摘要:
Compounds of Formula I with activity against HIV, including pharmaceutical compositions and methods for using these compounds in treating human immunodeficiency virus (HIV) infection, are set forth:
摘要:
The invention relates to compounds of the formula (I) ##STR1## in which R=(subst.) alkyl or (subst.) cycloalkyl, which are suitable as intermediates for preparing herbicidal sulfonylureas. According to the invention, the compounds (I) are prepared by(a) diazotizing a compound of the formula (II) ##STR2## in the presence of an acid H.sup.+ X.sup.-, where X.sup.- is an equivalent of an anion, to give the novel compounds (diazonium salts) of the formula (III) ##STR3## (b) reacting the compound of the formula (III) in the presence of iodide ions to give the compound (IV) and ##STR4## (c) reacting the compound of the formula (IV) with an isocyanate of the formula (V)R--N.dbd.C.dbd.O (V)in which R is as defined in formula (I), to give the compound of the formula (I).
摘要:
Substituted benzenesulfonylureas and -thioureas--processes for their preparation and their use as pharmaceuticals Benzenesulfonylureas and -thioureas of the formula I ##STR1## where R(1) is H or (fluoro)methyl, R(2) is H, Hal or (fluoro)(mercapto)alk(oxy)yl, E is O or S; Y is --�CR(3).sub.2 !.sub.n --, where R(3)=H or alkyl and n=1-4, X is H, Hal or alkyl and Z is Hal, NO.sub.2 or alk(yl)oxy, are described. The compounds I are used for treatment of disturbances in cardiac rhythm and prevention of sudden cardiac death caused by arrhythmia, and can therefore be used as antiarrhythmics. They are particularly suitable for those cases where arrhythmias are a consequence of a narrowing of a coronary vessel, such as angina pectoris or acute cardiac infarction.
摘要:
Fluorinated alkene compounds useful for and methods of controlling nematodes, insects, and acarids that prey on agricultural crops. Polar compounds, for example, 3,4,4-trifluoro-3-butene-l-amine or 3,4,4-trifluoro-3-butenoic acid, are particularly useful for systemic control of pests. Novel method and intermediates for the preparation of 3,4,4-trifluoro-3-butene-1-amine are also provided.
摘要:
There are described amino-substituted benzenesulfonylureas and -thioureas of the formula I ##STR1## The compounds I are used for the treatment of cardiac arrhythmias and for the prevention of sudden heart death caused by arrhythmias and can therefore be used as antiarrhythmics. They are particularly suitable for those cases in which arrhythmias are a result of constriction of a coronary vessel, such as in angina pectoris or in acute cardiac infarct.
摘要:
The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
摘要:
The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylures of the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, nitro, amino, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 haloalkyl or a --Q--R.sub.7, --CO--OR.sub.8 or --(CO).sub.n --NR.sub.9 R.sub.10 radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, halogen or alkoxyalkyl containing not more than 4 carbon atoms,R.sub.3 is C.sub.2 -C.sub.10 alkenyl which is substituted by one or more fluorine or bromine atoms or by one or more hydroxyl, cyano, nitro, --(Y).sub.m --CO--(Z).sub.n --R.sub.8, --SO.sub.2 --NR.sub.11 R.sub.12, --S(O).sub.P --C.sub.1 -C.sub.3 haloalkyl or --S(O).sub.n --C.sub.1 -C.sub.3 alkyl groups and which may additionally be substituted by one or more chlorine atoms,R.sub.4 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 haloalkoxy,R.sub.5 is hydrogen, halogen, --NR.sub.13 R.sub.14, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.2 haloalkoxy,R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy,X is oxygen or sulfur, andE is nitrogen or the methine group, and R.sub.7 is C.sub.1 -C.sub.4 alkyl which is substituted by halogen or C.sub.1 -C.sub.3 alkoxy or is C.sub.3 -C.sub.5 alkenyl,R.sub.8 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or C.sub.2 -C.sub.6 alkoxyalkyl, R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14, each independently of the other, are hydrogen or C.sub.1 -C.sub.3 alkyl,Q is oxygen, sulfur, the sulfinyl or sulfonyl bridge,Y is oxygen, sulfur or --NR.sub.16 --, wherein R.sub.16 is hydrogen or C.sub.1 -C.sub.3 alkyl,Z is oxygen, sulfur or --NR.sub.17 --, wherein R.sub.17 is hydrogen or C.sub.1 -C.sub.3 alkyl, m and n are each 0 or 1, andp is 0, 1 or 2, and to the salts of these compounds with amines, alkali metal bases or alkaline earth metal bases.These compounds have good pre- and postemergence selective herbicidal and growth regulating properties.
