摘要:
Tertiary hydroxyalkylxanthines having the general formula (I), characterized by the fact that at least one of the residues R.sup.1 and R.sup.3 represents a tertiary hydroxyalkyl group of formula (Ia) in which R.sup.4 represents an alkyl group having up to 3 carbon atoms and n a whole number from 2 to 5; the other residue which may remain R.sup.1 or R.sup.3 is a hydrogen atom or an aliphatic hydrocarbon residue R.sup.5 having up to 6 carbon atoms, in which the carbon chain may be separated by a maximum of two oxygen atoms or be substituted by an oxo group or two hydroxy groups at the most, and R.sup.2 represents an alkyl group with 1 to 4 carbon atoms. Also described is a process for manufacturing these compounds, which are suitable for the manufacture of medicines, in particular for use in the prevention and/or treatment of peripheral and/or cerebral irrigation disorders. ##STR1##
摘要:
Novel substituted 3-phenyl-7H-thiazolo[3,2-b][1,2,4]-triazin-7-ones of the formula I are disclosed ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 have the meaning recited in the specification. The compounds are suitable for prevention and treatment of inflammatory disorders.
摘要:
Compounds of general formula ##STR1## wherein R.sup.1 represents a member selected from the group consisting of (a) an unsubstituted at most binuclear aryl group having from 6 to 10 carbon atoms, such groups substituted by from 1 to 3 equal or different radicals selected from the group consisting of alkyl, halogenoalkyl, alkoxy, dialkylamino each having up to 4 carbon atoms in the alkyl moiety, halogen phenyl, carboxyl, cyano, nitro and hydroxy groups,(b) a 5- to 6-membered heteroaromatic ring wherein the heteroatom is selected from nitrogen, oxygen and sulfur atoms and such rings anellated to a benzene nucleus;R.sup.2 represents a member selected from the group consisting of hydrogen, alkyl having up to 3 carbon atoms, phenyl, cycloalkyl having up to 6 carbon atoms in the ring and cycloalkyl bearing a hydrocarbon bridging radical having up to 2 carbon atoms;R.sup.3 represents hydrogen, hydroxy or acyloxy;R.sup.4 and R.sup.5 are the same or different and each represents a member selected from the group consisting of halogen, alkyl, and halogenoalkyl each having up to 3 carbon atoms, and nitro; andX represents nitrogen or methineand physiologically acceptable acid addition salts thereof and a pharmaceutical composition containing said compounds.
摘要翻译:通式(I)的化合物,其中R 1表示选自(a)至少有6至10个碳原子的双核芳基的基团,这些基团被1至3个相等或不同取代的基团 选自烷基部分中具有至多4个碳原子的烷基,卤代烷基,烷氧基,二烷基氨基的基团,卤素苯基,羧基,氰基,硝基和羟基,(b)5-至6-元杂芳环 其中所述杂原子选自氮,氧和硫原子,并且这样的环被安置在苯核上; R2表示选自氢,最多3个碳原子的烷基,苯基,环中具有至多6个碳原子的环烷基和含有至多2个碳原子的烃桥基的环烷基的成员; R3表示氢,羟基或酰氧基; R 4和R 5相同或不同,各自表示选自具有至多3个碳原子的卤素,烷基和卤代烷基的基团,和硝基; X表示氮或次甲基及其生理上可接受的酸加成盐,以及含有所述化合物的药物组合物。
摘要:
Novel 5-(3-alkyl-5-tert.butyl-4-hydroxyphenyl)-2-amino-6H-1,3,4-thiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkylR.sup.3 and R.sup.4 =independently of one another, optionally substituted and optionally O- or S-interrupted alkyl, alkenyl or alkynyl groups, it being possible for one of the two radicals to also be H,or R.sup.3 +R.sup.4 together with the nitrogen atom to which they are bound, may denote an optionally substituted 4- to 7-membered ring which optionally contains a further heteroatom (O, S or N),and the physiologically acceptable acid-addition salts thereof. The compounds are primarily suitable for prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders and/or pain.
摘要:
Use of xanthine derivatives for the treatment of nerve damage following an interruption in blood circulation.The invention relates to the use of xanthine derivatives of the formula I ##STR1## in which R.sup.2 is a (C.sub.1 -C.sub.4)-alkyl group and at least one of the symbols R.sup.1 and R.sup.3 is a radical of the formula II or III ##STR2## in which A is CHOH, CO or dioxolane, R.sup.4 is a hydrogen atom or a (C.sub.1 -C.sub.4)-alkyl group and n is 0 to 5, and in which R.sup.5 and R.sup.6 are hydrogen atoms or (C.sub.1 -C.sub.4)-alkyl groups or, together with the nitrogen atom to which they are bonded, form a 5- to 7-membered ring, it being possible for one carbon atom to be replaced by an oxygen or nitrogen atom, m is 1 or 2 and the other radical R.sup.1 or R.sup.3, if appropriate, is a hydrogen atom, a (C.sub.1 -C.sub.6)-alkyl group or a (C.sub.3 -C.sub.6)-alkenyl group, for the preparation of medicaments for the prophylaxis and treatment of nerve damage following an interruption in blood circulation, and novel xanthine derivatives, and to processes for their preparation.
