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    Glycine derivative monosodium salt tetrahydrate
    1.
    发明授权
    Glycine derivative monosodium salt tetrahydrate 失效
    甘氨酸衍生物单钠盐四水合物

    公开(公告)号：US5359121A

    公开(公告)日：1994-10-25

    申请号：US182366

    申请日：1994-01-18

    申请人： Katsuhiro Imaki ,  Hirohisa Wakatsuka

    发明人： Katsuhiro Imaki ,  Hirohisa Wakatsuka

    IPC分类号： C07C311/29 ,  C07C311/15

    CPC分类号： C07C311/29

    摘要： N-[o-(p-pivaloyloxybenzenesulfonylamino)benzoyl]glycine monosodium salt tetrahydrate of the formula (I): ##STR1## is non-hygroscopic, homogeneous and stable compound, and has an inhibitory effect on elastase. Accordingly, the compound may be useful for the treatment and/or prevention of diseases induced by the abnormal enhancing of degradation of elastin, collagen fiber and/or proteoglican by the action of elastase, e.g., pulmonary emphysema, atherosclerosis, rheumatoid arthritis, etc.

    摘要翻译： 式（I）的N- [对 - （对 - 新戊酰氧基苯磺酰基氨基）苯甲酰基]甘氨酸四钠水合物：（I）是不吸湿，均相和稳定的化合物，对弹性蛋白酶具有抑制作用。 因此，该化合物可用于治疗和/或预防由弹性蛋白酶（例如肺气肿，动脉粥样硬化，类风湿性关节炎等）的弹性蛋白，胶原纤维和/或蛋白多糖的异常增强引起的疾病的治疗和/或预防。

    3-phenoxy (or phenylthia) cyclopentanecarbonylamino acid analogues
    2.
    发明授权
    3-phenoxy (or phenylthia) cyclopentanecarbonylamino acid analogues 失效
    3-苯氧基（或苯基硫）环戊烷羰基氨基酸类似物

    公开(公告)号：US4888351A

    公开(公告)日：1989-12-19

    申请号：US268623

    申请日：1988-11-07

    申请人： Katsuhiro Imaki ,  Tadao Okegawa ,  Yoshinobu Arai

    发明人： Katsuhiro Imaki ,  Tadao Okegawa ,  Yoshinobu Arai

    IPC分类号： A61K31/195 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61P7/10 ,  A61P25/00 ,  C07C67/00 ,  C07C235/40 ,  C07C313/00 ,  C07C323/61 ,  C07D307/46 ,  C07D307/80 ,  C07D333/22

    CPC分类号： C07D333/22

    摘要： This invention relates to compounds presented by the general formula: ##STR1## [wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each)), R.sup.3 represents hydrogen, halogen, alkyl group or two of R.sup.3 and phenyl to which two of R.sup.3 are linked, together represent naphthyl of the formula: ##STR4## (wherein R.sup.10 represents hydrogen, halogen or alkyl), with the proviso that when R.sup.1 represents hydrogen, the atom may be replaced by R.sup.3, and n represents 1 to 3, with the proviso that when n represents two or more, plural R.sup.3 s may be different each, X represents oxygen or sulfur and R.sup.4 represents amino acid-residue], or a non-toxic salt thereof, and methods for their preparation and treating agents for cerebral edema containing them as active ingredients.

    Prostaglandin E.sub.1 analogues
    4.
    发明授权
    Prostaglandin E.sub.1 analogues 失效
    前列腺素E1类似物

    公开(公告)号：US4473587A

    公开(公告)日：1984-09-25

    申请号：US515909

    申请日：1983-07-21

    申请人： Takashi Muryobayashi ,  Katsuhiro Imaki ,  Yoshiki Sakai

    发明人： Takashi Muryobayashi ,  Katsuhiro Imaki ,  Yoshiki Sakai

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P1/16 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C07D307/937 ,  C08B37/00 ,  C07C177/00 ,  C07C49/653

    CPC分类号： C07D307/937 ,  C07C405/0025 ,  C08B37/0015

    摘要： Prostaglandin E.sub.1 analogues of the general formula: ##STR1## (wherein R.sup.1 represents a single bond or a straight- or branched-chain alkylene group of from 1 to 5 carbon atom(s), R.sup.2 represents a cycloalkyl group of from 4 to 7 carbon atoms either unsubstituted or substituted by at least one straight- or branched-chain alkyl group of from 1 to 8 carbon(s), and the double bond between C.sub.13 and C.sub.14 is trans) and cyclodextrin clathrate thereof, are useful in the prevention or treatment of cytodamage associated with digestive system disease, especially liver damage.

