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1. 发明授权

US06573248B2 Monocyclic L-nucleosides, analogs and uses thereof 有权
标题翻译：单环L-核苷类似物及其用途
公开(公告)号：US06573248B2
公开(公告)日：2003-06-03
申请号：US09969355
申请日：2001-12-31
申请人： Kandasamy Ramasamy , Robert Tam , Devron Averett
发明人： Kandasamy Ramasamy , Robert Tam , Devron Averett
IPC分类号： A61K3170
CPC分类号： C07H19/04
摘要： Novel monocyclic L-Nucleoside compounds have the general formula Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.
摘要翻译：新型单环L-核苷化合物具有通式。这些化合物的实施方案被认为可用于治疗各种疾病，包括感染，感染，肿瘤和自身免疫性疾病。从机理来看，新化合物的实施方案显示免疫调节活性，并且预期可用于调节细胞因子模式，包括Th1和Th2应答的调节。

2. 发明授权

US06423695B1 Cytokine related treatments of disease 有权
公开(公告)号：US06423695B1
公开(公告)日：2002-07-23
申请号：US09467443
申请日：1999-12-20
申请人： Robert Tam , Guangyi Wang , Devron Averett , Kandasamy Ramasamy
发明人： Robert Tam , Guangyi Wang , Devron Averett , Kandasamy Ramasamy
IPC分类号： A61K31675
CPC分类号： A61K31/675
摘要： Nucleosides and other compounds to selectively modulate Th1 and Th2 responses relative to each other in the treatment of disease. In one aspect of the invention, administration of a nucleoside or other compound reduces the dosage at which a primary drug is administered. In another aspect of the invention, an abnormality reflected in increased response in one group of cytokines is treated by administering a nucleoside or other compound that increases response in another group of cytokines. In yet another aspect of the invention, a patient is prophylactically treated by administering a nucleoside or other compound that selectively reduces Th1 activity without significantly reducing Th2 activity. In yet another aspect of the invention, a nucleoside or other compound is administered to a patient at a dose that reduces the patient's GTP pool to a degree that selectively reduces one of the Th1 or Th2 responses without significantly reducing the other response. Controlled release dosage forms are particularly contemplated to achieve that result.

3. 发明授权

US06613896B1 Method of producing tiazofurin and other C-nucleosides 失效
标题翻译：制备噻唑呋喃和其他C-核苷的方法
公开(公告)号：US06613896B1
公开(公告)日：2003-09-02
申请号：US09445713
申请日：2000-06-06
申请人： Kandasamy Ramasamy , Rajanikanth Bandaru , Devron Averett
发明人： Kandasamy Ramasamy , Rajanikanth Bandaru , Devron Averett
IPC分类号： C07H706
CPC分类号： C07D417/04 , C07H9/02 , C07H19/04
摘要： C-nucleosides are synthesized by a method in which a sugar is derivatized in a single step to provide a heterocycle at the C1 position, and then the heterocycle is aromatized in another single step. In one class of preferred embodiments a cyano sugar is converted into thiocarboxamide, and subsequently condensed to form an azole ring. In a second class of preferred embodiments a cyano sugar is condensed with an amino acid to provide the azole ring. In a third class of preferred embodiments a halo sugar is condensed with a preformed heterocycle to provide the azole ring.
摘要翻译： C-核苷通过其中糖在单一步骤中衍生化以在C1位置提供杂环的方法合成，然后在另一个单一步骤中使杂环芳构化。在一类优选实施方案中，将氰基糖转化为硫代羧酰胺，随后冷凝以形成唑环。在第二类优选实施方案中，将氰基糖与氨基酸缩合以提供唑环。在第三类优选实施方案中，将卤糖与预先形成的杂环缩合以提供唑环。

