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1. 发明专利

DE60114022D1 未知
公开(公告)号：DE60114022D1
公开(公告)日：2006-02-23
申请号：DE60114022
申请日：2001-05-30
申请人： UNIV WAYNE STATE , MOBASHERY SHAHRIAR , FRIDMAN RAFAEL
发明人： MOBASHERY SHAHRIAR , FRIDMAN RAFAEL
IPC分类号： A61K31/336 , A61P35/00 , C07D303/34 , C07D331/02
摘要： The invention provides compounds that inhibit MMPs; methods for treating or preventing cancer, angiogenesis, arthritis, connective tissue disease, cardiovascular disease, inflammation or autoimmune disease in a mammal; a method for inhibiting a matrix metalloproteinase in vivo or in vitro; and a method for imaging a tumor in vivo or in vitro.

2. 发明授权

EP1309579B1 INHIBITORS OF MATRIX METALLOPROTEINASES 有权
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：EP1309579B1
公开(公告)日：2005-10-12
申请号：EP01939690.2
申请日：2001-05-30
申请人： BOARD OF GOVERNORS OF WAYNE STATE UNIVERSITY , Mobashery, Shahriar , Fridman, Rafael
发明人： MOBASHERY, Shahriar , FRIDMAN, Rafael
IPC分类号： C07D303/34 , C07D331/02 , A61K31/336 , A61P35/00
CPC分类号： C07D331/02 , C07D303/34

3. 发明公开

EP1309579A1 INHIBITORS OF MATRIX METALLOPROTEINASES 有权
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：EP1309579A1
公开(公告)日：2003-05-14
申请号：EP01939690.2
申请日：2001-05-30
申请人： BOARD OF GOVERNORSOF WAYNE STATE UNIVERSITY , Mobashery, Shahriar , Fridman, Rafael
发明人： MOBASHERY, Shahriar , FRIDMAN, Rafael
IPC分类号： C07D303/34 , C07D331/02 , A61K31/336 , A61P35/00
CPC分类号： C07D331/02 , C07D303/34
摘要： The invention provides compounds that inhibit MMPs; methods for treating or preventing cancer, angiogenesis, arthritis, connective tissue disease, cardiovascular disease, inflammation or autoimmune disease in a mammal; a method for inhibiting a matrix metalloproteinase in vivo or in vitro; and a method for imaging a tumor vivo or vitro.

4. 发明专利

DE60114022T2 未知
公开(公告)号：DE60114022T2
公开(公告)日：2006-07-13
申请号：DE60114022
申请日：2001-05-30
申请人： UNIV WAYNE STATE , MOBASHERY SHAHRIAR , FRIDMAN RAFAEL
发明人： MOBASHERY SHAHRIAR , FRIDMAN RAFAEL
IPC分类号： C07D303/34 , A61K31/336 , A61P35/00 , C07D331/02
摘要： The invention provides compounds that inhibit MMPs; methods for treating or preventing cancer, angiogenesis, arthritis, connective tissue disease, cardiovascular disease, inflammation or autoimmune disease in a mammal; a method for inhibiting a matrix metalloproteinase in vivo or in vitro; and a method for imaging a tumor in vivo or in vitro.

5. 发明专利

AU6518201A Inhibitors of matrix metalloproteinases 未知
公开(公告)号：AU6518201A
公开(公告)日：2001-12-11
申请号：AU6518201
申请日：2001-05-30
申请人： UNIV WAYNE STATE , MOBASHERY SHAHRIAR , FRIDMAN RAFAEL
发明人： MOBASHERY SHAHRIAR , FRIDMAN RAFAEL
IPC分类号： A61P35/00 , C07D303/34 , C07D331/02 , A61K31/336
摘要： The invention provides compounds that inhibit MMPs; methods for treating or preventing cancer, angiogenesis, arthritis, connective tissue disease, cardiovascular disease, inflammation or autoimmune disease in a mammal; a method for inhibiting a matrix metalloproteinase in vivo or in vitro; and a method for imaging a tumor in vivo or in vitro.

