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1. 发明申请

WO2006135721A1 ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS 审中-公开
标题翻译：烷基胆碱和碱性氨基酸激酶调节剂
公开(公告)号：WO2006135721A1
公开(公告)日：2006-12-21
申请号：PCT/US2006/022414
申请日：2006-06-07
申请人： JANSSEN PHARMACEUTICA N.V. , BAINDUR, Nand , GAUL, Michael David , KREUTTER, Kevin, Douglas , XU, Guozhang , TUMAN, Robert, W. , JOHNSON, Dana, L. , BAUMANN, Christian, Andrew , KIM, Alexander, J.
发明人： BAINDUR, Nand , GAUL, Michael David , KREUTTER, Kevin, Douglas , XU, Guozhang , TUMAN, Robert, W. , JOHNSON, Dana, L. , BAUMANN, Christian, Andrew , KIM, Alexander, J.
IPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/517 , A61P35/00
CPC分类号： C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c kit and/or TrkB . The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.
摘要翻译：本发明涉及式I的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，G，Q和X如本文所定义，使用这些化合物作为蛋白质酪氨酸激酶调节剂，特别是FLT3抑制剂， /或c试剂盒和/或TrkB，使用这些化合物降低或抑制细胞或受试者中FLT3和/或c试剂盒和/或TrkB的激酶活性，以及使用这些化合物预防或治疗患有与FLT3和/或c试剂盒和/或TrkB相关的细胞增殖性疾病和/或障碍。本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

2. 发明申请

WO2005049579A2 IMMOBILIZED N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES FOR THE IDENTIFICATION OF BIOMOLECULAR TARGETS 审中-公开
标题翻译：固定化的三取代三环3-氨基吡唑用于鉴定生物分子靶标
公开(公告)号：WO2005049579A2
公开(公告)日：2005-06-02
申请号：PCT/US2004/037364
申请日：2004-11-10
申请人： JANSSEN PHARMACEUTICA N.V. , HO, Chih Y. , GALEMMO, JR., Robert A. , JOHNSON, Dana L. , MEI, Jay M. , BELKOWSKI, Stanley M. , CONNORS PH.D., Richard William
发明人： HO, Chih Y. , GALEMMO, JR., Robert A. , JOHNSON, Dana L. , MEI, Jay M. , BELKOWSKI, Stanley M. , CONNORS PH.D., Richard William
IPC分类号： C07D231/56
CPC分类号： C07D403/12 , C04B35/632 , C07D231/54 , C07D231/56 , C07D401/12 , C07D495/04 , G01N33/574 , G01N2333/71 , G01N2500/00
摘要： The present invention relates to immobilized N-substituted tricyclic 3-aminopyrazole compounds of Formula 1 as tools for the identification of bimolecular targets in cells of therapeutic significance, profiling the selectivity of compounds, prediction of possible related toxicities and exploration of mechanisms of action in biological systems for therapeutic indications related to compounds. These agents can be used to identify biomolecules with the potential to interact with the immobilized reagent. The identified biomolecule may be then be used as a therapeutic target, serve as a marker of drug action, or alternatively describe an untoward or toxic potential of the immobilized agent.
摘要翻译：本发明涉及固定化的式1的N-取代的三环3-氨基吡唑化合物作为用于鉴定治疗意义的细胞中的双分子靶的工具，分析化合物的选择性，预测可能的相关毒性以及探索与化合物相关的治疗适应症的生物系统中的作用机制。这些试剂可用于鉴定具有与固定化试剂相互作用的潜力的生物分子。然后可以将鉴定的生物分子用作治疗靶标，用作药物作用的标记，或者描述固定剂的不利或潜在毒性。

