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1. 发明授权

US06610684B2 Fused azepinone cyclin dependent kinase inhibitors 有权
标题翻译：融合氮杂环磷酸依赖性激酶抑制剂
公开(公告)号：US06610684B2
公开(公告)日：2003-08-26
申请号：US09739534
申请日：2000-12-14
申请人： Daniel W. Zaharevitz , Rick P. Gussio , Ravi K. Jalluri , Edward A. Sausville , Conrad Kunick , Laurent Meijer
发明人： Daniel W. Zaharevitz , Rick P. Gussio , Ravi K. Jalluri , Edward A. Sausville , Conrad Kunick , Laurent Meijer
IPC分类号： C07D48704
CPC分类号： C07D487/04 , C07D495/14
摘要： A new class of cyclin dependent kinase inhibitors that also have antiproliferative activity in human tumor cell line assays are described. Most of these compounds satisfy the formula wherein A is oxygen or sulfur coupled to the right by a single or double bond; R2 is selected from the group consisting of hydrogen, aryl, lower aliphatic substituents, particularly alkyl and lower alkyl ester; R4-R7 are independently selected from the group consisting of alkoxy, amino, acyl, aliphatic substituents, particularly alkyl, alkenyl and alkinyl substituents, aliphatic alcohols, particularly alkyl alcohols, aliphatic nitriles, particularly alkyl nitriles, cyano, nitro, carboxyl, halogen, hydrogen, hydroxyl, imino, and &agr;, &bgr;, unsaturated ketones; R8-R11 are independently selected from the group consisting of aliphatic substituents, particularly alkyl, alkenyl and alkinyl substituents, particularly lower aliphatic substituents, alipahatic alcohols, particularly alkyl alcohols, alkoxy, acyl, cyano, nitro, epoxy, haloalkyl groups, halogen, hydrogen and hydroxyl; R12 is selected from the group consisting of aliphatic groups, particularly lower alkyl groups, aliphatic alcohols, particularly alkyl alcohols, carboxylic acids and hydrogen. Compositions comprising effective amounts of such compounds also are described. These compounds and compositions can be used in a method for inhibiting the proliferation of living cells in a subject comprising administering an effective amount of the compound(s), or composition(s) comprising the compound(s), to a subject to inhibit the proliferation of living cells, such as neoplastic cells.
摘要翻译：描述了一类在人肿瘤细胞系测定中也具有抗增殖活性的细胞周期蛋白依赖性激酶抑制剂。这些化合物中的大多数满足甲醛，A是通过单键或双键向右连接的氧或硫; R2选自氢，芳基，低级脂族取代基，特别是烷基和低级烷基酯; R 4 -R 7独立地选自烷氧基，氨基，酰基，脂族取代基，特别是烷基，烯基和炔基取代基，脂族醇，特别是烷基醇，脂族腈，特别是烷基腈，氰基，硝基，羧基，卤素，氢，羟基，亚氨基和α，β，不饱和酮; R8-R11独立地选自脂族取代基，特别是烷基，烯基和炔基取代基，特别是低级脂族取代基，脂肪族醇，特别是烷基醇，烷氧基，酰基，氰基，硝基，环氧基，卤代烷基，卤素，氢和羟基; R 12选自脂族基团，特别是低级烷基，脂族醇，特别是烷基醇，羧酸和氢。还描述了包含有效量的这种化合物的组合物。这些化合物和组合物可用于抑制受试者中活细胞增殖的方法，包括向受试者施用有效量的化合物或包含该化合物的组合物以抑制受试者的抑制活细胞增殖，如肿瘤细胞。

2. 发明授权

US07605153B2 Use of paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells 失效
标题翻译：使用paullone衍生物生产用于治疗粘液性疾病的药物和与细胞中蛋白质寻址错误有关的疾病
公开(公告)号：US07605153B2
公开(公告)日：2009-10-20
申请号：US11786784
申请日：2007-04-12
申请人： Frédéric Becq , Laurent Meijer , Conrad Kunick
发明人： Frédéric Becq , Laurent Meijer , Conrad Kunick
IPC分类号： A61K31/55 , A61P11/00
CPC分类号： A61K31/55
摘要： The invention relates to paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivatives being of general formula (1): wherein X═C═O, C—S—CH3, C—S, —C—NHOH, Z—C or N, Y— with the adjacent ring, a phenyl or thienyl group, the ring(s) of said derivatives being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, —COM, —COOM, or —CH2COOM groups (where M=H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups) nitroso, or cyano, R5═H, or C1 to C5 alkyl and R12═H, or —C—CO2—(CH3)3 and the physiologically-acceptable salts and derivatives thereof.
摘要翻译：本发明涉及用于生产用于治疗粘液性疾病的药物的paullone衍生物和与细胞中的蛋白质寻址错误有关的疾病，所述衍生物为通式（1）：其中XCO，CS-CH3，CS，-C-NHOH， ZC或N，Y-与相邻的环，苯基或噻吩基，所述衍生物的环任选被一个或多个卤素原子取代，羟基，亚烷基羟基，亚炔基亚烷基羟基，炔羟基环己基，烷基，烷氧基，亚烷基烷氧基或亚烷基基团，其中亚烷基是饱和或不饱和的，该基团具有C1至C18的直链或支链，所述链任选被一个或多个羟基或氨基取代，或一个或多个三氟甲基-COM，-COOM 或-CH 2 COOM基团（其中M = H，C1至C18直链或支链烷基，任选被一个或多个羟基和/或氨基取代）亚硝基或氰基，R 5 -H或C 1至C 5烷基和R 12 - H或 - C-CO 2 - （CH 3）3及其生理学上可接受的盐和衍生物。

