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1. 发明申请

WO2009108804A2 STEROID ANALOGUES FOR NEUROPROTECTION 审中-公开
标题翻译：用于神经保护的甾体类似物
公开(公告)号：WO2009108804A2
公开(公告)日：2009-09-03
申请号：PCT/US2009035336
申请日：2009-02-26
申请人： UNIV EMORY , MACNEVIN CHRISTOPHER , STEIN DONALD G , LIOTTA DENNIS C , SAYEED IQBAL , GUTHRIE DAVID B , LOCKWOOD MARK A , NATCHUS MICHAEL G
发明人： MACNEVIN CHRISTOPHER , STEIN DONALD G , LIOTTA DENNIS C , SAYEED IQBAL , GUTHRIE DAVID B , LOCKWOOD MARK A , NATCHUS MICHAEL G
IPC分类号： C07J9/00 , A61P25/00
CPC分类号： A61K31/573 , C07J9/00
摘要： Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid analogues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.
摘要翻译：提供的是在类固醇环系统的C3和/或C20位置上被极性取代基官能化的类固醇类似物，其具有改善的水溶性。还提供了包含类固醇类似物的药物组合物和使用新型类固醇类似物在中枢神经系统损伤后治疗和预防患者神经变性的方法。

2. 发明申请

WO2008039898A2 METHODS FOR THE TREATMENT OF A TRAUMATIC CENTRAL NERVOUS SYSTEM INJURY 审中-公开
标题翻译：治疗TRAUMATIC中枢神经系统损伤的方法
公开(公告)号：WO2008039898A2
公开(公告)日：2008-04-03
申请号：PCT/US2007079655
申请日：2007-09-27
申请人： UNIV EMORY , STEIN DONALD G , LOWERY-NORTH DOUGLAS W , WRIGHT DAVID W , HOFFMAN STUART W , KELLERMANN ARTHUR L
发明人： STEIN DONALD G , LOWERY-NORTH DOUGLAS W , WRIGHT DAVID W , HOFFMAN STUART W , KELLERMANN ARTHUR L
IPC分类号： A61K31/57 , A61P25/00
CPC分类号： A61K31/57
摘要： Methods of treating a subject with a traumatic central nervous system injury, more particularly, a traumatic brain injury, are provided. The methods comprise a therapy comprising a constant or a two-level dosing regime of progesterone. In one method, a subject in need thereof is administered at least one cycle of therapy, wherein the cycle of therapy comprises administering a therapeutically effective two- level intravenous dosing regime of progesterone. The two-level dosing regime comprises a first time period, wherein a higher hourly dose of progesterone is administered to the subject, followed by a second time period, wherein a lower hourly dose of progesterone is administered to the subject.
摘要翻译：提供了用创伤性中枢神经系统损伤治疗受试者的方法，更具体地说，是创伤性脑损伤。所述方法包括包含孕酮恒定或两级给药方案的治疗。在一种方法中，需要治疗的受试者至少进行一次治疗循环，其中治疗循环包括施用孕酮的治疗有效的两级静脉内给药方案。两级给药方案包括第一时间段，其中向受试者施用较高剂量的孕酮，随后是第二时间段，其中向受试者施用较小时剂量的孕酮。

3. 发明申请

WO2010088409A3 METHODS OF NEUROPROTECTION USING NEUROPROTECTIVE STEROIDS AND A VITAMIN D 审中-公开
标题翻译：使用神经保护性甾体和维生素D进行神经保护的方法
公开(公告)号：WO2010088409A3
公开(公告)日：2011-02-17
申请号：PCT/US2010022433
申请日：2010-01-28
申请人： UNIV EMORY , STEIN DONALD G
发明人： STEIN DONALD G
IPC分类号： A61K31/56 , A61K31/59 , A61P25/00 , A61P25/16 , A61P25/28
CPC分类号： A61K31/592 , A61K31/56 , A61K31/593 , A61K2300/00
摘要： Described herein are compositions and methods for treating or preventing nervous system injury. In particular, the methods and compositions relate to the use of at least one neuroprotective steroid, such as progesterone, and vitamin D.
摘要翻译：本文描述了用于治疗或预防神经系统损伤的组合物和方法。特别地，所述方法和组合物涉及使用至少一种神经保护类固醇，例如孕酮和维生素D.

