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    Naphthalene anti-psoriatic agents
    3.
    发明公开
    Naphthalene anti-psoriatic agents 失效
    萘普生抗体药剂

    公开(公告)号：EP0150831A3

    公开(公告)日：1985-12-18

    申请号：EP85100783

    申请日：1985-01-25

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Jones, Gordon H. ,  Venuti, Michael C. ,  Young, John M.

    IPC分类号： C07C69/157 ,  C07C69/24 ,  C07C69/78 ,  C07C67/08 ,  A61K31/22 ,  A61K31/235

    CPC分类号： C07D213/89 ,  C07C46/00 ,  C07C50/10 ,  C07C50/14 ,  C07C50/24 ,  C07C50/32 ,  C07C255/00 ,  C07C317/00 ,  C07C323/00 ,  C07D213/64 ,  C07D239/38 ,  C07D333/64

    摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula:
    wherein:
    R' is alkoxy of one to twelve carbon atoms, of one to twelve carbon atoms, alkylthio of one to twelve carbon atoms, optionally substituted phenoxy or optionally substituted phenylthio; R 2 is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenylalkyl; R 3 is lower alkyl, lower alkoxy, or halo and m is 0, 1 or 2, or R 3 is optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, cyano, or S(O) n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and m is 1 and n is 0, 1 or 2; and W is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl.

    Verfahren zur stereospezifischen Herstellung von Verbindungen der Vitamin K1- und K2-Reihe sowie neue Ausgangsprodukte in diesem Verfahren
    5.
    发明公开
    Verfahren zur stereospezifischen Herstellung von Verbindungen der Vitamin K1- und K2-Reihe sowie neue Ausgangsprodukte in diesem Verfahren 失效
    一种用于和新的起始原料维生素K1的化合物K2系列，并且在这个过程中有规立构的制备方法。

    公开(公告)号：EP0015436A1

    公开(公告)日：1980-09-17

    申请号：EP80100822.8

    申请日：1980-02-19

    申请人： F. HOFFMANN-LA ROCHE & CO. Aktiengesellschaft

    发明人： Dötz, Karl Heinz, Dr.

    IPC分类号： C07C50/14 ,  C07C46/06 ,  C07C37/11 ,  C07C11/22

    CPC分类号： C07F11/00 ,  C07C1/326 ,  C07C11/28 ,  C07C46/06 ,  C07C50/14

    摘要： 57 Die Erfindung betrifft ein neues Verfahren zur Herstellung von Verbindungen der Vitamin K1- und K 2 -Reihe, insbesondere in der Form der E-Isomeren. Das Verfahren besteht darin, daß man einen Phenyl-carbon-carbonyl-Metallkomplex der Formel
    mit einem Enin der Formel CH3― C≡C―R2 II zu einer Verbindung der Formel
    umsetzt. Anschließend wird die Metall-Ring-Bindung gespalten und, erforderlichenfalls, das erhaltene Naphthoiderivat oxidiert.
    In den Formeln I, II und III bedeutet R 1 niederes Alkyl, Acyl oder Benzyl und R 2 einen Dimethylallyl-, Geranyl-, Farnesyl-oder analogen isoprenoiden Terpenylrest bzw. den Phytyl-Rest.
    Die Erfindung betrifft ferner neue Verbindungen der Formel CH3―C≡C―R 2 , worin R 2 einen Geranyl-, Farnesyl- oder analogen isoprenoiden Terpenylrest bzw. den Phytyl-Rest darstellt und der Formel
    worin R 1 und R 2 die obige Bedeutung haben.

    摘要翻译： 本发明涉及一种新的制备方法在与E异构体的形式的维生素K1和K2系列化合物，特别是。 该方法包括在一个CH3-C ^ C-R2式与式II的烯炔的苯基羧酸 - 羰基 - 金属络合物为式的化合物反应。 然后，在金属环键断裂，如果有必要，氧化得到的萘酚衍生物。 在式I，II和III中，R 1是低级烷基，酰基或苄基，R 2代表二甲基烯丙基，牻牛儿基，法呢基或类似类异戊二烯Terpenylrest或植基残基。 本发明还涉及式CH3-C ^ C-R 2，其中R 2代表牻牛儿基，法呢基或类似类异戊二烯Terpenylrest或植基残基和下式其中R 1和R 2具有上述含义的新化合物。

    VERFAHREN ZUR HERSTELLUNG VON 1,1'-BINAPHTALINYLIDEN-4,4'-DIONEN
    7.
    发明授权
    VERFAHREN ZUR HERSTELLUNG VON 1,1'-BINAPHTALINYLIDEN-4,4'-DIONEN 有权
    用于生产1,1'- BINAPHTALINYLIDEN -4,4-二酮

