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1. 发明申请

WO2007008514A3 INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 审中-公开
标题翻译：糖原合成酶激酶抑制剂3
公开(公告)号：WO2007008514A3
公开(公告)日：2007-10-04
申请号：PCT/US2006026137
申请日：2006-07-06
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , GAYSINA IRINA , PETUKHOV PAVEL , SRIDHAR JAYALAKSHMI , TUECKMANTEL WERNER
发明人： KOZIKOWSKI ALAN P , GAYSINA IRINA , PETUKHOV PAVEL , SRIDHAR JAYALAKSHMI , TUECKMANTEL WERNER
IPC分类号： A01N43/56
CPC分类号： C07D403/14 , C07D403/04
摘要： One aspect of the present invention relates to heterocyclic compounds that inhibit mammalian or human glycogen synthase kinase 3. Another aspect of the invention relates to pharmaceutical compositions comprising such a heterocyclic compound. The present invention also relates to methods of treating a mammal or human suffering from a malady that is based at least in part on abnormal activity of glycogen synthase kinase 3. The present invention also relates to methods of treating a mammal or human suffering from diabetes, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, ALS, MS, or schizophrenia.
摘要翻译：本发明的一个方面涉及抑制哺乳动物或人糖原合酶激酶3的杂环化合物。本发明的另一方面涉及包含这种杂环化合物的药物组合物。本发明还涉及治疗患有至少部分基于糖原合酶激酶3的异常活性的疾病的哺乳动物或人的方法。本发明还涉及治疗患有糖尿病的哺乳动物或人的方法，阿尔茨海默氏病，亨廷顿舞蹈病，帕金森病，艾滋病相关性痴呆，ALS，MS或精神分裂症。

2. 发明申请

WO2004024939A3 LIGANDS FOR THE PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR, AND METHODS OF USE THEREOF 审中-公开
标题翻译：过氧化物酶促增殖因子受体的配体及其使用方法
公开(公告)号：WO2004024939A3
公开(公告)日：2004-10-14
申请号：PCT/US0328931
申请日：2003-09-12
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , GLAZER ROBERT I , PETUKHOV PAVEL , WEI ZHI-LIANG
发明人： KOZIKOWSKI ALAN P , GLAZER ROBERT I , PETUKHOV PAVEL , WEI ZHI-LIANG
IPC分类号： A61K31/381 , A61K31/4015 , A61K31/423 , A61K31/428 , A61K31/44 , A61K31/45 , C07D207/456 , C07D213/62 , C07D261/08 , C07D333/30 , C07D413/06 , C07D413/12 , C07D471/04 , C07D498/02 , C12Q20060101
CPC分类号： C07D471/04 , C07D261/08 , C07D413/06 , C07D413/12
摘要： One aspect of the present invention relates to compounds that are active at a peroxisome proliferator-activated receptor (PPAR). In certain embodiments, the compound has a isoxazole or indole core. Another aspect of the present invention relates to a method of treating a mammal afflicted with cancer or non-insulin-dependent (type II) diabetes by administering a therapeutic amount of the compounds of the invention. In certain embodiments, the invention relates to a method of treating prostrate, stomach, or breast cancer. Another aspect of the invention relates to a method of identifying ligands active at a PPAR subtype using X-ray structural information. In certain embodiments, the method of identifying the ligand comprises using molecular modeling approaches including: in silico screening of chemical databases, de novo/rational drug design in which the ligand will be created computationally, and/or in silico screening of virtual combinatorial libraries.
摘要翻译：本发明的一个方面涉及在过氧化物酶体增殖物激活受体（PPAR）上有活性的化合物。在某些实施方案中，化合物具有异恶唑或吲哚核。本发明的另一方面涉及通过施用治疗量的本发明化合物治疗患有癌症或非胰岛素依赖型（II型）糖尿病的哺乳动物的方法。在某些实施方案中，本发明涉及治疗前列腺癌，胃癌或乳腺癌的方法。本发明的另一方面涉及使用X射线结构信息鉴定在PPAR亚型上活性的配体的方法。在某些实施方案中，鉴定配体的方法包括使用分子模拟方法，包括：化学数据库的计算机筛选，计算地创建配体的重新/合理的药物设计，和/或虚拟组合文库的计算机筛选。

