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1. 发明申请

US20180265460A1 METHOD OF FORMING PARACYCLOPHANE CONTAINING FUNCTIONAL GROUND WITH DISULFIDE BOND 审中-公开
公开(公告)号：US20180265460A1
公开(公告)日：2018-09-20
申请号：US15913940
申请日：2018-03-07
申请人： MAY-HWA ENTERPRISE CORPORATION
发明人： Hsien-Yeh Chen , Zhen-Yu Guan , Chih-Yu Wu
IPC分类号： C07C319/22 , C07C45/30 , C07C17/16 , C07C29/14 , C07C209/08 , C07C45/45 , C09D165/04 , C07C323/60 , C07C211/31 , C07C22/04 , C07C33/34 , C07C47/546
CPC分类号： C07C319/22 , C07C17/16 , C07C22/04 , C07C29/14 , C07C45/30 , C07C45/45 , C07C209/08 , C07C2603/92 , C08G2261/1426 , C08G2261/1432 , C08G2261/145 , C08G2261/3424 , C09D165/04 , C07C323/60 , C07C211/31 , C07C33/34 , C07C47/546
摘要： The present invention provides a method of forming paracyclyophane containing disulfide functional group. The paracyclophane is prepared by adding 3,3′-dithiodipropionic acid (DPDPA) and N-ethyl-N′-(3-(dimethylamino)propyl)carbodiimide (EDC) into 4-aminomethyl [2,2] paracyclophane. The present invention further provides a chemical film and a method of forming the same. The chemical film contains poly-p-xylylene with disulfide functional group and is formed on a substrate by a chemical vapor deposition process.

2. 发明授权

US09981977B2 Asymmetric electrophilic fluorination using an anionic chiral phase-transfer catalyst 有权
公开(公告)号：US09981977B2
公开(公告)日：2018-05-29
申请号：US14368105
申请日：2012-12-26
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Vivek Rauniyar , Aaron D. Lackner , Gregory L. Hamilton , F. Dean Toste , Robert J. Phipps , Hunter Shunatona , Natalja Frueh , Yiming Wang , Jeffrey Wu , Jigar Patel , Takashi Honjo
IPC分类号： C07D487/08 , C07F9/6574 , C07D215/20 , C07D217/22 , C07D221/10 , C07C231/12 , C07D263/10 , C07D263/52 , C07D265/16 , C07D491/052 , C07D498/10 , C07D209/76 , C07B53/00 , C07C45/30 , B01J31/02 , C07C45/29 , C07F9/09
CPC分类号： C07D487/08 , B01J31/0285 , B01J2231/4288 , B01J2231/48 , C07B53/00 , C07B2200/07 , C07C45/29 , C07C45/30 , C07C231/12 , C07C2601/04 , C07C2601/14 , C07C2601/16 , C07C2602/10 , C07C2602/24 , C07C2602/28 , C07C2603/72 , C07D209/76 , C07D215/20 , C07D217/22 , C07D221/10 , C07D263/10 , C07D263/52 , C07D265/16 , C07D491/052 , C07D498/10 , C07F9/09 , C07F9/65744 , C07C233/73 , C07C49/693 , C07C49/687 , C07C49/753 , C07C49/457
摘要： The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.

3. 发明申请

US20170313643A1 PROCESS FOR THE PREPARATION OF TREPROSTINIL 审中-公开
公开(公告)号：US20170313643A1
公开(公告)日：2017-11-02
申请号：US15518096
申请日：2015-09-28
申请人： CHINOIN GYÓGYSZER ÉS VEGYÉSZETI TERMÉKEK GYÁRA ZRT.
发明人： Imre JUHÁSZ , Irén HORTOBÁGYI , Tamás ALTSACH , István LÁSZLÓFI , Ágnes NAGYNÉ BORKÓ , Imre ROZSUMBERSZKI , Gábor HAVASI , Zsuzsanna KARDOS , Péter BUZDER-LANTOS
IPC分类号： C07C51/347 , C07C35/37 , C07C13/547 , C07C59/72 , C07C51/41 , C07C2603/14
CPC分类号： C07C51/347 , C07C13/547 , C07C35/37 , C07C41/26 , C07C41/30 , C07C41/48 , C07C43/315 , C07C45/30 , C07C45/305 , C07C45/65 , C07C51/09 , C07C51/412 , C07C59/72 , C07C67/14 , C07C67/29 , C07C67/293 , C07C69/76 , C07C2603/14 , C07C49/84 , C07C49/755 , C07C59/70
摘要： The invention provides a new process for the preparation of treprostinil of formula (I) and its salts using several new intermediates during the building of the ring system.

