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1. 发明申请

WO2010108187A2 COMPOUNDS AND METHODS FOR TREATING MAMMALIAN GASTROINTESTINAL MICROBIAL INFECTIONS 审中-公开
标题翻译：化合物和治疗哺乳动物胃肠道微生物感染的方法
公开(公告)号：WO2010108187A2
公开(公告)日：2010-09-23
申请号：PCT/US2010/028178
申请日：2010-03-22
申请人： BRANDEIS UNIVERSITY , UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC. , HEDSTROM, Lizbeth, K. , CUNY, Gregory, D. , GOLLAPALLI, Deviprasad, R. , KIRUBAKARAN, Sivapriya , STRIEPEN, Boris , GORLA, Suresh, Kumar , MAURYA, Sushi, K. , JOHNSON, Corey, Robert , KAVITHA, Mandapati , KHAN, JIHAN,
发明人： HEDSTROM, Lizbeth, K. , CUNY, Gregory, D. , GOLLAPALLI, Deviprasad, R. , KIRUBAKARAN, Sivapriya , STRIEPEN, Boris , GORLA, Suresh, Kumar , MAURYA, Sushi, K. , JOHNSON, Corey, Robert , KAVITHA, Mandapati , KHAN, JIHAN,
CPC分类号： C07D401/12 , C07C233/15 , C07C235/24 , C07C235/38 , C07C237/20 , C07C255/60 , C07C275/28 , C07C275/30 , C07C275/42 , C07C309/15 , C07D209/08 , C07D209/12 , C07D209/30 , C07D215/38 , C07D235/26 , C07D237/32 , C07D249/06 , C07D263/56 , C07D263/57 , C07D295/192 , C07D401/04 , C07D401/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/08 , C07D491/052
摘要： Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
摘要翻译：本文描述了可用作IMPDH抑制剂的化合物及其药学上可接受的盐和前药。在某些实施方案中，本发明的化合物选择性地抑制寄生IMPDH相对于宿主IMPDH。此外，本发明提供包含一种或多种本发明化合物的药物组合物。本发明还涉及治疗哺乳动物中各种寄生虫和细菌感染的方法。此外，化合物可以单独使用或与其它治疗或预防剂如抗病毒剂，抗炎剂，抗微生物剂和免疫抑制剂组合使用。

2. 发明申请

WO1997010249A1 TOXOPLASMA GONDII GLYCOCONJUGATES 审中-公开
标题翻译：豆科植物GONDII GLYCOCONJUGATES
公开(公告)号：WO1997010249A1
公开(公告)日：1997-03-20
申请号：PCT/EP1996004034
申请日：1996-09-12
申请人： AKZO NOBEL N.V. , KOOLEN, Marcus, Josephus, Marie , DAMM, Jan, Bas, Louis , STRIEPEN, Boris , SCHWARZ, Ralph, T.
发明人： AKZO NOBEL N.V.
IPC分类号： C07H03/06
CPC分类号： A61K39/002 , C07H3/06 , C07K16/20
摘要： The present invention relates to a glycoconjugate immunoreactive with Toxoplasma gondii antibodies, (monoclonal) antibodies against these glycoconjugates, and cell lines capable of producing monoclonal antibodies. The invention is further concerned with immunochemical reagents and methods for the detection of T. gondii or antibodies directed agains T. gondii. Furthermore the invention relates to a therapeutic reagent for the inhibition of replication of T. gondii parasites and a method for the production of a live attenuated T. gondii vaccine. It has now been found, and in contrast with earlier publications in this art, that several glycoconjugates are immunoreactive with Toxoplasma gondii specific antibodies comprising a glycan core structure having general formula (I) wherein R1 = Hydrogen, -PO3-CH2-CH2-NH2 (ethanolamine-phosphate), or -PO3-CH2-CH2-NH-X, wherein X = a T. gondii specific antigen; wherein R2 = alpha -O-R4, alpha (1-4)-O-anhydromannitol or alpha (1-4)-O-glucoseamine optionally alpha (1-6)-linked to the inositol moiety of a phosphatidylinositol membrane anchor; wherein R3 = a monosaccharide moiety, wherein R4 = Hydrogen or -L-R5, wherein L = a bivalent organic radical and R5 = a functional group that allows coupling to a carrier. A preferred embodiment of the monosaccharide moiety is a hexose moiety, more preferred is a glucose moiety, and most preferred is a glucose moiety which is bonded to the GalNAc-moiety by an alpha -1,4 glycosidic bond. It has been found that the glycoconjugates according to the present invention are particularly suitable for diagnosing T. gondii infected humans.
摘要翻译：本发明涉及与弓形体弓形体抗体免疫反应的糖缀合物，针对这些糖缀合物的（单克隆）抗体，以及能够产生单克隆抗体的细胞系。本发明进一步涉及免疫化学试剂和用于检测弓形虫或再次引导弓形虫的抗体的方法。此外，本发明涉及用于抑制弓形虫寄生虫复制的治疗试剂和一种减毒活的弓形虫疫苗的生产方法。现在已经发现，与本领域的早期出版物相反，几种糖缀合物与弓形体特异性抗体是免疫反应的，其包含通式（I）的聚糖核心结构，其中R1 =氢，-PO3-CH2-CH2-NH2 （乙醇胺 - 磷酸盐）或-PO 3 -CH 2 -CH 2 -NH-X，其中X =弓形虫特异性抗原; 其中R2 =α-O-R4，α（1-4）-O-脱水脱水葡萄糖醇或任选α（1-6）连接至磷脂酰肌醇膜锚的肌醇部分的α（1-4）-O-葡萄糖胺; 其中R3 =单糖部分，其中R4 =氢或-L-R5，其中L =二价有机基团，R5 =允许与载体结合的官能团。单糖部分的优选实施方案是己糖部分，更优选葡萄糖部分，最优选的是通过α-1,4糖苷键与GalNAc部分结合的葡萄糖部分。已经发现根据本发明的糖缀合物特别适用于诊断弓形虫感染的人。

