公开(公告)号：WO2023086821A1

公开(公告)日：2023-05-19

申请号：PCT/US2022/079542

申请日：2022-11-09

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT ,  WAYNE STATE UNIVERSITY

Inventor： GANGJEE, Aleem ,  MATHERLY, Larry H.

IPC: A61K31/519 ,  C07D471/04 ,  C07D487/04

Abstract: A method of inhibiting M2-like macrophages in a patient is provided comprising administering to a patient having ovarian cancer a therapeutically effective amount of a FRβ-transported C1 inhibitor compound having selective efficacy to FRβ expressing tumor cells. The method includes wherein the FRβ-transported C1 inhibitor compound is a substituted pyrrolo[2,3-d]pyrimidine antifolate inhibitor compound having selective efficacy to FRβ expressing tumor cells. The present invention provides a method for targeting both the tumor and the tumor microenvironment with the FRβ-transported C1 inhibitor compounds.

公开(公告)号：WO2016100495A1

公开(公告)日：2016-06-23

申请号：PCT/US2015/066062

申请日：2015-12-16

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT

Inventor： GANGJEE, Aleem

IPC: C07D491/048 ,  A61K31/519

CPC classification number: C07D491/048

Abstract: The present invention provides conformationally restricted 4-substituted 2,6-dimethylfuro[2,3- d ]pyrimidine compounds and pharmaceutical compositions comprising these compounds. Preferably, the compounds exhibit dual inhibition of microtubule assembly and receptor tyrosine kinases. Methods of treating cancer comprising administering a therapeutically effective amount of at least one conformationally restricted 4-substituted 2,6-dimethylfuro[2,3- d ]pyrimidine compound to a patient is disclosed.

Abstract translation: 本发明提供构型受限的4-取代的2,6-二甲基呋喃并[2,3-d]嘧啶化合物和包含这些化合物的药物组合物。 优选地，所述化合物显示对微管组装和受体酪氨酸激酶的双重抑制。 公开了治疗癌症的方法，包括向患者施用治疗有效量的至少一种构象限制的4-取代的2,6-二甲基呋喃并[2,3-d]嘧啶化合物。

公开(公告)号：WO2014011608A2

公开(公告)日：2014-01-16

申请号：PCT/US2013/049676

申请日：2013-07-09

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT

Inventor： JUOLA, Patrick ,  RYAN, Michael

CPC classification number: G06K9/00342 ,  A61B5/117 ,  A61B5/1171 ,  A61B5/1172 ,  G06K9/00335 ,  G06K9/00348

Abstract: A method for identifying an animal or human, including the steps of collecting and retaining an archive data set of measurements of two or more kinetic stylometrics of a first individual animal or human; collecting and retaining a test data set of measurements of the same two or more kinetic stylometrics of a test individual; and comparing archive and test data sets to determine similarity therefore, wherein similarity within any appropriate confidence interval confirms that the test individual and the first individual are the same. Using similar methods, social or other groups maybe kinetically stylometrically profiled for subsequent individual testing.

Abstract translation: 用于鉴定动物或人的方法，包括以下步骤：收集并保留第一个体动物或人的两种或更多种动力学测式的测量的档案数据集; 收集并保留测试个体的相同的两个或更多动力学测式的测量的测试数据组; 并比较存档和测试数据集以确定相似性，其中任何适当置信区间内的相似性证实测试个体和第一个体相同。 使用类似的方法，社交或其他群体可能会动态地进行风格测量，以便进行后续的单独测试。

公开(公告)号：WO2013016006A1

公开(公告)日：2013-01-31

申请号：PCT/US2012/046444

申请日：2012-07-12

Applicant: CABERTECH, INC. ,  DUQUESNE UNIVERSITY OF THE HOLY SPIRIT ,  MCGOWAN, Kenneth A. ,  GAWALT, Ellen S. ,  PALCHESKO, Rachelle

