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1.发明申请Phosphonated Fluoroquinolones, Antibacterial Analogs Thereof, and Methods for the Prevention and Treatment of Bone and Joint Infections 审中-公开磷酸化氟喹诺酮类抗生素类抗生素及预防和治疗骨关节感染的方法公开(公告)号：US20080287396A1
公开(公告)日：2008-11-20
申请号：US11912038
申请日：2006-04-21
申请人： Daniel Delorme , Tom Houghton , Ting Kang , Kelly Tanaka , Yanick LaFontaine , Evelyne Dietrich , Adel Rafai Far
发明人： Daniel Delorme , Tom Houghton , Ting Kang , Kelly Tanaka , Yanick LaFontaine , Evelyne Dietrich , Adel Rafai Far
IPC分类号： A61K31/675 , C07D401/02 , A61P31/04
CPC分类号： C07F9/65586 , C07F9/65583 , C07F9/6561
摘要： The present invention relates to phosphonated fluoroquinolones, antibacterial analogs thereof, and methods of using such compounds. These compounds are useful as antibiotics for prevention and/or the treatment of bone and joint infections, especially for the prevention and/or treatment of osteomyelitis.
摘要翻译： 本发明涉及膦酸化氟喹诺酮类，其抗菌类似物和使用这些化合物的方法。 这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。
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2.发明申请PHOSPHONATED RIFAMYCINS AND USES THEREOF FOR THE PREVENTION AND TREATMENT OF BONE AND JOINT INFECTIONS 有权磷酸缓释片及其用于预防和治疗骨和关节感染的用途公开(公告)号：US20110178001A1
公开(公告)日：2011-07-21
申请号：US13058518
申请日：2009-08-10
申请人： Evelyne Dietrich , Ranga Reddy , Kelly Tanaka , Ting Kang , Yanick Lafontaine , Adel Rafai Far
发明人： Evelyne Dietrich , Ranga Reddy , Kelly Tanaka , Ting Kang , Yanick Lafontaine , Adel Rafai Far
IPC分类号： A61K31/675 , C07F9/6561 , A61P31/04 , A61K38/14 , A61K38/12
CPC分类号： C07F9/6561 , A61K31/675 , A61K47/548
摘要： The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
摘要翻译： 本发明涉及膦酸化的利福霉素，以及制备和使用这些化合物的方法。 这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。
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3.发明授权Phosphonated rifamycins and uses thereof for the prevention and treatment of bone and joint infections 有权磷酸化的利福霉素及其用于预防和治疗骨和关节感染的用途公开(公告)号：US08524691B2
公开(公告)日：2013-09-03
申请号：US13058518
申请日：2009-08-10
申请人： Evelyne Dietrich , Ranga Reddy , Kelly Tanaka , Ting Kang , Yanick LaFontaine , Adel Rafai Far
发明人： Evelyne Dietrich , Ranga Reddy , Kelly Tanaka , Ting Kang , Yanick LaFontaine , Adel Rafai Far
IPC分类号： A01N57/00 , A61K31/66 , C07D225/04
CPC分类号： C07F9/6561 , A61K31/675 , A61K47/548
摘要： The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
摘要翻译： 本发明涉及膦酸化的利福霉素，以及制备和使用这些化合物的方法。 这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。
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4.发明授权Phosphonated Rifamycins and uses thereof for the prevention and treatment of bone and joint infections 有权磷酸化的利福霉素及其用于预防和治疗骨和关节感染的用途公开(公告)号：US08404664B2
公开(公告)日：2013-03-26
申请号：US12063300
申请日：2006-08-11
申请人： Yannick Stephane Rose , Stephane Ciblat , Ting Kang , Adel Rafai Far , Evelyne Dietrich , Yanick Lafontaine , Ranga Reddy
发明人： Yannick Stephane Rose , Stephane Ciblat , Ting Kang , Adel Rafai Far , Evelyne Dietrich , Yanick Lafontaine , Ranga Reddy
IPC分类号： A01N57/00 , A61K31/66 , C07D225/04
CPC分类号： C07F9/6561 , A61K47/548
摘要： The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
摘要翻译： 本发明涉及膦酸化的利福霉素，以及制备和使用这些化合物的方法。 这些化合物可用作预防和/或治疗骨和关节感染的抗生素，特别是用于预防和/或治疗骨髓炎。
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公开(公告)号：US20110263534A1
公开(公告)日：2011-10-27
申请号：US12063300
申请日：2006-08-11
申请人： Yannick Stephane Rose , Stephane Ciblat , Ting Kang , Adel Rafai Far , Evelyne Dietrich , Yanick Lafontaine , Ranga Reddy
发明人： Yannick Stephane Rose , Stephane Ciblat , Ting Kang , Adel Rafai Far , Evelyne Dietrich , Yanick Lafontaine , Ranga Reddy
IPC分类号： A61K31/675 , A61P31/04 , C07D498/16 , C07D498/06 , C07D498/22
CPC分类号： C07F9/6561 , A61K47/548
摘要： The present invention relates to phosphonated Rifamycins, and methods of making and using such compounds. These compounds are useful as antibiotics for prophylaxis and/or the treatment of bone and joint infections, especially for the prophylaxis and/or treatment of osteomyelitis.
