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    Anilide compounds, including use thereof in ACAT inhibitition
    1.
    发明授权
    Anilide compounds, including use thereof in ACAT inhibitition 失效
    酰苯胺化合物，包括其在ACAT抑制中的用途

    公开(公告)号：US06204278B1

    公开(公告)日：2001-03-20

    申请号：US08858244

    申请日：1997-05-19

    申请人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    发明人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    IPC分类号： A61K31423

    CPC分类号： C07D263/58 ,  C07D235/28 ,  C07D277/70

    摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: where Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NH6—; R6 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

    摘要翻译： 本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基 ，或低级烷氧基; 并且R 4和R 5可以一起形成其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代的低级亚烷基; X是-NH-或氧或硫原子; Y是-NH-，氧 或硫原子，或亚砜或砜基; Z为单键或-NH6-; R6表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

    Anilide compounds and pharmaceutical compositions comprising them
    2.
    发明授权
    Anilide compounds and pharmaceutical compositions comprising them 失效
    酰苯胺化合物和包含它们的药物组合物

    公开(公告)号：US06825223B2

    公开(公告)日：2004-11-30

    申请号：US09789967

    申请日：2001-02-21

    申请人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    发明人： Kimiyuki Shibuya ,  Katsumi Kawamine ,  Yukihiro Sato ,  Toshiyuki Edano ,  Souhei Tanabe ,  Masami Shiratsuchi

    IPC分类号： A61K31428

    CPC分类号： C07D263/58 ,  C07D235/28 ,  C07D277/70

    摘要： The invention provides novel anilide compounds and pharmaceutical compositions comprising them. The invention relates to compounds of a formula: wherein Ar is an optionally-substituted aryl group; R4 and R5 are the same or different, and each is a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and R4 and R5 may together form a lower alkylene group of which one or more methylene moieties may optionally be substituted by oxygen and/or sulfur atoms; X is —NH—, or an oxygen or sulfur atom; Y is —NH—, an oxygen or sulfur atom, or a sulfoxide or sulfone group; Z is a single bond, or —NR6—; R4 represents a hydrogen atom or a lower alkylene group; and n is an integer of from 0 to 15; and their salts and solvates. The compounds of the invention are useful as pharmaceutical compositions, especially as acyl coenzyme A cholesterol acyltransferase (ACAT) inhibitors.

    摘要翻译： 本发明提供了新的酰苯胺化合物和包含它们的药物组合物。本发明涉及下式的化合物：其中Ar是任选取代的芳基; R 4和R 5相同或不同，并且各自是氢原子，低级烷基 基团或低级烷氧基; 并且R 4和R 5可以一起形成低级亚烷基，其中一个或多个亚甲基部分可以任选地被氧和/或硫原子取代; X是-NH-或氧或硫原子; Y是-NH-， 氧或硫原子，或亚砜或砜基; Z为单键或-NR 6 - ; R 4表示氢原子或低级亚烷基; 和n为0至15的整数;以及它们的盐和溶剂化物。本发明的化合物可用作药物组合物，特别是作为酰基辅酶A胆固醇酰基转移酶（ACAT）抑制剂。

    Pyrimidine derivatives
    3.
    发明授权
    Pyrimidine derivatives 失效
    嘧啶衍生物

    公开(公告)号：US6008224A

    公开(公告)日：1999-12-28

    申请号：US849725

    申请日：1997-06-27

    申请人： Mitsuteru Hirata ,  Takeo Deushi ,  Yoshio Takahashi ,  Masahiro Tamura ,  Takeshi Ohshima ,  Toshiaki Oda ,  Hiroyuki Sonoki ,  Masami Shiratsuchi

    发明人： Mitsuteru Hirata ,  Takeo Deushi ,  Yoshio Takahashi ,  Masahiro Tamura ,  Takeshi Ohshima ,  Toshiaki Oda ,  Hiroyuki Sonoki ,  Masami Shiratsuchi

    IPC分类号： C07D239/69 ,  C07D401/04 ,  A61K31/505

    CPC分类号： C07D239/69

    摘要： The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## [wherein R.sup.1 represents a lower alkyl group; each of R.sup.2 and R.sup.3 represents H, alkyl, or alkoxy; each of R.sup.4 and R.sup.5 represents H or alkyl; R.sup.6 represents alkyl, --OR.sup.7, or --NR.sup.8 R.sup.9 ; and n is a number between 0 and 3 inclusive (wherein each of R.sup.7, R.sup.8, and R.sup.9 represents H, alkyl, aryl, aralkyl, amino, a heterocyclic ring, etc.)], as well as to a medicine containing the derivative or salt as the active ingredient. The present compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect and cell proliferation effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

