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1. 发明专利

JPH11322745A SUBSTITUTED TRICYCLIC COMPOUND AND COMPOSITION CONTAINING THE SAME 失效
公开(公告)号：JPH11322745A
公开(公告)日：1999-11-24
申请号：JP10965699
申请日：1999-04-16
申请人： LILLY CO ELI
发明人： BACH NICHOLAS J , BASTIAN JOLIE ANNE , BEIGHT DOUGLAS W , KINNICK MICHAEL DEAN , MARTINELLI MICHAEL JOHN , MIHELICH EDWARD DAVID , MORIN JOHN MICHAEL JR , SALL DANIEL JON , SAWYER JASON SCOTT , SMITH EDWARD C R , SUAREZ TULIO , WANG QIUPING , WILSON THOMAS M
IPC分类号： C07D491/052 , A61K31/00 , A61K31/40 , A61K31/407 , A61K31/435 , A61K31/4353 , A61K31/4365 , A61K31/437 , A61P7/00 , A61P19/00 , A61P19/02 , A61P29/00 , A61P43/00 , C07D209/88 , C07D471/02 , C07D471/04 , C07D471/12 , C07D491/04 , C07D495/04 , C07D513/04 , C07D515/02
摘要： PROBLEM TO BE SOLVED: To obtain a substituted tricyclic compound capable of inhibiting the release of a fatty acid mediated by human pancreatic secretory phospholipase A2 , useful for general treatment of conditions of bacteremic shock, adult difficulty in breathing, pancreatitis, etc. SOLUTION: This compound is shown by formula I (A is phenyl or the like; one of B and D is N and the other is Carbon; Z is cyclohexenyl or the like; dotted line is a double bond or a single bond; R is a 5-20C alkyl, a carbon cyclic group or the like; R is a group substituted with a non-obstructing substituent group; R ' is NHNH2 , NH2 or the like; R ' is OH or the like; R ' is a non- obstructing substituent group or the like) or its pharmaceutically acceptable racemic modification or the like such as a compound of formula II. The compound of formula I (A is phenyl; the hetero atom of Z is S, O or N) is synthesized by alkylating a corresponding indole-3-acetic ester, converting the alkylated ester to an alcohol, then alkylating the compound, subjecting the resultant substance to ring formation, then converting the resulting substance into an amide and a phenol and finally into an acid.

2. 发明申请

WO0200641A3 SPLA2 INHIBITORS 审中-公开
标题翻译： SPLA2抑制剂
公开(公告)号：WO0200641A3
公开(公告)日：2002-08-29
申请号：PCT/US0114855
申请日：2001-06-14
申请人： LILLY CO ELI , KINNICK MICHAEL DEAN , LIN HO-SHEN , MARTINELLI MICHAEL JOHN , MORIN JOHN MICHAEL , RICHETT MICHAEL ENRICO
发明人： KINNICK MICHAEL DEAN , LIN HO-SHEN , MARTINELLI MICHAEL JOHN , MORIN JOHN MICHAEL , RICHETT MICHAEL ENRICO
IPC分类号： A61K31/381 , A61K38/00 , A61P29/00 , A61P43/00 , C07D333/60 , C07D333/62 , C07D333/64 , C07D333/66 , C07D333/70 , C07D333/00
CPC分类号： C07D333/62 , C07D333/60 , C07D333/64 , C07D333/66 , C07D333/70
摘要： A class of novel benzo(b)thiophene 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（b）噻吩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。