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公开(公告)号：US08901072B2
公开(公告)日：2014-12-02
申请号：US13389993
申请日：2010-08-11
申请人： Adel Rafai Far , Kelly Tanaka , Evelyne Dietrich , Ranga Reddy , Ting Kang
发明人： Adel Rafai Far , Kelly Tanaka , Evelyne Dietrich , Ranga Reddy , Ting Kang
CPC分类号： C07K9/008 , A61K38/12 , A61K38/14 , A61K45/06 , A61K47/48038 , A61K47/48046 , A61K47/48215 , A61K47/542 , A61K47/543 , A61K47/60 , A61K2300/00
摘要： The invention relates to derivatives of glycopeptide and lipoglycopeptide antibiotics possessing an altered ionization state with respect to the parent glycopeptide or lipoglycopeptide antibiotic, and having the ability to be regenerated as the parent glycopeptide or lipoglycopeptide antibiotic under physiological conditions. These compounds are useful as antibiotics for the prevention and/or the treatment of bacterial infections.
摘要翻译： 本发明涉及相对于母体糖肽或脂多糖抗生素具有改变的电离状态的糖肽和脂多糖抗生素的衍生物，并且具有在生理条件下作为母体糖肽或脂多糖抗生素再生的能力。 这些化合物可用作预防和/或治疗细菌感染的抗生素。
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公开(公告)号：US20120149632A1
公开(公告)日：2012-06-14
申请号：US13389993
申请日：2010-08-11
申请人： Adel Rafai Far , Kelly Tanaka , Evelyne Dietrich , Ranga Reddy , Ting Kang
发明人： Adel Rafai Far , Kelly Tanaka , Evelyne Dietrich , Ranga Reddy , Ting Kang
CPC分类号： C07K9/008 , A61K38/12 , A61K38/14 , A61K45/06 , A61K47/48038 , A61K47/48046 , A61K47/48215 , A61K47/542 , A61K47/543 , A61K47/60 , A61K2300/00
摘要： The invention relates to derivatives of glycopeptide and lipoglycopeptide antibiotics possessing an altered ionization state with respect to the parent glycopeptide or lipoglycopeptide antibiotic, and having the ability to be regenerated as the parent glycopeptide or lipoglycopeptide antibiotic under physiological conditions. These compounds are useful as antibiotics for the prevention and/or the treatment of bacterial infections.
摘要翻译： 本发明涉及相对于母体糖肽或脂多糖抗生素具有改变的电离状态的糖肽和脂多糖抗生素的衍生物，并且具有在生理条件下作为母体糖肽或脂多糖抗生素再生的能力。 这些化合物可用作预防和/或治疗细菌感染的抗生素。
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8.发明授权公开(公告)号：US08946144B2
公开(公告)日：2015-02-03
申请号：US12520364
申请日：2007-12-21
IPC分类号： A61K38/00 , C07K9/00 , C07F9/6561
CPC分类号： C07K9/008 , A61K38/00 , C07F9/6561
摘要： The present invention is directed to antimicrobial compounds which have an affinity for binding bones. More particularly, the invention is directed to phosphonated derivatives of glycopeptide or lipoglycopeptide antibiotics. These compounds are useful as antibiotics for the prevention or treatment of bone and joint infections, especially for the prevention and treatment of osteomyelitis.