4. 发明授权

US09604911B2 Process for the synthesis of agomelatine 有权
公开(公告)号：US09604911B2
公开(公告)日：2017-03-28
申请号：US15100782
申请日：2014-12-04
申请人： LES LABORATOIRES SERVIER
发明人： Jean-François Briere , Raphaël Lebeuf , Vincent Levacher , Christophe Hardouin , Jean-Pierre Lecouve
IPC分类号： C07C231/12 , C07C303/28 , C07C309/66 , C07C309/73 , C07C231/06
CPC分类号： C07C231/12 , C07C41/16 , C07C41/18 , C07C41/26 , C07C41/32 , C07C43/23 , C07C45/30 , C07C213/02 , C07C217/58 , C07C217/60 , C07C231/02 , C07C231/06 , C07C231/065 , C07C231/10 , C07C235/34 , C07C253/30 , C07C303/28 , C07C303/30 , C07C309/65 , C07C309/66 , C07C309/73 , C07D307/92 , C07C255/37 , C07C233/18 , C07C43/215 , C07C47/277
摘要： Process for the industrial synthesis of the compound of formula (I):

5. 发明授权

US09169190B2 Methods for making retinoids and uses thereof 有权
标题翻译：维生素A的制备方法及用途
公开(公告)号：US09169190B2
公开(公告)日：2015-10-27
申请号：US13856631
申请日：2013-04-04
申请人： The UAB Research Foundation
发明人： Wayne J. Brouillette , Donald D. Muccio , Venkatram Reddy Atigadda , John M. Ruppert , Susan M. Lobo Ruppert
IPC分类号： C07C205/00 , C07C229/00 , C07C59/40 , C07C63/333 , C07C61/00 , A61K31/20 , A61K31/195 , C07C57/50 , C07C29/14 , C07C45/29 , C07C45/30 , C07C45/51 , C07C45/61 , C07C45/67 , C07C45/68 , C07C47/238 , C07C49/403 , C07C49/417 , C07C49/603 , C07C49/683 , C07C49/713 , C07C49/753 , C07C51/09 , C07C67/343 , C07C403/08 , C07C403/14 , C07C403/20 , C07D311/96 , C12C11/02 , C07C57/26
CPC分类号： A61K31/202 , A61K9/0014 , A61K45/06 , C07B2200/09 , C07C29/14 , C07C45/29 , C07C45/292 , C07C45/30 , C07C45/513 , C07C45/61 , C07C45/673 , C07C45/68 , C07C47/238 , C07C49/403 , C07C49/417 , C07C49/603 , C07C49/683 , C07C49/713 , C07C49/753 , C07C51/09 , C07C57/26 , C07C57/50 , C07C67/343 , C07C403/08 , C07C403/14 , C07C403/20 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/10 , C07C2602/28 , C07D311/96 , C12C11/02 , C07C33/16 , C07C69/618
摘要： Described herein are methods for making retinoids. Also described herein are retinoids and methods of use thereof.
摘要翻译：本文描述了制备类视黄醇的方法。本文还描述了类视黄醇及其使用方法。

