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1. 发明授权

US07385086B2 Antimicrobial compounds 失效
标题翻译：抗菌化合物
公开(公告)号：US07385086B2
公开(公告)日：2008-06-10
申请号：US10764451
申请日：2004-01-27
申请人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
发明人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
IPC分类号： C07C317/00 , C07C317/02 , C07C317/04 , C07C317/06 , C07C317/08
CPC分类号： C40B40/04 , C07C311/06 , C07C317/44
摘要： This invention provides compounds and methods for treating, with said compound, a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn-Z-CO—Y, where R is an alkyl groups having 6-20 carbon atoms, unsaturated hydrocarbon groups having 6-20 carbon atoms, or alkyl groups having 6-20 carbon atoms interrupted by at least one aromatic ring; Z is —CH2—, —CH2CH2—, —NH—NH—, —O—, ——NH—, —O—NH—, —CH2—NH—, —CH2—O—, —NH—O—, —NH—CH2—, —O—CH2—, and —CH═CH—; Y is —NH2, —O—CH2—C6H5, —CO—CO—O—CH3, and —O—CH3; and n is 1 or 2. It has been discovered that these compounds treat microbially-based infections caused by corynebacteria, nocardiae, rhodococcus, and mycobacteria. These compounds may be used to treat mycobacterial cells, such as Mycobacteria tuberculosis, drug resistant M. tuberculosis, M. avium intracellulare, M. leprae, M. paratuberculosis, and pathogenic Mycobacteria sp.
摘要翻译：本发明提供了通过向动物施用含有具有式R-SO n -Z-CO-Y的化合物的药物组合物，通过向所述化合物处理分枝杆菌感染的化合物和方法，其中R 是具有6-20个碳原子的烷基，具有6-20个碳原子的不饱和烃基或具有6-20个碳原子的烷基被至少一个芳环中断; Z是-CH 2 - ， - CH 2 CH 2 - ， - NH-NH-， - O - ， - NH-， -O-NH-，-CH 2 -NH-，-CH 2 -O-，-NH-O-，-NH-CH 2， -O - CH 2 - 和-CH-CH-; Y是-NH 2，-O-CH 2 -C 6 H 5，-CO-CO- O-CH 3，和-O-CH 3; 已发现这些化合物治疗由棒状杆菌，诺卡氏菌，罗红球菌和分枝杆菌引起的基于微生物的感染。这些化合物可用于治疗分枝杆菌细胞，例如结核分枝杆菌，耐药性结核分枝杆菌，胞内分枝杆菌，麻疯病，副结核分枝杆菌和致病性分枝杆菌属。

2. 发明授权

US5614551A Inhibitors of fatty acid synthesis as antimicrobial agents 失效
标题翻译：脂肪酸合成抑制剂作为抗菌剂
公开(公告)号：US5614551A
公开(公告)日：1997-03-25
申请号：US188421
申请日：1994-01-24
申请人： James D. Dick , Francis P. Kuhajda
发明人： James D. Dick , Francis P. Kuhajda
IPC分类号： A61K45/00 , A61K31/20 , A61K31/335 , A61K31/34 , A61K31/455 , A61P3/06 , A61P31/00 , A61P31/04 , A61P31/06 , A61P33/00 , A61P43/00 , A01N43/20 , A01N25/26 , A61K9/127
CPC分类号： A61K31/34 , A61K31/335
摘要： Fatty acid synthase (FAS) is overexpressed by certain infectious organisms that are resistant to most currently available antibiotics. Contrarywise, little FAS expression is identified in patient tissues. Inhibition of fatty acid synthesis is thus selectively toxic to invasive cells, while patient cells with low FAS activity are resistant. This invention provides a method of treating septic patients where fatty acid synthesis by invading cells is inhibited with resultant interruption of the disease process.
摘要翻译：脂肪酸合成酶（FAS）被某些对大多数现有抗生素具有抗性的感染性生物体过度表达。相反，在患者组织中鉴定出少量FAS表达。脂肪酸合成的抑制因此对侵入性细胞有选择性毒性，而具有低FAS活性的患者细胞具有抗性。本发明提供一种治疗败血症患者的方法，其中通过侵入细胞的脂肪酸合成被抑制并导致疾病过程的中断。

3. 发明授权

US06713654B1 Antimicrobial compounds 失效
标题翻译：抗菌化合物
公开(公告)号：US06713654B1
公开(公告)日：2004-03-30
申请号：US09486550
申请日：2000-08-28
申请人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
发明人： Craig A. Townsend , James D. Dick , Gary R. Pasternack , Francis P. Kuhajda , Nicole M. Parrish
IPC分类号： C07C31500
CPC分类号： C40B40/04 , C07C311/06 , C07C317/44
摘要： This invention provides methods for treating a mycobacterial infection by administering to an animal a pharmaceutical composition containing a compound having the formula R—SOn—Z—CO—Y, where R is an alkyl group having 6-20 carbons; Z is a radical selected from —CH2—, —O—, and —NH—, two of these radicals coupled together, or —CH2═CH2—; Y is —NH2, O—CH2—C6H5, —CO—CO—O—CH3, or O—CH3; and n is 1 or 2. It has been discovered that these compounds inhibit growth of microbial cells which synthesize &agr;-substitued, &bgr;-hydroxy fatty acids, particularly corynemycolic acid, nocardic acid, and mycolic acid. These compounds may be used to inhibit growth of mycobacterial cells, such as Mycobacterium tuberculosis, drug-resistant M. tuberculosis, M. avium intracellulare, and M. leprae.
摘要翻译：本发明提供了通过向动物施用含有具有式R-SOn-Z-CO-Y的化合物的药物组合物来治疗分枝杆菌感染的方法，其中R是具有6-20个碳原子的烷基; Z是选自-CH 2 - ， - O-和-NH-的基团，这些基团中的两个连接在一起，或-CH 2 = CH 2 - ; Y是-NH 2，O-CH 2 -C 6 H 5，-CO-CO-O-CH 3或O-CH 3; 已经发现，这些化合物抑制合成α-取代的β-羟基脂肪酸，特别是氯霉素酸，诺卡酸和霉菌酸的微生物细胞的生长。这些化合物可用于抑制分枝杆菌细胞的生长，例如结核分枝杆菌，耐药性结核分枝杆菌，胞内分枝杆菌和麻疯病。

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