Dosage principle for drugs useful for treating neoplastic diseases
AssigneeBasilea Pharmaceutica International AG
InventorsMarc Engelhardt, Anne Schmitt-Hoffmann, Patrice Larger
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Abstract
The present invention provides a novel dosage principle for compounds of formula I and pharmaceutically acceptable derivatives thereof as defined in the claims, wherein said compound or pharmaceutically acceptable derivative thereof is intravenously administered to said patient over a period of at least about 8 hours, wherein the dose of the compound of formula I or pharmaceutically acceptable derivative thereof is at least the molar equivalent of about 45 mg/m2 of the dihydrochloride salt of the compound of formula I-B as defined in the claims.
Claims52
A method of treating a neoplastic disease, comprising the step of administering a compound of formula I:
- wherein:
- R represents phenyl or pyridinyl;
- wherein phenyl is optionally substituted by one or two substituents independently selected from lower alkyl, lower alkoxy, hydroxyl, amino, lower alkylamino, lower dialkylamino, acetylamino, halogen and nitro;
- and wherein pyridinyl is optionally substituted by amino or halogen;
- R1 represents hydrogen or cyano-lower alkyl;
- and wherein the prefix lower denotes a radical having up to and including a maximum of 4 carbon atoms;
- or a pharmaceutically acceptable derivative thereof;
- to a patient in need thereof, which pharmaceutically acceptable derivative is a pharmaceutically acceptable salt, pro-drug or pharmaceutically acceptable salt of a pro-drug thereof, wherein the pro-drug is an amide formed from an amino group present within the R group of the compound of formula I and the carboxy group of glycine, alanine or lysine,
- wherein said compound of formula I or pharmaceutically acceptable derivative thereof is intravenously administered to said patient over a period of at least about 8 hours, wherein the dose of the compound of formula I or a pharmaceutically acceptable derivative thereof is at least the molar equivalent of about 45 mg/m2 of the dihydrochloride salt of the compound of formula I-B
- wherein the neoplastic disease is selected from epithelial neoplasms, squamous cell neoplasms, basal cell neoplasms, transitional cell papillomas and carcinomas, adenomas and adenocarcinomas, adnexal and skin appendage neoplasms, mucoepidermoid neoplasms, cystic neoplasms, mucinous and serous neoplasms, ducal-, lobular and medullary neoplasms, acinar cell neoplasms, complex epithelial neoplasms, specialized gonadal neoplasms, paragangliomas and glomus tumors, naevi and melanomas, soft tissue tumors and sarcomas, fibromatous neoplasms, myxomatous neoplasms, lipomatous neoplasms, myomatous neoplasms, complex mixed and stromal neoplasms, fibroepithelial neoplasms, synovial like neoplasms, mesothelial neoplasms, germ cell neoplasms, trophoblastic neoplasms, mesonephromas, blood vessel tumors, lymphatic vessel tumors, osseous and chondromatous neoplasms, giant cell tumors, miscellaneous bone tumors, odontogenic tumors, gliomas, neuroepitheliomatous neoplasms, meningiomas, nerve sheath tumors, granular cell tumors and alveolar soft part sarcomas, Hodgkin's and non-Hodgkin's lymphomas, other lymphoreticular neoplasms, plasma cell tumors, mast cell tumors, immunoproliferative diseases, leukemias, miscellaneous myeloproliferative disorders, lymphoproliferative disorders and myelodysplastic syndromes.
A method of treating a neoplastic disease, comprising the step of administering a compound of formula I:
- wherein:
- R represents phenyl or pyridinyl;
- wherein phenyl is optionally substituted by one or two substituents independently selected from lower alkyl, lower alkoxy, hydroxyl, amino, lower alkylamino, lower dialkylamino, acetylamino, halogen and nitro;
- and wherein pyridinyl is optionally substituted by amino or halogen;
- R′ represents hydrogen or cyano-lower alkyl;
- and wherein the prefix lower denotes a radical having up to and including a maximum of 4 carbon atoms:
- or a pharmaceutically acceptable derivative thereof;
- to a patient in need thereof, which pharmaceutically acceptable derivative is a pharmaceutically acceptable salt, pro-drug or pharmaceutically acceptable salt of a pro-drug thereof, wherein the pro-drug is an amide formed from an amino group present within the R group of the compound of formula I and the carboxy group of glycine, alanine or lysine, wherein said compound of formula I or pharmaceutically acceptable derivative thereof is intravenously administered to said patient over a period of at least about 8 hours, wherein the dose of the compound of formula I or a pharmaceutically acceptable derivative thereof is at least the molar equivalent of about 45 mg/m2 of the dihydrochloride salt of the compound of formula I-B
- wherein the neoplastic disease is solid tumor.
Dependencies are inferred from the claim text.