4. 发明申请

WO2006102644A9 METHODS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM INJURY VIA A TAPERED ADMINISTRATION PROTOCOL 审中-公开
标题翻译：通过锥形给药方案治疗中枢神经系统损伤的方法
公开(公告)号：WO2006102644A9
公开(公告)日：2006-11-23
申请号：PCT/US2006010984
申请日：2006-03-24
申请人： UNIV EMORY , STEIN DONALD G , CUTLER SARAH MELISSA
发明人： STEIN DONALD G , CUTLER SARAH MELISSA
CPC分类号： A61K31/57
摘要： The present invention provides methods for the treatment or the prevention of neuronal damage in the CNS. Specifically, the methods of the invention provide for the administration of a therapeutically effective amount of a progestin or progestin metabolite following a traumatic or ischemic injury to the CNS such that, prior to termination of administration of the progestin or progestin metabolite the administration is tapered to avoid withdrawal. The drug taper employed can involve a linear taper, an exponential taper, progressively dividing administered doses by 50%, or can be determined based on the treating physician's assessment of the patient's response to therapy. The tapered administration methods of the present invention may be used in combination with any therapeutic protocol or regimen for the administration of a therapeutically effective amount of a progestin or progestin metabolite to treat a traumatic or ischemic CNS injury.
摘要翻译：本发明提供了用于治疗或预防CNS中的神经元损伤的方法。具体而言，本发明的方法提供了在对CNS的创伤或缺血性损伤后施用治疗有效量的孕酮或孕激素代谢物，使得在施用孕激素或孕激素代谢物之前，施用逐渐减少至避免退出。所采用的药物锥度可以包括线性锥度，指数锥度，逐渐分配给药剂量50％，或者可以根据治疗医生对患者对治疗的反应的评估来确定。本发明递减给药方法可与用于治疗有效量的孕激素或孕激素代谢物的任何治疗方案或方案联合使用，以治疗创伤性或局部缺血性CNS损伤。

5. 发明申请

WO2006102644A3 METHODS FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM INJURY VIA A TAPERED ADMINISTRATION OF PROGESTERONE 审中-公开
标题翻译：用于治疗中枢神经系统损伤的方法
公开(公告)号：WO2006102644A3
公开(公告)日：2007-03-01
申请号：PCT/US2006010984
申请日：2006-03-24
申请人： UNIV EMORY , STEIN DONALD G , CUTLER SARAH MELISSA
发明人： STEIN DONALD G , CUTLER SARAH MELISSA
IPC分类号： A61K31/57 , A61P25/00 , A61P25/28
CPC分类号： A61K31/57
摘要： The present invention provides methods for the treatment or the prevention of neuronal damage in the CNS. Specifically, the methods of the invention provide for the administration of a therapeutically effective amount of a progestin or progestin metabolite following a traumatic or ischemic injury to the CNS such that, prior to termination of administration of the progestin or progestin metabolite the administration is tapered to avoid withdrawal. The drug taper employed can involve a linear taper, an exponential taper, progressively dividing administered doses by 50%, or can be determined based on the treating physician's assessment of the patient's response to therapy. The tapered administration methods of the present invention may be used in combination with any therapeutic protocol or regimen for the administration of a therapeutically effective amount of a progestin or progestin metabolite to treat a traumatic or ischemic CNS injury.
摘要翻译：本发明提供了治疗或预防CNS神经元损伤的方法。具体来说，本发明的方法提供了在对CNS的创伤性或缺血性损伤后给予治疗有效量的孕激素或孕激素代谢物，使得在终止施用孕激素或孕激素代谢物之前，给药被逐渐变细避免退出。所使用的药物锥度可以包括线性锥度，指数锥度，逐渐将施用剂量除以50％，或者可以基于治疗医师对患者对治疗反应的评估来确定。本发明的锥形给药方法可以与用于施用治疗有效量的孕激素或孕激素代谢物以治疗创伤性或缺血性CNS损伤的任何治疗方案或方案组合使用。