3. 发明申请

WO0034253A3 INTERMEDIATES AND REACTION SEQUENCE TO PRODUCE SAID INTERMEDIATES USEFUL FOR THE PREPARATION OF ANTINEOPLASTIC AND ANTIFUNGAL CRYPTOPHYCIN DERIVATIVES 审中-公开
标题翻译：产生中间体的中间体和反应序列可用于制备抗原和抗真菌蛋白衍生物
公开(公告)号：WO0034253A3
公开(公告)日：2000-11-16
申请号：PCT/US9928497
申请日：1999-12-02
申请人： LILLY CO ELI , UNIV HAWAII , UNIV WAYNE STATE
发明人： DHOKTE ULHAS PRABHAKAR , KHAU VIEN VAN , MARTINELLI MICHAEL JOHN
IPC分类号： C07D273/00 , C07D273/08 , C07D413/06 , C07F5/02 , C07F7/08
CPC分类号： C07D273/00 , Y02P20/55
摘要： A process for preparing a compound of the formula (I) wherein G is (C1-C12) alkyl, (C2-C12) alkenyl, (C2-C12) alkynyl, or Ar; Ar is an aromatic or heteroaromatic group or a substituted aromatic or heteroaromatic group; R is (C1-C6) alkyl; R is trityl or a suitable silyl protecting group; R is hydrogen or a suitable carboxy protecting group; and LG is a suitable hydroxy activating group; or a pharmaceutically acceptable salt thereof, useful in the preparation of cryptophycin derivatives. The processes involve an asymmetric crotylboration and, in the preferred embodiment, a subsequent asymmetric allylboration, providing for an efficient method for preparing Fragment A of the cryptophycin molecule. Also disclosed are novel intermediates useful for preparing cryptophycin compounds.
摘要翻译：制备式（I）化合物的方法，其中G为（C 1 -C 12）烷基，（C 2 -C 12）烯基，（C 2 -C 12）炔基或Ar; Ar是芳族或杂芳族基团或取代的芳族或杂芳族基团; R 3是（C 1 -C 6）烷基; R p1是三苯甲基或合适的甲硅烷基保护基; R p2是氢或合适的羧基保护基; LG是合适的羟基活化基团; 或其药学上可接受的盐，可用于制备隐球菌素衍生物。该方法涉及不对称的巴豆基底，并且在优选的实施方案中是随后的不对称烯丙基化，提供了制备密霉素分子的片段A的有效方法。还公开了可用于制备cryptophycin化合物的新型中间体。

4. 发明申请

WO02059108A8 MELANOCORTIN RECEPTOR AGONISTS 审中-公开
标题翻译：梅兰康汀受体激动剂
公开(公告)号：WO02059108A8
公开(公告)日：2003-11-06
申请号：PCT/US0200517
申请日：2002-01-23
申请人： LILLY CO ELI , BIGGERS CHRISTOPHER KELLY , BRINER KARIN , DOECKE CHRISTOPHER WILLIAM , FISHER MATTHEW JOSEPH , HERTEL LARRY WAYNE , MANCUSO VINCENT , MARTINELLI MICHAEL JOHN , MAYER JOHN PHILIP , ORNSTEIN PAUL LESLIE , RICHARDSON TIMOTHY IVO , SHAH JIKESH ARVIND , SHI QING , WU ZHIPEI , XIE CHAOYU
发明人： BIGGERS CHRISTOPHER KELLY , BRINER KARIN , DOECKE CHRISTOPHER WILLIAM , FISHER MATTHEW JOSEPH , HERTEL LARRY WAYNE , MANCUSO VINCENT , MARTINELLI MICHAEL JOHN , MAYER JOHN PHILIP , ORNSTEIN PAUL LESLIE , RICHARDSON TIMOTHY IVO , SHAH JIKESH ARVIND , SHI QING , WU ZHIPEI , XIE CHAOYU
IPC分类号： C07D217/12 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K38/00 , A61K45/00 , A61K45/06 , A61P3/00 , A61P3/04 , A61P3/10 , A61P15/00 , A61P15/08 , A61P15/10 , A61P43/00 , C07B61/00 , C07D209/18 , C07D209/44 , C07D217/14 , C07D217/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , A61K31/495 , A61K31/535 , A61K31/55 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14
CPC分类号： A61K45/06 , C07D209/44 , C07D217/14 , C07D217/26 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to melanocortin receptor agonists of formula (I), which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.
摘要翻译：本发明涉及式（I）的黑皮质素受体激动剂，其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍。

