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    CRYSTALLINE SALTS OF NALOXONE AND NALTREXONE
    1.
    发明申请
    CRYSTALLINE SALTS OF NALOXONE AND NALTREXONE 审中-公开
    NALOXONE和NALTREXONE的晶体盐

    公开(公告)号：WO2017053938A1

    公开(公告)日：2017-03-30

    申请号：PCT/US2016/053699

    申请日：2016-09-26

    申请人： PAIN THERAPEUTICS, INC. ,  ZAMLOOT, Michael

    发明人： ZAMLOOT, Michael ,  BARBIER, Remi ,  FRIEDMANN, Nadav ,  SRIRAMBHATLA, Vijay ,  WATT, Stephen

    IPC分类号： A61M11/00 ,  A61J1/00 ,  A61K9/00 ,  A61K31/485

    CPC分类号： A61K31/485 ,  A61K9/7038 ,  C07C55/10 ,  C07C59/285 ,  C07D489/08 ,  A61K2300/00

    摘要： This invention relates to crystalline salts of naloxone and of naltrexone and their use as opioid antagonists. The crystalline salts of the invention include naloxone saccharinate, naltrexone succinate and a methanol solvate of naltrexone succinate. A drug-in-adhesive transdermal patch containing the opioid analgesic fentanyl or an analog thereof and a crystalline salts of naloxone or naltrexone is disclosed. Also disclosed is a method of treating pain, such as acute, chronic or intermittent pain, by applying a drug-in-adhesive transdermal patch of the invention to the skin of a patient in need thereof.

    摘要翻译： 本发明涉及纳络酮和纳曲酮的结晶盐及其作为阿片样物质拮抗剂的用途。 本发明的结晶盐包括纳络酮糖精，琥珀酸纳曲酮和纳曲酮琥珀酸的甲醇溶剂化物。 公开了含有阿片类镇痛芬太尼或其类似物的药物粘合性透皮贴剂和纳洛酮或纳曲酮的结晶盐。 还公开了通过将本发明的药物粘附性透皮贴剂施用于有需要的患者的皮肤来治疗疼痛的方法，例如急性，慢性或间歇性疼痛。

    ISOMETHEPTENE ISOMER
    3.
    发明申请
    ISOMETHEPTENE ISOMER 审中-公开
    异构异构体

    公开(公告)号：WO2014113734A2

    公开(公告)日：2014-07-24

    申请号：PCT/US2014/012142

    申请日：2014-01-17

    申请人： TONIX PHARMACEUTICALS INC. ,  LEDERMAN, Seth ,  DAUGHERTY, Bruce ,  GERSHELL, Leland J. ,  RIDEOUT, Darryl ,  KAWASAKI, Andrew

    发明人： LEDERMAN, Seth ,  DAUGHERTY, Bruce ,  GERSHELL, Leland J. ,  RIDEOUT, Darryl ,  KAWASAKI, Andrew

    CPC分类号： C07C211/21 ,  A61K31/047 ,  A61K31/131 ,  A61K31/167 ,  A61K31/192 ,  A61K31/4045 ,  A61K31/4152 ,  A61K31/522 ,  A61K31/616 ,  A61K45/06 ,  C07B53/00 ,  C07B2200/07 ,  C07C59/285 ,  A61K2300/00

    摘要： The invention relates to a purified Isometheptene compound comprising the structure according to Formula (I), (Formula (I)) or a hydrochloride, or a pharmaceutically acceptable addition salt thereof. In particular, the disclosure relates to the synthesis, purification and characterization of an Isometheptene isomer mucate crystal 2, wherein the Isometheptene isomer 2 is stereochemically characterized as (R)-enantiomer, respectively. The Isometheptene (R)-enantiomer activity indicates a selective centrally acting selective ligand for Imidazoline subtype 1 (I1) receptor sites; and more specifically, the disclosure provides an antihypertensive composition for treatment of migraine and other neurovascular or neurogenic pain from abdominal distress. (R)-Isometheptene enantiomer or isomer 2 may be an anti-hypertensive agent with lower side effects than the racemate form. Therefore (R)-Isometheptene is believed to be effective against episodic tension-type headaches (ETTH). The (R)-Isometheptene enantiomer or isomer 2 is believed to effectively lower blood pressure, used alone or together with other headache ameliorating drugs. Methods of synthesis and treatment are described. Regarding (R)- Isometheptene crystals data of X-ray crystallography are presented.

