公开(公告)号：US09125899B1

公开(公告)日：2015-09-08

申请号：US13161766

申请日：2011-06-16

Applicant: Angela-Wandinger Ness ,  Laurie Hudson ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea

Inventor： Angela-Wandinger Ness ,  Laurie Hudson ,  Larry Sklar ,  Zurab Surviladze ,  Tudor Oprea

IPC: A61K31/403

CPC classification number: A61K31/407 ,  A61K31/403 ,  A61K31/415 ,  A61K45/06 ,  C07D231/06 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/158 ,  G01N33/573 ,  Y02A50/473 ,  Y02A50/486 ,  A61K2300/00

Abstract: The present invention relates to molecules which function as modulators (i.e., inhibitors and agonists) of the Ras-homologous (Rho) family of small GTPases (e.g. Rac, Cdc42 and Rho GTPases) and their use to treat diseases, including cancers (including solid tumors-medulloblastoma, ovarian, breast, head and neck, testicular, prostate among others and hematologic malignancies-B cell lymphoma, where these GTPases are overexpressed or hyperactivated), sporadic and genetic diseases where activation of Rho GTPases plays a pivotal role (Menkes disease, rheumatoid arthritis, atherosclerosis, diabetes (type 1), Huntington's disease and Alzheimer's disease) which are mediated through these proteins. Compounds according to the present invention may also be used as a therapy for the treatment of Entamoeba spp. or Acanthamoeba spp, infections, especially including Entamoeba histolytica.

Abstract translation: 本发明涉及用作小GTP酶（例如Rac，Cdc42和Rho GTP酶）的Ras同源（Rho）家族的调节剂（即抑制剂和激动剂）的分子及其用于治疗疾病的用途，包括癌症（包括固体 肿瘤 - 成神经管细胞瘤，卵巢癌，乳腺癌，头颈部，睾丸癌，前列腺癌和血液恶性肿瘤--B细胞淋巴瘤，其中这些GTP酶过度表达或过度活化），其中Rho GTP酶的活化起关键作用的散发性和遗传性疾病（Menkes disease ，类风湿性关节炎，动脉粥样硬化，糖尿病（1型），亨廷顿氏病和阿尔茨海默氏病）。 根据本发明的化合物也可以用作治疗阿米巴疫霉的疗法。 或Acanthamoeba spp，感染，特别是包括溶组织内阿米巴（Entamoeba histolytica）。

公开(公告)号：US20060148079A1

公开(公告)日：2006-07-06

申请号：US11029541

申请日：2005-01-03

Applicant: Virgil Paunescu ,  Erika Suciu ,  Calin Tatu ,  Tudor Oprea

Inventor： Virgil Paunescu ,  Erika Suciu ,  Calin Tatu ,  Tudor Oprea

IPC: C12N5/08

CPC classification number: C12N5/0676 ,  C12N2501/11 ,  C12N2501/117 ,  C12N2501/12 ,  C12N2501/165 ,  C12N2506/1353 ,  C12N2510/02

Abstract: A method for producing an ex vivo population of human insulin-producing cells that produce insulin in response to glucose from a patient is disclosed. The population of insulin producing cells is derived from human epithelial cells by causing those epithelial cells to differentiate into insulin producing cells. In one embodiment, the epithelial cells are derived from human mesenchymal stem cells (MSCs). The MSCs can be cultured from human bone marrow. In one embodiment, a culture of epithelial cell linage is generated by cultivating a sample of human cells containing a mixed culture containing human MSCs to produce an enriched culture of MSCs having a higher concentration of MSCs than the sample; and then differentiating cells from the enriched culture into cells of the epithelial cell lineage.

Abstract translation: 公开了一种用于产生响应于来自患者的葡萄糖产生胰岛素的人胰岛素产生细胞的离体群体的方法。 通过使这些上皮细胞分化成胰岛素生成细胞，产生胰岛素的细胞群体来源于人上皮细胞。 在一个实施方案中，上皮细胞衍生自人间充质干细胞（MSC）。 MSC可以从人骨髓培养。 在一个实施方案中，通过培养含有含有人MSC的混合培养物的人细胞样品产生具有比样品更高浓度的MSC的MSCs的富集培养物来产生上皮细胞培养物的培养物; 然后将细胞从富集的培养物分化成上皮细胞谱系的细胞。

公开(公告)号：US06675136B1

公开(公告)日：2004-01-06

申请号：US09462878

申请日：2000-01-14

Applicant: Johan Gottfries ,  Tudor Oprea

Inventor： Johan Gottfries ,  Tudor Oprea

IPC: G06F9455

CPC classification number: G06F19/704 ,  G06F19/708

Abstract: A computer based technique for the global investigation of property spaces is described. More particularly, a technique is described for the global investigation of chemical space, with reference to drugs, using a system comprised of molecules and descriptors that allows systematic mapping of the chemical space. The technique is used to generate a map of N-dimensional chemical space that allows one to examine, in a consistent manner with existing tools, the inner relationship between various molecules. The technique therefore allows one to investigate unexplored regions of the chemical space, avoiding redundancy, generating compounds with similar chemical information content, or to focus on subsets of the chemical space that are relevant to drug-like structures, without additional errors due to extrapolation.

Abstract translation: 描述了一种基于计算机的全球物业空间调查技术。 更具体地，描述了关于化学空间的全局调查的技术，参考药物，使用由分子和描述符组成的系统，其允许化学空间的系统映射。 该技术用于生成N维化学空间的图，其允许以与现有工具一致的方式检查各种分子之间的内在关系。 因此，该技术允许调查化学空间的未开发区域，避免冗余，产生具有相似化学信息含量的化合物，或者集中在与药物结构相关的化学空间的子集上，而不会由于外推而引起额外的错误。