, R4(C═O)NH—(C═O)NH—, —(CH2)b—NH(C═X)—(CH2)c—R4, R4—(CH2)b—O(C═)—(CH2)c—, —(CH2)b—O(C═O)—(CH2)c—R4, —NH(C═X)NH—R4, R4—O(C═O)O—, —O(C═)NH—R4, R4—O(C═O)NH—, —(CH2)b—(C═0)—(CH2)c—R4, —NH—S(O)2—R4, —C(OH)R4R5, —CH(OH)—R4, —(C═O)—NR4R5, —CN, —NO2, substituted C1 to C6 alkyl, substituted or unsubstituted C1 to C6 alkenyl, or substituted or unsubstituted C1 to C6 alkynyl, said substituted moieties substituted with a moiety of the formulae —R4, —R4R5, —O—R4, or —S(O)d—R4. These compounds are useful psychotherapeutics and are potent serotonin (5-HT1) agonists and antagonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain and chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotranmission. The compounds can also be used as centrally acting antihypertensives and vasodilators.
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