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    Pyridine derivatives
    1.
    发明授权
    Pyridine derivatives 失效

    公开(公告)号：US4317828A

    公开(公告)日：1982-03-02

    申请号：US233703

    申请日：1981-02-12

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Masaki Hayashi

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Masaki Hayashi

    IPC分类号： C07D213/18 ,  C07D213/30 ,  C07D213/48 ,  C07D213/55 ,  C07D213/57 ,  A61K31/435

    CPC分类号： C07D213/30 ,  C07D213/18 ,  C07D213/48 ,  C07D213/55 ,  C07D213/57 ,  Y10S514/826

    摘要： The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, E represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbon atoms, the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.1 represents a hydroxy group, or a grouping of the formula: --COOR.sup.4 or --COSR.sup.4, in which R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl group unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R.sup.5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R.sup.1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents in the prevention and treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death.

    Pyridine derivatives
    3.
    发明授权
    Pyridine derivatives 失效

    公开(公告)号：US4271170A

    公开(公告)日：1981-06-02

    申请号：US105672

    申请日：1979-12-20

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Masaki Hayashi

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Masaki Hayashi

    IPC分类号： C07D213/18 ,  C07D213/30 ,  C07D213/48 ,  C07D213/55 ,  C07D213/57 ,  A61K31/44 ,  C07D409/06

    CPC分类号： C07D213/30 ,  C07D213/18 ,  C07D213/48 ,  C07D213/55 ,  C07D213/57 ,  Y10S514/826

    摘要： The pyridine derivatives of the general formula: ##STR1## [wherein A represents an alkylene group containing from 1 to 5 carbon atoms unsubstituted or substituted by a hydroxy group, B represents a single bond, or an oxygen or sulphur atom, or an alkylene group containing from 1 to 5 carbon atoms, D represents a single bond, or an alkylene group containing from 1 to 5 carbon atoms, R represents a grouping of the formula: ##STR2## (in which R.sup.6 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms), Z represents a single bond, or an ethynylene group, or a grouping of the formula: ##STR3## in which R.sup.2 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a hydrogen, bromine or chlorine atom, or an alkyl group containing from 1 to 4 carbom atoms; the symbol represents a single or double bond, the carbon atom attached to R.sup.2 binds to B, and the carbon atom attached to R.sup.3 binds to D, R.sup.1 represents a hydroxy group, or a grouping of the formula: --COOR.sup.4 or --COSR.sup.4, in which R.sup.4 represents a hydrogen atom, or an alkyl group containing from 1 to 12 carbon atoms, or an aralkyl group containing from 7 to 13 carbon atoms, or a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 4 carbon atoms, or a phenyl unsubstituted or substituted by at least one halogen atom, trifluoromethyl group, alkyl or alkoxy or alkylthio group containing from 1 to 4 carbon atoms, nitro or phenyl group, R.sup.5 represents a hydrogen atom, or an alkyl group containing from 1 to 4 carbon atoms, with the proviso that, when B represents an oxygen or sulphur atom, Z represents a single bond and D represents an alkylene group containing from 1 to 5 carbon atoms], and non-toxic acid addition salts thereof and, when R.sup.1 represents a carboxy or thiocarboxy group, non-toxic salts thereof, possess a strong inhibitory activity on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents in the prevention or treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, myocardial infarction, cardiostenosis, cerebral infarction and acute cardiac death.

    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
    4.
    发明授权
    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient 失效
    罗丹宁衍生物，其制备方法和含有绕丹宁衍生物作为活性成分的醛糖还原酶抑制剂

    公开(公告)号：US4464382A

    公开(公告)日：1984-08-07

    申请号：US292076

    申请日：1981-08-12

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    IPC分类号： C12N9/99 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/08 ,  A61P27/02 ,  A61P27/12 ,  A61P43/00 ,  C07D277/20 ,  C07D277/36 ,  C07D333/00 ,  C07D417/06 ,  C07D417/14

    CPC分类号： C07D277/20

    摘要： The rhodanine derivatives of the general formula: ##STR1## wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted, (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted (5) a ##STR2## group (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## group; or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted; and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted, possess a strong inhibitory activity on aldose reductase.

    摘要翻译： 通式：（I）的绕丹宁衍生物其中（I）R 1和R 2一起表示四亚甲基或五亚甲基; （II）R1表示氢原子，R2表示（1）未被取代或被至少一个1-4个碳原子的烷基取代的4-7个碳原子的环烷基或环烯基，（2）蒽基或 萘基，（3）未取代或取代的苯基，（4）含有未取代或取代的氮，氧和硫原子中的至少一个的杂环基（5）基团（其中R 4表示 氢原子，卤素原子，苯基或1-5个碳原子的烷基; R5表示氢原子，苯基或1-5个碳原子的烷基）或基团; 或（III）可以相同或不同的R 1和R 2各自表示未取代或取代的苯基; 并且R 3表示氢原子，1-12个碳原子的烷基，7-13个碳原子的芳烷基，4-7个碳原子的环烷基或环烯基，其未被取代或被至少一个烷基 1-4个碳原子或未取代或取代的苯基对醛糖还原酶具有强烈的抑制活性。

