On January 25, 2000, Folkman, Moses J.; Ingber, Donald; Fujita, Takeshi published a patent.Application of 53788-12-8 The title of the patent was Preparation of O-substituted fumagillol derivatives with angiogenesis inhibitory activity. And the patent contained the following:
This invention relates to the preparation and use of O-substituted fumagillol derivatives of formula I [R1 = (substituted) 2-methyl-1-propenyl, (substituted) isobutyl; R2 = alkanoyl, aroyl, aromatic heterocycle-carbonyl, carbamoyl, alkyl, alkylsulfonyl, alkoxycarbonyl, etc.], or salts thereof preferably, O-(N-chloroacetylcarbamoyl)fumagillol, O-(N-chloroacetylcarbamoyl)dihydrofumagillol or O-(N-chloroacetylcarbamoyl)-6’b-hydroxyfumagillol, which have angiogenesis inhibitory activity, in the treatment and prevention of various diseases caused or advanced by abnormally hyperactive angiogenesis, especially various inflammatory diseases (rheumatism, psoriasis, etc.), diabetic retinopathy and cancer and other angiogenesis-dependent tumors, especially Kaposi’s sarcoma, breast cancer, colon cancer. Thus, II (AGM-1470) was prepared from fumagillol and chloroacetyl isocyanate in 71% yield. The T/C ratio of II in the B16 mouse melanoma model was 0.47 after 2 wk and 0.20 after 3 wk. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Application of 53788-12-8
The Article related to fumagillol derivative preparation angiogenesis inhibitor, kaposi sarcoma treatment fumagillol derivative preparation, breast cancer treatment fumagillol derivative preparation, antitumor fumagillol derivative preparation and other aspects.Application of 53788-12-8
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