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1. 发明授权

US11596716B2 Compounds and matrices for use in bone growth and repair 有权
公开(公告)号：US11596716B2
公开(公告)日：2023-03-07
申请号：US17136830
申请日：2020-12-29
申请人： Human BioMolecular Research Institute
发明人： John R Cashman , Daniel R Ryan , Sigeng Chen
IPC分类号： A61L27/38 , A61L27/12 , C07D215/44 , C07D487/04 , A61K31/519 , A61K33/42 , A61K38/18 , A61K31/4706 , A61K31/12 , A61K45/06 , A61K35/28 , A61L27/28 , A61L27/32 , A61L27/42 , A61L27/54 , A61L27/58 , C07C49/248 , C07C49/255 , C07C225/22 , G01N33/50 , C07C229/40 , C12Q1/6883
摘要： Compositions of small molecules, matrices, and isolated cells including methods of preparation, and methods for differentiation, trans-differentiation, and proliferation of animal cells into the osteoblast cell lineage were described. Examples of osteogenic materials that were administered to cells or co-cultured with cells are represented by compounds of Formula II, IV, and VI independently or preferably in combination with a matrix to afford bone cells. Small molecule-stimulated cells were also combined with a matrix, placed with a cellular adhesive or material carrier and implanted to a site in an animal for bone repair. Matrix pretreated with compounds of Formula II, IV, and VI were also used to cause cells to migrate to the matrix that is of use for therapeutic purposes.

2. 发明授权

US10874766B2 Compounds and matrices for use in bone growth and repair 有权
公开(公告)号：US10874766B2
公开(公告)日：2020-12-29
申请号：US14776995
申请日：2014-03-17
申请人： HUMAN BIOMOLECULAR RESEARCH INSTITUTE
发明人： John R. Cashman , Daniel R. Ryan , Sigeng Chen
IPC分类号： C07C229/40 , C12Q1/6883 , A61L27/38 , A61L27/12 , C07D215/44 , C07D487/04 , A61K31/519 , A61K33/42 , A61K38/18 , A61K31/4706 , A61K31/12 , A61K45/06 , A61K35/28 , G01N33/50 , A61L27/28 , A61L27/32 , A61L27/42 , A61L27/54 , A61L27/58 , C07C49/248 , C07C49/255 , C07C225/22
CPC分类号： A61L27/3895 , A61K31/12 , A61K31/4706 , A61K31/519 , A61K33/42 , A61K35/28 , A61K38/18 , A61K45/06 , A61L27/12 , A61L27/28 , A61L27/32 , A61L27/3834 , A61L27/3847 , A61L27/425 , A61L27/54 , A61L27/58 , C07C49/248 , C07C49/255 , C07C225/22 , C07C229/40 , C07D215/44 , C07D487/04 , C12Q1/6883 , G01N33/502 , G01N33/5044 , A61L2300/112 , A61L2300/412 , A61L2300/606 , A61L2300/64 , A61L2400/18 , A61L2420/02 , A61L2420/06 , A61L2430/02 , A61L2430/40 , C12Q2600/136 , C12Q2600/158 , G01N2333/916 , A61K33/42 , A61K2300/00 , A61K31/4706 , A61K2300/00 , A61K31/519 , A61K2300/00 , A61K31/12 , A61K2300/00 , A61K35/28 , A61K2300/00 , A61K38/18 , A61K2300/00
摘要： Compositions of small molecules, matrices, and isolated cells including methods of preparation, and methods for differentiation, trans-differentiation, and proliferation of animal cells into the osteoblast blast cell lineage were described. Examples of osteogenic materials that were administered to cells or co-cultured with cells are represented by compounds of Formula II, IV, and VI independently or preferably in combination with a matrix to afford bone cells. Small molecule-stimulated cells were also combined with a matrix, placed with a cellular adhesive or material carrier and implanted to a site in an animal for bone repair. Matrix pretreated with compounds of Formula II, IV, and VI were also used to cause cells to migrate to the matrix that is of use for therapeutic purposes.

