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1. 发明申请

WO1997022596A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1997022596A1
公开(公告)日：1997-06-26
申请号：PCT/GB1996003075
申请日：1996-12-13
申请人： ZENECA LIMITED , ZENECA-PHARMA S.A. , LOHMANN, Jean-Jacques, Marcel , HENNEQUIN, Laurent, François, André , THOMAS, Andrew, Peter
发明人： ZENECA LIMITED , ZENECA-PHARMA S.A.
IPC分类号： C07D239/94
CPC分类号： C07D403/12 , C07D239/88 , C07D239/94 , C07D401/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to quinazoline derivatives of formula (I) [wherein: Y represents -O-, -S-, -CH2-, -SO-, -SO2-, -NR CO-, -CONR -, -SO2NR -, -NR SO2- or -NR - (wherein R , R , R , R and R each independently represents hydrogen, alkyl or alkoxyalkyl); R represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino. R represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro; m is an integer from 1 to 5; R represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R represents a group which is or which contains an optionally substituted pyridone, phenyl or aromatic heterocyclic group] and salts thereof; processes for their preparation and pharmaceutical compositions containing a compound of formula (I) or a pharmaceutically acceptable salt thereof as 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 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：Y 1表示-O - ， - S - ， - CH 2 - ， - SO - ， - SO 2 - ， - NR 5 CO-，-CONR 6 - ， - SO 2 NR 7 - ，-NR 8 SO 2 - 或-NR 9 - （其中R 5，R 6，R 7，R 8和R 9 >各自独立地表示氢，烷基或烷氧基烷基）; R 1表示氢，羟基，卤代，硝基，三氟甲基，氰基，烷基，烷氧基，烷硫基，氨基或烷基氨基。 R 2表示氢，羟基，卤代，烷基，烷氧基，三氟甲基，氰基，氨基或硝基; m为1〜5的整数; R 3表示羟基，卤代，烷基，烷氧基，烷酰氧基，三氟甲基，氰基，氨基或硝基; R 4表示含有任选取代的吡啶酮，苯基或芳族杂环基团的基团及其盐; 其制备方法和含有式（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，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

2. 发明申请

WO1996020011A1 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO1996020011A1
公开(公告)日：1996-07-04
申请号：PCT/GB1995002991
申请日：1995-12-21
申请人： ZENECA LIMITED , TAYLORSON, Christopher, John , EGGELTE, Hendrikus, Johannes , TARRAGONA-FIOL, Antonio , RABIN, Brian, Robert , BOYLE, Francis, Thomas , HENNAM, John, Frederick , BLAKEY, David, Charles , MARSHAM, Peter, Robert , HEATON, David, William , DAVIES, David, Huw , SLATER, Anthony, Michael , HENNEQUIN, Laurent, François, André
发明人： ZENECA LIMITED
IPC分类号： A61K47/48
CPC分类号： B82Y5/00 , A61K47/6899 , C12N9/48
摘要： Improved systems for targetted enzyme prodrug therapy, especially antibody directed enzyme prodrug therapy (ADEPT), in which the enzyme used is a mutated form of a host enzyme in which the natural host enzyme, such as ribonuclease, recognises its natural substrate by an ion pair interaction and this interaction is reversed ("reversed polarity") in the design of mutated enzyme and complementary prodrug.
摘要翻译：用于靶向酶前药治疗的改进的系统，特别是抗体定向酶前药治疗（ADEPT），其中使用的酶是宿主酶的突变形式，其中天然宿主酶如核糖核酸酶通过离子对识别其天然底物在突变酶和互补前药的设计中，相互作用被逆转（“反极性”）。

