公开(公告)号：JPS5846492B2

公开(公告)日：1983-10-17

申请号：JP16110278

申请日：1978-12-28

Applicant: UBE INDUSTRIES

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

IPC: C07C51/60 ,  B01J27/00 ,  B01J27/14 ,  C07B61/00 ,  C07C51/00 ,  C07C63/10 ,  C07C63/22 ,  C07C67/00 ,  C07C201/00 ,  C07C205/59

公开(公告)号：JP2012180360A

公开(公告)日：2012-09-20

申请号：JP2012098050

申请日：2012-04-23

Applicant: Ube Industries Ltd ,  Mitsubishi Tanabe Pharma Corp ,  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 ,  A61K31/444 ,  A61K31/445 ,  A61K31/4545 ,  A61P11/00 ,  A61P17/00 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07C303/22 ,  C07C309/29

Abstract: PROBLEM TO BE SOLVED: To provide an (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid benzene sulfonate excellent in anti-histaminic activity and anti-allergic activity.SOLUTION: This (S)-4-[4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidino]butanoic acid benzene sulfonate is synthesized as follows: (±)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine is induced into a diastereomer salt; the salt is subjected to optical resolution using fractional crystallization procedure to obtain an optically active (S)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine; thereafter N-alkylation reaction of piperidine, hydrolysis reaction of ester and further neutralization treatment of benzene sulfonic acid are carried out.

Abstract translation: 待解决的问题：提供抗组氨酸活性和抗过敏活性优异的（S）-4- [4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶子基]丁酸苯磺酸盐 。 解决方案：如下合成（S）-4- [4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶子基]丁酸苯磺酸盐：（±）-4 - [（4-氯苯基 ）（2-吡啶基）甲氧基]哌啶诱导成非对映体盐; 使用分级结晶方法对盐进行光学拆分，得到光学活性的（S）-4 - [（4-氯苯基）（2-吡啶基）甲氧基]哌啶; 然后进行哌啶的N-烷基化反应，酯的水解反应和苯磺酸的进一步中和处理。 版权所有（C）2012，JPO＆INPIT

公开(公告)号：JPH10237070A

公开(公告)日：1998-09-08

申请号：JP35078497

申请日：1997-12-19

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 compound having an excellent stability suitable as a medicine by forming a salt of a specific derivative with benzene sulfonic acid, etc. SOLUTION: This acid adduct salt of an optically active piperidine derivative is an objective salt expressed by the formula and having an absoluyte configuration of (S) compound, preferably (S)-4- 4-[(4-chlorophenyl)(2-pyridyl) methoxy]piperidino}butanoic acid.benzene sulfonic acid salt. Further, in order to obtain the above salt, it is preferable to form the salt by using 0.8-2.5 fold mol of benzene sulfonic acid or benzoic acid based on 1mol of (S)-piperidine derivative expressed by the formula in a solvent such as ethanol a 5-50 deg.C reaction temperature.

公开(公告)号：JPH0225465A

公开(公告)日：1990-01-26

申请号：JP17514288

申请日：1988-07-15

Applicant: UBE INDUSTRIES

Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  TAKAMURA SHINJI ,  YAMANO KAYOKO ,  FUJIWARA HIROSHI

IPC: C07D211/46 ,  A61K31/4427 ,  A61K31/445 ,  A61P37/08 ,  A61P43/00 ,  C07D401/12

Abstract: NEW MATERIAL:A compound expressed by formula I (Ar and Ar are phenyl or phenyl or pyridyl having alkyl substituted by halogen, etc.; A is alkylene or alkenylene; B is alkyl, hydroxy, alkoxy, phenoxy, alkylamino, anilino, phenyl, etc., provided that at least either of Ar and Ar is pyridyl when B is phenyl or alkyl-substituted phenyl) and salts thereof. EXAMPLE:3-[4-[(4-Chlorophenyl)-2-pyridylmethoxy]-1-piperidyl]propionic acid. USE:An antihistaminic and antiallergic medicine. PREPARATION:For example, a compound expressed by formula II is reacted with a compound expressed by formula III (W is eliminative group) to afford the compound expressed by formula I.

