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1. 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。

2. 发明申请

WO9926609A3 THERAPEUTIC TREATMENT FOR CHRONIC MYELOID LEUKEMIA AND ACUTE LYMPHOID LEUKEMIA 审中-公开
标题翻译：慢性髓性白血病和急性淋巴细胞白血病的治疗方法
公开(公告)号：WO9926609A3
公开(公告)日：1999-08-26
申请号：PCT/US9823908
申请日：1998-11-06
申请人： LILLY CO ELI , JIROUSEK MICHAEL R , WAYS DOUGLAS KIRK , BALLAS LAWRENCE M , STRAMM LAWRENCE E
发明人： JIROUSEK MICHAEL R , WAYS DOUGLAS KIRK , BALLAS LAWRENCE M , STRAMM LAWRENCE E
IPC分类号： A61K45/00 , A61K31/00 , A61K31/404 , A61K31/407 , A61P35/02 , A61P43/00 , A61K31/40
CPC分类号： A61K31/407 , A61K31/00
摘要： A method for treating neoplasms associated with an oncogenic form of ABL such as CML and ALL is disclosed, particularly using the isozyme selective PKC inhibitor, (S)-3,4-[N, N'-1,1'-((2'' -ethoxy)-3''' (O)-4'''-(N, N-dimethylamino) -butane)-bis-(3, 3'-indoly1)]-1 (H)-pyrrole-2, 5-dione and its pharmaceutically acceptable salts.
摘要翻译：公开了一种用于治疗与致癌形式的ABL如CML和ALL相关的肿瘤的方法，特别是使用同工酶选择性PKC抑制剂（S）-3,4- [N，N'-1,1' - （（2 “（O）-4” - （N，N-二甲基氨基） - 丁烷） - 双（3,3'-吲哚-1）] - 1（H） - 吡咯-2 ，5-二酮及其药学上可接受的盐。

3. 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。

4. 发明申请

WO1993003730A1 PROTEIN KINASE C INHIBITION AND NOVEL COMPOUND BALANOL 审中-公开
标题翻译：蛋白激酶C抑制剂和新型化合物巴拉醇
公开(公告)号：WO1993003730A1
公开(公告)日：1993-03-04
申请号：PCT/US1992007124
申请日：1992-08-21
申请人： SPHINX PHARMACEUTICALS CORPORATION , HALLOCK, Yali, F. , JANZEN, William, P. , BALLAS, Lawrence, M. , KULANTHIVEL, Palaniappan , BOROS, Christie
发明人： SPHINX PHARMACEUTICALS CORPORATION
IPC分类号： A61K31/55
CPC分类号： C07D223/12
摘要： Balanol, which is derived from fungi of the genus Verticillium, especially the fungus Verticillium balanoides, is provided. Balanol, when substantially pure, is soluble in dimethyl sulfoxide, water, and methanol; insoluble in ethyl acetate and chloroform; gives a positive color reaction with polymolybdic acid, ninhydrin reagent, and ferric chloride; is negative with Dragendorff's reagent and Iodoplatinate spray; has an Rf value of approximately 0.58 with silica gel thin layer chromatography with n-butanol/acetic acid/water at a ratio of 4:1:1 respectively; and has a molecular weight of approximately 550. Compounds of the invention are useful for inhibiting protein kinase C and treating conditions related to, or affected by inhibition of protein kinase C, particularly cancer tumors, inflammatory disease, reperfusion injury, and cardiac dysfunctions related to reperfusion injury.
摘要翻译：提供了来源于轮枝孢属真菌的Balanol，特别是真菌（Verticillium balanoides）。当基本上纯的时，巴拉醇可溶于二甲基亚砜，水和甲醇; 不溶于乙酸乙酯和氯仿; 与多钼酸，茚三酮试剂和氯化铁发生阳性显色反应; 对于Dragendorff的试剂和碘酸盐喷雾是阴性的; 分别使用正丁醇/乙酸/水分别为4:1:1的硅胶薄层色谱法，Rf值约为0.58。并且具有约550的分子量。本发明的化合物可用于抑制蛋白激酶C并且治疗与蛋白激酶C的抑制有关或受其抑制，特别是癌症肿瘤，炎症性疾病，再灌注损伤和与下列疾病相关的心脏功能障碍再灌注损伤。

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