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    • 9. 发明专利
    • SALTS OF ISOPHOSPHORAMIDE MUSTARD AND ANALOGS THEREOF
    • NZ580341A
    • 2012-06-29
    • NZ58034108
    • 2008-04-04
    • ZIOPHARM ONCOLOGY INC
    • AMEDIO JOHN CWALLNER BARBARA PKOMARNITSKY PHILIP B
    • C07C229/26A61K31/13A61K31/133A61K31/198A61K31/4409A61K31/664A61P35/00C07C211/35C07C215/10C07C279/14C07D213/74C07F9/24
    • Disclosed is a crystalline compound having a structure of formula (I) wherein A+ is the conjugate acid of a hydroxylated aliphatic amine; and X and Y independently represent leaving groups. Examples of A+ are conjugate acid of mono-, bis- or tris-(2-hydroxyethyl)amine, 2-hydroxy-tertbutylamine, N,N-dimethyl-N-(2-hydroxyethyl)amine, and tris(hydroxymethyl)aminomethane (Tris). Also disclosed is a method for preparing a composition comprising a compound of formula (I) and a saline solution; a pharmaceutical composition or lyophilisate comprising a compound of formula (I) and the use of a compound of formula (I) in the manufacture of a medicament for treating a hyperproliferative disorder is selected from acute leukaemia, chronic leukemias, polycythaemia vera, lymphoma, Hodgkin's disease, non-Hodgkin's lymphoma, multiple myeloma, Waldenstrom's macroglobulinemia, heavy chain disease, myelodysplastic syndrome, hairy cell leukemia, myelodysplasia, sarcomas and carcinomas, synovioma, mesothelioma, Ewing's tumour, leiomyosarcoma, rhabdomyosarcoma, colon carcinoma, lymphoid malignancy, pancreatic cancer, breast cancer, lung cancers, ovarian cancer, prostate cancer, hepatocellular carcinoma, squamous cell carcinoma, basal cell carcinoma, adenocarcinoma, sweat gland carcinoma, sebaceous gland carcinoma, papillary carcinoma, papillary adenocarcinomas, medullary carcinoma, bronchogenic carcinoma, renal cell carcinoma, hepatoma, bile duct carcinoma, choriocarcinoma, Wilms' tumour, cervical cancer, testicular tumour, bladder carcinoma, and CNS tumours or cyclophosphamide (CPA) resistant condition.