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1.
公开(公告)号:WO2005108358A3
公开(公告)日:2006-05-26
申请号:PCT/US2005012191
申请日:2005-04-08
Applicant: LILLY CO ELI , DALLY ROBERT DEAN , SHEPHERD TIMOTHY ALAN , BENDER DAVID MICHAEL , ROJO GARCIA MARIA ISABEL
Inventor: DALLY ROBERT DEAN , SHEPHERD TIMOTHY ALAN , BENDER DAVID MICHAEL , ROJO GARCIA MARIA ISABEL
IPC: C07D401/12 , A61K31/401 , A61P25/00 , C07D207/08 , C07D207/12 , C07D209/52 , C07D211/22 , C07D217/12 , C07D217/16 , C07D241/08 , C07D403/12 , C07D413/04 , C07D413/14 , C07D453/06
CPC classification number: C07D413/04 , C07D207/08 , C07D207/12 , C07D211/26 , C07D211/42 , C07D217/18 , C07D241/04 , C07D241/08 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/14 , C07D417/12 , C07D471/08
Abstract: The present invention provides BACE inhibitors of Formula (I): methods for their use and preparation, and intermediates for their preparation.
Abstract translation: 本发明提供式(I)的BACE抑制剂:其用途和制备方法及其制备中间体。
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公开(公告)号:WO2006034093A2
公开(公告)日:2006-03-30
申请号:PCT/US2005033277
申请日:2005-09-20
Applicant: LILLY CO ELI , DURHAM TIMOTHY BARRETT , HAHN PATRIC JAMES , KOHN TODD JONATHAN , MCCARTHY JAMES RAY , BROUGHTON HOWARD BARFF , DALLY ROBERT DEAN , GONZALEZ-GARCIA MARIA ROSARIO , HENRY KENNETH JAMES JUNIOR , SHEPHERD TIMOTHY ALAN , ERICKSON JON ANDRE , BUENO-MELENDO ANA BELEN
Inventor: DURHAM TIMOTHY BARRETT , HAHN PATRIC JAMES , KOHN TODD JONATHAN , MCCARTHY JAMES RAY , BROUGHTON HOWARD BARFF , DALLY ROBERT DEAN , GONZALEZ-GARCIA MARIA ROSARIO , HENRY KENNETH JAMES JUNIOR , SHEPHERD TIMOTHY ALAN , ERICKSON JON ANDRE , BUENO-MELENDO ANA BELEN
CPC classification number: C07C271/20 , C07C233/36 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07C2603/74 , C07D265/30 , C07D265/32 , C07D413/12 , C07F7/1856
Abstract: The present invention provides BACE inhibitors of Formula (I); methods for their use and preparation, and intermediates useful for their preparation.
Abstract translation: 本发明提供式(I)的BACE抑制剂; 使用和制备方法,以及可用于制备的中间体。
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公开(公告)号:WO2005108391A1
公开(公告)日:2005-11-17
申请号:PCT/US2005/012189
申请日:2005-04-08
Applicant: ELI LILLY AND COMPANY , BUENO MELENDO, Ana, Belen , CHEN, Shu-Hui , ERICKSON, Jon, Andre , GONZALEZ-GARCIA, Maria, Rosario , GUO, Deqi , MARCOS LLORENTE, Alicia , MCCARTHY, James, Ray , SHEPHERD, Timothy, Alan , SHEEHAN, Scott, Martin , YIP, Yvonne, Yee Mai
Inventor: BUENO MELENDO, Ana, Belen , CHEN, Shu-Hui , ERICKSON, Jon, Andre , GONZALEZ-GARCIA, Maria, Rosario , GUO, Deqi , MARCOS LLORENTE, Alicia , MCCARTHY, James, Ray , SHEPHERD, Timothy, Alan , SHEEHAN, Scott, Martin , YIP, Yvonne, Yee Mai
IPC: C07D401/12
CPC classification number: C07D413/04 , C07D207/08 , C07D207/12 , C07D211/26 , C07D211/42 , C07D217/18 , C07D241/04 , C07D241/08 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/14 , C07D417/12 , C07D471/08
Abstract: The present invention provides BACE inhibitors of Formula (I): methods for their use, and intermediates and methods for their preparation.
Abstract translation: 本发明提供式(I)的BACE抑制剂:其用途及其制备方法。
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公开(公告)号:WO2005108358A2
公开(公告)日:2005-11-17
申请号:PCT/US2005/012191
申请日:2005-04-08
Applicant: ELI LILLY AND COMPANY , DALLY, Robert, Dean , SHEPHERD, Timothy, Alan , BENDER, David, Michael , ROJO GARCIA, Maria, Isabel
Inventor: DALLY, Robert, Dean , SHEPHERD, Timothy, Alan , BENDER, David, Michael , ROJO GARCIA, Maria, Isabel
IPC: C07D207/00
CPC classification number: C07D413/04 , C07D207/08 , C07D207/12 , C07D211/26 , C07D211/42 , C07D217/18 , C07D241/04 , C07D241/08 , C07D401/12 , C07D403/12 , C07D409/12 , C07D413/14 , C07D417/12 , C07D471/08
Abstract: The present invention provides BACE inhibitors of Formula (I): methods for their use and preparation, and intermediates for their preparation.
