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公开(公告)号：EP3607821A1
公开(公告)日：2020-02-12
申请号：EP19174479.6
申请日：2014-03-14
IPC分类号： A01N43/78 , A61K31/425 , C07C309/00
摘要： Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
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公开(公告)号：EP2952192B1
公开(公告)日：2019-05-15
申请号：EP15154363.4
申请日：2010-11-05
IPC分类号： A61K31/497 , A61P31/00
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3.发明授权
公开(公告)号：EP2853265B1
公开(公告)日：2017-07-26
申请号：EP14193060.2
申请日：2010-11-05
IPC分类号： A61K31/497
CPC分类号： C07D211/96 , A61K31/44 , A61K31/4412 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D211/86 , C07D213/02 , C07D213/69 , C07D401/06 , C07D401/14 , C07D417/06 , C07D491/113 , Y02A50/401 , Y02A50/465 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481
摘要： Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1±), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
摘要翻译： 本文公开了可以稳定缺氧诱导因子-1α（HIF-1±）以及缺氧诱导因子-2（HIF-2）的脯氨酰羟化酶抑制剂。 本文还公开了包含一种或多种公开的化合物的药物组合物。 还进一步公开了用于刺激哺乳动物中的细胞免疫应答的方法，例如增加吞噬作用，例如延长吞噬细胞（尤其是角质细胞，嗜中性粒细胞）的寿命。 因此，所公开的化合物提供了用于治疗与身体免疫应答有关的疾病的方法。
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4.发明公开Methods for increasing the stabilization of hypoxia inducible factor-1 alpha 有权Verfahren zurErhöhungder Stabilization von hypoxie-indizierbarem Faktor-1 Alpha
公开(公告)号：EP2853265A1
公开(公告)日：2015-04-01
申请号：EP14193060.2
申请日：2010-11-05
IPC分类号： A61K31/497
CPC分类号： C07D211/96 , A61K31/44 , A61K31/4412 , A61K31/4427 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K31/55 , A61K45/06 , C07D211/86 , C07D213/02 , C07D213/69 , C07D401/06 , C07D401/14 , C07D417/06 , C07D491/113 , Y02A50/401 , Y02A50/465 , Y02A50/47 , Y02A50/471 , Y02A50/473 , Y02A50/475 , Y02A50/478 , Y02A50/481
摘要： Disclosed herein are compositions comprising HIF-1α prolyl hydroxylase inhibitors useful in treating diseases, conditions, and/or syndromes related to the activity of HIF-1α, inter alia, infection, cancer, and wound healing
摘要翻译： 本文公开了包含HIF-1±脯氨酰羟化酶抑制剂的组合物，其可用于治疗与HIF-1±活性相关的疾病，病症和/或综合征，特别是感染，癌症和伤口愈合
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5.发明授权Human protein-tyrosine phosphatase inhibitors and their pharmaceutical use 有权人类蛋白酪氨酸磷酸酶的抑制剂，以及它们的药物使用
公开(公告)号：EP2041129B1
公开(公告)日：2014-09-03
申请号：EP07809909.0
申请日：2007-06-27
发明人： GRAY, Jeffrey Lyle , CLARK, Cynthia, Monesa , AMARASINGHE, Kande , MAIER, Mathew, Brian , NICHOLS, Ryan
IPC分类号： C07D417/12 , A61K31/425 , A61P35/00
CPC分类号： C07D417/12 , C07D417/14
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公开(公告)号：EP2766044A1
公开(公告)日：2014-08-20
申请号：EP12840725.1
申请日：2012-10-15
发明人： PETERS, Kevin , SHALWITZ, Robert
IPC分类号： A61K39/395
摘要： Disclosed are methods for treating eye diseases or conditions characterized by vascular instability, vascular leakage and neovacularization such as diabetic macular edema, age-related macular edema, choroidal neovascularization, diabetic retinopathy, trauma, ocular ischemia, retinal angiomatous proliferation, macular telangiectasia and uveitis.
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7.发明授权
公开(公告)号：EP3252079B1
公开(公告)日：2020-07-29
申请号：EP17169315.3
申请日：2007-04-05
IPC分类号： C07K16/40 , A61K39/395 , A61P9/10 , A61P27/02
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公开(公告)号：EP3505182A1
公开(公告)日：2019-07-03
申请号：EP18201774.9
申请日：2012-10-15
发明人： PETERS, Kevin , SHALWITZ, Robert
IPC分类号： A61K39/395
摘要： Disclosed are methods for treating Vascular Leak Syndrome and preventing cancer metastasis. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, sepsis, cancer or the presence of pathogens.
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9.发明公开ANTIBODIES THAT BIND HUMAN PROTEIN TYROSINE PHOSPHATASE BETA (HPTP-SS) AND USES THEREOF 审中-公开结合人类蛋白酪氨酸磷酸酶β（HPTP-SS）的抗体及其应用
公开(公告)号：EP3252079A1
公开(公告)日：2017-12-06
申请号：EP17169315.3
申请日：2007-04-05
IPC分类号： C07K16/40 , A61K39/395
摘要： Antibodies and antigen binding fragments thereof that bind to human protein tyrosine phosphatase beta (HPTPß), and uses thereof.
摘要翻译： 结合人蛋白酪氨酸磷酸酶β（HPTPβ）的抗体及其抗原结合片段及其用途。
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公开(公告)号：EP2967066A4
公开(公告)日：2016-11-02
申请号：EP14762974
申请日：2014-03-14
发明人： PETERS KEVIN , SHALWITZ ROBERT , JANUSZ JOHN , SMITH ALEXANDER
IPC分类号： A01N43/78 , A61K31/425 , C07C309/00
CPC分类号： C07D417/12 , A61K31/426 , A61K31/427 , A61K31/428 , A61K31/433 , A61K31/4439 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/513 , A61K31/538 , A61K38/179 , A61K39/3955 , C07D277/30 , C07D277/56 , C07D277/60 , C07D277/64 , C07D417/04
摘要： Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
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