    摘要翻译： 前列腺素E1类似物，通式如下：＆lt; IMAGE＆gt;（其中R 1表示单键或1〜5个碳原子的直链或支链亚烷基，R 2表示4〜7个碳原子的环烷基 原子是未取代的或被至少一个1至8个碳原子的直链或支链烷基取代，C13和C14之间的双键是反式）和环糊精包合物可用于预防或治疗 与消化系统疾病相关的细胞损伤，特别是肝损伤。

    Treatment of diseases caused by abnormal action of elastase
    5.
    发明授权
    Treatment of diseases caused by abnormal action of elastase 失效
    治疗由弹性蛋白酶异常作用引起的疾病

    公开(公告)号：US4975464A

    公开(公告)日：1990-12-04

    申请号：US337812

    申请日：1989-04-14

    申请人： Katsuhiro Imaki ,  Yoshinobu Arai ,  Hiroyuki Ohno

    发明人： Katsuhiro Imaki ,  Yoshinobu Arai ,  Hiroyuki Ohno

    IPC分类号： A61K31/255 ,  C07C279/18 ,  C07C309/63 ,  C07C309/65 ,  C07C309/66 ,  C07C311/00 ,  C07C311/08 ,  C07C311/29 ,  C07C311/46 ,  C07C327/16 ,  C07C329/10 ,  C07D213/65 ,  C07D213/75 ,  C07D277/04 ,  C07D277/22 ,  C07D295/26 ,  C07D521/00 ,  A61K31/24

    CPC分类号： C07D213/75 ,  C07C279/18 ,  C07C309/65 ,  C07C309/66 ,  C07C311/08 ,  C07C311/29 ,  C07C311/46 ,  C07C329/10 ,  C07D213/65 ,  C07D277/04 ,  C07D277/22 ,  C07D295/26

    摘要： Compounds presented by the general formula: ##STR1## wherein Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --OCONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --COHN-- SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each or R.sup.2 may be the same group or the different group and acid addition salts thereof have inhibitory effect on elastase, and, therefore, are useful for the treatment and/or prevention of diseases induced by abnormal enhancing of degradation of proteins such as elastin and the like, by the action of elastase in mammals, especially in human beings.

    摘要翻译： 由以下通式表示的化合物：其中Y是氧，R2是H，烷基，烷氧基，烷氧基甲基，-COOR3，-CH2COOR3，-CH = CH-COOR3，卤素，-CF3，-COR4， - OCOR4，-CH2OCOR4，-SO2R4，-OSO2R4，-CONR5R6，-OCONR5R6，-SO2NR5R6，-COHN-SO2NR5R6，-NHSO2R7，-NO2，-OH，-CH2OH，胍基，苄氧基，胍基苯硫基甲基，吗啉代磺酰基苯氧基甲基，吡啶氧基甲基或（1 ，1-二氧代噻唑-3-基）羰基，或当Y为硫时，R 2为H，烷基，烷氧基，卤素，-COOR 3，-CH 2 COOR 3，-NO 2或-SO 2 NR 5 R 6，n为1至5的整数， 当n表示2以上时，各个或R2可以是相同的基团，也可以是不同的基团，其酸加成盐对弹性蛋白酶具有抑制作用，因此可用于治疗和/或预防由异常增强引起的疾病 蛋白质如弹性蛋白等的降解，通过弹性蛋白酶在哺乳动物，特别是人类中的作用。

    Derivatives of p-guantidinobenzoic acid and pharmaceutical agents containing them as active ingredient
    7.
    发明授权
    Derivatives of p-guantidinobenzoic acid and pharmaceutical agents containing them as active ingredient 失效
    对胍丁基苯甲酸的衍生物和含有它们作为活性成分的药剂

    公开(公告)号：US4843094A

    公开(公告)日：1989-06-27

    申请号：US929317

    申请日：1986-11-12

    申请人： Katsuhiro Imaki ,  Yoshinobu Arai ,  Hiroyuki Ohno

    发明人： Katsuhiro Imaki ,  Yoshinobu Arai ,  Hiroyuki Ohno

    IPC分类号： C07C279/18 ,  C07C309/65 ,  C07C309/66 ,  C07C311/08 ,  C07C311/29 ,  C07C311/46 ,  C07C329/10 ,  C07D213/65 ,  C07D213/75 ,  C07D277/04 ,  C07D277/22 ,  C07D295/26

    CPC分类号： C07D213/75 ,  C07C279/18 ,  C07C309/65 ,  C07C309/66 ,  C07C311/08 ,  C07C311/29 ,  C07C311/46 ,  C07C329/10 ,  C07D213/65 ,  C07D277/04 ,  C07D277/22 ,  C07D295/26