    摘要翻译： PCT No.PCT / JP95 / 02605 Sec。 371日期：1997年6月27日 102（e）日期1997年6月27日PCT 1995年12月19日PCT公布。 公开号WO96 / 20177 PCT 日期：1996年7月4日本发明涉及下述式（1）所示的嘧啶衍生物或其衍生物的盐：其中R1表示低级烷基; R 2和R 3各自表示H，烷基或烷氧基; R 4和R 5各自表示H或烷基; R 6表示烷基，-OR 7或-NR 8 R 9; 并且n是0和3之间的数字（其中R7，R8和R9各自表示H，烷基，芳基，芳烷基，氨基，杂环等）]，以及含有该衍生物或 盐作为活性成分。 本发明化合物对内皮素具有强烈的结合抑制活性，具有强烈的血管收缩作用和细胞增殖作用。 因此，该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。

    Pyrimidine derivatives as endothelin antagonists
    9.
    发明授权
    Pyrimidine derivatives as endothelin antagonists 失效
    嘧啶衍生物作为内皮素拮抗剂

    公开(公告)号：US5883092A

    公开(公告)日：1999-03-16

    申请号：US29244

    申请日：1998-03-04

    申请人： Mitsuteru Hirata ,  Takeo Deushi ,  Yoshio Takahashi ,  Masahiro Tamura ,  Takeshi Ohshima ,  Toshiaki Oda ,  Tetsuya Ishikawa ,  Hiroyuki Sonoki ,  Masami Shiratsuchi

    发明人： Mitsuteru Hirata ,  Takeo Deushi ,  Yoshio Takahashi ,  Masahiro Tamura ,  Takeshi Ohshima ,  Toshiaki Oda ,  Tetsuya Ishikawa ,  Hiroyuki Sonoki ,  Masami Shiratsuchi

    IPC分类号： C07D403/04 ,  A61K31/506 ,  A61P9/00 ,  A61P9/12 ,  C07D213/00 ,  C07D239/52 ,  C07D239/545 ,  C07D295/00 ,  C07D401/14 ,  C07D413/04 ,  A61K31/505 ,  A61K31/535

    CPC分类号： C07D239/52

    摘要： The present invention is directed to a pyrimidine derivative of the following formula (1) or a salt of the derivative: ##STR1## �wherein R.sup.1 represents a hydroxyl group, a lower alkoxy group, a phenyloxy group which may have a substituent, an aralkyloxy group which may have a substituent, or --NR.sup.2 R.sup.3 ; X represents an oxygen atom or N--R.sup.4 ; m is 2 or 3; and n is 1 or 2 (wherein each of R.sup.2 and R.sup.3, which are identical to or different from each other, represents a hydrogen atom, a hydroxyl group, a lower alkyl group which may have a substituent, a phenyl group which may have a substituent, an aralkyl group which may have a substituent, or a heterocyclic group which may have a substituent; R.sup.4 represents a lower alkyl group, a phenyl group, a formyl group, or a lower alkoxycarbonyl group)!, as well as to a medicine containing the derivative or salt as the active ingredient. The compounds exhibit strong binding inhibitory activity against endothelin having potent vasoconstrictive effect. Therefore, the compounds are effective as remedies for various diseases including circulatory diseases.

    摘要翻译： PCT No.PCT / JP96 / 02494 Sec。 371日期：1998年3月4日 102（e）1998年3月4日PCT PCT 1996年9月4日PCT公布。 公开号WO97 / 09318 日期1997年3月13日本发明涉及下式（1）的嘧啶衍生物或衍生物的盐：其中R1表示羟基，低级烷氧基，苯氧基 其可以具有取代基，可以具有取代基的芳烷氧基或-NR2R3; X表示氧原子或N-R4; m为2或3; n为1或2（式中，R2，R3各自相同或不同，表示氢原子，羟基，可具有取代基的低级烷基，可具有取代基的苯基， 取代基，可以具有取代基的芳烷基或可以具有取代基的杂环基; R4表示低级烷基，苯基，甲酰基或低级烷氧基羰基）]以及药物 含有衍生物或盐作为活性成分。 该化合物对具有强烈血管收缩作用的内皮素表现出强烈的结合抑制活性。 因此，该化合物作为包括循环系统疾病在内的各种疾病的治疗方法是有效的。

