381233-75-6Relevant articles and documents
PYRROLIDINE-PYRAZOLES AS PYRUVATE KINASE ACTIVATORS
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Paragraph 366-368, (2021/10/11)
The subject matter described herein is directed to pyruvate kinase activating compounds of Formula I and pharmaceutical salts thereof, methods of preparing the compounds, pharmaceutical compositions comprising the compounds and methods of administering the compounds for the treatment of diseases associated with PKR and/or PKM2, such as pyruvate kinase deficiency, sickle cell disease, and beta-thalassemia.
BCL-2 FAMILY PROTEINS MODULATING COMPOUNDS FOR CANCER TREATMENT
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Page/Page column 55; 57, (2021/09/17)
The present invention relates to compounds, compositions and methods for treating cancers and disorders of cell proliferation and more particularly, methods of making and using compounds that modulate at least one of the proteins chosen from Bcl-2, Mcl-1,
Br vs. TsO Chemoselective Suzuki–Miyaura Cross-Coupling Reaction on Nicotinaldehyde Moiety for the Preparation of 2,3,5-Trisubstituted Pyridines
Hédou, Damien,Voisin-Chiret, Anne Sophie
supporting information, p. 3640 - 3649 (2020/06/10)
Br vs. TsO chemoselective pallado-catalyzed Suzuki–Miyaura reaction has been developed from the 5-bromo-2-tosyloxynicotinaldehyde for the preparation of polysubstituted pyridines. This methodology has been applied for the preparation of a terpyridine alde
URAT1 inhibitor and its application
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Paragraph 0187-0188, (2018/08/04)
The invention discloses a URAT1 inhibitor compound and its application of the compound. The URAT1 inhibitor compound is the compound or its pharmaceutically acceptable salt shown in structure of Formula (I). The experiment shows that the compound provided
BTK INHIBITOR
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Paragraph 0292, (2017/11/16)
Provided are a series of BTK inhibitors, and specifically disclosed are a compound, pharmaceutically acceptable salt thereof, tautomer thereof or prodrug thereof represented by formula (I), (II), (III) or (IV).
First evidence that oligopyridines, α-helix foldamers, inhibit Mcl-1 and sensitize ovarian carcinoma cells to Bcl-xL-targeting strategies
Gloaguen, Céline,Voisin-Chiret, Anne Sophie,Sopkova-De Oliveira Santos, Jana,Fogha, Jade,Gautier, Fabien,De Giorgi, Marcella,Burzicki, Grégory,Perato, Serge,Pétigny-Lechartier, Cécile,Simonin-Le Jeune, Karin,Brotin, Emilie,Goux, Didier,N'Diaye, Monique,Lambert, Bernard,Louis, Marie-Hélène,Ligat, Laetitia,Lopez, Frédéric,Juin, Philippe,Bureau, Ronan,Rault, Sylvain,Poulain, Laurent
, p. 1644 - 1668 (2015/03/18)
Apoptosis control defects such as the deregulation of Bcl-2 family member expression are frequently involved in chemoresistance. In ovarian carcinoma, we previously demonstrated that Bcl-xL and Mcl-1 cooperate to protect cancer cells against ap
MCL-1 MODULATING COMPOUNDS FOR CANCER TREATMENT
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Page/Page column 22; 28, (2015/09/28)
The invention relates to compounds of formula (I), and to their therapeutic use in the treatment of cancer : Wherein Y1, Y2, Ar1, Ar2, R1, R2, i, j, k, 1 are as defined in claim 1
SUBSTITUTED BENZOFURANYL AND BENZOXAZOLYL COMPOUNDS AND USES THEREOF
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Paragraph 00691, (2015/01/16)
The invention generally relates to substituted benzofuranyl and substituted benzoxazolyl compounds, and more particularly to a compound represented by Structural Formula (A) : or a pharmaceutically acceptable salt thereof, wherein the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of Structural Formula (A), or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment of cancer (e.g., mantle cell lymphoma), and other diseases and disorders.
Discovery of 2-(2-Oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl) benzonitrile (Perampanel): A novel, noncompetitive α-amino-3-hydroxy-5- methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist
Hibi, Shigeki,Ueno, Koshi,Nagato, Satoshi,Kawano, Koki,Ito, Koichi,Norimine, Yoshihiko,Takenaka, Osamu,Hanada, Takahisa,Yonaga, Masahiro
, p. 10584 - 10600 (2013/02/23)
Dysfunction of glutamatergic neurotransmission has been implicated in the pathogenesis of epilepsy and numerous other neurological diseases. Here we describe the discovery of a series of 1,3,5-triaryl-1H-pyridin-2-one derivatives as noncompetitive antagonists of AMPA-type ionotropic glutamate receptors. The structure-activity relationships for this series of compounds were investigated by manipulating individual aromatic rings located at positions 1, 3, and 5 of the pyridone ring. This culminated in the discovery of 2-(2-oxo-1-phenyl-5- pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel, 6), a novel, noncompetitive AMPA receptor antagonist that showed potent activity in an in vitro AMPA-induced Ca2+ influx assay (IC50 = 60 nM) and in an in vivo AMPA-induced seizure model (minimum effective dose of 2 mg/kg po). Perampanel is currently in regulatory submission for partial-onset seizures associated with epilepsy.
Synthetic approach to the chemical isostere of o -methyl honokiol
Cui, Minghua,Kim, Hak Sung
supporting information; experimental part, p. 311 - 313 (2012/02/15)
We established a synthetic method for the chemical isostere of the structurally unique natural product, 4-O-methyl honokiol by replacing two allyl groups with two different alkyl groups with the aim of developing synthetic analogues of the chemical isoste