- AZETIDINE AND SPIROAZETIDINE COMPOUNDS AND USES THEREOF
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The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
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- The discovery of CCR3/H1 dual antagonists with reduced hERG risk
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A series of dual CCR3/H1 antagonists based on a bispiperidine scaffold were discovered. Introduction of an acidic group overcame hERG liability. Bioavailability was optimised by modulation of physico-chemical properties and physical form to del
- Barton, Patrick,Brough, Steven,Evans, Richard,Luckhurst, Christopher A.,Mochel, Tobias,Perry, Matthew W. D.,Rigby, Aaron,Sanganee, Hitesh,Sisson, Adam,Springthorpe, Brian,Bahl, Ash,Bowers, Keith,Riley, Robert J.
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p. 6688 - 6693,6
(2012/12/12)
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- MMP INHIBITORS AND METHODS OF USE THEREOF
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Provided are MMP inhibitors having the Formula (I): wherein R1, R2 and Y are as defined herein, which are useful in the treatment and/or prevention of MMP-mediated diseases and disorders.
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Page/Page column 22
(2009/01/20)
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- NOVEL PIPERIDINES AS CHEMOKINE MODULATORS (CCR)
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Compounds of Formula (I) are modulators of chemokine (for example CCR3) activity (for use in, for example, treating asthma).
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Page/Page column 23
(2008/06/13)
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- Chemical compounds
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The invention provides compounds of formula (I): as modulators of chemokine and H1 receptor activity. The compounds are especially useful in the treatment of asthma and rhinitis.
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- Arylpiperazines and their use as metalloproteinase inhibiting agents (MMP)
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Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
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Page/Page column 43
(2010/02/06)
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- Compounds
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The invention provides compounds of general formula (I) wherein: R1represents optionally substituted, C1-C12alkyl or optionally substituted 3- to 10-membered saturated or unsaturated ring system comprising up to two ring carbon atoms that form carbonyl groups and comprising up to 4 ring heteroatoms independently selected from nitrogen, oxygen and sulfur; m is 0-1; Q represents OCH2, C1-C4alkylene or C2-C4alkenylene; T represents C(O)NH, or when m is 0, T may additionally represent a bond or NH, or when m is 1 and Q represents C1-C4alkylene, T may additionally represent NH; n is 1-4; each R2and R3independently represents H or C1-C4alkyl; V represents N, and W represents N or CH; X represents O, C(O), CH(OH), SO2, NH or N(C1-C6alkyl), provided that when W represents N, then X represents either C(O) or SO2and when W represents CH, then X is other than SO2; R4represents optionally substituted phenyl; R5and R6each independently represent H, C1-C6alkyl or hydroxyC1-C6alkyl, or R5and R6together with the nitrogen atom to which they are attached form a 4- to 7-membered saturated heterocyclic ring; R7and R8each independently represent H or C1-C6alkyl; and R9represents OH or —NR7R8; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.
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- Chemical compounds
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The invention concerns compounds of formula (I), and their use in therapy, particularly in the modulation of CCR3 activity.
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- Chemical compounds
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The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.
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