    Methylmethioninesulfonium compounds, process for their preparation, and pharmaceutical compositions containing them
    10.
    发明授权
    Methylmethioninesulfonium compounds, process for their preparation, and pharmaceutical compositions containing them 失效
    甲基亚氨基锍化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4216225A

    公开(公告)日：1980-08-05

    申请号：US906567

    申请日：1978-05-16

    申请人： Masami Shiratsuchi ,  Kiyoshi Kawamura ,  Hisashi Kunieda ,  Naoki Machida ,  Toshihiro Akashi ,  Masahiko Nagakura

    发明人： Masami Shiratsuchi ,  Kiyoshi Kawamura ,  Hisashi Kunieda ,  Naoki Machida ,  Toshihiro Akashi ,  Masahiko Nagakura

    IPC分类号： A61K31/195 ,  A61K31/16 ,  A61K31/22 ,  A61P1/04 ,  C07C67/00 ,  C07C325/00 ,  C07C381/12 ,  C07D213/82 ,  A61K31/55 ,  A61K31/215

    CPC分类号： C07D213/82

    摘要： Methylmethioninesulfonium compounds of the formula ##STR1## wherein X.crclbar. represents an anion;R.sup.1 represents a hydrogen atom or an acyl group of the formula -COR.sup.3 in which R.sup.3 represents an alkyl group with 1 to 20 carbon atoms, the group --CH.sub.2).sub.2 COOH or the group ##STR2## in which Z represents a direct bond or a methylene or vinylene linkage, Y represents C or N, R.sup.4 represents a member selected from the class consisting of a hydrogen atom, lower alkyl groups, lower alkoxy groups, di-lower-alkylamino groups and a sulfamoyl group, n is a number of 1 to 3, and two or more R.sup.4 groups may be identical or different; andR.sup.2 represents the group --COOR.sup.5 in which R.sup.5 represents a hydrogen atom, an alkyl group with 1 to 5 carbon atoms or a metal- or metal complex-forming moiety, or the group ##STR3## in which R.sup.6 groups may be identical or different, and each represent a hydrogen atom or an alkyl group with 1 to 5 carbon atoms, with the proviso that when R.sup.1 represents a hydrogen atom, R.sup.2 is not --COOH; when R.sup.1 represents a hydrogen atom and R.sup.2 represents --CONH.sub.2, X.crclbar. is not Cl.crclbar.; and when R.sup.1 is --COCH.sub.3 and R.sup.2 is --COOCH.sub.3, X.crclbar. is not I.crclbar..The compounds can be easily prepared from methionine as a starting material by a combination of known unit reactions such as methylsulfonium-forming reaction, acylation, amidation, esterification and metal salt-forming reaction. These compounds are especially useful for treating ulcers.

    摘要翻译： 其中X（ - ）表示阴离子的式“IMAGE”的甲基甲硫氨onium化合物; R 1表示氢原子或式-COR 3的酰基，其中R 3表示具有1至20个碳原子的烷基，基团-CH 2）2 COOH或其中Z表示直接键或基团 亚甲基或亚乙烯基，Y表示C或N，R4表示选自氢原子，低级烷基，低级烷氧基，二低级烷基氨基和氨磺酰基的成员，n为1 至3个，并且两个或更多个R 4基团可以相同或不同; 并且R 2表示其中R 5表示氢原子，具有1至5个碳原子的烷基或金属或金属络合物形成部分的基团-COOR 5或其中R6基团可以相同或不同的基团 并且各自表示氢原子或具有1至5个碳原子的烷基，条件是当R 1表示氢原子时，R 2不是-COOH; 当R 1表示氢原子且R 2表示-CONH 2时，X（ - ）不是Cl（ - ）; 当R1是-COCH3且R2是-COOCH3时，X（ - ）不是I（ - ）。 通过已知的单元反应如甲基锍形成反应，酰化，酰胺化，酯化和金属盐形成反应的组合，可以容易地从甲硫氨酸作为原料制备化合物。 这些化合物特别适用于治疗溃疡。