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1. 发明申请

US20140005132A1 CONTRACEPTIVE AGENTS 有权
标题翻译：承包商
公开(公告)号：US20140005132A1
公开(公告)日：2014-01-02
申请号：US13932778
申请日：2013-07-01
申请人： Gustavo Blanco , Gunda I. Georg , Shameem Sultana Syeda
发明人： Gustavo Blanco , Gunda I. Georg , Shameem Sultana Syeda
IPC分类号： C07J43/00 , C07J17/00 , C07J19/00
CPC分类号： C07J43/003 , C07C49/653 , C07C49/757 , C07C247/14 , C07C281/18 , C07D249/04 , C07D249/06 , C07J1/0011 , C07J7/00 , C07J7/002 , C07J17/005 , C07J19/00 , C07J19/005 , C07J41/0005 , C07J41/0027 , C07J41/005 , C07J51/00 , C07J71/0026
摘要： The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase α4 and are useful as contraceptive agents.
摘要翻译：本发明提供式I，II，III或IV的化合物：其中R1至R11，X和Y具有说明书中定义的任何值。这些化合物抑制Na，K-ATP酶α4，可用作避孕药。

2. 发明授权

US09670247B2 Contraceptive agents 有权
公开(公告)号：US09670247B2
公开(公告)日：2017-06-06
申请号：US13932778
申请日：2013-07-01
申请人： Gustavo Blanco , Gunda I. Georg , Shameem Sultana Syeda
发明人： Gustavo Blanco , Gunda I. Georg , Shameem Sultana Syeda
IPC分类号： A61K31/58 , C07J43/00 , C07J71/00 , C07J19/00 , C07J17/00 , C07C281/18 , C07C247/14 , C07C49/653 , C07C49/757 , C07D249/04 , C07D249/06 , C07J1/00 , C07J7/00 , C07J41/00 , C07J51/00
CPC分类号： C07J43/003 , C07C49/653 , C07C49/757 , C07C247/14 , C07C281/18 , C07D249/04 , C07D249/06 , C07J1/0011 , C07J7/00 , C07J7/002 , C07J17/005 , C07J19/00 , C07J19/005 , C07J41/0005 , C07J41/0027 , C07J41/005 , C07J51/00 , C07J71/0026
摘要： The invention provides compounds of formula I, II, III, or IV: wherein R1 to R11, X, and Y have any of the values defined in the specification. The compounds inhibit Na, K-ATPase α4 and are useful as contraceptive agents.

3. 发明授权

US07514463B2 Lonidamine analogues and their use in male contraception and cancer treatment 有权
标题翻译：罗丹明胺类似物及其在男性避孕和癌症治疗中的应用
公开(公告)号：US07514463B2
公开(公告)日：2009-04-07
申请号：US10922747
申请日：2004-08-20
申请人： Gunda I. Georg , Joseph S. Tash , Ramappa Chakrasali , Sudhakar Rao Jakkaraj
发明人： Gunda I. Georg , Joseph S. Tash , Ramappa Chakrasali , Sudhakar Rao Jakkaraj
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D231/56 , C07D471/04
摘要： Novel compounds useful for inhibiting spermatogenesis and cancer treatment, and in particular as inhibitors of heat shock proteins and/or elongation factor 1 alpha.
摘要翻译：用于抑制精子发生和癌症治疗的新型化合物，特别是作为热休克蛋白和/或延伸因子1α的抑制剂。

4. 发明授权

US06603015B2 Synthesis of epothilones 失效
公开(公告)号：US06603015B2
公开(公告)日：2003-08-05
申请号：US10014754
申请日：2001-12-11
申请人： Gunda I. Georg , Sajiv K. Nair , Emily Reiff , Ashok Rao Tunoori
发明人： Gunda I. Georg , Sajiv K. Nair , Emily Reiff , Ashok Rao Tunoori
IPC分类号： C07D27722
CPC分类号： C07D417/06 , C07B2200/07 , C07C45/29 , C07C67/31 , C07C67/343 , C07D277/24 , C07D493/04 , C07F7/1892 , C07C47/21 , C07C69/734 , C07C69/675
摘要： Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.

