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    Pyrimidine derivatives, process for preparing the same and herbicide using the same
    1.
    发明授权
    Pyrimidine derivatives, process for preparing the same and herbicide using the same 失效
    嘧啶衍生物，其制备方法和使用其的除草剂

    公开(公告)号：US5387575A

    公开(公告)日：1995-02-07

    申请号：US894557

    申请日：1992-06-05

    申请人： Katsumasa Harada ,  Takaaki Abe ,  Yuji Akiyoshi ,  Akio Matsushita ,  Mikio Kojima ,  Ikuo Shiraishi ,  Kaoru Yamamoto ,  Takashi Hayama ,  Shohei Fukuda

    发明人： Katsumasa Harada ,  Takaaki Abe ,  Yuji Akiyoshi ,  Akio Matsushita ,  Mikio Kojima ,  Ikuo Shiraishi ,  Kaoru Yamamoto ,  Takashi Hayama ,  Shohei Fukuda

    IPC分类号： A01N43/54 ,  A01N43/66 ,  C07D239/60 ,  C07D251/30 ,  C07D251/38 ,  C07D521/00 ,  C07D239/52 ,  A01N73/54

    CPC分类号： C07D231/12 ,  A01N43/54 ,  A01N43/66 ,  C07D233/56 ,  C07D239/60 ,  C07D249/08 ,  C07D251/30 ,  C07D251/38

    摘要： Disclosed are a pyrimidine or triazine compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents cyano group, a halogen atom, hydroxy group or --O--R.sup.7 where R.sup.7 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group or a cyano-lower alkyl group; R.sup.2 represents hydrogen atom or a lower alkyl group; R.sup.3 represents hydrogen atom or a lower alkyl group; R.sup.4 represents a 1-imidazolyl group, --NHSO.sub.2 --R.sup.8 where R.sup.8 represents a lower alkyl group or a phenyl group which may have a substituent, hydroxy group, a lower alkoxy group or a benzyloxy group when Z is nitrogen atom; or a 1-imidazolyl group, --NHSO.sub.2 --R.sup.8 where R.sup.8 has the same meaning as defined above, hydroxy group, OK, a lower alkoxy group which may have a substituent, a lower alkenyloxy group, a lower alkynyloxy group, a cycloalkoxy group which may have a substituent, a phenoxy group, a benzyloxy group, a lower alkylthio group, a phenylthio group or an alkylsulfonylamino group when Z is --CH.dbd. group; R.sup.5 represents a lower alkoxy group; R.sup.6 represents a lower alkoxy group or a lower alkyl group; X represents oxygen atom or sulfur atom; and Z represents nitrogen atom or --CH.dbd. group. processes for preparing the same and a herbicide containing the same as an active ingredient(s).

    摘要翻译： 公开了由下式（I）表示的嘧啶或三嗪化合物：其中R 7表示低级烷基，低级烯基，低级炔基，卤代烷基， 低级烷基或氰基 - 低级烷基; R2代表氢原子或低级烷基; R3表示氢原子或低级烷基; R 4表示当Z为氮原子时，可以具有取代基，羟基，低级烷氧基或苄氧基的低级烷基或苯基，-NHSO 2 -R 8， 或1-咪唑基，-NHSO 2 -R 8，其中R8具有与上述相同的含义，羟基，OK，可具有取代基的低级烷氧基，低级链烯氧基，低级炔氧基，环烷氧基 当Z为-CH =基团时，可具有取代基，苯氧基，苄氧基，低级烷硫基，苯硫基或烷基磺酰基氨基; R5代表低级烷氧基; R6代表低级烷氧基或低级烷基; X表示氧原子或硫原子; Z表示氮原子或-CH =基团。 其制备方法和含有其作为活性成分的除草剂。

    Triazine derivative, process for preparing the same and herbicide using the same
    2.
    发明授权
    Triazine derivative, process for preparing the same and herbicide using the same 失效
    三嗪衍生物，其制备方法和使用其的除草剂

