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公开(公告)号：US06252063B1
公开(公告)日：2001-06-26
申请号：US09432864
申请日：1999-11-02
申请人： Ross A. Miller , Scott S. Ceglia
发明人： Ross A. Miller , Scott S. Ceglia
IPC分类号： A61K314995
CPC分类号： C07D519/00
摘要： Crystalline salts of an amorphous, unstable carbapenem antibiotic having the formula: are disclosed, wherein R− represents beyslate, tosylate, napsylate, saccharate or alizarate.
摘要翻译： 公开了具有下式的无定形，不稳定的碳青霉烯类抗生素的结晶盐：其中R-代表异硬脂酸酯，甲苯磺酸酯，萘磺酸酯，糖酸酯或异柠檬酸酯。
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公开(公告)号：US20170174720A9
公开(公告)日：2017-06-22
申请号：US15135928
申请日：2016-04-22
申请人： Paul B. Savage , Saurabh Shashikant Chitre , Kunal Arvind Varia , Hayley Ann Reece , Thomas E. Jacks , Ross A. Miller , Jared Lynn Randall
发明人： Paul B. Savage , Saurabh Shashikant Chitre , Kunal Arvind Varia , Hayley Ann Reece , Thomas E. Jacks , Ross A. Miller , Jared Lynn Randall
IPC分类号： C07J41/00 , C07C309/29 , C07C309/35
CPC分类号： C07J41/0088 , C07B2200/13 , C07C309/29 , C07C309/35 , C07J41/0061
摘要： Disclosed herein are acid addition salts of cationic steroidal antimicrobials (“CSAs” or “ceragenins”) and methods of making the same. Particularly advantageous salt forms are identified, such as 1,5-naphthalenedisulfonic acid addition salts and sulfate addition salts. The acid addition salts may be formulated for treating subjects with ailments responsive to CSAs, including but not limited to treating bacterial infections. Accordingly, some embodiments include formulations and methods of administering acid addition salts of CSAs.
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公开(公告)号：US20160311851A1
公开(公告)日：2016-10-27
申请号：US15135969
申请日：2016-04-22
IPC分类号： C07J41/00
CPC分类号： C07J41/0088 , C07J9/005 , C07J41/0055 , C07J41/0061
摘要： Disclosed herein are methods of making ceragnenin compounds for treating, preventing, or diagnosing diseases, disorders, or conditions associated with bacterial or viral infections, cancer, inflammation, and osteogenesis. Ceragenin compounds display broad-spectrum antibacterial activity utilizing a mode of action similar to antimicrobial peptides, but without the high synthesis costs and susceptibility to proteolytic degradation. Ceragenin compounds reproduce the amphiphilic morphology found in many antimicrobial peptides and display potent and diverse biological activities, including anti-bacterial, anti-cancer, anti-inflammatory, bone growth promotion, and wound healing promotion.
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公开(公告)号：US20100280244A1
公开(公告)日：2010-11-04
申请号：US12811254
申请日：2008-12-22
IPC分类号： C07D239/52 , C07D239/54
CPC分类号： C07D413/12 , C07D239/52 , Y02P20/55
摘要： Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
摘要翻译： 公开了制备某些N-芳基烷基-1-（烷基或芳烷基）-2-酰基氨基烷基-5-羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺的方法。 在一个实施方案中，该方法包括酰化相应的N-芳烷基-1-（烷基或芳烷基）-2-氨基烷基-5-酯保护的羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺中的游离胺和 然后通过碱水解脱保护5-羟基。 该方法的羟基嘧啶酮羧酰胺产物是HTV整合酶抑制剂，其可用于治疗HTV感染，治疗AIDS或延缓AIDS的发作或进展。 还公开了可用作过程中间体的某些酯化的N-芳基烷基羟基嘧啶酮甲酰胺。
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公开(公告)号：US5908936A
公开(公告)日：1999-06-01
申请号：US76949
申请日：1998-05-13
IPC分类号： C07D275/06
CPC分类号： C07D275/06 , Y02P20/55
摘要： A process for synthesizing a compound of formula I: is disclosed wherein R represents halo or C.sub.1-6 alkyl, unsubstituted or substituted with OP, wherein P represents a protecting group.
摘要翻译： 公开了合成式I化合物的方法：其中R表示未取代或被OP取代的卤素或C 1-6烷基，其中P表示保护基。
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公开(公告)号：US5470976A
公开(公告)日：1995-11-28
申请号：US301949
申请日：1994-09-07
申请人： Guy R. Humphrey , Ross A. Miller
发明人： Guy R. Humphrey , Ross A. Miller
IPC分类号： C07D221/18 , C07J9/00 , C07J73/00
CPC分类号： C07J73/005 , C07J9/00
摘要： The novel process of this invention involves the reduction of certain .DELTA.-5 steroidal alkenes to selectively produce either the 5.alpha. or 5.beta. reduction products. Particularly, this invention involves reduction of .DELTA.-5 steroidal alkenes using a rhodium based catalyst in the presence of hydrogen to selectively yield 5.alpha. steroids or alternatively reduction of .DELTA.-5 steroidal alkenes in an ionizing medium with a trialkylsilane to selectively yield 5.beta. steroids.
