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11 条记录 (耗时 0.032 秒)

    1.
    发明申请
    "Pyrazolo [4,3-d]pyrimidines, processes for their preparation and methods of use" 审中-公开
    “吡唑并[4,3-d]嘧啶，其制备方法和使用方法”

    公开(公告)号：US20070167466A1

    公开(公告)日：2007-07-19

    申请号：US10555528

    申请日：2004-05-06

    申请人： Daniela Moravcova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Pavla Binarova ,  Petr Mlejnek ,  Borek Vojtesek ,  Stjepan Uldrijan ,  Thomas Schmulling ,  Miroslav Strnad

    发明人： Daniela Moravcova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Pavla Binarova ,  Petr Mlejnek ,  Borek Vojtesek ,  Stjepan Uldrijan ,  Thomas Schmulling ,  Miroslav Strnad

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： The invention relates to 3-,7-disubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I (I), and pharmaceutically acceptable salts thereof, wherein R3 is selected from the group consisting of alkyl, cycloalkyl, cycloalkyl alkyl, cycloheteroalkyl alkyl, cycloheteroalkyl, aryl, heterocycle, heteroaryl, arylalkyl, heteroarylalkyl, and heteroalkyl, wherein each of the groups may optionally be substituted, R7 is selected from the group consisting of halogen, hydroxyl, hydroxylamino, amino, carboxyl, cyano, nitro, amido, sulfo, sulfamido, carbamino, unsubstituted or substituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted arylalkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted heteroarylalkyl, substituted or unsubstituted cycloalkyl alkyl, substituted or unsubstituted cycloheteroalkyl alkyl; R7′-X— wherein X is an —NH—, —N(alkyl)-, -0- or —S— moiety and R7′ is selected from the group consisting of H, alkyl, cycloalkyl, aryl, alkylcycloalkyl, arylalkyl, heterocycle, heterocyclealkyl, substituted alkyl, substituted cycloalkyl, substituted aryl, substituted arylalkyl, substituted heterocycle, substituted heteroaryl, substituted heteroarylalkyl, substituted heteroalkyl, substituted cycloalkyl alkyl and substituted cycloheteroalkyl alkyl, wherein the groups are preferably substituted by more than one halogen, hydroxyl, amino, mercapto, carboxyl, cyano, nitro, amido, sulfo, sulfamido, carbamino, alkyl, alkoxy, and substituted alkyl group.

    摘要翻译： 本发明涉及由通式I（I）表示的3-，7-二取代的吡唑并[4,3-d]嘧啶及其药学上可接受的盐，其中R 3选自烷基，环烷基，环烷基烷基 ，杂环烷基烷基，环杂烷基，芳基，杂环，杂芳基，芳基烷基，杂芳基烷基和杂烷基，其中每个基团可任选被取代，R 7选自卤素，羟基，羟基氨基，氨基，羧基，氰基，硝基 取代或未取代的芳烷基，取代或未取代的杂烷基，取代或未取代的杂芳基烷基，取代或未取代的环烷基烷基，取代或未取代的环杂烷基烷基;取代或未取代的芳基烷基， 其中X是-NH-，-N（烷基） - ， - O-或-S-部分，并且R 7'选自H，烷基，环烷基，芳基，烷基环烷基，芳基烷基， 杂环，杂环烷基，取代的烷基，取代的环烷基，取代的芳基，取代的芳基烷基，取代的杂环，取代的杂芳基，取代的杂芳基烷基，取代的杂烷基，取代的环烷基烷基和取代的环杂烷基烷基，其中基团优选被多于一个的卤素，羟基， 氨基，巯基，羧基，氰基，硝基，酰胺基，磺基，氨基磺酰氨基，氨基氨基，烷基，烷氧基和取代的烷基。

    Pyrazolo[4,3-D]pyrimidines, processes for their preparation and methods for therapy
    2.
    发明申请
    Pyrazolo[4,3-D]pyrimidines, processes for their preparation and methods for therapy 失效
    吡唑并[4,3-D]嘧啶，其制备方法和治疗方法

    公开(公告)号：US20050080097A1

    公开(公告)日：2005-04-14

    申请号：US10952087

    申请日：2004-09-28

    申请人： Daniela Moravcova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Miroslav Strnad

    发明人： Daniela Moravcova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Miroslav Strnad

    IPC分类号： A61K31/136 ,  A61K31/337 ,  A61K31/519 ,  A61K31/704 ,  A61K33/24 ,  A61P3/10 ,  A61P9/00 ,  A61P9/08 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P25/00 ,  A61P25/28 ,  A61P27/02 ,  A61P29/00 ,  A61P31/00 ,  A61P31/12 ,  A61P33/00 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  C07D487/02

