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1. 发明申请

WO2009026717A1 INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY 审中-公开
标题翻译：蛋白酪氨酸激酶活性的抑制剂
公开(公告)号：WO2009026717A1
公开(公告)日：2009-03-05
申请号：PCT/CA2008/001538
申请日：2008-08-28
申请人： METHYLGENE INC. , CLARIDGE, Stephen William , ISAKOVIC, Ljubomir , MANNION, Michael , RAEPPEL, Stéphane , SAAVEDRA, Oscar Mario , GAUDETTE, Frédéric , ZHAN, Lijie , ZHOU, Nancy Z. , RAEPPEL, Franck , DÉZIEL, Robert , VAISBURG, Arkadii , UNO, Tetsuyuki
发明人： CLARIDGE, Stephen William , ISAKOVIC, Ljubomir , MANNION, Michael , RAEPPEL, Stéphane , SAAVEDRA, Oscar Mario , GAUDETTE, Frédéric , ZHAN, Lijie , ZHOU, Nancy Z. , RAEPPEL, Franck , DÉZIEL, Robert , VAISBURG, Arkadii , UNO, Tetsuyuki
IPC分类号： C07D495/04 , A61K31/00 , A61K31/4365 , A61P27/02 , A61P35/00 , A61P9/00
CPC分类号： C07D495/04
摘要： The invention relates to compounds of Formula (I) and their use for inhibiting protein tyrosine kinase activity In Formula (I), the group M is thieno[3,2,b]pyridinyl as shown, and the group D is a ring or ring system, and the groups Z, Ar, and G are as defined herein The invention relates particularly to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signalling, for example, the inhibition of VEGF receptor signalling and HGF receptor signalling The invention also provides compositions and methods for treating cell proliferative diseases and conditions, such as cancer, and for treating ophthalmic diseases, including age-related macular degeneration (AMD) and diabetic retinopathy (DR).
摘要翻译：本发明涉及式（I）化合物及其抑制蛋白质酪氨酸激酶活性的用途。在式（I）中，M基团如噻吩并[3,2，b]吡啶基，组D为环或环系统，并且基团Z，Ar和G如本文所定义。本发明特别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受体信号传导本发明还提供用于治疗细胞增殖性疾病和病症如癌症的组合物和方法，以及用于治疗眼科疾病，包括年龄相关性黄斑变性（AMD）和糖尿病性视网膜病变（DR）的组合物和方法。

2. 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

3. 发明申请

WO2007139729A1 NOVEL SULFONAMIDOMETHYLPHOSPHONATE INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-乳酸酶的新型磺酰亚胺磷酸盐抑制剂
公开(公告)号：WO2007139729A1
公开(公告)日：2007-12-06
申请号：PCT/US2007/011977
申请日：2007-05-21
申请人： MERCK & CO., INC. , METHYLGENE INC. , DININNO, Frank , HAMMOND, Milton, L. , DYKSTRA, Kevin , KIM, Seongkon , TAN, Qiang , YOUNG, Ketherine , HERMES, Jeffrey, Donald , RAEPPEL, Stephane , MANNION, Michael , ZHOU, Nancy, Z. , GAUDETTE, Frederic , VAISBURG, Arkadii , RAHIL, Jubrail , GEORGOPAPADAKOU, Nafsika
发明人： DININNO, Frank , HAMMOND, Milton, L. , DYKSTRA, Kevin , KIM, Seongkon , TAN, Qiang , YOUNG, Ketherine , HERMES, Jeffrey, Donald , RAEPPEL, Stephane , MANNION, Michael , ZHOU, Nancy, Z. , GAUDETTE, Frederic , VAISBURG, Arkadii , RAHIL, Jubrail , GEORGOPAPADAKOU, Nafsika
IPC分类号： C07F9/6539 , C07F9/655 , C07F9/6553 , C07F9/6558 , A61K31/662 , A61P31/04
CPC分类号： C07F9/655354 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/65586
摘要： This invention provides novel β-lactamase inhibitors of the aryl-and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases. Formula (I) or a pro-drug or pharmaceutically acceptable salt thereof, wherein: W represents: Formula (II).
摘要翻译：本发明提供了芳基 - 和杂芳基磺酰氨基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其前药或其药学上可接受的盐，其中：W表示：式（II）。