4. 发明授权

US06262241B1 Compound for detecting and modulating RNA activity and gene expression 失效
标题翻译：用于检测和调节RNA活性和基因表达的化合物
公开(公告)号：US06262241B1
公开(公告)日：2001-07-17
申请号：US08383666
申请日：1995-02-03
申请人： Phillip Dan Cook , David J. Ecker , Charles John Guinosso , Oscar Leobardo Acevedo , Andrew Kawasaki , Kandasamy Ramasamy
发明人： Phillip Dan Cook , David J. Ecker , Charles John Guinosso , Oscar Leobardo Acevedo , Andrew Kawasaki , Kandasamy Ramasamy
IPC分类号： C12Q168
CPC分类号： C12N15/113 , A61K38/00 , A61K47/51 , A61K48/00 , C07H19/04 , C07H19/06 , C07H19/10 , C07H19/16 , C07H19/20 , C07H21/00 , C07H23/00 , C07J43/003 , C12N9/0069 , C12N15/1131 , C12N15/1132 , C12N15/1133 , C12N15/1135 , C12N15/1137 , C12N15/1138 , C12N2310/3125 , C12N2310/315 , C12N2310/318 , C12N2310/32 , C12N2310/321 , C12N2310/322 , C12N2310/33 , C12N2310/333 , C12N2310/336 , C12N2310/3521 , C12N2310/3523 , C12N2310/3527 , C12N2310/3531 , C12N2310/3533 , C12Q1/68 , C12Y113/11012
摘要： Compositions and methods for modulating the activity of RNA and DNA are disclosed. In accordance with preferred embodiments, antisense compositions are prepared comprising targeting and reactive portions. Reactive portions which act, alternatively, through phosphorodiester bond cleavage, through backbone sugar bond cleavage or through base modification are preferrably employed. Groups which improve the pharmacodynamic and pharmacokinetic properties of the oligonucleotides are also useful in accordance with certain embodiments of this invention. Delivery of the reactive or non-reactive functionalities into the minor groove formed by the hybridization of the composition with the target RNA is also preferrably accomplished. Therapeutics, diagnostics and research methods and also disclosed. Synthetic nucleosides and nucleoside fragments are also provided useful for elaboration of oligonucleotides and oligonucleotide analogs for such purposes.
摘要翻译：公开了调节RNA和DNA活性的组合物和方法。根据优选实施方案，制备包含靶向和反应部分的反义组合物。优选使用通过骨架糖键切割或通过碱改性而作用或通过磷酸酯键断裂的反应性部分。根据本发明的某些实施方案，提高寡核苷酸的药效学和药代动力学性质的组也是有用的。通过组合物与靶RNA的杂交形成的反应性或非反应性官能团的递送也是优选的。治疗，诊断和研究方法也被披露。合成核苷和核苷片段也可用于制备用于这些目的的寡核苷酸和寡核苷酸类似物。

5. 发明授权

US5681940A Sugar modified nucleosides and oligonucleotides 失效
标题翻译：糖修饰核苷和寡核苷酸
公开(公告)号：US5681940A
公开(公告)日：1997-10-28
申请号：US333545
申请日：1994-11-02
申请人： Guangyi Wang , Kandasamy Ramasamy , Wilfried E. Seifert
发明人： Guangyi Wang , Kandasamy Ramasamy , Wilfried E. Seifert
IPC分类号： C12N15/09 , A61K31/52 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7068 , A61K31/7072 , A61K31/7076 , A61K31/708 , A61K31/7088 , A61K48/00 , A61P29/00 , A61P31/00 , A61P31/12 , A61P35/00 , C07D239/47 , C07D239/54 , C07D403/04 , C07D405/04 , C07D409/04 , C07D473/00 , C07D473/18 , C07D473/34 , C07H19/04 , C07H19/06 , C07H19/073 , C07H19/10 , C07H19/16 , C07H21/00 , C07H19/00 , A01N43/04 , C07H21/02
CPC分类号： C07H19/06 , C07H19/10 , C07H21/00
摘要： A number of modified nucleosides are disclosed composed of modified sugar moieties which contain substituents at C1 and C4 positions, or branched substituents at C3 and C5 positions of deoxyribose or ribose. Each nucleoside is converted to or properly protected and then converted to the corresponding phosphoramidites. These phosphoramidites are used to assemble oligonucleotides in which there is at least one forenoted nucleosides. These sugar modified oligonucleotides have the potential to be used as antisense therapies since they are expected to enhance nuclease resistance and cellular uptake while they maintain sequence-specificity and affinity to nucleic acid targets in vitro or in vivo.
摘要翻译：公开了一些修饰的核苷，其由在C1和C4位置含有取代基的修饰的糖部分或脱氧核糖或核糖的C3和C5位置的支链取代基组成。将每个核苷转化成或适当保护，然后转化成相应的亚磷酰胺。这些亚磷酰胺用于组装寡核苷酸，其中存在至少一种预先注射的核苷。这些糖修饰的寡核苷酸具有用作反义治疗的潜力，因为它们预期在体外或体内维持序列特异性和对核酸靶标的亲和力，从而增强核酸酶抗性和细胞摄取。