    CPC分类号： C07D487/04

    摘要： The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I and pharmaceutically acceptable salts thereof, wherein R3 is an optionally substituted alkyl, cycloalkyl, cycloheteroalkyl, cycloalkyl alkyl, aryl or alkylaryl group; R5 is halogen, —NHNH2, —NHOH, NHCONH2, guanylo (NH—C(NH)NH2) an optionally substituted C1-C6 alkyl, alkenyl, alkinyl, C3-C15 cycloalkyl, Rf (C3-C15 cycloalkyl), heterocycle, heteroalkyl, aryl, heteroaryl, arylalkyl, cycloheteroalkyl, cycloheteroalkyl alkyl, heteroarylalkyl group, the group —C(O)—Ra, —C(O)NRbRc, —SO3Rd, or —NHC(O)Re, wherein Ra and Rf are an optionally substituted C1-C6 alkyl, alkenyl, or alkinyl group, Rb, Rc and Rd are independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, alkenyl, or alkinyl group, and Re is a hydroxy, amino, alkoxy, alkylamino, optionally substituted C1-C6 alkyl, alkenyl or alkinyl group; or the group —X—R5′, wherein X is —NH—, —O—, —S— or —N(alkyl)- and R5′ is hydrogen, an optionally substituted C1-C6 alkyl, alkenyl, alkinyl, C3-C15 cycloalkyl, Rf(C3-C15 cycloalkyl), aryl, heterocycle, hetero C1-C6 alkyl, arylalkyl, heteroaryl, cycloheteroalkyl, cycloheteroalkyl alkyl, or heteroarylalkyl group, the group —C(O)—Ra, —C(O)NRbRc, —SO3Rd, or —NHC(O)Re, wherein Ra, Rb, Rc, Rd, Re and Rf have the above meaning, and R7 is halogen, —NHNH2, NHOH, NHCONH2, guanylo (NH—C(NH)NH2) or the group —X—R7′, wherein X has the above meaning and the meaning of R7′ is as defined for R5′.

    摘要翻译： 本发明涉及由通式I表示的3-，5-，7-三取代的吡唑并[4,3-d]嘧啶及其药学上可接受的盐，其中R3是任选取代的烷基，环烷基，环杂烷基，环烷基烷基，芳基 或烷基芳基; R5是卤素，-NHNH2，-NHOH，NHCONH2，胍基（NH-C（NH）NH2），任选取代的C1-C6烷基，烯基，炔基，C3-C15环烷基，Rf（C3-C15环烷基），杂环，杂烷基 ，芳基，杂芳基，芳基烷基，环杂烷基，环杂烷基烷基，杂芳基烷基，基团-C（O）-Ra，-C（O）NRbRc，-SO3Rd或-NHC（O）Re，其中Ra和Rf是任选的 取代的C1-C6烷基，烯基或炔基，Rb，Rc和Rd独立地选自H，任选取代的C 1 -C 6烷基，烯基或炔基，Re是羟基，氨基，烷氧基， 烷基氨基，任选取代的C 1 -C 6烷基，烯基或炔基; 或基团-X-R5'，其中X是-NH-，-O - ， - S-或-N（烷基） - ，并且R 5'是氢，任选取代的C 1 -C 6烷基，烯基，炔基， C 15环烷基，R f（C 3 -C 15环烷基），芳基，杂环，杂C1-C6烷基，芳基烷基，杂芳基，环杂烷基，环杂烷基烷基或杂芳基烷基，基团-C（O）-Ra，-C（O）NRbRc ，-SO 3 R d或-NHC（O）R e，其中R a，R b，R c，R d，R e和R f具有上述含义，并且R 7是卤素，-NHNH 2，NHOH，NHCONH 2，胍基（NH-C（NH） ）或组-XR <高亮

    Azapurine derivatives
    3.
    发明申请
    Azapurine derivatives 失效
    阿氮嘌呤衍生物

    公开(公告)号：US20060035909A1

    公开(公告)日：2006-02-16

    申请号：US11051059

    申请日：2005-02-04

    申请人： Kveta Fuksova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Miroslav Strnad

    发明人： Kveta Fuksova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Miroslav Strnad

