专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明授权

US07429595B2 Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents 有权
标题翻译： 6,9-二取代的2-（反-1,4-二氨基环己基） - 嘌呤的酰基和磺酰基衍生物及其作为抗增殖剂的用途
公开(公告)号：US07429595B2
公开(公告)日：2008-09-30
申请号：US10677683
申请日：2003-10-02
申请人： David Borcherding , Jennifer A. Dumont , Norton P. Peet , Paul S. Wright
发明人： David Borcherding , Jennifer A. Dumont , Norton P. Peet , Paul S. Wright
IPC分类号： C07D473/16 , A61K31/52 , A61P35/00 , A61P35/02
CPC分类号： C07D473/16
摘要： The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4 -diaminocyclohexyl)-purines of the formula where Z is selected from the group consisting of —S(O)2—, and —C(O)—.
摘要翻译：本发明涉及下式的6,9-二取代的2-（反式-1,4-二氨基环己基） - 嘌呤的酰基和磺酰基衍生物，其中Z选自-S（O）2 - 和-C（O） - 。

2. 发明授权

US06861524B2 Acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines and their use as antiproliferative agents 有权
标题翻译： 6,9-二取代的2-（反-1,4-二氨基环己基） - 嘌呤的酰基和磺酰基衍生物及其作为抗增殖剂的用途
公开(公告)号：US06861524B2
公开(公告)日：2005-03-01
申请号：US09998976
申请日：2001-10-31
申请人： David Borcherding , Jennifer A. Dumont , Norton P. Peet , Paul S. Wright
发明人： David Borcherding , Jennifer A. Dumont , Norton P. Peet , Paul S. Wright
IPC分类号： A61P35/00 , A61P37/06 , C07D473/16 , A61K31/52
CPC分类号： C07D473/16
摘要： The present invention is directed to acyl and sulfonyl derivatives of 6,9-disubstituted 2-(trans-1,4-diaminocyclohexyl)-purines of the formula where Z is selected from the group consisting of —S(O)2—, and —C(O)—.
摘要翻译：本发明涉及式（Ⅳ）的6,9-二取代的2-（反-1,4-二氨基环己基） - 嘌呤的酰基和磺酰基衍生物，Z选自-S（O）2 - ， - C（O） - 。

3. 发明授权

US06642231B2 6,9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines 失效
标题翻译： 6,9-二取代的2- [反 - （4-氨基环己基）氨基]嘌呤
公开(公告)号：US06642231B2
公开(公告)日：2003-11-04
申请号：US10178494
申请日：2002-06-24
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 comprises 6-9-Disubstituted 2-[trans-(4-aminocyclohexyl]aminopurines that are useful in 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：本发明包括可用于抑制细胞周期蛋白依赖性激酶，特别是cdk-2的6-9-二取代的2- [反 - （4-氨基环己基）氨基嘌呤，本发明还提供了一种预防神经元细胞凋亡的方法和方法抑制肿瘤的发展。

4. 发明授权

US06413974B1 6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines 有权
标题翻译： 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。

5. 发明授权

US06479487B1 6, 9-disubstituted 2-[trans-(4-aminocyclohexyl)amino] purines 失效
标题翻译： 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. 发明申请

US20130108629A1 Factor VIII-Fc Chimeric and Hybrid Polypeptides, and Methods of Use Thereof 有权
标题翻译：因子VIII-Fc嵌合和杂交多肽及其使用方法
公开(公告)号：US20130108629A1
公开(公告)日：2013-05-02
申请号：US13513424
申请日：2010-12-06
申请人： Jennifer A. Dumont , Susan Low , Alan J. Bitonti , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron McKinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
发明人： Jennifer A. Dumont , Susan Low , Alan J. Bitonti , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron McKinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
IPC分类号： C07K14/755 , C07K16/46
CPC分类号： A61K38/37 , A61K47/643 , A61K47/6811 , C07K14/755 , C07K16/46 , C07K2319/30
摘要： The present invention provides methods of administering Factor VIII; methods of administering chimeric and hybrid polypeptides comprising Factor VIII; chimeric and hybrid polypeptides comprising Factor VIII; polynucleotides encoding such chimeric and hybrid polypeptides; cells comprising such polynucleotides; and methods of producing such chimeric and hybrid polypeptides using such cells.
摘要翻译：本发明提供了施用因子VIII的方法; 包含因子VIII的嵌合和杂交多肽的施用方法; 包含因子VIII的嵌合和杂合多肽; 编码这种嵌合和杂交多肽的多核苷酸; 包含这种多核苷酸的细胞; 以及使用这种细胞产生这种嵌合和杂合多肽的方法。