3. 发明申请

WO1998013350A1 QINOLINE DERIVATIVES INHIBITING THE EFFECT OF GROWTH FACTORS SUCH AS VEGF 审中-公开
标题翻译：抑制生长因子如VEGF的作用的喹啉衍生物
公开(公告)号：WO1998013350A1
公开(公告)日：1998-04-02
申请号：PCT/GB1997002587
申请日：1997-09-23
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André , PLE, Patrick, Alan
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D215/22
CPC分类号： C07D215/233 , C07D215/44 , C07D215/48 , C07D231/12 , C07D233/56 , C07D249/08 , C07D401/12 , C07D417/12 , C07D471/04
摘要： The invention relates to the use of compounds of formula (I) wherein: R 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-; G represents phenyl or a 5-10 membered heteroaromatic cyclic or bicyclic group; Y , Y , Y and Y each independently represents carbon or nitrogen; R represents fluoro or hydrogen; m is an integer from 1 to 3; R represents hydrogen, hydroxy, halogeno, cyano, nitro, trifluoromethyl; C1-3alkyl, -NR R (wherein R and R can each be hydrogen or C1-3alkyl), or a group R -X - wherein X represents -CH2- or a heteroatom linker group and R 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 R 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：本发明涉及式（I）化合物的用途，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，烷氧基烷基或任选取代的基团取代的烷基，烯基或炔基链，其选自吡啶酮，苯基和杂环，其中烷基，烯基或炔基链可以具有杂原子连接基团，或者R 6是选自吡啶酮，苯基和杂环的任选取代的基团及其盐，用于制备用于用于生产温血动物如人的抗血管生成和/或血管通透性降低作用，制备此类衍生物的方法，含有式（I）化合物或其药学上可接受的盐作为活性成分的药物组合物和式（I）的化合物。式（I）化合物及其药学上可接受的盐抑制VEGF的作用，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

4. 发明申请

WO1997034876A1 CINNOLINE DERIVATIVES AND USE AS MEDICINE 审中-公开
标题翻译： CINNOLINE DORIVATIVES和用作医药
公开(公告)号：WO1997034876A1
公开(公告)日：1997-09-25
申请号：PCT/GB1997000650
申请日：1997-03-11
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D237/28
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 an integer from 1 to 5; R represents hydrogen, hydroxy, halogeno, nitro, cyano, trifluoromethyl, C1-3alkyl, C1-3alkoxy, C1-3alkylthio or NR R (wherein R and R , which may be the same or different, each represents hydrogen or C1-3alkyl); R represents hydrogen, hydroxy, fluoro, chloro, methoxy, amino or nitro; R represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R represents hydrogen, hydroxy, halogeno, cyano, nitro, amino, trifluoromethyl, C1-3alkyl or a group R -X (wherein X represents -O-, -CH2-, -S-, -SO-, -SO2-, -NR CO-, -CONR -, -SO2NR -, -NR SO2- or -NR - (wherein R , R , R , R and R each independently represents hydrogen, C1-3alkyl or C1-3alkoxy C2-3alkyl) and R is an optionally substituted alkyl, carbocyclic or heterocyclic 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 antiangiogenic and/or vascular permeability reducing effect in a warm-blooded animal such as a human being, 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：本发明涉及式（I）的噌啉衍生物的用途，其中Z表示-O - ， - NH - ， - S-或-CH 2 - ; m为1〜5的整数; 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）; R 2表示氢，羟基，氟，氯，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; 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 - ， - NR 8 CO - ， - CONR 9 - ， - SO 2 NR 10 - ，-NR 11 SO 2 - 或-NR 12 - （其中R R 9，R 10，R 11和R 12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 5是任选取代的烷基，可以是饱和或不饱和的并且可以直接连接到噌啉环的碳环或杂环基团，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，制备用于制备在温血动物如人类中的抗血管生成和/或血管渗透性降低作用，制备这种衍生物的方法，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和化合物的式（I ）。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。

5. 发明申请

WO1997007769A2 CHEMICAL COMPOUNDS 审中-公开
标题翻译：化学化合物
公开(公告)号：WO1997007769A2
公开(公告)日：1997-03-06
申请号：PCT/GB1996001975
申请日：1996-08-13
申请人： ZENECA LIMITED , BLAKEY, David, Charles , DAVIES, David, Huw , DOWELL, Robert, Ian , HENNAM, John, Frederick , MARSHAM, Peter, Robert , SLATER, Anthony, Michael , HENNEQUIN, Laurent, François, André
发明人： ZENECA LIMITED
IPC分类号： A61K00/00
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 tumour 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。