Inventor： MCGOWAN, Kenneth A. ,  GAWALT, Ellen S. ,  PALCHESKO, Rachelle

IPC: A61K9/00

CPC classification number: A61L27/10 ,  A61F2/28 ,  A61F2/30942 ,  A61F2002/30677 ,  A61F2002/30957 ,  A61F2310/00179 ,  A61L27/12 ,  A61L27/54 ,  A61L2300/406 ,  A61L2300/414 ,  C12N5/0654 ,  C12N2501/155 ,  C12N2533/18 ,  C12N2533/54

Abstract: A functionalized composition and resulting functionalized body or prosthesis for in vitro and in vivo use comprising at least one calcium phosphate containing phase that is functionalized with a linker group comprising at least one of an organic acid molecule, a phosphonic acid, an amine, Ν,Ν-dicyclohexylcarbodiimide, and 3-maleimidopropionic acid N-hydroxysuccinimide ester, wherein the linker group provides for a reactive location for the attachment of the chemical or biologically active moiety to the calcium phosphate containing phase. The functionalized compositions have a pliable physical property when mixed with water and adhere to natural bone and subsequently harden at ambient temperatures. Methods of manufacturing a functionalized artificial prosthesis that may be used as artificial bones, joints, in-vitro support structures, and in-vivo support structures for cells, tissues, organs, and nerve growth and regeneration are disclosed. Methods of repairing a bone, vertebrae, or tissue structures using the functionalized compositions are provided.

Abstract translation: 功能化组合物和所得到的用于体外和体内使用的官能化体或假体，其包含至少一种含磷酸钙的相，其被包含有机酸分子，膦酸，胺， α-二环己基碳二亚胺和3-马来酰亚胺基丙酸N-羟基琥珀酰亚胺酯，其中连接基团提供用于将化学或生物活性部分连接到含磷酸钙的相的反应位置。 当与水混合时，官能化组合物具有柔软的物理性质并且粘附到天然骨上，随后在环境温度下硬化。 公开了可用作人造骨骼，关节，体外支持结构和用于细胞，组织，器官和神经生长和再生的体内支持结构的功能化人造假体的方法。 提供使用官能化组合物修复骨，椎骨或组织结构的方法。

公开(公告)号：WO2012106522A2

公开(公告)日：2012-08-09

申请号：PCT/US2012/023643

申请日：2012-02-02

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT ,  GANGJEE, Aleem

Inventor： GANGJEE, Aleem

IPC: A61K31/519 ,  C07D487/04

CPC classification number: C07D495/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048

Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.

Abstract translation: 本发明提供了具有抗微管蛋白活性的双环和三环嘧啶酪氨酸激酶抑制剂。 本发明的组合物在有效的血管内皮生长因子受体抑制活性和抗微管蛋白活性的单一药剂中具有双重活性。 还描述了这些组合物的水溶性盐。 公开了用本发明的组合物和盐治疗患有癌症，黄斑变性和关节炎的患者的方法。

公开(公告)号：WO2019173500A1

公开(公告)日：2019-09-12

申请号：PCT/US2019/020992

申请日：2019-03-06

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT

Inventor： GANGJEE, Aleem

IPC: A61K31/495 ,  A61K31/505 ,  A61K31/519 ,  C07D231/00 ,  C07D487/02 ,  C07D487/04

Abstract: A compound that is a pyrazolo[4,3-d]pyrimidine, and optionally a salt or a hydrate thereof, is disclosed. A pharmaceutical composition comprising a compound that is a pyrazolo[4,3-d]pyrimidine, and optionally a salt or a hydrate of the compound, and includes an optional pharmaceutically acceptable carrier, is provided. A method of treating a patient with cancer including administering a therapeutically acceptable amount of one or more of these compounds and pharmaceutical compositions is set forth.

公开(公告)号：WO2019046612A1

公开(公告)日：2019-03-07

申请号：PCT/US2018/048905

申请日：2018-08-30

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT ,  WAYNE STATE UNIVERSITY

Inventor： GANGJEE, Aleem ,  MATHERLY, Larry H.

