摘要:
Phenylethanolaminotetralincarboxamide derivative represented by general formula (I) and pharmacologically acceptable salts thereof, wherein A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino which may bear oxygen on the ring; the asterisked carbon atom represents a carbon atom with an R- or S-configuration or a mixture of such atoms; and the carbon atom labeled with (S) represents a carbon atom with an S-configuration. These compounds have selective β2-adrenergic receptor stimulating effects while reducing the burden on the heart, such as tachycardia, and are useful as preventives for threatened abortion and premature birth, bronchodilator, and agents for remission and lithagogue for urinary calculus.
摘要:
Novel phenylaminoalkylcarboxylic acid derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, which have an excellent effect of stimulating β3-adrenergic receptor and are useful as preventives or remedies for obesity, hyperglycemia, diseases caused by accelerated intestinal motion, frequent urination or urinary incontinence, depression, cholelithiasis, diseases caused by accelerated biliary motion, etc. In said formula, R1 represents hydroxy, lower alkyl, aralkoxy, amino, alicyclic amino optionally substituted by hydroxy or lower alkyl, or mono- or di(lower alkyl)amino; R2 represents hydroxy or lower alkyl; R3 represents hydrogen or halogeno; R?4 and R5¿ represent each hydrogen, halogeno or lower alkyl; A represents lower alkylene; the carbon atom bearing the mark (R) is a carbon atom with the (R) configuration; and the carbon atom bearing the mark (S) is one with the (S) configuration.
摘要:
A fused heterocyclic derivative represented by the general formula (I) (wherein R is hydrogen, OH, etc.; R is hydrogen, halogeno, or alkyl; R and R each is hydrogen, OH, halogeno, etc.; Q is alkylene, etc.; ring A is aryl or heteroaryl; and G is the group represented by the formula (G1) or (G2)), (G1) (G2) a pharmacologically acceptable salt of the derivative, or a prodrug of either. They have excellent inhibitory activity against human SGLT and are useful as preventive or therapeutic agents for diseases attributable to hyperglycemia, such as diabetes, postprandial hyperglycemia, impaired glucose tolerance, complications of diabetes, and obesity.
摘要:
Novel aminoethylphenoxyacetic acid derivatives represented by general formula (I) and pharmacologically acceptable salts thereof, which have effects of stimulating both of beta 2- and beta 3-adrenergic receptors and are useful in the pain remission and calculi removal promotion in urinary lithiasis; wherein R represents hydrogen, lower alkyl or aralkyl; R represents hydrogen or halogeno; and the carbon atoms with the marks of (R) and (S) are those having the (R)- and (S)-configurations respectively.
摘要:
5-Amidino-2-hydroxybenzenesulfonamide derivatives represented by the following general formula [I] exhibiting a potent and selective inhibitory activity on activated blood coagulation factor X and thus being useful as preventives or remedies for diseases in the onset of which activated blood coagulation factor X participates: [I] wherein R1 represents optionally substituted lower alkyl, optionally substituted lower alkoxy, optionally substituted alkenyl, cycloalkyl, lower acyl, etc.; Q represents hydrogen or optionally substituted lower alkyl; and Z represents hydrogen, hydroxy, etc.; pharmacologically acceptable salts thereof, medicinal compositions containing the same and intermediates in the production thereof. These compounds are useful as preventives or remedies for various diseases such as brain infarction, cerebral thrombosis, cerebral embolism, TIA, cerebral vascular jerk, Alzheimer’s diseases, myocardial infarction, heart attack, heart failure, thrombosis, pulmonary infarction and pulmonary embolism.
摘要:
Novel 2-methylpropionic acid derivatives represented by general formula (I) and pharmacologically acceptable salts thereof which have an excellent beta 3 adrenaline receptor stimulating effect and are useful as preventives or remedies for obesity, hyperglycemia, diseases caused by accelerated intestinal motion, frequent urination, urinary incontinence, depression, cholelithiasis or diseases caused by accelerated biliary motion. In said Formula (I) R represents hydrogen, lower alkyl or aralkyl; R represents hydrogen, lower alkyl or halogeno; A represents oxygen or imino; the carbon atom to which (R) is attached stands for one with the R-configuration; and the carbon atom to which (S) is attached stands for one with the S-configuration.
摘要:
3,4-Disubstituted phenylethanolaminotetralincarboxamide derivatives represented by general formula (I) and their pharmacologically acceptable salts having a selective β2-adrenergic receptor stimulating effect with a relieved burden on the heart such as frequent pulse. In said formula, A represents lower alkylene; B represents amino, di(lower alkyl)amino or 3- to 7-membered alicyclic amino optionally containing oxygen in the ring; n is an integer of 1 or 2; the carbon atom marked with '*' means a carbon atom or the R- or S- configuration or a mixture thereof; and the carbon atom marked with '(S)' means a carbon atom of the S-configuration. These compounds are useful as a preventive for threatened abortion/premature birth, a bronchodilator and a pain-relieving and lithagogue agent in ureterolithiasis.
摘要:
A compound having potent irritative activity against a human β3-adrenergic receptor and high selectivity therefor and represented by the general formula (I) (wherein R1 is hydrogen or lower alkyl; R2 and R3 each independently is hydrogen or lower alkyl; R4, R5, and R6 each independently is hydrogen, halogeno, lower alkyl, or lower alkoxy; R7 is hydrogen or lower alkyl; R8 is hydrogen, halogeno, lower alkyl, lower alkoxy, etc.; R9 is -COR10, -A1-COR10, -O-A2-COR10, etc.; Ar is optionally substituted phenyl or heteroaryl; and A is a bond, -OCH2, etc.), a prodrug of the compound, or a pharmacologically acceptable salt of either.
摘要:
Compounds represented by the general formula (I) which exhibit potent stimulating activity on beta3-adrenaline receptor and high selectivity therefor, or pharmacologically acceptable salts thereof; pharmaceutical compositions containing the same; and use thereof: (I) wherein R and R are each hydrogen or lower alkyl; R , R , R , and R are each hydrogen, halogeno, lower alkyl, or lower alkoxy; R and R are each hydrogen, halogeno, lower alkyl, halo lower alkyl, lower alkoxy, cycloalkyl, aryl, heteroaryl, cyano, hydroxyl, lower acyl, carboxyl, or the like; and R is -C(O)-R , -A -C(O)-R , -O-A -C(O)-R , or tetrazol-5-yl.
摘要:
Novel phenoxyacetic acid derivatives represented by general formula (I), and pharmacologically acceptable salts thereof, which exhibit an excellent beta 3-adrenergic receptor stimulating effect and are useful as preventive or therapeutic agents for obesity, hyperglycemia, diseases due to hyperkinesia of intestine, pollakiuria, urinary incontinence, depression, cholelithiasis or diseases due to hyperkinesia of biliary tract: wherein R is hydroxyl or the like; one of R and R is hydrogen, halogeno or the like, and the other thereof is hydrogen; and R is halogeno or the like.