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Claims for Patent: 4,307,100

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Claims for Patent: 4,307,100

Title: Nor bis-indole compounds usable as medicaments
Abstract:Compounds with antitumoral activity corresponding to the formula (I): ##STR1## wherein R'.sub.1 is a hydrogen atom or an alkoxy, acyl, formyl or haloacyl radical; R'.sub.2 is a hydrogen atom or an alkyl radical; R'.sub.3 and R".sub.3 are a hydrogen atom, hydroxyl radical or an alkanoyloxy radical, and together are a carbonyl group, and R'.sub.3 and R'.sub.5 together are an epoxy bridge or a double bond; R'.sub.4 is a hydrogen atom or an alkyloxycarbonyl, hydroxymethyl, alkanoyloxymethyl or acetamido radical; R'.sub.5 and R".sub.5 are a hydrogen atom or a hydroxyl, alkanoyloxyl, ethyl or 2-hydroxyethyl radical; R'.sub.6 is a hydrogen atom or an ethyl, 2-hydroxyethyl or acetyl radical; R.sub.1 is a hydrogen atom or an alkyl, formyl or acyl radical; R.sub.2 is a hydrogen atom or alkoxy radical; R.sub.3 is a hydrogen atom or a hydroxyl or alkanoyloxyl radical, and together with R.sub.4 is an epoxy bridge or a double bond; R.sub.4 is a hydrogen atom or a hydroxyl, alkanoyloxyl radical, and together with R.sub.5 is an epoxy bridge; R.sub.6 is an alkyloxycarbonyl, hydrazido, acetamido, hydroxymethyl or alkanoyloxymethyl radical; and R.sub.5 and R.sub.7 are a hydrogen atom or a hydroxyl and alkanoyloxyl radical; acid addition and quaternary ammonium salts thereof and 12-chloro derivatives thereof.
Inventor(s): Langlois; Nicole (Bures S. Yvette, FR), Langlois; Yves (Bures S. Yvette, FR), Andriamialisoa; Ratremaniaina Z. (Les Ulis, FR), Potieo; Pierre (Bois d'Arcy, FR), Mangeney; Pierre (Paris, FR)
Assignee: Agence Nationale de Valorisation de la Recherche (ANVAR) (Paris, FR)
Application Number:06/067,439
Patent Claims: 1. Compounds corresponding to the following formula (I): ##STR18## wherein R'.sub.1 is selected from the group consisting of a hydrogen atom and an alkoxy, acyl, formyl and haloacyl radical, said alkoxy radical containing from 1 to 5 carbon atoms, said acyl and haloacyl radical containing from 2 to 5 carbon atoms;

R'.sub.2 is selected from the group consisting of a hydrogen atom and an alkyl radical, said alkyl radical containing from 1 to 5 carbon atoms;

R'.sub.3 and R".sub.3 are independently selected from the group consisting of a hydrogen atom and a hydroxyl radical and an alkanoyloxy radical, said alkanoyloxy radical containing from 2 to 5 carbon atoms, and together are an oxo group, and R'.sub.3 and R'.sub.5 together are an epoxy bridge or a double bond;

R'.sub.4 is selected from the group consisting of a hydrogen atom and an alkyloxycarbonyl, hydroxymethyl, alkanoyloxymethyl and acetamido radical;

R'.sub.5 and R".sub.5 are independently selected from the group consisting of a hydrogen atom and a hydroxyl, alkanoyloxyl, ethyl and 2-hydroxyethyl radical, said alkanoyxloxyl radical having from 2 to 5 carbon atoms;

R'.sub.6 is selected from the group consisting of a hydrogen atom and an ethyl, 2-hydroxyethyl and acetyl radical;

R.sub.1 is selected from the group consisting of a hydrogen atom and an alkyl, formyl and acyl radical, said alkyl radical having from 1 to 5 carbon atoms, said acyl radical having from 2 to 5 carbon atoms;

R.sub.2 is selected from the group consisting of a hydrogen atom and alkoxy radical, said alkoxy radical containing from 1 to 5 carbon atoms;

R.sub.3 is selected from the group consisting of a hydrogen atom and a hydroxyl and alkanoyloxyl radical, said alkanoyloxyl radical containing from 2 to 5 carbon atoms, and together with R.sub.4 is selected from the group consisting of an epoxy bridge and a double bond;

R.sub.4 is selected from the group consisting of a hydrogen atom and a hydroxyl, alkanoyloxyl radical of from 2 to 5 carbon atoms, and together with R.sub.5 is an epoxy bridge;

R.sub.6 is selected from the group consisting of an alkyloxycarbonyl, hydrazido, acetamido, hydroxymethyl and alkanoyloxymethyl radical; and

R.sub.5 and R.sub.7 are selected from the group consisting of a hydrogen atom and a hydroxyl and alkanoyloxyl radical of from 2 to 5 carbon atoms;

acid addition and quaternary ammonium salts thereof and 12-chloro derivative thereof.

2. Compounds corresponding to claim 1 corresponding to the following formula (Ia): ##STR19## wherein R'.sub.3 is selected from the group consisting of a hydrogen atom and a hydroxy radical;

R'.sub.5 is selected from the group consisting of a hydrogen atom and a hydroxy radical;

R'.sub.3 and R'.sub.5 are together selected from the group consisting of an epoxy bridge and a double bond;

R".sub.5 is selected from the group consisting of a hydrogen atom and an ethyl radical;

R.sub.1 is selected from the group consisting of a hydrogen atom, an alkyl, formyl and acyl radical, said alkyl radical having 1 to 5 carbon atoms, said acyl radical having from 2 to 5 carbon atoms;

R.sub.2 is selected from the group consisting of a hydrogen atom and a methoxy radical;

R.sub.7 is an alkanoyloxyl radical of from 2 to 5 carbon atoms; (the dotted line represents a possible double bond); and the corresponding salts thereof.

3. Compounds selected from the group consisting of

5'-noranhydrovinblastine,

5'-noranhydrovincristine,

5'-norleurosine,

12-chloro-5'-noranhydrovinblastine, and

5'-nor-N.sub.a -desmethyl-N.sub.a -formyl leurosine.

4. Pharmaceutical compositions for the treatment of leukemia comprising an effective amount of at least one compound according to claim 1.

5. Method of treating leukemia comprising administering an effective amount of at least one compound according to claim 1.

6. Compounds corresponding to formula (IV): ##STR20## wherein the radicals are as defined in connection with formula (I); and X represents a halogen atom and R.sub.8 represents a halogen atom.
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