    IPC分类号： A61K31/519 ,  C07D487/02

    CPC分类号： C07D239/48 ,  C07D249/04 ,  C07D409/12 ,  C07D487/04

    摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof. The invention further relates to the use of said compounds in the treatment of hyperproliferative skin disorders, viral infections, cancer, rheumatoid arthritis, lupus, type I diabetes, multiple sclerosis, restenosis, polycystic kidney disease, graft rejection, graft versus host disease and gout, or for psoriasis, parasitoses such as those caused by fungi or protists, or Alzheimer's disease. Further aspects of the invention relate to the use of such compounds in the inhibition of cell proliferation, in the induction of apoptosis, to modulate the activity of adrenergic and/or purinergic receptors or to suppress immunostimulation. The invention also relates to the use of 2,6,9-trisubstituted 8-azapurines in maintaining mammalian ooctyes at the germinal vesicle stage.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸式盐。 本发明还涉及所述化合物在治疗过度增生性皮肤病，病毒感染，癌症，类风湿性关节炎，狼疮，I型糖尿病，多发性硬化，再狭窄，多囊肾病，移植排斥，移植物抗宿主病和痛风中的用途 ，或用于牛皮癣，诸如由真菌或原生生物引起的寄生虫或阿尔茨海默病。 本发明的其它方面涉及这些化合物在抑制细胞增殖，诱导凋亡中调节肾上腺素能和/或嘌呤能受体的活性或抑制免疫刺激的用途。 本发明还涉及2,6,9-三取代的8-氮杂嘌呤在维持生殖囊泡阶段的哺乳动物卵母的用途。

    Substituted [1,2,3] triazolo[4,5-D]pyrimidines as cdk inhibitors
    4.
    发明授权
    Substituted [1,2,3] triazolo[4,5-D]pyrimidines as cdk inhibitors 失效
    取代[1,2,3]三唑并[4,5-D]嘧啶，为cdk抑制剂

    公开(公告)号：US07816350B2

    公开(公告)日：2010-10-19

    申请号：US11051059

    申请日：2005-02-04

    申请人： Kveta Fuksova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Miroslav Strnad

    发明人： Kveta Fuksova ,  Libor Havlicek ,  Vladimir Krystof ,  Rene Lenobel ,  Miroslav Strnad

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/00 ,  A61P25/28 ,  A61P17/06 ,  A61P3/10 ,  A61P13/12 ,  A61P37/02 ,  A61P31/20 ,  A61P31/22

    CPC分类号： C07D239/48 ,  C07D249/04 ,  C07D409/12 ,  C07D487/04

    摘要： The present invention relates to a compound of formula I, or a pharmaceutically acceptable acid salt thereof. The invention further relates to the use of such compounds in the treatment of hyperproliferative skin disorders, viral infections, cancer, rheumatoid arthritis, lupus, type I diabetes, multiple sclerosis, restenosis, polycystic kidney disease, graft rejection, graft versus host disease and gout, or for psoriasis, parasitoses such as those caused by fungi or protists, or Alzheimer's disease.Further aspects of the invention relate to the use of such compounds in the inhibition of cell proliferation, in the induction of apoptosis, to modulate the activity of adrenergic and/or purinergic receptors or to suppress immunostimulation. The invention also relates to the use of 2,6,9-trisubstituted 8-azapurines in maintaining mammalian ooctyes at the germinal vesicle stage.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的酸式盐。 本发明还涉及这些化合物在治疗过度增生性皮肤病，病毒感染，癌症，类风湿性关节炎，狼疮，I型糖尿病，多发性硬化，再狭窄，多囊肾病，移植排斥，移植物抗宿主病和痛风中的用途 ，或用于牛皮癣，诸如由真菌或原生生物引起的寄生虫或阿尔茨海默病。 本发明的其它方面涉及这些化合物在抑制细胞增殖，诱导凋亡中调节肾上腺素能和/或嘌呤能受体的活性或抑制免疫刺激的用途。 本发明还涉及2,6,9-三取代的8-氮杂嘌呤在维持生殖囊泡阶段的哺乳动物卵母的用途。

    Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy
    9.
    发明授权
    Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy 失效

    公开(公告)号：US07745450B2

    公开(公告)日：2010-06-29

    申请号：US10952087

    申请日：2004-09-28

    申请人： Daniela Moravcová ,  Libor Havlicek ,  Vladimir Krystof ,  René Lenobel ,  Miroslav Strnad

    发明人： Daniela Moravcová ,  Libor Havlicek ,  Vladimir Krystof ,  René Lenobel ,  Miroslav Strnad

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P35/04 ,  A61P17/06 ,  A61P17/08 ,  A61P25/28 ,  A61P3/10 ,  A61P37/06

