Hainan Hdeton Science and Technology Co., Ltd.

Lifearc

Suzhou Yabao Pharmaceutical R&d Co., Ltd.

Meridian Laboratories, Inc.

Ling Wu

Jianfeng Gao

Yong Ren

Shuqin Yu

Lin Zhu

Edward Giles Mciver

Yan Xia

Yang Song

Yuanyuan Xu

Chunjun Chu

Miao Liu

Justin Stephen Bryans

Provided are a substituted tricyclic heterocyclic compound of formula I or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt, ester or a prodrug thereof, a pharmaceutical composition including the same and uses thereof. The substituted tricyclic heterocyclic compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be used for treating a disorder caused by at least one of cancer and neurodegenerative diseases. Further the compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be also used for preventing or treating a disorder caused by, associated with or accompanied by any abnormal kinase activity. 

Substituted tricyclic heterocyclic compounds and use thereof

A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056 M-13051 M), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 &#x3bc;m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

Pharmaceutical composition containing docetaxel-cyclodextrin inclusion complex and its preparing process

A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056M-13051M), comprises docetaxel and hydroxypropyl-beta-cyclodextrin and/or sulfobutyl-beta-cyclodextrin in a ratio of 1:10-150. The method includes steps as follows: docetaxel dissolved in ethanol is added into water solution of cyclodextrin via stirring, until docetaxel is completely dissolved; said solution is filtered in 0.2-04 &#x3bc;m microporous membrane then ethanol is removed through reduced pressure to obtain the inclusion complex in a liquid form; or ethanol, followed by water is removed through reduced pressure, then dried to obtain the inclusion complex in a solid form.

A pharmaceutical composition comprising cyclodextrin/paclitaxel inclusion, which consists of paclitaxel, cyclodextrin and a pharmaceutically acceptable excipient, wherein the mass ratio of the paclitaxel to cyclodextrin is 1:10-150, the said cyclodextrin is hydroxylpropyl-sulfobutyl-7-&#x3b2;-cyclodextrin, or sulfobutylether-7-&#x3b2;-cyclodextrin, or their mixture; the stability constant of the cyclodextrin/paclitaxel inclusion is Ka=5396M&#x2212;1&#x2212;1412M&#x2212;1. The preparation method of the pharmaceutical composition is as follow: (a) A solution of cyclodextrin is added dropwise to a solution of paclitaxel in ethanol. (b) The resulting mixture is filtered through microporous membrane of 0.2-0.4 &#x3bc;m after being dissolved. (c) Ethanol is removed under reduced pressure to give a liquid inclusion which has the ethanol level of less than 2%, or alternatively water is also removed under reduced pressure, the resulting product is dried giving a solid inclusion.

Pharmaceutical composition comprising cyclodextrin paclitaxel inclusion and preparation method thereof

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Jiangsu, China

Ling Wu