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1. 发明申请

WO2008155534A3 NEUROSTEROID COMPOUNDS 审中-公开
标题翻译：神经鞘瘤化合物
公开(公告)号：WO2008155534A3
公开(公告)日：2009-04-09
申请号：PCT/GB2008002067
申请日：2008-06-17
申请人： BIONATURE E A LTD , TOWLER PHILIP DEAN , GRAVANIS ACHILLEAS , CALOGEROPOULOU THEODORA , CASTANAS ELIAS , MARGIORIS ANDREAS , CHARALAMBOPOULOS IOANNIS , AVLONITIS NIKOLAOS , MINAS VASSILIOS , ALEXAKI VASILEIA-ISMINI , TSATSANIS CHRISTOS , ALEXIS MICHAEL N , REMBOUTSIKA EUMORPHIA , VERGOU VARVARA , NEOPHYTOU CONSTANTINOS
发明人： GRAVANIS ACHILLEAS , CALOGEROPOULOU THEODORA , CASTANAS ELIAS , MARGIORIS ANDREAS , CHARALAMBOPOULOS IOANNIS , AVLONITIS NIKOLAOS , MINAS VASSILIOS , ALEXAKI VASILEIA-ISMINI , TSATSANIS CHRISTOS , ALEXIS MICHAEL N , REMBOUTSIKA EUMORPHIA , VERGOU VARVARA , NEOPHYTOU CONSTANTINOS
IPC分类号： C07J21/00 , A61K31/58 , A61P25/00 , A61P25/14 , A61P25/16
CPC分类号： C07J21/00
摘要： The present invention relates to novel neurosteroid derivatives with anti-apoptotic, neuroprotective and neurogenic properties that act on the nervous system as well as methods for making the same and their applications in the treatment and/or prevention or amelioration of neurodegenerative diseases related to neuronal apoptosis or neuronal injury, or conditions related to or resulting from apoptosis, including but not limited to Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis and amyotrophic lateral sclerosis (ALS), retinal degeneration and detachment, peripheral neuropathy caused by genetic abnormalities, diabetes, polio, herpes, AIDS and chemotherapy, brain trauma, or ischemia and stroke. The active compounds are represented by Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, B, X, Y and Z are defined in the description of the invention. The present invention also includes compositions which comprise one or more of the compounds of Formula (I).
摘要翻译：本发明涉及具有作用于神经系统的抗细胞凋亡，神经保护和神经原性质的新型神经甾体衍生物及其制备方法及其在治疗和/或预防或改善与神经细胞凋亡有关的神经退行性疾病中的应用或神经元损伤，或与细胞凋亡有关或由凋亡导致的病症，包括但不限于阿尔茨海默氏病，帕金森氏病，亨廷顿病，多发性硬化和肌萎缩性侧索硬化（ALS），视网膜变性和脱离，由基因异常引起的周围神经病，糖尿病，小儿麻痹症，疱疹，艾滋病和化疗，脑外伤，或缺血和中风。活性化合物由式（I）表示：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，A，B，X，Y和Z在本发明的说明书中定义。本发明还包括包含一种或多种式（I）化合物的组合物。

2. 发明申请

WO2008155534A9 NEUROSTEROID COMPOUNDS 审中-公开
标题翻译：神经细胞化合物
公开(公告)号：WO2008155534A9
公开(公告)日：2009-12-03
申请号：PCT/GB2008002067
申请日：2008-06-17
申请人： BIONATURE E A LTD , GRAVANIS ACHILLEAS , CALOGEROPOULOU THEODORA , CASTANAS ELIAS , MARGIORIS ANDREAS , CHARALAMBOPOULOS IOANNIS , AVLONITIS NIKOLAOS , MINAS VASSILIOS , ALEXAKI VASILEIA-ISMINI , TSATSANIS CHRISTOS , ALEXIS MICHAEL N , REMBOUTSIKA EUMORPHIA , VERGOU VARVARA , NEOPHYTOU CONSTANTINOS , TOWLER PHILIP DEAN
发明人： GRAVANIS ACHILLEAS , CALOGEROPOULOU THEODORA , CASTANAS ELIAS , MARGIORIS ANDREAS , CHARALAMBOPOULOS IOANNIS , AVLONITIS NIKOLAOS , MINAS VASSILIOS , ALEXAKI VASILEIA-ISMINI , TSATSANIS CHRISTOS , ALEXIS MICHAEL N , REMBOUTSIKA EUMORPHIA , VERGOU VARVARA , NEOPHYTOU CONSTANTINOS
IPC分类号： C07J21/00 , A61K31/58 , A61P25/00 , A61P25/14 , A61P25/16
CPC分类号： C07J21/00
摘要： The present invention relates to novel neurosteroid derivatives with anti-apoptotic, neuroprotective and neurogenic properties that act on the nervous system as well as methods for making the same and their applications in the treatment and/or prevention or amelioration of neurodegenerative diseases related to neuronal apoptosis or neuronal injury, or conditions related to or resulting from apoptosis, including but not limited to Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis and amyotrophic lateral sclerosis (ALS), retinal degeneration and detachment, peripheral neuropathy caused by genetic abnormalities, diabetes, polio, herpes, AIDS and chemotherapy, brain trauma, or ischemia and stroke. The active compounds are represented by Formula (I): wherein R1, R2, R3, R4, R5, R6, R7, A, B, X, Y and Z are defined in the description of the invention. The present invention also includes compositions which comprise one or more of the compounds of Formula (I).
摘要翻译：本发明涉及作用于神经系统的具有抗凋亡，神经保护和神经源性质的新型神经甾体衍生物及其制备方法及其在治疗和/或预防或改善与神经细胞凋亡有关的神经变性疾病中的应用或神经元损伤，或与凋亡相关或由凋亡引起的病症，包括但不限于阿尔茨海默病，帕金森病，亨廷顿病，多发性硬化和肌萎缩性侧索硬化（ALS），视网膜变性和脱离，遗传异常引起的周围神经病变，糖尿病，脊髓灰质炎，疱疹，艾滋病和化疗，脑外伤或缺血和中风。活性化合物由式（I）表示：其中R 1，R 2，R 3，R 4，R 5，R 6，R 7，A，B，X，Y和Z在本发明的描述中定义。本发明还包括包含一种或多种式（I）化合物的组合物。

