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公开(公告)号:US20050043298A1
公开(公告)日:2005-02-24
申请号:US10915919
申请日:2004-08-11
IPC分类号: C07D491/18 , C07D498/18 , C07D513/18 , C07D519/00 , A61K31/542 , A61K31/498 , A61K31/538 , C07D491/14 , C07D498/14
CPC分类号: C07D498/18 , C07D491/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′-and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮松霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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公开(公告)号:US20070155715A1
公开(公告)日:2007-07-05
申请号:US11638756
申请日:2006-12-14
申请人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Joseph Raker , Xiang Yu , James Siedlecki , Yingfei Yang
发明人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Joseph Raker , Xiang Yu , James Siedlecki , Yingfei Yang
IPC分类号: A61K31/5383 , C07D491/22
CPC分类号: C07D498/18 , C07D519/00
摘要: The present invention features rifamycin analogs and methods of using these compounds to treat a variety of microbial infections.
摘要翻译: 本发明特征为利福霉素类似物和使用这些化合物治疗各种微生物感染的方法。
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公开(公告)号:US20050197333A1
公开(公告)日:2005-09-08
申请号:US11020870
申请日:2004-12-22
申请人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Joseph Raker , Xiang Yu , James Siedlecki , Yingfei Yang
发明人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Joseph Raker , Xiang Yu , James Siedlecki , Yingfei Yang
IPC分类号: A61K31/498 , A61K31/5383 , A61K31/542 , A61P31/04 , A61P31/10 , C07D491/14 , C07D498/14 , C07D498/18 , C07D513/18 , C07D519/00
CPC分类号: C07D498/18 , C07D513/18 , C07D519/00
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, 4′- and/or 6′ halo and/or alkoxy analogs, and various 5′ substituents that incorporate a cyclic amine moiety.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其他形式中,苯并恶嗪利霉素,苯并噻嗪可的霉素和苯并二氮霉素霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物,4'-和/或6'卤素和/或烷氧基类似物,以及各种5'取代基 加入环胺部分。
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公开(公告)号:US20070238747A1
公开(公告)日:2007-10-11
申请号:US11804141
申请日:2007-05-17
申请人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Xiang Yu , James Siedlecki , Yingfei Yang
发明人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Xiang Yu , James Siedlecki , Yingfei Yang
IPC分类号: A61K31/4355 , C07D498/14 , C07D498/16
CPC分类号: C07D498/16 , C07D498/22 , C07D513/22
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其它形式中,苯并恶嗪利霉素,苯并噻嗪可霉素和苯并二氮霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物和/或各种稠合环体系,其中苯环为4',5'或5' ,6'位。
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公开(公告)号:US20050137189A1
公开(公告)日:2005-06-23
申请号:US11008597
申请日:2004-12-09
申请人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Xiang Yu , James Siedlecki , Yingfei Yang
发明人: John van Duzer , Arthur Michaelis , William Geiss , Douglas Stafford , Xiang Yu , James Siedlecki , Yingfei Yang
IPC分类号: A61K20060101 , A61K31/395 , A61K31/498 , A61K31/4985 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K31/542 , A61P9/10 , A61P31/00 , A61P31/04 , A61P31/10 , C07D491/14 , C07D498/12 , C07D498/14 , C07D498/22 , C07D513/22 , C07D515/12 , C07D519/00
CPC分类号: C07D498/16 , C07D498/22 , C07D513/22
摘要: The present invention features rifamycin analogs that can be used as therapeutics for treating or preventing a variety of microbial infections. In one form, the analogs are acetylated at the 25-position, as is rifamycin. In another form, the analogs are deacetylated at the 25-position. In yet other forms, benzoxazinorifamycin, benzthiazinorifamycin, and benzdiazinorifamycin analogs are derivatized at various positions of the benzene ring, including 3′-hydroxy analogs, and/or various fused ring systems with the benzene ring at the 4′,5′ or 5′,6′ positions.
