873383-11-0Relevant articles and documents
OXAAZAQUINAZOLINE-7(8H)-KETONE COMPOUND, PREPARATION METHOD THERFOR AND PHARMACEUTICAL APPLICATION THEREOF
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, (2022/03/22)
Disclosed are an oxazaazaquinazolin-7(8H)-ketone compound with a selective inhibition effect on KRAS gene mutation and pharmaceutically acceptable salts thereof, stereoisomers, solvent compounds or prodrugs (as shown in formula I or formula II, see the details of the definition to each group in the formulas in the specification), as well as the pharmaceutical composition containing the compound, and the application thereof in preparation of cancer medicine.
MACROCYCLIC MCL-1 INHIBITORS AND METHODS OF USE
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Paragraph 00359, (2019/03/05)
The present disclosure provides for compounds of Formula (I) wherein A2, A3, A4, A6, A7, A8, A15, RA, R5, R9, R10A, R10B, R11, R12, R13, R14, R16, W, X, and Y have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including cancer. Also provided are pharmaceutical compositions comprising compounds of Formula (I).
INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE
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Paragraph 00267, (2018/12/03)
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
ISOQUINOLINES AS INHIBITORS OF HPK1
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Paragraph 0709; 0710, (2018/10/21)
Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.
BTK INHIBITOR
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Paragraph 0412, (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).
NEW COMPOUNDS
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, (2015/10/06)
The present invention provides certain compounds according to formula (I) which are inhibitors of SSAO activity wherein V, W, X, Y, Z, R1 and R2 are as defined in the specification.
Asymmetric Homogeneous Hydrogenation of 2-Pyridones
Wysocki, Jedrzej,Schlepphorst, Christoph,Glorius, Frank
supporting information, p. 1557 - 1562 (2015/06/30)
An asymmetric homogeneous hydrogenation of 2(1H)-pyridones has been developed, using a ruthenium complex bearing two chiral N-heterocyclic carbene (NHC) ligands. To the best of our knowledge, the presented reaction is the first example of a homogeneous asymmetric conversion of 2-pyridones into the corresponding enantioenriched 2-piperidones.
NRF2 REGULATORS
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Page/Page column 323, (2015/07/07)
The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
IMIDAZO[4,5-C]PYRIDINE AND PYRROLO[2,3-C]PYRIDINE DERIVATIVES AS SSAO INHIBITORS
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Page/Page column 65-66, (2014/09/29)
The compounds of formula (I) are inhibitors of semicarbazide- sensitive amine oxidase (SSAO) activity useful in the treatment of inflammation, an inflammatory disease, an immune or an autoimmune disorder, or inhibition of tumour growth.
Heteroaromatic and aniline derivatives of piperidines as potent ligands for vesicular acetylcholine transporter
Li, Junfeng,Zhang, Xiang,Zhang, Zhanbin,Padakanti, Prashanth K.,Jin, Hongjun,Cui, Jinquan,Li, Aixiao,Zeng, Dexing,Rath, Nigam P.,Flores, Hubert,Perlmutter, Joel S.,Parsons, Stanley M.,Tu, Zhude
, p. 6216 - 6233 (2013/09/02)
To identify suitable lipophilic compounds having high potency and selectivity for vesicular acetylcholine transporter (VAChT), a heteroaromatic ring or a phenyl group was introduced into the carbonyl-containing scaffold for VAChT ligands. Twenty new compounds with ALogD values between 0.53 and 3.2 were synthesized, and their in vitro binding affinities were assayed. Six of them (19a, 19e, 19g, 19k, and 24a-b) displayed high affinity for VAChT (Ki = 0.93-18 nM for racemates) and moderate to high selectivity for VAChT over σ1 and σ2 receptors (Ki = 44-4400-fold). These compounds have a methyl or a fluoro substitution that provides the position for incorporating PET radioisotopes C-11 or F-18. Compound (-)-[11C]24b (Ki = 0.78 nM for VAChT, 1200-fold over σ receptors) was successfully synthesized and evaluated in vivo in rats and nonhuman primates. The data revealed that (-)-[11C]24b has highest binding in striatum and has favorable pharmacokinetics in the brain.