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1. 发明申请

WO0033839B1 NON-PEPTIDE ANTAGONISTS OF GLP-1 RECEPTOR AND METHODS OF USE 审中-公开
标题翻译： GLP-1受体的非肽拮抗剂及其使用方法
公开(公告)号：WO0033839B1
公开(公告)日：2000-09-28
申请号：PCT/US9929065
申请日：1999-12-08
申请人： AGOURON PHARMA , TRUESDALE LARRY KENNETH , BYCHOWSKI RICHARD A , GONZALEZ JAVIER , KUKI ATSUO , RAJAPAKSE RANJAN JAGATH , TENG MIN , KIEL DAN , DHANOA DALJIT S , HONG YUFENG , CHOU TSO SHENG , LING ANTHONY L , JOHNSON MICHAEL DAVID , GREGOR VLAD EDWARD
发明人： TRUESDALE LARRY KENNETH , BYCHOWSKI RICHARD A , GONZALEZ JAVIER , KUKI ATSUO , RAJAPAKSE RANJAN JAGATH , TENG MIN , KIEL DAN , DHANOA DALJIT S , HONG YUFENG , CHOU TSO-SHENG , LING ANTHONY L , JOHNSON MICHAEL DAVID , GREGOR VLAD EDWARD
IPC分类号： C07D491/147 , A61K31/437 , A61K31/519 , A61P5/48 , A61P43/00 , C07D471/04 , C07D471/10 , C07D471/14 , C07D491/04 , C07D491/14 , C07D521/00 , A61K31/4985 , A61K31/5377 , C07D237/00 , C07D413/14 , C07D471/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14
摘要： Non-peptide compounds that act as antagonists of the intestinal hormone glucagon-like peptide 1 (GLP-1) have a 9H- beta -carboline central motif. The compounds exhibit advantageous physical, chemical and biological properties and inhibit GLP-1 peptide binding to the GLP-1 receptor and/or prevent activation of the receptor by bound GLP-1. The invention further relates to a method of inhibiting the binding of GLP-1 to the GLP-1 receptor and a method of inhibiting the activation of the GLP-1 receptor. Intermediate compounds useful for making non-peptide GLP-1 receptor antagonists are also described.
摘要翻译：作为肠激素胰高血糖素样肽1（GLP-1）的拮抗剂的非肽化合物具有9H-β-咔啉中心基序。该化合物表现出有利的物理，化学和生物学特性，并且抑制GLP-1肽与GLP-1受体的结合和/或通过结合的GLP-1阻止受体活化。本发明还涉及抑制GLP-1与GLP-1受体结合的方法以及抑制GLP-1受体活化的方法。还描述了可用于制备非肽GLP-1受体拮抗剂的中间体化合物。

4. 发明申请

WO9901423A8 GLUCAGON ANTAGONISTS/INVERSE AGONISTS 审中-公开
标题翻译： GLUCAGON ANTAGONISTS / INVERSE AGONISTS
公开(公告)号：WO9901423A8
公开(公告)日：2001-05-17
申请号：PCT/DK9800287
申请日：1998-06-30
申请人： NOVO NORDISK AS , ALANEX CORP , LING ANTHONY , GREGOR VLAD , GONZALES JAVIER , HONG YUFENG , KIEL DAN , KUKI ATSUO , SHI SHENGHUA , NAERUM LARS , MADSEN PETER , SAMS CHRISTIAN , LAU JESPER , PLEWE MICHAEL BRUNO , FENG JUN , TENG MIN , JOHNSON MICHAEL DAVID , TESTON KIMBERLY ANN , SIDELMANN ULLA GROVE , KNUDSEN LOTTE BJERRE
发明人： LING ANTHONY , GREGOR VLAD , GONZALES JAVIER , HONG YUFENG , KIEL DAN , KUKI ATSUO , SHI SHENGHUA , NAERUM LARS , MADSEN PETER , SAMS CHRISTIAN , LAU JESPER , PLEWE MICHAEL BRUNO , FENG JUN , TENG MIN , JOHNSON MICHAEL DAVID , TESTON KIMBERLY ANN , SIDELMANN ULLA GROVE , KNUDSEN LOTTE BJERRE
IPC分类号： C07C251/86 , C07C255/29 , C07C309/65 , C07C311/49 , C07C317/28 , C07C323/45 , C07D209/48 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D231/12 , C07D295/185 , C07D307/12 , C07D307/52 , C07D309/06 , C07D317/58 , C07C243/18 , A61K31/15 , A61K31/40 , C07D209/04
CPC分类号： C07D209/48 , C07C251/86 , C07C255/29 , C07C309/65 , C07C311/49 , C07C317/28 , C07C323/45 , C07C2601/02 , C07C2601/14 , C07D209/86 , C07D213/30 , C07D213/80 , C07D215/12 , C07D231/12 , C07D295/185 , C07D307/12 , C07D307/52 , C07D309/06 , C07D317/58
摘要： Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof. The compounds act to antagonize the action of the glucagon peptide hormone.
摘要翻译：包含中心酰肼基序的非肽化合物及其合成方法。该化合物起拮抗胰高血糖素肽激素的作用。

