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11. 发明申请

US20050261508A1 Aminosterol compounds useful as inhibitors of the sodium/proton exchanger (NHE), pharmaceutical methods and compositions employing such inhibitors, and processes for evaluating the NHE-inhibitory efficacy of compounds 审中-公开
标题翻译：可用作钠/质子交换剂（NHE）抑制剂的氨基甾醇化合物，使用这种抑制剂的药物方法和组合物，以及评价化合物的NHE抑制功效的方法
公开(公告)号：US20050261508A1
公开(公告)日：2005-11-24
申请号：US11046906
申请日：2005-02-01
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
IPC分类号： A61K31/56 , C07J9/00 , C07J41/00 , G01N33/50
CPC分类号： G01N33/5011 , A61K31/56 , C07J9/00 , C07J41/0005 , G01N33/5008 , G01N33/5044 , G01N33/505 , G01N33/5061 , G01N33/5064 , G01N33/5088 , G01N33/5091 , G01N2500/00
摘要： Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.
摘要翻译：描述了可用作钠/质子交换器（NHE）的抑制剂的氨基甾醇化合物。还包括使用这种氨基甾醇化合物的方法，包括使用作为NHE光谱抑制剂的化合物的那些以及仅使用一种特异性NHE抑制剂的化合物。还公开了有利的筛选技术和用于评价化合物治疗活性的测定法。

12. 发明授权

US06962909B2 Treatment of neovascularization disorders with squalimine 失效
标题翻译：用squalimine治疗新生血管形成障碍
公开(公告)号：US06962909B2
公开(公告)日：2005-11-08
申请号：US09985417
申请日：2001-11-02
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
IPC分类号： A61K31/56 , C07J9/00 , C07J41/00 , G01N33/50 , C07C305/12
CPC分类号： G01N33/5011 , A61K31/56 , C07J9/00 , C07J41/0005 , G01N33/5008 , G01N33/5044 , G01N33/505 , G01N33/5061 , G01N33/5064 , G01N33/5088 , G01N33/5091 , G01N2500/00
摘要： Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.
摘要翻译：描述了可用作钠/质子交换器（NHE）的抑制剂的氨基甾醇化合物。还包括使用这种氨基甾醇化合物的方法，包括使用作为NHE光谱抑制剂的化合物的那些以及仅使用一种特异性NHE抑制剂的化合物。还公开了有利的筛选技术和用于评价化合物治疗活性的测定法。

13. 发明授权

US06388108B1 Aminosterol compounds and uses thereof 失效
标题翻译：氨基甾醇化合物及其用途
公开(公告)号：US06388108B1
公开(公告)日：2002-05-14
申请号：US09762999
申请日：2001-05-29
申请人： Meena Rao , Binyamin Feibush , William Kinney , Michael Zasloff , Lincoln Noecker
发明人： Meena Rao , Binyamin Feibush , William Kinney , Michael Zasloff , Lincoln Noecker
IPC分类号： A61K3156
CPC分类号： A61K31/575 , Y02A50/473
摘要： Newly isolated aminosterol compounds and pharmaceutical compositions based on the aminosterol compounds are described. Methods for the treatment of various disorders, for example, a microbial infection, are also described.
摘要翻译：描述了基于氨基甾醇化合物的新分离的氨基甾醇化合物和药物组合物。还描述了治疗各种病症的方法，例如微生物感染。

14. 发明授权

US5847172A Certain aminosterol compounds and pharmaceutical compositions including these compounds 失效
公开(公告)号：US5847172A
公开(公告)日：1998-12-08
申请号：US487443
申请日：1995-06-07
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
IPC分类号： A61K31/56 , C07J9/00 , C07J41/00 , G01N33/50
CPC分类号： G01N33/5011 , A61K31/56 , C07J41/0005 , C07J9/00 , G01N33/5008 , G01N33/5044 , G01N33/505 , G01N33/5061 , G01N33/5064 , G01N33/5088 , G01N33/5091 , G01N2500/00
摘要： Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.

