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    N-Aryl-Stickstoffheterocyclen
    3.
    发明公开
    N-Aryl-Stickstoffheterocyclen 失效
    N-芳基Stickstoffheterocyclen。

    公开(公告)号：EP0363585A1

    公开(公告)日：1990-04-18

    申请号：EP89114065.9

    申请日：1989-07-29

    申请人： BAYER AG

    发明人： Fischer, Reiner, Dr. ,  Lindel, Hans, Dr. ,  Schallner, Otto, Dr. ,  Marhold, Albrecht, Dr. ,  Ooms, Pieter, Dr. ,  Santel, Hans-Joachim, Dr. ,  Schmidt, Robert R., Dr. ,  Lürssen, Klaus, Dr. ,  Strang, Harry, Dr.

    IPC分类号： C07D471/04 ,  C07D513/04 ,  C07D233/86 ,  C07C265/12 ,  C07C331/28 ,  C07C271/58 ,  C07C211/46 ,  A01N43/50 ,  A01N43/78 ,  A01N43/84 ,  A01N43/86

    CPC分类号： C07D471/04 ,  A01N43/50 ,  A01N43/90 ,  A01N47/06 ,  A01N47/22 ,  C07C261/02 ,  C07C265/12 ,  C07C271/58 ,  C07C309/66 ,  C07C331/10 ,  C07C331/28 ,  C07D233/78 ,  C07D513/04

    摘要： Die Erfindung betrifft neue N-Aryl-Stickstoffheterocyclen der Formel (I)
    in welcher

    Het für einen Heterocyclus der Formel

    steht,
    R 1 für Wasserstoff oder Halogen steht,
    R 2 für Alkyl steht und
    R 3 für jeweils gegebenenfalls substituiertes Alkyl, Alkenyl, Alkinyl oder Cycloalkyl steht oder für einen Rest
    oder einen Rest -S0 2 -R s steht,
    wobei
    X 1 und X 2 jeweils für Sauerstoff oder Schwefel stehen,
    R 4 für Alkyl, Alkoxyalkyl, Halogenalkyl, Alkoxy, Alkoxyalkoxy, Halogenalkoxy, Halogenalkoxyalkoxy oder Alkoxyalkylamino steht,
    R 5 für Alkyl, Halogenalkyl oder für gegebenenfalls substituiertes Aryl steht,
    R 6 und R 7 entweder unabhängig voneinander jeweils für Wasserstoff, Alkyl, Alkenyl, Alkinyl oder Cycloalkyl stehen oder gemeinsam für einen zweifach verknüpften Alkandiylrest stehen und
    R 8 für Wasserstoff, Alkyl, Alkenyl, Alkinyl, Alkoxyalkyl oder Cycloalkyl steht,

    mehrere Verfahren zu ihrer Herstellung und ihre Verwendung als Herbizide und Pfalnzenwachstumsregulatoren.

    摘要翻译： 本发明涉及式（I）的N-芳基 - 氮杂环，其中Het是式（I）的杂环或R 1是氢或卤素，R 2是烷基，R 在每种情况下，在任何情况下，任选取代的烷基，烯基，炔基，环烷基或下式的基团或其基团-SO 2 -R 5，其中X 1和X 2各自为 氧或硫，R 4是烷基，烷氧基烷基，卤代烷基，烷氧基，烷氧基烷氧基，卤代烷氧基，卤代烷氧基烷氧基或烷氧基烷基氨基，R 5是烷基，卤代烷基或任选取代的芳基，R 6和R 7各自 氢，烷基，烯基，炔基或环烷基或一起是连接两次的烷二基，R 8是氢，烷基，烯基，炔基，烷氧基烷基或环烷基，其制备方法 以及其作为除草剂和植物生长调节剂的用途。

    IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    7.
    发明公开
    IRREVERSIBLE SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
    雄激素受体和应用过程为不可逆的，选择性调节剂

    公开(公告)号：EP1487783A2

    公开(公告)日：2004-12-22

    申请号：EP03710820.6

    申请日：2003-02-24

    申请人： University of Tennessee Research Foundation

    发明人： DALTON, James ,  MILLER, Duane, D. ,  KIRKOVSKY, Leonid, I. ,  HWANG, Dong Jin ,  STEINER, Mitchell, S. ,  VEVERKA, Karen, A. ,  MUKHERJEE, Arnab

    IPC分类号： C07C233/05 ,  C07C255/50 ,  C07C331/28 ,  A61K31/16 ,  A61K31/26 ,  A61K31/275

    CPC分类号： C07C331/10 ,  A61K31/16 ,  A61K31/26 ,  A61K31/275 ,  C07C261/02 ,  C07C265/12 ,  C07C331/28

    摘要： In one embodiment, this invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). The SARM compounds have unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. In one embodiment, the SARM compounds bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are androgen receptor antagonists which bind irreversibly to the androgen receptor. In another embodiment, the SARM compounds are alkylating agents. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

    FLUORINATED ALKYLTHIOCYANATE PROCESS
    10.
    发明公开
    FLUORINATED ALKYLTHIOCYANATE PROCESS 失效
    用于生产氟化烷基硫氰酸

    公开(公告)号：EP0946505A1

    公开(公告)日：1999-10-06

    申请号：EP97950908.0

    申请日：1997-12-10

    申请人： E.I. DU PONT DE NEMOURS AND COMPANY

    发明人： JACOBSON, Stephen, Ernest

    IPC分类号： B01J31 ,  C07B61 ,  C07C331

    CPC分类号： C07C331/10 ,  C07C331/04 ,  C07C331/12 ,  C07C331/14

    摘要： A process for the preparation of a thiocyanate of the Formula (II): Rf-Am-(CH2)n-SCN wherein Rf is a C2-C20 perfluoroalkyl radical, or a C5-C38 perfluoroalkyl radical having at least one ether oxygen atom; n is 1 to 3; m is 0 or 1; A is O, S, CO2, N(R1)R2, CON(R1)R2, SO2N(R1)R2 or (OCH2CHR3)aO; wherein a is 3 to about 15; R1 is H or alkyl radical of 1 to about 4 carbon atoms; R2 is C1-C12alkylene; and R3 is H or CH2Cl; said process comprising reacting a fluorinated iodide of the Formula (I): Rf-Am-(CH2)n-I wherein Rf, A, m and n are as defined above, with a thiocyanate salt M+(SCN)- wherein M is sodium or potassium, in the presence of a catalyst comprising a quaternary ammonium salt of the Formula (R¿4?)3(R5)N?+Y-¿ wherein R¿4? is butyl; R5 is methyl or butyl; and Y is Cl, Br, I, or HSO4; to yield the fluorinated thiocyanate of Formula (II) as defined above is disclosed.