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    Chemical compounds
    2.
    发明授权
    Chemical compounds 失效
    化合物

    公开(公告)号：US06436691B1

    公开(公告)日：2002-08-20

    申请号：US09011769

    申请日：1998-02-13

    申请人： Anthony Michael Slater ,  David Charles Blakey ,  David Huw Davies ,  John Frederick Hennam ,  Laurent Francois Andre Hennequin ,  Peter Robert Marsham ,  Robert Ian Dowell

    发明人： Anthony Michael Slater ,  David Charles Blakey ,  David Huw Davies ,  John Frederick Hennam ,  Laurent Francois Andre Hennequin ,  Peter Robert Marsham ,  Robert Ian Dowell

    IPC分类号： C12N964

    CPC分类号： B82Y5/00 ,  A61K47/6899 ,  C12N9/48

    摘要： Antibody Directed Enzyme Prodrug Therapy (ADEPT) systems for use in cancer based on mutated carboxypeptidase B (CPB) enzymes. Enzyme conjugates for ADEPT are substantially non-immunogenic in humans comprising a targeting moiety (for example an antibody) capable of binding with a tumor associated antigen, the targeting moiety being linked to a mutated form of a CPB enzyme capable of converting a prodrug into an antineoplastic drug wherein the prodrug is not significantly convertible into antineoplastic drug in humans by natural unmutated enzyme. A preferred enzyme mutant is human pancreatic CPB comprising a Lys or Arg residue at position 253. Suitable mustard prodrugs are disclosed in the specification.

    摘要翻译： 基于突变的羧肽酶B（CPB）酶的用于癌症的抗体定向酶前药治疗（ADEPT）系统。 用于ADEPT的酶缀合物在人中基本上是非免疫原性的，其包含能够与肿瘤相关抗原结合的靶向部分（例如抗体），所述靶向部分与能够将前药转化成为前体药物的CPB酶的突变形式连接 抗肿瘤药物，其中前药在天然未突变酶中不能显着转化成人类的抗肿瘤药物。 优选的酶突变体是人胰腺CPB，其包含位置253处的Lys或Arg残基。合适的芥子酰胺前药在说明书中公开。

    Anti-cancer compounds
    3.
    发明授权
    Anti-cancer compounds 失效
    抗癌化合物

    公开(公告)号：US5747499A

    公开(公告)日：1998-05-05

    申请号：US732273

    申请日：1996-10-29

    申请人： Vassilios Bavetsias ,  Francis Thomas Boyle ,  Laurent Francois Andre Hennequin ,  Jonathan Hugh Marriott

    发明人： Vassilios Bavetsias ,  Francis Thomas Boyle ,  Laurent Francois Andre Hennequin ,  Jonathan Hugh Marriott

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P29/00 ,  A61P35/00 ,  A61P37/08 ,  A61P43/00 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D403/04

    CPC分类号： C07D401/12 ,  C07D239/70 ,  Y02P20/55

    摘要： Cyclopentaquinazoline of the formula (I): ##STR1## wherein R.sup.1 is hydrogen, amino, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 hydroxyalkyl or C.sub.1-4 fluoroalkyl; wherein R.sup.2 is hydrogen, C.sub.1-4 alkyl, C.sub.3-4 alkenyl, C.sub.3-4 alkynyl, C.sub.2-4 hydroxyalkyl, C.sub.2-4 halogenoalkyl or C.sub.1-4 cyanoalkyl; Ar.sup.1 is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; and wherein R.sup.3 is a group of the formula: --A.sup.1 --Ar.sup.2 --A.sup.2 --Y.sup.1 in which A.sup.1, A.sub.2, Y.sup.1 and Ar.sub.2 are defined in claim 1; or a pharmaceutically acceptable salt or ester there of are of therapeutic value particularly in the treatment of cancer.

    摘要翻译： PCT No.PCT / GB95 / 01016 Sec。 371日期1996年10月29日第 102（e）日期1996年10月29日PCT提交1995年5月4日PCT公布。 WO95 / 30673 PCT出版物 日期：1995年11月16日式（I）的环戊基喹唑啉：其中R 1是氢，氨基，C 1-4烷基，C 1-4烷氧基，C 1-4羟基烷基或C 1-4氟代烷基; 其中R2是氢，C1-4烷基，C3-4烯基，C3-4炔基，C2-4羟烷基，C2-4卤代烷基或C1-4氰基烷基; Ar 1是亚苯基，噻吩二基，噻唑二基，吡啶二基或嘧啶二基，其可任选地具有一个或两个选自卤代，羟基，氨基，硝基，氰基，三氟甲基，C 1-4烷基和C 1-4烷氧基的取代基; 并且其中R 3是下列基团：A 1 -A 2 -A 2 -Y 1 y其中A 1，A 2，Y 1和Ar 2如权利要求1中所定义; 或其药学上可接受的盐或酯具有治疗价值，特别是在治疗癌症中。

    3-Cyano-quinoline derivatives
    5.
    发明授权
    3-Cyano-quinoline derivatives 失效
    3-氰基 - 喹啉衍生物

    公开(公告)号：US07173136B2

    公开(公告)日：2007-02-06

    申请号：US10532958

    申请日：2003-10-28

    申请人： Laurent Francois Andre Hennequin

    发明人： Laurent Francois Andre Hennequin

    IPC分类号： C07D215/38 ,  C07D215/44

    CPC分类号： C07D405/12

    摘要： The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or anti-proliferative agent in the containment and/or treatment of solid tumour disease

    摘要翻译： 本发明涉及式（I）的喹啉衍生物，其中Z 1，m，R 1，n，R 3，Z， > 2 和R 14具有上文在说明书中定义的任何含义; 其制备方法，含有它们的药物组合物及其在制备用作在实体瘤疾病的遏制和/或治疗中的抗侵袭或抗增殖剂的药物中的用途

    Quinazoline derivatives as VEGF inhibitors
    7.
    发明授权
    Quinazoline derivatives as VEGF inhibitors 有权
    喹唑啉衍生物作为VEGF抑制剂

    公开(公告)号：US07173038B1

    公开(公告)日：2007-02-06

    申请号：US10129336

    申请日：2000-11-01

    申请人： Andrew Peter Thomas ,  Elaine Sophie Elizabeth Stokes ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Elaine Sophie Elizabeth Stokes ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31/53 ,  A61K31/517 ,  A61K31/519 ,  C07D239/72

    CPC分类号： C07D401/12

    摘要： The invention relates to quinazoline derivatives of formula (I), wherein m is an integer from 1 to 3; R1 represents halogeno or C1-3alkyl; X1 represents —O—; R2 is selected from one of the following three groups: 1) C1-5alkylR3 (wherein R3 is piperidin-4-yl which may bear one or two substituents selected from hydroxy, halogeno, C1-4hydroxyalkyl and C1-4alkoxy; 2) C2-5alkenylR3 (wherein R3 is as defined hereinbefore); 3) C2-5alkynylR3 (wherein R3 is as defined hereinbefore); and wherein any alkyl, alkenyl or alkynyl group may bear one or more substituents selected from hydroxy, halogeno and amino; and salts thereof, processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as a active ingredient. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of number of disease states including cancer and rheumatoid arthritis.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中m为1至3的整数; R 1表示卤代或C 1-3烷基; X 1表示-O-; R 2选自以下三个基团之一：1）C 1-5烷基R 3（其中R 3，R 3，R 3， SUP>是可以具有一个或两个选自羟基，卤代，C 1-4 - 羟基烷基和C 1-4 - 烷氧基的取代基的哌啶-4-基; 2）C （其中R 3如上文所定义）;或其中R 3和R 3如上定义。 3）C 2-5炔基R 3（其中R 3如上定义）; 并且其中任何烷基，烯基或炔基可以具有一个或多个选自羟基，卤代和氨基的取代基; 及其盐，其制备方法，含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物。 式（I）化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗包括癌症和类风湿性关节炎在内的疾病状态的数量方面具有价值。

    Cinnoline compounds
    9.
    发明授权
    Cinnoline compounds 失效

    公开(公告)号：US06887874B2

    公开(公告)日：2005-05-03

    申请号：US10333592

    申请日：2001-08-07

    申请人： Laurent Francois Andre Hennequin

    发明人： Laurent Francois Andre Hennequin

    IPC分类号： A61K31/502 ,  A61K31/541 ,  A61P3/10 ,  A61P9/10 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/06 ,  C07D401/14 ,  C07D403/12 ,  C07D417/14 ,  C07D471/04 ,  C07D401/12

