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1. 发明专利

AU780528B2 Fused azepinone cyclin dependent kinase inhibitors 未知
公开(公告)号：AU780528B2
公开(公告)日：2005-03-24
申请号：AU1500901
申请日：2001-01-16
申请人： US HEALTH , KUNICK CONRAD , CENTRE NAT RECH SCIENT
发明人： KUNICK CONRAD , MEIJER LAURENT , ZAHAREVITZ DANIEL W , GUSSIO RICK , JALLURI RAVI K , SAUSVILLE EDWARD A
IPC分类号： C07D487/04 , C07D495/14

2. 发明申请

WO2011042860A2 New derivatives of thieno[2,3-b]pyridine and 5,6,7,8-tetrahydrothieno[2,3-b]quinoline in particular useful in the treatment of malaria 审中-公开
标题翻译：噻吩并[2,3-b]吡啶和5,6,7,8-四氢噻吩并[2,3-b]喹啉的新衍生物特别可用于治疗疟疾
公开(公告)号：WO2011042860A2
公开(公告)日：2011-04-14
申请号：PCT/IB2010054496
申请日：2010-10-05
申请人： CENTRE NAT RECH SCIENT , MEIJER LAURENT , KUNICK CONRAD , BRANDT WIEBKE , DOERIG CHRISTIAN , TECH UNI CAROLO WILHELMINA ZU BRAUNSCHWEIG
发明人： MEIJER LAURENT , KUNICK CONRAD , BRANDT WIEBKE , DOERIG CHRISTIAN
IPC分类号： C07D495/04 , A61K31/4365 , A61K31/519 , A61P33/06 , C07D495/14
CPC分类号： C07D495/04 , C07D495/14
摘要： 51 ABSTRACT New derivatives of thieno[2,3-b]pyridine and 5,6,7,8-tetrahydrothieno[2,3-b]quinoline in 5 particular useful in the treatment of malaria The present invention is related to compounds of formula (I) N S R1 R2 R4 R3Ar AA' (I)10 in particular useful for the treatment of malaria, and to pharmaceutical compositions containing them.
摘要翻译： 51摘要特别可用于治疗疟疾的噻吩并[2,3-b]吡啶和5,6,7,8-四氢噻吩并[2,3-b]喹啉的新衍生物本发明涉及式（I）NS R1 R2 R4 R3Ar AA'（I）10特别可用于治疗疟疾，以及含有它们的药物组合物。

3. 发明专利

AU778735B2 Fused azepinone cyclin dependent kinase inhibitors 未知
公开(公告)号：AU778735B2
公开(公告)日：2004-12-16
申请号：AU4571499
申请日：1999-06-16
申请人： US GOV HEALTH & HUMAN SERV , KUNICK CONRAD , CENTRE NAT RECH SCIENT
发明人： KUNICK CONRAD , MEIJER LAURENT , ZAHAREVITZ DANIEL W , GUSSIO RICK , JALLURI RAVI K , SAUSVILLE EDWARD A
IPC分类号： A61K31/55 , A61P35/00 , A61P43/00 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , 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 formulawherein 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 alpha, beta, 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.

4. 发明专利

CA2335115C FUSED AZEPINONE CYCLIN DEPENDENT KINASE INHIBITORS 未知
公开(公告)号：CA2335115C
公开(公告)日：2009-01-27
申请号：CA2335115
申请日：1999-06-16
申请人： US GOV HEALTH & HUMAN SERV , KUNICK CONRAD , CENTRE NAT RECH SCIENT
发明人： SAUSVILLE EDWARD A , KUNICK CONRAD , GUSSIO RICK , JALLURI RAVI K , MEIJER LAURENT , ZAHAREVITZ DANIEL W
IPC分类号： C07D487/04 , A61K31/55 , A61P35/00 , A61P43/00 , C07D471/04 , C07D471/14 , C07D487/14 , 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 formula (1); 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, aliphati c alcohols, particularly alkyl alcohols, aliphatic nitriles, particularly alky l nitriles, cyano, nitro, carboxyl, halogen, hydrogen, hydroxyl, imino, and .alpha., .beta. unsaturated ketones; R8-R11 are independently selected from the group consisting of aliphatic substituents, particularly alkyl, alkenyl and alkinyl substituents, particularly lower aliphatic substituents, aliphatic 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 compoundsalso are described. These compounds and composition s 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 neoplasti c cells.

