Use of the disorazoles and their derivatives for the treatment of benign and malignant oncoses
OwnerHerbert Irschik, Rolf Jansen +4inventors
InventorsHerbert Irschik, Rolf Jansen, Florenz Sasse, Silke Baasner, Peter Schmidt, Eckhard Gunther
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Abstract
The invention relates to disorazoles of the general formula I, which are employed as medicaments, preferably for the treatment of oncoses, in particular in the case of pharmaceutical resistance to other active compounds and in the case of metastasizing carcinoma. The possible uses are not restricted to oncoses. 1
Claims15
A medicament containing at least one disorazole derivative of the general formula I
- 6
- in which independently of one another
- R1 is:
- (i) hydrogen
- (i) OR4
- (i) part of a double bond to C5′
- R2, R3 and R4 are:
- (i) hydrogen
- (ii) unsubstituted or substituted (C1-C6)-alkyl,
- (iii) (C1-C4)-alkyl substituted by one or more fluorine atoms, preferably a trifluoromethyl group,
- (iv) unsubstituted or substituted (C1-C4)-alkyl-(C6-C14)-aryl, unsubstituted or substituted (C1-C4)-alkyl-heteroaryl
- (V) (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylaminocarbonyl (C1-C4)-alkylaminothiocarbonyl, (C1-C6)-alkyl-carbonyl or (C1-C6)-alkoxycarbonyl-(C1-C6)-alkyl,
- it being possible for the substitution of the alkyl radical by F, Cl, Br, I, CN, NH2, NH—(C1-C20)-alkyl, NH—(C3-C12)-cycloalkyl, OH, O—(C1-C20)-alkyl to take place singly or, on identical or different atoms, multiply by identical or different
- substituents, and it being possible for the substitution of an aryl radical by F, Cl, Br, I, CN, NH2, NH—(C1-C20)-alkyl, OH, O—(C1-C20)-alkyl and/or (C3-C8)-heterocyclyl having 1 to 5 heteroatoms, preferably nitrogen, oxygen, sulfur to take place singly or, on identical or different atoms, multiply by identical or different substituents, and
- X, Y are:
- in each case individually independently of one another or together oxygen, sulfur, two vicinal hydroxyl groups, two vicinal methoxy groups, part of a double bond,
- a compound being excluded in which R1 is methoxy, R2, R3 are hydrogen, X is oxygen and Y is the part of a double bond,
- its tautomers, E/Z isomers, stereoisomers, including the diastereomers and enantiomers, and the physiologically tolerable salts thereof.
The use of disorazole derivatives of the general formula I
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- in which independently of one another
- R1 is:
- (i) hydrogen
- (ii) OR4
- (iii) part of a double bond to C5′
- R2, R3 and R4 are:
- (i) hydrogen
- (ii) unsubstituted or substituted (C1-C6)-alkyl,
- (iii) (C1-C4)-alkyl substituted by one or more fluorine atoms, preferably a trifluoromethyl group,
- (iv) unsubstituted or substituted (C1-C4)-alkyl-(C6-C14)-aryl, unsubstituted or substituted (C1-C4)-alkyl-heteroaryl,
- (v) (C1-C4)-alkoxycarbonyl, (C1-C4)-alkylaminocarbonyl (C1-C4)-alkylaminothiocarbonyl, (C1-C6)-alkyl-carbonyl or (C1-C6)-alkoxycarbonyl-(C1-C6)-alkyl,
- it being possible for the substitution of the alkyl radical by F, Cl, Br, I, CN, NH2, NH—(C1-C20)-alkyl, NH—(C3-C12)-cycloalkyl, OH, O—(C1-C20)-alkyl to take place singly or, on identical or different atoms, multiply by identical or different substituents, and it being possible for the substitution of an aryl radical by F, Cl, Br, I, CN, NH2, NH—(C1-C20)-alkyl, OH, O—(C1-C20)-alkyl and/or (C3-C8)-heterocyclyl having 1 to 5 heteroatoms, preferably nitrogen, oxygen, sulfur to take place singly or, on identical or different atoms, multiply by identical or different substituents, and
- X, Y are:
- in each case individually independently of one another or together oxygen, sulfur, two vicinal hydroxyl groups, two vicinal methoxy groups, part of a double bond,
- a compound being excluded in which R1 is methoxy, R2, R3 are hydrogen, X is oxygen and Y is the part of a double bond,
- its tautomers, E/Z isomers, stereoisomers, including the diastereomers and enantiomers, and the physiologically tolerable salts thereof,
- for the production of a medicament for the treatment of benign or malignant oncoses in humans or animals.
The use of disorazole derivatives of the general formula I for the production of a medicament for the treatment of a disease in humans or animals which is based on the rapid and uncontrolled proliferation of endogenous cells.
The use of disorazole derivatives of the general formula I for the production of a medicament for the treatment of diseases which respond to immunomodulatory action, such as psoriasis, arteriosclerosis, arthritis, keratosis, muliple sclerosis and cancer.
The use of disorazole derivatives of the general formula I for the production of a medicament for the treatment of infective diseases, such as cachexia, malaria, AIDS and infection-related fever and pain.
The use of disorazole derivatives of the general formula I for the production of a medicament for the treatment of inflammatory and allergic diseases, inflammations mediated by eosinophils or proliferative diseases such as airway diseases, bronchial asthma, allergic rhinitis, allergic conjunctivitis, eczema and Crohn's disease.
Dependencies are inferred from the claim text.