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    6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines
    4.
    发明授权
    6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines 失效
    6,9-二取代的2- [反 - （4-氨基环己基）氨基]嘌呤

    公开(公告)号：US06479487B1

    公开(公告)日：2002-11-12

    申请号：US09247053

    申请日：1999-02-09

    申请人： Jennifer A. Dumont ,  Alan J. Bitonti ,  David R. Borcherding ,  Norton P. Peet ,  H. Randall Munson, Jr. ,  Patrick W. Shum

    发明人： Jennifer A. Dumont ,  Alan J. Bitonti ,  David R. Borcherding ,  Norton P. Peet ,  H. Randall Munson, Jr. ,  Patrick W. Shum

    IPC分类号： C07D47316

    CPC分类号： C07D473/00

    摘要： The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or R3R4N—R5- wherein R2 is selected from the group consisting of C9-C12 alkyl, Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C1-C4 alkyl, and wherein each C9-C12 alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E, wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each E is independently selected from the group consisting of Hal, OH, and C1-C8 alkyl; R3 and R4 are selected from the group consisting of hydrogen, C1-C4 alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen; R5 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl, cyclopentenyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof, with the proviso that when R2 is the group wherein n is 1 or greater; R1 is isopropyl or cyclopentyl; R6 is hydrogen, C1-C4 alkyl, or (CH2)m-phenyl; and Z is phenyl, heterocycle, or cycloalkyl, that Z is substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of In addition, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.

    摘要翻译： 本发明提供新的式（I）化合物，其中R选自R2，R2NH-或R3R4N-R5-，其中R2选自C9-C12烷基，Z选自 的苯基，杂环，环烷基和萘烷; 并且M选自氢，C 1 -C 4烷基，并且其中每个C 9 -C 12烷基或Z任选被1至3个可以相同或不同的取代基取代，并且其选自 D，E，其中每个D独立地选自三氟甲基，三氟甲氧基和C 1 -C 4烷氧基; 每个E独立地选自Hal，OH和C 1 -C 8烷基; R 3和R 4选自氢，C 1 -C 4烷基和（CH 2）y - 苯基，其中y是整数0 -8，条件是R3和R4不都是氢; R5是C1-C8亚烷基; 并且R 1选自环戊基，环戊烯基和异丙基，以及其药学上可接受的盐，旋光异构体和水合物，条件是当R 2是n为1或更大的基团时; R1是异丙基或环戊基; R6是氢，C1-C4烷基或（CH2）m-苯基; Z是苯基，杂环或环烷基，Z被1至3个可以相同或不同的取代基取代，并且选自由以下组成的组。另外，本发明提供抑制细胞周期蛋白依赖性激酶的方法 ，特别是cdk-2。本发明还提供了一种预防神经元细胞凋亡的方法和抑制肿瘤发生的方法。

    6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines
    5.
    发明授权
    6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines 有权
    6,9-二取代的2- [反 - （4-氨基环己基）氨基]嘌呤

    公开(公告)号：US06413974B1

    公开(公告)日：2002-07-02

    申请号：US09247052

    申请日：1999-02-09

    申请人： Jennifer A. Dumont ,  Alan J. Bitonti ,  David R. Borcherding ,  Norton P. Peet ,  H. Randall Munson, Jr. ,  Patrick W. Shum

    发明人： Jennifer A. Dumont ,  Alan J. Bitonti ,  David R. Borcherding ,  Norton P. Peet ,  H. Randall Munson, Jr. ,  Patrick W. Shum

    IPC分类号： C07D47316

    CPC分类号： C07D473/00 ,  C07D473/16

    摘要： The present invention provides novel compounds of the formula (I) wherein R is selected from the group consisting of R2, R2NH—, or H2N—R3— wherein R2 is selected from the group consisting of C1-C8 alkyl and  wherein Z is selected from the group consisting of phenyl, heterocycle and cycloalkyl, each R4 is independently hydrogen or C1-C4 alkyl, and n is an integer 1-8; wherein each C1-C8 alkyl and Z is optionally substituted with 1 to 3 substituents, which may be the same or different, selected from the group consisting of Ha1, OH, and C1-C4 alkyl; R3 is C1-C8 alkylene; and R1 is selected from the group consisting of cyclopentyl and isopropyl, and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof. In addition, the present invention provides a method of inhibiting cell cycle progression. More specifically, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2. The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms. In addition, the present invention provides a composition comprising an assayable amount of a compound of Formula (I) in admixture or otherwise in association with an inert carrier. The present invention also provides a pharmaceutical composition comprising an effective inhibitory amount of a compound of Formula (I) in admixture or otherwise in association with one or more pharmaceutically acceptable carriers or excipients.