6. 发明授权

US09000050B2 SHIP1 modulators and related methods 有权
标题翻译： SHIP1调制器及相关方法
公开(公告)号：US09000050B2
公开(公告)日：2015-04-07
申请号：US13817106
申请日：2011-08-22
申请人： Xiaoxia Wang , Labros George Meimetis , Matthew Bruce Nodwell , Raymond Andersen
发明人： Xiaoxia Wang , Labros George Meimetis , Matthew Bruce Nodwell , Raymond Andersen
IPC分类号： A61K31/045 , A61K31/015 , C07C43/23 , C07C215/44 , C07C251/44 , C07D223/32 , C07C69/65 , C07C39/17 , C07C49/747 , C07C49/753 , C07C37/50 , C07C41/18 , C07C45/30 , C07C45/65 , C07C67/08 , C07C69/734 , C07C213/02 , C07C215/64 , C07C249/08
CPC分类号： C07C43/23 , A61K31/045 , C07B2200/07 , C07C37/50 , C07C39/17 , C07C41/18 , C07C45/30 , C07C45/65 , C07C49/747 , C07C49/753 , C07C67/08 , C07C69/65 , C07C69/734 , C07C213/02 , C07C215/44 , C07C215/64 , C07C249/08 , C07C251/44 , C07C2603/40 , C07D223/32
摘要： Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R1, R2 and A are as defined herein are disclosed. Such compounds have enhanced water solubility and have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Enantioselective methods for preparation of compounds of structure (I), compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluents and methods of SHIP1 modulation by administration of such compounds to an animal in need thereof are also disclosed.
摘要翻译：结构（I）的化合物：包括立体异构体及其药学上可接受的盐，其中R1，R2和A如本文所定义。这些化合物具有增强的水溶性并且具有作为SHIP1调节剂的活性，因此可用于治疗将受益于SHIP1调节的各种疾病，病症或病症中的任何一种。还公开了用于制备结构（I）化合物的对映选择性方法，包含结构（I）化合物与药学上可接受的载体或稀释剂的组合物的组合物以及通过将这些化合物施用于有需要的动物的SHIP1调节方法。

7. 发明申请

US20140357900A1 PREPARATION METHOD OF LYCOPENE INTERMEDIATE 3-METHYL-4,4-DIALKOXY-1-BUTALDEHYDE 审中-公开
标题翻译：中间体3-甲基-4,4-二甲氧基-1-苯甲醛的制备方法
公开(公告)号：US20140357900A1
公开(公告)日：2014-12-04
申请号：US14369137
申请日：2012-12-10
申请人： NANJING UNIVERSITY OF TECHNOLOGY , ZHEJIANG MEDICINE CO., LTD. XINCHANG PHARMACEUTICAL FACTORY
发明人： Chunlei Lv , Shiqing Pl , Jianhui Chen , Dingqiang Lu , Pingkai Ouyang
IPC分类号： C07C45/30 , C07C41/22
CPC分类号： C07C45/30 , C07C41/22 , C07C45/00 , C07C45/516 , C07C47/198
摘要： Disclosed is a preparation method of the lycopene intermediate 3-methyl-4,4-dialkoxy-1-butaldehyde. The preparation method comprises the following steps: (1) reacting 2-methyl-3,3-dialkoxy-1-halopropane with magnesium powder in the solvent of anhydrous tetrahydrofuran at a temperature of 45˜65° C. to generate a mixture of Grignard reagents under the protection of an inert gas; and (2) adding N,N-disubstituted carboxamide to the mixture of Grignard reagents and reacting at a temperature of 10° C.˜35° C. to obtain 3-methyl-4,4-dialkoxy-1-butaldehyde. The process route of the present invention is simple and direct, the operation is easy, the conditions are mild and the yield is good, and thus the invention has commercial value.
摘要翻译：公开了番茄红素中间体3-甲基-4,4-二烷氧基-1-丁醛的制备方法。制备方法包括以下步骤：（1）在45〜65℃的温度下，将2-甲基-3,3-二烷氧基-1-卤代丙烷与镁粉末在无水四氢呋喃的溶剂中反应，生成格利雅在惰性气体保护下的试剂; 和（2）将N，N-二取代的甲酰胺加入到格氏试剂混合物中，并在10℃〜35℃的温度下反应，得到3-甲基-4,4-二烷氧基-1-丁醛。本发明的工艺路线简单直接，操作容易，条件温和，产量好，因此本发明具有商业价值。

