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1. 发明申请

WO9900128A9 ANTITHROMBOTIC AGENTS 审中-公开
标题翻译：抗血栓药物
公开(公告)号：WO9900128A9
公开(公告)日：1999-08-05
申请号：PCT/US9813416
申请日：1998-06-26
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , CRAFT TRELIA JOYCE , FRANCISKOVICH JEFFRY BERNARD , GOODSON THEODORE JUNIOR , HALL STEVEN EDWARD , HERRON DAVID KENT , KLIMKOWSKI VALENTINE JOSEPH , KYLE JEFFREY ALAN , MASTERS JOHN JOSEPH , MENDEL DAVID , MILOT GUY , SAWYER JASON SCOTT , SHUMAN ROBERT THEODORE , SMITH GERALD FLOYD , TEBBE ANNE LOUISE , TINSLEY JENNIFER MARIE , WEIR LEONARD CRAYTON , WIKEL JAMES HOWARD , WILEY MICHAEL ROBERT , YEE YING KWONG
发明人： BEIGHT DOUGLAS WADE , CRAFT TRELIA JOYCE , FRANCISKOVICH JEFFRY BERNARD , GOODSON THEODORE JUNIOR , HALL STEVEN EDWARD , HERRON DAVID KENT , KLIMKOWSKI VALENTINE JOSEPH , KYLE JEFFREY ALAN , MASTERS JOHN JOSEPH , MENDEL DAVID , MILOT GUY , SAWYER JASON SCOTT , SHUMAN ROBERT THEODORE , SMITH GERALD FLOYD , TEBBE ANNE LOUISE , TINSLEY JENNIFER MARIE , WEIR LEONARD CRAYTON , WIKEL JAMES HOWARD , WILEY MICHAEL ROBERT , YEE YING KWONG
IPC分类号： C07D249/18 , A61K31/404 , A61K31/41 , A61K31/416 , A61K31/4184 , A61K31/454 , A61K31/4545 , A61P7/02 , A61P9/10 , C07D209/08 , C07D209/30 , C07D231/56 , C07D235/06 , C07D235/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D409/12 , A61K31/40 , A61K31/415 , A61K31/445 , A61K31/495 , A61K31/505 , C07D209/04 , C07D209/12 , C07D209/18 , C07D235/04 , C07D249/16
CPC分类号： C07D401/14 , C07D209/08 , C07D209/30 , C07D231/56 , C07D235/06 , C07D401/12 , C07D403/12 , C07D409/12
摘要： This application relates to a compound of formula (I) (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.
摘要翻译：本申请涉及如本文所定义的式（I）化合物（或其前药或其化合物或其前药的可药用盐），其药物组合物及其作为因子Xa抑制剂的用途，以及其制备方法及其中间体。

2. 发明申请

WO0144182A3 NEW SYNTHESIS OF SPLA2 INHIBITORS 审中-公开
标题翻译： SPLA2抑制剂的新合成
公开(公告)号：WO0144182A3
公开(公告)日：2002-03-07
申请号：PCT/US0032446
申请日：2000-12-11
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , SAWYER JASON SCOTT
发明人： BEIGHT DOUGLAS WADE , SAWYER JASON SCOTT
IPC分类号： C07D209/08 , C07C233/25 , C07C209/08 , C07C233/33
CPC分类号： C07D209/08 , Y02P20/55
摘要： A method of making a compound, comprises deprotecting a compound of formula (I), to form the compound of formula (II); where formula (I) isand, formula (II) isand where Rr is H, R10 or -C(O)R10; R2 is R20 -OR20, -SR20, -NR20R20'or -C(O)R20; R3, R4, R5, R6 and R7 are each individually H, halogen, R, -OR, -SR, -NRR', -C(O)R, -C(O)OR, -S(O)R or -S(O)2R; provided that at least one of R4 and R5 is not H; each R, R10 and R20 is individually alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; each R' and R20' is individually H, alkyl, alkenyl, alkynyl, aryl or heterocyclic radical; and P is a protecting group. The method provides an alternative route to indole-3-glyoxyamide compounds.
摘要翻译：制备化合物的方法包括使式（I）化合物脱保护，形成式（II）化合物; 式（I）和式（II）中Rr为H，R10或-C（O）R10; R2是R20 -OR20，-SR20，-NR20R20或-C（O）R20; R 3，R 4，R 5，R 6和R 7各自独立地为H，卤素，R，-OR，-SR，-NRR'， - C（O）R，-C（O）OR，-S（O） S（O）2; 条件是R 4和R 5中的至少一个不是H; 每个R，R 10和R 20分别是烷基，烯基，炔基，芳基或杂环基; 每个R'和R 20'独立地为H，烷基，烯基，炔基，芳基或杂环基; 而P是保护基。该方法提供了吲哚-3-乙酰氧基酰胺化合物的替代途径。