6. 发明申请

WO1998013354A1 QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：喹诺酮衍生物和含有它们的药物组合物
公开(公告)号：WO1998013354A1
公开(公告)日：1998-04-02
申请号：PCT/GB1997002588
申请日：1997-09-23
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André , JOHNSTONE, Craig , STOKES, Elaine, Sophie, Elizabeth , LOHMANN, Jean-Jacques, Marcel , CLAYTON, Edward
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D239/94
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; R represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or -NR R (wherein R and R , which may be the same or different, each represents hydrogen or C1-3alkyl); R represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X represents -O-, -CH2-, -S-, -SO-, -SO2-, -NR CO-, -CONR -, -SO2NR -, -NR SO2- or -NR - (wherein R , R , R , R and R each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R 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 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 - （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 2-8环烷基） 1-3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，炔基或烷基可带有选自烷基和5或6元饱和碳环或杂环基的末端任选取代的基团及其盐; 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。

7. 发明申请

WO1997042187A1 OXINDOLE DERIVATIVES 审中-公开
标题翻译：氧化物衍生物
公开(公告)号：WO1997042187A1
公开(公告)日：1997-11-13
申请号：PCT/GB1997001211
申请日：1997-05-02
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew, Peter , HENNEQUIN, Laurent, François, André , LOHMANN, Jean-Jacques, Marcel , PLE, Patrick
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D403/04
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D401/14 , C07D403/04 , C07D403/14
摘要： The invention relates to compounds of formula (I), wherein: R represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino, nitro, C2-4alkanoyl, C1-4alkanoylamino, C1-4alkoxycarbonyl, C1-4alkylthio, C1-4alkylsulphinyl, C1-4alkylsulphonyl, carbamoyl, N -C1-4alkylcarbamoyl, N , N -di(C1-4alkyl)carbamoyl, aminosulphonyl, N -C1-4alkylaminosulphonyl, N , N -di(C1-4)alkyl)aminosulphonyl, C1-4alkylsulphonylamino, or a group R X wherein X represents a direct bond, C2-4alkanoyl, -CONR R -, -SO2NR R - or -SO2R - (wherein R and R , each independently represents hydrogen or C1-2alkyl and R , R and R each independently represents C1-4alkyl and wherein R is linked to R , R or R ) and R represents an optionally substituted group selected from phenyl and a 5 or 6-membered heterocyclic group; n is an integer from 0 to 4; R represents hydrogen, C1-4alkyl, C1-4alkoxymethyl, di(C1-4alkoxy)methyl or C1-4alkanoyl; m is an integer from 0 to 4; and R represents hydroxy, halogeno, nitro, trifluoromethyl, C1-3alkyl, cyano, amino or R X (wherein X represents a direct bond, -CH2-, or a single or double heteroatom linker group including -S-, -SO- and -NR - (wherein R represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl), and R is an 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 R is an optionally substituted group selected from pyridone, phenyl and a heterocyclic ring. The compounds of formula (I) and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF and FGF, properties 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：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，硝基，C 2-4烷酰基，C 1-4烷酰基氨基， C 1-4烷氧基羰基，C 1-4烷硫基，C 1-4烷基亚磺酰基，C 1-4烷基磺酰基，氨基甲酰基，N，C 1-4烷基氨基甲酰基，N，N，N，（C 1-4烷基）氨基甲酰基，氨基磺酰基，N，C 1-4烷基氨基磺酰基，N，N，N-二（C 1-4）烷基）氨基磺酰基， C 1-4烷基磺酰基氨基或基团R 4 X 1其中X 1表示直接键，C 2-4烷酰基，-CONR 5 - ， - SO 2 NR 7 R 8 - 或-SO 2 R 9 - （其中R 5和R 7各自独立地表示氢或C 1-2烷基，R 6，R 8和R 9各自独立地表示C 1-4烷基，并且其中 R 4与R 6，R 8或R 9连接），R 4表示任选取代的选自苯基和5或6元杂环基的基团; n为0〜4的整数; R 1表示氢，C 1-4烷基，C 1-4烷氧基甲基，二（C 1-4烷氧基）甲基或C 1-4烷酰基; m为0〜4的整数; 并且R 3表示羟基，卤代，硝基，三氟甲基，C 1-3烷基，氰基，氨基或R 10 X 2（其中X 2表示直接键，-CH 2 - 或单或双杂原子连接基团包括-S-，-SO-和-NR 15 - （其中R 15表示氢，C 1-3烷基或C 1-3烷氧基C 2-3 - 烷基），R 10是任选地被羟基，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取代，该烷基，烯基或炔基链可具有杂原子连接基团，或R 10 式（I）化合物及其药学上可接受的盐抑制VEGF和FGF的作用，在治疗多种疾病状态（包括癌症）中的价值性质和类风湿关节炎。