    公开(公告)号：US5529977A

    公开(公告)日：1996-06-25

    申请号：US326830

    申请日：1994-10-21

    申请人： Katsumasa Harada ,  Takaaki Abe ,  Yuji Akiyoshi ,  Akio Matsushita ,  Mikio Kojima ,  Ikuo Shiraishi ,  Kaoru Yamamoto ,  Takashi Hayama

    发明人： Katsumasa Harada ,  Takaaki Abe ,  Yuji Akiyoshi ,  Akio Matsushita ,  Mikio Kojima ,  Ikuo Shiraishi ,  Kaoru Yamamoto ,  Takashi Hayama

    IPC分类号： A01N43/54 ,  A01N43/66 ,  C07D239/60 ,  C07D251/30 ,  C07D251/38 ,  C07D521/00 ,  C07D251/34 ,  C07D251/16 ,  C07D403/12

    CPC分类号： C07D231/12 ,  A01N43/54 ,  A01N43/66 ,  C07D233/56 ,  C07D239/60 ,  C07D249/08 ,  C07D251/30 ,  C07D251/38

    摘要： Disclosed are a pyrimidine or triazine compound represented by the following formula (I): ##STR1## wherein R.sup.1 represents cyano group, a halogen atom, hydroxy group or --O--R.sup.7 where R.sup.7 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group or a cyano-lower alkyl group; R.sup.2 represents hydrogen atom or a lower alkyl group; R.sup.3 represents hydrogen atom or a lower alkyl group; R.sup.4 represents a 1-imidazolyl group, --NHSO.sub.2 --R.sup.8 where R.sup.8 represents a lower alkyl group or a phenyl group which may have a substituent, hydroxy group, a lower alkoxy group or a benzyloxy group when Z is nitrogen atom; or a 1-imidazolyl group, --NHSO.sub.2 --R.sup.8 where R.sup.8 has the same meaning as defined above, hydroxy group, OK, a lower alkoxy group which may have a substituent, a lower alkenyloxy group, a lower alkynyloxy group, a cycloalkoxy group which may have a substituent, a phenoxy group, a benzyloxy group, a lower alkylthio group, a phenylthio group or an alkylsulfonylamino group when Z is --CH.dbd. group; R.sup.5 represents a lower alkoxy group; R.sup.6 represents a lower alkoxy group or a lower alkyl group; X represents oxygen atom or sulfur atom; and Z represents nitrogen atom or --CH.dbd. group.processes for preparing the same and a herbicide containing the same as an active ingredient(s).

    摘要翻译： 公开了由下式（I）表示的嘧啶或三嗪化合物：其中R 1表示氰基，卤素原子，羟基或-O-R 7，其中R 7表示低级烷基，低级烯基 基，低级炔基，卤代低级烷基或氰基 - 低级烷基; R2表示氢原子或低级烷基; R3表示氢原子或低级烷基; R 4表示当Z为氮原子时，可以具有取代基，羟基，低级烷氧基或苄氧基的低级烷基或苯基，-NHSO 2 -R 8， 或1-咪唑基，-NHSO 2 -R 8，其中R8具有与上述相同的含义，羟基，OK，可具有取代基的低级烷氧基，低级链烯氧基，低级炔氧基，环烷氧基 当Z为-CH =基团时，可具有取代基，苯氧基，苄氧基，低级烷硫基，苯硫基或烷基磺酰基氨基; R5代表低级烷氧基; R6代表低级烷氧基或低级烷基; X表示氧原子或硫原子; Z表示氮原子或-CH =基团。 其制备方法和含有其作为活性成分的除草剂。

    Sulfonamide derivative, process for preparing the same and herbicide using the same
    3.
    发明授权
    Sulfonamide derivative, process for preparing the same and herbicide using the same 失效
    磺酰胺衍生物，其制备方法和使用其的除草剂