    Carboxy-imidazole derivatives, compositions and use
    5.
    发明授权
    Carboxy-imidazole derivatives, compositions and use 失效
    羧基咪唑衍生物，组合物和用途

    公开(公告)号：US4346099A

    公开(公告)日：1982-08-24

    申请号：US304531

    申请日：1981-09-22

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Takanori Okada ,  Masaki Hayashi

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Takanori Okada ,  Masaki Hayashi

    IPC分类号： C07D521/00 ,  A61K31/415

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The imidazole derivatives of the general formula: ##STR1## [wherein m represents an integer of 4 to 9, R.sup.1 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, and one of R.sup.2 and R.sup.3 represents a hydrogen atom, and the other represents a halogen atom or a phenyl group, or R.sup.2 and R.sup.3 together represent --(CH.sub.2).sub.n --(in which n represents an integer of 4 to 6) or represent .dbd.CH.sub.2 ] and non-toxic salts thereof, which have a specifically inhibitory effect on the biosynthesis of thromboxane A.sub.2 (abbreviated as TXA.sub.2 hereafter) and are, therefore, useful as treating agents for diseases caused by TXA.sub.2 such as inflammation, cerebral apoplexy, myocardial infarction, acute cardiac death, cardiostenosis and thrombus etc.

    摘要翻译： 具有下式的咪唑衍生物：其中m表示4至9的整数，R 1表示氢原子或含有1至12个碳原子的直链或支链烷基，一个 R 2和R 3表示氢原子，另一个表示卤素原子或苯基，或者R 2和R 3一起表示 - （CH 2）n - （其中n表示4〜6的整数）或表示= CH 2] 它们对凝血恶烷A2（以下简称TXA2）的生物合成具有特异性抑制作用，因此可用作TXA2引起的疾病如炎症，脑中风，心肌梗死，急性 心源性死亡，心脏病和血栓等。

    1-Substituted imidazoles for inhibition of thromboxane synthetase
    6.
    发明授权
    1-Substituted imidazoles for inhibition of thromboxane synthetase 失效
    1-取代的咪唑用于抑制血栓素合成酶

    公开(公告)号：US4256757A

    公开(公告)日：1981-03-17

    申请号：US35181

    申请日：1979-05-02

    申请人： Masaki Hayashi ,  Tadao Tanouchi ,  Masanori Kawamura ,  Ikuo Kajiwara

    发明人： Masaki Hayashi ,  Tadao Tanouchi ,  Masanori Kawamura ,  Ikuo Kajiwara

    IPC分类号： C07D233/60 ,  A61K31/415 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/12 ,  A61P29/00 ,  C07C29/10 ,  C07D309/12

    CPC分类号： C07C29/10 ,  C07D309/12

    摘要： The imidazole derivatives of the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, the symbol .dbd. represents a double bond that bond is E or Z, or a triple bond, and m and n, which may be the same or different, each represent zero, or an integer of 1 to 10, and non-toxic acid addition salts thereof, and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof are new compounds. These compounds have a strong inhibitory effect on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy and asthma.

    摘要翻译： 通式为：其中R 1表示氢原子或含有1至12个碳原子的直链或支链烷基的咪唑衍生物，符号=表示键为E的双键或 Z或三键，m和n可以相同或不同，分别表示0或1-10的整数，以及无毒的酸加成盐，当R 1表示氢原子时， 其无毒盐是新化合物。 这些化合物对来自兔血小板微粒体的血栓素合成酶具有强烈的抑制作用，并且可用作炎症，高血压，血栓，脑中风和哮喘的治疗活性剂。

    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient
    7.
    发明授权
    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredient 失效
    罗丹宁衍生物，其制备方法和含有绕丹宁衍生物作为活性成分的醛糖还原酶抑制剂

    公开(公告)号：US4831045A

    公开(公告)日：1989-05-16

    申请号：US96091

    申请日：1987-09-10

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    IPC分类号： C12N9/99 ,  A61K31/425 ,  A61K31/426 ,  A61K31/44 ,  A61P3/08 ,  A61P27/02 ,  A61P27/12 ,  A61P43/00 ,  C07D277/20 ,  C07D277/36 ,  C07D333/00 ,  C07D417/06 ,  C07D417/14

    CPC分类号： C07D277/20

    摘要： The rhodanine derivatives of the general formula: ##STR1## [wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted by at least one of (a) halogen atom, (b) trifluoromethyl group, (c) hydroxyl group, (d) nitro group, (e) carboxyl group, (f) amino group which may be substituted by alkyl group(s) of 1-4 carbon atoms, (g) alkyl, alkoxy or alkylthio group of 1-5 carbon atoms, (h) phenyl group, (i) heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of the above-described substituents (a) to (h), and (j) alkyl group of 1-4 carbon atoms which is substituted by at least one of the above-described substituents (c), (h) and (i), (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of oxo group and the above-described substituents (a) to (h) and (j), or (5) a ##STR2## (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j); and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j)] and, when R.sup.3 represents a hydrogen atom, non-toxic salts of the acids possess a strong inhibitory activity on aldose reductase, and are useful for the prevention and treatment of nerve disturbances such as neuralgia, retinopathy, diabetic cataract and renal disturbances such as tubular nephropathy.

