Yamasa Shoyu Kabushiki Kaisha

Yamasa Corporation

Yamasa Shuyu Kabushiki Kaisha

Haruhiko Machida

Akira Matsuda

Shinji Sakata

Tohru Ueda

Yuichi Yoshimura

Kenji Takenuki

Mikari Watanabe

Hiroaki Mitsuya

Hiroshi Ohrui

Shiro Shigeta

Satoru Kohgo

Eiichi Kodama

Tadashi Miyasaka

Toichi Abiru

Kohei Yamada

Hitoshi Kusakabe

Akira Kuninaka

Hiroshi Yoshino

Kenjiro Kodama

Kenji Kitano

Fumitaka Kano

Shinji Miura

Noriyuki Ashida

Katsushi Ijichi

Yuichirow Midorikawa

4&prime;-C-ethynyl pyrimidine nucleosides and pharmaceutical compositions thereof

The invention provides 4&prime;-C-ethynyl pyrimidine nucleosides (other than 4&prime;-C-ethynylthymidine) represented by formula &lsqb;I&rsqb;:

4&prime;-C-ethynyl pyrimidine nucleoside compounds and pharmaceutical compositions

1-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)cytosine

9-(2-deoxy-2-fluoro-4-thio-beta-D-arabinofuranosyl)purine derivatives

The present invention provides a novel purine 4'-thioarabinonucleoside represented by the following formula �1!: ##STR1## wherein B represents a purine base other than adenine. Also disclosed are a method for preparing the purine 4'-thioarabinonucleoside and pharmaceutical compositions containing the purine 4'-thioarabinonucleoside.

Purine 4'-thioarabinonucleosides

The present invention relates to a novel 1-.beta.-D-arabinofuranosyl-(E)-5-(2-halogenovinyl)uracil derivative represented by the following formula (I), whose concentration in blood as XVAU can be kept high for many hours when it is administered orally. The present invention also relates to an antiviral agent comprising as an active ingredient the compound of the present invention. Further, the present invention relates to a method for treating viral diseases which comprises administering to a patient with a viral disease a safe and effective amount of the compound of the present invention. ##STR1## wherein X represents a halogen; and R.sup.1, R.sup.2, and R.sup.3, which may be the same or different, each represent a hydrogen atom, a lower alkyl group or an aralkyl group, provided that R.sup.1, R.sup.2 and R.sup.3 are not hydrogen at the same time.

1-.beta.-D-arabinofuranosyl-(E)-5-(2-halogenovinyl)uracil derivatives

Disclosed are novel 2'-alkylidenepyrimidine nucleoside derivatives represented by formula [I]: ##STR1## R.sup.1 is an amino group or a hydroxy group, R.sup.2 is a hydrogen atom, a halogen atom or a lower alkyl group, R.sup.3 is a hydrogen atom or a lower alkyl group, and R.sup.4 is a hydrogen atom or a phosphate residue, or salts thereof. These novel compounds can be produced from uridine or cytidine derivatives by alkylidenating the 2'-position in the sugar moiety thereof with Wittig's reagent. Furthermore, the compounds have remarkable antiviral activities and therefore can provide novel antiviral agents.

2'-alkylidenepyrimidine nucleoside derivatives, process for production

Disclosed are novel 2'-alkylidenepyrimidine nucleoside derivatives represented by formula [I]: ##STR1## wherein R.sup.1 is an amino group or a hydroxy group, R.sup.2 is a hydrogen atom, a halogen atom or a lower alkyl group, R.sup.3 is a hydrogen atom or a lower alkyl group, and R.sup.4 is a hydrogen atom or a phosphate residue, or salts thereof. These novel compounds can be produced from uridine or cytidine derivatives by alkylidenating the 2'-position in the sugar moiety thereof with Wittig's reagent. Furthermore, the compounds have remarkable antiviral activities and therefore can provide novel antiviral agents.

2'-alkylidenepyrimidine nucleoside compounds and a process 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

1-.beta.-D-arabinofuranosyl-(E)-5-(2-halogenovinyl)uracil-5'-phosphates of the formula (I): ##STR1## and wherein X is halogen, pharmaceutically acceptable salts thereof, are produced by phosphorylation of the non-phosphorylated precursors of the compounds (I), and are useful as anti-viral agents.

1-.beta.-D-Arabinofuranosyl-(E)-5-(2-halogenovinyl)-uracil-5'-phosphate,

A novel compound, (E)-5-(2-halogenovinyl)-arabinofuranosyluracil; a process for producing the same comprising reacting 5-vinylarabinofuranosyluracil with a halogen; and use of the same as an anti-DNA virus agent, especially anti-herpes virus agent and anti-varicella-zoster virus agent.

(E)-5-(2-Halogenovinyl)-arabinofuranosyluracil, process for preparation

An antiviral agent comprising 1-.beta.-D-arabinofuranosylthymine as a therapeutically efficacious component in a pharmaceutical form for absorption through the alimentary canal of the human or lower animal to be treated.

Antiviral agent comprising 1-.beta.-D-arabinofuranosylthymine

The enzyme pterin deaminase may be used as an antitumor agent, and can be produced from cultures of the fungal genera Aspergillus, Mucor, Rhizopus, and Penicillium.

Process for producing pterin deaminases having antitumor activity

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Choshi, Japan

Haruhiko Machida