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    • 34. 发明授权
    • Substituted alkanediphosphonic acids and pharmaceutical use
    • 取代的烷二膦酸和药用
    • US4939130A
    • 1990-07-03
    • US315962
    • 1989-02-27
    • Knut A. JaeggiLeo Widler
    • Knut A. JaeggiLeo Widler
    • C07F9/38A61K31/66A61K31/665A61K31/67A61K31/675A61P3/00A61P3/02A61P3/14A61P9/10A61P29/00A61P35/00A61P43/00C07F9/547C07F9/645C07F9/6503C07F9/6506C07F9/6518C07F9/653C07F9/6539
    • C07F9/65061C07F9/65032C07F9/65033C07F9/65062C07F9/65181C07F9/65182C07F9/6539
    • Alkanediphosphonic acids, in particular heteroarylalkanediphosphonic acids of formula ##STR1## wherein R.sub.1 is a 5-membered heteroaryl radical which may be fused with benzene or cyclohexene nuclei and which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl or phenyl which is substituted by lower alkyl, lower alkoxy and/or halogen, or by lower alkoxy, hydroxy, di-lower alkylamino, lower alkylthio and/or halogen, and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen, and R.sub.2 is hydrogen, hydroxy, amino, lower alkylthio or halogen, and salts thereof, have regulatory action on calcium metabolism and can be used as medicaments for the treatment of diseases associated with impairment of calcium metabolism. The compounds are obtained for example by converting, in a compound of formula ##STR2## wherein X.sub.1 is a functionally modified phosphono group and X.sub.2 is a free or functionally modified phosphono group, X.sub.1 and, if appropriate X.sub.2, into the free phosphono group.
    • 烷基膦酸,特别是式(I)的杂芳烷基亚烷基二酸,其中R 1是可与苯或环己烯核稠合的5元杂芳基,并且其含有2至4个N原子或1或4个N原子 2个N原子以及1个O-或S-原子,并且是被低级烷基,苯基或被低级烷基,低级烷氧基和/或卤素取代的苯基未被取代或C取代,或被低级烷氧基,羟基 ,二低级烷基氨基,低级烷硫基和/或卤素,和/或在能够被低级烷基,低级烷氧基和/或卤素取代的N-原子上被N-取代,并且R 2是氢,羟基,氨基, 低级烷硫基或卤素及其盐具有对钙代谢的调节作用,可用作治疗与钙代谢损伤有关的疾病的药物。 化合物例如通过在其中X 1是官能改性的膦酰基并且X 2是游离或官能改性的膦酰基的式(II)化合物中转化为X1,并且如果合适的话,X2转化成游离膦酰基 组。
    • 35. 发明授权
    • Diphosphonate derivatives, pharmaceutical compositions and methods of
use for calcium disturbances
    • 二膦酸衍生物,药物组合物和钙紊乱的使用方法
    • US4777163A
    • 1988-10-11
    • US77228
    • 1987-07-24
    • Elmar BosiesRudi Gall
    • Elmar BosiesRudi Gall
    • A61K31/66A61K31/675A61P3/00A61P3/14A61P43/00C07F9/38C07F9/6506C07F9/6518C07F9/653C07F9/6539C07F9/6541C07F9/6544C07F9/65
    • C07F9/6539C07F9/65062C07F9/65181C07F9/65182C07F9/653C07F9/65324C07F9/6541
    • The present invention produces alkyldiphosphonic acid derivative of the general formula: ##STR1## wherein Het is a heteroaromatic five-membered ring containing to 3 heteroatoms which can be partly hydrogenated and optionally substituted one or more times by alkyl, alkoxy, phenyl, cyclohexyl, cyclohexylmethyl, halogen or amino, and two adjacent alkyl substituents can together also form a ring, Y is a hydrogen atom or a lower alkyl radical, X is a hydrogen atom, a hydroxyl group or an amino group optionally substituted by lower alkyl and R is a hydrogen atom or a lower alkyl radical, with the proviso that Het is not a pyrazole ring; as well as the pharmacologically acceptable salts thereof.The present invention also provides processes for the prepearation of these compounds and pharmaceutical compositions containing them useful for the treatment or prophylaxis of calcium metabolism disturbances or disease as for example osteoporosis, Bechterew's disease, bone metastases, urolithiasis, heterotropic ossifications, rheumatoid arthritis osteoarthritis or degenerative arthrosis.
