877149-15-0Relevant academic research and scientific papers
PYRROLO[2,3-B]PYRIDINES AS HPK1 INHIBITOR AND USES THEREOF
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Page/Page column 61, (2020/06/10)
Disclosed herein is a compound of Formula (I), or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions comprising thereof. Also disclosed is a method of treating HPK1 related disorders or diseases by using the compound disclosed herein.
Discovery of Potent and Selective 7-Azaindole Isoindolinone-Based PI3KγInhibitors
Miles, Dillon H.,Yan, Xuelei,Thomas-Tran, Rhiannon,Fournier, Jeremy,Sharif, Ehesan U.,Drew, Samuel L.,Mata, Guillaume,Lawson, Kenneth V.,Ginn, Elaine,Wong, Kent,Soni, Divyank,Dhanota, Puja,Shaqfeh, Stefan G.,Meleza, Cesar,Chen, Ada,Pham, Amber T.,Park, Timothy,Swinarski, Debbie,Banuelos, Jesus,Schindler, Ulrike,Walters, Matthew J.,Walker, Nigel P.,Zhao, Xiaoning,Young, Stephen W.,Chen, Jie,Jin, Lixia,Leleti, Manmohan Reddy,Powers, Jay P.,Jeffrey, Jenna L.
supporting information, p. 2244 - 2252 (2020/12/17)
The successful application of immunotherapy in the treatment of cancer relies on effective engagement of immune cells in the tumor microenvironment. Phosphoinositide 3-kinase γ(PI3Kγ) is highly expressed in tumor-associated macrophages, and its expression levels are associated with tumor immunosuppression and growth. Selective inhibition of PI3Kγoffers a promising strategy in immuno-oncology, which has led to the development of numerous potent PI3Kγinhibitors with variable selectivity profiles. To facilitate further investigation of the therapeutic potential of PI3Kγinhibition, we required a potent and PI3Kγ-selective tool compound with sufficient metabolic stability for use in future in vivo studies. Herein, we describe some of our efforts to realize this goal through the systematic study of SARs within a series of 7-azaindole-based PI3Kγinhibitors. The large volume of data generated from this study helped guide our subsequent lead optimization efforts and will inform further development of PI3Kγ-selective inhibitors for use in immunomodulation.
2,3,5-TRISUBSTITUTED PYRAZOLO[1,5-A]PYRIMIDINE COMPOUNDS
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Paragraph 0231; 0235, (2020/12/29)
Compounds that inhibit PI3Kγ, and compositions containing the compound(s) and methods for synthesizing the compounds, are described herein. Also described are the use of such compounds and compositions for the treatment of a diverse array of diseases, dis
Polycyclic compound inhibiting MNK1 and MNK2
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Paragraph 0265-0271, (2019/10/04)
The invention relates to a polycyclic compound inhibiting MNK1 and MNK2. Specifically, the invention provides a compound, or a stereoisomer and a tautomer thereof, or a pharmaceutically acceptable salt thereof, or a prodrug thereof, or a hydrate thereof,
Isoindoline, azaisoindoline, dihydroindenone and dihydroazaindenone inhibitors of Mnk1 and Mnk2
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Page/Page column 111, (2018/11/21)
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2
BIOREVERSABLE PROMOIETIES FOR NITROGEN-CONTAINING AND HYDROXYL-CONTAINING DRUGS
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Page/Page column 141; 142, (2015/06/18)
Disclosed are promoieties of the following formula which can be used to form prodrugs of nitrogen-containing or hydroxyl-containing drug or a pharmaceutically active agent: (I) and pharmaceutical compositions comprising the prodrugs.
ISOINDOLONE COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS
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Page/Page column 63, (2008/06/13)
The present invention is directed to compounds of formula (I), wherein R1 is a ring and n is a number from 1 to 8. The invention also relates to use of the compounds in therapy as metabotropic glutamate receptor modulators, particularly in neurological and psychiatric disorders.