    公开(公告)号：EP1263705B1

    公开(公告)日：2003-11-19

    申请号：EP01923675.1

    申请日：2001-03-16

    申请人： Lonza AG

    发明人： HAUCK, Michael ,  HEVELING, Josef ,  WELLIG, Alain

    IPC分类号： C07C46/06 ,  C07C50/14

    CPC分类号： C07C46/06 ,  C07C50/14

    摘要： The invention relates to a method for producing 1,1' binaphthalenylidene-4,4'-diones of general formula (I), wherein R1 represents C¿1-6? alkyl, C1-6 alkoxy, phenyl, substituted phenyl, benzyl or benzyloxy; R?2, R3, R4, and R5¿ independently of one another represent hydrogen, C¿1-6? alkyl, C1-6 alkoxy, phenyl, substituted phenyl, benzyl or benzyloxy. Production takes place by oxidative coupling of the corresponding naphthols in the presence of a peroxide and a precious metal catalyst.

    Preparation process of naphthoquinone derivatives and intermediates for the preparation thereof
    9.
    发明公开
    Preparation process of naphthoquinone derivatives and intermediates for the preparation thereof 失效
    Verfahren zur Herstellung von Naphthochinonen sowie Zwischenprodukte bei deren Herstellung。

    公开(公告)号：EP0636598A1

    公开(公告)日：1995-02-01

    申请号：EP94111565.1

    申请日：1994-07-25

    申请人： EISAI CHEMICAL CO., LTD.

    发明人： Hamamura, Kimio ,  Seki, Chiaki ,  Konishi, Masayuki

    IPC分类号： C07C46/00 ,  C07C50/20 ,  C07C50/18 ,  C07C50/14

    CPC分类号： C07C50/14 ,  C07C46/00 ,  C07C49/617 ,  C07C49/653 ,  C07C50/10

    摘要： Disclosed herein are a naphthoquinone derivative represented by the following formula:

    wherein R¹ means a hydrogen atom or methyl group, R² is a hydrogen atom or methyl group, n stands for 0 or an integer of 1-9, and a linkage --- is a single bond or double bond with the proviso that if n is an integer of 2-9, the linkages may be identical with or different optionally from each other, such as a vitamin K derivative; and a process for producing the naphthoquinone derivative at a high yield without forming any geometric isomer; as well as 1,4,4 a ,5,8,9 a -hexahydro-4 a α-alkenyl-1α,4α-methanoanthraquinone derivatives and 1,4,4 a ,5,8,9 a -hexahydro-1α,4α-methanoanthraquinone derivatives which are useful as intermediates for the preparation of the naphthoquinone derivatives.

    摘要翻译： 本文公开了由下式表示的萘醌衍生物：其中R 1表示氢原子或甲基，R 2表示氢原子或甲基，n表示0或1- 9，并且键 - 是单键或双键，条件是如果n是2-9的整数，则所述键可以彼此相同或不同，例如维生素K衍生物; 以及高产率生产萘醌衍生物而不形成任何几何异构体的方法; 以及1,4,4a，5,8,9a-六氢-4aα-烯基-1α，4α-甲基蒽醌衍生物和1,4,4a，5,8,9a-六氢-1α，4α - 甲基蒽醌衍生物，其可用作制备萘醌衍生物的中间体。

    Naphthalene anti-psoriatic agents
    10.
    发明公开
    Naphthalene anti-psoriatic agents 失效
    萘普生抗体药剂

    公开(公告)号：EP0282056A3

    公开(公告)日：1990-05-09

    申请号：EP88103799.8

    申请日：1988-03-10

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Venuti, Michael C.

    IPC分类号： C07C69/157 ,  C07C69/24 ,  C07C43/23 ,  A61K31/22 ,  C07C67/28 ,  A61K31/09 ,  C07C41/26

    CPC分类号： C07C46/00 ,  C07C43/23 ,  C07C50/10 ,  C07C50/14 ,  C07C50/24

    摘要： Psoriasis in mammals is relieved by topically administering naphthalenes of the formula:
    wherein:
        R¹ is lower alkoxy or optionally substituted phenoxy;
        R² is hydrogen, lower alkyl, optionally substituted phenyl or optionally substituted phenyl-lower-alkyl;
        R³ is hydrogen, lower alkyl, lower alkoxy, halo, optionally substituted phenyl, optionally substituted phenyl-lower-alkyl or optionally substituted phenyl-lower-­alkoxy, and m is 1 or 2;
        X and Y are different and are selected from the group consisting of hydrogen, R⁴ and -C(O)W,
    wherein
        W is alkyl of one to seven carbon atoms, optionally substituted phenyl or optionally substituted benzyl; and
        R⁴ is lower alkyl or optionally substituted phenyl-lower-alkyl.