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    • 3. 发明授权
    • Substituted aminoalkylphosphinic acids
    • 取代的氨基烷基次膦酸
    • US5567840A
    • 1996-10-22
    • US461090
    • 1995-06-05
    • Roger G. HallLudwig MaierWolfgang Frostl
    • Roger G. HallLudwig MaierWolfgang Frostl
    • C07F9/30
    • C07F9/301
    • P-substituted aminoalkylphosphinic acids of the formula ##STR1## wherein R denotes an optionally fluorinated methyl group, R.sub.1 denotes hydrogen, lower alkyl, lower alkoxy, hydroxy, halogen or a fluorinated methyl group and R.sub.2 and R.sub.3 denote hydrogen or R.sub.2 denotes hydroxy, lower alkoxy or halogen and R.sub.3 is hydrogen or R.sub.2 and R.sub.3 together represent an oxo group, and their pharmaceutically acceptable salts are active as GABA.sub.B -agonists and can be used in the treatment of spinal spasticity, multiple sclerosis and cerebral palsy, trigeminus neuralgia, drug withdrawal syndromes and/or conditions of pain. They can be manufactured by methods known per se and suitable such methods are described.
    • 式(I)的P取代氨基烷基次膦酸其中R表示任意氟化的甲基,R 1表示氢,低级烷基,低级烷氧基,羟基,卤素或氟化甲基,R 2和R 3表示氢或R 2表示 羟基,低级烷氧基或卤素,R 3是氢或R 2和R 3一起代表氧基,其药学上可接受的盐作为GABAB-激动剂是有活性的,可用于治疗脊柱痉挛,多发性硬化和脑性麻痹,三叉神经痛神经痛 戒毒综合征和/或疼痛状况。 它们可以通过本身已知的方法制造,并且描述合适的这种方法。
    • 4. 发明授权
    • Substituted propane-phosphinic acid compounds
    • 取代的丙烷 - 次膦酸化合物
    • US5300679A
    • 1994-04-05
    • US968101
    • 1992-10-29
    • Eric K. BaylisHelmut BittigerWolfgang FrostlRoger G. HallLudwig MaierStuart J. MickelHans-Rudolf Olpe
    • Eric K. BaylisHelmut BittigerWolfgang FrostlRoger G. HallLudwig MaierStuart J. MickelHans-Rudolf Olpe
    • C07F9/30C07F9/48A61K31/13A61K31/185
    • C07F9/301C07F9/48Y02P20/55
    • Compounds of the formula I ##STR1## wherein R denotes an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic or araliphatic radical having 2 or more carbon atoms, and wherein one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen or an aliphatic, cycloaliphatic, araliphatic or aromatic radical, another one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen or, in the case of R.sup.1 and R.sup.2, is hydroxy, and the remaining one of R.sup.1, R.sup.2 and R.sup.3 is hydrogen, or wherein R denotes methyl, R.sub.1 denotes hydrogen or hydroxy, R.sub.2 denotes an aromatic radical and R.sub.3 represents hydrogen, and their salts have GABA.sub.B -antagonistic properties and can be used as GABA.sub.B -antagonists. They are obtained when in a compound of formula II ##STR2## in which R, R.sup.1, R.sup.2 and R.sup.3 have their previous significances, Z represents --NH.sub.2 and R.sup.4 denotes a hydroxy-protective group R.sup.5 or, when R.sup.1 and R.sup.3 denote hydrogen and R.sup.2 denotes hydrogen or alkyl, denotes an alkali metal or ammonium ion R.sup.6, or Z represents a protected or latent amino group Z.sup.o and R.sup.4 denotes hydrogen or a hydroxy-protective group R.sup.5, any group R.sup.5 or R.sup.6 is replaced by hydrogen, and/or any group Z.sup.o is converted into --NH.sub.2.
    • 式I的化合物(I)其中R表示具有2个或更多个碳原子的脂族,脂环族,脂环族 - 脂族或芳脂族基团,其中R1,R2和R3中的一个表示氢或脂族,脂环族 ,芳脂族或芳族基团,R 1,R 2和R 3中的另一个为氢,或在R 1和R 2的情况下为羟基,其余的R 1,R 2和R 3为氢,或其中R为甲基,R 1为 氢或羟基,R 2表示芳族基团,R 3表示氢,并且它们的盐具有GABAB拮抗性质,可用作GABAB-拮抗剂。 当其中R,R 1,R 2和R 3具有其先前含义的式II化合物(II)时,它们是得到的,Z表示-NH 2,R4表示羟基保护基R5,或者当R1和R3表示 氢和R2表示氢或烷基,表示碱金属或铵离子R6,或Z表示保护或潜在氨基Zo,R4表示氢或羟基保护基R5,任何基团R5或R6被氢代替,以及 /或任何基团Zo被转化为-NH 2。
    • 7. 发明授权
    • Herbicidal N-2-(nitro-5-phenoxy-phenyl)-aminoalkylphosphonic acid and
esters
    • 除草剂N-2-(硝基-5-苯氧基 - 苯基) - 氨基烷基膦酸和酯
    • US4618358A
    • 1986-10-21
    • US651968
    • 1984-09-19
    • Ludwig Maier
    • Ludwig Maier
    • A01N57/22A01N57/24C07F9/30C07F9/32C07F9/38C07F9/40C07F9/48C07F9/58A01N57/06A01N57/08
    • C07F9/588A01N57/22A01N57/24C07F9/301C07F9/3211C07F9/3808C07F9/383C07F9/4006C07F9/4018C07F9/4816
    • The present invention relates to (2-nitro-5-aryloxyphenylamino)alkylphosphonic, -alkylphosphinic and -alkylphosphonous acid derivatives of the general formula I ##STR1## wherein X is halogen, CF.sub.3, NO.sub.2, CN, CONH.sub.2 or CSNH.sub.2,Y is nitrogen or --CH.dbd.,R is hydrogen, C.sub.1 -C.sub.4 alkyl or aralkyl containing 1 to 4 carbon atoms in the alkyl moiety,R.sub.1 is C.sub.1 -C.sub.4 alkyl,R.sub.2 is C.sub.1 -C.sub.4 alkyl, phenyl or --PO(OR.sub.6).sub.2,R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl,R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl or a cation,R.sub.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 alkoxy, hydroxyl or an --O-cation group,R.sub.6 is hydrogen or C.sub.1 -C.sub.4 alkyl,m is a value from 0 to 3,n is 0 or 1,p is a value from 0 to 3, andq is 0 or 1,with the proviso that R.sub.1 and R.sub.3 taken together may also be an unsubstituted or substituted C.sub.1 -C.sub.3 alkylene chain and at least one of the symbols n, p and q is a value different from 0.These compounds have useful herbicidal properties.
