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    • 2. 发明授权
    • Oxime ethers and pharmaceutical compositions containing the same
    • 肟醚和含有它的药物组合物
    • US4395413A
    • 1983-07-26
    • US162674
    • 1980-06-24
    • Zoltan BudaiAranka Lay nee KonyaTibor MezeiLujza PetoczKatalin GrasserIbolya KosoczkyEniko Szirt nee KiszellyPeter Gorog
    • Zoltan BudaiAranka Lay nee KonyaTibor MezeiLujza PetoczKatalin GrasserIbolya KosoczkyEniko Szirt nee KiszellyPeter Gorog
    • A61K31/15A61K31/495A61P25/04C07C67/00C07C239/00C07C249/10C07C251/58C07D295/02C07D295/088C07D295/08
    • C07D295/088Y10S514/926Y10S514/927
    • 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.
    • 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。
    • 5. 发明授权
    • Pyrido[2,3-e]-as-triazine derivatives and pharmaceutical compositions
    • 吡啶并[2,3-e] -as-三嗪衍生物和药物组合物
    • US4324786A
    • 1982-04-13
    • US143778
    • 1980-04-25
    • Andras MessmerPal BenkoGyorgy HajosLujza PetoczIbolya KosoczkyPeter Gorog
    • Andras MessmerPal BenkoGyorgy HajosLujza PetoczIbolya KosoczkyPeter Gorog
    • A61K31/53A61K31/535A61P25/00A61P25/04A61P25/20A61P29/00C07D221/04C07D253/10C07D471/04C07D471/14
    • C07D471/04
    • 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.
    • 通式(I)的新的吡啶并[2,3-e] -as-三嗪衍生物,其中R 1和R 2各自代表C 1-20烷基羰基,卤代(C 1-4烷基) - 羰基 ,C 1-4烷氧基羰基,苯甲酰基,苯基 - (C 1-4烷基) - 羰基或苯基 - (C 2-4烯基) - 羰基或5-10元单环或双环含氮杂环酸残基(优选 含有任选的一个或多个杂环中的一个或多个另外的氮,氧和/或硫原子,以及任选地一个或多个相同或不同的选自卤素,C 1-4烷氧基,硝基和羟基的取代基被连接到 芳族或杂环,此外,R 1和R 2中的一个也可以代表氢原子,或者R 1和R 2可以与相邻的氮原子一起形成具有任选地C 1-6烷基取代基的吡唑-2,4环的位置 3,R3代表氢,卤素,C1-4烷氧基,氨基,单 - (C1-6烷基) - 氨基,二 - (C1-6烷基) - 氨 羟基,烷基化或酰化羟基,吗啉代,哌嗪子基,N-(C 1-6烷基) - 哌嗪基,N-苄基哌嗪子基或N-吡啶基哌嗪子基及其药学上可接受的酸加成盐, 未取代的1,2-二氢 - 吡啶并[2,3-e] -as-三嗪衍生物。 根据本发明的新化合物作用于中枢神经系统,并施加镇静,止痛,麻醉增强,丁苯那嗪拮抗和消炎作用。 根据本发明的新化合物可以在治疗中有利地应用。
    • 6. 发明授权
    • Pyrido[3,2-e]-as-triazines
    • 吡啶并[3,2-e] -as-三嗪
    • US4320127A
    • 1982-03-16
    • US152833
    • 1980-05-23
    • Pal BenkoAndras MessmerGyorgy HajosSandor BatoriLujza PetoczIboly KosoczkyPeter Gorog
    • Pal BenkoAndras MessmerGyorgy HajosSandor BatoriLujza PetoczIboly KosoczkyPeter Gorog
    • A61K31/53A61P25/00A61P25/04A61P25/20A61P29/00C07D471/04C07D471/14
    • C07D471/04C07D471/14
    • 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.
    • 本发明涉及式I的新的吡啶并[3,2-e] -as-三嗪衍生物及其药学上可接受的酸加成盐,其中R1代表C1-20烷基羰基,卤素C1 -4-烷基 - 羰基,苯甲酰基,苯基-C 1-4烷基 - 羰基或吡啶基 - 羰基; R2是氢原子或C1-4烷基 - 羰基; 或R 1和R 2与相邻的氮原子一起形成在3位上带有C1-6烷基取代基的吡唑-2,4-二酮环; R 3是氢原子,C 1-20烷基,苯基,苯基-C 1-3烷基,呋喃基或吡啶基或​​任选被一至三个C 1-4烷氧基取代的苯基。 通过酰化相应的1,2-未取代的1,2-二氢吡啶并[3,2-e] -as-三嗪衍生物制备式I化合物。 新化合物对中枢神经系统起重要作用,具有镇痛,消炎作用,可用于治疗。
    • 7. 发明授权
    • Benzo-as-triazine derivatives
    • 苯并三嗪衍生物
    • US4316022A
    • 1982-02-16
    • US135143
    • 1980-03-28
    • Gyorgy HajosAndras MessmerPal BenkoLujza PetoczPeter GorogIbolya Kasoczky
    • Gyorgy HajosAndras MessmerPal BenkoLujza PetoczPeter GorogIbolya Kasoczky
    • A61K31/53A61K31/5513A61P23/00A61P29/00C07D249/08C07D253/10C07D487/04C07D487/14C07D401/14C07D403/14
    • C07D487/04C07D487/14
    • 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.
    • 本发明涉及式(I)和(Ia)的新的苯并三嗪衍生物及其药学上可接受的酸加成盐,其中R 1和R 2各自代表氢, C1-20烷基羰基,具有任选一个或多个卤素的苯基羰基或苯基 - (C 1-4烷基) - 羰基,可以相同或不同的羟基或C 1-3烷氧基取代基,此外,吡啶基羰基,吡嗪基羰基, 呋喃基羰基,氯乙酰基或C 1-4烷氧基羰基,或者R 1和R 2可以与相邻的氮原子一起形成在4位具有任选的C 1-6烷基取代基的吡唑环,条件是R1和R2之一 总是不同于氢,R3代表氢,巯基,C1-4烷基巯基,氨基,C1-4烷基氨基,任选具有N-烷基或2-吡啶基取代基的哌嗪基,吗啉代基或 哌啶子基,R4代表氢,卤素, C 1-4烷基或C 1-4烷氧基。 式(I)和(Ia)的化合物通过酰化各自的2,4,5-未取代的4,5-二氢 - 苯并 - 三嗪衍生物来制备。 式(I)和(Ia)的新化合物具有镇痛,消炎和麻醉增效作用。