3. 发明申请

WO2008065387A3 POTENTIATION OF ERYTHROPOIETIN (EPO) ACTION BY MEMBRANE STEROID RECEPTOR AGONISTS 审中-公开
标题翻译：血管紧张素受体激动剂治疗肾上腺皮质激素（EPO）的作用
公开(公告)号：WO2008065387A3
公开(公告)日：2008-07-31
申请号：PCT/GB2007004537
申请日：2007-11-27
申请人： BIONATURE E A LTD , OWEN DEBORAH , CASTANAS ELIAS , KAMPA MARILENA , PELEKANOU VASSILIKI
发明人： CASTANAS ELIAS , KAMPA MARILENA , PELEKANOU VASSILIKI
IPC分类号： A61K38/18 , A61K8/63 , A61K8/64 , A61K31/593
CPC分类号： A61K31/593 , A61K38/1816 , A61K2300/00
摘要： The present invention relates to the use of membrane steroid receptor agonists as potentiators of the action of erythropoietin (EPO). The present invention also relates to the combined use of membrane steroid receptor agonists and erythropoietin to control apoptosis, proliferation, differentiation, migration and regeneration of cells, in different organs and tissues. Compositions comprising (i) a membrane steroid receptor agonist and (ii) erythropoietin are also provided, as are kits comprising (i) a membrane steroid receptor agonist and (ii) erythropoietin.
摘要翻译：本发明涉及膜类固醇受体激动剂作为红细胞生成素（EPO）作用的增强剂的用途。本发明还涉及膜类固醇受体激动剂和促红细胞生成素在不同器官和组织中的细胞凋亡，增殖，分化，迁移和再生的组合使用。还提供了包含（i）膜类固醇受体激动剂和（ii）促红细胞生成素的组合物，包括（i）膜类固醇受体激动剂和（ii）促红细胞生成素的试剂盒。

