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1. 发明申请

US20060211728A1 Thalidomide analogs 有权
公开(公告)号：US20060211728A1
公开(公告)日：2006-09-21
申请号：US10572485
申请日：2004-09-17
申请人： Nigel Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William Figg
发明人： Nigel Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William Figg
IPC分类号： A61K31/4745 , A61K31/4709 , A61K31/454 , A61K31/4439 , C07D403/02
CPC分类号： C07D209/44 , C07D209/46 , C07D211/84 , C07D211/86 , C07D211/88 , C07D401/04 , C07D413/04 , C07D471/04
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.

2. 发明申请

US20130035363A1 Thalidomide Analogs 有权
标题翻译：沙利度胺类似物
公开(公告)号：US20130035363A1
公开(公告)日：2013-02-07
申请号：US13648625
申请日：2012-10-10
申请人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
发明人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
IPC分类号： A61K31/4035 , A61P3/04 , A61P19/02 , A61P31/04 , A61P1/00 , A61P35/00 , A61P25/00 , A61P25/28 , A61P25/16 , A61P7/04 , A61P27/02 , A61P29/00 , A61P1/04
CPC分类号： H04M1/72522 , C07D209/44 , G06F3/01 , G06F3/0346 , H04M2250/12 , H04M2250/22 , H04M2250/74
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNFα) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
摘要翻译：公开了调节肿瘤坏死因子α（TNFα）活性和血管生成的沙利度胺类似物。在特别公开的实施方案中，沙利度胺类似物是等熵含硫类似物。还公开了用类似物治疗受试者的方法。

3. 发明授权

US07973057B2 Thalidomide analogs 有权
标题翻译：沙利度胺类似物
公开(公告)号：US07973057B2
公开(公告)日：2011-07-05
申请号：US10572485
申请日：2004-09-17
申请人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
发明人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： C07D209/44 , C07D209/46 , C07D211/84 , C07D211/86 , C07D211/88 , C07D401/04 , C07D413/04 , C07D471/04
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
摘要翻译：公开了调节肿瘤坏死因子α（TNF-α）活性和血管发生的沙利度胺类似物。在特别公开的实施方案中，沙利度胺类似物是等熵含硫类似物。还公开了用类似物治疗受试者的方法。

4. 发明授权

US08546430B2 Thalidomide analogs 有权
标题翻译：沙利度胺类似物
公开(公告)号：US08546430B2
公开(公告)日：2013-10-01
申请号：US13153355
申请日：2011-06-03
申请人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
发明人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： C07D209/44 , C07D209/46 , C07D211/84 , C07D211/86 , C07D211/88 , C07D401/04 , C07D413/04 , C07D471/04
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
摘要翻译：公开了调节肿瘤坏死因子α（TNF-α）活性和血管生成的沙利度胺类似物。在特别公开的实施方案中，沙利度胺类似物是等熵含硫类似物。还公开了用类似物治疗受试者的方法。

5. 发明申请

US20110245210A1 THALIDOMIDE ANALOGS 有权
标题翻译：噻吗啉类似物
公开(公告)号：US20110245210A1
公开(公告)日：2011-10-06
申请号：US13153355
申请日：2011-06-03
申请人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
发明人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
IPC分类号： A61K31/625 , A61K31/4439 , C07D401/04 , A61K31/437 , C07D471/04 , A61K31/538 , C07D413/04 , C07D211/88 , A61K31/4035 , C07D209/50 , A61P35/00
CPC分类号： C07D209/44 , C07D209/46 , C07D211/84 , C07D211/86 , C07D211/88 , C07D401/04 , C07D413/04 , C07D471/04
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNF-α) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
摘要翻译：公开了调节肿瘤坏死因子α（TNF-α）活性和血管发生的沙利度胺类似物。在特别公开的实施方案中，沙利度胺类似物是同基性含硫类似物。还公开了用类似物治疗受试者的方法。

