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1. 发明授权

US09527881B2 Steroid analogues for neuroprotection 有权
标题翻译：用于神经保护的类固醇类似物
公开(公告)号：US09527881B2
公开(公告)日：2016-12-27
申请号：US12918036
申请日：2009-02-26
申请人： Christopher Macnevin , Donald G. Stein , Dennis C. Liotta , Iqbal Sayeed , David B. Guthrie , Mark A. Lockwood , Michael G. Natchus
发明人： Christopher Macnevin , Donald G. Stein , Dennis C. Liotta , Iqbal Sayeed , David B. Guthrie , Mark A. Lockwood , Michael G. Natchus
IPC分类号： A61K31/58 , A61K31/56 , A61P21/00 , C07G3/00 , C07J21/00 , C07J41/00 , C07J7/00 , C07J9/00
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

US20110263553A1 STEROID ANALOGUES FOR NEUROPROTECTION 有权
标题翻译：用于神经保护的甾体类似物
公开(公告)号：US20110263553A1
公开(公告)日：2011-10-27
申请号：US12918036
申请日：2009-02-26
申请人： Christopher Macnevin , Donald G. Stein , Dennis C. Liotta , Iqbal Sayeed , David B. Guthrie , Mark A. Lockwood , Michael G. Natchus
发明人： Christopher Macnevin , Donald G. Stein , Dennis C. Liotta , Iqbal Sayeed , David B. Guthrie , Mark A. Lockwood , Michael G. Natchus
IPC分类号： A61K31/58 , C07J7/00 , A61P21/00 , C07J21/00 , A61K31/56 , C07J41/00 , C07G3/00
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。

3. 发明申请

US20130310350A1 METHOD FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM CANCERS AND COMPOSITIONS RELATED THERETO 有权
标题翻译：治疗中枢神经系统癌症及其相关组合物的方法
公开(公告)号：US20130310350A1
公开(公告)日：2013-11-21
申请号：US13783706
申请日：2013-03-04
申请人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
发明人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
IPC分类号： A61K31/57
CPC分类号： A61K31/57 , A61K45/06 , A61K2300/00
摘要： Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.
摘要翻译：本文公开的化合物，通常是孕酮或其类似物或衍生物在治疗中枢神经系统癌症，特别是神经母细胞瘤和成胶质细胞瘤中的用途。与目前可用的化学治疗剂相比，该治疗提供了降低的毒性。孕酮可以单独施用或与其它治疗剂组合或联合施用。

4. 发明申请

US20140296195A1 METHOD FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM CANCERS AND COMPOSITIONS RELATED THERETO 审中-公开
标题翻译：治疗中枢神经系统癌症及其相关组合物的方法
公开(公告)号：US20140296195A1
公开(公告)日：2014-10-02
申请号：US14302038
申请日：2014-06-11
申请人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
发明人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
IPC分类号： A61K31/57 , A61K45/06
CPC分类号： A61K31/57 , A61K45/06 , A61K2300/00
摘要： Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.
摘要翻译：本文公开的化合物，通常是孕酮或其类似物或衍生物在治疗中枢神经系统癌症，特别是神经母细胞瘤和成胶质细胞瘤中的用途。与目前可用的化学治疗剂相比，该治疗提供了降低的毒性。孕酮可以单独施用或与其它治疗剂组合或联合施用。

5. 发明申请

US20120058978A1 METHOD FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM CANCERS AND COMPOSITIONS RELATED THERETO 有权
标题翻译：治疗中枢神经系统癌症及其相关组合物的方法
公开(公告)号：US20120058978A1
公开(公告)日：2012-03-08
申请号：US13222021
申请日：2011-08-31
申请人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
发明人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
IPC分类号： A61K31/57 , A61P35/00
CPC分类号： A61K31/57 , A61K45/06 , A61K2300/00
摘要： Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.
摘要翻译：本文公开的化合物，通常是孕酮或其类似物或衍生物在治疗中枢神经系统癌症，特别是神经母细胞瘤和成胶质细胞瘤中的用途。与目前可用的化学治疗剂相比，该治疗提供了降低的毒性。孕酮可以单独施用或与其它治疗剂组合或联合施用。

