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1. 发明授权

US09365508B2 Aroyl thiourea derivatives 有权
标题翻译：芳酰基硫脲衍生物
公开(公告)号：US09365508B2
公开(公告)日：2016-06-14
申请号：US13377145
申请日：2010-06-09
申请人： Sonia Lain , Nicholas James Westwood , David Philip Lane
发明人： Sonia Lain , Nicholas James Westwood , David Philip Lane
IPC分类号： C07C335/26 , C07C327/54
CPC分类号： C07C335/26 , C07C327/54
摘要： The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar′ are as defined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases.
摘要翻译：本发明提供式（I）化合物：其中X，Y，Z 1 R 1，R 2，R 3，Ar和Ar'如本文所定义）及其生理上可接受的盐，溶剂合物，酯或酰胺，包含这些化合物和用于医药的化合物，例如用于治疗或预防涉及细胞增殖的疾病，例如癌症，以及用于治疗或预防其它疾病。

2. 发明申请

US20120149778A1 COMPOUNDS 有权
标题翻译：化合物
公开(公告)号：US20120149778A1
公开(公告)日：2012-06-14
申请号：US13377145
申请日：2010-06-09
申请人： Sonia Lain , Nicholas James Westwood , David Philip Lane
发明人： Sonia Lain , Nicholas James Westwood , David Philip Lane
IPC分类号： A61K31/17 , A61P35/00 , A61P25/28 , A61P25/16 , A61P19/00 , A61P37/00 , A61P7/06 , A61P3/10 , A61P21/00 , A61P29/00 , A61P3/04 , A61P9/04 , A61P31/18 , A61P33/06 , A61P3/00 , C07D295/15 , A61P7/00 , C07C335/26
CPC分类号： C07C335/26 , C07C327/54
摘要： The invention provides compounds according to formula (I): (wherein X, Y, Z1 R1, R2, R3, Ar and Ar′ are as defined herein), and physiologically acceptable salts, solvates, esters or amides thereof, pharmaceutical compositions comprising these compounds and the compounds for use in medicine, for example for the treatment or prophylaxis of diseases involving cell proliferation, such as cancer, and for the treatment or prophylaxis of other diseases.
摘要翻译：本发明提供式（I）化合物：其中X，Y，Z 1 R 1，R 2，R 3，Ar和Ar'如本文所定义）及其生理上可接受的盐，溶剂合物，酯或酰胺，包含这些化合物和用于医药的化合物，例如用于治疗或预防涉及细胞增殖的疾病，例如癌症，以及用于治疗或预防其它疾病。

3. 发明申请

US20080249025A1 Methods and Means For Inhibition of CDK4 Activity 审中-公开
标题翻译：抑制CDK4活性的方法和手段
公开(公告)号：US20080249025A1
公开(公告)日：2008-10-09
申请号：US12133242
申请日：2008-06-04
申请人： Kathryn Lindsay Ball , David PHilip Lane
发明人： Kathryn Lindsay Ball , David PHilip Lane
IPC分类号： A61K38/10 , C12N5/02 , C12N15/01 , A61P43/00 , A61K38/08
CPC分类号： C07K14/4703 , A61K38/00
摘要： p21WAF1 interacts with cyclin D1 and Cdk4. Peptide fragments of p21 inhibit the interaction and/or affect Cdk4 activity. The peptides, derivative peptides and non-peptidyl mimetics thereof are useful in affecting activity of Cdk4, such as RB phosphorylation and cellular proliferation, indicative of therapeutic usefullness in treatment of tumors and other hyperproliferative disorders. Assay and screening methods allow identification of such modulators, especially inhibitors, of Cdk4 activity.
摘要翻译： p21 WAF1与细胞周期蛋白D1和Cdk4相互作用。 p21的肽片段抑制相互作用和/或影响Cdk4活性。肽，衍生肽和非肽基模拟物可用于影响Cdk4的活性，例如RB磷酸化和细胞增殖，指示治疗肿瘤和其他过度增生性疾病的治疗有用性。测定和筛选方法允许鉴定Cdk4活性的这种调节剂，特别是抑制剂。

