公开(公告)号：US5401863A

公开(公告)日：1995-03-28

申请号：US219568

申请日：1994-03-29

Applicant: Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee

Inventor： Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee

IPC: A61K31/165 ,  A61K31/47 ,  A61K31/65 ,  A61P31/04 ,  C07C231/12 ,  C07C237/26 ,  C07D213/74 ,  C07D215/38 ,  C07D307/66 ,  C07D333/36 ,  C07C221/00

CPC classification number: C07C237/26 ,  C07C2103/46

Abstract: Novel 9-amino-7-(substituted amino)-6-demethyl-6-deoxytetracyclines having activity against a wide spectrum of organisms including organisms which are resistant to tetracyclines are disclosed. Also disclosed are intermediates and methods for making the novel compounds of the present invention.

Abstract translation: 公开了具有抗四环素抗性的生物体的广谱生物体的新型9-氨基-7-（取代氨基）-6-脱甲基-6-脱氧四环素。 还公开了制备本发明新化合物的中间体和方法。

公开(公告)号：USRE40183E1

公开(公告)日：2008-03-25

申请号：US11145508

申请日：2005-06-03

Applicant: Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee ,  Adma A. Ross

Inventor： Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee ,  Adma A. Ross

IPC: A61K31/65 ,  C07C233/64

CPC classification number: C07D333/34 ,  C07C237/26 ,  C07C2603/46 ,  C07D205/04 ,  C07D277/46 ,  C07D307/68 ,  C07D333/24 ,  C07D333/38

Abstract: The invention is drawn to 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds of the formula wherein R, X, R5 and R6 are defined in the specification. The compounds of the invention are useful as broad spectrum antibiotics.

Abstract translation: 本发明涉及下式的7-取代-9-（取代氨基）-6-去甲基-6-脱氧四环素化合物其中R，X，R 5和R 6 >在规范中定义。 本发明的化合物可用作广谱抗生素。

公开(公告)号：US6110901A

公开(公告)日：2000-08-29

申请号：US839728

申请日：1992-02-19

Applicant: Yakov Gluzman ,  Michael Ostrander

Inventor： Yakov Gluzman ,  Michael Ostrander

IPC: A61K45/06 ,  A61K31/70

CPC classification number: A61K31/708 ,  A61K31/7068 ,  A61K31/7072 ,  A61K45/06

Abstract: The present invention relates to methods for controlling and/or treating RNA-replicating viral infections which afflict human beings, animals and/or plants. Specifically, the RNA chain terminating agents, 3'-deoxyribouracil, 3'-deoxyriboguanine and 3'-deoxyribocytosine are useful in treating RNA-replicating viral infections.

Abstract translation: 本发明涉及用于控制和/或治疗折磨人类，动物和/或植物的RNA复制性病毒感染的方法。 具体地，RNA链终止剂，3'-脱氧核糖尿嘧啶，3'-脱氧核糖鸟嘌呤和3'-脱氧胞嘧啶可用于治疗RNA复制型病毒感染。

公开(公告)号：US5571693A

公开(公告)日：1996-11-05

申请号：US433129

申请日：1995-05-03

Applicant: Beth A. Rasmussen ,  Francis P. Tally ,  Yakov Gluzman

Inventor： Beth A. Rasmussen ,  Francis P. Tally ,  Yakov Gluzman

IPC: C12N15/09 ,  C12N9/86 ,  C12N15/55 ,  C12Q1/18 ,  C12Q1/34 ,  C07H21/04 ,  C12N1/21 ,  C12N5/10 ,  C12P21/00

CPC classification number: C12N9/86 ,  C12Q1/18 ,  G01N2333/986

Abstract: This invention is directed to the elucidation of DNA sequences encoding Class B beta-lactamase enzymes from Bacteroides fragilis and the amino acid sequences of those enzymes. This invention is also directed to screening methods for identifying antibiotics which are resistant to such beta-lactamase enzymes or for identifying compounds which inactivate such beta-lactamase enzymes.

