88002-33-9Relevant academic research and scientific papers
ANNULATED GLYCOSIDASE INHIBITORS
-
Page/Page column 120, (2019/03/12)
Compounds of formula (I) wherein A, R, W1, W2, W3, W4, W5, W6, L, Q, Rx and u have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
ANTI-PULMONARY TUBERCULOSIS NITROIMIDAZOLE DERIVATIVE
-
Paragraph 0444; 0447; 0448, (2017/12/31)
Disclosed is a substituted nitroimidazole derivative, which is mainly used for treating related diseases caused by mycobacterial infections, such as Mycobacterium tuberculosis, especially being suitable for diseases caused by resistant Mycobacterium tuberculosis.
HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS
-
Paragraph 0318-0319, (2017/11/30)
Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections.
BICYCLIC AZAHETEROCYCLIC COMPOUNDS AS NR2B NMDA RECEPTOR ANTAGONISTS
-
Paragraph 0190, (2016/07/05)
Disclosed are chemical entities of Formula (I): wherein R1 and Z are defined herein, as NR2B subtype selective receptor antagonists. Also disclosed are pharmaceutical compositions comprising a chemical entity of Formula (I), and methods of treating various diseases and disorders associated with NR2B antagonism, e.g., diseases and disorders of the CNS, such as depression, by administering a chemical entity of Formula (I).
Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
-
Paragraph 0535; 0536, (2018/10/03)
PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
-
Paragraph 1093; 1095, (2015/11/16)
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Design, synthesis, and structure-activity relationship studies of novel fused heterocycles-linked triazoles with good activity and water solubility
Cao, Xufeng,Sun, Zhaoshuan,Cao, Yongbing,Wang, Ruilian,Cai, Tongkai,Chu, Wenjing,Hu, Wenhao,Yang, Yushe
supporting information, p. 3687 - 3706 (2014/05/20)
Triazoles with fused-heterocycle nuclei were designed and evaluated for their in vitro activity on the basis of the binding mode of albaconazole using molecular docking, along with SAR of antifungal triazoles. Tetrahydro-[1,2,4] triazolo[1,5-a]pyrazine and tetrahydro-thiazolo[5,4-c]pyridine nuclei were preferable to the other four fused-heterocycle nuclei investigated. Potent in vitro activity, broad spectrum and better water solubility were attained when triazoles containing nitrogen aromatic heterocycles were attached to these two nuclei. The most potent compounds 27aa and 45x, with low hERG inhibition and hepatocyte toxicity, both exhibited excellent activity against Candida, Cryptococcus, and Aspergillus spp., as well as selected fluconazole-resistant strains. A high water-soluble compound 58 (the disulfate salt of 45x) displayed unsatisfactory in vivo activity because of its poor PK profiles. Mice infected with C.alb. SC5314 and C.alb. 103 (fluconazole-resistant strain) and administered with 27aa displayed significantly improved survival rates. 27aa also showed favorable pharmacokinetic (PK) profiles.
Cyanoamino Compounds in Synthesis Syntheses of Some Heterocycles
Vercek, Bojan,Ogorevc, Bozidar,,Stanovnik, Branko,Tisler, Miha
, p. 789 - 798 (2007/10/02)
Transformations of some heterocyclic cyanoamino compounds leading to various heterocyclic systems are described. s-Triazolo(1,5-a)azines are obtained either in a direct synthetic approach or via the substituted aminotetrazoles, substituted 3-amino-5-oxo-1,2,4-oxadiazolines, and from N-ethoxycarbonyl N'-heteroaryl thioureas or N-heteroaryl N'-hydroxyguanidine.The cyanoamino group reacts also with o-difunctional benzenes to give the corresponding substituted derivatives of benzimidazole, benzoxazole or benzothiazole. - Keywords: Cyclization with N-N bond formation; Heterocyclic compounds; Rearrangements