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

WO2005040259A1 IMPROVED NUCLEATING ADDITIVE FORMULATIONS OF BICYCLO[2.2.1]HEPTANE DICARBOXYLATE SALTS 审中-公开
标题翻译：改善BICYCLO的添加剂配方[2.2.1]二丙二酸二乙酯盐
公开(公告)号：WO2005040259A1
公开(公告)日：2005-05-06
申请号：PCT/US2004/025071
申请日：2004-08-04
申请人： MILLIKEN & COMPANY , MANNION, Michael J. , JONES, Jeffrey R.
发明人： MANNION, Michael J. , JONES, Jeffrey R.
IPC分类号： C08K5/098
CPC分类号： C08K3/36 , C08K5/0083 , C08K5/098
摘要： Milled, small particle size, solid bicyclo[2.2.1]heptane dicarboxylate salt-containing thermoplastic nucleating additive formulations further comprising at least one anticaking agent for improved haze reduction, improved nucleation performance, and prevention of potential cementation (via agglomeration) of the salt component present therein are provided. Such small particle size dicarboxylate salts provide desirable properties within thermoplastic articles, particularly as nucleating agents, but apparently suffer from certain clarity issues and agglomeration problems (due to the flat and thin plate structures of such compounds and the propensity they exhibit to cohere to each other during storage), making utilization thereof less desirable for certain applications. Thus, an improvement has been provided to permit full benefit of the excellent crystallization temperatures, stiffness, and calcium stearate compatibility such dicarboxylate salts accord within target low haze thermoplastics. Furthermore, unexpected improvements in dusting reduction have been found upon the utilization of such anticaking additives in combination with the aforementioned nucleating salts. Thermoplastic additive compositions and methods of producing thermoplastics with such nucleator/anticaking additive combinations are also contemplated within this invention.
摘要翻译：固体双环[2.2.1]庚烷二羧酸盐的热塑性成核添加剂制剂，其还包含至少一种用于改善雾度降低的抗结块剂，改进的成核性能以及防止盐的潜在胶结（通过附聚）提供其中存在的组分。这种小粒度的二羧酸盐在热塑性制品中，特别是作为成核剂提供了期望的性质，但显然存在某些澄清问题和附聚问题（由于这些化合物的平板和薄板结构以及它们彼此凝聚的倾向在存储期间），使其利用对于某些应用不太理想。因此，已经提供了一种改进，以使得完全有益于优异的结晶温度，刚度和硬脂酸钙相容性，这样的二羧酸盐符合目标低雾度热塑性塑料。此外，在将这种防结块添加剂与上述成核盐结合使用时，已经发现除尘减少的意想不到的改进。在本发明中也考虑了热塑性添加剂组合物和用这种成核剂/抗结块添加剂组合生产热塑性塑料的方法。

6. 发明申请

WO2009109035A1 INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY 审中-公开
标题翻译：蛋白酪氨酸激酶活性的抑制剂
公开(公告)号：WO2009109035A1
公开(公告)日：2009-09-11
申请号：PCT/CA2009/000228
申请日：2009-02-27
申请人： METHYLGENE INC. , MANNION, Michael , RAEPPEL, Stéphane , CLARIDGE, Stephen William , GAUDETTE, Frédéric , ZHAN, Lijie , ISAKOVIC, Ljubomir , SAAVEDRA, Oscar Mario , UNO, Tetsuyuki , KISHIDA, Masashi , VAISBURG, Arkadii
发明人： MANNION, Michael , RAEPPEL, Stéphane , CLARIDGE, Stephen William , GAUDETTE, Frédéric , ZHAN, Lijie , ISAKOVIC, Ljubomir , SAAVEDRA, Oscar Mario , UNO, Tetsuyuki , KISHIDA, Masashi , VAISBURG, Arkadii
IPC分类号： C07D495/04 , A61K31/4365
CPC分类号： C07D495/04 , C07F9/6561
摘要： This invention relates to compounds 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. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.
摘要翻译：本发明涉及抑制蛋白酪氨酸激酶活性的化合物。特别地，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。本发明还提供了用于治疗细胞增殖性疾病和病症以及眼科疾病，病症和病症的化合物，组合物和方法。

7. 发明申请

WO2008073142A3 NOVEL INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-LACTAMASE的新型抑制剂
公开(公告)号：WO2008073142A3
公开(公告)日：2008-10-02
申请号：PCT/US2007011979
申请日：2007-05-21
申请人： MERCK & CO INC , METHLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , CHEN HELEN , RAEPPEL STEPHANE , MANNION MICHAEL , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHL JUBRAIL , GEORGOPAPADAKOU NAFSIKA , ZHOU NANCY Z
IPC分类号： A61P31/04 , A61K31/67 , A61K31/675 , C07F9/6539 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
CPC分类号： C07F9/655354 , C07F9/65395 , C07F9/6541 , C07F9/6553 , C07F9/6558 , C07F9/6561
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroarylsulfonarnidomethylphosphonate monoester class having nitrogen-based cations or quarternary ammomium groups. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了具有氮基阳离子或季铵基团的芳基和杂芳基磺酰基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其药学上可接受的盐。

