摘要:
Racemic or optionally active 2-(propargyloxyimino)-1,7,7-trimethyl-bicyclo[2,2,1]heptane of the formula (I) ##STR1## or a mixture of these isomers is prepared by reacting a racemic or optically active 1,7,7-trimethyl-bicyclo[2,2,1]heptane derivative of the general formula (II), ##STR2## wherein Y stands for oxygen atom, sulfur atom or oxime group, with a propyne derivative of the general formula (III),R--CH.sub.2 --C.tbd.CH (III)whereinR stands for halogen atom or aminooxy group, with the proviso that if Y represents oxime group, R may stand only for halogen, and if R represents aminooxy group, Y may stand only for oxygen or sulfur atom.The resulting product is new and possesses strong plant growth promoting and insecticidal effects.This is a division of application Ser. No. 065,156, filed Aug. 9, 1979, now U.S. Pat. No. 4,244,888, Jan. 13, 1981.
摘要:
Racemic or optically active 2-(propargyloxyimino)-1,7,7-trimethyl-bicyclo[2,2,1]heptane of the formula (I) ##STR1## or a mixture of these isomers is prepared by reacting a racemic or optically active 1,7,7-trimethyl-bicyclo[2,2,1]heptane derivative of the general formula (II), ##STR2## wherein Y stands for oxygen atom, sulfur atom or oxime group, with a propyne derivative of the general formula (III),R--CH.sub.2 --C.tbd.CH (III) whereinR stands for halogen atom or aminooxy group, with the proviso that if Y represents oxime group, R may stand only for halogen, and if R represents aminooxy group, Y may stand only for oxygen or sulfur atom.The resulting product is new and possesses strong plant growth promoting and insecticidal effects.
摘要:
The invention relates to new N-substituted amino propane sulfonic acid derivatives of the Formula I ##STR1## and salts and hydrates thereof, a process for the preparation thereof and plant growth regulating agents comprising the same whereinR.sup.1 and R.sup.2 may be identical or different and stand for hydrogen, halogen, lower alkyl or lower alkoxy andR stands for furyl; or lower alkyl or phenyl the two latter groups being optionally substituted by one or more halogeno atom(s).
摘要:
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.
摘要:
The invention relates to pharmaceutical compositions possessing valuable antianginal activity. These compositions show higher activity and more favorable therapeutic indices than the reference compound Prenylamine. Preparation of different kinds of pharmaceutical compositions, such as tablets, dragees, capsules and injectable solutions, containing compounds of general formula (I) ##STR1## or their acid addition salts as active ingredients, is disclosed, wherein in formula (I)R is phenyl or 4-chlorophenyl;R.sup.1 and R.sup.2 each represent hydrogen, methyl or isopropyl;R.sup.3 and R.sup.4 are hydrogen, or together form a chemical bond;n is an integer from 4 to 6;A means trimethylene, if n is 4 or 6; or ethylene, if n is 5.
摘要:
The invention relates to novel oxime ethers of the formula I ##STR1## wherein R stands for a phenyl group which may be substituted by a halogen atom or by one or more C.sub.1 -C.sub.4 alkoxy, hydroxyl, nitro or di(C.sub.1 -C.sub.3 alkyl)amino groups,R.sup.1 and R.sup.2 denote each a hydrogen atom or together a valence bond,A denotes a C.sub.2 -C.sub.4 straight or branched-chain alkylene group,N denotes an integer from 3 to 10, andR.sup.3 and R.sup.4 denote a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, furthermore to acid addition salts and quaternary ammonium salts thereof. These new compounds are biologically active, and possess primarily local analgesic, spasmolytic, nicotine-lethality inhibiting, tetrabenazine-antagonistic and tetra-cor-spasm inhibiting effects.
摘要翻译:本发明涉及式I(I)的新型肟醚,其中R代表可被卤素原子取代的苯基或一个或多个C 1 -C 4烷氧基,羟基,硝基或二(C1- C 3烷基)氨基,R 1和R 2各自表示氢原子或价键一起,A表示C 2 -C 4直链或支链亚烷基,N DENOTES AN INTEGER为3〜10,R 3和R 4表示氢 原子或C1-C4烷基,此外还涉及其酸加成盐和季铵盐。 这些新化合物具有生物活性,主要具有局部镇痛,解痉,尼古丁致死抑制,四苯并嗪拮抗和四痉挛抑制作用。
摘要:
The new compounds of the general Formula I ##STR1## (wherein A stands for a C.sub.2-4 straight or branched chain alkylene group;R.sup.1 and R.sup.2 may be same or different and each stands for hydrogen, halogen, lower alkyl or lower alkoxy; orR.sup.1 and R.sup.2 together form a methylenedioxy group;R.sup.3 and R.sup.4 may be the same or different and each stands for C.sub.1.ident. alkyl or C.sub.3.notident. cycloalkyl orR.sup.3 and R.sup.4 together with the nitrogen atom, they are attached to, form a 4-7 membered ring which may contain as additional ring member an oxygen or sulfur atom or a further nitrogen atom and the latter nitrogen atom may optionally bear a C.sub.1-3 alkyl or benzyl substituent)and pharmaceutically acceptable acid addition salts and quaternary ammonium salts thereof possess valuable therapeutical properties and exert particularly useful transquillant-sedative, antidepressant, antiepileptic, antiparkinson, analgesic, local anaesthetic, gastric acid secretion inhibiting and/or antianginal effect.The new compounds of the general Formula I may be prepared by methods known per se.
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:
The invention relates to selected stereoisomers having the E, E or E, Z configuration and within the Formula (I) ##STR1## wherein N is 2-4, A is alkylene or 2 or 3 carbon atoms, R is phenyl or substituted phenyl and R.sup.1 and R.sup.2 are lower alkyl, or, together with the carbon to which attached, form a heterocyclic ring; and pharmaceutically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions comprising the same.The compounds of the general formula (I) can be used in therapy due to their narcosis potentiating, analgesic and antiarrhythmial effect.
摘要:
The invention relates to novel basic ethers of the general formula /I/ and pharmaceutically acceptable acid addition salts and quaternary salts thereof, ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and represent a C.sub.1-5 alkyl group or a C.sub.3-6 cycloalkyl group or they form, together with the adjacent nitrogen atom, a heterocyclic ring containing 4-7 carbon atoms and optionally a further hetero atom, e.g. an oxygen, sulfur or nitrogen atom, and this latter may be optionally substituted by a C.sub.1-3 alkyl, benzyl or phenyl group,R represents a phenyl, phenyl-/C.sub.1-3 alkyl/ or thienyl group optionally substituted by one or more halogen or C.sub.1-3 alkoxy substituent/s/,A represents a C.sub.2-5 straight or branched alkylene chain, and represents a valence bond of .alpha. or .beta. configuration.The new compounds of the general formula /I/ possess valuable anticonvulsive, motility inhibiting, hexobarbital narcose potentiating and analgesic effects, which are, in case of certain compounds, complemented by week antiserotonine, gastro-intestinal-tract inhibiting and antiinflammatory effects, and can be applied to advantage in the therapy.