Abstract translation: 本发明提供式(I)的BACE抑制剂:其用途和制备方法及其制备中间体。
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公开(公告)号:WO2010056563A1
公开(公告)日:2010-05-20
申请号:PCT/US2009/063020
申请日:2009-11-03
Applicant: ELI LILLY AND COMPANY , DALLY, Robert, Dean , JOSEPH, Sajan , SHEPHERD, Timothy, Alan
Inventor: DALLY, Robert, Dean , JOSEPH, Sajan , SHEPHERD, Timothy, Alan
IPC: C07D473/00 , A61K31/52 , A61P35/00
CPC classification number: C07D487/04 , C07D473/34
Abstract: The present invention provides AKT and p70 S6 kinase inhibitors of Formula (I). The present invention also provides pharmaceutical compositions comprising compounds of Formula (I), uses of compounds of Formula (I) and methods of using compounds of Formula (I).
Abstract translation: 本发明提供式(I)的AKT和p70 S6激酶抑制剂。 本发明还提供包含式(I)化合物,式(I)化合物的用途和使用式(I)化合物的方法的药物组合物。
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6.BENZIMIDAZOLES AND BENZOTHIAZOLES AS INHIBITORS OF MAP KINASE 审中-公开
Title translation: 苯并咪唑和苯并噻唑作为MAP KINASE的抑制剂公开(公告)号:WO2004014900A1
公开(公告)日:2004-02-19
申请号:PCT/US2003/019890
申请日:2003-07-31
Applicant: ELI LILLY AND COMPANY , BONJOUKLIAN, Rosanne , DE DIEGO GOMEZ, Jose, Eugenio , DE DIOS, Alfonso , HAMDOUCHI, Chafiq, Hamdouchi , LI, Tiechao , LOPEZ DE URALDE GARMENDIA, Beatriz , VIETH, Michal , YORK, Jeremy, Schulenburg , DALLY, Robert, Dean , DEL PRADO CATALINA, Miriam, Filadelfa , JARAMILLO, Carlos , MARTIN CABREJAS, Luisa, Maria , MONTERO SALGADO, Carlos , PLEITE, Sheila , SANCHEZ-MARTINEZ, Concepcion , SHEPHERD, Timothy, Alan , WIKEL, James, Howard
Inventor: BONJOUKLIAN, Rosanne , DE DIEGO GOMEZ, Jose, Eugenio , DE DIOS, Alfonso , HAMDOUCHI, Chafiq, Hamdouchi , LI, Tiechao , LOPEZ DE URALDE GARMENDIA, Beatriz , VIETH, Michal , YORK, Jeremy, Schulenburg , DALLY, Robert, Dean , DEL PRADO CATALINA, Miriam, Filadelfa , JARAMILLO, Carlos , MARTIN CABREJAS, Luisa, Maria , MONTERO SALGADO, Carlos , PLEITE, Sheila , SANCHEZ-MARTINEZ, Concepcion , SHEPHERD, Timothy, Alan , WIKEL, James, Howard
IPC: C07D409/14
CPC classification number: C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , C07D513/04
Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl. The disclosed compounds inhibit p-38 kinase and are useful in the treatment of metastasis or rheumatoid arthritis.
Abstract translation: 本发明提供式I的激酶抑制剂:其中W代表由苯基或噻吩取代的咪唑,恶唑,吡唑,噻唑三唑。 所公开的化合物抑制p-38激酶,并且可用于治疗转移或类风湿性关节炎。
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公开(公告)号:WO0011023A3
公开(公告)日:2000-06-15
申请号:PCT/US9918908
申请日:1999-08-18
Applicant: LILLY CO ELI , BORROMEO PETER STANLEY , COHEN JEFFREY DANIEL , GREGORY GEORGE STUART , HENLE STACY KAY , HITCHCOCK STEPHEN ANDREW , JUNGHEIM LOUIS NICKOLAUS , MAYHUGH DANIEL RAY , SHEPHERD TIMOTHY ALAN , TURNER WILLIAM WILSON JR
Inventor: BORROMEO PETER STANLEY , COHEN JEFFREY DANIEL , GREGORY GEORGE STUART , HENLE STACY KAY , HITCHCOCK STEPHEN ANDREW , JUNGHEIM LOUIS NICKOLAUS , MAYHUGH DANIEL RAY , SHEPHERD TIMOTHY ALAN , TURNER WILLIAM WILSON JR
IPC: A61K9/08 , A61K9/72 , A61K38/00 , A61P31/10 , A61P33/00 , C07K1/06 , C07K7/50 , C07K7/54 , C07K7/56 , C07K7/64 , A61K38/12
Abstract: A method for modifying the cyclic peptide ring system of Echinocandin-type compounds to produce new analogs having antifungal activity is provided. The inventive process comprises opening the cyclic peptide ring, cleaving the terminal ornithine unit, inserting at least one new amino acid or other synthetic unit and closing the ring to produce a new cyclic peptide ring structure. The process allows one to incorporate features such as water-solubility into the cyclic peptide ring nucleus, sites for further modification, increase or decrease the number of amino acid or peptide units within the ring nucleus, and increase or decrease the total number of members within the ring. The invention further provides novel Echinocandin type compounds and their use as antifungal or anti-parasitic agents.