摘要翻译： 本发明的新方法涉及减少某些DELTA-5甾体烯烃以选择性地产生5α或5β还原产物。 特别地，本发明涉及在氢气存在下使用铑基催化剂还原DELTA-5甾体烯烃，以选择性地产生5个α类固醇，或者在具有三烷基硅烷的电离介质中选择性地还原DELTA-5甾体烯烃以选择性地产生5β类固醇 。
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公开(公告)号：US10370403B2
公开(公告)日：2019-08-06
申请号：US15135969
申请日：2016-04-22
摘要： Disclosed herein are methods of making ceragnenin compounds for treating, preventing, or diagnosing diseases, disorders, or conditions associated with bacterial or viral infections, cancer, inflammation, and osteogenesis. Ceragenin compounds display broad-spectrum antibacterial activity utilizing a mode of action similar to antimicrobial peptides, but without the high synthesis costs and susceptibility to proteolytic degradation. Ceragenin compounds reproduce the amphiphilic morphology found in many antimicrobial peptides and display potent and diverse biological activities, including anti-bacterial, anti-cancer, anti-inflammatory, bone growth promotion, and wound healing promotion.
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公开(公告)号：US08686141B2
公开(公告)日：2014-04-01
申请号：US12811254
申请日：2008-12-22
IPC分类号： C07D239/52 , C07D413/12
CPC分类号： C07D413/12 , C07D239/52 , Y02P20/55
摘要： Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)-2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrimidinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.
摘要翻译： 公开了制备某些N-芳基烷基-1-（烷基或芳烷基）-2-酰基氨基烷基-5-羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺的方法。 在一个实施方案中，该方法包括酰化相应的N-芳烷基-1-（烷基或芳烷基）-2-氨基烷基-5-酯保护的羟基-6-氧代-1,6-二氢嘧啶-4-甲酰胺中的游离胺和 然后通过碱水解脱保护5-羟基。 该方法的羟基嘧啶酮羧酰胺产物是HTV整合酶抑制剂，其可用于治疗HTV感染，治疗AIDS或延缓AIDS的发作或进展。 还公开了可用作过程中间体的某些酯化的N-芳基烷基羟基嘧啶酮甲酰胺。
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公开(公告)号：US5817802A
公开(公告)日：1998-10-06
申请号：US776735
申请日：1997-02-05
申请人： Guy R. Humphrey , Ross A. Miller
发明人： Guy R. Humphrey , Ross A. Miller
IPC分类号： C07D221/18 , C07J9/00 , C07J73/00
CPC分类号： C07J73/005 , C07J9/00
摘要： The novel process of this invention involves the reduction of certain .DELTA.-5 steroidal alkenes to selectively produce either the 5.alpha. or 5.beta. reduction products. Particularly, this invention involves reduction of .DELTA.-5 steroidal alkenes using a rhodium based catalyst in the presence of hydrogen to selectively yield 5.alpha. steroids or alternatively reduction of .DELTA.-5 steroidal alkenes in an ionizing medium with a trialkylsilane to selectively yield 5.beta. steroids.
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公开(公告)号：US5696266A
公开(公告)日：1997-12-09
申请号：US508804
申请日：1995-07-28
申请人： Guy R. Humphrey , Ross A. Miller
发明人： Guy R. Humphrey , Ross A. Miller
IPC分类号： C07D221/18 , C07J9/00 , C07J73/00
CPC分类号： C07J73/005 , C07J9/00
摘要： The novel process of this invention involves the reduction of certain .DELTA.-5 steroidal alkenes to selectively produce either the 5.alpha. or 5.beta. reduction products. Particularly, this invention involves reduction of .DELTA.-5 steroidal alkenes using a rhodium based catalyst in the presence of hydrogen to selectively yield 5.alpha. steroids or alternatively reduction of .DELTA.-5 steroidal alkenes in an ionizing medium with a trialkylsilane to selectively yield 5.beta. steroids.
摘要翻译： 本发明的新方法涉及减少某些DELTA-5甾体烯烃以选择性地产生5α或5β还原产物。 特别地，本发明涉及在氢气存在下使用铑基催化剂还原DELTA-5甾体烯烃，以选择性地产生5个α类固醇，或者在具有三烷基硅烷的电离介质中选择性地还原DELTA-5甾体烯烃以选择性地产生5β类固醇 。
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