15. 发明授权

US5795885A Method of inhibiting profileration of cells by administering an aminosterol compound 失效
标题翻译：通过施用氨基甾醇化合物抑制细胞增殖的方法
公开(公告)号：US5795885A
公开(公告)日：1998-08-18
申请号：US483057
申请日：1995-06-07
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Mark Anderson , Jon Williams , Michael McLane
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Mark Anderson , Jon Williams , Michael McLane
IPC分类号： C07J41/00 , G01N33/50 , A61K31/56
CPC分类号： G01N33/5011 , C07J41/0005 , G01N33/5008 , G01N33/5044 , G01N33/5047 , G01N33/5061 , G01N33/5064 , G01N33/5088 , G01N2500/00
摘要： Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also disclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.
摘要翻译：描述了可用作钠/质子交换器（NHE）的抑制剂的氨基甾醇化合物。还公开了使用这种氨基甾醇化合物的方法，包括那些使用作为NHE光谱的抑制剂的化合物以及仅使用一种特异性NHE抑制剂的化合物的方法。还公开了有利的筛选技术和用于评价化合物治疗活性的测定法。

16. 发明申请

US20130281419A1 Therapeutic Uses for an Aminosterol Compound 有权
标题翻译：氨基甾醇化合物的治疗用途
公开(公告)号：US20130281419A1
公开(公告)日：2013-10-24
申请号：US13673500
申请日：2012-11-09
申请人： Michael Zasloff , Jon Williams , William Kinney , Mark Anderson , Michael McLane
发明人： Michael Zasloff , Jon Williams , William Kinney , Mark Anderson , Michael McLane
IPC分类号： A61K31/575
CPC分类号： A61K31/575 , C07J41/0055
摘要： A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436 as shown in FIG. 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. Various pharmaceutical products may be produced including this pharmaceutical composition. Such pharmaceutical products may be used for the treatment of obesity or diabetes. Methods for using the pharmaceutical compositions also are described. In these methods, various diseases are treated or other body functions are activated or inhibited by administering an effective amount of the pharmaceutical composition. For example, diabetes and obesity may be treated by administering an effective amount of the pharmaceutical compositions. Weight gain and growth factor production can be inhibited by administering an effective amount of these pharmaceutical compositions. Appetite can be suppressed by administering an effective amount of the pharmaceutical compositions, and a diuretic effect can be produced.
摘要翻译：药物组合物包含作为活性成分的如图14所示的根据式1436的化合物。 1，或其药学上可接受的盐，和药学上可接受的载体或赋形剂。可以生产包括该药物组合物的各种药物。这样的药物可以用于治疗肥胖或糖尿病。还描述了使用药物组合物的方法。在这些方法中，通过施用有效量的药物组合物来治疗各种疾病或其他身体功能被激活或抑制。例如，可以通过施用有效量的药物组合物来治疗糖尿病和肥胖症。通过施用有效量的这些药物组合物可以抑制体重增加和生长因子产生。可以通过施用有效量的药物组合物来抑制食欲，并且可以产生利尿作用。

17. 发明授权

US07410959B1 Therapeutic uses for aminosterol compounds 有权
标题翻译：氨基甾醇化合物的治疗用途
公开(公告)号：US07410959B1
公开(公告)日：2008-08-12
申请号：US09885247
申请日：2000-07-13
申请人： Michael Zasloff , Jon Williams , William Kinney , Mark Anderson , Michael McLane
发明人： Michael Zasloff , Jon Williams , William Kinney , Mark Anderson , Michael McLane
IPC分类号： A61K31/56 , A61K31/555 , A01N55/02 , C07J41/00
CPC分类号： A61K31/575 , C07J41/0055
摘要： A pharmaceutical composition includes, as an active ingredient, a compound according to formula 1436 as shown in FIG. 1, or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or excipient. Various pharmaceutical products may be produced including this pharmaceutical composition. Such pharmaceutical products may be used for the treatment of obesity or diabetes. Methods for using the pharmaceutical compositions also are described. In these methods, various diseases are treated or other body functions are activated or inhibited by administering an effective amount of the pharmaceutical composition. For example, diabetes and obesity may be treated by administering an effective amount of the pharmaceutical compositions. Weight gain, and growth factor production can be inhibited by administering an effective amount of these pharmaceutical compositions. Appetite can be suppressed by administering an effective amount of the pharmaceutical compositions, and a diuretic effect can be produced.
摘要翻译：药物组合物包含作为活性成分的如图14所示的根据式1436的化合物。 1，或其药学上可接受的盐，和药学上可接受的载体或赋形剂。可以生产包括该药物组合物的各种药物。这样的药物可以用于治疗肥胖或糖尿病。还描述了使用药物组合物的方法。在这些方法中，通过施用有效量的药物组合物来治疗各种疾病或其他身体功能被激活或抑制。例如，可以通过施用有效量的药物组合物来治疗糖尿病和肥胖症。通过施用有效量的这些药物组合物可以抑制体重增加和生长因子产生。可以通过施用有效量的药物组合物来抑制食欲，并且可以产生利尿作用。

