The present invention relates to stable dosage forms of levomilnacipran and pharmaceutically acceptable salts thereof. Processes for the preparation of these dosage forms and methods of using these dosage forms are also described.

The present invention generally relates to a process using a mechanochemical approach exploiting the mechanical milling of reactants for the manufacturing of acetyl Iopamidol and, more generally, of key intermediates of radiographic contrast agents, and of the contrast agents themselves.

The present invention relates to a process for synthesis of Eliglustat and intermediate compounds thereof. In particular, the present invention belongs to the field of synthesis of organic compounds, relates to a process for synthesis of Eliglustat and pharmaceutically acceptable salts thereof, and relates to the intermediate compounds used in the process and a process for preparation of the intermediate compounds. Compared with the existing synthetic processes, the process for preparing Eliglustat according to the present invention utilizes novel intermediates and steps for synthesis, has advantages of convenient operations, high yield, good purity of intermediates and desired product, and it is easy to apply the process in the industrial production.

The invention disclose a compound of formula (I), wherein, R.sub.1 is selected from H or C1-C6 hydrocarbon group, NH.sub.2, OH, O(CH.sub.2).sub.nCH.sub.3 (n=0, 1 or 2), N(CH.sub.3).sub.2, or CH.sub.2N(CH.sub.3).sub.2, R.sub.2 is selected from an amino acid ##STR00001##
or an hydroxy acid ##STR00002##
or OH (R.sub.1, R.sub.2 are not CH.sub.3 and OH at the same time), wherein X, Y are ##STR00003##
H, CH.sub.3, CH.sub.2OH, CH(OH)CH.sub.3, CH.sub.2SH, CH(CH.sub.3).sub.2, CH.sub.2CH(CH.sub.3).sub.2, CH(CH.sub.3)CH.sub.2CH.sub.3, CH.sub.2CH.sub.2SCH.sub.3, CH.sub.2COOH, CH.sub.2CONH.sub.2, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2NH.sub.2, or CH.sub.2CH.sub.2CONH.sub.2, R.sub.3-R.sub.5 are H or C1-C6 hydrocarbon group. The compound has a low toxicity, can significantly inhibit the migration and invasion of tumor cells in vitro, and can inhibit tumor metastasis in vivo in mice at low concentration, while showing notable sensitizing effect on cytotoxic anti-tumor drugs such as Paclitaxel etc. ##STR00004##

A method of producing a polypeptide compound, wherein a peptide compound represented by formula (P) is obtained by inducing an amide formation reaction between an amino-protected lactam compound represented by formula (R1) and an amino acid ester or peptide ester compound represented by formula (R2).

##STR00001##

The definitions for the reference signs in formulae (R1), (R2), and (P) are as set forth in the claims.

The present disclosure relates to an N-(substituted naphthyl-ethyl) substituted amide compound and uses thereof serving as a melatonin receptor agonist and 5-HT.sub.2C receptor antagonist, and specifically relates to the compound of formula (I) or a pharmaceutically acceptable salt thereof, a solvate or a mixture of them, and a pharmaceutical composition, where X, R.sub.1, and R.sub.2 are as defined in the present text. ##STR00001##

The inventive concepts disclosed and/or claimed herein relate generally to catalysts and, more particularly, but not by way of limitation, to a heterogeneous, metal-free hydrogenation catalyst containing frustrated Lewis pairs. In one non-limiting embodiment, the heterogeneous, metal-free catalyst comprises hexagonal boron nitride (h-BN) having frustrated Lewis pairs therein.

The inventive concepts disclosed and/or claimed herein relate generally to catalysts and, more particularly, but not by way of limitation, to a heterogeneous, metal-free hydrogenation catalyst containing frustrated Lewis pairs. In one non-limiting embodiment, the heterogeneous, metal-free catalyst comprises hexagonal boron nitride (h-BN) having frustrated Lewis pairs therein.

The inventive concepts disclosed and/or claimed herein relate generally to catalysts and, more particularly, but not by way of limitation, to a heterogeneous, metal-free hydrogenation catalyst containing frustrated Lewis pairs. In one non-limiting embodiment, the heterogeneous, metal-free catalyst comprises hexagonal boron nitride (h-BN) having frustrated Lewis pairs therein.

The present disclosure relates to methods and compounds for liquid phase oligonucleotide synthesis employing the use of small molecules with lipophilic groups. Methods for making an oligonucleotide by liquid phase oligonucleotide synthesis using the compounds described herein are also provided.