    • 本发明涉及通式I(I)的(2-硝基-5-芳氧基苯基氨基)烷基膦酸烷基亚膦酸和烷基亚膦酸衍生物,其中X是卤素,CF 3,NO 2,CN,CONH 2或CSNH 2,Y R1是C1-C4烷基,R2是C1-C4烷基,苯基或-PO(OR6)2,R3是氮或-CH =,R是氢,C1-C4烷基或在烷基部分含有1至4个碳原子的芳烷基 氢或C1-C4烷基,R4是氢,C1-C4烷基或阳离子,R5是氢,C1-C4烷基,C1-C4卤代烷基,C1-C4烷氧基,羟基或-O-阳离子基团,R6是氢或C1-C4烷基, m为0至3的数,n为0或1,p为0至3,q为0或1,条件是R 1和R 3一起也可以是未取代或取代的C 1 -C 3亚烷基 链和n,p和q中的至少一个符号是不同于0的值。这些化合物具有有用的除草性质。
    • 9. 发明授权
    • Herbicidally active
2-nitro-5-(2'-chloro-4'-trifluoromethylphenoxy)phenylphosphinic acid
derivatives
    • 除草活性2-硝基-5-(2'-氯-4'-三氟甲基苯氧基)苯基次膦酸衍生物
    • US4434108A
    • 1984-02-28
    • US280388
    • 1981-07-06
    • Ludwig Maier
    • Ludwig Maier
    • A01N57/22A01N57/30A01N57/34C07F9/30C07F9/32C07F9/34C07F9/36C07F9/46
    • A01N57/34A01N57/22A01N57/30C07F9/304C07F9/3229C07F9/34C07F9/36
    • The invention relates to novel herbicidally active and plant-growth regulating 2-substituted 5-phenoxyphenylphosphinic acid derivatives of the formula ##STR1## wherein R.sub.1 is an unsubstituted or substituted alkyl or aryl radical, R.sub.2 is a hydroxyl group, lower alkoxy, alkylthio, alkylamino, dialkylamino or chlorine, X is halogen or is selected from the group consisting of --CF.sub.3, --NO.sub.2 or --CN, n is 0 to 3, and Y is selected from the group consisting of --NO.sub.2, --NH.sub.2, --OH, --CN, or is halogen. Preferred compounds are 2-nitro-5-(2'-chloro-4'-trifluoromethylphenoxy)phenylalkylphosphinic acids and lower alkyl esters thereof. The invention also relates to the production of the novel phosphinic acid derivatives, starting from a 3,4-dinitrodiphenyl ether and reaction with a O,O-dialkylalkyl- or -arylphosphonite as first step. The invention further relates to herbicidal and plant growth regulating compositions which contain one of these novel compounds as active component, and also to the use of these compounds and compositions for controlling weeds (also selectively), for inhibiting plant growth and desiccating parts of plants above the ground, as well as for totally destroying existing plant growth.
    • 本发明涉及新颖的除草活性和植物生长调节式(I)的2-取代的5-苯氧基苯基次膦酸衍生物,其中R1是未取代或取代的烷基或芳基,R2是羟基,低级烷氧基, 烷硫基,烷基氨基,二烷基氨基或氯,X为卤素或选自-CF 3,-NO 2或-CN,n为0至3,Y选自-NO 2,-NH 2, OH,-CN或卤素。 优选的化合物是2-硝基-5-(2'-氯-4'-三氟甲基苯氧基)苯基烷基次膦酸及其低级烷基酯。 本发明还涉及从3,4-二硝基二苯醚开始并与O,O-二烷基烷基 - 或芳基亚膦酸酯反应的新的次膦酸衍生物的制备作为第一步。 本发明还涉及含有这些新化合物之一作为活性组分的除草和植物生长调节组合物,还涉及这些化合物和组合物用于控制杂草(也是选择性的)的用途,用于抑制上述植物的植物生长和干燥部分 地面,以及完全破坏现有的植​​物生长。