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1. 发明申请

WO2007072179A3 HISTONE DEACETYLASE INHIBITORS FOR ENHANCING ACTIVITY OF ANTIFUNGAL AGENTS 审中-公开
标题翻译：用于增强抗真菌药物活性的脱乙酰壳多糖酶抑制剂
公开(公告)号：WO2007072179A3
公开(公告)日：2007-10-11
申请号：PCT/IB2006003697
申请日：2006-12-19
申请人： METHYLGENE INC , GEORGOPAPADAKOU NAFSIKA , HU WENQI , CAMPEOL NADIA , BEDARD JEAN , DEZIEL ROBERT , AJAMIAN ALAIN
发明人： GEORGOPAPADAKOU NAFSIKA , HU WENQI , CAMPEOL NADIA , BEDARD JEAN , DEZIEL ROBERT , AJAMIAN ALAIN
IPC分类号： C07C259/06 , A61K31/165 , A61K31/166 , A61K31/351 , A61K31/4196 , A61K31/496 , A61K31/506 , A61P31/10
CPC分类号： C07C259/06 , A01N43/653 , A01N43/84 , A61K31/165 , A61K31/166 , A61K31/19 , A61K31/35 , A61K31/351 , A61K31/404 , A61K31/4196 , A61K31/496 , A61K31/506 , A61K45/06 , A01N37/28 , A01N43/16 , A01N43/38 , A01N61/00 , A01N2300/00 , A61K2300/00
摘要： The present invention relates to compounds, compositions thereof and methods to selectively treat fungal infections More particularly this invention relates to compounds, compositions thereof and methods for selectively enhancing fungal sensitivity to antifungal compounds The compounds are hydroxamate-based inhibitors of histone deacetylase (HDAC) which show synergistic activity with antifungal agents against fungal species at concentrations of inhibitor non toxic to mammalian cells.
摘要翻译：本发明涉及化合物，其组合物和选择性处理真菌感染的方法更具体地说，本发明涉及化合物，其组合物和选择性提高对真菌化合物的真菌敏感性的方法。该化合物是组氨酸脱乙酰酶（HDAC）的基于异羟肟酸盐的抑制剂，其中在对哺乳动物细胞无毒性的抑制剂浓度下，与抗真菌剂显示出与抗真菌剂的协同作用。

2. 发明申请

WO2008035209A3 QUINOLINE AND QUINAZOLINE DERIVATIVES AS INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY 审中-公开
标题翻译：喹啉和喹唑啉衍生物作为蛋白酪氨酸激酶活性的抑制剂
公开(公告)号：WO2008035209A3
公开(公告)日：2011-03-03
申请号：PCT/IB2007003264
申请日：2007-05-30
申请人： METHYLGENE INC , RAEPPEL STEPHANE , CLARIDGE STEPHEN WILLIAM , SAAVEDRA OSCAR MARIO , VAISBURG ARKADII , DEZIEL ROBERT , ZHAN LIJIE , MANNION MICHAEL , GAUDETTE FREDERIC , ZHOU NANCY Z , ISAKOVIC LJUBOMIR
发明人： RAEPPEL STEPHANE , CLARIDGE STEPHEN WILLIAM , SAAVEDRA OSCAR MARIO , VAISBURG ARKADII , DEZIEL ROBERT , ZHAN LIJIE , MANNION MICHAEL , GAUDETTE FREDERIC , ZHOU NANCY Z , ISAKOVIC LJUBOMIR
IPC分类号： C07D401/12 , A61K31/4709 , A61K31/517 , A61K31/5377 , A61P35/00 , C07D401/14 , C07D403/12 , C07D413/14
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D413/14 , C12N9/1205
摘要： The invention relates to quinoline and qumazoline derivatives that inhibit protein tyrosine kinase activity In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling The invention also provides compositions and methods for treating cell proliferative diseases and conditions
摘要翻译：本发明涉及抑制蛋白酪氨酸激酶活性的喹啉和喹唑啉衍生物。具体地，本发明涉及抑制生长因子受体的蛋白酪氨酸激酶活性的化合物，导致受体信号传导的抑制，例如VEGF受体信号传导的抑制和 HGF受体信号传导更具体地，本发明涉及用于抑制VEGF受体信号传导和HGF受体信号传导的化合物，组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