3. 发明授权

US08901341B2 Amino acid derivatives and absorbable polymers therefrom 有权
标题翻译：氨基酸衍生物和可吸收的聚合物
公开(公告)号：US08901341B2
公开(公告)日：2014-12-02
申请号：US13886611
申请日：2013-05-03
申请人： Bezwada Biomedical, LLC
发明人： Rao S. Bezwada
IPC分类号： C07C229/40 , A61K47/34 , C07C265/12 , C07C237/36 , C07C265/14 , C07C229/42 , A61L27/18 , A61L31/06 , A61L31/10 , A61L15/26 , A61L17/10 , A61L24/04 , C07C229/36 , C08G18/77 , C08G18/78 , C08G18/48 , C08G18/38
CPC分类号： C07C235/12 , A61K47/34 , A61L15/26 , A61L17/10 , A61L24/046 , A61L26/0019 , A61L27/18 , A61L31/06 , A61L31/10 , A61L2420/00 , C07C229/36 , C07C229/42 , C07C235/10 , C07C237/36 , C07C265/12 , C07C265/14 , C08G18/38 , C08G18/48 , C08G18/4837 , C08G18/6607 , C08G18/771 , C08G18/7812 , C08G2101/00 , Y10T428/139 , Y10T428/249921 , Y10T442/10 , C08L77/04
摘要： The present invention relates to the discovery of new class of hydrolysable amino acid derivatives and absorbable polyester amides, polyamides, polyepoxides, polyureas and polyurethanes prepared therefrom. The resultant absorbable polymers are useful for drug delivery, tissue engineering, tissue adhesives, adhesion prevention, bone wax formulations, medical device coatings, stents, stent coatings, highly porous foams, reticulated foams, wound care, cardiovascular applications, orthopedic devices, surface modifying agents and other implantable medical devices. In addition, these absorbable polymers should have a controlled degradation profile.
摘要翻译：本发明涉及从其制备的新类可水解氨基酸衍生物和可吸收聚酯酰胺，聚酰胺，聚环氧化物，聚脲和聚氨酯的发现。所得的可吸收聚合物可用于药物递送，组织工程，组织粘合剂，防粘连，骨蜡制剂，医疗器械涂层，支架，支架涂层，高度多孔泡沫，网状泡沫，伤口护理，心血管应用，矫形装置，表面修饰药剂和其他可植入医疗器械。此外，这些可吸收聚合物应具有受控的降解特征。

4. 发明申请

US20140350045A1 PHENOXYISOBUTYRIC ACID COMPOUNDS AND METHOD OF SYNTHESIS 审中-公开
标题翻译：酚氧化合物和合成方法
公开(公告)号：US20140350045A1
公开(公告)日：2014-11-27
申请号：US13940008
申请日：2013-07-11
申请人： IRAJ LALEZARI , JILL FABRICANT
发明人： IRAJ LALEZARI , JILL FABRICANT
IPC分类号： C07D307/87 , C07D215/14 , C07D215/52 , C07C235/72 , C07D215/50 , C07D219/04 , C07C275/42 , C07C229/40
CPC分类号： C07D307/87 , A61K8/411 , A61K8/42 , A61K8/4926 , A61Q19/08 , C07C215/76 , C07C229/40 , C07C233/75 , C07C235/72 , C07C235/74 , C07C275/34 , C07C275/42 , C07D215/12 , C07D215/14 , C07D215/50 , C07D215/52 , C07D219/04
摘要： The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).
摘要翻译：本发明提供了一种合成取代的苯氧基甲基丙酸和相关化合物的方法。该化合物可用于抑制AGEs（高级糖化终产物）的形成。

