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1. 发明申请

WO2005092878A3 SCHWEINFURTHIN ANALOGUES 审中-公开
标题翻译：辛伐他汀类似物
公开(公告)号：WO2005092878A3
公开(公告)日：2006-05-04
申请号：PCT/US2005010482
申请日：2005-03-29
申请人： UNIV IOWA RES FOUND , US GOV HEALTH & HUMAN SERV , WIEMER DAVID F , NEIGHBORS JEFFREY D , BEUTLER JOHN A
发明人： WIEMER DAVID F , NEIGHBORS JEFFREY D , BEUTLER JOHN A
IPC分类号： C07D311/78 , C07D311/00 , C07D311/80
CPC分类号： C07D311/80 , C07D311/78
摘要： Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.
摘要翻译：用于制备可用于治疗癌症的对映体富集的施魏呋喃类似物的方法和中间体，以及具有抗癌活性的新型施魏因乙酰类似物，包含此类类似物的组合物和包括施用此类类似物的治疗方法。

2. 发明申请

WO2009158516A1 SCHWEINFURTHIN ANALOGUES 审中-公开
标题翻译：辛伐他汀类似物
公开(公告)号：WO2009158516A1
公开(公告)日：2009-12-30
申请号：PCT/US2009/048690
申请日：2009-06-25
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , WIEMER, David, F. , NEIGHBORS, Jeffrey, D. , HOHL, Raymond, J. , KUDER, Craig
发明人： WIEMER, David, F. , NEIGHBORS, Jeffrey, D. , HOHL, Raymond, J. , KUDER, Craig
IPC分类号： C07D311/80 , A61K31/352 , A61P35/00
CPC分类号： C07D311/80
摘要： The invention provides fluorescent schweinfurthin analogs of formula(I) which are useful as probes and for the treatment of cancer and other diseases.
摘要翻译：本发明提供了可用作探针和用于治疗癌症和其它疾病的式（I）的荧光施赖呋喃蛋白类似物。

3. 发明申请

WO2019182904A1 PHOSPHONAMIDATE BUTYROPHILIN LIGANDS 审中-公开
公开(公告)号：WO2019182904A1
公开(公告)日：2019-09-26
申请号：PCT/US2019/022529
申请日：2019-03-15
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , UNIVERSITY OF CONNECTICUT , WIEMER, David, F. , WIEMER, Andrew, J.
发明人： WIEMER, David, F. , WIEMER, Andrew, J.
IPC分类号： A61P37/02 , A61P37/04
摘要： The invention provides a compound of formula I: or a salt thereof, wherein R 1 -R 4 have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful in immunotherapy as a potential treatment, or co-treatment, for cancer or infectious diseases.

4. 发明申请

WO2019182904A8 PHOSPHONAMIDATE BUTYROPHILIN LIGANDS 审中-公开
公开(公告)号：WO2019182904A8
公开(公告)日：2019-09-26
申请号：PCT/US2019/022529
申请日：2019-03-15
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , UNIVERSITY OF CONNECTICUT , WIEMER, David, F. , WIEMER, Andrew, J.
发明人： WIEMER, David, F. , WIEMER, Andrew, J.
IPC分类号： A61P37/02 , A61P37/04
摘要： The invention provides a compound of formula I: or a salt thereof, wherein R 1 -R 4 have any of the values described in the specification, as well as compositions comprising a compound of formula I. The compounds are useful in immunotherapy as a potential treatment, or co-treatment, for cancer or infectious diseases.

5. 发明申请

WO2013148584A1 SCHWEINFURTHIN ANALOGUES 审中-公开
标题翻译：辛伐他汀类似物
公开(公告)号：WO2013148584A1
公开(公告)日：2013-10-03
申请号：PCT/US2013/033722
申请日：2013-03-25
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , KODET, John , NEIGHBORS, Jeffrey, D. , WIEMER, David, F.
发明人： KODET, John , NEIGHBORS, Jeffrey, D. , WIEMER, David, F.
IPC分类号： C07D405/06 , C07D405/14 , A61K31/404 , A61K31/416 , A61P35/00
CPC分类号： C07D405/06 , C07D405/14
摘要： The invention provides a compound of formula (I): wherein R 1 -R 5 have any of the values defined in the specification. The compounds are useful for the treatment of cancer and other diseases.
摘要翻译：本发明提供式（I）化合物：其中R1-R5具有说明书中定义的任何值。这些化合物可用于治疗癌症和其他疾病。