7. 发明授权

US09050318B2 Factor VIII-Fc chimeric and hybrid polypeptides, and methods of use thereof 有权
标题翻译：因子VIII-Fc嵌合和杂交多肽及其使用方法
公开(公告)号：US09050318B2
公开(公告)日：2015-06-09
申请号：US13513424
申请日：2010-12-06
申请人： Jennifer A. Dumont , Susan Low , Alan J. Bitonti , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron McKinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
发明人： Jennifer A. Dumont , Susan Low , Alan J. Bitonti , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron McKinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
IPC分类号： A61K39/395 , A61K38/37 , A61K47/48 , C07K14/755 , C07K16/46
CPC分类号： A61K38/37 , A61K47/643 , A61K47/6811 , C07K14/755 , C07K16/46 , C07K2319/30
摘要： The present invention provides methods of administering Factor VIII; methods of administering chimeric and hybrid polypeptides comprising Factor VIII; chimeric and hybrid polypeptides comprising Factor VIII; polynucleotides encoding such chimeric and hybrid polypeptides; cells comprising such polynucleotides; and methods of producing such chimeric and hybrid polypeptides using such cells.
摘要翻译：本发明提供了施用因子VIII的方法; 包含因子VIII的嵌合和杂交多肽的施用方法; 包含因子VIII的嵌合和杂合多肽; 编码这种嵌合和杂交多肽的多核苷酸; 包含这种多核苷酸的细胞; 以及使用这种细胞产生这种嵌合和杂合多肽的方法。

8. 发明申请

US20140294821A1 FACTOR VIII CHIMERIC AND HYBRID POLYPEPTIDES, AND METHODS OF USE THEREOF 有权
标题翻译：因子VIII二元和混合多聚物及其使用方法
公开(公告)号：US20140294821A1
公开(公告)日：2014-10-02
申请号：US14131600
申请日：2012-07-06
申请人： Jennifer A. Dumont , Susan Low , Alan J. Bitonti , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron Mckinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
发明人： Jennifer A. Dumont , Susan Low , Alan J. Bitonti , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron Mckinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
IPC分类号： A61K47/48 , A61K38/37
CPC分类号： A61K47/6803 , A61K38/37 , A61K47/60 , A61K47/68 , C07K14/755 , C07K2319/00 , C07K2319/31 , G01N33/86
摘要： The present invention provides methods of administering Factor VIII (processed FVIII, single chain FVIII, or a combination thereof); methods of administering chimeric and hybrid polypeptides comprising Factor VIII; chimeric and hybrid polypeptides comprising Factor VIII; polynucleotides encoding such chimeric and hybrid polypeptides; cells comprising such polynucleotides; and methods of producing such chimeric and hybrid polypeptides using such cells
摘要翻译：本发明提供了施用因子VIII（加工的FVIII，单链FVIII或其组合）的方法; 包含因子VIII的嵌合和杂交多肽的施用方法; 包含因子VIII的嵌合和杂合多肽; 编码这种嵌合和杂交多肽的多核苷酸; 包含这种多核苷酸的细胞; 以及使用这种细胞产生这种嵌合和杂合多肽的方法