5. 发明申请

US20140039056A1 BROMFENAC ORGANIC SALTS AND PREPARATION METHOD, COMPOSITION AND USE THEREOF 审中-公开
标题翻译： BROMFENAC有机盐及其制备方法，组合物及其用途
公开(公告)号：US20140039056A1
公开(公告)日：2014-02-06
申请号：US13994587
申请日：2011-12-13
申请人： Jidong Liu , Yuchun Yang , Jiuliang Wang , Hai Tang
发明人： Jidong Liu , Yuchun Yang , Jiuliang Wang , Hai Tang
IPC分类号： C07C229/40 , C07C227/14 , C07C213/08 , C07C215/40
CPC分类号： C07C229/40 , A61K31/13 , A61K31/131 , A61K31/196 , C07C213/08 , C07C215/40 , C07C227/14
摘要： Provided are bromfenac organic salts and preparation method, composition and use thereof. The bromfenac organic salt has the structure as shown in the following Formula I, wherein A represents an organic base. Also provided are a method for the preparation of the bromfenac organic salt, a composition comprising the bromfenac organic salts, a use of the bromfenac organic salts or the composition thereof in manufacture of a medicament for treatment and/or prophylaxis of an inflammation or for analgesia, and a method for treatment and/or prophylaxis of an inflammation or for analgesia.
摘要翻译：提供溴芬酸有机盐及其制备方法，组合物和用途。溴芬酸有机盐具有如下式I所示的结构，其中A表示有机碱。还提供了制备溴芬酸有机盐的方法，包含溴芬酸有机盐的组合物，溴芬酸有机盐或其组合物在制备用于治疗和/或预防炎症或镇痛的药物中的用途，以及治疗和/或预防炎症或镇痛的方法。

6. 发明申请

US20130012735A1 SITAGLIPTIN INTERMEDIATE COMPOUNDS, PREPARATION METHODS AND USES THEREOF 有权
标题翻译： SITAGLIPTIN中间体化合物，其制备方法及其用途
公开(公告)号：US20130012735A1
公开(公告)日：2013-01-10
申请号：US13636486
申请日：2011-03-22
申请人： Hongjun Gao , Min Li
发明人： Hongjun Gao , Min Li
IPC分类号： C07C227/16 , C07C229/40 , C07C69/96
CPC分类号： C07C68/06 , C07C68/065 , C07C69/96 , C07C227/18 , C07C229/24 , C07C229/34 , C07C269/04 , C07D487/04 , Y02P20/55 , C07C271/22
摘要： Sitagliptin intermediate compounds of formula (f) and methods of preparation and use thereof are disclosed. Compounds of formula (f) are prepared by the following steps: compounds of formula (a) are subjected to electrophilic reaction with benzyl halides to form compounds of formula (b), which then react with compounds of formula (i) to form novel compounds of formula (e). Gignard agents formed from 2,4,5-trifluoro brmobenzene and magnesium metal react with compounds of formula (e) to afford compounds of formula (f), which are novel intermediates for the preparation of Sitagliptin intermediates of formula (g). Compounds of formula (f) are subjected to reduction by Pd/C, debenzylation, substitution of protecting group to form compounds of formula (g). Compounds of formula (a), (b), (i), (e), (f), and (g) have the following structures, in which R is protecting group of carboxyl and R2 is (substituted) hydrocarbyl.
摘要翻译：公开了式（f）的西格列汀中间体化合物及其制备和使用方法。通过以下步骤制备式（f）化合物：使式（a）化合物与苄基卤进行亲电子反应，形成式（b）化合物，然后与式（ⅰ）化合物反应形成新化合物的式（e）。由2,4,5-三氟Brmobenzene和镁金属形成的Gignard试剂与式（e）化合物反应，得到式（f）化合物，它们是制备式（g）的西他列汀中间体的新型中间体。式（f）的化合物通过Pd / C进行还原，脱苄基，保护基的取代形成式（g）的化合物。式（a），（b），（i），（e），（f）和（g）的化合物具有以下结构，其中R是保护基团的羧基，R 2是（取代的）烃基。

