利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

46 条记录 (耗时 0.02 秒)

    6-keto-prostaglandin E.sub.1 derivatives
    1.
    发明授权
    6-keto-prostaglandin E.sub.1 derivatives 失效
    6-酮前列腺素E1衍生物

    公开(公告)号：US4783480A

    公开(公告)日：1988-11-08

    申请号：US7657

    申请日：1987-01-28

    申请人： Hirohisa Wakatsuka ,  Tadao Okegawa ,  Yoshinobu Arai

    发明人： Hirohisa Wakatsuka ,  Tadao Okegawa ,  Yoshinobu Arai

    IPC分类号： A61K31/557 ,  A61K31/5575 ,  A61P1/16 ,  A61P7/02 ,  A61P9/12 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07C405/00 ,  C08B37/00 ,  C07C177/00

    CPC分类号： C07C405/0041 ,  C08B37/0015

    摘要： A 6-keto-prostaglandin E.sub.1 derivative of the formula: ##STR1## (wherein R.sup.1 represents an amino acid or amino alcohol residue, R.sup.2 represents a single bond or an alkylene group of from 1 to 4 carbon atoms, R.sup.3 represents (i) an alkyl group of from 1 to 8 carbon atoms, (ii) a cycloalkyl group of from 4 to 7 carbon atoms, which may be unsubstituted or substituted by at least one alkyl group of from 1 to 8 carbon atoms or (iii) a phenyl or phenoxy group, which may be unsubstituted or substituted by chlorine, trifluoromethyl or alkyl of from 1 to 3 carbon atoms, provided that when R.sup.2 represents a single bond R.sup.3 does not represent phenoxy)cyclodextrin clathrates thereof and non-toxic salts thereof possess selective cytoprotective activity.

    摘要翻译： 下式的6-酮前列腺素E1衍生物：其中R1表示氨基酸或氨基醇残基，R2表示单键或1〜4个碳原子的亚烷基，R3表示（ i）1至8个碳原子的烷基，（ii）4至7个碳原子的环烷基，其可以是未被取代的或被至少一个1至8个碳原子的烷基取代，或（iii） 苯基或苯氧基，其可以是未取代的或被氯，三氟甲基或具有1至3个碳原子的烷基取代，条件是当R 2表示单键时，R3不表示苯氧基）环糊精包合物和其无毒盐具有 选择性细胞保护活性。

    Prostaglandin I.sub.2 analogues
    2.
    发明授权
    Prostaglandin I.sub.2 analogues 失效
    前列腺素I2类似物

    公开(公告)号：US4178367A

    公开(公告)日：1979-12-11

    申请号：US878571

    申请日：1978-02-16

    申请人： Hayashi Masaki ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hiroyuki Ito ,  Hirohisa Wakatsuka

    发明人： Hayashi Masaki ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hiroyuki Ito ,  Hirohisa Wakatsuka

    IPC分类号： C07C405/00 ,  C07D307/937 ,  C07F9/40 ,  A61K31/34 ,  C07D307/93

    CPC分类号： C07D307/937 ,  C07C405/00 ,  C07F9/4018

    摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## (wherein Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen, methyl or ethyl, R.sup.3 represents a single bond, or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, each represent hydrogen or an alkyl group containing from 1 to 8 carbon atoms, n represents 3, 4, 5 or 6, the wavy line attached to the carbon atoms in positions 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof, and the double bond between C.sub.6 -C.sub.6 is Z or E) are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2.

    摘要翻译： 前列腺素I2类似物具有下式：其中Y表示反式亚乙烯基或亚乙基，R 1表示氢或含有1至12个碳原子的烷基，R 2表示氢，甲基或乙基，R 3表示单键， 或含有1至4个碳原子的亚烷基，可以相同或不同的R 4，R 5和R 6各自表示氢或含有1至8个碳原子的烷基，n表示3,4,5或6 连接在式中描述的位置11和15处的碳原子的波浪线代表α-或β-构型或其混合物，并且C6-C6之间的双键是Z或E）是具有典型的药理学性质的新化合物 前列腺素，例如PGI2。

    Prostaglandin 12 analogues and their pharmaceutical compositions
    3.
    发明授权
    Prostaglandin 12 analogues and their pharmaceutical compositions 失效
    前列腺素12类似物及其药物组合物

    公开(公告)号：US4399147A

    公开(公告)日：1983-08-16

    申请号：US872635

    申请日：1978-01-26

    申请人： Masaki Hayashi ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hirohisa Wakatsuka ,  Hiroyuki Ito

