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1. 发明公开

EP0841924A1 BENZIMIDAZOLE COMPOUNDS 失效
标题翻译：苯并咪唑CONNECTIONS
公开(公告)号：EP0841924A1
公开(公告)日：1998-05-20
申请号：EP96925875.0
申请日：1996-07-30
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： A61K31 , A61P35 , A61P43 , C07D235
CPC分类号： C07D235/06 , A61K31/4184 , A61K31/675 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18
摘要： A range is disclosed of benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

2. 发明公开

EP0749415A1 BENZAMIDE ANALOGS, USEFUL AS PARP (ADP-RIBOSYLTRANSFERASE, ADPRT) DNA REPAIR ENZYME INHIBITORS 失效转让
标题翻译：苯甲酰胺类似物，FOR USE AS PARP（ADP-核糖基转移酶，ADPRT）DNSREPARATURENZYM抑制剂
公开(公告)号：EP0749415A1
公开(公告)日：1996-12-27
申请号：EP95910653.0
申请日：1995-03-09
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： C07D239 , A61K31 , A61K45 , A61N5 , A61P35 , A61P43 , C07C235 , C07C247 , C07C255 , C07D263 , C07D317 , C07D327 , C07D473
CPC分类号： C07D263/56 , C07C235/46 , C07C247/16 , C07C255/54 , C07D239/91 , C07D263/57 , C07D317/68 , C07D473/34 , C07D473/40
摘要： A range of 3-oxybenzamide compounds (I) and related quinazolinone compounds (II) are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula (I) X and Y together may form a bridge -X-Y- that represents the grouping (a), (b) or (c) wherein R5 is H, alkyl, aryl or aralkyl.

3. 发明授权

EP0966476B1 Quinazolinone compounds 失效
标题翻译：喹唑啉酮化合物
公开(公告)号：EP0966476B1
公开(公告)日：2002-09-04
申请号：EP98902115.9
申请日：1998-01-30
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： C07F9/6512 , A61K31/675 , C07D239/91
CPC分类号： C07D239/91 , C07F9/65128
摘要： Phosphate derivatives are disclosed of quinazolinone compounds having structural formula (I) or a pharmaceutically acceptable salt thereof, wherein X' represent hydroxyl, alkyl, alkoxy, or O-Z where Z is a phosphate or phosphate derivative; Y' represents hydrogen, alkyl or an optionally substituted aryl group or optionally substituted aralkyl group; and R' is hydrogen, alkyl, or CH2-O-Z where Z is again a phosphate or phosphate derivative; subject to the proviso that if neither X' nor R' contains Z, Y' is an aryl or aralkyl group having an O-Z substituent therein with Z once again being a phosphate or phosphate derivative as hereinabove defined. These compounds are useful as prodrugs for providing active PARP inhibiting substances for medical use in conjunction with a cytotoxic drug or radiotherapy in order to increase the effectiveness of the latter, especially in connection with antitumor treatment.

4. 发明授权

EP0841924B1 BENZIMIDAZOLE COMPOUNDS 失效
标题翻译：苯并咪唑CONNECTIONS
公开(公告)号：EP0841924B1
公开(公告)日：2002-10-02
申请号：EP96925875.5
申请日：1996-07-30
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： A61K31/415 , A61P35/00 , C07D235/06
CPC分类号： C07D235/06 , A61K31/4184 , A61K31/675 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18
摘要： A range is disclosed of benzimidazole-4-carboxamide compounds (I) which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. In formula (I), R and R' may each be selected independently from hydrogen, alkyl, hydroxyalkyl (e.g. CH2CH2OH), acyl (e.g. acetyl or benzoyl) or an optionally substituted aryl (e.g. phenyl) or aralkyl (e.g. benzyl or carboxybenzyl) group. R is generally a substituted phenyl group in the most preferred compounds. The compounds may also be used in the form of pharmaceutically acceptable salts or pro-drugs.

5. 发明公开

EP0971925A1 PYRIMIDOPYRIMIDINE COMPOUNDS 失效
标题翻译：嘧啶并嘧啶CONNECTIONS
公开(公告)号：EP0971925A1
公开(公告)日：2000-01-19
申请号：EP98913955.5
申请日：1998-04-01
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： A range of dipyridamole analogues useful for inhibiting transport of nucleosides or purines across cell membranes, thereby to potentiate the activity of various cytotoxic antitumour drugs, is diclosed. These analogues comprise compounds having general structural formula (I) or pharmaceutically acceptable salts thereof; wherein R1 is chloro and R3 is diethanolamino, or R1 and R3 are identical and are selected from allyl, halo, diethanolamino, solketalo and a group having the formula: -O-Rz or -NHRz, Rz being selected from alkyl, hydroxyalkyl, alkoxyalkyl, dialkoxyalkyl and 2-oxo-alkyl wherein the or each alkyl and/or alkoxy moiety has less than six carbon atoms, and R2 and R4 are identical and are selected from piperidino, N-tetrahydroisoquinolyl, and a benzylamino group having structural formula (II) wherein R5 is H, or an optionally substituted alkyl or benzyl group, and R6 and R7 represent H or optional substituents in the aromatic nucleus selected from halo, alkyl, alkoxy, hydroxy, trifluoromethyl, azido, cyano, nitro, carboxyl, carboxylic ester, amino or a substituted amino NRxRy where Rx and Ry each represent hydrogen or alkyl, subject to the provisos that (a) if R1 and R3 are both chloro or diethanolamino, R2 and R4 are not both benzylamino, i.e. R2 and R4 do not correspond to structure II with R5, R6 and R7 each being hydrogen, and (b) if R2 and R4 are both piperidino, R1 and R3 are not both chloro, diethanolamino, solketalo or (2,3-dimethoxy)propoxy.

