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    • 6. 发明授权
    • Benzophenonehydrazones
    • 二苯甲酮腙
    • US5340837A
    • 1994-08-23
    • US83245
    • 1993-06-25
    • Roger G. HallAlfons PascualOdd Kristiansen
    • Roger G. HallAlfons PascualOdd Kristiansen
    • A01N33/26A01N35/02A01N41/04A01N41/06A01N43/30A01N47/02A01N47/12A01N47/40C07C251/86C07C251/88C07C255/61C07C255/66C07C307/06C07C309/65C07C309/66C07C311/05C07C311/51C07D317/46C07D307/87
    • A01N43/30A01N35/02A01N41/04A01N41/06A01N47/02A01N47/12A01N47/40C07C251/86C07C307/06C07C309/65C07C309/66C07C311/51C07D317/46
    • Compounds of the formula ##STR1## wherein each of o and p, independently of the other, is 0, 1, 2, 3, 4 or 5, the radicals R.sub.1 being the same or different when o is greater than 1 and the radicals R.sub.2 being the same or different when p is greater than 1;each of R.sub.1 and R.sub.2, independently of the other, is C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, halogen, --NO.sub.2, --OH, C.sub.1 -C.sub.4 alkoxy, halo-C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylthio, halo-C.sub.1 -C.sub.4 alkylthio, --O--S(.dbd.O)--R.sub.6, --O--S(.dbd.O).sub.2 --R.sub.6, phenoxy or --N(R.sub.11)SO.sub.2 R.sub.12 and/or two substituents R.sub.1 and/or two substituents R.sub.2 are, independently of one another, together --Y--Z--Y--;R.sub.3 is hydrogen, C.sub.1 -C.sub.4 alkyl or halo-C.sub.1 -C.sub.4 alkyl;R.sub.4 is hydrogen, C.sub.1 -C.sub.4 alkyl, halo-C.sub.1 -C.sub.4 alkyl, unsubstituted phenyl or naphthyl or mono- or di-substituted phenyl or naphthyl;R.sub.5 is --S--R.sub.7, --S(.dbd.O)--R.sub.7, --S(.dbd.O).sub.2 --R.sub.7, --NO.sub.2, --CN, --C(.dbd.O)--R.sub.8 or --C(.dbd.O)--OR.sub.8 ;R.sub.6 is C.sub.1 -C.sub.8 alkyl, or halo-C.sub.1 -C.sub.8 alkyl or phenyl;X is N or C(R.sub.9);each Y, independently of the other, is O or S; andZ is methylene, eth-1,2-ylene, halomethylene or haloeth-1,2-ylene;and the tautomers and salts thereof can be used as pesticidal compositions and can be prepared in a manner known per se.
    • 式(I)的化合物其中o和p各自独立地为0,1,2,3,4或5,当o大于1时,基团R 1相同或不同,并且 当p大于1时,基团R2相同或不同; R 1和R 2各自独立地为C 1 -C 4烷基,卤代C 1 -C 4烷基,卤素,-NO 2,-OH,C 1 -C 4烷氧基,卤代C 1 -C 4烷氧基,C 1 -C 4烷硫基,卤代C 1 -C 4烷硫基, -OS(= O)-R6,-OS(= O)2 -R6,苯氧基或-N(R11)SO2R12和/或两个取代基R1和/或两个取代基R2彼此独立地是-YZY- ; R3是氢,C1-C4烷基或卤代-C1-C4烷基; R4是氢,C1-C4烷基,卤代C1-C4烷基,未取代的苯基或萘基或单或二取代的苯基或萘基; R5是-S-R7,-S(= O)-R7,-S(= O)2-R7,-NO2,-CN,-C(= O)-R8或-C(= O) R 6是C 1 -C 8烷基或卤代C 1 -C 8烷基或苯基; X为N或C(R9); 每个Y独立于O或S; 并且Z是亚甲基,乙-1,2-亚烯基,卤代亚甲基或卤代乙烯基1,2-亚烯基; 并且其互变异构体和盐可以用作农药组合物,并且可以以本身已知的方式制备。
    • 7. 发明授权
    • Substituted propane-phosphinic acid compounds
    • 取代的丙烷 - 次膦酸化合物
    • US5190933A
    • 1993-03-02
    • US845871
    • 1992-03-03
    • Eric K. BaylisLudwig MaierStuart J. MickelHans-Rudolf OlpeHelmut BittigerWolfgang FrostlRoger G. Hall
    • Eric K. BaylisLudwig MaierStuart J. MickelHans-Rudolf OlpeHelmut BittigerWolfgang FrostlRoger G. Hall
    • C07F9/30C07F9/48
    • C07F9/48C07F9/301Y02P20/55
    • 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。
    • 9. 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。
    • 10. 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。