5. 发明专利

AU1500901A Fused azepinone cyclin dependent kinase inhibitors 未知
公开(公告)号：AU1500901A
公开(公告)日：2002-07-18
申请号：AU1500901
申请日：2001-01-16
申请人： CENTRE NAT RECH SCIENT , US GOV HEALTH & HUMAN SERV , KUNICK CONRAD
发明人： KUNICK CONRAD , MEIJER LAURENT , ZAHAREVITZ DANIEL W , GUSSIO RICK , JALLURI RAVI K , SAUSVILLE EDWARD A
IPC分类号： C07D487/04 , C07D495/14

6. 发明专利

CA2397560A1 UTILISATION DE DERIVES DE PAULLONES POUR LA FABRICATION DE MEDICAMENTS 未知
公开(公告)号：CA2397560A1
公开(公告)日：2001-08-23
申请号：CA2397560
申请日：2001-02-15
申请人： CENTRE NAT RECH SCIENT , KUNICK CONRAD
发明人： MEIJER LAURENT , KUNICK CONRAD
IPC分类号： A61K9/06 , A61K9/08 , A61K9/20 , A61K9/48 , A61K31/55 , A61P9/00 , A61P13/12 , A61P17/06 , A61P25/00 , A61P25/28 , A61P31/00 , A61P31/12 , A61P35/00 , A61P43/00 , C07D487/04 , C07D209/00 , C07D223/00
摘要： L'invention vise l'utilisation pour la fabrication de médicaments inhibiteur s de la GSK-3.beta. de dérivés de paullones. Application pour le traitement de pathologies impliquant GSK-3.beta. et CDK5.

7. 发明专利

AU4571499A Fused azepinone cyclin dependent kinase inhibitors 未知
公开(公告)号：AU4571499A
公开(公告)日：2000-01-05
申请号：AU4571499
申请日：1999-06-16
申请人： CENTRE NAT RECH SCIENT , US GOV HEALTH & HUMAN SERV , KUNICK CONRAD
发明人： KUNICK CONRAD , MEIJER LAURENT , ZAHAREVITZ DANIEL W , GUSSIO RICK , JALLURI RAVI K , SAUSVILLE EDWARD A
IPC分类号： A61K31/55 , A61P35/00 , A61P43/00 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , 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 formulawherein 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 alpha, beta, 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.

8. 发明申请

WO9965910A9 FUSED AZEPINONE CYCLIN DEPENDENT KINASE INHIBITORS 审中-公开
标题翻译：融合AZEPINONE CYCLIN依赖性激酶抑制剂
公开(公告)号：WO9965910A9
公开(公告)日：2000-03-16
申请号：PCT/US9913579
申请日：1999-06-16
申请人： US HEALTH , KUNICK CONRAD , MEIJER LAURENT , ZAHAREVITZ DANIEL W , GUSSIO RICK , JALLURI RAVI K , SAUSVILLE EDWARD A
发明人： KUNICK CONRAD , MEIJER LAURENT , ZAHAREVITZ DANIEL W , GUSSIO RICK , JALLURI RAVI K , SAUSVILLE EDWARD A
IPC分类号： A61K31/55 , A61P35/00 , A61P43/00 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D495/14
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 formula (I); wherein A is oxygen or sulfur coupled to the right by a single or double bond; R>2 4 7 8 11 12
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式（I）; 其中A是通过单键或双键偶联到右侧的氧或硫; R 2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; 特别是低级脂族取代基，脂族醇，特别是烷基醇，烷氧基，酰基，氰基，硝基，环氧基，环烷基，环烷基，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。

9. 发明专利

AT536184T 未知
公开(公告)号：AT536184T
公开(公告)日：2011-12-15
申请号：AT05809765
申请日：2005-10-14
申请人： CENTRE NAT RECH SCIENT , UNIV POITIERS
发明人： BECQ FREDERIC , MEIJER LAURENT , KUNICK CONRAD
IPC分类号： A61K31/55 , A61P11/12
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.

10. 发明专利

FR2876584B1 未知
公开(公告)号：FR2876584B1
公开(公告)日：2007-04-13
申请号：FR0410961
申请日：2004-10-15
申请人： CENTRE NAT RECH SCIENT CNRSE , UNIV POITIERS
发明人： BECQ FREDERIC , MEIJER LAURENT , KUNICK CONRAD
IPC分类号： A61K31/55 , A61P11/00 , A61P29/00
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.

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