5. 发明授权

US06211412B1 Synthesis of epothilones 失效
标题翻译：埃坡霉素的合成
公开(公告)号：US06211412B1
公开(公告)日：2001-04-03
申请号：US09280207
申请日：1999-03-29
申请人： Gunda I. Georg , Sajiv K. Nair , Emily Reiff , Ashok Rao Tunoori , John T. Henri
发明人： Gunda I. Georg , Sajiv K. Nair , Emily Reiff , Ashok Rao Tunoori , John T. Henri
IPC分类号： C07C4541
CPC分类号： C07D417/06 , C07B2200/07 , C07C45/29 , C07C67/31 , C07D277/24 , C07D493/04 , C07F7/1892 , C07C47/21 , C07C69/734
摘要： Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment C using a stereoselective Noyori-type reduction, and the coupling of epothilone segments B and C using an aldol condensation reaction. The synthesis methods may be used to prepare naturally occurring segments as well as a large number of related analogs and homologs thereof. Final epothilones in accordance with the invention may also be of the naturally occurring variety (16-membered macrolides), while the homologs and analogs thereof are preferably up to 20-membered macrolides.
摘要翻译：提供了用于合成制备最终埃坡霉素所需的各种埃坡霉素前体的商业上可行的方法，包括使用立体选择性Noyori型还原合成埃坡霉素片段C的技术，以及使用醛醇缩合反应偶联埃坡霉素片段B和C. 合成方法可用于制备天然存在的片段以及大量相关的类似物及其同系物。根据本发明的最终埃坡霉素也可以是天然存在的品种（16-元大环内酯），而其同系物和类似物优选为至多20-元大环内酯。

6. 发明授权

US6100428A Nickel promoted guanylation of amines with isothioureas and thioureas 失效
标题翻译：镍促进胺与异硫脲和硫脲的胍基化
公开(公告)号：US6100428A
公开(公告)日：2000-08-08
申请号：US412844
申请日：1999-10-06
申请人： Laxminarayan Bhat , Gunda I. Georg
发明人： Laxminarayan Bhat , Gunda I. Georg
IPC分类号： C07C277/08 , C07C279/18 , C07C279/24 , C07C311/64 , C07D295/215 , C07D295/26 , C07C279/16 , C07C271/20 , C07C303/40
CPC分类号： C07D295/215 , C07C277/08 , C07C311/64 , C07D295/26 , C07C2101/02 , C07C2101/14 , Y02P20/55
摘要： An improved method for guanylating amines is provided. Broadly, the amines are reacted with a guanylating agent in the presence of a nickel catalyst. Preferably, the nickel catalyst comprises nickel in the zero oxidation state. Suitable nickel(0) catalysts are derived from nickel-boride alloys, nickel-phosphide alloys, aluminum-nickel alloys, nickel on kieselguhr, and nickel on silica/alumina catalysts. Preferred guanylating agents are thioureas and isothioureas. In one embodiment, protecting groups are selectively attached to the guanylating agents to yield particular substituted guanidines. The preferred protecting groups are Boc groups, Cbz groups, and arylsulfonyl groups. The reactions are particularly well suited for guanylating primary and secondary amines. The methods of the invention can be carried out under ambient conditions to provide high yields of the corresponding guanidines, with the nickel catalyst being essentially completely recoverable for reuse.
摘要翻译：提供了一种改进的脒基化胺的方法。广泛地，胺与脒基化剂在镍催化剂存在下反应。优选地，镍催化剂包括处于零氧化状态的镍。合适的镍（0）催化剂衍生自镍 - 硼化物合金，镍 - 磷化物合金，铝 - 镍合金，硅藻土上的镍和二氧化硅/氧化铝催化剂上的镍。优选的脒基化剂是硫脲和异硫脲。在一个实施方案中，保护基选择性连接到脒基化剂以产生特定的取代的胍。优选的保护基是Boc基团，Cbz基团和芳基磺酰基。反应特别适用于脒基化的伯胺和仲胺。本发明的方法可以在环境条件下进行以提供高产率的相应的胍，镍催化剂基本上完全可回收再利用。

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