900175-01-1Relevant academic research and scientific papers
CYCLOHEXYL GPR40 AGONISTS FOR THE TREATMENT OF TYPE II DIABETES
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Page/Page column 185, (2018/05/24)
Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR40 receptor. Such compounds are represented by Formula (I) as follows: (Formula (I)) wherein R1, R2, R3, A, W, L, Ra, and G are defined herein: and by Formula (II) as follows: (Formula (II)) wherein R1B, WB, LB, and GB are defined herein.
Heterogenized Wilkinson-type catalyst for transfer hydrogenation of carbonyl compounds
Bogar, Krisztian,Krumlinde, Patrik,Bacsik, Zoltan,Hedin, Niklas,Baeckvall, Jan-E.
scheme or table, p. 4409 - 4414 (2011/10/01)
Wilkinson's catalyst [RhCl(PPh3)3] was heterogenized on common silica by the use of a grafting/anchoring technique. The immobilized catalyst showed high activity and selectivity in transfer hydrogenation reactions of a range of carbonyl compounds in 2-propanol. Reactions carried out in 2-propanol at reflux afforded the corresponding alcohols in high yields in short reaction times. The heterogeneous feature of the catalyst allows for easy recovery and efficient reuse in the same reaction up to 5 times without any detectible loss of catalytic activity. Wilkinson's catalyst [RhCl(PPh 3)3] has been immobilized on silica through a monodentate phosphane ligand and used in the transfer hydrogenation of alkyl and aryl carbonyl compounds. The use of 2-propanol as both hydrogen donor and solvent allows for high yields of the corresponding alcohols under mild reaction conditions. The recyclability of this heterogenized Rh catalyst is also demonstrated.
Phenylglycinamide and pyridylglycinamide derivatives useful as anticoagulants
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Page/Page column 80, (2010/11/25)
The present invention provides novel phenylglycinamide derivatives of Formula (I) or (IV): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables W, W1, Y, Z, R7, R8, R9, and R11 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
High-yielding metalloenzymatic dynamic kinetic resolution of fluorinated aryl alcohols
Bogár, Krisztián,B?ckvall, Jan-E.
, p. 5471 - 5474 (2008/02/10)
Dynamic kinetic resolution (DKR) of various fluorinated aryl alcohols by a combination of lipase-catalyzed enzymatic resolution with in situ ruthenium-catalyzed alcohol racemization is described. (R)-Selective Candida antarctica lipase B (CALB) was employed for transesterification of different fluoroaryl alcohols in DKR reactions delivering the corresponding acetates in high yield (≥97%) with excellent enantiomeric excess (≥98%).
PHENYLGLYCINAMIDE DERIVATIVES USEFUL AS ANTICOAGULANTS
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Page/Page column 155, (2008/06/13)
The present invention relates generally to phenylglycinamide derivatives that inhibit serine proteases. In particular it is directed to novel phenylglycinamide derivatives, and analogues thereof, which are useful as selective inhibitors of serine protease enzymes of the coagulation cascade; for example thrombin, factor VIIa, factor Xa, factor XIa, factor IXa, and/or plasma kallikrein. In particular, it relates to compounds that are factor VIIa inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds and methods of using the same.
Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Page/Page column 27, (2008/06/13)
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Page 32, (2008/06/13)
Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