8. 发明申请

US20140350253A1 ASYMMETRIC ELECTROPHILIC FLUORINATION USING AN ANIONIC CHIRAL PHASE-TRANSFER CATALYST 有权
标题翻译：使用阴离子型相转移催化剂的不对称电泳荧光
公开(公告)号：US20140350253A1
公开(公告)日：2014-11-27
申请号：US14368105
申请日：2012-12-26
申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
发明人： Vivek Rauniyar , Aaron D. Lackner , Gregory L. Hamilton , F. Dean Toste , Robert J. Phipps , Hunter Shunatona , Natalja Frueh , Yiming Wang , Jeffrey Wu , Jigar Patel , Takashi Honjo
IPC分类号： C07D487/08 , C07C45/29 , C07D498/10 , C07D263/52 , B01J31/02 , C07F9/09
CPC分类号： C07D487/08 , B01J31/0285 , B01J2231/4288 , B01J2231/48 , C07B53/00 , C07B2200/07 , C07C45/29 , C07C45/30 , C07C231/12 , C07C2601/04 , C07C2601/14 , C07C2601/16 , C07C2602/10 , C07C2602/24 , C07C2602/28 , C07C2603/72 , C07D209/76 , C07D215/20 , C07D217/22 , C07D221/10 , C07D263/10 , C07D263/52 , C07D265/16 , C07D491/052 , C07D498/10 , C07F9/09 , C07F9/65744 , C07C233/73 , C07C49/693 , C07C49/687 , C07C49/753 , C07C49/457
摘要： The discovery of distinct modes of asymmetric catalysis has the potential to rapidly advance chemists' ability to build enantioenriched molecules. As an example, the use of chiral cation salts as phase-transfer catalysts for anionic reagents has enabled a vast set of enantioselective transformations. A largely overlooked analogous mechanism wherein a chiral anionic catalyst brings a cationic species into solution is itself a powerful method. The concept is broadly applicable to a number of different reaction pathways, including to the enantioselective fluorocyclization of olefins, and dearomatization of aromatic systems with a cationic electrophile-transferring (e.g., fluorinating) agent and a chiral phosphate catalyst. The reactions proceed in high yield and stereoselectivity. The compounds and methods of the invention are of particular value, especially considering the scarcity of alternative approaches.
摘要翻译：发现不同模式的不对称催化有可能迅速提高化学家建立对映体的分子的能力。作为例子，使用手性阳离子盐作为阴离子试剂的相转移催化剂使得能够进行大量的对映选择性转化。主要被忽略的类似机理，其中手性阴离子催化剂将阳离子物质引入溶液本身是强有力的方法。该概念广泛地适用于许多不同的反应途径，包括烯烃的对映选择性氟环化，以及芳族体系与阳离子亲电试剂转移（例如氟化）试剂和手性磷酸酯催化剂的脱芳构化。反应以高产率和立体选择性进行。本发明的化合物和方法特别有价值，特别考虑到替代方法的稀缺性。

9. 发明申请

US20130317106A1 METHODS FOR MAKING RETINOIDS AND USES THEREOF 有权
标题翻译：制备反应物的方法及其用途
公开(公告)号：US20130317106A1
公开(公告)日：2013-11-28
申请号：US13856631
申请日：2013-04-04
申请人： The UAB Research Foundation
发明人： Wayne J. Brouillette , Donald D. Muccio , Venkatram Reddy Atigadda , John M. Ruppert , Susan M. Lobo Ruppert
IPC分类号： C07C57/50 , C07C57/26
CPC分类号： A61K31/202 , A61K9/0014 , A61K45/06 , C07B2200/09 , C07C29/14 , C07C45/29 , C07C45/292 , C07C45/30 , C07C45/513 , C07C45/61 , C07C45/673 , C07C45/68 , C07C47/238 , C07C49/403 , C07C49/417 , C07C49/603 , C07C49/683 , C07C49/713 , C07C49/753 , C07C51/09 , C07C57/26 , C07C57/50 , C07C67/343 , C07C403/08 , C07C403/14 , C07C403/20 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2602/10 , C07C2602/28 , C07D311/96 , C12C11/02 , C07C33/16 , C07C69/618
摘要： Described herein are methods for making retinoids. Also described herein are retinoids and methods of use thereof.
摘要翻译：本文描述了制备类视黄醇的方法。本文还描述了类视黄醇及其使用方法。