6. 发明授权

US06552183B1 Moncyclic L-nucleosides analogs 有权
标题翻译：单环L-核苷类似物
公开(公告)号：US06552183B1
公开(公告)日：2003-04-22
申请号：US09633493
申请日：2000-08-07
申请人： Kandasamy Ramasamy , Robert Tam , Devron Averett
发明人： Kandasamy Ramasamy , Robert Tam , Devron Averett
IPC分类号： C07H19044
CPC分类号： C07H19/04
摘要： Novel monocyclic L-Nucleoside compounds have the general formula Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.
摘要翻译：新型单环L-核苷化合物具有通式。这些化合物的实施方案被认为可用于治疗各种疾病，包括感染，感染，肿瘤和自身免疫性疾病。从机理来看，新化合物的实施方案显示免疫调节活性，并且预期可用于调节细胞因子模式，包括Th1和Th2应答的调节。

7. 发明授权

US07638496B2 Nucleoside analogs with carboxamidine modified monocyclic base 有权
标题翻译：具有甲脒改性单环碱的核苷类似物
公开(公告)号：US07638496B2
公开(公告)日：2009-12-29
申请号：US10227235
申请日：2002-08-22
申请人： Robert Tam , Kandasamy Ramasamy , Zhi Hong , Johnson Lau
发明人： Robert Tam , Kandasamy Ramasamy , Zhi Hong , Johnson Lau
IPC分类号： A01N43/04 , A61K31/70
CPC分类号： A61K31/7056 , A61K31/70 , C07H19/056 , C07H19/14
摘要： Novel nucleoside analog compounds are disclosed. The novel compounds or pharmaceutically acceptable esters or salts thereof may be used in pharmaceutical compositions, and such compositions may be used to treat an infection, an infestation, a neoplasm, or an autoimmune disease. The novel compounds may also be used to modulate aspects of the immune system, including modulation of Type 1 and Type 2 activity.
摘要翻译：公开了新的核苷类似物化合物。新化合物或其药学上可接受的酯或其盐可以用于药物组合物中，并且这些组合物可用于治疗感染，感染，肿瘤或自身免疫性疾病。新化合物也可用于调节免疫系统的方面，包括调节1型和2型活性。

8. 发明授权

US06211201B1 Multivalent salts of pyridostigmine and related compounds 有权
标题翻译：吡斯的明和相关化合物的多价盐
公开(公告)号：US06211201B1
公开(公告)日：2001-04-03
申请号：US09308723
申请日：1999-06-29
申请人： Colin Granger , Robert Orr , Kandasamy Ramasamy
发明人： Colin Granger , Robert Orr , Kandasamy Ramasamy
IPC分类号： A61K31444
CPC分类号： C07D239/34 , C07C271/42 , C07D213/65
摘要： A quaternary ammonium cholinergic agent is complexed with a multivalent anion, or with multiple monovalent anions. The complex may be administered orally to a patient to treat pain, or for some other purpose. Numerous modifications are contemplated, including modifications to the ring structure of the compound, substitution and functionalization of the ring. Other contemplated modifications include the use of different anions, including various monovalent and polyvalent anions, and both organic and inorganic anions. The compounds have utility as cholinergic agents, and especially in the treatment of mysasthenia gravis, chest pain, and carpal tunnel syndrome.
摘要翻译：季铵胆碱能药剂与多价阴离子或多价单价阴离子络合。复合物可以口服给予患者以治疗疼痛或用于其它目的。考虑到许多修饰，包括化合物的环结构的修饰，环的取代和官能化。其他预期的修改包括使用不同的阴离子，包括各种单价和多价阴离子，以及有机和无机阴离子。该化合物具有胆碱能药物的功效，特别是治疗重症肌无力，胸痛和腕管综合症。

