公开(公告)号：JPS645592B2

公开(公告)日：1989-01-31

申请号：JP15807681

申请日：1981-10-06

Applicant: UBE INDUSTRIES

Inventor： FUKUI KYOSHI ,  KITA JUNICHIRO ,  FUJIMURA SUSUMU ,  MATSUO FUMIO

IPC: C07D207/456 ,  A01N37/32

公开(公告)号：JPS642098B2

公开(公告)日：1989-01-13

申请号：JP16360379

申请日：1979-12-18

Applicant: UBE INDUSTRIES

Inventor： FUKUI KYOSHI ,  KITA JUNICHIRO ,  JIBIKI HIROSHI ,  KAKEYA NOBORU ,  FUJIMURA SUSUMU ,  OKIMOTO KYOMI

IPC: C07B61/00

公开(公告)号：JPS641463B2

公开(公告)日：1989-01-11

申请号：JP14777879

申请日：1979-11-16

Applicant: UBE INDUSTRIES

Inventor： FUKUI KYOSHI ,  OKIMOTO KYOMI ,  KITA JUNICHIRO ,  SUGIHARA HIROSHI ,  FUJIMURA SUSUMU ,  KAKEYA NOBORU

IPC: C07B61/00

公开(公告)号：JPS6021142B2

公开(公告)日：1985-05-25

申请号：JP5439477

申请日：1977-05-13

Applicant: UBE INDUSTRIES

Inventor： MAZAKI MITSUO ,  FUKUI KYOSHI ,  KITA JUNICHIRO

IPC: C07D201/02

公开(公告)号：JPS5111772A

公开(公告)日：1976-01-30

申请号：JP8231074

申请日：1974-07-19

Applicant: UBE INDUSTRIES

Inventor： MAZAKI MITSUO ,  KITA JUNICHIRO ,  MATSUNAMI SATOSHI ,  FUJIMURA SUSUMU

IPC: A01N59/16 ,  A61K31/555 ,  A61P17/00 ,  C07D213/70 ,  C07D213/75 ,  C07D213/80 ,  C07F7/22 ,  C08K5/37

公开(公告)号：JP2011063619A

公开(公告)日：2011-03-31

申请号：JP2010264019

申请日：2010-11-26

Applicant: Mitsubishi Tanabe Pharma Corp ,  Ube Industries Ltd ,  宇部興産株式会社 ,  田辺三菱製薬株式会社

Inventor： KITA JUNICHIRO ,  FUJIWARA HIROSHI ,  TAKAMURA SHINJI

IPC: C07D401/12 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4545 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To provide a benzenesulfonic acid salt of (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid having excellent antihistaminic activities and antiallergic activities, and to provide a process for producing the salt. SOLUTION: The process for producing the optically active substance compound represented by formula (IV) includes deriving (±)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine into a diastereomer salt, and optically resolving the resultant diastereomer salt by a method for fractional crystallization. COPYRIGHT: (C)2011,JPO&INPIT

Abstract translation: 待解决的问题：提供具有优异的抗组胺活性和抗过敏活性的（S）-4- [4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶子基]丁酸的苯磺酸盐，以及 以提供生产盐的方法。 解决方案：由式（IV）表示的光学活性物质化合物的制备方法包括将（±）-4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶衍生成非对映异构体盐，并光学拆分 通过分级结晶的方法得到的非对映异构体盐。 版权所有（C）2011，JPO＆INPIT

公开(公告)号：JP2000198784A

公开(公告)日：2000-07-18

申请号：JP2000032961

申请日：2000-02-10

Applicant: UBE INDUSTRIES ,  TANABE SEIYAKU CO

Inventor： KITA JUNICHIRO ,  FUJIWARA HIROSHI ,  TAKAMURA SHINJI

IPC: C07D401/12 ,  A61K31/4427 ,  A61K31/445 ,  A61K31/4545 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00

Abstract: PROBLEM TO BE SOLVED: To obtain the subject new compound excellent in antihistaminic activity and antiallergic activity, having a few hygroscopic property, excellent in physicochemical property and useful as a medicine. SOLUTION: This new compound is benzenesulfonic acid salt of a compound represented by formula I. The new compound is preferably obtained by subjecting 1 mol compound of formula I to salt formation reaction with 0.9-1.2 mol benzenesulfonic acid in a solvent such as ethyl acetate, preferably at 10-35 deg.C. The solvent is preferably used in an amount of 1 to 10 L based on 1 mol compound of formula I. The temperature at salt deposition is preferably -10 to 15 deg.C. The compound of formula I is obtained by reacting an optically active (S)-4-[(4-chlorophenyl) (2-pyridyl)methoxy]piperidin with a compound of formula II (W is an eleiminable group; R is a lower alkyl) (e.g. ethyl 4- bromobutanoate) in an inert solvent in the presence of a base and then subjecting the resultant compound of formula III to hydrolysis reaction.

