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1. 发明申请

WO0054584B1 METHOD OF PREPARING CRYOGENICALLY PRESERVED ADHERENT CELL CONTAINING PLATE FOR TISSUE CULTURE APPLICATIONS 审中-公开
标题翻译：制备用于组织培养的低温保存的粘附细胞的平板的方法应用
公开(公告)号：WO0054584B1
公开(公告)日：2000-11-23
申请号：PCT/US0006921
申请日：2000-03-17
申请人： BIO TECH IMAGING INC , YOUNG SUSAN M , KING CHESTER F , MATLOCK SHAWN A
发明人： YOUNG SUSAN M , KING CHESTER F , MATLOCK SHAWN A
IPC分类号： A01N1/02 , C12N1/04
CPC分类号： A01N1/02 , A01N1/0221 , A01N1/0268 , C12N1/04
摘要： A process for applying and storing adherent cells on a tissue culture plate (20) for preparing tissue culture plates for use in tissue culture experiments. In the process, adherent cells are removed from a flask using trypsin after being incubated in a CO2 incubator. The cell suspension is created using the adherent cells and a liquid culture medium, which is centrifuged and tested for volume using a hemacytometer. The cell suspension is placed in the wells of a tissue culture plate (20) and then incubated. A cryopreservative is deposited into each well and the tissue culture plate is sealed with an adhesive foil cover and a cryogenically preserved using liquid nitrogen. The tissue culture plate (20) is then placed into a plastic, waterproof, resealable bag, enabling it to be stored at -80 DEG C for up to 3 months and shipped without damaging the morphological or functional nature of the adherent cells. The tissue culture plate forms part of a cryopreserved cell culture assembly which includes frozen adherent cells attached to the bottom wall surface of a well in the tissue culture plate.
摘要翻译：一种在组织培养板（20）上施加和储存贴壁细胞以制备用于组织培养实验的组织培养板的方法。在该过程中，在CO 2培养箱中孵育后，使用胰蛋白酶从烧瓶中除去贴壁细胞。使用贴壁细胞和液体培养基产生细胞悬液，离心并使用血细胞计数器测定体积。将细胞悬浮液置于组织培养板（20）的孔中，然后温育。将冷冻保存液沉积到每个孔中，并将组织培养板用粘性箔覆盖物密封，并使用液氮进行低温保存。然后将组织培养板（20）放入塑料防水可再密封袋中，使其可以在-80℃下保存长达3个月，并且运输时不会损害贴壁细胞的形态或功能性质。组织培养板形成冷冻保存的细胞培养组件的一部分，其包括附着于组织培养板中孔的底壁表面的冷冻粘附细胞。

2. 发明申请

WO2007019180A3 COMPOUNDS FOR BINDING TO ERALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF 审中-公开
标题翻译：用于结合至ERALPHA / BETA和GPR30的化合物，通过这些受体介导的治疗疾病状态和条件的方法及其鉴定
公开(公告)号：WO2007019180A3
公开(公告)日：2008-04-10
申请号：PCT/US2006030130
申请日：2006-08-02
申请人： STC UNM , CHEMDIV INC , ARROWHEAD CT INC , PROSSNITZ ERIC R , TKATCHENKO SERGEY E , REVANKAR CHETANA M , SKLAR LARRY A , ARTERBURN JEFFREY B , CIMINO DANIEL F , OPREA TUDOR I , BOLOGA CRISTIAN-GEORGE , EDWARDS BRUCE S , KISELYOV ALEXANDOR , YOUNG SUSAN M
发明人： PROSSNITZ ERIC R , TKATCHENKO SERGEY E , REVANKAR CHETANA M , SKLAR LARRY A , ARTERBURN JEFFREY B , CIMINO DANIEL F , OPREA TUDOR I , BOLOGA CRISTIAN-GEORGE , EDWARDS BRUCE S , KISELYOV ALEXANDOR , YOUNG SUSAN M
IPC分类号： A61K31/435 , C07D215/04 , C07D215/12 , C07D215/16 , C07D221/06 , C07D405/10 , C07D491/048 , C07D491/052 , C07D491/147
CPC分类号： C07D221/16 , C07D405/04 , C07D405/14
摘要： The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ERa and ERß). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.
摘要翻译：本发明在分子生物学/药理学领域，并提供调节GPR30以及经典雌激素受体α和β（ERα和ERβ）的作用的化合物。这些化合物可以用作一种或多种所公开的雌激素受体的激动剂和/或拮抗剂。通过这些受体中的一种或多种介导的疾病包括癌症（特别是乳腺，生殖和其他激素依赖性癌症，白血病，结肠癌，前列腺癌），生殖（泌尿 - 泌尿）包括子宫内膜炎，前列腺炎，多囊卵巢综合征，膀胱控制，激素相关疾病，听觉障碍，心血管疾病，包括潮热和大量出汗，高血压，中风，肥胖，骨质疏松症，血液病，血管疾病或诸如静脉血栓形成，动脉粥样硬化等疾病，以及许多其他疾病和中枢和周围神经系统，包括抑郁症，失眠，焦虑，多发性硬化，神经病变，神经变性疾病如帕金森病和阿尔茨海默病，以及炎性肠病，克罗恩病，腹腔（腹腔）疾病和肠道相关疾病。用于预防或减少性交后怀孕的可能性的避孕指示是本发明的另一方面。

