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    Substituted benzoylphenylureas compounds useful as pesticides
    1.
    发明授权
    Substituted benzoylphenylureas compounds useful as pesticides 失效
    用作农药的取代苯甲酰基苯基化合物

    公开(公告)号：US4847258A

    公开(公告)日：1989-07-11

    申请号：US86339

    申请日：1987-08-17

    申请人： Elmar Sturm ,  Robert W. Lang ,  Odd Kristiansen

    发明人： Elmar Sturm ,  Robert W. Lang ,  Odd Kristiansen

    IPC分类号： A01N47/34 ,  C07D239/34

    CPC分类号： C07D239/34 ,  A01N47/34

    摘要： The invention relates to novel N-benzoyl-N,-4-(5-phenylpyrimid-2-yloxy)phenylureas of formula ##STR1## wherein X.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio,X.sub.2 is halogen, methyl, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio,Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are each independently hydrogen, halogen, methyl, trifluoromethyl or methoxy,Z is methyl, halomethyl containing 1 to 3 halogen atoms or pentafluoroethyl; andR.sub.1, R.sub.2 and R.sub.3 are each independently hydrogen, halogen, C.sub.1 -C.sub.3 alkyl, trifluoromethyl or C.sub.1 -C.sub.3 alkoxy,to the preparation thereof and to intermediates for the synthesis of these compounds, as well as to compositions containing them for use in pest control, especially for controlling representatives of the order Acarina that attack plants and animals and for controlling insects. The novel compounds exhibit especially pronounced activity against plant-destructive mites.

    摘要翻译： 本发明涉及式（I）其中X 1为氢，卤素，C 1 -C 3烷氧基或C 1 -C 3烷硫基的新的N-苯甲酰基-N，4-（5-苯基嘧啶-2-基氧）苯基脲，X2 是卤素，甲基，C 1 -C 3烷氧基或C 1 -C 3烷硫基，Y 1，Y 2，Y 3和Y 4各自独立地为氢，卤素，甲基，三氟甲基或甲氧基，Z为甲基，含1至3个卤素原子的卤代甲基或五氟乙基; R 1，R 2和R 3各自独立地为氢，卤素，C 1 -C 3烷基，三氟甲基或C 1 -C 3烷氧基，并且用于合成这些化合物的中间体，以及含有它们用于病虫害防治的组合物， 特别是控制攻击植物和动物并控制昆虫的蜱虫的代表。 新型化合物对植物破坏性螨具有特别显着的活性。

    Novel production processes
    2.
    发明授权
    Novel production processes 失效
    新型生产工艺

    公开(公告)号：US4822919A

    公开(公告)日：1989-04-18

    申请号：US90200

    申请日：1987-08-26

    申请人： Pierre Martin ,  Robert W. Lang

    发明人： Pierre Martin ,  Robert W. Lang

    IPC分类号： A01N43/36 ,  A01N47/16 ,  C07C45/45 ,  C07C49/255 ,  C07D207/34 ,  C07C49/248

    CPC分类号： C07D207/34 ,  A01N43/36 ,  A01N47/16 ,  C07C45/455 ,  C07C49/255

    摘要： There is described a process for producing fungicidally active 4-phenylpyrrole derivatives of the formula I ##STR1## wherein R is halogen, C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl, andn is 0, 1 or 2, which process comprises reacting a 3-trifluoromethyl-4-phenylpyrrole of the formula II ##STR2## wherein R.sub.n is as defined under the formula I, and R.sub.1 is hydrogen or an acyl group, at elevated temperature and elevated pressure, with ammonia. Important intermediates and the production thereof are also described.

    摘要翻译： 描述了制备式I的杀真菌活性4-苯基吡咯衍生物（I）的方法，其中R是卤素，C 1 -C 6烷基或C 1 -C 6 - 卤代烷基，n是0,1或2，其中 方法包括在升高的温度和升高的压力下，使氨与式II的3-三氟甲基-4-苯基吡咯反应，其中Rn如式I所定义，R 1是氢或酰基。 还描述了重要的中间体及其生产。

    .alpha.-Hydroxy thioethers
    7.
    发明授权
    .alpha.-Hydroxy thioethers 失效
    α-羟基硫醚

    公开(公告)号：US4808572A

    公开(公告)日：1989-02-28

    申请号：US936671

    申请日：1986-12-01

    申请人： Andreas Beck ,  Werner Breitenstein ,  Andreas von Sprecher ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Beck ,  Werner Breitenstein ,  Andreas von Sprecher ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： A61K31/16 ,  A61K31/165 ,  A61K31/19 ,  A61K31/195 ,  A61K31/215 ,  A61K31/22 ,  A61K31/23 ,  A61K38/00 ,  A61K45/00 ,  A61P11/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C67/00 ,  C07C313/00 ,  C07C321/18 ,  C07C323/00 ,  C07C323/52 ,  C07C323/58 ,  C07C323/59 ,  C07C323/60 ,  C07K1/113 ,  C07K5/02 ,  C07K5/06 ,  C07C149/243

