- SYNTHESIS OF 20-NOR-SALVINORIN A
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The invention provides 20-nor-salvinorin A, an analog of the kappa-opioid agonist salvinorin A. The 20-nor-salvinorin A is an active kappa-opioid modulator and can be used for treatment of medical conditions wherein modulation of the kappa-opioid receptor
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Page/Page column 19; 21; 22
(2019/01/07)
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- Amidoalkylindoles as Potent and Selective Cannabinoid Type 2 Receptor Agonists with in Vivo Efficacy in a Mouse Model of Multiple Sclerosis
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Selective CB2 agonists represent an attractive therapeutic strategy for the treatment of a variety of diseases without psychiatric side effects mediated by the CB1 receptor. We carried out a rational optimization of a black market designer drug SDB-001 that led to the identification of potent and selective CB2 agonists. A 7-methoxy or 7-methylthio substitution at the 3-amidoalkylindoles resulted in potent CB2 antagonists (27 or 28, IC50 = 16-28 nM). Replacement of the amidoalkyls from 3-position to the 2-position of the indole ring dramatically increased the agonist selectivity on the CB2 over CB1 receptor. Particularly, compound 57 displayed a potent agonist activity on the CB2 receptor (EC50 = 114-142 nM) without observable agonist or antagonist activity on the CB1 receptor. Furthermore, 57 significantly alleviated the clinical symptoms and protected the murine central nervous system from immune damage in an experimental autoimmune encephalomyelitis (EAE) mouse model of multiple sclerosis.
- Shi, Ying,Duan, Yan-Hui,Ji, Yue-Yang,Wang, Zhi-Long,Wu, Yan-Ran,Gunosewoyo, Hendra,Xie, Xiao-Yu,Chen, Jian-Zhong,Yang, Fan,Li, Jing,Tang, Jie,Xie, Xin,Yu, Li-Fang
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p. 7067 - 7083
(2017/09/07)
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- INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof; compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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Paragraph 0092; 0095-0096
(2013/10/22)
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- INDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Indoles having inhibitory activity on RSV replication and having the formula I the prodrugs, N-oxides, addition salts, quaternary amines, metal complexes and stereochemically isomeric forms thereof, compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 18
(2012/06/30)
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- AZAINDOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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Azaindoles having inhibitory activity on RSV replication and having the formula (I) compositions containing these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 21
(2012/06/30)
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- AZABENZIMIDAZOLES AS RESPIRATORY SYNCYTIAL VIRUS ANTIVIRAL AGENTS
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A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary metal complex, or a stereochemically isomeric form thereof; (formula I) compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.
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Page/Page column 21
(2012/06/30)
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- (Chloro-phenylthio-methylene)dimethylammonium chloride (CPMA) an efficient reagent for selective chlorination and bromination of primary alcohols
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(Chloro-phenylthio-methylene)dimethylammonium chloride reacts smoothly with a variety of alcohols, to afford the corresponding alkyl chloride in good yields. In the presence of tetrabuthylammonium bromide the corresponding bromide is obtained. Selective halogenation of primary hydroxyl groups in the presence of an unprotected secondary one is described. The mild reaction conditions involved are compatible with the major alcohol protecting groups as well as with acid sensitive functions like epoxides. (C) 2000 Elsevier Science Ltd.
- Gomez,Gellibert,Wagner,Mioskowski
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p. 6049 - 6052
(2007/10/03)
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- Enzymatic synthesis of L-6-hydroxynorleucine
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L-6-Hydroxynorleucine, a key chiral intermediate used for synthesis of a vasopeptidase inhibitor, was prepared in 89% yield and >99% optical purity by reductive amination of 2-keto-6-hydroxyhexanoic acid using glutamate dehydrogenase from beef liver. In an alternate process, racemic 6- hydroxynorleucine produced by hydrolysis of 5-(4-hydroxybutyl)hydantoin was treated with D-amino acid oxidase to prepare a mixture containing 2-keto-6- hydroxyhexanoic acid and L-6-hydroxynorleucine followed by the reductive amination procedure to convert the mixture entirely to L-6-hydroxynorleucine, with yields of 91 to 97% and optical purities of >99%.
- Hanson, Ronald L.,Schwinden, Mark D.,Banerjee, Amit,Brzozowski, David B.,Chen, Bang-Chi,Patel, Bharat P.,McNamee, Clyde G.,Kodersha, Gus A.,Kronenthal, David R.,Patel, Ramesh N.,Szarka, Laszlo J.
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p. 2247 - 2252
(2007/10/03)
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- 29Si NMR spectra of tert-butyldimethylsilylated alcohols
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29Si NMR spectra of a series of tert-butyldimethylsilyl derivatives of simple alcohols were measured under standard conditions in chloroform-d. The chemical shifts are linearly related to those in analogous trimethylsilyl derivatives. The corre
- Schraml, Jan,Kvi?c?alova?, Magdalena,Blechta, Vratislav,C?erma?k, Jan
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p. 659 - 662
(2007/10/03)
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- Vitamin D analogues
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STR1 The present invention relates to compounds of formula (I), in which formula R stands for an alkyl group containing from 7 to 12 carbon atoms optionally substituted with a hydroxy group; and derivatives of the compounds of formula (I) in which one or more hydroxy groups have been transformed into --O-acyl or --O-glycosyl or phosphate ester groups, such masked groups being hydrolyzable in vivo, in pure form or in mixtures. The present compounds find use in both the human and veterinary practice in the treatment and prophylaxis of autoimmune diseases, including diabetes mellitus, hypertension, inflammatory diseases such as rheumatoid arthritis and asthma as well as diseases characterized by abnormal cell differentiation and/or cell proliferation, and/or imbalance in the immune system.
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- The Diene-Transmissive -Cycloaddition Strategy: Stereoselective Synthesis of Advanced Intermediates to Quassinoids
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Complex intermediates to quassinoids, some optically active and containing many functional groups, were synthesized via a diene-transmissive Diels-Alder strategy.The stereochemistry of the key inter- and intramolecular cycloadditions was controlled by ste
- Spino, Claude,Liu, Gang,Tu, Noah,Girard, Suzanne
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p. 5596 - 5608
(2007/10/02)
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