摘要:
Novel 5-(substituted phenyl)-oxazolidinones and their sulfur analogs of Formula I ##STR1## wherein R.sub.1 is optionally substituted lower alkyl, cycloalkyl or cycloalkylalkyl;R.sub.2 is hydrogen, optionally substituted lower alkyl, cycloalkyl, cycloalkylalkyl, optionally substituted aryl, optionally substituted aralkyl, alkenyl or a heterocyclic group;R.sub.3 is hydrogen, optionally substituted lower alkyl, alkenyl, alkynyl, optionally substituted aryl, optionally substituted aralkyl, or optionally substituted acyl;R.sub.4 is hydrogen or optionally substituted lower alkyl;R.sub.5 is hydrogen or optionally substituted lower alkyl or optionally substituted lower alkoxycarbonyl; andX is oxygen or sulfur, have valuable pharmacological effects.
摘要翻译:式(I)的新型5-(取代苯基)恶唑烷酮及其硫类似物,其中R 1为任选取代的低级烷基,环烷基或环烷基烷基; R 2是氢,任选取代的低级烷基,环烷基,环烷基烷基,任选取代的芳基,任选取代的芳烷基,烯基或杂环基; R 3是氢,任选取代的低级烷基,烯基,炔基,任选取代的芳基,任选取代的芳烷基或任选取代的酰基; R4是氢或任选取代的低级烷基; R5是氢或任选取代的低级烷基或任选取代的低级烷氧基羰基; X为氧或硫,具有宝贵的药理作用。
摘要:
4-(Polyalkoxyphenyl)-2-pyrrolidones of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrocarbon; R.sub.3 is hydrogen or methoxy;R is O-alkyl, O-aryl, O-aralkyl, NH.sub.2, NH-alkyl, NH-aryl, NH-aralkyl, N(alkyl).sub.2, N(aryl).sub.2 or ##STR2## AND X is O or S, are neuropsychotropic agents.
摘要:
3-Substituted beta-carbolines of the formula ##STR1## wherein R.sup.A is H, F, Cl, Br, I, NO.sub.2, CN, CH.sub.3, CF.sub.3, SCH.sub.3, NR.sup.16 R.sup.17 or NHCOR.sup.16,wherein R.sup.16 and R.sup.17 are the same or different and each is hydrogen or alkyl, alkenyl or alkynyl each of up to 6 C-atoms, aralkyl or cycloalkyl each of up to 10 C-atoms,or wherein R.sup.16 and R.sup.17 together form a saturated or unsaturated 3-7 membered heterocyclic ring;said compounds possess valuable psychotropic properties which make them useful for example as tranquilizers.
摘要:
3-substituted beta-carbolines of the formula ##STR1## wherein R.sup.C is hydrogen, lower alkyl, alkoxyalkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms, aralkyl of up to 8 C-atoms, or (CH.sub.2).sub.n OR.sup.20wherein R.sup.20 is alkyl of up to 6 C-atoms, cycloalkyl of 3-6 C-atoms or aralkyl of up to 8 C-atoms and n is an integer of 1 to 3;Y is oxygen, two hydrogen atoms or NOR.sup.1,wherein R.sup.1 is hydrogen, lower alkyl, aryl or aralkyl of up to 6 C-atoms, COR.sup.2, wherein R.sup.2 is lower alkyl of up to 6 C-atoms,or Y is CHCOOR.sup.3, wherein R.sup.3 is hydrogen or lower alkylor Y is NNR.sup.4 R.sup.5,wherein R.sup.4 and R.sup.5 can be the same or different and each is hydrogen, lower alkyl, C.sub.6-10 -aryl, C.sub.7-10 -aralkyl or CONR.sup.6 R.sup.7,wherein R.sup.6 and R.sup.7 can be the same or different and each is hydrogen or lower alkyl or R.sup.4 and R.sup.5 together with the connecting N-atom, for a 5- or 6-membered heterocyclic ring which optionally may also contain an O-atom or up to 3 N-atoms and which optionally may be substituted by a lower alkyl group;Z is hydrogen, or alkoxy or aralkoxy each of up to 10 C-atoms and each optionally substituted by hydroxy, or Z is alkyl of up to 6 C-atoms, C.sub.6-10 -aryl or C.sub.7-10 -aralkyl each of which may optionally be substituted by a COOR.sup.8 -- or a CONR.sup.9 R.sup.10 group,wherein R.sup.8 is alkyl of up to 6 C-atoms, and R.sup.9 and R.sup.10 can be the same or different and each is hydrogen or alkyl of up to 6 C-atoms;or Z is NR.sup.9 R.sup.10, wherein R.sup.9 and R.sup.10 are as defined above;or Z is NR.sup.11 CHR.sup.12 R.sup.13,wherein R.sup.11 and R.sup.12 each is hydrogen or together form a N.dbd.C double bond,wherein R.sup.13 is C.sub.1-10 -alkyl or NR.sup.14 R.sup.15,wherein R.sup.14 and R.sup.15 are the same or different and each is hydrogen, OH or alkyl or alkoxy each of up to 6 C-atoms,or wherein R.sup.12 and R.sup.13 together are oxygen, in which case, R.sup.11 is hydrogen;or Z is COOR.sup.2 wherein R.sup.2 is as defined above;or Y and Z, together with the connecting C-atom, may form a 5- or 6-membered heterocyclic ring which contains an O-atom, adjoining O- and N-atoms or up to 4 N atoms and which optionally may be substituted by a lower alkyl group, hydroxy or oxo have valuable psychotropic properties which make them useful for example as tranquilizers.
