- Synthesis method of ciclopirox olamine
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The invention discloses a synthesis method of ciclopirox olamine. The synthesis method includes following steps: (1), preparing dimethyl methacrylate; (2), preparing cyclohexane formyl chloride; (3), preparing 5-oxo-3-methyl-5-cyclohexyl-3-methyl pentenoate; (4), preparing 1-hydroxy-4-methyl-6-cyclohexyl-2(1H)-pyridone; (5), preparing 1-hydroxy-4-methyl-6-cyclohexyl-2(1H)-pyridone-2-amino-ethylate ciclopirox olamine. The synthesis method has the advantages of high yield, high product quality, low running cost, automatic running of equipment, high stability and easiness in meeting industrial needs.
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- Visible-Light-Induced C2 Alkylation of Pyridine N-Oxides
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A photoredox catalytic method has been developed for the direct C2 alkylation of pyridine N-oxides. This reaction is compatible with a range of synthetically relevant functional groups for providing efficient synthesis of a variety of C2-alkylated pyridine N-oxides under mild conditions. Mechanistic studies are consistent with the generation of a radical intermediate along the reaction pathway.
- Zhang, Wen-Man,Dai, Jian-Jun,Xu, Jun,Xu, Hua-Jian
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p. 2059 - 2066
(2017/02/26)
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- METHODS OF BLADDER CANCER TREATMENT WITH CICLOPIROX, CICLOPIROX OLAMINE, OR A CICLOPIROX PRODRUG
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A method of treating bladder cancer is provided. The method of treating bladder cancer can include: providing a pharmaceutical composition having ciclopirox or ciclopirox olamine or a ciclopirox-POM prodrug having a structure of one of the formulae provided herein or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof; and administering the pharmaceutical composition to a subject having the bladder cancer. The ciclopirox or ciclopirox olamine or a ciclopirox-POM prodrug can be administered in a therapeutically effective amount.
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Paragraph 094
(2016/06/06)
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- METHOD OF TREATMENT WITH PRODRUGS OF 6-CYCLOHEXYL-1-HYDROXY-4-METHYLPYRIDIN IN-2-1H-ONE AND DERIVATIVES THEREOF
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A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, Trichophyton rubrum, Trichophyton mentagrophytes, Epidermophyton floccosum, and Microsporum canis, candidiasis (moniliasis), Candida albicans, tinea (pityriasis) vesicolor, Malassezia furfur, acute myeloid leukemia, acute lymphoid leukemia, chronic myelogenous leukemia, lymphoma or multiple myeloma.
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Paragraph 0062
(2015/04/28)
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- Protective solutions for organs
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Described is a protective solution for avoiding ischemic, storage or ischemia/reperfusion to organs, or to isolated cell systems, or to tissue components after perfusion, surgery, transplantation, or cryopreservation and subsequent reperfusion, which contains alkali ions, and if need be also alkaline earth ions as the electrolyte, a buffer e.g. on a histidine derivation basis, as well as a polyol and/or a saccharide, has an osmolarity of about 290 mosm/l to about 350 mosm/l, as well as a pH value of about 6.8 to about 7.4, and to which hydroxamic acid, and/or one or more hydroxamic acid derivatives are added.
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- Antimycotic nail varnish
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A nail varnish comprising a water-insoluble film-forming substance and an antimycotic compound which is a 1-hydroxy-2-pyridone I of the general formula STR1 in which R1 is a hydrocarbon group which contains from 6 to 9 carbon atoms, but is free from olefinic and acetylenic bonds, one of the groups R2 and R4 is hydrogen and the other is hydrogen, methyl or ethyl and R3 is alkyl having up to two carbon atoms, said antimycotic ingredient being present in free form or in the form of a salt.
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- The chemistry of antimicrobially active 1-hydroxy-2-pyridones
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The unsaturated δ-keto esters obtained by condensation of acid chlorides with esters of di- or trialkyl-acrylic acids can be cyclized with hydroxylamine to yield 1-hydroxy-2-pyridones. However, in many cases a two-steps synthesis may be of advantage in preparative respect, the ketoesters being cyclized to 2-pyrones, which then are reacted with hydroxylamine in the presence of certain bases to give. The hydroxy-pyridones show pronounced antifungal activity in vitro as well as in experimental guinea pig dermatophytosis.
- Lohaus,Dittmar
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p. 1311 - 1316
(2007/10/02)
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- Process for the preparation of 1-hydroxy-pyridones
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Method for making 6-substituted-1-hydroxy-2-pyridones, which may also be substituted in one or more of the 3-, 4-, and 5-positions, by reaction of the corresponding 2-pyrone with hydroxylamine or its salts in the presence of imidazole or a 2-aminopyridine which may be mono- or di-methyl substituted.
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- Process for the manufacture of 1-hydroxy-2-pyridones
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New 1-hydroxy-2-pyridones of the general formula SPC1 In which R1 is alkyl of 1 to 17 carbon atoms, cycloalkyl of 5 to 8 carbon atoms, cyclohexylalkyl or phenalkyl both having 1 to 3 carbon atoms in the alkylene chain or α-furyl, all of which may be substituted by halogen, and R2 to R4 are hydrogen or lower alkyl, or two adjacent substituents together form a trimethylene or tetramethylene chain, and in which R1 to R4 together contain at least 2 carbon atoms, are prepared by contacting unsaturated δ-keto esters or mixtures thereof with hydroxylamine and subjecting the products to cyclization.
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