9. 发明授权

US10010622B2 Factor VIII chimeric and hybrid polypeptides, and methods of use thereof 有权
公开(公告)号：US10010622B2
公开(公告)日：2018-07-03
申请号：US14131600
申请日：2012-07-06
申请人： Jennifer A. Dumont , Susan Low , Alan J. Bitoni , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron McKinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
发明人： Jennifer A. Dumont , Susan Low , Alan J. Bitoni , Glenn Pierce , Alvin Luk , Haiyan Jiang , Byron McKinney , Matt Ottmer , Jurg Sommer , Karen Nugent , Lian Li , Robert Peters
IPC分类号： C07K14/755 , A61K47/48 , A61K38/37 , G01N33/86 , A61K47/60 , A61K47/68
CPC分类号： A61K47/6803 , A61K38/37 , A61K47/60 , A61K47/68 , C07K14/755 , C07K2319/00 , C07K2319/31 , G01N33/86
摘要： The present invention provides methods of administering Factor VIII (processed FVIII, single chain FVIII, or a combination thereof); methods of administering chimeric and hybrid polypeptides comprising Factor VIII; chimeric and hybrid polypeptides comprising Factor VIII; polynucleotides encoding such chimeric and hybrid polypeptides; cells comprising such polynucleotides; and methods of producing such chimeric and hybrid polypeptides using such cells.

10. 发明授权

US06399633B1 Use of 4-H-1-benzopryan-4-one derivatives as inhibitors of smooth muscle cell proliferation 失效
标题翻译：使用4-H-1-苯并呋喃-4-酮衍生物作为平滑肌细胞增殖的抑制剂
公开(公告)号：US06399633B1
公开(公告)日：2002-06-04
申请号：US09468665
申请日：1999-12-21
申请人： Jennifer A. Dumont , Winston Campbell Patterson
发明人： Jennifer A. Dumont , Winston Campbell Patterson
IPC分类号： A61K31445
CPC分类号： A61K31/453
摘要： The use of 4-H-1-benzopyran-4-one derivatives as inhibitors of smooth muscle cell proliferation. Smooth muscle cell (SMC) proliferation is a critical component of neointimal formation in many animal models of vascular injury, and in many human lesions as well. Cell cycle inhibition by gene transfer techniques can block SMC proliferation and lesion formation in many animal models, although these methods are not yet applicable to the treatment of human disease. Flavopiridol is a recently identified, potent, orally available cyclin-dependent kinase inhibitor. Given the role of smooth muscle cell (SMC) proliferation in vascular disease, we tested the effects of flavopiridol, a recently identified cyclin-dependent kinase inhibitor, on SMC growth in vitro and in vivo. Flavopiridol (75 nmol/L) potently blocked SMC proliferation, an effect that was associated with downregulation of cyclin-dependent kinase activity and cell cycle-related gene expression. We examined the effects of flavopiridol on SMC proliferation in vivo in the rat carotid injury model. Flavopiridol (5 mg/kg) decreased neointimal size by 35% and 39% at 7 and 14 days, respectively, after balloon injury. Flavopiridol may be a potential therapeutic tool in the treatment of SMC-rich vascular lesions. 4-H-1-benzopyran-4-one derivatives inhibit smooth muscle cell proliferation at low dosage levels.
摘要翻译：使用4-H-1-苯并吡喃-4-酮衍生物作为平滑肌细胞增殖的抑制剂。平滑肌细胞（SMC）增殖是血管损伤的许多动物模型以及许多人类病变中新内膜形成的关键组成部分。通过基因转移技术的细胞周期抑制可以阻断许多动物模型中的SMC增殖和病变形成，尽管这些方法尚不适用于人类疾病的治疗。黄酮类药物是最近确定的，有效的，口服的细胞周期蛋白依赖性激酶抑制剂。鉴于血管疾病中平滑肌细胞（SMC）增殖的作用，我们测试了最近鉴定的细胞周期蛋白依赖性激酶抑制剂的flavopiridol对体外和体内SMC生长的影响。 Flavopolidol（75 nmol / L）有效阻断了SMC增殖，这与细胞周期蛋白依赖性激酶活性和细胞周期相关基因表达下调有关。我们在大鼠颈动脉损伤模型中检查了flavopiridol对体内SMC增殖的影响。球囊损伤后，分别在5天和4天时，黄曲霉毒素（5mg / kg）的新内膜大小分别降低了35％和39％。黄霉素可能是治疗富含SMC的血管病变的潜在治疗手段。 4-H-1-苯并吡喃-4-酮衍生物在低剂量水平下抑制平滑肌细胞增殖。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式