    CPC分类号： C07K5/0606 ,  A61K31/19 ,  A61K31/215 ,  C07C323/00 ,  A61K38/00

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: a is an integer of from 1 to 7,R.sup.o represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted at the terminal carbon atom by a free or acylated hydroxy group, by a halogen atom having an atomic number of at most 17, or by methoxy, or represents C.sub.1-3 -perfluoroalkyl,R.sup.2 represents an optionally unsaturated aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene or alternatively, if R.sup.1 represents a halogenated radical and/or B represents phenylene or ethylene, a single bond or vinylene,B represents a single bond, ethynylene or phenylene,R.sup.3 represents hydroxy, C.sub.1-7 -alkoxy or an optionally substituted amino group, and--X-- represents a single bond, a methylene group of an optionally N-acylated primary aminomethylene group,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新型不对称硫醚，其中通式具有以下含义：a为1至7的整数，R 4表示氢或C 1-7 - 烷酰基，R 1表示C 1-3 - 烷基， 可以在末端碳原子上被游离或酰化的羟基，原子数至多为17的卤素原子或甲氧基取代，或表示C1-3-全氟烷基，R2表示任选不饱和的脂肪族基，其具有 5至15个碳原子，A代表乙烯，或者，如果R1代表卤代基，和/或B代表亚苯基或亚乙基，则单键或亚乙烯基，B代表单键，亚乙炔基或亚苯基，R3代表羟基，C1-7 - 烷氧基或任选取代的氨基，-X-表示单键，任选N-酰化的伯氨基亚甲基的亚甲基，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除平滑肌的收缩b 由白细胞三烯生成，因此适用于治疗过敏性疾病，特别是哮喘病症。

    Aromatic thioethers
    8.
    发明授权
    Aromatic thioethers 失效
    芳香硫醚

    公开(公告)号：US4785004A

    公开(公告)日：1988-11-15

    申请号：US941676

    申请日：1986-12-15

    申请人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    发明人： Andreas Von Sprecher ,  Werner Breitenstein ,  Andreas Beck ,  Robert W. Lang ,  Konrad Oertle

    IPC分类号： C07D215/54 ,  C07D311/24 ,  C07C149/40 ,  A61K31/235

    CPC分类号： C07D311/24 ,  C07D215/54

    摘要： Novel asymmetric thioethers of the formula ##STR1## in which the general symbols have the following meanings: R.sup.0 represents hydrogen or C.sub.1-7 -alkanoyl,R.sup.1 represents C.sub.1-3 -alkyl which may be substituted by one or more halogen atoms having an atomic number of at most 17,R.sup.2 represents an aliphatic radical having from 5 to 15 carbon atoms,A represents ethylene, a single bond or vinylene,B.sup.1 represents C.sub.1-7 -alkylene or phenylene,B.sup.2 represents a single bond, ethylene or phenylene, andM represents an aromatic radical of the partial formula ##STR2## in which the symbols have the following meanings: R.sup.3 represents hydrogen or C.sub.1-4 -alkyl,X represents NH, O, S or if R.sup.4 represents hydrogen, a single bond,one of the symbols R.sup.4 and R.sup.5 represents hydrogen and the other represents the group --CO--R.sup.6, orR.sup.4 and R.sup.5 together represent the radical --CO--C(R.sup.6).dbd.C(R.sup.7)--or--CO--C(R.sup.7).dbd.C(R.sup.6)--orR.sup.4 R.sup.5, together with X, represent the radical --N.dbd.C(R.sup.8)--C(R.sup.6).dbd.CH--,in whichR.sup.6 represents --(CH.sub.2).sub.b --COOR.sup.3 (in which b=0 to 2)R.sup.7 represents hydrogen or C.sub.1-4 -alkyl andR.sup.8 represents hydrogen, methyl, mythoxy or halogen,and their salts are active as leucotriene antagonists since they eliminate the contractions of smooth muscles brought about by leucotrienes, and are therefore suitable for the treatment of allergic, especially asthmatic, conditions.

    摘要翻译： 式（I）的新颖的不对称硫醚，其中通式符号具有以下含义：R 0表示氢或C 1-7 - 烷酰基，R 1表示可以被一个或多个具有 原子数最多为17，R 2表示具有5至15个碳原子的脂族基团，A表示乙烯，单键或亚乙烯基，B1表示C1-7 - 亚烷基或亚苯基，B2表示单键，乙烯或亚苯基 ，M表示部分结构式（M）的芳族基团，其中符号具有以下含义：R 3表示氢或C 1-4 - 烷基，X表示NH，O，S或如果R 4表示氢，则 单键，R4和R5之一表示氢，另一个表示-CO-R6基团，或R4和R5一起代表基团-CO-C（R6）= C（R7）-OR-CO-C（ R7）= C（R6） - 或R4R5与X一起代表基团-N = C（R8）-C（R6）= CH-，其中R6表示 - （CH2）b-COOR3（其中b = 0至2）R7表示氢或C1-4烷基，R8表示氢，甲基，乙氧基或卤素，并且它们的盐作为白三烯拮抗剂是有活性的，因为它们消除了由白三烯引起的平滑肌的收缩，因此适用于 治疗过敏，特别是哮喘，病情。

