公开(公告)号：US20090306136A1

公开(公告)日：2009-12-10

申请号：US12296788

申请日：2007-04-13

Applicant: Akira Matsumura ,  Hidenori Mikamiyama ,  Bin Shao ,  Naoki Tsuno ,  Jiangchao Yao

Inventor： Akira Matsumura ,  Hidenori Mikamiyama ,  Bin Shao ,  Naoki Tsuno ,  Jiangchao Yao

IPC: A61K31/4468 ,  G01N33/53 ,  A61K31/4545 ,  A61K31/454 ,  C07D401/06 ,  C07D211/56 ,  A61P25/00

CPC classification number: C07D211/58 ,  A61K31/4468 ,  A61K31/4545

Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula (I): and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3, Z, p and q are defined as set forth in the specification. The invention is also directed to the use compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract translation: 本发明涉及式（I）的氮杂环丁烷基，吡咯烷基，哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐，前药或溶剂化物，其中R1-R3，Z，p和q如说明书所述定义。 本发明还涉及使用式（I）化合物来治疗，预防或改善对阻断钙通道，特别是N型钙通道的病症。 本发明的化合物特别适用于治疗疼痛。

公开(公告)号：US09290787B2

公开(公告)日：2016-03-22

申请号：US14119149

申请日：2012-05-15

Applicant: Xinde Xu ,  Mingqing Jiao ,  Dong Shao ,  Bin Shao ,  Leiming Yu

Inventor： Xinde Xu ,  Mingqing Jiao ,  Dong Shao ,  Bin Shao ,  Leiming Yu

IPC: C07C1/00 ,  C12P23/00 ,  A23L1/303 ,  A23L1/275 ,  A61K31/015

CPC classification number: C12P23/00 ,  A23L5/44 ,  A23L33/155 ,  A23V2002/00 ,  A61K31/015 ,  A23V2250/702

Abstract: The present invention provides a method for producing and purifying β-carotene by Blakeslea trispora fermentation and use thereof. The method comprises the following steps: a) separately inoculating the Blakeslea trispora strains onto a PDA culture medium so as to obtain a spore suspension; b) propagating spores in a seeding tank so as to obtain seeds for fermentation; c) inoculating the seeds for fermentation onto a fermenter and fermenting said seeds; d) adjusting the fermentation liquid to be basic by using an organic or inorganic base, and filtering so as to obtain wet mycelia; e) treating the wet mycelia with a hydrophobic non-polar organic solvent; f) mixing the wet mycelia with an organic solvent of ester and obtaining a concentrated solution by extracting; g) adding a saturated monohydric alcohol into the concentrated solution, and filtering and crystallizing so as to obtain pure ss-carotene. The content of the ss-carotene in the present invention exceeds 96%, and the yield is above 85%.

Abstract translation: 本发明提供了通过三孢a菌发酵及其应用来生产和提纯β-胡萝卜素的方法。 该方法包括以下步骤：a）将单孢菌菌株分别接种到PDA培养基上，得到孢子悬浮液; b）在播种槽中繁殖孢子，以获得用于发酵的种子; c）将种子接种发酵到发酵罐上并发酵所述种子; d）通过使用有机或无机碱调节发酵液为碱性，过滤以获得湿菌丝体; e）用疏水性非极性有机溶剂处理湿菌丝体; f）将湿菌丝体与酯的有机溶剂混合，通过萃取获得浓缩溶液; g）向浓缩溶液中加入饱和一元醇，过滤结晶，得到纯β-胡萝卜素。 本发明中β-胡萝卜素的含量超过96％，收率高于85％。

公开(公告)号：US09163008B2

公开(公告)日：2015-10-20

申请号：US14342054

申请日：2012-08-31

Applicant: Chiyou Ni ,  Bin Shao ,  Laykea Tafesse ,  Jiangcho Yao ,  Mark Youngman ,  Minnie Park

Inventor： Chiyou Ni ,  Bin Shao ,  Laykea Tafesse ,  Jiangcho Yao ,  Mark Youngman ,  Minnie Park

IPC: A61K31/506 ,  C07D413/04 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D233/90 ,  C07D401/12 ,  C07D403/04 ,  C07D405/12 ,  C07D239/34 ,  C07D239/42 ,  C07D401/04

CPC classification number: C07D239/42 ,  A61K31/506 ,  C07D233/90 ,  C07D239/34 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04

Abstract: The present disclosure provides substituted pyrimidine compounds of Formula (I), and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein A1, X, A2, W1, W2, E, Z, and R4 are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. Compounds of the present disclosure are especially useful for treating pain.

