52311-59-8Relevant articles and documents
3-OXAZOLINONE COMPOUND, PREPARATION METHOD THEREFOR AND PHARMACEUTICAL APPLICATION THEREOF
-
Paragraph 0061; 0066; 0081; 0083, (2021/04/16)
The present invention relates to a novel 3-indazolinone compound that regulates or inhibits the activity of indoleamine 2,3-dioxygenase (IDO), the method for the preparation thereof and the use thereof in medicine. In particular, the present invention relates to a compound represented by the general formula (I) and a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound or a pharmaceutically acceptable salt thereof, a method for treating or preventing IDO-mediated diseases, especially tumors, by use of the compound or a pharmaceutically acceptable salt thereof, and a method for preparing the compound or a pharmaceutically acceptable salt thereof. The present invention further relates to use of the compound or a pharmaceutically acceptable salt thereof or a composition comprising the compound or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for treating or preventing IDO-mediated diseases, especially tumors.Wherein the substituents of the general formula (I) are defined the same as that in the specification.
Access to Chiral Seven-Member Cyclic Amines via Rh-Catalyzed Asymmetric Hydrogenation
Li, Pan,Huang, Yi,Hu, Xinquan,Dong, Xiu-Qin,Zhang, Xumu
supporting information, p. 3855 - 3858 (2017/07/26)
A highly efficient asymmetric hydrogenation of azepine/oxazepine-type seven-member cyclic imine hydrochlorides was successfully developed using Rh/bisphosphine-thiourea ligand ZhaoPhos, affording various chiral seven-member cyclic amines with full conversions, high yields, and excellent enantioselectivities (up to 96% yield, >99% ee). Additionally, this asymmetric hydrogenation can proceed well on gram scale with excellent ee value. Moreover, control experimental results displayed that the anion-bonding interaction between the chloride ion of the substrate and thiourea motif of the ZhaoPhos played an important role to obtain excellent enantioselectivity.
AMINO SUBSTITUTED DIARYL [A, D] CYCLOHEPTENE ANALOGS AS MUSCARINIC AGONISTS AND METHODS OF TREATMENT OF NEUROPSYCHIATRIC DISORDERS
-
Page/Page column 39, 40, (2011/04/14)
Disclosed herein are analogs of clozapine and pharmaceutically acceptable salts, esters, amides, or prodrugs thereof; methods of synthesizing the analogs; and methods of using the analogs for treating neuorpsychiatric disorders. In some embodiments, the analogs are amino substituted diaryl[a,d]cycloheptenes.