公开(公告)号：US06429223B1

公开(公告)日：2002-08-06

申请号：US09715767

申请日：2000-11-17

申请人： Ching-San Lai ,  Tingmin Wang

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： A61K3148

CPC分类号： A61K47/555 ,  A61K47/54 ,  A61K47/545

摘要： In accordance with the present invention, there are provided modified forms of nonsteroidal anti-inflammatory drugs (NSAIDs). Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

摘要翻译： 根据本发明，提供非甾体抗炎药（NSAID）的修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂，其提供NSAIDs的治疗益处，同时引起副作用的发生率低得多，然后通常用这些药剂观察到。

公开(公告)号：US06407135B1

公开(公告)日：2002-06-18

申请号：US09453608

申请日：1999-12-03

申请人： Ching-San Lai ,  Tingmin Wang

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： C07D20704

CPC分类号： C07C333/16

摘要： In accordance with the present invention, there are provided conjugates of nitric oxide scavengers (e.g., dithiocarbamates, or “DC”) and pharmacologically active agents (e.g., NSAIDs). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which cause a much lower incidence of side-effects due to the protective effects imparted by modifying the pharmacologically active agents as described herein. In addition, invention conjugates are more effective than unmodified pharmacologically active agents because cells and tissues contacted by the pharmacologically active agent(s) are protected from the potentially damaging effects of nitric oxide overproduction induced thereby as a result of the co-production of nitric oxide scavenger (e.g., dithiocarbamate), in addition to free pharmacologically active agent, when invention conjugate is cleaved.

摘要翻译： 根据本发明，提供了一氧化氮清除剂（例如二硫代氨基甲酸盐或“DC”）和药理活性剂（例如NSAID）的缀合物。 本发明共轭物提供了一类新的药理活性剂（例如抗炎剂），其由于通过改变如本文所述的药理学活性剂而赋予的保护作用，导致副作用的低得多的发生率。 此外，发明共轭物比未改性的药理活性剂更有效，因为与药理活性剂接触的细胞和组织被保护免受由于一氧化氮的共同产生而导致的一氧化氮过量产生的潜在的破坏性作用 除了游离的药理学活性剂之外，当发明结合物被切割时，清除剂（例如，二硫代氨基甲酸盐）。

公开(公告)号：US20110040105A1

公开(公告)日：2011-02-17

申请号：US12988109

申请日：2009-04-15

申请人： Christian H. Huber ,  Young Mi Khulman ,  Sagun K. Tandel ,  Stephen R. Johannsen ,  Tingmin Wang ,  Paul Angell

发明人： Christian H. Huber ,  Young Mi Khulman ,  Sagun K. Tandel ,  Stephen R. Johannsen ,  Tingmin Wang ,  Paul Angell

IPC分类号： C07D295/023 ,  C07C315/04

CPC分类号： C07D207/06 ,  C07C309/89 ,  C07C313/04 ,  C07C317/18 ,  C07C317/22 ,  C07C317/44

摘要： Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.

摘要翻译： 描述了可用于制备根据式（I）的药用有用化合物，这种化合物的形式和用于此类方法的中间体的方法。

公开(公告)号：US06191273B1

公开(公告)日：2001-02-20

申请号：US09148762

申请日：1998-09-04

申请人： Phillip Dan Cook ,  Haoyun An ,  Becky Haly ,  Tingmin Wang

发明人： Phillip Dan Cook ,  Haoyun An ,  Becky Haly ,  Tingmin Wang

IPC分类号： C07D48702

CPC分类号： C40B40/04 ,  C07D471/08 ,  C40B50/08

摘要： Novel chemical compounds and mixtures of same are provided having antibacterial and other utilities. The mixtures preferably are formed by reacting a cyclic scaffold moiety with a set of chemical substituients. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.