4. 发明授权

US07141541B1 Use of peptides 失效
标题翻译：使用肽
公开(公告)号：US07141541B1
公开(公告)日：2006-11-28
申请号：US10019198
申请日：2000-06-21
申请人： Christopher Gregory Proud , Terrence Patrick Herbert , David Philip Lane , Robin Fahraeus
发明人： Christopher Gregory Proud , Terrence Patrick Herbert , David Philip Lane , Robin Fahraeus
IPC分类号： A61K38/00 , A61K49/00
CPC分类号： C07K14/4705 , A61K38/00 , C07K14/4747
摘要： We claim a therapeutic method of inducing programmed cell death comprising administering to a recipient a peptide of 10–25 amino acids, comprising the sequence: (KR)xxYxxx(F/Q)L(L/M) wherein x is any amino acid.
摘要翻译：我们要求诱导程序性细胞死亡的治疗方法，包括向受体施用10-25个氨基酸的肽，其包含序列：（KR）xxYxxx（F / Q）L（L / M），其中x是任何氨基酸。

5. 发明授权

US6020149A Methods of screening for anti-microbial agents and for inhibiting microbial growth 失效
标题翻译：筛选抗微生物剂和抑制微生物生长的方法
公开(公告)号：US6020149A
公开(公告)日：2000-02-01
申请号：US929738
申请日：1997-09-15
申请人： Frances Victoria Fuller-Pace , David Philip Lane
发明人： Frances Victoria Fuller-Pace , David Philip Lane
IPC分类号： C12N15/09 , A61K39/395 , A61P31/04 , C12N5/10 , C12N9/16 , C12N9/22 , C12N15/55 , C12Q1/18 , C12Q1/42
CPC分类号： A61K31/70 , C12N9/22 , C12Q1/18 , C12Q1/42
摘要： A method for determining the anti-microbial activity of a putative anti-microbial agent includes combining a microbially required nucleotide phosphatase, a nucleoside phosphate and the substance to be tested, and assessing the extent of degradation of the nucleoside phosphate in the presence and absence of the substance. The method thus allows the determination of the extent of inhibition of the nucleotide phosphatase by the substance. Preferably the method determines the degree of inhibition of an RNA helicase such as DbpA, which acts selectively on prokaryotic ribosomal RNA. Suitable DbpA inhibitors as well as genetic material encoding for an active form of DbpA are used.
摘要翻译：用于测定推定的抗微生物剂的抗微生物活性的方法包括将微生物需要的核苷酸磷酸酶，磷酸核苷和待测物质组合，并且在存在和不存在下测定磷酸核苷的降解程度物质。因此，该方法允许确定该物质对核苷酸磷酸酶的抑制程度。优选地，该方法确定RNA解旋酶如DbpA的抑制程度，DbpA选择性地作用于原核核糖体RNA。使用合适的DbpA抑制剂以及编码活性形式的DbpA的遗传物质。

6. 发明授权

US07083983B2 Inhibitors of the interaction between P53 and MDM2 失效
标题翻译：抑制P53和MDM2之间的相互作用
公开(公告)号：US07083983B2
公开(公告)日：2006-08-01
申请号：US09214371
申请日：1997-07-04
申请人： David Philip Lane , Volker Böttger , Angelika Böttger , Steven Michael Picksley , Heinz-Kurt Hochkeppel , Carlos Garcia-Echeverria , Patrick Chène , Pascal Furet
发明人： David Philip Lane , Volker Böttger , Angelika Böttger , Steven Michael Picksley , Heinz-Kurt Hochkeppel , Carlos Garcia-Echeverria , Patrick Chène , Pascal Furet
IPC分类号： G01N33/566 , G01N33/53 , A61K38/00 , A61K38/12 , A61K51/00
CPC分类号： C07K7/04 , A61K38/00 , C07K2319/00
摘要： The present invention relates to compounds capable of binding to the oncogene protein MDM2, processes for the preparation of such compounds, pharmaceutical preparations comprising such compounds, and uses of said compounds, e.g. in the therapeutic (including prophylactic) treatment of an animal or especially of the human body. The present further relates to methods of and compounds for inhibiting the growth of tumor cells which comprise the wild type p53 suppressor by interfering with the interaction between human p53 and human MDM2.
摘要翻译：本发明涉及能够结合致癌基因蛋白MDM2的化合物，制备这些化合物的方法，包含这些化合物的药物制剂，以及所述化合物的用途，例如，在动物或特别是人体的治疗（包括预防性）治疗中。本发明还涉及通过干扰人p53与人MDM2之间的相互作用来抑制包含野生型p53抑制因子的肿瘤细胞生长的方法和化合物。

