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4 条记录 (耗时 0.013 秒)

    Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it
    1.
    发明授权
    Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it 失效
    噻唑并[3,2-a]嘧啶的衍生物及其制备方法和含有它的药物

    公开(公告)号：US4383996A

    公开(公告)日：1983-05-17

    申请号：US339460

    申请日：1981-12-28

    申请人： Takeo Oba ,  Kiyoshi Bannai ,  Toshio Tanaka ,  Kenzo Watanabe ,  Tatsuyuki Naruchi ,  Keiji Komoriya ,  Seizi Kurozumi ,  Kenji Hoshina

    发明人： Takeo Oba ,  Kiyoshi Bannai ,  Toshio Tanaka ,  Kenzo Watanabe ,  Tatsuyuki Naruchi ,  Keiji Komoriya ,  Seizi Kurozumi ,  Kenji Hoshina

    IPC分类号： C07D513/04 ,  A61K31/505

    CPC分类号： C07D513/04 ,  Y10S514/825 ,  Y10S514/885

    摘要： A derivative of thiazolo [3,2-a] pyrimidine expressed by formula (I) ##STR1## (where R indicates a phenyl group or a benzyl group which has a halogen atom, a lower alkyl or lower alkyloxy group as a substituent group, an alicyclic group or an arylethyl group), and a process for the preparation of a compound of formula (I) comprising cyclizing a compound expressed by formula (II) by application of heat ##STR2## (where a definition of R is as same as that given in case of formula (I) and R' indicates a halogen atom or lower alkyloxy group). A drug which contains this compound as active ingredient is useful for curing autoimmune diseases such as rheumatoid arthritis, nephritis, etc.

    摘要翻译： PCT No.PCT / JP80 / 00090 Sec。 371日期：1981年12月28日 102（e）日期1981年12月28日PCT提交1980年4月28日PCT公布。 公开号WO81 / 03174 1981年11月12日，由式（I）表示的噻唑并[3,2-a]嘧啶衍生物（I）（其中R表示苯基或具有卤素原子的苄基，较低 烷基或低级烷氧基作为取代基，脂环基或芳乙基），以及制备式（I）化合物的方法，其包括使式（II）表示的化合物通过加热 （II）（其中R的定义与式（I）的情况相同，R'表示卤素原子或低级烷氧基）。 含有该化合物作为活性成分的药物可用于治疗自身免疫性疾病如类风湿性关节炎，肾炎等。

    Aminocarboxylic acids, amino alcohols, or the derivatives thereof, processes for production thereof, and pharmaceutical uses thereof
    3.
    发明授权
    Aminocarboxylic acids, amino alcohols, or the derivatives thereof, processes for production thereof, and pharmaceutical uses thereof 失效

