Yamasa Shoyu Kabushiki Kaisha

Yoshitomi Pharmaceutical Industries, Ltd.

Yamasa Corporation

Yamasa Shoyu Co., Ltd.

Other

Toa Eiyo Ltd.

Yamasa Shuyu Kabushiki Kaisha

Shinji Sakata

Takanori Miyashita

Haruhiko Machida

Akira Matsuda

Takuma Sasaki

Tohru Ueda

Akihiro Fujii

Tetsuro Fujishima

Masahiro Imaizumi

Kazuhiko Kondo

Kentaro Kogi

Keiji Yamagami

Toichi Abiru

Toyofumi Yamaguchi

Manami Morozumi

Yuichi Yoshimura

Takashi Ono

Toshiyuki Shibata

Fumitaka Kano

Mikari Watanabe

Atsushi Sakai

Noriyuki Ashida

Takayuki Ogawa

Katsushi Ijichi

Satoshi Shutou

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

Antineoplastic

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

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

Novel stable, non-hygroscopic 2'-deoxy-2'-methylidenecytidine dihydrate and its methods for production, and compositions with improved solubility containing same and saccharide(s).

2'-deoxy-2'-methylidenecytidine dihydrate, methods for its production

Anxiolytic drugs

1-amino-5-halogenouracils, process for their preparation, and central

Pyrimidine 2'-deoxy-2'-methylidene nucleoside compounds: ##STR1## wherein R.sup.1 represents amino, hydroxy, silylamino, silyloxy, acylamino or acyloxy; R.sup.2 represents hydrogen, halogen, a lower alkyl, a lower alkenyl, a lower alkynyl or haloalkyl; R.sup.3 and R.sup.4 represent the same or different hydrogen, silyl, acyl or aminoacyl, or a pharmaceutically acceptable salt or hydrate thereof, except that R.sup.1 is amino or hydroxy, and both of R.sup.3 and R.sup.4 are hydrogen. Said compounds possess excellent antitumor and antiviral activities, thus providing novel anticancer and antiviral agent.

Pyrimidine 2'-methylidene nucleoside compounds

The invention is directed to a microbially pure culture of Brevibacterium acetylicum AT-6-7, ATCC 39311 or a mutant thereof which has nucleoside phosphorylase activity.

Pure culture of Brevibacterium acetylicum AT-6-7, ATCC 39311

Nucleoside 5'-alkyl- or alkenyl phosphate compounds represented by the following formula [I] ##STR1## wherein B is a purine base having a substituent or a 5-substituted uracil base, and R.sup.1 is an alkyl or alkenyl group having 14 to 26 carbon atoms, and pharmaceutically acceptable salts thereof are novel derivatives of arabinonucleosides which can have properties suitable for clinical application as antiviral agents, particularly for treating viral hepatitis.

Nucleoside 5'-alkyl- or alkenylphosphate

Glycosylation or transglycosylation of a specified guanine derivative, namely 9-substituted or non-substituted guanine of formula [I] with a 3-deoxyribose donor such as 3'-deoxyadenosine in the presence of a nucleoside phosphorylase source such as of microorganism origin is disclosed.

Process for producing 3-deoxyguanosine

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

Growing community of inventors

Choshi, Japan

Shinji Sakata