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1. 发明申请

WO0238553A3 TRIAZOLE DERIVATIVES AND THEIR USE AS PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONISTS 审中-公开
标题翻译：三唑衍生物及其作为过氧化物酶促反应物激活的受体激动剂
公开(公告)号：WO0238553A3
公开(公告)日：2003-05-01
申请号：PCT/US0142928
申请日：2001-11-09
申请人： LILLY CO ELI , MANTLO NATHAN BRYAN , COLLADO CANO IVAN , DOMINIANNI SAMUEL JAMES , ETGEN GARRET JAY JUNIOR , GARCIA-PAREDES CRISTINA , JOHNSTON RICHARD DUANE , LETOURNEAU MICHAEL EDWARD , MARTINELLI MICHAEL JOHN , MAYHUGH DANIEL RAY , SAEED ASHRAF , THOMPSON RICHARD CRAIG , WANG XIADONG , COFFEY DAVID SCOTT , SCHMID CHRISTOPHER RANDALL , VICENZI JEFFREY THOMAS , XU YANPING
发明人： MANTLO NATHAN BRYAN , COLLADO CANO IVAN , DOMINIANNI SAMUEL JAMES , ETGEN GARRET JAY JUNIOR , GARCIA-PAREDES CRISTINA , JOHNSTON RICHARD DUANE , LETOURNEAU MICHAEL EDWARD , MARTINELLI MICHAEL JOHN , MAYHUGH DANIEL RAY , SAEED ASHRAF , THOMPSON RICHARD CRAIG , WANG XIADONG , COFFEY DAVID SCOTT , SCHMID CHRISTOPHER RANDALL , VICENZI JEFFREY THOMAS , XU YANPING
IPC分类号： A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P43/00 , C07C257/22 , C07C281/04 , C07C281/06 , C07D249/12 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , A61K31/427
CPC分类号： C07C281/06 , C07C257/22 , C07C281/04 , C07D249/12 , C07D401/06 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： he present invention is directed to compounds represented by the following structural formula (I'), and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.
摘要翻译：本发明涉及由以下结构式（I'）表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1是选自C 1 -C 8烷基，芳基-C 0-2 - 烷基，杂芳基-C 0-2 - 烷基，C 3 -C 6环烷基芳基-C 0-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 6环烷基和杂芳基的取代或未取代的基团。 X是C2-C5亚烷基连接体，连接体的一个碳原子可被O，NH或S取代.Y是C，O，S，NH或单键。此外，E是（CH 2）n COOH，其中n是0,1,2或3或C（R3）（R4）A，其中A是酸性官能团，例如羧基，羧酰胺取代或未取代的磺酰胺，或取代或未取代的四唑。 R3是H，饱和或不饱和的C1-C5烷基，C1-C5烷氧基。另外，R 4为H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 5烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4的基团，形成C 3 -C 4环烷基。

2. 发明申请

WO0116111A3 Hypoglycemic sulfonyl pyrazolones and pyrazolines 审中-公开
标题翻译：低血糖磺酰吡唑啉酮和吡唑啉
公开(公告)号：WO0116111A3
公开(公告)日：2001-08-23
申请号：PCT/US0020778
申请日：2000-08-16
申请人： DOMINIANNI SAMUEL JAMES , LILLY CO ELI
发明人： DOMINIANNI SAMUEL JAMES
IPC分类号： C07D231/28 , C07D413/12 , A61K31/4155 , A61P3/10
CPC分类号： C07D413/12 , C07D231/28
摘要： This invention provides compounds of formula (I) and their pharmaceutically acceptable salts, pharmaceutical formulations of said compounds, and methods for treating hyperglycemia associated with non-insulin dependent diabetes and for treating hyperlipidemia.

3. 发明公开

EP0789570A4 ORAL HYPOGLYCEMIC AGENTS 失效
标题翻译：口服降糖MEDIUM
公开(公告)号：EP0789570A4
公开(公告)日：1998-09-30
申请号：EP95937687
申请日：1995-10-31
申请人： LILLY CO ELI
发明人： DOMINIANNI SAMUEL JAMES , FITCH LORA LOUISE , SCHMIEGEL KLAUS KURT
IPC分类号： C07D413/12 , A61K31/41 , A61K31/42 , A61P3/08 , A61P3/10 , C07D413/10 , C07D417/10 , C07D417/12 , C07D419/12 , C07D263/30
CPC分类号： C07D413/10 , C07D417/10 , C07D417/12

