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    Thiazolidin-4-one derivatives and acid addition salts thereof useful for treating PAF mediated diseases
    2.
    发明授权
    Thiazolidin-4-one derivatives and acid addition salts thereof useful for treating PAF mediated diseases 失效
    噻唑烷-4-酮衍生物及其适用于治疗PAF介导性疾病的酸添加物

    公开(公告)号：US5106860A

    公开(公告)日：1992-04-21

    申请号：US624566

    申请日：1990-12-10

    申请人： Masao Enomoto ,  Atsuyuki Kojima ,  Yoshihiro Komuro ,  Shigeaki Morooka ,  Shunji Aono ,  Yuzuru Sanemitsu ,  Masato Mizutani ,  You Tanabe

    发明人： Masao Enomoto ,  Atsuyuki Kojima ,  Yoshihiro Komuro ,  Shigeaki Morooka ,  Shunji Aono ,  Yuzuru Sanemitsu ,  Masato Mizutani ,  You Tanabe

    IPC分类号： C07D417/04

    CPC分类号： C07D417/04

    摘要： Thiazolidin-4-one derivative represented by the following general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl,or(ii) a residue represented by the general formula ##STR2## wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2;R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl,or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

    Thiazolidin-4-one derivatives useful for treating diseases caused by platelet activating factor
    3.
    发明授权
    Thiazolidin-4-one derivatives useful for treating diseases caused by platelet activating factor 失效
    可用于治疗血小板活化因子引起的疾病的噻唑烷-4-酮衍生物

    公开(公告)号：US4992455A

    公开(公告)日：1991-02-12

    申请号：US196058

    申请日：1988-05-19

    申请人： Masao Enomoto ,  Atsuyuki Kojima ,  Yoshihiro Komuro ,  Shigeaki Morooka ,  Shunji Aono ,  Yuzuru Sanemitsu ,  Masato Mizutani ,  You Tanabe

    发明人： Masao Enomoto ,  Atsuyuki Kojima ,  Yoshihiro Komuro ,  Shigeaki Morooka ,  Shunji Aono ,  Yuzuru Sanemitsu ,  Masato Mizutani ,  You Tanabe

    IPC分类号： C07D417/04

    CPC分类号： C07D417/04

    摘要： Thiazolidin-4-one derivative represented by the folowing general formula (I) and acid addition salts thereof ##STR1## wherein; R.sup.1 and R.sup.2 are the same or different and denote each(i) a residue represented by the general formula--A--R.sup.4 wherein, A denotes a single bond, C.sub.1 -C.sub.8 alkylene, C.sub.2 -C.sub.8 alkenylene, or C.sub.2 -C.sub.8 alkynylene and R.sup.4 denotes hydrogen, C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, or C.sub.1 -C.sub.6 haloalkyl, or(ii) a residue represented by the general formula{(CH.sub.2).sub.n O}.sub.m {(CH.sub.2).sub.n' O}B--R.sup.5 wherein, B denotes a single bond or C.sub.1 -C.sub.6 alkylene, R.sup.5 denotes hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.8 alkenyl, C.sub.3 -C.sub.8 cycloalkyl, substituted silyl, or substituted or unsubstituted aryl, n and n' denote each an integer of 2 to 4, m denotes an integer of 1 to 3, and m' denotes an integer of 0 to 2; andR.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, allyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanol) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR2## (R.sup.10 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms), with the proviso that, when R.sup.1 is hydrogen and R.sup.2 is methyl, R.sup.3 denotes hydrogen, C.sub.1 -C.sub.2 alkyl, 2-propynyl, or a residue represented by(a) the general formula--CH.sub.2).sub.l R.sup.6 wherein, R.sup.6 denotes halogen, an aryl group substituted or unsubstituted by one or more hydroxy or C.sub.1 -C.sub.4 alkoxy groups, or a residue represented by the general formula --D--R.sup.7 (D denotes oxygen or sulfur and R.sup.7 denotes hydrogen, C.sub.1 -C.sub.4 alkyl, or C.sub.1 -C.sub.4 alkanoyl) and l denotes an integer of 2 to 4,(b) the general formula--CH.sub.2).sub.k CO--E--R.sup.8 wherein, E denotes oxygen, sulfur, imino, or C.sub.1 -C.sub.4 alkylimino, R.sup.8 denotes hydrogen or C.sub.1 -C.sub.4 alkyl, or --(E--R.sup.8) denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms, and k denotes an integer of 1 to 3, or(c) the general formula--F--R.sup.9 wherein, F denotes C.sub.2 -C.sub.6 alkylene and R.sup.9 denotes a nitrogen-containing heterocyclic aromatic residue or an amino group represented by the general formula ##STR3## (R.sup.10 denotes hydrogen, C.sub.2 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkanoyl and R.sup.11 denotes hydrogen or C.sub.1 -C.sub.4 alkyl or R.sup.10 in combination with R.sup.11 denotes a 5- to 7-membered cyclic amino group which optionally contains other hetero atoms.Having selective PAF-antagonistic activities, these compounds are very useful as preventive and curative agents for PAF-induced diseases, for example, various kinds of inflammation, allergic diseases, circulatory diseases, and gastro-intestinal diseases.

