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序号	专利名	申请号	申请日	公开（公告）号	公开（公告）日	发明人
1	与嘌呤核苷磷酸化酶或核苷水解酶的前体药物的改进的治疗用途相关的应用	CN201710819433.3	2012-02-20	CN107496910A	2017-12-22	威廉·B·帕克; 埃里克·J·索尔舍尔
本申请详述了，一种嘌呤核苷磷酸化酶或核苷水解酶或编码任意一个这些酶的表达的载体，连同被嘌呤核苷磷酸化酶或核苷水解酶裂解的前药，在用于产生复制型或非复制型靶细胞的直接注射抑制方面的用途。靶细胞通常不表达引入的嘌呤核苷磷酸化酶或核苷水解酶。酶和前药适合于混合，并且以单次量或以分次注射的方式注射或给药到靶细胞。通过将靶细胞暴露于X射线辐射来提高药物及前药的效力。不管针对靶细胞的给药途径如何，前药的给药与X射线放射疗法组合来杀死或是抑制靶细胞的功能是有效的。
2	嘌呤核苷磷酸化酶作为核苷前体药物的酶激活剂	CN200980140441.9	2009-08-17	CN102186497A	2011-09-14	威廉·B·帕克; 埃里克·J·索尔舍尔
一种用于抑制哺乳动物癌细胞或病毒感染细胞的方法，包括提供阴道毛滴虫嘌呤核苷磷酸化酶或尾部突变的嘌呤核苷磷酸化酶临近哺乳动物癌细胞或病毒感染细胞和将酶接触嘌呤核苷磷酸化酶可裂解底物以产生细胞毒性嘌呤类似物。该方法包括将含有磷酸化酶或编码相同的磷酸化酶的DNA序列的载体导入细胞中和输送有效量的底物例如9-(β-D-阿拉伯呋喃糖基)-2-氟腺嘌呤(F-araA)至所述细胞。
3	嘌呤核苷磷酸化酶作为核苷前体药物的酶激活剂	CN200980140441.9	2009-08-17	CN102186497B	2015-02-25	威廉·B·帕克; 埃里克·J·索尔舍尔
一种用于抑制哺乳动物癌细胞或病毒感染细胞的方法，包括提供阴道毛滴虫嘌呤核苷磷酸化酶或尾部突变的嘌呤核苷磷酸化酶临近哺乳动物癌细胞或病毒感染细胞和将酶接触嘌呤核苷磷酸化酶可裂解底物以产生细胞毒性嘌呤类似物。该方法包括将含有磷酸化酶或编码相同的磷酸化酶的DNA序列的载体导入细胞中和输送有效量的底物例如9-(β-D-阿拉伯呋喃糖基)-2-氟腺嘌呤(F-araA)至所述细胞。
4	クロファラビンの合成方法	JP2016564008	2015-04-22	JP6263645B2	2018-01-17	ザブドキンアレキサンドル; マトヴィエンコヴィクトル; マトヴィイエンコイアロスラヴ; シプチェンコヴォロディームィル

5	クロファラビンの合成方法	JP2016564008	2015-04-22	JP2017513884A	2017-06-01	アレキサンドルザブドキン; ヴィクトルマトヴィエンコ; イアロスラヴマトヴィイエンコ; ヴォロディームィルシプチェンコ
抗癌ヌクレオシドであるクロファラビンを高収率で生成するための方法を開示する。本方法は、2-クロロアデニンとヌクレオシドとの間の酵素的グリコシル基転移による2-クロロアデノシンの調製、ベンゾイル化、異性化、スルホン酸エステル形成、フッ素化、および脱保護を含む。
6	ＰＮＰａｓｅの製造法	JP2004562927	2003-12-25	JPWO2004058959A1	2006-04-27	正俊村井
高効率で簡便にPNPaseを製造することができ、また医薬品原料としての核酸重合体の合成において問題となるエンドトキシンの混入を低減できる、PNPaseの製造法を提供することである。PNPase遺伝子とT7プロモーターとを連結する発現ベクターにより、T7 RNAポリメラーゼ遺伝子を有する大腸菌等を形質転換したものを用いることなどにより、PNPaseを製造する。また、PNPaseの精製工程をより簡便にするために、タグ遺伝子を有する発現ベクターを利用したり、培養時間を長くする。
7	Purine nucleoside phosphorylase as an enzyme activator of nuclease prodrug	JP2011523217	2009-08-17	JP5567016B2	2014-08-06	ウィリアム・ビー・パーカー; エリック・ジェイ・ソーシャー
A process for inhibiting a mammalian cancerous cell or virally infected cell includes providing a Trichomonas vaginalis purine nucleoside phosphorylase enzyme or a tail mutant purine nucleoside phosphorylase enzyme in proximity to the mammalian cancerous cell or the virally infected cell and exposing the enzyme to a purine nucleoside phosphorylase enzyme cleavable substrate to yield a cytotoxic purine analog. The process includes introducing to the cell a vector containing the phosphorylase enzyme, or a DNA sequence coding for the same and delivering to the cell an effective amount of the substrate such as 9-(²-D-arabinofuranosyl)-2-fluoroadenine (F-araA).
