494772-07-5Relevant articles and documents
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement
Barlaam, Bernard,De Savi, Chris,Dishington, Allan,Drew, Lisa,Ferguson, Andrew D.,Ferguson, Douglas,Gu, Chungang,Hande, Sudhir,Hassall, Lorraine,Hawkins, Janet,Hird, Alexander W.,Holmes, Jane,Lamb, Michelle L.,Lister, Andrew S.,McGuire, Thomas M.,Moore, Jane E.,O'Connell, Nichole,Patel, Anil,Pike, Kurt G.,Sarkar, Ujjal,Shao, Wenlin,Stead, Darren,Varnes, Jeffrey G.,Vasbinder, Melissa M.,Wang, Lei,Wu, Liangwei,Xue, Lin,Yang, Bin,Yao, Tieguang
supporting information, p. 15189 - 15213 (2021/11/01)
Optimization of a series of azabenzimidazoles identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective CDK9 inhibitors. With the goal of discovering a highly selective and potent CDK9 inhibitor administrated intravenously that would enable transient target engagement of CDK9 for the treatment of hematological malignancies, further optimization focusing on physicochemical and pharmacokinetic properties led to azaindoles 38 and 39. These compounds are highly potent and selective CDK9 inhibitors having short half-lives in rodents, suitable physical properties for intravenous administration, and the potential to achieve profound but transient inhibition of CDK9 in vivo.
AZETIDIN-3-YLMETHANOL DERIVATIVES AS CCR6 RECEPTOR MODULATORS
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Page/Page column 247, (2021/11/06)
The present invention relates to compounds of Formula (I), their synthesis and use as CCR6 receptor modulators for the treatment or prevention of various diseases, conditions or disorders.
NOVEL PHENYL PROPIONIC ACID DERIVATIVES AND USES THEREOF
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Paragraph 211-212; 213-215, (2018/07/05)
The present invention relates to the compounds according to Formula (I), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of meta
SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS
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Paragraph 0222; 0223, (2014/05/08)
Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R1, R2, R3, R4 and m are as defined in the specification.
New Positive allosteric modulators of nicotinic acetylcholine receptor
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Paragraph 0184, (2013/03/26)
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.
AMINES OR AMINO ALCOHOLS AS GLYT1 INHIBITORS
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Page/Page column 37, (2010/08/22)
The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.
CYCLOALKYLOXY-AND HETEROCYCLOALKYLOXYPYRIDINE COMPOUNDS AS MODULATORS OF THE HISTAMINE H3 RECEPTOR
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Page/Page column 12, (2009/05/28)
Certain cycloalkyloxy- and heterocycloalkyloxypyridine compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.
NOVEL BENZYL(IDENE)-LACTAM DERIVATIVES
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Page/Page column 38, (2008/06/13)
The present invention relates to novel benzyl(idene)-lactam derivatives, compounds of the formula (I) wherein R1 is a group of the formula G1 or G2 depicted below, wherein R1, R3, R6, R13, X, a, n and m are as defined herein, their pharmaceutically acceptable salts, and pharmaceutical compositions which include selective antagonists, inverse agonists and partial agonists of serotonin 1 (5-HT1) receptors, specifically, of one or both of the 5-HT1A and 5-HT1B receptors. The compounds of the invention are useful in treating or preventing depression, anxiety, obsessive compulsive disorder (OCD) and other disorders for which a 5-HT1 agonist or antagonist is indicated and have reduced potential for cardiac side effects, in particular QTc prolongation.