摘要:
Compounds of general Formula I are disclosed ##STR1## wherein R.sup.1 is C.sub.1-4 -alkyl,R.sup.3 is hydrogen, C.sub.1-4 -alkyl, acyl, aryl,R.sup.5 is hydrogen, C.sub.1-4 -alkyl,X is oxygen, CH.sub.2 or NR.sup.4 with R.sup.4 =hydrogen, C.sub.1-4 -alkyl andY is an aromatic or nonaromatic ring system which can optionally contain one to two hetero atoms and can be substituted, and the stereoisomers and their mixtures,as well as their preparation and use as medicinal agents.
摘要:
5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, andR.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.
摘要:
Substituted 5H-pyrimido[5,4-b]indoles of Formula I ##STR1## wherein R.sup.2 is halogen; the oxadiazolyl group ##STR2## wherein R" is lower alkyl with up to 3 carbon atoms; C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, or ##STR3## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR4## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, C.sub.3-5 -alkenyl, cycloalkyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; andR.sup.A is hydrogen; the oxadiazolyl group ##STR5## wherein R" is lower alkyl with up to 3 carbon atoms; halogen, nitro, OR.sup.I, SO.sub.n R.sup.I with n being 0, 1, or 2, ##STR6## wherein R.sup.I is hydrogen, C.sub.1-5 -alkyl, cycloalkyl, aralkyl, or aryl; ##STR7## wherein R.sup.II and R.sup.III are hydrogen, C.sub.1-5 -alkyl, cycloalkyl, C.sub.3-5 -alkenyl, aralkyl, aryl, or, with the connecting N-atom, a 5- or 6-membered heterocyclic ring; orPO(OR).sub.2 wherein R is C.sub.1-5 -alkyl, exhibit strong affinity for binding to benzodiazepine receptors.The novel compounds are suitable for use in psychopharmaceutical preparations.
摘要:
Imidazole derivatives of general formula I ##STR1## wherein R.sup.1 represents hydrogen or halogen in the o-, m- or p-position, and the halogen can occur once or repeatedly in the phenyl radical,R.sup.4 represents ##STR2## with R.sup.6 and R.sup.9 representing hydrogen or a straight or branched alkyl group with 1 to 6 carbon atoms, R.sup.7 and R.sup.8 are the same or different and represent hydrogen or a straight or branched alkyl group with 1 to 6 carbon atoms or R.sup.7 and R.sup.8 together with the nitrogen atom represent a saturated heterocyclic five-membered or six-membered ring optionally containing another heteroatom, andR.sup.5 represents hydrogen, an alkyl group with 1 to 6 carbon atoms or an alkoxyalkyl group with 1 to 6 carbon atoms, which are suitable as psychopharmaceuticals, are described.
摘要:
5- or 6-substituted .beta.-carboline-3-carboxylic acid esters of Formula I ##STR1## wherein R.sup.1 is hydrogen, nitrilo, halogen, lower alkyl or lower alkoxy, and R.sup.3 is a branched C.sub.3-6 alkyl group which is optionally substituted by halogen, or a C.sub.3-6 cycloalkyl group which is optionally methyl-substituted, are valuable pharmaceuticals.
摘要:
Compounds of formula I ##STR1## in which R.sup.A, B (which is CR.sup.4) and R.sup.3 and have the meaning indicated in the application, as well as their production and their use in pharmaceutical agents, are described.