8. 发明申请

WO1997030035A1 QUINAZOLINE DERIVATIVES AS VEGF INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为VEGF抑制剂
公开(公告)号：WO1997030035A1
公开(公告)日：1997-08-21
申请号：PCT/GB1997000365
申请日：1997-02-10
申请人： ZENECA LIMITED , ZENECA PHARMA S.A. , THOMAS, Andrew Peter , JOHNSTONE, Craig , HENNEQUIN, Laurent, François, André
发明人： ZENECA LIMITED , ZENECA PHARMA S.A.
IPC分类号： C07D239/94
CPC分类号： C07D239/88 , C07D239/93 , C07D239/94
摘要： The invention relates to quinazoline derivatives of formula (I) [wherein: Z represents -O-, -NH- or -S-; m is an integer from 1 to 5; R represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, C1-3alkyl, C1-3alkoxy, C1-3alkylthio, or -NR R (wherein R and R , which may be the same or different, each represents hydrogen or C1-3alkyl); R represents hydrogen, hydroxy, halogeno, methoxy, amino or nitro; R represents hydroxy, halogeno, C1-3alkyl, C1-3alkoxy, C1-3alkanoyloxy, trifluoromethyl, cyano, amino or nitro; X represents -O-, -CH2-, -S-, -SO-, -SO2-, -NR -, -NR CO-, -CONR -, -SO2NR - or -NR SO2-, (wherein R , R , R , R and R each represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl); R represents 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 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 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）的喹唑啉衍生物[其中：Z表示-O - ， - NH-或-S-; m为1〜5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 - ， - NR 8 CO - ， - CONR 9 - 或其中R 7，R 8，R 9，R 10和R 11各自表示氢，C 1-3烷基或C 1-3烷氧基C 2- 1-3烷基）; R 4表示基团，其为烯基，炔基或任选取代的烷基，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5或6元饱和碳环或杂环基] 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，其在治疗许多疾病状态（包括癌症和类风湿性关节炎）中是有价值的。

