Yamasa Shoyu Kabushiki Kaisha

Toa Eiyo Ltd.

Yamasa Corporation

Other

Toichi Abiru

Akira Matsuda

Toyofumi Yamaguchi

Kentaro Kogi

Kazuki Endo

Tohru Ueda

Junzo Kamei

Takanori Miyashita

Tadashi Miyasaka

Haruhiko Machida

Shinji Sakata

Takashi Konno

Tomokazu Hosokawa

Miwa Misawa

Yohko Watanabe

The present invention relates to an agent for the prophylaxis or treatment of diabetic neuropathy, which contains cytidine 5'-diphosphocholine (CDP-choline) as an active ingredient. The agent for the prophylaxis or treatment of diabetic neuropathy of the present invention is effective for neuropathy mainly caused by metabolic disturbance of carbohydrate and is also superior in safety. Neuropathy includes peripheral neuropathy and dysautonomia. CDP-choline is effective even by oral administration.

Pharmaceutical composition for diabetic neuropathy

Medicinal composition for diabetic neuropathy

Medicinal compositions for treating eye diseases which contain as the active ingredient 2-alkynyladenosine derivatives having an acetylene union at the 2-position of adenine base. Having a long-lasting and remarkable effect of lowering ocular tension, these compositions are useful as remedies for eye diseases accompanying increased ocular tension or optic nerve failures, such as glaucoma and hypertonia oculi.

Medicinal compositions for treating eye diseases

The present invention relates to a novel compound represented by the following formula [I] which is useful as a synthetic intermediate of a 2-alkynyladenosine. The present invention also relates to a process for producing the compound and a process for producing a 2-alkynyladenosine [IV] by way of the compound. Further, the present invention relates to a 2-alkynyladenosine derivative represented by the following formula [V] having excellent storage stability and, to a method of storing the 2-alkynyladenosine in the form of that derivative. ##STR1## [I] A=a leaving group, [II] A=NH.sub.2, [V] A=NHR.sup.4, wherein R.sup.1 through R.sup.4 represent a hydrogen atom or a protective group, and n denotes an integer of 1 to 15, provided that R.sup.1 through R.sup.4 do not represent a hydrogen atom simultaneously.

Process for preparing synthetic intermediates of 2-alkynyladenosines and

Tri-O-acetyl-2-alkynyladenosines

Therapeutic 2-alkynyl adenosine agent for ischemic diseases of the heart

Disclosed herein are a novel 2-substituted adenosine derivative having the following formula [I] ##STR1## wherein R represents a hydrogen atom or a hydroxyl group, m is an integer of 2 to 7, n is 0 or an integer of 1 to 3, and R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each independently represent a hydrogen atom, a hydroxy protective group or a phosphoric acid residue, and salts thereof. The above compounds are excellent in a circulation ameliorating effect such as a vasodepressor activity, and have high selectivity for A.sub.2 receptors, but cause less undesirable side effects such as a suppresssive effect on the heart. They are therefore effective when used in pharmaceutical compositions for circulatory diseases.

2-substituted adenosine derivatives and pharmaceutical compositions for

A 2-alkynyladenosine represented by general formula [I]: ##STR1## wherein n is an integer of from 2 to 15, has been found to have excellent properties as an antihypertensive agent. On the basis of this finding, the present invention has provided an antihypertensive agent comprising an antihypertensive effective amount of a compound of the above formula [I] and a pharmaceutically acceptable carrier. The present invention also discloses a novel compound 2-alkynyladenosine of formula [I] shown above wherein n is 6 to 15.

2-alkynyladenosines as antihypertensive agents

Growing community of inventors

Sawara, Japan

Toichi Abiru