摘要:
New pyrido[2,3-e]-as-triazine derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2 each stand for a C.sub.1-20 alkylcarbonyl, halogenated (C.sub.1-4 alkyl)-carbonyl, C.sub.1-4 alkoxycarbonyl, benzoyl, phenyl-(C.sub.1-4 alkyl)-carbonyl or phenyl-(C.sub.2-4 alkenyl)-carbonyl group or a 5-10-membered mono- or bicyclic nitrogen-containing heterocyclic acid residue (preferably a pyridylcarbonyl group) containing optionally one or more additional nitrogen, oxygen and/or sulfur atoms in the heterocyclic ring, and optionally one or more identical or different substituents selected from the group consisting of halogen, C.sub.1-4 alkoxy, nitro and hydroxy are attached to the aromatic or heterocyclic rings, furthermore one of R.sup.1 and R.sup.2 may also stand for hydrogen atom, orR.sup.1 and R.sup.2 may form, together with the adjacent nitrogen atoms, a pyrazole-2,4 ring having optionally a C.sub.1-6 alkyl substituent in position 3, andR.sup.3 stands for hydrogen, halogen, C.sub.1-4 alkoxy, amino, mono-(C.sub.1-6 alkyl)-amino, di-(C.sub.1-6 alkyl)-amino, hydroxy, alkylated or acylated hydroxy, morpholino, piperazino, N-(C.sub.1-6 alkyl)-piperazino, N-benzylpiperazino or N-pyridylpiperazino group,and pharmaceutically acceptable acid addition salts thereof are prepared by acylating the respective 1,2-unsubstituted 1,2-dihydro-pyrido[2,3-e]-as-triazine derivatives.The new compounds according to the invention act on the central nervous system and exert sedative, analgesic, narcosis potentiating, tetrabenazine antagonizing and antiphlogistic effects. The new compounds according to the invention can be applied to advantage in the therapy.
摘要:
Novel aminoisoquinoline derivatives of the general formula (I) ##STR1## wherein R.sub.1 represents a hydrogen atom or a C.sub.1-4 alkyl group,R.sub.2 represents a hydrogen atom,R.sub.3 represents a hydrogen atom,R.sub.4 represents a morpholinyl group or a piperazinyl group substituted with a pyridyl group, andpharmaceutically acceptable acid addition salts and quaternary derivatives thereof have been prepared. The novel compounds exert narcosis potentiating effects.
摘要:
The invention relates to new pyrido[3,2-e]-as-triazine derivatives of the formula I and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 stands for a C.sub.1-20 alkyl-carbonyl group, halogen-C.sub.1-4 alkyl-carbonyl, benzoyl, phenyl-C.sub.1-4 alkyl-carbonyl, or pyridyl-carbonyl group;R.sub.2 is a hydrogen atom or a C.sub.1-4 alkyl-carbonyl group; or R.sub.1 and R.sub.2 form together with the adjacent nitrogen atoms a pyrazole-2,4-dione ring which carries a C.sub.1-6 alkyl substituent in position 3;R.sub.3 is a hydrogen atom, a C.sub.1-20 alkyl, phenyl, phenyl-C.sub.1-3 alkyl, furyl or pyridyl group or a phenyl group optionally substituted by one to three C.sub.1-4 alkoxy-groups.The compounds of the formula I are prepared by acylating the respective 1,2-un-substituted 1,2-dihydropyrido [3,2-e]-as-triazine derivatives. The new compounds exert valuable effects on the central nervous system and possess analgesic, antiphlogistic effects, and can be applied to advantage in therapy.
摘要:
The invention relates to new benzo-as-triazine derivatives of the formulae (I) and (Ia) and pharmaceutically acceptable acid addition salts thereof, ##STR1## wherein R.sub.1 and R.sub.2 each represent hydrogen, a C.sub.1-20 alkylcarbonyl group, a phenylcarbonyl or phenyl-(C.sub.1-4 alkyl)-carbonyl group having optionally one or more halogen, hydroxy or C.sub.1-3 alkoxy substituents which may be the same or different, furthermore a pyridylcarbonyl, a pyrazinylcarbonyl, a furylcarbonyl, a chloroacetyl or a C.sub.1-4 alkoxycarbonyl group, orR.sub.1 and R.sub.2 may form, together with the adjacent nitrogen atoms, a pyrazole ring having optionally a C.sub.1-6 alkyl substituent in position 4,with the proviso that one of R.sub.1 and R.sub.2 is always different from hydrogen,R.sub.3 stands for hydrogen, mercapto group, a C.sub.1-4 alkylmercapto group, amino group, a C.sub.1-4 alkylamino group, a piperazino group having optionally an N-alkyl or 2-pyridyl substituent, a morpholino group or a piperidino group, andR.sub.4 stands for hydrogen, halogen, C.sub.1-4 alkyl or C.sub.1-4 alkoxy group.The compounds of the formulae (I) and (Ia) are prepared by acylating the respective 2,4,5-unsubstituted 4,5-dihydro-benzo-as-triazine derivatives.The new compounds of the formulae (I) and (Ia) possess analgesic, antiphlogistic and narcosis-potentiating effects.
