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    Method for separating of optically pure thiophene compounds using simulated moving bed chromatography
    91.
    发明授权
    Method for separating of optically pure thiophene compounds using simulated moving bed chromatography 有权
    使用模拟移动床层析分离光学纯噻吩化合物的方法

    公开(公告)号：US07767832B2

    公开(公告)日：2010-08-03

    申请号：US11721366

    申请日：2004-12-20

    申请人： Jae Suk Koh ,  Chun Young Kim ,  Byoung In Lee ,  Sang Soo Lee ,  Seong Jun Lee ,  Jong Ho Lim ,  Seon Yeong Jeon ,  Jun Bae Hong

    发明人： Jae Suk Koh ,  Chun Young Kim ,  Byoung In Lee ,  Sang Soo Lee ,  Seong Jun Lee ,  Jong Ho Lim ,  Seon Yeong Jeon ,  Jun Bae Hong

    IPC分类号： C07D495/06

    CPC分类号： C07D495/04 ,  C07B57/00

    摘要： Disclosed herein is a method of producing an optically active thiophene-based compound using a simulated moving bed adsorption separation process, and more specifically, a method of continuously separating a racemic thiophene-based compound into its optically active thiophene-based compounds having high purity, through optical resolution using the simulated moving bed process. According to the method of the current invention, a racemic mixture of a thiophene-based compound can be continuously separated into its optically active thiophene-based compounds having high purity, which is an intermediate of optically active dorzolamide acting as a topical therapeutic agent for glaucoma, using a simulated moving bed adsorption separation technique, thereby increasing industrial usability.

    摘要翻译： 本文公开了使用模拟移动床吸附分离方法制造光学活性噻吩类化合物的方法，更具体地说，是将外消旋噻吩类化合物连续分离成其高纯度的光学活性噻吩类化合物的方法， 通过使用模拟移动床过程的光学分辨率。 根据本发明的方法，可以将噻吩类化合物的外消旋混合物连续分离成其高纯度的光学活性噻吩类化合物，其是用作青光眼的局部治疗剂的光学活性多吡咯酰胺的中间体 ，使用模拟移动床吸附分离技术，从而提高工业可用性。

    Compounds
    93.
    发明授权
    Compounds 有权
    化合物

    公开(公告)号：US07553849B2

    公开(公告)日：2009-06-30

    申请号：US11152777

    申请日：2005-06-15

    申请人： Anders Björk ,  Karl Jansson

    发明人： Anders Björk ,  Karl Jansson

    IPC分类号： A61K31/4365 ,  C07D495/06

    CPC分类号： C07D495/04

    摘要： A compound of formula (I) wherein R is methyl, ethyl, n-propyl, iso-propyl, n-butyl or allyl; R′ is hydrogen, C1-C4 alkyl, C1-C3 alkoxy; halogen, trifluoromethyl or OCHxFy, R″ is hydrogen, fluoro or chloro, that R″ being fluoro or chloro only when R′ is fluoro or chloro; R3 is hydrogen or C1-C5 alkyl R4 is hydrogen, CH2OCOC(CH3)3, pharmaceutically acceptable inorganic or organic cations, or COR4′ wherein R4′ is C1-C5 alkyl, phenyl, benzyl or phenethyl; R7 is methyl or ethyl; one of A and B is sulphur and the other is C-R2; when A is S, R2 is selected from hydrogen and methyl, with the proviso that R2 is methyl only when R3 is not hydrogen; and when B is S, R2 is hydrogen; and any tautomer thereof. A pharmaceutical composition comprising a compound of formula (I), a method of treating malignant tumours or diseases resulting from autoimmunity or pathologic inflammation.

