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1. 发明授权

US06310082B1 Benzimidazole compounds 失效
标题翻译：苯并咪唑化合物
公开(公告)号：US06310082B1
公开(公告)日：2001-10-30
申请号：US09594776
申请日：2000-06-16
申请人： Roger J Griffin , Alan H Calvert , Nicola J Curtin , David R Newell , Bernard T Golding
发明人： Roger J Griffin , Alan H Calvert , Nicola J Curtin , David R Newell , Bernard T Golding
IPC分类号： A61K314184
CPC分类号： C07D235/06 , A61K31/4184 , A61K31/675 , C07D235/08 , C07D235/10 , C07D235/12 , C07D235/14 , C07D235/16 , C07D235/18
摘要： 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.
摘要翻译：苯并咪唑-4-甲酰胺化合物（I），其可以作为DNA修复酶聚（ADP-核糖）聚合酶或PARP酶（EC 2.4.2.30）的有效抑制剂，由此可以提供有用的治疗化合物，与 DNA损伤性细胞毒性药物或放射治疗以增强后者的作用。在式（I）中，R和R'可各自独立地选自氢，烷基，羟基烷基（例如CH 2 CH 2 OH），酰基（例如乙酰基或苯甲酰基）或任选取代的芳基（例如苯基）或芳烷基（例如苄基或羧基苄基）组。 R通常是最优选的化合物中的取代的苯基。化合物也可以以药学上可接受的盐或前药的形式使用。

2. 发明授权

US06677345B1 Cyclin dependent kinase inhibitors 失效
标题翻译：细胞周期蛋白依赖性激酶抑制剂
公开(公告)号：US06677345B1
公开(公告)日：2004-01-13
申请号：US09671676
申请日：2000-09-28
申请人： Roger J Griffin , Alan H Calvert , Nicola J Curtin , David R Newell , Bernard T Golding , Jane A Endicott , Martin E M Noble , Francis T Boyle , Philip J Jewsbury
发明人： Roger J Griffin , Alan H Calvert , Nicola J Curtin , David R Newell , Bernard T Golding , Jane A Endicott , Martin E M Noble , Francis T Boyle , Philip J Jewsbury
IPC分类号： A61K31505
CPC分类号： C07D239/48 , A61K31/505 , C07D239/02 , C07D239/50 , C07H19/167
摘要： A range is disclosed of pyrimidine derivatives (I) which can act as inhibitors of cyclin dependent kinases (CDK's) and which thereby can provide useful therapeutic compounds for use in treatment of tumours or other cell proliferation disorders. The compounds of this invention bind to CDK molecules in a manner that appears to differ from that of known CDK inhibitors such as olomoucine and roscovitine. In formula (I), X is O, S or CHRx where Rx is H or C1-4 alkyl; D is H or NZ1Z2 where Z1 and Z2 are each independently H, C1-4 alkyl, C1-4 hydroxyalkyl, optionally substituted aryl or optionally substituted aralkyl; A is selected from H, C1-4 alkyl, C1-4 alkoxy, hydroxy, CH2(CH2)nOH (n=1-4), and NRa1Ra2 where Ra1 and Ra2 are each independently H or C1-4 alkyl; Y is or includes an optionally substituted 4- to 8-membered carbocyclic or heterocyclic ring; D′ is H or NZ3Z4 where Z3 and Z4 are each independently H, C1-4 alkyl, C1-4 hydroxyalkyl, optionally substituted aryl or optionally-substituted aralkyl; E is selected from NO, NO2, N═N—Ar where Ar is an optionally substituted aryl or optionally substituted aralkyl, NRe1Re2 or Nre1Nre2Re3 (Re1, Re2 and Re3 each being independently H, C1-4 alkyl, C1-4 hydroxyalkyl, an optionally substituted aryl or an optionally substituted aralkyl), C(Re)═U (Re being hydrogen, C1-4 alkyl or substituted alkyl, e.g. hydroxyalkyl, or an unsubstituted or substituted aryl or aralkyl, e.g. benzyl, and U being selected from O, Nre′, NORe′ and N—NRe′Re″ where Re′ and Re″ are each independently H, C1-4 alkyl or CONH2), T, CH2T, CHT2 and CT3, where T is a halide I, Br, Cl or F.
摘要翻译：公开了可以作为细胞周期蛋白依赖性激酶（CDK's）抑制剂的嘧啶衍生物（I）的范围，由此可以提供用于治疗肿瘤或其它细胞增殖病症的有用的治疗化合物。本发明的化合物以与已知的CDK抑制剂如奥洛莫斯和罗斯考维胺似乎不同的方式结合CDK分子。在式（I）中，X是O，S或CHR x，其中R x是H或C 1-4烷基; D是H或NZ 1 Z 2，其中Z 1和Z 2各自独立地为H，C 1-4烷基，C 1-4羟基烷基，任选取代的芳基或任选取代的芳烷基; A选自H，C 1-4烷基，C 1-4烷氧基，羟基，CH 2（CH 2）n OH（n = 1-4）和NR a R a 2，其中R 1a和R 2a各自独立地为H或C 1-4烷基; Y是或包括任选取代的4-至8-元碳环或杂环; D'是H或NZ 3 Z 4，其中Z 3和Z 4各自独立地为H，C 1-4烷基，C 1-4羟基烷基，任选取代的芳基或任选取代的芳烷基; E选自NO，NO2，N = N-Ar，其中Ar是任选取代的芳基或任选取代的芳烷基，NRe1Re2或Nre1Nre2Re3（Re1，Re2和Re3各自独立地为H，C1-4烷基，C1-4羟基烷基，任选取代的芳基或任选取代的芳烷基），C（Re）= U（Re为氢，C 1-4烷基或取代烷基，例如羟烷基，或未取代或取代的芳基或芳烷基，例如苄基，U选自O ，Nre'，NORe'和N-NRe'Re“，其中Re'和Re'各自独立地为H，C 1-4烷基或CONH 2），T，CH 2 T，CHT 2和CT 3，其中T为卤化物I，Br ，Cl或F.