    CPC分类号： C07D487/04

    摘要： The invention relates to 3-, 5-, 7-trisubstituted pyrazolo[4,3-d]pyrimidines represented by the general formula I and pharmaceutically acceptable salts thereof, wherein R3 is an optionally substituted alkyl, cycloalkyl, cycloheteroalkyl, cycloalkyl alkyl, aryl or alkylaryl group; R5 is halogen, —NHNH2, —NHOH, NHCONH2, guanylo (NH—C(NH)NH2) an optionally substituted C1-C6 alkyl, alkenyl, alkynyl, C3-C15 cycloalkyl, Rf(C3-C15 cycloalkyl), heterocyclyl, heteroalkyl, aryl, heteroaryl, arylalkylene, arylalkenylene, arylalkynylene, cycloheteroalkyl, cycloheteroalkyl alkyl, heteroarylalkylene, heteroarylalkenylene, heteroarylalkynylene group, the group —C(O)—Ra, —C(O)NRbRc, —SO3Rd, or —NHC(O)Re, wherein Ra and Rf are an optionally substituted C1-C6 alkyl, alkenyl, or alkynyl group, Rb, Rc, and Rd are independently selected from the group consisting of H, optionally substituted C1-C6 alkyl, alkenyl, or alkynyl group, and Re is a hydroxy, amino, alkoxy, alkylamino, optionally substituted C1-C6 alkyl, alkenyl or alkynyl group; or the group —X—R5′, wherein X is —NH—, —O—, —S— or —N(alkyl)- and R5′ is hydrogen, an optionally substituted C1-C6 alkyl, alkenyl, alkynyl, C3-C15 cycloalkyl, Rf(C3-C15 cycloalkyl), aryl, heterocyclyl, hetero C1-C6 alkyl, arylalkylene, arylalkenylene, arylalkynylene, heteroaryl, cycloheteroalkyl, cycloheteroalkyl alkyl, or heteroarylalkylene, heteroarylalkenylene, heteroarylalkynylene group, the group —C(O)—Ra, —C(O)NRbRc, —SO3Rd, or —NHC(O)Re, wherein Ra, Rb, Rc, Rd, Re and Rf have the above meaning, and R7 is halogen, —NHNH2, NHOH, NHCONH2, guanylo (NH—C(NH)NH2) or the group —X—R7′, wherein X has the above meaning and the meaning of R7′ is as defined for R5′.

    4-arylazo-3,5-diamino-pyrazole compounds and use thereof
    10.
    发明授权
    4-arylazo-3,5-diamino-pyrazole compounds and use thereof 失效
    4-芳基偶氮-3,5-二氨基 - 吡唑化合物及其用途

    公开(公告)号：US08357673B2

    公开(公告)日：2013-01-22

    申请号：US11661003

    申请日：2005-09-01

    申请人： Petr Cankar ,  Iveta Frysova ,  Vladimir Krystof ,  Rene Lenobel ,  Jan Slouka ,  Miroslav Strnad ,  Peter Martin Fischer

    发明人： Petr Cankar ,  Iveta Frysova ,  Vladimir Krystof ,  Rene Lenobel ,  Jan Slouka ,  Miroslav Strnad ,  Peter Martin Fischer

    IPC分类号： A61K31/655 ,  A61P35/00 ,  A61P35/02 ,  C07D231/38 ,  C07D403/12

    CPC分类号： C07D231/38

    摘要： A series of mono- and binuclear 4-arylazo-3,5-diamino-pyrazoles which are useful for inhibition of cyclin-dependent kinases (preferably CDK9). Hence they can be used as antimitotic-, pro-apoptotic and antiinflammatory drugs, in particular, in chemotherapy of cancer and asthma, therapy of psoriasis and parasitoses as those caused by fungi or protists, treatment of Alzheimer's disease or as antineurodegenerative drugs, or to suppress immunostimulation. These compounds are useful in a variety of utilities, including as intermediates in the preparation of flame-retardants, diagnostic reagents and therapeutics, including antivirals and immunosuppressors.

    摘要翻译： 一系列用于抑制细胞周期蛋白依赖性激酶（优选CDK9）的单 - 和双核4-芳基偶氮-3,5-二氨基 - 吡唑。 因此，它们可以用作抗生素，促凋亡和抗炎药物，特别是癌症和哮喘的化疗，银屑病和寄生虫的治疗，如由真菌或原生生物引起的那些，阿尔茨海默病的治疗或抗神经退行性药物，或 抑制免疫刺激。 这些化合物可用于多种用途，包括作为制备阻燃剂，诊断试剂和治疗剂的中间体，包括抗病毒剂和免疫抑制剂。