    摘要翻译： 式（I）的化合物，其中R是甲基，乙基，正丙基，异丙基，正丁基或烯丙基; R'是氢，C 1 -C 4烷基，C 1 -C 3烷氧基; 卤素，三氟甲基或OCH x F y，R“是氢，氟或氯，只有当R'是氟或氯时，R”是氟或氯; R3是氢或C1-C5烷基R4是氢，CH2OCOC（CH3）3，药学上可接受的无机或有机阳离子，或COR4'，其中R4'是C1-C5烷基，苯基，苄基或苯乙基; R7是甲基或乙基; A和B之一是硫，另一个是C-R2; 当A为S时，R2选自氢和甲基，条件是仅当R3不为氢时R2为甲基; 当B为S时，R 2为氢; 及其互变异构体。 一种药物组合物，其包含式（I）化合物，治疗恶性肿瘤的方法或由自身免疫或病理性炎症引起的疾病。

    Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors
    94.
    发明授权
    Thieno-imino acid derivatives for use as matrix metalloproteinase inhibitors 有权
    噻吩并亚氨基酸衍生物用作基质金属蛋白酶抑制剂

    公开(公告)号：US07399770B2

    公开(公告)日：2008-07-15

    申请号：US11461189

    申请日：2006-07-31

    申请人： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister ,  Maxime Lampilas

    发明人： Manfred Schudok ,  Hans Matter ,  Armin Hofmeister ,  Maxime Lampilas

    IPC分类号： A61K31/4365 ,  C07D409/02 ,  C07D495/06

    CPC分类号： C07D495/04

    摘要： The invention is directed to a compound of the formula I wherein the variables are as defined herein, or a stereoisomeric form thereof, mixture of stereoisomeric forms, in any ratio, or a salt thereof. Another aspect of the present invention is directed to a pharmaceutical composition comprising, a pharmaceutically effective amount of one or more compounds of formula I according to claim 1 in admixture with a pharmaceutically acceptable carrier.The invention is also directed to a method for effecting the prophylaxis and therapy of degenerative joint diseases such as osteoarthroses, spondyloses, cartilage loss following joint trauma or a relatively long period of joint immobilization following meniscus or patella injuries or ligament ruptures, diseases of the connective tissue such as collagenoses, periodontal diseases, wound healing disturbances and chronic diseases of the locomotory apparatus such as inflammatory, immunological or metabolism-associated acute and chronic arthritides, arthropathies, myalgias and disturbances of bone metabolism, for the treatment of ulceration, atheroscleroses and stenoses, and for the treatment of inflammations, cancer diseases, tumor metastasis formation, cachexia, anorexia, cardiac insufficiency and septic shock or for the prophylaxis of myocardial and cerebral infarctions, in a patient in need thereof, comprising administering to the patient a pharmaceutically effective amount of the compound of formula I according to claim 1, or a pharmaceutically acceptable salt, solvate or prodrug thereof.Furthermore the invention is directed to a method for preparing a compound of formula I.

    摘要翻译： 本发明涉及式I化合物，其中变量如本文所定义，或其立体异构形式，立体异构体形式的任何比例的混合物或其盐。 本发明的另一方面涉及一种药物组合物，其包含药学有效量的一种或多种根据权利要求1的式I化合物与药学上可接受的载体的混合物。 本发明还涉及一种用于预防和治疗退行性关节疾病如骨关节炎，椎关节强硬，关节创伤后的软骨损失或半月板或髌骨损伤或韧带断裂后相对较长的关节固定的方法，连接性疾病 诸如胶原蛋白，牙周病，伤口愈合障碍和诸如炎症，免疫学或代谢相关的急性和慢性关节炎的关节病，关节病，肌痛和骨骼代谢紊乱的运动器官的组织，用于治疗溃疡，动脉粥样硬化和狭窄 ，并且用于在有需要的患者中治疗炎症，癌症疾病，肿瘤转移形成，恶病质，厌食症，心脏功能不全和败血性休克或用于预防心肌和脑梗死，包括向患者施用药学有效量 的compou 根据权利要求1的式I的或其药学上可接受的盐，溶剂合物或前药。 此外，本发明涉及制备式I化合物的方法。

    Process for the purification of thiophenes
    95.
    发明申请
    Process for the purification of thiophenes 审中-公开
    噻吩的纯化方法

