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1. 发明公开

US20230295088A1 INSULIN SENSITIZERS FOR THE TREATMENT OF DIABETES MELLITUS 审中-公开
公开(公告)号：US20230295088A1
公开(公告)日：2023-09-21
申请号：US18017826
申请日：2021-08-12
申请人： University of Iowa Research Foundation
发明人： Julien A. Sebag , Terry C. Yin , Robert J. Kerns
IPC分类号： C07D211/04 , G01N33/50 , A01K67/027 , C07C211/45 , A61P3/10
CPC分类号： C07D211/04 , G01N33/5008 , A01K67/0275 , C07C211/45 , A61P3/10 , G01N2333/62 , A01K2227/10 , A01K2267/0362
摘要： Compositions and methods for insulin sensitization are provided.

2. 发明授权

US10080746B2 Donepezil derivative and use thereof 有权
公开(公告)号：US10080746B2
公开(公告)日：2018-09-25
申请号：US15533865
申请日：2015-11-26
申请人： NORATECH PHARMACEUTICALS, INC.
发明人： Fei Liu , Cuixia Zhang , Chenggang Lin , Chunyan Zhou , Pan Chen , Wei Wang , Lulu Wang
IPC分类号： A61K31/445 , C07D211/04 , C07D211/22 , A61K31/045 , A61K47/44 , A61K31/235
CPC分类号： A61K31/445 , A61K9/0019 , A61K9/08 , A61K9/19 , A61K31/045 , A61K31/235 , A61K47/183 , A61K47/26 , A61K47/44 , C07D211/22 , A61K2300/00
摘要： The present invention relates to a donepezil derivative of general formula (I) or a pharmaceutically acceptable salt thereof, wherein R in the formula is as disclosed herein; and a method for preparation thereof; and a composition comprising an effective amount of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof. The present invention also relates to use of a compound of the general formula (I) or a pharmaceutically acceptable salt thereof in preparing a medicament for treating a disease resulted from an abnormality in acetylcholinesterase activity.

3. 发明授权

US09493402B2 Omega-aminoalkylamides of R-2-aryl-propionic acids as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells 有权
标题翻译： R-2-芳基 - 丙酸的ω-氨基烷基酰胺作为多形核和单核细胞趋化性的抑制剂
公开(公告)号：US09493402B2
公开(公告)日：2016-11-15
申请号：US13652199
申请日：2012-10-15
申请人： Dompé S.p.A.
发明人： Marcello Allegretti , Riccardo Bertini , Valerio Berdini , Cinzia Bizzarri , Maria Candida Cesta , Vito Di Cioccio , Gianfranco Caselli , Francesco Colotta , Carmelo Gandolfi
IPC分类号： A61K31/165 , A61K31/445 , A61K31/198 , C07D211/04 , C07D211/58 , C07D233/24 , C07D233/46 , C07D295/13 , C07D451/04 , C07C231/02 , C07C231/16 , C07C233/40 , C07C233/44 , C07C233/51 , C07C235/34 , C07C235/70 , C07C235/78 , C07C237/22 , C07C237/20 , C07C279/12 , C07C281/16 , A61K31/4453 , A61K31/5375
CPC分类号： C07C233/51 , A61K31/165 , A61K31/198 , A61K31/445 , A61K31/4453 , A61K31/5375 , C07B2200/07 , C07C231/02 , C07C231/16 , C07C233/40 , C07C233/44 , C07C235/34 , C07C235/70 , C07C235/78 , C07C237/20 , C07C237/22 , C07C279/12 , C07C281/16 , C07D211/04 , C07D211/58 , C07D233/24 , C07D233/46 , C07D295/13 , C07D451/04
摘要： (R)-2-Arylpropionamide compounds of formula (I), pharmaceutical preparations of the compounds and a process for making the compounds are described. The 2-Arylpropionamides of the invention are useful in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonuclear leukocytes and monocytes at inflammatory sites. In particular, the invention relates to the R enantiomers of omega-aminoalkylamides of 2-aryl propionic acids, of formula (I), for use as inhibitors of chemotaxis of neutrophils and monocytes induced by the C5a fraction of complement and by other chemotactic proteins whose biological activity is associated with activation of a 7-TD receptor. Selected compounds of formula (I) are dual inhibitors of both the C5a-induced chemotaxis of neutrophils and monocytes and the IL-8-induced chemotaxis of polymorphonuclear leukocytes.