6. 发明申请

WO2006102596A3 DOSAGE REGIMEN FOR THE TREATMENT OF A TRAUMATIC BRAIN INJURY WITH PROGESTERONE 审中-公开
标题翻译：用于治疗与前列腺素的TRAUMATIC脑损伤的剂量方案
公开(公告)号：WO2006102596A3
公开(公告)日：2007-01-18
申请号：PCT/US2006010797
申请日：2006-03-24
申请人： UNIV EMORY , HOFFMAN STUART W , KELLERMANN ARTHUR L , STEIN DONALD G , WRIGHT DAVID W , LOWERY-NORTH DOUGLAS W
发明人： HOFFMAN STUART W , KELLERMANN ARTHUR L , STEIN DONALD G , WRIGHT DAVID W , LOWERY-NORTH DOUGLAS W
IPC分类号： A61K31/57 , A61P25/00 , A61P25/28
CPC分类号： A61K31/57
摘要： Methods of treating a subject with a traumatic central nervous system injury, more particularly, a traumatic brain injury, are provided. The methods comprise a therapy comprising a constant or a two-level dosing regime of progesterone. In one method, a subject in need thereof is administered at least one cycle of therapy, wherein the cycle of therapy comprises administering a therapeutically effective two-level intravenous dosing regime of progesterone. The two-level dosing regime comprises a first time period, wherein a higher hourly dose of progesterone is administered to the subject, followed by a second time period, wherein a lower hourly dose of progesterone is administered to the subject.
摘要翻译：提供了用创伤性中枢神经系统损伤治疗受试者的方法，更具体地说，是创伤性脑损伤。所述方法包括包含孕酮恒定或两级给药方案的治疗。在一种方法中，需要治疗的受试者至少进行一次治疗循环，其中治疗循环包括施用孕酮的治疗有效的两级静脉内给药方案。两级给药方案包括第一时间段，其中向受试者施用较高剂量的孕酮，随后是第二时间段，其中向受试者施用较小时剂量的孕酮。

7. 发明公开

EP3033350A4 PROGESTERONE PHOSPHATE ANALOGS AND USES RELATED THERETO 有权转让
标题翻译：孕酮磷酸酯类似物和相关的应用
公开(公告)号：EP3033350A4
公开(公告)日：2017-03-15
申请号：EP14835820
申请日：2014-08-11
申请人： UNIV EMORY
发明人： GUTHRIE DAVID BRIAN , LOCKWOOD MARK ANDREW , NATCHUS MICHAEL G , LIOTTA DENNIS C , STEIN DONALD G , SAYEED IQBAL
IPC分类号： C07J71/00 , A61K31/56 , A61P25/00 , C07J7/00
CPC分类号： C07J41/0016 , A61K31/57 , A61K31/58 , A61K31/661 , A61K45/06 , C07J41/005 , C07J43/003 , C07J51/00 , A61K2300/00
摘要： This disclosure relates to progesterone phophate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke.

8. 发明公开

EP2260052A4 STEROID ANALOGUES FOR NEUROPROTECTION 审中-公开
标题翻译：类固醇类似物用于神经保护
公开(公告)号：EP2260052A4
公开(公告)日：2013-01-16
申请号：EP09715569
申请日：2009-02-26
申请人： UNIV EMORY
发明人： MACNEVIN CHRISTOPHER , STEIN DONALD G , LIOTTA DENNIS C , SAYEED IQBAL , GUTHRIE DAVID B , LOCKWOOD MARK A , NATCHUS MICHAEL G
IPC分类号： C07J9/00 , A61P25/00
CPC分类号： A61K31/573 , C07J9/00

9. 发明专利

CA2716095C STEROID ANALOGUES FOR NEUROPROTECTION 未知
公开(公告)号：CA2716095C
公开(公告)日：2017-02-07
申请号：CA2716095
申请日：2009-02-26
申请人： UNIV EMORY
发明人： MACNEVIN CHRISTOPHER , STEIN DONALD G , LIOTTA DENNIS C , SAYEED IQBAL , GUTHRIE DAVID B , LOCKWOOD MARK A , NATCHUS MICHAEL G
IPC分类号： C07J41/00 , A61P25/00 , C07J43/00
摘要： Provided are steroid analogues functionalized with polar substituents at the C3 and/or C20 positions of the steroid ring system that exhibit improved water solubility. Also provided are pharmaceutical compositions comprising the steroid ana-logues and methods using the novel steroid analogues for the treatment and prevention of neurodegeneration in a patient following injury to the central nervous system.

10. 发明专利

PL1868614T3 Schemat dawkowania do leczenia urazowego uszkodzenia mózgu progesteronem 未知
公开(公告)号：PL1868614T3
公开(公告)日：2013-01-31
申请号：PL06748657
申请日：2006-03-24
申请人： UNIV EMORY
发明人： HOFFMAN STUART W , KELLERMANN ARTHUR L , STEIN DONALD G , WRIGHT DAVID W , LOWERY-NORTH DOUGLAS W , CUTLER SARAH MELISSA
IPC分类号： A61K31/57 , A61P25/00 , A61P25/28

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