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1. 发明申请

US20100279861A1 Antifungal Agents 审中-公开
标题翻译：抗真菌剂
公开(公告)号：US20100279861A1
公开(公告)日：2010-11-04
申请号：US12680835
申请日：2008-08-12
申请人： Gerald F Bills , Javier Collado , Craig A. Parish , Fernando Pelaez , Gonzalo Platas , Terry Roemer
发明人： Gerald F Bills , Javier Collado , Craig A. Parish , Fernando Pelaez , Gonzalo Platas , Terry Roemer
IPC分类号： A01N43/40 , C12P17/18 , C12N1/14 , A61K38/02 , A61K38/12 , A61K31/7048 , A61K31/513 , A61K31/4745 , C07D498/16 , A01N43/80 , A61P31/04 , A01P3/00 , A01P5/00 , A01P7/04 , A01P13/00 , A01P15/00
CPC分类号： A01N65/04 , A01N43/90 , A01N65/00 , A61K31/42 , C07D498/16
摘要： Novel isoxazolidinone compounds useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops are described. Two novel strains of fungi, ATCC No. PAT-7894 and ATCC No. PAT-7895, are disclosed for the preparation of the described isoxazolidinone compounds.
摘要翻译：描述了可用于治疗和/或预防人和动物真菌感染以及作物中植物病原真菌控制的新型异恶唑烷酮化合物。公开了两种真菌菌株，ATCC No.PAT-7894和ATCC No.PAT-7895，用于制备所述的异恶唑烷酮化合物。

2. 发明申请

US20050019931A1 Nucleic acids encoding antifungal drug targets and methods of use 审中-公开
标题翻译：编码抗真菌药物靶标的核酸和使用方法
公开(公告)号：US20050019931A1
公开(公告)日：2005-01-27
申请号：US10741849
申请日：2003-12-19
申请人： Terry Roemer , Bo Jiang , Charles Boone , Howard Bussey
发明人： Terry Roemer , Bo Jiang , Charles Boone , Howard Bussey
IPC分类号： A61K38/00 , C07K14/40 , C12N1/18 , C12N15/74 , C12N15/81
CPC分类号： C12N15/81 , A61K38/00 , C07K14/40 , C12N15/815
摘要： The present invention provides Candida albicans genes that are demonstrated to be essential and are potential targets for drug screening. The nucleotide sequence of the target genes can be used for various drug discovery purposes, such as expression of the recombinant protein, hybridization assay and construction of nucleic acid arrays. The uses of proteins encoded by the essential genes, and genetically engineered cells comprising modified alleles of essential genes in various screening methods are also encompassed by the invention.
摘要翻译：本发明提供了证明是必需的白色念珠菌基因，并且是药物筛选的潜在靶标。靶基因的核苷酸序列可以用于各种药物发现目的，例如重组蛋白的表达，杂交测定和核酸阵列的构建。在各种筛选方法中，由必需基因编码的蛋白质的使用以及包含必需基因的修饰的等位基因的遗传工程改造的细胞也包括在本发明中。

3. 发明授权

US11141403B2 Benzimidazoles and indoles as taro inhibitors 有权
公开(公告)号：US11141403B2
公开(公告)日：2021-10-12
申请号：US16061481
申请日：2016-12-13
申请人： MERCK SHARP & DOHME CORP. , John P. Caldwell , Ginny Dai Ho , Sookhee N. Ha , Sandra J. Koseoglu , Marc A. Labroli , Sang Ho Lee , Christina Madsen-Duggan , Mihir Mandal , Jianping Pan , Weidong Pan , Terry Roemer , Jing Su , Christopher Michael Tan , Zheng Tan , Hao Wang , Christine Yang , Shu-Wei Yang
发明人： John P. Caldwell , Ginny Dai Ho , Sookhee N. Ha , Sandra J. Koseoglu , Marc A. Labroli , Sang Ho Lee , Christina Madsen-Duggan , Mihir Mandal , Jianping Pan , Weidong Pan , Terry Roemer , Jing Su , Christopher Michael Tan , Zheng Tan , Hao Wang , Christine Yang , Shu-Wei Yang
IPC分类号： A61K31/397 , A61P31/04 , A61K31/407 , C07D235/08 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D471/04
摘要： Novel compounds of the structural formula I, and the pharmaceutically acceptable salts thereof, are inhibitors of TarO and may be useful in the prevention, treatment and suppression of diseases mediated by TarO, such as bacterial infections, including gram negative bacterial infections and gram positive bacterial infections such as MRSA and MRSE, alone or in combination with a β-lactam antibiotic.