3. 发明申请

WO2008041053A2 INHIBITORS OF VEGF RECEPTOR AND HGF RECEPTOR SIGNALING 审中-公开
标题翻译： VEGF受体和HGF受体信号的抑制剂
公开(公告)号：WO2008041053A2
公开(公告)日：2008-04-10
申请号：PCT/IB2006004306
申请日：2006-05-19
申请人： METHYLGENE INC , SAAVEDRA OSCAR MARIO , CLARIDGE STEPHEN WILLIAM , ZHAN LIJIE , RAEPPEL FRANCK , VAISBURG ARKADII , RAEPPEL STEPHANE , DEZIEL ROBERT , MANNION MICHAEL , ZHOU NANCY , GAUDETTE FREDERIC , ISAKOVIC LJUBOMIR , WAHHAB AMAL , GRANGER MARIE-CLAUDE , BERNSTEIN NAOMY
发明人： SAAVEDRA OSCAR MARIO , CLARIDGE STEPHEN WILLIAM , ZHAN LIJIE , RAEPPEL FRANCK , VAISBURG ARKADII , RAEPPEL STEPHANE , DEZIEL ROBERT , MANNION MICHAEL , ZHOU NANCY , GAUDETTE FREDERIC , ISAKOVIC LJUBOMIR , WAHHAB AMAL , GRANGER MARIE-CLAUDE , BERNSTEIN NAOMY
CPC分类号： C07D495/04
摘要： The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions
摘要翻译：本发明涉及VEGF受体信号传导和HGF受体信号转导的抑制。本发明提供了用于抑制VEGF受体信号传导和HGF受体信号传导的化合物和方法。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

4. 发明申请

WO2007054831A3 INHIBITORS OF VEGF RECEPTOR AND HGF RECEPTOR SIGNALING 审中-公开
标题翻译： VEGF受体和HGF受体信号的抑制剂
公开(公告)号：WO2007054831A3
公开(公告)日：2007-10-04
申请号：PCT/IB2006003903
申请日：2006-05-19
申请人： METHYLGENE INC , SAAVEDRA OSCAR MARIO , CLARIDGE STEPHEN WILLIAM , ZHAN LIJIE , RAEPPEL FRANCK , VAISBURG ARKADII , RAEPPEL STEPHANE , DEZIEL ROBERT , MANNION MICHAEL , ZHOU NANCY Z , ISAKOVIC LJUBOMIR
发明人： SAAVEDRA OSCAR MARIO , CLARIDGE STEPHEN WILLIAM , ZHAN LIJIE , RAEPPEL FRANCK , VAISBURG ARKADII , RAEPPEL STEPHANE , DEZIEL ROBERT , MANNION MICHAEL , ZHOU NANCY Z , ISAKOVIC LJUBOMIR
IPC分类号： C07D495/04 , A61K31/4365 , A61P35/00 , C07D487/04
CPC分类号： C07D495/04 , A61K31/519 , A61K31/522
摘要： The invention relates to the inhibition of vascular endothelial growth factor (VEGF) receptor signaling and hepatocyte growth factor (HGF) receptor signaling The invention provides compound A and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. Formula (A).
摘要翻译：本发明涉及血管内皮生长因子（VEGF）受体信号传导和肝细胞生长因子（HGF）受体信号传导的抑制本发明提供化合物A和抑制VEGF受体信号传导和HGF受体信号传导的方法。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。式（A）。

5. 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。

6. 发明申请

WO2008055068A3 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
标题翻译： HISTONE DEACETYLASE的抑制剂
公开(公告)号：WO2008055068A3
公开(公告)日：2009-03-05
申请号：PCT/US2007082668
申请日：2007-10-26
申请人： METHYGENE INC , EN VIVO PHARMACEUTICALS INC , DEZIEL ROBERT , LEIT SILVANA , BEAULIEU PATRICK , CHANTIGNY YVES ANDRE , MANCUSO JOHN , TESSIER PIERRE , SHAPIRO GIDEON , CHESWORTH RICHARD , SMIL DAVID
发明人： DEZIEL ROBERT , LEIT SILVANA , BEAULIEU PATRICK , CHANTIGNY YVES ANDRE , MANCUSO JOHN , TESSIER PIERRE , SHAPIRO GIDEON , CHESWORTH RICHARD , SMIL DAVID
IPC分类号： C07D209/22 , A61K31/55 , A61K31/5513 , A61K31/553 , A61K31/554 , A61P43/00 , C07D209/70 , C07D221/12 , C07D223/26 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/14 , C07D243/24
CPC分类号： C07D498/04 , C07C259/06 , C07C259/10 , C07D209/02 , C07D209/08 , C07D209/52 , C07D209/94 , C07D221/12 , C07D223/16 , C07D223/20 , C07D223/22 , C07D223/24 , C07D223/26 , C07D223/28 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/24 , C07D243/38 , C07D265/38 , C07D267/14 , C07D267/18 , C07D267/20 , C07D279/22 , C07D279/26 , C07D281/16 , C07D285/36 , C07D291/08 , C07D295/155 , C07D313/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/06 , C07D413/12 , C07D471/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D487/08 , C07D487/14 , C07D491/08 , C07D495/04 , C07D513/04 , C07H13/10
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein (B), Q, J, L and Z are as defined in the specification.
摘要翻译：本发明涉及抑制组蛋白脱乙酰酶的化合物。更具体地，本发明提供式（I）的化合物，其中（B），Q，J，L和Z如说明书中所定义。

