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    Methods of preparing new taxoids and pharmaceutical compositions containing them
    1.
    发明授权
    Methods of preparing new taxoids and pharmaceutical compositions containing them 失效
    制备新紫杉烷和含有它们的药物组合物的方法

    公开(公告)号：US06232477B1

    公开(公告)日：2001-05-15

    申请号：US09528448

    申请日：2000-03-17

    申请人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commerçon

    发明人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commerçon

    IPC分类号： C07D30514

    CPC分类号： C07D305/14

    摘要： Methods of preparing new taxoids of general formula (I) are presented: in which: R4 represents an alkanoyloxy radical in which the alkanoyl portion contains 2 to 6 carbon atoms in an unbranched or branched chain, this radical unsubstituted or substituted with one or more halogen atoms, an alkoxy radical containing 1 to 4 carbon atoms, or alternatively R4 represents a cycloalkanoyloxy radical in which the cycloalkanoyl portion contains 4 to 8 carbon atoms, or alternatively R4 represents a benzoyloxy radical; R5 represents an alkoxy radical containing 1 to 4 carbon atoms, substituted by an alkylthio radical containing 1 to 4 carbon atoms; and Z represents a hydrogen atom or a radical of general formula:

    摘要翻译： 提供了制备通式（I）的新紫杉烷的方法：其中：R4表示烷酰氧基，其中链烷酰基部分在无支链或支链上含有2-6个碳原子，该未取代的基团或被一个或多个卤素 原子，含有1至4个碳原子的烷氧基，或者R4表示环烷酰氧基，其中环烷酰基部分含有4至8个碳原子，或者R4表示苯甲酰氧基; R5表示含有1至4个碳原子的烷氧基 被含有1至4个碳原子的烷硫基取代; 和Z表示氢原子或通式如下的基团：

    Taxoids, their preparation and pharmaceutical compositions containing them
    2.
    发明授权
    Taxoids, their preparation and pharmaceutical compositions containing them 失效
    紫杉烷类，它们的制备方法和含有它们的药物组合物

    公开(公告)号：US06194582B1

    公开(公告)日：2001-02-27

    申请号：US09126590

    申请日：1998-07-31

    申请人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon

    发明人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon

    IPC分类号： C07D26304

    CPC分类号： C07D305/14

    摘要： New taxoids of general formula (I), their preparation, and pharmaceutical compounds containing them. In general formula (I), for example, Ar represents an aryl radical, R represents an alkoxyacetyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.

    摘要翻译： 通式（I）的新紫杉烷类，其制备方法和含有它们的药物化合物。在通式（I）中，例如，Ar表示芳基，R表示烷氧基乙酰基，R 1表示苯甲酰基或式 R2-O-CO-，其中R2表示任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。 通式（I）的新产品具有显着的抗肿瘤活性。

    Taxoids, their preparation and pharmaceutical compositions containing them
    3.
    发明授权
    Taxoids, their preparation and pharmaceutical compositions containing them 有权
    紫杉烷类，它们的制备方法和含有它们的药物组合物

    公开(公告)号：US6040466A

    公开(公告)日：2000-03-21

    申请号：US271300

    申请日：1999-03-17

    申请人： Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on

    发明人： Herve Bouchard ,  Jean-Dominique Bourzat ,  Alain Commer.cedilla.on

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14

    摘要： New taxoids and methods of preparing new taxoids of general formula (I): ##STR1## in which: R.sub.4 represents an alkanoyloxy radical in which the alkanoyl portion contains 2 to 6 carbon atoms in an unbranched or branched chain, this radical unsubstituted or substituted with one or more halogen atoms, an alkoxy radical containing 1 to 4 carbon atoms, or alternatively R.sub.4 represents a cycloalkanoyloxy radical in which the cycloalkanoyl portion contains 4 to 8 carbon atoms, or alternatively R.sub.4 represents a benzoyloxy radical;R.sub.5 represents an alkoxy radical containing 1 to 4 carbon atoms, substituted by an alkylthio radical containing 1 to 4 carbon atoms; andZ represents a hydrogen atom or a radical of general formula: ##STR2## wherein such new taxoids display noteworthy anti-tumor and anti-leukemic properties.

