Yoshitomi Pharmaceutical Industries, Ltd.

Sumitomo Pharmaceuticals Company Limited

Yamasa Shoyu Co., Ltd.

Sankyo Company, Limited

Yamasa Corporation

Yamasa Shoyu Kabushiki Kaisha

Other

Taiho Pharmaceutical Company Limited

Takuma Sasaki

Akira Matsuda

Tohru Ueda

Akihiro Fujii

Keiji Yamagami

Shinji Sakata

Takanori Miyashita

Mitsuaki Maeda

Noriaki Minakawa

Yoshikazu Yanagi

Tomoyuki Shibata

Masakatsu Kaneko

Tomowo Kobayashi

Hitoshi Hotoda

Yoshihiro Mitsuhashi

Yuichi Yoshimura

Takashi Ono

Shinji Miura

Tohru Ueda, Deceased

Satoshi Shutou

Hiroshi Satoh

Masatomo Nojima

Liposoluble platinum (II) complex and preparation thereof

Ozonide compounds with inhibitory activity for urokinase production and angiogenesis

2'-deoxy-2'-(substituted or unsubstituted)methylidene-4'-thionucleosides

2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, anticancer compositions containing one or more of these compounds and methods for production of these compounds. Said compounds and salts thereof exhibit noticeable antitumor activities and are useful as anticancer agents.

2'-methylidenepyrimidine nucleoside compounds

Antineoplastic

Compounds of formula (I): ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from the group consisting of hydrogen atoms, optionally substituted alkanoyl groups and alkenylcarbonyl groups, PROVIDED THAT at least one of R.sup.1, R.sup.2 and R.sup.3 represents an unsubstituted alkanoyl group having from 5 to 24 carbon atoms, said substituted alkanoyl group or said alkenylcarbonyl group; and one of R.sup.4 and R.sup.5 represents a hydrogen atom and the other represents a cyano group; have valuable anti-tumor activity.

Pyrimidine nucleoside derivatives having anti-tumor activity, their

The pyrimidine compounds of the present invention are represented by the following formula: ##STR1## and pharmaceutically acceptable salts thereof, wherein, R.sup.1 represents a hydroxyl or an amino which may be substituted by an acyl group; R.sup.2 represents a hydrogen atom or an alkyl having 1 to 4 carbons; R.sup.3 represents a hydrogen or a hydroxyl; and R.sup.4 and R.sup.5 each represent a hydrogen or together form a group --R.sup.6 R.sup.7 Si--O--SiR.sup.6' R.sup.7' --, wherein R.sup.6, R.sup.7, R.sup.6' and R.sup.7' are the same or different from one another and each represent an alkyl having 1 to 4 carbons. The compounds of the present invention exhibit an excellent antitumor effect.

2'-Cyano pyrimidine nucleoside compounds

2'-Methylidenepyrimidine nucleoside compounds of the general formula: ##STR1## wherein R.sup.1 stands for amino or hydroxy group; R.sup.2 stands for a halogen or a lower alkyl when R.sup.1 is amino or R.sup.2 stands for an alkyl having 2 to 4 carbon atoms, an alkynyl having 2 to 4 carbon atoms or a haloalkyl when R.sup.1 is hydroxy group; and R.sup.3 stands for hydrogen or a phosphoric acid residue, or salts thereof, compositions containing one or more of these compounds and methods for production of these compounds are disclosed. Said compounds and salts thereof exhibit noticeable antitumor activities.

2'methylidenepyrimidine nucleoside compounds, their use and method for

Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl. Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position. Furthermore, the compounds have remarkable antitumor activities and therefore can provide novel antitumor agents.

Imidazole derivatives and use thereof

Disclosed are imidazole derivatives represented by formula [I]: ##STR1## wherein R is a hydrogen atom or ##STR2## wherein R.sup.2 is a hydrogen atom or a hydroxy protecting group, R.sup.2 protecting either a single hydroxy or two hydroxies together when R.sup.2 is a hydroxy protecting group, and R.sup.3 is a hydrogen atom or OR.sup.2 ; A is CONH.sub.2 or CN; and R.sup.1 is a hydrogen atom, lower alkyl, hydroxy lower alkyl, or phenyl. Also disclosed are six processes for producing these novel compounds among which a typical process comprises reacting a starting imidazole compound having a halogen at the 5-position thereof with an acetylene derivative to alkynylate the 5-position. Furthermore, the compounds having remarkable antitumor activities and therefore can provide novel antitumor agents.

Imidazole derivatives, process for production thereof, and use thereof

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

New delivatives of platinum (IT) complex which are liposoluble and applicable as antibacterial agents or anticancer agents specific to the affected parts of patients and selectively transferred to the parts when they are used in combination with lipidol, the delivatives being represented by the general formula of: ##STR1## (wherein R.sub.1 and R.sub.2 each stands for a ligand ammine which may have an organic substituent or may be bonded to each other through a bivalent organic group and R.sub.3 represents a bile acid residue). These delivatives being prepared by nitrifying a cis-dichloro-di-(substituted or unsubstituted)-ammine platinum (II) and then reacting the resulting aqua type product with a corresponding alkali metal salt of bile acid.

Growing community of inventors

Kanazawa, Japan

Takuma Sasaki