摘要翻译： 提供新的化合物及其混合物具有抗菌和其他效用。 混合物优选通过使环状支架部分与一组化学取代基反应而形成。 根据本发明形成的图书馆本身具有效用，并且是商品。 它们可用于筛选农药，药物和其他生物活性化合物。

公开(公告)号：US20110218156A1

公开(公告)日：2011-09-08

申请号：US13016720

申请日：2011-01-28

申请人： Alexander Chucholowski ,  Alisher Khasanov ,  Tingmin Wang ,  Tong Zhu

发明人： Alexander Chucholowski ,  Alisher Khasanov ,  Tingmin Wang ,  Tong Zhu

IPC分类号： A61K38/14 ,  C08B37/16 ,  C12N5/07 ,  C07K9/00 ,  A61K31/7088 ,  A61K31/713

CPC分类号： A61K47/61 ,  A61K47/60 ,  Y10T428/2982

摘要： In accordance with the present invention, it has been discovered that the uptake of negatively charged entities into cells can be enhanced by noncovalently associating such charged entities with molecular entities comprising an amphiphilic core with positively charged arms, wherein a plurality of lipophilic (e.g., bile acid) moieties are covalently attached to the positively charged arms. The molecular entities form well defined stoichiometric complexes with negatively charged entities. Various compositions and methods for stabilizing anionic charged entities and for enhancing the cellular uptake of any anionic charged entities, e.g. double-stranded or hairpin nucleic acid, are provided.

摘要翻译： 根据本发明，已经发现，通过将这样的带电物质与包含具有带正电荷的臂的两亲核心的分子实体非共价结合，可以增强对带负电的实体进入细胞的吸收，其中多个亲脂性（例如，胆汁 酸）部分共价连接到带正电臂。 分子实体与带负电荷的实体形成明确的化学计量络合物。 用于稳定阴离子带电实体和用于增强任何阴离子带电实体的细胞摄取的各种组合物和方法，例如， 双链或发夹核酸。

公开(公告)号：US06306842B1

公开(公告)日：2001-10-23

申请号：US09586344

申请日：2000-06-02

申请人： Ching-San Lai ,  Tingmin Wang

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： A01N3736

CPC分类号： C07D261/08 ,  A61K47/55

摘要： In accordance with the present invention, there are provided conjugates of a combination of pharmacologically active agents (e.g., NSAIDs and selective COX-2 inhibitors). Invention conjugates provide a new class of pharmacologically active agents (e.g., anti-inflammatory agents) which provide the therapeutic benefits of both NSAIDs and selective COX-2 inhibitors, while causing a much lower incidence of side-effects then are typically observed with such agents due to the protective effects imparted by modifying the pharmacologically active agents as described herein.

摘要翻译： 根据本发明，提供了药理活性剂（例如NSAID和选择性COX-2抑制剂）的组合的缀合物。 本发明共轭物提供了一类新的药理学活性剂（例如抗炎剂），其提供了NSAID和选择性COX-2抑制剂的治疗益处，同时引起副作用的发生率低得多，然后通常用这些药剂观察到 由于通过改变本文所述的药理活性剂而赋予的保护作用。

公开(公告)号：US20110172447A1

公开(公告)日：2011-07-14

申请号：US13069426

申请日：2011-03-23

申请人： David Kucera ,  Gregory J. Haley ,  Erik J. Rueden ,  Tingmin Wang

发明人： David Kucera ,  Gregory J. Haley ,  Erik J. Rueden ,  Tingmin Wang

IPC分类号： C07D307/20

CPC分类号： C07D513/04 ,  C07D307/20 ,  C07D493/04

摘要： The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer. Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.

