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1. 发明授权

US09783567B2 Processes and intermediates for preparing anti-HIV agents 有权
公开(公告)号：US09783567B2
公开(公告)日：2017-10-10
申请号：US15046399
申请日：2016-02-17
申请人： Gilead Sciences, Inc.
发明人： Richard Hung Chiu Yu , Brandon Heath Brown , Richard P. Polniaszek , Benjamin R. Graetz , Keiko Sujino , Duong Tran , Alan Scott Triman , Kenneth M. Kent , Steven Pfeiffer
IPC分类号： C07H19/00 , C07H19/22 , C07H19/20 , C07H19/02 , C07H19/04 , C07H19/173 , C07D473/34 , C07F9/40 , C07F9/44 , C07F9/6561 , C07H19/16 , C07H23/00
CPC分类号： C07H19/20 , C07D473/34 , C07F9/4075 , C07F9/4449 , C07F9/65616 , C07H19/02 , C07H19/04 , C07H19/16 , C07H19/173 , C07H23/00
摘要： The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.

2. 发明授权

US08232387B2 Process for the preparation of cladribine 有权
标题翻译：克拉屈滨制备工艺
公开(公告)号：US08232387B2
公开(公告)日：2012-07-31
申请号：US12857939
申请日：2010-08-17
申请人： Julian Paul Henschke , Xiaoheng Zhang , Guodong Chu , Lijun Mei , Yung Fa Chen
发明人： Julian Paul Henschke , Xiaoheng Zhang , Guodong Chu , Lijun Mei , Yung Fa Chen
IPC分类号： C07H19/00 , C07H19/22 , A01N43/04 , A61K31/70
CPC分类号： C07H19/173 , C07H1/00
摘要： A process for the preparation of cladribine of API grade is provided by direct coupling of O-protected 2-deoxy-ribofuranose with silylated 2-chloroadenine followed by deprotection of the resultant protected nucleoside in a separate step and then a purification step. Following the coupling, the desired N-9-glycosylated β-anomer of the nucleoside is directly isolated as a solid from the coupling reaction mixture by filtration in relatively high purity and yield, and it does not require purification.
摘要翻译：通过将O-保护的2-脱氧 - 呋喃核糖与甲硅烷基化的2-氯腺嘌呤直接偶联，然后在单独的步骤中将所得的被保护的核苷脱保护，然后进行纯化步骤，提供API级克拉屈滨的制备方法。偶联后，通过过滤以相对较高的纯度和产率将核苷的所需N-9-糖基化 - 单体直接从偶联反应混合物中分离为固体，并且不需要纯化。

3. 发明授权

US08114986B2 Analogous compounds of 6-thioguanosine triphosphate, their use in medical fields and processes for their preparation 失效
标题翻译： 6-硫代鸟苷三磷酸类似物，用于医疗领域及其制备方法
公开(公告)号：US08114986B2
公开(公告)日：2012-02-14
申请号：US11989054
申请日：2006-07-24
申请人： Giancarlo Naccari , Sergio Baroni
发明人： Giancarlo Naccari , Sergio Baroni
IPC分类号： C07H19/22
CPC分类号： C07H19/16 , C07H19/20
摘要： The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III). And wherein X represents either carbon or nitrogen atom within aromatic ring, Y represents either oxygen or sulphur atom and an additional group Q, group Qi or groups Qi (Qi indicates that the group or several groups may be bound to any unsaturated moiety of the ring) are selected from the group consisting of —OH, —COOH, —N(CH3)2, —N(CH2—CH3)2|—CO—CH3, —CO—O—CH3, —O—CH3, —S—CH3, —SO2—CH3, —CN, —NO2 or -Halogen elements, and wherein R5 may be formula (IV) and metal and ammonium salts thereof, wherein n is between O and 5, or oxygen or phosphorus is partially or completely replaced by nitrogen, sulphur, methyleno groups or their derivatives. The invention also concerns the uses of the above mentioned compounds in medical field and the process for their preparation.
摘要翻译：本发明涉及通式（I）的6-硫代鸟嘌呤三磷酸的类似化合物。通式（I）的化合物; 其中所述糖部分中的虚线键可以是单键或双键，并且其中彼此相同或不同的R 1，R 2，R 3，R 4或R 5具有通式 - （Int）m-Ter，其中m在0和 12和Int和Ter是内部和末端构建单元，其中Int选自式（II）; 和Ter选自由式（III）组成的组。并且其中X表示芳族环中的碳原子或氮原子，Y表示氧或硫原子，另外的基团Q，基团Q 1或基团Q 1（Qi表示该基团或若干基团可以与环的任何不饱和部分结合）选自-OH，-COOH，-N（CH 3）2，-N（CH 2 -CH 3）2 | -CO-CH 3，-CO-O-CH 3，-O-CH 3，-S- CH 3，-SO 2 -CH 3，-CN，-NO 2或H原子元素，其中R 5可以是式（IV）及其金属和铵盐，其中n在0和5之间，或氧或磷被部分或完全替代通过氮，硫，亚甲基或其衍生物。本发明还涉及上述化合物在医疗领域中的用途及其制备方法。

