- COMPOUNDS
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Compounds of formula (IA) and formula (IB), which are useful as inhibitors of indoleamine 2,3-dioxygenase and/or tryptophan dioxygenase, are provided. Also provided are pharmaceutical compositions, kits comprising said compounds, and methods and uses pert
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Page/Page column 124-125
(2018/08/20)
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- PHARMACEUTICAL COMPOUND
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Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the general formula (I) detailed within.
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Page/Page column 117; 118; 124; 126
(2017/01/26)
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- NOVEL SUBSTITUTED IMIDAZOPYRIDINE COMPOUNDS AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND/OR TRYPTOPHAN-2,3-DIOXYGENASE
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Disclosed herein are substituted imidazopyridine compounds of formula (I) which are inhibitors of indoleamine 2,3-dioxygenase (IDO) and/or tryptophan-2,3-dioxygenase (TDO) enzymes: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO- and/or TDO-associated disease or disorder.
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Page/Page column 37
(2017/12/15)
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- Design, optimization, and in vivo evaluation of a series of pyridine derivatives with dual NK1 antagonism and SERT inhibition for the treatment of depression
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A series of substituted pyridines, ether linked to a phenylpiperidine core were optimized for dual NK1/SERT affinity. Optimization based on NK1/SERT binding affinities, and minimization of off-target ion channel activity lead to the
- Gillman, Kevin W.,Parker, Michael F.,Silva, Mark,Degnan, Andrew P.,Tora, George O.,Lodge, Nicholas J.,Li, Yu-Wen,Lelas, Snjezana,Taber, Matthew,Krause, Rudolf G.,Bertekap, Robert L.,Newton, Amy E.,Pieschl, Rick L.,Lengyel, Kelly D.,Johnson, Kim A.,Taylor, Sarah J.,Bronson, Joanne J.,MacOr, John E.
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p. 407 - 411
(2013/02/23)
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- SUBSTITUTED HETEROCYCLIC ETHERS AND THEIR USE IN CNS DISORDERS
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The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
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Page/Page column 28
(2009/09/05)
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- SUBSTITUTED HETEROCYCLIC ETHERS AND THEIR USE IN CNS DISORDERS
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The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.
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Page/Page column 26
(2008/06/13)
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- AMINOCYCLOPENTYL PYRIDOPYRAZINONE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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Compounds of Formula I and Formula II (wherein A, E, j, k, m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R24, R25, R26, R27, R28, R29, R30, R31, R32, R33, R34, X, Y and Z are as defined herein) which are modulators of chemokine receptor activity and are useful in the prevention or treatment of certain inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis. 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 chemokine receptors are involved.
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Page/Page column 24
(2010/11/27)
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