    发明人： Masaki Hayashi ,  Yoshinobu Arai ,  Yoshitaka Konishi ,  Katsuichi Shimoji ,  Shuichi Ohuchida ,  Hirohisa Wakatsuka ,  Hiroyuki Ito

    IPC分类号： C07D307/935 ,  A61K31/34 ,  A61K31/343 ,  A61P43/00 ,  C07C405/00 ,  C07D307/937 ,  A61K31/557

    CPC分类号： C07D307/937 ,  C07C405/00

    摘要： Prostaglandin I.sub.2 analogues of the formula: ##STR1## [wherein X represents trans-vinylene or an ethylene group unsubstituted or substituted by a bromine atom at the C-5 position, Y represents trans-vinylene or ethylene, R.sup.1 represents hydrogen or an alkyl group containing from 1 to 12 carbon atoms, R.sup.2 represents hydrogen or methyl or ethyl, R.sup.3 represents a single bond or an alkylene group containing from 1 to 4 carbon atoms, R.sup.4 represents hydrogen, an alkyl group containing from 1 to 8 carbon atoms, a cycloalkyl group containing from 4 to 7 carbon atoms unsubstituted or substituted by at least one alkyl group containing from 1 to 8 carbon atoms, or a phenyl or phenoxy group unsubstituted or carrying at least one substituent selected from halogen atoms, the trifluoromethyl group and alkyl groups containing from 1 to 3 carbon atoms, and the wavy line attached to the carbon atoms in positions 6, 11 and 15 depicted in the formula represents .alpha.- or .beta.-configuration or mixtures thereof] are new compounds possessing pharmacological properties typical of prostaglandins, for example PGI.sub.2, and are more stable than PGI.sub.2.

    摘要翻译： 前列腺素I2类似物，具有下式：其中X表示反式亚乙烯基或未被取代或被C-5位上的溴原子取代的亚乙基，Y表示反式亚乙烯基或亚乙基，R 1表示氢或烷基 含有1至12个碳原子，R 2表示氢或甲基或乙基，R 3表示单键或含有1至4个碳原子的亚烷基，R 4表示氢，含有1至8个碳原子的烷基，环烷基 含有未取代或被至少一个含有1至8个碳原子的烷基取代的4至7个碳原子的基团，或未取代或携带至少一个选自卤素原子的取代基的苯基或苯氧基，三氟甲基和含有 1至3个碳原子，并且连接在式中描述的6,11和15位的碳原子上的波浪线代表α-或β-构型或其混合物] 是具有典型的前列腺素的药理学性质的新化合物，例如PGI 2，并且比PGI2更稳定。

    Derivatives of p-substituted phenyl ester of pivalic acid
    4.
    发明授权
    Derivatives of p-substituted phenyl ester of pivalic acid 失效
    新戊酸对取代苯基酯的衍生物

    公开(公告)号：US5017610A

    公开(公告)日：1991-05-21

    申请号：US364994

    申请日：1989-06-12

    申请人： Katsuhiro Imaki ,  Yoshinobu Arai ,  Tadao Okegawa

    发明人： Katsuhiro Imaki ,  Yoshinobu Arai ,  Tadao Okegawa

    IPC分类号： C07C235/56 ,  C07C235/64 ,  C07C311/29 ,  C07C323/59 ,  C07C323/63 ,  C07D207/16 ,  C07D209/20 ,  C07D211/62 ,  C07D211/96 ,  C07D213/42 ,  C07D213/75 ,  C07D213/76 ,  C07D295/26 ,  C07D319/20 ,  C07D521/00

    CPC分类号： C07D213/42 ,  C07C235/56 ,  C07C235/64 ,  C07C311/29 ,  C07C323/59 ,  C07C323/63 ,  C07D207/16 ,  C07D209/20 ,  C07D211/62 ,  C07D211/96 ,  C07D213/75 ,  C07D213/76 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/26 ,  C07D319/20