6. 发明申请

WO2006026380A3 GERANYLGERANYL PYROPHOSPHATE SYNTHASE INHIBITORS 审中-公开
标题翻译： GERANYLGERANYL磷酸酯合酶抑制剂
公开(公告)号：WO2006026380A3
公开(公告)日：2006-06-22
申请号：PCT/US2005030304
申请日：2005-08-25
申请人： UNIV IOWA RES FOUND , WIEMER DAVID F , HOHL RAYMOND J
发明人： WIEMER DAVID F , HOHL RAYMOND J
IPC分类号： A61K31/663 , A61K51/04 , A61P9/06 , A61P15/00 , A61P33/00 , A61P35/00 , A61P43/00 , C07F9/38 , C07F9/40
CPC分类号： C07F9/4031 , C07F9/3847 , C07F9/3873 , C07F9/405
摘要： The invention provides novel pyrophosphate synthase inhibitors of formula (I), wherein R 1 is a saturated or unsaturated: (C 5 -C 20 )alkyl chain that optionally comprises one or more aryl rings in the chain and that is optionally substituted with one or more halo, trifluoromethyl, -OR a , -P(=O)(OR a ) 2 , or -NR b R c ; R 2 is a saturated or unsaturated (C 5 -C 20 )alkyl chain that optionally comprises one or more aryl rings in the chain and that is optionally substituted with one or more halo, trifluoromethyl, -OR a , -P(=O)(OR a ) 2 , or -NR b R c ; R 2 ; each R 3 , R 4 , R 5 , and R 6 is independently OH or (C 1 -C 6 )alkoxy; each R a is independently H, (C 1 -C 6 )alkyl, or aryl; and .each R b and R c is independently H, (C 1 -C 6 )alkyl, or aryl; or R b and R c together with the nitrogen to which they are attached form a pyrrolidino, piperidino, morpholino, or thiomorpholino ring; wherein any aryl is optionally substituted with one or more (C 1 -C 6 )alkyl, (C 1 -C 6 )alkoxy, (C 1 -C 6 )alkanoyl, (C 1 -C 6 )alkanoyloxy, (C 1 -C 6 )alkoxycarbonyl, halo, cyano, nitro, carboxy, trifluoromethyl, trifluoromethoxy, NR d R e , or S(O) 2 NR d R e , wherein each R d and R e is independently H or (C 1 -C 6 )alkyl; or a pharmaceutically acceptable salt or prodrug thereof. Also provided are compositions comprising such inhibitors and methods for their use.
摘要翻译：本发明提供了新的式（I）焦磷酸合酶抑制剂，其中R 1是饱和或不饱和的：（C 5 -C 20）烷基链，其任选地在链中包含一个或多个芳环，并且任选地被一个或多个卤素，三氟甲基，-OR a， - （= O）（OR a） 2 SUB，或-NR b R c C; R 2是任选地包含一个或多个芳环的饱和或不饱和（C 5 -C 20 -C 20）烷基链该链并且其任选地被一个或多个卤素，三氟甲基，-OR 1， - （= O）（OR 1）2 - >，或-NR b R c C; [R _{2 ; 每个R 3，R 4，R 5和R 6独立地是OH或（C 1 -C 4） 1 -C _{6 ）烷氧基; 每个R a a独立地为H，（C 1 -C 6 -C 6）烷基或芳基; 和每个R b和R c独立地是H，（C 1 -C 6 -C 6）烷基，或芳基; 或R b和R c与它们所连接的氮一起形成吡咯烷子基，哌啶子基，吗啉代或硫代吗啉环; 其中任何芳基任选被一个或多个（C 1 -C 6 -C 6）烷基取代，（C 1 -C 6 - （C 1 -C 6）烷酰基，（C 1 -C 6）烷氧基，（C 1 -C 6 -C 6）烷酰基，（C 1 -C 6 - 烷酰氧基，（C 1 -C 6 -C 6）烷氧基羰基，卤素，氰基，硝基，羧基，三氟甲基，三氟甲氧基，NR d R 或（S）（O）2 NR d R e，其中每个R d和 R e独立地为H或（C 1 -C 6 -C 6）烷基; 或其药学上可接受的盐或前药。还提供了包含这些抑制剂的组合物及其使用方法。}}