摘要翻译: 本发明的特征是利福霉素类似物可用作治疗或预防各种微生物感染的治疗剂。 在一种形式中,类似物在25位被乙酰化,就像利福霉素一样。 在另一种形式中,类似物在25位脱乙酰化。 在其它形式中,苯并恶嗪利霉素,苯并噻嗪可霉素和苯并二氮霉素类似物在苯环的不同位置衍生化,包括3'-羟基类似物和/或各种稠合环体系,其中苯环为4',5'或5' ,6'位。
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公开(公告)号:US20080027060A1
公开(公告)日:2008-01-31
申请号:US11835134
申请日:2007-08-07
申请人: Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Cowen , Paul Greenspan , Leslie McQuire , Ruben Tommasi , John van Duzer
发明人: Eva Altmann , Claudia Betschart , Keigo Gohda , Miyuki Horiuchi , Rene Lattmann , Martin Missbach , Junichi Sakaki , Michihiro Takai , Naoki Teno , Scott Cowen , Paul Greenspan , Leslie McQuire , Ruben Tommasi , John van Duzer
IPC分类号: A61K31/404 , A61K31/166 , A61K31/341 , A61K31/415 , A61K31/495 , A61P19/02 , A61P29/00 , C07D207/09 , C07D209/08 , C07D333/24 , C07D307/54 , C07D295/14 , C07D295/04 , C07D231/12 , C07D213/56 , C07D207/33 , C07C233/64 , A61P19/10 , A61K31/5375 , A61K31/44 , A61K31/381 , A61K31/40
CPC分类号: C07C255/29 , C07C255/44 , C07C271/22 , C07C317/44 , C07C323/52 , C07C323/62 , C07C2601/02 , C07C2601/14 , C07D207/327 , C07D209/18 , C07D209/42 , C07D211/06 , C07D213/64 , C07D213/81 , C07D213/82 , C07D215/48 , C07D231/14 , C07D233/54 , C07D233/64 , C07D241/44 , C07D249/06 , C07D261/18 , C07D275/02 , C07D295/088 , C07D295/15 , C07D295/155 , C07D307/24 , C07D307/54 , C07D307/68 , C07D307/85 , C07D317/68 , C07D333/24 , C07D333/38 , C07D333/40 , C07D333/70 , C07D405/12 , C07D409/12 , C07D417/12 , C07K5/06043 , C07K5/06078
摘要: N-terminal substituted dipeptide nitriles as defined are useful as inhibitors of cysteine cathepsins, e.g. cathepsins B, K, L and S, and can be used for the treatment of cysteine cathepsin dependent diseases and conditions, including inflammation, rheumatoid arthritis, osteoarthritis, osteoporosis, tumors (especially tumor invasion and tumor metastasis), coronary disease, atherosclerosis (including atherosclerotic plaque rupture and destabilization). Particular dipeptide nitriles are compounds of formula I, or physiologically-acceptable and -cleavable esters or a salts thereof wherein: the symbols are as defined. In particular it has been found that by appropriate choice of groups R, R2, R3, R4, R5, X1, Y and L, the relative selectivity of the compounds as inhibitors of the various cysteine cathepsin types, e.g. cathepsins B, K, L and S may be altered, e.g. to obtain inhibitors which selectively inhibit a particular cathepsin type or combination of cathepsin types.
摘要翻译: 定义的N-末端取代的二肽腈可用作半胱氨酸组织蛋白酶的抑制剂,例如, 组织蛋白酶B,K,L和S,可用于治疗半胱氨酸组织蛋白酶依赖性疾病和病症,包括炎症,类风湿性关节炎,骨关节炎,骨质疏松症,肿瘤(特别是肿瘤侵袭和肿瘤转移),冠状动脉疾病,动脉粥样硬化(包括 动脉粥样硬化斑块破裂和不稳定)。 特别的二肽腈是式I化合物或生理上可接受的和可切割的酯或其盐,其中符号如上所定义。 特别地,已经发现通过适当选择基团R 1,R 2,R 3,R 4,R 5, / SUB>,X 1,Y和L,化合物作为各种半胱氨酸组织蛋白酶类型的抑制剂的相对选择性,例如 组织蛋白酶B,K,L和S可以被改变,例如, 以获得选择性抑制特定组织蛋白酶类型或组织蛋白酶类型组合的抑制剂。
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公开(公告)号:US20050049270A1
公开(公告)日:2005-03-03
申请号:US10963293
申请日:2004-10-12
申请人: Prakash Jagtap , Erkan Baloglu , John van Duzer , Csaba Szabo , Andrew Salzman , Aloka Roy , William Williams , Alexander Nivoroshkin
发明人: Prakash Jagtap , Erkan Baloglu , John van Duzer , Csaba Szabo , Andrew Salzman , Aloka Roy , William Williams , Alexander Nivoroshkin
IPC分类号: C07D221/18 , C07D471/04 , C07D491/04 , C07D495/04 , C07D221/22 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号: C07D221/18 , C07D471/04 , C07D491/04 , C07D495/04
摘要: The invention provides novel classes of Isoquinoline Derivatives. Pharmaceutical compositions and methods of making and using the compounds, are also described.
摘要翻译: 本发明提供了新类别的异喹啉衍生物。 还描述了制备和使用化合物的药物组合物和方法。
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