3. 发明申请

WO0250028A8 SUBSTITUTED BENZOINDOLES AS SPLA2 INHIBITORS 审中-公开
标题翻译：替代苯扎林作为SPLA2抑制剂
公开(公告)号：WO0250028A8
公开(公告)日：2005-03-17
申请号：PCT/US0143184
申请日：2001-12-06
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
发明人： BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
IPC分类号： A61K31/403 , A61P1/04 , A61P3/00 , A61P3/12 , A61P5/06 , A61P5/18 , A61P7/00 , A61P7/04 , A61P9/00 , A61P11/00 , A61P11/02 , A61P11/06 , A61P13/12 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/06 , A61P19/08 , A61P21/00 , A61P29/00 , A61P31/04 , A61P31/06 , A61P31/10 , A61P31/12 , A61P35/00 , A61P37/08 , A61P43/00 , C07D209/60 , C07D209/00 , A61K31/40
CPC分类号： C07D209/60
摘要： A novel class of benz[f]indole compounds see structure (I) is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of inflammatory diseases such as septic shock.
摘要翻译：公开了一类新的苯并[f]吲哚化合物结构（I）以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎性疾病如败血性休克的用途。

4. 发明申请

WO0250030A8 CYCLOALKYLFUSED [G]-INDOLE COMPOUNDS AS SPLA2-INHIBITORS IN THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译： CYCLOALKYLFUSED [G] -INDOLE化合物作为SPLA2抑制剂治疗炎症性疾病
公开(公告)号：WO0250030A8
公开(公告)日：2003-11-13
申请号：PCT/US0143187
申请日：2001-12-06
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
发明人： BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
IPC分类号： A61K31/403 , A61P1/00 , A61P1/18 , A61P11/02 , A61P11/06 , A61P11/08 , A61P17/02 , A61P19/02 , A61P29/00 , A61P31/04 , A61P43/00 , C07D209/60 , C07D209/70 , C07D409/10 , C07D209/42 , A61K31/40 , C07D209/12 , C07D209/14 , C07D209/22 , C07D209/30
CPC分类号： C07D209/70 , C07D209/60 , C07D409/10
摘要： A class of cycloalkylfused (g) indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
摘要翻译：公开了一类环烷基稠合（g）吲哚化合物以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎症性疾病如败血性休克的用途。

5. 发明申请

WO02057231A8 BENZ(G) INDOLES AND THEIR USE AS SPLA2 INHIBITORS 审中-公开
标题翻译： BENZ（G）INDOLES及其作为SPLA2抑制剂的用途
公开(公告)号：WO02057231A8
公开(公告)日：2003-11-13
申请号：PCT/US0143182
申请日：2001-12-06
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
发明人： BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
IPC分类号： A61K31/404 , A61P29/00 , A61P43/00 , C07D209/12 , C07D209/60 , A61K31/403
CPC分类号： C07D209/60
摘要： A novel class of benz[g]indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
摘要翻译：公开了一类新的苯并[g]吲哚化合物以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎症性疾病如脓毒性休克的用途。

6. 发明申请

WO0250029A8 TETRACYCLIC DERIVATIVES AS SPLA2 INHIBITORS 审中-公开
标题翻译：作为SPLA2抑制剂的四环衍生物
公开(公告)号：WO0250029A8
公开(公告)日：2003-11-13
申请号：PCT/US0143186
申请日：2001-12-06
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , JANDZINSKI JOHN DAVID , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT
发明人： BEIGHT DOUGLAS WADE , JANDZINSKI JOHN DAVID , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT
IPC分类号： A61K31/403 , A61P1/04 , A61P1/18 , A61P11/00 , A61P11/06 , A61P17/02 , A61P19/02 , A61P29/00 , A61P31/00 , A61P37/08 , A61P43/00 , C07D209/80 , C07D495/14 , A61K31/407
CPC分类号： C07D209/80 , C07D495/14
摘要： A novel class of tetracyclic compounds of formula (I) is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
摘要翻译：公开了新一类式（I）的四环化合物以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎性疾病如脓毒性休克的用途。