    摘要翻译： 新的紫杉烷类和通式（I）的新紫杉烷类的制备方法：其中：R4表示烷酰氧基，其中链烷酰基部分在无支链或支链上含有2-6个碳原子，该未取代的基团或被一个或多个 卤原子，含有1至4个碳原子的烷氧基，或者R4表示环烷酰氧基，其中环烷酰基部分含有4至8个碳原子，或者R4表示苯并氧基; R5代表含有1至4个碳原子的烷氧基，被含有1至4个碳原子的烷硫基取代; Z表示氢原子或通式的基团：其中这种新的紫杉醇显示出显着的抗肿瘤和抗白血病性质。

    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    4.
    发明授权
    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
    法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途

    公开(公告)号：US6013662A

    公开(公告)日：2000-01-11

    申请号：US999408

    申请日：1997-12-29

    申请人： Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    发明人： Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    IPC分类号： C07D209/56 ,  C07D209/72 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  A01N43/38 ,  C07D235/08 ,  C07D401/08

    CPC分类号： C07D401/12 ,  C07D209/56 ,  C07D209/72 ,  C07D403/04 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14

    摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or elsea ##STR2## radical, R.sub.1 and R.sub.2 =hydrogen or halogen or alkyl, alkyloxy which is optionally substituted, alkylthio, alkyloxycarbonyl or else R.sub.1 and R.sub.2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R.sub.3 and R.sub.4 =hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio, carboxyl or alkyloxycarbonyl, R.sub.5 =hydrogen, alkyl, alkylthio, X=O or S or --NH--, --CO--, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.

    摘要翻译： 式（I）的新产品，其制备方法，含有它们的药物组合物及其在制备药物中的用途。 在式（I）中，以下取代基是优选的：Ar表示取代或稠合的苯基或多环或杂环芳族基，R表示通式 - （CH 2）m -X1（CH 2）n Z 其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或者基团，R 1和R 2 =氢或卤素或任选被取代的烷基， 烷基硫代，烷氧基羰基，或者R1和R2相对于彼此的邻位，形成任选取代的含有1或2个杂原子的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基，羧基或烷氧基羰基， R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O或S 外消旋形式，以及光学异构体（非对映异构体和对映体）和式（I）的产物的盐。 式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。

    Taxoids, their preparation and pharmaceutical compositions containing them
    7.
    发明授权
    Taxoids, their preparation and pharmaceutical compositions containing them 失效
    紫杉烷类，它们的制备方法和含有它们的药物组合物

    公开(公告)号：US5550261A

    公开(公告)日：1996-08-27

    申请号：US483693

    申请日：1995-06-07

    申请人： Herv e Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon

    发明人： Herv e Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon

    IPC分类号： A61K31/335 ,  A61K31/337 ,  A61K31/42 ,  A61P35/00 ,  C07D305/14 ,  C07D405/12 ,  C07D413/12

    CPC分类号： C07D305/14 ,  Y02P20/55

    摘要： New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I),Ar represents an aryl radical,R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical,R.sub.1 represents a benzoyl radical or a radical of formula R.sub.2 --O--CO-- in which R.sub.2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical.The new products of general formula (I) have a remarkable antitumor activity. ##STR1##

    摘要翻译： 通式（I）的新紫杉烷类，其制备方法和含有它们的药物组合物。 在通式（I）中，Ar表示芳基，R表示氢原子或乙酰基，烷氧基乙酰基或烷基，R1表示苯甲酰基或式R2-O-CO-基团，其中R2表示任选取代的 烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。 通式（I）的新产品具有显着的抗肿瘤活性。 （一）

    Taxoids, their preparation and pharmaceutical composition containing them
    9.
    发明授权
    Taxoids, their preparation and pharmaceutical composition containing them 失效
    紫杉烷，它们的制备和含有它们的药物组合物

    公开(公告)号：US07074821B1

    公开(公告)日：2006-07-11

    申请号：US08162984

    申请日：1993-12-08

    申请人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon

    发明人： Hervé Bouchard ,  Jean-Dominique Bourzat ,  Alain Commercon

    IPC分类号： C07D305/00 ,  A61K31/335

    CPC分类号： C07D305/14 ,  Y02P20/55

    摘要： New taxoids of general formula (I), their preparation and pharmaceutical compositions containing them.In general formula (I), Ar represents an aryl radical, R represents a hydrogen atom or an acetyl, alkoxyacetyl or alkyl radical, R1 represents a benzoyl radical or a radical of formula R2—O—CO— in which R2 represents an optionally substituted alkyl radical, an alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical. The new products of general formula (I) have a remarkable antitumor activity.