    摘要翻译： 本发明涉及包含根据式（I），（式（I））或盐酸盐的结构或其药学上可接受的加成盐的纯化异构体化合物。 特别地，本公开涉及异葎草酮异构体粘蛋白晶体2的合成，纯化和表征，其中异构异构体异构体2分别被立体化学表征为（R） - 对映异构体。 对映异构体异构体活性表示咪唑啉亚型1（I1）受体位点的选择性中心作用选择性配体; 并且更具体地，本公开提供了用于治疗偏头痛和其他神经血管或神经源性疼痛的抗高血压组合物。 （R） - 异亚丙基对映异构体或异构体2可以是具有低于外消旋形式的副作用的抗高血压剂。 因此（R） - 美沙芬被认为对于发作型紧张型头痛（ETTH）有效。 据信（R） - 异构体异构体2有效地降低血压，单独使用或与其他头痛改善药物一起使用。 描述合成和处理方法。 关于（R） - 异构体色素晶体的X射线晶体学数据。

    SOLID FORMS OF TENOFOVIR DISOPROXIL
    4.
    发明申请
    SOLID FORMS OF TENOFOVIR DISOPROXIL 审中-公开
    TENOFOVIR DISOPROXIL的固体形式

    公开(公告)号：WO2009074351A3

    公开(公告)日：2009-11-12

    申请号：PCT/EP2008010826

    申请日：2008-12-11

    申请人： ULTIMORPHIX TECHNOLOGIES B V ,  DOVA EVANTHIA

    发明人： DOVA EVANTHIA

    IPC分类号： C07F9/6561 ,  A61K31/675

    CPC分类号： C07F9/65616 ,  C07C51/412 ,  C07C55/10 ,  C07C59/255 ,  C07C59/265 ,  C07C59/285 ,  C07C65/10

    摘要： The present invention provides Tenofovir disoproxil succinate, Tenofovir disoproxil L-tartrate, Tenofovir disoproxil oxalate, Tenofovir disoproxil saccharate, Tenofovir disoproxil citrate, Tenofovir disoproxil salicylate and various solid forms thereof, methods for the preparation thereof and their use in pharmaceutical applications, in particular in anti-HIV medicaments. The forms of Tenofovir disoproxil can be used in combination with other anti-HIV medicaments such as Efavirenz and Emtricitabine.

    摘要翻译： 本发明提供替诺福韦地索普西琥珀酸盐，替诺福韦地索普西L-酒石酸盐，替诺福韦地索普西草酸盐，替诺福韦地索普西糖酸盐，替诺福韦地索普西柠檬酸盐，替诺福韦地索普西水杨酸盐及其各种固体形式，其制备方法及其在药物应用中的用途， 抗HIV药物。 替诺福韦地索普西的形式可以与其他抗HIV药物例如依法韦仑和恩曲他滨组合使用。

    STABLE, NON-HYGROSCOPIC SALTS OF L(-)CARNITINE AND ALKANOYL L(-)CARNITINES, A PROCESS FOR THEIR PREPARATION AND SOLID, ORALLY ADMINISTRABLE COMPOSITIONS CONTAINING SUCH SALTS
    6.
    发明申请
    STABLE, NON-HYGROSCOPIC SALTS OF L(-)CARNITINE AND ALKANOYL L(-)CARNITINES, A PROCESS FOR THEIR PREPARATION AND SOLID, ORALLY ADMINISTRABLE COMPOSITIONS CONTAINING SUCH SALTS 审中-公开
    稳定的L（ - ）卡尼汀和烷基-L（ - ）链烯的非离子性盐，其制备和固体，含有这种盐的管理组合物的方法

    公开(公告)号：WO1997046512A1

    公开(公告)日：1997-12-11

    申请号：PCT/EP1997002693

    申请日：1997-05-26

    申请人： FASSI, Aldo

    IPC分类号： C07C229/22

    CPC分类号： C07C229/22 ,  C07C59/285

    摘要： Stable, non-hygroscopic salts of L(-)carnitine and alkanoyl L(-)carnitines with mucic acid of formula (I) are disclosed wherein the molar ratio between the carnitine moiety and mucic acid is 2:1. A process for producing the salts and solid orally administrable compositions containing same are also disclosed.

