Claims
- 1. A 4-desoxy-4-epipodophylloxtoxin derivative of the general formula: ##STR134## wherein R.sub.1 is a hydrogen atom, a methyl group, a benzyloxycarbonyl group, a lower alkanoyl group which may have one or more halogen atoms or a group of the formula --Si(Rx)(Ry)(Rz), where Rx, Ry and Rz are the same or different and each is a lower alkyl group or a phenyl group; R is a lower alkenyl group, a lower alkyl group having at least one hydroxyl group, a group of the formula --(CH.sub.2).sub.m CHO, where m is an integer of 0 to 3, a lower alkyl group having a ketoaldehyde group or a group of the formula --(CH.sub.2).sub.n NR.sub.2 R.sub.3, where n is an integer of 1 to 4: R.sub.2 and R.sub.3 are the same or different and each is a hydrogen atom, a group of the formula --N(Ra)(Rb), where Ra and Rb are the same or different and each is a lower alkyl group, a lower alkyl-substituted piperazino group or a lower alkyl group which may be substituted by hydroxy, piperidino or a group of the formula --N(Rc)(Rd), where Rc and Rd are the same or different and each is a lower alkyl group; provided that R.sub.2 and R.sub.3 are not both a group of the formula --N(Ra)(Rb); R.sub.2 and R.sub.3 may combine to form a cyclic structure which may optionally include additional nitrogen atoms and may further have a lower alkyl group or piperidino group, as a substituent, with the proviso that when R.sub.1 is a hydrogen atom, R is a group of the formula --(CH.sub.2).sub.m CHO, where m is an integer of 0 to 3, or a pharmaceutically acceptable salt thereof.
- 2. The 4-desoxy-4-epipodophyllotoxin derivative or a pharmaceutically acceptable salt thereof according to claim 1 wherein R.sub.1 is a methyl group, a benzyloxycarbonyl group, a lower alkanoyl group which may have one or more halogen atoms or a group of the formula --Si(Rx)(Ry)(Rz), where Rx, Ry and Rz are the same or different and each is a lower alkyl group or a phenyl group; R is a lower alkenyl group, a lower alkyl group having at least one hydroxyl group, a group of the formula --(CH.sub.2).sub.m CHO, where m is an integer of 0 to 3, a lower alkyl group having a ketoaldehyde group or a group of the formula --(CH.sub.2).sub.n NR.sub.2 R.sub.3, where n is an integer of 1 to 4: R.sub.2 and R.sub.3 are the same or different and each is a hydrogen atom, a group of the formula --N(Ra)(Rb), where Ra and Rb are the same or different and each is a lower alkyl group, a lower alkyl-substituted piperazino group or a lower alkyl group which may be substituted by hydroxy, piperidino or a group of the formula --N(Rc) (Rd), where Rc and Rd are the same or different and each is a lower alkyl group; R.sub.2 and R.sub.3 may combine to form a cyclic structure which may optionally include additional nitrogen atoms and may further have a lower alkyl group or piperidino group, as a substituent.
- 3. The 4-desoxy-4-epipodophyllotoxin derivative or a pharmaceutically acceptable salt thereof according to claim 1 wherein R.sub.1 is a hydrogen atom, R is a group of the formula --(CH.sub.2).sub.m CHO, where m is an integer of 0 to 3.
Priority Claims (3)
Number |
Date |
Country |
Kind |
87140 |
Jan 1991 |
JPX |
|
61706 |
Mar 1991 |
JPX |
|
90794 |
Apr 1991 |
JPX |
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Parent Case Info
This is a division, of application Ser. No. 08/375,565 filed Jan. 13, 1995 which is a continuation of application Ser. No. 07/924,079 filed Sep. 21, 1992, abandoned.
Foreign Referenced Citations (4)
Number |
Date |
Country |
61-103883 |
May 1986 |
JPX |
63-10789 |
Jan 1988 |
JPX |
2-191279 |
Jul 1990 |
JPX |
9009788 |
Sep 1990 |
WOX |
Non-Patent Literature Citations (3)
Entry |
Podophyllotoxin Analogs: effects on DNA Topoisomerase II, Tubulin Polymerization, Human Tumor Kb Cells, and Their VP-16-Resistant Varients (1989). |
Chemical Abstracts, vol. 112, No. 1, 1 Jan. 1990, JP-A-1 117 885. |
Chemical Abstracts, Vo. 115, No. 19, 11 Nov. 1991, JP-A-3 127 792. |
Divisions (1)
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Number |
Date |
Country |
Parent |
375565 |
Jan 1995 |
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Continuations (1)
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Number |
Date |
Country |
Parent |
924079 |
Sep 1992 |
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