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1. 发明申请

US20050208620A1 Compositions and methods for hydroxylating epothilones 有权
公开(公告)号：US20050208620A1
公开(公告)日：2005-09-22
申请号：US10915172
申请日：2004-08-09
申请人： Jonathan Basch , Shu-Jen Chiang , Suo-Win Liu , Akbar Nayeem , Yuhua Sun , Li You
发明人： Jonathan Basch , Shu-Jen Chiang , Suo-Win Liu , Akbar Nayeem , Yuhua Sun , Li You
IPC分类号： C07K14/79 , C12N9/02 , C12P17/18 , C07H21/04 , C12N1/21 , C12N9/06 , C12N15/74
CPC分类号： C12N9/0077 , C07K14/79 , C07K2299/00 , C12P17/181
摘要： Isolated nucleic acid sequences and polypeptides encoded thereby for epothilone B hydroxylase and mutants and variants thereof and a ferredoxin located downstream from the epothilone B hydroxylase gene are provided. Also provided are vectors and cells containing these vectors. In addition, methods for producing recombinant microorganisms, methods for using these recombinant microorganism to produce hydroxyalkyl-bearing epothilones and an epothilone analog produced by a mutant of epothilone B hydroxylase are provided.

2. 发明授权

US06884608B2 Compositions and methods for hydroxylating epothilones 失效
标题翻译：用于羟化埃坡霉素的组合物和方法
公开(公告)号：US06884608B2
公开(公告)日：2005-04-26
申请号：US10321188
申请日：2002-12-17
申请人： Jonathan David Basch , Shu-Jen David Chiang , Suo-Win Liu , Akbar Nayeem , Yuhua Sun , Li You
发明人： Jonathan David Basch , Shu-Jen David Chiang , Suo-Win Liu , Akbar Nayeem , Yuhua Sun , Li You
IPC分类号： C07K14/79 , C12N9/02 , C12P17/18
CPC分类号： C12N9/0077 , C07K14/79 , C07K2299/00 , C12P17/181
摘要： Isolated nucleic acid sequences and polypeptides encoded thereby for epothilone B hydroxylase and mutants and variants thereof and a ferredoxin located downstream from the epothilone B hydroxylase gene are provided. Also provided are vectors and cells containing these vectors. In addition, methods for producing recombinant microorganisms, methods for using these recombinant microorganism to produce hydroxyalkyl-bearing epothilones and an epothilone analog produced by a mutant of epothilone B hydroxylase are provided.
摘要翻译：提供了分离的核酸序列和由此编码的用于埃坡霉素B羟化酶及其突变体和变体以及位于埃坡霉素B羟化酶基因下游的铁氧还蛋白的多肽。还提供了含有这些载体的载体和细胞。此外，提供了用于制备重组微生物的方法，使用这些重组微生物制备含有羟烷基的埃坡霉素的方法和由埃坡霉素B羟化酶的突变体产生的埃坡霉素类似物。

3. 发明授权

US07214527B2 Compositions and methods for hydroxylating epothilones 有权
标题翻译：用于羟化埃坡霉素的组合物和方法
公开(公告)号：US07214527B2
公开(公告)日：2007-05-08
申请号：US10915172
申请日：2004-08-09
申请人： Jonathan David Basch , Shu-Jen David Chiang , Suo-Win Liu , Akbar Nayeem , Yuhua Sun , Li You
发明人： Jonathan David Basch , Shu-Jen David Chiang , Suo-Win Liu , Akbar Nayeem , Yuhua Sun , Li You
IPC分类号： C12N1/20 , C12N15/74 , C07H21/04
CPC分类号： C12N9/0077 , C07K14/79 , C07K2299/00 , C12P17/181
摘要： Isolated nucleic acid sequences and polypeptides encoded thereby for epothilone B hydroxylase and mutants and variants thereof and a ferredoxin located downstream from the epothilone B hydroxylase gene are provided. Also provided are vectors and cells containing these vectors. In addition, methods for producing recombinant microorganisms, methods for using these recombinant microorganism to produce hydroxyalkyl-bearing epothilones and an epothilone analog produced by a mutant of epothilone B hydroxylase are provided.
摘要翻译：提供了分离的核酸序列和由此编码的用于埃坡霉素B羟化酶及其突变体和变体以及位于埃坡霉素B羟化酶基因下游的铁氧还蛋白的多肽。还提供了含有这些载体的载体和细胞。此外，提供了用于制备重组微生物的方法，使用这些重组微生物制备含有羟烷基的埃坡霉素的方法和由埃坡霉素B羟化酶的突变体产生的埃坡霉素类似物。

