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    Prostratin and Structural or Functional Analogs Thereof
    3.
    发明申请
    Prostratin and Structural or Functional Analogs Thereof 有权
    Prostratin及其结构或功能类似物

    公开(公告)号：US20120101283A1

    公开(公告)日：2012-04-26

    申请号：US13287001

    申请日：2011-11-01

    申请人： Paul A. Wender ,  Jeffrey Warrington ,  Jung-Min Kee

    发明人： Paul A. Wender ,  Jeffrey Warrington ,  Jung-Min Kee

    IPC分类号： C07D231/54 ,  C07C49/617

    CPC分类号： C07C45/61 ,  C07C49/573

    摘要： This invention concerns product and process to convert a hydroxyl group (bold in R3C—OH) in a tigliane-type compound to a hydrogen (bold in R3C—H) to obtain deoxytigliane-type compounds or structural or functional analogs thereof. The process has wide application particularly to produce specific biologically active compounds in quantity for use as pharmaceuticals. In particular the process can be used to convert phorbol to a 12-deoxytigliane (prostratin), which is a therapeutic lead for the treatment of AIDS. New compositions of matter are also disclosed.

    摘要翻译： 本发明涉及将噻唑型化合物中的羟基（粗R 3 C-OH）转化成氢（粗R 3 C-H）的产物和方法，以获得脱氧三联体化合物或其结构或功能类似物。 该方法特别适用于生产用作药物的特定生物活性化合物。 特别地，该方法可用于将佛波醇转化为12-脱氧三联体（前列腺素），其是用于治疗AIDS的治疗铅。 还公开了新的物质组合物。

    Preparation process of naphthoquinone derivative and intermediate for the preparation thereof
    6.
    发明授权
    Preparation process of naphthoquinone derivative and intermediate for the preparation thereof 失效
    萘醌衍生物及其制备方法的制备方法

    公开(公告)号：US5412124A

    公开(公告)日：1995-05-02

    申请号：US280550

    申请日：1994-07-26

    申请人： Kimio Hamamura ,  Chiaki Seki ,  Masayuki Konishi

    发明人： Kimio Hamamura ,  Chiaki Seki ,  Masayuki Konishi

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

    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: ##STR1## wherein R.sup.1 means a hydrogen atom or methyl group, R.sup.2 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.sub.a,5,8,9.sub.a -hexahydro-4.sub.a .alpha.-alkenyl-1.alpha.,4.alpha.-methanoanthraquinone derivatives and 1,4,4.sub.a,5,8,9.sub.a -hexahydro-1.alpha.,4.alpha.-methanoanthraquinone derivatives which are useful as intermediates for the preparation of the naphthoquinone derivatives.

    摘要翻译： 本文公开的是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的整数， 连接是单键或双键，条件是如果n是2-9的整数，则连接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。

    Cyano containing indene derivatives
    8.
    发明授权
    Cyano containing indene derivatives 失效
    含氰基的茚衍生物

    公开(公告)号：US4873344A

    公开(公告)日：1989-10-10

    申请号：US124820

    申请日：1987-11-24

    申请人： Klaus P. Bogeso ,  Michael B. Sommer

    发明人： Klaus P. Bogeso ,  Michael B. Sommer

    IPC分类号： C07C255/47 ,  C07C45/65 ,  C07C45/67 ,  C07C49/617 ,  C07C49/67 ,  C07C49/693 ,  C07C49/697 ,  C07C49/755 ,  C07C62/38 ,  C07C67/00 ,  C07C253/00 ,  C07C253/30 ,  C07C255/45 ,  C07C255/58 ,  C07C311/37 ,  C07C315/04 ,  C07C317/14 ,  C07C317/48 ,  C07C319/20 ,  C07C323/38 ,  C07C323/63 ,  C07D207/32 ,  C07D207/337 ,  C07D207/416 ,  C07D213/57 ,  C07D317/06 ,  C07D317/60 ,  C07D333/24