    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredients
    8.
    发明授权
    Rhodanine derivatives, process for their preparation, and aldose reductase inhibitor containing the rhodanine derivatives as active ingredients 失效

    公开(公告)号：US4791126A

    公开(公告)日：1988-12-13

    申请号：US96808

    申请日：1987-09-10

    申请人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    发明人： Tadao Tanouchi ,  Masanori Kawamura ,  Akio Ajima ,  Tetsuya Mohri ,  Masaki Hayashi ,  Hiroshi Terashima ,  Fumio Hirata ,  Takeshi Morimura

    IPC分类号： C07D277/20 ,  C07D277/36 ,  A61K31/425

    CPC分类号： C07D277/20

    摘要： The rhodanine derivatives of the general formula: ##STR1## [wherein (I) R.sup.1 and R.sup.2 are taken together to represent a tetramethylene or pentamethylene group; (II) R.sup.1 represents a hydrogen atom, and R.sup.2 represents (1) a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, (2) an anthryl or naphthyl group, (3) a phenyl group which is unsubstituted or substituted by at least one of (a) halogen atom, (b) trifluoromethyl group, (c) hydroxyl group, (d) nitro group, (e) carboxyl group, (f) amino group which may be substituted by alkyl group(s) of 1-4 carbon atoms, (g) alkyl, alkoxy or alkylthio group of 1-5 carbon atoms, (h) phenyl group, (i) heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of the above-described substituents (a) to (h), and (j) alkyl group of 1-4 carbon atoms which is substituted by at least one of the above-described substituents (c), (h) and (i), (4) a heterocyclic group containing at least one of nitrogen, oxygen and sulfur atoms which is unsubstituted or substituted by at least one of oxo group and the above-described substituents (a) to (h) and (j), or (5) a ##STR2## group (wherein R.sup.4 represents a hydrogen atom, a halogen atom, phenyl group or an alkyl group of 1-5 carbon atoms; and R.sup.5 represents a hydrogen atom, a phenyl group or an alkyl group of 1-5 carbon atoms) or ##STR3## group; or (III) R.sup.1 and R.sup.2, which may be the same or different with each other, each represents a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j); and R.sup.3 represents a hydrogen atom, an alkyl group of 1-12 carbon atoms, an aralkyl group of 7-13 carbon atoms, a cycloalkyl or cycloalkenyl group of 4-7 carbon atoms which is unsubstituted or substituted by at least one alkyl group of 1-4 carbon atoms, or a phenyl group which is unsubstituted or substituted by at least one of the above-described substituents (a) to (j)] and, when R.sup.3 represents hydrogen atom, non-toxic salts of the acids possess a strong inhibitory activity on aldose reductase, and are useful for the prevention and treatment of nerve disturbances such as neuralgia, retinopathy, diabetic cataract and renal disturbances such as tubular nephropathy.

    1-Substituted imidazole derivatives
    10.
    发明授权
    1-Substituted imidazole derivatives 失效
    1-取代的咪唑衍生物

    公开(公告)号：US4355170A

    公开(公告)日：1982-10-19

    申请号：US35180

    申请日：1979-05-02

    申请人： Masaki Hayashi ,  Tadao Tanouchi ,  Masanori Kawamura ,  Yoichi Iguchi

    发明人： Masaki Hayashi ,  Tadao Tanouchi ,  Masanori Kawamura ,  Yoichi Iguchi

    IPC分类号： A61K31/415 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P29/00 ,  A61P43/00 ,  C07C29/10 ,  C07D233/60 ,  C07D309/12

    CPC分类号： C07D309/12 ,  C07C29/10

    摘要： The imidazole derivatives of the general formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 4 carbon atoms, R.sup.3 represents a straight- or branched-chain alkyl group containing from 1 to 10 carbon atoms, and m and n, which may be the same or different, each represent zero, or an integer of 1 to 10, and non-toxic acid addition salts thereof, and, when R.sup.1 represents a hydrogen atom, non-toxic salts thereof, are new compounds. These compounds have a strong inhibitory effect on thromboxane synthetase from rabbit platelet microsomes, and are useful as therapeutically active agents for inflammation, hypertension, thrombus, cerebral apoplexy and asthma.

    摘要翻译： 通式为：其中R 1表示氢原子，或含有1至12个碳原子的直链或支链烷基，R 2表示氢原子或直链或支链的咪唑衍生物 含有1至4个碳原子的链烷基，R 3表示含有1至10个碳原子的直链或支链烷基，m和n可以相同或不同，各自表示0，或 1〜10的整数，无毒性的酸加成盐，当R1表示氢原子时，其无毒性盐为新化合物。 这些化合物对来自兔血小板微粒体的血栓素合成酶具有强烈的抑制作用，并且可用作炎症，高血压，血栓，脑中风和哮喘的治疗活性剂。