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    • 11. 发明授权
    • Aminopropanol derivatives, process for their preparation and
pharmaceutical compositions comprising the same
    • 氨基丙醇衍生物,其制备方法和包含其的药物组合物
    • US5234934A
    • 1993-08-10
    • US876091
    • 1992-04-30
    • Zoltan BudaiKlara Reiter nee EssesEniko Sziri nee KiszellyGizella ZsilaGabor GiglerLujza PetoczMaria Szecsey nee HegedusMarton FeketeValeria HoffmannLaszlo Kapolnai
    • Zoltan BudaiKlara Reiter nee EssesEniko Sziri nee KiszellyGizella ZsilaGabor GiglerLujza PetoczMaria Szecsey nee HegedusMarton FeketeValeria HoffmannLaszlo Kapolnai
    • C07C251/58C07D213/16C07D295/088
    • C07D213/16C07C251/58C07D295/088C07C2101/02C07C2101/08C07C2101/14C07C2101/18
    • The invention relates to novel racemic or optically active aminopropanol derivatives of formula I ##STR1## wherein R and R.sup.1 are independently hydrogen atom, halogen atom, lower alkoxy, or together represent a methylene dioxy group,R.sup.2 and R.sup.3 together represent a chemical bond or independently stand for a hydrogen atom,R.sup.4 and R.sup.5 are independently hydrogen atom, C.sub.3-7 cycloalkyl group or straight or branched, saturated or unsaturated C.sub.1-12 alkyl group optionally substituted by one or more dialkyl-aminoalkyl, dimethoxyphenyl or phenyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a 4 to 7 membered ring optionally comprising an oxygen, sulfur or a further nitrogen atom, which ring is optionally substituted by a phenyl, benzyl or C.sub.1-3 alkyl group and the said substituents may carry a hydroxyl group, one or two methoxy groups, halogen atoms or trifluoromethyl groups, orR.sup.4 and R.sup.5 together with the adjacent nitrogen atom form a piperidine ring which is optionally substituted by a phenyl or benzyl group and, if desired, it comprises a double bond,R.sup.6 stands for hydrogen atom or benzoyl group, andn represents an integer from 3 to 6,acid-addition salts and quaternary ammonium derivatives thereof.Further the invention relates to processes for preparing these compounds.The compounds of the invention exert cardiac circulation controlling and/or improving, central nervous system tranquillizing and/or digestive system irregulations improving effects.
    • 本发明涉及式I的新型外消旋或光学活性氨基丙醇衍生物其中R和R 1独立地为氢原子,卤素原子,低级烷氧基或一起代表亚甲基二氧基,R2和R3一起表示化学键或 独立地代表氢原子,R4和R5独立地是氢原子,C3-7环烷基或任选被一个或多个二烷基氨基烷基,二甲氧基苯基或苯基取代的直链或支链,饱和或不饱和的C 1-12烷基,或R 4 和R5与相邻的氮原子一起形成任选地包含氧,硫或另外的氮原子的4至7元环,该环任选被苯基,苄基或C 1-3烷基取代,所述取代基可以携带 羟基,一个或两个甲氧基,卤素原子或三氟甲基,或R4和R5与相邻的氮原子一起形成哌啶环,其任选地是 由苯基或苄基构成,如果需要,它包含双键,R6代表氢原子或苯甲酰基,n代表3-6的整数,其酸加成盐和季铵衍生物。 本发明还涉及制备这些化合物的方法。 本发明的化合物发挥心脏循环控制和/或改善,中枢神经系统镇定和/或消化系统不调节改善作用。
    • 13. 发明授权
    • Bicyclo(2.2.1)heptane oximes used for plant growth regulating
    • 用于植物生长调节的双环(2.2.1)庚烷肟
    • US4425158A
    • 1984-01-10
    • US322675
    • 1981-11-18
    • Zoltan BudaiAttila Kis-TamasTibor MezeiAranka Lay nee KonyaZoltan VighAgnes Sokorai nee Janki
    • Zoltan BudaiAttila Kis-TamasTibor MezeiAranka Lay nee KonyaZoltan VighAgnes Sokorai nee Janki
    • A01N33/24A01N33/04A01N35/10A01P21/00C07C251/44C07C251/50
    • A01N35/10
    • The invention relates to new bicyclo(2.2.1)heptane derivatives of the general formula I ##STR1## wherein R represents a C.sub.1-12 alkyl group optionally substituted by a lower alkoxy group, a C.sub.2-4 alkenyl group or a phenyl-(lower alkyl) group optionally substituted on the phenyl ring by one or more lower alkoxy groups or halogen atoms.The invention relates further to plant growth regulating compositions comprising as active agent 0.001 to 95% by weight of a racemic and/or optically active compound of the general formula I, wherein R has the above defined meanings, along with a conventional organic or inorganic, solid and/or liquid carrier and/or filler and/or diluent and/or surfactant.The invention encompasses also the preparation of the compounds of the general formula I which comprises reacting a racemic or optically active compound of the general formula II ##STR2## wherein Y is an oxygen or sulfur atom or an oxim group, with a compund of the general formula IIIR - XwhereinR is as defined above, andX represents a leaving group, preferably a halogen atom, a sulfonyloxy or an aminooxy group, with the proviso that when using a compound of the general formula II, in which Y is an oxim group, X is other than aminooxy group,in the presence of a basic condensing agent, and optionally resolving the racemic compound of the general formula I obtained into its optically active antipodes.
