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    • 2. 发明申请
    • AN IMPROVED PROCESS FOR THE PREPARATION OF ATORVASTATIN AND INTERMEDIATES
    • 改进ATORVASTATIN和中间体的制备方法
    • WO2006089401A1
    • 2006-08-31
    • PCT/CA2006/000243
    • 2006-02-21
    • APOTEX PHARMACHEM INC.WANG, FanCHE, DaqingGUNTOORI, Bhaskar ReddyZHAO, YajunKINSMAN, Aaron, C.FAUGHT, JodyCHOW, Alan
    • WANG, FanCHE, DaqingGUNTOORI, Bhaskar ReddyZHAO, YajunKINSMAN, Aaron, C.FAUGHT, JodyCHOW, Alan
    • C07D207/34
    • C07D207/34
    • A process is provided for preparing (R)-5-[2-(4-fluorophenyl)-5-(l- methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo- 1-heptanoic acid, R-substituted ester 9 comprising: (a) reacting 5-(4-fluorophenyl)-2-(l -methylethyl)-l -(3-oxopropyl)-N,4- diphenyl-lH-pyrrole-3-carboxamide, 1, with the enolate form of (S)-2- hydroxy- 1 ,2,2-triphenylethyl acetate substituent in a chelating co- solvent; (b) hydrolysis of (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3-hydroxy- 1 -pentanoic acid, (S)-2 -hydroxy- 1 ,2,2-triphenylethyl ester (2a and 2b) using a base, preferably an alkali metal base, preferably in a solvent to form the (R,S)-5-[2-(4-fluorophenyl)-5-(l -methylethyl)-3-phenyl-4- [(phenylamino)carbonyl]- 1 H-pyrrol- 1 -yl]-3 -hydroxy- 1 -pentanoic acid, 7; (c) treating the carboxylic acid 7 with a chiral base to form a salt and purifying the salt to obtain enantiomerically enriched (R)-7 chiral base salt; (d) alkylation of the (R)-7 chiral base salt or the free acid derived from (R)-7, forming (R)-5-[2-(4-fluorophenyl)-5-(l-methylethyl)-3-phenyl- 4-[(phenylamino)carbonyl]-lH-pyrrol-l-yl]-5-hydroxy-3-oxo-l- heptanoic acid, R-substituted ester 9, wherein the R substituent is a Cl to C6 alkyl, C6 to C9 aryl or C7 to Cl0 aralkyl. Subsequently, R-substituted ester 9 may be converted into atorvastatin calcium 6 based on procedures known in the art.
    • 提供了制备(R)-5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸,R-取代的酯9,其包含:(a)使5-(4-氟苯基)-2-(1-甲基乙基)-1-(3-氧代丙基)-N ,4-二苯基-1H-吡咯-3-甲酰胺,1,在螯合助溶剂中具有(S)-2-羟基-1,2-二苯基乙基乙酸酯取代基的烯醇化物形式; (b)(R,S)-5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基 吡啶-3-基] -3-羟基-1-戊酸,(S)-2-羟基-1,2-二苯基乙酯(2a和2b),使用碱,优选碱金属碱,优选在溶剂中形成 (R,S)-5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基] 羟基-1-戊酸,7; (c)用手性碱处理羧酸7以形成盐并纯化该盐以获得对映体富集的(R)-7手性碱盐; (d)(R)-7手性碱盐或衍生自(R)-7的游离酸的烷基化,形成(R)-5- [2-(4-氟苯基)-5-(1-甲基乙基) 3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基] -5-羟基-3-氧代-1-庚酸R-取代的酯9,其中R取代基是C1至C6 烷基,C 6至C 9芳基或C 7至C 10芳烷基。 随后,基于本领域已知的方法,R取代的酯9可以转化成阿托伐他汀钙6。
    • 4. 发明申请
    • A NOVEL PROCESS FOR THE PREPARATION OF ESOMEPRAZOLE AND SALTS THEREOF
    • 用于制备异喹诺酮和其盐的新方法
    • WO2007140608A1
    • 2007-12-13
    • PCT/CA2007/001005
    • 2007-06-08
    • APOTEX PHARMACHEM INC.WANG, FanMONTEMAYOR, Laura, KayeCHE, DaqingHORNE, Stephen, E.
    • WANG, FanMONTEMAYOR, Laura, KayeCHE, DaqingHORNE, Stephen, E.
    • C07D401/12
    • C07D401/12Y02P20/55
    • A novel process for the preparation of omeprazole and its enantiomers, such as esomeprazole, as well as the preparation of related 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles, including pantoprazole, lansoprazole and rabeprazole, as recemates or single enantiomers, and their alkali or alkaline salts has been developed. The novel process involves the surprising discovery that protection of the free-base benzimidazole sulfoxide (e.g. omeprazole or esomeprazole), by reaction with an alkyl, aryl or aralkyl chloroformate following oxidation of the corresponding sulfide, eliminates the need for its direct isolation. Subsequent removal of the protecting group with a solution of alkali or alkaline earth alkoxide in a C1-C4 alcohol directly provides the corresponding salt. By eliminating the need to handle the free-base benzimidazole sulfoxide, this advantageous procedure provides increased chemical yields over processes described in the art.