3. 发明申请

WO2003097609A1 N-SUBSTITUTED TRICYCLIC 3-AMINOPYRAZOLES AS PDFG RECEPTOR INHIBITORS 审中-公开
标题翻译：作为PDFG受体抑制剂的N-取代三聚3-氨基吡唑
公开(公告)号：WO2003097609A1
公开(公告)日：2003-11-27
申请号：PCT/US2003/015193
申请日：2003-05-13
申请人： JANSSEN PHARMACEUTICA N.V. , HO, Chih, Yung , BRUNMARK, Bengt, Anders , EMANUEL, Stuart , GALEMMO JR., Robert, A. , JOHNSON, Dana, L. , LUDOVICI, Donald, W. , MAHAROOF, Umar , MEI, Jay, M. , SECHLER, Jan, L. , STROBEL, Eric, D. , TUMAN, Robert, W. , YEN, Hwa, Kwo
发明人： HO, Chih, Yung , BRUNMARK, Bengt, Anders , EMANUEL, Stuart , GALEMMO JR., Robert, A. , JOHNSON, Dana, L. , LUDOVICI, Donald, W. , MAHAROOF, Umar , MEI, Jay, M. , SECHLER, Jan, L. , STROBEL, Eric, D. , TUMAN, Robert, W. , YEN, Hwa, Kwo
IPC分类号： C07D231/54
CPC分类号： C07F9/65038 , C07D231/54 , C07D231/56 , C07D233/64 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D413/12 , C07D491/04 , C07D495/04
摘要： The invention is directed to N-substituted tricyclic 3-AMINOPYRAZOLE derivatives, which are useful as inhibitors of platelet-derived growth factor receptor (PDGF-R) kinase, and methods for the preparation of said derivatives. The present invention is further directed to pharmaceutical compositions comprising the compounds of the presentinvention and to methods for treating conditions such as tumors and other cell proliferative disorders.
摘要翻译：本发明涉及可用作血小板衍生生长因子受体（PDGF-R）激酶抑制剂的N-取代三环3-氨基吡唑衍生物，以及制备所述衍生物的方法。本发明进一步涉及包含本发明化合物的药物组合物和用于治疗诸如肿瘤和其它细胞增殖性疾病的病症的方法。

4. 发明申请

WO2009158345A1 SYSTEM FOR DECONTAMINATING WATER AND GENERATING WATER VAPOR 审中-公开
标题翻译：消除水和生成水蒸气的系统
公开(公告)号：WO2009158345A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048292
申请日：2009-06-23
申请人： VERNO HOLDINGS, LLC , RILEY, John, D. , JOHNSON, Dana, L.
发明人： RILEY, John, D. , JOHNSON, Dana, L.
IPC分类号： B01D1/00
CPC分类号： C02F1/043 , B01D1/225 , C02F1/048 , C02F1/08 , C02F1/18 , C02F2103/08 , C02F2209/02 , C02F2209/42 , F22B3/06 , Y02A20/109 , Y02A20/128 , Y02W10/37 , Y10S159/39 , Y10S159/901
摘要： A system and method for decontaminating water and generating water vapor includes introducing contaminated water in to a vessel. The water is moved through a series of rotating trays alternately separated by stationary baffles so as to swirl and heat the water to effect the vaporization thereof to produce a vapor having at least some of the contaminants separated therefrom. The vapor is removed from the vessel for condensing apart from the separated contaminants and the remaining water. The vapor may be passed through a turbine connected to an electric generator. Sensors in a controller may be employed to adjust the speed of rotation of the trays or water input into the vessel in response to the sensed conditions. The treated water may be recirculated and reprocessed through the vessel to increase the purification thereof.
摘要翻译：用于净化水和产生水蒸汽的系统和方法包括将污染的水引入到容器中。水通过一系列由固定挡板交替分离的旋转托盘移动，以便旋转和加热水以实现其蒸发，以产生至少部分污染物与之分离的蒸汽。蒸汽从容器中取出，用于与分离的污染物和剩余的水冷凝。蒸气可以通过连接到发电机的涡轮机。可以使用控制器中的传感器来响应于感测到的条件来调节托盘或输入到容器中的水的旋转速度。经处理的水可以再循环并通过容器再加工以增加其纯化。

5. 发明申请

WO2006138155A1 SYNERGISTIC MODULATION OF FLT3 KINASE USING A FLT3 INHIBITOR AND A FARNESYL TRANSFERASE INHIBITOR 审中-公开
标题翻译：使用FLT3抑制剂和FARNESYL转移酶抑制剂的FLT3激酶的协同调节
公开(公告)号：WO2006138155A1
公开(公告)日：2006-12-28
申请号：PCT/US2006/022412
申请日：2006-06-07
申请人： JANSSEN PHARMACEUTICA N.V. , BAUMANN, Christian, Andrew , GAUL, Michael David , TUMAN, Robert, W. , JOHNSON, Dana, L.
发明人： BAUMANN, Christian, Andrew , GAUL, Michael David , TUMAN, Robert, W. , JOHNSON, Dana, L.
IPC分类号： A61K31/4427 , A61P35/00 , A61K31/00
CPC分类号： A61K45/06 , A61K31/4427 , A61K31/454 , A61K2300/00
摘要： The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from compounds of Formula (I'). Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
摘要翻译：本发明涉及一种抑制FLT3酪氨酸激酶活性或表达或降低细胞或受试者中FLT3激酶活性或表达的方法，其包括施用法呢基转移酶抑制剂和选自式（I'）化合物的FLT3激酶抑制剂，。本发明包括预防和治疗方法，用于治疗患有（或易于）发展细胞增殖性病症或与FLT3相关的病症的受试者。