8. 发明申请

WO2007139729A8 NOVEL SULFONAMIDOMETHYLPHOSPHONATE INHIBITORS OF BETA-LACTAMASE 审中-公开
标题翻译： β-乳酸酶的新型磺酰亚胺磷酸盐抑制剂
公开(公告)号：WO2007139729A8
公开(公告)日：2008-02-28
申请号：PCT/US2007011977
申请日：2007-05-21
申请人： MERCK & CO INC , METHYLGENE INC , DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , RAEPPEL STEPHANE , MANNION MICHAEL , ZHOU NANCY Z , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHIL JUBRAIL , GEORGOPAPADAKOU NAFSIKA
发明人： DININNO FRANK , HAMMOND MILTON L , DYKSTRA KEVIN , KIM SEONGKON , TAN QIANG , YOUNG KATHERINE , HERMES JEFFREY DONALD , RAEPPEL STEPHANE , MANNION MICHAEL , ZHOU NANCY Z , GAUDETTE FREDERIC , VAISBURG ARKADII , RAHIL JUBRAIL , GEORGOPAPADAKOU NAFSIKA
IPC分类号： C07F9/6539 , A61K31/662 , A61P31/04 , C07F9/655 , C07F9/6553 , C07F9/6558
CPC分类号： C07F9/655354 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/65586
摘要： This invention provides novel ß-lactamase inhibitors of the aryl-and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of ß-lactamases and synergize the antibacterial effects of ß-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the ß-lactam antibiotics as a result of the presence of the ß-lactamases. Formula (I) or a pro-drug or pharmaceutically acceptable salt thereof, wherein: W represents: Formula (II).
摘要翻译：本发明提供了芳基 - 和杂芳基磺酰氨基甲基膦酸酯单酯类的新型β-内酰胺酶抑制剂。该化合物抑制三种类型的β-内酰胺酶，并且与β-内酰胺类抗生素（例如，亚胺培南和头孢他啶的抗菌作用）对抗β-内酰胺抗生素通常具有抗ß-内酰胺抗生素的微生物的协同作用是由于存在β-内酰胺酶。式（I）或其前药或其药学上可接受的盐，其中：W表示：式（II）。

9. 发明申请

WO2007054831A2 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：WO2007054831A2
公开(公告)日：2007-05-18
申请号：PCT/IB2006/003903
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
CPC分类号： C07D495/04 , A61K31/519 , A61K31/522
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受体信号传导的抑制。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

10. 发明申请

WO2007032797A1 SILICA-CONTAINING NUCLEATING AGENT COMPOSITIONS AND METHODS FOR USING SUCH COMPOSITIONS IN POLYOLEFINS 审中-公开
标题翻译：含硅的核化剂组合物和在聚烯烃中使用这些组合物的方法
公开(公告)号：WO2007032797A1
公开(公告)日：2007-03-22
申请号：PCT/US2006/022144
申请日：2006-06-07
申请人： MILLIKEN & COMPANY , LI, Jiang , XU, Jiannong , MANNION, Michael J.
发明人： LI, Jiang , XU, Jiannong , MANNION, Michael J.
IPC分类号： C08K5/00 , C08K5/06 , C08K3/36 , C08K13/02
CPC分类号： C08K5/0083 , C08K5/1575 , C08L23/02
摘要： Diacetals of sorbitols and xylitols are employed in polyolefins as nucleating agents. Diacetals of sorbitols and xylitol nucleating agents may be provided in granular or powder form from hoppers or mixing equipment into polyolefins during the formation of polymeric compositions and polymeric articles. Flow of diacetals of sorbitols and xylitols is improved by the use of certain silicas, in certain defined weight percentages. Submicron size range silica compounds may provide excellent flow enhancement properties when blended and used with such diacetals.
摘要翻译：山梨糖醇和木糖醇的二缩醛用作聚烯烃作为成核剂。山梨糖醇和木糖醇成核剂的二缩醛可以在形成聚合物组合物和聚合物制品期间以颗粒或粉末形式从料斗或混合设备提供到聚烯烃中。通过使用某些确定的重量百分比的某些二氧化硅，改善了山梨糖醇和木糖醇的二缩醛的流动。当与这种二缩醛共混并使用时，亚微米尺寸范围的二氧化硅化合物可以提供优异的流动增强性能。

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