摘要:
The present invention relates to an antidepressant containing as an active ingredient a triazine derivative or a pharmaceutically acceptable salt thereof, the derivative being represented by the following Formula (I): ##STR1## in which, R.sup.1 represents hydrogen, substituted or unsubstituted lower alkyl, or substituted or unsubstituted lower alkanoyl; R.sup.2 represents hydrogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkenyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group; R.sup.3 represents a substituted or unsubstituted heterocyclic group; X represents a single bond, O, S, S(O), S(O).sub.2, or NR.sup.4 (in which R.sup.4 represents hydrogen, or substituted or unsubstituted lower alkyl; or R.sup.2 and NR.sup.4 are combined to form a substituted or unsubstituted 4 to 6-membered saturated heterocyclic group); and A represents N or CR.sup.5 (in which R.sup.5 represents hydrogen, or substituted or unsubstituted lower alkyl).
摘要:
The present invention relates to novel xanthine derivatives and pharmaceutically acceptable salts thereof, represented by Formula (I): ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen, lower alkyl, lower alkenyl, or lower alkynyl, R.sup.4 represents lower alkyl, or substituted or unsubstituted aryl, R.sup.5 and R.sup.6 independently represent hydrogen, lower alkyl, and lower alkoxy, or R.sup.5 and R.sup.6 are combined together to represent --O--(CH.sub.2)p--O-- (p is an integer of 1 to 3), n represents 0, 1, or 2, and m represents 1 or 2. The compounds of the present invention have an adenosine A.sub.2 receptor antagonistic activity, and are useful for the treatment or prevention of various kinds of diseases caused by hyperergasia of adenosine A.sub.2 receptors (for example, Parkinson's disease, senile dementia, depression, asthma, and osteoporosis).
摘要:
Methods for the treatment of Parkinson's disease comprising administering to a patient an agent which contains, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 is cycloalkyl, --(CH.sub.2).sub.n --R.sup.5, wherein R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4, or ##STR2## wherein Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z is substituted or unsubstituted aryl, ##STR3## wherein R.sup.6 is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m is an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 are independently O or S.
摘要:
The present invention relates to an antidepressant containing as an active ingredient a xanthine derivative or a pharmaceutically acceptable salt thereof, the xanthine derivative being represented by Formula (I) : ##STR1## in which R.sup.1, R.sup.2, and R.sup.3 represent independently hydrogen, lower alkyl, lower alkenyl;R.sup.4 represents cycloalkyl, --(CH.sub.2).sub.n --R.sup.5 (in which R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or ##STR2## (in which Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen or lower alkyl; and Z represents substituted or unsubstituted aryl, ##STR3## (in which R.sup.6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 3), or a substituted or unsubstituted heterocyclic group);and X.sup.1 and X.sup.2 represent independently O or S.
摘要:
The present invention relates to a therapeutic agent for Parkinson's disease containing as an active ingredient a polycyclic compound or a pharmaceutically acceptable salt thereof, the compound being represented by the following Formula (I): ##STR1## and A represents N or CR.sup.5 (in which R.sup.5 represents hydrogen, or substituted or unsubstituted lower alkyl), or represented by the following Formula (II): ##STR2## wherein Y, R.sup.6 and R.sup.8 are as defined herein and B and the adjacent two carbon atoms are combined to form a substituted or unsubstituted, partially saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic group.
摘要:
Disclosed are xanthine derivatives represented by the following Formula (I): ##STR1## in which R.sup.1, R.sup.2, and R.sup.3 independently represent hydrogen or lower alkyl; Q.sup.1, Q.sup.2, and Q.sup.3 independently represent hydrogen, lower alkyl, lower alkoxy, or halogen; and X represents --COR.sup.4 (in which R.sup.4 represents hydrogen, hydroxy, lower alkyl, or lower alkoxy) or --SO.sub.2 R.sub.5 {in which R.sup.5 represents hydroxy, lower alkoxy, trifluoromethyl, ##STR2## in which R.sup.6 and R.sup.7 independently represent hydrogen, hydroxy-substituted or unsubstituted lower alkyl, aryl, or ##STR3## (in which m represents an integer of 1 to 3; and R.sup.8 and R.sup.9 independently represent hydrogen or lower alkyl), or ##STR4## (in which Y represents a single bond, oxygen, or N--R.sup.10 in which R.sup.10 represents hydrogen or lower alkyl; and n1 and n2 independently represent an integer of 1 to 3)}, and pharmaceutically acceptable salts thereof.