7. 发明授权

US06242201B1 Identification of the P21WaF1-PCNA interaction site and therapeutic applications thereof 失效
标题翻译：鉴定P21WaF1-PCNA相互作用位点及其治疗应用
公开(公告)号：US06242201B1
公开(公告)日：2001-06-05
申请号：US08817895
申请日：1997-08-22
申请人： David Philip Lane , Lynne Suzanne Cox , Emma Warbrick , David Moore Glover
发明人： David Philip Lane , Lynne Suzanne Cox , Emma Warbrick , David Moore Glover
IPC分类号： G01N33574
CPC分类号： C12N15/1055 , A61K38/00 , C07K14/4703 , C12N15/81 , C12Q1/6897
摘要： Substances are disclosed which have the property of binding to PCNA, the substances comprising (i) a fragment of the p21WAF1 protein including residues 141 to 160 of the p21WAF1 amino acid sequence, or an active portion or derivative thereof; or (ii) functional mimetics of these protein fragments. In particular, the PCNA binding activity is shown to lie within the sequence motif OTSMTDFY, with the residues shown in bold being critical for PCNA binding, with those underlined being important. These substances are useful in the treatments of disorders in which PCNA is implicated, e.g. hyperproliferative disorders such as cancer and psoriasis, the substances binding to PCNA to inactivate it or functionally deplete its level. Also disclosed is the use of a yeast two hybrid screening technique for screening candidate peptides for binding to PCNA.
摘要翻译：公开了具有与PCNA结合的性质的物质，所述物质包括（i）p21WAF1蛋白的片段，包括p21WAF1氨基酸序列的残基141至160，或其活性部分或衍生物; 或（ii）这些蛋白质片段的功能模拟物。特别地，PCNA结合活性显示位于序列基序OTSMTDFY内，粗体显示为PCNA结合关键，其中下划线是重要的。这些物质可用于治疗涉及PCNA的疾病，例如，过度增生性疾病如癌症和牛皮癣，结合PCNA的物质使其失活或功能丧失其水平。还公开了使用酵母双杂交筛选技术筛选候选肽结合PCNA。

8. 发明授权

US5702908A Interruption of binding of MDM2 and p53 protein and therapeutic application thereof 失效
标题翻译： MDM2和p53蛋白结合的中断及其治疗应用
公开(公告)号：US5702908A
公开(公告)日：1997-12-30
申请号：US277660
申请日：1994-07-20
申请人： Steven Michael Picksley , David Philip Lane
发明人： Steven Michael Picksley , David Philip Lane
IPC分类号： A61K38/00 , A61K48/00 , C07K14/47 , C07K14/82 , G01N33/53
CPC分类号： C07K14/82 , C07K14/4746 , A61K38/00 , A61K48/00
摘要： A method of identifying a compound which interferes with the binding of MDM2 to human p53 has been determined. This method comprises forming a mixture between MDM2 and a fragment of human p53 consisting of 6 to 28 amino acids comprising TFSDLW (SEQ ID NO:2), adding a test compound to the mixture and determining the quantity of protein bound to the other before and after adding the compound. A compound which decreases the amount of binding of the two proteins to each other is a compound which interferes with the binding of MDM2 to human p53.
摘要翻译：确定了干扰MDM2与人p53结合的化合物的方法。该方法包括在MDM2与由包含TFSDLW（SEQ ID NO：2）的6至28个氨基酸组成的人p53片段之间形成混合物，向混合物中加入测试化合物，并测定与之前和加入化合物。减少两种蛋白质彼此结合量的化合物是干扰MDM2与人p53结合的化合物。

