公开(公告)号：US06759523B2

公开(公告)日：2004-07-06

申请号：US09727315

申请日：2000-11-30

申请人： Eric Swayze ,  Richard H. Griffey ,  Yili Ding ,  Venkatraman Mohan

发明人： Eric Swayze ,  Richard H. Griffey ,  Yili Ding ,  Venkatraman Mohan

IPC分类号： C07H1522

CPC分类号： C07H15/234

摘要： The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.

摘要翻译： 本发明涉及具有糖基化2-脱氧链霉胺（2-DOS）环类的氨基糖苷类化合物的类似物，以及它们作为抗微生物感染的预防或治疗剂的制备和用途。 本发明的化合物包含至少一个芳基，杂芳基，取代的芳基或取代的杂芳基，代替与2-脱氧链霉胺环连接的糖基。

公开(公告)号：US20080015162A1

公开(公告)日：2008-01-17

申请号：US11745429

申请日：2007-05-07

申请人： Sanjay Bhanot ,  Richard Geary ,  Robert McKay ,  Brett Monia ,  Punit Seth ,  Andrew Siwkowski ,  Eric Swayze ,  Edward Wancewicz

发明人： Sanjay Bhanot ,  Richard Geary ,  Robert McKay ,  Brett Monia ,  Punit Seth ,  Andrew Siwkowski ,  Eric Swayze ,  Edward Wancewicz

IPC分类号： A61K48/00 ,  A61P43/00 ,  C07H21/04 ,  C12N15/87

CPC分类号： C12N15/113 ,  C12N15/1137 ,  C12N2310/11 ,  C12N2310/31 ,  C12N2310/315 ,  C12N2310/321 ,  C12N2310/322 ,  C12N2310/3231 ,  C12N2310/341 ,  C12N2310/3515 ,  C12Y203/0102 ,  C12N2310/3521

摘要： The present disclosure describes short antisense compounds, including such compounds comprising chemically-modified high-affinity monomers 8-16 monomers in length. Certain such short antisense compound are useful for the reduction of target nucleic acids and/or proteins in cells, tissues, and animals with increased potency and improved therapeutic index. Thus, provided herein are short antisense compounds comprising high-affinity nucleotide modifications useful for reducing a target RNA in vivo. Such short antisense compounds are effective at lower doses than previously described antisense compounds, allowing for a reduction in toxicity and cost of treatment. In addition, the described short antisense compounds have greater potential for oral dosing.

摘要翻译： 本公开描述了短反义化合物，包括长度为化学修饰的高亲和力单体8-16单体的这类化合物。 某些这样的短反义化合物可用于在增加的效力和改善的治疗指数的细胞，组织和动物中还原靶核酸和/或蛋白质。 因此，本文提供了包含用于在体内降低靶RNA的高亲和力核苷酸修饰的短反义化合物。 这样的短反义化合物在比以前描述的反义化合物低的剂量下是有效的，允许降低毒性和治疗成本。 此外，所述短反义化合物具有更大的口服给药潜力。

公开(公告)号：US20070287831A1

公开(公告)日：2007-12-13

申请号：US11747057

申请日：2007-05-10

申请人： Punit Seth ,  Eric Swayze

发明人： Punit Seth ,  Eric Swayze

IPC分类号： C07H19/00

CPC分类号： C07H19/04 ,  C07H21/00

摘要： The present invention provides 5′-modified bicyclic nucleoside analogs and oligomeric compounds comprising at least one of these nucleoside analogs. In preferred embodiments the nucleoside analogs have either (R) or (S)-chirality at the 5′-carbon. These bicyclic nucleoside analogs are useful for enhancing properties of oligomeric compounds including for example enhanced nuclease resistance.

摘要翻译： 本发明提供了包含这些核苷类似物中的至少一种的5'-修饰的双环核苷类似物和寡聚化合物。 在优选的实施方案中，核苷类似物在5'-碳上具有（R）或（S） - 亲和性。 这些双环核苷类似物可用于增强低聚化合物的性质，包括例如增强的核酸酶抗性。

公开(公告)号：US20050032805A1

公开(公告)日：2005-02-10

申请号：US10914256

申请日：2004-08-09

申请人： Elizabeth Jefferson ,  Eric Swayze ,  Punit Seth ,  Dale Robinson

发明人： Elizabeth Jefferson ,  Eric Swayze ,  Punit Seth ,  Dale Robinson

IPC分类号： C07D233/50 ,  A61K31/341 ,  A61K31/40 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/455 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/513 ,  A61K31/52 ,  A61K31/522 ,  A61P31/04 ,  C07C237/42 ,  C07D213/82 ,  C07D239/47 ,  C07D239/54 ,  C07D241/44 ,  C07D307/68 ,  C07D333/38 ,  C07D333/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/18 ,  C07D473/34 ,  C07D417/14 ,  C07D43/14

CPC分类号： C07D213/82 ,  C07D241/44 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/18 ,  C07D473/34

摘要： Provided are antibacterial biaryl compounds having micromolar MIC activity against Gram-negative and Gram-positive pathogens, including a methicillin-resistant S. aureus strain.