摘要翻译： 本公开涉及5-氨基-3-（2'-O-乙酰基-3'-脱氧-β-D-呋喃核糖基）-3H-噻唑并[4,5-d]嘧啶-2-酮的对甲苯磺酸盐， 并且用于治疗诸如病毒感染，肿瘤和癌症的病症。 还公开了制备5-氨基-3-（2'-O-乙酰基-3'-脱氧-β-呋喃核糖基）-3H-噻唑并[4,5-a]的对甲苯磺酸盐的方法， d]嘧啶-2-酮和制备呋喃糖化合物的方法，其是制备药物化合物的有用的中间体，例如5-氨基-3-（2'-O-乙酰基-3'-脱氧）的对甲苯磺酸盐 - 呋喃核糖基）-3H-噻唑并[4,5-d]嘧啶-2-酮等。

公开(公告)号：US07928085B2

公开(公告)日：2011-04-19

申请号：US11873202

申请日：2007-10-16

申请人： David Kucera ,  Gregory J. Haley ,  Erik J. Rueden ,  Tingmin Wang ,  Fritz Blatter ,  Martin Viertelhaus

发明人： David Kucera ,  Gregory J. Haley ,  Erik J. Rueden ,  Tingmin Wang ,  Fritz Blatter ,  Martin Viertelhaus

IPC分类号： C07H19/00 ,  A61K31/70 ,  A01N43/04

CPC分类号： C07D513/04 ,  C07D307/20 ,  C07D493/04

摘要： The present disclosure relates to p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-beta-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and to its use in treating conditions such as viral infections, tumors, and cancer. Also disclosed is a method of preparing the p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and methods for producing furanose compounds which are useful intermediates in the preparation of pharmaceutical compounds such as p-toluene sulfonic acid salt of 5-amino-3-(2′-O-acetyl-3′-deoxy-β-D-ribofuranosyl)-3H-thiazolo[4,5-d]pyrimidin-2-one and the like.

摘要翻译： 本公开涉及5-氨基-3-（2'-O-乙酰基-3'-脱氧-β-D-呋喃核糖基）-3H-噻唑并[4,5-d]嘧啶-2-酮的对甲苯磺酸盐， 并且用于治疗诸如病毒感染，肿瘤和癌症的病症。 还公开了制备5-氨基-3-（2'-O-乙酰基-3'-脱氧-β-呋喃核糖基）-3H-噻唑并[4,5-a]的对甲苯磺酸盐的方法， d]嘧啶-2-酮和制备呋喃糖化合物的方法，其是制备药物化合物的有用的中间体，例如5-氨基-3-（2'-O-乙酰基-3'-脱氧）的对甲苯磺酸盐 - 呋喃核糖基）-3H-噻唑并[4,5-d]嘧啶-2-酮等。

公开(公告)号：US06414135B1

公开(公告)日：2002-07-02

申请号：US09349035

申请日：1999-07-07

申请人： Phillip Dan Cook ,  Haoyun An ,  Tingmin Wang ,  Muthiah Manoharan

发明人： Phillip Dan Cook ,  Haoyun An ,  Tingmin Wang ,  Muthiah Manoharan

IPC分类号： C07H2100

CPC分类号： C07H21/00 ,  C07H19/10

摘要： The present invention is directed to nucleoside monomers wherein the 3′-O atom is replaced with a methylene group. The present invention also provides oligomers comprising a plurality of such monomers which are linked by methylenephosphonate linkages. Further, methods of preparing monomers and oligomers according to the present invention are provided.

摘要翻译： 本发明涉及其中3'-O原子被亚甲基代替的核苷单体。 本发明还提供了包含多个这样的单体的低聚物，其通过亚甲基膦酸酯键连接。 此外，提供了制备根据本发明的单体和低聚物的方法。

公开(公告)号：US06355666B1

公开(公告)日：2002-03-12

申请号：US09602688

申请日：2000-06-23

申请人： Ching-San Lai ,  Tingmin Wang

发明人： Ching-San Lai ,  Tingmin Wang

IPC分类号： A61K3148

CPC分类号： A61K47/555 ,  A61K47/54

摘要： In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

摘要翻译： 根据本发明，提供了非甾体抗炎药的正常修饰形式。 根据本发明的修饰的NSAID提供了一类新的抗炎剂，其提供NSAIDs的治疗益处，同时引起副作用的发生率低得多，然后通常用这些药剂观察到。