    Certain pyridyl-thiazolidin-4-one having anti-ulcer activity
    5.
    发明授权
    Certain pyridyl-thiazolidin-4-one having anti-ulcer activity 失效
    某些具有抗溃疡活性的吡啶基 - 噻唑烷-4-酮

    公开(公告)号：US5021435A

    公开(公告)日：1991-06-04

    申请号：US297313

    申请日：1989-01-17

    申请人： Naruhito Masai ,  Masao Enomoto ,  Atsuyuki Kojima ,  Hiroaki Masumori ,  Nobuyuki Hara ,  Youichi Hara ,  Shigeaki Morooka

    发明人： Naruhito Masai ,  Masao Enomoto ,  Atsuyuki Kojima ,  Hiroaki Masumori ,  Nobuyuki Hara ,  Youichi Hara ,  Shigeaki Morooka

    IPC分类号： A61K31/44 ,  A61P1/04 ,  C07D417/04

    CPC分类号： C07D417/04

    摘要： A 2-pyridyl-thiazolidin-4-one derivative represented by the formula: ##STR1## wherein R.sub.1 and R.sub.2 are each a hydrogen atom, an C.sub.1 -C.sub.20 alkyl group, an C.sub.2 -C.sub.20 alkenyl group, an C.sub.2 -C.sub.20 alkynyl group, an aryl group, a C.sub.3 -C.sub.8 cycloalkyl group or an aralkyl group which may have a substituent, R.sub.3 is a hydrogen atom, an C.sub.1 -C.sub.20 alkyl group, an C.sub.2 -C.sub.20 alkenyl group, an C.sub.2 -C.sub.20 alkynyl group, a C.sub.3 -C.sub.8 cycloalkyl group or an aralkyl group which may have a substituent, P is a pyridyl group or its N-substituted pyridinium salt which may have a substituent, said substituent being selected from the group consisting of halogen atom, cyano group, hydroxy group, amino group, lower alkyl group, lower alkoxy group, lower alkylamino group, halogenated lower alkyl group, acyl group, acyloxy group, acylthio group, acylamino group, carboxyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkyl substituted carbamoyl group, heterocyclic group, and lower cycloalkyl group, and n represents an integer of 0, 1 or 2, or a pharmaceutically acceptable salts thereof and an anti-ulcer agent which contains, as an effective ingredient, said 2-pyridyl-thiazolidine-4-one derivative or a pharmaceutically acceptable salt thereof.

    Bicyclooctane derivatives
    7.
    发明授权
    Bicyclooctane derivatives 失效
    双环辛烷衍生物

    公开(公告)号：US4493846A

    公开(公告)日：1985-01-15

    申请号：US243570

    申请日：1981-03-13

    申请人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Shunsuke Sami ,  Atsuyuki Kojima ,  Junki Katsube

    发明人： Keiichi Ono ,  Akihiko Sugie ,  Hajime Kawakami ,  Shunsuke Sami ,  Atsuyuki Kojima ,  Junki Katsube

    IPC分类号： C07C69/708 ,  A61K31/557 ,  C07C29/09 ,  C07C29/128 ,  C07C35/32 ,  C07C43/196 ,  C07C47/198 ,  C07C47/277 ,  C07C51/00 ,  C07C51/08 ,  C07C59/125 ,  C07C59/13 ,  C07C59/31 ,  C07C59/46 ,  C07C59/62 ,  C07C67/00 ,  C07C67/08 ,  C07C69/734 ,  C07C405/00 ,  C07D211/32 ,  C07D295/08 ,  C07D295/18 ,  C07C69/608 ,  C07C61/13 ,  C07C61/28 ,  C07C69/616

    CPC分类号： C07C255/00 ,  C07C29/095 ,  C07C29/1285 ,  C07C35/32 ,  C07C405/0083 ,  C07C43/196 ,  C07D211/32 ,  C07B2200/07 ,  C07B2200/09 ,  C07C2102/24 ,  Y10S514/925