5. 发明专利

ES2300378T3 AGONISTAS ALFA DE RECEPTORES ACTIVADOS POR PROLIFERADORES PEROXISOMALES. 未知
公开(公告)号：ES2300378T3
公开(公告)日：2008-06-16
申请号：ES01989704
申请日：2001-11-09
申请人： LILLY CO ELI
发明人： MANTLO NATHAN BRYAN , COLLADO CANO IVAN , DOMINIANNI SAMUEL JAMES , ETGEN GARRET JAY JUNIOR , GARCIA-PAREDES CRISTINA , JOHNSTON RICHARD DUANE
IPC分类号： C07D249/12 , A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/427 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P43/00 , C07C257/22 , C07C281/04 , C07C281/06 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： Un compuesto representado por la fórmula estructural I: (Ver fórmula) y las sales, los solvatos y los hidratos farmacéuticamente aceptables del mismo, en la que: (a) R1 se selecciona del grupo constituido por hidrógeno, un grupo sustituido o no sustituido seleccionado entre alquilo(C 1-C 8), aril-(alquilo(C 0-C 4)), heteroaril-(alquilo(C 0-C 4)), cicloalquilaril(C 3-C 6)- (alquilo(C 0-C 2)) y -CH2-C(O)-R17-R18, en la que R17 es O o NH, y R18 es bencilo opcionalmente sustituido; (b) W es O o S; (c) R2 es H o un grupo sustituido o no sustituido seleccionado del grupo constituido por alquilo(C1-C6), alilo (C1-C6), aril-(alquilo(C0-C4)), heteroaril-alquilo(C0-C4), sulfonamida, amida, OR10 y cicloalquilo(C3-C6); (d) X es un ligador de alquileno(C 2-C 5) opcionalmente sustituido, pudiendo estar un átomo de carbono del ligador reemplazado por O, NH o S; (e) Y es C, O, S, NH o un enlace simple; y (f) E se selecciona del grupo constituido por hidrógeno, C(R3)(R4)A, (CH2)nCOOR 19 , en el que el resto (CH2)n COOR 19 está sustituido o no está sustituido por uno a tres sustituyentes, cada uno de los cuales se selecciona independientemente del grupo constituido por alquilo(C 1-C 5), alcoxilo(C 1-C 5), haloalquilo(C 1-C 5), haloalcoxilo(C1-C5), nitro, ciano, CHO, hidroxilo, fenilo de ácido alcanoico(C1-C4), ariloxilo, SO2R7, SR7, benciloxilo, alquilcarboxamido y COOH, siendo R7 alquilo o haloalquilo, (Ver fórmula) y (Ver fórmula) en la que (i) n es 0, 1, 2 ó 3, (ii) A es un resto seleccionado del grupo constituido por carboxilo, alquilnitrilo(C1-C3), carboxamida, sulfonamida sustituida o no sustituida, acilsulfonamida sustituida o no sustituida y tetrazol sustituido o no sustituido; (iii) R3 es H, alquilo(C1-C5) saturado o insaturado, alcoxilo(C1-C5); (iv) R4 es H, halo, un grupo sustituido o no sustituido seleccionado entre alquilo(C1-C5), alcoxilo(C1-C5), cicloalquilo(C3-C6), aril (alquilo(C 0-C 4)) y fenilo, o R3 y R4 están combinados para formar un cicloalquilo(C 3-C 4); (v) R19 se selecciona del grupo constituido por hidrógeno, arilmetilo opcionalmente sustituido y alquilo (C1-C4) opcionalmente sustituido; (vi) R14 se selecciona del grupo constituido por CF3, fenilo sustituido o no sustituido, aril-(alquilo(C0- C4)) sustituido o no sustituido y alquilo(C1-C6); (g) R8 se selecciona independientemente del grupo constituido por hidrógeno, alquilo(C 1-C 4), alquilenilo(C 1- C4) y halo; (h) R9 se selecciona independientemente del grupo constituido por hidrógeno, alquilo(C 1-C 4), alquilenilo(C 1- C 4), halo, arilo sustituido o no sustituido, aril-(alquilo(C 1-C 4)) sustituido o no sustituido, heteroarilo sustituido o no sustituido, alilo(C1-C6) y OR10; y (i) R10 se selecciona independientemente del grupo constituido por hidrógeno y alquilo(C 1-C 4).

6. 发明专利

AU2002228592B2 Triazole derivatives and their use as peroxisome proliferator activated receptor alpha agonists 未知
公开(公告)号：AU2002228592B2
公开(公告)日：2006-04-27
申请号：AU2002228592
申请日：2001-11-09
申请人： LILLY CO ELI
发明人： MANTLO NATHAN BRYAN , JOHNSTON RICHARD DUANE , SAEED ASHRAF , CANO IVAN COLLADO , WANG XIADONG , MAYHUGH DANIEL RAY , VICENZI JEFFREY THOMAS , GARCIA-PAREDES CRISTINA , XU YANPING , DOMINIANNI SAMUEL JAMES , MARTINELLI MICHAEL JOHN , ETGEN GARRET JAY JUNIOR , SCHMID CHRISTOPHER RANDALL , TOURNEAU MICHAEL EDWARD LE , COFFEY DAVID SCOTT , THOMPSON RICHARD CRAIG
IPC分类号： C07D249/12 , A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P43/00 , C07C257/22 , C07C281/04 , C07C281/06 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12
摘要： A new and distinct hybrid of artichoke named ‘PS-H2015’, characterized by its numerous bud numbers, fleshiness of bracts, fleshiness of hearts, uniformity of head shapes; strong violet blush coloration; and ability to bolt in warm summer conditions (reduced vernalization requirements) allowing spring/summer planting and fall production.