Abstract translation: 本发明涉及解释从脆弱拟杆菌编码B类β-内酰胺酶的DNA序列和这些酶的氨基酸序列。 本发明还涉及用于鉴定对这种β-内酰胺酶具有抗性或用于鉴定灭活此类β-内酰胺酶的化合物的抗生素的筛选方法。

公开(公告)号：US5530117A

公开(公告)日：1996-06-25

申请号：US455923

申请日：1995-05-31

Applicant: Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee ,  Adma A. Ross

Inventor： Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee ,  Adma A. Ross

IPC: C07C237/26 ,  C07D205/04 ,  C07D277/22 ,  C07D277/46 ,  C07D307/68 ,  C07D333/24 ,  C07D333/34 ,  C07D333/38 ,  C07D205/08 ,  C07D211/06 ,  C07D265/30 ,  C07D293/10

CPC classification number: C07D333/38 ,  C07C237/26 ,  C07D205/04 ,  C07D277/46 ,  C07D307/68 ,  C07D333/24 ,  C07D333/34 ,  C07C2103/46

Abstract: The disclosure is drawn to novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds. These compounds are useful to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.

Abstract translation: 本发明涉及新的7-取代-9-（取代氨基）-6-脱甲基-6-脱氧四环素化合物。 这些化合物可用于治疗由广谱细菌生物引起的感染，包括耐四环素的细菌生物。

公开(公告)号：USRE40086E1

公开(公告)日：2008-02-19

申请号：US11318390

申请日：2005-12-23

Applicant: Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee ,  Adma A. Ross

Inventor： Joseph J. Hlavka ,  Phaik-Eng Sum ,  Yakov Gluzman ,  Ving J. Lee ,  Adma A. Ross

IPC: A61K31/65

CPC classification number: C07D333/38 ,  C07C237/26 ,  C07C2603/46 ,  C07D205/04 ,  C07D277/46 ,  C07D307/68 ,  C07D333/24 ,  C07D333/34

Abstract: The disclosure is drawn to a method of using novel 7-substituted-9-(substituted amino)-6-demethyl-6-deoxytetracycline compounds to treat infections caused by a wide spectrum of bacterial organisms, including those which are resistant to tetracycline.

Abstract translation: 本公开内容涉及使用新型7-取代-9-（取代氨基）-6-去甲基-6-脱氧四环素化合物治疗由广谱细菌生物引起的感染的方法，包括耐四环素的细菌生物。

公开(公告)号：US5792642A

公开(公告)日：1998-08-11

申请号：US459263

申请日：1995-06-02

Applicant: Beth A. Rasmussen ,  Francis P. Tally ,  Yakov Gluzman

Inventor： Beth A. Rasmussen ,  Francis P. Tally ,  Yakov Gluzman

IPC: C12N15/09 ,  C12N9/86 ,  C12N15/55 ,  C12Q1/18 ,  C12Q1/34 ,  C12N1/20 ,  C12N15/00 ,  C12P21/06

CPC classification number: C12N9/86 ,  C12Q1/18 ,  G01N2333/986

Abstract: This invention is directed to the elucidation of DNA sequences encoding Class B beta-lactamase enzymes from Bacteroides fragilis and the amino acid sequences of those enzymes. This invention is also directed to screening methods for identifying antibiotics which are resistant to such beta-lactamase enzymes or for identifying compounds which inactivate such beta-lactamase enzymes.

Abstract translation: 本发明涉及解释从脆弱拟杆菌编码B类β-内酰胺酶的DNA序列和这些酶的氨基酸序列。 本发明还涉及用于鉴定对这种β-内酰胺酶具有抗性或用于鉴定灭活此类β-内酰胺酶的化合物的抗生素的筛选方法。

公开(公告)号：US5705340A

公开(公告)日：1998-01-06

申请号：US459264

申请日：1995-06-02

Applicant: Beth A. Rasmussen ,  Francis P. Tally ,  Yakov Gluzman

Inventor： Beth A. Rasmussen ,  Francis P. Tally ,  Yakov Gluzman

IPC: C12N15/09 ,  C12N9/86 ,  C12N15/55 ,  C12Q1/18 ,  C12Q1/34 ,  C12Q1/68 ,  C12P17/00

CPC classification number: C12N9/86 ,  C12Q1/18 ,  G01N2333/986

Abstract: This invention is directed to the elucidation of DNA sequences encoding Class B beta-lactamase enzymes from Bacteroides fragilis and the amino acid sequences of those enzymes. This invention is also directed to screening methods for identifying antibiotics which are resistant to such beta-lactamase enzymes or for identifying compounds which inactivate such beta-lactamase enzymes.