4. 发明申请

US20150299187A1 ANTIMICROBIAL COMPOUNDS 有权
标题翻译：抗微生物化合物
公开(公告)号：US20150299187A1
公开(公告)日：2015-10-22
申请号：US14410538
申请日：2013-06-24
申请人： ISIS INNOVATION LIMITED
发明人： Mark MOLONEY , Yong-chu JEONG
IPC分类号： C07D471/04 , C07D409/06 , C07D211/04 , C07D403/06 , C07D405/06 , C07D417/06 , C07D207/444 , C07D401/06
CPC分类号： C07D471/04 , C07D207/44 , C07D207/444 , C07D211/04 , C07D213/69 , C07D401/06 , C07D403/06 , C07D405/06 , C07D409/06 , C07D417/06
摘要： The present invention relates to certain tetramic acid derivatives that are suitable for use in the preparation and development of antimicrobial (e.g. antibacterial or antifungal) compositions. The present invention also relates to the use of such compounds as antimicrobial (e.g. antibacterial or antifungal agents) and, in particular, as topical antibacterial or antifungal agents.
摘要翻译：本发明涉及适用于抗微生物（例如抗菌或抗真菌）组合物的制备和开发中的某些四聚酸衍生物。本发明还涉及这种化合物如抗微生物剂（例如抗细菌剂或抗真菌剂），特别是作为局部抗细菌剂或抗真菌剂的用途。

5. 发明授权

US09028976B2 Organic EL device 有权
标题翻译：有机EL器件
公开(公告)号：US09028976B2
公开(公告)日：2015-05-12
申请号：US13118273
申请日：2011-05-27
申请人： Akira Ebisawa , Hajime Amano , Sumiko Kitagawa , Tetsushi Inoue
发明人： Akira Ebisawa , Hajime Amano , Sumiko Kitagawa , Tetsushi Inoue
IPC分类号： H01L51/50 , C07C13/70 , C07C211/54 , C07D209/86 , C07D211/04 , C09K11/00 , C07C13/62 , C07D213/06
CPC分类号： C07D209/86 , C07C13/62 , C07C211/54 , C07C2603/24 , C07C2603/52 , C07D213/06 , C09K11/00 , H01L51/50 , H01L51/5012 , Y10S428/917
摘要： A highly stable organic EL material having the properties of both benzofluoranthene and anthracene structures is provided. The organic EL device has at least one organic compound layer containing a compound presented by the general formula (I) below: (in which L is a linking group linking any one of the positions 1 to 12 and any one of the positions 13 to 22; the unlinked positions 1 to 22 are substituted by any of a hydrogen atom, substituted or unsubstituted aryl group, substituted or unsubstituted heterocyclic group, substituted or unsubstituted alkyl group, and aromatic amino group; and L presents any of a single bond, substituted or unsubstituted arylene group, substituted or unsubstituted heterocyclic group, and substituted or unsubstituted alkylene group).
摘要翻译：提供了具有苯并荧蒽和蒽结构两者性质的高度稳定的有机EL材料。有机EL元件具有至少一种含有下述通式（I）表示的化合物的有机化合物层：（其中L是连接位置1至12和任一位置13至22中的任何一个的连接基团取代或未取代的芳基，取代或未取代的杂环基，取代或未取代的烷基和芳香族氨基中的任一个取代或未取代的芳基，L表示任意的单键，取代或未取代的芳基，未取代的亚芳基，取代或未取代的杂环基，取代或未取代的亚烷基）。

6. 发明授权

US08802866B2 Pyridinylimidazolone derivatives for the inhibition of PI3 kinases 有权
标题翻译：用于抑制PI3激酶的吡啶基咪唑啉酮衍生物
公开(公告)号：US08802866B2
公开(公告)日：2014-08-12
申请号：US13498366
申请日：2010-09-06
申请人： Ulrich Emde , Hans Peter Buchstaller , Markus Klein , Christina Esdar , Joerg Bomke
发明人： Ulrich Emde , Hans Peter Buchstaller , Markus Klein , Christina Esdar , Joerg Bomke
IPC分类号： C07D211/04
CPC分类号： C07D401/14 , A61K31/4178 , A61K31/44 , C07D401/04 , C07D409/14 , C07D471/04
摘要： Compounds of the formula (I), in which X1, X2, L, Y, R2, R3, R4, R5, R6, R7, R8, R9, R10 have the meanings indicated in claim 1, are PI3K inhibitors and can be employed, inter alia, for the treatment of autoimmune diseases, inflammation, cardiovascular diseases, neurodegenerative diseases and tumors.
摘要翻译：其中X 1，X 2，L，Y，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 9，R 10具有权利要求1所示含义的式（I）化合物是PI3K抑制剂，尤其用于治疗自身免疫疾病，炎症，心血管疾病，神经变性疾病和肿瘤。

