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公开(公告)号：US07491743B2
公开(公告)日：2009-02-17
申请号：US10930690
申请日：2004-08-30
申请人： Gregory D. Cuny , Junying Yuan , Prakash Jagtap , Alexei Degterev
发明人： Gregory D. Cuny , Junying Yuan , Prakash Jagtap , Alexei Degterev
IPC分类号： A61K31/415 , C07D403/02
CPC分类号： C07D409/06 , C07D403/06 , C07D405/06 , C07D413/06 , C07D471/04
摘要： The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis.
摘要翻译： 本发明涉及化合物和药物制剂及其在预防或治疗与细胞死亡有关的创伤，缺血，中风和退行性疾病的治疗中的用途。 本发明的方法和组合物特别可用于治疗与细胞坏死相关的神经障碍。
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公开(公告)号：US06703508B2
公开(公告)日：2004-03-09
申请号：US10012242
申请日：2001-12-04
申请人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Michelle L. R. Heffernan , Michael Z. Hoemann , Donald W. Kessler , Liming Shao , Xinhe Wu , Roger L. Xie
发明人： Brian M. Aquila , Thomas D. Bannister , Gregory D. Cuny , James R. Hauske , Michelle L. R. Heffernan , Michael Z. Hoemann , Donald W. Kessler , Liming Shao , Xinhe Wu , Roger L. Xie
IPC分类号： C07D21130
CPC分类号： C07D211/22 , C07D211/26
摘要： One aspect of the present invention relates to methods of synthesizing substituted piperidines. A second aspect of the present invention relates to stereoselective methods of synthesizing substituted piperidines. The methods of the present invention will find use in the synthesis of compounds useful for treatment of numerous ailments, conditions and diseases that afflict mammals, including but not limited to addiction and pain. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the substituted piperidines using the methods of the present invention. An additional aspect of the present invention relates to enantiomerically substituted pyrrolidines, piperidines, and azepines.
摘要翻译： 本发明的一个方面涉及合成取代的哌啶的方法。 本发明的第二方面涉及合成取代的哌啶的立体选择性方法。 本发明的方法将用于合成可用于治疗许多疾病，病症和疾病的哺乳动物，包括但不限于成瘾和疼痛。 本发明的另一方面涉及使用本发明的方法合成取代的哌啶的组合文库。 本发明的另一方面涉及对映体取代的吡咯烷，哌啶和吖庚因。
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公开(公告)号：US06605416B2
公开(公告)日：2003-08-12
申请号：US09017001
申请日：1998-02-02
申请人： Stanley C. Busman , Richard J. Ellis , Jeanne E. Haubrich , William D. Ramsden , Tran Van Thien , Gregory D. Cuny
发明人： Stanley C. Busman , Richard J. Ellis , Jeanne E. Haubrich , William D. Ramsden , Tran Van Thien , Gregory D. Cuny
IPC分类号： G03F730
CPC分类号： G03F7/0045 , C09B57/007 , G03F7/0382 , G03F7/0392 , Y10S430/121 , Y10S430/127 , Y10S430/145 , Y10S430/146
摘要： Photochemical acid progenitors in combination with dihydroperimidine squarylium dyes have been found to be particularly effective at generating acid upon irradiation with near-infrared radiation. It has been found that dihydroperimidine squarylium dyes that are particularly useful in this invention have an oxidation potential greater than about 0.5 V relative to SCE as measured in dichloromethane.
摘要翻译： 已经发现光化学酸性祖细胞与二氢嘧啶方菁染料的组合在用近红外辐射照射时产生酸是特别有效的。 已经发现在本发明中特别有用的二氢嘧啶方酸菁染料相对于在二氯甲烷中测得的SCE，其氧化势大于约0.5V。
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34.发明授权Quinoline-indole antimicrobial agents, uses and compositions related thereto 失效喹啉 - 吲哚抗微生物剂，其用途和组合物公开(公告)号：US06376670B1
公开(公告)日：2002-04-23
申请号：US09658690
申请日：2000-09-08
IPC分类号： A61K3144
CPC分类号： C07D401/14 , C07D209/12 , C07D209/14 , C07D215/52 , C07D401/04 , C07D405/04 , C07D405/14 , C07D409/04 , C07D453/02 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms, via a non-lytic mechanism. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms, via a non-lytic mechanism.
摘要翻译： 本发明提供通过非裂解机制抑制细菌微生物生长的方法和药物制剂。 另外，本发明提供了通过非裂解机制杀死细菌微生物的方法和药物制剂。
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公开(公告)号：US06207679B1
公开(公告)日：2001-03-27
申请号：US09045051
申请日：1998-03-19
申请人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi
发明人： Gregory D. Cuny , James R. Hauske , Donald L. Heefner , Michael Z. Hoemann , Gnanasambandam Kumaravel , Anita Melikian-Badalian , Richard F. Rossi
IPC分类号： A61K314709
CPC分类号： C07D401/14 , C07D209/12 , C07D209/14 , C07D215/52 , C07D401/04 , C07D405/04 , C07D409/04 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.