Abstract translation: 本发明涉及解释从脆弱拟杆菌编码B类β-内酰胺酶的DNA序列和这些酶的氨基酸序列。 本发明还涉及用于鉴定对这种β-内酰胺酶具有抗性或用于鉴定灭活此类β-内酰胺酶的化合物的抗生素的筛选方法。

公开(公告)号：US5371206A

公开(公告)日：1994-12-06

申请号：US177502

申请日：1994-01-05

Applicant: Andrew P. Seddon ,  Peter Bohlen ,  Yakov Gluzman

Inventor： Andrew P. Seddon ,  Peter Bohlen ,  Yakov Gluzman

IPC: A61K38/22 ,  A61P17/00 ,  C07K1/00 ,  C07K1/22 ,  C07K14/50 ,  C12N1/21 ,  C12N5/10 ,  C12N7/00 ,  C12N15/09 ,  C12N15/12 ,  C12P21/02 ,  C12R1/19 ,  C12R1/92 ,  C12V15/01 ,  C12V15/18

CPC classification number: C07K14/503

Abstract: The present invention relates to novel chimeric fibroblast growth factors (FGF) wherein the alanine at amino acid 3 and serine 5 of native human recombinant basic fibroblast growth factor are replaced with glutamic acid. The N-terminus sequence of the present chimeric FGFs identify homology with that of human acidic fibroblast growth factor. The mitogenic properties of the native human recombinant basic FGF are exhibited by the present chimeric FGFs, and they are efficiently expressed in E. coli at significantly greater yields that previously reported. Novel variants of this new glu.sup.3,5 basic fibroblast growth factor, such as those in which cysteine 78 and cysteine 96 are replaced, e.g., with serine or other amino acids, to produce stabilized versions of the glu.sup.3,5 basic FGF and eliminate disulfide scrambled forms, are also described.

Abstract translation: 本发明涉及新型嵌合成纤维细胞生长因子（FGF），其中天然人重组碱性成纤维细胞生长因子的氨基酸3和丝氨酸5的丙氨酸被谷氨酸替代。 本发明嵌合FGFs的N-末端序列与人酸性成纤维细胞生长因子的N末端序列具有同源性。 天然人重组碱性FGF的促有丝分裂特性由本发明的嵌合FGF表现出来，并且在大肠杆菌中以以前报道的显着更高的产量有效地表达。 这种新的glu3,5碱性成纤维细胞生长因子的新变体，例如用半胱氨酸78和半胱氨酸96被替换的那些，例如用丝氨酸或其他氨基酸，以产生glu3,5碱性FGF的稳定化形式并消除二硫键扰乱 形式也被描述。

公开(公告)号：US5877004A

公开(公告)日：1999-03-02

申请号：US462334

申请日：1995-06-05

Applicant: Thomas R. Jones ,  Viera P. Muzithras ,  Yakov Gluzman

Inventor： Thomas R. Jones ,  Viera P. Muzithras ,  Yakov Gluzman

IPC: C07K14/045 ,  C12N7/01 ,  C12N9/24 ,  C12Q1/34 ,  C12Q1/68 ,  C12N15/38

CPC classification number: C07K14/005 ,  C12N9/2402 ,  C12N9/2434 ,  C12Q1/34 ,  C12Q1/68 ,  C12Q1/6897 ,  C12Y302/01031 ,  C12N2710/16122 ,  G01N2333/045

Abstract: This invention relates to a method for identifying non-essential genes of the human cytomegalovirus (HCMV) genome through the insertion of a .beta.-glucuronidase marker gene into a specified HCMV gene, such that, if the product of the HCMV gene is not expressed, the gene is identified as non-essential for replication of HCMV. This invention also relates to a method of screening for compounds which inhibit HCMV by the insertion of the .beta.-glucuronidase marker gene into a HCMV gene, such that the enzyme marker is expressed and cleaves a conjugate chemical substrate in an assay system to yield a detectable fluorescing product or to result in a color change. This invention further provides the gene responsible in HCMV early cytopathic effect.

Abstract translation: 本发明涉及通过将β-葡糖醛酸糖苷酶标记基因插入特定HCMV基因中鉴定人巨细胞病毒（HCMV）基因组的非必需基因的方法，使得如果HCMV基因的产物未被表达， 该基因被鉴定为对于HCMV的复制非必需的。 本发明还涉及通过将β-葡糖醛酸糖苷酶标记基因插入到HCMV基因中筛选抑制HCMV的化合物的方法，使得酶标记物在测定系统中表达并切割缀合物化学底物以产生可检测的 荧光产品或导致颜色变化。 本发明还提供了负责HCMV早期致细胞病变作用的基因。