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    Farnesyl transferase inhibitors, their preparation, the pharmaceutical compositions which contain them and their use in the preparation of medicaments
    3.
    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。

    Process for the preparation of taxane derivatives
    5.
    发明授权
    Process for the preparation of taxane derivatives 失效
    紫杉烷衍生物的制备方法

    公开(公告)号：US5861515A

    公开(公告)日：1999-01-19

    申请号：US962011

    申请日：1997-10-31

    申请人： Alain Commercon ,  Eric Didier ,  Elie Fouque

    发明人： Alain Commercon ,  Eric Didier ,  Elie Fouque

    IPC分类号： A61K31/335 ,  A61K31/337 ,  A61K31/42 ,  A61K31/421 ,  A61P35/00 ,  C07D263/04 ,  C07D263/06 ,  C07D305/14 ,  C07D413/12

    CPC分类号： C07D263/04 ,  C07D305/14 ,  C07D413/10 ,  C07D413/12 ,  Y02P20/55

    摘要： This invention relates to a method of preparing taxane derivatives of formula (VIII) by esterification of protected baccatin III or 10-deacetylbaccatin III by means of an acid of formula (VII), elimination of protection groupings and acylation of the amine function of the side chain. In formulae (VIII) and (VII): Ar stands for aryl, R.sub.3 is a trihalomethyl radical or phenyl substituted by a trihalomethyl radical, R.sub.4 is a hydrogen atom or is the same as R.sub.1. G.sub.1 and G.sub.2 are hydroxy protecting groups. ##STR1##

    摘要翻译： 本发明涉及通过用式（Ⅶ）的酸酯化保护的浆果赤霉素III或10-脱乙酰基浆果赤霉素III，消除保护基和酰胺化功能的方法来制备式（Ⅷ）的紫杉烷衍生物的方法 链。 在式（VIII）和（VII）中：Ar表示芳基，R3表示三卤代甲基或被三卤甲基取代的苯基，R4表示氢原子或与R1相同。 G1和G2是羟基保护基。

    L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1! heptane compounds
    7.
    发明授权
    L-tartaric acid salt of a (1R) diastereomer of a 2-azadihydroxybicyclo�2.2.1!heptane compound and the preparation of 2-azabicyclo�2.2.1! heptane compounds 失效
    2-氮杂双环[2.2.1]庚烷化合物的（1R）非对映异构体的L-酒石酸盐和2-氮杂双环[2.2.1]庚烷化合物的制备

    公开(公告)号：US5831096A

    公开(公告)日：1998-11-03

    申请号：US873284

    申请日：1997-06-10

    申请人： Patrick Leon ,  Michael O'Brien ,  Denis Largeau ,  Matthew Powers ,  Ching Tsuei

    发明人： Patrick Leon ,  Michael O'Brien ,  Denis Largeau ,  Matthew Powers ,  Ching Tsuei

    IPC分类号： C07D491/18 ,  C07D209/02 ,  C07D209/52 ,  C07D491/12

    CPC分类号： C07D209/52 ,  C07D209/02 ,  Y02P20/55

    摘要： A method for the preparation of a compound of formula ##STR1## wherein R is hydrogen or, respectively, a group of formula ##STR2## R.sub.1 is alkyl; Ar is optionally substituted aryl; and R.sub.3' and R.sub.3" are hydrogen, alkyl or phenyl, or R.sub.3' and R.sub.3" taken together with the carbon atom to which they are attached form cycloalkyl, or salt thereof, comprising acid facilitated acetalizing or ketalizing of a compound of formula ##STR3## wherein R.sub.3' and R.sub.3" are as defined above, and R.sub.4' and R.sub.4" are alkoxy, or taken together with the carbon atom to which they are attached form carbonyl, with a compound of formula ##STR4## wherein * represents an R chirality; R, R.sub.1 and Ar are as defined above, or salt thereof in isopropanol.

    摘要翻译： 其中R为氢或分别为式（II）或（II）的基团的式的化合物的方法R1为烷基; Ar是任选取代的芳基; 并且R 3'和R 3“是氢，烷基或苯基，或者R 3'和R 3”与它们所连接的碳原子一起形成环烷基，或其盐，其包含酸容易地使下式化合物进行缩醛化或缩酮化 其中R 3'和R 3“如上定义，并且R 4'和R 4”是烷氧基，或者与它们所连接的碳原子一起形成羰基的化合物与式 ）其中*表示R手性; R，R 1和Ar如上所定义，或其盐在异丙醇中。

    Process for the preparation of a 1,3-oxazolidine-5-carboxylic acid
    9.
    发明授权
    Process for the preparation of a 1,3-oxazolidine-5-carboxylic acid 失效
    制备1,3-恶唑烷-5-羧酸的方法

    公开(公告)号：US5811550A

    公开(公告)日：1998-09-22

    申请号：US897650

    申请日：1997-07-21

    申请人： Jean-Noel Denis ,  Andrew-Elliot Greene ,  Alice Kanazawa

    发明人： Jean-Noel Denis ,  Andrew-Elliot Greene ,  Alice Kanazawa

    IPC分类号： C07D263/06 ,  C07D263/04

    CPC分类号： C07D263/04

    摘要： Method for the preparation of 1,3-oxazolidin 5-carboxylic acid having the general formula (I) ##STR1## from a product having the general formula (II) ##STR2## In the general formulas (I) and (II), Ar is an aryl radical, R.sub.1 is a benzoyl radical or a radical R.sub.2 --O--CO-- wherein R.sub.2 is an alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkenyl, bicycloalkyl, phenyl or heterocyclyl radical, Ph is an optionally substituted phenyl radical, X is the residue of an optically active organic base or an alkoxy radical optionally substituted by a phenyl radical. The acids of formulas (I) and (II) are particularly useful in preparing taxol, Taxotere or analogs thereof which have remarkable antitumor and antileukemia properties.

    摘要翻译： PCT No.PCT / FR93 / 01133 Sec。 371日期1995年5月19日 102（e）日期1995年5月19日PCT提交1993年11月18日PCT公布。 公开号WO94 / 12482 日本时间1994年6月9日制备具有通式（I）或（II）的1,3-恶唑烷-5-羧酸的方法在通式（I）和（II）中，Ar为 芳基，R 1是苯甲酰基或基团R 2 -O-CO-，其中R 2是烷基，烯基，炔基，环烷基，环烯基，双环烷基，苯基或杂环基，Ph是任选取代的苯基，X是 光学活性有机碱或任选被苯基取代的烷氧基的残基。 式（I）和（II）的酸特别可用于制备具有显着的抗肿瘤和抗白血病性质的紫杉醇，泰索帝或其类似物。