    CPC分类号： C07D207/337 ,  C07C255/00 ,  C07C45/676 ,  C07C49/697 ,  C07C62/38 ,  C07D213/57 ,  C07D317/60 ,  C07D333/24

    摘要： The present invention relates to novel indene derivatives with the general formula I: ##STR1## wherein R.sup.1 is (a) a phenyl group optionally substituted with one or two groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, lower alkylsulfonyl, dilower alkylamino, acylamino such as acetylamino, cyano, trifluoromethyl, trifluoromethoxy, pyrrole and dilower alkylpyrrole,(b) a polycyclic aromatic or heteroaromatic group, such as naphthalene or quinoline,(c) a heteroaromatic group such as thiophene, pyridine, and pyrrole, optionally substituted with one or more groups selected from halogen, lower alkyl, lower alkoxy, lower alkylthio, trifluoromethyl or trifluoromethoxy,R.sub.2 is selected from H, halogen, lower alkyl, benzyl, lower alkylthio, methoxy, lower alkylsulfonyl, dilower alkylsulfamoyl, acylamino such as acetylamino, benzylamino, dilower alkylamino, cyano, pyrrole, dilower alkylpyrrole, trifluoromethyl and trifluoromethoxy,R.sup.3 is CN, COOR.sup.4, --CON(R.sup.4).sub.2 or COR.sup.4, where R.sup.4 is a lower alkyl group, and "n" is an integer of from 1-3 inclusive.The indene derivatives of formula I are, when R.sup.1 is as defined under (a) above, valuable intermediates which are useful in the preparation of pharmacologically effective indane and indene derivatives known from e.g. U.S. Pat. Nos. 4,443,448 and 4,525,360.Moreover, the invention relates to a method for the preparation of the compounds of formula I and to a method for the preparation of compounds of the following formula IV: ##STR2## wherein R.sup.1, R.sup.2 and "n" are as defined above.

    摘要翻译： 本发明涉及具有通式I的新颖的茚衍生物：其中R 1是（a）任选被一个或两个选自卤素，低级烷基，低级烷氧基，低级烷硫基，低级烷基磺酰基， 二氯烷基氨基，酰氨基如乙酰氨基，氰基，三氟甲基，三氟甲氧基，吡咯和二烯烷基吡咯，（b）多环芳族或杂芳族基团如萘或喹啉，（c）杂芳基如噻吩，吡啶和吡咯， 任选被一个或多个选自卤素，低级烷基，低级烷氧基，低级烷硫基，三氟甲基或三氟甲氧基的基团取代，R 2选自H，卤素，低级烷基，苄基，低级烷硫基，甲氧基，低级烷基磺酰基，二低级烷基氨磺酰基， 作为乙酰氨基，苄氨基，二元烷基氨基，氰基，吡咯，二元烷基吡咯，三氟甲基和三氟甲氧基，R3是CN，COOR4，-CON（R4）2或COR4，其中 R4是低级烷基，“n”是1-3的整数。 当R1如上述（a）中所定义时，式I的茚衍生物是有用的中间体，它们可用于制备药物学有效的二氢化茚和茚衍生物，其从例如， 美国专利 第4,443,448号和第4,525,360号。 此外，本发明涉及制备式I化合物的方法和制备下式IV化合物的方法：其中R 1，R 2和“n”如上所定义。

    Chemical process
    9.
    发明授权
    Chemical process 失效
    化学工艺

    公开(公告)号：US4480133A

    公开(公告)日：1984-10-30

    申请号：US472196

    申请日：1983-03-04

    申请人： Jerry M. Roper

    发明人： Jerry M. Roper

    IPC分类号： C07C45/51 ,  C07C49/617 ,  C07C49/623 ,  C07C49/683 ,  C07C45/45

    CPC分类号： C07C49/623 ,  C07C45/512 ,  C07C49/617 ,  C07C49/683

    摘要： Novel 2,4-dihydrocarbylspiro[5.5]undeca-1,4,8-trien-3-one compounds are prepared by reacting an N,N-dihydrocarbyl,2,6-dihydrocarbyl-4-aminomethylphenol with a conjugated diene and an alkyl halide in a liquid solvent medium.

    摘要翻译： 通过使N，N-二烃基，2,6-二烃基-4-氨基甲基苯酚与共轭二烯和烷基的反应制备新的2,4-二烃基螺[5.5]十一碳-1,4,8-三烯-3-酮化合物 卤化物在液体溶剂介质中。