4. 发明申请

US20110009609A1 2'-HYDROXY-PROTECTED RIBONUCLEOSIDE DERIVATIVE AND PRODUCTION METHOD THEREOF 失效
标题翻译： 2'-羟基保护的核糖核苷衍生物及其生产方法
公开(公告)号：US20110009609A1
公开(公告)日：2011-01-13
申请号：US12919295
申请日：2009-02-26
申请人： Hirofumi Maeda , Akio Fujii , Masaru Mitsuda
发明人： Hirofumi Maeda , Akio Fujii , Masaru Mitsuda
IPC分类号： C07H19/22 , C07H19/00
CPC分类号： C07H19/067 , C07H19/167
摘要： The present invention relates to a method for producing a 2′-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2′-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2′,3′-hydroxy groups are not protected.
摘要翻译：本发明涉及通过在由铜化合物和光学活性配体组成的金属络合物的存在下使核糖核苷与酰化剂反应来制备2'-羟基保护的核苷衍生物的方法。通过本发明的方法，可以容易地制备作为制备寡核苷酸的重要中间体的2'-羟基保护的核糖核苷衍生物，其从2'，3'-羟基的核苷衍生物具有良好的区域选择性没有保护。

5. 发明授权

US07763465B1 Unique novel Bacillus thuringiensis gene with lepidopteran activity 有权
公开(公告)号：US07763465B1
公开(公告)日：2010-07-27
申请号：US12402781
申请日：2009-03-12
申请人： Andre R. Abad , Hua Dong , Sue B. Lo , Xiaomei Shi
发明人： Andre R. Abad , Hua Dong , Sue B. Lo , Xiaomei Shi
IPC分类号： A01H5/00 , C07H19/00 , C07H19/22 , C12N5/00 , C07K17/00 , C07K14/00 , C07K1/00
CPC分类号： C07K14/325 , C12N15/8286 , Y02A40/162
摘要： The invention provides nucleic acids, and variants and fragments thereof, obtained from strains of Bacillus thuringiensis encoding polypeptides having pesticidal activity against insect pests, including Lepidoptera. Particular embodiments of the invention provide isolated nucleic acids encoding pesticidal proteins, pesticidal compositions, DNA constructs, and transformed microorganisms and plants comprising a nucleic acid of the embodiments. These compositions find use in methods for controlling pests, especially plant pests.

6. 发明授权

US07569555B2 Method for stimulating the immune, inflammatory or neuroprotective response 有权
标题翻译：刺激免疫，炎症或神经保护作用的方法
公开(公告)号：US07569555B2
公开(公告)日：2009-08-04
申请号：US11079886
申请日：2005-03-15
申请人： David K. R. Karaolis
发明人： David K. R. Karaolis
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/22
CPC分类号： A61K31/7084 , A61K31/7076 , A61K39/39 , A61K2039/55511 , A61K2039/55561
摘要： Cycic di-GMP, or a cyclic dinucleotide analogue thereof that has the same effect as cyclic di-GMP, stimulates or enhances immune or inflammatory response in a patient or enhances the immune response to a vaccine by serving as an adjuvant. Cyclic di-GMP, or a cyclic dinucleotide analogue thereof, also has neuroprotective properties for use as a neuroprotective agent to inhibit, treat, or ameliorate the effects of injuries, diseases, disorders or conditions that result in neurodegeneration.
摘要翻译：具有与环状二-GMP相同作用的环状二-GMP或其环状二核苷酸类似物刺激或增强患者的免疫或炎症反应，或通过作为佐剂增强对疫苗的免疫应答。环状二-GMP或其环二核苷酸类似物也具有用作神经保护剂以抑制，治疗或改善导致神经变性的损伤，疾病，病症或病症的作用的神经保护性质。