6. 发明申请

WO2006135629A1 SYNERGISTIC MODULATION OF FLT3 KINASE USING ALKYLQUINOLINES AND ALKYLQUINAZOLINES 审中-公开
标题翻译：使用烷基喹啉和烷基喹喔啉的FLT3激酶的协同调节
公开(公告)号：WO2006135629A1
公开(公告)日：2006-12-21
申请号：PCT/US2006/022100
申请日：2006-06-07
申请人： JANSSEN PHARMACEUTICA N.V. , BAUMANN, Christian, Andrew , GAUL, Michael David , TUMAN, Robert, W. , JOHNSON, Dana, L.
发明人： BAUMANN, Christian, Andrew , GAUL, Michael David , TUMAN, Robert, W. , JOHNSON, Dana, L.
IPC分类号： A61K31/517 , A61P35/00 , A61K31/4709 , A61K31/00
CPC分类号： A61K31/4709 , A61K31/00 , A61K31/496 , A61K31/517 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： The invention is directed to a method of inhibiting FLT3 tyrosine kinase activity or expression or reducing FLT3 kinase activity or expression in a cell or a subject comprising the administration of a farnesyl transferase inhibitor and a FLT3 kinase inhibitor selected from alkylquinoline and alkylquinazoline compounds of Formula (I'): where R 1 , R 2 , R 3 , Z, G, Q and X are as defined herein. Included within the present invention is both prophylactic and therapeutic methods for treating a subject at risk of (or susceptible to) developing a cell proliferative disorder or a disorder related to FLT3.
摘要翻译：本发明涉及抑制FLT3酪氨酸激酶活性或在细胞或受试者中表达或降低FLT3激酶活性或表达的方法，其包括施用法呢基转移酶抑制剂和FLT3激酶抑制剂，所述法尼基转移酶抑制剂和FLT3激酶抑制剂选自烷基喹啉和烷基喹唑啉化合物（式 I'）：其中R 1，R 2，R 3，Z，G，Q和X如本文所定义。本发明包括预防和治疗方法，用于治疗患有（或易于）发展细胞增殖性病症或与FLT3相关的病症的受试者。

7. 发明申请

WO1996040772A2 AGONIST PEPTIDE DIMERS 审中-公开
标题翻译：激动剂二聚体
公开(公告)号：WO1996040772A2
公开(公告)日：1996-12-19
申请号：PCT/US1996009469
申请日：1996-06-06
申请人： ORTHO PHARMACEUTICAL CORPORATION , JOHNSON, Dana, L. , ZIVIN, Robert, A.
发明人： ORTHO PHARMACEUTICAL CORPORATION
IPC分类号： C07K14/505
CPC分类号： C07K14/505 , A61K38/00 , C07K1/1072
摘要： The present invention is directed to the dimerization of agonists and antagonists of cell surface receptors and particularly to peptide dimers which behave as cell surface receptor agonists in their dimeric form. Such receptors belong to the dimerization-mediated activation class often observed among receptors for growth and differentiation factors. The agonists of this class of receptors is understood to effect dimerization of the receptor and thus signal initiation. The present invention exemplifies dimers of erythropoietin (EPO) agonists and antagonists comprising a core amino acid sequence of X3X4X5GPX6TWX7X8 (SEQ ID NO: 1) wherein each amino acid is indicated by standard one letter abbreviation; X3 can be C, A, alpha -amino- gamma -bromobutyric acid or Hoc; X4 can be R, H, L or W; X5 can be M, F, or I; X6 is idependently selected from any one of the 20 genetically coded L-amino acids or the stereoisomeric D-amino acids; X7 can be D, E, I, L or V; and X8 can be C, A, alpha -amino- gamma -bromobutyric acid or Hoc, provided that either X3 or X8 is C or Hoc.
摘要翻译：本发明涉及细胞表面受体的激动剂和拮抗剂的二聚，特别涉及其二聚体形式的作为细胞表面受体激动剂的肽二聚体。这种受体属于通常在生长和分化因子的受体中观察到的二聚化介导的活化类型。这类受体的激动剂被理解为影响受体的二聚化，从而使信号起始。本发明例示了包含X3X4X5GPX6TWX7X8（SEQ ID NO：1）的核心氨基酸序列的促红细胞生成素（EPO）激动剂和拮抗剂的二聚体，其中每个氨基酸由标准单字母缩写表示; X3可以是C，A，α-氨基-γ-溴丁酸或Hoc; X4可以是R，H，L或W; X5可以是M，F或I; X6独立地选自20个遗传编码的L-氨基酸或立体异构体D-氨基酸中的任一个; X7可以是D，E，I，L或V; X 8可以是C，A，α-氨基-γ-溴丁酸或Hoc，条件是X 3或X 8为C或Hoc。