4. 发明申请

US20110077395A1 INHIBITORS OF 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I 审中-公开
标题翻译： 11-羟基脱氢酶脱氢酶I型抑制剂
公开(公告)号：US20110077395A1
公开(公告)日：2011-03-31
申请号：US12958706
申请日：2010-12-02
申请人： James J. Li , Lawrence G. Hamann , Zheming Ruan , Christopher B. Cooper , Shung C. Wu , Ligaya M. Simpkins , Haixia Wang , Akbar Nayeem , Stanley R. Krystek
发明人： James J. Li , Lawrence G. Hamann , Zheming Ruan , Christopher B. Cooper , Shung C. Wu , Ligaya M. Simpkins , Haixia Wang , Akbar Nayeem , Stanley R. Krystek
IPC分类号： C07D401/06 , C07D401/12 , C07D213/82 , C07D413/06 , C07D401/14 , C07D487/04
CPC分类号： C07D213/70 , A61K31/421 , A61K31/426 , A61K31/4439 , A61K31/4965 , A61K31/497 , A61K31/506 , C07D213/71 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/14 , C07D487/04 , C07D487/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：其立体异构体或前药或其药学上可接受的盐，其中G，L，Q，Z，R 6，R 7和R 8在本文中定义。

5. 发明授权

US07091331B2 Nucleic acid molecules and polypeptides encoding baboon TAFI 有权
标题翻译：编码狒狒TAFI的核酸分子和多肽
公开(公告)号：US07091331B2
公开(公告)日：2006-08-15
申请号：US10379836
申请日：2003-03-04
申请人： James K. Tamura , Gary R. Matsueda , Mei-Yin Hsu , Akbar Nayeem
发明人： James K. Tamura , Gary R. Matsueda , Mei-Yin Hsu , Akbar Nayeem
IPC分类号： C07H21/01 , C07H21/04 , C07K1/14
CPC分类号： C12N9/48 , A61K38/00
摘要： The present invention relates to the isolation and identification of novel baboon nucleic acid molecules and proteins and polypeptides encoded by such nucleic acid molecules, or degenerate variants thereof, which proteins and polypeptides comprise novel baboon thrombin-activatable fibrinolysis inhibitors or “TAFI” enzyme molecules. Because the novel baboon TAFI proteins and polypeptides of the invention inhibit the breakdown of blood clots, they may be therapeutically useful for the treatment of blood disorders wherein clotting needs to be regulated or promoted, such as hemophilia or von Willebrand's disease or in other situations, such as trauma, wherein blood clotting or coagulation needs to be regulated or promoted. The sequences of the invention are also useful in screening methods for the identification of compounds that modulate the expression of the baboon TAFI nucleic acids and/or the activity of the baboon TAFI proteins and polypeptides of the invention. Such agonist or antagonist compounds may be useful in the treatment of various blood clotting disorders and conditions requiring hemostatic control such as hemophilia or various thrombotic diseases such as deep venous thrombosis, coronary artery disease, stroke associated with atrial fibrillation and recurrent thrombosis following stroke or myocardial infarction.
摘要翻译：本发明涉及分离和鉴定由这种核酸分子或其简并变体编码的新型狒狒核酸分子和蛋白质和多肽，其蛋白质和多肽包含新型狒狒凝血酶可激活的纤维蛋白溶解抑制剂或“TAFI”酶分子。因为本发明的新型狒狒TAFI蛋白质和多肽抑制血凝块的分解，所以它们可用于治疗需要调节或促进凝血的血液病症，例如血友病或血管性血友病或其他情况，例如创伤，其中需要调节或促进凝血或凝血。本发明的序列也可用于鉴定调节狒狒TAFI核酸表达的化合物和/或本发明的狒狒TAFI蛋白和多肽的活性的筛选方法。这样的激动剂或拮抗剂化合物可用于治疗各种血液凝固病症和需要止血控制的病症，例如血友病或各种血栓形成疾病如深静脉血栓形成，冠状动脉疾病，与心房颤动相关的中风和中风或心肌复发性血栓形成梗死。

