公开(公告)号：US06323212B1

公开(公告)日：2001-11-27

申请号：US08108643

申请日：1997-02-10

Applicant: Hiroshi Nagase ,  Koji Kawai ,  Kuniaki Kawamura ,  Jun Hayakawa ,  Takashi Endoh

Inventor： Hiroshi Nagase ,  Koji Kawai ,  Kuniaki Kawamura ,  Jun Hayakawa ,  Takashi Endoh

IPC: C07D48900

CPC classification number: C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D489/08

Abstract: A morphinan derivative or its pharmacologically allowed acid addition salt represented with compound I, an analgesic and diuretic having its derivative or its salt as the active ingredient, and its production process are described. The compound of the present invention possesses strong analgesic activity and diuretic action as a highly selective &kgr;-opioid agonist, allowing it to be used as a useful analgesic and diuretic.

公开(公告)号：US06403798B2

公开(公告)日：2002-06-11

申请号：US09793024

申请日：2001-02-26

Applicant: Fang-Ting Chiu ,  Young S. Lo

Inventor： Fang-Ting Chiu ,  Young S. Lo

IPC: C07D48900

CPC classification number: C07D489/06

Abstract: A method for the preparation of oxycodone, and salts thereof, from codeine comprising oxidation of codeine to codeinone, formation of an dienolsilyl ether congener of codeinone in strong amine base, oxidation of the dienolsilyl ether congener using peracetic acid, and hydrogenation of the resulting 14-hydroxycodeinone product.

Abstract translation: 制备可待因的可待因的方法及其盐，所述可待因包括可待因氧化可卡因酮，在强胺碱中形成二烯醇基醚同系物，使用过乙酸的二烯醇醚同族物的氧化，以及所得的14 - 羟可待因酮产品。

公开(公告)号：US06277859B1

公开(公告)日：2001-08-21

申请号：US09541793

申请日：2000-03-31

Applicant: Hiroshi Nagase ,  Koji Kawai ,  Kuniaki Kawamura ,  Jun Hayakawa ,  Takashi Endoh

Inventor： Hiroshi Nagase ,  Koji Kawai ,  Kuniaki Kawamura ,  Jun Hayakawa ,  Takashi Endoh

IPC: C07D48900

CPC classification number: C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D489/08

Abstract: A morphinan derivative or its pharmacologically allowed acid addition salt represented with compound I, an analgesic and diuretic having its derivative or its salt as the active ingredient, and its production process are described. The compound of the present invention possesses strong analgesic activity and diuretic action as a highly selective &kgr;-opioid agonist, allowing it to be used as a useful analgesic and diuretic.

Abstract translation: 描述了以化合物I表示的吗啡喃衍生物或其药理学允许的酸加成盐，其衍生物或其盐作为活性成分的止痛剂和利尿剂及其制备方法。 本发明化合物作为高度选择性的κ-阿片样物质激动剂具有强的止痛活性和利尿作用，可用作有用的镇痛和利尿剂。