Abstract translation: 提供了用于修饰棘白菌素型化合物的环肽环体系以产生具有抗真菌活性的新型类似物的方法。 本发明的方法包括打开环肽环,切割末端鸟氨酸单元,插入至少一个新氨基酸或其他合成单元并闭合环以产生新的环肽环结构。 该方法允许将诸如水溶性的特征结合到环肽环核中,进一步修饰的位点,增加或减少环核内氨基酸或肽单元的数目,以及增加或减少环内肽的总数 戒指。 本发明还提供了新型棘白菌素类化合物及其作为抗真菌剂或抗寄生虫剂的用途。
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公开(公告)号:WO2005073205A1
公开(公告)日:2005-08-11
申请号:PCT/US2005/000021
申请日:2005-01-18
Applicant: ELI LILLY AND COMPANY , DALLY, Robert, Dean , DODGE, Jeffrey, Alan , HUMMEL, Conrad, Wilson , JONES, Scott, Alan , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan , WEBER, Wayne, Woodrow, II
Inventor: DALLY, Robert, Dean , DODGE, Jeffrey, Alan , HUMMEL, Conrad, Wilson , JONES, Scott, Alan , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan , WEBER, Wayne, Woodrow, II
IPC: C07D295/08
CPC classification number: C07D209/46 , C07D209/48 , C07D295/088 , C07D295/192 , C07D307/83 , C07D311/78 , C07D333/64 , C07D409/04
Abstract: The present invention relates to a selective estrogen receptor modulators of formula I (I); or a pharmaceutical acid addition salt thereof; and of formula II (II); or a pharmaceutical salt thereof; useful, e.g., for treating endometriosis and/or uterine leiomyoma/leiomyomata.
Abstract translation: 本发明涉及式I(I)的选择性雌激素受体调节剂; 或其药用酸加成盐; 和式II(II); 或其药学盐; 有用的,例如用于治疗子宫内膜异位症和/或子宫平滑肌瘤/平滑肌瘤。
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9.SELECTIVE ESTROGEN RECEPTOR MODULATORS FOR THE TREATMENT OF VASOMOTOR SYMPTOMS 审中-公开
Title translation: 用于治疗VASOMOTOR症状的选择性雌激素受体调节剂公开(公告)号:WO2005073204A1
公开(公告)日:2005-08-11
申请号:PCT/US2005/000020
申请日:2005-01-18
Applicant: ELI LILLY AND COMPANY , DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan
Inventor: DALLY, Robert, Dean , DODGE, Jeffrey, Alan , FRANK, Scott, Alan , HINKLIN, Ronald, Jay , SHEPHERD, Timothy, Alan , WALLACE, Owen, Brendan
IPC: C07D295/08
CPC classification number: C07D295/088 , C07D221/18 , C07D311/78 , C07D335/04
Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.
Abstract translation: 本发明涉及式I或Ia的选择性雌激素受体调节剂:(I)(Ia); 或其药用酸加成盐; 可用于治疗血管舒缩症状,特别是潮热,盗汗等影响更年期周围妇女的症状。
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公开(公告)号:WO2008140947A1
公开(公告)日:2008-11-20
申请号:PCT/US2008/062143
申请日:2008-05-01
Applicant: ELI LILLY AND COMPANY , DALLY, Robert, Dean , HUANG, Jianping , JOSEPH, Sajan , SHEPHERD, Timothy, Alan , HOLST, Christian L.
Inventor: DALLY, Robert, Dean , HUANG, Jianping , JOSEPH, Sajan , SHEPHERD, Timothy, Alan , HOLST, Christian L.
IPC: C07D487/04 , A61K31/437 , A61P35/00
CPC classification number: C07D487/04
Abstract: The present invention provides p70 S6 kinase inhibitors of the formula: pharmaceutical formulations comprising them, and methods for their use.
Abstract translation: 本发明提供了下式的P70 S6激酶抑制剂:包含它们的药物制剂,以及它们的使用方法。
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