6. 发明公开

EP0966476A1 QUINAZOLINONE COMPOUNDS 失效
标题翻译：喹唑啉酮化合物
公开(公告)号：EP0966476A1
公开(公告)日：1999-12-29
申请号：EP98902115.0
申请日：1998-01-30
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： A61K31 , A61P35 , A61P43 , C07D239 , C07D403 , C07F9
CPC分类号： C07D239/91 , C07F9/65128
摘要： Phosphate derivatives are disclosed of quinazolinone compounds having structural formula (I) or a pharmaceutically acceptable salt thereof, wherein X' represent hydroxyl, alkyl, alkoxy, or O-Z where Z is a phosphate or phosphate derivative; Y' represents hydrogen, alkyl or an optionally substituted aryl group or optionally substituted aralkyl group; and R' is hydrogen, alkyl, or CH2-O-Z where Z is again a phosphate or phosphate derivative; subject to the proviso that if neither X' nor R' contains Z, Y' is an aryl or aralkyl group having an O-Z substituent therein with Z once again being a phosphate or phosphate derivative as hereinabove defined. These compounds are useful as prodrugs for providing active PARP inhibiting substances for medical use in conjunction with a cytotoxic drug or radiotherapy in order to increase the effectiveness of the latter, especially in connection with antitumor treatment.
摘要翻译：公开了具有结构式（I）的喹唑啉酮化合物或其药学上可接受的盐的磷酸酯衍生物，其中X'代表羟基，烷基，烷氧基或O-Z，其中Z是磷酸酯或磷酸酯衍生物; Y'代表氢，烷基或任选取代的芳基或任选取代的芳烷基; 和R'是氢，烷基或CH2-O-Z，其中Z又是磷酸酯或磷酸酯衍生物; 条件是如果X'和R'都不含Z，则Y'是其中具有O-Z取代基的芳基或芳烷基，其中Z再次为如上文所定义的磷酸酯或磷酸酯衍生物。这些化合物作为提供用于医学用途的活性PARP抑制物质的联合细胞毒性药物或放射疗法的前体药物是有用的，以提高后者的效力，特别是与抗肿瘤治疗有关。

7. 发明授权

EP0749415B1 BENZAMIDE ANALOGS, USEFUL AS PARP (ADP-RIBOSYLTRANSFERASE, ADPRT) DNA REPAIR ENZYME INHIBITORS 失效转让
标题翻译： ANALOG苯甲酰胺，用作PARP（ADP-核糖基转移酶，ADPRT）DNA修复酶抑制剂
公开(公告)号：EP0749415B1
公开(公告)日：1999-09-08
申请号：EP95910653.5
申请日：1995-03-09
申请人： NEWCASTLE UNIVERSITY VENTURES LIMITED
发明人： GRIFFIN, Roger, John , CALVERT, Alan, Hilary , CURTIN, Nicola, Jane , NEWELL, David, Richard , GOLDING, Bernard, Thomas
IPC分类号： C07C235/46 , C07D263/54 , C07D239/90 , C07D239/91 , C07D317/46 , C07D327/04 , A61K31/41 , A61K31/47 , A61K31/335 , A61K31/39
CPC分类号： C07D263/56 , C07C235/46 , C07C247/16 , C07C255/54 , C07D239/91 , C07D263/57 , C07D317/68 , C07D473/34 , C07D473/40
摘要： A range of 3-oxybenzamide compounds (I) and related quinazolinone compounds (II) are disclosed which can act as potent inhibitors of the DNA repair enzyme poly(ADP-ribose) polymerase or PARP enzyme (EC 2.4.2.30), and which thereby can provide useful therapeutic compounds for use in conjunction with DNA-damaging cytotoxic drugs or radiotherapy to potentiate the effects of the latter. The compounds disclosed include 3-benzyloxybenzamides, 3-oxybenzamides in which a chain of 5 or more methylene groups terminate in a halogen atom or in a purin-9-yl moiety, certain benzoxazole-4-carboxamide compounds and certain quinazolinone compounds. In formula (I) X and Y together may form a bridge -X-Y- that represents the grouping (a), (b) or (c) wherein R5 is H, alkyl, aryl or aralkyl.

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