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1. 发明专利

JP2008094847A Inhibitor of histone deacetylase 有权
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：JP2008094847A
公开(公告)日：2008-04-24
申请号：JP2007281356
申请日：2007-10-30
申请人： Methylgene Inc , メシルジーン、インコーポレイテッド
发明人： MORADEI OSCAR , PAQUIN ISABELLE , LEIT SILVANA , FRECHETTE SYLVIE , VAISBURG ARKADII , BESTERMAN JEFFREY M , TESSIER PIERRE , MALLAIS TAMMY C
IPC分类号： C07D207/335 , A61K31/167 , A61K31/341 , A61K31/357 , A61K31/381 , A61K31/402 , A61K31/404 , A61K31/41 , A61K31/4155 , A61K31/4184 , A61K31/4192 , A61K31/42 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4406 , A61K31/4535 , A61K31/496 , A61K31/498 , A61K31/505 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K31/695 , A61K31/7088 , A61K48/00 , A61P31/10 , A61P33/00 , A61P35/00 , A61P43/00 , C07C233/25 , C07C233/80 , C07C235/50 , C07C235/52 , C07C235/58 , C07C237/20 , C07C237/32 , C07C237/34 , C07C237/40 , C07C255/60 , C07C323/42 , C07D207/32 , C07D207/325 , C07D207/327 , C07D209/08 , C07D213/40 , C07D213/73 , C07D233/54 , C07D233/84 , C07D249/06 , C07D257/04 , C07D263/56 , C07D263/57 , C07D277/20 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D277/64 , C07D307/52 , C07D307/54 , C07D307/84 , C07D319/18 , C07D333/16 , C07D333/18 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/34 , C07D333/36 , C07D333/58 , C07D333/60 , C07D333/70 , C07D409/04 , C07D409/12 , C07D409/14 , C07D413/04 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07F5/05 , C07F7/18
CPC分类号： C07F7/1856 , C07C233/25 , C07C235/58 , C07C237/20 , C07C237/40 , C07C255/60 , C07C323/42 , C07D207/325 , C07D207/327 , C07D207/335 , C07D209/08 , C07D213/73 , C07D233/54 , C07D233/84 , C07D249/06 , C07D257/04 , C07D263/57 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D307/52 , C07D307/54 , C07D307/84 , C07D319/18 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/34 , C07D333/36 , C07D333/58 , C07D333/60 , C07D333/70 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a novel histone deacetylase-inhibiting compound effective for treating cell proliferative diseases and conditions. SOLUTION: Specific benzamide compounds, concretely, N-[2-amino-5-(2-thienyl)phenyl]-4-�[(5-chloro-6-fluoro-1H-benzimidazol-2-yl)amino]methyl}benzamide, N-[2-amino-5-(2-thienyl)phenyl]-5-�[(3, 4, 5-trimethoxyphenyl)amino]methyl}-1-benzofuran-2-carboxamide and the like are cited. COPYRIGHT: (C)2008,JPO&INPIT
摘要翻译：待解决的问题：提供一种有效治疗细胞增殖性疾病和病症的新型组蛋白脱乙酰酶抑制化合物。具体地，N- [2-氨基-5-（2-噻吩基）苯基] -4-[（5-氯-6-氟-1H-苯并咪唑-2-基）氨基]苯甲酰胺化合物 ]甲基}苯甲酰胺，N- [2-氨基-5-（2-噻吩基）苯基] -5-a [（3,4,5-三甲氧基苯基）氨基]甲基} -1-苯并呋喃-2-甲酰胺等被引用。版权所有（C）2008，JPO＆INPIT