9. 发明授权

US6130326A Monocyclic L-Nucleosides, analogs and uses thereof 失效
标题翻译：单环L-核苷类似物及其用途
公开(公告)号：US6130326A
公开(公告)日：2000-10-10
申请号：US291903
申请日：1999-04-14
申请人： Kandasamy Ramasamy , Robert Tam , Devron Averett
发明人： Kandasamy Ramasamy , Robert Tam , Devron Averett
IPC分类号： C07H15/20 , A61K31/4155 , A61K31/4196 , A61K31/427 , A61K31/70 , A61K31/7056 , A61K31/706 , A61K31/7068 , A61K31/7072 , A61P31/00 , A61P33/00 , A61P35/00 , A61P37/02 , A61P37/06 , C07D405/04 , C07D405/12 , C07D517/00 , C07H7/06 , C07H19/00 , C07H19/04 , C07H19/044 , C07H19/048 , C07H19/052 , C07H19/056 , C07H19/067 , C07H19/12
CPC分类号： C07H19/04
摘要： Novel monocyclic L-Nucleoside compounds have the general formula ##STR1## Embodiments of these compounds are contemplated to be useful in treating a wide variety of diseases including infections, infestations, neoplasms, and autoimmune diseases. Viewed in terms of mechanism, embodiments of the novel compounds show immunomodulatory activity, and are expected to be useful in modulating the cytokine pattern, including modulation of Th1 and Th2 response.
摘要翻译：新颖的单环L-核苷化合物具有通式这些化合物的实施方案被认为可用于治疗各种疾病，包括感染，感染，赘生物和自身免疫性疾病。从机理来看，新化合物的实施方案显示免疫调节活性，并且预期可用于调节细胞因子模式，包括Th1和Th2应答的调节。

10. 发明授权

US5969135A Oligonucleotide analogs with an amino acid or a modified amino alcohol residue 失效
标题翻译：具有氨基酸或修饰的氨基醇残基的寡核苷酸类似物
公开(公告)号：US5969135A
公开(公告)日：1999-10-19
申请号：US551947
申请日：1995-11-02
申请人： Kandasamy Ramasamy , Wilfried E. Seifert
发明人： Kandasamy Ramasamy , Wilfried E. Seifert
IPC分类号： C07D239/54 , C07D403/06 , C07D403/14 , C07D473/00 , C07F9/02
CPC分类号： C07D239/54 , C07D403/06 , C07D403/14
摘要： The present invention provides various novel oligonucleotide analogs having one or more properties that make the subject compounds superior to conventional oligonucleotides for use in procedures employing oligonucleotides. The compounds of the invention are oligonucleotide analogs in which the furanose ring of a naturally occurring nucleic acid is replaced with an amino acid or a modified amino alcohol residue. Some embodiments of the novel compounds of the invention are particularly useful for the antisense control of gene expression. The compounds of the invention may also be used as nucleic acid hybridization probes or as primers. Another aspect of the invention is to provide monomeric precursors of the oligonucleotide analogs of the invention. These monomeric precursors may be used to synthesize the subject polynucleotide analogs. Another aspect of the invention is to provide formulations of the subject polynucleotide analogs that are designed for the treatment or prevention of disease conditions. Yet another aspect of the invention is to provide methods for treating or preventing diseases, particularly viral infections and cell growth disorders. The subject disease treatment methods comprise the step of administering an effective amount of the subject polynucleotide analogs for use as antisense inhibitors.
摘要翻译：本发明提供了具有使得本发明化合物优于常规寡核苷酸的一种或多种性质的各种新型寡核苷酸类似物，用于使用寡核苷酸的方法中。本发明的化合物是其中天然存在的核酸的呋喃糖环被氨基酸或修饰的氨基醇残基替代的寡核苷酸类似物。本发明的新化合物的一些实施方案对于基因表达的反义控制特别有用。本发明的化合物也可以用作核酸杂交探针或引物。本发明的另一方面是提供本发明的寡核苷酸类似物的单体前体。这些单体前体可用于合成受试多核苷酸类似物。本发明的另一方面是提供被设计用于治疗或预防疾病状况的受试多核苷酸类似物的制剂。本发明的另一方面是提供用于治疗或预防疾病，特别是病毒感染和细胞生长障碍的方法。受试者疾病治疗方法包括施用有效量的用作反义抑制剂的受试多核苷酸类似物的步骤。

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