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    OXADIAZOLE DERIVATIVE HAVING ENDOTHELIAL LIPASE INHIBITORY ACTIVITY
    4.
    发明申请
    OXADIAZOLE DERIVATIVE HAVING ENDOTHELIAL LIPASE INHIBITORY ACTIVITY 有权
    具有内皮脂肪酶抑制活性的氧化氮衍生物

    公开(公告)号：US20120253040A1

    公开(公告)日：2012-10-04

    申请号：US13516441

    申请日：2010-12-14

    Applicant: Koji Masuda ,  Shiro Kida ,  Naoki Yoshikawa ,  Manabu Katou ,  Terukazu Kato ,  Mado Nakajima ,  Eiichi Kojima ,  Mitsuhiro Yonehara

    Inventor： Koji Masuda ,  Shiro Kida ,  Naoki Yoshikawa ,  Manabu Katou ,  Terukazu Kato ,  Mado Nakajima ,  Eiichi Kojima ,  Mitsuhiro Yonehara

    IPC: C07D271/10 ,  C07D413/10 ,  C07D241/36 ,  C07D513/04 ,  C07D417/12 ,  C07D215/14 ,  C07D285/135

    CPC classification number: A61K31/423 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/433 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/5377 ,  C07D413/06 ,  C07D417/06 ,  C07D417/14 ,  C07D513/04

    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is aromatic carbocycle or aromatic heterocycle, Z is —NR5—, —O— or —S—, R5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl, substituted or unsubstituted aryl or the like, R1 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, R2 and R3 are each independently hydrogen, halogen, hydroxy or the like, R4 is a group represented by the formula: —(CR6R7)n-R8, wherein R6 and R7 are each independently hydrogen, halogen, hydroxy or the like, n is an integer of 0 to 3, R8 is carboxy, cyano, substituted or unsubstituted alkyl or the like, Rx is halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl or the like, m is an integer of 0 to 3.

    Abstract translation: 公开了可用作内皮脂肪酶抑制剂的化合物。 由下式表示的化合物：其药学上可接受的盐或其溶剂化物，其中环A是芳族碳环或芳族杂环，Z是-NR5-，-O-或-S-，R5是氢，取代或未取代的烷基， 取代或未取代的烯基，取代或未取代的炔基，取代或未取代的芳基等，R 1是氢，卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的烯基等， 独立地是氢，卤素，羟基等，R 4是由下式表示的基团： - （CR 6 R 7）n -R 8，其中R 6和R 7各自独立地为氢，卤素，羟基等，n为0〜 3，R8为羧基，氰基，取代或未取代的烷基等，Rx为卤素，羟基，氰基，硝基，羧基，取代或未取代的烷基，取代或未取代的烯基等，m为0〜3的整数。

    Azole type dioxolane derivatives
    5.
    发明授权
    Azole type dioxolane derivatives 失效
    唑型二氧戊环衍生物

    公开(公告)号：US4612322A

    公开(公告)日：1986-09-16

    申请号：US632852

    申请日：1984-07-20

    Applicant: Masaru Ogata ,  Hiroshi Matsumoto ,  Shiro Kida ,  Katsuya Tawara

    Inventor： Masaru Ogata ,  Hiroshi Matsumoto ,  Shiro Kida ,  Katsuya Tawara

    IPC: A01N43/653 ,  A01N43/832 ,  A61K31/41 ,  A61P31/04 ,  A61P31/10 ,  C07D249/08 ,  C07D317/00 ,  C07D327/00 ,  C07D405/06 ,  C07D411/06 ,  C07D521/00 ,  A01N43/50

    CPC classification number: C07D231/12 ,  C07D233/56 ,  C07D249/08

    Abstract: A compound of the formula: ##STR1## (wherein Az is imidazolyl or triazolyl;R is C.sub.1 -C.sub.5 alkyl or phenyl optionally substituted by 1 to 3 members selected from halogen, C.sub.1 -C.sub.5 alkyl, and C.sub.1 -C.sub.5 alkoxy;X.sup.1 and X.sup.2 each is hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, or C.sub.1 -C.sub.5 alkoxy;Y is C.dbd.O, C.dbd.S, S.dbd.O, or R.sup.1 --C--R.sup.2 ; andR.sup.1 and R.sup.2 each is hydrogen, C.sub.1 -C.sub.3 alkyl or, taken together may form C.sub.4 -C.sub.6 alkylene)or its acid addition salt being useful as an antimycotic agent is prepared by reacting a corresponding diol with a cyclizing agent.

    Abstract translation: 下式的化合物（其中Az为咪唑基或三唑基; R为C1-C5烷基或任选被1至3个选自卤素，C 1 -C 5烷基和C 1 -C 5烷氧基的成员取代的苯基; X 1和X 2 各自为氢，卤素，C1-C5烷基或C1-C5烷氧基; Y为C = O，C = S，S = O或R1-C-R2; R1和R2各自为氢，C1-C3烷基 或一起可以形成C4-C6亚烷基）或其酸加成盐可用作抗真菌剂通过使相应的二醇与环化剂反应来制备。

    ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON ENDOTHELIAL LIPASE
    8.
    发明申请
    ACETIC ACID AMIDE DERIVATIVE HAVING INHIBITORY ACTIVITY ON ENDOTHELIAL LIPASE 有权
    醋酸酰胺衍生物对内皮脂肪酸的抑制活性

