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1. 发明申请

WO2008130879A2 TETRAHYDROINDOLE AND TETRAHYDROINDAZOLE DERIVATIVES 审中-公开
标题翻译：四氢吲哚和四氢吲哚衍生物
公开(公告)号：WO2008130879A2
公开(公告)日：2008-10-30
申请号：PCT/US2008/060173
申请日：2008-04-14
申请人： SERENEX, INC. , HUANG, Kenneth, He , OMMEN, Andy, J. , BARTA, Thomas, E. , HUGHES, Philip, F. , VEAL, James, M. , MA, Wei , SMITH, Emilie, D. , WOODWARD, Angela, R. , MCCALL, W., Stephen
发明人： HUANG, Kenneth, He , OMMEN, Andy, J. , BARTA, Thomas, E. , HUGHES, Philip, F. , VEAL, James, M. , MA, Wei , SMITH, Emilie, D. , WOODWARD, Angela, R. , MCCALL, W., Stephen
IPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14 , A61K31/416 , A61K31/4025 , A61K31/4178 , A61K31/4402 , A61K31/445 , A61P29/00 , A61P31/10 , A61P31/12 , A61P35/00
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14
摘要： The invention provides indole and indazole compounds of Formula (I) or pharmaceutically acceptable salts thereof which are useful for treating and/or preventing diseases and/or disorders ameliorated by the inhibition of Heat-Shock Protein 90. The invention further provides pharmaceutical compositions comprising compounds of Formula (I) and methods of preparing compounds of Formula (I).
摘要翻译：本发明提供了用于治疗和/或预防通过抑制热休克蛋白90而改善的疾病和/或病症的式（I）的吲哚和吲唑化合物或其药学上可接受的盐。本发明还提供了包含式（I）化合物的药物组合物和制备式（I）化合物的方法。

2. 发明申请

WO9420062A3 BALANOIDS 审中-公开
公开(公告)号：WO9420062A3
公开(公告)日：1996-08-15
申请号：PCT/US9402283
申请日：1994-03-02
申请人： NICHOLS GINA M & LF , SPHINX PHARMA CORP , HALL STEVEN EDWARD , BALLAS LAWRENCE M , KULANTHAIVEL PALANIAPPAN , BOROS CHRISTIE , JIANG JACK B , JAGDMANN GUNNAR ERIK JR , LAI YEN SHI , BIGGERS CHRISTOPHER K , HU HONG , HALLOCK YALI , HUGHES PHILIP F , DEFAUW JEAN MARIE , LYNCH MICHAEL PATRICK , LAMPE JOHN WILLIAM CROSSLEY , MENALDINO DAVID STEVEN , HEERDING JULIA MARIE , JANZEN WILLIAM P , HOLLINSHEAD SEAN PATRICK
发明人： HALL STEVEN EDWARD , BALLAS LAWRENCE M , KULANTHAIVEL PALANIAPPAN , BOROS CHRISTIE , JIANG JACK B , JAGDMANN GUNNAR ERIK JR , LAI YEN-SHI , BIGGERS CHRISTOPHER K , HU HONG , HALLOCK YALI , HUGHES PHILIP F , DEFAUW JEAN MARIE , LYNCH MICHAEL PATRICK , LAMPE JOHN WILLIAM CROSSLEY , MENALDINO DAVID STEVEN , HEERDING JULIA MARIE , JANZEN WILLIAM P , HOLLINSHEAD SEAN PATRICK , NICHOLS JEFFREY BAILEY
IPC分类号： C07D333/36 , A61K31/165 , A61K31/24 , A61K31/34 , A61K31/341 , A61K31/38 , A61K31/381 , A61K31/415 , A61K31/42 , A61K31/425 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/495 , A61K31/50 , A61K31/55 , A61P9/00 , A61P25/00 , A61P29/00 , A61P31/12 , A61P35/00 , A61P43/00 , C07C69/734 , C07C233/23 , C07C233/41 , C07C235/48 , C07C235/54 , C07C235/84 , C07C255/52 , C07C311/09 , C07C325/00 , C07D207/14 , C07D207/48 , C07D211/56 , C07D223/12 , C07D257/04 , C07D307/22 , C07D313/04 , C07D337/04 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07F9/572 , A61K
CPC分类号： C07D257/04 , C07C235/54 , C07C255/52 , C07C311/09 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D207/14 , C07D207/48 , C07D211/56 , C07D223/12 , C07D313/04 , C07D337/04 , C07D401/12 , C07D417/12 , C07F9/5721
摘要： A novel class of therapeutic compounds, denominated Balanoids, is disclosed. Balanoids have protein kinase C inhibitory activity and selectivity among the isoforms of protein kinase C. Balanoids are useful for treatment of diseases related to protein kinase C in animals, especially humans and is especially indicated for treatment of inflammatory diseases.
摘要翻译：公开了一类新型的治疗化合物，称为平衡物。平衡蛋白在蛋白激酶C的同种型中具有蛋白激酶C抑制活性和选择性。平衡物可用于治疗动物，特别是人类中与蛋白激酶C相关的疾病，并且特别用于治疗炎性疾病。