公开(公告)号：JPS6348262B2

公开(公告)日：1988-09-28

申请号：JP14245880

申请日：1980-10-14

Applicant: UBE INDUSTRIES

Inventor： FUKUI KYOSHI ,  KITA JUNICHIRO ,  FUJIMURA SUSUMU ,  KAKEYA NOBORU

IPC: C07C255/28 ,  C07C67/00 ,  C07C229/30 ,  C07C229/36 ,  C07C231/10 ,  C07C253/00 ,  C07C255/30 ,  C07C255/42 ,  C07C313/00 ,  C07C327/58

公开(公告)号：JPS6033423B2

公开(公告)日：1985-08-02

申请号：JP11159080

申请日：1980-08-13

Applicant: UBE INDUSTRIES

Inventor： TAWARA SUSUMU ,  NISHIHIRA KEIGO ,  MYATAKE TAKASHI ,  SAWADA HIROYUKI ,  KITA JUNICHIRO

IPC: C07B61/00 ,  B01J23/00 ,  B01J23/40 ,  C07C67/00 ,  C07C209/00 ,  C07C209/26 ,  C07C209/68 ,  C07C211/09

公开(公告)号：JPS607984B2

公开(公告)日：1985-02-28

申请号：JP13233780

申请日：1980-09-25

Applicant: UBE INDUSTRIES

Inventor： FUKUI KYOSHI ,  KAKEYA NOBORU ,  JIBIKI HIROSHI ,  KITA JUNICHIRO

IPC: C07D233/96

公开(公告)号：JPH10120649A

公开(公告)日：1998-05-12

申请号：JP23062997

申请日：1997-08-27

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 ,  A61K31/395 ,  A61K31/397 ,  A61K31/40 ,  A61K31/435 ,  A61K31/439 ,  A61K31/445 ,  A61P7/02 ,  A61P9/10 ,  C07D207/08 ,  C07D207/12 ,  C07D211/54 ,  C07D451/02 ,  C07D451/14

Abstract: PROBLEM TO BE SOLVED: To obtain a new compound having inhibitory actions on platelet coagu lation and arteriosclerosis progression, etc., and being useful as a preventive or treating medicine for embolism and thrombosis. etc. SOLUTION: This compound is shown by formula I [R is a phenyl (substituted with a 1-4C alkyl or the like); R is a 1-8C aliphatic acyl (substituted with OH or the like) etc.; R is a condensed 3- to 7-membered cyclic saturated amino substituted with mercapto or the like], e.g. 1-(α-cyclopropylcarbonyl 1-2-fluorobenzyl)-4mercaptopiperidine. The compound of formula I is obtained by reacting a compound of formula III (R is the R a whose OH, etc., is conferred into a halogen, etc.), which resulted from the reaction between a compound of formula II [R a is the R with a protected OH; R a is a condensed 3- to 7-membered saturated cyclic amino with a substituting OH, etc.] and a halogenating agent, etc., with a compound of the formula M-S-COR (R is a 1-4C alkyl; M is an alkali metal), followed by conducting a treatment as necessary.

公开(公告)号：JPH05294929A

公开(公告)日：1993-11-09

申请号：JP28722891

申请日：1991-10-08

Applicant: UBE INDUSTRIES

Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  TAKAMURA SHINJI ,  YAMANO KAYOKO ,  FUJIWARA HIROSHI

IPC: A61K31/445 ,  A61K31/4465 ,  A61P11/00 ,  A61P17/00 ,  A61P37/08 ,  A61P43/00 ,  C07D211/46

Abstract: PURPOSE:To obtain a new piperidine derivative having strong anti-histamine activity and antiallergic activity and useful as an anti-histamic agent reduced in action enhancing sleepiness. CONSTITUTION:The objective compound of formula I [Ar and Ar are phenyl which may have substituent groups (halogen, NO2, lower alkoxy, lower alkyl or halo-lower alkyl); A is 2-6C linear alkylene or branched linear alkylene having >=2C main chain or alkenylene; B is lower alkyl, OH, lower alkoxy, phenoxy, NH2, lower alkylamino or anilino) or a compound of formula II (Ar and Ar are pyridyl and further, Ar is phenyl which have a substituent group other than halogen; B is above-mentioned B or phenyl which may be substituted with a lower alkyl) or its pharmaceutically permissible acid addition salt, e.g. 4-[4-(diphenylmethoxy)-1-piperidyl]butanoic acid ethyl fumaric acid salt. This compound can readily be produced from a compound of formula III and a compound of formula IV (W is eliminable group).

公开(公告)号：JPH0533953B2

公开(公告)日：1993-05-20

申请号：JP17514288

申请日：1988-07-15

Applicant: UBE INDUSTRIES

Inventor： EDA SHOEI ,  KITA JUNICHIRO ,  TAKAMURA SHINJI ,  YAMANO KAYOKO ,  FUJIWARA HIROSHI

IPC: C07D211/46 ,  A61K31/4427 ,  A61K31/445 ,  A61P37/08 ,  A61P43/00 ,  C07D401/12