摘要:
Novel imidazo- and triazolothiadiazines of the general formula I ##STR1## in which R.sup.1 =C.sub.1 -C.sub.4 -alkyl,R.sup.2 =H or C.sub.1 -C.sub.3 -alkyland the structural element --A--B--=--CH.sub.2 --CH.sub.2 --, --CH CH--, --CH.dbd.N--, --CH.sub.2 --CO-- or --CO--CH.sub.2 --,and the physiologically aceptable acid-addition salts thereof, are prepared by reacting 2-halo-1-phenylalkanones of the formula II ##STR2## (meaning of R.sup.1 and R.sup.2 as in formula I, X=halogen) with compounds of the formula III ##STR3## (meaning of --A--B-- as in formula I) and, if appropriate, converting the compounds of the formula I formed into the physiologically acceptable acid-addition salts thereof by means of suitable acids.The compounds of the formula I and the physiologically acceptable acid-addition salts thereof are principally suitable for the prevention and treatment of inflammatory--in particular inflammatory rheumatic--disorders.Some of the intermediates formed during the preparation of the compounds of the formula I are also novel, namely 1-amino-2-mercaptoimidazole ##STR4## and 1-amino-2-thioxo-5-imidazolidinone ##STR5##
摘要:
A compound of general formula ##STR1## wherein X represents a radical selected from the group consisting of one of the formulae ##STR2## in which R.sup.1 represents a radical selected from the group(a) a hydrogen atom,(b) an amino group, when X represents an --OR.sup.1 moiety,(c) an alkyl group having from 1 to 6 carbon atoms(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents of the group halogen atoms, alkyl, alkoxy, halogenalkyl groups each having up to 4 carbon atoms, cycloalkyl groups having 3 to 6 carbon atoms, nitro and cyano groups; andR.sup.2 and R.sup.3, which may be the same or different, each represents a radical selected from the group(a) a hydrogen atom,(b) an alkyl group having from 1 to 6 carbon atoms, an unsubstituted cycloalkyl group having from 3 to 7 carbon atoms, such cycloalkyl group substituted by at most 3 substituents of the group hydroxy groups and alkoxycarbonyl groups having 1 to 4 carbon atoms,(c) an aralkyl group, a diaralkyl group each having 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted in at least one of the radicals in the alkyl moiety by hydroxy groups, and in the aryl moieties by at most 3 substituents selected from the group consisting of alkoxy groups having from 1 to 4 carbon atoms and halogen atoms,(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents selected from the group consisting of alkyl, alkoxy, halogenoalkyl groups each having up to 4 carbon atoms and halogen atoms,(e) a hydroxy group when the other of R.sup.2 and R.sup.3 is hydrogen,(f) R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, represent a 5- to 7-membered ring selected from the group consisting of an unsubstituted ring, a ring being substituted by an alkyl group having from 1 to 4 carbon atoms, and a ring being interrupted by a heteroatom selected from the group consisting of oxygen, sulphur and further nitrogen atom, and(g) R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached, represent a ring from the group a 5-membered heteroaromatic ring containing up to 4 nitrogen atoms and such a ring being anelled to a benzene- or uracil-ring, and physiologically acceptable acid addition salts thereof, a process for their preparation and a pharmaceutical composition containing them.
摘要:
Compounds of general formula ##STR1## wherein R.sup.1 represents a radical selected from the group consisting of an alkyl group having from 1 to 6 carbon atoms, an unsubstituted aryl group having 6 carbon atoms, an aryl group having 6 carbon atoms being substituted by at least one radical selected from the group consisting of a chlorine atom, alkyl and alkoxy each having up to 2 carbon atoms; and R.sup.2 represents an alkyl group having from 1 to 6 carbon atoms.
摘要:
Pharmaceutical preparations having hypolipidemic activity, which contain in addition to a pharmaceutically acceptable carrier an effective amount of an imidazolyl-(2)-carbinol of the general formula I ##STR1## in which R represents hydrogen, lower alkyl, phenyl or benzyl, R.sub.1 and R.sub.2 each represent hydrogen or together the group --CH.dbd.CH--CH.dbd.CH--, R.sub.3 and R.sub.4 represent hydrogen, lower alkyl, phenyl, lower haloalkyl, lower alkylphenyl, lower alkoxyphenyl, lower haloalkoxyphenyl, mono- or dihalophenyl, imidazolyl or benzylimidazolyl or R.sub.3 and R.sub.4 are together fluoryl of the formula ##STR2## or of a physiologically tolerable acid addition salt thereof, and process for preparing them.
摘要:
A compound of one of formulae (I) and (II) (of formula sheet) whereinR.sup.1 represents a radical selected from the group consisting of hydrogen alkyl containing up to 6 carbon atoms and being unsubstituted or substituted by at least one of the groups alkoxy and phenylalkoxy containing up to 4 carbon atoms in the alkoxy moiety; aryl or aralkyl each containing from 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy and haloalkyl containing up to 4 carbon atoms, halogen and nitro; a 5- or 6-membered heteroaromatic ring containing up to 2 hetero atoms chosen from O,N and S, at most one of which is different from nitrogen; an alkyl group containing from 1 to 4 carbon atoms substituted by such a heteroaromatic ring;R.sup.2 and R.sup.3, which are the same or different, each represents a hydrogen atom or, alkyl containing up to 4 carbon atoms and being unsubstituted or substituted by at least one substituent selected from the group consisting of alkyl, alkoxy and haloalkyl containing up to 4 carbon atoms, halogen and nitro; taken together R.sup.2 and R.sup.3 alternatively represent a --CH.dbd.CH--CH.dbd.CH-- group which is unsubstituted or substituted by a substituent selected from the group consisting of alkyl, alkoxy and haloalkyl, each containing up to 4 carbon atoms, halogen and nitro;R.sup.4 is selected from the group consisting of hydrogen alkyl, aryl and aralkyl containing up to 4 carbon atoms in each alkyl moiety; andA represents a single bond or alkylene containing from 1 to 6 carbon atoms; with the proviso that R.sup.1 is other than a hydrogen atom or methyl group when A represents a single bond and R.sup.2 and R.sup.3 taken together represent an unsubstituted --CH.dbd.CH--CH.dbd.CH-- group; physiologically acceptable salts thereof, a synthesis therefor and a pharmaceutical composition containing it.