摘要翻译:公开了由下式(I)表示的黄嘌呤衍生物:其中R 1,R 2和R 3独立地表示氢或低级烷基; Q1,Q2和Q3独立地表示氢,低级烷基,低级烷氧基或卤素; 或其中R 4表示氢,羟基,低级烷基或低级烷氧基)或-SO 2 R 5(其中R 5表示羟基,低级烷氧基,三氟甲基, 取代或未取代的低级烷基,芳基或者(其中m表示1〜3的整数; R 8和R 9分别表示氢或低级烷基),或者(其中Y表示单键,氧 ,或其中R 10表示氢或低级烷基的N-R 10,n1和n2独立地表示1〜3的整数)}及其药学上可接受的盐。
摘要:
Agents for the treatment of Parkinson's disease contain, as an active ingredient, a xanthine derivative or a pharmaceutically acceptable salt thereof. The xanthine derivative is represented by the formula: ##STR1## in which R.sup.1, R.sup.2 are R.sup.3 are independently hydrogen, lower alkyl, lower alkenyl, or lower alkynyl; and R.sup.4 represents cycloalkyl, --(CH.sub.2).sub.n --R.sup.5 (in which R.sup.5 represents substituted or unsubstituted aryl or a substituted or unsubstituted heterocyclic group; and n is an integer of 0 to 4), or ##STR2## in which Y.sup.1 and Y.sup.2 represent independently hydrogen, halogen, or lower alkyl; and Z represents substituted or unsubstituted aryl, ##STR3## in which R.sup.6 represents hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, nitro, or amino; and m represents an integer of 1 to 4, or a substituted or unsubstituted heterocyclic group; and X.sup.1 and X.sup.2 represent independently O or S.
摘要:
Compounds of the general formula ##STR1## wherein: X is halogen or trifluoromethyl;R.sub.1 is hydrogen, halogen or trifluoromethyl;R.sub.2 is hydrogen methyl or hydroxymethyl;R.sub.3 is hydrogen or lower alkyl; andY is methylene, methylene substituted with a lower alkyl or hydroxyl group, sulfinyl, sulfonyl, oxygen or sulfur, exhibit a cerebral protective effect and are applicable to the treatment of cerebral ischaemia and cerebral hypoxia.The compounds may be made by acylating a suitable piperidine or morpholine with the appropriate cinnamoyl chloride, and if necessary oxidizing the reaction product.
摘要:
Compounds of the general formula ##STR1## wherein: X is halogen or trifluoromethyl;R.sub.1 is hydrogen, halogen or trifluoromethyl;R.sub.2 is hydrogen, methyl or hydroxymethyl;R.sub.3 is hydrogen or lower alkyl; andY is methylene, methylene substituted with a lower alkyl or hydroxyl group, sulfinyl, sulfonyl, oxygen or sulfur, exhibit a cerebral protective effect and are applicable to the treatment of cerebral ischaemia and cerebral hypoxia.The compounds may be made by acylating a suitable piperidine or morpholine with the appropriate cinnamoyl chloride, and if necessary oxidizing the reaction product.
摘要:
A method and apparatus for driving a hollow pile into the ground. By using a hollow rod having a short auger fixedly secured to a leading end portion thereof, excavated earth and sand are lifted to and around the upper portion of the auger where compressed air is spouted from nozzle orifices formed in the hollow rod thereby lifting the excavated earth and sand through the hollow pile and consequently discharging the same from the hollow pile. As earth and sand are discharged from the hollow pile, the pile is sunk or driven into the ground.