    公开(公告)号：US20110251386A1

    公开(公告)日：2011-10-13

    申请号：US13124788

    申请日：2009-10-15

    Applicant: Koji Masuda ,  Shiro Kida ,  Kyohei Hayashi ,  Manabu Katou ,  Naoki Yoshikawa ,  Akira Kugimiya ,  Mado Nakajima ,  Nobuyuki Tanaka

    Inventor： Koji Masuda ,  Shiro Kida ,  Kyohei Hayashi ,  Manabu Katou ,  Naoki Yoshikawa ,  Akira Kugimiya ,  Mado Nakajima ,  Nobuyuki Tanaka

    IPC: C07D417/12 ,  C07D417/10 ,  C07D277/30 ,  C07D263/57 ,  C07D277/64 ,  C07D513/04

    CPC classification number: C07D235/16 ,  A61K31/4184 ,  A61K31/423 ,  A61K31/428 ,  A61K31/429 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D263/56 ,  C07D263/57 ,  C07D277/30 ,  C07D277/64 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D513/04

    Abstract: Disclosed is a compound which is useful as an endothelial lipase inhibitor.A pharmaceutical composition having inhibitory activity on endothelial lipase comprising a compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein Ring A is nitrogen-containing hetero ring, Ring A may be substituted with a substituent other than a group represented by the formula: —C(R1R2)—C(═O)—NR3R4 and a group represented by the formula: —R5, a broken line represents the presence or the absence of a bond, Z is —NR6—, ═N—, —O—, or —S—, R6 is halogen, substituted or unsubstituted alkyl or the like, R1 and R2 are each independently hydrogen, halogen, hydroxy, cyano, nitro, carboxy or substituted or unsubstituted alkyl, R3 is hydrogen or substituted or unsubstituted alkyl, R4 is hydrogen, substituted or unsubstituted alkyl or the like, R3 and R4 taken together with the adjacent nitrogen atom to which they are attached may form a substituted or unsubstituted ring, R5 is hydrogen, halogen, hydroxy, cyano, nitro, carboxy, substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted alkynyl or the like.

    Abstract translation: 公开了可用作内皮脂肪酶抑制剂的化合物。 一种具有对内皮脂肪酶具有抑制活性的药物组合物，其包含由下式表示的化合物：其药学上可接受的盐或其溶剂合物，其中环A是含氮杂环，环A可以被除代表的基团以外的取代基取代 通式为-C（R 1 R 2）-C（= O）-NR 3 R 4和由式-R 5表示的基团，虚线表示键的存在或不存在，Z为-NR 6 - ，= ，-O-或-S-，R 6为卤素，取代或未取代的烷基等，R 1和R 2各自独立地为氢，卤素，羟基，氰基，硝基，羧基或取代或未取代的烷基，R 3为氢或取代 或未取代的烷基，R 4为氢，取代或未取代的烷基等，R 3和R 4与它们所连接的相邻氮原子一起形成取代或未取代的环，R 5为氢，卤素，羟基，氰基，硝基 ，ca 取代或未取代的烷基，取代或未取代的链烯基，取代或未取代的炔基等。

    Preparation of compounds of lignan series
    9.
    发明授权
    Preparation of compounds of lignan series 失效
    木脂素系列化合物的制备

    公开(公告)号：US5488134A

    公开(公告)日：1996-01-30

    申请号：US356199

    申请日：1994-12-16

    Applicant: Sachio Mori ,  Shozo Takechi ,  Shiro Kida

    Inventor： Sachio Mori ,  Shozo Takechi ,  Shiro Kida

    IPC: C07C69/94 ,  C07C69/76

    CPC classification number: C07C69/94

    Abstract: This invention relates to a process for preparation of the compounds of lignan series in a regioselective manner. This invention provide a process for preparing a compound of the formula (I):which process is characterized by that a lactone compound represented by the formula (II) is allowed to react with a compound of the formula: R.sup.7 Cl in the presence of a base, then the resulting compound is subjected to addition reaction with an acetylenic compound of the formula (III), then the resulting compound is reduced;in which R.sup.1 is alkyl, cycloalkyl, cycloalkyl lower alkyl, or aralkyl and the like; R.sup.2 and R.sup.3 each is lower alkoxy and the like; R.sup.4 is lower alkoxy or hydrogen; and R.sup.5 and R.sup.6 each is lower alkyl; and R.sup.7 is tri(lower alkyl)silyl. ##STR1##

    Abstract translation: PCT No.PCT / JP94 / 00612 Sec。 371日期1994年12月16日第 102（e）1994年12月16日PCT PCT 1994年4月12日PCT公布。 出版物WO94 / 24087 本发明涉及以区域选择性方式制备木脂素系列化合物的方法。 本发明提供了制备式（I）化合物的方法：该方法的特征在于使式（II）表示的内酯化合物与下式化合物反应：在碱的存在下， 然后将所得化合物与式（III）的炔属化合物进行加成反应，然后将所得化合物还原; 其中R1是烷基，环烷基，环烷基低级烷基或芳烷基等; R2和R3各自为低级烷氧基等; R4是低级烷氧基或氢; R5和R6各自为低级烷基; 而R7是三（低级烷基）甲硅烷基。 （一）图像（二）<图像>（三）

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