5. 发明专利

JP2006348043A INDAZOLE AND USE THEREOF FOR INHIBITING PROTEIN KINASE 审中-公开
公开(公告)号：JP2006348043A
公开(公告)日：2006-12-28
申请号：JP2006232927
申请日：2006-08-30
申请人： AGOURON PHARMA
发明人： KANIA ROBERT STEVEN , BENDER STEVEN LEE , BORCHARDT ALLEN J , BRAGANZA JOHN F , CRIPPS STEPHAN JAMES , HUA YE , JOHNSON MICHAEL DAVID , JOHNSON THEODORE OTTO JR , LUU HIEP THE , PALMER CYNTHIA LOUISE , REICH SIEGFRIED HEINZ , TEMPCZYK-RUSSEL ANNA MARIA , TENG MIN , THOMAS CHRISTINE , VERNEY MICHAEL DAVID , WALLACE MICHAEL BRENNAN , COLLINS MICHAEL RAYMOND
IPC分类号： C07D231/56 , A61K31/416 , A61K31/4162 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P3/10 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D231/00 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D491/056
摘要： PROBLEM TO BE SOLVED: To provide a compound having protein kinase-inhibiting activities and useful as a therapeutic drug of malignant tumor. SOLUTION: The compound of the formula [wherein, R 1 is a substituted or nonsubstituted aryl, a heteroaryl, CH=CH-R 3 or CH=N-R 3 (R 3 is a substituted or nonsubstituted alkyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl); Y is O, S, C=CH 2 , C=O, S=O, SO 2 , CH 2 , CHCH 3 , NH or N-(1-8C alkyl); R 8 is a substituted or nonsubstituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl, heteroaryl, alkoxy or aryloxy; and R 10 is hydrogen, a halogen or a lower alkyl] is provided. COPYRIGHT: (C)2007,JPO&INPIT

6. 发明申请

WO0102369A3 Indazole compounds and pharmaceutical compositionsfor inhibiting protein kinases and methods for th eir use 审中-公开
标题翻译：吲唑化合物和用于抑制蛋白激酶的药物组合物及其用途
公开(公告)号：WO0102369A3
公开(公告)日：2002-04-25
申请号：PCT/US0018263
申请日：2000-06-30
申请人： AGOURON PHARMA
发明人： KANIA ROBERT STEVEN , BENDER STEVEN LEE , BORCHARDT ALLEN J , BRAGANZA JOHN F , CRIPPS STEPHAN JAMES , HUA YE , JOHNSON MICHAEL DAVID , JOHNSON THEODORE OTTO JR , LUU HIEP THE , PALMER CYNTHIA LOUISE , REICH SIEGFRIED HEINZ , TEMPCZYK-RUSSELL ANNA MARIA , TENG MIN , THOMAS CHRISTINE , VARNEY MICHAEL DAVID , WALLACE MICHAEL BRENNAN , COLLINS MICHAEL RAYMOND
IPC分类号： A61K31/416 , A61K31/4178 , A61K31/4184 , A61K31/4188 , A61K31/4196 , A61K31/4245 , A61K31/427 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61P3/10 , A61P9/10 , A61P17/06 , A61P19/02 , A61P27/02 , A61P27/06 , A61P29/00 , A61P35/00 , A61P43/00 , C07D209/18 , C07D231/00 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D491/056
CPC分类号： C07D403/12 , C07D209/18 , C07D231/56 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/12 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04
摘要： Indazole compounds that modulate and/or inhibit the activity of certain protein kinases are described. These compounds and pharmaceutical compositions containing them are capable of mediating tyrosine kinase signal transduction and thereby modulate and/or inhibit unwanted cell proliferation. The invention is also directed to the therapeutic or prophylactic use of pharmaceutical compositions containing such compounds, and to methods of treating cancer and other disease states associated with unwanted angiogenesis and/or cellular proliferation, such as diabetic retinopathy, neovascular glaucoma, rheumatoid arthritis, and psoriasis, by administering effective amounts of such compounds.