7. 发明申请

US20080221166A1 AMINOAMIDES AS OREXIN ANTAGONISTS 失效
标题翻译： AMINOAMIDES作为OREXIN ANTAGONISTS
公开(公告)号：US20080221166A1
公开(公告)日：2008-09-11
申请号：US12037975
申请日：2008-02-27
申请人： Luca Gobbi , Henner Knust , Parichehr Malherbe , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
发明人： Luca Gobbi , Henner Knust , Parichehr Malherbe , Matthias Nettekoven , Emmanuel Pinard , Olivier Roche , Mark Rogers-Evans
IPC分类号： A61K31/4427 , C07C233/00 , A61K31/165 , C07D211/04 , A61K31/44
CPC分类号： C07D213/36 , A61K9/2018 , A61K9/4858 , C07C237/20 , C07C2601/02 , C07C2601/04
摘要： The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.
摘要翻译：本发明涉及式I化合物，其中Ar 1，Ar 2，Ar 3，n和R 1，其中R 8和R 8如本文所定义，并且与药学上合适的酸加成盐，光学纯对映异构体，外消旋物或非对映体混合物。这些化合物是食欲肽受体拮抗剂，并且可用于治疗涉及食欲素途径的疾病，例如睡眠障碍。

8. 发明申请

US20080194829A1 Process for catalytically preparing aromatic or heteroaromatic nitriles 有权
标题翻译：用于催化制备芳族或杂芳族腈的方法
公开(公告)号：US20080194829A1
公开(公告)日：2008-08-14
申请号：US11986398
申请日：2007-11-21
申请人： Nikolaus Muller , Wolfgang Magerlein , Alain Cotte , Matthias Beller , Thomas Schareina , Alexander Zapf
发明人： Nikolaus Muller , Wolfgang Magerlein , Alain Cotte , Matthias Beller , Thomas Schareina , Alexander Zapf
IPC分类号： C07D211/04 , C07C255/49
CPC分类号： C07B37/04 , C07C1/26 , C07C17/10 , C07C2529/40 , C07D213/61 , C07C9/00 , C07C19/075
摘要： A process is described for catalytically preparing optionally substituted aromatic or heteroaromatic nitrites of the general formula (I) Ar—CN (I) by reacting the corresponding aryl halides of the general formula (II) Ar—X (II) in which X is chlorine, bromine, iodine, triflate, nonaflate, mesylate or tosylate and Ar is an optionally substituted aromatic or heteroaromatic radical, characterized in that the reaction is performed in the presence of a palladium compound, a phosphine of the general formula (III) or (IV) where R is an alkyl radical and R′, R″ and R′″ are each an alkyl radical or an aryl radical or heteroaryl radical and A is an alkylene or arylene radical, and potassium hexacyanoferrate(II) or potassium hexacyanoferrate(III), optionally in a solvent and optionally with addition of a base.
摘要翻译：描述了用于催化制备通式（I）的任选取代的芳香族或杂芳族亚硝酸盐的方法，该方法包括通式（I）的化合物。通过使通式（II）的相应的芳基卤反应<？in-line-formula description =“In-Line Formulas”end =“in-line-formula description =”In-line Formulas“end =”tail“ “铅”→Ar-X（II）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中X为氯，溴，碘，三氟甲磺酸酯，壬酸酯，甲磺酸酯或甲苯磺酸酯并且Ar是任选取代的芳族或杂芳族基团，其特征在于反应在钯化合物，通式（III）或（IV）的膦的存在下进行，其中R是烷基，R'，R “和”R“分别是烷基或芳基或杂芳基，A是亚烷基或亚芳基，六氰基铁酸钾（II）或六氰基铁酸钾（III），选择性在溶剂中并任选加入碱。

