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1. 发明申请

US20140187546A1 Cystine Diamide Analogs for the Prevention of Cystine Stone Formation in Cystinuria 有权
标题翻译：胱氨酸二酰胺类似物用于预防胱氨酸尿中胱氨酸石形成
公开(公告)号：US20140187546A1
公开(公告)日：2014-07-03
申请号：US14146103
申请日：2014-01-02
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Amrik Sahota
IPC分类号： C07C323/60 , C07D295/185 , C07C319/24
CPC分类号： C07D295/185 , C07C323/60 , C07C2101/02 , C07C2601/02 , C07D211/16
摘要： Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
摘要翻译：提高L-胱氨酸在尿中用于治疗尿胱症的结构的胱氨酸类似物及其药学上可接受的盐，溶剂合物和前药，其中每个R和R'对独立地选自（i）或（ii） ; （i）R和R'独立地选自氢，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的醇，取代或未取代的芳基，取代或未取代的环烷基，取代或未取代的杂环，以及取代或未取代的杂芳基，或（ii）R和R'一起形成取代或未取代的杂环结构，或取代或未取代的杂芳基环结构; X是氢或烷基; Y是O或S.

2. 发明申请

US20230002337A1 CYSTINE DIAMIDE ANALOGS FOR THE PREVENTION OF CYSTINE STONE FORMATION IN CYSTINURIA 有权
公开(公告)号：US20230002337A1
公开(公告)日：2023-01-05
申请号：US17821376
申请日：2022-08-22
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Amrik Sahota
IPC分类号： C07D295/185 , C07C323/60 , C07D211/16
摘要： Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.

3. 发明申请

US20180148408A1 DIRECT INHIBITORS OF KEAP1-NRF2 INTERACTION AS ANTIOXIDANT INFLAMMATION MODULATORS 审中-公开
公开(公告)号：US20180148408A1
公开(公告)日：2018-05-31
申请号：US15718987
申请日：2017-09-28
申请人： Rutgers, The State University of New Jersey , The Broad Institute, Inc.
发明人： Longqin Hu , Sadagopan Magesh , Lin Chen , Timothy Lewis , Ben Munoz , Lili Wang
IPC分类号： C07D209/48 , A61K31/472 , C07D207/452 , C07D405/12 , C07D401/06 , A61K31/4725 , C07D401/14 , G01N33/50 , C07D217/16 , C07D335/06
CPC分类号： C07D209/48 , A61K31/472 , A61K31/4725 , C07D207/452 , C07D217/16 , C07D335/06 , C07D401/06 , C07D401/14 , C07D405/12 , G01N33/5023
摘要： A method of identifying compounds as direct inhibitors of Keap1-Nrf2 interaction through high-throughput screening and lead development. The direct inhibitors of Keap1-Nrf2 interaction are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential drug candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, and Parkinson's. Novel compounds are identified and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds identified or compositions containing such compounds are also disclosed.

4. 发明申请

US20160362386A1 CYSTINE DIAMIDE ANALOGS FOR THE PREVENTION OF CYSTINE STONE FORMATION IN CYSTINURIA 审中-公开
标题翻译： CYSTINE DIAMIDE ANALOGS FOR CYSTINURIA CYSTINE STONE
公开(公告)号：US20160362386A1
公开(公告)日：2016-12-15
申请号：US15248912
申请日：2016-08-26
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Amrik Sahota
IPC分类号： C07D295/185 , C07D211/16 , C07C323/60
CPC分类号： C07D295/185 , C07C323/60 , C07C2601/02 , C07D211/16
摘要： Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
摘要翻译：提高L-胱氨酸在尿中用于治疗尿胱症的结构的胱氨酸类似物及其药学上可接受的盐，溶剂合物和前药，其中每个R和R'对独立地选自（i）或（ii） ; （i）R和R'独立地选自氢，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的醇，取代或未取代的芳基，取代或未取代的环烷基，取代或未取代的杂环，以及取代或未取代的杂芳基，或（ii）R和R'一起形成取代或未取代的杂环结构，或取代或未取代的杂芳基环结构; X是氢或烷基; Y是O或S.

5. 发明申请

US20230043330A1 Cystine Diamide Analogs For Cystinuria 有权
公开(公告)号：US20230043330A1
公开(公告)日：2023-02-09
申请号：US17757244
申请日：2020-12-11
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Haifa Albanyan
IPC分类号： C07D295/185 , C07D241/04 , C07D295/13 , C07C323/41 , C07D211/58 , C07D471/10
摘要： This document discloses novel cystine analogs, methods of making cystine analogs, compositions containing cystine analogs and methods of using such analogs for inhibiting cystine stone formation and treatment of cystinuria.

