Yoshitomi Pharmaceutical Industries, Ltd.

Yamasa Corporation

Yamasa Shoyu Kabushiki Kaisha

Yamasa Shoyu Co., Ltd.

Other

Toa Eiyo Ltd.

Takanori Miyashita

Shinji Sakata

Akira Matsuda

Takuma Sasaki

Tohru Ueda

Toichi Abiru

Akihiro Fujii

Toyofumi Yamaguchi

Kazuhiko Kondo

Keiji Yamagami

Kentaro Kogi

Takashi Ono

Toshiyuki Shibata

Hiroshi Sato

Yutaka Noda

Hideaki Maeda

Atsushi Sakai

Takayuki Ogawa

Satoshi Shutou

Kenya Mori

Yohko Watanabe

The present invention is directed to crystals of P -(2&prime;-deoxycytidine 5&prime;-)P -(uridine 5&prime;-)tetraphosphate (dCP4U) or a salt thereof and to a process for producing the crystals. The present invention also provides a process for producing dCP4U involving reacting uridine 5&prime;-monophosphate (UMP), 2&prime;-deoxycytidine 5&prime;-monophosphate (dCMP), diphenyl phosphorochloridate (DPC), and pyrophosphate (PPi). The crystals of dCP4U obtained through the process according to the present invention have high purity and high stability and no hygroscopicity as compared with a freeze-dried product, and thereby serve as a useful raw material for preparing a pharmaceutical. The process for producing dCP4U according to the present invention permits use of inexpensive UMP as a raw material and realizes high yield. Thus, the process is suitable for large-scale synthesis of dCP4U.

Dinucleotide tetraphosphate crystals

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

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

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

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

Growing community of inventors

Choshi, Japan

Takanori Miyashita