    摘要翻译： 通式（I）的新紫杉烷类，其制备方法和含有它们的药物组合物。 在通式（I）中，Ar表示芳基，R表示氢原子或乙酰基，烷氧基乙酰基或烷基，R 1表示苯甲酰基或式R 2的基团 其中R 2表示任选取代的烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基。 通式（I）的新产品具有显着的抗肿瘤活性。

    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    10.
    发明授权
    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments 失效
    法呢基转移酶抑制剂，它们的制备，含有它们的药物组合物及其在制备药物中的用途

    公开(公告)号：US6124465A

    公开(公告)日：2000-09-26

    申请号：US346540

    申请日：1999-07-02

    申请人： Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    发明人： Jean-Dominique Bourzat ,  Alain Commer.cedilla.on ,  Norbert Dereu ,  Patrick Mailliet ,  Fabienne Sounigo-Thompson ,  Jean-Paul Martin ,  Marc Capet ,  Michel Cheve

    IPC分类号： C07D209/56 ,  C07D233/56 ,  C07D401/08 ,  C07D209/80 ,  C07F9/28

    CPC分类号： C07D209/56

    摘要： Novel products of formula (I), their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments. ##STR1## In the formula (I), the following substituents are among the preferred: Ar represents a substituted or condensed phenyl radical or a polycyclic or heterocyclic aromatic radical, R represents a radical of general formula --(CH.sub.2).sub.m --X.sub.1 --(CH.sub.2).sub.n --Z in which X.sub.1 =single bond, O, S; m=0, 1; n=0, 1, 2; it being possible for the CH.sub.2 radicals to be substituted; Z represents carboxyl, COOR.sub.6 (R.sub.6 =alkyl), CON(R.sub.7)(R.sub.8) (R.sub.7 =hydrogen or alkyl and R.sub.8 =hydrogen, hydroxyl, arylsulphonyl, heterocyclyl, optionally substituted amino, optionally substituted alkyloxy or optionally substituted alkyl), PO(OR.sub.9).sub.2 (R.sub.9 =hydrogen or alkyl), an --NH--CO--T (T=hydrogen or optionally substituted alkyl) radical, or else--a ##STR2## radical, R.sub.1 and R.sub.2 =hydrogen or halogen or alkyl, alkyloxy, which is optionally substituted, alkylthio, alkyloxycarbonyl or else R.sub.1 and R.sub.2, at the ortho position with respect to one another, form an optionally substituted heterocycle containing 1 or 2 heteroatoms, R.sub.3 and R.sub.4 =hydrogen or halogen or alkyl, alkenyl, alkyloxy, alkylthio. carboxyl or alkyloxycarbonyl, R.sub.5 =hydrogen, alkyl, alkylthio, X=O or S or --NH--, --CO--, methylene, vinyldiyl, alkene-1,1-diyl or cycloalkane-1,1-diyl, and Y=O or S, in the racemic form, as well as the optical isomers (diastereomers and enantiomers) and the salts of the product of formula (I). The compounds of formula (I) are farnesyl transferase inhibitors which exhibit notable antitumor and antileukemic properties.

    摘要翻译： 式（I）的新产品，其制备方法，含有它们的药物组合物及其在制备药物中的用途。 在式（I）中，以下取代基是优选的：Ar表示取代或稠合的苯基或多环或杂环芳族基，R表示通式 - （CH 2）m -X1（CH 2）n Z 其中X1 =单键，O，S; m = 0,1， n = 0,1,2; CH2基可以被取代; Z代表羧基，COOR6（R6 =烷基），CON（R7）（R8）（R7 =氢或烷基，R8 =氢，羟基，芳基磺酰基，杂环基，任选取代的氨基，任选取代的烷氧基或任选取代的烷基），PO OR 9）2（R 9 =氢或烷基），-NH-CO-T（T =氢或任选取代的烷基）基团，或者 - 基团，R 1和R 2 =氢或卤素或烷基，烷氧基， 取代的烷硫基，烷氧基羰基，或者R1和R2相对于彼此的邻位，形成含有1或2个杂原子的任选取代的杂环，R 3和R 4 =氢或卤素或烷基，烯基，烷氧基，烷硫基。 羧基或烷氧基羰基，R5 =氢，烷基，烷硫基，X = O或S或-NH-，-CO-，亚甲基，乙烯基二烯基，烯-1,1-二基或环烷烃-1,1-二基，Y = O 或S，外消旋形式，以及光学异构体（非对映体和对映体）和式（I）的产物的盐。 式（I）化合物是具有显着的抗肿瘤和抗白血病性质的法呢基转移酶抑制剂。