8	Purine nucleoside phosphorylase as an enzyme activator of nuclease prodrug	JP2011523217	2009-08-17	JP2012500224A	2012-01-05	ウィリアム・ビー・パーカー; エリック・ジェイ・ソーシャー
A process for inhibiting a mammalian cancerous cell or virally infected cell includes providing a Trichomonas vaginalis purine nucleoside phosphorylase enzyme or a tail mutant purine nucleoside phosphorylase enzyme in proximity to the mammalian cancerous cell or the virally infected cell and exposing the enzyme to a purine nucleoside phosphorylase enzyme cleavable substrate to yield a cytotoxic purine analog. The process includes introducing to the cell a vector containing the phosphorylase enzyme, or a DNA sequence coding for the same and delivering to the cell an effective amount of the substrate such as 9-(beta-D-arabinofuranosyl)-2-fluoroadenine (F-araA).
9	Enzymatic nucleic acid treatment of a disease or condition related to the expression level of C-raf	JP54844898	1998-05-05	JP2001525667A	2001-12-11	カーペイスキー，アレグザンダー; キシチ，ケヴィン; ジャーヴィス，テイル; スウィードラー，デーヴィッド; トンプソン，ジェームズ; バーギン，アレックス; パリー，トム; ビュードリー，アンバー; ベイジェルマン，レオニド; ベロン，ローレント; マクスウィゲン，ジェームズ・エイ; マチュリック−アダミック，ジェイセンカ; レイノルズ，マーク; ワークマン，クリストファー・ティー
(57)【要約】Ｒａｆ遺伝子の発現を調節する核酸触媒、核酸触媒の輸送、スクリーニング、同定、合成、脱保護、精製の方法、および核酸分子を同定する方法が記載される。
10	Bacteria-Mediated Therapy for Cancer	US14276274	2014-05-13	US20140341853A1	2014-11-20	Vanna Hovanky
Methods for treating tumors and malignant tumors in regions that are adjacent to the gastrointestinal tract are provided. Therapeutically effective amounts of transformed bacteria are administered to subjects in need of treatment. Bacteria are transformed to produce proteins exhibiting therapeutic effects. These therapeutic effects can be the production of an enzyme that catalyzes the conversion of a prodrug into a drug and/or a protein that has therapeutic activity on its own. Bacteria may be provided to the gastrointestinal tract of the subject in need of treatment or preventative measures. In some cases, a prodrug is additionally administered.
11	Purine nucleoside phosphorylase as enzymatic activator of nucleoside prodrugs	US13059178	2009-08-17	US08628767B2	2014-01-14	William B. Parker; Eric J. Sorscher
A process for inhibiting a mammalian cancerous cell or virally infected cell includes providing a Trichomonas vaginalis purine nucleoside phosphorylase enzyme or a tail mutant purine nucleoside phosphorylase enzyme in proximity to the mammalian cancerous cell or the virally infected cell and exposing the enzyme to a purine nucleoside phosphorylase enzyme cleavable substrate to yield a cytotoxic purine analog. The process includes introducing to the cell a vector containing the phosphorylase enzyme, or a DNA sequence coding for the same and delivering to the cell an effective amount of the substrate such as 9-(β-D-arabinofuranosyl)-2-fluoroadenine (F-araA).