6. 发明申请

US20140221480A1 METHODS OF MANAGING BRAIN INFLAMMATION 审中-公开
标题翻译：管理脑炎的方法
公开(公告)号：US20140221480A1
公开(公告)日：2014-08-07
申请号：US14173942
申请日：2014-02-06
申请人： Fang Hua , Donald G. Stein , Iqbal Sayeed
发明人： Fang Hua , Donald G. Stein , Iqbal Sayeed
IPC分类号： A61K31/24
CPC分类号： A61K31/18
摘要： This disclosure relates to methods of managing brain injury such as inflammation due to trauma induced brain injury and ischemic stroke by administering resatorvid or derivative there of a subject in need thereof. In certain embodiments, the disclosure relates to methods of treating cerebral ischemia comprising administering an effective amount of resatorvid to a subject in need thereof. In certain embodiments, the effective amount is 3 mg/kg. In certain embodiments, resatorvid is administered by injection.
摘要翻译：本公开涉及通过在有需要的受试者施用resatorvid或衍生物来管理脑损伤（例如由于创伤诱导的脑损伤和缺血性中风引起的炎症）的方法。在某些实施方案中，本公开涉及治疗脑缺血的方法，包括向有需要的受试者施用有效量的resatorvid。在某些实施方案中，有效量为3mg / kg。在某些实施方案中，resatorvid通过注射施用。

7. 发明授权

US08778915B2 Method for the treatment of central nervous system cancers and compositions related thereto 有权
标题翻译：治疗中枢神经系统癌症及其相关组合物的方法
公开(公告)号：US08778915B2
公开(公告)日：2014-07-15
申请号：US13783706
申请日：2013-03-04
申请人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
发明人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
IPC分类号： A61K31/56
CPC分类号： A61K31/57 , A61K45/06 , A61K2300/00
摘要： Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.
摘要翻译：本文公开的化合物，通常是孕酮或其类似物或衍生物在治疗中枢神经系统癌症，特别是神经母细胞瘤和成胶质细胞瘤中的用途。与目前可用的化学治疗剂相比，该治疗提供了降低的毒性。孕酮可以单独施用或与其它治疗剂组合或联合施用。

8. 发明授权

US08435972B2 Method for the treatment of central nervous system cancers and compositions related thereto 有权
标题翻译：治疗中枢神经系统癌症及其相关组合物的方法
公开(公告)号：US08435972B2
公开(公告)日：2013-05-07
申请号：US13222021
申请日：2011-08-31
申请人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
发明人： Donald G. Stein , Iqbal Sayeed , Fahim Atif
IPC分类号： A61K31/56
CPC分类号： A61K31/57 , A61K45/06 , A61K2300/00
摘要： Use of compounds disclosed herein, typically progesterone or analog or derivative thereof, in the treatment of central nervous system cancers, specifically neuroblastoma and glioblastoma is provided. The treatment offers a reduced toxicity as compared to the currently available chemotherapeutic agents. The progesterone may be administered alone or in combination with, or in conjunction with other therapeutic agents.
摘要翻译：本文公开的化合物，通常是孕酮或其类似物或衍生物在治疗中枢神经系统癌症，特别是神经母细胞瘤和成胶质细胞瘤中的用途。与目前可用的化学治疗剂相比，该治疗提供了降低的毒性。孕酮可以单独施用或与其它治疗剂组合或联合施用。

9. 发明申请

US20080318914A1 METHODS FOR THE TREATMENT OF A TRAUMATIC CENTRAL NERVOUS SYSTEM INJURY 有权
标题翻译：治疗TRAUMATIC中枢神经系统损伤的方法
公开(公告)号：US20080318914A1
公开(公告)日：2008-12-25
申请号：US12117217
申请日：2008-05-08
申请人： Stuart W. Hoffman , Arthur L. Kellermann , Donald G. Stein , David W. Wright , Douglas W. Lowery-North
发明人： Stuart W. Hoffman , Arthur L. Kellermann , Donald G. Stein , David W. Wright , Douglas W. Lowery-North
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。

10. 发明申请

US20120289491A1 METHODS FOR THE TREATMENT OF A CENTRAL NERVOUS SYSTEM INJURY VIA A TAPERED ADMINISTRATION PROTOCOL 有权
标题翻译：通过管理管理协议处理中枢神经系统损伤的方法
公开(公告)号：US20120289491A1
公开(公告)日：2012-11-15
申请号：US13550148
申请日：2012-07-16
申请人： Donald G. Stein , Sarah Butler
发明人： Donald G. Stein , Sarah Butler
IPC分类号： A61K31/56 , A61P25/00
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。

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