- BENZOCYCLOBUTANE DERIVATIVES USEFUL AS DUAL SGLT1/SGLT2 MODULATORS
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The present invention is directed to benzocyclobutane derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity. More particularly, the compounds of the present invention are useful in the treatment of for example, Type II diabetes mellitus, Syndrome X, and complications and symptoms associated with said disorders.
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Page/Page column 106-109
(2018/05/27)
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- The mechanism of the ortho-methylation of nitrobenzenes by dimethylsulfonium methylide
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Nitrobenzenes carrying an ortho substituent are selectively methylated at the free ortho position by reaction with dimethylsulfonium methylide. The importance of the ortho substituent is demonstrated by the failure of the methylation of nitrobenzene and 3- and 4-nitroanisole. This is explained by the out-of-plane geometry of the nitro group in the ortho-substituted derivative, which enables a specific interaction between the ylide and the nitro group favourable for attack of the methylide C atom at the neighbouring free ortho position. As shown by appropriate deuterium-labelling studies, the addition is followed by an E1-like β-elimination with displacement of dimethyl sulfide and subsequent protonation of the elimination product. The nucleophilic ortho-methylation of 2-nitroanisole by dimethylsulfonium methylide is explained by a reaction sequence including intermediates A to D. Copyright
- Haiss, Peter,Zeller, Klaus-Peter
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experimental part
p. 295 - 301
(2011/02/28)
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- Antioxidative activities of oxindole-3-acetic acid derivatives from supersweet corn powder
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The components contributing to the antioxidative activity of supersweet corn powder (SSCP), which is commonly used in corn soup and snacks in Japan, were clarified and the effects investigated. 7-(0-/3-Glucosy-loxy)oxindole-3- acetic acid (GOA) was found
- Midoh, Naoki,Tanaka, Akihito,Nagayasu, Makiko,Furuta, Chie,Suzuki, Katsuya,Ichikawa, Takeshi,Isomura, Takashi,Nomura, Kenzo
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experimental part
p. 1794 - 1801
(2011/06/17)
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- Cytokine inhibitors
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Disclosed are compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclos
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Page/Page column 18
(2008/06/13)
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- Cytokine inhibitors
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Disclosed are compounds of formula (I) Where Ar1, X, Y, Q, W, R3, R4, R5, R6 and Ry are defined herein. The compounds of the invention inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. The compounds are also useful for treating diseases or conditions related to oncology and anticoagulant or fibrinolytic therapy. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
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Page/Page column 53; 54
(2010/02/08)
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- An efficient and practical synthesis of N,N-diethyl-7-indolyloxyacetamide via 7-hydroxyindole
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An efficient and practical synthesis of N, N-diethyl-7-indolyloxyacetamide (1) from 3-hydroxy-2-nitrotoluene (4) via 7-hydroxyindole (2) is described. Treatment of 3-benzyloxy-2-nitrotoluene (5) obtained from 4 with DMF dimethyl acetal and pyrrolidine afforded the (E)-2-nitro-β-pyrrolidinostyrene 6, which can be readily converted into the 2-nitrophenylacetaldehyde semicarbazone 7 without isolation of 6. Hydrogenation of 7 over Pd/C, followed by reaction of the resulting 2 with 2-chloro-N, N-diethylacetamide produced 1 in good yield.
- Harada, Hiroshi,Fujii, Akihito,Kato, Shiro
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p. 507 - 514
(2007/10/03)
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- Chemical compounds
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Compounds of the general structural formula (I) and use of the compounds and salts and solvates thereof, as therapeutic agents.
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- 5-HT4 receptor agonists
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Compounds of formula (I) and pharmaceutically acceptable salts thereof are selective agonists for 5-HT4 receptors. STR1 wherein Ak is a C3 -C6 alkyl group, and R is a C2 -C6 alkyl group, a C3 -C6 alkenyl group, a C3 -C6 alkynyl group, a C3 -C7 cycloalkyl group or a C3 -C6 cycloalkylmethyl group.
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- Substituted 1,3,4,9-tetrahydropyrano[3,4,-b]indole-1-acetic acids, pharmaceutical compositions containing them, and methods for treating inflammatory conditions and for analgesic purposes using them
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Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole-1-acetic acid nucleus bearing a substituent in position 1,5, 6, 7 and 8. The derivatives are useful anti-inflammatory and analgesic agents and methods for their preparation
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- Indole derivatives pharmaceutical preparations based thereon, and β-receptor stimulation therewith
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Indole derivatives of Formula I STR1 wherein R1 is hydrogen, alkyl of 1-6 carbon atoms, or benzyl R2 is hydrogen, alkyl of up to 4 carbon atoms, free or esterified hydroxyalkyl of up to 4 carbon atoms, or free, amidated or esterified
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