    摘要翻译： 本发明提供新的式（I）化合物，其中R选自R2，R2NH-或H2N-R3-，其中R2选自C1-C8烷基，其中Z选自 的苯基，杂环和环烷基，每个R 4独立地为氢或C 1 -C 4烷基，n为整数1-8;其中每个C 1 -C 8烷基和Z任选被1至3个取代基取代，所述取代基可以相同或 不同的，选自H 1，OH和C 1 -C 4烷基; R 3是C 1 -C 8亚烷基; 并且R 1选自环戊基和异丙基，以及其药学上可接受的盐，旋光异构体及其水合物。此外，本发明提供抑制细胞周期进程的方法。 更具体地，本发明提供抑制细胞周期蛋白依赖性激酶，特别是cdk-2的方法。本发明还提供了一种预防神经元细胞凋亡的方法和抑制肿瘤发展的方法。另外，本发明提供 包含可测定量的式（I）化合物与惰性载体混合或以其它方式与惰性载体结合的组合物。 本发明还提供包含有效抑制量的式（I）化合物与一种或多种药学上可接受的载体或赋形剂混合或以其它方式结合的药物组合物。

    PC5 as a factor IX propeptide processing enzyme
    7.
    发明授权
    PC5 as a factor IX propeptide processing enzyme 有权
    PC5作为因子IX前肽加工酶

    公开(公告)号：US07566565B2

    公开(公告)日：2009-07-28

    申请号：US11728045

    申请日：2007-03-23

    申请人： Robert T. Peters ,  Alan J. Bitonti

    发明人： Robert T. Peters ,  Alan J. Bitonti

    IPC分类号： C12N15/00 ,  C12N5/00

    CPC分类号： C12N9/644 ,  C07K2319/30 ,  C12N9/6454 ,  C12Y304/21022

    摘要： Compositions and methods for preparing Factor IX, Factor IX-containing fusion proteins, and Factor IX-containing conjugates with processing of Factor IX propeptide by PC5, are provided. In one embodiment PC5 is used to process a precursor polypeptide for a Factor IX-Fc monomer-dimer hybrid.

    摘要翻译： 提供了通过PC5处理因子IX前体肽制备因子IX，含因子IX的融合蛋白和含有因子IX的缀合物的组合物和方法。 在一个实施方案中，PC5用于处理因子IX-Fc单体 - 二聚体杂交体的前体多肽。

    Esters of castanospermine in the treatment of cerebral malaria
    9.
    发明授权
    Esters of castanospermine in the treatment of cerebral malaria 失效
    睾丸精胺治疗脑疟疾

    公开(公告)号：US5214050A

    公开(公告)日：1993-05-25

    申请号：US846656

    申请日：1992-03-05

    申请人： Alan J. Bitonti ,  Peter P. McCann ,  Albert Sjoerdsma

    发明人： Alan J. Bitonti ,  Peter P. McCann ,  Albert Sjoerdsma

    IPC分类号： A61K31/36 ,  A61K31/445

    CPC分类号： A61K31/445 ,  A61K31/36

    摘要： Red blood cells which are infected with the parasite P. falciparum cause the cells to become sticky and less deformable. This results in a build-up of cells on the vascular wall and creates occlusions to blood flow which are thought to cause the cerebral, renal and liver complications of P. falciparum infections. Certain esters of castanospermine prevent or reduce the adhesion of falciparum infected blood cells to the vascular endothelial wall and are a useful adjunct in the treatment of malaria.

    摘要翻译： 被恶性疟原虫感染的红细胞导致细胞变得粘稠且变形少。 这导致血管壁上的细胞积聚并且产生被认为引起恶性疟原虫感染的脑，肾和肝并发症的血流阻塞。 睾丸精胺的某些酯防止或减少恶性疟原虫感染的血细胞对血管内皮壁的粘附，并且是治疗疟疾的有用辅助物质。