- Design and synthesis of a biaryl series as inhibitors for the bromodomains of CBP/P300
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A novel, potent, and orally bioavailable inhibitor of the bromodomain of CBP, compound 35 (GNE-207), has been identified through SAR investigations focused on optimizing al bicyclic heteroarene to replace the aniline present in the published GNE-272 series. Compound 35 has excellent CBP potency (CBP IC50 = 1 nM, MYC EC50 = 18 nM), a selectively index of >2500-fold against BRD4(1), and exhibits a good pharmacokinetic profile.
- Lai, Kwong Wah,Romero, F. Anthony,Tsui, Vickie,Beresini, Maureen H.,de Leon Boenig, Gladys,Bronner, Sarah M.,Chen, Kevin,Chen, Zhongguo,Choo, Edna F.,Crawford, Terry D.,Cyr, Patrick,Kaufman, Susan,Li, Yingjie,Liao, Jiangpeng,Liu, Wenfeng,Ly, Justin,Murray, Jeremy,Shen, Weichao,Wai, John,Wang, Fei,Zhu, Caicai,Zhu, Xiaoyu,Magnuson, Steven
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- IMIDAZOPIPERAZINONE INHIBITORS OF TRANSCRIPTION ACTIVATING PROTEINS
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The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of transcription activating proteins such as CBP and P300 for the treatment or prevention of diseases such as proliferative diseases, inflammatory disorders, autoimmune diseases, and fibrotic diseases.
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Paragraph 0577; 0586
(2019/10/20)
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- AMINOISOXAZOLINE COMPOUNDS AS AGONISTS OF ALPHA7-NICOTINIC ACETYLCHOLINE RECEPTORS
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The present invention relates to novel aminoisoxazoline compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of α7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.
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- PYRAZOLOPYRIDINE DERIVATIVES FOR THE TREATMENT OF CANCER
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The present invention relates to a compound formula (I): and to salts thereof, wherein R1, R2X, and Y have any of the values defined herein, and compositions and uses thereof. The compounds are useful as inhibitors of CBP and/or EP300. Also included are pharmaceutical compositions comprising a compound of formula (I) or a pharmaceutically acceptable salt thereof, and methods of using such compounds and salts in the treatment of various CBP and/or EP300-mediated disorders such as cancer, inflammatory disorders and autoimmune diseases.
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Page/Page column 92; 93
(2017/12/29)
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- Fe(ii), Ru(ii) and Re(i) complexes of endotopic, sterically non-hindering, U-shaped 8,8′-disubstituted-3,3′-biisoquinoline ligands: Syntheses and spectroscopic properties
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The redox behaviour, optical-absorption spectra and emission properties of U-shaped and elongated disubstituted biisoquinoline ligands and of derived octahedral Fe(ii), Ru(ii), and Re(i) complexes are reported. The ligands are 8,8′-dichloro-3,3′-biisoquin
- Ventura, Barbara,Barigelletti, Francesco,Durola, Fabien,Flamigni, Lucia,Sauvage, Jean-Pierre,Wenger, Oliver S.
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p. 491 - 498
(2008/09/17)
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