6. 发明授权

US08853253B2 Thalidomide analogs 有权
标题翻译：沙利度胺类似物
公开(公告)号：US08853253B2
公开(公告)日：2014-10-07
申请号：US13648625
申请日：2012-10-10
申请人： Nigel H. Greig , Harold Holloway , Tony Giordano , Qian-sheng Yu , William D. Figg
发明人： Nigel H. Greig , Harold Holloway , Arnold Brossi , Xiaoxiang Zhu , Tony Giordano , Qian-sheng Yu , William D. Figg
IPC分类号： A61K31/40
CPC分类号： H04M1/72522 , C07D209/44 , G06F3/01 , G06F3/0346 , H04M2250/12 , H04M2250/22 , H04M2250/74
摘要： Thalidomide analogs that modulate tumor necrosis factor alpha (TNFα) activity and angiogenesis are disclosed. In particularly disclosed embodiments, the thalidomide analogs are isosteric sulfur-containing analogs. Also disclosed are methods of treating a subject with the analogs.
摘要翻译：公开了调节肿瘤坏死因子α（TNFα）活性和血管生成的沙利度胺类似物。在特别公开的实施方案中，沙利度胺类似物是等熵含硫类似物。还公开了用类似物治疗受试者的方法。

7. 发明申请

US20080319032A1 TETRAHYDROBENZOTHIAZOLE ANALOGUES AS NEUROPROTECTIVE AGENTS 审中-公开
标题翻译：四氢苯并噻唑类似物作为神经保护剂
公开(公告)号：US20080319032A1
公开(公告)日：2008-12-25
申请号：US11939515
申请日：2007-11-13
申请人： Nigel H Greig , Mark Mattson , Xiaoxiang Zhu , Qian-Sheng Yu , Harold Wayne Holloway
发明人： Nigel H Greig , Mark Mattson , Xiaoxiang Zhu , Qian-Sheng Yu , Harold Wayne Holloway
IPC分类号： A61K31/428 , C12N5/00 , C07D277/68 , A61K31/423 , A61P3/10 , A61P25/00 , C07D263/58
CPC分类号： C07D263/58 , C07D277/68 , C07D277/82 , C07D513/04
摘要： This invention relates generally to tetrahydrobenzothiazole analogues and tetrahydrobenzooxyzole analogues, to pharmaceutical compositions which include these compounds and a pharmaceutically acceptable carrier, and to methods of treatment using these compounds. The invention also encompasses pharmaceutically acceptable esters, amides, and salts of such compounds. The invention further provides a method of reducing or delaying apoptosis in a population of cells, comprising contacting the population of cells with a tetrahydrobenzothiazole analogue or a tetrahydrobenzooxyzole analogue, thereby reducing or delaying apoptosis in the population of cells.
摘要翻译：本发明一般涉及四氢苯并噻唑类似物和四氢苯并氧唑类似物，包括这些化合物和药学上可接受的载体的药物组合物，以及使用这些化合物的治疗方法。本发明还包括这些化合物的药学上可接受的酯，酰胺和盐。本发明进一步提供减少或延缓细胞群中凋亡的方法，包括使细胞群与四氢苯并噻唑类似物或四氢苯并氧唑类似物接触，从而减少或延缓细胞群中的凋亡。

8. 发明申请

US20060293250A1 Crystalline sugar compositions and method of making 审中-公开
标题翻译：结晶糖组合物和制备方法
公开(公告)号：US20060293250A1
公开(公告)日：2006-12-28
申请号：US11449515
申请日：2006-06-08
申请人： Michael Major , Robert Peterson , Daniel Linse , Szymon Kosinski , Xiaoxiang Zhu
发明人： Michael Major , Robert Peterson , Daniel Linse , Szymon Kosinski , Xiaoxiang Zhu
IPC分类号： A61K31/7024 , C07H13/02 , C07H5/04
CPC分类号： C07H15/00 , C07H5/04 , C07H13/00 , C07H13/02
摘要： Described are novel crystalline pivaloyl furanoses and methods of crystallizing the pivaloyl furanoses. These compounds are useful as intermediates in the synthesis of compounds such as the deoxyjirimycins and nojirimycins and are particularly useful as intermediates for production on a multi-kg scale. Particular crystalline compounds include 1,2,3,6-tetrapivaloyl-α-D-galactofuranose, 1,2,3,6-tetrapivaloyl-α-L-altrofuranose, and 5-azido-5-deoxy-1,2,3,6-tetrapivaloyl-α-D-galactofuranose.
摘要翻译：描述了新颖的结晶新戊酰呋喃糖和结晶新戊酰呋喃糖的方法。这些化合物可用作合成化合物如脱氧吉西林和nojirimycins的中间体，并且特别适用于以多kg规模生产的中间体。特殊的结晶化合物包括1,2,3,6-四新戊酰-α-D-半乳糖呋喃糖，1,2,3,6-四新戊酰-α-L-吡喃核糖和5-叠氮基-5-脱氧-1,2 ，6-四新戊酰-α-D-半乳糖呋喃糖。