    摘要翻译： 公开了具有式（I）的粘酸的L（ - ）肉碱和烷酰基L（ - ）肉碱的稳定的非吸湿盐，其中肉碱部分和粘酸之间的摩尔比为2:1。 还公开了含有该盐的盐和固体可口服给药组合物的制备方法。

    ESTERIFIED ANHYDROPENTITOLS AND METHODS OF MAKING THE SAME
    7.
    发明申请
    ESTERIFIED ANHYDROPENTITOLS AND METHODS OF MAKING THE SAME 审中-公开
    确定的抗肿瘤药物及其制备方法

    公开(公告)号：WO2016028851A1

    公开(公告)日：2016-02-25

    申请号：PCT/US2015/045816

    申请日：2015-08-19

    申请人： ARCHER DANIELS MIDLAND COMPANY

    发明人： STENSRUD, Kenneth ,  WICKLUND, Lori

    IPC分类号： C07D307/04 ,  C07D307/20

    CPC分类号： C07D307/20 ,  C07C59/105 ,  C07C59/285 ,  C07C67/14 ,  C07C213/08 ,  C07C219/06 ,  C07C303/30 ,  C07C309/68 ,  C12P17/04 ,  C12Y301/01003

    摘要： Amphipathic amine-esters derived from anhydropentitols are prepared through a short sequence of synthetic steps. The process is initiated by the esterification of an anhydropentitol with a fatty acid chloride or a lipase enzyme to form anhydropentitol fatty acid esters, preferably leaving at least one free hydroxyl. The free hydroxyl group(s) are then sulfonated, forming sulfonated anhydropentitol fatty acid esters. The sulfonyl moiety on the sulfonated anhydropentitol fatty acid esters are then subject to nucleophilic displacement by a hydrophilic moiety, illustrated by a primary amine such as AEE or AEEA. The synthetic pathway is efficient and affords modest to high yields of target amphiphilic compounds, which are useful at least as surfactants and plasticizer substitutes for petroleum derived compounds.

    摘要翻译： 通过短程序的合成步骤制备由脱水三醇衍生的两亲胺 - 酯。 该方法是通过将异氢
    异丙醇与脂肪酰氯或脂肪酶进行酯化反应来形成脱氢异戊醇脂肪酸酯，优选
    留下至少一种游离羟基。 然后将游离羟基磺化，形成磺化的脱水异构醇脂肪酸酯。 然后通过亲水部分对磺化的脱水异构醇脂肪酸酯上的磺酰部分进行亲核置换，如由伯胺如AEE或AEEA所示。 合成途径是有效的，并提供适度的高产量的目标两亲化合物，其至少可用作石油衍生化合物的表面活性剂和增塑剂替代物。

    SOLID FORMS OF TENOFOVIR DISOPROXIL
    9.
    发明申请
    SOLID FORMS OF TENOFOVIR DISOPROXIL 审中-公开
    固体形式的TENOFOVIR DISOPROXIL

    公开(公告)号：WO2009074351A2

    公开(公告)日：2009-06-18

    申请号：PCT/EP2008/010826

    申请日：2008-12-11

    申请人： ULTIMORPHIX TECHNOLOGIES B.V. ,  DOVA, Evanthia

    发明人： DOVA, Evanthia

    IPC分类号： C07F9/6561 ,  A61K31/675

    CPC分类号： C07F9/65616 ,  C07C51/412 ,  C07C55/10 ,  C07C59/255 ,  C07C59/265 ,  C07C59/285 ,  C07C65/10

    摘要： The present invention provides Tenofovir disoproxil succinate, Tenofovir disoproxil L-tartrate, Tenofovir disoproxil oxalate, Tenofovir disoproxil saccharate, Tenofovir disoproxil citrate, Tenofovir disoproxil salicylate and various solid forms thereof, methods for the preparation thereof and their use in pharmaceutical applications, in particular in anti-HIV medicaments. The forms of Tenofovir disoproxil can be used in combination with other anti-HIV medicaments such as Efavirenz and Emtricitabine.

    摘要翻译： 本发明提供了替诺福韦组合物，替诺福韦酯，酒石酸替诺福韦，替诺福韦酯，草酸替诺福韦酯，柠檬酸替诺福韦酯，水杨酸替诺福韦酯，其各种固体形式，其制备方法及其在制药应用中的用途， 抗艾滋病毒药物。 替诺福韦组合的替诺福韦可与其他抗艾滋病药物如依法韦仑和恩曲他滨联合使用。