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    METHOD FOR PRODUCING MALEATE USING WET CRYSTAL
    151.
    发明申请
    METHOD FOR PRODUCING MALEATE USING WET CRYSTAL 审中-公开
    使用水溶液生产胶体的方法

    公开(公告)号：US20130317214A1

    公开(公告)日：2013-11-28

    申请号：US13990380

    申请日：2011-11-30

    申请人： Takeshi Tsubuki

    发明人： Takeshi Tsubuki

    IPC分类号： C07D413/04

    CPC分类号： C07D413/04 ,  C07C57/145 ,  C07D413/14

    摘要： [Problem] To efficiently (without carrying out column purification) provide a high-purity maleate having excellent storage stability, solubility, crystallinity and ease of handling according to the present invention.[Solution] This method for producing the maleate represented by formula (1) includes obtaining the compound represented by formula (2) by reacting the compound represented by formula (3) with the compound represented by formula (4) in the presence of a salt, precipitating crystals of the compound represented by formula (2) by mixing the obtained compound represented by formula (2) with acetone and water, and obtaining the maleate represented by formula (1) by adding maleic acid to an acetone solution of the compound represented by formula (2), prepared by dissolving the crystals of the obtained compound represented by formula (2) in acetone.

    摘要翻译： [问题]为了有效地（不进行柱纯化），提供根据本发明的具有优异的储存稳定性，溶解性，结晶性和易于处理的高纯度马来酸酯。 [解决方案]制备由式（1）表示的马来酸酯的方法包括通过使由式（3）表示的化合物与式（4）表示的化合物在盐的存在下反应而获得式（2）表示的化合物 通过将由式（2）表示的所得化合物与丙酮和水混合，沉淀出式（2）表示的化合物的晶体，并通过将马来酸加入到所述化合物的丙酮溶液中得到由式（1）表示的马来酸酯 通过将由式（2）表示的所得化合物的晶体溶解在丙酮中制备的式（2）。

    Method for producing 3-substituted-4-fluoropyrrolidine derivative
    152.
    发明授权
    Method for producing 3-substituted-4-fluoropyrrolidine derivative 有权
    3-取代-4-氟吡咯烷衍生物的制备方法

    公开(公告)号：US08501965B2

    公开(公告)日：2013-08-06

    申请号：US13700772

    申请日：2011-05-30

    申请人： Masashi Suzuki ,  Muneki Nagao

    发明人： Masashi Suzuki ,  Muneki Nagao

    IPC分类号： C07D207/04

    CPC分类号： C07D207/10 ,  Y02P20/55

    摘要： An inexpensive and industrially advantageous method for producing optically active syn-3-(N-substituted-aminomethyl)-4-fluoropyrrolidine which may be an intermediate for producing pharmaceuticals is provided. The present invention relates a method for producing a syn-1-protected-4-fluoro-3-(N-substituted-N-nitrobenzenesulfonyl)pyrrolidine derivative or it's enantiomer, or their salts comprising the process of fluorinating a compound represented by the general formula (6) (in the formula, PG1 represents a protecting group for an amino group, R1 represents a C1 to C6 alkyl group which may be substituted or a C3 to C8 cycloalkyl group which may be substituted, and Ns represents a 2-nitrobenzenesulfonyl group or a 4-nitrobenzenesulfonyl group) or it's enantiomer using a nucleophilic fluorinating agent and an organic base having an amidine or guanidine structure.

    摘要翻译： 提供了一种制备光学活性的顺式-3-（N-取代氨基甲基）-4-氟吡咯烷的便​​宜且工业上有利的方法，其可以是制备药物的中间体。 本发明涉及一种用于制备顺式-1-保护的4-氟-3-（N-取代-N-硝基苯磺酰基）吡咯烷衍生物或其对映体或其盐的方法，该方法包括将通式 式（6）（式中，PG1表示氨基的保护基，R1表示可被取代的C1〜C6烷基或可被取代的C3〜C8环烷基，Ns表示2-硝基苯磺酰基 基团或4-硝基苯磺酰基）或其对映异构体，使用亲核氟化剂和具有脒或胍结构的有机碱。

    TABLET HAVING HOLLOW STRUCTURE
    156.
    发明申请
    TABLET HAVING HOLLOW STRUCTURE 审中-公开
    具有中空结构的片材

    公开(公告)号：US20120100212A1

    公开(公告)日：2012-04-26

    申请号：US13382666

    申请日：2010-07-05

    申请人： Mamoru Fukuda ,  Akinori Goto

    发明人： Mamoru Fukuda ,  Akinori Goto

    IPC分类号： A61K9/36 ,  A61K9/22

    CPC分类号： A61K9/0065 ,  A61K9/2072 ,  A61K9/2095

    摘要： A water floatable tablet, which is either: (a) a tablet comprising at least one filler selected from the group consisting of a sugar alcohol, a sugar, a cellulose derivative, and a starch and a component which exhibits a hydrophobic effect, wherein the tablet has a hollow cavity in a center section; or (b) a tablet obtained by a process including: (1) forming a crust comprising at least one filler selected from the group consisting of a sugar alcohol, a sugar, a cellulose derivative, and a starch on an outer surface of a core comprising a sublimation solid, to obtain a dry coated tablet having the core positioned at a center section; (2) heating the dry coated tablet, to obtain a tablet having a hollow cavity; and (3) contacting the tablet having a hollow cavity with a component which exhibits a hydrophobic effect.