3. 发明授权

US06303618B1 Cyclin dependent kinase inhibiting purine derivatives 失效
标题翻译：细胞周期蛋白依赖激酶抑制嘌呤衍生物
公开(公告)号：US06303618B1
公开(公告)日：2001-10-16
申请号：US09481708
申请日：2000-01-12
申请人： Roger J Griffin , Alan H Calvert , Nicola J Curtin , David R Newell , Bernard T Golding , Jane A Endicott , Martin E M Noble , Francis T Boyle , Philip J Jewsbury
发明人： Roger J Griffin , Alan H Calvert , Nicola J Curtin , David R Newell , Bernard T Golding , Jane A Endicott , Martin E M Noble , Francis T Boyle , Philip J Jewsbury
IPC分类号： A61K3152
CPC分类号： C07H15/26 , C07D473/18 , C07D473/30 , C07D473/40
摘要： Method of treating a tumour or other cell proliferation disorder which comprises administering an effective amount of a purine compound which inhibits cyclic dependent kinase activity. Novel purine compounds and pharmaceutical compositions are also disclosed.
摘要翻译：治疗肿瘤或其他细胞增殖病症的方法，其包括施用有效量的抑制环状依赖性激酶活性的嘌呤化合物。还公开了新的嘌呤化合物和药物组合物。

4. 发明授权

US06297250B1 Pyrimidopyrimidine compounds 失效
标题翻译：嘧啶并嘧啶化合物
公开(公告)号：US06297250B1
公开(公告)日：2001-10-02
申请号：US09410742
申请日：1999-10-01
申请人： Roger J Griffin , Nicola J Curtin , Bernard T Golding , Alan H. Calvert , David R. Newell
发明人： Roger J Griffin , Nicola J Curtin , Bernard T Golding , Alan H. Calvert , David R. Newell
IPC分类号： A61K31519
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 antitumor drugs, is disclosed. 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
摘要翻译：公开了一系列可用于抑制核苷或嘌呤跨细胞膜转运的双嘧达莫类似物，从而增强各种细胞毒性抗肿瘤药物的活性。这些类似物包括具有通式结构式（I）的化合物或其药学上可接受的盐; 其中R 1是氯并且R 3是二乙醇氨基，或者R 1和R 3是相同的并且选自烯丙基，卤素，二乙醇氨基，溶剂酮和具有下式的基团：-O-Rz或-NHRz，Rz选自烷基，羟基烷基，烷氧基烷基，二烷氧基烷基和2-氧代 - 烷基，其中烷基和/或烷氧基部分具有少于6个碳原子，并且R 2和R 4相同，并且选自具有结构式（II）的哌啶子基，N-四氢异喹啉基和苄基氨基）其中R 5是H或任选取代的烷基或苄基，R 6和R 7在选自卤素，烷基，烷氧基，羟基，三氟甲基，叠氮基，氰基，硝基，羧基，羧酸酯的芳香核中代表H或任选的取代基，氨基或取代氨基NRxRy，其中Rx和Ry各自表示氢或烷基，条件是（a）如果R1和R3都是氯或二乙醇氨基，则R2和R4不都是苄氨基，即R2和R4不对应结构II与 R5，R6和R7各自为氢，和（b）如果R2和R4都是哌啶子基，则R1和R3不同时为氯，二乙醇氨基，溶剂酮或（2,3-二甲氧基）丙氧基

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