10. 发明授权

US08507562B2 Synthesis of (1)-beta-elemene, (-)-beta-elemenal, (-)-beta-elemenol, (-)-beta-elemene fluoride and their analogues, intermediates, and composition and uses thereof 有权
标题翻译：（ - ） - β-榄香烯，（ - ） - β-榄香烯，（ - ） - β-榄香烯氟化物及其类似物，中间体及其组成和用途的合成
公开(公告)号：US08507562B2
公开(公告)日：2013-08-13
申请号：US11649558
申请日：2007-01-04
申请人： Lan Huang
发明人： Lan Huang
IPC分类号： A61K31/11 , A61K31/045 , A61K31/025 , A61K31/015
CPC分类号： C07F9/65848 , C07C1/324 , C07C13/19 , C07C17/16 , C07C33/14 , C07C35/18 , C07C45/298 , C07C45/30 , C07C47/21 , C07C49/557 , C07C49/647 , C07C2601/14 , C07C2601/16 , C07C22/00 , C07C47/225
摘要： The present invention provides convergent processes for preparing (−)-beta-elemene, (−)-beta-elemenal, (−)-beta-elemenol, and (−)-beta-elemene fluoride and analogues thereof. Also provided are intermediates useful for preparing (−)-beta-elemene. The present invention further provides novel compositions based on analogues of (−)-beta-elemene, (−)-beta-elemenal, (−)-beta-elemenol, (−)-beta-elemene fluoride and methods for the treatment of cancer, such as brain tumor, lung cancer, breast cancer, prostate cancer, ovarian cancer, colorectal cancer, gastric intestional cancer, and stomach cancer.The inventors propose a combination therapy using 1) one or more of the following anti-cancer agents: including, but not limited to, Cisplatin, 5-FU, Taxol, Taxol derivatives, and any anti-cancer agent, and 2) one or more of the following (−)-beta-elemene and its analogs, including (−)-beta-elemene, (−)-beta-elemenal, (−)-beta-elemenol, (−)-beta-elemene fluoride, and their analogs, and (−)-beta-elemene's intermediate in its chemical synthesis, for the treatment of cancer, especially for the treatment of brain tumor, lung cancer, ovarian cancer, bladder cancer, cervical cancer, colon cancer, breast cancer, and prostate cancer.
摘要翻译：本发明提供（ - ） - β-榄香烯，（ - ） - β-元素，（ - ） - β-榄香烯和（ - ） - β-榄香烯氟化物及其类似物的收敛方法。还提供了可用于制备（ - ） - β-榄香烯的中间体。本发明还提供了基于（ - ） - β-榄香烯，（ - ） - β-元素，（ - ） - β-榄香烯，（ - ） - β-榄香烯氟化物类似物和治疗癌症的新方法，如脑肿瘤，肺癌，乳腺癌，前列腺癌，卵巢癌，结肠直肠癌，胃肠癌和胃癌。本发明人提出了使用以下1种或多种抗癌药物的组合疗法：包括但不限于顺铂，5-FU，紫杉醇，紫杉醇衍生物和任何抗癌剂，以及2）一种或多种（ - ） - β-榄香烯及其类似物，包括（ - ） - β-榄香烯，（ - ） - β-元素，（ - ） - β-榄香烯，（ - ） - 他们的类似物和（ - ） - β-榄香烯在其化学合成中的中间体，用于治疗癌症，特别是用于治疗脑肿瘤，肺癌，卵巢癌，膀胱癌，子宫颈癌，结肠癌，乳腺癌和前列腺癌。

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