C07C225/16

A NOVEL PROCESS FOR CHIRAL RESOLUTION OF HIGHLY PURE (6R)-6-(DIMETHYLAMINO)-4,4-DIPHENYL-HEPTANONE FROM RACEMIC METHADONE HYDROCHLORIDE

The present invention discloses an improved process for preparing pure (6R)-6-(dimethylamino)-4,4-diphenyl-3-heptanone and its hydrochloride salt.

Inhibitors of the N-terminal domain of the androgen receptor

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

Inhibitors of the N-terminal domain of the androgen receptor

The present disclosure provides compounds and methods for inhibiting or degrading the N-terminal domain of the androgen receptor, as well as methods for treating cancers such as prostate cancer.

COMPOSITIONS COMPRISING A POLYMERIC NETWORK

The present invention relates to a composition comprising a polymeric network having at least one unit of formula (I), (II), and/or (III); (I) (II) (III) wherein said composition is obtained by contacting at least one compound A comprising at least two functions selected from the group of function of formula X—C(═O)—CHR.sup.1—C(═O)—R.sup.2, —C(═O)—C—R.sup.2; or —C(═O)—CR.sup.1═CR.sup.2—NR.sup.4R.sup.5; wherein at least 25% by weight of compounds A have a functionality ≦5, with % by weight relative to the total weight of compounds A; with at least one compound B comprising at least one NH.sub.2, or NH.sub.3.sup.+ groups; wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to a compound comprising at least two units and at most 5 units of formula (I), (II), and/or (III); wherein R.sup.1, R.sup.2, R.sup.3, X, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to processes for preparing said composition and said compounds, to material, articles, and polymers comprising or using said compositions and compounds, and the use thereof.

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COMPOSITIONS COMPRISING A POLYMERIC NETWORK

The present invention relates to a composition comprising a polymeric network having at least one unit of formula (I), (II), and/or (III); (I) (II) (III) wherein said composition is obtained by contacting at least one compound A comprising at least two functions selected from the group of function of formula X—C(═O)—CHR.sup.1—C(═O)—R.sup.2, —C(═O)—C—R.sup.2; or —C(═O)—CR.sup.1═CR.sup.2—NR.sup.4R.sup.5; wherein at least 25% by weight of compounds A have a functionality ≦5, with % by weight relative to the total weight of compounds A; with at least one compound B comprising at least one NH.sub.2, or NH.sub.3.sup.+ groups; wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to a compound comprising at least two units and at most 5 units of formula (I), (II), and/or (III); wherein R.sup.1, R.sup.2, R.sup.3, X, L.sup.1 and L.sup.2 have the same meaning as that defined in the claims. The present invention also relates to processes for preparing said composition and said compounds, to material, articles, and polymers comprising or using said compositions and compounds, and the use thereof.

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Curcumin analogs

Provided herein are curcumin analogues that are able to interact with amyloid β (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds in the treatment of Alzheimer's Disease or a related disorder.

Curcumin analogs

Provided herein are curcumin analogues that are able to interact with amyloid β (Aβ) and to attenuate the copper-induced crosslinking of Aβ. Also provided herein are methods of using the compounds in the treatment of Alzheimer's Disease or a related disorder.

A Process for Preparation of Dexmethylphenidate Hydrochloride

The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-throe-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer. The process is economical, environmental friendly and results in increased yield and optically pure dexmethylphenidate hydrochloride.

A Process for Preparation of Dexmethylphenidate Hydrochloride

The present invention relates to a process for preparation of dexmethylphenidate hydrochloride from racemic methylphenidate. The process involves the treatment of racemic mixture of dl-throe-methylphenidate base in the presence of di-pivaloyl-D-tartaric acid (D-DPTA) in a solvent to isolate dipivaloyl tartrate salt of d-threo-methylphenidate. The dipivaloyl tartrate salt of d-threo-methylphenidate is treated with a base to obtain a d-threo-methylphenidate base, which is extracted using a suitable solvent. The d-threo-methylphenidate base is treated with hydrochloric acid-isopropyl alcohol solution to obtain slurry of d-threo-methylphenidate hydrochloride also known as dexmethylphenidate hydrochloride. The dexmethylphenidate hydrochloride slurry is filtered and washed with acetone. The invention also discloses a process for recovery of D-DPTA from the salt mother liquor and from the spent aqueous layer. The process is economical, environmental friendly and results in increased yield and optically pure dexmethylphenidate hydrochloride.

NOVEL PENTADIENOYL PIPERIDINE DERIVATIVE AND USE THEREOF
20170320825 · 2017-11-09 ·

The present invention relates to a novel pentadienoyl piperidine derivative, a pharmaceutical composition containing the same for prevention or treatment of metabolic diseases, and a functional food composition using the same for improvement or relief of metabolic diseases. The pentadienoyl piperidine derivative of the present invention inhibits the differentiation of preadipocytes, reduces body weight, visceral fat, blood lipid levels, and blood glucose levels, improves a blood liver function index, and suppresses metabolic inflammation responses. Thus, ultimately, the derivative can be usefully used as a medicine or a functional food composition, which exhibits the preventive or therapeutic activity for metabolic diseases selected from the group consisting of obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome.