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    Quinazoline Derivatives as Angiogenesis Inhibitors
    41.
    发明申请
    Quinazoline Derivatives as Angiogenesis Inhibitors 审中-公开
    喹唑啉衍生物作为血管生成抑制剂

    公开(公告)号：US20120046300A1

    公开(公告)日：2012-02-23

    申请号：US13164310

    申请日：2011-06-20

    申请人： Laurent Francois Andre Hennequin

    发明人： Laurent Francois Andre Hennequin

    IPC分类号： A61K31/517 ,  A61P7/00 ,  C07D401/12

    CPC分类号： C07D401/14 ,  C07D403/10 ,  C07D403/14

    摘要： The present invention relates to compounds of the formula I: wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic, and which optionally may contain 1-3 heteroatoms selected independently from O, N and S; is —O— —NH— or —S—; is 0, 1, 2, 3, 4 or 5; is 0, 1, 2 or 3; and R2 and R1 are as defined herein; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I 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化合物：其中：环C是8,9,10,12或13元双环或三环部分，其部分可以是饱和或不饱和的，其可以是芳族或非芳族的，以及 其任选地可以含有1-3个独立地选自O，N和S的杂原子; 是-O-NH-或-S-; 是0，1，2，3，4或5; 是0，1，2或3; 并且R 2和R 1如本文所定义; 及其盐; 它们用于制造用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物中的用途; 制备这些化合物的方法; 含有式I化合物或其药学上可接受的盐的药物组合物和通过给予式I化合物或其药学上可接受的盐治疗涉及血管生成的疾病状态的方法。 式I的化合物抑制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。

    Quinazoline derivatives as angiogenesis inhibitors
    42.
    发明授权
    Quinazoline derivatives as angiogenesis inhibitors 失效
    喹唑啉衍生物作为血管生成抑制剂

    公开(公告)号：US07989460B2

    公开(公告)日：2011-08-02

    申请号：US10566842

    申请日：2004-08-05

    申请人： Laurent Francois Andre Hennequin

    发明人： Laurent Francois Andre Hennequin

    IPC分类号： A61K31/517

    CPC分类号： C07D401/14 ,  C07D403/10 ,  C07D403/14

    摘要： The present invention relates to compounds of the formula I: wherein: ring C is an 8, 9, 10, 12 or 13-membered bicyclic or tricyclic moiety which moiety may be saturated or unsaturated, which may be aromatic or non-aromatic, and which optionally may contain 1-3 heteroatoms selected independently from O, N and S; is —O— —NH— or —S—; is 0, 1, 2, 3, 4 or 5; is 0, 1, 2 or 3; and R2 and R1 are as defined herein; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals; processes for the preparation of such compounds; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I 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化合物：其中：环C是8,9,10,12或13元双环或三环部分，其部分可以是饱和或不饱和的，其可以是芳族或非芳族的，以及 其任选地可以含有1-3个独立地选自O，N和S的杂原子; 是-O-NH-或-S-; 是0，1，2，3，4或5; 是0，1，2或3; 并且R 2和R 1如本文所定义; 及其盐; 它们用于制造用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物中的用途; 制备这些化合物的方法; 含有式I化合物或其药学上可接受的盐的药物组合物和通过给予式I化合物或其药学上可接受的盐治疗涉及血管生成的疾病状态的方法。 式I的化合物抑制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。

    Quinazoline derivatives and pharmaceutical compositions containing them
    44.
    再颁专利
    Quinazoline derivatives and pharmaceutical compositions containing them 失效
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：USRE42353E1

    公开(公告)日：2011-05-10

    申请号：US12170027

    申请日：1997-09-23

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Edward Clayton ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： C07D239/72 ,  C07D401/00 ,  C07D403/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (1) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, —CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and 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（1）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6可以相同或不同，各自表示氢或C 1-3烷基 ）; R2代表氢，羟基，卤代，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; X 1表示-O - ， - CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO-，-CONR 8 - ， - SO 2 NR 9 - ， - NR 10 SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10 和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可带有末端任选取代的 选自烷基和5或6元饱和碳环或杂环基团的基团，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在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。

    Quinoline Derivatives Having Vegf Inhibiting Activity
    45.
    发明申请
    Quinoline Derivatives Having Vegf Inhibiting Activity 审中-公开
    喹啉衍生物具有抑制活性

    公开(公告)号：US20080312273A1

    公开(公告)日：2008-12-18

    申请号：US11947533

    申请日：2007-11-29

    申请人： Laurent Francois Andre Hennequin

    发明人： Laurent Francois Andre Hennequin

    IPC分类号： A61K31/47 ,  C07D215/16 ,  A61P9/00

    CPC分类号： C07D401/12 ,  C07D401/14

    摘要： The invention relates to compounds of 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 direct bond; Z is linked to any one of G1, G2, G3, and G4; n is an integer from 0 to 5; m is an integer from 0 to 3; Ra represents hydrogen or fluoro; Rb, R1 and R2 are defined herein and salt thereof, process for the preparation so 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 a 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 diseases states including cancer and rheumatoid arthritis.

    摘要翻译： 本发明涉及式（I）化合物，其中：G 1，G 2，G 3，G 4和G 5中的任一个为氮，其余四个为-CH-或G 1，G 3，G 3，G 4和G 5均为-CH- ; Z是-O-，-NH-，-S-，-CH 2 - 或直接键; Z连接到G1，G2，G3和G4中的任一个; n为0〜5的整数， m是0至3的整数; Ra表示氢或氟; 本文定义了Rb，R1和R2及其盐，制备方法使得这些化合物，含有式I化合物的药物组合物或其药学上可接受的盐作为活性成分，以及式I化合物在制备 用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物。 式I化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

    Quinazoline compounds
    46.
    发明授权
    Quinazoline compounds 失效
    喹唑啉化合物

    公开(公告)号：US07160889B2

    公开(公告)日：2007-01-09

    申请号：US10240658

    申请日：2001-04-03

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

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

    IPC分类号： C07D239/00 ,  C07D239/70 ,  A01N47/40

    CPC分类号： C07D401/12 ,  C07D239/94 ,  C07D403/12 ,  C07D417/12

    摘要： The invention concerns quinazoline derivatives of Formula (I) wherein ring A is phenyl or a 5-or 6-membered heterocyclic ring which may be saturated, partially saturated or unsaturated and may be aromatic or non-aromatic and which contains 1, 2 or 3 ring heteroatoms selected from O, N and S; Z is —O—, —NH— or —S—; and X1, R1, R2, R3, m and R4 have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in producing an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, and in the treatment of disease states such as cancer, rheumatoid arthritis and psorlasis.

    摘要翻译： 本发明涉及式（I）的喹唑啉衍生物，其中环A是苯基或5-或6-元杂环，其可以是饱和的，部分饱和的或不饱和的，并且可以是芳族或非芳族的并且含有1,2或3 选自O，N和S的环杂原子; Z是-O - ， - NH-或-S-; 和X 1，R 1，R 2，R 3，m和R 4， SUP>具有描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在温血动物中产生抗血管生成和/或血管通透性降低作用的用途，以及治疗疾病状态如癌症，类风湿性关节炎和游丝氨酸酶的用途。

    Quinoline derivatives inhibiting the effect of growth factors such as VEGF
    48.
    发明授权
    Quinoline derivatives inhibiting the effect of growth factors such as VEGF 失效
    喹啉衍生物抑制生长因子如VEGF的作用

    公开(公告)号：US06809097B1

    公开(公告)日：2004-10-26

    申请号：US09254440

    申请日：1999-03-09

    申请人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin ,  Patrick Ple

    发明人： Andrew Peter Thomas ,  Laurent Francois Andre Hennequin ,  Patrick Ple

    IPC分类号： C07D21522

    CPC分类号： C07D215/233 ,  C07D215/44 ,  C07D215/48 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D401/12 ,  C07D417/12 ,  C07D471/04

    摘要： Compounds of the formula (I): wherein: R2 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; n is an integer from 0 to 5; Z represents —O—, —NH—, —S— or —CH2—; G1 represents phenyl or a 5-10 membered heteroaromatic cyclic or bicyclic group; Y1, Y2, Y3 and Y4 each independently represents carbon or nitrogen; R1 represents fluoro or hydrogen; m is an integer from 1 to 3; R3 represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl, C1-3alkyl, —NR4R5 (wherein R4 and R5, can each be hydrogen or C1-3alkyl), or a group R6—X1— wherein X1 represents —CH2— or a heteroatom linker group and R6 is an alkyl, alkenyl or alkynyl chain optionally substituted by for example hydroxy, amino, nitro, alkyl, cycloalkyl, alkoxyalkyl, or an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring, which alkyl, alkenyl or alkynyl chain may have a heteroatom linker group, or R6 is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals such as humans, processes for the preparation of such derivatives, pharmaceutical compositions containing a compound of formula I or a pharmaceutically 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： 式（I）的化合物：其中：R 2表示羟基，卤代，C 1-3烷基，C 1-3烷氧基，C 1-3烷酰氧基，三氟甲基，氰基，氨基或硝基; n为0〜5的整数， Z表示-O - ， - NH - ， - S-或-CH 2 - ; G 1表示苯基或5-10元杂芳族环状或双环基团; Y 1，Y 2，Y 3和Y 4各自独立地表示碳或氮; R 1表示氟或氢; m为1〜3的整数; R 3表示氢，羟基，卤代，氰基，硝基，三氟甲基，C 1-3烷基，-NR 4 R 5（其中R 4和R 5各自可以是氢或C 1-3烷基 ）或基团R 6 -X 1 - ，其中X 1表示-CH 2 - 或杂原子连接基团，R 6是任选被例如羟基，氨基， ，硝基，烷基，环烷基，烷氧基烷基或选自吡啶酮，苯基和杂环的任选取代的基团，该烷基，烯基或炔基链可具有杂原子连接基团，或R 6为任选取代的基团， 吡啶酮，苯基和杂环及其盐在制备用于在温血动物如人类中产生抗血管生成和/或血管通透性降低作用的药物中的用途，制备这些衍生物的方法，药物 含有式I化合物或其药学上可接受的盐的组合物具有活性 式I化合物和式I化合物及其药学上可接受的盐抑制VEGF在治疗许多疾病状态（包括癌症和类风湿性关节炎）中的价值的性质。

    Quinazoline derivatives and pharmaceutical compositions containing them
    49.
    发明授权
    Quinazoline derivatives and pharmaceutical compositions containing them 有权
    喹唑啉衍生物和含有它们的药物组合物

    公开(公告)号：US06673803B2

    公开(公告)日：2004-01-06

    申请号：US10080716

    申请日：2002-02-25

    申请人： Andrew Peter Thomas ,  Craig Johnstone ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    发明人： Andrew Peter Thomas ,  Craig Johnstone ,  Elaine Sophie Elizabeth Stokes ,  Jean-Jacques Marcel Lohmann ,  Laurent Francois Andre Hennequin

    IPC分类号： A61K31517

    CPC分类号： C07D401/12 ,  A61F13/02 ,  A61F13/023 ,  A61F2013/00221 ,  A61F2013/8408 ,  A61K31/517 ,  A61K31/541 ,  C07D239/94 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12

    摘要： The invention relates to quinazoline derivatives of formula (I) wherein m is an integer from 1 to 2; R1 represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or —NR5R6 (wherein R5 and R6, which may be the same or different, each represents hydrogen or C1-3alkyl); R2 represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R3 represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X1 represents —O—, CH2—, —S—, —SO—, —SO2—, —NR7CO—, —CONR8—, —SO2NR9—, —NR10SO2— or —NR11— (wherein R7, R8, R9, R10 and R11 each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl);R4 represents an optionally substituted 5 or 6 membered saturated carbocyclic or heterocyclic group or a group which is alkenyl, alkynyl or optionally substituted alkyl, which alkyl group may contain a heteroatom linking group, which alkenyl, alkynyl or alkyl group may carry a terminal optionally substituted group selected from alkyl and a 5 or 6 membered saturated carbocyclic or heterocyclic group, and salts thereof; processes for their preparation, pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula (I) and 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）的喹唑啉衍生物，其中m为1至2的整数; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，C 1-3烷基，C 1-3烷氧基，C 1-3烷硫基或-NR 5 R 6（其中R 5和R 6） ，其可以相同或不同，各自表示氢或C 1-3烷基）; R 2表示氢，羟基，卤代，甲氧基，氨基或硝基; R 3表示羟基，卤代，C 1-3烷基，C 1-3烷氧基，C 1-3烷酰氧基，三氟甲基，氰基，氨基或硝基; X 1表示-O-，CH 2 - ， - S - ， - SO - ， - SO 2 - ， - NR 7 CO - ， - CONR 8 - ， - SO 2 NR 9 - SO 2 - 或-NR 11 - （其中R 7，R 8，R 9，R 10和R 11各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - ）; R 4表示任选取代的5或6元饱和碳环或杂环基团或为烯基，炔基或任选取代的烷基的基团，该烷基可含有杂原子连接基团，该烯基，炔基或烷基可以 携带选自烷基和5或6元饱和碳环或杂环基的任选被取代的基团及其盐; 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在治疗许多疾病状态（包括癌症和类风湿性关节炎）中具有价值的性质。

    Chemical compounds
    50.
    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。