    公开(公告)号：US20050065352A1

    公开(公告)日：2005-03-24

    申请号：US10942409

    申请日：2004-09-16

    申请人： Lutz Brassat ,  Stephan Kirchmeyer

    发明人： Lutz Brassat ,  Stephan Kirchmeyer

    IPC分类号： C07D495/06 ,  C07D333/16 ,  C07D333/32 ,  C07D495/04 ,  C08G61/12 ,  H05K3/42 ,  C07D335/00

    CPC分类号： C07D495/04 ,  C07D333/32 ,  C08G61/126 ,  H01G11/48 ,  H05K3/424 ,  Y02E60/13

    摘要： The invention relates to a process for the purification of thiophenes by means of precipitation. The purified thiophenes are liquid at room temperature, have a purity of at least 99.50 wt. %, and are represented by the following general formula (I), wherein R1 and R2 independently of each other are, for example, a linear or branched C1-C20-alkyl group, or together form a fused C1-C20-dioxyalylene ring. The process involves: (I) precipitating the thiophene by cooling a solution of the thiophene and at least one solvent; or (II) precipitating the thiophene by adding the thiophene to a cooled solution of solvent and optionally the thiophene. The solutions are cooled to a temperature below the melting point of the thiophene.

    摘要翻译： 本发明涉及通过沉淀纯化噻吩的方法。 纯化的噻吩在室温下是液体，纯度至少为99.50wt。 ％，并且由以下通式（I）表示，其中R 1和R 2彼此独立地是例如直链或支链C 1 -C 20 - 烷基，或一起形成稠合C1 -C 20 - 二氧杂环戊烯环。 该方法包括：（I）通过冷却噻吩和至少一种溶剂的溶液来沉淀噻吩; 或（II）通过将噻吩加入到冷却的溶剂和任选的噻吩中来沉淀噻吩。 将溶液冷却至低于噻吩的熔点的温度。

    Electroconductive composition
    98.
    发明授权
    Electroconductive composition 失效
    导电组合物

    公开(公告)号：US5871670A

    公开(公告)日：1999-02-16

    申请号：US793716

    申请日：1997-03-03

    申请人： Bruno Hilti ,  Ernst Minder ,  Jurgen Pfeiffer

    发明人： Bruno Hilti ,  Ernst Minder ,  Jurgen Pfeiffer

    IPC分类号： C07D335/02 ,  C07D339/04 ,  C07D339/06 ,  C07D339/08 ,  C07D345/00 ,  C07D495/06 ,  C07D495/22 ,  C07D517/06 ,  C07D517/22 ,  C08K5/45 ,  C08L101/00 ,  H01B1/12 ,  H01B1/20 ,  C08K5/00

    CPC分类号： H01B1/121 ,  Y10S524/91 ,  Y10S524/911

    摘要： A composition comprising a matrix of a thermoplastic, thermosetting or a structurally crosslinked polymer, in which is incorporated an electroconductive network of crystal needles of a charge transfer complex (abbreviated to CT complex) from an electron donor and an electron acceptor, characterized in that:(1) the matrix contains uniformly distributed an excess, with respect to the CT complex formation, either of at least one electron donor or at least one electron acceptor as weakly polymer-soluble finely divided particles,(2) the CT complex is formed either by at least one weakly polymer-soluble electron donor and at least one polymer-soluble electron acceptor or by at least one weakly polymer-soluble electron acceptor and at least one polymer-soluble electron donor, and(3) microcrystalline needles grow from the weakly polymer-soluble particles in the polymer mass, which microcrystalline needles are in contact with and connect the weakly polymer-soluble particles to form a network which penetrates the polymer mass.

    摘要翻译： PCT No.PCT / EP95 / 03537。 371日期1997年3月3日 102（e）1997年3月3日PCT PCT 1995年9月8日PCT公布。 公开号WO96 / 09629 日期：1996年3月28日一种包含热塑性，热固性或结构交联聚合物基体的组合物，其中掺入电子转移络合物（缩写为CT络合物）的晶体针的电导网络和电子受体 其特征在于：（1）相对于CT络合物形成，基质含有均匀分布的过量的至少一种电子给体或至少一种电子受体作为弱聚合物可溶的细碎颗粒，（2） CT复合物由至少一种弱聚合物可溶电子给体和至少一种聚合物可溶电子受体或至少一种弱聚合物可溶电子受体和至少一种聚合物可溶电子给体形成，和（3）微晶 针从聚合物物质中的弱聚合物可溶性颗粒生长，微晶针与弱聚合物可溶性颗粒接触并连接 以形成穿透聚合物质量的网络。