- Preparation method and crystal structure of 5-fluorouracil phenformin salt
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The invention provides a salt of 5-fluorouracil and phenformin as well as a preparation method and crystal structure of the salt, and relates to the field of medicinal chemistry. A molecular formula of the 5-fluorouracil phenformin salt is C14H18FN7O2, and a basic structure unit is composed of a phenformin cation and a 5-fluorouracil anion; the salt belongs to a monoclinic system, and the space group is P2/n; and the preparation method comprises the steps of using the 5-fluorouracil bulk drug and a phenformin free base as raw materials, mixing the 5-fluorouracil bulk drug and the phenforminfree base according to a molar ratio of 1:1, dissolving the mixture into a mixed solvent of methanol and acetonitrile for a reaction, performing recrystallization by using ethanol as a solvent to obtain the high-purity 5-fluorouracil phenformin salt. According to the 5-fluorouracil phenformin salt provided by the invention, the solubility of the 5-fluorouracil is improved, and the synergistic antitumor activity of the 5-fluorouracil and the phenformin is facilitated; and no crystalline solvent molecules exist in the salt structure, and the skeleton structure of the salt crystal can be maintained under long-term storage at room temperature.
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Paragraph 0026
(2020/01/08)
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- PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING IMMUNE DISEASES OR INFLAMMATORY DISEASES, CONTAINING BIGUANIDE DERIVATIVE COMPOUND AS ACTIVE INGREDIENT
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The present invention relates to a biguanide derivative compound capable of effectively preventing and treating immune diseases. The biguanide-based derivative compound according to the present invention inhibits the generation of IL-17 and TNF-α, which are inflammatory cytokines, increases the activity of regulatory T cells having an immunomodulatory function, and exhibits excellent therapeutic effects in animal models of immune diseases. Accordingly, the biguanide-based derivative compound can be usefully used as an immunosuppressant or a pharmaceutical composition capable of preventing or treating various immune diseases, such as autoimmune diseases, inflammatory diseases, and transplant rejection, caused by the dysregulation of immune responses.
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Paragraph 0085
(2017/12/27)
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- A novel metformin derivative, HL010183, inhibits proliferation and invasion of triple-negative breast cancer cells
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Mounting evidence suggests that metformin (N,N-dimethylbiguanide), a widely prescribed drug for the treatment of type II diabetes, exerts an anti-tumor effect on several cancers including breast cancer. Breast cancer has been estimated as one of the most commonly diagnosed types of cancer among women. In particular, triple-negative breast cancers are associated with poor prognosis and metastatic growth. In the present study, we synthesized a novel metformin derivative 5 (HL010183) and metformin salts, 9a, 9b, and 9c (metformin gamma-aminobutyric acid (GABA) salt, metformin pregabalin salt and metformin gabapentin salt), which exerted more potent inhibitory effects on the proliferation and invasiveness of Hs578T triple-negative breast carcinoma cells than metformin. Importantly, 5 showed approximately 100-fold more potent effects compared to metformin. In a triple-negative breast cancer xenograft model, 5 showed a comparable degree of inhibitory effect on in vivo tumor growth at the 100 mg/kg dose to that of metformin at 500 mg/kg. Our results clearly demonstrate that 5 exerts a potent anti-tumor effect both in vitro and in vivo, paving the way for a strategy for treatment of triple-negative breast cancer.
- Koh, Minsoo,Lee, Jong-Cheol,Min, Changhee,Moon, Aree
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p. 2305 - 2313
(2013/05/09)
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- CURABLE COMPOSITION
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The present invention has its object to provide a curable composition which comprises a guanidine compound as a non-organotin type catalyst, is less discolored, has good surface curability, depth curability, strength rise and adhesiveness, and can retain the curability even after storage; the above object can be achieved by a curable composition which comprises: (A) an organic polymer containing a silyl group capable of crosslinking under siloxane bond formation, the silyl group being a group represented by the general formula (1): -SiX 3 (1) (wherein X represents a hydroxyl group or a hydrolyzable group and the three X groups may be mutually the same or different), (B) a guanidine compound (B-1) as a silanol condensation catalyst, and (C) a plasticizer, wherein the content of the component (B-1) is not lower than 0.1 part by weight but lower than 8 parts by weight per 100 parts by weight of the component (A), and a non-phthalate ester plasticizer accounts for 80 to 100% by weight of the (C) component plasticizer.
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