    公开(公告)号：US4402975A

    公开(公告)日：1983-09-06

    申请号：US284562

    申请日：1981-07-17

    申请人： Toru Takeshita ,  Kenji Hoshina ,  Akira Ohtsu ,  Tatsuyuki Naruchi

    发明人： Toru Takeshita ,  Kenji Hoshina ,  Akira Ohtsu ,  Tatsuyuki Naruchi

    IPC分类号： A61K31/135 ,  A61K31/195 ,  A61K31/24 ,  C07D295/18 ,  C07C101/34

    CPC分类号： C07C229/34 ,  A61K31/135 ,  C07C225/18 ,  C07C233/51 ,  C07C2101/14 ,  Y10S514/927 ,  Y10S514/928

    摘要： A compound represented by the following formula ##STR1## wherein R.sup.1 represents a hydrogen atom, an acyl group or an alkoxycarbonyl group; X.sup.1 represents an alkylene group having 3 to 6 carbon atoms, a 1,4-cyclohexylene group, or a 1,4-phenylene group, the alkylene group may be substituted by an alkyl group having 1 to 6 carbon atoms, and the 1,4-phenylene group may be substituted by 1 or 2 substituents selected from halogen atoms and alkoxy groups having 1 to 6 carbon atoms; R.sup.2 represents a hydrogen atom or a hydroxyl group and R.sup.3 represents hydrogen atom, or R.sup.2 and R.sup.3 together may form an oxo group (.dbd.O), and when X.sup.1 is other than the 1,4-phenylene group, R.sup.2 represents a hydrogen atom and R.sup.3 represents a bond between the carbon atoms to which R.sup.3 is bonded and that carbon atom of X.sup.1 which is adjacent to said carbon atom; X.sup.2 represents an alkylene group having 1 to 5 carbon atoms which may be substituted by an alkyl group having 1 to 6 carbon atoms or an amino group; and R.sup.4 represents the group --COOR.sup.5, --CH.sub.2 OR.sup.6 or --CONR.sup.7 R.sup.8 in which R.sup.5 represents a hydrogen atom or an alkyl group having 1 to 6 carbon atoms, R.sup.6 represents a hydrogen atom or an acyl group having 1 to 6 carbon atoms, and R.sup.7 and R are identical or different and represent a hydrogen atom or an alkyl group having 1 to 6 carbon atoms or taken together may form a 5- or 6-membered ring; or an acid addition salts of said compound wherein R.sup.1 represents a hydrogen atom or X.sup.2 represents an alkylene group having an amino group, or salts of said compound wherein R.sup.5 represents a hydrogen atom.The compounds represented by the above formula or their pharmaceutically acceptable salts are useful as anti-ulcer agents.The present invention also provides a process for producing the compounds or their pharmaceutically acceptable salts, which comprises acylating a protected derivative at the amino group of a corresponding acid halide with a corresponding substituted benzene in the presence of a Lewis acid; or reducing a corresponding compound in the presence of an inert solvent under conditions which induce reduction of the carbonyl group of said corresponding compound without substantially reducing the phenylene group of said corresponding compound; or dehydrating a corresponding compound.

    Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient
    4.
    发明授权
    Fused pyrimidine derivative, process for preparation of same and pharmaceutical preparation comprising same as active ingredient 失效
    熔融嘧啶衍生物，其制备方法和包含与活性成分相同的药物制剂

    公开(公告)号：US5378700A

    公开(公告)日：1995-01-03

    申请号：US839769

    申请日：1992-06-09

    申请人： Yasuji Sakuma ,  Masaichi Hasegawa ,  Kenichiro Kataoka ,  Kenji Hoshina ,  Noboru Yamazaki ,  Takashi Kadota ,  Hisao Yamaguchi

    发明人： Yasuji Sakuma ,  Masaichi Hasegawa ,  Kenichiro Kataoka ,  Kenji Hoshina ,  Noboru Yamazaki ,  Takashi Kadota ,  Hisao Yamaguchi

    IPC分类号： A61K31/505 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55 ,  C07D471/04 ,  C07D487/04

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Disclosed is a fused pyrimidine of the formula [I] ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined in the specification, Y represents a linking group of the formula ##STR2## wherein n is an integer of from 4 to 6, ##STR3## wherein A is a hydrogen atom or alkyl group; and Z represents a hydrogen atom, or other substituents; or Y and Z together represent an unsubstituted or substituted alkyl, alkenyl or arylalkyl group; or a 5- to 7-member heterocyclic ring which has a nitrogen atom, and further, an oxygen or sulfur atom as a hetero atom other than the nitrogen atom, being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I), a 5- to 7-member unsaturated heterocyclic ring which has 1 to 3 nitrogen atoms being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I), or a fused biheterocyclic ring constructed with 5- or 6-membered aromatic or non-aromatic rings, which has 1 to 3 nitrogen atoms in any position, being bonded via the nitrogen atom therein to the 4-position of the pyrimidine ring of the formula (I); andm is an integer of from 1 to 3;and a pharmaceutically acceptable acid addition salt thereof, as well as a process for producing same and a pharmaceutical preparation useful for a treatment of hypoxemia associated with respiratory diseases.

    摘要翻译： PCT No.PCT / JP90 / 01313 Sec。 371日期：1992年6月9日 102（e）日期1992年6月9日PCT提交1990年10月11日PCT公布。 出版物WO91 / 05784 日期：1991年5月2日。公开是式[I]的融合嘧啶其中R 1，R 2和R 3如说明书中所定义，Y表示式的连接基团，其中n 是4至6的整数，其中A是氢原子或烷基; O（S） Z表示氢原子或其它取代基; 或Y和Z一起表示未取代或取代的烷基，烯基或芳基烷基; 或具有氮原子的5-至7-元杂环，以及作为氮原子以外的杂原子的氧或硫原子通过氮原子键合到嘧啶环的4-位上 式（I）的通式（I）中的氮原子数为1〜3的5〜7元不饱和杂环与式（I）的嘧啶环的4-位连接， 在其中具有1至3个氮原子的5-或6-元芳族或非芳族环经由其中的氮原子键合到式（I）的嘧啶环的4-位上构成的双杂环， ; m为1〜3的整数， 和其药学上可接受的酸加成盐，以及其制备方法和用于治疗与呼吸系统疾病相关的低氧血症的药物制剂。