- INHIBITORS OF TRANSCRIPTIONAL ENHANCED ASSOCIATE DOMAIN (TEAD) AND USES THEREOF
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Provided herein are compounds of Formula (I''), Formula (I'), Formula (I), Formula (II'), and Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and
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Paragraph 00297
(2021/12/28)
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- HETEROCYCLIC COMPOUNDS AS BET INHIBITORS
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Novel bromodomain and extraterminal domain (BET) inhibitors and to therapeutic methods of treating conditions and diseases using these novel BET inhibitors are provided.
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Paragraph 0290; 0294
(2020/05/29)
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- Pyridine N-oxidation derivative as well as preparation method and application thereof
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The invention relates to a pyridine N-oxidation derivative as well as a preparation method and an application thereof, in particular to a compound shown in a general formula (I), a preparation methodof the compound, pharmaceutical composition containing the compound and an application of the compound as a BRD4 inhibitor in treating related diseases such as cancer, inflammation, chronic liver diseases, diabetes, cardiovascular diseases, AIDS and the like, wherein in the general formula (I), all substituent groups are the same as definitions in the description.
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Paragraph 0611; 0618-0620
(2019/08/06)
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- Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABAAα2/α3 binding site agonists for the treatment of anxiety disorders
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A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA Aα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
- Goodacre, Simon C.,Street, Leslie J.,Hallett, David J.,Crawforth, James M.,Kelly, Sarah,Owens, Andrew P.,Blackaby, Wesley P.,Lewis, Richard T.,Stanley, Joanna,Smith, Alison J.,Ferris, Pushpinder,Sohal, Bindi,Cook, Susan M.,Pike, Andrew,Brown, Nicola,Wafford, Keith A.,Marshall, George,Castro, José L.,Atack, John R.
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- Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones as α2/α3 subtype selective GABAA agonists for the treatment of anxiety
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Imidazo[1,2-a]pyrazin-8-ones, imidazo[1,2-d][1,2,4]triazin-8-ones and imidazo[2,1-f][1,2,4]triazin-8-ones are high affinity GABAA agonists. Compound 16d has good oral bioavailability in rat, functional selectivity for the GABAAα2 and
- Goodacre, Simon C.,Hallett, David J.,Carling, Robert W.,Castro, Jose L.,Reynolds, David S.,Pike, Andrew,Wafford, Keith A.,Newman, Robert,Atack, John R.,Street, Leslie J.
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p. 1582 - 1585
(2007/10/03)
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- The expedient synthesis of 4,2′-difluoro-5′-(7- trifluoromethylimidazo[1,2-a]pyrimidin-3-yl)biphenyl-2-carbonitrile, a GABA α2/3 agonist
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An expedient regioselective synthesis of a GABA α2/3 agonist 1 is described. The key step is an efficient regioselective palladium-catalyzed coupling of 7-trifluoromethylimidazo[1,2-a]pyrimidine (5) to 5′-chloro-4,2′-difluorobiphenyl-2-carbonitrile (15).
- Cameron, Mark,Foster, Bruce S.,Lynch, Joseph E.,Shi, Yao-Jun,Dolling, Ulf-H.
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p. 398 - 402
(2012/12/22)
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- Imidazo[1,2-b][1,2,4]triazines as α2/α3 subtype selective GABAA agonists for the treatment of anxiety
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Imidazo[1,2-a]pyrimidines and imidazo[1,2-b][1,2,4]triazines are ligands for the benzodiazepine binding site of GABAA receptors that are functionally selective for the α2/α3 subtypes over the α1 subtype. SAR studies to optimise this functional
- Jennings, Andrew S.R.,Lewis, Richard T.,Russell, Michael G.N.,Hallett, David J.,Street, Leslie J.,Castro, Jose L.,Atack, John R.,Cook, Susan M.,Lincoln, Rachael,Stanley, Joanna,Smith, Alison J.,Reynolds, David S.,Sohal, Bindi,Pike, Andrew,Marshall, George R.,Wafford, Keith A.,Sheppard, Wayne F.A.,Tye, Spencer J.
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p. 1477 - 1480
(2007/10/03)
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- Discovery of imidazo[1,2-b][1,2,4]triazines as GABAA α2/3 subtype selective agonists for the treatment of anxiety
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The identification of a series of imidazo[1,2-b][1,2,4]triazines with high affinity and functional selectivity for the GABAA α3-containing receptor subtype is described, leading to the identification of a clinical candidate, 11. Compound 11 shows good bioavailability and half-life in preclinical species, and it is a nonsedating anxiolytic in both rat and squirrel monkey behavioral models.
- Russell, Michael G. N.,Carling, Robert W.,Street, Leslie J.,Hallett, David J.,Goodacre, Simon,Mezzogori, Elena,Reader, Michael,Cook, Susan M.,Bromidge, Frances A.,Newman, Robert,Smith, Alison J.,Wafford, Keith A.,Marshall, George R.,Reynolds, David S.,Dias, Rebecca,Ferris, Pushpindar,Stanley, Jo,Lincoln, Rachael,Tye, Spencer J.,Sheppard, Wayne F. A.,Sohal, Bindi,Pike, Andrew,Dominguez, Maria,Atack, John R.,Castro, José L.
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p. 1235 - 1238
(2007/10/03)
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- IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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A class of 8-fluoro-3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group, or by a pyrrolidinonyl group, which is directly attached or bridged by an oxygen atom or by a -NH- or -OCH2- linkage, being selective ligands for GABAA receptors, in particular having high affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
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