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22 条记录 (耗时 0.036 秒)

    Process of making substituted pyrazoles
    4.
    发明授权
    Process of making substituted pyrazoles 有权
    制备取代的吡唑的方法

    公开(公告)号：US06407238B1

    公开(公告)日：2002-06-18

    申请号：US09698442

    申请日：2000-10-27

    申请人： James A. Baron ,  Vittorio Farina ,  Nizar Haddad

    发明人： James A. Baron ,  Vittorio Farina ,  Nizar Haddad

    IPC分类号： C07D40304

    CPC分类号： C07D231/12

    摘要： Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.

    摘要翻译： 公开了在酸性条件下由具有各种1,3-双官能底物的取代的二苯甲酮腙制备取代的吡唑的方法。 吡唑化合物可用于制备药物化合物。

    7,8-cyclopropataxanes
    5.
    发明授权
    7,8-cyclopropataxanes 失效
    7,8-环丙烷

    公开(公告)号：US5254580A

    公开(公告)日：1993-10-19

    申请号：US29819

    申请日：1993-03-11

    申请人： Shu-Hui Chen ,  Vittorio Farina

    发明人： Shu-Hui Chen ,  Vittorio Farina

    IPC分类号： C07D305/14 ,  A01N43/02 ,  C07C305/00

    CPC分类号： C07D305/14

    摘要： An antitumor compound of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is t-butyloxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.3 is OCOR, --OCOOR, H, or OH; R.sup.4 is hydrogen; or R.sup.3 and R.sup.4 jointly form a carbonyl group; and R is C.sub.1-6 alkyl.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.

    摘要翻译： 式I的抗肿瘤化合物，其中R 1为-COR z，其中R z为叔丁氧基，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或苯基，任选被 一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CF 3基团; R 2是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或式-W-Rx的基团，其中W是键，C 2-6亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，呋喃基，噻吩基或苯基，此外Rx可以任选地被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CF 3基团取代; R3是OCOR，-OCOOR，H或OH; R4是氢; 或R3和R4共同形成羰基; 且R为C 1-6烷基。 本发明还提供了药物制剂（组合物）和用式I化合物治疗哺乳动物肿瘤的方法。

    6,7-modified paclitaxels
    7.
    发明授权
    6,7-modified paclitaxels 失效
    6,7修饰紫杉醇

    公开(公告)号：US5380751A

    公开(公告)日：1995-01-10

    申请号：US128619

    申请日：1993-09-28

    申请人： Shu-Hui Chen ,  Vittorio Farina ,  Gregory Roth ,  John Kadow

    发明人： Shu-Hui Chen ,  Vittorio Farina ,  Gregory Roth ,  John Kadow

    IPC分类号： A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07F7/18 ,  A61K31/335

    CPC分类号： C07D407/12 ,  C07D305/14 ,  C07D409/12 ,  C07D413/12 ,  C07F7/1856

    摘要： The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.Z is RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.a is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR;R.sup.b and R.sup.c are both hydroxy or together form a bond with the carbon atoms to which they are attached; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.

    摘要翻译： 本发明提供式I的紫杉醇衍生物，其中R 1是其中R Z是RO-或R的-CORz; R 2是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或式-W-Rx的基团，其中W是键，C 2-6亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，苯基或杂芳基，此外Rx可任选地被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CF 3基团取代; R a是-OCOR，H，OH，-OR，-OSO 2 R，-OCONRoR，-OCONHR，-OCOO（CH 2）t R或-OCOOR; Rb和Rc都是羟基或与它们所连接的碳原子一起形成键; 并且R和R 4独立地是C 1-6烷基，C 2-6烯基，C 3-6环烷基，C 2-6炔基或苯基，任选地被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或 -CF3组。 本发明还提供了药物制剂（组合物）和用式I化合物治疗哺乳动物肿瘤的方法。

    Processes for making cephems from allenylazetidinone derivatives
    8.
    发明授权
    Processes for making cephems from allenylazetidinone derivatives 失效
    从烯丙基氮杂环丁酮衍生物制备头孢烯的方法

    公开(公告)号：US5162521A

    公开(公告)日：1992-11-10

    申请号：US711250

    申请日：1991-06-06

    申请人： Vittorio Farina ,  Stephen R. Baker

    发明人： Vittorio Farina ,  Stephen R. Baker

    IPC分类号： C07D501/00 ,  C07D501/10

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： This invention relates to a novel process for making a cephem of formula II from 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate of formula I. In another aspect, this invention is concerned with a process of further converting a compound of formula II into an antibacterial cephem of formula III. ##STR1## In formulae I, II and III, R.sup.1 is hydrogen, a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.

    摘要翻译： 本发明涉及由式I的2-（3-氨基-2-氧代 - 氮杂环丁烷-1-基）-2,3-丁二烯酸制备式II的头孢烯的新方法。另一方面，本发明涉及 其具有将式II化合物进一步转化成式III的抗菌头孢烯的方法。 在式I，II和III中，R 1是氢，常规的氨基保护基或酰基; R2是芳族杂环或芳基; R3是常规的羧基保护基或-CO 2 R 3一起形成生理上可水解的酯; 并且R 4是选自C 1-6烷基，C 2-6烯基，C 2-6炔基，环C 3-6烷基和芳基的基团。 n为0或2。

    Taxol derivatives
    9.
    发明授权
    Taxol derivatives 失效
    紫杉醇衍生物

    公开(公告)号：US5248796A

    公开(公告)日：1993-09-28

    申请号：US900365

    申请日：1992-06-18

    申请人： Shu-Hui Chen ,  Vittorio Farina

    发明人： Shu-Hui Chen ,  Vittorio Farina

    IPC分类号： C07D305/14

    CPC分类号： C07D305/14 ,  C07C2103/80

    摘要： The present invention relates to 10-desacetoxy-11,12-dihydrotaxol-10,12(18)-diene derivatives which are useful as antitumor agents and as intermediates for the preparation of 10-desacetoxytaxol. Also disclosed is a novel process for the preparation of 10-desacetoxytaxol which comprises treating hydroxy protected 10-deacetyltaxol with 1,1,2-trifluoro-2-chlorotriethylamine followed by catalytic hydrogenation.

    摘要翻译： 本发明涉及可用作抗肿瘤剂的10-脱乙酰氧基-11,12-二氢塔考醇-10,12（18） - 二烯衍生物，作为制备10-脱乙酰氧基紫杉醇的中间体。 还公开了一种用于制备10-脱乙酰氧基紫杉醇的新方法，其包括用1,1,2-三氟-2-氯三乙胺处理羟基保护的10-脱乙酰紫杉醇，然后催化氢化。

    Fluoro taxols
    10.
    发明授权
    Fluoro taxols 失效

    公开(公告)号：US5192796A

    公开(公告)日：1993-03-09

    申请号：US907261

    申请日：1992-07-01

    申请人： Shu-Hui Chen ,  Vittorio Farina

    发明人： Shu-Hui Chen ,  Vittorio Farina

    摘要： This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is benzoyl or t-butyloxycarbonyl; R.sup.2 is acetoxy, hydrogen or hydroxy; and the wavy line indicates either the .alpha.- or the .beta.-configuration.Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.