12	Novel immobilized biocatalysts usable for the production of natural nucleosides and modified analogues by enzymatic transglycosylation reactions	US10752166	2004-01-05	US20040142438A1	2004-07-22	Giancarlo Tonon; Emanuele Capra; Gaetano Orsini; Gabriele Zuffi
The preparation of novel biocatalysts is described; the biocatalysts are produced by the co-immobilization of the recombinant enzymes uridine phosphorylase and purine nucleoside phosphorylase by means of covalent bonds on solid substrates functionalized with epoxy groups. The novel biocatalysts are usable for successive reaction cycles, are resistant to heat and to the presence of solvents, and can advantageously be used in the industrial production of natural nucleosides and of modified analogues of pharmaceutical interest.
13	Deprotection of RNA	US09957841	2001-09-21	US06673918B2	2004-01-06	Laurent Bellon; Christopher T. Workman
Method for one-pot deprotection of RNA molecules.
14	Nucleoside triphosphates and their incorporation into oligonucleotides	US09918728	2001-07-31	US20030105308A1	2003-06-05	Leonid Beigelman; Shawn Zinnen
The present invention relates to novel nucleotide triphosphates, methods of synthesis and process of incorporating these nucleotide triphosphates into oligonucleotides, and isolation of novel nucleic acid catalysts (e.g., ribozymes or DNAzymes). Also, provided are the use of novel enzymatic nucleic acid molecules to inhibit gene expression and their applications in human therapy.
15	Method for screening nucleic acid catalysts	US09216584	1998-12-18	US06548657B1	2003-04-15	Alex Burgin; Leonid Beigelman; Laurent Bellon
Nucleic acid catalysts, method of screening for variants of nucleic acid catalysts, synthesis of ribozyme libraries and discovery of gene sequences are described.
16	Method for target site selection and discovery	US10103480	2002-03-21	US20020192685A1	2002-12-19	James D. Thompson
Nucleic acid catalysts, method of screening/selection for nucleic acid catalysts, synthesis of ribozyme libraries and discovery of gene sequences involved in a biological process are described.
17	Deprotection of RNA	US09957841	2001-09-21	US20020103366A1	2002-08-01	Laurent Bellon; Christopher T. Workman
Method for one-pot deprotection of RNA molecules.
18	Method for screening nucleic acid catalysts	US09094381	1998-06-09	US06280936B1	2001-08-28	Alex Burgin; Leonid Beigelman; Laurent Bellon
Nucleic acid catalysts, method of screening for variants of nucleic acid catalysts, synthesis of ribozyme libraries and discovery of gene sequences are described.
19	METHOD FOR THE SYNTHESIS OF CLOFARABINE	US15306265	2015-04-22	US20170044204A1	2017-02-16	Alexander ZABUDKIN; Victor MATVIENKO; Iaroslav MATVIIENKO; Volodymyr SYPCHENKO
The present invention relates to a method for the high yield production of the anticancer nucleoside clofarabine, the method comprising the preparation of 2-chloroadenosine by enzymatic transglycosylation between 2-chloroadenine and nucleosides, benzoylation, isomerization, sulfonate ester formation, fluorination, and deprotection.
20	PURINE NUCLEOSIDE PHOSPHORYLASE AS ENZYMATIC ACTIVATOR OF NUCLEOSIDE PRODRUGS	US14800864	2015-07-16	US20160022784A1	2016-01-28	Steven E. EALICK; William B. PARKER; Eric J. SORSCHER
A process for inhibiting a mammalian cancerous cell or virally infected cell includes providing a Trichomonas vaginalis purine nucleoside phosphorylase enzyme or a tail mutant purine nucleoside phosphorylase enzyme in proximity to the mammalian cancerous cell or the virally infected cell and exposing the enzyme to a purine nucleoside phosphorylase enzyme cleavable substrate to yield a cytotoxic purine analog. The process includes introducing to the cell a vector containing the phosphorylase enzyme, or a DNA sequence coding for the same and delivering to the cell an effective amount of the substrate such as 9-(β-D-arabinofuranosyl)-2-fluoroadenine (F-araA).

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