Jiangsu Tasly Diyi Pharmaceutical Co., Ltd.

Yunrong Jing

Guocheng Wang

Yongfeng Wang

Wei Zhou

The present invention provides taxanes compounds with a formula (I) or formula (II) structure, a method for preparing the compounds, as well as the use of the compositions containing the compounds, pharmaceutically acceptable salts and solvates thereof as active ingredients in manufacturing oral antitumor medicaments,  In formula (I), Ris &#x2014;COR, &#x2014;COORor &#x2014;CONRR; Ris a C1-C6 alkyl, a C1-C6 alkenyl, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; Ris &#x2014;OR, &#x2014;OCOOR, &#x2014;OCOSRor &#x2014;OCONRR; Ris &#x2014;OR, &#x2014;OCOOR, &#x2014;OCOSR, &#x2014;OCONRRor H; wherein, Ris a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; Rand Rare respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. In formula (II), Ris &#x2014;CORor &#x2014;COOR; Ris an aromatic group; Ris &#x2014;OR; wherein, Ris a C1-C6 alkyl, a C1-C6 alkenyl, a C1-C6 alkynyl, a substituted hydrocarbon group, an aromatic group or a heterocyclic group.

Taxanes compounds, preparation method therefor, and uses thereof

Provided are taxanes compounds having the structure of formula I, preparation method thereof, and uses of compositions having the compound, pharmaceutical salts and solvates thereof as active ingredients in the preparation of oral antitumor drugs. In the formula, Ris &#x2014;COR, &#x2014;COOR, and &#x2014;CONRR; Ris C1-C6 alkyl, C1-C6 alkenyl group, a substituted hydrocarbon group, a heterocyclic group, an aromatic group or a substituted aromatic group; Ris &#x2014;OR, &#x2014;OCOOR, &#x2014;OCOSR, and &#x2014;OCONRR; Ris &#x2014;OR, &#x2014;OCOOR, &#x2014;OCOSR, &#x2014;OCONRR, H, and OH; Ris C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl group, a substituted hydrocarbon group, an aromatic group or a heterocyclic group; and Rand Rare respectively hydrogen, a hydrocarbon group, a substituted hydrocarbon group or a heterocyclic group. 

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Tianjin, China

Yunrong Jing