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    Pharmaceutical compositions containing fatty acid amide derivatives
    2.
    发明授权
    Pharmaceutical compositions containing fatty acid amide derivatives 失效
    含有脂肪酸酰胺衍生物的药物组合物

    公开(公告)号：US3995059A

    公开(公告)日：1976-11-30

    申请号：US174149

    申请日：1971-08-23

    申请人： Toshitsugu Fukumaru ,  Noritaka Hamma ,  Hiroshi Nakatani ,  Hideaki Fukushima ,  Katsuyuki Toki

    发明人： Toshitsugu Fukumaru ,  Noritaka Hamma ,  Hiroshi Nakatani ,  Hideaki Fukushima ,  Katsuyuki Toki

    IPC分类号： C07C233/00 ,  C07C233/02 ,  C07D295/185 ,  A01N9/20 ,  A01N9/24

    CPC分类号： C07D295/185 ,  C07C233/00 ,  C07C233/02

    摘要： A pharmaceutical composition consisting essentially of pharmaceutically effective amount of an N-substituted fatty acid amide of the formula, ##EQU1## wherein R is a C.sub.13 - C.sub.25 aliphatic hydrocarbon chain or a C.sub.13 - C.sub.25 hydroxylated aliphatic hydrocarbon chain and RCO-- is other than isostearoyl; R' is d- or l-.alpha.-C.sub.1 - C.sub.4 alkylbenzyl, racemic-, d- or l-.alpha.-C.sub.1 - C.sub.4 alkylbenzyl substituted in the benzene ring with one or two substituents selected from the group consisting of C.sub.1 - C.sub.4 alkyl, C.sub.1 - C.sub.4 alkoxy, halogen and nitro, or racemic-, d- or l-.alpha.-benzylbenzyl; R" is hydrogen; or R' and R" together are cyclohexyl; and when RCO-- is isotearoyl R' is alkyl, alkenyl, cycloalkyl, alkylcycloalkyl, hydroxycycloalkyl, alkoxycycloalkyl, alkylphenyl, hydroxyphenyl, alkoxyphenyl, halogenophenyl, halogen-alkyl-substituted phenyl, halogenoalkyl- and halogen-substituted phenyl, alkoxy- and halogen-substituted phenyl, benzyl, racemic-, d- or l-.alpha.-C.sub.1 - C.sub.4 alkylbenzyl, benzyl substituted in the benzene ring with lower alkyl or lower alkoxy, racemic-, d- or l-.alpha.-benzylbenzyl or hydroxybenzyl, and R" is hydrogen or any one of the groups represented by R', and a pharmaceutically acceptable carrier, which is useful for lowering elevated levels of cholesterol in the blood.

    摘要翻译： 基本上由药学有效量的式R'R-CO-N ANGLE R“的N-取代脂肪酸酰胺组成的药物组合物，其中R是C 13 -C 25脂族烃链或C 13 -C 25羟基化脂族烃 链和RCO-不是异硬脂酰基; R'是在苯环中被一个或两个选自C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基，C 1 -C 4烷基， C 1 -C 4烷氧基，卤素和硝基，或外消旋 - ，d-或1-α-苄基苄基; R“是氢; 或R'和R“一起为环己基; 当RCO-为异月桂酰基R'为烷基，烯基，环烷基，烷基环烷基，羟基环烷基，烷氧基环烷基，烷基苯基，羟基苯基，烷氧基苯基，卤代苯基，卤代 - 烷基取代的苯基，卤代烷基 - 和卤素取代的苯基，烷氧基 - 和卤素取代 苯基，苄基，外消旋 - ，d-或1-α-C 1 -C 4烷基苄基，在苯环中被低级烷基或低级烷氧基取代的苄基，外消旋 - ，d-或1-α-苄基苄基或羟基苄基，R“ 是氢或由R'表示的基团中的任何一个，以及可用于降低血液中胆固醇升高的药学上可接受的载体。

    Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric acid)-cyclohexane).alpha.-methyl substituted
    3.
    发明授权
    Diheterocyclic esters of 4-(1,1-bis-(phenoxy-propionic or -butoyric acid)-cyclohexane).alpha.-methyl substituted 失效
    4-（1,1-双 - （苯氧基 - 丙酸） - 环己烷）（60-甲基取代的）的二杂环酯

    公开(公告)号：US4092324A

    公开(公告)日：1978-05-30

    申请号：US716666

    申请日：1976-08-23

    申请人： Yoshio Suzuki ,  Masayoshi Minai ,  Noritaka Hamma ,  Eiichi Murayama ,  Shunji Aono

    发明人： Yoshio Suzuki ,  Masayoshi Minai ,  Noritaka Hamma ,  Eiichi Murayama ,  Shunji Aono

    IPC分类号： C07D211/46 ,  C07D213/30 ,  C07D213/75 ,  C07D213/55

    CPC分类号： C07D213/30 ,  C07D211/46 ,  C07D213/75

    摘要： Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A preresents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent).