    摘要： Compounds presented by the general formula: ##STR1## [wherein when Y is oxygen, R.sup.2 is H, alkyl, alkoxy, alkoxymethyl, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --CH.dbd.CH--COOR.sup.3, halogen, --CF.sub.3, --COR.sup.4, --OCOR.sup.4, --CH.sub.2 OCOR.sup.4, --SO.sub.2 R.sup.4, --OSO.sub.2 R.sup.4, --CONR.sup.5 R.sup.6, --SO.sub.2 NR.sup.5 R.sup.6, --CONH--SO.sub.2 NR.sup.5 R.sup.6, --NHSO.sub.2 R.sup.7, --NO.sub.2, --OH, --CH.sub.2 OH, guanidino, benzyloxy, guanidinophenylthiomethyl, morpholinosulfonylphenoxymethyl, pyridyloxymethyl, or (1,1-dioxothiazol-3-yl)carbonyl, or when Y is sulfur, R.sup.2 is H, alkyl, alkoxy, halogen, --COOR.sup.3, --CH.sub.2 COOR.sup.3, --NO.sub.2, or --SO.sub.2 NR.sup.5 R.sup.6, and n represents an integer of one to five, and when n represents more than two, each of R.sup.2 may be the same group or the different group.] and acid addition salts thereof have inhibitory effect on elastase, and, therefore, are useful for the treatment and/or prevention of diseases induced by abnormal enhancing of degradation of proteins such as elastin and the like, by the action of elastase in mammals, especially in human beings.

    摘要翻译： 由以下通式表示的化合物：其中当Y为氧时，R 2为H，烷基，烷氧基，烷氧基甲基，-COOR 3，-CH 2 COOR 3，-CH = CH-COOR 3，卤素，-CF 3，-COR 4 ，-OCOR4，-CH2OCOR4，-SO2R4，-OSO2R4，-CONR5R6，-SO2NR5R6，-CONH-SO2NR5R6，-NHSO2R7，-NO2，-OH，-CH2OH，胍基，苄氧基，胍基苯硫基甲基，吗啉代磺酰基苯氧基甲基，吡啶氧基甲基，或（1， 或者当Y为硫时，R 2为H，烷基，烷氧基，卤素，-COOR 3，-CH 2 COOR 3，-NO 2或-SO 2 NR 5 R 6，n为1〜5的整数， 当n表示两个以上时，R2各自可以是相同的基团或不同的基团。]及其酸加成盐对弹性蛋白酶具有抑制作用，因此可用于治疗和/或预防由异常引起的疾病 通过弹性蛋白酶在哺乳动物，特别是人类中的作用，增强蛋白质如弹性蛋白等的降解。

    3-phenoxy (or phenylthio)--cyclopentanecarbonylamino acid analogues
    8.
    发明授权
    3-phenoxy (or phenylthio)--cyclopentanecarbonylamino acid analogues 失效
    3-苯氧基（或苯硫基） - 环戊烷羰基氨基酸类似物

    公开(公告)号：US4829078A

    公开(公告)日：1989-05-09

    申请号：US158457

    申请日：1988-02-22

    申请人： Katsuhiro Imaki ,  Tadao Okegawa ,  Yoshinobu Arai

    发明人： Katsuhiro Imaki ,  Tadao Okegawa ,  Yoshinobu Arai

    IPC分类号： A61K31/195 ,  A61K31/34 ,  A61K31/341 ,  A61K31/343 ,  A61K31/38 ,  A61K31/381 ,  A61P7/10 ,  A61P25/00 ,  C07C67/00 ,  C07C235/40 ,  C07C313/00 ,  C07C323/61 ,  C07D307/46 ,  C07D307/80 ,  C07D333/22

    CPC分类号： C07D333/22

    摘要： This invention relates to compounds presented by the general formula: ##STR1## [wherein R.sup.1 and R.sup.2 are: (i) R.sup.1, R.sup.2 and carbon atoms to which R.sup.1 and R.sup.2 are linked, together represent the group of the general formula: ##STR2## (wherein R.sup.5 and R.sup.6 represent hydrogen, alkyl, cycloalkyl, cycloalkyl-alkyl or phenyl, independently, with the proviso that R.sup.5 and R.sup.6 is not hydrogen atoms at the same time), or(ii) R.sup.1 represents hydrogen and R.sup.2 represents the group of the formula: --COR.sup.7 (wherein R.sup.7 represents the group of the formula: ##STR3## (wherein Y represents a single-bond, alkylene, alkenylene, W represents oxygen or sulfur, m represents 1 to 3, R.sup.8 represents hydrogen, halogen, nitro, hydroxy, alkyl or alkoxy, with the proviso that when m represents two or more, plural R.sup.8 s may be different each, and R.sup.9 represents hydrogen, alkyl or phenyl group, with the proviso that two of R.sup.9 may be different each)), R.sup.3 represents hydrogen, halogen, alkyl group or two of R.sup.3 and phenyl to which two of R.sup.3 are linked, together represent naphthyl of the formula: ##STR4## (wherein R.sup.10 represents hydrogen, halogen or alkyl), with the proviso that when R.sup.1 represents hydrogen, the atom may be replaced by R.sup.3, and n represents 1 to 3, with the proviso that when n represents two or more, plural R.sup.3 s may be different each, X represents oxygen or sulfur and R.sup.4 represents amino acid-residue], or a non-toxic salt thereof, and methods for their preparation and treating agents for cerebral edema containing them as active ingredients.