摘要:
The invention relates to novel oxime ethers of the general formula /I/ and acid addition salts and quaternary ammonium derivatives thereof, ##STR1## wherein A represents a C.sub.2-6 straight or branched alkylene chain,R and R.sup.1 each represent a C.sub.1-6 alkyl group or they form together with the adjacent nitrogen atom a heterocyclic ring containing 4 to 7 carbon atoms and optionally a further hetero atom, i.e. an oxygen, sulfur or nitrogen atom, and said ring may be optionally substituted by a C.sub.1-3 alkyl, phenyl or benzyl group,R.sup.2 and R.sup.3 each denote a hydrogen atom or together form a valency bond,R.sup.4 denotes a C.sub.1-10 alkyl or C.sub.2-10 alkenyl group, andn denotes an integer from 3 to 7.The compounds of the general formula /I/ are prepared according to the invention by reacting a cycloalkane derivative of the general formula /II/ ##STR2## wherein R.sup.2, R.sup.3, R.sup.4 and n have the same meaning as above, whereasY denotes an oxygen or sulphur atom or a .dbd.N--OH group with an aminoalkyl derivative of the general formula /III/ ##STR3## wherein R, R.sup.1 and A have the same meaning as stated above andZ means a halogen atom or a H.sub.2 N--O-- group or a salt thereof in the presence of a basic condensing agent.The new compounds of the general formula /I/ possess valuable nicotine-lethality inhibiting, local anaesthetic, analgesic effects, which are, in case of certain compounds, complemented by anti-hypertensive, maximum electroshock and tetracorspasm inhibiting, ulcus inhibiting and motility inhibiting effects, and can be applied to advantage in the therapy.
摘要翻译:本发明涉及通式I I的新型肟醚及其酸加成盐和季铵衍生物,其中A表示C2-6直链或支链亚烷基链,R和R1各自表示C1 -6烷基,或者它们与相邻的氮原子一起与含有4至7个碳原子的杂环和任选的另外的杂原子(即氧,硫或氮原子)一起形成,并且所述环可以任选地被C 1-3 烷基,苯基或苄基,R2和R3各自表示氢原子或一起形成价键,R4表示C1-10烷基或C2-10烯基,n表示3至7的整数。 根据本发明通过使通式/ II / IMAGE / II /的环烷烃衍生物与其中R2,R3,R4和n具有与上述相同的含义反应制备通式/ I / I,而Y表示氧或 硫原子或a =具有氨基烷基衍生物的N-OH基团 通式/ III / / III /其中R,R 1和A具有与上述相同的含义,Z表示在碱性缩合剂存在下的卤素原子或H 2 N-O-基或其盐。 新型化合物/ I /具有有价值的尼古丁杀伤力抑制,局部麻醉,止痛作用,在某些化合物的情况下,补充有抗高血压,最大电休克和四疣抑制作用,抑制溃疡和运动抑制作用 ,并且可以在治疗中有利地应用。
摘要:
New compounds are disclosed of the formulae ##STR1## or pharmaceutically effective salts thereof, wherein R is hydrogen, C.sub.1-12 alkyl, or R is phenyl or phenyl-C.sub.1 to C.sub.4 alkyl wherein the phenyl can be substituted with 1 to 3 halogen, C.sub.1 to C.sub.4 alkyl, or C.sub.1 to C.sub.4 alkoxy substituents; andX.sub.1, X.sub.2 and X.sub.3 are hydrogen, C.sub.1 to C.sub.6 alkanoyl, or C.sub.1 to C.sub.6 haloalkanoyl; and where X.sub.1 is hydrogen, X.sub.2 and X.sub.3 are not simultaneously hydrogen. The compounds possess antiphlogistic, analgesic, anticonvulsive, or tranquilizing properties.
摘要:
The invention relates to novel pyrazolo[1,5-c]quinazoline derivatives of the general formula I ##STR1## wherein R represents a hydrogen atom, a C.sub.1-4 alkyl group or an acyl group,R.sub.1 represents a hydrogen atom, a C.sub.1-12 alkyl group, a C.sub.3-8 cycloalkyl group, a C.sub.2-4 alkenyl group, an aralkyl group, wherein the alkyl group has 1 to 4 carbon atoms, a phenylalkenyl group, wherein the alkenyl group has 2 to 4 carbon atoms, furthermore a carboxy group or a phenyl group optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C.sub.1-4 alkoxy, nitro or di(C.sub.1-4 alkyl)amino groups, orR and R.sub.1 may form together a valence bond,R.sub.2 represents a hydrogen atom, a C.sub.1-4 alkyl or a phenyl group, orR.sub.1 and R.sub.2 may form together a C.sub.2-7 alkylene group,R.sub.3 represents a nitro group, an amino group, an alkylamino group, a dialkylamino group, wherein the alkyl groups have 1 to 4 carbon atoms, an alkylideneimino group, wherein the alkylidene group has 1 to 4 carbon atoms, a benzylideneimino group or an acylamino group,and pharmaceutically acceptable acid addition salts thereof.The novel compounds of the general formula I can be employed primarily as analgesic agents.
摘要:
Apparatus and method for modeling of thrombogenesis using haemostasis measuring devices. A sleeve member is provided on a blood-carrying tube to simulate an environment of a human artery. When punctured with a small needle, bleeding is simulated, permitting blood to be trapped between the sleeve and blood-carrying tube. The trapped blood communicates with the blood flowing in the tube, resulting in thrombus formation.