6. 发明申请

WO2002057281A3 AMINOGLYCOSIDES AS ANTIBIOTICS 审中-公开
公开(公告)号：WO2002057281A3
公开(公告)日：2002-07-25
申请号：PCT/US2001/045639
申请日：2001-11-01
申请人： WAYNE STATE UNIVERSITY , HADDAD, Jalal , KOTRA, Lakshmi , MOBASHERY, Shahriar
发明人： HADDAD, Jalal , KOTRA, Lakshmi , MOBASHERY, Shahriar
IPC分类号： C07H15/224
摘要： The present invention provides aminoglycosides and pharmaceutical compositions that include the aminoglycosides. The aminogylcosides are useful to treat or prevent infectious diseases (e.g., bacterial infections) in a mammal (e.g., human).

7. 发明申请

WO2011026107A1 PHTHALANILATE COMPOUNDS AND METHODS OF USE 审中-公开
标题翻译：邻苯二甲酸酯化合物及其使用方法
公开(公告)号：WO2011026107A1
公开(公告)日：2011-03-03
申请号：PCT/US2010/047322
申请日：2010-08-31
申请人： UNIVERSITY OF NOTRE DAME DU LAC , MOBASHERY, Shahriar , HESEK, Dusan , CHANG, Mayland
发明人： MOBASHERY, Shahriar , HESEK, Dusan , CHANG, Mayland
IPC分类号： A01N37/18 , A61K31/16 , A61K31/165
CPC分类号： C07D513/04 , C07C233/15 , C07C233/26 , C07C233/59 , C07C233/60 , C07C233/66 , C07C233/69 , C07C233/73 , C07C233/75 , C07C233/81 , C07C235/16 , C07C235/74 , C07C235/84 , C07C271/58 , C07C327/48 , C07C333/08 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/46 , C07D213/75 , C07D215/40 , C07D295/108 , C07D295/135 , C07D295/155 , C07D295/192 , C07D307/52 , C07D319/16 , C07D339/08 , C07D495/04 , C07D501/34
摘要： The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo .
摘要翻译：本发明提供了抗微生物化合物和组合物，以及使用它们的方法。化合物和组合物包括例如式I-X中任一项的化合物。本发明还提供了制备该化合物的方法及其制备用途的中间体。该化合物可以具有高度特异性和选择性的活性，例如抗菌活性和/或酶促抑制活性。因此，化合物和组合物可用于治疗细菌感染，或在体外或体内抑制或杀死细菌。

8. 发明申请

WO2009082398A1 ANTIBACTERIAL COMPOUNDS AND METHODS OF USING SAME 审中-公开
标题翻译：抗菌化合物及其使用方法
公开(公告)号：WO2009082398A1
公开(公告)日：2009-07-02
申请号：PCT/US2007/088602
申请日：2007-12-21
申请人： UNIVERSITY OF NOTRE DAME DU LAC , MOBASHERY, Shahriar , O'DANIEL, Peter, I. , CHANG, Mayland
发明人： MOBASHERY, Shahriar , O'DANIEL, Peter, I. , CHANG, Mayland
IPC分类号： C12P21/02
CPC分类号： C07D271/06 , C07D413/12 , C07F9/65318
摘要： Embodiments of the present invention provide novel antibactehals that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus .
摘要翻译：本发明的实施方案提供靶向青霉素结合蛋白或其它重要细胞靶标的新型抗细胞因子。还提供了使用本文所述化合物抑制细菌生长（繁殖等）的方法。各种实施方案表现出对革兰氏阳性细菌的活性，例如肠球菌和金黄色葡萄球菌的某些菌株。