7. 发明公开

EP1137413A4 NON-PEPTIDE ANTAGONISTS OF GLP-1 RECEPTOR AND METHODS OF USE 有权
标题翻译：非肽类GLP-1受体拮抗剂和方法中使用的
公开(公告)号：EP1137413A4
公开(公告)日：2002-06-26
申请号：EP99960663
申请日：1999-12-08
申请人： AGOURON PHARMA
发明人： TRUESDALE LARRY KENNETH , BYCHOWSKI RICHARD A , GONZALEZ JAVIER , KUKI ATSUO , RAJAPAKSE RANJAN JAGATH , TENG MIN , KIEL DAN , DHANOA DALJIT S , HONG YUFENG , CHOU TSO-SHENG , LING ANTHONY L , JOHNSON MICHAEL DAVID , GREGOR VLAD EDWARD
IPC分类号： C07D491/147 , A61K31/437 , A61K31/519 , A61P5/48 , A61P43/00 , C07D471/04 , C07D471/10 , C07D471/14 , C07D491/04 , C07D491/14 , C07D521/00 , A61K31/435 , A61K31/4985 , A61K31/5377 , C07D237/00 , C07D413/14 , C07D471/12
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D471/04 , C07D471/14 , C07D491/04 , C07D491/14

8. 发明专利

CA2672472A1 MODULAR SPACECRAFT 未知
公开(公告)号：CA2672472A1
公开(公告)日：2008-12-04
申请号：CA2672472
申请日：2007-12-05
申请人： JOHNSON MICHAEL DAVID , HALL BARON KEITH
发明人： JOHNSON MICHAEL DAVID , HALL BARON KEITH
IPC分类号： B64G1/40 , B64G1/22
摘要： A modular spacecraft incorporating a launch vehicle interface design that also functions as a berthing or docking interface for the spacecraft. The v ehicle interface utilizes existing launch vehicle components to minimize cos t and time to flight. In addition, the spacecraft is constructed from off-th e- shelf launch vehicle components that enable a low cost construction as we ll as a secondary payload carrying functionality.

9. 发明专利

AU2007354271A1 Modular spacecraft 未知
公开(公告)号：AU2007354271A1
公开(公告)日：2008-12-04
申请号：AU2007354271
申请日：2007-12-05
申请人： HALL BARON KEITH , JOHNSON MICHAEL DAVID
发明人： JOHNSON MICHAEL DAVID , HALL BARON KEITH
IPC分类号： B64G1/40

10. 发明申请

WO2011126800A2 TWO-AXIS INCLINOMETER HEAD OF BED ELEVATION ALARM AND METHOD OF OPERATION 审中-公开
标题翻译：双轴高度报警的双轴测量头和操作方法
公开(公告)号：WO2011126800A2
公开(公告)日：2011-10-13
申请号：PCT/US2011030169
申请日：2011-03-28
申请人： EGRESSON LLC , JOHNSON MICHAEL DAVID , CLARK ROBERT LOUIS
发明人： JOHNSON MICHAEL DAVID , CLARK ROBERT LOUIS
IPC分类号： A61G7/018 , A61G7/00 , A61G7/012
CPC分类号： A61G7/018 , A61G7/05 , A61G2203/42
摘要： An apparatus used for reducing the incidence of aspiration in patients using a two-axis inclinometer is disclosed. The apparatus uses a two-axis inclinometer that is attached in the region of the patient's upper body to measure the absolute angular elevation of the patient's upper body, which is then transmitted to a display or other output device. In one embodiment, the instrument can be mounted to the head of a bed in a plurality of orientations and accurately measure the absolute angular elevation of the patient's upper body. In other embodiments the absolute angular elevation of the patient's upper body information is processed and transmitted to the nurses' station or to a data recorder. The disclosure also relates to a method for measuring the physical orientation of a patient, using such two-axis inclinometer apparatus.
摘要翻译：公开了一种用于减少使用双轴倾斜仪的患者吸入发生率的装置。该装置使用安装在患者上半身的区域中的双轴倾斜计，以测量患者上身的绝对角度高度，然后将其传送到显示器或其他输出装置。在一个实施例中，仪器可以以多个取向安装到床的头部并且精确地测量患者的上身的绝对角度高度。在其他实施例中，患者的上身信息的绝对角度仰角被处理并发送到护士站或数据记录器。本公开还涉及使用这种双轴倾斜仪装置来测量患者的物理方向的方法。

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