摘要翻译： 提供对革兰氏阴性和革兰氏阳性病原体具有微摩尔MIC活性的抗菌联芳基化合物，包括耐甲氧西林金黄色葡萄球菌菌株。

公开(公告)号：US06849660B1

公开(公告)日：2005-02-01

申请号：US09630122

申请日：2000-08-01

申请人： Elizabeth Jefferson ,  Eric Swayze

发明人： Elizabeth Jefferson ,  Eric Swayze

IPC分类号： C07D233/50 ,  A61K31/341 ,  A61K31/40 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/455 ,  A61K31/496 ,  A61K31/497 ,  A61K31/498 ,  A61K31/513 ,  A61K31/52 ,  A61K31/522 ,  A61P31/04 ,  C07C237/42 ,  C07D213/82 ,  C07D239/47 ,  C07D239/54 ,  C07D241/44 ,  C07D307/68 ,  C07D333/38 ,  C07D333/40 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/06 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/18 ,  C07D473/34 ,  A61K31/445 ,  A61K31/34 ,  A61K31/44 ,  C07D307/02 ,  C07D315/00 ,  C07D333/32 ,  C07D333/36 ,  C07D335/00

CPC分类号： C07D213/82 ,  C07D241/44 ,  C07D307/68 ,  C07D333/38 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/18 ,  C07D473/34

摘要： Provided are antibacterial compounds having Formula I: In such compositions, X is O or S; Y is CH2; n is 0 or 1. One of R1 and R1′ is —C(O)NR5R5′, —C(O)—Q—NR5R5′, —CH2NR5R5′ or —S(O)2NR5R5′ and the other is H or R3. One of R2 and R2′ is —NHC(O)R6 or —NHS(O)2R6 and the other is H or R4. Q is an amino acid or peptide. R3 is H, halogen, —NR5R5′ or —NHC(O)R6; and R4 is selected from the group consisting of H, halogen, hydroxyl, amino, carboxyl, alkyl, alkenyl and alkynyl. R5 is selected from the group consisting of H, alkyl, alkenyl or alkynyl optionally substituted with halogen, OH, amino, amidinyl, guanidinyl, urea, alkyl, carboxyl, oxo, carboxamide; R5′ is H or R5 and R5′ together form a 5-16 member heterocycle optionally substituted with halogen, OH, amino, alkyl, carboxyl, carbonyl or carboxamide. R6 is selected from the group consisting of H; amino; alkyl, alkenyl or alkynyl, each optionally substituted with halogen, amino, amidinyl, guanidinyl, urea, carboxyl or carboxamide; a 5-16 member carbocycle or heterocycle; and a 5-16 member heterocycle-substituted alkyl or carbocycle-substituted alkyl, wherein said carbocycle and heterocycle are optionally substituted with halogen, OH, amino, alkyl, carboxyl, oxo or carboxamide.

摘要翻译： 提供具有式I的抗菌化合物：在这种组合物中，X是O或S; Y是CH2; n是0或1. R1和R1'之一是-C（O）NR5R5'，-C（O）-Q-NR5R5'，-CH2NR5R5'或-S（O）2NR5R5'，另一个是H或R3 。 R2和R2之一是-NHC（O）R6或-NHS（O）2R6，另一个是H或R4。 Q是氨基酸或肽。 R3是H，卤素，-NR5R5'或-NHC（O）R6; 并且R 4选自H，卤素，羟基，氨基，羧基，烷基，烯基和炔基。 OH选自H，烷基，烯基或炔基，任选被卤素，OH，氨基，脒基，胍基，脲，烷基，羧基，氧代，羧酰胺取代; R5'是H或R5，R5'一起形成任选被卤素，OH，氨基，烷基，羧基，羰基或羧酰胺取代的5-16元杂环。 R6选自H; 氨基; 烷基，烯基或炔基，各自任选被卤素，氨基，脒基，胍基，脲，羧基或羧酰胺取代; 5-16个碳环或杂环; 和5-16元杂环取代的烷基或碳环取代的烷基，其中所述碳环和杂环任选被卤素，OH，氨基，烷基，羧基，氧代或羧酰胺取代。

公开(公告)号：US06541456B1

公开(公告)日：2003-04-01

申请号：US09452606

申请日：1999-12-01

申请人： Eric Swayze ,  Richard H. Griffey ,  Yili Ding ,  Venkatraman Mohan

发明人： Eric Swayze ,  Richard H. Griffey ,  Yili Ding ,  Venkatraman Mohan

IPC分类号： A61K317036

CPC分类号： C07H15/234

摘要： The present invention is directed to analogs of aminoglycoside compounds of the class having a glycosylated 2-deoxystreptamine (2-DOS) ring as well as their preparation and use as prophylactic or therapeutics against microbial infection. Compounds of the invention comprises at least one aryl, heteroaryl, substituted aryl or substituted heteroaryl group in place of a glycosyl group attached to the 2-deoxystreptamine ring.