- Seven-membered ring compound and application thereof in prevention and treatment of diabetes and metabolic syndrome
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The invention discloses a seven-membered ring compound and application thereof in prevention and treatment of diabetes and metabolic syndrome. The structure of the seven-membered ring compound is as shown in a general formula I, and definitions of substituent groups are as shown in the specification and claims. The seven-membered ring compound of the invention has an extremely excellent effect ofpreventing or treating diabetes and metabolic syndrome.
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Paragraph 0188-0192
(2020/06/09)
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- Synthesis of Novel Diaziridinyl Quinone Isoxazole Hybrids and Evaluation of Their Anti-Cancer Activity as Potential Tubulin-Targeting Agents
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Two series of diaziridinyl quinone isoxazole derivatives were prepared and evaluated for their cytotoxic activity against MCF7, HeLa, BT549, A549 and HEK293 cell lines and interaction with tubulin. Compounds (6a-m) showed promising activity against all the 5 human cancer cell lines. Compounds 6a, 6e and 6 m were potent [IC 50 ranging between 2.21 μg to 2.87 μg] on ER-positive MCF7 cell line similar to the commercially available drug molecule Doxorubicin. The results from docking models are in consistent with the experimental values which demonstrated the favourable binding modes of compounds 6a-m to the interface of α- and β-tubulin dimer.
- Kumar, P. Ravi,Yennam, Satyanarayana,Raghavulu,Velatooru, Loka Reddy,Kotla, Siva Reddy,Penugurti, Vasudevarao,Hota, Prasanta K.,Behera, Manoranjan,Jaya Shree
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p. 406 - 414
(2019/07/10)
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- LIPIDS AND LIPID COMPOSITIONS FOR THE DELIVERY OF ACTIVE AGENTS
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This invention provides for a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein RA, RB, R2 and R4 are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
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Page/Page column 81
(2016/03/19)
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- Synthesis of novel isoxazole-benzoquinone hybrids via 1,3-dipolar cycloaddition reaction as key step
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An efficient method for the preparation of novel 2-(5-arylisoxazol-3-yl) cyclohexa-2,5-diene-1,4-dione hybrids via 1,3-dipolar cycloaddition followed by an oxidation reaction using ceric ammonium nitrate (CAN) has been described. Using this method, various aryl as well as alkyl substituted isoxazole-benzoquinone hybrids were synthesized in high yields.
- Ravi Kumar,Behera, Manoranjan,Raghavulu,Jaya Shree,Yennam, Satyanarayana
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scheme or table
p. 4108 - 4113
(2012/08/28)
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- Total synthesis of natural enantiomers of heliespirones A and C via the diastereoselective intramolecular Hosomi-Sakurai reaction
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A full account of the development of a novel type of the intramolecular Hosomi-Sakurai reactions of the substrates with a pbenzoquinone and an allylsilane moieties connected by an ether linkage is described. This transformation proceeds via an addition-elimination sequence and provides the products with two stereogenic centers through a 1,3(or 1,4)-asymmetric induction in good to excellent diastereoselectivities. A reasonable mechanistic possibility for the reaction, determination of the stereochemistry for the product, and scope and limitation of the transformation are also discussed. The methodology developed here can successfully be applied to the enantiocontrolled total synthesis of the natural enantiomers of (-)-heliespirone A and (+)-heliespirone C, which have been isolated from sunflower Helianthus annuus L. as allelochemicals.
- Miyawaki, Akari,Kikuchi, Daisuke,Niki, Masu,Manabe, Yuki,Kanematsu, Makoto,Yokoe, Hiromasa,Yoshida, Masahiro,Shishido, Kozo
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p. 8231 - 8243
(2013/01/15)
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- Total synthesis of the fungal metabolite (±)-acremine G: Acceleration of a biomimetic Diels-Alder reaction on silica gel
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A total synthesis of the bioactive tetracyclic natural product acremine G has been achieved in which a regio- and stereoselective biomimetic Diels-Alder reaction between two readily assembled building blocks, accelerated on a solid support (silica gel), forms the key step.
- Mehta, Goverdhan,Khan, Tabrez Babu,Sunil Kumar
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scheme or table
p. 5116 - 5119
(2010/11/16)
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- BENZOFURAN AND BENZOTHIOPHENE-2-CARBOXYLIC ACID AMIDE DERIVATIVES
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The present invention relates to compounds of formula I wherein X, A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
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Page/Page column 22
(2009/02/11)
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- Novel triazole derivatives, process for their preparation and pharmaceutical compositions containing them
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The invention relates to a compound of formula in which R1, X1, X2, X3, X4, R4, Y1, Y2 and Y3 are as defined in claim 1. These compounds are CCK-receptor agonists.
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- Triazole derivatives and pharmaceutical compositions comprising them
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The present invention relates to compounds of formula (I) and their pharmaccutically acceptable salts, solvates, hydrates and polymorphs. These compounds are powerful and selective CCK1 receptor agonists.
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Page/Page column 6
(2010/02/05)
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- Synthesis of quinones from hydroquinone dimethyl ethers. Oxidative demethylation with cobalt(III) fluoride
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The oxidative demethylation of 1,4-dimethoxynaphthalene and 1,4- dimethoxybenzene derivatives with cobalt(III) fluoride proceeded in good to excellent yield to afford the corresponding naphthoquinone and benzoquinone derivatives.
- Tomatsu, Ayumi,Takemura, Syunji,Hashimoto, Kimiko,Nakata, Masaya
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p. 1474 - 1476
(2007/10/03)
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- 2,5-Dialkoxy Substituted Oligo- and Poly(1,4-phenyleneethenylene)s
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O-Alkylation and regioselective Rieche formylation of 2-methylhydroquinone (1) yields the 2,5-dialkoxy-4-methylbenzaldehydes 4a-j.The corresponding azomethines 5a-j enter in a strongly alkaline medium a selfcondensation reaction leading to the title compounds 6/7a-j.These conjugated oligomers and polymers possess highly regular structures with exclusively (E)-configurated double bonds.GPC, IR, 1H-, 13C-NMR and MS-FD measurements were used for their characterization.Somewhat different results were obtained for the similarly prepared Schiff base 5l which contains chlorine substituents in the side chains.Cleavage of hydrogen chloride leads not only to unsaturated alkoxy groups; additionally, cyclization reactions (5l8l) are observed.
- Kretzschmann, H.,Meier, H.
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p. 247 - 254
(2007/10/02)
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- Synthesis of 4,7-Dimethoxyindoles Bearing Substituents at the C-5 and C-6 Positions and Studies on their Demethylation Products
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Syntheses of some 4,7-dimethoxyindoles bearing methyl, amino or acetamido groups at the C-5 and C-6 positions were investigated.The presence of these substituents made possible the isolation of the corresponding 4,7-dihydroxyindole derivatives obtained by long reflux with aluminium chloride in benzene solution.
- Malesani, Giorgio,Galiano, Fabio,Ferlin, Maria Grazia,Masiero, Sergio
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p. 563 - 569
(2007/10/02)
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- Treatment of senile geriatric patients to restore performance
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Compounds of the formula STR1 wherein R1, R2 and R3 are alike or different and each is (lower)alkyl, including the racemic mixtures and the dextrorotatory and levorotatory isomers, and the pharmaceutically acceptable nontoxic salt thereof have been found to restore the performance of mammals, including man, and upon use in clinical studies in human geriatric patients have had a profound effect upon their mental alertness and attitudes without producing the undesirable stimulant side effects associated with the use of amphetamines.
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