3. 发明申请

US20080076756A1 Use of paullone derivatives for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells 失效
标题翻译：使用paullone衍生物生产用于治疗粘液性疾病的药物和与细胞中蛋白质寻址错误有关的疾病
公开(公告)号：US20080076756A1
公开(公告)日：2008-03-27
申请号：US11786784
申请日：2007-04-12
申请人： Frederic Becq , Laurent Meijer , Conrad Kunick
发明人： Frederic Becq , Laurent Meijer , Conrad Kunick
IPC分类号： A61K31/55 , A61P11/00
CPC分类号： A61K31/55
摘要： The invention relates to paullone derivaties for the production of medicaments for the treatment of mucoviscidosis and diseases related to protein addressing errors in cells, said derivaties being of general formula (1): wherein X═C═O, C—S—CH3, C—S,—C—NHOH, Z═C or N, Y═with the adjacent ring, a phenyl or thiazolyl group, the ring(s) of said derivaties being optionally substituted with one or more halogen atoms, hydroxy, alkylenehydroxy, alkynealkylenehydroxy, alkynehydroxycyclohexyl, alkyl, alkoxy, alkylenealkoxy, or alkylenecyano groups where the alkylene group is either saturated or unsaturated, the groups having a straight or branched chain with C1 to C18, said chain being optionally substituted with one or more hydroxy or amino groups, or one or more trifluoromethyl, —COM, —COOM, or —CH2COOM groups (where M═H, C1 to C18 straight or branched chain alkyl, optionally substituted with one or more hydroxy and/or amino groups) nitroso, or cyano, R5═H, or C1 to C5 alkyl and R12═H, or —C—CO2—(CH3)3 and the physiologically-acceptable salts and derivatives thereof.
摘要翻译：本发明涉及用于生产用于治疗粘液性疾病的药物的paullone衍生物和与细胞中的蛋白质寻址错误有关的疾病，所述衍生物为通式（1）：其中XCO，CS-CH 3 ，CS，-C-NHOH，ZC或N，Y-与相邻的环，苯基或噻唑基，所述衍生物的环任选被一个或多个卤素原子取代，羟基，亚烷基羟基，亚炔基亚烷基羟基，炔基羟基环己基烷基，烷氧基，亚烷基烷氧基或亚烷基亚烷基，其中亚烷基是饱和或不饱和的，该基团具有C1至C18的直链或支链，所述链任选被一个或多个羟基或氨基取代，或一个或多个更多的三氟甲基，-COM，-COOM或-CH 2 COOM基团（其中MH，C1至C18直链或支链烷基，任选被一个或多个羟基和/或氨基取代）亚硝基，或氰基，R 5 -H或 C 1 -C 5烷基和R 12 -H或-C-CO 2 - （CH 3 3）3 - 及其生理上可接受的盐和衍生物。

4. 发明授权

US07232814B2 Use of paullone derivatives for making medicines 失效
标题翻译：使用paullone衍生物制造药物
公开(公告)号：US07232814B2
公开(公告)日：2007-06-19
申请号：US10203977
申请日：2001-02-15
申请人： Laurent Meijer , Conrad Kunick
发明人： Laurent Meijer , Conrad Kunick
IPC分类号： A61K31/55
CPC分类号： C07D487/04 , A61K31/55 , Y02A50/409 , Y02A50/411
摘要： The invention concerns the use for producing of GSK-3β inhibiting medicines from paullone derivatives. The invention is useful for treating pathologies involving GSK-3β and CDK5.
摘要翻译：本发明涉及用于从巴勒斯坦衍生物生产GSK-3β抑制药物的用途。本发明可用于治疗涉及GSK-3β和CDK5的病理学。

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