9. 发明申请

WO1995030673A1 ANTI-CANCER COMPOUNDS CONTAINING CYCLOPENTAQUINAZOLINE RING 审中-公开
标题翻译：含有环丙基环己烷环的抗癌化合物
公开(公告)号：WO1995030673A1
公开(公告)日：1995-11-16
申请号：PCT/GB1995001016
申请日：1995-05-04
申请人： BRITISH TECHNOLOGY GROUP LIMITED , ZENECA LIMITED , BAVETSIAS, Vassilios , BOYLE, Francis, Thomas , HENNEQUIN, Laurent, François, André , MARRIOTT, Jonathan, Hugh
发明人： BRITISH TECHNOLOGY GROUP LIMITED , ZENECA LIMITED
IPC分类号： C07D403/12
CPC分类号： C07D401/12 , C07D239/70 , Y02P20/55
摘要： Cyclopentaquinazoline of formula (I), wherein R is hydrogen, amino, C1-4 alkyl, C1-4 alkoxy, C1-4 hydroxyalkyl or C1-4 fluoroalkyl; wherein R is hydrogen, C1-4 alkyl, C3-4 alkenyl, C3-4 alkynyl, C2-4 hydroxyalkyl, C2-4 halogenoalkyl or C1-4 cyanoalkyl; Ar is phenylene, thiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which may optionally bear one or two substituents selected from halogeno, hydroxy, amino, nitro, cyano, trifluoromethyl, C1-4 alkyl and C1-4 alkoxy; and wherein R is a group of the formula: -A -Ar -A -Y , in which A is a bond between the alpha -carbon atom of the group -CONHCH(CO2H)- and Ar or is a C1-2 alkylene group; Ar is phenylene, tetrazoldiyl, tiophenediyl, thiazolediyl, pyridinediyl or pyrimidinediyl which in the case of phenylene may optionally bear one or two substituents on the ring selected from halogeno, nitro, C1-4 alkyl and C1-4 alkoxy; A is a C1-3 alkylene or C2-3 alkenylene group; and a pharmaceutically acceptable salt or ester thereof are of therapeutic value particularly in the treatment of cancer.
摘要翻译：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氟烷基; 其中R 2是氢，C 1-4烷基，C 3-4烯基，C 3-4炔基，C 2-4羟基烷基，C 2-4卤代烷基或C 1-4氰基烷基; Ar 1是可以任选地带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烷氧基的取代基的亚苯基，噻吩二基，噻唑二基，吡啶二基或嘧啶二基。并且其中R 3是下列基团：-A 1 -Ar 2 -A 2 -Y 1，其中A 1是α-碳原子之间的键基团-CONHCH（CO 2 H） - 和Ar 2或是C 1-2亚烷基; Ar 2是亚苯基，四唑基，噻吩二基，噻唑二基，吡啶二基或嘧啶二基，其在亚苯基的情况下可以在选自卤代，硝基，C 1-4烷基和C 1-4烷氧基的环上任选地具有一个或两个取代基; A 2是C 1-3亚烷基或C 2-3亚烯基; 其药学上可接受的盐或酯具有治疗价值，特别是治疗癌症。

10. 发明申请

WO1994007869A1 QUINAZOLINE DERIVATIVES 审中-公开
标题翻译：喹诺酮衍生物
公开(公告)号：WO1994007869A1
公开(公告)日：1994-04-14
申请号：PCT/GB1993002015
申请日：1993-09-28
申请人： ZENECA LIMITED , BRITISH TECHNOLOGY GROUP LTD. , BARKER, Andrew, John , BOYLE, Francis, Thomas , HENNEQUIN, Laurent, François, André
发明人： ZENECA LIMITED , BRITISH TECHNOLOGY GROUP LTD.
IPC分类号： C07D239/90
CPC分类号： C07D401/12 , C07D239/90 , C07F9/65128
摘要： The invention relates to quinazoline derivatives of formula (I) wherein R1 includes hydrogen, amino, (1-4C)alkyl and (1-4C)alkoxy; R2 includes hydrogen, (1-4C)alkyl, (3-4C)alkenyl and (3-4C)alkynyl; Ar1 is phenylene or a 5- or 6-membered aromatic heterocyclene ring; Ar2 is optionally substituted phenyl or heteroaryl; and Q includes nitro, cyano, carbamoyl, (1-4C)alkylsulphonyl and NŸ ,NŸ -di-((1-4C)alkyl)sulphamoyl; or pharmaceutically acceptable salts thereof; to processes for their manufacture; to pharmaceutical compositions containing them; and to their use as anti-tumour agents.
摘要翻译：本发明涉及式（I）的喹唑啉衍生物，其中R 1包括氢，氨基，（1-4C）烷基和（1-4C）烷氧基; R2包括氢，（1-4C）烷基，（3-4C）烯基和（3-4C）炔基; Ar 1是亚苯基或5或6元芳族杂环烯环; Ar 2是任选取代的苯基或杂芳基; 并且Q包括硝基，氰基，氨基甲酰基，（1-4C）烷基磺酰基和N，N， - 二 - （（1-4C）烷基）氨磺酰基; 或其药学上可接受的盐; 制造过程; 含有它们的药物组合物; 并将其用作抗肿瘤剂。

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