    公开(公告)号：US5376620A

    公开(公告)日：1994-12-27

    申请号：US41998

    申请日：1993-04-02

    申请人： Takaaki Abe ,  Yuji Akiyoshi ,  Hiroshi Shiraishi ,  Ikuo Shiraishi ,  Mikio Kojima ,  Takashi Hayama ,  Takaaki Kuwata

    发明人： Takaaki Abe ,  Yuji Akiyoshi ,  Hiroshi Shiraishi ,  Ikuo Shiraishi ,  Mikio Kojima ,  Takashi Hayama ,  Takaaki Kuwata

    IPC分类号： A01N43/54 ,  A01N43/66 ,  C07D239/60 ,  C07D251/34 ,  C07D251/38 ,  C07D401/12

    CPC分类号： C07D401/12 ,  A01N43/54 ,  A01N43/66 ,  C07D239/60 ,  C07D251/34 ,  C07D251/38

    摘要： Disclosed are a sulfonamide compound represented by the following formula (I): ##STR1## wherein Y represents a lower akyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group, a cyano-lower alkyl group or --C(CH.sub.3).sub.2 (OR.sup.1) where R.sup.1 represents a lower akyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group or a cyano-lower alkyl group; Q represents a substituted or unsubstituted pyridyl group or --NR.sup.2 R.sup.3 where R.sup.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group; and R.sup.3 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a phenyl group or a benzyl group; or R.sup.2 and R.sup.3 may be combined to form a cycloamino group; X represents an oxygen atom or a sulfur atom; and Z represents a nitrogen atom or --CH.dbd. group;processes for preparing the same and a herbicide containing the same as an active ingredient(s).

    摘要翻译： 公开了由下式（I）表示的磺酰胺化合物：其中Y表示低级烷基，低级烯基，低级炔基，卤代低级烷基，氰基 - 低级烷基 基团或-C（CH 3）2（OR 1），其中R 1表示低级烷基，低级烯基，低级炔基，卤代低级烷基或氰基 - 低级烷基; Q表示取代或未取代的吡啶基或-NR2R3，其中R2表示氢原子，低级烷基，低级烷氧基; R3表示低级烷基，低级烯基，低级炔基，苯基或苄基。 或者R 2和R 3可以组合形成环氨基; X表示氧原子或硫原子; Z表示氮原子或-CH =基团; 其制备方法和含有其作为活性成分的除草剂。

    Process for preparing 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ol
    5.
    发明授权
    Process for preparing 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ol 失效
    制备6,7-二烷氧基-3,4-二氢异喹啉-8-醇的方法

    公开(公告)号：US5446164A

    公开(公告)日：1995-08-29

    申请号：US199691

    申请日：1994-02-22

    申请人： Kiyofumi Ishikawa ,  Takashi Hayama

    发明人： Kiyofumi Ishikawa ,  Takashi Hayama

    IPC分类号： C07D217/02 ,  C07D217/18 ,  C07D217/20 ,  C07D217/26 ,  C07D401/06 ,  C07D491/04 ,  C07D491/056 ,  C07D217/16

    CPC分类号： C07D401/06 ,  C07D217/18 ,  C07D217/26 ,  C07D491/04

    摘要： This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the Bischler-Napieralski reaction, a process for synthesizing 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols via the compounds, and use of the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols for preparation of the 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols.It is possible, according to this invention, to obtain the 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols, which have hitherto been difficult to synthesize, via the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols in a high yield.