4. 发明申请

US20130203726A1 FtsZ INHIBITORS AS POTENTIATORS OF BETA-LACTAM ANTIBIOTICS AGAINST METHICILLIN-RESISTANT STAPHYLOCOCCUS 审中-公开
标题翻译： FtsZ抑制剂作为抗甲氧西林硫杆菌抗菌素抗肿瘤药物的潜力
公开(公告)号：US20130203726A1
公开(公告)日：2013-08-08
申请号：US13583480
申请日：2011-03-04
申请人： Terry Roemer , Sang Ho Lee , Lisa Wang Jarantow
发明人： Terry Roemer , Sang Ho Lee , Lisa Wang Jarantow
IPC分类号： A61K31/545 , A61K31/397 , A61K31/4025 , A61K31/437
CPC分类号： A61K31/545 , A61K31/198 , A61K31/397 , A61K31/4025 , A61K31/407 , A61K31/43 , A61K31/437 , A61K45/06 , A61K2300/00
摘要： The present invention relates to the use of inhibitors of FtsZ, an ancestral tubulin of prokaryotes, to restore susceptibility to β-lactam antibiotics, including carbapenems and cephalosporins, particularly in methicillin-resistant Staphylococcus aureus (MRSA), methicillin-resistant Staphyloccus epidermis (MRSE), and other coagulase negative staphylococci (MRCNS).
摘要翻译：本发明涉及使用原核生物的祖先微管蛋白FtsZ的抑制剂来恢复对β-内酰胺类抗生素（包括碳青霉烯类和头孢菌素）的敏感性，特别是耐甲氧西林金黄色葡萄球菌（MRSA），甲氧西林耐药性葡萄球菌表皮（MRSE））和其他凝固酶阴性葡萄球菌（MRCNS）。

5. 发明授权

US06783985B1 Gene disruption methodologies for drug target discovery 失效
标题翻译：药物靶点发现的基因破坏方法
公开(公告)号：US06783985B1
公开(公告)日：2004-08-31
申请号：US09792024
申请日：2001-02-20
申请人： Terry Roemer , Bo Jiang , Charles Boone , Howard Bussey
发明人： Terry Roemer , Bo Jiang , Charles Boone , Howard Bussey
IPC分类号： C12N1501
CPC分类号： C12R1/645 , A61K39/00 , C07K14/37 , C07K14/40 , C07K2319/00 , C12N15/1034 , C12N15/65 , C12N15/80 , C12N15/90 , C12R1/725
摘要： The present invention provides methods and compositions that enable the experimental determination as to whether any gene in the genome of a diploid pathogenic organism is essential, and whether it is required for virulence or pathogenicity. The methods involve the construction of genetic mutants in which one allele of a specific gene is inactivated while the other allele of the gene is placed under conditional expression. The identification of essential genes and those genes critical to the development of virulent infections, provides a basis for the development of screens for new drugs against such pathogenic organisms. The present invention further provides Candida albicans genes that are demonstrated to be essential and are potential targets for drug screening. The nucleotide sequence of the target genes can be used for various drug discovery purposes, such as expression of the recombinant protein, hybridization assay and construction of nucleic acid arrays. The uses of proteins encoded by the essential genes, and genetically engineered cells comprising modified alleles of essential genes in various screening methods are also encompassed by the invention.
摘要翻译：本发明提供了能够对二倍体致病生物体的基因组中的任何基因是否必需的实验测定以及是否需要毒力或致病性的方法和组合物。该方法包括构建遗传突变体，其中特定基因的一个等位基因被灭活而基因的其他等位基因置于条件表达下。识别必需基因和对致病性感染发展至关重要的那些基因，为开发针对这种致病生物的新药筛选提供了基础。本发明进一步提供了被证实是必需的白念珠菌基因，并且是药物筛选的潜在靶标。靶基因的核苷酸序列可以用于各种药物发现目的，例如重组蛋白的表达，杂交测定和核酸阵列的构建。在各种筛选方法中，由必需基因编码的蛋白质的使用以及包含必需基因的修饰的等位基因的遗传工程改造的细胞也包括在本发明中。

6. 发明授权

US06562595B2 Dominant selectable marker for gene transformation and disruption in yeasts 有权
标题翻译：用于酵母基因转化和破坏的主导选择标记
公开(公告)号：US06562595B2
公开(公告)日：2003-05-13
申请号：US09785669
申请日：2001-02-16
申请人： Terry Roemer , Howard Bussey , John Davison
发明人： Terry Roemer , Howard Bussey , John Davison
IPC分类号： C12N1500
CPC分类号： C12N15/81 , A61K38/00 , C07K14/40 , C12N9/1029
摘要： The present invention provides a novel dominant selectable marker system in yeast that is based on an aminoglycoside, nourseothricin (NST). This compound possesses a powerful antifungal activity against Candida albicans and S. cerevisiae. The invention provides a cognate drug resistance marker for use in gene transformation and disruption experimentation in Candida albicans and Saccharomyces cerevisiae. In particular, the invention presents: 1) direct utility for gene manipulations in both clinically and experimentally relevant strains regardless of genotype and without affecting growth rate, or hyphal formation; and 2) applicability to antifungal drug discovery, including target validation and various forms of drug screening assays.
摘要翻译：本发明提供了一种基于氨基糖苷类（NST）的酵母中的新型显性选择标记系统。该化合物对白色念珠菌和酿酒酵母具有强大的抗真菌活性。本发明提供了用于白色念珠菌和酿酒酵母的基因转化和破坏实验的同源药物抗性标记。特别地，本发明提出：1）直接用于临床和实验相关菌株中的基因操作，而不管基因型如何，而不影响生长速率或菌丝形成; 和2）适用于抗真菌药物发现，包括目标验证和各种形式的药物筛选测定。