摘要翻译： 本发明涉及对结合骨的亲和力的抗微生物化合物。 更具体地，本发明涉及糖肽或脂多糖抗生素的膦酸化衍生物。 这些化合物可用作预防或治疗骨和关节感染的抗生素，特别是用于预防和治疗骨髓炎。
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9.发明申请公开(公告)号：US20100113333A1
公开(公告)日：2010-05-06
申请号：US12520364
申请日：2007-12-21
CPC分类号： C07K9/008 , A61K38/00 , C07F9/6561
摘要： The present invention is directed to antimicrobial compounds which have an affinity for binding bones. More particularly, the invention is directed to phosphonated derivatives of glycopeptide or lipoglycopeptide antibiotics. These compounds are useful as antibiotics for the prevention or treatment of bone and joint infections, especially for the prevention and treatment of osteomyelitis.
摘要翻译： 本发明涉及对结合骨的亲和力的抗微生物化合物。 更具体地，本发明涉及糖肽或脂多糖抗生素的膦酸化衍生物。 这些化合物可用作预防或治疗骨和关节感染的抗生素，特别是用于预防和治疗骨髓炎。
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10.发明申请TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, THEIR PREPARATION AND USE AS SELECTIVE INHIBITORS OF THE CLOTTING FACTORS IIA AND XA 有权TRYPSIN样丝氨酸蛋白酶抑制剂，其制备和用作选择性抑制剂IIA和XA的选择性抑制剂公开(公告)号：US20120252743A1
公开(公告)日：2012-10-04
申请号：US13332900
申请日：2011-12-21
申请人： Peter Herold , Stjepan Jelakovic , Mohammed Daghish , Claudia Reichelt , Alexander Schulze , Andrea Schweinitz , Friedrich-Alexander Ludwig , Adel Rafai Far , Ting Kang
发明人： Peter Herold , Stjepan Jelakovic , Mohammed Daghish , Claudia Reichelt , Alexander Schulze , Andrea Schweinitz , Friedrich-Alexander Ludwig , Adel Rafai Far , Ting Kang
CPC分类号： C07K5/06121 , A61K38/00 , C07K5/06104 , C07K5/06113 , C07K5/06191
摘要： The invention provides methods of making and using compounds of the formula: or a pharmaceutically acceptable salt thereof; wherein n is an integer between 1 and 2 inclusively; m is an integer between 0 and 2 inclusively; X is selected from the group consisting of CH or N; R1 is selected from the group consisting of —CH2NH2, and R2 is selected from the group consisting of —H, —OH, —NH2 and acetyl; R3 is selected from the group consisting of —H, benzyloxycarbonyl and benzylsulfonyl; and R4 is selected from the group consisting of —OH, wherein p is an integer between 0 and 2 inclusively, Y is selected from the group consisting of —O—, —S—, —S(═O)—, —SO2—, methylene, —CH(OH)—, —CH(NH2)—, —CH(CH2—OH)—, —CH(CH2—NH2)— or —N(R6)—, R5 is selected from the group consisting of —H or a simple (C1-C3) alkyl and R6 is selected from the group consisting of —H, a simple (C1-C3) alkyl or a simple (C1-C3) acyl. These compounds are useful as anticoagulant agents as a result of their selective dual inhibition of thrombin and prothrombinase.
摘要翻译： 本发明提供制备和使用下式的化合物或其药学上可接受的盐的方法： 其中n是1和2之间的整数; m是0和2之间的整数; X选自CH或N; R1选自-CH2NH2，R2选自-H，-OH，-NH2和乙酰基; R3选自-H，苄氧基羰基和苄基磺酰基; 并且R 4选自-OH，其中p是包括0和2之间的整数，Y选自-O - ， - S - ， - S（= O） - ， - SO 2 - ，亚甲基，-CH（OH） - ， - CH（NH 2） - ， - CH（CH 2 -OH） - ， - CH（CH 2 -NH 2） - 或-N（R 6） - ，R 5选自 -H或简单（C 1 -C 3）烷基，R 6选自-H，简单（C 1 -C 3）烷基或简单（C 1 -C 3）酰基）。 由于它们选择性双重抑制凝血酶和凝血酶原酶，这些化合物可用作抗凝血剂。
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