    摘要翻译： 本发明涉及新的6,7-二烷氧基-3,4-二氢异喹啉-8-醇，一种用于以6,7-二烷氧基-3,4-二氢异喹啉-8-醇的方式选择性地并以高产率制备Bischler -Napieralski反应，通过该化合物合成6,7-二烷氧基-1,2,3,4-四氢异喹啉-8-醇的方法，以及使用6,7-二烷氧基-3,4-二氢异喹啉-8-醇 用于制备6,7-二烷氧基-1,2,3,4-四氢异喹啉-8-醇。 根据本发明，通过6,7-二烷氧基-3，得到迄今为止难以合成的6,7-二烷氧基-1,2,3,4-四氢异喹啉-8-醇， 4-二氢异喹啉-8-醇。

    Aminophosponic acid derivative
    7.
    发明授权
    Aminophosponic acid derivative 失效
    氨基磷酸衍生物

    公开(公告)号：US5380921A

    公开(公告)日：1995-01-10

    申请号：US55872

    申请日：1993-05-04

    申请人： Kiyofumi Ishikawa ,  Takehiro Fukami ,  Takashi Hayama ,  Kenji Matsuyama ,  Kazuhito Noguchi ,  Mitsuo Yano

    发明人： Kiyofumi Ishikawa ,  Takehiro Fukami ,  Takashi Hayama ,  Kenji Matsuyama ,  Kazuhito Noguchi ,  Mitsuo Yano

    IPC分类号： A61K31/66 ,  A61K31/675 ,  A61K38/00 ,  A61P9/08 ,  A61P9/12 ,  A61P11/08 ,  A61P13/02 ,  A61P15/00 ,  C07F9/38 ,  C07F9/40 ,  C07K5/06 ,  C12N9/99 ,  C07F9/08

    CPC分类号： C07K5/06191 ,  C07F9/3808 ,  A61K38/00

    摘要： There are provided novel aminophosphonic acid derivatives of the general formula [I]: ##STR1## wherein n is an integer of 2 or 3; R.sup.1 is a phenyl, naphthyl, indolyl, benzothienyl, benzofuryl or benzoxazolyl group which may have 1 to 3 substituents selected from the group consisting of hydroxyl and lower alkyloxy groups, or a hydrogen atom; R.sup.2 is a lower alkyl group, a benzyl group, a 4-hydroxybenzyl group, a 3-indolylmethyl group or a .beta.-phenethyl group; and A is an optional residue of an amino acid selected from the group consisting of tryptophane, tyrosine, phenylalanine, homophenylalanine, naphthylalanine or N.sup..omega. -nitroarginine, and their pharmaceutically acceptable salts. The compounds according to the present invention and their pharmaceutically acceptable salts exhibit an inhibitory activity against endothelin-converting enzyme, and are expected to be useful as a drug treating various diseases with which endothelin is concerned.

    摘要翻译： 提供了通式[I]的新型氨基膦酸衍生物：其中n为2或3的整数; R1是可以具有1至3个选自羟基和低级烷氧基或氢原子的取代基的苯基，萘基，吲哚基，苯并噻吩基，苯并呋喃基或苯并恶唑基; R2是低级烷基，苄基，4-羟基苄基，3-吲哚基甲基或β-苯乙基; A是任选的氨基酸残基，其选自色氨酸，酪氨酸，苯丙氨酸，高苯丙氨酸，萘丙氨酸或N，ω-硝基精氨酸，及其药学上可接受的盐。 根据本发明的化合物及其药学上可接受的盐表现出对内皮素转化酶的抑制活性，并且预期可用作治疗涉及内皮素的各种疾病的药物。

    Pyrazinone derivatives
    8.
    发明授权
    Pyrazinone derivatives 失效
    吡嗪酮衍生物

    公开(公告)号：US06914062B2

    公开(公告)日：2005-07-05

    申请号：US10312500

    申请日：2001-06-28

    申请人： Takashi Hayama ,  Nobuhiko Kawanishi ,  Tooru Takaki

    发明人： Takashi Hayama ,  Nobuhiko Kawanishi ,  Tooru Takaki

    IPC分类号： A61P35/00 ,  A61P43/00 ,  C07D213/75 ,  C07D277/48 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04 ,  A01N43/58 ,  A01N43/60 ,  A61K31/495 ,  A61K31/50 ,  C07D475/00