8. 发明申请

WO2010121046A1 4-AZETIDINYL-1-PHENYL-CYCLOHEXANE ANTAGONISTS OF CCR2 审中-公开
标题翻译： CCR2的4-亚苄基-1-苯基环己烷阴离子
公开(公告)号：WO2010121046A1
公开(公告)日：2010-10-21
申请号：PCT/US2010/031265
申请日：2010-04-15
申请人： JANSSEN PHARMACEUTICA NV , ZHANG, Xuqing , HUFNAGEL, Heather , HOU, Cuifen , JOHNSON, Dana L. , SUI, Zhihua
发明人： ZHANG, Xuqing , HUFNAGEL, Heather , HOU, Cuifen , JOHNSON, Dana L. , SUI, Zhihua
IPC分类号： C07D401/08 , C07D403/08 , C07D413/08 , C07D417/08 , A61K31/4427 , A61K31/437 , A61K31/433 , A61P3/10 , A61P29/00 , C07D205/04 , C07D403/10 , C07D405/08
CPC分类号： C07D205/04 , C07D403/08 , C07D403/10 , C07D405/08 , C07D413/08 , C07D417/08
摘要： The present invention comprises compounds of Formula (I) wherein: X, R 1 , R 2 , R 3 , and R 4 are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).
摘要翻译：本发明包括式（I）的化合物，其中：X，R 1，R 2，R 3和R 4如说明书中所定义。本发明还包括预防，治疗或改善综合征，病症或疾病的方法，其中所述综合征，病症或疾病是II型糖尿病，肥胖症和哮喘。本发明还包括通过施用治疗有效量的至少一种式（I）化合物来抑制哺乳动物CCR2活性的方法。

9. 发明申请

WO2010068663A1 4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANOL ANTAGONISTS OF CCR2 审中-公开
标题翻译： CCR2的4-AZETIDINYL-1-HETEROARYL-CYCLOHEXANOL ANTAGONISTS
公开(公告)号：WO2010068663A1
公开(公告)日：2010-06-17
申请号：PCT/US2009/067307
申请日：2009-12-09
申请人： JANSSEN PHARMACEUTICA NV , ZHANG, Xuqing , HUFNAGEL, Heather, Rae , HOU, Cuifen , JOHNSON, Dana, L. , SUI, Zhihua , FEGELY, Barry , BRESLIN, David
发明人： ZHANG, Xuqing , HUFNAGEL, Heather, Rae , HOU, Cuifen , JOHNSON, Dana, L. , SUI, Zhihua , FEGELY, Barry , BRESLIN, David
IPC分类号： C07D401/08 , C07D403/08 , C07D407/14 , C07D409/08 , C07D413/08 , C07D417/08 , C07D417/14 , A61K31/422 , A61K31/4178 , A61K31/4427 , A61K31/506 , A61P7/12
CPC分类号： C07D401/08 , C07D403/08 , C07D407/14 , C07D409/08 , C07D413/08 , C07D417/08 , C07D417/14
摘要： The present invention comprises compounds of Formula (I). wherein: R 1 , R 2 , R 3 , and R 4 are as defined in the specification. The invention also comprises pharmaceutical compositions comprising the compounds of formula (I) and methods of preventing, treating or ameliorating a CCR2 mediated syndrome, disorder or disease, for example, type II diabetes, obesity or asthma, by administering the compounds of formula (I).
摘要翻译：本发明包括式（I）的化合物。其中：R1，R2，R3和R4如说明书中所定义。本发明还包括药物组合物，其包含式（I）化合物和通过施用式（I）的化合物来预防，治疗或改善CCR2介导的综合征，病症或疾病，例如II型糖尿病，肥胖或哮喘的方法）。

10. 发明申请

WO2006076442A3 TRIAZOLOPYRIMIDINE DERIVATIVES 审中-公开
标题翻译：三唑并嘧啶衍生物
公开(公告)号：WO2006076442A3
公开(公告)日：2007-08-23
申请号：PCT/US2006000999
申请日：2006-01-11
申请人： JANSSEN PHARMACEUTICA NV , LUDOVICI DONALD W , CONNORS RICHARD W , COATS STEVEN J , LIU LI , DE CORTE BART L , JOHNSON DANA L , SCHULZ MARK J
发明人： LUDOVICI DONALD W , CONNORS RICHARD W , COATS STEVEN J , LIU LI , DE CORTE BART L , JOHNSON DANA L , SCHULZ MARK J
IPC分类号： C07K14/47 , C07K14/435
CPC分类号： C07K14/4738 , C07D487/04 , C12N9/1205 , C12Q1/485 , G01N2500/02
摘要： The invention relates to the discovery of triazolopyrimidine derivatives of formula (I), which have been found to exhibit inhibitory activity against the serine-tyrosine and tyrosine kinases.
摘要翻译：本发明涉及已发现对丝氨酸 - 酪氨酸和酪氨酸激酶具有抑制活性的式（I）三唑并嘧啶衍生物的发现。

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