7. 发明申请

WO2004011478A3 ANTI-VIRAL 7-DEAZA D-NUCLEOSIDES AND USES THEREOF 审中-公开
标题翻译：抗病毒7-脱氧D-核苷及其用途
公开(公告)号：WO2004011478A3
公开(公告)日：2004-06-24
申请号：PCT/CA0301121
申请日：2003-07-25
申请人： MICROLOGIX BIOTECH INC , MEKOUAR KHALID , DEZIEL ROBERT
发明人： MEKOUAR KHALID , DEZIEL ROBERT
IPC分类号： C07H19/14 , A61K31/7064 , A61P31/12 , A61P31/20 , C07H19/00 , C07H19/22 , A61K31/70
CPC分类号： C07H19/00 , C07H19/22
摘要： The present invention relates generally to anti-viral compounds, particularly anti-viral 7-deaza D-nucleosides and analogues, or derivatives thereof. The invention also relates to the use of such compounds to treat or prevent hepatitis B virus (HBV) infections, and to the use of such compounds to examine the biological mechanisms of HBV infection.
摘要翻译：本发明一般涉及抗病毒化合物，特别是抗病毒7-脱氮D-核苷及其类似物或其衍生物。本发明还涉及这些化合物用于治疗或预防乙型肝炎病毒（HBV）感染的用途，以及这些化合物用于检查HBV感染的生物学机制的用途。

8. 发明申请

WO2008055068A8 INHIBITORS OF HISTONE DEACETYLASE 审中-公开
公开(公告)号：WO2008055068A8
公开(公告)日：2008-07-24
申请号：PCT/US2007082668
申请日：2007-10-26
申请人： METHYGENE INC , EN VIVO PHARMACEUTICALS INC , DEZIEL ROBERT , LEIT SILVANA , BEAULIEU PATRICK , CHANTIGNY YVES ANDRE , MANCUSO JOHN , TESSIER PIERRE , SHAPIRO GIDEON , CHESWORTH RICHARD , SMIL DAVID
发明人： DEZIEL ROBERT , LEIT SILVANA , BEAULIEU PATRICK , CHANTIGNY YVES ANDRE , MANCUSO JOHN , TESSIER PIERRE , SHAPIRO GIDEON , CHESWORTH RICHARD , SMIL DAVID
IPC分类号： C07D223/26 , A61K31/55 , A61K31/554 , C07D243/24 , C07D267/20 , C07D281/16 , C07D291/08 , C07D401/14 , C07D471/04
CPC分类号： C07D498/04 , C07C259/06 , C07C259/10 , C07D209/02 , C07D209/08 , C07D209/52 , C07D209/94 , C07D221/12 , C07D223/16 , C07D223/20 , C07D223/22 , C07D223/24 , C07D223/26 , C07D223/28 , C07D225/08 , C07D239/28 , C07D239/34 , C07D239/42 , C07D243/24 , C07D243/38 , C07D265/38 , C07D267/14 , C07D267/18 , C07D267/20 , C07D279/22 , C07D279/26 , C07D281/16 , C07D285/36 , C07D291/08 , C07D295/155 , C07D313/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/06 , C07D413/12 , C07D471/04 , C07D471/08 , C07D471/14 , C07D487/04 , C07D487/08 , C07D487/14 , C07D491/08 , C07D495/04 , C07D513/04 , C07H13/10
摘要： This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of formula (I) wherein (B), Q, J, L and Z are as defined in the specification.

