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19 条记录 (耗时 0.015 秒)

    Carbostyril derivatives, and antihistaminic agents containing the same
    11.
    发明授权
    Carbostyril derivatives, and antihistaminic agents containing the same 失效
    卡波他汀衍生物和含有它们的抗组胺剂

    公开(公告)号：US4482560A

    公开(公告)日：1984-11-13

    申请号：US357769

    申请日：1982-03-12

    申请人： Kazuo Banno ,  Takafumi Fujioka ,  Yasuo Oshiro ,  Kazuyuki Nakagawa

    发明人： Kazuo Banno ,  Takafumi Fujioka ,  Yasuo Oshiro ,  Kazuyuki Nakagawa

    IPC分类号： C07D401/12 ,  A61K31/4704 ,  A61P11/06 ,  C07D211/14 ,  C07D211/52 ,  C07D215/22 ,  C07D215/227 ,  A61K31/47 ,  C07D215/26

    CPC分类号： C07D215/227 ,  C07D211/14 ,  C07D211/52

    摘要： Novel carbostyril derivatives and their salts having antihistaminic effects and are useful as antihistaminic agents, represented by the general formula (1), ##STR1## wherein R.sup.1 is a hydrogen atom, a lower alkenyl group, a lower alkynyl group or a lower alkyl group which may have phenyl group(s) as the substituted group(s); R.sup.2 is a hydrogen atom, a lower alkyl group or a phenyl group; R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), or a phenyl group which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, lower alkyl groups and lower alkoxy groups; R.sup.4 is a hydrogen atom, a hydroxyl group or a lower alkanoyl group; X is a halogen atom; Y is a lower alkylene group which may have hydroxyl group(s) as the substituent(s); n is 0, 1 or 2; the carbon-carbon bond between 3- and 4-positions in the carbostyril skeleton is a single or double bond; provided that when R.sup.3 is a lower alkyl group having phenyl group(s) as the substituted group(s), then R.sup.4 should be neither a hydroxyl group nor a lower alkanoyl group.

    摘要翻译： 新颖的喹诺酮衍生物及其具有抗组胺作用的盐，可用作抗组胺剂，由通式（1）表示，其中R1是氢原子，低级烯基，低级炔基或低级炔基 可以具有苯基作为取代基的烷基; R2是氢原子，低级烷基或苯基; R3是具有苯基作为取代基的低级烷基或可具有1至3个选自卤素原子，低级烷基和低级烷氧基的取代基的苯基; R4是氢原子，羟基或低级烷酰基; X是卤原子; Y是可以具有羟基作为取代基的低级亚烷基; n为0,1或2; 喹诺酮骨架中3-和4-位之间的碳 - 碳键是单键或双键; 条件是当R3为具有苯基作为取代基的低级烷基时，则R4不应为羟基也不应为低级烷酰基。

    3,4-Dihydrocarbostyril derivatives and process for preparing the same
    12.
    发明授权
    3,4-Dihydrocarbostyril derivatives and process for preparing the same 失效
    3,4-二氢喹诺酮衍生物及其制备方法

    公开(公告)号：US4147869A

    公开(公告)日：1979-04-03

    申请号：US795042

    申请日：1977-05-09

    申请人： Kazuyuki Nakagawa ,  Yasuo Oshiro

    发明人： Kazuyuki Nakagawa ,  Yasuo Oshiro

    IPC分类号： C07D215/38 ,  C07D215/40 ,  C07D401/12

    CPC分类号： C07D215/40 ,  C07D215/38 ,  Y10S514/821 ,  Y10S514/826

    摘要： 3,4-Dihydrocarbostyril derivatives represented by the formula (I) ##STR1## wherein R.sub.1 represents an alkylcarbonyl group, a cycloalkylcarbonyl group, an alkylsulfonyl group, a phenylsulfonyl group, a carbamoyl group or an alkoxycarbonyl group, R.sub.2 and R.sub.3, which may be the same or different, each represents a hydrogen atom, an alkyl group, a phenylalkyl group or a phenoxyalkyl group, or R.sub.2 and R.sub.3 can form, when taken together with the nitrogen atom to which they are attached, a heterocyclic group selected from the group consisting of piperidino, pyrrolidino, morpholino and 1-piperazinyl which may be substituted with a phenyl group or an alkyl group having 1 to 4 carbon atoms, with the proviso that, when the group --NHR.sub.1 is attached to the 8-position of the 3,4-dihydrocarbostyril nucleus in which R.sub.1 represents an alkylcarbonyl group and one of R.sub.2 and R.sub.3 represents a hydrogen atom, then the other group of R.sub.2 and R.sub.3 cannot be an alkyl group, pharmaceutically acceptable acid addition salts thereof, and process for preparing the same.