5. 发明申请

WO02059117A8 PIPERAZINE- AND PIPERIDINE-DERIVATIVES AS MELANOCORTIN RECEPTOR AGONISTS 审中-公开
标题翻译：哌拉西平和哌啶衍生物作为梅毒胆碱受体激动剂
公开(公告)号：WO02059117A8
公开(公告)日：2003-11-06
申请号：PCT/US0200515
申请日：2002-01-23
申请人： LILLY CO ELI , BRINER KARIN , DOECKE CHRISTOPHER WILLIAM , MANCUSO VINCENT , MARTINELLI MICHAEL JOHN , RICHARDSON TIMOTHY IVO , ROTHHAAR ROGER RYAN , SHI QING , XIE CHAOYU
发明人： BRINER KARIN , DOECKE CHRISTOPHER WILLIAM , MANCUSO VINCENT , MARTINELLI MICHAEL JOHN , RICHARDSON TIMOTHY IVO , ROTHHAAR ROGER RYAN , SHI QING , XIE CHAOYU
IPC分类号： C07D217/12 , A61K31/454 , A61K31/496 , A61K31/5377 , A61K31/5513 , A61K38/00 , A61K45/00 , A61K45/06 , A61P3/00 , A61P3/04 , A61P3/10 , A61P15/00 , A61P15/08 , A61P15/10 , A61P43/00 , C07B61/00 , C07D209/18 , C07D209/44 , C07D217/14 , C07D217/26 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D417/12 , C07D413/14 , A61K31/44 , A61K31/495
CPC分类号： A61K45/06 , C07D209/44 , C07D217/14 , C07D217/26 , C07D401/12 , C07D401/14 , C07D405/12 , C07D409/12 , C07D417/12
摘要： The present invention relates to melanocortin receptor agonists of formula I,which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.
摘要翻译：本发明涉及式I的黑皮质素受体激动剂，其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍。

6. 发明申请

WO02059107A8 SUBSTITUTED PIPERIDINES/PIPERAZINES AS MELANOCORTIN RECEPTOR AGONISTS 审中-公开
标题翻译：作为MELANOCORTIN受体激动剂的替代哌啶/哌嗪
公开(公告)号：WO02059107A8
公开(公告)日：2003-11-06
申请号：PCT/US0200516
申请日：2002-01-23
申请人： LILLY CO ELI , BACKER RYAN THOMAS , BRINER KARIN , DOECKE CHRISTOPHER WILLIAM , FISHER MATTHEW JOSEPH , KUKLISH STEVEN LEE , MANCUSO VINCENT , MARTINELLI MICHAEL JOHN , MULLANEY JEFFREY THOMAS , XIE CHAOYU
发明人： BACKER RYAN THOMAS , BRINER KARIN , DOECKE CHRISTOPHER WILLIAM , FISHER MATTHEW JOSEPH , KUKLISH STEVEN LEE , MANCUSO VINCENT , MARTINELLI MICHAEL JOHN , MULLANEY JEFFREY THOMAS , XIE CHAOYU
IPC分类号： A61K31/4725 , A61K31/496 , A61K31/5377 , A61P3/04 , A61P3/10 , A61P15/00 , A61P15/10 , C07B61/00 , C07D209/44 , C07D217/26 , C07D401/12 , C07D401/14 , A61K31/44 , A61K31/495
CPC分类号： C07D401/12 , C07D209/44 , C07D217/26 , C07D401/14
摘要： The present invention relates to melanocortin receptor agonists of formula I, which is useful in the treatment of obesity, diabetes and male and/or female sexual dysfunction.
摘要翻译：本发明涉及式I的黑皮质素受体激动剂，其可用于治疗肥胖症，糖尿病和男性和/或女性性功能障碍。

