Daiichi Pharmaceutical Co., Ltd.

Daiichi Seiyaku Co., Ltd.

Tsunehiko Soga

Hirofumi Terasawa

Takashi Ishiyama

Tsuneo Kusama

Makoto Sato

Makoto Takemura

Tetsuo Shiba

Hiroo Matsumoto

Toshiyuki Nishi

Kunio Higashi

Kiyoshi Nakayama

Kouichi Uoto

Yasuyuki Takeda

Akiko Tohgo

This invention is to provide a novel taxol derivative useful as an antitumor compound having respective substituent groups, represented by the following formula (I) which can be orally administered

Pentacyclic taxan compound

Pentacyclic Compound

Pentacyclic compound

The present invention relates to a novel taxol derivative having an antitumor-activity which is represented by formula (1).

Deacetoxytaxol derivatives

A compound represented by formula (I): ##STR1## wherein R.sup.1 represents --CO--Z.sup.1 --N(Z.sup.11)--CO--Z.sup.2 --H or --CO--Z.sup.3 --H, wherein Z.sup.1, Z.sup.2, and Z.sup.3 each represent an alkylene group having from 1 to 20 carbon atoms, a phenylene group, or a combination thereof, and Z.sup.11 represents a hydrogen atom, an alkyl group having from 1 to 20 carbon atoms which may be substituted with a phenyl group, a phenyl group which may be substituted with an alkyl group having from 1 to 20 carbon atoms, or an alkylene group having from 1 to 20 carbon atoms which may contain therein a phenylene group; R.sup.2 represents --CO--Z.sup.4 --N(Z.sup.12)--CO--Z.sup.5 --H, --CO--Z.sup.6 --H or a hydrogen atom, wherein Z.sup.4, Z.sup.5, and Z.sup.6 each have the same meaning as Z.sup.1, and Z.sup.12 has the same meaning as Z.sup.11 ; Q.sup.1 and Q.sup.2 each represent a carboxyl group or a phosphonoxy group; Q.sup.3 represents a hydrogen atom, a carboxyl group or a phosphonoxy group; m represents 0 or an integer of from 1 to 20; n represents 0 or an integer of from 1 to 20; Y.sup.1 represents an alkylene group having from 1 to 10 carbon atoms which may contain one or more substituents selected from --OCOR.sup.11 and --NHCOR.sup.12, wherein R.sup.11 represents --Z.sup.13 or --Z.sup.7 --N (Z.sup.14)--CO--Z.sup.8 --H (wherein Z.sup.7 and Z.sup.8 each have the same meaning as Z.sup.1, and Z.sup.13 and Z.sup.14 each have the same meaning as Z.sup.11) and R.sup.12 represents --Z.sup.15 or --Z.sup.9 --N(Z.sup.16)--CO--Z.sup.10 --H (wherein Z.sup.9 and Z.sup.10 each have the same meaning as Z.sup.1, and Z.sup.15 and Z.sup.16 each have the same meaning as Z.sup.11), and a salt thereof. The compound inhibits TNF derivation by endotoxin and is therefore useful for the treatment of multiorganic insufficiencies.

Amino sugar derivatives

A disaccharide compound represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification and a salt thereof are disclosed. The compound exhibits excellent antitumor activity and low toxicity and is useful as an antitumor agent.

2-Deoxy-2-aminoglucopyranoside derivatives

New derivatives of penem and pharmacutically acceptable salt thereof are herein disclosed; these compounds being useful as an antibacterial agent which has an extremely wide antibacterial spectrum, exhibits a high sensitivity to bacteria resistant to conventional penicillins and cephalosporin antibiotics and is excellent in its physico-chemical stability, solubility to water and biological stability, in particular, stability to decomposition by enzyme such as dehydropeptidase I in kidney, .beta.-lactamase; these derivatives of penem being able to be prepared by reacting 2-substituted sulfinyl derivative of penem with a thiol compound and then optionally removing protective group(s) and further alkylating the reaction product or vice versa.

Derivatives of penem

Phosphorus containing disaccharide derivatives

New derivatives of penem and pharmaceutically acceptable salt thereof are herein disclosed; these compounds being useful as an antibacterial agent which has an extremely wide antibacterial spectrum, exhibits a high sensitivity to bacteria resistant to conventional penicillins and cephalosporing antibiotics and is excellent in its physico-chemical stability, solubility to water and biological stability, in particular, stability to decomposition by enzyme such as dehydropeptidase I in kidney, .beta.-lactamase; these derivatives of penem being able to be prepared by reacting 2-substituted sulfinyl derivative of penem with a thiol compound and then optionally removing protective group(s) and further alkylating the reaction product or vice versa.

Mercapto-bicycloheterocyclics useful as intermediates for penem

Growing community of inventors

Tokyo, Japan

Tsunehiko Soga