Y 1 is selected from hydroxyl, alkylamino, alkanoylamino, Y 2 , Y 3 and Y 4 are independently selected from hydrogen, halogen, alkyl, alkoxy, trifluoromethyl, hydroxyl and benzyloxy; and Q 1 is either where Q 2 and Q 3 are independently selected from hydrogen and alkyl; X is selected from cyano, carboxyl, 5-tetrazolyl and alkylsulphonylcarbamoyl; and n is 0 or an integer selected from 1. 2. 3, 4, 5 and 6: salts of said compounds and, when X is carboxyl, esters and amides thereof,
provided that
when Y 1 is hydroxyl Y 2 , Y 3 and Y 4 are all hydrogen and Q 1 is either then X is alkylsulphonylcarbamoyl.
These compounds are of value in medicine in the palliation of haemoglobinopathies, in particular sickle-cell anaemia and also in the palliation of pulmonary dysfunction, protection from the effects of hypoxia and the radio-sensitization of tumours. The invention is also directed to methods for the preparation of the ether compounds, to pharmaceutical formulations containing them and to the preparation of such formulations.
摘要:
The invention relates to 1-amino-phthalazine derivatives of general formula (I), wherein A, B = possibly substituted C1-4-alkylene; L = a simple bond or C1-2-alkylene, possibly substituted -CH=CH-, or -C=C- or cycloprop-1,2--diyl; R1 = possibly substituted aryl or heteroaryl; R2, R3 = H, C1-3-alkyl, C1-3-fluoralkyl or R2 et R3 forming together with a bearing them carbon atom, a cycloprop-1,1-diyl; R4 = H, C1-5-alkyl, C1-3-fluoralkyl, C3-6-cycloalkyl, C3-6-cycloalkyl-C1-3-alkylene, C1-3-alkyl-O-C1-3-alkylene, HO-C1-3-alkylene, C1-3-alkyl-X-C1-3-alkylene, wherein X = S, SO or S02; or R4 = RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O-, aryl-O-C1-3-alkylene, aryl-C1-3-alkylene-O-C1-3-alkylene, heteroaryl or heteroaryl-C1-3-alkylene; R5 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3-alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R5 = RaRbN-, RaRbN-C1-3-alkylene, aryl, aryl-C1-3-alkylene, aryl-O- or heteroaryl; R6 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, -CN, RaRbN-, RaRbN-C1-3-alkylene, aryl or heteroaryl ; R7 = H, halogen, C1-5-alkyl, C1-3-fluoralkyl, C1-5-alkoxy, C1-3-fluoroalkoxy, HO-C1-3--alkylene, -CN, C1-3-alkyl-X-, wherein X = S, SO or SO2; or R7, = RaRbN-, RaRbN-C1-3--alkylene, ReRbNC(O)-, C1-3-alkyl-C(O)-, aryl, aryl-0- or heteroaryl ; R8 = H, halogen, C1-5-alkyl, C1-5-alkoxy, C1-3-fluoroalkoxy ; in the form of base or acid additional salt and in the form of a hydrate or solvent. A method for preparing and using the inventive derivatives for therapeutically purpose is also disclosed.
摘要:
The instant invention is concerned with acetylphenols which are useful as antiobesity and antidiabetic compounds. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering or modulating triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for increasing gut motility or for treating atherosclerosis are also disclosed.
摘要:
The invention relates to 3-cyano-2,4,5-trifluoro-benzoyl fluoride and intermediate products for the production thereof and a method for the production of 3-cyano-2,4,5-trifluoro-benzoyl fluoride starting from 5-fluoro-1,3-xylol (VIII), which is chlorinated twice in the presence of a catalyst with ionic conditions in the nucleus to obtain 2,4-dichloro-5-fluoro-1,3-dymethylbenzol (VII), which is then chlorinated with radical conditions in the side chains to obtain 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethyl benzol (VI), which is subsequently saponified by the optionally isolatable 2,4-dichloro-5-fluoro-3-dichloromethyl benzoic acid (V) to obtain 2,4-dichloro-5-fluoro-3-formyl-benzoic acid (IV) whose aldehyde group is converted to 2,4-dichloro-5-fluoro-3-N-hydroxyiminomethyl-benzoic acid (III), whereupon water is eliminated using an acid chloride while at the same time converting the carboxyl group into a chlorocarbonyl group to obtain nitrile 2,4-dichloro-3-cyano-5-fluoro-benzoyl-chloride (II), which is finally subjected to a fluorine/chlorine exchange.
摘要:
The invention provides a process for modifying CNSL comprising subjecting the CNSL to ozonolysis to form ozonolysis reaction products followed by reduction of the ozonolysis reaction products to give a mixture of phenolic components and aldehydes. In a preferred embodiment, the invention provides a process for modifying CNSL which comprises the steps of first reacting CNSL with ozone to form a mixture containing ozonolysis reaction products, and secondly treating the mixture under reducing conditions to form a further mixture containing phenolic components with an eight carbon chain having a terminal CHO group and alkyl components of varying lengths with either one or two terminal CHO groups. The resulting CNSL aldehydes can be used to form adhesives for use in the manufacture of composites such as wood particle board.
摘要:
This invention provides smoking compositions which contain a vanillin carboxylate type flavorant-release additive. Under cigarette smoking conditions, a combustible filler and/or paper wrapper additive such as 5-carboxyethylvanillin pyrolyzes and releases ethylvanillin as a volatile flavorant component of the cigarette smoke.