摘要翻译： 本发明提供抑制细菌微生物生长的方法和药物制剂。 此外，本发明提供杀死细菌微生物的方法和药物制剂。
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36.发明授权Di- and tetra-hydroquinoline-indole antimicrobial agents, uses and compositions related thereto 失效二 - 和四氢喹啉 - 吲哚抗菌剂，其用途和组合物公开(公告)号：US06180640B2
公开(公告)日：2001-01-30
申请号：US09344619
申请日：1999-06-25
IPC分类号： A61K314741
CPC分类号： C07D401/04 , C07D471/04 , C07D491/04
摘要： The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.
摘要翻译： 本发明提供抑制细菌微生物生长的方法和药物制剂。 此外，本发明提供杀死细菌微生物的方法和药物制剂。
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公开(公告)号：US09518032B2
公开(公告)日：2016-12-13
申请号：US13695036
申请日：2011-04-29
申请人： Alan D. D'Andrea , Gregory D. Cuny , Ross L. Stein , Marcie Glicksman , April Case , Jun Xian , David Wilson , Min Huang
发明人： Alan D. D'Andrea , Gregory D. Cuny , Ross L. Stein , Marcie Glicksman , April Case , Jun Xian , David Wilson , Min Huang
IPC分类号： C07D263/60 , A61K45/06 , C07D405/06 , A61K31/136 , C07D217/24 , A61K31/472 , C07C225/30 , A61K31/423 , A61K31/4725
CPC分类号： A61K31/423 , A61K31/136 , A61K31/472 , A61K31/4725 , A61K45/06 , C07C225/30 , C07D217/24 , C07D263/60 , C07D405/06
摘要： Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.
摘要翻译： 提供泛素特异性蛋白酶1（USP1）活性的小分子抑制剂及其用于治疗和表征癌症的方法。 本发明的小分子USP1抑制剂特别可用于治疗对DNA交联剂有抗性的癌症。
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公开(公告)号：US09126938B2
公开(公告)日：2015-09-08
申请号：US13390910
申请日：2010-08-17
申请人： David Cohen , Neil Wagle , Gregory D. Cuny , Jun Xian , Marcie Glicksman , Ross L. Stein , Ekaterina Y. Shishova
发明人： David Cohen , Neil Wagle , Gregory D. Cuny , Jun Xian , Marcie Glicksman , Ross L. Stein , Ekaterina Y. Shishova
IPC分类号： C07D239/42 , A61K31/505 , A61P1/16 , A61P3/04 , A61P3/10 , A61P9/10 , A61P11/06 , C07D213/60 , A61K31/44 , C07D239/32
CPC分类号： C07D239/69 , A61K31/44 , A61K31/505 , C07C311/21 , C07D213/60 , C07D213/76 , C07D213/89 , C07D217/22 , C07D239/32 , C07D239/42
摘要： This invention relates to compounds of Formulas I, II, and III, and their use as inhibitors of phosphatidylcholine transfer protein (PC-TP). The invention further relates to pharmaceutical compositions and methods of treatment of disorders related to the inhibition of PC-TP using the compounds of Formulas I, II, and III. Such disorders include obesity and disorders associated with obesity.
摘要翻译： 本发明涉及式I，II和III的化合物及其作为磷脂酰胆碱转移蛋白抑制剂（PC-TP）的用途。 本发明还涉及使用式I，II和III的化合物治疗与PC-TP的抑制相关的病症的药物组合物和方法。 这种疾病包括肥胖症和与肥胖相关的疾病。
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39.发明授权Compounds and methods for treating mammalian gastrointestinal microbial infections 有权用于治疗哺乳动物胃肠道微生物感染的化合物和方法公开(公告)号：US08969342B2
公开(公告)日：2015-03-03
申请号：US13257418
申请日：2010-03-22
申请人： Lizbeth K. Hedstrom , Gregory D. Cuny , Deviprasad R. Gollapalli , Boris Striepen , Suresh Kumar Gorla , Mandapati Kavitha
发明人： Lizbeth K. Hedstrom , Gregory D. Cuny , Deviprasad R. Gollapalli , Boris Striepen , Suresh Kumar Gorla , Mandapati Kavitha
IPC分类号： A61K31/535
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。
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公开(公告)号：US20130253005A1
公开(公告)日：2013-09-26
申请号：US13695036
申请日：2011-04-29
申请人： Alan D. D'Andrea , Gregory D. Cuny , Ross L. Stein , Marcie Glicksman , April Case , Jun Xian , David Wilson , Min Huang
发明人： Alan D. D'Andrea , Gregory D. Cuny , Ross L. Stein , Marcie Glicksman , April Case , Jun Xian , David Wilson , Min Huang
IPC分类号： C07D263/60 , A61K45/06 , C07D405/06 , A61K31/136 , C07D217/24 , A61K31/472 , C07C225/30 , A61K31/423 , A61K31/4725
CPC分类号： A61K31/423 , A61K31/136 , A61K31/472 , A61K31/4725 , A61K45/06 , C07C225/30 , C07D217/24 , C07D263/60 , C07D405/06
摘要： Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.
摘要翻译： 提供泛素特异性蛋白酶1（USP1）活性的小分子抑制剂及其用于治疗和表征癌症的方法。 本发明的小分子USP1抑制剂特别可用于治疗对DNA交联剂有抗性的癌症。
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