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    Compounds for binding to ER alpha/beta and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof
    2.
    发明授权
    Compounds for binding to ER alpha/beta and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof 有权
    用于结合ERα/β和GPR30的化合物，治疗通过这些受体介导的疾病状态和病症的方法及其鉴定

    公开(公告)号：US08487100B2

    公开(公告)日：2013-07-16

    申请号：US12967871

    申请日：2010-12-14

    Applicant: Eric R Prossnitz ,  Sergey E Tkatchenko ,  Chetana M Revankar ,  Larry A Sklar ,  Jeffrey B Arterburn ,  Daniel F Cimino ,  Tudor I Oprea ,  Cristian-George Bologa ,  Bruce S Edwards ,  Alexandor Kiselyov ,  Susan M Young

    Inventor： Eric R Prossnitz ,  Sergey E Tkatchenko ,  Chetana M Revankar ,  Larry A Sklar ,  Jeffrey B Arterburn ,  Daniel F Cimino ,  Tudor I Oprea ,  Cristian-George Bologa ,  Bruce S Edwards ,  Alexandor Kiselyov ,  Susan M Young

    IPC: A61K31/4375 ,  C07D221/06

    CPC classification number: C07D221/16 ,  C07D405/04 ,  C07D405/14

    Abstract: 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 disoders 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.

    Abstract translation: 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，神经变性解码器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。

    Bifunctional metnase/intnase inhibitors and related compositions and methods of treatment of cancer
    3.
    发明授权
    Bifunctional metnase/intnase inhibitors and related compositions and methods of treatment of cancer 有权
    双功能metnase / intnase抑制剂和相关的治疗癌症的组合物和方法

    公开(公告)号：US08889689B2

    公开(公告)日：2014-11-18

    申请号：US13574941

    申请日：2011-01-26

    Applicant: Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

    Inventor： Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

    IPC: A61K31/497 ,  A61K45/06 ,  C07D401/12 ,  C07D215/56 ,  A61K31/4709 ,  A61K31/47

    CPC classification number: C07D215/56 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/475 ,  A61K31/496 ,  A61K31/7048 ,  A61K45/06 ,  A61N5/1001 ,  A61N5/1045 ,  A61N2005/1087 ,  A61N2005/1098 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  A61K2300/00

    Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-I) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers. In certain aspects of such treatments, compounds, compositions and methods of treatment of the invention are administered as a monotherapy (in some cases, to patients who have exhibited resistance to Topo IIalpha inhibitors such as VP-16), or are co-administered with a Topo IIalpha inhibitor or other anti-cancer agents as otherwise described herein or in combination with radiation therapy.

    Abstract translation: 本发明涉及新的癌症治疗组合物和相关的治疗方法。 更具体地说，本发明部分涉及同时损伤DNA的DNA复制和修复蛋白质Metnase和/或Intnase（也称为Gypsy整合酶，Gypsy Integrease-1，Gypsy Retransposon Integrase 1或GIN-1）的小型化学双功能抑制剂， 以及利用抑制剂增加包括放射治疗在内的癌症治疗方案的有效性的治疗方法。 在优选的实施方案中，本发明的化合物，组合物和治疗方法用于治疗患有白血病的患者（例如急性骨髓性白血病（AML）和相关的癌症）。在这些治疗的某些方面，化合物，组合物和治疗方法 本发明作为单一疗法（在某些情况下，对已显示出对Topo IIalpha抑制剂如VP-16具有抗性的患者）施用，或者与本文另有描述的Topo IIal抑制剂或其它抗癌剂共同施用，或 结合放射治疗。

    Methods and related compositions for the treatment of cancer
    4.
    发明授权
    Methods and related compositions for the treatment of cancer 有权
    用于治疗癌症的方法和相关组合物

    公开(公告)号：US08835506B2

    公开(公告)日：2014-09-16

    申请号：US12990334

    申请日：2009-06-05

    Applicant: Todd A. Thompson ,  Debra Mackenzie ,  Tudor I. Oprea ,  Larry A. Sklar ,  Bruce S. Edwards ,  Mark Haynes

    Inventor： Todd A. Thompson ,  Debra Mackenzie ,  Tudor I. Oprea ,  Larry A. Sklar ,  Bruce S. Edwards ,  Mark Haynes

    IPC: A01N33/02 ,  A61K31/165 ,  A61K31/445

    CPC classification number: A61K31/437 ,  A61K31/135 ,  A61K31/165 ,  A61K31/445 ,  A61K45/06 ,  A61N5/10

    Abstract: A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death. While the exact mechanism of cancer cell degradation and death is not completely understood, the treated cancer cells, including refractory prostate cancer cells, give indications of cell death through an autophagic mechanism. Pharmaceutical compositions related to the presently disclosed methods are also disclosed.