7. 发明授权

US07452870B2 Drug-eluting stents coated with P2Y12 receptor antagonist compound 失效
标题翻译：用P2Y 12受体拮抗剂化合物涂覆的药物洗脱支架
公开(公告)号：US07452870B2
公开(公告)日：2008-11-18
申请号：US11267834
申请日：2005-11-04
申请人： José L. Boyer , James G. Douglass, III , Sammy R. Shaver
发明人： José L. Boyer , James G. Douglass, III , Sammy R. Shaver
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/22
CPC分类号： C07H19/04 , A61K31/675 , A61K31/7072 , A61K31/7076 , A61K31/7084 , C07H19/10 , C07H19/20 , C07H19/207 , C07H21/00
摘要： The present invention provides a P2Y12 receptor antagonist compound-eluting stent, wherein the stent is coated with one or more P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.
摘要翻译：本发明提供P2Y 12受体拮抗剂化合物洗脱支架，其中支架涂覆有一种或多种P2Y 12受体拮抗剂化合物或其药学上可接受的盐，溶剂化物，或其水合物。当支架置于狭窄或损伤的动脉血管中时，治疗有效量的P2Y 12受体拮抗剂化合物从支架连续洗脱至支架的局部环境。 P2Y 12受体拮抗剂化合物洗脱支架可用于预防血栓形成和再狭窄，并且有效抑制血管平滑肌细胞的收缩，抑制细胞增殖和减少炎症。

8. 发明授权

US07396825B2 Agonists of A2A adenosine receptors for treatment of diabetic nephropathy 有权
标题翻译： A2A腺苷受体激动剂治疗糖尿病肾病
公开(公告)号：US07396825B2
公开(公告)日：2008-07-08
申请号：US11121169
申请日：2005-05-03
申请人： Mark D. Okusa , Joel M. Linden , Timothy L. Macdonald , Alaa S. Awad
发明人： Mark D. Okusa , Joel M. Linden , Timothy L. Macdonald , Alaa S. Awad
IPC分类号： A01N43/04 , A61K31/70 , C07H19/00 , C07H19/22
CPC分类号： A61K31/7076 , A61K31/70
摘要： The present invention provides a therapeutic method for treating diabetic kidney disease, e.g., diabetic nephropathy that includes the administration of an effective amount of an A2A adenosine receptor agonist. Optionally, the method includes administration of a type IV PDE inhibitor.
摘要翻译：本发明提供治疗糖尿病肾病的治疗方法，例如包括施用有效量的Aβ2A腺苷受体激动剂的糖尿病性肾病。任选地，该方法包括施用IV型PDE抑制剂。

9. 发明申请

US20070203334A1 Process for preparing a synthetic intermediate for preparation of branched nucleosides 有权
标题翻译：制备分支核苷合成中间体的方法
公开(公告)号：US20070203334A1
公开(公告)日：2007-08-30
申请号：US11644304
申请日：2006-12-22
申请人： Benjamin Mayes , Adel Moussa
发明人： Benjamin Mayes , Adel Moussa
IPC分类号： C07H19/048 , C07D309/30 , C07D305/12 , C07H19/22
CPC分类号： C07H15/24 , C07D307/33 , C07D309/30 , C07H19/048 , C07H19/22
摘要： A process is provided for the preparation of a key intermediate in the preparation of 2′-branched nucleoside compounds. The process includes contacting a protected precursor 3,4-O-isopropylidene-2-C-substituted-D-arabinono-1,5-lactone with a fluorinating agent under anhydrous conditions and converting the precursor into a protected 2-deoxy-2-halo-2-C-disubstituted ribono-1,5-lactone and optionally into a 2-deoxy-2-halo-2-C-disubstituted ribono-1,4-lactone.
摘要翻译：提供了制备2支支化核苷化合物的关键中间体的方法。该方法包括在无水条件下将受保护的前体3,4-O-异亚丙基-2-C取代的-MacLCAPS> D - 阿拉蛋酸-1,5-内酯与氟化剂接触并将前体转化为保护的2-脱氧-2-卤-2- C - 二取代的ribono-1,5-内酯，任选地加入到2-脱氧-2-卤代-2- C-二取代的核糖内-1,4-内酯中。

10. 发明申请

US20070167383A1 NUCLEOSIDE COMPOUNDS FOR TREATING VIRAL INFECTIONS 审中-公开
标题翻译：用于治疗病毒感染的核苷酸化合物
公开(公告)号：US20070167383A1
公开(公告)日：2007-07-19
申请号：US11559475
申请日：2006-11-14
申请人： Christopher Roberts , Jesse Keicher , Natalia Dyatkina
发明人： Christopher Roberts , Jesse Keicher , Natalia Dyatkina
IPC分类号： A61K31/7076 , C07H19/20 , C07H19/22
CPC分类号： C07H19/14 , A61K31/7076
摘要： Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus.
摘要翻译：公开了用于治疗由黄病毒科家族病毒（例如丙型肝炎病毒）引起的病毒感染的化合物，组合物和方法。

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