摘要:
The invention relates to N-phenylsulfonyl-N'-pyrimidinylureas and N-phenylsulfonyl-N-triazinylureas of the general formula ##STR1## wherein R.sub.1 is hydrogen, halogen, nitro, amino, C.sub.1 -C.sub.5 alkyl, C.sub.1 -C.sub.4 haloalkyl or a --Q--R.sub.7, --CO--OR.sub.8 or --(CO).sub.n --NR.sub.9 R.sub.10 radical,R.sub.2 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 haloalkoxy, halogen or alkoxyalkyl containing not more than 4 carbon atoms,R.sub.3 is C.sub.2 -C.sub.10 alkenyl which is substituted by one or more fluorine or bromine atoms or by one or more hydroxyl, cyano, nitro, --(Y).sub.m --CO--(Z).sub.n --R.sub.8, --SO.sub.2 --NR.sub.11 R.sub.12, --S(O).sub.p --C.sub.1 -C.sub.3 haloalkyl or --S(O).sub.n --C.sub.1 -C.sub.3 alkyl groups and which may additionally be substituted by one or more chlorine atoms,R.sub.4 is C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 haloalkoxy,R.sub.5 is hydrogen, halogen, --NR.sub.13 R.sub.14, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.2 haloalkoxy,R.sub.6 is hydrogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy,X is oxygen or sulfur, andE is nitrogen or the methine group, andR.sub.7 is C.sub.1 -C.sub.4 alkyl which is substituted by halogen or C.sub.1 -C.sub.3 alkoxy or is C.sub.3 -C.sub.5 alkenyl,R.sub.8 is C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl or C.sub.2 -C.sub.6 alkoxyalkyl,R.sub.9, R.sub.10, R.sub.11, R.sub.12, R.sub.13 and R.sub.14, each independently of the other, are hydrogen or C.sub.1 -C.sub.3 alkyl,Q is oxygen, sulfur, the sulfinyl or sulfonyl bridge,Y is oxygen, sulfur or --NR.sub.16 --, wherein R.sub.16 is hydrogen or C.sub.1 -C.sub.3 alkyl,Z is oxygen, sulfur or --NR.sub.17 --, wherein R.sub.17 is hydrogen or C.sub.1 -C.sub.3 alkyl,m and n are each 0 or 1, andp is 0, 1 or 2, and to the salts of these compounds with amines, alkali metal bases or alkaline earth metal bases.These compounds have good pre- and postemergence selective herbicidal and growth regulating properties.
WHICH IN THE FREE FROM OR IN THE FORM OF THEIR SALTS HAVE BLOOD SUGAR LOWERING PROPERTIES AND ARE DISTINGUISHED BY A STRONG AND LONG-LASTING HYPOGLYCEMIC ACTION. IN THE FORMULA X REPRESENTS (R-O-),Z-PHENYL OR 3-(R-O-),5-Z''-THIEN-2-YL WHEREIN R STANDS FOR AN ALKYL GROUP HAVING 1 TO 4 CARBON ATOMS, Z STANDS FOR A HALOGEN ATOM, AN ALKYL OR ALKOXY GROUP BOTH HAVING 1 TO 4 CARBON ATOMS, AND Z'' STANDS FOR A HALOGEN ATOM OR AN ALKYL GROUP HAVING 1 TO 4 CARBON ATOMS.