3. 发明申请

WO2011159523A3 METHOD AND APPARATUS FOR USE WITH AN INFLOW CONTROL DEVICE 审中-公开
标题翻译：使用流入控制装置的方法和装置
公开(公告)号：WO2011159523A3
公开(公告)日：2012-04-05
申请号：PCT/US2011039472
申请日：2011-06-07
申请人： SCHLUMBERGER CA LTD , SCHLUMBERGER SERVICES PETROL , SCHLUMBERGER HOLDINGS , SCHLUMBERGER TECHNOLOGY BV , PRAD RES & DEV LTD , SCHLUMBERGER TECHNOLOGY CORP , THORKILDSEN TAGE , JOKELA TIMO , PETUKHOV PAVEL , DESTAD MARIUS , RIISEM EDVIN EIMSTAD
发明人： THORKILDSEN TAGE , JOKELA TIMO , PETUKHOV PAVEL , DESTAD MARIUS , RIISEM EDVIN EIMSTAD
IPC分类号： E21B34/08 , E21B43/02 , E21B43/12
CPC分类号： E21B34/063 , E21B43/04 , E21B43/08 , Y10T137/1624 , Y10T137/1789
摘要： A technique includes running a completion assembly downhole into a well. The assembly includes a valve and a material that is adapted to initially configure the valve to prevent fluid flow through the valve in at least one direction. The technique includes performing a downhole completion operation in the well and disintegrating the material to allow the prevented fluid flow through a nozzle of the valve. The nozzle is used to regulate production or injection in the well.
摘要翻译：一种技术包括将井下的完井组件运行到井中。组件包括阀和材料，其适于初始构造阀以防止流体在至少一个方向上流过阀。该技术包括在井中进行井下完井操作并使材料崩解，以防止流体流过阀的喷嘴。喷嘴用于调节井中的生产或注入。

4. 发明申请

WO2008019025A3 ISOFORM-SELECTIVE HDAC INHIBITORS 审中-公开
标题翻译： ISOFORM-SELECTIVE HDAC抑制剂
公开(公告)号：WO2008019025A3
公开(公告)日：2008-09-12
申请号：PCT/US2007017205
申请日：2007-08-02
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , JUNG MIRA , DRITSCHILO ANTATOLY , GAYSIN ARSEN , PETUKHOV PAVEL , TUECKMANTEL WERNER , YUAN HONGBIN
发明人： KOZIKOWSKI ALAN P , JUNG MIRA , DRITSCHILO ANTATOLY , GAYSIN ARSEN , PETUKHOV PAVEL , TUECKMANTEL WERNER , YUAN HONGBIN
IPC分类号： C07D277/04 , A61K31/44 , C07D277/08
CPC分类号： C07D277/46 , C07C259/06 , C07C323/60
摘要： One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.
摘要翻译：本发明的一个方面涉及同种型选择性HDAC抑制剂。还提供了使癌细胞对放射疗法的细胞毒性作用敏感的方法。本发明还提供治疗癌症的方法，治疗神经疾病的方法和治疗疟疾的方法。此外，本发明提供了包含本发明的HDAC抑制剂的药物组合物; 和包含本发明的HDAC抑制剂的试剂盒。

5. 发明申请

WO2007008514A2 INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 审中-公开
标题翻译： GLYCOGEN SYNTHASE KINASE的抑制剂3
公开(公告)号：WO2007008514A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/026137
申请日：2006-07-06
申请人： GEORGETOWN UNIVERSITY , KOZIKOWSKI, Alan, P. , GAYSINA, Irina , PETUKHOV, Pavel , SRIDHAR, Jayalakshmi , TUECKMANTEL, Werner
发明人： KOZIKOWSKI, Alan, P. , GAYSINA, Irina , PETUKHOV, Pavel , SRIDHAR, Jayalakshmi , TUECKMANTEL, Werner
IPC分类号： A61K31/426
CPC分类号： C07D403/14 , C07D403/04
摘要： One aspect of the present invention relates to heterocyclic compounds that inhibit mammalian or human glycogen synthase kinase 3. Another aspect of the invention relates to pharmaceutical compositions comprising such a heterocyclic compound. The present invention also relates to methods of treating a mammal or human suffering from a malady that is based at least in part on abnormal activity of glycogen synthase kinase 3. The present invention also relates to methods of treating a mammal or human suffering from diabetes, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, ALS, MS, or schizophrenia.
摘要翻译：本发明的一个方面涉及抑制哺乳动物或人糖原合成酶激酶3的杂环化合物。本发明的另一方面涉及包含这种杂环化合物的药物组合物。本发明还涉及治疗至少部分基于糖原合成酶激酶3的异常活性的患有疾病的哺乳动物或人的方法。本发明还涉及治疗患有糖尿病的哺乳动物或人的方法，阿尔茨海默病，亨廷顿氏病，帕金森病，AIDS相关性痴呆，ALS，MS或精神分裂症。