7. 发明授权

US07129341B1 Identification of Candida albicans essential fungal specific genes and use thereof in antifungal drug discovery 失效
标题翻译：鉴定白色念珠菌必需真菌特异性基因及其在抗真菌药物发现中的应用
公开(公告)号：US07129341B1
公开(公告)日：2006-10-31
申请号：US10018105
申请日：2000-05-05
申请人： Terry Roemer , Howard Bussey , John Davison
发明人： Terry Roemer , Howard Bussey , John Davison
IPC分类号： C07H21/00 , C07H21/04
CPC分类号： C07K14/40 , C12Q1/6895
摘要： The invention relates to the identification and disruption of essential fungal specific genes isolated in the yeast pathogen Candida albicans namely CaKRE5, CaALR1, and CaCDC24 and to the use thereof in antifungal diagnosis and as essential antifungal targets in a fungal species for antifungal drug discovery. More specifically, the invention relates to the CaKRE5, CaALR1, and CaCDC24 genes, to their use to screen for antifungal compounds and to the drugs identified by such.
摘要翻译：本发明涉及在酵母病原体白色念珠菌即CaKRE5，CaALR1和CaCDC24中分离的必需真菌特异性基因的鉴定和破坏以及其在抗真菌诊断中的用途以及作为真菌药物发现的真菌物种中的必需抗真菌靶标。更具体地，本发明涉及CaKRE5，CaALR1和CaCDC24基因，用于筛选抗真菌化合物和由其鉴定的药物。

8. 发明申请

US20050079619A1 Gene disruption methodologies for drug target discovery 审中-公开
标题翻译：药物靶点发现的基因破坏方法
公开(公告)号：US20050079619A1
公开(公告)日：2005-04-14
申请号：US10882104
申请日：2004-06-29
申请人： Terry Roemer , Bo Jiang , Charles Boone , Howard Bussey
发明人： Terry Roemer , Bo Jiang , Charles Boone , Howard Bussey
IPC分类号： A61K39/00 , C07K14/37 , C07K14/40 , C12N15/10 , C12N15/65 , C12N15/80 , C12N15/90 , C12N1/18 , C12N15/74
CPC分类号： C12R1/645 , A61K39/00 , C07K14/37 , C07K14/40 , C07K2319/00 , C12N15/1034 , C12N15/65 , C12N15/80 , C12N15/90 , C12R1/725
摘要： The present invention provides methods and compositions that enable the experimental determination as to whether any gene in the genome of a diploid pathogenic organism is essential, and whether it is required for virulence or pathogenicity. The methods involve the construction of genetic mutants in which one allele of a specific gene is inactivated while the other allele of the gene is placed under conditional expression. The identification of essential genes and those genes critical to the development of virulent infections, provides a basis for the development of screens for new drugs against such pathogenic organisms. The present invention further provides Candida albicans genes that are demonstrated to be essential and are potential targets for drug screening. The nucleotide sequence of the target genes can be used for various drug discovery purposes, such as expression of the recombinant protein, hybridization assay and construction of nucleic acid arrays. The uses of proteins encoded by the essential genes, and genetically engineered cells comprising modified alleles of essential genes in various screening methods are also encompassed by the invention.
摘要翻译：本发明提供了能够对二倍体致病生物体的基因组中的任何基因是否必需的实验测定以及是否需要毒力或致病性的方法和组合物。该方法包括构建遗传突变体，其中特定基因的一个等位基因被灭活而基因的其他等位基因置于条件表达下。识别必需基因和对致病性感染发展至关重要的那些基因，为开发针对这种致病生物的新药筛选提供了基础。本发明进一步提供了被证实是必需的白念珠菌基因，并且是药物筛选的潜在靶标。靶基因的核苷酸序列可以用于各种药物发现目的，例如重组蛋白的表达，杂交测定和核酸阵列的构建。在各种筛选方法中，由必需基因编码的蛋白质的使用以及包含必需基因的修饰的等位基因的遗传工程改造的细胞也包括在本发明中。

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