2. 发明申请

WO0071703A3 INHIBITION OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制作用
公开(公告)号：WO0071703A3
公开(公告)日：2001-07-19
申请号：PCT/IB0001252
申请日：2000-05-03
申请人： METHYLGENE INC
发明人： MACLEOD ALAN R , LI ZUOMEI , BESTERMAN JEFFREY M
IPC分类号： G01N33/50 , A61K31/7088 , A61K38/00 , A61K45/00 , A61K48/00 , A61P35/00 , C12N9/80 , C12N15/09 , C12N15/113 , C12Q1/02 , C12Q1/34 , G01N33/15 , C12N15/11 , A61K31/7125 , C07H21/00 , C12Q1/44 , C12Q1/68
CPC分类号： C12N15/1137 , A61K38/00 , C12N2310/315 , C12N2310/321 , C12N2310/345 , C12N2310/346 , C12N2310/3521
摘要： The invention relates to the inhibition of histone deacetylase expression and enzymatic activity and, in particular, to the inhibition of a specific histone deacetylase. The invention also relates to compositions comprising antisense oligonucleotides and methods of using the same to inhibit a histone deacetylase. Also disclosed are methods for identifying a histone deacetylase involved in induction of cell proliferation, and methods for identifying compounds that interact with and reduce the enzymatic activity of such a histone deacetylase.
摘要翻译：本发明涉及组蛋白脱乙酰酶表达和酶活性的抑制，特别是抑制特定的组蛋白脱乙酰酶。本发明还涉及包含反义寡核苷酸的组合物及其用于抑制组蛋白脱乙酰酶的方法。还公开了用于鉴定参与细胞增殖诱导的组蛋白脱乙酰酶的方法，以及用于鉴定与这种组蛋白脱乙酰酶的酶活性相互作用并降低其活性的化合物的方法。

3. 发明申请

WO2004048393A2 NOVEL INHIBITORS OF beta-LACTAMASE 审中-公开
标题翻译：新的β-内酰胺酶抑制剂
公开(公告)号：WO2004048393A2
公开(公告)日：2004-06-10
申请号：PCT/US0336929
申请日：2003-11-19
申请人： METHYLGENE INC , BESTERMAN JEFFREY M , RAHIL JUBRAIL , VAISBURG ARKADII
发明人： BESTERMAN JEFFREY M , RAHIL JUBRAIL , VAISBURG ARKADII
IPC分类号： C07F9/24 , C07F9/38 , C07F9/40 , C07F9/42 , C07F9/44 , C07F9/572 , C07F9/58 , C07F9/60 , C07F9/6506 , C07F9/6524 , C07F9/653 , C07F9/6539 , C07F9/6541 , C07F9/655 , C07F9/6553 , C07F9/6558 , C07F9/00
CPC分类号： C07F9/65586 , C07F9/2491 , C07F9/3808 , C07F9/4006 , C07F9/4084 , C07F9/425 , C07F9/4407 , C07F9/5721 , C07F9/5728 , C07F9/585 , C07F9/588 , C07F9/60 , C07F9/65061 , C07F9/6524 , C07F9/65312 , C07F9/6539 , C07F9/65395 , C07F9/6541 , C07F9/65515 , C07F9/65517 , C07F9/655345 , C07F9/655354 , C07F9/65583
摘要： The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel beta-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic beta-lactamase inhibitors presently available, and which do not require beta-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
摘要翻译：本发明涉及细菌抗生素抗性，并且特别涉及用于克服细菌抗生素抗性的组合物和方法。本发明提供了新型β-内酰胺酶抑制剂，其在结构上与天然产物和目前可得的半合成β-内酰胺酶抑制剂无关，并且不需要β-内酰胺药效团。本发明还提供了用于抑制细菌生长的药物组合物和方法。