3. 发明申请

WO2010108187A3 COMPOUNDS AND METHODS FOR TREATING MAMMALIAN GASTROINTESTINAL MICROBIAL INFECTIONS 审中-公开
标题翻译：化合物和治疗MAMMALIAN胃肠道微生物感染的方法
公开(公告)号：WO2010108187A3
公开(公告)日：2011-03-31
申请号：PCT/US2010028178
申请日：2010-03-22
申请人： UNIV BRANDEIS , UNIV GEORGIA , HEDSTROM LIZBETH K , CUNY GREGORY D , GOLLAPALLI DEVIPRASAD R , KIRUBAKARAN SIVAPRIYA , STRIEPEN BORIS , GORLA SURESH KUMAR , MAURYA SUSHI K , JOHNSON COREY ROBERT , KAVITHA MANDAPATI , KHAN JIHAN
发明人： HEDSTROM LIZBETH K , CUNY GREGORY D , GOLLAPALLI DEVIPRASAD R , KIRUBAKARAN SIVAPRIYA , STRIEPEN BORIS , GORLA SURESH KUMAR , MAURYA SUSHI K , JOHNSON COREY ROBERT , KAVITHA MANDAPATI , KHAN JIHAN
IPC分类号： C07D249/06 , A61K31/4192 , A61P19/02 , A61P37/00 , C07D401/12 , C07D401/14 , C07D417/14
CPC分类号： C07D401/12 , C07C233/15 , C07C235/24 , C07C235/38 , C07C237/20 , C07C255/60 , C07C275/28 , C07C275/30 , C07C275/42 , C07C309/15 , C07D209/08 , C07D209/12 , C07D209/30 , C07D215/38 , C07D235/26 , C07D237/32 , C07D249/06 , C07D263/56 , C07D263/57 , C07D295/192 , C07D401/04 , C07D401/14 , C07D409/04 , C07D413/04 , C07D417/04 , C07D417/14 , C07D471/08 , C07D491/052
摘要： Described herein are compounds, and pharmaceutically acceptable salts and prodrugs thereof, which are useful as inhibitors of IMPDH. In certain embodiments, a compound of the invention selectively inhibits a parasitic IMPDH versus a host IMPDH. Further, the invention provides pharmaceutical compositions comprising one or more compounds of the invention. The invention also relates to methods of treating various parasitic and bacterial infections in mammals. Moreover, the compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
摘要翻译：本文描述了可用作IMPDH抑制剂的化合物及其药学上可接受的盐和前药。在某些实施方案中，本发明的化合物选择性地抑制寄生IMPDH相对于宿主IMPDH。此外，本发明提供包含一种或多种本发明化合物的药物组合物。本发明还涉及治疗哺乳动物中各种寄生虫和细菌感染的方法。此外，化合物可以单独使用或与其它治疗剂或预防剂如抗病毒剂，抗炎剂，抗微生物剂和免疫抑制剂组合使用。

4. 发明申请

WO2007143557A3 COMPOUNDS AND METHODS FOR TREATING MAMMALIAN GASTROINTESTINAL PARASITIC INFECTIONS 审中-公开
公开(公告)号：WO2007143557A3
公开(公告)日：2007-12-13
申请号：PCT/US2007/070233
申请日：2007-06-01
申请人： BRANDEIS UNIVERSITY MS134 , HEDSTROM, Lizbeth, K. , STRIEPEN, Boris
发明人： HEDSTROM, Lizbeth, K. , STRIEPEN, Boris
IPC分类号： A01N57/00 , A61K31/675
摘要： One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5'-monophosphate-dehydrogenase over human inosine-5'-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.

5. 发明申请

WO2007143557A2 COMPOUNDS AND METHODS FOR TREATING MAMMALIAN GASTROINTESTINAL PARASITIC INFECTIONS 审中-公开
标题翻译：化合物和治疗哺乳动物胃肠道寄生虫感染的方法
公开(公告)号：WO2007143557A2
公开(公告)日：2007-12-13
申请号：PCT/US2007070233
申请日：2007-06-01
申请人： BRANDEIS UNIVERSITY MS134 , HEDSTROM LIZBETH K , STRIEPEN BORIS
发明人： HEDSTROM LIZBETH K , STRIEPEN BORIS
IPC分类号： A61K31/4439
CPC分类号： A61K31/4439
摘要： One aspect of the present invention relates to compounds, and pharmaceutically acceptable salts and prodrugs thereof, that are useful as inhibitors of IMPDH. The invention also provides pharmaceutical compositions comprising the compounds of the invention which selectively inhibit parasitic IMPDH. In certain embodiments, the present invention relates to selective inhibition of C. parvum inosine-5'-monophosphate-dehydrogenase over human inosine-5'-monophosphate-dehydrogenase (IMPDH type I and type II). These compounds may be used alone or in combination with other therapeutic or prophylactic agents, such as anti-virals, anti-inflammatory agents, antimicrobials and immunosuppressants.
摘要翻译：本发明的一个方面涉及可用作IMPDH抑制剂的化合物及其药学上可接受的盐和前药。本发明还提供包含选择性抑制寄生性IMPDH的本发明化合物的药物组合物。在某些实施方案中，本发明涉及对人肌苷-5'-单磷酸脱氢酶（IMPDH I型和II型）的副细胞肌球蛋白-5'-单磷酸脱氢酶的选择性抑制。这些化合物可以单独使用或与其它治疗或预防剂如抗病毒剂，抗炎剂，抗微生物剂和免疫抑制剂组合使用。

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