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    Process for producing eburnane derivatives
    1.
    发明授权
    Process for producing eburnane derivatives 失效
    生产伊本恩衍生物的方法

    公开(公告)号：US4316028A

    公开(公告)日：1982-02-16

    申请号：US93606

    申请日：1979-11-13

    申请人： Junki Katsube ,  Keiichi Ono ,  Hajime Kawakami

    发明人： Junki Katsube ,  Keiichi Ono ,  Hajime Kawakami

    IPC分类号： C07D461/00 ,  C07D471/14

    CPC分类号： C07D471/14 ,  C07D461/00

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 alkyl group and R is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and their salts, which are useful as cerebral vasodilator; and a compound of the formula: ##STR2## wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.3 is a hydrogen atom or the formula: --CO.sub.2 R.sup.1 (R.sup.1 is a C.sub.1 -C.sub.6 alkyl group) and W is an oxygen atom, an imino group or ##STR3## but not an imino group in case that R.sup.3 is a hydrogen atom, which are intermediates of the compound (I), useful per se as cerebral vasodilator and/or antihypertensive agents.

    摘要翻译： 下式的化合物：其中R1是C1-C6烷基，R是氢原子或C1-C6烷基，它们的盐可用作脑血管扩张剂; 和下式的化合物：其中R 2是氢原子或C 1 -C 6烷基，R 3是氢原子或式-CO 2 R 1（R 1是C 1 -C 6烷基）和W 在R3是氢原子的情况下是氧原子，亚氨基或亚氨基，而不是亚氨基，它是作为脑血管扩张剂和/或抗高血压药物的化合物（I）的中间体。

    Diphenylalkanoether and diphenylalkanone oximeether derivatives
    2.
    发明授权
    Diphenylalkanoether and diphenylalkanone oximeether derivatives 失效
    二苯基烷基醚和二苯基烷酮肟醚衍生物

    公开(公告)号：US4482573A

    公开(公告)日：1984-11-13

    申请号：US550583

    申请日：1983-11-10

    申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  C07C93/08

    CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

    摘要： Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4) alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4) alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, and ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon), ##STR3## is a group of the formula: ##STR4## or the formula: ##STR5## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

    Cerebral vasodilator eburnane derivatives
    3.
    发明授权
    Cerebral vasodilator eburnane derivatives 失效
    脑血管扩张剂伊本恩衍生物

    公开(公告)号：US4382936A

    公开(公告)日：1983-05-10

    申请号：US259179

    申请日：1981-04-30

    申请人： Junki Katsube ,  Keiichi Ono ,  Hajime Kawakami

    发明人： Junki Katsube ,  Keiichi Ono ,  Hajime Kawakami

    IPC分类号： C07D461/00 ,  A61K31/445 ,  C07D471/14 ,  C07D471/22 ,  A61K31/435

    CPC分类号： C07D471/14 ,  C07D461/00 ,  Y10S514/929

    摘要： A compound of the formula: ##STR1## wherein R.sup.1 is a C.sub.1 -C.sub.6 alkyl group and R is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, and their salts, which are useful as cerebral vasodilator; and a compound of the formula: ##STR2## wherein R.sup.2 is a hydrogen atom or a C.sub.1 -C.sub.6 alkyl group, R.sup.3 is a hydrogen atom or the formula: --CO.sub.2 R.sup.1 (R.sup.1 is a C.sub.1 -C.sub.6 alkyl group) and W is an oxygen atom, an imino group or ##STR3## but not an imino group in case that R.sup.3 is a hydrogen atom, which are intermediates of the compound (I), useful per se as cerebral vasodilator and/or antihypertensive agents.

    摘要翻译： 下式的化合物：其中R1是C1-C6烷基，R是氢原子或C1-C6烷基，它们的盐可用作脑血管扩张剂; 和下式的化合物：其中R 2是氢原子或C 1 -C 6烷基，R 3是氢原子或式-CO 2 R 1（R 1是C 1 -C 6烷基）和W 在R3是氢原子的情况下是氧原子，亚氨基或亚氨基，而不是亚氨基，它是作为脑血管扩张剂和/或抗高血压药物的化合物（I）的中间体。

    Bicyclooctane derivatives
    4.
    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。

    Diphenylalkanoether and diphenylalkanone oximeether derivatives
    7.
    发明授权
    Diphenylalkanoether and diphenylalkanone oximeether derivatives 失效
    二苯基烷基醚和二苯基烷酮肟醚衍生物

    公开(公告)号：US4620036A

    公开(公告)日：1986-10-28

    申请号：US592446

    申请日：1984-03-22

    申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  C07C131/00

    CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

    摘要： Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4 )alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4)alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 - C.sub.4 alkyl group, an ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon), ##STR3## is a group of the formula: ##STR4## or the formula: ##STR5## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