4. 发明申请

WO02069947A3 ANTISENSE OLIGONUCLEOTIDES AND TRICHOSTATIN ANALOGUE HISTONE DEACETYLASE-4 INHIBITORS AGAINST CANCER 审中-公开
标题翻译：反义寡核苷酸和三氯杀虫蛋白类似物HISTONE DEACETYLASE-4抑制剂
公开(公告)号：WO02069947A3
公开(公告)日：2003-10-09
申请号：PCT/IB0202002
申请日：2002-01-14
申请人： METHYLGENE INC
发明人： BESTERMAN JEFFREY M , BONFILS CLAIRE , WOO SOON HYUNG , VAISBURG ARKADII , DELORME DANIEL , FOURNEL MARIELLE , LAVOIE RICO , LI ZUOMEI
IPC分类号： C07D213/56 , A61K31/167 , A61K31/18 , A61K31/4035 , A61K31/44 , A61K31/4418 , A61K31/7088 , A61K31/711 , A61K38/00 , A61K45/06 , A61K48/00 , A61P35/00 , A61P43/00 , C07D209/48 , C07K14/47 , C12N5/02 , C12N9/16 , C12N15/113 , C12N15/12 , C12N15/62 , A61K31/165 , C07C225/22 , C07C225/24 , C07C235/38 , C07C235/78 , C07C237/10 , C07C237/20 , C07C251/48 , C07C259/06 , C07C271/22 , C07C271/28 , C07C275/34 , C07C275/40 , C07D295/14 , C07D295/20 , C12N15/11
CPC分类号： C12N15/1137 , A61K31/167 , A61K31/18 , A61K31/4035 , A61K31/4418 , A61K31/711 , A61K38/00 , A61K45/06 , C07K14/4702 , C07K2319/23 , C12N9/16 , C12N15/62 , C12N2310/315 , C12N2310/321 , C12N2310/341 , C12N2310/346 , C12Y305/01098 , C12N2310/3521
摘要： This invention relates to the inhibition of histone deacetylase (HDAC) expression and enzymatic activity. The invention provides methods and reagents for inhibiting HDAC-4 and HDAC-1 by inhibiting expression at the nucleic acid level or inhibiting enzymatic activity at the protein level. Specific inhibitors are antisense oligonucleotides against HDAC-4 and HDAC-1 and trichostatin analoques .
摘要翻译：本发明涉及组蛋白脱乙酰酶（HDAC）表达和酶活性的抑制。本发明提供了抑制HDAC-4和HDAC-1通过抑制核酸水平的表达或抑制蛋白质水平的酶活性的方法和试剂。特异性抑制剂是针对HDAC-4和HDAC-1和曲古菌素镇痛剂的反义寡核苷酸。

5. 发明公开

EP2605770A4 ANTIFUNGAL AGENTS AND USES THEREOF 审中-公开
标题翻译： THEREOF抗真菌药物应用
公开(公告)号：EP2605770A4
公开(公告)日：2014-12-10
申请号：EP11817615
申请日：2011-08-19
申请人： METHYLGENE INC
发明人： BESTERMAN JEFFREY M
IPC分类号： A61K31/165 , A61K31/137 , A61K31/351 , A61K31/404 , A61K31/4196 , A61K31/496 , A61K45/06 , A61P31/10 , C07D209/14 , C07D309/10
CPC分类号： A61K31/165 , A61K31/137 , A61K31/351 , A61K31/404 , A61K31/4196 , A61K31/496 , A61K45/06 , C07D209/04 , C07D309/10 , A61K2300/00

6. 发明公开

EP1922414A4 HISTONE DEACETYLASE WHOLE CELL ENZYME ASSAY 审中-公开
标题翻译： HISTON-DEACETYLASE-ENZYMTEST MIT INTAKTEN ZELLEN
公开(公告)号：EP1922414A4
公开(公告)日：2008-11-05
申请号：EP05858685
申请日：2005-09-21
申请人： METHYLGENE INC
发明人： ZUOMEI LI , BESTERMAN JEFFREY M , BONFILS CLAIRE
IPC分类号： C12Q1/34
CPC分类号： C12Q1/44 , C12Q1/34 , G01N2500/02
摘要： The invention relates to enzymatic assays for assessing protein deacetylase activity of a protein deacetylase family, such as the histone deacetylase (HDAC) family or a sirtuin family. More particularly, the invention relates to such assays utilizing primary intact whole cells taken directly from the body of a mammal. Total protein deacetylase activity or isotype-specific activity is measured using assays which include a cell-permeable substrate that allows the production of a detectable reporter molecule in response to deacetylase activity. The effect of inhibitors and activators of the protein deacetylase family on protein deacetylase activity can also be measured.
摘要翻译：本发明涉及用于评估蛋白脱乙酰酶家族（例如组蛋白脱乙酰酶（HDAC）家族或沉默调节蛋白家族）的蛋白脱乙酰酶活性的酶测定法。更具体地说，本发明涉及利用直接从哺乳动物体内取得的原代完整全细胞的此类测定。使用测定法测定总蛋白脱乙酰酶活性或同种型特异性活性，所述测定法包括允许响应脱乙酰酶活性产生可检测报道分子的细胞可渗透底物。也可以测量蛋白质脱乙酰酶家族的抑制剂和活化剂对蛋白质脱乙酰酶活性的影响。

