- NOVEL 4,6-DISUBSTITUTED AMINOPYRIMIDINE DERIVATIVES HAVING BOTH AROMATIC AND HALOGENIC SUBSTITUENTS
-
Certain 4,6-disubstituted aminopyrimidine derivatives having both aromatic and halogenic substituents.
- -
-
Paragraph 0417; 0418
(2014/03/24)
-
- AMIDE COMPOUNDS AND MEDICINAL USE THEREOF
-
The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.
- -
-
-
- Isothiazolones
-
Isothiazolones having the general structure STR1 where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R1 and R2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
- -
-
-
- Arylthio compounds
-
Antibacterial and antiviral phenylthiols and dithiobisbenzamides have the formula STR1 where n is 1 or 2, Y is hydrogen when n is 1, and a single bond when n is 2; and R1 and R11 are substituent groups, R4 is hydrogen or alkyl, and Z is hydrogen, alkyl, cycloalkyl or sulfamoylphenyl.
- -
-
-
- Chromogenic thiol indicators based on an isobenzothiazolone ring system
-
Newly synthesized chromogenic thiol-indicating benzoisthiazolone derivatives having the structure: STR1 where R1, R2 and R3 are as defined in the specification, are useful in the detection of thiols, particularly in an aqueous system. This process comprises contacting the aqueous system with a chromogenic thiol-indicating benzoisothiazolone derivative as described herein. Chromophoric changes due to thiol-mediated reduction of the benzothiazolone derivative then occur. Such changes can be in a solution or on an indicator surface in contact or having been in contact with the aqueous system. The chromophoric changes, due to a bathochromic shift in characteristics light absorption upon reduction of the benzoisothiazolone derivative, are proportional to the amount or rate of appearance of thiols in the aqueous system.
- -
-
-
- A Mild and Convenient Oxidation of Aryl Nitriles to Aryl Amides by Aqueous Sodium Perborate
-
A series of benzonitriles has been reacted with sodium perborate in water and a cosolvent to produce the corresponding amides in good yield.The procedure is a mild and convenient alternative for the synthesis of aryl amides.
- Reed, Kathryn L.,Gupton, John T.,Solarz, Traci L.
-
p. 563 - 571
(2007/10/02)
-
- Cycloaracylation of Enamines, I. - Synthesis of 4-Quinolone-3-carboxylic Acids
-
Starting with o-halobenzoyl chlorides 4 and open-chain secondary enamines 5, a new synthesis of 4-quinolone-3-carboxylic acids 12 is described.The reaction of 7-haloquinolone-3-carboxylic acids 12a-k with aliphatic amines 14 produces highly active antibacterial 7-aminoquinolone-3-carboxylic acids 15.The main product of the 1-cyclopropyl series, "ciprofloxacin" (15a), is being developed as a broad-spectrum chemotherapeutic agent.
- Grohe, Klaus,Heitzer, Helmut
-
-