7. 发明申请

US20120114633A1 Inhibitors Of Bacterial Type III Secretion System 有权
标题翻译：细菌III型分泌系统的抑制剂
公开(公告)号：US20120114633A1
公开(公告)日：2012-05-10
申请号：US13263071
申请日：2010-04-06
申请人： Donald T. Moir , Daniel Aiello , Norton P. Peet , John D. Williams
发明人： Donald T. Moir , Daniel Aiello , Norton P. Peet , John D. Williams
IPC分类号： A61K31/5377 , C07D513/04 , C07D413/12 , C07D265/32 , C07C229/40 , C07C237/20 , C07D211/34 , A61K31/36 , A61K31/429 , A61K31/5375 , A61K31/216 , A61K31/167 , A61K31/4409 , A61K39/40 , A61P31/04 , A61P37/04 , A61K38/18 , C07D317/60
CPC分类号： A61K31/4245 , A61K31/16 , A61K31/167 , A61K31/216 , A61K31/34 , A61K31/36 , A61K31/381 , A61K31/407 , A61K31/4152 , A61K31/4184 , A61K31/427 , A61K31/429 , A61K31/496 , A61K31/5375 , A61K45/06 , Y02A50/406 , Y02A50/473 , Y02A50/475 , Y02A50/481
摘要： Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.
摘要翻译：公开了显示抑制由细菌III型分泌系统介导的效应物毒素分泌或易位的能力的有机化合物。所公开的III型分泌系统抑制剂化合物可用于抵抗革兰氏阴性菌如沙门氏菌属，志贺氏菌属，假单胞菌属，耶尔森氏菌属，肠致病性肠炎和肠毒素性大肠杆菌和衣原体属的感染。具有这种III型分泌系统。

8. 发明授权

US08071388B2 Compositions and methods for biodetection by nucleic acid-templated chemistry 失效
标题翻译：通过核酸模板化学生物检测的组合物和方法
公开(公告)号：US08071388B2
公开(公告)日：2011-12-06
申请号：US12391898
申请日：2009-02-24
申请人： Yumei Huang , James M. Coull
发明人： Yumei Huang , James M. Coull
IPC分类号： G01N33/68 , G01N33/00 , C07D209/04 , C07D207/46 , C07D209/56 , C07H21/04 , C07C229/40
CPC分类号： C07H21/04 , C07D209/08 , C07D209/14 , C07D209/56 , C07D209/58 , C09B23/0091 , C09B23/105 , G01N33/5308 , G01N33/533 , Y10T436/143333 , Y10T436/145555
摘要： The invention provides compositions and methods for the detection of biological targets, (e.g. nucleic acids and proteins) by nucleic acid-templated chemistry, for example, by generating fluorescent polymethine dyes.
摘要翻译：本发明提供了通过核酸模板化学，例如通过产生荧光聚甲炔染料来检测生物学靶标（例如核酸和蛋白质）的组合物和方法。