    摘要翻译： 作为具有良好吸收性和低毒性的抗动脉硬化剂的双苯氧基羧酸衍生物，它们是由通式表示的新化合物，其中R 1和R 2表示氢原子或低级烷基，并且A表示（ 其中，在R 3为氢原子的情况下，R 4表示氨基 - 低级烷基，N-低级烷基氨基烷基，杂环基或杂环基取代的烷基;或者，R 3和R 4可以通过中间杂原子 原子形成杂环基，如果所述杂原子是氮原子，则该氮原子可以具有作为取代基的低级烷基）或者其中R5表示氢原子，羟烷基或其衍生物，和 R6表示羟基烷基或杂环基;或者R5和R6可以连接形成环状基团，或者可以通过另一个中间杂原子连接形成杂环基，如果所述杂原子是氮原子 ，该氮原子可以具有低级烷基作为取代基）。

    Fluorine derivatives of vitamin D.sub.3 and process for producing the same
    5.
    发明授权
    Fluorine derivatives of vitamin D.sub.3 and process for producing the same 失效
    维生素D3的氟衍生物及其制备方法

    公开(公告)号：US5030626A

    公开(公告)日：1991-07-09

    申请号：US512560

    申请日：1990-04-24

    申请人： Noritaka Hamma ,  Yoshikazu Saito ,  Toshio Nishizawa ,  Takashi Katsumata ,  Itsuro Sugata

    发明人： Noritaka Hamma ,  Yoshikazu Saito ,  Toshio Nishizawa ,  Takashi Katsumata ,  Itsuro Sugata

    IPC分类号： A61K31/59 ,  A61P3/02 ,  A61P3/14 ,  A61P29/00 ,  A61P35/00 ,  A61P43/00 ,  C07C67/00 ,  C07C401/00 ,  C07J9/00 ,  C07J31/00

    CPC分类号： C07C401/00 ,  C07J31/006 ,  C07J9/00 ,  Y02P20/55 ,  Y10S514/825

    摘要： There are disclosed herein novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D.sub.3 providing excellent pharmacological effects, and a process for the preparation thereof. These novel compounds are represented by the general formula ##STR1## wherein R.sub.1 and R.sub.2 each denotes a hydrogen atom or a protecting group for the hydroxyl group; R.sub.3 and R.sub.4 each denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group and R.sub.4 ' and R.sub.5 ' each denotes a hydrogen atom, or alternatively R.sub.3 and R.sub.3 ' together or R.sub.4 and R.sub.4 ' together denote an oxo group; provided that R.sub.3, R.sub.3 ', R.sub.4 and R.sub.4 ' cannot denote hydrogen atoms simultaneously. The process for the preparation comprises subjecting a previtamin D.sub.3 derivative represented by the formula ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.3 ', R.sub.4 and R.sub.4 ' are as defined above, to thermal isomerization to give a vitamin D.sub.3 derivative represented by the general formula ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.3 ', R.sub.4 and R.sub.4 ' are as defined above, and optionally subjecting it to a deprotection reaction.

    摘要翻译： 本文公开了具有优异药理作用的26,26,26,27,27,27-六氟维生素D3的新型衍生物及其制备方法。 这些新化合物由通式“IMAGE”表示，其中R 1和R 2各自表示氢原子或羟基的保护基; R 3和R 4各自表示氢原子，羟基或保护的羟基，R 4'和R 5'各自表示氢原子，或者R 3和R 3'一起或R 4和R 4'一起表示氧代基; 条件是R3，R3'，R4和R4'不能同时表示氢原子。 制备方法包括将由式（IMAGE）表示的上述维生素D3衍生物（其中R 1，R 2，R 3，R 3'，R 4和R 4'如上定义）进行热异构化，得到由通式 其中R 1，R 2，R 3，R 3'，R 4和R 4'如上所定义，并且任选地使其进行去保护反应。