6. 发明申请

WO2005007091A3 HISTONE DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： HISTONE DEACETYLASE抑制剂及其使用方法
公开(公告)号：WO2005007091A3
公开(公告)日：2005-04-28
申请号：PCT/US2004021663
申请日：2004-07-07
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , DRITSCHILO ANATOLY , JUNG MIRA , PETUKHOV PAVEL , CHEN BIN
发明人： KOZIKOWSKI ALAN P , DRITSCHILO ANATOLY , JUNG MIRA , PETUKHOV PAVEL , CHEN BIN
IPC分类号： A01N37/10 , A01N43/40 , A01N43/42 , A61K20060101 , C07C259/04 , C07C271/02 , C07C275/24 , C07C275/26 , C07C275/40 , C07C323/44 , C07C323/60 , C07D215/48 , C07D215/54
CPC分类号： C07D215/54 , C07C271/02 , C07C275/24 , C07C275/26 , C07C275/40 , C07C323/44 , C07C323/60 , C07C2603/74 , C07D215/48
摘要： One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
摘要翻译：本发明的一个方面涉及HDAC抑制剂。还提供了使癌细胞对放射疗法的细胞毒性作用敏感的方法。本发明还提供治疗癌症的方法和治疗神经疾病的方法。此外，本发明进一步提供了包含本发明的HDAC抑制剂的药物组合物，以及包含含有本发明的HDAC抑制剂的容器的试剂盒。

7. 发明申请

WO2005007091A2 HISTONE DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：组织脱乙酰酶抑制剂及其使用方法
公开(公告)号：WO2005007091A2
公开(公告)日：2005-01-27
申请号：PCT/US2004/021663
申请日：2004-07-07
申请人： GEORGETOWN UNIVERSITY , KOZIKOWSKI, Alan, P. , DRITSCHILO, Anatoly , JUNG, Mira , PETUKHOV, Pavel , CHEN, Bin
发明人： KOZIKOWSKI, Alan, P. , DRITSCHILO, Anatoly , JUNG, Mira , PETUKHOV, Pavel , CHEN, Bin
IPC分类号： A61K
CPC分类号： C07D215/54 , C07C271/02 , C07C275/24 , C07C275/26 , C07C275/40 , C07C323/44 , C07C323/60 , C07C2603/74 , C07D215/48
摘要： One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
摘要翻译：本发明的一个方面涉及HDAC抑制剂。还提供了使癌细胞对放射治疗的细胞毒性作用敏感的方法。本发明还提供了治疗癌症的方法和治疗神经疾病的方法。另外，本发明还提供了包含本发明的HDAC抑制剂的药物组合物和包含含有本发明的HDAC抑制剂的容器的试剂盒。

8. 发明申请

WO2004024939A2 LIGANDS FOR THE PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR, AND METHODS OF USE THEREOF 审中-公开
标题翻译：过氧化物酶体增殖物激活受体的配体及其使用方法
公开(公告)号：WO2004024939A2
公开(公告)日：2004-03-25
申请号：PCT/US2003/028931
申请日：2003-09-12
申请人： GEORGETOWN UNIVERSITY , KOZIKOWSKI, Alan, P. , GLAZER, Robert, I. , PETUKHOV, Pavel , WEI, Zhi-Liang
发明人： KOZIKOWSKI, Alan, P. , GLAZER, Robert, I. , PETUKHOV, Pavel , WEI, Zhi-Liang
IPC分类号： C12Q
CPC分类号： C07D471/04 , C07D261/08 , C07D413/06 , C07D413/12
摘要： One aspect of the present invention relates to compounds that are active at a peroxisome proliferator-activated receptor (PPAR). In certain embodiments, the compound has a isoxazole or indole core. Another aspect of the present invention relates to a method of treating a mammal afflicted with cancer or non-insulin-dependent (type II) diabetes by administering a therapeutic amount of the compounds of the invention. In certain embodiments, the invention relates to a method of treating prostrate, stomach, or breast cancer. Another aspect of the invention relates to a method of identifying ligands active at a PPAR subtype using X-ray structural information. In certain embodiments, the method of identifying the ligand comprises using molecular modeling approaches including: in silico screening of chemical databases, de novo /rational drug design in which the ligand will be created computationally, and/or in silico screening of virtual combinatorial libraries.
摘要翻译：本发明的一个方面涉及对过氧化物酶体增殖物激活受体（PPAR）有活性的化合物。在某些实施方案中，该化合物具有异恶唑或吲哚核心。本发明的另一个方面涉及通过施用治疗量的本发明化合物治疗患有癌症或非胰岛素依赖性（II型）糖尿病的哺乳动物的方法。在某些实施方案中，本发明涉及治疗前列腺癌，胃癌或乳腺癌的方法。本发明的另一方面涉及使用X射线结构信息鉴定在PPAR亚型上有活性的配体的方法。在某些实施方案中，鉴定配体的方法包括使用分子建模方法，包括：在计算机化学数据库筛选中，从头/合理的药物设计，其中配体将是在计算机上创建和/或虚拟组合库的计算机筛选。