    摘要翻译： 由式（I）表示的3,4-二氢吡咯烷子衍生物其中R1表示烷基羰基，环烷基羰基，烷基磺酰基，苯基磺酰基，氨基甲酰基或烷氧基羰基，R2和R3， 其可以相同或不同，各自表示氢原子，烷基，苯基烷基或苯氧基烷基，或者当与所连接的氮原子一起时，R 2和R 3可以形成选自下列的杂环基 由可以被苯基或具有1至4个碳原子的烷基取代的哌啶子基，吡咯烷子基，吗啉代和1-哌嗪基组成的组，条件是当基团-NHR1连接到8-位时 的3,4-二氢喹诺酮环，其中R 1表示烷基羰基，R 2和R 3中的一个表示氢原子，则另一组R 2和R 3不能为烷基，其药学上可接受的酸加成盐 及其制备方法。

    Method for treating hypoxia
    16.
    发明授权
    Method for treating hypoxia 失效
    低氧治疗方法

    公开(公告)号：US4914094A

    公开(公告)日：1990-04-03

    申请号：US326845

    申请日：1989-03-21

    申请人： Yasuo Oshiro ,  Masaaki Osaki ,  Tetsuro Kikuchi

    发明人： Yasuo Oshiro ,  Masaaki Osaki ,  Tetsuro Kikuchi

    IPC分类号： A61K31/47 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    CPC分类号： A61K31/495 ,  A61K31/47 ,  A61K31/535 ,  A61K31/54 ,  A61K31/55

    摘要： A method for curing and/or improving hypoxia characterized by administering a compound represented by the general formula (1), ##STR1## said compounds have been known in prior art literatures, for example, as carbostyril derivatives in Japanese Patent Kokai No. 54-160389 (1979), etc., as benzoxazine derivatives in Japanese Patent Kokai No. 59-70675 (1984), and as benzoazepine derivatives in Japanese Patent Kokai No. 57-193461 (1982), and they have been known as central nervous system controlling agents and antihistaminic agents.The present invention was established on the basis of the findings that the compounds represented by the general formula (1) possess excellent pharmacological activities for curing and/or improving hypoxia and also possess excellent anti-oxidative activities, which could not have been anticipated from the disclosures in the prior art literatures.

    摘要翻译： 用于治疗和/或改善缺氧的方法，其特征在于给予由通式（1）表示的化合物，所述化合物在现有技术文献中是已知的，例如，作为日本专利公开号的喹诺酮衍生物 日本专利公开号59-70675（1984）中作为苯并恶嗪衍生物的日本专利公开昭54-160389号（1979）等，作为日本专利公开57-193461（1982）中的苯并氮杂衍生物，它们已知为 中枢神经系统控制剂和抗组胺剂。 本发明是基于由通式（1）表示的化合物具有优异的用于固化和/或改善缺氧的药理活性并且还具有优异的抗氧化活性的发现而建立的，这是不可预期的 在现有技术文献中的公开内容。

    Indane derivatives and salts thereof
    17.
    发明授权
    Indane derivatives and salts thereof 失效

    公开(公告)号：US4792628A

    公开(公告)日：1988-12-20

    申请号：US39779

    申请日：1987-04-16

    申请人： Yasuo Oshiro ,  Hiraki Ueda ,  Kazuyuki Nakagawa

    发明人： Yasuo Oshiro ,  Hiraki Ueda ,  Kazuyuki Nakagawa

    IPC分类号： A61K31/13 ,  A61K31/135 ,  A61K31/15 ,  C07C45/67 ,  C07C45/68 ,  C07C45/71 ,  C07C49/747 ,  C07C49/755 ,  C07C233/00 ,  C07C233/12 ,  C07C233/16 ,  C07C311/00 ,  C07C311/02 ,  C07C311/15 ,  C07D295/08 ,  C07D295/26 ,  C07C87/457

    CPC分类号： C07D295/26 ,  C07C205/45 ,  C07C323/00 ,  C07C45/67 ,  C07C45/673 ,  C07C45/68 ,  C07C45/71 ,  C07C49/747 ,  C07C49/755