6. 发明申请

US20060235028A1 Inhibitors of 11-beta hydroxysteroid dehydrogenase type I 审中-公开
标题翻译： 11-β型羟基类固醇脱氢酶Ⅰ型抑制剂
公开(公告)号：US20060235028A1
公开(公告)日：2006-10-19
申请号：US11403092
申请日：2006-04-12
申请人： James Li , Lawrence Hamann , Zheming Ruan , Christopher Cooper , Shung Wu , Ligaya Simpkins , Haixia Wang , Akbar Nayeem , Stanley Krystek
发明人： James Li , Lawrence Hamann , Zheming Ruan , Christopher Cooper , Shung Wu , Ligaya Simpkins , Haixia Wang , Akbar Nayeem , Stanley Krystek
IPC分类号： A61K31/4965 , A61K31/506 , A61K31/497 , A61K31/4439 , A61K31/426 , A61K31/421
CPC分类号： C07D213/70 , A61K31/421 , A61K31/426 , A61K31/4439 , A61K31/4965 , A61K31/497 , A61K31/506 , C07D213/71 , C07D213/81 , C07D213/82 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/14 , C07D409/04 , C07D413/14 , C07D487/04 , C07D487/08
摘要： Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds have the structure: or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein G, L, Q, Z, R6, R7, and R8 are defined herein.
摘要翻译：提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。这些新化合物具有以下结构：其立体异构体或前药或其药学上可接受的盐，其中G，L，Q，Z，R 6，R 7和R > 8 在本文中定义。

7. 发明申请

US20060183686A1 NOVEL NUCLEIC ACID MOLECULES AND POLYPEPTIDES ENCODING BABOON TAFI 有权
标题翻译：新型核酸分子和多核苷酸编码BABOON TAFI
公开(公告)号：US20060183686A1
公开(公告)日：2006-08-17
申请号：US11405095
申请日：2006-04-17
申请人： James Tamura , Gary Matsueda , Mei-Yin Hsu , Akbar Nayeem
发明人： James Tamura , Gary Matsueda , Mei-Yin Hsu , Akbar Nayeem
IPC分类号： A61K38/54 , C12Q1/68 , C07H21/04 , C12P21/06 , C12N9/99
CPC分类号： C12N9/48 , A61K38/00
摘要： The present invention relates to the isolation and identification of novel baboon nucleic acid molecules and proteins and polypeptides encoded by such nucleic acid molecules, or degenerate variants thereof, which proteins and polypeptides comprise novel baboon thrombin-activatable fibrinolysis inhibitors or “TAFI” enzyme molecules. Because the novel baboon TAFI proteins and polypeptides of the invention inhibit the breakdown of blood clots, they may be therapeutically useful for the treatment of blood disorders wherein clotting needs to be regulated or promoted, such as hemophilia or von Willebrand's disease or in other situations, such as trauma, wherein blood clotting or coagulation needs to be regulated or promoted. The sequences of the invention are also useful in screening methods for the identification of compounds that modulate the expression of the baboon TAFI nucleic acids and/or the activity of the baboon TAFI proteins and polypeptides of the invention. Such agonist or antagonist compounds may be useful in the treatment of various blood clotting disorders and conditions requiring hemostatic control such as hemophilia or various thrombotic diseases such as deep venous thrombosis, coronary artery disease, stroke associated with atrial fibrillation and recurrent thrombosis following stroke or myocardial infarction.
摘要翻译：本发明涉及分离和鉴定由这种核酸分子或其简并变体编码的新型狒狒核酸分子和蛋白质和多肽，其蛋白质和多肽包含新型狒狒凝血酶可激活的纤维蛋白溶解抑制剂或“TAFI”酶分子。因为本发明的新型狒狒TAFI蛋白质和多肽抑制血凝块的分解，所以它们可用于治疗需要调节或促进凝血的血液病症，例如血友病或血管性血友病或其他情况，例如创伤，其中需要调节或促进凝血或凝血。本发明的序列也可用于鉴定调节狒狒TAFI核酸表达的化合物和/或本发明的狒狒TAFI蛋白和多肽的活性的筛选方法。这样的激动剂或拮抗剂化合物可用于治疗各种血液凝固病症和需要止血控制的病症，例如血友病或各种血栓形成疾病如深静脉血栓形成，冠状动脉疾病，与心房颤动相关的中风和中风或心肌复发性血栓形成梗死。