9. 发明申请

WO2011159523A2 METHOD AND APPARATUS FOR USE WITH AN INFLOW CONTROL DEVICE 审中-公开
标题翻译：使用流入控制装置的方法和装置
公开(公告)号：WO2011159523A2
公开(公告)日：2011-12-22
申请号：PCT/US2011/039472
申请日：2011-06-07
申请人： SCHLUMBERGER CANADA LIMITED , SERVICES PETROLIERS SCHLUMBERGER , SCHLUMBERGER HOLDINGS LIMITED , SCHLUMBERGER TECHNOLOGY B.V. , PRAD RESEARCH AND DEVELOPMENT LIMITED , SCHLUMBERGER TECHNOLOGY CORPORATION , THORKILDSEN, Tage , JOKELA, Timo , PETUKHOV, Pavel , DESTAD, Marius , RIISEM, Edvin Eimstad
发明人： THORKILDSEN, Tage , JOKELA, Timo , PETUKHOV, Pavel , DESTAD, Marius , RIISEM, Edvin Eimstad
IPC分类号： E21B34/08 , E21B43/02 , E21B43/12
CPC分类号： E21B34/063 , E21B43/04 , E21B43/08 , Y10T137/1624 , Y10T137/1789
摘要： A technique includes running a completion assembly downhole into a well. The assembly includes a valve and a material that is adapted to initially configure the valve to prevent fluid flow through the valve in at least one direction. The technique includes performing a downhole completion operation in the well and disintegrating the material to allow the prevented fluid flow through a nozzle of the valve. The nozzle is used to regulate production or injection in the well.
摘要翻译：一种技术包括将井下的完井组件运行到井中。组件包括阀和材料，其适于初始构造阀以防止流体在至少一个方向上流过阀。该技术包括在井中进行井下完井操作并使材料崩解，以防止流体流过阀的喷嘴。喷嘴用于调节井中的生产或注入。

10. 发明申请

WO2004041211A3 INHIBITORS OF beta-SECRETASE, AND THEIR USE FOR THE PREVENTION OR TREATMENT OF ALZHEIMER'S DISEASE OR MILD COGNITIVE IMPAIRMENT 审中-公开
标题翻译： β-分泌酶抑制剂及其用于预防或治疗阿尔茨海默病或轻度认知障碍的用途
公开(公告)号：WO2004041211A3
公开(公告)日：2004-09-10
申请号：PCT/US0335219
申请日：2003-11-03
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , AISEN PAUL S , PETUKHOV PAVEL
发明人： KOZIKOWSKI ALAN P , AISEN PAUL S , PETUKHOV PAVEL
IPC分类号： A61K20060101 , A61K31/34 , A61K31/38 , A61K31/40 , C07C233/00 , C07C275/14 , C07C275/16 , C07C275/20 , C07C275/24 , C07D207/10 , C07D307/02 , C07D307/66 , C07D333/36 , C07D405/00
CPC分类号： C40B40/04 , C07C275/14 , C07C275/16 , C07C275/20 , C07C275/24 , C07D307/66 , C07D333/36
摘要： One aspect of the present invention relates to urea-containing compounds. In certain embodiments, the urea-containing compounds of the present invention comprise a heteroaromatic moiety. Another aspect of the present invention relates to a method of inhibiting a beta-secretase using a urea-containing compound of the present invention. A third aspect of the present invention relates to a method of treating Alzheimer's Disease or mild cognitive impairment using a urea-containing compound of the present invention.
摘要翻译：本发明的一个方面涉及含脲化合物。在某些实施方案中，本发明的含脲化合物包含杂芳族部分。本发明的另一方面涉及使用本发明的含脲化合物来抑制β-分泌酶的方法。本发明的第三方面涉及使用本发明的含尿素化合物治疗阿尔茨海默氏病或轻度认知障碍的方法。

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