6. 发明授权

US11129901B2 Peptide-linked ester prodrugs activated by prostate-specific antigen 有权
公开(公告)号：US11129901B2
公开(公告)日：2021-09-28
申请号：US16482775
申请日：2018-02-02
申请人： RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
发明人： Longqin Hu , Herve Aloysius
IPC分类号： A61K47/64 , A61P35/00 , A61K31/704 , C07K7/02
摘要： The present disclosure is directed to a series of target-selective chemotherapeutic ester prodrugs comprising PSA-cleavable peptides that promote the delivery of free doxorubicin and other chemotherapeutic agents into the prostate and/or prostate tumors with greater efficiency.

7. 发明授权

US11628221B2 Peptide linker and combination for prodrugs activated by prostate-specific antigen 有权
公开(公告)号：US11628221B2
公开(公告)日：2023-04-18
申请号：US17481102
申请日：2021-09-21
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Herve Aloysius
IPC分类号： A61K47/64 , A61P35/00 , A61K31/704 , C07K7/02
摘要： The present disclosure is directed to a series of target-selective chemotherapeutic ester prodrugs comprising PSA-cleavable peptides that promote the delivery of free doxorubicin and other chemotherapeutic agents into the prostate and/or prostate tumors with greater efficiency.

8. 发明申请

US20220112160A1 SMALL MOLECULE DIRECT INHIBITORS OF KEAP1-NRF2 PROTEIN-PROTEIN INTERACTION 有权
公开(公告)号：US20220112160A1
公开(公告)日：2022-04-14
申请号：US17423688
申请日：2020-01-16
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Dhulfiqar A. Abed
IPC分类号： C07C323/67 , C07C315/04 , C07D407/12 , C07D403/12 , C07D209/14 , C07D209/48 , C07D405/14 , C07D333/58
摘要： This patent document discloses novel compounds and methods of preventing or treating diseases or conditions related to Keap1-Nrf2 interaction activity by use of the novel compounds. As direct inhibitors of Keap1-Nrf2 interaction, the compounds disclosed herein are more specific and free of various undesirable effects than existing indirect inhibitors, and are potential dmg candidates of chemopreventive and therapeutic agents for treatment of various diseases or conditions involving oxidative stress and/or inflammation, including but not limited to cancers, diabetes, Alzheimer's, Parkinson's, and inflammatory bowel disease including ulcerative colitis.

9. 发明授权

US09428453B2 Cystine diamide analogs for the prevention of cystine stone formation in cystinuria 有权
标题翻译：胱氨酸二酰胺类似物用于预防胱氨酸尿中胱氨酸石形成
公开(公告)号：US09428453B2
公开(公告)日：2016-08-30
申请号：US14146103
申请日：2014-01-02
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu , Amrik Sahota
IPC分类号： C07C323/60 , C07D295/185
CPC分类号： C07D295/185 , C07C323/60 , C07C2101/02 , C07C2601/02 , C07D211/16
摘要： Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.
摘要翻译：提高L-胱氨酸在尿中用于治疗尿胱症的结构的胱氨酸类似物及其药学上可接受的盐，溶剂合物和前药，其中每个R和R'对独立地选自（i）或（ii） ; （i）R和R'独立地选自氢，取代或未取代的烷基，取代或未取代的烯基，取代或未取代的醇，取代或未取代的芳基，取代或未取代的环烷基，取代或未取代的杂环，以及取代或未取代的杂芳基，或（ii）R和R'一起形成取代或未取代的杂环结构，或取代或未取代的杂芳基环结构; X是氢或烷基; Y是O或S.

10. 发明授权

US11420949B2 Cystine diamide analogs for the prevention of cystine stone formation in cystinuria 有权
公开(公告)号：US11420949B2
公开(公告)日：2022-08-23
申请号：US17068354
申请日：2020-10-12
申请人： Rutgers, The State University of New Jersey
发明人： Longqin Hu
IPC分类号： C07D295/185 , C07D211/16 , C07C323/60
摘要： Cystine analogs that improve the solubility of L-cystine in urine for treatment of cystinuria and which have the structure: and pharmaceutically acceptable salts, solvates and prodrugs thereof, wherein each R and R′ pair are independently selected from (i) or (ii); (i) R and R′ are independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alcohol, substituted or unsubstituted aryl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocyclic, and substituted or unsubstituted heteroaryl, or (ii) R and R′ together form a substituted or unsubstituted heterocyclic ring structure, or a substituted or unsubstituted heteroaryl ring structure; X is hydrogen, or an alkyl; and Y is O or S.

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