Mitsubishi Kasei Corporation

Mitsubishi Chemical Industries Limited

Mitsubishi Chemical Corporation

Arakawa Chemical Industries, Ltd.

Mistubishi Kasei Corporation

Akihiro Tobe

Ryoji Kikumoto

Kunihiro Ninomiya

Yasuhiro Morinaka

Issei Nitta

Mamoru Sugano

Hidenobu Ikoma

Shinji Tonomura

Mitsuo Egawa

Satoshi Yamazaki

Yoshikuni Tamao

Ryoichi Ando

Chizuko Takahashi

Harukazu Fukami

Shinichiro Fujimori

Ken-Ichi Saito

Naoko Ando

Shuji Morita

Akira Maruyama

Tomoko Bessho

Hirokazu Masuda

Heitaro Iwata

Toshio Matsuda

Akemichi Baba

Shigeru Ogawa

Kunihiro Ninomiya, Deceased

Haruko Harada

Ken-ichi Saito

Kenichi Saito

Tomoshi Yamazaki

Makoto Kawamura

Toshiro Sasaki

Hiromi Okushima

Makio Kobayashi

Tetsuro Shimpuku

Junko Hayashi

Youichirou Ezaki

Asami Seino

Tadashi Tanaka

Tomoko Tamura

Kazuo Honda

Mariko Kitsukawa

Hideki Bessho

Kozue Enda

Kohtaro Matsuo

Ken-ichi Sato

A pharmaceutical composition for treating hyperkinetic disorders, which contains as an active ingredient an effective amount of 2-(4-methylamino butoxy)diphenylmethane, is provided. A method of treating hyperkinetic disorders with said pharmaceutical composition and use of said diphenylmethane for preparing said composition are also provided.

Treatment of hyperkinetic disorders

A novel 4-acylaminopyridine derivative represented by the following formula (I) is disclosed. ##STR1## The 4-acylaminopyridine derivative of the present invention is useful as a medicine for treating disturbances of memory such as senile dementia and Alzheimer's disease, since it has an action of directly activating malfunctioned cholinergic neuron.

4-Acylaminopyridine derivative

A novel ketone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Ketone derivatives

A novel cinnoline derivative having an antagonistic activity against serotonin 5-HT.sub.3 receptor, its pharmaceutically acceptable salts, its N-oxide derivatives or solvates thereof, and pharmaceutical formulations containing the same for the prevention and/or treatment of various disorders such as nausea and/or emesis caused by anticancer drugs or X-ray treatment, central nervous disorders such as anxiety and/or neuropathy, gastroenteric diseases such as indigestion, chronic gastritis, digestive ulcer, irritable bowel syndromes and the like, hemicrania, cluster headache, trigeminal neuralgia, arrhythmia and the like.

Cinnoline-3-carboxylic acid derivatives

4-acylaminopyridine derivative

Aminoketone derivatives according to the present invention strongly inhibit thiol protease such as calpain, papain, cathepsin B, cathepsin H, cathepsin L or the like and have excellent properties concerning absorbance on oral administration, tissue distribution and cell membrane permeability. The aminoketone derivatives cart thus be used as therapeutic agents for treating muscular dystrophy, cataract, cardiac infarction, stroke, Alzheimer's disease, amyotrophy, osteoporosis and hypercalcemia and so on. It may also be used as therapeutic agents for preventing metastasis of cancer. In addition, the present derivatives are also applicable as intermediates for the preparation of ketone derivatives, which have inhibitory activity against thiol protease.

Aminoketone derivatives

A novel cyclopropenone derivative (I) which possesses a potent inhibitory activity against thiol protease such as papain, cathepsin B, cathepsin H, cathepsin L, calpain or the like with excellent properties regarding oral absorbance, tissue transference and cell membrane permeability, and are clinically useful in the treatment of various diseases such as muscular dystrophy, amyotrophy. Also provided are a process for producing the compound (I) and a pharmaceutical composition containing the same.

Cyclopropenone derivatives

The thieno[3.2-b]pyridine derivative of the present invention promote the gastric emptying in male ddy mice and the gastric contraction in dogs sutured with a strain-gauge transducer. It is believed that the derivatives have the action to enhance gastric motor action and gastric emptying. Therefore, the compound of the present invention are effective for the prevention and therapeutical treatment of the symptoms caused by gastric hypanakinesis, such as heartburn, abdominal distension feeling, anorexia, unpleasant feeling on upper abdomen, abdominalgia, nausea, vomiting, etc. caused by the underlying diseases such as acute and chronic gastritis, stomach and duodenum ulcer, gastroneurosis, gastroptosis, etc. The present invention also encompasses a pharmaceutical composition containing as the effective ingredient a compound of the present invention, and a method for producing the same.

Thieno[3,2-b]pyridine derivatives

Disclosed are antihypertensive pharmaceutical compositions and compounds which include the thiocarbamoylacetonitrile having the formula: ##STR1## wherein: R.sup.1 is selected from the group consisting of hydrogen, a C.sub.1 to C.sub.6 alkyl, a C.sub.3 to C.sub.6 cycloalkyl or --(CH.sub.2).sub.n --A (where A is selected from the group consisting of a C.sub.6 to C.sub.12 aryl, a 5- or 6-membered heterocyclic group or a fused heterocyclic group constituted by 9 or 10 atoms, each of which may be substituted by at least one substitute group selected from a C.sub.1 to C.sub.6 alkyl and a halogen and n is 0 or an integer of 1 to 6),

Antihypertensive thiocarbamoylascetonitrile compounds

Optically active alkylenedioxybenzene derivatives of the formula: ##STR1## wherein m is an integer of 2-5, and n is an integer of 1-3, and acid addition salts thereof. A pharmaceutical composition containing a compound (I) or racemate, and a method of treating anxiety in a warm-blooded animal by administering the above compound (I) to said animal are also provided.

Optically active alkylenedioxybenzene derivatives and their use in

Disclosed herein are anxiolytic drugs containing as an active ingredient a piperazine derivative represented by the following general formula (I): ##STR1## wherein m represents an integer from 2 to 4,

Anxiolytic drug

Growing community of inventors

Yokohama, Japan

Akihiro Tobe