18. 发明申请

US20070088003A1 Asthma associated factors as targets for treating atopic allergies including asthma and related disorders 审中-公开
标题翻译：哮喘相关因素作为治疗特应性过敏的目标，包括哮喘和相关疾病
公开(公告)号：US20070088003A1
公开(公告)日：2007-04-19
申请号：US11401469
申请日：2006-04-11
申请人： Roy Levitt , Nicholas Nicolaides , William Kinney , Steve Jones
发明人： Roy Levitt , Nicholas Nicolaides , William Kinney , Steve Jones
IPC分类号： A61K31/585 , A61K31/58 , A61K31/66 , A61K31/56
CPC分类号： A61K31/56 , A61K31/58 , A61K31/66 , C07J17/00 , C07J41/0005 , C07J41/0055 , C07J41/0061 , C07J43/003 , C07J51/00 , G01N33/5047 , G01N2333/54 , Y10S514/826
摘要： This invention relates to methods for treating asthma or allergy in a mammal by administering a 3-aminosteroid compound to a mammal in need thereof. The 3-aminosteroid compound being capable of down regulating the IL-9 pathway and alleviating asthmatic responses to allergen. Exemplary 3-aminosteroid compounds used in the methods of the invention include compounds having the chemical formula (I), wherein X, R1, R2, R3, and R4 groups are as defined herein. The invention also relates to certain novel compounds of formula (I). Moreover, the invention also provides methods for identifying an immunomodulatory 3-aminosteroid compound.
摘要翻译：本发明涉及通过向有需要的哺乳动物施用3-氨基甾体化合物来治疗哺乳动物的哮喘或变态反应的方法。 3-氨基甾体化合物能够下调IL-9途径并减轻对变应原的哮喘反应。用于本发明方法的示例性3-氨基甾体化合物包括具有化学式（I）的化合物，其中X，R 1，R 2，R 3，和/或<！ - SIPO - >如下所定义。本发明还涉及某些新的式（I）化合物。此外，本发明还提供了鉴定免疫调节性3-氨基甾体化合物的方法。

19. 发明申请

US20060183928A1 Aminosterol compounds useful as inhibitors of the sodium/proton exchanger (NHE), pharmaceutical methods and compositions employing such inhibitors, and processes for evaluating the NHE-inhibitory efficacy of compounds 审中-公开
公开(公告)号：US20060183928A1
公开(公告)日：2006-08-17
申请号：US10824661
申请日：2004-04-15
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Steven Jones
IPC分类号： C07J41/00
CPC分类号： G01N33/5011 , A61K31/56 , C07J9/00 , C07J41/0005 , G01N33/5008 , G01N33/5044 , G01N33/505 , G01N33/5061 , G01N33/5064 , G01N33/5088 , G01N33/5091 , G01N2500/00
摘要： Aminosterol compounds are described that are useful as inhibitors of the sodium/proton exchanger (NHE). Methods of using such aminosterols compounds are also enclosed, including those employing compounds that are inhibitors of a spectrum of NHEs as well as those using compounds that are inhibitors of only one specific NHE. Advantageous screening techniques and assays for evaluating a compound's therapeutic activity are also disclosed.

20. 发明申请

US20050187202A1 Regioselective and stereoselective oxidation of fused ring systems useful for the preparation of aminosterols 有权
标题翻译：用于制备氨基甾醇的稠环系统的区域选择性和立体选择性氧化
公开(公告)号：US20050187202A1
公开(公告)日：2005-08-25
申请号：US11083961
申请日：2005-03-21
申请人： William Kinney , Xuehai Zhang , Ronald Michalak
发明人： William Kinney , Xuehai Zhang , Ronald Michalak
IPC分类号： C07B61/00 , C07J9/00 , C07J21/00 , C07J31/00 , C07J41/00 , A61K31/56
CPC分类号： C07J9/00 , C07J21/006 , C07J31/006 , C07J41/0005
摘要： An efficient method for the synthesis of aminosterol compounds such as squalamine and compound 1436 is described. A method of the invention provides for regioselective sulfonation of a fused ring system. The fused ring system base can be, for example, a steroid ring base. The aminosterol compounds are effective as, among others, antibiotics, antiangiogenic agents and NHE3 inhibitors.
摘要翻译：描述了合成氨基甾醇化合物如角鲨胺和化合物1436的有效方法。本发明的方法提供稠环系统的区域选择性磺化。稠环系统碱可以是例如类固醇环基。氨基甾醇化合物尤其是抗生素，抗血管生成剂和NHE3抑制剂是有效的。

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