    • 本发明产生以下通式的烷基二膦酸衍生物:其中Het是含有3个杂原子的杂芳族五元环,其可以被部分氢化并任选地被烷基,烷氧基,苯基, 环己基,环己基甲基,卤素或氨基,两个相邻的烷基取代基可一起形成环,Y为氢原子或低级烷基,X为氢原子,羟基或任选被低级烷基取代的氨基, R是氢原子或低级烷基,条件是Het不是吡唑环; 以及其药理学上可接受的盐。 本发明还提供了这些化合物的预切方法和含有它们的药物组合物的方法,所述方法可用于治疗或预防钙代谢紊乱或疾病,例如骨质疏松症,Bechterew氏病,骨转移,尿石症,异质性骨化,类风湿性关节炎骨关节炎或退行性 关节。
    • 36. 发明授权
    • Triazolylalkenes as fungicides and plant growth regulants
    • 三唑基烯烃作为杀真菌剂和植物生长调节剂
    • US4497647A
    • 1985-02-05
    • US466825
    • 1983-02-16
    • Alfred MeyerWalter KunzLudwig MaierHermann Rempfler
    • Alfred MeyerWalter KunzLudwig MaierHermann Rempfler
    • A01N43/653A01N47/06A01N47/12C07D233/60C07D249/08C07D521/00C07F9/6518A01N43/50A01N43/64
    • C07D231/12A01N43/653C07D233/56C07D249/08C07F9/65181
    • The invention relates to novel azolyl-olefin derivatives of the general formula I ##STR1## wherein R.sub.1 is an azolyl group,R.sub.2 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.1 -C.sub.4 alkyl substituted by unsubstituted or substituted phenyl, C.sub.1 -C.sub.4 alkoxycarbonyl or C.sub.2 -C.sub.6 alkenyl, or is C.sub.3 -C.sub.8 cycloalkyl which is substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl groups,R.sub.3 is C.sub.1 -C.sub.12 alkyl, C.sub.3 -C.sub.8 cycloalkyl which is substituted by 1 to 4 C.sub.1 -C.sub.4 alkyl groups, or is the --C(R.sub.4)(R.sub.5)--[CH(R.sub.4)].sub.n --X--R.sub.6 group, wherein n is 0 or 1 andR.sub.4 and R.sub.5, each independently of the other, are hydrogen or C.sub.1 -C.sub.4 alkyl,X is oxygen or sulfur,R.sub.6 is a radical selected from the group consisting of C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, phenyl, naphthyl, biphenyl, benzylphenyl, benzoxyphenyl, phenoxyphenyl and aralkyl, which radical is substituted by one or more of halogen, cyano, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.5 alkoxy, C.sub.1 -C.sub.5 haloalkoxy, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 haloalkyl, C.sub.1 -C.sub.3 haloalkylthio, nitro, --COOR.sub.7 or --CON(R.sub.8)(R.sub.9), whereinR.sub.7 is C.sub.1 -C.sub.4 alkyl andR.sub.8 and R.sub.9, each independently of the other, are hydrogen or C.sub.1 -C.sub.4 alkyl, and the acid addition salts quaternary azolium salts and metal complexes thereof.The invention also describes methods of preparing these compounds as well as agrochemical compositions which contain one of said compounds as active ingredient. The invention further describes a method of controlling phytopathogenic microorganisms and/or of regulating plant growth which comprises the use of the novel compounds.
    • 本发明涉及通式Ⅰ(I)的新的唑基 - 烯烃衍生物,其中R1是唑基,R2是C1-C12烷基,C3-C8环烷基,被未取代或取代的苯基取代的C1-C4烷基,C1-C4烷氧基羰基 或C 2 -C 6烯基,或者是被1至4个C 1 -C 4烷基取代的C 3 -C 8环烷基,R 3是C 1 -C 12烷基,被1至4个C 1 -C 4烷基取代的C 3 -C 8环烷基,或者是-C )(R5) - [CH(R4)] nX-R6基团,其中n为0或1,R4和R5各自独立地为氢或C1-C4烷基,X为氧或硫,R6为自由基 选自C 1 -C 8烷基,C 3 -C 8环烷基,C 3 -C 6烯基,C 3 -C 6炔基,苯基,萘基,联苯基,苄基苯基,苯氧基苯基,苯氧基苯基和芳烷基,该基团被一个或多个卤素,氰基, C 1 -C 4烷基,C 1 -C 5烷氧基,C 1 -C 5卤代烷氧基,C 1 -C 3烷硫基,C 1 -C 3卤代烷基,C 1 -C 3卤代烷硫基,硝基,-COOR 7或-CON(R 8)(R 9) 9,各自独立地是氢或C 1 -C 4烷基,和酸加成盐季氮鎓盐及其金属络合物。 本发明还描述了制备这些化合物的方法以及含有所述化合物之一作为活性成分的农药组合物。 本发明还描述了一种控制植物病原微生物和/或调节植物生长的方法,其包括使用新化合物。
    • 37. 发明授权
    • Combating pests with N-phosphonylcarbonyl-carbamates
    • 防治害虫与N-膦酰基羰基 - 氨基甲酸酯
    • US4357329A
    • 1982-11-02
    • US276406
    • 1981-06-22
    • Gerhard HeywangEngelbert KuhleIngeborg HammannBernhard Homeyer
    • Gerhard HeywangEngelbert KuhleIngeborg HammannBernhard Homeyer
    • A01N57/18C07F9/38C07F9/40C07F9/6518C07F9/655A01N57/24A01N57/22
    • A01N57/18C07F9/4065C07F9/65181
    • N-Phosphonylcarbonyl-N-methylcarbamic acid esters of the formula ##STR1## in which R.sup.1 and R.sup.2 can be identical or different and each represents alkyl, alkenyl or alkynyl, it being possible for any of these radicals to be substituted by halogen, andR.sup.3 represents alkyl, phenyl, naphthyl, benzodioxolanyl, dihydrobenzofuranyl or indanyl, it being possible for any of these radicals to carry one or more substituents selected from alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, alkynoxy, alkylthio, alkenylthio, alkynylthio, dialkylamino, halogenoalkyl, halogen, nitro, cyano, cycloalkyl, formamidino, dioxanyl and dioxolanyl, orR.sup.3 represents a radical of the formula ##STR2## in which R.sup.4 and R.sup.5 can be identical or different and each represents alkyl, alkoxy, alkylthio, alkylthioalkyk, cyano, alkoxycarbonyl, dialkylcarbamoyl, dialkoxyphosphoryl or triazolyl, orR.sup.4 and R.sup.5, together with the C atom to which they are bonded, form a dithiolane, dithiane, oxythiolane or oxathiane ring which is optionally substituted by methyl or phenyl,which are pesticidally active.