9. 发明申请

WO1991005555A2 N-ACYL PEPTIDE METALLOENDOPEPTIDASE INHIBITORS AND METHODS OF USING SAME 审中-公开
标题翻译： N-乙酰哌嗪类抗生素抑制剂及其使用方法
公开(公告)号：WO1991005555A2
公开(公告)日：1991-05-02
申请号：PCT/US1990005904
申请日：1990-10-15
申请人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ... , WAYNE STATE UNIVERSITY , GHOSH, Soumitra, Shankar , MOBASHERY, Shahriar
发明人： THE SALK INSTITUTE BIOTECHNOLOGY/INDUSTRIAL ... , WAYNE STATE UNIVERSITY
IPC分类号： A61K31/40
CPC分类号： C07K5/0827 , A61K38/00 , C07C233/51 , C07D207/16 , C07K5/06026 , C07K5/06078 , C07K5/06191 , C07K5/0806 , C07K5/0808
摘要： Inhibitors of the Zn -metalloendopeptidases, enkephalinase, angiotensin-converting enzyme, and collagenase, intermediates for synthesizing the inhibitors, and methods of making and using the inhibitors, are provided. The enkephalinase inhibitors of the invention are useful as analgesics or antihypertensives. The angiotensin-converting enzyme inhibitors of the invention are useful as anti-hypertensives. The collagenase inhibitors of the invention are useful in treating diseases, such as corneal ulceration, periodontal disease, and arthritis, which involve undesirable collagen degradation. The inhibitors of the invention are peptide or peptide ester derivatives of the intermediates of the invention, whichare N-acyl derivatives of amino acids of the formula X10-NH-CHR9-(CO2H), wherein X10 is selected from the group consisting of N=C-CHR20-(C=O)- and X21(CR22R23)(CHR24)(C=O)-, wherein R20 is hydrogen or alkyl of 1 to 3 carbon atoms, R22, R23 and R24 are each independently hydrogen or alkyl of 1 to 3 carbon atoms, and X21 is fluoro, chloro or bromo; and R9 is benzyl, alkyl of 1-5 carbon atoms, or hydrogen.
摘要翻译：提供了Zn 2+ - 金属间环肽酶，脑啡肽酶，血管紧张素转化酶和胶原酶的抑制剂，用于合成抑制剂的中间体，以及制备和使用抑制剂的方法。本发明的脑啡肽酶抑制剂可用作镇痛药或抗高血压药。本发明的血管紧张素转换酶抑制剂可用作抗高血压药。本发明的胶原酶抑制剂可用于治疗涉及不期望的胶原蛋白降解的疾病，例如角膜溃疡，牙周病和关节炎。本发明的抑制剂是本发明中间体的肽或肽酯衍生物，其为式X10-NH-CHR9-（CO2H）的氨基酸的N-酰基衍生物，其中X10选自N = C-CHR 20 - （C = O） - 和X 21（CR 22 R 23）（CHR 24）（C = O） - ，其中R 20是氢或1至3个碳原子的烷基，R 22，R 23和R 24各自独立地是氢或 1至3个碳原子，X 21为氟，氯或溴; 并且R 9为苄基，1-5个碳原子的烷基或氢。

10. 发明申请

WO2022005976A2 ANTIBACTERIAL PICOLINAMIDE COMPOUNDS 审中-公开
公开(公告)号：WO2022005976A2
公开(公告)日：2022-01-06
申请号：PCT/US2021/039381
申请日：2021-06-28
申请人： UNIVERSITY OF NOTRE DAME DU LAC , MOBASHERY, Shahriar , CHANG, Mayland , SPERI, Enrico
发明人： MOBASHERY, Shahriar , CHANG, Mayland , SPERI, Enrico
IPC分类号： A01N25/00 , A01N37/44 , A01N43/10
摘要： Here we report the discovery of 2-(4-(3-(trifluoromethoxy)phenoxy)picolinamido) benzo[d]oxazole-5-carboxylate as an antibacterial with potent and selective activity against C. difficile. Its MIC50 and MIC90 values, documented across 101 strains of C. difficile, are 0.12 and 0.25 µg/mL, respectively. The compound is effective against C. difficile both at the logarithmic (vegetative) and stationary phases of growth. It targets cell-wall biosynthesis, as assessed both by macromolecular biosynthesis assays and by scanning-electron microscopy. Animals infected with a lethal dose of C. difficile and treated with compound 1 had better survival compared to treatment with vancomycin, which is the front-line antibiotic used for severe recurrent C. difficile infection.

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