436161-77-2Relevant academic research and scientific papers
POLYCYCLIC COMPOUND ACTING AS IDO INHIBITOR AND/OR IDO-HDAC DUAL INHIBITOR
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Paragraph 0197-0198, (2020/08/09)
The present invention provides polycyclic compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC. Specifically, the present invention provides compounds represented by the following formula (I), wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an antitumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the antitumor response rate of the antibody and broaden the types of tumors to be treated.
HETEROARYLAMINOISOQUINOLINES, METHODS FOR THEIR PREPARATION AND THERAPEUTIC USES THEREOF
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Page/Page column 105; 106, (2016/08/23)
The application is directed to compounds of formula (IA) : and specifically compounds of formula (I) and their salts and solvates, wherein R1, R11, R12, R13, R4, R5, n, A1, A2, and A3 are as set forth in the specification, as well as to a method for their preparation, pharmaceutical compositions comprising the same, and use thereof for the treatment and/or prevention of conditions associated with the alteration of the activity of β-galactosidase, specially galactosidase beta-1 or GLB1, including GM1 gangliosidoses and Morquio syndrome, type B.
CYANOQUINOLINE DERIVATIVES
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Paragraph 0246-0251, (2013/04/25)
Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.
CYANOQUINOLINE DERIVATIVES
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Paragraph 0354, (2013/09/12)
Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2
Unusually low barrier to carbamate C-N rotation
Deetz, Martin J.,Forbes, Christopher C.,Jonas, Marco,Malerich, Jeremiah P.,Smith, Bradley D.,Wiest, Olaf
, p. 3949 - 3952 (2007/10/03)
The barrier for rotation about an N-alkylcarbamate C(carbonyl)-N bond is around 16 kcal/mol. In the case of an N-phenylcarbamate, the rotational barrier is lowered to 12.5 kcal/mol, but with N-(2-pyrimidyl)carbamates the barriers are so low (9 kcal/mol)