    摘要： A compound of the formula ##STR1## wherein X.sup.1 is a free or esterified carboxyl group, a hydroxymethyl group, a cyano group, a group of the formula: ##STR2## (R.sup.a and R.sup.b are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group, a benzyl group, a phenyl group, a phenyl group substituted with a halogen atom or a C.sub.1 -C.sub.4 alkyl group, or, when taken together with the adjacent nitrogen atom to which they are attached, they represent a 5 to 7-membered saturated heterocyclic group) or a group of the formula: ##STR3## (R.sup.a and R.sup.b are each as defined above), Y is an ethylene group or a vinylene group, R.sup.1 is a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sup.2 is a hydrogen atom or R.sub.1 and R.sub.2, when taken together, means a single linkage to form a double bond between the carbon atoms which they are linked, R.sup.3 is a hydroxyl group or a protected hydroxyl group, R.sup.4 is a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group, R.sup.5 is a hydrogen atom, a C.sub.3 -C.sub.8 alkenyl group, a C.sub.3 -C.sub.8 alkynyl group, a C.sub.1 -C.sub.8 alkyl group, a C.sub.3 -C.sub.7 cycloalkyl group or a group of the formula: --(CH.sub.2).sub.n --B (n is 1 or 2 and B is a C.sub.1 -C.sub.4 alkoxyl group, a C.sub.3 -C.sub.7 cycloalkyl group, or a phenyl or phenoxy group optionally substituted with a halogen atom, a C.sub.1 -C.sub.4 alkyl group, a trifluoromethyl group or a C.sub.1 -C.sub.4 alkoxyl group), A is a group of either one of the formulae: ##STR4## (R.sup.6 and R.sup.7 are each independently a hydrogen atom or a C.sub.1 -C.sub.4 alkyl group) and ##STR5## m.sub.1 is 1 or 2 and m.sub.2 is 0, 1 or 2, and the non-toxic pharmaceutically acceptable salts threreof. Said compounds have strong anti-ulcerogenic activity and are useful in treatment of gastraintestinal ulcer.

    摘要翻译： 下式的化合物其中X1是游离或酯化的羧基，羟甲基，氰基，下式的基团：（R a和R b各自独立地是氢原子，C 1 -C 4 烷基，C3-C7环烷基，苄基，苯基，被卤素原子或C1-C4烷基取代的苯基，或者当与它们所连接的相邻氮原子一起时， 它们表示5至7元饱和杂环基）或下式的基团：（R a和R b各自如上所定义），Y是亚乙基或亚乙烯基，R 1是氢原子， 羟基或受保护的羟基，R2是氢原子或R1和R2，当它们一起表示在它们连接的碳原子之间形成双键的单键，R3是羟基或被保护的羟基 R4是氢原子或C1-C4烷基，R5是氢原子，C3-C8链烯基，C3-C8烷基 正丁基，C 1 -C 8烷基，C 3 -C 7环烷基或下式基团： - （CH 2）n B（n为1或2，B为C 1 -C 4烷氧基，C 3 -C 7环烷基 或任选被卤素原子取代的苯基或苯氧基，C 1 -C 4烷基，三氟甲基或C 1 -C 4烷氧基），A是以下基团之一： R 7各自独立地为氢原子或C 1 -C 4烷基），并且M 1为1或2，m 2为0,1或2，以及无毒的药学上可接受的盐。 所述化合物具有强的抗溃疡活性，可用于治疗胃肠溃疡。

    Aminoazole derivatives and their production and use
    8.
    发明授权
    Aminoazole derivatives and their production and use 失效

    公开(公告)号：US5180731A

    公开(公告)日：1993-01-19

    申请号：US732169

    申请日：1991-07-18

    申请人： Yukinori Ozato ,  Nobuhiko Tamura ,  Hiroaki Masumori ,  Michihiro Yamamoto ,  Atsuyuki Kojima ,  Fumio Nishikaku ,  Yoshihiko Kimura

    发明人： Yukinori Ozato ,  Nobuhiko Tamura ,  Hiroaki Masumori ,  Michihiro Yamamoto ,  Atsuyuki Kojima ,  Fumio Nishikaku ,  Yoshihiko Kimura

    IPC分类号： C07D261/14 ,  C07D263/48 ,  C07D271/06 ,  C07D271/07 ,  C07D277/38 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D277/48 ,  C07D413/06 ,  C07D413/10

    CPC分类号： C07D271/07 ,  C07D261/14 ,  C07D263/48 ,  C07D277/40 ,  C07D277/42 ,  C07D277/46 ,  C07D277/48 ,  C07D413/06 ,  C07D413/10