    • 本发明涉及通式I的新的双环(2.2.1)庚烷衍生物,其中R表示任选被低级烷氧基,C 2-4链烯基或苯基 - ( 低级烷基)基团,其任选在苯环上被一个或多个低级烷氧基或卤素原子取代。 本发明进一步涉及植物生长调节组合物,其包含作为活性剂0.001至95重量%的通式I的外消旋和/或旋光活性化合物,其中R具有上述定义的含义,以及常规的有机或无机, 固体和/或液体载体和/或填料和/或稀释剂和/或表面活性剂。 本发明还包括通式I的化合物的制备,其包括使通式II的外消旋或旋光活性化合物其中Y是氧或硫原子或肟基,与下列化合物反应: 通式III R-X其中R如上定义,X​​表示离去基团,优选卤素原子,磺酰氧基或氨基氧基,条件是当使用通式II的化合物时,其中Y为 肟基,X不是氨基氧基,在碱性缩合剂的存在下,并且任选地将所得通式I的外消旋化合物拆分成其光学活性对映体。
    • 16. 发明授权
    • Bicyclo(2.2.1)heptane oximes
    • 双环(2.2.1)庚烷肟
    • US4511737A
    • 1985-04-16
    • US551941
    • 1983-11-15
    • Zoltan BudaiAttila Kis-TamasTibor MezeiAranka LayZoltan VighAgnes Sokorai
    • Zoltan BudaiAttila Kis-TamasTibor MezeiAranka LayZoltan VighAgnes Sokorai
    • A01N33/24A01N33/04A01N35/10A01P21/00C07C251/44C07C251/50C07C131/02
    • A01N35/10
    • The invention relates to new bicyclo(2.2.1)heptane derivatives of the general formula I ##STR1## wherein R represents a C.sub.1-12 alkyl group optionally substituted by a lower alkoxy group, a C.sub.2-4 alkenyl group or a phenyl-(lower alkyl) group optionally substituted on (I), phenyl ring by one or more lower alkoxy groups or halogen atoms.The invention relates further to plant growth regulating compositions comprising as active agent 0.001 to 95% by weight of a racemic and/or optically active compound of the general formula I, wherein R has the above defined meanings, along with a conventional organic or inorganic, solid and/or liquid carrier and/or filler and/or diluent and/or surfactant.The invention encompasses also the preparation of the compounds of the general formula (I) which comprises reacting a racemic or optically active compound of the general formula (II) ##STR2## wherein Y is an oxygen or sulfur atom or an oxim group, with a compound of the general formula (III)R--XwhereinR is as defined above, andX represents a leaving group, preferably a halogen atom, a sulfonyloxy or an aminooxy group, with the proviso that when using a compound of the general formula (II), in which Y is an oxim group, X is other than aminooxy group,in the presence of a basic condensing agent, and optionally resolving the racemic compound of the general formula (I) obtained into its optically active antipodes.
    • 本发明涉及通式I(I)的新型双环(2.2.1)庚烷衍生物,其中R表示任选被低级烷氧基取代的C 1-12烷基,C 2-4链烯基或苯基 - (低级烷基)基团,其任选地在(I)上取代,苯基环由一个或多个低级烷氧基或卤素原子取代。 本发明进一步涉及植物生长调节组合物,其包含作为活性剂0.001至95重量%的通式I的外消旋和/或旋光活性化合物,其中R具有上述定义的含义,以及常规的有机或无机, 固体和/或液体载体和/或填料和/或稀释剂和/或表面活性剂。 本发明还包括通式(I)的化合物的制备,其包括使通式(II)的外消旋或光学活性化合物其中Y是氧或硫原子或肟基的(II) 与通式(III)RX的化合物,其中R如上定义,X​​表示离去基团,优选卤素原子,磺酰氧基或氨基氧基,条件是当使用通式 (II),其中Y是肟基,X不是氨基氧基,在碱性缩合剂的存在下,并且任选地将通式(I)的外消旋化合物拆分成其光学活性对映体。
    • 18. 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。