Abstract translation: 本公开提供式（I）的取代的嘧啶化合物及其药学上可接受的盐，前药和溶剂合物，其中A1，X，A2，W1，W2，E，Z和R4如本说明书所述 。 本公开还涉及式（I）化合物用于治疗对钠通道阻断有反应的病症。 本公开的化合物特别可用于治疗疼痛。

公开(公告)号：US09156830B2

公开(公告)日：2015-10-13

申请号：US14118113

申请日：2012-05-16

Applicant: Noriyuki Kurose ,  Yasuyoshi Iso ,  Naoko Yamaguchi ,  Bin Shao ,  Laykea Tafesse ,  Xiaoming Zhou ,  Jianming Yu

Inventor： Noriyuki Kurose ,  Yasuyoshi Iso ,  Naoko Yamaguchi ,  Bin Shao ,  Laykea Tafesse ,  Xiaoming Zhou ,  Jianming Yu

IPC: A61K31/497 ,  C07D413/14 ,  C07D401/14 ,  C07D401/04 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14 ,  C07D271/10 ,  C07D271/06 ,  C07D405/14

CPC classification number: C07D413/14 ,  C07D271/06 ,  C07D271/10 ,  C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/14

Abstract: The invention relates to compounds of Formula I: wherein Ar1, Ar2, Ar3, L1, L2, Y, Z and v are defined in the specification, and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of Formula I or a pharmaceutically acceptable derivative thereof.

Abstract translation: 本发明涉及式I化合物：其中Ar1，Ar2，Ar3，L1，L2，Y，Z和v在本说明书中定义，及其药学上可接受的衍生物，包含有效量的式I化合物或 药物可接受的衍生物，以及治疗或预防诸如疼痛，UI，溃疡，IBD和IBS的病症的方法，包括向有需要的动物施用有效量的式I化合物或其药学上可接受的衍生物。

公开(公告)号：US08593123B2

公开(公告)日：2013-11-26

申请号：US12979167

申请日：2010-12-27

Applicant: Jia Chen ,  Bin Shao

Inventor： Jia Chen ,  Bin Shao

IPC: G05F1/40

CPC classification number: H02M3/1563

Abstract: Switching voltage regulator embodiments are provided with hysteretic control to thereby switch between pulse-width modulation and pulse-frequency modulation operational modes. The switching is in response to different levels of an error voltage Verr in the feedback loop of voltage regulators. The hysteretic control is configured to provide a dc hysteretic response to changes in the error voltage Verr and also an ac hysteretic response to these changes. These two responses can be independently set to thereby enhance operational speed of the voltage regulators and also enhance immunity to transient noise signals that are generated by the mode switching. The voltage regulator embodiments facilitate instant return from the pulse-frequency modulation operational mode to the pulse-width modulation operational mode so that the stability of the feedback control of the regulator is enhanced. This feature is especially useful when the feedback loop is configured to include current-mode control as it minimizes the time duration in which the feedback loop operates in a voltage-mode control. The instant return insures that the feedback loop is immediately returned to the greater stability of the current-mode control.

Abstract translation: 开关稳压器实施例具有迟滞控制，从而在脉冲宽度调制和脉冲 - 频率调制操作模式之间切换。 开关响应于电压调节器的反馈回路中的不同电平的误差电压Verr。 迟滞控制被配置为对误差电压Verr的变化提供直流迟滞响应，并且还对对这些变化的迟滞响应。 可以独立地设置这两个响应，从而提高电压调节器的操作速度，并且还增强对由模式切换产生的瞬态噪声信号的抗扰性。 电压调节器实施例便于从脉冲 - 频率调制操作模式到脉宽调制操作模式的即时返回，从而增强了调节器的反馈控制的稳定性。 当反馈回路配置为包括电流模式控制时，该功能特别有用，因为它使反馈回路在电压模式控制中工作的持续时间最小化。 即时返回确保反馈回路立即返回到电流模式控制的更大稳定性。