    Abstract translation: 治疗和/或预防癌症的方法包括在癌细胞中引起增加的细胞内颗粒度的给药剂，至少足以抑制这些细胞增殖的量，优选以足以导致癌细胞死亡的量。 该方法特别涉及难治性癌症，特别是激素难治性前列腺癌。 所鉴定的试剂导致癌细胞中的细胞内颗粒度增加，并且将粘附的癌细胞转化为非贴壁癌细胞，导致癌细胞死亡。 使用本发明，癌细胞在相对低的药物浓度下经历增加的细胞内粒度，同时也抑制细胞增殖。 增加的浓度导致粘附的癌细胞转化为非粘附的癌细胞，然后转移到细胞死亡。 虽然癌细胞降解和死亡的确切机制尚未完全了解，但治疗的癌细胞（包括难治性前列腺癌细胞）通过自噬机制给予细胞死亡的指示。 还公开了与目前公开的方法相关的药物组合物。

    METHODS AND RELATED COMPOSITIONS FOR THE TREATMENT OF CANCER
    5.
    发明申请
    METHODS AND RELATED COMPOSITIONS FOR THE TREATMENT OF CANCER 有权
    用于治疗癌症的方法和相关组合物

    公开(公告)号：US20110224141A1

    公开(公告)日：2011-09-15

    申请号：US12990334

    申请日：2009-06-05

    Applicant: Todd A. Thompson ,  Debra Mackenzie ,  Tudor I. Oprea ,  Larry A. Sklar ,  Bruce S. Edwards ,  Mark Haynes

    Inventor： Todd A. Thompson ,  Debra Mackenzie ,  Tudor I. Oprea ,  Larry A. Sklar ,  Bruce S. Edwards ,  Mark Haynes

    IPC: A61K31/454 ,  A61K31/496 ,  A61K38/08 ,  A61K31/56 ,  A61P35/00

    CPC classification number: A61K31/437 ,  A61K31/135 ,  A61K31/165 ,  A61K31/445 ,  A61K45/06 ,  A61N5/10

    Abstract: A method of treatment and/or prevention of cancer comprises administering agents which cause increased intracellular granularity in cancer cells, at least in an amount sufficient to inhibit proliferation of such cells and preferably in an amount sufficient to lead to cancer cell death. The method is particularly directed to refractory cancer, particularly hormone refractory prostate cancer. The agents identified cause increased intracellular granularity in the cancer cells, and also convert adherent cancer cells to non-adherent cancer cells, leading to cancer cell death. Using the present invention, cancer cells undergo increased intracellular granularity at relatively low agent concentrations, while also inhibiting cell proliferation. Increased concentrations lead to conversion of adherent cancer cells to non-adherent cancer cells, then to cell death. While the exact mechanism of cancer cell degradation and death is not completely understood, the treated cancer cells, including refractory prostate cancer cells, give indications of cell death through an autophagic mechanism. Pharmaceutical compositions related to the presently disclosed methods are also disclosed.

    Abstract translation: 治疗和/或预防癌症的方法包括在癌细胞中引起增加的细胞内颗粒度的给药剂，至少足以抑制这些细胞增殖的量，优选以足以导致癌细胞死亡的量。 该方法特别涉及难治性癌症，特别是激素难治性前列腺癌。 所鉴定的试剂导致癌细胞中的细胞内颗粒度增加，并且将粘附的癌细胞转化为非贴壁癌细胞，导致癌细胞死亡。 使用本发明，癌细胞在相对低的药物浓度下经历增加的细胞内粒度，同时也抑制细胞增殖。 增加的浓度导致粘附的癌细胞转化为非粘附的癌细胞，然后转移到细胞死亡。 虽然癌细胞降解和死亡的确切机制尚未完全了解，但治疗的癌细胞（包括难治性前列腺癌细胞）通过自噬机制给予细胞死亡的指示。 还公开了与目前公开的方法相关的药物组合物。

    Compounds for binding to ERα/β and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof
    6.
    发明授权
    Compounds for binding to ERα/β and GPR30, methods of treating disease states and conditions mediated through these receptors and identification thereof 有权
    用于结合ERα/ bgr的化合物 和GPR30，治疗通过这些受体介导的疾病状态和病症的方法及其鉴定

    公开(公告)号：US07875721B2

    公开(公告)日：2011-01-25

    申请号：US11497751

    申请日：2006-08-02

    Applicant: Eric R. Prossnitz ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    Inventor： Eric R. Prossnitz ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    IPC: A61K31/435 ,  C07D221/06

    CPC classification number: C07D221/16 ,  C07D405/04 ,  C07D405/14

    Abstract: 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 endometritis, 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.