8. 发明授权

US08420365B2 11βhydroxysteroid dehydrogenase type 1 有权
标题翻译： 11＆amp;羟基类固醇脱氢酶1型
公开(公告)号：US08420365B2
公开(公告)日：2013-04-16
申请号：US12681916
申请日：2008-10-08
申请人： David Gordon , Yuval Blat , Akbar Nayeem , Mark S. Kirby , Bin He
发明人： David Gordon , Yuval Blat , Akbar Nayeem , Mark S. Kirby , Bin He
IPC分类号： C12N9/02
CPC分类号： C12Y101/01146 , C12N9/0006
摘要： The invention provides gene-targeted non-human animals comprising a genetically modified 11βHSD1 gene encodes a mutant 11βHSD1 polypeptide which is modulated by human 11βHSD1 modulating compounds. The invention further provides cells expressing mutant 11βHSD1 and cells isolated from gene-targeted animals, which cells produce a mutant 11βHSD1. The invention further provides methods of identifying agents that modulate 11βHSD1 activity, and are useful to treat 11βHSD1-related metabolic disorders.
摘要翻译：本发明提供了基因靶向的非人动物，其包含基因修饰的11和bgr HSD1基因，其编码由人11和HSD1调节化合物调节的突变体11和bgr; HSD1多肽。本发明还提供表达突变体11和bgr; HSD1的细胞和从基因靶向动物分离的细胞，所述细胞产生突变体11和bgr; HSD1。本发明还提供了鉴定调节11和HSD1活性的试剂的方法，并且可用于治疗与HSD1相关的代谢紊乱。

9. 发明申请

US20100209990A1 11 BETA HYDROXYSTEROID DEHYDROGENASE TYPE 1 有权
标题翻译： 11氢氧化钠脱氢酶1型
公开(公告)号：US20100209990A1
公开(公告)日：2010-08-19
申请号：US12681916
申请日：2008-10-08
申请人： David Gordon , Yuval Blat , Akbar Nayeem , Mark S. Kirby , Bin He
发明人： David Gordon , Yuval Blat , Akbar Nayeem , Mark S. Kirby , Bin He
IPC分类号： C12N9/00 , C12N15/52 , C12N5/02
CPC分类号： C12Y101/01146 , C12N9/0006
摘要： The invention provides gene-targeted non-human animals comprising a genetically modified 11βHSD1 gene encodes a mutant 11βHSD1 polypeptide which is modulated by human 11βHSD1 modulating compounds. The invention further provides cells expressing mutant 11βHSD1 and cells isolated from gene-targeted animals, which cells produce a mutant 11βHSD1. The invention further provides methods of identifying agents that modulate 11βHSD1 activity, and are useful to treat 11βHSD1-related metabolic disorders.
摘要翻译：本发明提供了基因靶向的非人动物，其包含基因修饰的11和bgr HSD1基因，其编码由人11和HSD1调节化合物调节的突变体11和bgr; HSD1多肽。本发明还提供表达突变体11和bgr; HSD1的细胞和从基因靶向动物分离的细胞，所述细胞产生突变体11和bgr; HSD1。本发明还提供了鉴定调节11和HSD1活性的试剂的方法，并且可用于治疗与HSD1相关的代谢紊乱。

10. 发明申请

US20060257921A1 Novel nucleic acid molecules and polypeptides encoding baboon TAFI 审中-公开
公开(公告)号：US20060257921A1
公开(公告)日：2006-11-16
申请号：US11490419
申请日：2006-07-20
申请人： James Tamura , Gary Matsueda , Mei-Yin Hsu , Akbar Nayeem
发明人： James Tamura , Gary Matsueda , Mei-Yin Hsu , Akbar Nayeem
IPC分类号： C12Q1/68 , C07H21/04 , C12P21/04 , C07K14/745
CPC分类号： C12N9/48 , A61K38/00
摘要： The present invention relates to the isolation and identification of novel baboon nucleic acid molecules and proteins and polypeptides encoded by such nucleic acid molecules, or degenerate variants thereof, which proteins and polypeptides comprise novel baboon thrombin-activatable fibrinolysis inhibitors or “TAFI” enzyme molecules. Because the novel baboon TAFI proteins and polypeptides of the invention inhibit the breakdown of blood clots, they may be therapeutically useful for the treatment of blood disorders wherein clotting needs to be regulated or promoted, such as hemophilia or von Willebrand's disease or in other situations, such as trauma, wherein blood clotting or coagulation needs to be regulated or promoted. The sequences of the invention are also useful in screening methods for the identification of compounds that modulate the expression of the baboon TAFI nucleic acids and/or the activity of the baboon TAFI proteins and polypeptides of the invention. Such agonist or antagonist compounds may be useful in the treatment of various blood clotting disorders and conditions requiring hemostatic control such as hemophilia or various thrombotic diseases such as deep venous thrombosis, coronary artery disease, stroke associated with atrial fibrillation and recurrent thrombosis following stroke or myocardial infarction.

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