- NOVEL THYROMIMETICS
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Compounds are provided having the structure of Formula (I): or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope, or salt thereof, wherein A, X1, X2, Q, R1, R2 and n are as defined herein. Such compounds function as thyromimetics and have utility for treating diseases such as neurodegenerative disorders and fibrotic diseases. Pharmaceutical compositions containing such compounds are also provided, as are methods of their use and preparation.
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Page/Page column 143-144
(2020/09/19)
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- Metal-Free C-O Bond Functionalization: Catalytic Intramolecular and Intermolecular Benzylation of Arenes
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A catalytic, metal-free intramolecular rearrangement of benzyl phenyl ethers using nitrosonium salt as a catalyst is described. The optimized reaction conditions enabled a catalytic and metal-free Friedel-Crafts alkylation reaction with benzylic alcohols, producing water as the stoichiometric byproduct. A comprehensive scope (>50 examples) for both approaches and application in drug synthesis were demonstrated. Mechanistic studies suggest a Lewis acid-based mechanism for the metal-free Friedel-Crafts reaction.
- Bering, Luis,Jeyakumar, Kirujan,Antonchick, Andrey P.
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supporting information
p. 3911 - 3914
(2018/07/22)
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- 5a-Carba-β-d-glucopyranose derivatives as novel sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes
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5a-Carba-β-d-glucopyranose derivatives were synthesized and identified as novel SGLT2-selective inhibitors. These inhibitors exhibited potent SGLT2 inhibition with high selectivity over SGLT1. Among the tested compounds, 6f indicated the most potent hSGLT2 inhibition and the highest selectivity over hSGLT1. Moreover, the pharmacokinetics data also showed that 6h, which had the same aglycon structure as sergliflozin-active (3-active), had a threefold longer half-life time (T1/2) than sergliflozin (3) with a high distribution volume in db/db mice. Subsequently, 6h lowered blood glucose levels as much as 3 and showed longer hypoglycemic action than 3 in db/db mice.
- Ohtake, Yoshihito,Sato, Tsutomu,Matsuoka, Hiroharu,Nishimoto, Masahiro,Taka, Naoki,Takano, Koji,Yamamoto, Keisuke,Ohmori, Masayuki,Higuchi, Takashi,Murakata, Masatoshi,Kobayashi, Takamitsu,Morikawa, Kazumi,Shimma, Nobuo,Suzuki, Masayuki,Hagita, Hitoshi,Ozawa, Kazuharu,Yamaguchi, Koji,Kato, Motohiro,Ikeda, Sachiya
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experimental part
p. 5334 - 5341
(2011/10/19)
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- NOVEL CYCLOHEXANE DERIVATIVE, PRODRUG THEREOF AND SALT THEREOF, AND THERAPEUTIC AGENT CONTAINING THE SAME FOR DIABETES
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A cyclohexane derivative having the function of reducing a blood sugar level and having preferable properties required of medicines, such as long-lasting drug activity, metabolic stability, and safety; and a medicinal composition for use in the prevention or treatment of diseases attributable to hyperglycemia, such as diabetes, e.g., insulin dependent diabetes mellitus (type 1 diabetes) or noninsulin-dependent diabetes mellitus (type 2 diabetes), complications of diabetes, and obesity. The derivative is a compound represented by the formula (I): (wherein A is -O-, -CH2-, or -NH-; n is an integer selected between 0 and 1; R6 and R7 each independently is hydrogen or C1-6 alkyl; m is an integer selected among 1-3; Q is selected among the following formulae Q1 to Q5; Ar1 is optionally substituted arylene or optionally substituted heteroarylene, provided that the heteroarylene may be bonded to an aromatic carbocycle or aromatic heterocycle to form a fused ring; and Ar2 is optionally substituted aryl or optionally substituted heteroaryl), a prodrug of the compound, or a pharmaceutically acceptable salt of either. Also provided are a medicine, a medicinal composition, or the like each containing the compound.
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Page/Page column 47-48
(2008/06/13)
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- METHOD FOR PRODUCING 2-BENZYLPHENOL COMPOUND
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[Task] Provide a process for producing a 2-benzylphenol compound easily, efficiently and selectively. [Means for Achievement] A process for producing a 2-benzylphenol compound represented by the following general formula (2) (in the formula, R1, R2, R3 and R4 may be the same or different and are each independently hydrogen atom, alkyl group or the like; and R5, R6, R7, R8 and R9 may be the same or different and are each independently hydrogen atom, alkyl group or the like), characterized by reacting, in the presence of a dehydrogenating agent, a benzylidenecyclohexanone compound represented by the following general formula (1) (in the formula, R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the same definitions as given above). [Effect] A 2-benzylphenol compound substantially free from isomers can be produced from a benzylidenecyclohexanone compound (an easily obtainable raw material) selectively, efficiently and in a simple operation, under mild conditions without using any special reactor.
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- METHOD FOR PRODUCING 2-BENZYLPHENOL COMPOUND
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Disclosed is a simple method for efficiently and selectively producing a 2-benzylphenol compound. Specifically disclosed is a method for producing a 2-benzylphenol compound represented by the following general formula (2): (wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 represent the same as defined in the general formula (1) below) which is characterized by reacting a benzylidenecyclohexane compound represented by the following general formula (1): (wherein R1, R2, R3 and R4 may be the same or different and respectively represent a hydrogen atom, an alkyl group or the like; and R5, R6, R7, R8 and R9 may be the same or different and respectively represent a hydrogen atom, an alkyl group or the like) in the presence of a dehydrogenation agent. Consequently, a 2-benzylphenol compound substantially containing no isomers can be produced selectively and efficiently under mild conditions by a simple procedure using an easily-available benzylidenecyclohexane compound as the raw material without requiring a special reaction equipment.
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Page/Page column 33
(2008/06/13)
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- ARYL 5-THIO-D-GLUCOPYRANOSIDE DERIVATIVES AND REMEDIES FOR DIABETES CONTAINING THE SAME
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There is provided a 5-thio-β-D-glucopyranoside compound of the following formula, which has an inhibitory effect on SGLT2 activity, or a pharmaceutically acceptable salt thereof or a hydrate thereof. There is also provided a pharmaceutical preparation, pa
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Page/Page column 20
(2010/02/11)
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