    Fluorine derivatives of vitamin D.sub.3 and process for producing the same
    6.
    发明授权
    Fluorine derivatives of vitamin D.sub.3 and process for producing the same 失效
    维生素D3的氟衍生物及其制备方法

    公开(公告)号：US4853378A

    公开(公告)日：1989-08-01

    申请号：US108497

    申请日：1987-10-14

    申请人： Noritaka Hamma ,  Yoshikazu Saito ,  Toshio Nishizawa ,  Takashi Katsumata

    发明人： Noritaka Hamma ,  Yoshikazu Saito ,  Toshio Nishizawa ,  Takashi Katsumata

    IPC分类号： C07C401/00 ,  C07J9/00 ,  C07J71/00

    CPC分类号： C07C401/00 ,  C07J71/001 ,  C07J9/00 ,  Y02P20/55

    摘要： There are disclosed novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D.sub.3 having fluorine atom at the 23- and/or 24-position which have an excellent pharmacological activity and a process for production thereof. The novel compounds are represented by the general formula: ##STR1## wherein R.sub.1 ' denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sub.2 denotes a hydrogen atom or a protecting group for hydroxyl group, R.sub.3 denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R.sub.4 and R.sub.4 ' each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R.sub.4 and R.sub.4 ' are combined to denote an oxo group, with a proviso that at least one of R.sub.3, R.sub.4 and R.sub.4 ' denote a fluorine atom. The process for production thereof comprises subjecting to thermal isomerization a compound represented by the general formula: ##STR2## wherein R.sub.1 ', R.sub.2, R.sub.3, R.sub.4 and R.sub.4 ' are the same as defined above, to thermal isomerization and optionally further to deprotection reaction.

    Novel bisphenoxy carboxylic acid derivatives and their salts
    8.
    发明授权
    Novel bisphenoxy carboxylic acid derivatives and their salts 失效

    公开(公告)号：US4008265A

    公开(公告)日：1977-02-15

    申请号：US491033

    申请日：1974-07-23

    申请人： Yoshio Suzuki ,  Masayoshi Minai ,  Noritaka Hamma ,  Eiichi Murayama ,  Shunji Aono

    发明人： Yoshio Suzuki ,  Masayoshi Minai ,  Noritaka Hamma ,  Eiichi Murayama ,  Shunji Aono

    IPC分类号： C07D211/46 ,  C07D213/30 ,  C07D213/75 ,  C07D295/185 ,  C07C69/66

    CPC分类号： C07D213/30 ,  C07D211/46 ,  C07D213/75 ,  C07D295/185 ,  Y10S514/824

    摘要： Bisphenoxy carboxylic acid derivatives useful as an antiarteriosclerosis agent with good absorbability and low toxicity, which are novel compounds represented by the general formula, ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen atoms or lower alkyl groups and A represents ##STR2## (wherein in case R.sub.3 is a hydrogen atom, R.sub.4 represents an amino-lower-alkyl group, an N-lower-alkylaminoalkyl group, a heterocyclic group, or a heterocyclic group-substituted alkyl group; or R.sub.3 and R.sub.4 may join through an intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent) or ##STR3## (wherein R.sub.5 represents a hydrogen atom, a hydroxyalkyl group or a derivative thereof, and R.sub.6 represents a hydroxyalkyl group or a heterocyclic group; or R.sub.5 and R.sub.6 may join to form a cyclic group, or may join through another intermediary hetero atom to form a heterocyclic group and if said hetero atom is a nitrogen atom, this nitrogen atom can bear a lower alkyl group as a substituent), are prepared by reacting a bisphenoxy acid represented by the general formula, ##STR4## wherein R.sub.1 and R.sub.2 have the same meanings as defined above, or a reactive derivative thereof with a hetero atom-containing alcohol compound represented by the general formula, ##STR5## wherein R.sub.3 and R.sub.4 have the same meanings as defined above, an amine derivative represented by the general formula, ##STR6## wherein R.sub.5 and R.sub.6 have the same meanings as defined above, or a salt thereof. Alternatively, the bisphenoxy carboxylic acid derivatives represented by the said general formula (I), wherein A is ##STR7## R.sub.5 is hydrogen and R.sub.6 is a hydroxyalkyl group, are prepared by heating a bisphenoxy acid derivative represented by the general formula, ##STR8## wherein R.sub.1 and R.sub.2 have the same meanings as defined above and X represents an alkylene chain.