5117-85-1Relevant academic research and scientific papers
PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
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Paragraph 0256-0258, (2020/11/30)
Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
HIV PROTEASE INHIBITORS
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Paragraph 0564; 0565, (2017/08/26)
The present invention is directed to 2,6-morpholine derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein Z1, Z2, V1, V2, V3, R6, R6A, and X are defined herein. The invention also relates to methods of using the 2,6-morpholine derivatives of the invention for the inhibition of HV protease, the inhibition of HV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Volution lactone compound and synthesis method and application thereof
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Paragraph 0048-0049, (2017/05/12)
The invention discloses a volution lactone compound. The chemical structural formula of the volution lactone compound is shown in the specification. A preparing method of the volution lactone compound includes the steps that (1) cyclopentanone serves as a raw material and is subjected to a cyanohydrintion reaction, then cyano groups are hydrolyzed and esterified, and hydroxyl-cyclopentanecarboxylic acid ethyl ester is obtained; (2) a sulfonation reaction is carried out; (3) a butt joint ring formation reaction is carried out; (4) an alkylation reaction is carried out, wherein the cyclizing product obtained in the step (3), a reaction solvent and a catalyst are mixed, 3-bromopropylene is added into the mixed liquid, the solvent is removed in a pressure-reduction mode after reacting, water and benzene are added, extracting and layering are carried out, an organic phase substance is obtained, solvent pressure-reduction removing and filtering are carried out, and the final product volution lactone compound is obtained. The volution lactone compound has the advantage that a pesticide good in pest killing effect, long in lasing period and low in toxicity is obtained.
Anesthetic compounds and related methods of use
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Page/Page column 64, (2015/11/09)
Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.
Synthesis, spectral, and structural characteristics of cyanohydrines derived from aliphatic cyclic ketones1
Hosten,Betz
, p. 2222 - 2227 (2015/02/02)
A series of cyanohydrines derived from cyclic aliphatic ketones was synthesized by acid-catalyzed nucleophilic addition reaction under the action of potassium cyanide. The products were characterized by means of multi-nuclear NMR spectroscopy (1H, 13C, 14N, 15N), mass spectrometry, elemental analysis, UV-Vis spectroscopy, refraction index measurements as well as vibrational spectroscopy. The structure of the cyanohydrine of cyclohexanone was elucidated by means of single crystal X-ray diffraction.
Novel 4H-1,2,4-triazol-3-yl cycloalkanols as potent antitubercular agents
Desai, Nutan H. Palsule,Bairwa, Ranjeet,Kakwani, Manoj,Tawari, Nilesh,Ray,Rajan,Degani, Mariam
, p. 401 - 408 (2013/03/13)
Enzymes of shikimate pathway, dehydroquinase and shikimate kinase represent comparatively newer targets for antitubercular research. Molecular hybridization approach was implemented by integrating the essential features of inhibitors acting on these enzymes of shikimate pathway. Considering the flexibility of alicyclic ring of reported dehydroquinase (DHQ) inhibitors and triazole ring, key feature of the virtual hits of Mtb shikimate kinase, a series of structurally novel, substituted 4H-1,2,4-triazol-3-yl cycloalkanols were designed as antimycobacterial agents. Docking studies of the molecules was carried out on the enzyme DHQ. All the synthesized compounds exhibited promising activity (MIC 0.59-15.5 μg/ml) against H37Rv strains of Mycobacterium tuberculosis using resazurin microtiter assay. Five of the evaluated compounds exhibit MIC 50 values indicate compounds are non-toxic, with selectivity indices >28. These compounds could serve as leads for further optimization to obtain novel antimycobacterial agents.
ANESTHETIC COMPOUNDS AND RELATED METHODS OF USE
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Paragraph 00199, (2013/07/25)
Provided herein are compounds according to formula (I): Provided herein is also a pharmaceutical composition comprising a compound according to formula (I) and a pharmaceutically acceptable carrier, and a method for providing anesthesia in a subject by administering such a pharmaceutical composition.
Asymmetric synthesis of both the enantiomers of antidepressant venlafaxine and its analogues
Bhuniya, Rajib,Nanda, Samik
scheme or table, p. 1990 - 1992 (2012/05/05)
Chemoenzymatic asymmetric synthesis of antidepressant agent venlafaxine and its analogue have been reported in this communication. The main highlight of the reported synthesis is the stereoselective synthesis of cyanohydrins by (S)-hydroxynitrile lyase (Hevea brasiliensis) followed by lipase catalyzed kinetic resolution.
BENZAMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
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Page/Page column 77, (2012/09/11)
The invention relates to benzamide derivatives of formula (I),wherein R1, R2, R3, R4, R5, R6, n and Y are as defined in the description, their preparation and their use as pharmaceutically active compounds.
Reactivity of the 4-amino-5H-1,2-oxathiole-2,2-dioxide heterocyclic system: A combined experimental and theoretical study
De Castro, Sonia,Teresa Peromingo,Lozano, Angel E.,Camarasa, Maria-Jose,Velazquez, Sonsoles
supporting information; experimental part, p. 9620 - 9632 (2009/10/01)
The reactivity of the 4-amino-5H-1,2-oxathiole-2,2-dioxide (or β-amino-γ-sultone) heterocyclic system has scarcely been studied. Here we describe the reactivity of this system towards electrophiles and amines on readily available model substrates differently substituted at the C-5 position. A variety of C-electrophiles, carbonyl electrophiles (such as acyl chlorides, isocyanates, or aldehydes) and halogen or nitrogen electrophiles have been explored. Both the C-3 and 4-amino positions of the β-amino-γ- sultone system are able to undergo electrophilic reactions, and the reaction products depend on the electrophile used and on the reaction conditions. On the other hand, nucleophilic attack of amines occurs at the C-4 position of the β-amino-γ-sultone system only in spiranic substrates bearing alicyclic substituents at the C-5 position. A comparative computational study between spiranic and non-spiranic substrates suggests that conformational changes, undergone on intermediate compounds, account for the observed reactivity differences. Moreover, these conformational changes seem to bring about an increase of electron density on the N-4 and C-3 atoms of the enaminic system, and a possible enhancement in the reactivity of spiranic substrates towards electrophiles in the presence of amines. Experimental data consistent with this predicted enhanced reactivity is also presented.