7. 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。

8. 发明申请

WO0034252A3 PROCESS FOR THE PREPARATION OF CRYPTOPHYCIN DERIVATIVES 审中-公开
标题翻译：制备喹喔啉衍生物的方法
公开(公告)号：WO0034252A3
公开(公告)日：2000-12-07
申请号：PCT/US9928496
申请日：1999-12-02
申请人： LILLY CO ELI , UNIV HAWAII , UNIV WAYNE STATE
发明人： DHOKTE ULHAS PRABHAKAR , KHAU VIEN VAN , MARTINELLI MICHAEL JOHN
IPC分类号： C07D273/00 , C07D413/06 , C07D273/08 , C07F7/18
CPC分类号： C07D273/00 , C07D413/06
摘要： Processes for the preparation of Cryptophycins of the formula (II), wherein G is (C1-C12) alkyl, (C2-C12) alkenyl, (C2-C12) alkynyl, or Ar; R is halogen and R is OH or glycinate ester; or R or R may be taken together to form an epoxide ring; or R or R may be taken together to form a bond; R is (C1-C6) alkyl; R and R are each independently hydrogen or (C1-C6) alkyl; or R and R , may be taken together to form a cyclopropyl or cyclobutyl ring; R is hydrogen, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, -(CH2)m-(C3-C5)cycloalkyl or benzyl; R , R is hydrogen or (C1-C6) alkyl; R is hydrogen, (C1-C6) alkyl, phenyl or benzyl; R is hydrogen or (=0); Y is CH, O, NR , S, SO, SO2, wherein R is hydrogen or (C1-C3) alkyl; R is (C1-C6) alkyl, substituted (C1-C6)alkyl, (C3-C8)cycloalkyl, substituted (C3-C8)cycloalkyl, a heteroaromatic or substituted heteroaromatic group or a group of formula (IA), (IB) OR (IC). The processes involve an asymmetric crotylboration and, in the preferred embodiment, a subsequent asymmetric allylboration, providing for an efficient method for preparing Fragment A of the Cryptophycin molecule.
摘要翻译：其中G为（C 1 -C 12）烷基，（C 2 -C 12）烯基，（C 2 -C 12）炔基或Ar的式（II）的半胱氨酸的制备方法; R 1是卤素，R 2是OH或甘氨酸酯; 或R 1或R 2可以一起形成环氧化物环; 或R 1或R 2可以一起形成键; R 3是（C 1 -C 6）烷基; R 7和R 8各自独立地为氢或（C 1 -C 6）烷基; 或R 7和R 8可以一起形成环丙基或环丁基环; R 9是氢，（C 1 -C 6）烷基，（C 2 -C 6）烯基，（C 2 -C 6）炔基， - （CH 2）m - （C 3 -C 5）环烷基或苄基; R 10，R 14是氢或（C 1 -C 6）烷基; R 11是氢，（C 1 -C 6）烷基，苯基或苄基; R 50为氢或（= O）; Y是CH，O，NR 12，S，SO，SO 2，其中R 12是氢或（C1-C3）烷基; R 6是（C 1 -C 6）烷基，取代的（C 1 -C 6）烷基，（C 3 -C 8）环烷基，取代的（C 3 -C 8）环烷基，杂芳族或取代的杂芳族基团或式（IA）（IB）或（IC）。该方法涉及不对称的巴豆基底，并且在优选的实施方案中为后续的不对称烯丙基化，提供了制备Cryptophycin分子的片段A的有效方法。

9. 发明公开

EP1091738A4 BICYCLIC sPLA 2 INHIBITORS 有权
标题翻译： BICYCLIC SPLA 2 HEMDERDERN
公开(公告)号：EP1091738A4
公开(公告)日：2003-03-05
申请号：EP99930602
申请日：1999-06-23
申请人： LILLY CO ELI
发明人： HUTCHISON DARRELL ROBERT , MARTINELLI MICHAEL JOHN , WILSON THOMAS MICHAEL
IPC分类号： A61K31/519 , A61K31/675 , A61P5/18 , A61P11/06 , A61P19/00 , A61P19/02 , A61P29/00 , A61P43/00 , C07D487/04 , C07F9/6561 , A61K31/505 , A61K31/535 , C07D413/12 , C07F9/02
CPC分类号： C07D487/04 , C07F9/6561

10. 发明公开

EP0799215A4 PROCESS FOR PREPARING BENZYL-SUBSTITUTED RHODANINE DERIVATIVES 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG冯BENZYL-SUBSTITUIERTEN罗丹丹衍生物
公开(公告)号：EP0799215A4
公开(公告)日：1998-03-11
申请号：EP95943829
申请日：1995-12-14
申请人： LILLY CO ELI
发明人： HANSEN MARVIN MARTIN , HARKNESS ALLEN ROBERT , KHAU VIEN VAN , MARTINELLI MICHAEL JOHN
IPC分类号： C07C323/56 , C07D277/14 , C07D277/34 , C07C321/06
CPC分类号： C07D277/14 , C07C323/56

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