Nippon Zoki Pharmaceutical Co., Ltd.

Taisuke Hasegawa

Kaoru Okamoto

Takashi Ogino

Kunihiko Higashiura

Kazuhito Furukawa

Kiyoshi Fukuda

Taizo Ito

Takayuki Kotani

Akio Namimatsu

Hiroki Muramoto

Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent.

Process for producing thiabenzoazulene-propionic acid derivative

Benzothiazole derivatives, pharmaceutically acceptable salts thereof, and therapeutic agents containing said compounds as an effective component possess a lipid lowering activity and are useful pharmaceuticals for the treatment of hyperlipemia. The lipid lowering agents are of the formula: ##STR1## wherein R.sub.1 is halogen, trifluoromethyl, acetamido or --OX.sub.1 ; X.sub.1 is hydrogen, alkyl or acyl; R.sub.2 is hydrogen, halogen, alkyl, hydroxyalkyl, trifluoromethyl, nitro, amino which may be substituted with alkyl or acyl, carboxy which may be esterified with alkyl, or --OX.sub.2 ; X.sub.2 is hydrogen, alkyl, acyl, carboxyalkyl which may be esterified with alkyl; n is an integer from 1 to 3 denoting the number of substituents R.sub.2 ; and plural R.sub.2 may be the same or different when n is 2 or 3; with the proviso that R.sub.1 is a group other than halogen when R.sub.2 is hydrogen. The benzothiazole derivatives and their pharmaceutically acceptable salts significantly decrease cholesterol, triglyceride and low-density lipoprotein in blood.

Benzothiazole derivatives

A rapid-acting remedy for asthma having a bronchodilating action contains at least one pyrido�2,3-d!pyrimidine derivative represented by the general formula (A) or pharmaceutically acceptable salts or metal complexes thereof as an effective component: ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and each of R.sup.1 and R.sup.2 is hydrogen, alkyl or benzyl; R.sup.3 is hydrogen, hydroxyl, dialkylaminomethyleneamino or --NH--X; X is hydrogen, alkyl, alkenyl, hydroxyl, amino, hydroxyalkyl, benzyl or acyl; R.sup.4 is hydrogen, alkyl, halogen, nitro, amino, hydroxyl, benzyloxy, cyano, carboxyl, alkoxycarbonyl, alkoxysulfonyl, aminosulfonyl, dialkylaminosulfonyl or sulfo; and R.sup.5 is hydrogen, alkyl or amino. The rapid-acting remedy for bronchial asthma is capable of relieving the symptom of laboring breath at the onset of asthma due to its excellent bronchodilating action. It can be used as a therapy not only for allergic asthma but also for various bronchial asthmas such as endogenous asthma, exogenous asthma and dust asthma.

Bronchodilating pyrido�2,3-d!pyrimidine derivatives

The present invention provides purine derivatives and pharmaceutically acceptable salts thereof which exhibit an inhibitory action towards nasal mucus secretion and are useful as pharmaceuticals for treatment of nasal secretion and rhinitis. The purine derivatives are represented by the following general formula: ##STR1## wherein R is alkyl or cycloalkyl, or optionally-substituted phenyl or phenylalkyl; R' is hydrogen or --COOX; and X is alkyl, alkenyl, alkoxyalkyl, phenyl or phenylalkyl. The compounds are useful as therapeutic and preventive agents for various types of rhinitis accompanied by acceleration of nasal mucus secretion and by the sneezing reflex such as allergic rhinitis. The compounds may be administered orally and exhibit low toxicity, little side effect and high safety. Accordingly, continuous long term administration of the pharmaceutical compositions may be performed for highly effective treatment of rhinitis.

Growing community of inventors

Katoh-gun, Japan

Taisuke Hasegawa