摘要:
The substituted 5-(phenoxyalkanoylamino)-uracil compounds have the following formula I: ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen; a branched or linear alkyl group having 1 to 6 carbon atoms; a branched or straight chain alkenyl or alkynyl group having 1 to 6 carbons atoms; a cycloalkyl group having from 3 to 7 carbon atoms or a cycloalkylmethyl group having a cycloalkyl residue of 3 to 7 carbon atoms; or a phenylalkyl group having an alkyl residue having from 1 to 3 carbon atoms and a phenyl residue, the phenyl residue being unsubstituted or having a halogen, methoxy, methyl or trifluoromethyl substituent; R.sub.3 is a hydrogen, methyl or amino groups; R.sub.4 is halogen, methoxy or methyl groups, and n is 1 or 2. Pharmaceutical compositions for treating cerebrovascular, neuronal-degenerative and senility-induced disorders associated with learning, memory and cognitive dysfunctions are described which contain a therapeutically effective amount of the substituted 5-(phenoxyalkanoylamino)-uracil in a pharmaceutically acceptable carrier.
摘要:
The invention is directed to N-acetyl-4-phenyl-pyrrolidin-2-ones, which, because of their pronounced cerebroprotective effect in human medicine, can be used for the prophylaxis and treatment of cerebral functional disorders. Pursuant to the invention, these compounds are synthesized by reacting 4-phenyl-pyrrolidin-2-ones with a reactive derivative of a carboxylic acid, or by cyclizing N-acylaminobutyric acid derivatives.
摘要:
5-(w-Aminoacyl)-5,10-dihydro-11H-dibenzo(b,e)(1,4)-diazepine-11-ones, and their preparation are disclosed for treatment of antiarrhythmia and as an anticholinergic drug.
摘要:
A method for preparing high bulk density crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine which comprises precipitating a high bulk density crystaline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine from a starting material that is(a) a solution in an inorganic or organic acid, and precipitating with a base, or(b) a solution in a chlorinated hydrocarbon, and precipitating with an aliphatic hydrocarbon, or(c) from an aliphatic ester of an aliphatic carboxylic acid and an aliphatic alcohol.The compact, crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine, so obtained, has a bulk density of from about 220 to about 360 g/l and is most suitable for pharmaceutical preparations.
摘要:
A method for preparing high bulk density crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine which comprises precipitating a high bulk density crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine from a starting material that is(a) a solution in an inorganic or organic acid, and precipitating with a base, or(b) a solution in a chlorinated hydrocarbon, and precipitating with an aliphatic hydrocarbon, or(c) from an aliphatic ester of an aliphatic carboxylic acid and an aliphatic alcohol.The compact, crystalline 3-cyano-2-morpholino-5-(pyrid-4-yl)-pyridine, so obtained, has a bulk density of from about 220 to about 360 g/l and is most suitable for pharmaceutical preparations.
摘要:
New 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines of formula I and their pharmaceutically acceptable salts were found to be suitable actives for the treatment of cardiac arrhythmia. Previously unknown 3-carbalkoxyamino-5-(alpha-halogenpropionyl)-5H-dibenz[b,f]azepines are obtained from 3-carbalkoxyamino-5H-dibenz[b,f]azepines by reaction with alpha-halogenpropionyl halides. Through their reaction with ammonia, primary amines or secondary amines, the new 3-carbalkoxyamino-5-(alpha-aminopropionyl)-5H-dibenz[b,f]azepines are obtained, which can be optionally converted into their pharmaceutically acceptable acid addition salts.
摘要:
New 3-carbalkoxyamino-5-aminoacyl-5H-dibenz[b,f]azepines and their pharmaceutically acceptable acid addition salts, and methods for their synthesis are described. These compounds are useful as antiarrhythmic agents in the treatment of heart disorders. The new compounds are made by reacting a 3-carbalkoxyamino-5-halogenacyl-5H-dibenz[b,f]azepines with an amine to form the desired target product, which can be optionally converted into its pharmaceutically acceptable acid addition salt.
摘要:
The invention relates to novel crosslinkable copolymers of formula wherein the variables are as defined in the claims. The copolymers of the invention are especially useful for the manufacture of biomedical moldings, for example ophthalmic moldings such as in particular contact lenses.
摘要:
An ophthalmic lens suited for extended-wear periods of at least one day on the eye without a clinically significant amount of corneal swelling and without substantial wearer discomfort. The lens has a balance of oxygen permeability and ion or water permeability, with the ion or water permeability being sufficient to provide good on-eye movement, such that a good tear exchange occurs between the lens and the eye. A preferred lens is a copolymerization product of a oxyperm macromer and an ionoperm monomer. The invention encompasses extended wear contact lenses, which include a core having oxygen transmission and ion transmission pathways extending from the inner surface to the outer surface.