公开(公告)号：US20120296126A1

公开(公告)日：2012-11-22

申请号：US13521044

申请日：2010-03-18

Applicant: Xinde Xu ,  Bin Shao ,  Hongjuan Chao ,  Xuejun Lao ,  Xiaoxia Sun

Inventor： Xinde Xu ,  Bin Shao ,  Hongjuan Chao ,  Xuejun Lao ,  Xiaoxia Sun

IPC: C07C29/56

CPC classification number: C07C403/24 ,  C07C2601/16 ,  C09B61/00

Abstract: The invention makes public a preparing method for xanthophyll crystals with higher content of zeaxanthin from plant oleoresin. The current methods generally are to get quite pure crystal forms of xanthophyll or zeaxanthin, and they refer to several separation steps. The invention mixes the xanthophyll diester-containing plant oleoresins and food grade alcohol solvents to form even solution, and then soap-dissolve the solution under an alkaline environment; then replenish organic solvents and emulsifiers into the reaction solution and drop some alkali solution into the solution to make partial xanthophyll crystals be transformed to be zeaxanthin through epimerization reaction; after the reaction is finished, add the mixed solvents of alcohol solvent and water to separate out the crystals; use the method of centrifugation or filtration to get the crystals; wash the crystals several times with the mixed solution of deionized water and alcohols to remove the impurities among the crystals; recrystallize the gained crystals with absolute ethyl alcohol, and then dry the crystals to get the products. The invention can gain mixture crystals that contain xanthophyll and zeaxanthin at one time in quite high collection rate, and it is convenient for the followed product application.

Abstract translation: 本发明公开了植物油树脂中玉米黄质含量较高的叶黄素晶体的制备方法。 目前的方法通常是获得相当纯的叶黄素或玉米黄质的晶体形式，它们是指几个分离步骤。 本发明混合含有叶黄素二酯的植物油树脂和食品级醇溶剂，形成均匀的溶液，然后在碱性环境下将溶液皂溶; 然后将有机溶剂和乳化剂补充到反应溶液中，并将一些碱溶液滴入溶液中，使部分叶黄素晶体通过差向异构化反应转化为玉米黄质; 反应完成后，加入醇溶剂和水的混合溶剂分离出晶体; 使用离心或过滤方法得到晶体; 用去离子水和醇的混合溶液洗涤晶体数次以除去晶体中的杂质; 用绝对乙醇重结晶获得的晶体，然后干燥晶体得到产物。 本发明可以以非常高的收集率一次获得含有叶黄素和玉米黄质的混合物晶体，对于随后的产品应用是方便的。

公开(公告)号：US08247442B2

公开(公告)日：2012-08-21

申请号：US12225743

申请日：2007-03-29

Applicant: Zhengming Chen ,  Khondaker Islam ,  Bin Shao ,  Jiangchao Yao ,  Donald J. Kyle

Inventor： Zhengming Chen ,  Khondaker Islam ,  Bin Shao ,  Jiangchao Yao ,  Donald J. Kyle

IPC: A61K31/40 ,  C07D207/14

CPC classification number: C07D211/42 ,  C07D207/14 ,  C07D401/12

Abstract: The invention relates to azetidinyl, pyrrolidinyl, piperidinyl, and hexahydroazepinyl compounds of Formula I and pharmaceutically acceptable salts, prodrugs, or solvates thereof, wherein R1-R3 and Z are defined as set forth in the specification. The invention is also directed to the use compounds of Formula I to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

Abstract translation: 本发明涉及式I的氮杂环丁烷基，吡咯烷基，哌啶基和六氢氮杂卟啉化合物及其药学上可接受的盐，前药或溶剂合物，其中R1-R3和Z如说明书所述定义。 本发明还涉及使用式I的化合物来治疗，预防或改善对阻断钙通道，特别是N型钙通道有响应的病症。 本发明的化合物特别适用于治疗疼痛。

公开(公告)号：US20090291947A1

公开(公告)日：2009-11-26

申请号：US12350450

申请日：2009-01-08

Applicant: Bin Shao ,  Jiangchao Yao

Inventor： Bin Shao ,  Jiangchao Yao

IPC: A61K31/535 ,  C07D265/36 ,  A61P3/10

CPC classification number: C07D409/12 ,  C07D207/48 ,  C07D403/12 ,  C07D409/14

Abstract: The present invention relates to Proline Analog Compounds that are ligands for cannabinoid receptors, compositions comprising a Proline Analog Compound and a pharmaceutically-acceptable carrier, methods of making such Proline Analog Compounds, and methods for treating or preventing a Condition comprising administering an effective amount of a Proline Analog Compound to an animal in need thereof.