7. 发明专利

ZA200302517B Peroxisome proliferator activated receptor alpha agonists. 未知
公开(公告)号：ZA200302517B
公开(公告)日：2004-06-30
申请号：ZA200302517
申请日：2003-03-31
申请人： LILLY CO ELI
发明人： MANTLO NATHAN BRYAN , DOMINIANNI SAMUEL JAMES , GARCIA-PAREDES CRISTINA , LETOURNEAU MICHAEL EDWARD , MAYHUGH DANIEL RAY , THOMPSON RICHARD CRAIG , COFFEY DAVID SCOTT , VICENZI JEFFREY THOMAS , CANO IVAN COLLADO , ETGEN GARRET JAY JUNIOR , JOHNSTON RICHARD DUANE , MARTINELLI MICHAEL JOHN , SAEED ASHRAF , WANG XIADONG , SCHMID CHRISTOPHER RANDALL , XU YANPING
IPC分类号： A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P43/00 , C07C257/22 , C07C281/04 , C07C281/06 , C07D249/12 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , A61K , C07C
摘要： A new and distinct hybrid of artichoke named ‘PS-H2015’, characterized by its numerous bud numbers, fleshiness of bracts, fleshiness of hearts, uniformity of head shapes; strong violet blush coloration; and ability to bolt in warm summer conditions (reduced vernalization requirements) allowing spring/summer planting and fall production.

8. 发明专利

NO20032059L 未知
公开(公告)号：NO20032059L
公开(公告)日：2003-06-24
申请号：NO20032059
申请日：2003-05-08
申请人： LILLY CO ELI
发明人： MANTLO NATHAN BRYAN , CANO IVAN COLLADO , DOMINIANNI SAMUEL JAMES , ETGEN JR GARRET JAY , GARCIA-PAREDES CRISTINA , JOHNSTON RICHARD DUANE , LETOURNEAU MICHAEL EDWARD , MARTINELLI MICHAEL JOHN , MAYHUGH DANIEL RAY , SAEED ASHRAF , THOMPSON RICHARD CRAIG , WANG XIADONG , COFFEY DAVID SCOTT , SCHMID CHRISTOPHER RANDALL , VICENZI JEFFREY THOMAS , XU YANPING
IPC分类号： A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P43/00 , C07C257/22 , C07C281/04 , C07C281/06 , C07D249/12 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , A61P9/10 , A61P9/12
摘要： A new and distinct hybrid of artichoke named ‘PS-H2015’, characterized by its numerous bud numbers, fleshiness of bracts, fleshiness of hearts, uniformity of head shapes; strong violet blush coloration; and ability to bolt in warm summer conditions (reduced vernalization requirements) allowing spring/summer planting and fall production.

9. 发明专利

CA2421154A1 PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR ALPHA AGONISTS 未知
公开(公告)号：CA2421154A1
公开(公告)日：2002-05-16
申请号：CA2421154
申请日：2001-11-09
申请人： LILLY CO ELI
发明人： SCHMID CHRISTOPHER RANDALL , COFFEY DAVID SCOTT , DOMINIANNI SAMUEL JAMES , ETGEN GARRET JAY JUNIOR , VICENZI JEFFREY THOMAS , GARCIA-PAREDES CRISTINA , COLLADO CANO IVAN , MANTLO NATHAN BRYAN , XU YANPING , WANG XIADONG , THOMPSON RICHARD CRAIG , MAYHUGH DANIEL RAY , SAEED ASHRAF , MARTINELLI MICHAEL JOHN , JOHNSTON RICHARD DUANE , LETOURNEAU MICHAEL EDWARD
IPC分类号： A61K31/4196 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/4709 , A61K31/5377 , A61P3/00 , A61P3/04 , A61P3/06 , A61P3/10 , A61P9/00 , A61P43/00 , C07C257/22 , C07C281/04 , C07C281/06 , C07D249/12 , C07D401/06 , C07D403/12 , C07D405/06 , C07D405/12 , C07D407/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/12 , A61K31/427
摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C 1- C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2- alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted grou p selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O , NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide , or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalky l, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

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