PHARMACEUTICAL COMPOUND - LILLY INDUSTRIES LTD

Title:

PHARMACEUTICAL COMPOUND

Document Type and Number:

Japanese Patent JP2527860

Kind Code:

B2

Abstract:

PURPOSE: To provide a novel compd. which is useful for treating diseases of central nervous system as a latent psychorelaxant which exhibits relaxing, anxiety-removing, or antiemetic action and is highly active while hardly causing side effects.
CONSTITUTION: This compd. is 2-methyl -10 -(4 -methyl-1 -piperazinyl) -4H-thieno -[2,3-b][1,5]benzodiazepine of formula I or a salt thereof and is prepd. by reacting N-methylpiperazine with a compd. of formula II (wherein Q is a cleavable group) (pref. 4-amino -2 -methyl -10H -thieno[2,3 -b]benzodiazepine) at 50-200°C, pref. in the presence of titanium tetrachloride. A compd. of formula II wherein Q is -NH2, -OH, or -SH and a salt of a compd. of formula II wherein Q is -NH2 are novel substances and are obtd. pref. by catalytically reducing a novel nitro compd. of formula III (wherein R is an ester group) obtd. by reacting thiophene with o-fluoronitrobenzene or o-chloronitrobenzene.

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Inventors:

CHAKRABARTI JIBAN KUMAR (GB)
HOTTEN TERRENCE MICHAEL (GB)
TUPPER DAVID EDWARD (GB)

Application Number:

JP22821591A

Publication Date:

August 28, 1996

Filing Date:

April 24, 1991

Export Citation:

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Assignee:

LILLY INDUSTRIES LTD (GB)

International Classes:

A61K31/55; A61P1/08; C07D495/06; A61P25/02; A61P25/18; A61P25/20; A61P43/00; C07D241/04; C07D243/12; C07D333/20; C07D333/38; C07D495/04; C07D513/04; C07D; (IPC1-7): C07D495/04; A61K31/55

Attorney, Agent or Firm:

中村稔（外７名）

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