    摘要： Indane derivatives and their salts represented by the general formula (1), ##STR1## wherein R.sup.1 is an amino group which may have lower alkyl groups as the substituents, a hydroxylimino group, an alkanoylamino group having 1 to 10 carbon atoms which may have halogen atoms as the substituents, a lower alkylsulfonylamino group, a phenylsulfonylamino group which may have lower alkyl groups as the substituents on the phenyl ring, a benzoylamino group having lower alkyl groups as the substituents on the phenyl ring, and a phenyl-lower alkylamino group having a hydroxyl groups or a lower alkyl groups as the substituents on the phenyl ring, R.sup.2 is a hydrogen atom, a lower alkyl group, a halogen atom, a nitro group, an amino group, an amino-lower alkyl group, a lower alkanoylamino group, a lower alkanoylamino-lower alkyl group which may have halogen atoms as the substituents, a lower alkylthio group, a 1-piperidinesulfonyl group, or a lower alkenyl group; R.sup.3 is a hydrogen atom, a lower alkyl group, or a halogen atom; R.sup.4 and R.sup.5 are the same or different from each other, and are each a hydrogen atom, or a lower alkyl group; provided that when R.sup.1 is a hydroxylimino group, then R.sup.2 and R.sup.3 should not be hydrogen atoms at the same time.The indane derivatives and their salts are useful as preventive and curative agents for various diseases and disorders caused by the excessive formation and accumulation of the active oxygen radicals and the peroxidized substances in the living body, and/or the defects of phylaxis mechanisms of the living body, for example anti-arreriosclerotic agents, carcinogenesis preventive agents, carcinostatic agents, anti-inflammatory agents, analgesics, autoimmune disease curative agents, platelets aggregation inhibitory agents, hypotensive agents, anti-hyperlipemic agents, retinosis of immature infant and cataract preventive and curative agents.The indane derivatives and their salts are also useful as antioxidants for oils and fats being contained in processed foods.

    Pharmaceutically useful carbostyril derivatives
    18.
    发明授权
    Pharmaceutically useful carbostyril derivatives 失效
    药用有用的喹诺酮衍生物

    公开(公告)号：US4734416A

    公开(公告)日：1988-03-29

    申请号：US24602

    申请日：1979-03-28

    申请人： Kazuo Banno ,  Takafuni Fujioka ,  Yasuo Oshiro ,  Kazuyuki Nakagawa

    发明人： Kazuo Banno ,  Takafuni Fujioka ,  Yasuo Oshiro ,  Kazuyuki Nakagawa

    IPC分类号： C07D215/06 ,  A61K31/4704 ,  A61K31/495 ,  A61P25/00 ,  A61P25/20 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D205/06 ,  C07D215/16 ,  C07D215/22 ,  C07D215/227 ,  C07D215/26 ,  C07D215/28 ,  C07D241/04 ,  C07D243/08 ,  C07D295/04 ,  C07D403/12 ,  C07D405/12 ,  C07D403/02

    CPC分类号： C07D215/227 ,  C07D215/16 ,  C07D215/22 ,  C07D215/28

    摘要： Carbostyril derivatives having antihistamic action and central nervous controlling action are useful as antihistamic agents or central nervous controlling agents. The derivatives are represented by the general formula, ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, an alkynyl group having 2 to 4 carbon atoms or a phenylalkyl group having an alkylene group containing 1 to 4 carbon atoms; R.sup.2 is a hydrogen atom, an alkyl group having 1 to 4 carbon atoms or a phenyl group; R.sup.3 is a hydrogen atom, a hydroxy group, an alkyl group having 1 to 4 carbon atoms, an alkanolyoxy group having 1 to 4 carbon atoms or a 3,4,5-trimethoxybenzoyloxy group; R.sup.4 is a hydrogen atom or an alkyl group having 1 to 4 carbon atoms; R.sup.5 is a cycloalkyl group having 3 to 8 carbon atoms, a phenyl group (which may have 1 to 3 substituted groups selected from the group consisting of halogen atoms, alkyl groups having 1 to 4 carbon atoms and alkoxy groups having 1 to 4 carbon atoms), an alkyl group having 1 to 4 carbon atoms (having one substituted group such as a hydroxy group, a phenyl group or an alkanoyloxy group having 1 to 4 carbon atoms), an alkanoyl group having 1 to 4 carbon atoms or benzoyl group; X is a halogen atom; n is 0, or an integer of 1 or 2; Q is an integer of 2 or 3, l and m are respectively an integer of 0 or 1-6, but the sum of l and m should not exceed 6; the carbon-carbon bond at the 3- and 4-positions in the carbostyril skeleton is a single or double bond; and the substituted position of the side chain of ##STR2## is any one of the 4-, 5-, 6-, 7- or 8-positions.