3. 发明申请

WO2007019180A2 COMPOUNDS FOR BINDING TO ERALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF 审中-公开
标题翻译：用于结合至ERALPHA / BETA和GPR30的化合物，通过这些受体介导的治疗疾病状态和条件的方法及其鉴定
公开(公告)号：WO2007019180A2
公开(公告)日：2007-02-15
申请号：PCT/US2006/030130
申请日：2006-08-02
申请人： SCIENCE & TECHNOLOGY CORPORATION @ UNM , CHEMDIV, INC. , PROSSNITZ, Eric, R. , TKATCHENKO, Sergey, E. , REVANKAR, Chetana, M. , SKLAR, Larry, A. , ARTERBURN, Jeffrey, B. , CIMINO, Daniel, F. , OPREA, Tudor, I. , BOLOGA, Cristian-George , EDWARDS, Bruce, S. , KISELYOV, Alexandor , YOUNG, Susan, M.
发明人： PROSSNITZ, Eric, R. , TKATCHENKO, Sergey, E. , REVANKAR, Chetana, M. , SKLAR, Larry, A. , ARTERBURN, Jeffrey, B. , CIMINO, Daniel, F. , OPREA, Tudor, I. , BOLOGA, Cristian-George , EDWARDS, Bruce, S. , KISELYOV, Alexandor , YOUNG, Susan, M.
IPC分类号： C04B28/34 , C09K8/46
CPC分类号： C07D221/16 , C07D405/04 , C07D405/14
摘要： The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ERα and ERβ). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors. Diseases which are mediated through one or more of these receptors include cancer (particularly breast, reproductive and other hormone-dependent cancers, leukemia, colon cancer, prostate cancer), reproductive (genito-urological) including endometreitis, prostatitis, polycystic ovarian syndrome, bladder control, hormone-related disorders, hearing disorders, cardiovascular conditions including hot flashes and profuse sweating, hypertension, stroke, obesity, osteoporosis, hematologic diseases, vascular diseases or conditions such as venous thrombosis, atherosclerosis, among numerous others and disorders of the central and peripheral nervous system, including depression, insomnia, anxiety, multiple sclerosis, neuropathy, neurodegenerative disorders such as Parkinson's disease and Alzheimer's disease, as well as inflammatory bowel disease, Crohn's disease, coeliac (celiac) disease and related disorders of the intestine. A contraceptive indication to prevent or reduce the likelihood of pregnancy after intercourse is a further aspect of the present invention.
摘要翻译：本发明在分子生物学/药理学领域，并提供调节GPR30以及经典雌激素受体α和β（ERα和ERβ）的作用的化合物。这些化合物可以用作一种或多种所公开的雌激素受体的激动剂和/或拮抗剂。通过这些受体中的一种或多种介导的疾病包括癌症（特别是乳腺，生殖和其他激素依赖性癌症，白血病，结肠癌，前列腺癌），生殖（泌尿 - 泌尿）包括子宫内膜炎，前列腺炎，多囊卵巢综合征，膀胱控制，激素相关疾病，听觉障碍，心血管疾病，包括潮热和大量出汗，高血压，中风，肥胖，骨质疏松症，血液病，血管疾病或诸如静脉血栓形成，动脉粥样硬化等疾病，以及许多其他疾病和中枢和周围神经系统，包括抑郁症，失眠，焦虑，多发性硬化，神经病变，神经变性疾病如帕金森病和阿尔茨海默病，以及炎性肠病，克罗恩病，腹腔（腹腔）疾病和肠道相关疾病。用于预防或减少性交后怀孕的可能性的避孕指示是本发明的另一方面。