    • 其中R 1和R 2可以相同或不同并且各自代表烷基,烯基或炔基,这些基团中的任何一个可以被卤素取代的N-膦酰基羰基-N-甲基氨基甲酸酯, 代表烷基,苯基,萘基,苯并二恶烷基,二氢苯并呋喃基或茚满基,这些基团中的任何一个可以携带一个或多个选自烷基,烯基,炔基,烷氧基,链烯氧基,炔氧基,烷硫基,烯硫基,炔硫基,二烷基氨基,卤代烷基 ,卤素,硝基,氰基,环烷基,甲脒基,二烷基和二氧戊环基,或R 3表示下式的基团,其中R 4和R 5可以相同或不同,并且各自表示烷基,烷氧基,烷硫基,烷硫基烷基,氰基, ,二烷基氨基甲酰基,二烷氧基磷酰基或三唑基,或者R4和R5与它们所键合的C原子一起形成二硫杂环戊烷,二噻烷,氧硫杂环丁烷或氧硫杂环, 由甲基或苯基取代,它们具有杀虫活性。
    • 40. 发明授权
    • Pesticidal compositions and methods
    • US3326751A
    • 1967-06-20
    • US3326751D
    • C07D249/14C07F9/6518
    • C07F9/65181
    • The invention comprises compounds of the general formula (or a tantomeric form thereof) in which X is a C2-C6 alkyl group or a phenyl group and R is a C1-C4 alkyl group or a phenyl, chlorophenyl- or methoxyphenyl group or such phenyl or substituted phenyl group containing a methyl group as a nuclear substituent. They may be obtained by reacting an amino-triazole derivative of formula or a tautomer thereof or a metal compound of such derivative in which the H atom of the >NH group in the nucleus is replaced by a metal, e.g. Na or K, with a compound of the general formula:- wherein Hlg is a halogen atom, e.g. Cl, n = O or 1 and Y1 and Y2 are halogen, e.g. Cl, or each is a -N(CH3)2 group or Y1 is N(CH3)2 and Y2 is halogen, and then if n = 1 and Y1 and Y2 are halogen atoms, reacting the resulting product with dimethylamine, or, if n = 1, Y1 is N(CH3)2 and Y2 is halogen reacting the resulting product with dimethylamine or if n = 0 and Y and Y2 are halogen atoms reacting the resulting product with dimethylamine followed by oxidation, or if n = 0, Y1 is N(CH3)2 and Y2 is halogen reacting the resulting product with dimethylamine followed by oxidation, or if n = 0 and Y1 and Y2 both represent -N(CH3)2, oxidizing the resulting product. The reaction between the aminotriazole derivative and the phosphorus halide compound IV is preferably carried out in the presence of a halogen-hydracid binding agent, e.g. a tertiary alkylamine, an N,N-dialkyl aniline, pyridine or homologue thereof or a metal or ammonium compound, and any subsequent oxidation step may be carried out with H2O2. The condensation reactions may be carried out in a solvent, e.g. an aliphatic or aromatic hydrocarbon, an aliphatic ether, a tertiary amine, a nitrile, ester, ketone, alcohol, nitrobenzene, CCl4 or dimethylformamide. The products have insecticidal properties and are also effective in combating moulds.ALSO:A composition for combating noxious organisms, e.g. insects, red spider or mildew contains as active ingredient a compound of the following general formula (or tautomeric form thereof): in which X is a C2-C6 alkyl group or a phenyl group and R is a C1-C4 alkyl group or a phenyl, chlorophenyl or methoxyphenyl group or such phenyl or substituted phenyl group containing a methyl group as a nuclear substituent (see Division C2). The composition may comprise the active ingredient in admixture with a liquid or solid carrier with or without a surface-active agent e.g. a dispersion, emulsifying and/or wetting agent and may be in the form of a dust, miscible oil or wettable powder. Specified solvents for use in preparing miscible oils are xylene, toluene, dioxane, petroleum distillates rich in aromatics, tetrahydronaphthalene and cyclohexane. Specified solid carriers include pipe clay, chalk, sawdust, tobacco dust, and ground coconut shells.