9. 发明授权

US06962792B1 Methods and means for inhibition of Cdk4 activity 失效
标题翻译：抑制Cdk4活性的方法和手段
公开(公告)号：US06962792B1
公开(公告)日：2005-11-08
申请号：US09180269
申请日：1997-05-08
申请人： Kathryn Lindsay Ball , David Philip Lane
发明人： Kathryn Lindsay Ball , David Philip Lane
IPC分类号： G01N33/50 , A61K31/7088 , A61K38/00 , A61K45/00 , A61K48/00 , A61P35/00 , A61P43/00 , C07K7/08 , C07K14/47 , G01N33/15 , G01N33/566 , G01N33/53 , G01N33/569
CPC分类号： C07K14/4703 , A61K38/00
摘要： p21WAF1 interacts with cyclin D1 and Cdk4. Peptide fragments of p21 inhibit the interaction and/or affect Cdk4 activity. The peptides, derivative peptides and non-peptidyl mimetics thereof are useful in affecting activity of Cdk4, such as RB phosphorylation, and cellular proliferation, indicative of therapeutic usefulness in treatment of tumours and other hyperproliferative disorders. Assay and screening methods allow identification of such modulators, especially inhibitors, of Cdk4 activity.
摘要翻译： p21 WAF1与细胞周期蛋白D1和Cdk4相互作用。 p21的肽片段抑制相互作用和/或影响Cdk4活性。肽，衍生肽和非肽基模拟物可用于影响Cdk4的活性，例如RB磷酸化和细胞增殖，指示治疗肿瘤和其他过度增生性疾病的治疗有用性。测定和筛选方法允许鉴定Cdk4活性的这种调节剂，特别是抑制剂。

10. 发明授权

US06569833B1 Cyclin dependent kinase binding peptides 失效
标题翻译：细胞周期蛋白依赖性激酶结合肽
公开(公告)号：US06569833B1
公开(公告)日：2003-05-27
申请号：US09043560
申请日：1999-04-07
申请人： Robin Fahraeus , David Philip Lane
发明人： Robin Fahraeus , David Philip Lane
IPC分类号： A61K3800
CPC分类号： C07K14/4703 , A61K38/00 , C07K14/4738 , C07K2319/02
摘要： The present disclosure identifies substances having the property of binding to cyclin dependent kinase (cdk) comprising: (i) a peptide including amino acid residue 84 to 103 of full length p16 protein, or an active portion or derivative thereof; or (ii) a functional mimetic of the fragment, active portion or derivative; the substance excludes full length p16, p15, p18 and p19 proteins. These substances are useful in tumor suppression by inhibiting the phosphorylation of Rb protein. Also described herein is the resolution of the amino acid motifs responsible for binding cdks, an FLD motif, corresponding to amino acid residues 90 to 92 of full length p16 protein, and an LVVL motif, corresponding to amino acid residues 94 to 97 of full length p16 protein. The substances disclosed herein can be used in the treatment of hyperproliferative disorders and to screen and design molecules having the similar properties.
摘要翻译：本公开内容鉴定具有结合细胞周期蛋白依赖性激酶（cdk）的性质的物质，其包含：（i）包含全长p16蛋白的氨基酸残基84至103的肽或其活性部分或衍生物; 或（ii）片段，活性部分或衍生物的功能模拟物; 该物质不包括全长p16，p15，p18和p19蛋白。这些物质通过抑制Rb蛋白的磷酸化可用于肿瘤抑制。本文还描述了负责结合cdks的氨基酸基序的分辨率，对应于全长p16蛋白的90至92的氨基酸残基的FLD基序和对应于全长的氨基酸残基94至97的LVVL基序 p16蛋白。本文公开的物质可用于治疗过度增殖性疾病并筛选和设计具有相似性质的分子。

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