    Abstract translation: 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ER和bgr）的作用的化合物。 这些化合物可以作为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（泌尿系）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。

    NOVEL BIFUNCTIONAL METNASE/INTNASE INHIBITORS AND RELATED COMPOSITIONS AND METHODS OF TREATMENT OF CANCER
    7.
    发明申请
    NOVEL BIFUNCTIONAL METNASE/INTNASE INHIBITORS AND RELATED COMPOSITIONS AND METHODS OF TREATMENT OF CANCER 有权
    新型双功能蛋白酶/终止抑制剂及相关组合物及治疗癌症的方法

    公开(公告)号：US20120302582A1

    公开(公告)日：2012-11-29

    申请号：US13574941

    申请日：2011-01-26

    Applicant: Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

    Inventor： Robert Hromas ,  Andrei Leitao ,  Tudor I. Oprea ,  Larry A. Sklar ,  Elizabeth A. Williamson ,  Justin Wray ,  Wei Wang

    IPC: A61K31/496 ,  C07D401/10 ,  A61N5/10 ,  C07D401/14 ,  A61P35/00 ,  A61P35/02 ,  A61K31/47 ,  C07D215/56

    CPC classification number: C07D215/56 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/475 ,  A61K31/496 ,  A61K31/7048 ,  A61K45/06 ,  A61N5/1001 ,  A61N5/1045 ,  A61N2005/1087 ,  A61N2005/1098 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  A61K2300/00

    Abstract: This invention relates to novel cancer treatment compositions and associated therapeutic methods. More particularly, this invention relates in part to small chemical bifunctional inhibitors of DNA replication and repair proteins Metnase and/or Intnase (also termed Gypsy Integrase, Gypsy Integrease-1, Gypsy Retransposon Integrase 1, or GIN-I) that simultaneously damage DNA, and to a therapeutic method that utilizes the inhibitors to increase the effectiveness of cancer treatment protocols, including radiation therapy. In preferred embodiments, compounds, compositions and methods of treatment of the invention are used to treat a patient suffering from leukemia (e.g. acute myeloid leukemia (AML) and related cancers. In certain aspects of such treatments, compounds, compositions and methods of treatment of the invention are administered as a monotherapy (in some cases, to patients who have exhibited resistance to Topo IIalpha inhibitors such as VP-16), or are co-administered with a Topo IIalpha inhibitor or other anti-cancer agents as otherwise described herein or in combination with radiation therapy.

    Abstract translation: 本发明涉及新的癌症治疗组合物和相关的治疗方法。 更具体地说，本发明部分涉及同时损伤DNA的DNA复制和修复蛋白质Metnase和/或Intnase（也称为Gypsy整合酶，Gypsy Integrease-1，Gypsy Retransposon Integrase 1或GIN-1）的小型化学双功能抑制剂， 以及利用抑制剂增加包括放射治疗在内的癌症治疗方案的有效性的治疗方法。 在优选的实施方案中，本发明的化合物，组合物和治疗方法用于治疗患有白血病的患者（例如急性骨髓性白血病（AML）和相关的癌症）。在这些治疗的某些方面，化合物，组合物和治疗方法 本发明作为单一疗法（在某些情况下，对已显示出对Topo IIalpha抑制剂如VP-16具有抗性的患者）施用，或者与本文另有描述的Topo IIal抑制剂或其它抗癌剂共同施用，或 结合放射治疗。

    COMPOUNDS FOR BINDING TO ER ALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF
    9.
    发明申请
    COMPOUNDS FOR BINDING TO ER ALPHA/BETA AND GPR30, METHODS OF TREATING DISEASE STATES AND CONDITIONS MEDIATED THROUGH THESE RECEPTORS AND IDENTIFICATION THEREOF 有权
    用于与ALPHA / BETA和GPR30结合的化合物，通过这些受体介导的治疗疾病状态的方法和鉴定方法

    公开(公告)号：US20110092533A1

    公开(公告)日：2011-04-21

    申请号：US12967871

    申请日：2010-12-14

    Applicant: Eric R. PROSSNITZ ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    Inventor： Eric R. PROSSNITZ ,  Sergey E. Tkatchenko ,  Chetana M. Revankar ,  Larry A. Sklar ,  Jeffrey B. Arterburn ,  Daniel F. Cimino ,  Tudor I. Oprea ,  Cristian-George Bologa ,  Bruce S. Edwards ,  Alexander Kiselyov ,  Susan M. Young

    IPC: A61K31/435 ,  C07D405/10 ,  C07D221/16 ,  C07D405/14 ,  A61P43/00

    CPC classification number: C07D221/16 ,  C07D405/04 ,  C07D405/14

    Abstract: 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 disoders 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.

    Abstract translation: 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ER和bgr）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，神经变性解码器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。

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