    Diphenylalkanoether derivatives
    8.
    发明授权
    Diphenylalkanoether derivatives 失效
    二苯基烷烃醚衍生物

    公开(公告)号：US4459410A

    公开(公告)日：1984-07-10

    申请号：US308655

    申请日：1981-10-05

    申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  C07D295/08 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12

    CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

    摘要： Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkysulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylmino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4)alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in additon to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, an ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon), ##STR3## is a group of the formula: ##STR4## or the formula: ##STR5## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

    Diphenylalkanoether and diphenylalkanone oximeether derivatives
    9.
    发明授权
    Diphenylalkanoether and diphenylalkanone oximeether derivatives 失效

    公开(公告)号：US4426394A

    公开(公告)日：1984-01-17

    申请号：US316972

    申请日：1981-10-30

    申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  A61K31/34 ,  A61K31/135 ,  A61K31/38

    CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

    摘要： Diphenylalkanoether and diphenylalkanone oximeether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4)alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, an ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon, ##STR3## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

    Diphenylalkanoether and diphenylalkanone oximeether derivatives
    10.
    发明授权
    Diphenylalkanoether and diphenylalkanone oximeether derivatives 失效
    二苯基烷基醚和二苯基烷酮肟醚衍生物

    公开(公告)号：US4388469A

    公开(公告)日：1983-06-14

    申请号：US136565

    申请日：1980-04-02

    申请人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    发明人： Keiichi Ono ,  Hajime Kawakami ,  Junki Katsube

    IPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  C07D333/04 ,  A61K31/135 ,  A61K31/34 ,  A61K31/38 ,  C07C87/28 ,  C07D307/34

    CPC分类号： C07D213/30 ,  C07D295/088 ,  C07D307/42 ,  C07D333/16 ,  Y10S514/929

    摘要： Diphenylalkanoether and diphenylalkanone oxime-ether derivatives of the formula: ##STR1## wherein R.sup.1 and R.sup.2 are each independently an aryl group optionally substituted with 1 to 3 substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, nitro, cyano, di(C.sub.1 -C.sub.4)alkylamino, amino, benzyloxy, hydroxyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl, C.sub.1 -C.sub.4 alkanoylamino, C.sub.1 -C.sub.4 alkylamino and N-(C.sub.1 -C.sub.4)alkyl-N-(C.sub.1 -C.sub.4)alkanoylamino, Z.sup.1 is a group of the formula: ##STR2## (wherein R.sup.3 and R.sup.4 are each independently a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group or an ar(C.sub.1 -C.sub.4)alkyl group or, when taken together with the adjacent nitrogen atom to which they are attached, represent a nitrogen-containing 5 to 7-membered saturated heterocyclic group optionally having an oxygen atom or an additional nitrogen atom as the hetero atom in addition to the said nitrogen atom and, in case of having the additional nitrogen atom, bearing a hydrogen atom, a C.sub.1 -C.sub.4 alkyl group, an ar(C.sub.1 -C.sub.4)alkyl group or a phenyl group thereon), ##STR3## is a group of the formula: ##STR4## or the formula: ##STR5## A.sup.1 is a C.sub.2 -C.sub.6 alkylene group and A.sup.2 is a C.sub.2 -C.sub.4 alkylene group, and non-toxic, pharmaceutically acceptable acid addition salts thereof, which have cerebral vasodilating activity and antihypoxic activity.

    摘要翻译： 二苯基链烷醇醚和下式的二苯基烷酮肟 - 醚衍生物：其中R 1和R 2各自独立地是任选被1至3个选自卤素，C 1 -C 4烷基，C 1 -C 4烷氧基，硝基 ，氰基，二（C1-C4）烷基氨基，氨基，苄氧基，羟基，C1-C4烷硫基，C1-C4烷基亚磺酰基，C1-C4烷基磺酰基，C1-C4烷酰基氨基，C1-C4烷基氨基和N-（C1-C4）烷基 -N-（C 1 -C 4）烷酰基氨基，Z 1是下式的基团：其中R 3和R 4各自独立地为氢原子，C 1 -C 4烷基或芳（C 1 -C 4）烷基或 当与它们所连接的相邻氮原子一起取代时，除了所述氮原子之外，代表任选具有氧原子或另外的氮原子作为杂原子的含氮5至7元饱和杂环基，和 在具有另外的氮原子的情况下，带有氢原子，C1-C4烷基，ar（ C 1 -C 4）烷基或其上的苯基），IMAGE是下式的基团：下式：其中A 1为C 2 -C 6亚烷基，且A 2为C 2 -C 4亚烷基 及其无毒的药学上可接受的酸加成盐，其具有脑血管舒张活性和抗低氧活性。