    摘要： A derivative of general formula: ##STR1## wherein Y is --SO.sub.2 -- or ##STR2## (i) R.sup.1 and R.sup.2, which may be the same or different, each represent, (1) --H, (2) C1-16 alkyl or (3) the formula: --X-- .circle.A --(R.sup.4).sub.n wherein X is a single-bond, --SO.sub.2 --, C1-4 alkylene, C1-4 alkylene substituted by ##STR3## -- .circle.A -- is carbocyclic or heterocyclic ring, n is 1.about.5, R.sup.4 is (1) --H or C1-8 alkyl, (2) C1-14 alkoxy, (3) C1-6 alkylthio, (4) --OH, halogen, --NO.sub.2 or trihalomethyl, (5) the formula: --NR.sup.41 R.sup.42 wherein R.sup.41 and R.sup.42 each represents halogen or C1-4 alkyl, (6) tetrazole, (7) --SO.sub.3 H or --CH.sub.2 OH, (8) the formula: --SO.sub.2 NR.sup.41 R.sup.42 (9) the formula: --Z.sup.41 --COOR.sup.43 wherein Z.sup.41 is single-bond, C1-4 alkylene or C2-4 alkenylene, R.sup.43 is --H, C1-4 alkyl or benzyl, (10) the formula: --CONR.sup.41 R.sup.42 (11) the formula: --COO--Z.sup.42 --COOR.sup.43 wherein Z.sup.42 is C1-4 alkylene, R.sup.43 is --H, C1-4 alkyl or benzyl, (12) the formula: --COO--Z.sup.42 --CONR.sup.41 R.sup.42 (13) the formula: --OCO--R.sup.45 wherein R.sup.45 is C1-8 alkyl or p-guanidinophenyl, (14) the formula: --CO--R.sup.46 wherein R.sup.46 is C1-4 alkyl, (15) the formula: --O--Z.sup.43 --COOR.sup.450 wherein Z.sup.43 is C1-6 alkylene, R.sup.450 represents a hydrogen, C1-8 alkyl or p-guanidinophenyl, (16) the formula: ##STR4## wherein ##STR5## is an amino acid residue, R.sup.47 is bond, C1-4 alkyl, R.sup.48 is --H or C1-4 alkyl, R.sup.49 is --OH, C1-4 alkoxy, --NH.sub.2, amino substituted by one or two C1-4 alkyl, carbamoylmethoxy or carbamoylmethoxy substituted by one or two C1-4 alkyl at N atom of carbamoyl, wherein ##STR6## is C3-6 heterocyclic ring, (ii) R.sup.1, R.sup.2 and N atom bonded to R.sup.1 and R.sup.2 together represents heterocyclic ring containing at least a N atom(s) and substituted by --COOH or unsubstituted heterocyclic ring containing at least a N atom(s), R.sup.3 is (1) --H, (2) --OH, (3) C1-6 alkyl, (4) halogen, (5) C1-4 alkoxy or (6) C2-5 acyloxy, m is 1-4.or non-toxic salt or an acid addition salt thereof possess inhibitory activity on elastase, and therefore is useful for treating and/or preventing agent for pulmonary emphysema, atherosclerosis and rheumatoid arthritis and the like.

    3-phenoxy (or phenylthia) cyclopentanecarbonylamino acid analogues
    5.
    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.

    3-Phenoxy (or phenylthio)-cyclopentanecarbonylamino acid analogues
    10.
    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：US4783476A

    公开(公告)日：1988-11-08

    申请号：US942109

    申请日：1986-12-16

    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 ,  A61K31/415

    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.

    摘要翻译： 本发明涉及由以下通式表示的化合物：其中R 1和R 2是：（i）R 1，R 2和R 1和R 2连接的碳原子一起表示通式的基团： （其中R 5和R 6独立地表示氢，烷基，环烷基，环烷基 - 烷基或苯基，条件是R 5和R 6不同时为氢原子），或（ii）R 1表示氢，R 2表示 基团：-COR 7（其中R 7表示下式的基团：其中Y表示单键，亚烷基，亚烯基，W表示氧或硫，m 表示1〜3，R8表示氢，卤素，硝基，羟基，烷基或烷氧基，条件是当m表示两个或多个时，多个R 8可以各自不同，并且R 9表示氢，烷基或苯基，条件是 R 2中的两个可以各自不同），R 3表示氢，卤素，烷基或R 3中的两个，苯基至w 其中两个R 3连接，一起代表下式的萘基：其中R 10表示氢，卤素或烷基，条件是当R 1表示氢时，该原子可被R 3取代，n表示1 至3，条件是当n表示两个或更多个时，多个R 3可以不同，每个X表示氧或硫，R 4表示氨基酸残基或其无毒盐，及其制备方法及其制备方法 脑水肿含有它们作为活性成分。