- Integration of lead optimization with crystallography for a membrane-bound ion channel target: Discovery of a new class of AMPA receptor positive allosteric modulators
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A novel series of AMPAR positive modulators is described that were identified by high throughput screening. The molecules of the series have been optimized from a high quality starting point hit to afford excellent developability, tolerability, and effica
- Ward, Simon E.,Harries, Mark,Aldegheri, Laura,Austin, Nigel E.,Ballantine, Stuart,Ballini, Elisa,Bradley, Daniel M.,Bax, Benjamin D.,Clarke, Brian P.,Harris, Andrew J.,Harrison, Stephen A.,Melarange, Rosemary A.,Mookherjee, Claudette,Mosley, Julie,Dal Negro, Gianni,Oliosi, Beatrice,Smith, Kathrine J.,Thewlis, Kevin M.,Woollard, Patrick M.,Yusaf, Shahnaz P.
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experimental part
p. 78 - 94
(2011/03/19)
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- COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE
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Compounds of formula (I), and salts and solvates thereof are provided: Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
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Page/Page column 17
(2010/06/16)
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- DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS ACTIVE AGENT
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Disclosed herein are novel compounds of Formula (1) as defined in the specification having excellent inhibitory activity against dipeptidyl peptidase-IV (DPP-IV), methods of preparing the same and pharmaceutical compositions comprising the same as an active agent.
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Page/Page column 38
(2009/07/25)
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- COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE
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Compound of formula (I) and salts thereof are provided: wherein A, R1, R, R2 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
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Page/Page column 41-42
(2008/12/07)
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- COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEROF IN MEDICINE
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Compound of formula (I) and salts thereof are provided: wherein X, Y, Z, R1, R2 and R3 are as defined in the specification. Processes for preparation, pharmaceutical compositions, and uses thereof as a medicament, for example in the treatment of a disease or condition mediated by a reduction or imbalance in glutamate receptor function, such as schizophrenia or cognition impairment, are also disclosed.
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Page/Page column 39-40
(2009/01/24)
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- DIPEPTIDYL PEPTIDASE-IV INHIBITING COMPOUNDS, METHODS OF PREPARING THE SAME, AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME AS AN ACTIVE AGENT
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The present invention relates to novel compounds exhibiting good inhibitory activity versus Dipeptidyl Peptidase-IV(DPP-IV), methods of preparing the same and pharmaceutical compositions containing the same as an active agent.
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Page/Page column 18; 61
(2010/11/24)
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- PIPERIDINO PYRIMIDINE DIPEPTIDYL PEPTIDASE INHIBITORS FOR THE TREATMENT OF DIABETES
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The present invention is directed to compounds which are inhibitors of the dipeptidyl peptidase-IV enzyme ("DP-IV inhibitors") and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.
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