7. 发明申请

WO2017011686A1 FLUORESCENT PRODRUGS 审中-公开
标题翻译：荧光素材
公开(公告)号：WO2017011686A1
公开(公告)日：2017-01-19
申请号：PCT/US2016/042331
申请日：2016-07-14
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , WIEMER, David, F. , BARNEY, Rocky, J. , WIEMER, Andrew
发明人： WIEMER, David, F. , BARNEY, Rocky, J. , WIEMER, Andrew
IPC分类号： G01N33/543 , G01N33/53
CPC分类号： G01N33/5005 , A61K41/0038 , A61K47/548 , G01N33/582 , G01N2800/7028
摘要： The invention provides a drug conjugate comprising: 1) a therapeutic agent that comprises a phosphate, phosphonate, carboxy, or phosphoramidate group, and 2) a fluorescent group linked to the phosphate, phosphonate, carboxy, or phosphoramidate group to form the corresponding ester and salts thereof. The conjugates are useful for therapy and as probes. The invention also provides therapeutic methods for treating diseases with conjugates of the invention as well as methods for determining optimal dosages of a conjugate or a therapeutic agent for a given patient using a conjugate of the invention
摘要翻译：本发明提供一种药物结合物，其包含：1）包含磷酸盐，膦酸盐，羧基或氨基磷酸酯基团的治疗剂，和2）与磷酸盐，膦酸盐，羧基或氨基磷酸酯基团连接以形成相应的酯的荧光基团，的盐。缀合物可用于治疗和探针。本发明还提供了用本发明的缀合物治疗疾病的治疗方法以及使用本发明的缀合物确定给定患者的缀合物或治疗剂的最佳剂量的方法

8. 发明申请

WO2010108190A1 PRENYLATED BISPHOSPHONATES AS ANTI-TUBERCULOSIS AGENTS 审中-公开
标题翻译：作为抗结核药物的先天性二硫磷酸酯
公开(公告)号：WO2010108190A1
公开(公告)日：2010-09-23
申请号：PCT/US2010/028187
申请日：2010-03-22
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , WIEMER, David, F. , BARNEY, Rocky, J. , HOHL, Raymond, J.
发明人： WIEMER, David, F. , BARNEY, Rocky, J. , HOHL, Raymond, J.
IPC分类号： A61K31/404 , A61K31/663 , A61P31/06 , A61K9/20
CPC分类号： A61K31/663 , A61K9/008 , A61K9/2018 , A61K9/2054 , A61K31/404 , A61K47/02 , A61K47/10
摘要： The invention provides methods to treat a mycobacterium infection and methods to inhibit mycobacterial polyprenyl pyrophosphate synthesis with a compound of formula I. The invention also provides novel compounds of formula I as well as salts and prodrugs thereof.
摘要翻译：本发明提供了治疗分枝杆菌感染的方法和用式I化合物抑制分枝杆菌聚丙烯酰焦磷酸酯合成的方法。本发明还提供了新的式I化合物及其盐和前药。

9. 发明申请

WO2006026380A2 GERANYLGERANYL PYROPHOSPHATE SYNTHASE INHIBITORS 审中-公开
标题翻译： GERANYLGERANYL磷酸酯合酶抑制剂
公开(公告)号：WO2006026380A2
公开(公告)日：2006-03-09
申请号：PCT/US2005/030304
申请日：2005-08-25
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , WIEMER, David, F. , HOHL, Raymond, J.
发明人： WIEMER, David, F. , HOHL, Raymond, J.
CPC分类号： C07F9/4031 , C07F9/3847 , C07F9/3873 , C07F9/405
摘要： The invention provides novel pyrophosphate synthase inhibitors of formula I as well as compositions comprising such inhibitors and methods for their use.
摘要翻译：本发明提供了式I的新型焦磷酸合酶抑制剂以及包含这些抑制剂的组合物及其使用方法。

10. 发明申请

WO2005092878A2 SCHWEINFURTHIN ANALOGUES 审中-公开
标题翻译：辛伐他汀类似物
公开(公告)号：WO2005092878A2
公开(公告)日：2005-10-06
申请号：PCT/US2005/010482
申请日：2005-03-29
申请人： UNIVERSITY OF IOWA RESEARCH FOUNDATION , GOVERNMENT OF THE UNITED STATES OF AMERICA AS REPRESENTED BY THE SECRETARY OF THE DEPARTMENT OF HEALTH AND HUMAN SERVICES , WIEMER, David F. , NEIGHBORS, Jeffrey D. , BEUTLER, John A.
发明人： WIEMER, David F. , NEIGHBORS, Jeffrey D. , BEUTLER, John A.
IPC分类号： C07D311/00
CPC分类号： C07D311/80 , C07D311/78
摘要： Methods and intermediates for preparing enantiomerically enriched Schweinfurthin analogs which are useful for the treatment of cancer, as well as novel Schweinfurthin analogs having anti-cancer activity, compositions comprising such analogs and therapeutic methods comprising administering such analogs.
摘要翻译：用于制备可用于治疗癌症的对映体富集的施魏呋喃类似物的方法和中间体，以及具有抗癌活性的新型施魏因乙酰类似物，包含此类类似物的组合物和包括施用此类类似物的治疗方法。

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