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1. 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。

2. 发明申请

US20080221075A1 Therapeutic Uses For Aminosterol Compounds 审中-公开
标题翻译：氨基甾醇化合物的治疗用途
公开(公告)号：US20080221075A1
公开(公告)日：2008-09-11
申请号：US12041440
申请日：2008-03-03
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 , C07J41/00 , A61P3/04
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。

3. 发明申请

US20050026917A1 Tricyclic indanyls as integrin inhibitors 有权
标题翻译：三环茚满酮作为整合素抑制剂
公开(公告)号：US20050026917A1
公开(公告)日：2005-02-03
申请号：US10900764
申请日：2004-07-28
申请人： William Kinney , Diane Luci , Bruce Maryanoff
发明人： William Kinney , Diane Luci , Bruce Maryanoff
IPC分类号： A61P9/10 , A61P35/04 , C07D401/12 , C07D471/04 , A61K31/53 , A61K31/519 , C07D487/02
CPC分类号： C04B35/632 , C07D401/12 , C07D471/04
摘要： The present invention is directed to substituted indanyl compounds of Formula (I): Useful for treating integrin-mediated disorders such as, but not limited to unstable angina, thromboemboic disorders, osteoporosis, growth and metastasis of malignant tumors, diabetic retinopathy, arthritis, viral disease and surgical adhesions.
摘要翻译：本发明涉及式（I）的取代的茚满基化合物：可用于治疗整联蛋白介导的病症，例如但不限于不稳定性心绞痛，血栓栓塞障碍，骨质疏松症，恶性肿瘤的生长和转移，糖尿病性视网膜病变，关节炎，病毒疾病和手术粘连。

4. 发明授权

US5840740A Aminosterol compounds and a method of treating infection using the aminosterol compounds 失效
标题翻译：氨基甾醇化合物和使用氨基酯化合物治疗感染的方法
公开(公告)号：US5840740A
公开(公告)日：1998-11-24
申请号：US483059
申请日：1995-06-07
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Meena Rao
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Meena Rao
IPC分类号： C07J41/00 , G01N33/50 , A01K31/575 , A07J41/00
CPC分类号： G01N33/5011 , C07J41/0005 , G01N33/5008 , G01N33/505 , G01N33/5061 , G01N33/5064 , G01N33/5088 , G01N33/5091 , G01N2500/00
摘要： Disclosed are aminosterol compounds 1360 and 1361: ##STR1## which can be obtained in isolated or purified form from the liver of the dogfish shark.
摘要翻译：公开的氨基甾醇化合物1360和1361：可以从狗鱼的肝脏中分离或纯化的形式获得。

5. 发明申请

US20090105204A1 Therapeutic Uses for Aminosterol Compounds 审中-公开
标题翻译：氨基甾醇化合物的治疗用途
公开(公告)号：US20090105204A1
公开(公告)日：2009-04-23
申请号：US12254656
申请日：2008-10-20
申请人： Michael Zasloff , Jon Wiliams , William Kinney , Mark Anderson , Michael McLane
发明人： Michael Zasloff , Jon Wiliams , William Kinney , Mark Anderson , Michael McLane
IPC分类号： A61K31/575 , A61P9/10 , A61P3/10 , A61P3/04
CPC分类号： C07J41/0005 , A61K31/575
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。

6. 发明授权

US5994336A Method of inhibiting proliferation 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：US5994336A
公开(公告)日：1999-11-30
申请号：US479455
申请日：1995-06-07
申请人： Michael Zasloff , Ann Shinnar , William Kinney , Meena Rao
发明人： Michael Zasloff , Ann Shinnar , William Kinney , Meena Rao
IPC分类号： C07J41/00 , G01N33/50 , A61K31/575
CPC分类号： G01N33/5044 , C07J41/0005 , G01N33/5008 , G01N33/5011 , G01N33/5047 , G01N33/5061 , G01N33/5088 , G01N33/5091 , G01N2500/00
摘要： A method of inhibiting the proliferation of a wide variety of cells is described. This method includes administering an effective amount of a compound having the following structure: ##STR1## or a pharmaceutically acceptable salt thereof. The proliferation of the following types of cells can be inhibited by this method: lymphocytes, fibroblasts, epithelial cells, smooth muscle cells, and human ovarian cancer cells.
摘要翻译：描述了抑制多种细胞增殖的方法。该方法包括给予有效量的具有以下结构的化合物：或其药学上可接受的盐。通过这种方法可以抑制以下类型细胞的增殖：淋巴细胞，成纤维细胞，上皮细胞，平滑肌细胞和人卵巢癌细胞。

7. 发明授权

US5856535A Aminosterol ester compounds 失效
标题翻译：氨基甾醇酯化合物
公开(公告)号：US5856535A
公开(公告)日：1999-01-05
申请号：US769689
申请日：1996-12-18
申请人： Michael Zasloff , William Kinney , Steven Jones
发明人： Michael Zasloff , William Kinney , Steven Jones
IPC分类号： A61K31/575 , A61K31/58 , A61P35/00 , C07J41/00 , C07J43/00
CPC分类号： C07J41/0005 , C07J43/003
摘要： An aminosterol compound according to the following formula: ##STR1## wherein: R.sub.1 is a member selected from the group of: ##STR2## R.sub.2 is H or OH; R.sub.3 is H or OH;R.sub.4 is H or OH; andR.sub.5 is a C.sub.1 to C.sub.12 alkyl group.Preferably, R.sub.5 is a C.sub.1 to C.sub.6 alkyl group, and a methyl group is particularly preferred.
摘要翻译：根据下式的氨基甾醇化合物：其中：R 1是选自以下的成员：其中R 1是H或OH; R3是H或OH; R4是H或OH; R5为C1〜C12烷基。优选地，R 5是C 1〜C 6烷基，特别优选甲基。

8. 发明申请

US20080039454A1 Urotensin II receptor antagonists 失效
标题翻译：促肾上腺素II受体拮抗剂
公开(公告)号：US20080039454A1
公开(公告)日：2008-02-14
申请号：US11881268
申请日：2007-07-26
申请人： Shyamali Ghosh , William Kinney , Edward Lawson , Diane Luci , Bruce Maryanoff , Francois Sommen , Yongchun Pan
发明人： Shyamali Ghosh , William Kinney , Edward Lawson , Diane Luci , Bruce Maryanoff , Francois Sommen , Yongchun Pan
IPC分类号： A61K31/538 , A61K31/4709 , A61P13/00 , A61P25/00 , A61P9/00 , C07D401/06 , C07D413/06
CPC分类号： C07D413/06 , C07D401/06 , C07D413/14 , C07D451/02
摘要： The invention is directed to Urotensin II receptor antagonists. More specifically, the present invention relates to certain novel compounds and methods for preparing compounds, compositions, intermediates and derivatives thereof. Pharmaceutical compositions and methods for treating or ameliorating a Urotensin-II mediated disorder using compounds of the invention are also described.
摘要翻译：本发明涉及尿激素II受体拮抗剂。更具体地，本发明涉及某些新化合物及其制备方法，其组合物，中间体及其衍生物。还描述了使用本发明的化合物治疗或改善促rotensin-II介导的病症的药物组合物和方法。

9. 发明申请

US20060166950A1 Treatment of neovascularization disorders with squalamine 审中-公开
标题翻译：用石斑鱼治疗新生血管形成障碍
公开(公告)号：US20060166950A1
公开(公告)日：2006-07-27
申请号：US11376117
申请日：2006-03-16
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 , 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.
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。

10. 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。

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