4. 发明申请

WO2009070331A3 COMPOUNDS AND METHODS FOR THE SELECTIVE INHIBITION OF ABCB1, ABCC1 AND ABCG2 TRANSPORTERS AND THE TREATMENT OF CANCERS, ESPECIALLY DRUG RESISTANT CANCERS AND HIGH THROUGHPUT FLOW CYTOMETRY ASSAY TO DETECT SELECTIVE INHIBITORS 审中-公开
标题翻译：选择性抑制ABCB1，ABCC1和ABCG2转运蛋白以及治疗癌症，特别是抗药性癌症和高通量流式细胞测定以检测选择性抑制剂的化合物和方法
公开(公告)号：WO2009070331A3
公开(公告)日：2009-07-23
申请号：PCT/US2008013209
申请日：2008-11-28
申请人： STC UNM , LARSON RICHARD S , SKLAR LARRY A , EDWARDS BRUCE S , IVNITSKI-STEELE IRENA D , OPREA TUDOR I , LOVATO DEBBIE M , KHAWAJA HADYA M , WINTER STUART S , YOUNG SUSAN M
发明人： SKLAR LARRY A , EDWARDS BRUCE S , IVNITSKI-STEELE IRENA D , OPREA TUDOR I , LOVATO DEBBIE M , KHAWAJA HADYA M , WINTER STUART S , YOUNG SUSAN M
IPC分类号： A61K31/415 , A61K31/12 , A61P35/00
CPC分类号： A61K31/12 , A61K31/415 , A61K45/06 , A61K2300/00
摘要： Compounds disclosed which inhibit ABCBl transporter protein are useful for treating diseases in which ABCBl transporter protein mediates the disease state, including numerous cancers, including hematopoietic cancers, including various leukemias, especially T-lineage acute lymphoblastic leukemia, as well as cancerous tumors, especially forms which exhibit multiple drug resistance. Pharmaceutical compositions which comprise an inhibitor of ABCBl transporter protein and at least one additional anticancer agent, optionally in combination with a pharmaceutically acceptable carrier, additive or excipient are another aspect of the present invention. A flow cytometry based, high-throughput screening (HST) assay that quantifies ABCBl efflux is also disclosed. Methods of identifying inhibitors of ABCBl, ABCG2 and ABCCl transporter proteins are also disclosed.
摘要翻译：公开的抑制ABCB1转运蛋白的化合物可用于治疗其中ABCB1转运蛋白介导疾病状态的疾病，包括多种癌症，包括造血系统癌症，包括各种白血病，尤其是T-系急性淋巴细胞白血病，以及癌性肿瘤，特别是癌表现出多重耐药性。包含ABCB1转运蛋白抑制剂和至少一种另外的抗癌剂，任选地与药学上可接受的载体，添加剂或赋形剂组合的药物组合物是本发明的另一方面。还公开了量化ABCB1流出的基于流式细胞术的高通量筛选（HST）测定法。还公开了鉴定ABCB1，ABCG2和ABCCl转运蛋白的抑制剂的方法。

5. 发明申请

WO2009070331A2 COMPOUNDS AND METHODS FOR THE SELECTIVE INHIBITION OF ABCB1, ABCC1 AND ABCG2 TRANSPORTERS AND THE TREATMENT OF CANCERS, ESPECIALLY DRUG RESISTANT CANCERS AND HIGH THROUGHPUT FLOW CYTOMETRY ASSAY TO DETECT SELECTIVE INHIBITORS 审中-公开
标题翻译：选择性抑制ABCB1，ABCC1和ABCG2转运蛋白的化合物和方法以及癌症治疗，特别是耐药性和高通量流式细胞计数测定来检测选择性抑制剂
公开(公告)号：WO2009070331A2
公开(公告)日：2009-06-04
申请号：PCT/US2008/013209
申请日：2008-11-28
申请人： STC.UNM , LARSON, Richard, S. , SKLAR, Larry, A. , EDWARDS, Bruce, S. , IVNITSKI-STEELE, Irena, D. , OPREA, Tudor, I. , LOVATO, Debbie, M. , KHAWAJA, Hadya, M. , WINTER, Stuart, S. , YOUNG, Susan, M.
发明人： SKLAR, Larry, A. , EDWARDS, Bruce, S. , IVNITSKI-STEELE, Irena, D. , OPREA, Tudor, I. , LOVATO, Debbie, M. , KHAWAJA, Hadya, M. , WINTER, Stuart, S. , YOUNG, Susan, M.
IPC分类号： A61K31/415 , A61K31/12 , A61P35/00
CPC分类号： A61K31/12 , A61K31/415 , A61K45/06 , A61K2300/00
摘要： Compounds disclosed which inhibit ABCBl transporter protein are useful for treating diseases in which ABCBl transporter protein mediates the disease state, including numerous cancers, including hematopoietic cancers, including various leukemias, especially T-lineage acute lymphoblastic leukemia, as well as cancerous tumors, especially forms which exhibit multiple drug resistance. Pharmaceutical compositions which comprise an inhibitor of ABCBl transporter protein and at least one additional anticancer agent, optionally in combination with a pharmaceutically acceptable carrier, additive or excipient are another aspect of the present invention. A flow cytometry based, high-throughput screening (HST) assay that quantifies ABCBl efflux is also disclosed. Methods of identifying inhibitors of ABCBl, ABCG2 and ABCCl transporter proteins are also disclosed.
摘要翻译：公开的抑制ABCB1转运蛋白的化合物可用于治疗其中ABCB1转运蛋白介导疾病状态的疾病，包括许多癌症，包括造血癌，包括各种白血病，特别是T-lineage急性成淋巴细胞性白血病，以及癌性肿瘤，特别是形式其表现出多种耐药性。包含ABCB1转运蛋白抑制剂和任选与药学上可接受的载体，添加剂或赋形剂组合的至少一种另外的抗癌剂的药物组合物是本发明的另一方面。还公开了量化ABCB1流出的基于流式细胞术的高通量筛选（HST）测定。还公开了鉴定ABCB1，ABCG2和ABCC1转运蛋白抑制剂的方法。

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