    • 一种用于制备奥美拉唑及其对映异构体的新方法,例如艾美拉唑,以及相关的2-(2-吡啶基甲基 - 亚磺酰基)-1H-苯并咪唑(包括泮托拉唑,兰索拉唑和雷贝拉唑)作为受体或单一对映异构体的制备, 并开发了它们的碱金属盐或碱金属盐。 该新方法涉及令人惊奇的发现:在相应的硫化物氧化后,通过与烷基,芳基或氯甲酸烷基酯反应来保护游离碱性苯并咪唑亚砜(例如奥美拉唑或埃索美拉唑)消除了对其直接分离的需要。 随后用碱金属或碱土金属醇溶液在C1-C4醇中除去保护基团直接提供相应的盐。 通过消除处理游离碱性苯并咪唑亚砜的需要,与本领域中描述的方法相比,该有利的方法提供了增加的化学产率。
    • 7. 发明申请
    • USER DEVICE, NETWORK NODE AND METHODS THEREOF
    • 用户设备,网络节点及其方法
    • WO2017133780A1
    • 2017-08-10
    • PCT/EP2016/052443
    • 2016-02-05
    • HUAWEI TECHNOLOGIES CO., LTD.WANG, FanBERGGREN, Fredrik
    • WANG, FanBERGGREN, Fredrik
    • H04W74/08H04W72/04H04W72/12
    • H04W74/0816H04W72/0453H04W72/1294
    • The invention relates to a user device and a network node for a wireless communication system (500). The user device (100) comprises a transceiver (102) configured to receive a transmission grant (TG) indicating a set of frequency resources assigned for transmission to a network node (300); a processor (104) configured to determine a channel access outcome based on a channel access procedure performed in the set of frequency resources; wherein the transceiver (102) is configured to transmit a first signal (S1) to the network node (300) in the set of frequency resources according to the channel access outcome. The network node (300) comprises a transceiver (302) configured to transmit a transmission grant (TG) to a user device (100), the transmission grant indicating (TG) a set of frequency resources assigned for transmission from the user device (100) to the network node (300) and for performing a channel access procedure; receive a first signal (S1) from the user device (100) in the set of frequency resources. Furthermore, the invention also relates to corresponding methods, a wireless communication system, a computer program, and a computer program product.
    • 本发明涉及用于无线通信系统(500)的用户装置和网络节点。 用户设备(100)包括:收发器(102),被配置为接收指示被分配用于向网络节点(300)传输的频率资源集合的传输许可(TG); 处理器(104),其被配置为基于在所述一组频率资源中执行的信道接入过程来确定信道接入结果; 其中所述收发器(102)配置成根据所述信道接入结果在所述一组频率资源中向所述网络节点(300)发送第一信号(S1)。 所述网络节点(300)包括被配置为向用户设备(100)发送传输授权(TG)的收发器(302),所述传输授权指示(TG)分配用于从所述用户设备 )到网络节点(300)并用于执行信道接入过程; 在该组频率资源中接收来自用户设备(100)的第一信号(S1)。 此外,本发明还涉及相应的方法,无线通信系统,计算机程序和计算机程序产品。
    • 9. 发明申请
    • SUBFRAME TIMING WITH VARIABLE STARTING TIME
    • 具有可变启动时间的子帧时序
    • WO2016180451A1
    • 2016-11-17
    • PCT/EP2015/060242
    • 2015-05-08
    • HUAWEI TECHNOLOGIES CO., LTD.WANG, FanBERGGREN, Fredrik
    • WANG, FanBERGGREN, Fredrik
    • H04L5/00
    • H04L5/0048H04L5/0007H04L5/0044H04L5/0053H04L5/0078H04W72/0446H04W72/1273
    • The present invention relates to a transmitter device and a receiver device. The transmitter device (100) comprises a processer (102) configured to map at least one first signal to a first subframe (SF1), map at least one second signal to a second subframe (SF2) having a variable time offset in relation to the first subframe (SF1); and a transceiver (104) configured to transmit the first signal in the first subframe (SF1), transmit the second signal in the second subframe (SF2). The receiver device (300) comprises a receiving device (304) configured to receive a first signal transmitted in a first subframe (SF1), and receive a second signal transmitted in a second subframe (SF2) having a variable time offset in relation to the first subframe (SF1); and a processor (302) configured to process the received first signal, and process the received second signal. Furthermore, the present invention also relates to corresponding methods, a computer program, and a computer program product.
    • 本发明涉及发射机设备和接收机设备。 发射机设备(100)包括被配置为将至少一个第一信号映射到第一子帧(SF1)的处理器(102),将至少一个第二信号映射到具有相对于第一子帧(SF1)的可变时间偏移的第二子帧 第一子帧(SF1); 以及收发器(104),被配置为在所述第一子帧(SF1)中发送所述第一信号,在所述第二子帧(SF2)中发送所述第二信号。 接收机设备(300)包括接收设备(304),接收设备(304)被配置为接收在第一子帧(SF1)中发送的第一信号,并且接收在第二子帧(SF2)中发送的第二信号,该第二子帧具有相对于 第一子帧(SF1); 以及处理器(302),被配置为处理所接收的第一信号,并处理所接收的第二信号。 此外,本发明还涉及相应的方法,计算机程序和计算机程序产品。