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.
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.
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.
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.
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.
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.
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.
Bradykinin B1 receptor antagonists: An α-hydroxy amide with an improved metabolism profile
Kuduk, Scott D.,Chang, Ronald K.,DiPardo, Robert M.,Di Marco, Christina N.,Murphy, Kathy L.,Ransom, Richard W.,Reiss, Duane R.,Tang, Cuyue,Prueksaritanont, Thomayant,Pettibone, Douglas J.,Bock, Mark G.
scheme or table, p. 5107 - 5110 (2009/05/26)
A series of carbo- and heterocyclic α-hydroxy amide-derived bradykinin B1 antagonists was prepared and evaluated. A 4,4-difluorocyclohexyl α-hydroxy amide was incorporated along with a 2-methyl tetrazole in lieu of an oxadiazole to afford a suitable compound with good pharmacokinetic properties, CNS penetration, and clearance by multiple metabolic pathways.