IPC: A61K31/519 ,  C07D487/04

Abstract: Pyrrolopyrimidine compounds and pharmaceutically acceptable salt thereof are provided. Pharmaceutical compositions having these compounds and acceptable pharmaceutical carriers are disclosed. Pyrrolopyrimidine compounds and pharmaceutically acceptable salts are set forth that are useful to treat a patient having pancreatic, colon, and lung cancers, to target mitochondrial metabolism, and to target serine hydroxymethyltransferase 2 (SHMT2) and 5,10-methylene tetrahydrofolate dehydrogenase 2 (MTHFD2).

公开(公告)号：WO2015153955A1

公开(公告)日：2015-10-08

申请号：PCT/US2015/024216

申请日：2015-04-03

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT

Inventor： GANGJEE, Aleem

IPC: A61K31/519 ,  C07D487/04 ,  A61P35/00

CPC classification number: C07D487/04

Abstract: This invention provides substituted bicyclic pyrimidine compounds and pharmaceutically acceptable salts, hydrates, and solvates of the compounds, each having tubulin and multiple receptor inhibition properties. Methods of treating a patient diagnosed with cancer is disclosed comprising administering to the patient a therapeutically effective amount of the substituted bicyclic pyrimidine compounds and pharmaceutically acceptable salts, hydrates, and solvates of the compounds, for treating cancer.

Abstract translation: 本发明提供了取代的双环嘧啶化合物和化合物的药学上可接受的盐，水合物和溶剂合物，它们各自具有微管蛋白和多重受体抑制性质。 公开了治疗诊断患有癌症的患者的方法，其包括向患者施用治疗有效量的用于治疗癌症的化合物的取代的双环嘧啶化合物和药学上可接受的盐，水合物和溶剂合物。

公开(公告)号：WO2011046596A2

公开(公告)日：2011-04-21

申请号：PCT/US2010/002726

申请日：2010-10-12

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT, A NONPROFIT CORPORATION ORGANIZED UNDER THE LAWS OF THE COMMONWEALTH OF PENNSYLVANIA ,  WITT-ENDERBY, Paula, A. ,  DAVIS, Vicki, L. ,  LAPINSKY, David, J.

Inventor： WITT-ENDERBY, Paula, A. ,  DAVIS, Vicki, L. ,  LAPINSKY, David, J.

IPC: A61K31/135 ,  A61K31/4045 ,  A61P35/00

CPC classification number: A61K31/135 ,  A61K31/4045 ,  A61K2300/00

Abstract: A particularly constructed tamoxifen-melatonin hybrid ligand gives new and unexpectedly improved results in the prevention and treatment of cancer, particularly breast cancer. The hybrid ligand comprises either tamoxifen or 4-hydroxytamoxifen and also melatonin, with the tamoxifen or 4-hydroxytamoxifen and melatonin's being linked by an unsubstituted C 2 -C 6 alkyl linker between the tamoxifen amine and the carbonyl of melatonin.

Abstract translation: 特别构建的他莫昔芬 - 褪黑激素混合配体在预防和治疗癌症，特别是乳腺癌方面提供了新的和出人意料地改善的结果。 杂合配体包含他莫昔芬或4-羟基他莫昔芬以及褪黑激素，其中他莫昔芬或4-羟基他莫昔芬与褪黑激素之间通过未取代的C≡C≡6烷基连接基连接 他莫昔芬胺和褪黑激素的羰基。

公开(公告)号：WO2010006025A1

公开(公告)日：2010-01-14

申请号：PCT/US2009/049901

申请日：2009-07-08

Applicant: DUQUESNE UNIVERSITY OF THE HOLY SPIRIT ,  GANGJEE, Aleem

Inventor： GANGJEE, Aleem

IPC: A01N43/52

CPC classification number: C07D491/048 ,  C07D239/70 ,  C07D487/04

Abstract: The present invention provides bicyclic compounds, pharmaceutically acceptable salts, prodrugs, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.

Abstract translation: 本发明提供具有抗有丝分裂活性，抗多药耐药性活性的双环化合物，其药学上可接受的盐，前体药物，溶剂合物和水合物，例如P-糖蛋白抑制和抗肿瘤活性，并且其抑制紫杉醇敏感和抗性肿瘤 细胞。 还提供了利用这些化合物治疗肿瘤细胞并抑制癌细胞有丝分裂的方法。