9. 发明申请

US20050137223A1 Glucoimidazole and polyhydroxycyclohexenyl amine derivatives to treat gaucher disease 审中-公开
标题翻译：葡糖咪唑和多羟基环己烯胺衍生物治疗高血糖病
公开(公告)号：US20050137223A1
公开(公告)日：2005-06-23
申请号：US10988427
申请日：2004-11-12
申请人： Jian-Qiang Fan , Xiaoxiang Zhu , Kamlesh Sheth
发明人： Jian-Qiang Fan , Xiaoxiang Zhu , Kamlesh Sheth
IPC分类号： A61K20060101 , A61K31/437 , A61K31/445 , A61K31/454 , A61K31/4745 , A61K31/50 , A61K31/501 , A61K48/00 , A61P43/00 , C07D211/40 , C07D471/02 , C07D471/04
CPC分类号： C07D487/04
摘要： The present invention provides glucoimidazole (GIZ) and polyhydroxycyclohexenyl amine (PHCA) derivatives, methods of making them, and methods of use where the GIZ and PHCA derivatives have a short, flexible linker emanating from the corresponding position of the ring oxygen in a pyranose; and a lipophilic moiety connected to the linker and pharmaceutically acceptable salts thereof. More particularly, the present invention further provides a method for treating individuals having Gaucher disease by administering the novel GIZ or PHCA derivatives as “active-site specific chaperones” for the mutant glucocerebrosidase associated with the disease.
摘要翻译：本发明提供了葡糖咪唑（GIZ）和多羟基环己烯胺（PHCA）衍生物，其制备方法，以及GIZ和PHCA衍生物具有从吡喃糖中的环氧相应位置发出的短柔性连接体的使用方法; 和与该连接体连接的亲油部分及其药学上可接受的盐。更具体地，本发明还提供了通过将新型GIZ或PHCA衍生物作为与该疾病相关的突变型葡糖脑苷脂酶的“活性位点特异性伴侣”来治疗患有戈谢病的个体的方法。

10. 发明授权

US07741340B2 Hydroxy piperidine derivatives to treat gaucher disease 有权
标题翻译：羟基哌啶衍生物治疗胃癌
公开(公告)号：US07741340B2
公开(公告)日：2010-06-22
申请号：US10988428
申请日：2004-11-12
申请人： Jian-Qiang Fan , Xiaoxiang Zhu , Kamlesh Sheth
发明人： Jian-Qiang Fan , Xiaoxiang Zhu , Kamlesh Sheth
IPC分类号： A61K31/445
CPC分类号： C07D487/04
摘要： The present invention provides novel hydroxy piperidine (HP) derivatives having (i) a positive charge at the position corresponding to the anomeric position of a pyranose ring; (ii) a short, flexible linker emanating from the corresponding position of the ring oxygen in a pyranose; and (iii) a lipophilic moiety connected to the linker and pharmaceutically acceptable salts thereof. The linker can be absent if the lipophilic moiety corresponds to a hydrocarbon chain with a linear length of 6 or more carbons. The present invention further provides a method for treating individuals having Gaucher disease by administering the novel HP derivative as “active-site specific chaperones” for the mutant glucocerebrosidase associated with the disease.
摘要翻译：本发明提供了新颖的羟基哌啶（HP）衍生物，其具有（i）在对应于吡喃糖环的端基异位的位置处的正电荷; （ii）从吡喃糖中环氧的相应位置发出的短柔性连接体; 和（iii）与接头连接的亲油部分及其药学上可接受的盐。如果亲油部分对应于线性长度为6个或更多个碳的烃链，则该接头可以不存在。本发明还提供了通过将新型HP衍生物作为与疾病相关的突变型葡糖脑苷脂酶的“活性位点特异性伴侣”来治疗患有戈谢病的个体的方法。

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