86544-77-6Relevant academic research and scientific papers
SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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Page/Page column 51, (2010/04/23)
The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
7-AZAINDOLE DERIVATIVES AND THEIR USE IN THE INHIBITION OF C-JUN N-TERMINAL KINASE
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Page/Page column 229, (2008/12/08)
The present invention provides a compound of formula (I); or a pharmaceutically acceptable salt thereof, the use of a compound of formula (I) or a pharmaceutically acceptable salt thereof in the inhibition of c-Jun N-terminal kinase (JNK) activity and the use in medicine and particularly in the treatment of neurodegenerative disorders, inflammatory diseases and/or and autoimmune diseases. The invention also provides processes for the manufacture of said compounds of formula (I) or a pharmaceutically acceptable salt thereof and compositions containing them
CRYSTAL AND SALT OF 1-CYCLOPROPYLMETHYL-4-Y2-(3,3,5,5)-TETRAMETHYLCYCLOHEXYL)PHENYL¨PIPERAZINE
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, (2008/06/13)
Salts and crystals of 1-cyclopropylmethyl-4-[2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine have excellent cell adhesion inhibitory action and cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflam
CRYSTAL AND SALT OF 1-CYCLOPROPYLMETHYL-4-[2-(3,3,5,5)-TETRAMETHYLCYCLOHEXYL)PHENYL]PIPERAZINE
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Page/Page column 15-16, (2008/06/13)
A crystal and salt of 1-cyclopropylmethyl-4-[2-(3,3,5,5)-tetramethylcyclohexyl)phenyl]piperazine have excellent cellular adhesion inhibiting potency and cellular infiltration inhibiting potency. Therefore, these crystal and salt are useful as a preventive
INTERMEDIATE IN PRODUCTION OF [2-(3,3,5,5-TETRAMETHYLCYCLOHEXYL)PHENYL]PIPERAZINE COMPOUND
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Page/Page column 36-37, (2008/06/13)
A compound represented by the general formula below or a salt thereof is a useful intermediate in the production of a [2-(3,3,5,5-tetramethylcyclohexyl)phenyl]piperazine compound that has excellent cell adhesion inhibitory effect and cell invasion inhibitory effect and therefore is useful as a therapeutic or prophylactic agent for various inflammatory diseases and autoimmune diseases induced by the adhesion and invasion of leukocytes, such as inflammatory bowel diseases (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome, rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. [Chemical formulae] wherein R1 and R2 independently represent a hydrogen atom or an amino-protecting group for an amino group, or R1 and R2 may together form a pyrrole ring which may have a substituent.
1,2-Di(cyclic)substituted benzene compounds
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Page/Page column 61, (2008/06/13)
In one aspect, the present invention provides compounds having formula (1) or (100), a salt thereof or a hydrate of the foregoing, which compounds exhibit excellent cell adhesion inhibitory action or cell infiltration inhibitory action, and are useful as therapeutic or prophylactic agents for various inflammatory diseases and autoimmune diseases associated with adhesion and infiltration of leukocytes, such as inflammatory bowel disease (particularly ulcerative colitis or Crohn's disease), irritable bowel syndrome; rheumatoid arthritis, psoriasis, multiple sclerosis, asthma and atopic dermatitis. wherein R10 represents optionally substituted cycloalkyl, etc., R20-23 represent hydrogen, alkyl, alkoxy, etc., R30-32 represent hydrogen, alkyl, oxo, etc., and R40 represents optionally substituted alkyl, etc.
The Conversion of Vinyl Triflates into γ'-Hydroxy-α,β-enones
Arcadi, Antonio,Cacchi, Sandro,Marinelli, Fabio
, p. 4955 - 4964 (2007/10/02)
Vinyl triflates have been converted into γ'-hydroxy-α,β-enones through their palladium-catalysed coupling with 1-butyn-4-ols followed by the reaction of the obtained 1-hydroxy-3-yn-5-enes in an acidic CH2Cl2/3N HCl two-phase system in the presence of n-Bu
A METHOD FOR THE REGIOSPECIFIC SYNTHESIS OF ENOL TRIFLATES BY ENOLATE TRAPPING
Mc Murray, John E.,Scott, William J.
, p. 979 - 982 (2007/10/02)
Enol triflates can be prepared in high yield from regiospecifically generated enolates by trapping with N-phenyltrifluoromethanesulfonimide.