3. 发明申请

WO2008130879A3 TETRAHYDROINDOLE AND TETRAHYDROINDAZOLE DERIVATIVES 审中-公开
标题翻译：四氢吡喃衍生物和四氢吲哚衍生物
公开(公告)号：WO2008130879A3
公开(公告)日：2008-12-18
申请号：PCT/US2008060173
申请日：2008-04-14
申请人： SERENEX INC , HUANG KENNETH HE , OMMEN ANDY J , BARTA THOMAS E , HUGHES PHILIP F , VEAL JAMES M , MA WEI , SMITH EMILIE D , WOODWARD ANGELA R , MCCALL W STEPHEN
发明人： HUANG KENNETH HE , OMMEN ANDY J , BARTA THOMAS E , HUGHES PHILIP F , VEAL JAMES M , MA WEI , SMITH EMILIE D , WOODWARD ANGELA R , MCCALL W STEPHEN
IPC分类号： C07D231/56 , A61K31/4025 , A61K31/416 , A61K31/4178 , A61K31/4402 , A61K31/445 , A61P29/00 , A61P31/10 , A61P31/12 , A61P35/00 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14
CPC分类号： C07D231/56 , C07D401/12 , C07D403/12 , C07D405/12 , C07D405/14
摘要： The invention provides indole and indazole compounds of Formula (I) or pharmaceutically acceptable salts thereof which are useful for treating and/or preventing diseases and/or disorders ameliorated by the inhibition of Heat-Shock Protein 90. The invention further provides pharmaceutical compositions comprising compounds of Formula (I) and methods of preparing compounds of Formula (I).
摘要翻译：本发明提供了可用于治疗和/或预防通过抑制热休克蛋白90改善的疾病和/或障碍的式（I）的吲哚和吲唑化合物或其药学上可接受的盐。本发明还提供了包含化合物的式（I）化合物和式（I）化合物的制备方法。

4. 发明申请

WO1997026300A1 COMBINATORIAL PROCESS FOR PREPARING SUBSTITUTED INDANE LIBRARIES 审中-公开
标题翻译：用于准备取代的印度图书馆的组合过程
公开(公告)号：WO1997026300A1
公开(公告)日：1997-07-24
申请号：PCT/US1997001004
申请日：1997-01-22
申请人： ELI LILLY AND COMPANY , HOLLINSHEAD, Sean, P. , HUGHES, Philip, F. , MENDOZA, Jose, S. , MITCH, Charles, H. , WARD, John, S. , WILSON, Joseph, W.
发明人： ELI LILLY AND COMPANY
IPC分类号： C09B29/00
CPC分类号： C07D213/82 , C07C257/12 , C07C311/20 , C07C2602/08 , C07C2602/10 , C07D295/13 , C07D333/38 , C07D333/70 , C40B40/00
摘要： This invention relates to a novel solid phase process for the preparation of indane combinatorial librairies (1). These libraries have use for drug discovery and are used to form wellplate components (3) of novel assay kits, as illustrated in the figure.
摘要翻译：本发明涉及一种用于制备茚满组合文库的新型固相方法（1）。这些文库可用于药物发现，并用于形成新型测定试剂盒的孔板组分（3），如图所示。

5. 发明申请

WO1997025983A1 INDANE DERIVATIVES FOR ANTIPSYCHOTIC COMPOSITIONS 审中-公开
标题翻译：用于抗生素组合物的吲哚衍生物
公开(公告)号：WO1997025983A1
公开(公告)日：1997-07-24
申请号：PCT/US1997000997
申请日：1997-01-22
申请人： ELI LILLY AND COMPANY , HOLLINSHEAD, Sean, P. , HUFF, Bret, E. , HUGHES, Philip, F. , MENDOZA, Jose, S. , MITCH, Charles, H. , STASZAK, Michael, A. , WARD, John, S. , WILSON, Joseph, W.
发明人： ELI LILLY AND COMPANY
IPC分类号： A61K31/18
CPC分类号： C07D213/82 , C07C257/12 , C07C311/20 , C07C2602/08 , C07C2602/10 , C07D295/13 , C07D333/38 , C07D333/70 , C40B40/00
摘要： The present invention provides novel indane-like compounds which can be useful for treating psychosis and other conditions associated with the modulation of a muscarinic receptor. The invention provides formulations and methods for using the novel compounds.
摘要翻译：本发明提供了可用于治疗与调节毒蕈碱受体相关的精神病和其它病症的新型吲哚类化合物。本发明提供了使用新化合物的制剂和方法。