9. 发明申请

WO02076982A3 NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS 审中-公开
标题翻译：非核苷酸逆转录酶抑制剂
公开(公告)号：WO02076982A3
公开(公告)日：2002-12-12
申请号：PCT/CA0200385
申请日：2002-03-21
申请人： BOEHRINGER INGELHEIM CA LTD , OGILVIE WILLIAM W , DEZIEL ROBERT , NAUD JULIE , O'MEARA JEFFREY
发明人： OGILVIE WILLIAM W , DEZIEL ROBERT , NAUD JULIE , O'MEARA JEFFREY
IPC分类号： A61K31/551 , A61P31/14 , A61P31/18 , A61P43/00 , C07D471/14 , A61K31/55
CPC分类号： C07D471/14
摘要： A compound of formula (I) wherein A is a connecting chain of (C1-3) alkyl; B is O or S; R is H, (C1-6) alkyl, halo, CF3, or OR wherein R is H or (C1-6)alkyl; R is H or Me; R is H or Me; R is H, (C1-4) alkyl, (C3-4) cycloalkyl and (C1-4)alkyl(C3-7)cycloalkyl; W is selected form formula (i), (ii) or (iii) wherein, a) one of Y is SO2 and the other Y is NR , provided that both are not the same, wherein R is H, (C1-6)alkyl,(C3-6) cycloalkyl, the alkyl being substituted, COR , COOR or CONR R ; and each R is H, (C1-4) alkyl, (C3-6) cycloalkyl, or (C1-4) alkyl-(C3-6) cycloalkyl; or b) E is CR R wherein R and R is H, or alkyl and J is CH2; or J is CR R and E is CH2, and the dotted line represents a single bond; or c) E is C(O) and J is CR R or J is C(O) and E is CR R and the dotted line represents a single bond; or d) E and J are CR R and the dotted line represents a double bond. Compounds of formula I have activity against HIV WT and double mutant strains.
摘要翻译：式（I）的化合物，其中A是（C 1-3）烷基的连接链; B是O或S; R 1是H，（C 1-6）烷基，卤素，CF 3或OR 1a，其中R 1a是H或（C 1-6）烷基; R 2是H或Me; R 3是H或Me; R 4是H，（C 1-4）烷基，（C 3-8）环烷基和（C 1-4）烷基（C 3-7）环烷基; W选自式（i），（ii）或（iii），其中a）Y中的一个是SO 2，另一个Y是NR 5，条件是两者不同，其中R 5是H ，（C 1-6）烷基，（C 3-6）环烷基，取代的烷基，COR 50，COOR 5或CONR 5 R 5; 并且每个R 8是H，（C 1-4）烷基，（C 3-6）环烷基或（C 1-4）烷基 - （C 3-6）环烷基; 或b）E是CR 8a R 8b，其中R 8a和R 8b是H，或烷基，J是CH 2; 或J为CR 8a R 8b且E为CH 2，虚线表示单键; 或c）E是C（O），J是CR 8a R 8b或J是C（O），E是CR 8a R 8b，虚线代表单键; 或d）E和J是CR 8a R 8b，虚线表示双键。式I化合物具有抗HIV WT和双突变株的活性。

10. 发明公开

EP1973872A4 INHIBITORS OF HISTONE DEACETYLASE AND PRODRUGS THEREOF 审中-公开
标题翻译：组蛋白去乙酰化酶抑制剂和前体
公开(公告)号：EP1973872A4
公开(公告)日：2012-05-09
申请号：EP07855542
申请日：2007-12-19
申请人： METHYLGENE INC
发明人： DEZIEL ROBERT , AJAMIAN ALAIN
IPC分类号： C07C311/21 , A61K31/10 , A61K31/16 , A61K31/17 , A61K31/18 , A61K31/34 , A61K31/381 , A61K31/433 , A61K31/435 , A61P35/00 , C07C259/10 , C07C275/42 , C07C317/44 , C07D285/135 , C07D307/54 , C07D333/34 , C07D333/62
CPC分类号： C07C311/21 , C07C259/06 , C07C259/10 , C07C275/42 , C07C279/14 , C07C311/13 , C07C311/29 , C07C311/44 , C07C313/06 , C07C317/44 , C07C2601/02 , C07C2601/04 , C07D213/30 , C07D213/70 , C07D215/24 , C07D235/02 , C07D271/08 , C07D285/135 , C07D307/91 , C07D309/06 , C07D317/30 , C07D317/60 , C07D333/34 , C07D333/62 , C07D409/04

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