7. 发明申请

WO0212249A3 SUBSTITUTED PYRROLE COMPOUNDS AND THEIR USE AS SPLA2 INHIBITORS 审中-公开
标题翻译：取代的吡咯化合物及其作为SPLA2抑制剂的用途
公开(公告)号：WO0212249A3
公开(公告)日：2002-07-18
申请号：PCT/US0121106
申请日：2001-07-20
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , MORIN JOHN MICHAEL JUNIOR , SAWYER JASON SCOTT , SMITH EDWARD C R
发明人： BEIGHT DOUGLAS WADE , MORIN JOHN MICHAEL JUNIOR , SAWYER JASON SCOTT , SMITH EDWARD C R
IPC分类号： A61K31/407 , A61P1/04 , A61P1/18 , A61P11/00 , A61P11/06 , A61P11/08 , A61P19/02 , A61P19/06 , A61P27/16 , A61P29/00 , A61P31/04 , A61P37/08 , A61P43/00 , C07D495/04
CPC分类号： C07D495/04
摘要： A class of novel substituted pyrrole is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
摘要翻译：公开了一类新颖的取代吡咯以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎症性疾病如败血性休克的用途。

8. 发明申请

WO0134137A3 ONCOLYTIC COMBINATIONS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：恶性组合治疗癌症
公开(公告)号：WO0134137A3
公开(公告)日：2002-02-14
申请号：PCT/US0031039
申请日：2000-11-09
申请人： LILLY CO ELI , FLEISCH JEROME HERBERT , BENJAMIN ROGER STUART , SAWYER JASON SCOTT , TEICHER BEVERLY ANN , BEIGHT DOUGLAS WADE , SMITH EDWARD C R , MCMILLEN WILLIAM THOMAS
发明人： FLEISCH JEROME HERBERT , BENJAMIN ROGER STUART , SAWYER JASON SCOTT , TEICHER BEVERLY ANN , BEIGHT DOUGLAS WADE , SMITH EDWARD C R , MCMILLEN WILLIAM THOMAS
IPC分类号： A61K45/00 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/402 , A61K31/415 , A61K31/4164 , A61K31/4192 , A61K31/42 , A61K31/421 , A61K31/426 , A61K31/433 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K45/06 , A61P35/00 , A61P43/00
CPC分类号： A61K45/06 , A61K31/70
摘要： Leukotriene (LTB4) antagonists enhance the effectiveness of 2',2'-difluoronucleoside anti-cancer agents.
摘要翻译：白三烯（LTB4）拮抗剂增强2'，2'-二氟核苷抗癌剂的有效性。

9. 发明申请

WO0250034A3 TETRACYCLIC CARBAZOLE DERIVATES AND THEIR USE AS SPLA2 INHIBITORS 审中-公开
标题翻译：四环卡巴唑衍生物及其作为SPLA2抑制剂的用途
公开(公告)号：WO0250034A3
公开(公告)日：2003-01-16
申请号：PCT/US0143185
申请日：2001-12-06
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT
发明人： BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT
IPC分类号： A61K31/403 , A61P1/00 , A61P1/18 , A61P7/00 , A61P11/00 , A61P11/06 , A61P17/02 , A61P17/06 , A61P19/02 , A61P19/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D209/80 , C07D209/94 , A61K31/40
CPC分类号： C07D209/80 , C07D209/94
摘要： A novel class of tetracyclic compounds is disclosed represented by the formula (I), or a pharmaceutically acceptable salt, solvate, or prodrug derivative thereof; wherein; A is independently C, or N; n is 1, 2 or 3; together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
摘要翻译：公开了由式（I）表示的新一类四环化合物或其药学上可接受的盐，溶剂化物或前药衍生物; 其中; A独立地为C或N; n为1,2或3; 以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎性疾病如脓毒性休克的用途。

10. 发明申请

WO02057231A3 BENZ(G) INDOLES AND THEIR USE AS SPLA2 INHIBITORS 审中-公开
标题翻译： BENZ（G）吲哚及其作为SPLA2抑制剂的用途
公开(公告)号：WO02057231A3
公开(公告)日：2003-01-09
申请号：PCT/US0143182
申请日：2001-12-06
申请人： LILLY CO ELI , BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
发明人： BEIGHT DOUGLAS WADE , KINNICK MICHAEL DEAN , LIN HO-SHEN , MORIN JOHN MICHAEL JUNIOR , RICHETT MICHAEL ENRICO , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R
IPC分类号： A61K31/404 , A61P29/00 , A61P43/00 , C07D209/12 , C07D209/60 , A61K31/403
CPC分类号： C07D209/60
摘要： A novel class of benz[g]indole compounds is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of Inflammatory Diseases such as septic shock.
摘要翻译：公开了一类新颖的苯并[g]吲哚化合物以及这些化合物用于抑制sPLA2介导的脂肪酸释放以治疗炎症性疾病如败血性休克的用途。

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