6. 发明申请

WO1994020062A2 BALANOIDS 审中-公开
公开(公告)号：WO1994020062A2
公开(公告)日：1994-09-15
申请号：PCT/US1994002283
申请日：1994-03-02
申请人： NICHOLS, Gina, M. +lf , SPHINX PHARMACEUTICALS CORPORATION , HALL, Steven, Edward , BALLAS, Lawrence, M. , KULANTHAIVEL, Palaniappan , BOROS, Christie , JIANG, Jack, B. , JAGDMANN, Gunnar, Erik, Jr. , LAI, Yen-Shi , BIGGERS, Christopher, K. , HU, Hong , HALLOCK, Yali , HUGHES, Philip, F. , DEFAUW, Jean, Marie , LYNCH, Michael, Patrick , LAMPE, John, William, Crossley , MENALDINO, David, Steven , HEERDING, Julia, Marie , JANZEN, William, P. , HOLLINSHEAD, Sean, Patrick
发明人： NICHOLS, Gina, M. +lf , SPHINX PHARMACEUTICALS CORPORATION , NICHOLS, Jeffrey, Bailey +di
IPC分类号： A61K00/00
CPC分类号： C07D257/04 , C07C235/54 , C07C255/52 , C07C311/09 , C07C2601/08 , C07C2601/14 , C07C2601/18 , C07D207/14 , C07D207/48 , C07D211/56 , C07D223/12 , C07D313/04 , C07D337/04 , C07D401/12 , C07D417/12 , C07F9/572
摘要： A novel class of therapeutic compounds, denominated Balanoids, is disclosed. Balanoids have protein kinase C inhibitory activity and selectivity among the isoforms of protein kinase C. Balanoids are useful for treatment of diseases related to protein kinase C in animals, especially humans and is especially indicated for treatment of inflammatory diseases.
摘要翻译：公开了一类新型的治疗化合物，称为平衡物。平衡蛋白在蛋白激酶C的同种型中具有蛋白激酶C抑制活性和选择性。平衡物可用于治疗动物，特别是人类中与蛋白激酶C相关的疾病，并且特别用于治疗炎性疾病。

7. 发明申请

WO1993020695A1 POLYHYDROXYLATED DIBENZ (C,E) AZEPINES AS PROTEIN KINASE C INHIBITORS 审中-公开
标题翻译：作为蛋白激酶C抑制剂的聚甲氧基二苯胺（C，E）
公开(公告)号：WO1993020695A1
公开(公告)日：1993-10-28
申请号：PCT/US1993000193
申请日：1993-01-11
申请人： SPHINX PHARMACEUTICALS CORPORATION , JIANG, Jack, B. , HUGHES, Philip, F.
发明人： SPHINX PHARMACEUTICALS CORPORATION
IPC分类号： A01N43/46
CPC分类号： C07D223/18
摘要： The invention provides compounds having formula (I) wherein: R1, R2, R3, R4, R5 and R6, independently, are H, halo, methoxy or hydroxyl, provided that at least one of R1, R2, R3, R4, R5 and R6 is hydroxyl, R7 and R8 are H or taken together form a carbonyl; R12 and R13 are H or taken together form a carbonyl; A is H or CR9R10R11; R9 and R10 are H or taken together form a carbonyl; R11 is H, C1 - C17 alkyl, C1 - C17 alkenyl, C1 - C17 alkynyl, or aryl; and, R14 and R15, independently are H, halo, methoxy or hydroxyl when at least 5 of R1 - R6 are hydroxyl, and H when less than 5 of R1 - R6 are hydroxyl. The compounds are useful for inhibiting protein kinase C, and treating conditions affected by protein kinase C activity, particularly cancer tumors, inflammatory disease, reperfusion injury and cardiac dysfunctions related to reperfusion injury.
摘要翻译：本发明提供具有式（I）的化合物，其中：R 1，R 2，R 3，R 4，R 5和R 6独立地是H，卤素，甲氧基或羟基，条件是R 1，R 2，R 3，R 4，R 5和 R6是羟基，R7和R8是H或一起形成羰基; R 12和R 13是H或一起形成羰基; A为H或CR9R10R11; R9和R10是H或一起形成羰基; R 11是H，C 1 -C 17烷基，C 1 -C 17烯基，C 1 -C 17炔基或芳基; 当R 1至R 5中的至少5个为羟基时，R 14和R 15独立地为H，卤素，甲氧基或羟基，当小于5的R 1 -R 6为羟基时，R 14和R 15独立地为H。这些化合物可用于抑制蛋白激酶C，以及治疗受蛋白激酶C活性，特别是癌症肿瘤，炎性疾病，再灌注损伤和与再灌注损伤相关的心脏功能障碍的影响。

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