    摘要： A compound of the formula: ##STR1## wherein A is the group of the formula:Ar.sup.1 --D--Ar.sup.2 --wherein Ar.sup.1 is a phenyl or thienyl group which may be optionally substituted with at least one of the same or different halogen atom; Ar.sup.2 is a phenylene or thienylene group which may be optionally substituted with at least one of the same or different halogen atom; D is a divalent radical selected from the group consisting of >C.dbd.N--OR .sup.4 [wherein R.sup.4 is a hydrogen atom or lower alkyl group], >C.dbd.O, ##STR2## >CHOH, >NH radical, or single bond, ##STR3## wherein R.sup.5 is a lower alkoxy or phenyl group which may be optionally substituted with at least one of the same or different halogen atom; E is a methine group or a nitrogen atom; F is a vinylene group or an oxygen atom, ##STR4## wherein R.sup.6 is a lower alkoxy group; R.sup.7 is a lower alkyl group; R.sup.8 is a benzoyl group which may be optionally substituted with at least one of the same or different halogen atom, B is a divalent azole group; R.sup.1 is a hydrogen atom or a lower alkyl group; R.sup.2 is a hydrogen atom, lower alkyl, aryl-lower alkyl, or the group of the formula:R.sup.9 --G--wherein R.sup.9 is a hydrogen atom, lower alkyl, halo-lower alkyl, amino-lower alkyl, aryl or aryl-lower alkyl group or the group of the formula: ##STR5## wherein R.sup.10 is a hydrogen atom or lower alkyl group; R.sup.11 is a hydrogen atom, lower alkyl, lower alkenyl, lower cycloalkyl, aryl-lower alkyl, aryl or aroyl group; or the group of the formula: --NR.sup.10 R.sup.11 is a 5-, 6- or 7-membered saturated heterocyclic ring; or the group of the formula:R.sup.12 --O--wherein R.sup.12 is a lower alkyl or polyhalo-lower alkyl group; G is a divalent group selected from the group consisting of >C.dbd.O, >C.dbd.S, >(C.dbd.O).sub.2 or >SO.sub.2 radical; or the group of the formula: --NR.sup.1 R.sup.2 is a 5-, 6- or 7-membered saturated heterocyclic ring: R.sup.3 is a hydrogen atom or lower alkyl group, or its acid addition salts, which is useful for immunomodulator.

    Novel cyclopropylmethylamine derivatives
    9.
    发明授权
    Novel cyclopropylmethylamine derivatives 失效
    新型环丙基甲胺衍生物

    公开(公告)号：US4103030A

    公开(公告)日：1978-07-25

    申请号：US635331

    申请日：1975-11-26

    申请人： Atsuyuki Kojima ,  Yoshito Kameno ,  Junki Katsube ,  Shigeho Inaba ,  Hisao Yamamoto

    发明人： Atsuyuki Kojima ,  Yoshito Kameno ,  Junki Katsube ,  Shigeho Inaba ,  Hisao Yamamoto

    IPC分类号： A61K31/13 ,  A61K31/135 ,  A01N9/20 ,  A01N9/24 ,  C07C91/16 ,  C07C91/28

    摘要： Novel cyclopropylmethylamine compounds of the formula: ##STR1## wherein Ar.sup.1 represents a phenyl group having one or more substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy and trifluoromethyl, of which at least one is present at the o- or m-position, Ar.sup.2 represents an unsubstituted phenyl group or a phenyl group substituted with one or more substituents selected from the group consisting of halogen and C.sub.1 -C.sub.4 alkyl, R represents hydrogen, C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl and R' represents C.sub.1 -C.sub.4 alkyl or C.sub.2 -C.sub.4 hydroxyalkyl, and their non-toxic salts, which possess various useful pharmacological activities and can be produced by reduction of the corresponding compounds of the formula: ##STR2## wherein Ar.sup.1, Ar.sup.2, R and R' are each as defined above or by condensation of the corresponding compounds of the formula: ##STR3## wherein Ar.sup.1 and Ar.sup.2 are each as defined above and X is a conventional leaving (removable) group with amines of the formula: ##STR4## wherein R and R' are each as defined above.

    摘要翻译： 新的下式的环丙基甲胺化合物：其中Ar 1表示具有一个或多个选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基和三氟甲基的取代基的苯基，其中至少一个存在于 或位置，Ar 2表示未取代的苯基或被一个或多个选自卤素和C 1 -C 4烷基的取代基取代的苯基，R表示氢，C 1 -C 4烷基或C 2 -C 4羟烷基， R'表示C1-C4烷基或C2-C4羟基烷基及其无毒盐，它们具有各种有用的药理活性，可以通过还原相应的下式化合物来制备：其中Ar1，Ar2，R和 R'各自如上所定义，或通过下式的相应化合物的缩合：其中Ar 1和Ar 2各自如上所定义，X是具有下式的胺的常规离去（可除去）基团：其中 R和R'各自如上所定义。