    摘要翻译： 一种可漂浮浮片，其为：（a）包含至少一种选自糖醇，糖，纤维素衍生物和淀粉的填料的片剂和显示疏水作用的成分，其中， 片剂在中心部分具有中空腔; 或（b）通过以下方法获得的片剂：（1）在芯的外表面上形成包含至少一种选自糖醇，糖，纤维素衍生物和淀粉的填料的外皮 包括升华固体，以获得具有位于中心部分的芯的干涂片剂; （2）加热干燥的包衣片，得到具有中空腔的片剂; 和（3）使具有中空腔的片剂与显示疏水作用的成分接触。

    Cyclic amino benzoic acid derivative
    157.
    发明授权
    Cyclic amino benzoic acid derivative 失效
    环状氨基苯甲酸衍生物

    公开(公告)号：US07902367B2

    公开(公告)日：2011-03-08

    申请号：US11659854

    申请日：2005-08-11

    申请人： Masahiro Nomura ,  Yasuo Takano ,  Kazuhiro Yumoto ,  Takehiro Shinozaki ,  Shigeki Isogai ,  Koji Murakami

    发明人： Masahiro Nomura ,  Yasuo Takano ,  Kazuhiro Yumoto ,  Takehiro Shinozaki ,  Shigeki Isogai ,  Koji Murakami

    IPC分类号： C07D401/00 ,  A01N43/40

    CPC分类号： C07D417/12 ,  C07D211/22 ,  C07D211/26 ,  C07D211/42 ,  C07D211/56 ,  C07D211/60

    摘要： The present invention relates to cyclic amino benzoic acid derivatives which are effective in therapy of lipid metabolism abnormality, diabetes and the like as a human peroxisome proliferators-activated receptor (PPAR) agonist, in particular, as an agonist against human PPARα isoform, and addition salts thereof, and pharmaceutical compositions containing these compounds.A cyclic amino benzoic acid derivative represented by the general formula (1) [wherein a ring Ar represents an aryl group which may have substituent, or the like; Y represents a C1-C4 alkylene, C2-C4 alkenylene, C2-C4 alkynylene, or the like; Z represents an oxygen atom, sulfur atom or —(CH2)n— (n represents 0, 1 or 2); X represents a hydrogen atom, halogen atom, lower alkyl group which may be substituted with a halogen atom, or the like; R represents a hydrogen atom or lower alkyl group, and —COOR substitutes for an ortho position or metha position of binding position of ring W] or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明涉及有效治疗脂质代谢异常的环状氨基苯甲酸衍生物，作为人类过氧化物酶体增殖物激活受体（PPAR）激动剂的糖尿病等，特别是作为对人PPARα同种型的激动剂的添加 其盐，以及含有这些化合物的药物组合物。 由通式（1）表示的环状氨基苯甲酸衍生物[其中环Ar表示可具有取代基的芳基等; Y表示C1-C4亚烷基，C2-C4亚链烯基，C2-C4亚炔基等; Z表示氧原子，硫原子或 - （CH 2）n - （n表示0,1或2）; X表示氢原子，卤素原子，可被卤素原子取代的低级烷基等; R代表氢原子或低级烷基，-COOR代替环W的结合位置的邻位或甲基位置]或其药学上可接受的盐。

    Process for producing muscarine receptor antagonist and intermediate therefor
    159.
    发明授权
    Process for producing muscarine receptor antagonist and intermediate therefor 有权
    生产毒蕈碱受体拮抗剂及其中间体的方法

    公开(公告)号：US07868183B2

    公开(公告)日：2011-01-11

    申请号：US11721378

    申请日：2005-12-13

    申请人： Yuuji Ishiguro ,  Yasuhiro Aizawa ,  Masahiro Aono

    发明人： Yuuji Ishiguro ,  Yasuhiro Aizawa ,  Masahiro Aono

    IPC分类号： C07D233/64

    CPC分类号： C07D233/56

    摘要： The industrial production of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide, a urinary incontinence remedy, necessitates elimination of problems concerning the use of a synthetic adsorbent, e.g., HP-20, the efficiency of operation with the same, purification efficiency, etc. An acid salt, e.g., hydrochloride or phosphate, of 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide or a hydrate of any of these salts is used as an intermediate. This intermediate is neutralized and then purified. Thus, high-purity 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide is easily obtained in satisfactory yield. The industrial-scale production process has been thus established.

    摘要翻译： 4-（2-甲基-1-咪唑基）-2,2-二苯基丁酰胺（尿失禁药物）的工业化生产需要消除使用合成吸附剂的问题，例如HP-20，操作效率 相同的，净化效率等。使用4-（2-甲基-1-咪唑基）-2,2-二苯基丁酰胺或任何这些盐的水合物的酸式盐，例如盐酸盐或磷酸盐作为中间体。 将该中间体中和，然后纯化。 因此，以良好的产率容易地获得高纯度的4-（2-甲基-1-咪唑基）-2,2-二苯基丁酰胺。 工业规模化生产过程已经形成。