Shanghai Pharmaceuticals Holding Co., Ltd.

Mitsubishi Tanabe Pharma Corporation

Other

Jianshu Xie

Toru Iijima

Guangxin Xia

Takayuki Kawaguchi

Jingkang Shen

Hiroshi Sugama

Miki Hirai

Hidenori Akatsuka

Yoichi Takahashi

Nobumasa Awai

Naoko Ueda

Jiansheng Han

Guohui Jia

Dexu Zhu

Mitsumi Muramatsu

Cheng Ni

Ming-Wei Wang

The present invention provides novel pharmaceutically acceptable salts of a morpholine derivative, including a malate, a tartrate, a hydrochloride, an acetate, and a naphthalene disulfonate thereof, wherein the tartrate has 3 crystal salt forms: crystal form A, crystal form B and dihydrate; the malate, the hydrochloride, and the acetate each have one crystal salt form; the naphthalene disulfonate is amorphous. When compared to the known morpholine derivative free base, the present invention has one or more improved properties, e.g., a better crystalline state, greatly improved water solubility, light stability and thermal stability, etc. The present invention further provides preparation methods for the salts of morpholine derivative and the crystal forms thereof, pharmaceutical compositions and use thereof.

Salts of morpholine derivative, crystal forms thereof, processes for producing the same, pharmaceutical compositions including the same, and use thereof

The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein Ris a cycloalkyl group and the like, Ris an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is &#x2014;O&#x2014; and the like, and Rto Rare the same or different and a hydrogen atom and the like; or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.

Nitrogen-containing saturated heterocyclic compound

The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: wherein Ris a cycloalkyl group and the like, Ris an optionally substituted aryl and the like, R is a lower alkyl and the like, T is a carbonyl group, Z is &#x2014;O&#x2014; and the like, and Rto Rare the same or different and a hydrogen atom and the like;or a pharmaceutically acceptable salt, that is useful as a renin inhibitor.

The present invention provides a morpholine derivative of the formula [I]; wherein Ris a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, a cycloalkyl group or an alkyl group; Ris a substituted alkyl group, an optionally substituted aryl group, an optionally substituted heterocyclo group, an optionally substituted alkylcarbonyl group, an optionally substituted arylcarbonyl group, an optionally substituted heterocyclo-substituted carbonyl group or a cycloalkylcarbonyl group; T is a methylene group or a carbonyl group; R, R, Rand Rare the same or different and a hydrogen atom, an optionally substituted carbamoyl group or an optionally substituted alkyl group;or pharmaceutically acceptable salts thereof. These compounds are useful as a renin inhibitor.

Morpholine derivative

Methods and compositions for treating or preventing bacterial infection

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Shanghai, China

Jianshu Xie