公开(公告)号：JPH11315020A

公开(公告)日：1999-11-16

申请号：JP4963899

申请日：1999-02-26

Applicant: SANKYO CO ,  UBE INDUSTRIES

Inventor： ASAI FUMITOSHI ,  SUGIDACHI KAZUHIRO ,  IKEDA TOSHIHIKO ,  KOIKE HIROYUKI ,  INOUE TERUHIKO ,  TAKADA KATSUNORI ,  IWAMURA AKIRA ,  KITA JUNICHIRO ,  YONEDA KENJI

IPC: C07D205/04 ,  A61K31/00 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K31/435 ,  A61K31/445 ,  A61K31/46 ,  A61P7/00 ,  A61P7/02 ,  A61P9/00 ,  A61P9/10 ,  C07D207/12 ,  C07D211/20 ,  C07D211/54 ,  C07D211/72 ,  C07D451/02 ,  C07D451/04

Abstract: PROBLEM TO BE SOLVED: To obtain a medicine useful for a prophylactic or therapeutic agent of embolism, thrombosis or arteriosclerosis by including a specific cyclic amine derivative having an excellent blood platelet coagulation inhibiting action or arteriosclerosis exacerbation suppressing action. SOLUTION: This medicine includes the cyclic amine derivative expressed by formula I (R is phenyl; R is 1 to 8C aliphatic acyl, benzoyl or the like; R is a substituted 3 to 7 membered saturated cyclic amine which is substituted with mercapto or a mercapto substituted with an 1 to 4C alkyl or the like) or its salt. 1-(α-Cyclopropylcarbonyl-2-fluorobenzyl)-4-mercaptopiperidine or the like is preferred as the compound of formula I. The compound of formula I is obtained by reacting a compound of formula II (R a is the same as R excluding that the hydroxyl group of the R is protected; R a partially differs from R as to its substituent) with a halogenating agent such as carbon tetrabromide or the like then reacting with a compound of the formula: M- S-COR (M is an alkali metal; R is 1 to 4C alkyl).

公开(公告)号：JPH04182467A

公开(公告)日：1992-06-30

申请号：JP30719090

申请日：1990-11-15

Applicant: UBE INDUSTRIES

Inventor： KITA JUNICHIRO ,  TAKAMURA SHINJI ,  YAMANO KAYOKO ,  FUJIWARA HIROSHI ,  HONDA HIROKO ,  TANAKA KUMIKO

IPC: A61K31/4427 ,  A61K31/443 ,  A61K31/445 ,  A61K31/451 ,  A61P37/08 ,  C07D211/46 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D405/14

Abstract: NEW MATERIAL:A compound of formula I [Ar , Ar are phenyl or pyridyl which can be substituted; X is 1-10C alkylene, group of formula II (n is 1-8); Y is O, CONH; Z is halogen, alkyl, phenyl substituted with OH, CN, etc., group of formula III or IV (R is H, alkyl, OH, etc.; R is carboxyl, CN, phenyl, tetrazolyl, etc.; R is H, alkyl; R is H, alkoxycarbonyl)] and a salt thereof. EXAMPLE:1-[3-(4-Acetyl-3-hydroxy-2-n-propylphenoxy)propyl]-[(4-chlorop henyl-2- pyridylmethoxy]piperidine.fumaric acid salt. USE:A medicine having anti-histamine activity and anti-leukotriene activity. PREPARATION:For example, a compound of formula V is reacted with a compound of formula W-X-Y-Z (W is Cl, Br, methanesulfonyloxy) to obtain the compound of formula I.

公开(公告)号：JPH0257062B2

公开(公告)日：1990-12-03

申请号：JP7290784

申请日：1984-04-13

Applicant: UBE INDUSTRIES

Inventor： FUKUI KYOSHI ,  KITA JUNICHIRO

IPC: C07C257/14 ,  C07C67/00 ,  C07C239/00