    CPC分类号： C07D401/14 ,  C07D403/12

    摘要： The invention relatest to compounds of the formula (I) wherein either any one of G1, G2, G3, G4 and G5 is nitrogen and the other four are —CH—, or G1, G2, G3, G4 and G5 are all —CH—; Z is —O—, —NH—, —S—, —CH2— or a direct bond; Z is linked to any one of G1, G2, G3 and G4 which is a free carbon atom; n is an integer from 0 to 5; any of the substitutents R1 may be attached at any free carbon atom of the indole, azaindole or indazole group; m is an integer from 0 to 3; Ra represents hydrogen; Rb represents hydrogen or another value as defined herein; R1 represents hydrogen, oxo, hydroxy, halogeno, C1-4alkyl, C1-4alkoxy, C1-4alkoxy, C1-4-alkyl, aminoC1-4alkyl, C1-3alkylaminoC1-4alkyl, di(C1-3alkyl)aminoC1-4alkyl, —C1-5alkyl(ring B) wherein ring B is selected from azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, N-methylpiperazinly, N-ethylpiperazinyl, morpholino and thiomorpholino; R2 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3aklylsulphanyl, —NR3R4 (wherein R3 and R4, which may be the same or different, each represents hydrogen or C1-3alkyl), or R5X1— (wherein R5 and X1 are as defined herein) and salts thereof, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and the use of a compound of formula I in the manufacture of medicament for the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    Cinnoline derivatives and use as medicine
    10.
    发明授权
    Cinnoline derivatives and use as medicine 失效
    噌啉衍生物用作药物

    公开(公告)号：US06514971B1

    公开(公告)日：2003-02-04

    申请号：US09142839

    申请日：1999-04-13

    申请人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31502

    CPC分类号： C07D401/12 ,  A61K31/502 ,  A61K31/5377 ,  C07D237/28 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to the use of cinnoline derivatives of formula (I) wherein Z represents —O—, —NH—, —S— or —CH2—; m is a n integer from 1 to 5; R1 represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoromethyl, Cp1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR6R7 (wherein R6 and R7, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, auoro, chioro, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4 represents hydrogen, hydroxy, halogeno, cyano, nitro, amino, trifluoromethyl, C1-3alkyl or a group R5—X1 (wherein X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR8CO—, —CONR9—, —SO2NR10—, —NR11SO2— or NR12— (wherein R8, R9, R10, R11 and R12 each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl) and R5 is an optionally substituted alkyl, carbocylic or heterocylic group which may be saturated or unsaturated and may be directly linked to the cinnoline ring or be linked via a carbon chain which may have heteroatom linking groups within it and salts thereof, in the manufacture of a medicament for use in the production of an anti angiogenic and/or vascular permeability reducing effect in a warmn-blooded animal such as a human being, processes for the preparation of such derivatives, pharmnaceutical compositions containing a compound of formula (I) or a pharmnaceutically acceptable salt thereof as active ingredient and compounds of formula (I). The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.

    摘要翻译： 本发明涉及式（I）的噌啉衍生物，其中Z表示-O - ， - NH - ， - S-或-CH 2 - ; m是1至5的n整数; R 1表示氢，羟基，卤代，硝基，氰基，三氟甲基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或NR 6 R 7（其中R 6和R 7可以相同或不同，各自表示氢或C 1-3烷基）。 R2代表氢，羟基，酰基，氯，甲氧基，氨基或硝基; R3表示羟基，卤代，C1-3烷基，C1-3烷氧基，C1-3烷酰氧基，三氟甲基，氰基，氨基或硝基; R 4表示氢，羟基，卤代，氰基，硝基，氨基，三氟甲基，C 1-3烷基或基团R 5 -X 1（其中X 1表示-O-，-CH 2 - ， - S - ， - SO-，-SO 2 - NR8CO-，-CONR9-，-SO2NR10-，-NR11SO2-或NR12-​​（其中R8，R9，R10，R11和R12各自独立地表示氢，C1-3烷基或C1-3烷氧基C2-3烷基），R5是任选取代的 烷基，碳环或杂环基团，其可以是饱和或不饱和的，并且可以直接连接到噌啉环，或者可以通过其中具有杂原子连接基团的碳链和其盐连接，制备用于 在温血动物例如人中产生抗血管生成和/或血管通透性降低作用，制备此类衍生物的方法，含有式（I）化合物或其药物上可接受的盐作为活性物质的药物组合物 成分和式（I）的化合物。式（I）的化合物 I）及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。