Kotobuki Pharmaceutical Co Ltd

Kotobuki Seiyaku Co. Ltd.

Kotokuki Seiya Kau Co., Ltd.

Naoto Ueyama

Tsuyoshi Tomiyama

Akira Tomiyama

Motoharu Sonegawa

Tomoyuki Kawai

Takashi Yanagisawa

Akira Ohno

Shuuichi Wakabayashi

Tadashi Shirai

Hiromi Baba

Hiroshi Tomiyama

Yumiko Ichikawa

Masahiro Yanagiya

Satoru Takeuchi

Yasufumi Ohkura

Takeyuki Imamaki

Makoto Haketa

The purposes of this invention are preparation of the non-mucin type synthetic compounds-carrier conjugated compounds which are stable against enzymes, and which have the ability of specific reactivity to induce immune response for cancer and HIV. A compound of the general formula (1),

Non-mucin type synthetic compounds or its carrier conjugated compounds

A method for preparation of a cycloheptimidazole compound having formula (5),

Method for preparing cycloheptimidazoles

The present invention relates to compounds of formula (1).

3-Substituted-2-halocycloheptenone compounds and a method for manufacturing same

New therapeutic agents of isoquinuclidine derivatives are represented by the following formula or its hydrochloride salts. ##STR1## (wherein R.sub.1 is hydrogen, carboxyl group, ethoxycarbonyl group, 4-(ethoxycarbonyl)phenyl group, 4-(carboxy)phenyl group, 2-(carboxy)-thiophene-5-yl group, quinoline-5-yl group, 4-(quinoline-5-yl)phenyl group or 4-(3-oxo-2-azabicyclo[2.2.2]octane-2-yl)-phenyl group; R.sub.2 is hydrogen or allyl group; Both X.sub.1 and X.sub.2 are hydrogen and X.sub.1 and X.sub.2 may form an oxo group; m stands for an integer of 0 to 2.) These compounds, have excellent inhibitory activities against squalene synthase, and are useful as a treatment agent for hypercholesterolemia.

Isoquinuclidine derivatives, method of manufacturing the same and

New therapeutic agent of carboxymethylidenecycloheptimidazole derivatives and method for the manufacture thereof are disclosed, which are represented by the following formula or its alkali addition salts ##STR1## (wherein R.sub.1 represents a lower alkyl; R.sub.2 represents H or isopropyl group; R.sub.3 represent H, a lower alkyl or --C(CH.sub.3)H--OCOOR.sub.4 (R.sub.4 is a lower alkyl or cyclohexyl) and .dbd.CHCOOR.sub.3 is substituted group at 4 or 8 position; A represents ##STR2## These compounds are useful as anti-hypertensive, anti-congestive heart failure agents and intraocular pressure lowering agents.

Carboxymethylidenecycloheptimidazole derivatives, method of

New therapeutic agents of cycloheptimidazole derivatives are disclosed, which are represented by the following formula or its alkali-addition salts. ##STR1## (wherein R.sub.1 represents H or isopropyl group; R.sub.2 represents a lower alkyl; R.sub.3 represents a carboxylic acid or tetrazole group. A and A.sub.1 are substituted groups at 4 or 8 position and A.sub.1 is a hydrogen or hydroxy group when A is a hydrogen or A and A.sub.1 is an oxo group. The dotted line '- - - -' is two double bonds or saturated single bonds). These compounds are useful as anti-hypertensive or anti-congestive heart failure agents.

Cycloheptimidazole derivatives, method of manufacturing the same and

Derivatives of cyclic guanidine are disclosed, which are represented by the following formula:

Cyclic guanidine derivatives, anti-ulceratives and method of

Cyclic guanidine derivatives, anti-ulceratives and methods of

A new series of 1,5-benzothiazepine analogues are disclosed. These compounds are represented by the following general formula: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrogen, a lower alkyl, nitro, amino, lower-alkyl-oxy or halogen group, X represents O or S. These compounds are useful as anti-hypertensive agents.

Growing community of inventors

Ueda, Japan

Naoto Ueyama