111769-27-8Relevant articles and documents
PYRAZOLO[3,4-B]PYRIDINE COMPOUNDS, AND THEIR USE AS PHOSPHODIESTERASE INHIBITORS
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Page 94, (2008/06/13)
The invention relates to a compound of formula (I) or a salt thereof: wherein:R1 is C1-4alkyl, C1-3fluoroalkyl, -CH2CH2OH or -CH2CH2CO2C1-2alkyl;R2 is a hydrogen atom (H), methyl or C1fluoroalkyl;R3 is optionally substituted C3-8cycloalkyl or optionally substituted mono-unsaturated-C5-7cycloalkenyl or an optionally substituted heterocyclic group of sub-formula (aa), (bb) or (cc); in which n1 and n2 independently are 1 or 2; and in which Y is O, S, SO2, or NR10; or R3 is a bicyclic group (dd) or (ee): ; and wherein X is NR4R5 or OR5a. The compounds are phosphodiesterase (PDE) inhibitors, in particular PDE4 inhibitors. Also provided is the use of a compound of formula (I), or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the treatment and/or prophylaxis of an inflammatory and/or allergic disease in a mammal such as a human, for example chronic obstructive pulmonary disease (COPD), asthma, or allergic rhinitis.
Preparation of Optically Active Cyclic Ether Derivatives of Amino Acids and Peptides
Barlos, Kleomenis,Papaioannou, Dionysios,Patrianakou, Stella,Sanida, Chariklia,Tsegenidis, Theodoros
, p. 474 - 475 (2007/10/02)
Treatment of N-tritylmethioninol (1) or peptides (6), incorporating methionyl and amino alcohol residues, with MeI, followed by base mediated cyclisation of the thus derived sulphonium salts, provides the title compounds in excellent yields.