4. 发明申请

WO2004047866A3 USE OF THE CORTICOLIBERIN-UROCORTIN SYSTEM IN THE TREATMENT OF INFLAMMATORY DISEASES 审中-公开
标题翻译：在治疗炎症疾病中使用抗抑郁素 - 乌洛托品系统
公开(公告)号：WO2004047866A3
公开(公告)日：2004-07-29
申请号：PCT/IB0305429
申请日：2003-11-26
申请人： BIONATURE E A LTD , MARGIORIS ANDREW N , GRAVANIS ACHILLE
发明人： MARGIORIS ANDREW N , GRAVANIS ACHILLE
IPC分类号： A61K31/506 , A61K38/22 , A61K45/00 , A61P29/00 , G01N33/68
CPC分类号： A61K31/506
摘要： The invention relates to the use of corticotropin-releasing hormone (CRH) receptor-1 (RI) antagonists and/or CRH-R2 receptor agonists for the treatment of inflammatory diseases via regulation of monocyte / macrophage cell activation, proliferation, differentiation, apoptosis, and inflammatory cytokine production. As CRH system we define natural and synthetic CRH and urocortin (UCN) agonists and antagonists for the CRH-R1 and CRH-R2 receptors and their subtypes as well as the CRH-binding protein (BP), a CRH pseudo receptor. The invention is directed towards pharmacological intervention for the amelioration or treatment of inflammatory diseases using the CR. system-mediated control of monocyte / macrophage cells which play a key role in initiating and maintaining the inflammatory response via production of pro-inflammatory cytokines such as is the interleukin (IL)-1, IL-6 and tumor necrosis factor (TNF)-alpha. By the term inflammation we define the response of an organism to noxious endogenous or exogenous stimuli causing tissue injury. Inflammation is a host defence mechanism, which might harm the defending organism. The invention also provides methods for the in vitro and in vivo evaluation of natural and synthetic CRH system modulators for the control of the monocyte / macrophage system.
摘要翻译：本发明涉及促肾上腺皮质激素释放激素（CRH）受体-1（RI）拮抗剂和/或CRH-R2受体激动剂用于通过调节单核细胞/巨噬细胞活化，增殖，分化，凋亡，和炎性细胞因子产生。作为CRH系统，我们定义了CRH-R1和CRH-R2受体及其亚型的天然和合成CRH和尿皮质素（UCN）激动剂和拮抗剂以及CRH伪受体CRH结合蛋白（BP）。本发明涉及使用CR改善或治疗炎性疾病的药物干预。系统介导的单核细胞/巨噬细胞的控制，其通过产生促炎细胞因子（例如白细胞介素（IL）-1，IL-6和肿瘤坏死因子（TNF））起始和维持炎症反应起关键作用。 α。在炎症的术语中，我们定义生物体对引起组织损伤的有害内源性或外源性刺激的反应。炎症是宿主防御机制，可能会伤害捍卫生物。本发明还提供了用于控制单核细胞/巨噬细胞系统的天然和合成CRH系统调节剂的体外和体内评估的方法。

5. 发明专利

EA021840B1 ПРИМЕНЕНИЕ СТЕРОИДНЫХ СОЕДИНЕНИЙ ПРИ ВОСПАЛИТЕЛЬНЫХ И АУТОИММУННЫХ ЗАБОЛЕВАНИЯХ 未知
公开(公告)号：EA021840B1
公开(公告)日：2015-09-30
申请号：EA201270399
申请日：2010-09-13
申请人： BIONATURE E A LTD
发明人： PANOUTSAKOPOULOU VASILIKI , ANGELAKOPOULOU MARIA , CALOGEROPOULOU THEODORA , GRAVANIS ACHILLEAS , LAZARIDIS LAKOVOS , NEOPHYTOU CONSTANTINOS
IPC分类号： A61K31/56 , A61K31/575 , A61P11/06 , A61P17/06 , A61P21/04 , A61P43/00
摘要： Данноеизобретениеотноситсяк способупрофилактикиилилечениявоспалительногосостояния, включающемувведениепациентуэффективногоколичествасоединения, выбранногоизследующих: 17β-спиро[5-андростен-17,2'-оксиран]-3β-ол; (20S)-3β,21-дигидрокси-17β,20-эпокси-5-прегнен; (20S)-3β-гидрокси-17β,20-эпокси-20-(2-бромэтинил)-5-андростен; 3β,21-дигидрокси-17α,20-эпокси-5-прегнени ихфармацевтическиприемлемыхэфирови фармацевтическиприемлемыхсолей, атакжек применениюуказанныхсоединенийдляпрофилактикиилилечениявоспалительногосостояния.

6. 发明专利

MX2012002834A USO DE COMPUESTOS ESTEROIDES PARA TRASTORNOS INFLAMATORIOS Y AUTOINMUNITARIOS. 未知
公开(公告)号：MX2012002834A
公开(公告)日：2012-04-10
申请号：MX2012002834
申请日：2010-09-13
申请人： BIONATURE E A LTD
发明人： GRAVANIS ACHILLEAS , CALOGEROPOULOU THEODORA , NEOPHYTOU CONSTANTINOS , PANOUTSAKOPOULOU VASILIKI , ANGELAKOPOULOU MARIA , LAZARIDIS LAKOVOS
IPC分类号： A61K31/56 , A61K31/575 , A61P11/06 , A61P17/06 , A61P21/04 , A61P43/00
摘要： Esta invención pertenece al uso de los compuestos esteroides, incluyendo análogos de espiroesteroide en el tratamiento, prevención o mejoramiento de los síntomas de condiciones inflamatorias. Los compuestos esteroides son útiles para tratar una gama de condiciones inflamatorias, incluyendo, pero no limitadas a, asma, inflamación pulmonar, condiciones inflamatorias retinales, trastornos autoinmunitarios tales como artritis reumatoide, diabetes tipo I, lupus eritematoso sistémico, colitis ulcerativa. y enfermedades inflamatorias del intestino y miopatías, así como esclerosis múltiple. Los compuestos activos son representados por la. Fórmula (I): en donde R1, R2, R3, R4, R5, R6, R7, A, B, X, Y y Z son como se definen en la descripción de la invención.