Abstract translation: 本发明涉及作为大麻素受体配体的脯氨酸类似物化合物，包含脯氨酸类似物化合物和药学上可接受的载体的组合物，制备此类脯氨酸类似物的方法，以及用于治疗或预防病症的方法，包括给予有效量的 脯氨酸类似物化合物给有需要的动物。

公开(公告)号：US07485738B2

公开(公告)日：2009-02-03

申请号：US11857248

申请日：2007-09-18

Applicant: Xinde Xu ,  Lihua Zhang ,  Boqiu Chen ,  Di Zhou ,  Shuangming Ye ,  Chiyu Ding ,  Hongping Lv ,  Bin Shao

Inventor： Xinde Xu ,  Lihua Zhang ,  Boqiu Chen ,  Di Zhou ,  Shuangming Ye ,  Chiyu Ding ,  Hongping Lv ,  Bin Shao

IPC: C07C51/353

CPC classification number: C07C403/24 ,  A23L5/44 ,  A23L33/10 ,  C07C2601/16 ,  C09B61/00 ,  C09B67/0025 ,  C09B67/0096

Abstract: This invention has disclosed a method for preparation of food-grade zeaxanthin through chemical isomerizaton reaction from lutein. The technical issues to be solved in this invention are quite low product yield obtained with existing methods, need of purification treatment process, and inadaptability to industrialized production. The technical schemes of this invention are: a. Mix xanthophyll crystal or its fatty acid ester with food-grade glycol or propylene glycol, for full dissolution under 60-90° C. temperature. Add organic alkali into the mixed liquor acquired from step 1, for isomerization reaction to take place under inertial environment. c. Dilute the reaction solution gained from step b with the mixed solution of deionized water and ethanol, and separate the obtained crystal with conventional separating method. d. Vacuum dries the acquired crystal from step c, to get the zeaxanthin crystal. Glycol or propylene glycol is used in this invention for isomerization reaction under inertial environment after it has fully dissolved raw material under proper temperature. The product yield is reachable to more than 60%, very adaptable to industrialized product, without the need for further purification treatment.

Abstract translation: 本发明公开了通过叶黄素化学异构化反应制备食品级玉米黄质的方法。 本发明要解决的技术问题是用现有方法获得的产品产率相当低，需要净化处理工艺，以及对工业化生产的适应性。 本发明的技术方案是：a。 将叶黄素晶体或其脂肪酸酯与食品级二醇或丙二醇混合，在60-90℃的温度下完全溶解。 将有机碱添加到从步骤1获得的混合液中，以在惯性环境下进行异构化反应。 C。 用去离子水和乙醇的混合溶液稀释从步骤b获得的反应溶液，并用常规分离方法分离得到的晶体。 d。 真空干燥步骤c获得的晶体，得到玉米黄质晶体。 乙二醇或丙二醇在本发明中在适当温度下完全溶解原料之后，在惯性环境下用于异构化反应。 产品产量可达60％以上，非常适用于工业化产品，无需进一步净化处理。

公开(公告)号：US20080194627A9

公开(公告)日：2008-08-14

申请号：US11518448

申请日：2006-09-11

Applicant: Bin Shao ,  R. Goehring ,  Samuel Victory

Inventor： Bin Shao ,  R. Goehring ,  Samuel Victory

IPC: A61K31/4545 ,  A61K31/455 ,  C07D403/02

CPC classification number: C07D213/81 ,  C07D213/82 ,  Y10T436/145555

Abstract: This invention relates aryl substituted pyridines of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Ar and R1—R4 are set in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract translation: 本发明涉及式I的芳基取代的吡啶：或其药学上可接受的盐，前药或溶剂化物，其中Ar和R 1 -R 4定义在说明书中。 本发明还涉及式I化合物用于治疗全身和局部缺血后的神经元损伤，用于治疗或预防神经变性疾病如肌萎缩性侧索硬化（ALS）以及治疗，预防或改善的用途 作为抗惊厥剂，作为抗惊厥剂，作为抗躁狂抑制剂，作为局部麻醉剂，作为抗心律失常药物和用于治疗或预防糖尿病性神经病变。