9. 发明申请

US20110130448A1 FUNCTIONALIZED PHENOLIC ESTERS AND AMIDES AND POLYMERS THEREFROM 有权
标题翻译：功能化的酚醛和乳酸和聚合物
公开(公告)号：US20110130448A1
公开(公告)日：2011-06-02
申请号：US12962195
申请日：2010-12-07
申请人： Rao S. Bezwada
发明人： Rao S. Bezwada
IPC分类号： A61K31/353 , C07C69/773 , C07C235/56 , C07C229/40 , C07C69/732 , C07D311/36 , A61K31/235 , A61K31/167 , A61K31/216 , A61P39/06 , A61P31/00 , A61P3/02 , A23L1/30 , A23L1/302
CPC分类号： A61K31/192 , A61K31/353 , A61K31/405 , C07C69/734 , C07C69/92
摘要： The present invention relates to a compound of the formula: R-AR—O—Y—R′ Wherein R represents one or more members selected from H, alkoxy, benzyloxy, aldehyde, halogen, carboxylic acid, —NO2, —NH2, —NHCOCH3, and —NH—Y—R′, which is attached directly to AR or attached through an aliphatic chain. The carboxylic acid moiety in R includes but is not limited to the following carboxylic acids: benzoic acids, cinnamic acids, ferulic acid, caffeic acid, syringic acid, salicyclic acid, vanillic acid, phenylacetic acids, phenylpropionic acids, and sinapinic acid. -AR—O— is a biologically active phenolic moiety comprising 1 to 6 substituted or unsubstituted aryl rings that are directly bonded to each other, fused together, or joined through a linking group. Y represents a member selected from: —COCH2O— (glycolic ester moiety) —COCH(CH3)O— (lactic ester moiety) —COCH2OCH2CH2O— (dioxanone ester moiety) —COCH2CH2CH2CH2CH2O— (caprolactone ester moiety) —CO(CH2)mO— where m is an integer between 2-4 and 6-24 inclusive —COCH2—O—(CH2CH2O)n— where n is an integer between 2 and 24, inclusive; and R′ is either hydrogen or a benzyl or an alkyl group, the alkyl group being either straight-chained or branched. The resultant functionalized phenolic compounds, used singly or in combinations, and their polymers have controllable degradation profiles, releasing the active component over a desired time range. The polymers are useful for biomaterials and biomedical devices, wherein said biologically active phenolic moiety is a residue of a phenolic compound.
摘要翻译：本发明涉及式R-AR-O-Y-R'的化合物，其中R代表一个或多个选自H，烷氧基，苄氧基，醛，卤素，羧酸，-NO 2，-NH 2， NHCOCH 3和-NH-Y-R'，其直接连接到AR或通过脂族链连接。 R中的羧酸部分包括但不限于以下羧酸：苯甲酸，肉桂酸，阿魏酸，咖啡酸，丁香酸，水杨酸，香草酸，苯乙酸，苯基丙酸和芥子酸。 -AR-O-是包含1至6个取代或未取代的芳环的生物活性酚部分，其直接键合，稠合在一起或通过连接基团连接。 Y表示选自-COCH 2 O-（乙醇酸酯部分）-COCH（CH 3）O-（乳酸酯部分）-COCH 2 OCH 2 CH 2 O-（二氧杂环己酮酯部分）-COCH 2 CH 2 CH 2 CH 2 CH 2 O-（己内酯部分）-CO（CH 2）m O- 其中m是2-4和6-24之间的整数，包括-COCH 2 -O-（CH 2 CH 2 O）n - ，其中n是2和24之间的整数，包括端值; 并且R'是氢或苄基或烷基，烷基是直链或支链的。所得到的单独或组合使用的官能化酚类化合物及其聚合物具有可控的降解特征，在期望的时间范围内释放活性组分。聚合物可用于生物材料和生物医学装置，其中所述生物活性酚部分是酚类化合物的残基。

10. 发明申请

US20110130438A1 ANILINE ANALOGS AS GLYCOGEN SYNTHASE ACTIVATORS 失效
标题翻译：苯胺类似物作为GLYCOGEN SYNTHASE激活剂
公开(公告)号：US20110130438A1
公开(公告)日：2011-06-02
申请号：US12908176
申请日：2010-10-20
申请人： David Robert Bolin , Matthew Michael Hamilton
发明人： David Robert Bolin , Matthew Michael Hamilton
IPC分类号： A61K31/40 , C07C229/40 , A61K31/195 , C07D207/08 , A61P3/00
CPC分类号： C07C233/25 , A61K31/095 , A61K31/194 , A61K31/195 , A61K31/401 , C07C233/47 , C07C233/60 , C07C311/08 , C07C311/09 , C07C2601/08 , C07D207/08 , C07D207/16
摘要： Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.
摘要翻译：本文提供式（I）的化合物及其药学上可接受的盐，其中取代基如说明书中公开的那些。这些化合物和含有它们的药物组合物可用于治疗代谢疾病和病症，例如II型糖尿病。

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