    CPC分类号： C07D213/75 ,  C07D277/48 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04

    摘要： The present invention relates to a compound of the general formula (I): [Ar1 is aryl fused to the adjacent pyrazinone ring at the 5th and 6th positions, etc., X is CO, etc., Y is CH, etc., Z is CH, etc., V is CH, etc., Wn is —(CH2)n— (n is zero to four), R1 is H or optionally substituted lower alkyl, etc., R2 is H, etc., R3 and R4 are the same or different and are each H, etc., R5 and R6 are the same or different and are each H, hydroxy, etc.] or a pharmaceutically acceptable salt or ester thereof; a pharmaceutical composition, an inhibitor of Cdk4 and/or Cdk6 or an anti-cancer agent, containing the same as an active ingredient; and a process for preparing them.

    摘要翻译： 本发明涉及通式（I）的化合物：[Ar 1]在第5和6位与相邻的吡嗪酮环稠合的芳基等，X是CO等， Y是CH等，Z是CH等，V是CH等，W n是 - （CH 2）n - （n为0至4），R 1为H或任选取代的低级烷基等，R 2为H等，R 3 R 3和R 4相同或不同，各自为H等，R 5和R 6相同或不同， 不同且各自为H，羟基等]或其药学上可接受的盐或酯; 药物组合物，Cdk4和/或Cdk6抑制剂或抗癌剂，其含有活性成分; 和一个准备它们的过程。

    6,7-dialkoxy-3,4-diydroisoquinolin-8-yl compounds
    9.
    发明授权
    6,7-dialkoxy-3,4-diydroisoquinolin-8-yl compounds 失效
    6,7-二烷氧基-3,4-二氢异喹啉-8-基化合物

    公开(公告)号：US5498717A

    公开(公告)日：1996-03-12

    申请号：US288551

    申请日：1994-08-10

    申请人： Kiyofumi Ishikawa ,  Takashi Hayama

    发明人： Kiyofumi Ishikawa ,  Takashi Hayama

    IPC分类号： C07D217/02 ,  C07D217/18 ,  C07D217/20 ,  C07D217/26 ,  C07D401/06 ,  C07D491/04 ,  C07D491/056 ,  C07D217/14 ,  C07D217/16

    CPC分类号： C07D401/06 ,  C07D217/18 ,  C07D217/26 ,  C07D491/04

    摘要： This invention relates to novel 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols, a process for preparing the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols reioselectively and in a high yield utilizing the Bischler-Napieralski reaction, a process for synthesizing 6,7-dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols via the compounds, and use of the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols for preparation of the 6,7-dialkoxy-1, 2,3,4-tetrahydroisoquinolin-8-ols.It is possible according to this invention, to obtain the 6,7 -dialkoxy-1,2,3,4-tetrahydroisoquinolin-8-ols, which have hitherto been difficult to synthesize, via the 6,7-dialkoxy-3,4-dihydroisoquinolin-8-ols in a high yield.

    摘要翻译： 本发明涉及新的6,7-二烷氧基-3,4-二氢异喹啉-8-醇，一种用于以6,7-二烷氧基-3,4-二氢异喹啉-8-醇的方式选择性地并以高产率制备Bischler -Napieralski反应，通过该化合物合成6,7-二烷氧基-1,2,3,4-四氢异喹啉-8-醇的方法，以及使用6,7-二烷氧基-3,4-二氢异喹啉-8-醇 用于制备6,7-二烷氧基-1,2,3,4-四氢异喹啉-8-醇。 根据本发明，可以通过6,7-二烷氧基-3,4,4-四氢异喹啉-3,4,4-四烷氧基-3,4,4-四氢异喹啉-8-酮，得到迄今为止难以合成的6,7-二烷氧基-1,2,3,4-四氢异喹啉-8-醇 - 二氢异喹啉-8-醇。