9. 发明申请

US20080146813A1 Facile synthesis of a series of liquid crystalline 2-(4'-alkylphenyl)-5-cyanopyridines 有权
标题翻译：一系列液晶2-（4'-烷基苯基）-5-氰基吡啶的简便合成
公开(公告)号：US20080146813A1
公开(公告)日：2008-06-19
申请号：US11609910
申请日：2006-12-13
申请人： Win-Long Chia , Ru-Sung Lu
发明人： Win-Long Chia , Ru-Sung Lu
IPC分类号： C07D211/04
CPC分类号： C07D213/85
摘要： The invention relates to a facile synthesis of a series of 2-(4′-alkylphenyl)-5-cyanopyridine liquid crystal compounds which are represented by the following formula (I): wherein Cn is a linear alkyl having 1-12 carbon atoms. The synthesis of the liquid crystalline 2-(4′-alkylphenyl)-5-cyanopyridine is completed in a two-step reaction. First, a Grignard reagent (such as 4-alkylphenylmagnesium bromide) is added to a 3-cyanopyridinium salt (such as N-phenyloxycarbonyl-3-cyanopyridinium chloride) to get a 1,2-dihydropyridine. Then the 1,2-dihydropyridine is oxidized with o-chloronil to obtain the 2-(4′-alkylphenyl)-5-cyanopyridine.
摘要翻译：本发明涉及由下式（I）表示的一系列2-（4'-烷基苯基）-5-氰基吡啶液晶化合物的容易合成：其中C n是直链具有1-12个碳原子的烷基。液晶2-（4'-烷基苯基）-5-氰基吡啶的合成在两步反应中完成。首先，向3-氰基吡啶鎓盐（如N-苯氧基羰基-3-氰基吡啶鎓氯化物）中加入格氏试剂（如4-烷基苯基溴化镁），得到1,2-二氢吡啶。然后用邻氯醌氧化1,2-二氢吡啶，得到2-（4'-烷基苯基）-5-氰基吡啶。

10. 发明申请

US20080118405A1 Bifunctional Chemical, Preparation and Use for Detecting Nucleic Acid 有权
标题翻译：双功能化学，检测核酸的制备和应用
公开(公告)号：US20080118405A1
公开(公告)日：2008-05-22
申请号：US11875755
申请日：2007-10-19
申请人： Sabrina Conoci , Salvatore Sortino
发明人： Sabrina Conoci , Salvatore Sortino
IPC分类号： B01J19/00 , C07D211/04
CPC分类号： C07D213/30
摘要： A bifunctional compound comprising a molecular unit (I) intercalating between nucleobases (B) of nucleic acids, an active molecular unit (AD) capable of emitting a detectable signal, and optionally a spacer unit, in which the active molecular unit (AD) is selected from amongst chemical entities having a structure such as to interact electronically with the intercalating molecular unit (I) in such a way that, during the reaction of oxidation, the reduction-oxidation potential (EI+/I) of the semicouple I+/I defined by the intercalating molecular unit (I) is lower than the reduction-oxidation potential (EB+/B) of the semicouple B+/B defined by the nucleobases (B), and in such a way that, during the reaction of reduction, the reduction-oxidation potential (EI/I−) of the semicouple I/I− defined by the intercalating molecular unit (I) is higher than the reduction-oxidation potential (EB/B−) of the semicouple B/B− defined by the nucleobases (B). Moreover the use of the compound for detecting nucleic acids, a process for its synthesis, and a system comprising the same are described.
摘要翻译：包含嵌入核酸碱基（B）之间的分子单元（I），能够发射可检测信号的活性分子单元（AD）和任选的间隔单元的双功能化合物，其中活性分子单元（AD）为选自具有如下结构的化学实体，其结构使得与插层分子单元（I）以电子方式相互作用，使得在氧化反应期间，所述半导体I + / I的还原氧化电位（EI + / I）被定义插层分子单元（I）的含量低于由核碱基（B）定义的半组分B + / B的还原 - 氧化电位（EB + / B），并且在还原反应期间还原由插入分子单元（I）定义的半配偶I / I的氧化电位（EI / I）高于由核碱基限定的半组分B / B-的还原 - 氧化电位（EB / B-）（B）。此外，描述了化合物用于检测核酸的用途，其合成方法和包含其的体系。

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