7. 发明申请

WO2006078752A3 INHIBITORS OF DNA METHYLTRANSFERASE 审中-公开
标题翻译： DNA甲基转移酶抑制剂
公开(公告)号：WO2006078752A3
公开(公告)日：2007-02-15
申请号：PCT/US2006001791
申请日：2006-01-18
申请人： METHYLGENE INC , WAHHAB AMAL , BESTERMAN JEFFREY M , DELORME DANIEL , ISAKOVIC LJUBOMIR , LLEWELLYN DAVID , RAHIL JUBRAIL , SAAVEDRA OSCAR , DEZIEL ROBERT
发明人： WAHHAB AMAL , BESTERMAN JEFFREY M , DELORME DANIEL , ISAKOVIC LJUBOMIR , LLEWELLYN DAVID , RAHIL JUBRAIL , SAAVEDRA OSCAR , DEZIEL ROBERT
IPC分类号： C07H19/16 , A61K31/7076 , A61P35/02
CPC分类号： C07H19/16
摘要： The invention relates to the inhibition of DNA methyltransferase isoforms DNMT1 and DNMT3b2. The invention provides compounds and methods for inhibiting DNMT1 and DNMT3b2.
摘要翻译：本发明涉及DNA甲基转移酶同工型DNMT1和DNMT3b2的抑制。本发明提供了抑制DNMT1和DNMT3b2的化合物和方法。

8. 发明申请

WO2005030705A9 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2005030705A9
公开(公告)日：2006-04-20
申请号：PCT/US2004031591
申请日：2004-09-24
申请人： METHYLGENE INC , MORADEI OSCAR , PAQUIN ISABELLE , LEIT SILVANA , FRECHETTE SYLVIE , VAISBURG ARKADII , BESTERMAN JEFFREY M , TESSIER PIERRE , MALLAIS TAMMY C
发明人： MORADEI OSCAR , PAQUIN ISABELLE , LEIT SILVANA , FRECHETTE SYLVIE , VAISBURG ARKADII , BESTERMAN JEFFREY M , TESSIER PIERRE , MALLAIS TAMMY C
IPC分类号： A61P35/00 , C07C233/25 , C07C235/58 , C07C237/20 , C07C237/40 , C07C255/60 , C07C323/42 , C07D207/32 , C07D207/325 , C07D207/327 , C07D207/335 , C07D209/08 , C07D213/73 , C07D233/54 , C07D233/84 , C07D249/06 , C07D257/04 , C07D263/56 , C07D263/57 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D307/52 , C07D307/54 , C07D307/84 , C07D319/18 , C07D333/16 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/34 , C07D333/36 , C07D333/58 , C07D333/60 , C07D333/70 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04 , C07D487/04 , C07F7/18 , A61K31/16 , A61K31/33 , A61K31/381
CPC分类号： C07F7/1856 , C07C233/25 , C07C235/58 , C07C237/20 , C07C237/40 , C07C255/60 , C07C323/42 , C07D207/325 , C07D207/327 , C07D207/335 , C07D209/08 , C07D213/73 , C07D233/54 , C07D233/84 , C07D249/06 , C07D257/04 , C07D263/57 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/40 , C07D307/52 , C07D307/54 , C07D307/84 , C07D319/18 , C07D333/20 , C07D333/22 , C07D333/24 , C07D333/34 , C07D333/36 , C07D333/58 , C07D333/60 , C07D333/70 , C07D409/04 , C07D409/12 , C07D409/14 , C07D417/12 , C07D471/04
摘要： The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶。本发明提供了抑制组蛋白脱乙酰酶酶活性的化合物和方法。本发明还提供了治疗细胞增殖性疾病和病症的组合物和方法。