    Alkanophenones useful for treating allergies
    9.
    发明授权
    Alkanophenones useful for treating allergies 失效
    用于治疗过敏的苯胺酮

    公开(公告)号：US5149717A

    公开(公告)日：1992-09-22

    申请号：US795227

    申请日：1991-11-15

    申请人： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

    发明人： Andreas von Sprecher ,  Andreas Beck ,  Bruno Schaub ,  Robert W. Lang

    IPC分类号： C07D311/24 ,  C07D405/04

    CPC分类号： C07D405/04 ,  C07D311/24

    摘要： Substituted alkanophenones of general formula ##STR1## in which R.sub.1 is unsubstituted or fluorinated lower alkyl, R.sub.2 is hydrogen, or unsubstituted or fluorinated lower alkyl or lower alkenyl, X is lower alkylene, oxy, thio or a direct bond, alk is lower alkylene, n is 1 or 2, R.sub.3 is phenyl that is unsubstituted or is substituted by unsubstituted or fluorinated lower alkyl, by etherified or esterified hydroxy, by unsubstituted or lower alkylated amino and/or by free, esterified or amidated carboxy, or is lower alkyl that is unsubstituted, substituted by fluoro and chloro or substituted by free esterified or amidated carboxy, R.sub.4 is free, esterified or amidated carboxy or 5-tetrazolyl, and R.sub.5 is hydrogen or lower alkyl, have leucotriene-antagonistic properties and can be used as anti-allergic active ingredients in medicaments.

    摘要翻译： 其中R 1为未取代或氟化的低级烷基，R 2为氢或未取代或氟化的低级烷基或低级烯基，X为低级亚烷基，氧基，硫基或直接键的通式为（Ⅰ）的取代的烷基苯醌， 低级亚烷基，n是1或2，R3是未取代的或被未取代或氟化的低级烷基取代的苯基，被醚化或酯化的羟基，被未取代或低级烷基化的氨基和/或被游离的，酯化的或酰胺化的羧基取代，或者是 未取代的低级烷基，被氟和氯取代或被游离的酯化或酰胺化的羧基取代，R4是游离的，酯化的或酰胺化的羧基或5-四唑基，R 5是氢或低级烷基，具有白三烯拮抗性质，并且可以使用 作为药物中的抗过敏活性成分。

    N-phenylpyrrolidines
    10.
    发明授权
    N-phenylpyrrolidines 失效
    N-苯基吡咯烷酮

    公开(公告)号：US5108482A

    公开(公告)日：1992-04-28

    申请号：US521806

    申请日：1990-05-10

    申请人： Robert W. Lang ,  Urs Muller

    发明人： Robert W. Lang ,  Urs Muller

    IPC分类号： A01N25/32 ,  A01N43/36 ,  C07D207/24 ,  C07D207/28

    CPC分类号： C07D207/24 ,  A01N25/32 ,  A01N43/36 ,  C07D207/28

    摘要： The 1-(3,5-bis-trifluoromethylphenyl)-2-thioxopyrrolidine-4-carboxylic acid derivatives of the formula I below are suitable for protecting crop plants against the phytotoxic action of herbicides and for regulating the plant growth.The 1-(3,5-bis-trifluoromethylphenyl)-2-thioxopyrrolidine-4-carboxylic acid derivatives are those of the formula I ##STR1## wherein A is --COOR.sub.1, --COSR.sub.1, --COO.sup..crclbar. M.sup..sym., --CONR.sub.2 R.sub.3 or --COCl; R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl; R.sub.2 and R.sub.3 independently of one another are hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.3 -C.sub.7 cycloalkyl; or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are bonded are a saturated 3- to 7-membered heterocycle which can contain an additional hetero atom selected from the group comprising O, N and S and which is unsubstituted or up to trisubstituted by C.sub.1 14 C.sub.4 alkyl; and M.sup..sym. is the equivalent of an alkali metal cation or an alkaline earth metal cation or HN.sup..sym. (R.sub.2).sub.3, and their isomers in optically pure or enriched form.

    摘要翻译： 下式I的1-（3,5-双 - 三氟甲基苯基）-2-硫代吡咯烷-4-羧酸衍生物适用于保护作物免受除草剂的植物毒性作用和调节植物生长。 1-（3,5-双 - 三氟甲基苯基）-2-硫代吡咯烷-4-羧酸衍生物是式I的那些（I），其中A是-COOR 1，-COSR 1，-COO（ - ）M（ +），-CONR 2 R 3或-COCl; R1是氢，C1-C4烷基，C2-C6链烯基或C2-C6炔基; R2和R3彼此独立地是氢，C1-C4烷基或C3-C7环烷基; 或者R 2和R 3与它们所键合的氮原子一起是饱和的3-至7-元杂环，其可以含有选自O，N和S的另外的杂原子，并且是未被取代或被至 C114 C4烷基; 并且M（+）是碱金属阳离子或碱土金属阳离子或HN（+）（R2）3的当量，以及其光学纯的或富集形式的它们的异构体。