摘要:
A trialkylamine derivative represented by general formula (1) or a pharmacologically acceptable salt thereof, wherein R?1 and R2¿ may be the same or different from each other and each represents lower alkyl; R?3, R4 and R5¿ may be the same or different from one another and each represents hydrogen, lower alkyl, lower alkoxy, lower alkoxycarbonyl or halogen; R?6 and R7¿ may the same or different from each other and each represents hydrogen or lower alkyl; R8 represents hydrogen, lower alkyl, lower alkoxy or halogen; X represents oxygen, sulfur, -CH=N- or -CH=CH-; Y represents oxygen, sulfur, methylene, =N-R11 (wherein R11 represents lower alkyl), =SO or =SO¿2?; Z represents -OCO(CH2)p∩ or -OCH2(CH2)p∩ (wherein p represents a number of 0 to 4 and symbol ∩ represents the linkage with a benzene ring; and m and n represent each a number of 0 to 3 and the sum of m and n is 3 or less, provided that the case where m is 0, n is 1 or 2, R?1 and R2¿ represent each methyl, X represents -CH=CH-, Y represents -CH¿2?-, and Z represents -O-CO∩ is excluded). These compounds have an excellent activity of ameliorating digestive tract movement and hence are widely utilized in the treatment of digestive system diseases.
摘要:
Aryl substituted thiophenes 3-ols, its dihydro derivatives, 1-oxide and 1,1-dioxide analogs, as well as aryl substituted furans, are 5-lipoxygenase inhibitors useful in the treatment of inflammation and other leukotriene-mediated diseases.
摘要:
9,10-Dihydro-4H-benzo(4,5) cyclohepta(1,2-b) thiophen-4,5-imines of the formula wherein R is hydrogen, alkyl, alkenyl, phenyl (or substituted phenyl) alkyl, cycloalkyl, cycloalkylalkyl, dialkylaminoalkyl, R 2 is hydrogen, alkyl, alkenyl, phenylalkyl, cycloalkylalkyl, dialkylaminoalkyl and R 3 and R. are hydrogen, halogen, alkoxy, trifluoromethylthio, cyano, carboxy or hydroxy, are useful as antianxiety agents, as muscle relaxants and in the treatment of extrapyramidal disorders such as in Parkinson's disease.
摘要:
Tricyclic chemical modulators of FOXO transcription factor proteins are disclosed. The compounds are useful to treat cancer, age-onset proteotoxicity, stress-induced depression, inflammation, and acne. The compounds are of the following and similar genera (i), (ii) and (iii), in which Het is an aromatic heterocyclic ring and Y is a point of attachment of various side chains and rings. An example of such a compound is 4-chloro- N -(3-(10,11-dihydro-5H-benzo[b]pyrido[2,3-f]azepin-5-yl)propyl)benzenesulfonamide (iv).
摘要:
The present invention relates to methods of treating pathological disorders susceptible to steroid hormone nuclear receptor modulation comprising administering to a patient in need thereof an effective amount of a compound of the formula (I): or a pharmaceutically acceptable salt thereof. In addition, the present invention provides novel pharmaceutical compounds of Formula (I), including the pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions which comprise as an active ingredient a compound of Formula (I).
摘要:
This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.