9. 发明申请

WO2004005513A3 METHODS FOR SPECIFICALLY INHIBITING HISTONE DEACETYLASE-7 AND 8 审中-公开
标题翻译：特异性抑制组蛋白脱乙酰酶-7和8的方法
公开(公告)号：WO2004005513A3
公开(公告)日：2004-07-01
申请号：PCT/IB0303052
申请日：2003-06-12
申请人： METHYLGENE INC
发明人： BESTERMAN JEFFREY M , LI ZUOMEI , DELORME DANIEL , BONFILS CLAIRE
IPC分类号： A61K31/167 , A61K31/4015 , A61K31/505 , A61K31/5377 , A61K31/7088 , A61K38/00 , C07C237/20 , C07C237/40 , C07C323/44 , C07D209/48 , C07D213/73 , C07D235/28 , C07D239/42 , C07D277/82 , C07D295/135 , C07D317/66 , C12N15/113 , C12N15/11 , A61K31/70 , C07H21/00
CPC分类号： C07D209/48 , A61K31/167 , A61K31/4015 , A61K31/505 , A61K31/5377 , A61K31/7088 , A61K38/00 , C07C237/20 , C07C237/40 , C07C323/44 , C07D213/73 , C07D235/28 , C07D239/42 , C07D277/82 , C07D295/135 , C07D317/66 , C12N15/1137 , C12N2310/315 , C12N2310/321 , C12N2310/341 , C12N2310/345 , C12N2310/346 , C12N2310/3521
摘要： This invention relates to the inhibition of histone deacetylase (HDAC) expression and enzymatic activity. The invention provides methods and reagents for inhibiting HDAC-7 and HDAC-8 by inhibiting expression at the nucleic acid level or inhibiting enzymatic activity at the protein level.
摘要翻译：本发明涉及组蛋白脱乙酰酶（HDAC）表达和酶活性的抑制。本发明提供了通过抑制核酸水平的表达或抑制蛋白质水平的酶活性来抑制HDAC-7和HDAC-8的方法和试剂。

10. 发明申请

WO0023112A9 MODULATION OF GENE EXPRESSION BY COMBINATION THERAPY 审中-公开
标题翻译：基因表达调控联合治疗
公开(公告)号：WO0023112A9
公开(公告)日：2000-08-31
申请号：PCT/US9924278
申请日：1999-10-19
申请人： METHYLGENE INC , BESTERMAN JEFFREY M , MACLEOD ALAN ROBERT , SIDERS WILLIAM M
发明人： BESTERMAN JEFFREY M , MACLEOD ALAN ROBERT , SIDERS WILLIAM M
IPC分类号： C12N15/09 , A61K31/165 , A61K31/19 , A61K31/513 , A61K31/517 , A61K31/706 , A61K31/7068 , A61K31/7088 , A61K31/7125 , A61K38/00 , A61K45/00 , A61K45/06 , A61K48/00 , A61P35/00 , C12N5/10 , C12N15/113
CPC分类号： C12N15/1137 , A61K38/00 , A61K45/06 , C12N2310/315 , C12N2310/321 , C12N2310/341 , C12N2310/346 , C12Y201/01045 , C12Y203/01048 , C12N2310/3521
摘要： The invention relates to the modulation of gene expression. In particular, the invention relates to compositions comprising antisense oligonucleotides which inhibit expression of a gene in operable association with protein effectors of a product of that gene, and methods of using the same. In addition, the invention relates to the modulation of mammalian gene expression regulated by methylation.
摘要翻译：本发明涉及基因表达的调节。特别地，本发明涉及包含反义寡核苷酸的组合物，所述反义寡核苷酸抑制与该基因的产物的蛋白质效应子可操作相关的基因的表达，以及使用该基因的方法。另外，本发明涉及由甲基化调节的哺乳动物基因表达的调节。

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