    摘要翻译： 具有抗组胺作用和中枢神经控制作用的卡波他特尔衍生物可用作抗组胺剂或中枢神经控制剂。 衍生物由通式（1）表示，其中R 1是氢原子，具有1至6个碳原子的烷基，具有2至4个碳原子的烯基，具有2至4个碳原子的炔基 原子或具有1〜4个碳原子的亚烷基的苯基烷基; R2是氢原子，碳原子数1〜4的烷基或苯基; R3为氢原子，羟基，碳原子数1〜4的烷基，碳原子数1〜4的烷氧基或3,4,5-三甲氧基苯甲酰氧基。 R4是氢原子或碳原子数1〜4的烷基。 R5是具有3-8个碳原子的环烷基，苯基（其可以具有1至3个选自卤素原子，具有1至4个碳原子的烷基和具有1至4个碳原子的烷氧基的取代基） ），碳原子数1〜4的烷基（具有羟基，苯基或碳原子数1〜4的烷酰氧基的一个取代基），碳原子数1〜4的烷酰基或苯甲酰基; X是卤原子; n为0或1或2的整数; Q为2或3的整数，l和m分别为0或1-6的整数，但l和m之和不应超过6; 喹诺酮骨架中3-和4-位的碳 - 碳键是单键或双键; 并且“IMAGE”侧链的取代位置是4-，5-，6-，7-或8-位中的任何一个。

    Sesquiterpene derivatives having anti-complementary activity
    19.
    发明授权
    Sesquiterpene derivatives having anti-complementary activity 失效
    倍半萜衍生物具有抗互补活性

    公开(公告)号：US4229466A

    公开(公告)日：1980-10-21

    申请号：US906300

    申请日：1978-05-15

    申请人： Wasei Miyazaki ,  Hirotsugu Kaise ,  Yoshimasa Nakano ,  Taketoshi Izawa ,  Yasuo Oshiro ,  Masanao Shinohara

    发明人： Wasei Miyazaki ,  Hirotsugu Kaise ,  Yoshimasa Nakano ,  Taketoshi Izawa ,  Yasuo Oshiro ,  Masanao Shinohara

    IPC分类号： C07D307/94 ,  C07D493/10 ,  C07D493/20 ,  C12P17/04 ,  A61K31/335 ,  A61K31/34 ,  C07D307/77 ,  C07D307/92

    CPC分类号： C07D307/94 ,  C07D493/10 ,  C12P17/04

    摘要： A sesquiterpene derivative expressed by the general formula (I): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group or a lower alkanoyl group; R.sup.2 and R.sup.3, which may be the same or different, each represents a formyl group, a hydroxymethyl group, a hydroxyl group, a carboxyl group, a lower alkanoyloxymethyl group, or a group of the formula --CH.dbd.CR.sup.7 R.sup.8, wherein R.sup.7 and R.sup.8, which may be the same or different, each represents a hydrogen atom, a cyano group, a lower alkoxycarbonyl group or a carboxyl group, or R.sup.2 and R.sup.3 may combine to form a lactone ring of the formula ##STR2## in which R.sup.9 represents a hydrogen atom or a hydroxyl group; R.sup.4 and R.sup.6, which may be the same or different, each represents a hydroxyl group or a lower alkanoyloxy group; R.sup.5 represents a hydrogen atom; R.sup.4 and R.sup.5 may together form an oxo group (.dbd.O); and R.sup.4 and R.sup.6 may combine to form a lower alkylidenedioxy group, the pharmaceutically acceptable salts thereof, processes for the production of the compounds of the general formula (I) and the salts thereof, pharmaceutical composition containing the compounds of the general formula (I) and the salts thereof, and method of use of the compounds of the general formula (I) and the salts thereof.

    摘要翻译： 由通式（I）表示的倍半萜衍生物：其中R 1表示氢原子，低级烷基或低级烷酰基; R2和R3可以相同或不同，分别表示甲酰基，羟甲基，羟基，羧基，低级烷酰氧基甲基或式-CH = CR7R8的基团，其中R7和R8 可以相同或不同，各自表示氢原子，氰基，低级烷氧基羰基或羧基，或者R 2和R 3可以结合形成式“IMAGE”的内酯环，其中R 9表示 氢原子或羟基; R 4和R 6可以相同或不同，分别表示羟基或低级烷酰氧基; R5代表氢原子; R4和R5可以一起形成氧代基（= O）; 并且R4和R6可以结合形成低级亚烷基二氧基，其药学上可接受的盐，通式（I）化合物及其盐的制备方法，含有通式（I）化合物的药物组合物， 及其盐，以及通式（I）的化合物及其盐的使用方法。