7. 发明专利

AU2008265046A1 Neurosteroid compounds 未知
公开(公告)号：AU2008265046A1
公开(公告)日：2008-12-24
申请号：AU2008265046
申请日：2008-06-17
申请人： BIONATURE E A LTD
发明人： MINAS VASSILIOS , ALEXIS MICHAEL N , GRAVANIS ACHILLEAS , CALOGEROPOULOU THEODORA , VERGOU VARVARA , AVLONITIS NIKOLAOS , CASTANAS ELIAS , CHARALAMBOPOULOS IOANNIS , NEOPHYTOU CONSTANTINOS , MARGIORIS ANDREAS , REMBOUTSIKA EUMORPHIA , TSATSANIS CHRISTOS , ALEXAKI VASILEIA-ISMINI
IPC分类号： A61K31/58 , A61P25/00 , A61P25/14 , A61P25/16 , C07J21/00

8. 发明专利

CA2670955A1 POTENTIATION OF ERYTHROPOIETIN (EPO) ACTION BY MEMBRANE STEROID RECEPTOR AGONISTS 未知
公开(公告)号：CA2670955A1
公开(公告)日：2008-06-05
申请号：CA2670955
申请日：2007-11-27
申请人： BIONATURE E A LTD
发明人： PELEKANOU VASSILIKI , KAMPA MARILENA , CASTANAS ELIAS
IPC分类号： A61K38/18 , A61K8/63 , A61K8/64 , A61K31/593
摘要： The present invention relates to the use of membrane steroid receptor ago nists as potentiators of the action of erythropoietin (EPO). The present inv ention also relates to the combined use of membrane steroid receptor agonist s and erythropoietin to control apoptosis, proliferation, differentiation, m igration and regeneration of cells, in different organs and tissues. Composi tions comprising (i) a membrane steroid receptor agonist and (ii) erythropoi etin are also provided, as are kits comprising (i) a membrane steroid recept or agonist and (ii) erythropoietin.

9. 发明专利

AU2007327099A1 Potentiation of erythropoietin (EPO) action by membrane steroid receptor agonists 未知
公开(公告)号：AU2007327099A1
公开(公告)日：2008-06-05
申请号：AU2007327099
申请日：2007-11-27
申请人： BIONATURE E A LTD
发明人： KAMPA MARILENA , CASTANAS ELIAS , PELEKANOU VASSILIKI
IPC分类号： A61K38/18 , A61K8/63 , A61K8/64 , A61K31/593
摘要： The present invention relates to the use of membrane steroid receptor agonists as potentiators of the action of erythropoietin (EPO). The present invention also relates to the combined use of membrane steroid receptor agonists and erythropoietin to control apoptosis, proliferation, differentiation, migration and regeneration of cells, in different organs and tissues. Compositions comprising (i) a membrane steroid receptor agonist and (ii) erythropoietin are also provided, as are kits comprising (i) a membrane steroid receptor agonist and (ii) erythropoietin.

10. 发明专利

AU2003302368B2 Use of the corticoliberin-urocortin system in the treatment of inflammatory diseases 未知
公开(公告)号：AU2003302368B2
公开(公告)日：2007-10-11
申请号：AU2003302368
申请日：2003-11-26
申请人： BIONATURE E A LTD
发明人： GRAVANIS ACHILLE , MARGIORIS ANDREW N
IPC分类号： A61K31/506 , A61K38/22 , A61K45/00 , A61P29/00 , G01N33/68
摘要： The invention relates to the use of corticotropin-releasing hormone (CRH) receptor-1 (R1) antagonists and/or CRH-R2 receptor agonists for the treatment of inflammatory diseases via regulation of monocyte/macrophage cell activation, proliferation, differentiation, apoptosis, and inflammatory cytokine production. As CRH system we define natural and synthetic CRH and urocortin (UCN) agonists and antagonists for the CRH-R1 and CRH-R2 receptors and their subtypes as well as the CRH-binding protein (BP), a CRH pseudo-receptor. The invention is directed towards pharmacological intervention for the amelioration or treatment of inflammatory diseases using the CRH system-mediated control of monocyte/macrophage cells which play a key role in initiating and maintaining the inflammatory response via production of pro-inflammatory cytokines such as is the interleukin (IL)-1, IL-6 and tumor necrosis factor (TNF)-alpha. By the term inflammation we define the response of an organism to noxious endogenous or exogenous stimuli causing tissue injury. Inflammation is a host defence mechanism, which might harm the defending organism. The invention also provides methods for the in vitro and in vivo evaluation of natural and synthetic CRH system modulators for the control of the monocyte/macrophage system.

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